GOSSYPOL

OTHER NAME(S):

Coton Velu, Cotonnier Herbacé, Cottonseed Oil Extract, Extrait d’Huile de Coton, Gosipol, Gossypium herbaceum, Gossypium hirsutum, Karpasa.<br/><br/>

Overview

Overview Information

Gossypol is a substance that is found in the cotton plant. It is removed from the seeds and used for medicine.

Men take gossypol for birth control. Women take it for disorders of the uterus including endometriosis, abnormal bleeding, and cancer; as well as for ovarian cancer. Gossypol is also used for treating HIV/AIDS.

Sometimes women use gossypol cream or gel as birth control. It is applied to the inside of the vagina to kill sperm.

How does it work?

Gossypol interferes with sperm development and function.

Uses

Uses & Effectiveness?

Possibly Effective for

  • Male contraception (birth control), when taken by mouth. Taking gossypol by mouth seems to reduce sperm count and function in 60% to 100% of men. In 50% to 77% of men, sperm recover within 3-24 months after treatment is stopped. In about 10% of men, sperm counts remain very low for over 4.5 years. In some men, continual use of gossypol can cause permanent loss of the ability to father a child.

Insufficient Evidence for

  • Cancer. Early research suggests that taking gossypol by mouth does not help shrink tumors in people with advanced cancer.
  • Problems of the uterus (womb) and ovaries.
  • HIV/AIDS.
  • Killing sperm, when applied inside the vagina.
  • Other conditions.
More evidence is needed to rate the effectiveness of gossypol for these uses.

Side Effects

Side Effects & Safety

Gossypol is POSSIBLY UNSAFE for use without close supervision by a healthcare professional. When men take gossypol by mouth, the effects on sperm are unpredictable and might cause permanent inability to father a child (sterility) with long-term use. When women take gossypol by mouth, it might be toxic to cells lining the uterus and could prevent normal function of the ovaries.

Gossypol can also cause loss of energy, changes in appetite, decreased sexual desire (libido), changes in body potassium levels, and digestive tract problems. High doses of gossypol (100 times the dose used for birth control) can cause malnutrition, blood circulation problems, heart failure, changes in hair color, and other problems.

There isn't enough information to know whether gossypol is safe to use directly on the skin. It can cause a burning sensation.

Special Precautions & Warnings:

Pregnancy and breast-feeding: It’s LIKELY UNSAFE to take gossypol if you are pregnant. It might cause a miscarriage. It is POSSIBLY UNSAFE to take gossypol if you are breast-feeding.

Low potassium levels (hypokalemia): Gossypol may make low potassium levels worse. Avoid using it if you have this condition.

Urinary tract irritation: Gossypol may make urinary tract irritation worse. Avoid using it if you have this condition.

Interactions

Interactions?

Moderate Interaction

Be cautious with this combination

!
  • Digoxin (Lanoxin) interacts with GOSSYPOL

    Large amounts of gossypol can decrease potassium levels in the body. Low potassium levels can increase the side effects of digoxin (Lanoxin).

  • NSAIDs (Nonsteroidal anti-inflammatory drugs) interacts with GOSSYPOL

    NSAIDs are anti-inflammatory medications used for decreasing pain and swelling. NSAIDs can cause irritation to the stomach and intestines. Gossypol can also cause irritation to the stomach and intestines. Taking NSAIDs along with gossypol might increase the chances of adverse effects. Avoid taking NSAIDs and gossypol together.<br><nb>Some NSAIDs include ibuprofen (Advil, Motrin, Nuprin, others), indomethacin (Indocin), naproxen (Aleve, Anaprox, Naprelan, Naprosyn), piroxicam (Feldene), aspirin, and others.

  • Stimulant laxatives interacts with GOSSYPOL

    Stimulant laxatives speed up the bowels. Overuse of stimulant laxatives can cause low minerals in the body. Gossypol can also decrease minerals in the body. Do not take gossypol along with stimulant laxatives.

  • Theophylline interacts with GOSSYPOL

    Theophylline might decrease some of the effects of gossypol.

