Bromelain is the proteolytic enzyme from juice wastes of pineapple stem and ripe or unripe fruits combined with solvents, such as acetone or methanol, or following filtration (Leung and Foster, 1996; Samuelsson, 1992; Schulz et al., 1998). For the past 25 years, proteolytic enzymes that contain chemically active thiol groups that can tenderize meat have been used by the food industry (Samuelsson, 1992). Other enzymes such as papain, derived from papaya latex (Carica papaya), and ficin, from fig latex (Ficus species), also contain thiol groups. Other uses of proteolytic enzymes include animal skin preparation, fish oil production, soap manufacture, and cloth shrinkage (Leung and Foster, 1996).
In Europe, a patented tape that contains bromelain is used for debriding escharotic skin (Leung and Foster, 1996). Bromelain is also used to treat traumatic or post-surgical swelling; Commission E approves the use of bromelain to quell surgical swelling, particularly nasal sinus swelling. This approval, however, has been questioned by some scientists, who note that the Commission E's assessment involved five studies, three positive and two negative, leading to an equivocal proof of efficacy (Schulz et al., 1998).
In pharmacological tests, bromelain inhibits platelet aggregation, which explains, at least partially, its anti-inflammatory activity (Taussig and Batkin, 1988). Bromelain may also therapeutically influence fibrinolysis, tumor growth, drug absorption, blood coagulation and the debridement of third-degree burns (Taussig and Batkin, 1988). Another study demonstrated intestinal and antibacterial effects beneficial in the treatment of diarrhea (Mynott et al., 1997).
One obstacle to determining bromelain's therapeutic effects in humans is its bioavailability. Because the proteins contained in bromelain are usually broken down prior to absorption in the gastrointestinal tract, bromelain's active enzymes may not survive digestion. In rats, bromelain absorption rate is about 50%; other animal tests show that some undegraded protein winds up in lymph and the bloodstream (Schulz et al., 1998). Human rates are unknown, but one study using 19 healthy human males suggests that small amounts of undegraded bromelain may pass through the gastrointestinal tract intact (Castell et al., 1997).
The source of commercial bromelain tends to be the pineapple stem (Leung and Foster, 1996; Schulz et al., 1998); ripe fruits are sold as food products. Historically, the juice, fruit, and stem latex were used. In Hawaii, Japan, and Taiwan, folk medicine and contemporary descriptions of fruit latex report its use to cleanse and heal wounds and burns, to relieve digestive disturbances, and to treat some cancers (Taussig and Batkin, 1988).
Description
Bromelain (EC 3.4.22.4) is the genuine mixture of bromelin A and B, the proteolytic enzymes of pineapple fruit, Ananas comosus (L.) Merrill [Fam. Bromeliaceae], in effective dosage.
Chemistry and Pharmacology
Bromelain constituents are a mixture of basic glycoproteins similar to papain (Bruneton, 1995). The fruit consists of soluble monosaccharides and disaccharides, organic acids, and vitamins (Bruneton, 1995).
In various animal experiments (egg white-, carrageen-, dextran-, and yeast-induced edemas, traumatic edema, adrenalin-caused edema of the lungs), an edema-inhibiting effect was demonstrated with high dosages of bromelain upon oral and intraperitoneal administration. Upon oral intake, bromelain can prolong prothrombin and bleeding time, as well as inhibit the aggregation of thrombocytes. There is no information available on the absorption of the compound in humans after oral ingestion. Only older data are known regarding acute and chronic toxicity of the compound. The LD50 after parenteral application is 85.2 mg/kg for rats, 30-35 mg/kg for mice, and for rabbits greater than 20 mg/kg of body weight. There are no data for mutagenicity and carcinogenicity. With rats and rabbits, there were no indications of embryotoxic or teratogenic effects.
Uses
The Commission E approved the use of bromelain for acute post-operative and post-traumatic conditions of swelling, especially of the nasal and paranasal sinuses. Additionally, bromelain, combined with pancreatic extracts of titrated trypsin, amylase, and lipase enzymes, is suggested as treatment for the symptoms of dyspepsia and exocrine hepatic insufficiency (Bruneton, 1995).
Contraindications
Hypersensitivity to bromelain.
Side Effects
Occasionally gastric disturbances or diarrhea. Sometimes allergic reactions.
Use During Pregnancy and Lactation
No restrictions known.
Interactions with Other Drugs
An increased tendency for bleeding in the case of simultaneous administration of anticoagulants and inhibitors of thrombocytic aggregation may occur. The levels of tetracyclines in plasma and urine are increased by simultaneous intake of bromelain.
Dosage and Administration
Unless otherwise prescribed: 80-320 mg, two to three times daily for oral ingestion for 8 to 10 days. If necessary, administration may be prolonged.
Solid dosage forms: 80-320 mg of bromelain (200-800 FIP units) in 2 or 3 doses.
References
Bruneton, J. 1995. Pharmacognosy, Phytochemistry, Medicinal Plants. Paris: Lavoisier Publishing.
