1) Taussig SJ, Batkin S. Bromelain, the enzyme
complex of pineapple (Ananas comosus) and its clinical application. An
update. J Ethnopharmacol. 1988 Feb-Mar;22(2):191-203.
Source
Department of Food Science and Human Nutrition, School of Tropical Agriculture, University of Hawaii, Honolulu.
Abstract
After a short description of the uses of pineapple as folk medicine by
the natives of the tropics, the more important new pharmaceutical
applications of bromelain, reported between 1975 and 1978, are
presented. Although the exact chemical structure of all active
components of bromelain is not fully determined, this substance has
shown distinct pharmacological promise. Its properties include: (1)
interference with growth of malignant cells; (2) inhibition of platelet
aggregation; (3) fibrinolytic activity; (4) anti-inflammatory action;
(5) skin debridement properties. These biological functions of
bromelain, a non-toxic compound, have therapeutic values in modulating:
(a) tumor growth; (b) blood coagulation; (c) inflammatory changes; (d)
debridement of third degree burns; (e) enhancement of absorption of
drugs. The mechanism of action of bromelain affecting these varied
biological effects relates in part to its modulation of the arachidonate
cascade.
2) Source
Emeruwa AC. Antibacterial substance from Carica papaya fruit extract. J Nat Prod. 1982 Mar-Apr;45(2):123-7.
Abstract
Ripe and unripe Carica papaya fruits (epicarp, endocarp, seeds and
leaves) were extracted separately and purified. All the extracts except
that of leaves produced very significant antibacterial activity on
Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas
aeruginosa and Shigella flexneri. The MIC of the substance was small
(0.2-0.3 mg/ml) for gram-positive bacteria and large (1.5-4 mg/ml) for
gram-negative bacteria. The substance was bactericidal and showed
properties of a protein. Other proteins previously found in C. papaya
did not show antibacterial activity.
3) Source
Pearson TA, Mensah GA, Alexander RW, Anderson JL, Cannon RO 3rd,
Criqui M, Fadl YY, Fortmann SP, Hong Y, Myers GL, Rifai N, Smith SC Jr,
Taubert K, Tracy RP, Vinicor F; Centers for Disease Control and
Prevention; American Heart Association. A statement for healthcare
professionals from the Centers for Disease Control and Prevention and
the American Heart Association. Circulation. 2003 Jan 28;107(3):499-511.
II. Evidence for Inflammation as a Key Pathogenetic Mechanism in Atherosclerosis
A role for inflammation has become well established over the past
decade or more in theories describing the atherosclerotic disease
process.4,5 From a pathological viewpoint, all stages, ie, initiation,
growth, and complication of the atherosclerotic plaque,6,7 might be
considered to be an inflammatory response to injury. The major injurious
factors that promote atherogenesis—cigarette smoking, hypertension,
atherogenic lipoproteins, and hyperglycemia—are well established. These
risk factors give rise to a variety of noxious stimuli that elicit
secretion of both leukocyte soluble adhesion molecules, which facilitate
the attachment of monocytes to endothelial cells, and chemotactic
factors, which encourage the monocytes' migration into the subintimal
space. The transformation of monocytes into macrophages and the uptake
of cholesterol lipoproteins are thought to initiate the fatty streak.
Further injurious stimuli may continue the attraction and accumulation
of macrophages, mast cells, and activated T cells within the growing
atherosclerotic lesion. Oxidized low-density lipoproteins may be one of
several factors that contribute to loss of smooth muscle cells through
apoptosis in the atherosclerotic plaque cap, and secretion of
metalloproteinases and other connective tissue enzymes by activated
macrophages may break down collagen, weakening the cap and making it
prone to rupture. This disruption of the atherosclerotic plaque then
exposes the atheronecrotic core to arterial blood, which induces
thrombosis. Thus, virtually every step in atherogenesis is believed to
involve cytokines, other bioactive molecules, and cells that are
characteristic of inflammation.
http://circ.ahajournals.org/content/107/3/499.full
4) Leonard BE. Inflammation, depression and dementia: are they connected? Neurochem Res. 2007 Oct;32(10):1749-56.
Source
Department of Psychiatry and Neuropsychology, Brain and Behaviour
Research Institute, University of Maastricht, Maastricht, The
Netherlands. belucg@iol.ie
Abstract
Chronic inflammation is now considered to be central to the
pathogenesis not only of such medical disorders as cardiovascular
disease, multiple sclerosis, diabetes and cancer but also of major
depression. If chronic inflammatory changes are a common feature of
depression, this could predispose depressed patients to
neurodegenerative changes in later life. Indeed there is now clinical
evidence that depression is a common antecedent of Alzheimer's disease
and may be an early manifestation of dementia before the cognitive
declines becomes apparent. This review summarises the evidence that
links chronic low grade inflammation with changes in brain structure
that could precipitate neurodegenerative changes associated with
Alzheimer's disease and other dementias. For example, neuronal loss is a
common feature of major depression and dementia. It is hypothesised
that the progress from depression to dementia could result from the
activation of macrophages in the blood, and microglia in the brain, that
release pro-inflammatory cytokines. Such cytokines stimulate a cascade
of inflammatory changes (such as an increase in prostaglandin E2, nitric
oxide in addition to more pro-inflammatory cytokines) and a
hypersecretion of cortisol. The latter steroid inhibits protein
synthesis thereby reducing the synthesis of neurotrophic factors and
preventing reairto damages neuronal networks. In addition, neurotoxic
end products of the tryptophan-kynurenine pathway, such as quinolinic
acid, accumulate in astrocytes and neurons in both depression and
dementia. Thus increased neurodegeneration, reduced neuroprotection and
neuronal repair are common pathological features of major depression and
dementia. Such changes may help to explain why major depression is a
frequent prelude to dementia in later life.
5) Barzilay JI, Abraham L, Heckbert SR, Cushman M, Kuller LH, Resnick
HE, Tracy RP. The relation of markers of inflammation to the
development of glucose disorders in the elderly: the Cardiovascular
Health Study. Diabetes. 2001 Oct;50(10):2384-9.Back to previous page
Source
Division of Endocrinology, Kaiser Permanente of Georgia, and the
Division of Endocrinology, Emory University School of Medicine, Atlanta,
Georgia 30084, USA. joshua.barzilay@kp.org
Abstract
Several studies suggest that inflammation plays a role in the
pathogenesis of some glucose disorders in adults. We tested this
hypothesis in a longitudinal cohort study of older individuals who had
normal fasting glucose (FG) values at baseline. We compared the baseline
levels of six inflammatory markers in participants who had developed
glucose disorders at follow-up with those of participants whose FG
remained normal at follow-up. Participants were members of the
Cardiovascular Health Study, a prospective study of risk factors for
cardiovascular disease in adults > or =65 years. All 5,888
participants had baseline testing, including FG and markers of
inflammation: white blood cell and platelet counts and albumin,
fibrinogen, C-reactive protein (CRP), and factor VIIIc levels. At 3-4
years of follow-up, 4,481 (84.5%) of those who were alive had FG levels
retested. Participants who developed diabetes (n = 45) had higher median
levels of CRP at baseline than those who remained normoglycemic. On
multivariate analysis, those with elevated CRP levels (75th percentile
[2.86 mg/l] vs. 25th percentile [0.82 mg/l]) were 2.03 times (95%
confidence intervals, 1.44-2.86) more likely to have diabetes on
follow-up. Adjustment for confounders and other inflammatory markers did
not appreciably change this finding. There was no relationship between
the development of diabetes and other markers of inflammation.
Inflammation, as measured by CRP levels, is associated with the
development of diabetes in the elderly. Understanding the role of
inflammation in the pathogenesis of glucose disorders in this age-group
may lead to better classification and treatment of glucose disorders
among them.
6) Festa A, D'Agostino R Jr, Howard G, Mykkänen L, Tracy RP, Haffner
SM. Chronic subclinical inflammation as part of the insulin resistance
syndrome: the Insulin Resistance Atherosclerosis Study (IRAS).
Circulation. 2000 Jul 4;102(1):42-7.
Source
Department of Medicine, University of Texas Health Science Center at San Antonio, 78228-3900, USA. festa@magnet.at
Abstract
BACKGROUND:
Inflammation has been suggested as a risk factor for the development
of atherosclerosis. Recently, some components of the insulin resistance
syndrome (IRS) have been related to inflammatory markers. We
hypothesized that insulin insensitivity, as directly measured, may be
associated with inflammation in nondiabetic subjects.
METHODS AND RESULTS:
We studied the relation of C-reactive protein (CRP), fibrinogen, and
white cell count to components of IRS in the nondiabetic population of
the Insulin Resistance Atherosclerosis Study (IRAS) (n=1008; age, 40 to
69 years; 33% with impaired glucose tolerance), a multicenter,
population-based study. None of the subjects had clinical coronary
artery disease. Insulin sensitivity (S(I)) was measured by a frequently
sampled intravenous glucose tolerance test, and CRP was measured by a
highly sensitive competitive immunoassay. All 3 inflammatory markers
were correlated with several components of the IRS. Strong associations
were found between CRP and measures of body fat (body mass index, waist
circumference), S(I), and fasting insulin and proinsulin (all
correlation coefficients >0.3, P<0.0001). The associations were
consistent among the 3 ethnic groups of the IRAS. There was a linear
increase in CRP levels with an increase in the number of metabolic
disorders. Body mass index, systolic blood pressure, and S(I) were
related to CRP levels in a multivariate linear regression model.Back to previous page
CONCLUSIONS:
We suggest that chronic subclinical inflammation is part of IRS. CRP, a
predictor of cardiovascular events in previous reports, was
independently related to S(I). These findings suggest potential benefits
of anti-inflammatory or insulin-sensitizing treatment strategies in
healthy individuals with features of IRS.
INFLAMMATION IS ASSOCIATED WITH INSULIN RESISTANCE.
7) Walker JA, Cerny FJ, Cotter JR, Burton HW. Attenuation of
contraction-induced skeletal muscle injury by bromelain. Med Sci Sports
Exerc. 1992 Jan;24(1):20-5.
Source
Department of Physical Therapy/Exercise Science, State University of New York, Buffalo 14214.
Abstract
The proteolytic enzyme, bromelain, reportedly has therapeutic effects
in the treatment of inflammation and soft tissue injuries. We tested the
hypothesis that bromelain attenuates skeletal muscle injury induced by
lengthening contractions. The left extensor digitorum longus (EDL)
muscle of anesthetized hamsters was injured using a motorized foot pedal
which repeatedly flexed/extended the foot through a range of 125
degrees. The EDL muscle was electrically stimulated for 400 ms during
plantarflexion. Animals were assigned randomly to either a 0-d group
(evaluated 3-h post-injury) or to untreated (UT) or bromelain-treated
(T) groups, evaluated 3, 7, or 14 d post-injury. Following injury, T
received 5 mg.kg-1 b.w. of bromelain, twice daily. Maximum isometric
tetanic force (Po) was measured in vitro, then muscles were fixed,
sectioned, and examined for evidence of fiber damage. The Po of injured
muscles from T were higher than Po of injured muscles from UT at 3 (18.7
+/- 0.4 vs 16.5 +/- N.cm-2 and 14 d (20.5 +/- 0.6 vs 18.2 +/- 0.6
N.cm-2) (P less than 0.05), but not 7 d (19.5 +/-0.7 vs 17.7 +/- 0.8
N.cm-2). The Po of UT injured muscles were significantly lower than Po
of contralateral control muscles at all time periods. Po of injured
muscles from T were lower than Po from control muscles at 3 and 7 d (P
less than 0.05), but not 14 d. The number of intact fibers of 3-d UT
injured muscles was lower than the number of intact fibers in control
muscles (P < 0.05). No difference in fiber number between controls
and the 3-d treated group was observed. Thus, daily oral bromelain
treatments of 10 mg +/- kg-1 attenuated the development of
contraction-induced injury in hamster EDL muscles.
8) Walker AF, Bundy R, Hicks SM, Middleton RW. Bromelain reduces mild
acute knee pain and improves well-being in a dose-dependent fashion in
an open study of otherwise healthy adults. Phytomedicine. 2002
Dec;9(8):681-6.
Source
Hugh Sinclair Unit of Human Nutrition, The University of Reading, UK. a.f.walker@reading.ac.uk
Abstract
There is preliminary clinical evidence to support the contention that
the anti-inflammatory and analgesic properties of bromelain help to
reduce symptoms of osteo- and rheumatoid arthritis. However, there have
been no controlled studies of its effects on joint health in healthy
subjects who lack such diagnosis. The current study investigated the
effects of bromelain on mild acute knee pain of less than 3 months
duration in otherwise healthy adults. The study was an open,
dose-ranging postal study in volunteers who had been recruited through
newspaper and magazine articles. Two validated questionnaires (WOMAC
knee health Index and the Psychological Well-Being Index) were completed
at baseline and after one month's intervention with bromelain, randomly
allocated to volunteers as either 200 mg or 400 mg per day. Seventy
seven subjects completed the study. In both treatment groups, all WOMAC
symptom dimension scores were significantly reduced compared with
baseline, with reductions in the final battery (total symptom score) of
41 and 59% (P = 0.0001 and <0.0001) in the low and high dose groups
respectively. In addition, improvements in total symptom score (P =
0.036) and the stiffness (P = 0.026) and physical function (P = 0.021)
dimensions were significantly greater in the high-dose (400 mg per day)
compared with the low-dose group. Compared to baseline, overall
psychological well-being was significantly improved in both groups after
treatment (P = 0.015 and P = 0.0003 in the low and high dose groups
respectively), and again, a significant dose-response relationship was
observed. We conclude that bromelain may be effective in ameliorating
physical symptoms and improving general well-being in otherwise healthy
adults suffering from mild knee pain in a dose-dependant manner. Double
blind, placebo-controlled studies are now warranted to confirm these
results.