  • Warfarin (Coumadin) interacts with GOSSYPOL

    Gossypol can work as a laxative. In some people gossypol can cause diarrhea. Diarrhea can increase the effects of warfarin and increase the risk of bleeding. If you take warfarin do not to take excessive amounts of gossypol.

  • Water pills (Diuretic drugs) interacts with GOSSYPOL

    Large amounts of gossypol can decrease potassium levels in the body. "Water pills" can also decrease potassium in the body. Taking gossypol along with "water pills" might decrease potassium in the body too much.<br><nb>Some "water pills" that can deplete potassium include chlorothiazide (Diuril), chlorthalidone (Thalitone), furosemide (Lasix), hydrochlorothiazide (HCTZ, HydroDiuril, Microzide), and others.

Dosing

Dosing

The following doses have been studied in scientific research:

BY MOUTH:

  • For male birth control: 15-20 mg is used daily for 12-16 weeks, followed by a maintenance dose of 7.5-10 mg per day. Treatment should be carefully monitored by a healthcare professional, because the effects of gossypol are unpredictable and might lead to permanent loss of the ability to father a child.

View References

REFERENCES:

  • Qian, S. Z. Gossypol-hypokalaemia interrelationships. Int.J.Androl 1985;8(4):313-324. View abstract.
  • Qian, S. Z., Jing, G. W., Wu, X. Y., Xu, Y., Li, Y. Q., and Zhou, Z. H. Gossypol related hypokalemia. Clinicopharmacologic studies. Chin Med.J.(Engl.) 1980;93(7):477-482. View abstract.
  • Rabe, T., Grunwald, K., and Runnebaum, B. [Future prospects in contraception]. Arch.Gynecol.Obstet. 1995;257(1-4):541-547. View abstract.
  • Randel, R. D., Chase, C. C., Jr., and Wyse, S. J. Effects of gossypol and cottonseed products on reproduction of mammals. J.Anim Sci. 1992;70(5):1628-1638. View abstract.
  • Rao, A. G. A stoichiometric analysis of bovine serum albumin-gossypol interactions: a fluorescence quenching study. Indian J.Biochem.Biophys. 1992;29(2):179-182. View abstract.
  • Ray, S., Verma, P., and Kumar, A. Development of male-fertility-regulating agents. Med.Res.Rev. 1991;11(5):437-472. View abstract.
  • Reidenberg, M. M. Environmental inhibition of 11beta-hydroxysteroid dehydrogenase. Toxicology 4-3-2000;144(1-3):107-111. View abstract.
  • Reidenberg, M. M., Gu, Z. P., Lorenzo, B., Coutinho, E., Athayde, C., Frick, J., Alvarez, F., Brache, V., and Emuveyan, E. E. Differences in serum potassium concentrations in normal men in different geographic locations. Clin.Chem. 1993;39(1):72-75. View abstract.
  • Rekha, G. K. and Sladek, N. E. Inhibition of human class 3 aldehyde dehydrogenase, and sensitization of tumor cells that express significant amounts of this enzyme to oxazaphosphorines, by the naturally occurring compound gossypol. Adv.Exp.Med.Biol. 1997;414:133-146. View abstract.
  • Ridley, A. J. and Blasco, L. Testosterone and gossypol effects on human sperm motility. Fertil.Steril. 1981;36(5):638-642. View abstract.
  • Rosenberg, L. J., Adlakha, R. C., Desai, D. M., and Rao, P. N. Inhibition of DNA polymerase alpha by gossypol. Biochim.Biophys.Acta 5-5-1986;866(4):258-267. View abstract.
  • Royer, R. E. and Vander Jagt, D. L. Gossypol binds to a high-affinity binding site on human serum albumin. FEBS Lett. 6-27-1983;157(1):28-30. View abstract.
  • Royer, R. E., Deck, L. M., Campos, N. M., Hunsaker, L. A., and Vander Jagt, D. L. Biologically active derivatives of gossypol: synthesis and antimalarial activities of peri-acylated gossylic nitriles. J.Med.Chem. 1986;29(9):1799-1801. View abstract.
