On the pharmacology of bromelain: an update with special regard to animal studies on dose-dependent effects.

Planta Med (GERMANY, WEST) Jun 1990, 56 (3) p249-53

Bromelain, a standardized complex of proteases from the pineapple plant, is absorbed unchanged from the intestine of animals at a rate of 40%; in animal experiments it was found to have primarily anti-edema, antiinflammatory, and coagulation-inhibiting effects. These effects are due to an enhancement of the serum fibrinolytic activity and inhibition of the fibrinogen synthesis, as well as a direct degradation of fibrin and fibrinogen. Bromelain lowers kininogen and bradykinin serum and tissue levels and has an influence on prostaglandin synthesis, thus acting antiinflammatory. In in vitro and in animal studies, experimentally induced tumours could be inhibited by . Although many studies do not give extensive statistical data, the effects of bromelain in animal studies seem to be dose-dependent. Further investigations have to be carried out.


Phospholipid epitopes for mouse antibodies against bromelain-treated mouse erythrocytes.

Immunology (ENGLAND) Sep 1987, 62 (1) p11-6

The reactivity of mouse antibodies against bromelain- treated mouse erythrocytes (BrMRBC) with phospholipid epitopes was assessed by ELISA, using four clones of monoclonal anti-BrMRBC antibodies that had idiotypes distinct from one another. The four antibodies could bind to low-density lipoproteins (LDL) from human and chicken, but not to LDL from mouse and rat. As to liposomes of natural phospholipids, all the clones reacted with liposomes of phosphatidylcholine, and some of them could react with liposomes of sphingomyelin, phosphatidylglycerol, phosphatidylic acid or cardiolipin. For liposomes of synthetic phosphatidylcholine with different fatty acids, the length of carbon chains and the number of unsaturated carbon chains of the fatty acids markedly affected the binding of each monoclonal antibody to the liposomes. The addition of dicetyl phosphate or stearylamine to phosphatidylcholine liposomes changed the reactivity of the liposomes. These results support the view that mouse anti-BrMRBC antibodies can recognize appropriately spaced phosphorylcholine residues on the surface of phospholipid liposomes, LDL and cells. The four clones had similar capacities for binding to LDL as well as to BrMRBC, but they had obviously different capacities for binding to phospholipid liposomes; the epitopes on phospholipid liposomes used in the present study were not so perfect as to react well with every anti-BrMRBC antibody.


Gaining Intestinal Control Over Allergens

The importance of an optimal functioning gastrointestinal tract in maintaining healthy immune function cannot be overemphasized.

By reducing the absorption of pathogenic and potentially allergenic substances, a healthy intestinal immune system helps prevent undesirable immune reactions. When the normal, healthy condition of the intestinal tract changes and the sensitive mucous lining is broken down, toxic or allergy-provoking substances are allowed to leak into the blood, which can then cause illness.

The intestinal tract helps us control allergy-causing substances in several ways. Certain nutrients assist in healing and restoring integrity of the intestinal lining so that it provides an effective physical barrier against undesirable substances. The GI tract also provides an environment whereby inactivation of allergens is possible. Glutamine, glucosamine, and other nutrients, as provided by Intestamine powder, play an important role in intestinal health. Quercetin and Bromelain are two additional nutrients that are involved in this process.

Protective Effect of Quercetin. Quercetin is a flavonoid found widely in plants that has been studied for a variety of potential health effects. The potent antioxidant activity of quercetin serves an important function within the intestinal lumen by helping protect intestinal cells from free radical damage. By deactivating potential intestinal irritants and encouraging the production of protective gastric mucus, quercetin helps prevent allergens from leaking across into the bloodstream.

Quercetin is active against a variety of oxygen-free radicals and protects against the harmful effects of oxidized LDL cholesterol. Uncontrolled free radical reactions can contribute to tissue inflammation, metabolic disorders, and cell damage.

Specific effects of quercetin on metabolic pathways responsible for controlling inflammation have been investigated. It has been shown to inhibit IgE-medicated mast cell activation and inhibit IgG histamine release, which are involved in the body's allergic response mechanisms. Quercetin also inhibits the lipoxygenase enzyme which is required for the synthesis of proinflammatory arachidonic acid metabolites.

The beneficial effects of quercetin also extends to protecting cells from the deleterious consequences of glutathione depletion. Glutathione is a major defense mechanism against free radicals and subsequent mitochondrial damage. Even moderate reductions in glutathione content of intestinal cells can result in increased lipid peroxides. By inhibiting oxidative damage to glutathione-depleted cells, quercetin is an important contributor to maintaining cellular health and detoxification pathways.