9) Ley CM, Tsiami A, Ni Q, Robinson N. A review of the use of
bromelain in cardiovascular diseases. Zhong Xi Yi Jie He Xue Bao. 2011
Jul;9(7):702-10.
Source
Social Care and Human Sciences, School of Psychology, University of West London, Middlesex, TW8 9GA, UK.
Abstract
BACKGROUND:
In 2004 an estimated 17.1 million people died from cardiovascular
diseases (CVDs) worldwide, representing 29% of all global deaths.
According to the American Heart Association, heart disease and stroke
are the main cause of death and disability among people with type 2
diabetes. Additional safe and effective approaches are needed for the
prevention and management of CVDs which may include nutritional
supplements.
OBJECTIVE:
To identify the potential of bromelain (a food supplement) on the risk factors associated with CVDs.
SEARCH STRATEGY:
An electronic and manual search was conducted during November 2009 to
March 2010. The databases searched included: Ovid MEDLINE; All EBM
Reviews-Cochrane Database of Systematic Reviews (Cochrane DSR), American
College of Physicians (ACP) Journal Club, Database of Abstracts of
Reviews of Effects (DARE), Cochrane Central Register of Controlled
Trials (CCTR), Cochrane Methodology Register (CMR), Health Technology
Assessment (HTA) and National Health Service Economic Evaluation
Database (NHSEED); Allied and Complementary Medicine (AMED); British
Nursing Index and Archive; EMBASE; Health Management Information
Consortium (HMIC); ScienceDirect and Electronic Thesis Online Services
(ETHOS). Only papers in the English language were included.Back to previous page
INCLUSION CRITERIA:
Randomised controlled trials (RCTs), human studies, animal studies and
experimental studies related to bromelain for CVDs. Data extraction and
analysis: The quality assessment of all the selected studies was
conducted by the authors. Data from 3 animal trials and 3 human trials
were included in the review. Data collected included: type of trial,
drug dosage, duration, outcome measures, characteristics of bromelain
used, significance of results and conclusion.
RESULTS:
Out of 223 papers retrieved, 6 papers met the inclusion criteria and
could be included in the review. These comprised of 3 animal and 3 human
trials, each of which investigated the use of bromelain for CVDs.
Results suggested that bromelain could be used for treating acute
thrombophlebitis, as it decreases aggregation of blood platelets, has a
cardio-protective effect, ameliorates rejection-induced arterial wall
remodelling, prevents thrombin-induced human platelet aggregation as
well as reduces thrombus formation.
CONCLUSION:
No substantive study of bromelain and clinical CVDs has been carried
out in human populations. Only a few studies on bromelain and CVDs were
published from 1948 to 2010. This may be an area worthy to be explored
in future CVDs research.
10) Loskutoff DJ, Quigley JP. PAI-1, fibrosis, and the elusive
provisional fibrin matrix. J Clin Invest. 2000 Dec;106(12):1441-3.
Whether induced surgically or by hypertension, infections, extreme
heat, or caustic chemicals, tissue injury invariably leads to
vasodilatation, with subsequent leakage of plasma proteins into the
connective tissues, rapid activation of the coagulation cascade, and
deposition of fibrin. A central paradigm in the field is that the fibrin
is organized into a "provisional fibrin matrix," which acts as a road
map to direct the migration of invading cells. Leukocytes and possibly
fibroblasts migrate into the area and elaborate cytokines which, in
turn, stimulate resident cells to synthesize and deposit collagens and
other insoluble fibrillar components into the evolving extracellular
matrix (ECM).
Fibrotic disease occurs when normal control of this process is
compromised and excess fibrous material accumulates in the tissues. It
is generally assumed that the persistence of fibrin in the matrix
promotes fibrosis, and that the extent of fibrosis is limited by that
remove the fibrin (i.e., the fibrinolytic system). In a recent issue of
the JCI, Hattori et al. (1) affirm previous suggestions that plasminogen
activator inhibitor-1 (PAI-1) promotes pathological fibrosis but
challenges the concept that fibrin is required.
11) Felton GE. Fibrinolytic and antithrombotic action of bromelain
may eliminate thrombosis in heart patients. Med Hypotheses. 1980
Nov;6(11):1123-33.
Abstract
It has been established that a bromelain plasminogen activator will
produce plasmin in rat experiments. In addition the plasmin cleaves
Hageman factor in a way that leads to a strong release of kallikrein but
a weak release of thrombin. A possible mechanism is suggested to
explain how the body can maintain thrombin at a level too low to cause
platelet aggregation but adequate to stimulate release of prostaglandins
and enzymes for more than 24 hours from a single dose of the pineapple
enzymes. Since bromelain therapy leads to formation of platelets with
increased resistance to aggregation, it is obvious that the dominant
endogenous prostaglandins being produced must be from the group that
increases platelet cyclicAMP levels (prostacyclin, PGE1, etc.). The
combination of fibrinolytic and antithrombic properties appear to be
effective and two large scale tests on heart patients have shown a
practically complete elimination of thrombosis.
12) Bracale G, Selvetella L. [Clinical study of the efficacy of and
tolerance to seaprose S in inflammatory venous disease. Controlled study
versus serratio-peptidase]. Minerva Cardioangiol. 1996
Oct;44(10):515-24.
[Article in Italian]
Source
Divisione di Chirurgia Vascolare, Università degli Studi di Napoli, Federico II.
Abstract
This study was designed to compare the efficacy and safety of seaprose
S and serratio-peptidase in the treatment of venous inflammatory
disease. Forty patients entered the study (11 males, 29 females), mean
age 54.3 years (range 30-77), mean weight 74.8 kg (range 51-96), with
superficial thrombophlebitis. The trial was conducted following a
controlled, between patients, randomized experimental design. Seaprose S
was administered as 30 mg tablets at a daily dosage of 90 mg (one tab
t.i.d.), and serratio-peptidase as 5 mg tablets, at a dose of 30 mg per
day (two tabs t.i.d.), both orally, for 14 days. Twenty patients
received seaprose S and 20 serratio-peptidase. The findings indicate
that seaprose S was more effective and better tolerated than
serratio-peptidase. Although the group of patients assigned to seaprose S
had considerably more severe initial symptoms, by the end of treatment
spontaneous pain was reduced 68.7% from the baseline mean score (from
3.2 to 1.0), as compared with a 63.3% reduction in the
serratio-peptidase group (from 3.0 to 1.1). Pain on pressure was reduced
61.1% with seaprose S (from 3.6 to 1.4), compared to 57.6% with the
reference treatment (from 3.3 to 1.4). Edema was reduced respectively
75% (from 1.6 to 0.4) and 56.2% (from 1.6 to 0.7); erythema diminished
72.4% (from 2.9 to 0.8) and 58.3% (from 2.4 to 1.0); nighttime cramps
were 61.1% less (from 1.8 to 0.7) compared with 52.9% (from 1.7 to 0.8);
hemorrhagic suffusion was 53.3% less (from 1.5 to 0.7) compared with
41.7% (from 1.2 to 0.7); cutaneous dystrophy was reduced by 11.1% (from
1.8 to 1.6) and 7.7% (from 1.3 to 1.2). At the end of the treatment with
seaprose S efficacy was assessed as good or excellent in 85% of the
cases, compared with 65% for serratio-peptidase. Seaprose S caused no
adverse reactions. During serratio-peptidase treatment one patient
reported diarrhea, requiring temporary dosage reduction and specific
treatment. It can thus be confirmed that seaprose S was effective and
well tolerated in patients with inflammatory venous diseases.
13) Braga PC, Moretti M, Piacenza A, Montoli CC, Guffanti EE. Effects
of seaprose on the rheology of bronchial mucus in patients with chronic
bronchitis. A double-blind study vs placebo. Int J Clin Pharmacol Res.
1993;13(3):179-85.
Source
Centre for Respiratory Pharmacology, School of Medicine, University of Milan, Italy.
Abstract
There are changes in the rheological characteristics of mucus
(viscoelasticity) in several pulmonary pathologies, and especially in
chronic bronchitis. Seaprose, a proteolytic enzyme, is one of the
pharmacological possibilities for affecting the rheology of bronchial
mucus to correct mucostasis and improve its clearance. The action of
this drug on the viscoelasticity of bronchial mucus was assessed in a
double-blind vs placebo study with 20 randomly balanced chronic
bronchitis patients using a new kind of portable rheometer with special
features designed for routine bronchial mucus analysis in clinical
practice at the patient's bedside. It was found that in the group of
patients who were given the placebo, there were no particular changes in
the rheological behaviour of mucus, while in those patients who were
given seaprose there were significant changes in both viscosity and
elasticity at the end of treatment. Eight days after the end of
treatment with seaprose, there was still a significant beneficial effect
on the viscoelasticity of mucus and a sort of "post-mucolytic effect"
can be postulated. Seaprose also had antiinflammatory action, and since
in chronic bronchitis there are variable degrees of inflammations, its
beneficial long-lasting effect could also be ascribed to this
concomitant action.
14) Moretti M, Bertoli E, Bulgarelli S, Testoni C, Guffanti EE,
Marchioni CF, Braga PC. Effects of seaprose on sputum biochemical
components in chronic bronchitic patients: a double-blind study vs
placebo. Int J Clin Pharmacol Res. 1993;13(5):275-80.
Source
Istituto di Tisiologia e Malattie dell' Apparato Respiratorio, Università di Modena, Italy.
Abstract
Seaprose is a semialkaline proteinase endowed with proteolytic effect
and antiinflammatory activity tested in different clinical trials. There
is clinical evidence that seaprose reduces sputum viscoelastic
properties in chronic hypersecretory bronchitis. The present study
evaluated (in a double-blind design vs. placebo) the activity of
seaprose on bronchial inflammation, mucus glycoprotein secretion and
bronchial humoral defence mechanism in chronic bronchitic patients
clinically stable (10 per group). Markers of bronchial inflammation
(albumin, albumin/total protein ratio) and bronchial infection (DNA), of
mucus glycoproteins (fucose and N-acetylneuraminic acid) and of humoral
defence mechanism (secretory-IgA) were tested in sputum. We found that
ten-day treatment with seaprose (90 mg/day) reduced sputum albumin
during the observation period, the difference being statistically
significant at the 18th day. The sputum albumin/total protein ratio also
decreased by 50% at the end of the study. In the same group, sputum
DNA, secretory-IgA, fucose and N-acetylneuraminic acid remained
unchanged after treatment. The placebo group did not show any
significant changes in the sputum marker substances. This study provides
experimental evidence for the antiinflammatory activity of seaprose on
bronchial mucosa in chronic bronchitic patients studied in a stable
phase of their disease. Furthermore the drug does not seem to affect
mucus glycoprotein secretion or secretory-IgA production.
15) Fitzhugh DJ, Shan S, Dewhirst MW, Hale LP.Bromelain treatment
decreases neutrophil migration to sites of inflammation. Clin Immunol.
2008 Jul;128(1):66-74.
Source
Department of Pathology, DUMC 3712, Duke University Medical Center, Durham, NC 27710, USA.
Abstract
Bromelain, a mixture of proteases derived from pineapple stem, has
been reported to have therapeutic benefits in a variety of inflammatory
diseases, including murine inflammatory bowel disease. The purpose of
this work was to understand potential mechanisms for this
anti-inflammatory activity. Exposure to bromelain in vitro has been
shown to remove a number of cell surface molecules that are vital to
leukocyte trafficking, including CD128a/CXCR1 and CD128b/CXCR2 that
serve as receptors for the neutrophil chemoattractant IL-8 and its
murine homologues. We hypothesized that specific proteolytic removal of
CD128 molecules by bromelain would inhibit neutrophil migration to IL-8
and thus decrease acute responses to inflammatory stimuli. Using an in
vitro chemotaxis assay, we demonstrated a 40% reduction in migration of
bromelain- vs. sham-treated human neutrophils in response to rhIL-8.
Migration to the bacterial peptide analog fMLP was unaffected,
indicating that bromelain does not induce a global defect in leukocyte
migration. In vivo bromelain treatment generated a 50-85% reduction in
neutrophil migration in 3 different murine models of leukocyte migration
into the inflamed peritoneal cavity. Intravital microscopy demonstrated
that although in vivo bromelain treatment transiently decreased
leukocyte rolling, its primary long-term effect was abrogation of firm
adhesion of leukocytes to blood vessels at the site of inflammation.