  • Royer, R. E., Kibirige, M., Tafoya, C. R., Deck, L. M., and Vander Jagt, D. L. Binding of gossypol derivatives to human serum albumin. J.Pharm.Sci. 1988;77(3):237-240. View abstract.
  • Royer, R. E., Mills, R. G., Deck, L. M., Mertz, G. J., and Vander Jagt, D. L. Inhibition of human immunodeficiency virus type I replication by derivatives of gossypol. Pharmacol.Res. 1991;24(4):407-412. View abstract.
  • Sadykov, A. S., Ismailov, A. I., Zakhidov, S. T., and Baram, N. I. [Effect of gossypol on spermatogenesis and fertility in man and mammals]. Ontogenez 1985;16(4):346-357. View abstract.
  • Sagach, V. F., Kindybalyuk, A. M., and Kovalenko, T. N. Functional hyperemia of skeletal muscle: role of endothelium. J Cardiovasc.Pharmacol. 1992;20 Suppl 12:S170-S175. View abstract.
  • Sampath, D. S. and Balaram, P. Resolution of racemic gossypol and interaction of individual enantiomers with serum albumins and model peptides. Biochim.Biophys.Acta 6-19-1986;882(2):183-186. View abstract.
  • Shelley, M. D., Hartley, L., Groundwater, P. W., and Fish, R. G. Structure-activity studies on gossypol in tumor cell lines. Anticancer Drugs 2000;11(3):209-216. View abstract.
  • Sheriff, D. S., Ghwarsha, K., Elgengan, K. B., and el Fakhri, M. Effect of gossypol on the activity of erythrocyte Na+-K+ ATPase activity in vitro. Clin.Chem. 1987;33(2 Pt 1):309. View abstract.
  • Shidaifat, F., Canatan, H., Kulp, S. K., Sugimoto, Y., Zhang, Y., Brueggemeier, R. W., Somers, W. J., Chang, W. Y., Wang, H. C., and Lin, Y. C. Gossypol arrests human benign prostatic hyperplastic cell growth at G0/G1 phase of the cell cycle. Anticancer Res. 1997;17(2A):1003-1009. View abstract.
  • Silvestre, L., Varin, C., and Bouchard, P. [Male contraception in 1987]. Rev Prat. 9-21-1987;37(38):2302-2311. View abstract.
  • Song, D., Lorenzo, B., and Reidenberg, M. M. Inhibition of 11 beta-hydroxysteroid dehydrogenase by gossypol and bioflavonoids. J.Lab Clin.Med. 1992;120(5):792-797. View abstract.
  • Stein, R. C., Joseph, A. E., Matlin, S. A., Cunningham, D. C., Ford, H. T., and Coombes, R. C. A preliminary clinical study of gossypol in advanced human cancer. Cancer Chemother.Pharmacol. 1992;30(6):480-482. View abstract.
  • Szarvas, F. Andrology today. Ther Hung. 1990;38(2):47-56. View abstract.
  • Taitzoglou, I. A., Tsantarliotou, M., Kouretas, D., and Kokolis, N. A. Gossypol-induced inhibition of plasminogen activator activity in human and ovine acrosomal extract. Andrologia 1999;31(6):355-359. View abstract.
  • Tang, M. Y. [Electron microscopic observation of the effect of gossypol on atypical hyperplasia of the endometrium]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1988;10(2):124-126. View abstract.
  • Tegos, G., Stermitz, F. R., Lomovskaya, O., and Lewis, K. Multidrug pump inhibitors uncover remarkable activity of plant antimicrobials. Antimicrob.Agents Chemother. 2002;46(10):3133-3141. View abstract.
  • Teng, C. S. c-fos protein expression in apoptotic rat spermatocytes induced by gossypol. Contraception 1998;57(4):281-286. View abstract.
  • Teng, C. S. Reversible changes in the content of cellular and microtubular tubulin in spermatogenic cells after gossypol treatment. Contraception 1997;55(1):41-46. View abstract.
  • Thomas, M., von, Hagen, V, Moustafa, Y., Montmasson, M. P., and Monet, J. D. Effects of gossypol on the cell cycle phases in T-47D human breast cancer cells. Anticancer Res. 1991;11(4):1469-1475. View abstract.
