Gossypol Herb Description - Drug Interactions, Dosage and Some of its Useful Properties
Common Forms of Gossypol
Available as extracts.
Gossypol is found in the roots, seeds, and stems of the cotton plant, Gossypium hirsutum. These plants grow in Florida and are cultivated throughout the southern United States . The seeds of the Gossypium species vary widely in the quantity of gossypol content.
A polyphenolic binaphthyl dialdehyde (dextro- and levo-rotatory enantiomers), gossypol is the active constituent of cottonseed and other parts of the cotton plant. Cottonseed is also high in protein and low in fat.
In animal and human sperm cells, gossypol produces visible morphologic damage and reductions in motility, accounting for the compound's antifertility actions. Gossypol's effects are related to its ability to impair the enzyme lactate dehydrogenase X of sperm and spermgenerating cells .
Gossypol exerts numerous effects on DNA replication, synthesis, and structural integrity. Tumorigenic potential, common in agents with similar DNA activity, has been reported with gossypol in small studies. Observed disruptions in DNA function in sperm and other cells, combined with gossypol's known inhibition of oxidative phosphorylation, have led researchers to suggest antitumorigenic potential for gossypol. In vitro studies have demonstrated gossypol's inhibitory effect on the growth of malignant human cancer cells and of cultured human benign prostatic hyperplasia cells . Derivatives of gossypol have shown anti tumorigenic activity against breast tumor epithelial cell lines .
Laboratory studies suggest that gossypol and a derivative (gossylic iminolactone) have anti-HIV activity; this activity is not considered to be caused by inhibition of reverse transcriptase .
U.S. patent rights have been granted to investigate the acetic acid derivative of gossypol as a treatment for breast and prostate cancers. Early study results indicate a lower adverse effect profile for this derivative than for other drugs used for these cancers .
Reported Uses and Benefits
Gossypol is claimed to be useful for easing labor and delivery and for promoting normal menstruation; these uses have not been validated.
Studies have shown gossypol to be an effective oral male contraceptive.Questions regarding the reversibility of these effects have precluded commercial development of this agent. Sperm counts usually return to normal about 3 months after the herb is discontinued, but long-term followup of patients has indicated that spermatogenesis may not always return to normal . One clinical trial examined gossypol administration as a contraceptive pill for about 1 year in 151 men from various countries . Subjects received 15 mg/day of gossypol for 12 to 16 weeks initially. After spermatogenesis was suppressed, patients were randomized to a smaller dose of either 7.5 or 10 mg/day for 40 weeks. Slightly more than 50% of patients achieved and maintained suppression of spermatogenesis. Eight of 43 patients experienced insufficient return of sperm counts at 1 year after cessation of gossypol therapy. Serum potassium levels appeared to fluctuate within the normal range.
A clinical trial examining gossypol, 10 mg P.O. twice daily, in 27 patients with recurrent glial cell tumors suggested some potential of gossypol as an antineoplastic for gliomas, . Although promising, this information should be interpreted as preliminary data.
Other topical formulations of gossypol have been tested as vaginal spermicides and found to be comparable to other, existing spermicidal products. Gossypol appears effective in the presence of cervical mucus at low concentrations with minimal apparent systemic toxicity .
For antifertility, Chinese studies used 20 mg/day P.O. for 60 to 90 days until the sperm count was reduced to a threshold of 4 million sperm/ml; then, doses of about 50 mg weekly were maintained.
CV: circulatory problems, heart failure, peripheral edema.
GI: diarrhea, hepatotoxicity.
GU: nephrotoxicity (with high doses).
Metabolic: hypokalemia (either caused by renal tubular damage or inhibition of llbeta-hydroxysteroid dehydrogenase: remains to be proven conclusively), malnutrition.
Musculoskeletal: muscle weakness, rapid muscle fatigue. Skin: hair discoloration.
Interactions and Side Effects for Gossypol
Nephrotoxic drugs ( amphotericin B): Increased risk of nephrotoxicity. Avoid administration with gossypol.
Potassium-wasting drugs (diuretics): May lead to significant potassium depletion. Do not use together.
Contraindications and Precautions
Avoid using gossypol in pregnant or breast-feeding patients; effects are unknown. Use cautiously in patients with renal dysfunction because renal damage can occur.
Alert Cotton seeds are potentially toxic and can cause death. Domesticated animals have been poisoned from consuming feed that contained cotton seeds; postmortem examinations revealed hepatic and pulmonary edema and heart tissue degeneration. Ruminating animals (bovines) appear to be less sensitive than nonruminants to the herb's toxic effects.
Monitor BUN and serum creatinine and potassium levels in patient using gossypol.
Periodically test muscle strength of patient taking this herb.
Inform the patient who wants to use gossypol for its contraceptive effects that other products are available.
Caution the patient that permanent infertility can occur with longterm use.
Points of Interest
Gossypol was first identified as an antifertility agent in Chinese epidemiological studies conducted during the 1950s.
There is considerable debate as to whether gossypol should be pursued further as an antifertility agent for men. The World Health Organization has recommended that research on this agent be discontinued because of its potential to induce permanent infertility and hypokalemia. Published editorials highlight this interesting controversy in depth .
Commercial processing of cottonseed oil removes the gossypol content of the cotton seeds.
Gossypol-free cottonseed flour has been suggested as an economic and abundant source of protein and has been used in baked goods, livestock feed, and snacks.
Gossypol continues to show promise as an oral contraceptive for men. Its routine systemic use is daunted by the potential for irreversible sterility. Commentaries have suggested the adverse effect profile may be sufficient to disregard use of the product, but this remains controversial. Further study is needed to determine optimal dosing, route of administration, and incidence of adverse reactions. Its use as a topical vaginal spermicide may be valuable, but definitive evidence of safety and efficacy in larger human clinical trials is needed to establish a role for this agent in contraception.
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