Quercetin Bromelain
180 Capsules
Ingredients per
capsule:
Quercetin ...........250 mg
Bromelain (1500 G.D.U.
per gram)...125 mg
[Gelatin Digesting Units]
Excipients:
rice powder, magnesium stearate, silicon dioxide.
Suggested
Use: 1 or 2 capsules three times daily, preferably 30 to 60
minutes before meals.
Ingredients
Quercetin is a
potent and versatile flavonoid and phytonutrient. Bromelain is
an enzyme complex derived from the pineapple stem. (Note: G.D.U.
stands for “Gelatin-Digesting Units,” a commonly accepted
measure of enzyme activity.)
Benefits
Down-regulates the
Body’s Response to Environmental Challenges
Quercetin is a
member of the flavonoid family, a diverse group of low
molecular-weight compounds found throughout the plant kingdom.
Flavonoids exhibit numerous biological activities, many of which
are directly beneficial to human health. Quercetin, which
belongs to the “flavonol” subgroup, is one of the most versatile
and important flavonoids.
Quercetin has a broad range of
activity, much of which stems from its interaction with
calmodulin, a calcium-regulatory protein.1 Calmodulin transports
calcium ions across cellular membranes, initiating numerous
cellular processes. Quercetin appears to act as a calmodulin
antagonist.1 Through this mechanism, quercetin functions at the
cell-membrane level with a membrane-stabilizing action.2
Quercetin inhibits calmodulin-dependent enzymes present at cell
membranes such as ATPases and phospholipase, thereby influencing
membrane permeability.3 Quercetin affects other
calmodulin-dependent enzymes that control various cellular
functions, including the secretion of histamine from mast
cells.4 A number of investigations have corroborated quercetin’s
ability to reduce histamine secretion from mast cells in various
tissues, and also from basophils.5,6,7,8,9,10
Quercetin
modifies the body’s response to antigenic substances.*
Suppression of histamine secretion from mast cells is one of
quercetin’s most clinically important effects. Quercetin acts on
ATPase at the membranes of histamine-containing granules in mast
cells.3 Mast-cell degranulation and subsequent release of
histamine into the bloodstream is an integral part of the body’s
response to environmental challenges.
Maintains Tissue
Comfort by Regulating Enzymes*
Quercetin’s enzyme-inhibiting
action extends to enzymes such as phospholipase, which catalyzes
the release of arachidonic acid from phospholipids stored in
cell membranes.4,10 Arachidonic acid serves as the key substrate
for substances such as thromboxanes, inflammatory prostaglandins
and leukotrienes. In addition, quercetin inhibits the enzymes
cyclooxygenase and lipoxygenase, which catalyze the conversion
of arachidonic acid into its metabolites.4,10,11,12 Reducing
levels of these metabolites, as well as histamine levels, is
beneficial in maintaining the normal comfort level of body
tissues and structures.
Quercetin has also been shown to
limit the function of adhesion molecules on endothelial cells.13
Adhesion molecules are involved in physiologic processes that
influence tissue comfort.13
Bromelain is a complex substance
derived from the pineapple stem largely composed of proteolytic
(protein-digesting) enzymes. Bromelain acts by a variety of
mechanisms to help maintain tissues in a normal state of
comfort.14,15 Several investigators, including Taussig16 and
Ako, et. al.,17 have presented evidence that bromelain is a
fibrinolytic agent, i.e., it induces the breakdown of fibrin, a
plasma protein that blocks tissue drainage. The generally
accepted mechanisms involve direct proteolysis of fibrin by
bromelain and activation of plasmin, a serum protease.16 Plasmin
acts on fibrinogen (the precursor to fibrin), forming peptides
which stimulate PGE1, a prostaglandin that helps maintain tissue
comfort.16
Helps Maintain Health of Blood Vessels by
Modifying Oxidation of LDL Cholesterol* — Quercetin’s
Antioxidant Action
Quercetin is a versatile and effective
antioxidant that scavenges a variety of free-radicals such as
hydroxyl and lipid peroxy radicals.18 Quercetin also chelates
ions of transition metals such as iron, which can initiate
formation of oxygen free radicals.18 LDL cholesterol is
vulnerable to oxidation by lipid peroxides. Oxidized LDL is
absorbed by macrophages and arterial endothelial cells, leading
to the formation of “foam cells,” and eventually plaque
deposits, in arterial walls. Quercetin has been shown to protect
LDL from oxidation, both by lipid peroxides and transition metal
ions.19
Helps Maintain Normal Blood Viscosity*
Quercetin
inhibits blood platelet aggregation (clumping), by potentiating
PGI2, an anti-aggregatory prostaglandin, and by raising platelet
cyclic AMP levels.20 Human studies have revealed that bromelain
also reduces platelet aggregation.21
These properties qualify
both quercetin and bromelain as valuable dietary ingredients for
maintaining cardiovascular health.*
Bromelain May Enhance
Quercetin Absorption
In addition to the actions described above
that support the effects of quercetin, bromelain may also assist
the absorption of quercetin in the G.I. tract. (Quercetin is
generally believed to be poorly absorbed, although a recent
study by Hollman et. al.,22 which concluded that humans do in
fact absorb appreciable amounts of quercetin, contradicts this
assumption.) Studies have shown that bromelain enhances
absorption of antibiotics, presumably by increasing permeability
of the gut wall.23, 24 Given that quercetin is a low
molecular-weight compound, it is plausible that simultaneously
ingested bromelain likewise enhances quercetin
absorption.