  • Trevino, C. L., Felix, R., Castellano, L. E., Gutierrez, C., Rodriguez, D., Pacheco, J., Lopez-Gonzalez, I., Gomora, J. C., Tsutsumi, V., Hernandez-Cruz, A., Fiordelisio, T., Scaling, A. L., and Darszon, A. Expression and differential cell distribution of low-threshold Ca(2+) channels in mammalian male germ cells and sperm. FEBS Lett. 4-9-2004;563(1-3):87-92. View abstract.
  • Tripathi, A. K., Desai, P. V., Pradhan, A., Khan, S. I., Avery, M. A., Walker, L. A., and Tekwani, B. L. An alpha-proteobacterial type malate dehydrogenase may complement LDH function in Plasmodium falciparum. Cloning and biochemical characterization of the enzyme. Eur.J Biochem. 2004;271(17):3488-3502. View abstract.
  • Tso, W. W. and Lee, C. S. Cottonseed oil as a vaginal contraceptive. Arch.Androl 1982;8(1):11-14. View abstract.
  • Tsui, Y. C., Creasy, M. R., and Hulten, M. A. The effect of the male contraceptive agent Gossypol on human lymphocytes in vitro: traditional chromosome breakage, micronuclei, sister chromatid exchange, and cell kinetics. J.Med.Genet. 1983;20(2):81-85. View abstract.
  • Tuszynski, G. P. and Cossu, G. Differential cytotoxic effect of gossypol on human melanoma, colon carcinoma, and other tissue culture cell lines. Cancer Res. 1984;44(2):768-771. View abstract.
  • Vainio, P., Thuren, T., Wichman, K., Luukkainen, T., and Kinnunen, P. K. Hydrolysis of phospholipid monolayers by human spermatozoa. Inhibition by male contraceptive gossypol. Biochim.Biophys.Acta 4-11-1985;814(2):405-408. View abstract.
  • Van Poznak, C., Seidman, A. D., Reidenberg, M. M., Moasser, M. M., Sklarin, N., Van Zee, K., Borgen, P., Gollub, M., Bacotti, D., Yao, T. J., Bloch, R., Ligueros, M., Sonenberg, M., Norton, L., and Hudis, C. Oral gossypol in the treatment of patients with refractory metastatic breast cancer: a phase I/II clinical trial. Breast Cancer Res.Treat. 2001;66(3):239-248. View abstract.
  • Vander Jagt, D. L., Deck, L. M., and Royer, R. E. Gossypol: prototype of inhibitors targeted to dinucleotide folds. Curr.Med.Chem. 2000;7(4):479-498. View abstract.
  • Vlietinck, A. J., De Bruyne, T., Apers, S., and Pieters, L. A. Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection. Planta Med. 1998;64(2):97-109. View abstract.
  • Vongsorasak, L. and Svasti, J. Gossypol prevents activation of purified proenzyme of human seminal plasma acidic proteinase. Biochim.Biophys.Acta 9-4-1986;883(2):271-276. View abstract.
  • Vongsorasak, L. and Svasti, J. Inhibition of liquefaction and protein degradation in human semen by gossypol. Int.J.Androl 1985;8(6):472-483. View abstract.
  • Vranova, J., Jezova, M., Scsukova, S., and Kolena, J. Inhibitory effect of gossypol on basal and luteinization factor-stimulated progesterone synthesis in porcine granulosa cells. Physiol Res. 1999;48(2):119-128. View abstract.
  • Vyas, R. K. and Kalla, N. R. Effect of optical isomers of gossypol on mammalian spermatozoa: an in vitro study. Acta Eur.Fertil. 1990;21(2):95-98. View abstract.
  • Waites, G. M. Male fertility regulation: the challenges for the year 2000. Br.Med Bull. 1993;49(1):210-221. View abstract.
  • Waites, G. M. The contribution of Asian scientists to global research in andrology. Asian J Androl 1999;1(1-2):7-12. View abstract.
  • Waites, G. M., Wang, C., and Griffin, P. D. Gossypol: reasons for its failure to be accepted as a safe, reversible male antifertility drug. Int.J.Androl 1998;21(1):8-12. View abstract.