These changes in adhesion were correlated with rapid re-expression of
the bromelain-sensitive CD62L/L-selectin molecules that mediate rolling
following in vivo bromelain treatment and minimal re-expression of CD128
over the time period studied. Taken together, these studies demonstrate
that bromelain can effectively decrease neutrophil migration to sites
of acute inflammation and support the specific removal of the CD128
chemokine receptor as a potential mechanism of action.Back to previous page
16) Berg A, Peters M, Deibert P, König D, Birnesser H. Bromelain -
Overview and diskussion of therapeutic application and its importance in
sports medicine and sports traumatology. Deutsche Zeitschrift Für
Sportmedizin. Jahrgang 56, Nr. 1 (2005) [German]
Bromelain, a plant-derived proteolytic enzyme, is commercially
available and has been approved as a pharmaceutical preparation.
Bromelain is mainly prescribed for the treatment and prevention of
inflammatory, posttraumatic or postoperative swelling. The mode of
action has been investigated in cell-culture and animal experiments. In
controlled clinical studies in humans, orally-administered Bromelain has
proven its
pharmaceutical efficacy by significantly reducing soft-tissue edema in
the above-mentioned conditions. Therefore, Bromelain is also of
interest for sports medicine and sports traumatology. Oral treatment
with Bromelain has few and only transient and mild side-effects and may
therefore be an effective alternative for non-steroidal
anti-inflammatory drugs in the treatment of posttraumatic edema and
swelling. This review summarizes present knowledge regarding the mode of
action of Bromelain and gives an overview about its practical
applications from a sports-medical point of view.
17) Hong J, Bose M, Ju J, Ryu JH, Chen X, Sang S, Lee MJ, Yang CS.
Modulation of arachidonic acid metabolism by curcumin and related
beta-diketone derivatives: effects on cytosolic phospholipase A(2),
cyclooxygenases and 5-lipoxygenase. Carcinogenesis. 2004
Sep;25(9):1671-9
Source
Susan Lehman Cullman Laboratory for Cancer Research, Department of
Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State
University of New Jersey, Piscataway, NJ 08854, USA.
Abstract
Aberrant arachidonic acid metabolism is involved in the inflammatory
and carcinogenic processes. In this study, we investigated the effects
of curcumin, a naturally occurring chemopreventive agent, and related
beta-diketone derivatives on the release of arachidonic acid and its
metabolites in the murine macrophage RAW264.7 cells and in HT-29 human
colon cancer cells. We also examined their effects on the catalytic
activities and protein levels of related enzymes: cytosolic
phospholipase A(2) (cPLA(2)), cyclooxygenases (COX) as well as
5-lipoxygenase (5-LOX). At 10 micro M, dibenzoylmethane (DBM),
trimethoxydibenzoylmethane (TDM), tetrahydrocurcumin (THC) and curcumin
effectively inhibited the release of arachidonic acid and its
metabolites in lipopolysaccharide (LPS)-stimulated RAW cells and
A23187-stimulated HT-29 cells. Inhibition of phosphorylation of cPLA(2),
the activation process of this enzyme, rather than direct inhibition of
cPLA(2) activity appears to be involved in the effect of curcumin. All
the curcuminoids (10 micro M) potently inhibited the formation of
prostaglandin E(2) (PGE(2)) in LPS-stimulated RAW cells. Curcumin (20
micro M) significantly inhibited LPS-induced COX-2 expression; this
effect, rather than the catalytic inhibition of COX, may contribute to
the decreased PGE(2) formation. Without LPS-stimulation, however,
curcumin increased the COX-2 level in the macrophage cells. Studies with
isolated ovine COX-1 and COX-2 enzymes showed that the curcuminoids had
significantly higher inhibitory effects on the peroxidase activity of
COX-1 than that of COX-2. Curcumin and THC potently inhibited the
activity of human recombinant 5-LOX, showing estimated IC(50) values of
0.7 and 3 micro M, respectively. The results suggest that curcumin
affects arachidonic acid metabolism by blocking the phosphorylation of
cPLA(2), decreasing the expression of COX-2 and inhibiting the catalytic
activities of 5-LOX. These activities may contribute to the
anti-inflammatory and anticarcinogenic actions of curcumin and its
analogs.
18) Sreejayan, Rao MN. Nitric oxide scavenging by curcuminoids. J Pharm Pharmacol. 1997 Jan;49(1):105-7.
Source
Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Manipal, India.
Abstract
Because curcumin, a compound with anti-inflammatory and anticancer
activity, inhibits induction of nitric oxide synthase in activated
macrophages and has been shown to be a potent scavenger of free radicals
we have investigated whether it can scavenge nitric oxide directly.
Curcumin reduced the amount of nitrite formed by the reaction between
oxygen and nitric oxide generated from sodium nitroprusside. Other
related compounds, e.g. demethoxycurcumin, bisdemethoxycurcumin and
diacetylcurcumin were as active as curcumin, indicating that the methoxy
and the phenolic groups are not essential for the scavenging activity.
The results indicate curcumin to be a scavenger of nitric oxide. Because
this compound is implicated in inflammation and cancer, the therapeutic
properties of curcumin against these conditions might be at least
partly explained by its free-radical scavenging properties, including
those toward nitric oxide.
19) Otsuki N, Dang NH, Kumagai E, Kondo A, Iwata S, Morimoto C.
Aqueous extract of Carica papaya leaves exhibits anti-tumor activity and
immunomodulatory effects. J Ethnopharmacol. 2010 Feb 17;127(3):760-7.
Source
Division of Clinical Immunology, Advanced Clinical Research Center,
The Institute of Medical Science, The University of Tokyo, Tokyo, Japan.
Abstract
AIM OF THE STUDY:
Various parts of Carica papaya Linn. (CP) have been traditionally used
as ethnomedicine for a number of disorders, including cancer. There
have been anecdotes of patients with advanced cancers achieving
remission following consumption of tea extract made from CP leaves.
However, the precise cellular mechanism of action of CP tea extracts
remains unclear. The aim of the present study is to examine the effect
of aqueous-extracted CP leaf fraction on the growth of various tumor
cell lines and on the anti-tumor effect of human lymphocytes. In
addition, we attempted to identify the functional molecular weight
fraction in the CP leaf extract.
MATERIALS AND METHODS:
The effect of CP extract on the proliferative responses of tumor cell
lines and human peripheral blood mononuclear cells (PBMC), and cytotoxic
activities of PBMC were assessed by [(3)H]-thymidine incorporation.
Flow cytometric analysis and measurement of caspase-3/7 activities were
performed to confirm the induction of apoptosis on tumor cells. Cytokine
productions by PBMC were measured by ELISA. Gene profiling of the
effect of CP extract treatment was performed by microarray analysis and
real-time RT-PCR.
RESULTS:
We observed significant growth inhibitory activity of the CP extract
on tumor cell lines. In PBMC, the production of IL-2 and IL-4 was
reduced following the addition of CP extract, whereas that of IL-12p40,
IL-12p70, IFN-gamma and TNF-alpha was enhanced without growth
inhibition. In addition, cytotoxicity of activated PBMC against K562 was
enhanced by the addition of CP extract. Moreover, microarray analyses
showed that the expression of 23 immunomodulatory genes, classified by
gene ontology analysis, was enhanced by the addition of CP extract. In
this regard, CCL2, CCL7, CCL8 and SERPINB2 were representative of these
upregulated genes, and thus may serve as index markers of the
immunomodulatory effects of CP extract. Finally, we identified the
active components of CP extract, which inhibits tumor cell growth and
stimulates anti-tumor effects, to be the fraction with M.W. less than
1000.
CONCLUSION:
Since Carica papaya leaf extract can mediate a Th1 type shift in human
immune system, our results suggest that the CP leaf extract may
potentially provide the means for the treatment and prevention of
selected human diseases such as cancer, various allergic disorders, and
may also serve as immunoadjuvant for vaccine therapy.
20) Gayathri B, Manjula N, Vinaykumar KS, Lakshmi BS, Balakrishnan A.
Pure compound from Boswellia serrata extract exhibits anti-inflammatory
property in human PBMCs and mouse macrophages through inhibition of
TNFalpha, IL-1beta, NO and MAP kinases. Int Immunopharmacol. 2007
Apr;7(4):473-82. Source
Centre for Biotechnology, Anna University, Chennai, India.
Abstract
The aim of the present study is to probe the anti-inflammatory
potential of the plant Boswellia serrata by studying the effect of the
crude extract and the pure compound isolated from it on key inflammatory
mediators like TNFalpha, IL-1beta, and NO thus enabling the
understanding of the key signaling events involved. The crude methanolic
extract and the pure compound were analysed for their inhibitory effect
on TNFalpha, IL-1beta and IL-6. The results demonstrated that all three
cytokines are down regulated when PBMCs are cultured in the presence of
crude extract or the pure compound at various time points. Observations
on Th1/Th2 cytokines revealed marked down regulation of Th1 cytokines
IFNgamma and IL-12 while the Th2 cytokines IL-4 and IL-10 were up
regulated upon treatment with crude extract and pure compound. The
extract and the pure compound isolated also showed considerable
inhibition of NO production in activated RAW 264.7 cells, possibly via
suppression of inducible NO synthase mRNA expression. Further to
elucidate the underlying mechanism of action the effect of 12-ursene
2-diketone on LPS-induced activation of MAPK has also been examined. Our
results demonstrated that 12-ursene 2-diketone inhibits the expression
of pro-inflammatory cytokines and mediators via inhibition of
phosphorylation of the MAP kinases JNK and p38 while no inhibition was
seen in ERK phosphorylation in LPS-stimulated PBMCs. The above study
therefore indicates that the crude methanolic extract and the isolated
pure compound are capable of carrying out a natural anti-inflammatory
activity at sites where chronic inflammation is present by switching off
the pro-inflammatory cytokines and mediators, which initiate the
process.
21) Kokkiripati PK, Bhakshu LM, Marri S, Padmasree K, Row AT,
Raghavendra AS, Tetali SD. Gum resin of Boswellia serrata inhibited
human monocytic (THP-1) cell activation and platelet aggregation. J
Ethnopharmacol. 2011 Sep 1;137(1):893-901.
Source
Department of Plant Sciences, University of Hyderabad, Hyderabad 500046, India.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE:
Stem bark gum resin extract of Boswellia serrata is traditionally used
in India for its hemostatic, antiinflammatory and cardiovascular health
effects and it is named as Śallakī in Ayurvedic medicine.
AIM OF THE STUDY:
This study was conducted to evaluate the antioxidative and
antithrombotic properties of stem bark gum resin extracts of Boswellia
serrata (BS).
MATERIALS AND METHODS:
The inhibitory activity of the BSWE and BSAE on FeCl(3) induced lipid
peroxidation (in vitro) in rat liver and heart homogenates was measured
spectrophotometrically. Their effect on H(2)O(2) induced reactive oxygen
species (ROS) generation in human monocytic (THP-1) cells was
investigated by tracking intensity of a cell permeable fluorescent dye,
H(2)DCFDA and subjecting the cell samples to confocal microscopy.
Further, the effect of BSAE and BSWE on ADP-induced platelet aggregation
was assessed using a multimode detection plate reader, plasma
coagulation times using an automated blood coagulation analyzer and on
human blood clotting factors Xa and XIa using chromogenic substrate.
Phytomarker analysis of the water (BSWE) and hydroalcoholic (BSAE)
extracts of BS-gum resin was done through HPLC using a standard compound
AKβBA.Back to previous page
RESULTS:
BSAE and BSWE inhibited, to varied extents, the lipid peroxidation in
liver (80%) and heart (50%) tissue homogenates of male Wistar rats.
Further, BSAE (30 μg dwt/mL) and BSWE (300 μg dwt/mL) attenuated ≥ 60%
of H(2)O(2) mediated ROS generation in THP-1 cells. In case of standard
compounds, ascorbate (20 μg dwt/mL) and butylated hydroxytoluene (BHT)
(10 μg dwt/mL) completely scavenged ROS in the cells. BSAE and BSWE at 3
mg dwt/mL completely inhibited ADP induced platelet aggregation and
activities were comparable to 20 μg/mL of heparin. The extracts also
showed very high activity in prolonging coagulation time periods. Both
types of extracts extended prothrombin time (PT) from ∼13 to >60s and
activated partial thromboplastin time (APTT) from ∼32s to >90s. BSAE
inhibited clotting factors Xa and XIa remarkably at 6 μg of dwt where
as BSWE did not show much effect on FXa and showed 30% inhibition on
FXIa at 120 μg. 10 μg of heparin was required to inhibit about 30%
activity of the above factors. HPLC analyses suggested that BSAE and
BSWE had AKβBA of 9% (w/w) and 7.8% (w/w) respectively.
CONCLUSION:
Present study demonstrated antioxidant and antithrombotic
anticoagulant activities of water and hydroalcoholic extracts of
Boswellia serrata's gum resin. We suggest that BS-gum resin as a good
source for lead/therapeutic compounds possessing antioxidant,
antiplatelet and anticoagulant activities.
22) Piacente S, Montoro P, Oleszek W, Pizza C. Yucca schidigera bark:
phenolic constituents and antioxidant activity. J Nat Prod. 2004
May;67(5):882-5.
Source
Dipartimento di Scienze Farmaceutiche, Università degli Studi di
Salerno, Via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy.