*This statement has not been evaluated by the
Food and Drug Administration. This product is not intended to
diagnose, treat, cure or prevent any disease.
Scientific
References
1. Nishino, H., et. al., “Quercetin interacts with
calmodulin, a calcium regulatory protein.” Experientia
1984;40:184-5.
2. Busse, W.W., Kopp, D.E., Middleton, E.,
“Flavonoid modulation of human neutrophil function.” J. Allergy
Clin. Immunol. 1984;73:801-9.
3. Havsteen, B,. “Flavonoids, a
class of natural products of high pharmacological potency.”
Biochemical Pharmacology 1983;32(7):1141-48.
4. Middleton, E.,
“The Flavonoids.” Trends in Pharmaceutical Sciences
1984;5:335-8.
5. Otsuka, H. et. al., “Histochemical and
functional characteristics of metachromatic cells in the nasal
epithelium in allergic rhinitis: Studies of nasal scrapings and
their dispersed cells.” J. Allergy Clin.
Immunol.1995;96:528-36.
6. Fox, C.C., et. al., “Comparison of
human lung and intestinal mast cells.” J. Allergy and Clin.
Immunol. 1988;81:89-94.
7. Pearce, F.L., Befus, A.D.,
Bienenstock, J., “Mucosal mast cells III. Effect of quercetin
and other flavonoids on antigen-induced histamine secretion from
rat intestinal mast cells.” J. Allergy and Clin. Immunol.
1984;73:819-23.
8. Middleton, E. Drzewiecki, G., Krishnarao,
D., “Quercetin: an inhibitor of antigen-induced human basophil
histamine release.” J. of Immunology 1981;127(2):546-50.
9.
Bennett, J.P., Gomperts, B.D., Wollenweber, E.,“ Inhibitory
effects of natural flavonoids on secretion from mast cell and
neutrophils.” Arzneim. Forsch/Drug Res. 1981;31(3):433-7.
10.
Middleton, E. Drzewiecki G., “Naturally occurring flavonoids and
human basophil histamine release.” Int. Archs Allergy appl.
Immun. 1985;77:155-7.
11. Yoshimoto, T. et. al., “Flavonoids:
potent inhibitors of arachidonate 5-lipoxygenase.” Biochemical
and Biophysical Research Communications 1983;116(2):612-18.
12.
Della Loggia, R., et. al., “Anti-inflammatory activity of
benzopyrones that are inhibitors of cyclo- and lipo-oxygenase.”
Pharmacological Research Communications 1988; 20(Supp.
V):91-94.
13. Middleton, E., Suresh, A., “Quercetin inhibits
lipopolysaccharide-induced expression of endothelial cell
intracellular adhesion molecule-1.” Int. Arch. Allergy Immunol.
1995;107:435-6.
14. Taussig, S.J., Batkin, S., “Bromelain, the
enzyme complex of pineapple (Ananas comosus) and its clinical
application.” An Update Journal of Ethnopharmacology
1988;22:191-203.
15. Lotz-Winter, H., “On the pharmacology of
bromelain: An update with special regard to animal studies on
dose-dependent effects.” Planta Medica 1990;56:249-53.
16.
Taussig, S.J., “The mechanism of the physiological action of
bromelain” Medical Hypothesis 1980;6:99-104.
17. Ako, H.
Cheung, A.H.S., Matsuura, P.K., “Isolation of a fibrinolysis
activator from commercial bromelain.” Arch. Int. Pharmacodyn.
1981;284:157-67.
18. Afanas’ev, I.B. et. al., “Chelating and
free radical scavenging mechanisms of inhibitory action of rutin
and quercetin in lipid peroxidation.” Biochemical Pharmacology
1989;38(11):1763-69.
19. De Whalley, C.V., “Flavonoids inhibit
the oxidative modification of low density lipoproteins by
macrophages.” Biochemical Pharmacology 39(11):1743-50.
20.
Beretz, A. Stierle, A., Anton, R. Cazenave, J., “Role of cyclic
AMP in the inhibition of human platelet aggregation by
quercetin, a flavonoid that potentiates the effect of
prostacyclin.” Biochemical Pharmacology
1981;31(22):3597-600.
21. Heinicke, R. van der Wal, L.
Yokoyama, M., “Effect of bromelain (Ananase®) on human platelet
aggregation. ”Experientia 1972;28(7):844.
22. Hollma, P. et.
al., “Absorption of dietary quercetin glycosides and quercetin
in healthy ileostomy volunteers.” Am. J. Clin. Nutr.
1995;62:1276-82.
23. Giller, F.B., “The effects of bromelain on
levels of penicillin in the cerebrospinal fluid of rabbits.” A.,
J. Pharm. 1962;134:238-244.
24. Bodi, T., “The effect of oral
bromelain on tissue permeability to antibiotics and pain
response to bradykinin; double-blind studies on human subjects.”
Clin. Med. 1965;72:61-65.
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