  • Waller, D. P., Fong, H. H., Cordell, G. A., and Soejarto, D. D. Antifertility effects of gossypol and its impurities on male hamsters. Contraception 1981;23(6):653-660. View abstract.
  • Wang, C. and Yeung, R. T. Gossypol and hypokalaemia. Contraception 1985;32(3):237-252. View abstract.
  • Wang, H. X. and Ng, T. B. Examination of lectins, polysaccharopeptide, polysaccharide, alkaloid, coumarin and trypsin inhibitors for inhibitory activity against human immunodeficiency virus reverse transcriptase and glycohydrolases. Planta Med 2001;67(7):669-672. View abstract.
  • Wang, W. C., Jiang, Y., Zhao, X. J., Wang, Y. X., Chen, Z. X., and Liu, X. H. [Changes of serum concentrations of testosterone, LH and FSH in men taking gossypol]. Yao Xue.Xue.Bao. 1985;20(9):696-698. View abstract.
  • Wang, X., Wang, J., Wong, S. C., Chow, L. S., Nicholls, J. M., Wong, Y. C., Liu, Y., Kwong, D. L., Sham, J. S., and Tsa, S. W. Cytotoxic effect of gossypol on colon carcinoma cells. Life Sci. 10-20-2000;67(22):2663-2671. View abstract.
  • Wang, Y. and Rao, P. N. Effect of gossypol on DNA synthesis and cell cycle progression of mammalian cells in vitro. Cancer Res. 1984;44(1):35-38. View abstract.
  • Wang, Y. F., Tang, M. Y., Han, M. L., and Zhu, Y. N. [Ultrastructural changes in smooth muscle cells in leiomyoma and the myometrium of the human uterus after gossypol treatment]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1987;9(4):298-301. View abstract.
  • Whaley, K. J., Sampath, D. S., and Balaram, P. Optically active gossypol as a circular dichroism probe of interactions with serum albumins. Biochim.Biophys.Acta 9-7-1984;801(1):127-130. View abstract.
  • Wichmann, K., Kapyaho, K., Sinervirta, R., and Janne, J. Effect of gossypol on the motility and metabolism of human spermatozoa. J.Reprod.Fertil. 1983;69(1):259-264. View abstract.
  • Wichmann, K., Krusius, T., Sinervirta, R., Puranen, J., and Janne, J. Studies on structure-activity relationship of gossypol, gossypol ethers and three naphthaldehydes in the inhibition of spermatozoal metabolism. Contraception 1986;33(5):519-528. View abstract.
  • Wichmann, K., Vaheri, A., and Luukkainen, T. Inhibiting herpes simplex virus type 2 infection in human epithelial cells by gossypol, a potent spermicidal and contraceptive agent. Am.J.Obstet.Gynecol. 3-1-1982;142(5):593-594. View abstract.
  • Woolley, R. J. Contraception--a look forward, Part II: Mifepristone and gossypol. J.Am.Board Fam.Pract. 1991;4(2):103-113. View abstract.
  • Wu, D. F. and Reidenberg, M. M. Stereoselective interaction between gossypol and rat plasma. Contraception 1990;41(4):377-388. View abstract.
  • Wu, D. F., Reidenberg, M. M., and Drayer, D. E. Determination of gossypol enantiomers in plasma after administration of racemate using high-performance liquid chromatography with precolumn chemical derivatisation. J.Chromatogr. 12-9-1988;433:141-148. View abstract.
  • Wu, D. F., Yu, Y. W., and Zheng, D. K. [Determination of (+)- and (-)-gossypol in human plasma using high performance liquid chromatography with pre-column chemical derivatization]. Yao Xue.Xue.Bao. 1988;23(12):927-932. View abstract.
  • Wu, D. F., Yu, Y. W., Tang, Z. M., and Wang, M. Z. Pharmacokinetics of (+/-)-, (+)-, and (-)-gossypol in humans and dogs. Clin.Pharmacol.Ther. 1986;39(6):613-618. View abstract.