Abstract
Two new phenolic constituents with unusual spirostructures, named
yuccaols D (1) and E (2), were isolated from the MeOH extract of Yucca
schidigera bark. Their structures were established by spectroscopic
(ESIMS and NMR) analysis. The new yuccaols D and E, along with
resveratrol (3), trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene (4),
yuccaols A-C (5-7), yuccaone A (8), larixinol (9), the MeOH extract of
Yucca schidigera bark, and the phenolic portion of this extract, were
assayed for antioxidant activity by measuring the free radical
scavenging effects using two different assays, namely, the Trolox
Equivalent Antioxidant Capacity (TEAC) assay and the coupled oxidation
of beta-carotene and linoleic acid (autoxidation assay). The significant
activities exhibited by the phenolic fraction and its constituents in
both tests show the potential use of Y. schidigera as a source of
antioxidant principles.
23) Cheeke PR, Piacente S, Oleszek W. Anti-inflammatory and
anti-arthritic effects of Yucca schidigera: a review. J Inflamm (Lond).
2006 Mar 29;3:6.
Source
Department of Animal Sciences, Oregon State University, Corvallis, OR 97333, USA. peter.r.cheeke@oregonstate.edu
Abstract
Yucca schidigera is a medicinal plant native to Mexico. According to
folk medicine, yucca extracts have anti-arthritic and anti-inflammatory
effects. The plant contains several physiologically active
phytochemicals. It is a rich source of steroidal saponins, and is used
commercially as a saponin source. Saponins have diverse biological
effects, including anti-protozoal activity. It has been postulated that
saponins may have anti-arthritic properties by suppressing intestinal
protozoa which may have a role in joint inflammation. Yucca is also a
rich source of polyphenolics, including resveratrol and a number of
other stilbenes (yuccaols A, B, C, D and E). These phenolics have
anti-inflammatory activity. They are inhibitors of the nuclear
transcription factor NFkappaB. NFkB stimulates synthesis of inducible
nitric oxide synthase (iNOS), which causes formation of the inflammatory
agent nitric oxide. Yucca phenolics are also anti-oxidants and
free-radical scavengers, which may aid in suppressing reactive oxygen
species that stimulate inflammatory responses. Based on these findings,
further studies on the anti-arthritic effects of Yucca schidigera are
warranted.
THE PHENOLS FOUND IN YUCCA SCHIDIGERA HAVE ANTI-INFLAMMATORY
ACTIVITIES AND INHIBIT NITRIC OXIDE, WHICH IS AN INFLAMMATORY AGENT.
THEY ALSO HAVE ANTIOXIDANT ACTIVITIES WHICH MAY MODULATE INFLAMMATORY
RESPONSE. FULL STUDY AVAILABLE HERE:
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1440857/ Anti-inflammatory
and anti-arthritic effects of yucca schidigera: A review (FULL STUDY)
24) Grzanna R, Lindmark L, Frondoza CG. Ginger--an herbal medicinal
product with broad anti-inflammatory actions. J Med Food. 2005
Summer;8(2):125-32.
Source
RMG Biosciences, Inc.
Abstract
The anti-inflammatory properties of ginger have been known and valued
for centuries. During the past 25 years, many laboratories have provided
scientific support for the long-held belief that ginger contains
constituents with antiinflammatory properties. The original discovery of
ginger's inhibitory effects on prostaglandin biosynthesis in the early
1970s has been repeatedly confirmed. This discovery identified ginger as
an herbal medicinal product that shares pharmacological properties with
non-steroidal anti-inflammatory drugs. Ginger suppresses prostaglandin
synthesis through inhibition of cyclooxygenase-1 and cyclooxygenase-2.
An important extension of this early work was the observation that
ginger also suppresses leukotriene biosynthesis by inhibiting
5-lipoxygenase. This pharmacological property distinguishes ginger from
nonsteroidal anti-inflammatory drugs. This discovery preceded the
observation that dual inhibitors of cyclooxygenase and 5-lipoxygenase
may have a better therapeutic profile and have fewer side effects than
non-steroidal anti-inflammatory drugs. The characterization of the
pharmacological properties of ginger entered a new phase with the
discovery that a ginger extract (EV.EXT.77) derived from Zingiber
officinale (family Zingiberaceae) and Alpina galanga (family
Zingiberaceae) inhibits the induction of several genes involved in the
inflammatory response. These include genes encoding cytokines,
chemokines, and the inducible enzyme cyclooxygenase-2. This discovery
provided the first evidence that ginger modulates biochemical pathways
activated in chronic inflammation. Identification of the molecular
targets of individual ginger constituents provides an opportunity to
optimize and standardize ginger products with respect to their effects
on specific biomarkers of inflammation. Such preparations will be useful
for studies in experimental animals and humans.
25) Ernst E, Pittler MH. Efficacy of ginger for nausea and vomiting: a
systematic review of randomized clinical trials. Br J Anaesth. 2000
Mar;84(3):367-71.
Source
Department of Complementary Medicine, School of Postgraduate Medicine and Health Sciences, University of Exeter, UK.
Abstract
Ginger (Zingiber officinale) is often advocated as beneficial for
nausea and vomiting. Whether the herb is truly efficacious for this
condition is, however, still a matter of debate. We have performed a
systematic review of the evidence from randomized controlled trials for
or against the efficacy of ginger for nausea and vomiting. Six studies
met all inclusion criteria and were reviewed. Three on postoperative
nausea and vomiting were identified and two of these suggested that
ginger was superior to placebo and equally effective as metoclopramide.
The pooled absolute risk reduction for the incidence of postoperative
nausea, however, indicated a non-significant difference between the
ginger and placebo groups for ginger 1 g taken before operation
(absolute risk reduction 0.052 (95% confidence interval -0.082 to
0.186)). One study was found for each of the following conditions:
seasickness, morning sickness and chemotherapy-induced nausea. These
studies collectively favoured ginger over placebo.
26) Huang TH, Tran VH, Duke RK, Tan S, Chrubasik S, Roufogalis BD,
Duke CC. Harpagoside suppresses lipopolysaccharide-induced iNOS and
COX-2 expression through inhibition of NF-kappa B activation. J
Ethnopharmacol. 2006 Mar 8;104(1-2):149-55.
Source
Pharmaceutical Chemistry and Herbal Medicines Research and Education
Centre, Faculty of Pharmacy A15, University of Sydney, NSW 2006,
Australia.
Abstract
Preparations of Harpagophytum procumbens, known as devil's claw, are
used as an adjunctive therapy for the treatment of pain and
osteoarthritis. Pharmacological evaluations have proven the
effectiveness of this herbal drug as an anti-inflammatory and analgesic
agent. The present study has investigated the mechanism of action of
harpagoside, one of the major components of Harpagophytum procumbens,
using human HepG2 hepatocarcinoma and RAW 264.7 macrophage cell lines.
Harpagoside inhibited lipopolysaccharide-induced mRNA levels and protein
expression of cyclooxygenase-2 and inducible nitric oxide in HepG2
cells. These inhibitions appeared to correlate with the suppression of
NF-kappaB activation by harpagoside, as pre-treating cells with
harpagoside blocked the translocation of NF-kappaB into the nuclear
compartments and degradation of the inhibitory subunit IkappaB-alpha.
Furthermore, harpagoside dose-dependently inhibited LPS-stimulated
NF-kappaB promoter activity in a gene reporter assay in RAW 264.7 cells,
indicating that harpagoside interfered with the activation of gene
transcription. These results suggest that the inhibition of the
expression of cyclooxygenase-2 and inducible nitric oxide by harpagoside
involves suppression of NF-kappaB activation, thereby inhibiting
downstream inflammation and subsequent pain event.
27) Kidd P. Glutathione: Systemic Protectant Against Oxidative and Free Radical Damage. Alt Med Rev. 1997; Vol.2 (3):155-76.
ABSTRACT
The tripeptide thiol glutathione (GSH) has facile electron-donating
capacity, linked to its sulfhydryl (―SH) group. Glutathione is an
important water-phase antioxidant and essential cofactor for antioxidant
enzymes; it provides protection also for the mitochondria against
endogenous oxygen radicals. Its high electron-donating capacity combined
with its high intracellular concentration endows GSH with great
reducing power, which is used to regulate a complex thiol-exchange
system (―SH ↔ ―S-S―). This functions at all levels of cell activity,
from the relatively simple (circulating cysteine/―SH thiols, ascorbate,
other small molecules) to the most complex (cellular ―SH proteins).
Glutathione is homeostatically controlled, both inside the cell and
outside. Enzyme systems synthesize it, utilize it, and regenerate it as
per the gamma-glutamyl cycle. Glutathione is most concentrated in the
liver (10 mM), where the "P450 Phase II" enzymes require it to convert
fat-soluble substances into water-soluble GSH conjugates, in order to
facilitate their excretion. While providing GSH for their specific
needs, the liver parenchymal cells export GSH to the outside, where it
serves as systemic source of ―SH/reducing power.
GSH depletion leads to cell death, and has been documented in many
degenerative conditions. Mitochondrial GSH depletion may be the ultimate
factor determining vulnerability to oxidant attack. Oral ascorbate
helps conserve GSH; cysteine is not a safe oral supplement, and of all
the oral GSH precursors probably the least flawed and most
cost-effective NAC (N-acetylcysteine). FULL STUDY AVAILABLE HERE:
http://www.dockidd.com/pdf/KiddGSHAMR.pdf
28) Dieber-Rotheneder M, Puhl H, Waeg G, Striegl G, Esterbauer H.
Effect of oral supplementation with D-alpha-tocopherol on the vitamin E
content of human low density lipoproteins and resistance to oxidation. J
Lipid Res. 1991 Aug;32(8):1325-32.
Source
Institute of Biochemistry, University of Graz, Austria.
Abstract
Twelve clinically healthy subjects participated in a vitamin E
supplementation study. Eight were given daily dosages of 150, 225, 800,
or 1200 IU RRR-alpha-tocopherol for 21 days (two persons per dose) and
four received placebo. Prior, during, and after the supplementation
period, alpha-tocopherol, gamma-tocopherol, and carotenoids were
determined in plasma and low density lipoprotein (LDL). The maximum
levels of alpha-tocopherol were 1.7- to 2.5-times the baseline values in
plasma and 1.7- to 3.1-times in LDL. A high correlation existed between
alpha-tocopherol in plasma and LDL. gamma-Tocopherol significantly
decreased in plasma and LDL during vitamin E supplementation. No
significant influence on the lipoprotein and lipid status and carotenoid
levels of the participants occurred throughout the supplementation. The
resistance of LDL against copper-mediated oxidation was also measured.
The oxidation resistance of LDL was significantly higher during vitamin E
supplementation. However, the efficacy of vitamin E in protecting LDL
varied from person to person. The statistical evaluation of all data
gave a correlation of r2 = 0.51 between alpha-tocopherol in LDL and the
oxidation resistance as measured by the length of the lag-phase
preceding the oxidation of LDL. No association was seen between levels
of carotenoids and vitamin E in plasma and LDL. The present study
clearly shows that in humans the oxidation resistance of LDL can be
increased by vitamin E supplementation. FULL STUDY AVAILABLE HERE:
http://www.jlr.org/content/32/8/1325.full.pdf
SUPPLEMENTING WITH VITAMIN E REDUCES LDL OXIDATION.
NOTE: 1 IU of tocopherol is defined as ⅔ milligrams of RRR-alpha-tocopherol (formerly named d-alpha-tocopherol)
29) Reaven PD, Khouw A, Beltz WF, Parthasarathy S, Witztum JL. Effect
of dietary antioxidant combinations in humans. Protection of LDL by
vitamin E but not by beta-carotene. Arterioscler Thromb. 1993
Apr;13(4):590-600.
Source
Department of Medicine, University of California, San Diego, La Jolla 92093-0682.
Abstract
Experimental and epidemiological evidence supports the hypothesis that
oxidation of low density lipoprotein (LDL) appears to be important in
mediating the atherogenicity of LDL. To test this hypothesis in humans,
it will be necessary to perform intervention studies in large
populations. We performed two studies to assess the effectiveness of
supplementation with beta-carotene and vitamin E, used alone and in
combination with each other, and with vitamin C, to protect LDL from
oxidation. In phase 1, after a placebo period, eight subjects were given
beta-carotene (60 mg/day) for 3 months, then beta-carotene plus vitamin
E (1,600 mg/day) for another 3 months, and then beta-carotene plus
vitamin E plus vitamin C (2 g/day) for 3 months. During phase 2,
beta-carotene and vitamin C were discontinued, and subjects took only
vitamin E for 5 months. During each period, LDL samples were isolated,
and measurements of susceptibility to oxidation were performed.
beta-Carotene levels in LDL increased nearly 20-fold, but LDL
susceptibility to oxidation did not change. Addition of vitamin E
increased LDL vitamin E levels nearly 2.5-fold, and this decreased LDL
oxidation 30-40%. During the vitamin C supplementation period, plasma
levels of beta-carotene and vitamin E rose, but only beta-carotene
increased in LDL. However, the susceptibility of LDL to oxidation in
this period was not decreased further. During phase 2, when subjects
took only vitamin E, LDL susceptibility to oxidation was decreased by
50% as measured by thiobarbituric acid-reactive substances, conjugated
dienes, and lipid peroxide formation as well as by macrophage
degradation. Thus, long-term supplementation with large doses of vitamin
E alone, but not beta-carotene, conferred increased protection to LDL
in in vitro assays of oxidation. These data should be useful in planning
therapeutic strategies to test the antioxidant hypothesis in humans.
