Gosipol

Related Terms

Apogossypol, apogossypol 1b, apogossypol hexaacetate, chiral gossypol, cottonseed, cottonseed flour, cottonseed oil, cottonseed protein, DDG, DDGA, deoxyhemigossypol, DHG, DHGA, GAA, GIL, GOS, gossylic iminolactone, gossylic lactone, gossylic nitrile, gossypium, Gossypium herbaceum, Gossypium hirsutum, gossypium oil, gossypol 1a, gossypol 1c, gossypol acetic acid, gossypol dimethyl ether, gossypol ethylamine, gossypol formic acid, gossypol hexamethyl ether, gossypol Schiff's base, gossypol tetramethyl ether, gossypolone, GP, naphthaldehyde, O-hydroxylnaphthaldehyde, polyphenolic bianphthyl gossypol, racemic gossypol.

Background

Gossypol is a pigment that is most commonly produced by the stem, seeds, and roots of the cotton plant. Gossypol was first identified as an infertility agent when studies were conducted in China to explain extremely low birth rates in a particular geographic region. The phenomenon was attributed to the use of crude cottonseed oil for cooking; further investigation revealed that the antifertility agent was gossypol.
Gossypol may cause infertility in men, potentially making it a promising alternative to surgical vasectomy. In early research, gossypol shows some evidence of benefit as a treatment for endometriosis and certain cancers, but further research is necessary.
At low doses and for short durations, gossypol is well tolerated. However, its use is limited by the fact that it may cause potassium depletion and infertility.
In traditional medicine practices, gossypol has been used to treat nasal polyps, uterine fibroids, and other types of cancer. A tea of fresh or roasted seeds has been used to treat bronchitis, diarrhea, dysentery, and hemorrhage. Cottonseed oil was used by early American slaves for abortion.
Further research is needed to determine if lower doses, possibly in combination with other therapies, may be effective and safe.

Evidence Table

These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. GRADE *
These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. GRADE *


According to human studies, gossypol has been found to suppress fertility in Chinese men. Gossypol may be an effective method of birth control for men and women, although some individuals have experienced irreversible infertility after using gossypol for more than two years.

A


According to human studies, gossypol has been found to suppress fertility in Chinese men. Gossypol may be an effective method of birth control for men and women, although some individuals have experienced irreversible infertility after using gossypol for more than two years.

A


Limited research suggests that gossypol may slow the growth of cancer in humans. However, gossypol may also promote cancer formation and may not be effective against all types of cancer. Further research is needed before a firm conclusion can be made.

C


Limited research suggests that gossypol may slow the growth of cancer in humans. However, gossypol may also promote cancer formation and may not be effective against all types of cancer. Further research is needed before a firm conclusion can be made.

C


Limited research suggests that gossypol may prevent the growth of endometrial cells (those that line the inside of the uterus) and prevent ovulation. Further research is needed before a firm conclusion can be made.

C


Limited research suggests that gossypol may prevent the growth of endometrial cells (those that line the inside of the uterus) and prevent ovulation. Further research is needed before a firm conclusion can be made.

C


Limited research suggests that, when applied to the vagina, gossypol may prevent the movement of spermatozoa. This may make it useful in preventing pregnancy or sexually transmitted diseases. Further research is needed before a firm conclusion can be made.

C


Limited research suggests that, when applied to the vagina, gossypol may prevent the movement of spermatozoa. This may make it useful in preventing pregnancy or sexually transmitted diseases. Further research is needed before a firm conclusion can be made.

C
* Key to grades

A: Strong scientific evidence for this use
B: Good scientific evidence for this use
C: Unclear scientific evidence for this use
D: Fair scientific evidence for this use (it may not work)
F: Strong scientific evidence against this use (it likley does not work)
* Key to grades

A: Strong scientific evidence for this use
B: Good scientific evidence for this use
C: Unclear scientific evidence for this use
D: Fair scientific evidence for this use (it may not work)
F: Strong scientific evidence against this use (it likley does not work)

Tradition / Theory

The below uses are based on tradition, scientific theories, or limited research. They often have not been thoroughly tested in humans, and safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. There may be other proposed uses that are not listed below.