Thus, quercetin has several valuable ways of assisting the gastrointestinal tract to interrupt the effects of ingested allergens.

Helpful Enzyme Action from Bromelain. Incompletely digested protein molecules can be absorbed by a damaged gut and initiate an allergic response, including inflammation. Maintaining healthy output of digestive enzymes and fluids is an important part of a healthy, responsive gastrointestinal immune system.

Protein digestion takes place both in the stomach and the small intestine. Pepsin and hydrochloric acid first denature large proteins in the stomach. These smaller polypeptides are then further broken down by intestinal proteases to amino acids and small peptides which are then readily absorbed.

Bromelain is a protein-specific enzyme obtained from pineapple which has a wide range of activity in varying pH ranges. It stays active in the stomach as well as the small intestine. Ingested bromelain enzyme complements the body's digestive system throughout the GI tract by its actions on protein breakdown.

Using bromelain together with quercetin offers a unique way to protect and support the intestinal tract in reducing the allergen load.


References

Alarcon de la Lastra C, Martin MJ, Motilv. Antiulcer and gastroprotective effects of quercetin: a gross and histologic study. Pharmacology 1994;48:56-62.

Hertog MGL, Holman PCH. Potential health effects of the dietary flavonol quercetin. Eur J Clin Nutr 1996;50:63-71.

Hollman P, et al. Absorption of dietary quercetin glycosides and quercetin in healthy ileostomy volunteers. Am J Clin Nutr 1995;62:1276-82.

Masson M. Bromelain in blunt injuries of the locomotor system. A study observed in general practice.

Skaper SD, et al. Quercetin protects cutaneous tissue- associated cell types including sensory neurons from oxidative stress induced by glutathione depletion: cooperative effects of ascorbic acid. Free Rad Biol Med 1997;22(4):669-78.


Bromelain

by George E. Meinig, DDS, FACD

Bromelain was first introduced in 1957. Since then it has proved an important aid to so many diseases that more than 600 research articles are now found in the scientific literature about this product. It is a proteolytic enzyme, one that decomposes protein in the body. One of its first noted benefits was as a digestant. Bromelain is derived from the stem of the pineapple plant. This enzyme is effective not only in the acid present in the stomach, but also in the alkaline environment of the intestine. It is considered a substitute for the digestants pepsin and tryptin. When I first became acquainted with it as a digestant, it didn't appear to be too effective. Since then, I have learned that patients were using too low a dosage. What will surprise you is the long list of diseases for which bromelain has proved helpful besides MSAL-digestion. Some of these are: angina, heart disease, rheumatoid arthritis, cellulitis, thrombophlebitis, surgical trauma, sports injuries, ecchymosis (black and blue areas), edema, pneumonia, scleroderma, sinusitis, shortens labor, and reduces appetite. Dr. Hans Nieper, world renowned physician, has had fabulous success in treating heart cases with bromelain, magnesium oratate, and potassium oratate. He reported this therapy was 95 percent successful in preventing heart attacks. Dr. Gary Gordon in Sacramento, California, using the same regime, had 85 percent success. Nieper's mortality rate in the treatment of strokes and heart attacks is only 2 percent, while that of the Cleveland clinic in Ohio, using conventional therapies, was 21 percent, and that of a Rotterdam Holland clinic, 19 percent. Dr. Nieper also reported bromelain was slowly and steadily effective in lowering blood pressure and was one of the most effective anti-arthritics (ANAVIT-F3). It stops platelet aggregation --the stickiness of blood cells. His clinic since 1975 has found its ability to break up fibrin has reduced leg amputation cases of diabetics and cardiovascular disease patients to zero.

Bromelain: A Literature Review and Discussion of its Therapeutic Applications Gregory S. Kelly, N.D. Abstract: First introduced as a therapeutic compound in 1957, bromelain's actions include: (1) inhibition of platelet aggregation; (2) fibrinolytic activity; (3) anti- inflammatory action; (4) anti-tumor action; (5) modulation of cytokines and immunity; (6) skin debridement properties; (7) enhanced absorption of other drugs; (8) mucolytic properties; (9) digestive assistance; (10) enhanced wound healing; and (11) cardiovascular and circulatory improvement. Bromelain is well absorbed orally and available evidence indicates that it's therapeutic effects are enhanced with higher doses. Although all of its mechanisms of action are still not completely resolved, it has been demonstrated to be a safe and effective supplement. (Alt Med Rev 1996; 1(4): 243-257)