30) Boshtam M, Rafiei M, Sadeghi K, Sarraf-Zadegan N. Vitamin E can
reduce blood pressure in mild hypertensives. Int J Vitam Nutr Res. 2002
Oct;72(5):309-14.
Source
Isfahan Cardiovascular Research Center, PO Box 81465-1148, Isfahan, Iran.
Abstract
This triple-blind placebo-controlled clinical trial was performed to
determine the effects of the anti-oxidant vitamin E on blood pressure
and heart rate in patients with mild hypertension. A total of 70 new
mild hypertensive subjects (systolic blood pressure, SBP: 140-160 mmHg;
diastolic blood pressure, DBP: 90-100 mmHg) without secondary
hypertension were selected from among people referred to the
Hypertension Unit of Isfahan Cardiovascular Research Center and divided
randomly into two groups of drug (DG) and placebo (PG). All subjects
were aged from 20 to 60 years old, without any other cardiovascular risk
factors. The drug group received vitamin E tablets (200 IU/day) and the
placebo group received placebo only for 27 weeks. At the beginning and
the end of the study, the blood vitamin E level was measured
fluorimetrically in all subjects according to the Hansen and Warwick
method [14, 15]. Blood pressure and heart rate were measured at the
beginning, during, and at the end of the study. Blood pressure was
measured by a physician using one random zero mercury sphygmomanometer.
Personal information and dietary habits of subjects were collected by
separate questionnaire. At the end of the study, it was found that the
vitamin E supplement had caused a remarkable decrease in SBP (-24% in DG
versus -1.6% in PG) and a less remarkable decrease in DBP (-12.5% in DG
versus -6.2% in PG) (p < 0.05). The change in heart rate was -4.3%
in DG, and -14.0% in PG (p < 0.05). It is concluded that a vitamin E
supplement of 200 IU/day can be effective in mild hypertensive patients
in the long term, probably due to nitric oxide, and improve their blood
pressure status. Therefore, vitamin E supplement could be recommended to
such patients.
31) Office of Dietary Supplements - National Institutes of Health
http://ods.od.nih.gov/factsheets/vitamine/#en6 last accessed 03/12/2012
Vitamin E is a fat-soluble antioxidant that stops the production of
ROS formed when fat undergoes oxidation. Scientists are investigating
whether, by limiting free-radical production and possibly through other
mechanisms, vitamin E might help prevent or delay the chronic diseases
associated with free radicals.
In addition to its activities as an antioxidant, vitamin E is involved
in immune function and, as shown primarily by in vitro studies of
cells, cell signaling, regulation of gene expression, and other
metabolic processes [1]. Alpha-tocopherol inhibits the activity of
protein kinase C, an enzyme involved in cell proliferation and
differentiation in smooth muscle cells, platelets, and monocytes [6].
Vitamin-E–replete endothelial cells lining the interior surface of blood
vessels are better able to resist blood-cell components adhering to
this surface. Vitamin E also increases the expression of two enzymes
that suppress arachidonic acid metabolism, thereby increasing the
release of prostacyclin from the endothelium, which, in turn, dilates
blood vessels and inhibits platelet aggregation [6].
32) Martha Clare Morris, ScD; Denis A. Evans, MD; Julia L. Bienias,
ScD; Christine C. Tangney, PhD; Robert S. Wilson, PhD. Vitamin E and
Cognitive Decline in Older Persons. Arch Neurol. 2002;59:1125-1132.
Background Previous studies raise the possibility that antioxidants protect against neurodegenerative diseases.
Objective To examine whether intake of antioxidant nutrients,
including vitamin E, vitamin C, and carotene, is associated with reduced
cognitive decline with age.
Design Longitudinal population-based study conducted from September
17, 1993, to November 20, 2000, with an average follow-up of 3.2 years.
Patients The patients were 2889 community residents, aged 65 to 102
years, who completed a food frequency questionnaire, on average 18
months after baseline.
Main Outcome Measure Cognitive change as measured by 4 tests (the
East Boston Memory Test, which tests immediate and delayed recall; the
Mini-Mental State Examination; and the Symbol Digit Modalities Test) at
baseline and 3 years for all participants, and at 6 months for 288
randomly selected participants.
Results We used random-effects models to estimate nutrient effects on
individual change in the average score of the 4 cognitive tests. The
cognitive score declined on average by 5.0 x 10-2 standardized units per
year. There was a 36% reduction in the rate of decline among persons in
the highest quintile of total vitamin E intake (-4.3 x 10-2
standardized units per year) compared with those in the lowest quintile
(-6.7 x 10-2 standardized units per year) (P = .05), in a model adjusted
for age, race, sex, educational level, current smoking, alcohol
consumption, total calorie (energy) intake, and total intakes of vitamin
C, carotene, and vitamin A. We also observed a reduced decline with
higher vitamin E intake from foods (P = .03 for trend). There was little
evidence of association with vitamin C or carotene intake.
Conclusion Vitamin E intake, from foods or supplements, is associated with less cognitive decline with age.
Back to previous page
33) Teixeira S. Bioflavonoids: proanthocyanidins and quercetin and
their potential roles in treating musculoskeletal conditions. J Orthop
Sports Phys Ther. 2002 Jul;32(7):357-63.
Source
Huber Associates, Auburn, ME 04210, USA. shan.tex@verizon.net
Abstract
As a clinician treating musculoskeletal conditions, one is continually
in search of safe and more effective treatment methods that will hasten
tissue healing. Chronic inflammation has been shown to cause connective
tissue degradation. Typically, nonsteroidal anti-inflammatory drugs
(NSAIDs) and/or corticosteroids are used to control the inflammatory
process, however, long-term use has been associated with potentially
serious side effects. The purpose of this article is to introduce and
describe literature on 2 natural compounds, namely, proanthocyanidin
(PCO) and quercetin, which are 2 specific types of bioflavonoids, and to
discuss their potential benefits in treating musculoskeletal
conditions. There is evidence to suggest that flavonoids may be
beneficial to connective tissue for several reasons, which include the
limiting of inflammation and associated tissue degradation, the
improvement of local circulation, as well as the promoting of a strong
collagen matrix. An overview of bioflavonoids as well as relevant
research, safety issues, absorption, and specific sources of PCO and
quercetin in foods and through supplementation is included.
Inflammation and Tissue Degradation
Inflammation is a normal biological process and the primary means by
which tissue healing is initiated and infection is limited in the human
body. However, chronic inflammation has been shown to cause connective
tissue degradation. This occurs through 2 primary mechanisms: (1)
proteolytic enzymes and (2) oxygen-free radicals such as superoxide ion
(O2), singlet, and hydroxyl radicals.
Proteolytic enzymes including elastase, collagenase, and hyaluronidase
are involved in the inflammatory process and are associated with the
presence of polymorphonuclear leukocytes (PMNs) and macrophages. They
have been shown to be more prevalent in
tissue with chronic conditions and to cause degradation of collagen,
elastin, and hyaluronic acid.FULL STUDY AVAILABLE HERE:
http://www.osptla.com/JOSPT%20Flavonoid%20Article.pdf
34) Ishita Chattopadhyay, Kaushik Biswas, Uday Bandyopadhyay and
Ranajit K. Banerjee. Turmeric and curcumin: Biological actions and
medicinal applications.
Current Science, 2004, Jul 10, vol. 87, no. 1
Turmeric (Curcuma longa) is extensively used as a spice, food
preservative and colouring material in India, China and South East Asia.
It has been used in traditional medicine as a household remedy for
various diseases, including biliary disorders, anorexia, cough, diabetic
wounds, hepatic disorders, rheumatism and sinusitis. For the last few
decades, extensive work has been done to establish the biological
activities and pharmacological actions of turmeric and its extracts.
Curcumin (diferuloylmethane), the main yellow bioactive component of
turmeric has been shown to have a wide spectrum of biological actions.
These include its antiinflammatory, antioxidant, anticarcinogenic,
antimutagenic, anticoagulant, antifertility, antidiabetic,
antibacterial, antifungal, antiprotozoal, antiviral, antifibrotic,
antivenom, antiulcer, hypotensive and hypocholesteremic activities. Its
anticancer effect is mainly mediated through induction of apoptosis.
Its antiinflammatory, anticancer and antioxidant roles may be clinically
exploited to control rheumatism, carcinogenesis and oxidative
stress-related pathogenesis. Clinically, curcumin has already been used
to reduce post-operative inflammation. Safety evaluation studies
indicate that both turmeric and curcumin are well tolerated at a very
high dose without any toxic effects. Thus, both turmeric and curcumin
have the potential for the development of modern medicine for the
treatment of various diseases. FULL STUDY AVAILABLE HERE:
http://repository.ias.ac.in/5196/1/306.pdf
OTHER RELATED RESEARCH
Hale LP, Greer PK, Sempowski GD. Bromelain treatment alters leukocyte
expression of cell surface molecules involved in cellular adhesion and
activation. Clin Immunol. 2002 Aug;104(2):183-90.
Source
Department of Pathology, Duke University, Durham, NC 27710, USA.
Abstract
Bromelain is a natural proteinase preparation derived from pineapple
stem that is marketed for oral use as a digestive aid and as an
antiinflammatory agent. Bromelain treatment in vitro has been previously
shown to selectively remove certain cell surface molecules that may
affect lymphocyte migration and activation. This study reports the
effects of bromelain on a broad range of cell surface molecules and on
lymphocytes, monocytes, and granulocytes under physiologically relevant
conditions. In vitro bromelain treatment of leukocytes in whole blood
proteolytically altered 14 of 59 leukocyte markers studied.
Constitutively expressed bromelain-sensitive molecules included CD7,
CD8alpha, CD14, CD16, CD21, CD41, CD42a, CD44, CD45RA, CD48, CD57,
CD62L, CD128a, and CD128b. The proteolytic effect of bromelain increased
as the concentration of plasma decreased, with EC50 ranging from
>1000 microg/ml for 100% plasma to approximately 1 microg/ml in the
absence of plasma, indicating the presence of an inhibitor of bromelain
in plasma. alpha2-macroglobulin purified from plasma mimicked the
inhibitory effect of whole plasma on bromelain activity. If proteolysis
is required for the antiinflammatory actions of oral bromelain, these
data suggest that the required concentrations are more likely to be
achieved locally in the gastrointestinal tract or in other tissue sites
where the plasma concentration is low, rather than in the bloodstream.
The cell surface molecules altered by bromelain are involved in
leukocyte homing and cellular adhesion and activation. Thus bromelain
could potentially exert an antiinflammatory effect by multiple
mechanisms, including alterations in leukocyte migration and activation.
THE ANTIINFLAMMATORY EFFECT OF BROMELAIN MAY BE CAUSED BY AN ALTERATION IN LEUKOCYTE MIGRATION AND ACTIVATION.
Masson M. [Bromelain in blunt injuries of the locomotor system. A
study of observed applications in general practice]. Fortschr Med. 1995
Jul 10;113(19):303-6.
[Article in German]
Abstract
METHOD: In an open case observation study involving patients with
blunt injuries to the musculoskeletal system, the efficacy and
tolerability of high-dose Bromelain POS, a plant-derived enzyme
preparation, were investigated. The investigating physician was an
orthopedic surgeon who, in addition to the usual therapeutic measures,
treated 59 of his patients with the bromelaine preparation. The duration
of the application was determined by the nature and severity of the
lesion, and varied between one and three weeks. The test criteria were
swelling, pain at rest and during movement, and tenderness. These
parameters were evaluated on the day of the injury and on five
subsequent dates. RESULTS: Treatment with bromelaine resulted in a clear
reduction in all four parameters tested. Both swelling and the symptoms
of pain had improved appreciably at all evaluation time points as
compared with baseline. The tolerability of the preparation was very
good, and patient compliance was correspondingly high.
What was dosage? Where is full study? What is bromelain pos?
Brien S, Lewith G, Walker A, Hicks SM, Middleton D. Bromelain as a
Treatment for Osteoarthritis: a Review of Clinical Studies. Evid Based
Complement Alternat Med. 2004 Dec;1(3):251-257.
Abstract
Bromelain, an extract from the pineapple plant, has been demonstrated
to show anti-inflammatory and analgesic properties and may provide a
safer alternative or adjunctive treatment for osteoarthritis. All
previous trials, which have been uncontrolled or comparative studies,
indicate its potential use for the treatment of osteoarthritis. This
paper reviews the mechanism of its putative therapeutic actions, those
clinical trials that have assessed its use in osteoarthritis to date, as
well as considering the safety implications of this supplement for
osteoarthritis and reviewing the evidence to date regarding the dosage
for treating this condition. The data available at present indicate the
need for trials to establish the efficacy and optimum dosage for
bromelain and the need for adequate prospective adverse event monitoring
in such chronic conditions as osteoarthritis.