Dosing

Adults (18 years and older)
The maximal tolerated dose of gossypol is reported to be 40 milligrams daily when taken by mouth.
To treat cancer, 10-70 milligrams of gossypol has been given daily by mouth for 4-78 weeks.
To function as a birth control agent, 7.5-20 milligrams of gossypol has been given daily by mouth for 10-44 weeks. A maintenance dose of 20 milligrams gossypol, given 2-3 times weekly for 8-22 months, has also been used. Also, 20 milligrams of gossypol has been given with 1.5 grams of potassium chloride or 50 milligrams of triamterene for 12 months.
To treat endometriosis (abnormal growth of uterine cells in other parts of the body), 20 milligrams of gossypol has been given twice daily by mouth for 20 days, followed by 20 milligrams twice weekly for six months.
To be used as a topical birth control agent, a gel containing 0.5 milligrams of gossypol per milliliter of gel has been applied to the vagina one hour before intercourse.

Safety

The U.S. Food and Drug Administration does not strictly regulate herbs and supplements. There is no guarantee of strength, purity or safety of products, and effects may vary. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy. Consult a healthcare provider immediately if you experience side effects.

Interactions

Interactions with Drugs
Gossypol may interact with agents that affect hormone levels, agents that affect potassium levels (particularly ACE inhibitors or angiotensin receptor blocking agents (ARBs)), alcohol, beta-blockers, birth control or fertility agents, cyclosporine, diuretics (agents that increase urination; particularly those that affect potassium levels), laxatives, metyrapone, nonsteroidal anti-inflammatory agents (NSAIDS), phenobarbital, steroids, sulfadiazine, and theophylline.

Attribution

This information is based on a systematic review of scientific literature edited and peer-reviewed by contributors to the Natural Standard Research Collaboration (www.naturalstandard.com).

Bibliography

Dodou K, Anderson RJ, Small DA, and Groundwater PW. Investigations on gossypol: past and present developments. Expert.Opin.Investig.Drugs 2005;14(11):1419-1434.
Final report on the safety assessment of Hydrogenated Cottonseed Oil, Cottonseed (Gossypium) Oil, Cottonseed Acid, Cottonseed Glyceride, and Hydrogenated Cottonseed Glyceride. Int J Toxicol. 2001;20 Suppl 2:21-29.
Kalla NR. Gossypol. Acta Eur.Fertil. 1990;21(1):5-6.
Kovacic P. Mechanism of drug and toxic actions of gossypol: focus on reactive oxygen species and electron transfer. Curr.Med.Chem. 2003;10(24):2711-2718.
Le Blanc M, Russo J, Kudelka AP, and Smith JA. An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines. Pharmacol.Res. 2002;46(6):551-555.
Liu GZ, Lyle KC. Clinical trial of gossypol as a male contraceptive drug. Part II. Hypokalemia study. Fertil.Steril. 1987;48(3):462-465.
Liu GZ, Ch'iu-Hinton K, Cao JA, Zhu CX, and Li BY. Effects of K salt or a potassium blocker on gossypol-related hypokalemia. Contraception 1988;37(2):111-117.
Miller LG. Herbal medicinals: selected clinical considerations focusing on known or potential drug-herb interactions. Arch.Intern.Med 11-9-1998;158(20):2200-2211.
Porat O. Effects of gossypol on the motility of mammalian sperm. Mol.Reprod.Dev. 1990;25(4):400-408.
Qian SZ. Gossypol-hypokalaemia interrelationships. Int.J.Androl 1985;8(4):313-324.
Royer RE, Mills RG, Deck LM, Mertz GJ, and Vander Jagt DL. Inhibition of human immunodeficiency virus type I replication by derivatives of gossypol. Pharmacol.Res. 1991;24(4):407-412.
Stein RC, Joseph AE, Matlin SA, Cunningham DC, Ford HT, and Coombes RC. A preliminary clinical study of gossypol in advanced human cancer. Cancer Chemother.Pharmacol. 1992;30(6):480-482.
Waites GM, Wang C, and Griffin PD. Gossypol: reasons for its failure to be accepted as a safe, reversible male antifertility drug. Int.J.Androl 1998;21(1):8-12.
Wu D. An overview of the clinical pharmacology and therapeutic potential of gossypol as a male contraceptive agent and in gynaecological disease. Drugs 1989;38(3):333-341.
Wu YW, Chik CL, and Knazek RA. An in vitro and in vivo study of antitumor effects of gossypol on human SW-13 adrenocortical carcinoma. Cancer Res. 7-15-1989;49(14):3754-3758.