  • Wu, F., Zhang, Z., Ye, W., and Qian, X. [Comparative study on the effect of gossypol and T7 on human spermatozoa ATPase activity]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1998;20(4):267-270. View abstract.
  • Wu, T., Sha, Y., Han, F., Duan, J., and Cheng, J. [Effects of gossypol acetic acid on human ejaculated sperm Ca2+ influx and rat vas deferens contraction action]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1996;18(5):375-379. View abstract.
  • Wu, Y. W., Chik, C. L., Albertson, B. D., Linehan, W. M., and Knazek, R. A. Inhibitory effects of gossypol on adrenal function. Acta Endocrinol.(Copenh) 1991;124(6):672-678. View abstract.
  • Wu, Y. W., Chik, C. L., and Knazek, R. A. 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. View abstract.
  • Xu, L. F., Wang, M., and Zhao, C. L. [Clinical effects and experimental study on gossypol in endometriosis]. Zhong.Xi.Yi.Jie.He.Za Zhi. 1989;9(8):462-4, 451. View abstract.
  • Xue, S. [A beam of dawn light of study on gossypol as a safe, effective, and reversible male antifertility contraceptive--evaluation of the studies by using low dose gossypol combined with steroid hormone for male contraception]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 2000;22(3):211-213. View abstract.
  • Xue, S. P., Liang, D. C., Fei, R. R., Chen, X. M., Ye, S. J., Liu, Y., Wu, Y. W., You, M. M., and Guo, X. Y. Subcellular site of antispermatogenic effect of gossypol and its possible molecular mechanism of action. Sci.Sin.[B] 1983;26(6):614-633. View abstract.
  • Yang, B., Cao, L., Xu, Y., Sun, Z. X., and Gu, Z. P. [The effects of gossypol on rat luteal cells, human decidual cells and cytotrophoblasts]. Yao Xue.Xue.Bao. 1997;32(8):573-577. View abstract.
  • Ye, W. S., Lang, J. C., and Hsu, T. C. [Clastogenicity of a male contraceptive, gossypol, in mammalian cell cultures with and without metabolic activation by S9 mix]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1986;8(2):100-105. View abstract.
  • Ye, W. S., Liang, J. C., and Hsu, T. C. Toxicity of a male contraceptive, gossypol, in mammalian cell cultures. In Vitro 1983;19(1):53-57. View abstract.
  • Ye, X. Q. [Clinical and experimental study of gossypol in the treatment of dysfunctional menorrhagia, endometriosis and fibromyoma of the uterus]. Zhong.Xi.Yi.Jie.He.Za Zhi. 1988;8(4):216-7, 197. View abstract.
  • Ye, Y. X., Bombick, D., Hirst, K., Zhang, G. X., Chang, C. C., Trosko, J. E., and Akera, T. The modulation of gap junctional communication by gossypol in various mammalian cell lines in vitro. Fundam.Appl.Toxicol. 1990;14(4):817-832. View abstract.
  • YU, T. W. [Ultrastructural study of the testis in 22 persons based on the effect of gossypol]. Zhonghua Bing.Li Xue.Za Zhi. 1987;16(1):60-61. View abstract.
  • Yu, Y. W. Probing into the mechanism of action, metabolism and toxicity of gossypol by studying its (+)- and (-)-stereoisomers. J.Ethnopharmacol. 1987;20(1):65-78. View abstract.
  • Yu, Y., Deck, J. A., Hunsaker, L. A., Deck, L. M., Royer, R. E., Goldberg, E., and Vander Jagt, D. L. Selective active site inhibitors of human lactate dehydrogenases A4, B4, and C4. Biochem.Pharmacol. 7-1-2001;62(1):81-89. View abstract.
  • Yu, Z. H. and Chan, H. C. Gossypol as a male antifertility agent--why studies should have been continued. Int.J.Androl 1998;21(1):2-7. View abstract.
  • Yurtcu, E., Ergun, M. A., and Menevse, A. Apoptotic effect of gossypol on human lymphocytes. Cell Biol.Int. 2003;27(9):791-794. View abstract.