Find full study. Not enough here to draw conclusions.
Fossati A. Antiinflammatory effects of seaprose-S on various inflammation models. Drugs Exp Clin Res. 1999;25(6):263-70.
AbstractBack to previous page
The antiinflammatory activity of seaprose-S in different experimental
models involving different biochemical mediators of inflammation was
investigated. In vivo experiments were performed using male
Sprague-Dawley rats and in vitro experiments were performed using
articular cartilage explants of pig joints. In acute experimental models
of inflammation, 0.5, 1 or 2 mg/kg of seaprose-S was injected
intravenously (i.v.) before challenge with inflammatory agents. In
adjuvant-induced arthritis, seaprose-S was given as a 2 mg/kg i.v. dose
once a day for 4 consecutive days from day 8 after injection of the
adjuvant. In cartilage-synovium cocultures, seaprose-S was incubated at a
concentration of 0.001 microM and 0.05 microM. Paw volume was measured
with a plethysmograph and proteoglycan synthesis was determined in
articular cartilage-synovium coculture by incorporation of 35S-sulfate.
Seaprose-S inhibited inflammation dose-dependently in carrageenan,
concanavalin-A, FeCl2, nystatin-induced paw edema and in
carrageenan-induced pleurisy and acetic acid-induced peritonitis. In
Freund's adjuvant-induced arthritis, seaprose-S significantly reduced
the primary and secondary lesions. In vitro on articular cartilage,
seaprose-S increased proteoglycan synthesis in the cartilage alone and
reduced the inhibition of proteoglycan synthesis in the cartilage
cocultured with minced synovium.
IN THIS ANIMAL STUDY SEAPROSE S WAS SHOWN TO HAVE ANTI-INFLAMMATORY ACTIVITY.
Esch PM, Gerngross H, Fabian A. [Reduction of postoperative swelling.
Objective measurement of swelling of the upper ankle joint in treatment
with serrapeptase-- a prospective study]. Fortschr Med. 1989 Feb
10;107(4):67-8, 71-2.
[Article in German]
Abstract
Using a quantitative standardized procedure, the swelling of the ankle
produced by supination trauma was measured. In the 66 patients with
fresh rupture of the lateral ligament treated surgically at our
Department between December 1986 and April 1987, a prospective study of
the effect of serrapeptase (Aniflazym) SILKWORM! on post-operative
swelling and pain was carried out in 3 randomized groups of patients. In
the group receiving the test substance, the swelling had decreased by
50% on the third post-operative day, while in the other two control
groups (elevation of the leg, bed rest, with and without the application
of ice) no reduction in swelling had occurred at that time. The
difference is statistically significant (p = 0.013). Decreasing pain
correlated for the most part with the reduction in swelling. Thus, the
patients receiving the test substance more rapidly became pain-free than
did the control groups. On the basis of these results, serrapeptase
would appear to be an effective preparation for the post-operative
reduction of swelling, in comparison with the classical conservative
measures, for example, the application of ice.
SERRAPEPTASE IN ANIFLAYZM IS FROM SILKWORMS, SO THIS STUDY IS NOT APPLICABLE
Selloum L, Bouriche H, Tigrine C, Boudoukha C. Anti-inflammatory
effect of rutin on rat paw oedema, and on neutrophils chemotaxis and
degranulation. Exp Toxicol Pathol. 2003 Mar;54(4):313-8.
Source
Laboratory of Applied Biochemistry, Department of Biology, Faculty of
Sciences, University of Ferhat ABBAS, 19000 Setif, Algeria.
laidsel@yahoo.com
Abstract
BACKGROUND:
Rutin, a natural flavone derivative, is known for its pharmacological
properties. We have previously reported that this flavonol exerted a
potent inhibitory effect on respiratory burst of fMet-Leu-Phe-stimulated
neutrophils, as well as on phosphoinositide 3-kinase gamma activity in a
cell free system. In the present study, the anti-inflammatory effect of
rutin was investigated in vivo and in vitro.
METHODS:
rutin or aspirin (100 mg/kg, body weight) were given orally to rats 1
hour before paw oedema induction, using lambda-carrageenan 1%. The rat
paw volume was measured by mean of plethysmometer, initially and during 6
hours. The chemotaxis of neutrophils towards 10(-7) M fMet-Leu-Phe was
performed using 48-well chemotaxis chamber. Neutrophils that migrated
through 5 microm pore size polycarbonate filter, in presence or in
absence of rutin, were counted microscopically. Elastase exocytosis of
either phorbol 12-myristate 13-acetate or fMet-Leu-Phe/cytochalasin
B-stimulated neutrophils was assessed in absence or in presence of rutin
using the synthetic substrate N-Suc-Ala-Ala-Ala-p-nitroanilide. The
absorbance of released p-nitroaniline was measured at 405 nm using
microplate reader.
RESULTS:
The maximal swelling in placebo group was observed at 5 hours, after
lambda-carrageenan injection. Oral administration of rutin reduced rat
paw swelling starting 2 hours after lambda-carrageenan injection. Rutin
reduced significantly (p < 0.05) and in a dose-dependant manner the
polymorphonuclear neutrophils chemotaxis to fMet-Leu-Phe. Furthermore,
elastase exocytosis, induced by both stimuli, was partially inhibited by
rutin up to 25 microM.
CONCLUSION:
The present study revealed that rutin possesses anti-inflammatory properties.
IN THIS ANIMAL STUDY, ORAL ADMINISTRATION OF RUTIN REDUCED SWELLING WITHIN TWO HOURS.
Guardia T, Rotelli AE, Juarez AO, Pelzer LE. Anti-inflammatory
properties of plant flavonoids. Effects of rutin, quercetin and
hesperidin on adjuvant arthritis in rat. Farmaco. 2001 Sep;56(9):683-7.
Source
Departamento de Farmacia, Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Argentina.
Abstract
The anti-inflammatory activities of three flavonoids were investigated
in rats using the Mizushima et al. model of acute and chronic
inflammation. Intraperitoneal administration of rutin, quercetin
(flavonols) and hesperidin (flavanone), given at daily doses equivalent
to 80 mg/kg, inhibited both acute and chronic phases of this
experimental model of inflammation. Rutin was the most active in the
chronic phase.
IN THIS ANIMAL STUDY RUTIN REDUCED INFLAMMATION IN THE ACUTE STAGE, BUT WAS MOST ACTIVE AT THE CHRONIC PHASE OF INFLAMMATION.
Rotelli AE, Guardia T, Juárez AO, de la Rocha NE, Pelzer LE.
Comparative study of flavonoids in experimental models of inflammation.
Pharmacol Res. 2003 Dec;48(6):601-6.
Source
Cátedra de Farmacología, Facultad de Química, Bioquímica y Farmacia,
Universidad Nacional de San Luis, Chacabuco y Pedernera, 5700 San Luis,
Argentina. arotelli@unsl.edu.ar
Abstract
The anti-inflammatory activities of flavonols (quercetin, rutin and
morin) and flavanones (hesperetin and hesperidin) were investigated in
animal models of acute and chronic inflammation. Rutin was only
effective in the chronic process, principally in adjuvant arthritis. On
neurogenic inflammation induced by xylene, only the flavanones were
effective; besides, these compounds were the most effective on
subchronic process. The most important compound in reducing paw oedema
induced by carrageenan was quercetin.
IN THIS ANIMAL STUDY RUTIN EFFECTIVELY REDUCED INFLAMMATION AT THE CHRONIC PHASE OF INFLAMMATION.
S Sontakke, V Thawani, S Pimpalkhute, P Kabra, S Babhulkar, L
Hingorani. Open, randomized, controlled clinical trial of Boswellia
serrata extract as compared to valdecoxib in osteoarthritis of knee.
Indian Journal of Pharmacology. 2007; 39(1) 27-29
Objective: To compare the efficacy, safety and tolerability of
Boswellia serrata extract (BSE) in osteoarthritis (OA) knee with
valdecoxib, a selective COX-2 inhibitor. Materials and Methods: In a
randomized, prospective, open-label, comparative study the efficacy,
safety and tolerability of BSE was compared with valdecoxib in 66
patients of OA of knee for six months. The patients were assessed by
WOMAC scale at baseline and thereafter at monthly interval till 1 month
after drug discontinuation. Antero-posterior radiographs of affected
knee joint were taken at baseline and after 6 months. Results: In BSE
group the pain, stiffness, difficulty in performing daily activities
showed statistically significant improvement with two months of therapy
which even lasted till one month after stopping the intervention. In
valdecoxib group the statistically significant improvement in all
parameters was reported after one month of therapy but the effect
persisted only as long as drug therapy continued. Three patients from
BSE group and two from valdecoxib group complained of acidity. One
patient from BSE group complained of diarrhea and abdominal cramps.
Conclusion: BSE showed a slower onset of action but the effect persisted
even after stopping therapy while the action of valdecoxib became
evident faster but waned rapidly after stopping the treatment.
SUBJECTS WITH PAINFUL KNEES SHOWED SIGNIFICANT IMPROVEMENT WITH TWO
MONTHS OF THERAPY ON BOSWELLIA. DOSE WAS 333MG 3X DAILY. FULL STUDY
AVAILABLE HERE: http://www.bioline.org.br/pdf?ph07006
Kimmatkar N, Thawani V, Hingorani L, Khiyani R. Efficacy and
tolerability of Boswellia serrata extract in treatment of osteoarthritis
of knee--a randomized double blind placebo controlled trial.
Phytomedicine. 2003 Jan;10(1):3-7.
Source
MS Orthopedics, Indira Gandhi Medical College, Nagpur, India.
Abstract
Osteoarthritis is a common, chronic, progressive, skeletal,
degenerative disorder, which commonly affects the knee joint. Boswellia
serrata tree is commonly found in India. The therapeutic value of its
gum (guggulu) has been known. It possesses good anti-inflammatory,
anti-arthritic and analgesic activity. A randomized double blind placebo
controlled crossover study was conducted to assess the efficacy, safety
and tolerability of Boswellia serrata Extract (BSE) in 30 patients of
osteoarthritis of knee, 15 each receiving active drug or placebo for
eight weeks. After the first intervention, washout was given and then
the groups were crossed over to receive the opposite intervention for
eight weeks. All patients receiving drug treatment reported decrease in
knee pain, increased knee flexion and increased walking distance. The
frequency of swelling in the knee joint was decreased. Radiologically
there was no change. The observed differences between drug treated and
placebo being statistically significant, are clinically relevant. BSE
was well tolerated by the subjects except for minor gastrointestinal
ADRs. BSE is recommended in the patients of osteoarthritis of the knee
with possible therapeutic use in other arthritis.
PATIENTS TREATED WITH BOSWELLIA EXTRACT HAD A DECREASE IN KNEE PAIN
AND SWELLING. IT ALSO IMPROVED KNEE FLEXION AND ALLOWED THEM TO INCREASE
WALKING DISTANCE. Note: No dosage was given in the abstract however
when referenced in another study it was said to be 999 mg. daily. Other
study available here:
http://www.academicjournals.org/AJB/PDF/pdf2012/9Feb/We%20et%20al.pdf
Sengupta K, Alluri KV, Satish AR, Mishra S, Golakoti T, Sarma KV, Dey
D, Raychaudhuri SP. A double blind, randomized, placebo controlled
study of the efficacy and safety of 5-Loxin for treatment of
osteoarthritis of the knee. Arthritis Res Ther. 2008;10(4):R85
Source
Cellular and Molecular Biology Division, Laila Impex R&D Center, Jawahar Autonagar, Vijayawada, India.
Abstract
INTRODUCTION:
5-Loxin is a novel Boswellia serrata extract enriched with 30%
3-O-acetyl-11-keto-beta-boswellic acid (AKBA), which exhibits potential
anti-inflammatory properties by inhibiting the 5-lipoxygenase enzyme. A
90-day, double-blind, randomized, placebo-controlled study was conducted
to evaluate the efficacy and safety of 5-Loxin in the treatment of
osteoarthritis (OA) of the knee.
METHODS:
Seventy-five OA patients were included in the study. The patients
received either 100 mg (n = 25) or 250 mg (n = 25) of 5-Loxin daily or a
placebo (n = 25) for 90 days. Each patient was evaluated for pain and
physical functions by using the standard tools (visual analog scale,
Lequesne's Functional Index, and Western Ontario and McMaster
Universities Osteoarthritis Index) at the baseline (day 0), and at days
7, 30, 60 and 90. Additionally, the cartilage degrading enzyme matrix
metalloproteinase-3 was also evaluated in synovial fluid from OA
patients. Measurement of a battery of biochemical parameters in serum
and haematological parameters, and urine analysis were performed to
evaluate the safety of 5-Loxin in OA patients.
RESULTS:
Seventy patients completed the study. At the end of the study, both
doses of 5-Loxin conferred clinically and statistically significant
improvements in pain scores and physical function scores in OA patients.
Interestingly, significant improvements in pain score and functional
ability were recorded in the treatment group supplemented with 250 mg
5-Loxin as early as 7 days after the start of treatment. Corroborating
the improvements in pain scores in treatment groups, we also noted
significant reduction in synovial fluid matrix metalloproteinase-3. In
comparison with placebo, the safety parameters were almost unchanged in
the treatment groups.