Castell, J.V., G. Friedrich, C.S. Kuhn, G.E. Poppe. 1997. Intestinal absorption of undegraded proteins in men: presence of bromelain in plasma after oral intake. Am J Physiol 273(1 Pt. 1):G139-146.
Leung, A.Y. and S. Foster. 1996. Encyclopedia of Common Natural Ingredients Used in Food, Drugs and Cosmetics, 2nd ed. New York: John Wiley & Sons, Inc.
Mynott, T.L., S. Guandalini, F. Raimondi, A. Fasano. 1997. Bromelain prevents secretion caused by Vibrio cholerae and Escherichia coli enterotoxins in rabbit ileum in vitro. Gastroenterol 113(1):175-184.
Samuelsson, G. 1992. Drugs of Natural Origin: A Textbook of Pharmacognosy. Stockholm: Sweden Pharmaceutical Press.
Schulz, V., R. Hänsel, V.E. Tyler. 1998. Rational Phytotherapy: A Physicians' Guide to Herbal Medicine. New York: Springer.
Taussig, S.J. and S. Batkin. 1988. Bromelain, the enzyme complex of pineapple (Ananas comosus) and its clinical application. An update. J Ethnopharmacol 22(2):191-203.
Additional Resources
Baur, X. et al. 1979. Allergic reactions, including asthma, to the pineapple protease bromelain following occupational exposure. Clin Allergy 9(5):443-450.
Der Marderosian, A. (ed.). 1999. The Review of Natural Products. St. Louis: Facts and Comparisons.
Duke, J.A. 1985. Handbook of Medicinal Herbs. Boca Raton: CRC Press.
Edenharder, R., K. John, H. Ivo-Boor. 1990. [Antimutagenic activity of vegetable and fruit extracts against in-vitro benzo(a)pyrene] [In German]. Z Gesamte Hyg 36(3):144-147.
International Commission on Pharmaceutical Enzymes. 1977. Farm Tijdschr Belg 54(85).
Lenarcic, B., A. Ritonja, B. Turk, I. Dolenc, V. Turk. 1992. Characterization and structure of pineapple stem inhibitor of cysteine proteinases. Biol Chem Hoppe Seyler 373(7):459-464.
Lotz-Winter, H. 1990. On the pharmacology of bromelain: an update with special regard to animal studies on dose-dependent effects. Planta Med 56(3):249-253.
Morton, J.F. 1977. Major Medicinal Plants. Springfield: C.C. Thomas.
Reynolds, J.E.F. (ed.). 1989. Martindale: The Extra Pharmacopoeia, 29th ed. London: The Pharmaceutical Press.
Rowan, A.D., D.J. Buttle, A.J. Barrett. 1990. The cysteine proteinases of the pineapple plant. Biochem J (266):869-875.
Stecher, P.G. et al. 1968. The Merck Index: An Encyclopedia of Chemicals and Drugs, 8th ed. Rahway, N.J.: Merck & Co., Inc.
Taussig, S.J., J. Szekerczes, S. Batkin. 1985. Inhibition of tumour growth in vitro by bromelain, an extract of the pineapple plant (Ananas comosus). Planta Med (6):538-539.
Werbach, M. and M. Murray. 1994. Botanical Influences on Illness: A Sourcebook of Clinical Research. Tarzana: Third Line Press.
This material was adapted from The Complete German Commission E Monographs—Therapeutic Guide to Herbal Medicines. M. Blumenthal, W.R. Busse, A. Goldberg, J. Gruenwald, T. Hall, C.W. Riggins, R.S. Rister (eds.) S. Klein and R.S. Rister (trans.). 1998. Austin: American Botanical Council; Boston: Integrative Medicine Communications.
1) The Overview section is new information.
2) Description, Chemistry and Pharmacology, Uses, Contraindications, Side Effects, Interactions with Other Drugs, and Dosage sections have been drawn from the original work. Additional information has been added in some or all of these sections, as noted with references.
3) The dosage for equivalent preparations (tea infusion, fluidextract, and tincture) have been provided based on the following example:
Unless otherwise prescribed: 2 g per day of [powdered, crushed, cut or whole] [plant part]
Infusion: 2 g in 150 ml of water
Fluidextract 1:1 (g/ml): 2 ml
Tincture 1:5 (g/ml): 10 ml
4) The References and Additional Resources sections are new sections. Additional Resources are not cited in the monograph but are included for research purposes.
This monograph, published by the Commission E in 1994, was modified based on new scientific research. It contains more extensive pharmacological and therapeutic information taken directly from the Commission E.
Excerpt from Herbal Medicine: Expanded Commission E Monographs Copyright 2000 American Botanical Council Published by Integrative Medicine Communications Available from the American Botanical Council.
This monograph, published by the Commission E in 1994, was modified based on new scientific research. It contains more extensive pharmacological and therapeutic information taken directly from the Commission E.