  • Zavos, P. M. and Zarmakoupis-Zavos, P. N. The inhibitory effects of gossypol on human sperm motility characteristics: possible modes of reversibility of those effects. Tohoku J.Exp.Med. 1996;179(3):167-175. View abstract.
  • Zha, S. W., Zha, J., and Huang, Y. F. [Male antifertility drugs and cell apoptosis]. Zhonghua Nan.Ke.Xue. 2008;14(1):75-78. View abstract.
  • Zhang, G. Y., Xiao, B., Chen, Z. W., Zhu, J. C., and Meng, G. D. Dynamic study of serum gonadotrophin and testosterone levels in gossypol-treated men. Long term follow-up study of 60 cases. Int.J.Androl 1985;8(3):177-185. View abstract.
  • Zhang, J. B., Yang, Y. Z., Yuan, J., and Xue, S. P. [Observations of in vitro fertilization capacity and the transformation of human sperm nuclei before and after administration of gossypol acetic acid]. Shi Yan.Sheng Wu Xue.Bao. 1985;18(1):59-65. View abstract.
  • Zhang, J. F., Zhang, J. B., and Yuan, J. [Experimental studies on the cytotoxic effect of gossypol in mice, rats and human tumor cell lines and its possible mechanism]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1986;8(6):486-489. View abstract.
  • Zhang, L. S. [Effect of gossypol on serum gonadotropin and testosterone levels: long-term follow-up study]. Zhonghua Yi.Xue.Za Zhi. 1985;65(8):464-467. View abstract.
  • Zhang, M., Liu, H., Guo, R., Ling, Y., Wu, X., Li, B., Roller, P. P., Wang, S., and Yang, D. Molecular mechanism of gossypol-induced cell growth inhibition and cell death of HT-29 human colon carcinoma cells. Biochem.Pharmacol. 7-1-2003;66(1):93-103. View abstract.
  • Zhang, S. F., Zhang, J. B., and Yuan, J. [Synergic effects of gossypol acetate and sulphadiazine on the LDH-x activity and viability of human sperm]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1985;7(3):229-231. View abstract.
  • Zhang, Y. W., Han, M. L., and Wang, Y. F. [Estrogen and progesterone cytosol receptor concentrations in patients with endometriosis and their changes after gossypol therapy]. Zhonghua Fu Chan Ke.Za Zhi. 1994;29(4):220-3, 253. View abstract.
  • Zhang, Y., Kulp, S. K., Sugimoto, Y., Brueggemeier, R. W., and Lin, Y. C. The (-)-enantiomer of gossypol inhibits proliferation of stromal cells derived from human breast adipose tissues by enhancing transforming growth factor beta1 production. Int.J.Oncol. 1998;13(6):1291-1297. View abstract.
  • Zhao, Y., Zhang, J. C., Ye, L. Z., Ma, S. W., Luo, H. Y., Han, M. L., Wang, Y. F., Ma, X. H., and Ge, Q. S. Studies on frequencies of sister chromatid exchange in peripheral blood lymphocytes before and after gossypol treatment. Proc.Chin Acad.Med.Sci.Peking.Union Med.Coll. 1986;1(1):34-36. View abstract.
  • Horstmann, M., Merseburger, A. S., Stenzl, A., and Kuczyk, M. [Systemic therapy of malignant adrenal tumors]. Urologe A 2006;45(5):605-608. View abstract.
  • Hoshiai, H., Uehara, S., Mori, R., Nagaike, F., Tsuiki, A., and Suzuki, M. Gossypol as oral contraceptive for male: trial case report. Tohoku J.Exp.Med. 1982;138(3):275-280. View abstract.
  • Hou, D. X., Uto, T., Tong, X., Takeshita, T., Tanigawa, S., Imamura, I., Ose, T., and Fujii, M. Involvement of reactive oxygen species-independent mitochondrial pathway in gossypol-induced apoptosis. Arch.Biochem.Biophys. 8-15-2004;428(2):179-187. View abstract.
  • Hover, C. G. and Kulkarni, A. P. A simple and efficient method for hemoglobin removal from mammalian tissue cytosol by zinc sulfate and its application to the study of lipoxygenase. Prostaglandins Leukot.Essent.Fatty Acids 2000;62(2):97-105. View abstract.