CONCLUSION:
5-Loxin reduces pain and improves physical functioning significantly
in OA patients; and it is safe for human consumption. 5-Loxin may exert
its beneficial effects by controlling inflammatory responses through
reducing proinflammatory modulators, and it may improve joint health by
reducing the enzymatic degradation of cartilage in OA patients.
100-250 MG OF 5-LOXIN, A BOSWELLIA EXTRACT, REDUCED INFLAMMATORY
RESPONSE AND CARTILAGE DEGRADATION WHILE IMPROVING PAIN AND PHYSICAL
FUNCTION SCORES. USE OF THIS STUDY WOULD DEPEND UPON THE TYPE OF EXTRACT
YOU ARE USING, AND MAY NOT APPLY.
A. Sharma, S. Bhatia, M. D. Kharya, V. Gajbhiye, N Ganesh, A. G.
Namdeo, K. R. Mahadik. Anti-inflammatory and analgesic activity of
different fractions of Boswellia serrata. Int Jnl of Phytomedicine. 2010
V 2 No 1
Abstract
The study was designed to investigate the anti-inflammatory and
analgesic effect of different fractions of Boswellia serrata. The effect
of different fractions of Boswellia serrata were studied using
carrageenan induced paw edema, acetic acid induced writhing response,
formalin induced pain, hot plate and tail flick method for studying
anti-inflammatory and analgesic activity, respectively. The different
fractions of B. serrata, essential oil (10 ml/kg), gum (100 mg/kg, resin
(100 mg/kg) oleo-resin (100 mg/kg) and oleo-gum-resin (100 mg/kg)
significantly reduces carrageenan induced inflammation in rats and shows
analgesic activity, as determined by acetic acid induced writhing
response, formalin induced pain, hot plate and tail flick method. The
different fractions of B. serrata showed prompt anti-inflammatory and
analgesic activity due to the inhibition of 5-lipoxygenase enzyme.
IN THIS ANIMAL STUDY BOSWELLIA REDUCED INFLAMMATION IN RATS.
Kuptniratsaikul V, Thanakhumtorn S, Chinswangwatanakul P,
Wattanamongkonsil L, Thamlikitkul V. Efficacy and safety of Curcuma
domestica extracts in patients with knee osteoarthritis. J Altern
Complement Med. 2009 Aug;15(8):891-7.
Source
Department of Rehabilitation Medicine, Faculty of Medicine Siriraj
Hospital, Mahidol University, Bangkok, Thailand. sivth@mahidol.ac.th
Abstract
OBJECTIVE:
The objective of this study was to determine the efficacy and safety
of Curcuma domestica extracts in pain reduction and functional
improvement in patients with knee osteoarthritis.
STUDY DESIGN AND SETTING:
The design and setting were a randomized controlled study at a university hospital in Bangkok, Thailand.
METHODS:
One-hundred and seven (107) patients with primary knee osteoarthritis
(OA) with pain score of > or =5 were randomized to receive ibuprofen
800 mg per day or C. domestica extracts 2 g per day for 6 weeks. The
main outcomes were improvement in pain on level walking, pain on stairs,
and functions of knee assessed by time spent during 100-m walk and
going up and down a flight of stairs. The adverse events were also
recorded.
RESULTS:
Fifty-two (52) and 55 patients were randomized to C. domestica
extracts and ibuprofen groups, respectively. Baseline characteristics of
the patients in both groups were not different. The mean scores of the
aforementioned outcomes at weeks 0, 2, 4, and 6 were significantly
improved when compared with the baseline values in both groups. There
was no difference in those parameters between the patients receiving
ibuprofen and C. domestica extracts, except pain on stairs (p = 0.016).
No significant difference of adverse events between both groups was
found (33.3% versus 44.2%, p = 0.36 in C. domestica extracts and
ibuprofen groups, respectively).
CONCLUSIONS:
C. domestica extracts seem to be similarly efficacious and safe as ibuprofen for the treatment of knee OA.
CANNOT USE/DOSAGE
Olas B, Wachowicz B, Nowak P, Stochmal A, Oleszek W, Glowacki R, Bald
E. Comparative studies of the antioxidant effects of a naturally
occurring resveratrol analogue --
trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene and resveratrol --
against oxidation and nitration of biomolecules in blood platelets. Cell
Biol Toxicol. 2008 Aug;24(4):331-40. Source
Department of General Biochemistry, Institute of Biochemistry, University of Lodz, Lodz, Poland. olasb@biol.uni.lodz.pl
Abstract
The action of two phenolic compounds isolated from the bark of Yucca
schidigera: trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene and its
analogue -- resveratrol (trans-3,4',5-trihydroxystilbene, present also
in grapes and wine) on oxidative/nitrative stress induced by
peroxynitrite (ONOO(-), which is strong physiological oxidant and
inflammatory mediator) in human blood platelets was compared. The
trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene, like resveratrol,
significantly inhibited protein carbonylation and nitration (measured by
enzyme-linked immunosorbent assay method) in the blood platelets
treated with peroxynitrite (0.1 mM) and markedly reduced an oxidation of
thiol groups of proteins (estimated with
5,5'-dithio-bis(2-nitro-benzoic acid)] or glutathione (measured by high
performance liquid chromatography method) in these cells. The
trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene, like resveratrol, also
caused a distinct reduction of platelet lipid peroxidation induced by
peroxynitrite. The obtained results indicate that in vitro
trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene and resveratrol have
very similar protective effects against peroxynitrite-induced
oxidative/nitrative damage to the human platelet proteins and lipids.
Moreover, trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene proved to be
even more potent than resveratrol in antioxidative tests. We conclude
that the novel tested phenolic compound --
trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene isolated from Y.
schidigera bark possessing Generally Recognized As Safe label given by
the Food and Drug Administration and allows their human dietary use --
seems to be a promising candidate for future evaluations of its
antioxidative activity and may be a good candidate for scavenging
peroxynitrite.
YUCCA SCHIDIGERA BARK MAY REDUCE INFLAMMATORY OXIDATIVE STRESS INDUCED BY PEROXYNITRITE
Piacente S, Montoro P, Oleszek W, Pizza C. Yucca schidigera bark:
phenolic constituents and antioxidant activity. J Nat Prod. 2004
May;67(5):882-5.
Source
Dipartimento di Scienze Farmaceutiche, Università degli Studi di
Salerno, Via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy.Back to previous page
Abstract
Two new phenolic constituents with unusual spirostructures, named
yuccaols D (1) and E (2), were isolated from the MeOH extract of Yucca
schidigera bark. Their structures were established by spectroscopic
(ESIMS and NMR) analysis. The new yuccaols D and E, along with
resveratrol (3), trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene (4),
yuccaols A-C (5-7), yuccaone A (8), larixinol (9), the MeOH extract of
Yucca schidigera bark, and the phenolic portion of this extract, were
assayed for antioxidant activity by measuring the free radical
scavenging effects using two different assays, namely, the Trolox
Equivalent Antioxidant Capacity (TEAC) assay and the coupled oxidation
of beta-carotene and linoleic acid (autoxidation assay). The significant
activities exhibited by the phenolic fraction and its constituents in
both tests show the potential use of Y. schidigera as a source of
antioxidant principles.
YUCCA SCHIDIGERA BARK DEMONSTRATES ANTIOXIDANT ACTIVITY.
Chantre P, Cappelaere A, Leblan D, Guedon D, Vandermander J, Fournie
B. Efficacy and tolerance of Harpagophytum procumbens versus diacerhein
in treatment of osteoarthritis. Phytomedicine. 2000 Jun;7(3):177-83.
Source
Laboratoires Arkopharma, Carros, France.
Abstract
In a double-blind, randomized, multicentre clinical study, the
efficacy and tolerance of a herbal medicine product, Harpadol (6
capsules/day, each containing 435 mg of powdered cryoground powder
Harpagophytum procumbens), was compared with diacerhein 100 mg/day in
the treatment, for 4 months, of 122 patients suffering from
osteoarthritis of the knee and hip. Assessments of pain and functional
disability were made on a 10 cm horizontal visual analogue scale;
severity of osteoarthritis was evaluated by Lequesne's index.
Spontaneous pain showed a significant improvement during the course of
the study and there was no difference in the efficacy of the two
treatments. Similarly, there was a progressive and significant reduction
in the Lequesne functional index and no statistical difference was
found between Harpadol and diacerhein. At completion of the study,
patients taking Harpadol were using significantly less NSAIDs and
antalgic drugs. The frequency of adverse events was significantly lower
in the Harpadol group. The most frequent event reported was diarrhea,
occurring in 8.1% and 26.7% of Harpadol and diacerhein patients
respectively. The global tolerance assessment by patients at the end of
treatment favoured Harpadol. The results of this study demonstrate that
Harpadol is comparable in efficacy and superior in safety to diacerhein.
CANNOT USE/DOSAGE
Chrubasik S, Junck H, Breitschwerdt H, Conradt C, Zappe H.
Effectiveness of Harpagophytum extract WS 1531 in the treatment of
exacerbation of low back pain: a randomized, placebo-controlled,
double-blind study. Eur J Anaesthesiol. 1999 Feb;16(2):118-29.
Source
Department of Medical Biometry, University of Heidelberg, Germany.
Abstract
Two daily doses of oral Harpagophytum extract WS 1531 (600 and 1200,
respectively, containing 50 and 100 mg of the marker harpagoside) were
compared with placebo over 4 weeks in a randomized, double-blind study
in 197 patients with chronic susceptibility to back pain and current
exacerbations that were producing pain worse than 5 on a 0-10 visual
analogue scale. The principal outcome measure, based on pilot studies,
was the number of patients who were pain free without the permitted
rescue medication (tramadol) for 5 days out of the last week. The
treatment and placebo groups were well matched in physical
characteristics, in the severity of pain, duration, nature and
accompaniments of their pain, the Arhus low back pain index and in
laboratory indices of organ system function. A total of 183 patients
completed the study. The numbers of pain-free patients were three, six
and 10 in the placebo group (P), the Harpagophytum 600 group (H600) and
the Harpagophytum 1200 group (H1200) respectively (P = 0.027, one-tailed
Cochrane-Armitage test). The majority of responders' were patients who
had suffered less than 42 days of pain, and subgroup analyses suggested
that the effect was confined to patients with more severe and radiating
pain accompanied by neurological deficit. However, subsidiary analyses,
concentrating on the current pain component of the Arhus index, painted a
slightly different picture, with the benefits seeming, if anything, to
be greatest in the H600 group and in patients without more severe pain,
radiation or neurological deficit. Patients with more pain tended to use
more tramadol, but even severe and unbearable pain would not guarantee
that tramadol would be used at all, and certainly not to the maximum
permitted dose. There was no evidence for Harpagophytum-related
side-effects, except possibly for mild and infrequent gastrointestinal
symptoms.
Heal-n-Soothe® CONTAINS DEVILS CLAW, BUT IT IS
UNCLEAR WHAT THE LEVEL OF HARPAGOSIDES ARE. 50-100 MG HARAGOSIDES WERE
USED IN THIS STUDY AND WORKED BETTER THAN PLACEBO.
Gagnier JJ, van Tulder M, Berman B, Bombardier C. Herbal medicine for
low back pain. Cochrane Database Syst Rev. 2006 Apr 19;(2):CD004504.
Source
Provincal Medical Centre, 5955 Ontario St., Unit 307, Windsor, Ontario, Canada, N8S1W6. j.gagnier@utoronto.ca
Abstract
BACKGROUND:
Low-back pain is a common condition and a substantial economic burden
in industrialized societies. A large proportion of patients with chronic
low-back pain use complementary and alternative medicine (CAM), visit
CAM practitioners, or both. Several herbal medicines have been purported
for use in low-back pain.
OBJECTIVES:
To determine the effectiveness of herbal medicine for non-specific low-back pain.
SEARCH STRATEGY:
We searched the following electronic databases: Cochrane Complementary
Medicine Field Trials Register (Issue 3, 2005), MEDLINE (1966 to July
2005), EMBASE (1980 to July 2005); checked reference lists in review
articles, guidelines and retrieved trials; and personally contacted
individuals with expertise in this very specialized area.
SELECTION CRITERIA:
We included randomized controlled trials, examining adults (over 18
years of age) suffering from acute, sub-acute or chronic non-specific
low-back pain. The interventions were herbal medicines, defined as
plants that are used for medicinal purposes in any form. Primary outcome
measures were pain and function.
DATA COLLECTION AND ANALYSIS:
Two authors (JJG & MVT) conducted the database searches. One
author contacted content experts and acquired relevant citations. Full
references and abstracts of the identified studies were downloaded. A
hard copy was retrieved for final inclusion decisions. Methodological
quality and clinical relevance were assessed separately by two
individuals. Disagreements were resolved by consensus.
MAIN RESULTS:
Ten trials were included in this review. Two high quality trials
examining the effects of Harpagophytum Procumbens (Devil's Claw) found
strong evidence that daily doses standardized to 50 mg or 100 mg
harpagoside were better than placebo for short-term improvements in pain
and rescue medication. Another high quality trial demonstrated relative
equivalence to 12.5 mg per day of rofecoxib (Vioxx). Two trials
examining the effects of Salix Alba (White Willow Bark) found moderate
evidence that daily doses standardized to 120 mg or 240 mg salicin were
better than placebo for short-term improvements in pain and rescue
medication. An additional trial demonstrated relative equivalence to
12.5 mg per day of rofecoxib. Three low quality trials on Capsicum
Frutescens (Cayenne), examining various topical preparations, found
moderate evidence that Capsicum Frutescens produced more favourable
results than placebo and one trial found equivalence to a homeopathic
ointment.
AUTHORS' CONCLUSIONS:
Harpagophytum Procumbens, Salix Alba and Capsicum Frutescens seem to
reduce pain more than placebo. Additional trials testing these herbal
medicines against standard treatments are needed. The quality of
reporting in these trials was generally poor. Trialists should refer to
the CONSORT statement extension for reporting trials of herbal medicine
interventions.
Heal-n-Soothe® CONTAINS DEVILS CLAW, BUT IT
IS UNCLEAR WHAT THE LEVEL OF HARPAGOSIDES ARE. 50-100 MG HARAGOSIDES
WERE USED IN THESE STUDIES AND WORKED BETTER THAN PLACEBO.
REFERENCE NOTE ABOUT DEVIL'S CLAW: Devil's claw has been studied for
low back pain, muscle pain, and osteoarthritis using daily doses of
crude tuber up to 9 g daily, 1 to 3 g of extract, and 50 to 100 mg of
harpagoside. Standardized preparations include LI 174 ( Rivoltan ),
Doloteffin (more than 50 mg harpagoside), and WS 1531. A level of more
than 1% harpagoside in root is considered acceptable. Commercial sources
of devil's claw extract contain 1.4% to 2% harpagoside.
Göbel H, Heinze A, Ingwersen M, Niederberger U, Gerber D. [Effects of
Harpagophytum procumbens LI 174 (devil's claw) on sensory, motor und
vascular muscle reagibility in the treatment of unspecific back pain].
Schmerz. 2001 Feb;15(1):10-8.
[Article in German]
Source
Neurologisch-verhaltensmedizinische, Schmerzklinik Kiel in Kooperation
mit der Universität Kiel. h.gobel@neurologie.uni-kiel.de
Abstract
PROBLEM:
This randomised, double-blind, placebo controlled study was intended
to investigate the effects of Harpagophytum procumbens (Devil's Claw) on
sensory, motor and vascular mechanisms of muscle pain. In addition to
clinical efficacy and tolerability, possible action mechanisms were
analysed by means of experimental algesimetric methods.
METHODOLOGY:
The study was performed on patients with slight to moderate muscular
tension or slight muscular pain of the back, shoulder and neck. On a
double-blind randomised basis the verum group received 2x1 film tablets
per day, i. e. 2x480 mg/day, of Harpagophytum extract LI 174
(Rivoltan(R)) at 8.00 a.m. and 8.00 p.m. over a certain period. The
duration of the therapy was 4 weeks. Data recording at 14-day intervals
was made using a visual analogue scale, pressure algometer test,
recording of antinociceptive muscular reflexes, muscle stiffness test,
EMG surface activity, muscular ischaemia test, clinical global score and
subjective patient and physician ratings.
RESULTS:
A total of 31 patients in the verum group and 32 in the placebo group
were treated. After four weeks of treatment there was found to be a
clear clinical efficacy of the verum on the clinical global score and in
the patient and physician ratings. Highly significant effects were
found in the visual analogue scale, the pressure algometer test, the
muscle stiffness test and the muscular ischaemia test. No difference
from placebo was found in the recording of antinociceptive muscular
reflexes or in the EMG surface activity. Tolerability was good; no
serious adverse effects occurred.
CONCLUSIONS:
A highly significant clinical efficacy was achieved with a monotherapy
of Harpagophytum dry extract LI 174 after four weeks' treatment at a
dosage of 2x480 mg/day in cases of slight to moderate muscular pain.
With regard to the action mechanisms investigated, it may be concluded
that treatment with Harpagophytum extract LI 174 may be expected to have
a significant influence on sensory and vascular muscular response and
bring about a reduction in muscle stiffness. No central nervous effects
were discovered.
CANNOT USE/DOSAGE
Leblan D, Chantre P, Fournié B. Harpagophytum procumbens in the
treatment of knee and hip osteoarthritis. Four-month results of a
prospective, multicenter, double-blind trial versus diacerhein. Joint
Bone Spine. 2000;67(5):462-7.
Source
Laboratoires Arkopharma, Carros, France.
Abstract
OBJECTIVE:
To evaluate the efficacy and safety of Harpagophytum in the treatment
of hip and knee osteoarthritis comparatively with the slow-acting drug
for osteoarthritis, diacerhein.
PATIENTS AND METHODS:
A multicenter, randomized, double-blind, parallel-group study was
conducted in 122 patients with hip and/or knee osteoarthritis. Treatment
duration was four months and the primary evaluation criterion was the
pain score on a visual analog scale. Harpagophytum 2,610 mg per day was
compared with diacerhein 100 mg per day.
RESULTS:
After four months, considerable improvements in osteoarthritis
symptoms were seen in both groups, with no significant differences for
pain, functional disability, or the Lequesne score. However, use of
analgesic (acetaminophen-caffeine) and nonsteroidal anti-inflammatory
(diclofenac) medications was significantly reduced in the Harpagophytum
group, which also had a significantly lower rate of adverse events.
CONCLUSION:
In this study, Harpagophytum was at least as effective as a reference
drug (diacerhein) in the treatment of knee or hip osteoarthritis and
reduced the need for analgesic and nonsteroidal anti-inflammatory
therapy.
CANNOT USE/DOSAGE
Sasaki T, Kojima S. Ga uptake and heparan sulfate content of Ehrlich solid tumor in mice. Eur J Nucl Med. 1986;12(4):182-6.
Abstract
The relationship between 67Ga uptake and heparan sulfate (HS) content
in Ehrlich solid tumor (EST) of mice was investigated, and the effect of
cyanomethylamine, papain, streptozotocin, or bleomycin pretreatment on
67Ga uptake in EST was studied. 67Ga uptakes in EST and kidney were much
higher than other tissues, and these tissues also contained large
amounts of HS. 67Ga uptakes and HS synthesis in the EST were inhibited
by pretreatment with cyanomethylamine or papain (inhibitors of
fibrosis). Parallel reductions of 67Ga uptake and HS synthesis in EST
were observed in EST transplanted into streptozotocin-induced diabetic
mice. The weight of EST in the bleomycin-injected group was decreased to
less than half of the control, but no effect was observed on 67Ga
uptake per gram of EST. These results suggest that 67Ga uptake in the
tumor and inflammatory lesions are related to the quantity of HS in
these tissues, and the correlation between the uptake of 67Ga and the
rate of cellular proliferation is secondary.
PAPAIN IS AN INHIBITOR OF FIBROSIS BUT COULD NOT FIND HUMAN STUDIES TO SUPPORT SAME.
Skyrme-Jones RA, O'Brien RC, Berry KL, Meredith IT. Vitamin E
supplementation improves endothelial function in type I diabetes
mellitus: a randomized, placebo-controlled study. J Am Coll Cardiol.
2000 Jul;36(1):94-102.
Source
Centre for Heart and Chest Research, Monash Medical Centre and Monash University, Melbourne, Australia.
Abstract
OBJECTIVES:
We sought to determine, in a double-blind, placebo-controlled,
randomized study, whether vitamin E supplementation (1,000 IU for three
months) would improve impaired conduit and resistance vessel endothelial
vasodilator function (EVF) and systemic arterial compliance (SAC) in
type I diabetes mellitus (DM).
BACKGROUND:
Oxidative stress is thought to be important in the pathogenesis of
impaired EVF. Consistent with this hypothesis, we have recently shown
that impaired EVF is related to low density lipoprotein (LDL) vitamin E
content (VEC) in young subjects with type 1 DM.
METHODS:
We assessed EVF in the brachial artery (using noninvasive ultrasound,
flow-mediated vasodilation [FMD]; n = 41) and in the forearm resistance
vessels (by flow responses to intrabrachial acetylcholine [ACh]; n = 21)
and measured SAC (simultaneous aortic blood flow and carotid pressure
measurements; n = 41) before and after active or placebo therapy.
RESULTS:
The LDL VEC was increased by 127% after supplementation, resulting in a
significant reduction in the oxidative susceptibility of LDL. There was
no time-dependent change in FMD or in the response to ACh or SAC in the
placebo group. A significant improvement in FMD (2.6 +/- 0.6% to 7.0
+/- 0.7%, p < 0.005) and the dose response to ACh (p < 0.05) were
observed in those randomized to vitamin E therapy. Systemic arterial
compliance was not affected by vitamin E (0.41 +/- 0.03 vs. 0.49 +/-
0.06 arbitrary compliance units, p = NS). The change in FMD was related
to the change in LDL VEC (r = 0.42, p < 0.05) and the change in the
oxidative susceptibility of LDL (r = 0.64, p < 0.0001).
CONCLUSIONS:
Short-term daily oral supplementation with vitamin E improves EVF in
both the conduit and resistance vessels of young subjects with type I
DM.
CANNOT USE/DOSAGE
Li Y, Schellhorn HE. New developments and novel therapeutic perspectives for vitamin C. J Nutr. 2007 Oct;137(10):2171-84.
Source
Department of Biology, McMaster University, Hamilton, Ontario, Canada L8S 4K1.
Abstract
Vitamin C is required for collagen synthesis and biosynthesis of
certain hormones and recommended dietary intake levels are largely based
these requirements. However, to function effectively as an antioxidant
(or a pro-oxidant), relatively high levels of this vitamin must be
maintained in the body. The instability of vitamin C combined with its
relatively poor intestinal absorption and ready excretion from the body
reduce physiological availability of this vitamin. This inability to
maintain high serum levels of vitamin C may have serious health
implications and is particularly relevant in the onset and progression
of degenerative disease, such as cancer and cardiovascular disease
(CVD), which have a strong contributing oxidative damage factor. In this
review, we examine recent studies on the regulation of transport
mechanisms for vitamin C, related clinical ramifications, and potential
implications in high-dose vitamin C therapy. We also evaluate recent
clinical and scientific evidence on the effects of this vitamin on
cancer and CVD, with focus on the key mechanisms of action that may
contribute to the therapeutic potential of this vitamin in these
diseases. Several animal models that could be utilized to address
unresolved questions regarding the feasibility of vitamin C therapy are
also discussed.
Singh RK, Rai D, Yadav D, Bhargava A, Balzarini J, De Clercq E.
Synthesis, antibacterial and antiviral properties of curcumin
bioconjugates bearing dipeptide, fatty acids and folic acid. Eur J Med
Chem. 2010 Mar;45(3):1078-86. Epub 2010 Jan 19.
Source
Nucleic Acids Research Laboratory, Department of Chemistry, University of Allahabad, Allahabad 211002, India.
Abstract
Curcumin bioconjugates, viz. di-O-tryptophanylphenylalanine curcumin
(2), di-O-decanoyl curcumin (3), di-O-pamitoyl curcumin (4),
di-O-bis-(gamma,gamma)folyl curcumin (6), C(4)-ethyl-O-gamma-folyl
curcumin (8) and 4-O-ethyl-O-gamma-folyl curcumin (10) have been
synthesized and tested for their antibacterial and antiviral activities.
The conjugates 2, 3, 4, 6 and 8 have shown very promising antibacterial
activity with MIC ranging between 0.09 and 0.67 microM against
Gram-positive cocci and Gram-negative bacilli. Further, the conjugates
2, 3, 6, 8 and 10 have been screened for their antiviral activities
against HSV, VSV, FIPV, PIV-3, RSV and FHV and the molecules 2 and 3
have shown good results with EC(50) 0.011 microM and 0.029 microM
against VSV and FIPV/FHV, respectively. However, the molecules did not
show expected results against HIV-1 III(B) and ROD strains in MTT assay.
Maheshwari RK, Singh AK, Gaddipati J, Srimal RC. Multiple biological
activities of curcumin: a short review. Life Sci. 2006 Mar
27;78(18):2081-7. Epub 2006 Jan 18.
Source
Department of Pathology, Uniformed Services University of the Life
Sciences, Center for Combat Casualty and Life Sustainment Research,
Bethesda, Maryland 20814, USA. maheshwari@usuhs.mil
Abstract
Turmeric (Curcuma longa rhizomes), commonly used as a spice is well
documented for its medicinal properties in Indian and Chinese systems of
medicine. It has been widely used for the treatment of several
diseases. Epidemiological observations, though inconclusive, are
suggestive that turmeric consumption may reduce the risk of some form of
cancers and render other protective biological effects in humans. These
biological effects of turmeric have been attributed to its constituent
curcumin that has been widely studied for its anti-inflammatory,
anti-angiogenic, anti-oxidant, wound healing and anti-cancer effects. As
a result of extensive epidemiological, clinical, and animal studies
several molecular mechanisms are emerging that elucidate multiple
biological effects of curcumin. This review summarizes the most
interesting in vitro and in vivo studies on the biological effects of
curcumin.Back to previous page
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