  • Hu, Y. F., Chang, C. J., Brueggemeier, R. W., and Lin, Y. C. Gossypol inhibits basal and estrogen-stimulated DNA synthesis in human breast carcinoma cells. Life Sci. 1993;53(25):L433-L438. View abstract.
  • Hu, Y. F., Chang, C. J., Brueggemeier, R. W., and Lin, Y. C. Presence of antitumor activities in the milk collected from gossypol-treated dairy cows. Cancer Lett. 11-25-1994;87(1):17-23. View abstract.
  • Huang, H. F. and Wang, M. [Effects of gossypol acetate, danazol, progesterone and GnRH-A on estrogen and progesterone receptors of human endometrial cells]. Zhongguo Zhong.Xi.Yi.Jie.He.Za Zhi. 1994;14(6):352-3, 325. View abstract.
  • Huang, H. F. and Wang, M. [Effects of gossypol acetate, progesterone, danazol and GnRH-A (gonadotropin release hormone-A) on the DNA-synthesis of human endometrial cell in vitro]. Zhong.Xi.Yi.Jie.He.Za Zhi. 1990;10(8):476-8, 453. View abstract.
  • Iglesias, Cortit L. [New advances in contraception and sterilization]. Med Clin.(Barc.) 11-2-1985;85(14):588-595. View abstract.
  • Ikeda, M. Inhibition kinetics of NAD-linked enzymes by gossypol acetic acid. Andrologia 1990;22(5):409-416. View abstract.
  • Jan, C. R., Lin, M. C., Chou, K. J., and Huang, J. K. Novel effects of gossypol, a chemical contraceptive in man: mobilization of internal Ca(2+) and activation of external Ca(2+) entry in intact cells. Biochim.Biophys.Acta 4-17-2000;1496(2-3):270-276. View abstract.
  • Jaroszewski, J. W., Kaplan, O., and Cohen, J. S. Action of gossypol and rhodamine 123 on wild type and multidrug-resistant MCF-7 human breast cancer cells: 31P nuclear magnetic resonance and toxicity studies. Cancer Res. 11-1-1990;50(21):6936-6943. View abstract.
  • Jarvis, W. D., Turner, A. J., Povirk, L. F., Traylor, R. S., and Grant, S. Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C. Cancer Res. 4-1-1994;54(7):1707-1714. View abstract.
  • Jiang, J., Ghosh, P. K., Kulp, S. K., Sugimoto, Y., Liu, S., Czekajewski, J., Chang, H. L., and Lin, Y. C. Effects of gossypol on O2 consumption and CO2 production in human prostate cancer cells. Anticancer Res. 2002;22(3):1491-1496. View abstract.
  • Jin, Y., Chen, H. C., Wo, W. H., Yang, M. Z., and Xue, S. P. Effects of gossypol on Na+, K+ transmembrane fluxes in human red cells. Proc.Chin Acad.Med.Sci.Peking.Union Med.Coll. 1989;4(2):91-95. View abstract.
  • Johnsen, O., Mas, Diaz J., and Eliasson, R. Gossypol; a potent inhibitor of human sperm acrosomal proteinase. Int.J.Androl 1982;5(6):636-640. View abstract.
  • Joseph, A. E., Matlin, S. A., and Knox, P. Cytotoxicity of enantiomers of gossypol. Br.J.Cancer 1986;54(3):511-513. View abstract.
  • Joseph, P., Srinivasan, S. N., and Kulkarni, A. P. Purification and partial characterization of lipoxygenase with dual catalytic activities from human term placenta. Biochem.J 7-1-1993;293 ( Pt 1):83-91. View abstract.
  • Kable, E. P. and Parsons, P. G. Potency, selectivity and cell cycle dependence of catechols in human tumour cells in vitro. Biochem.Pharmacol. 5-1-1988;37(9):1711-1715. View abstract.
  • Kalla, N. R. and Vasudev, M. Studies on the male antifertility agent-gossypol acetic acid. II. Effect of gossypol acetic acid on the motility and ATPase activity of human spermatozoa. Andrologia 1981;13(2):95-98. View abstract.
  • Kalla, N. R. Gossypol. Acta Eur.Fertil. 1990;21(1):5-6. View abstract.
  • Kalla, N. R., Gadru, N., and Foo, T. W. Studies on the male antifertility agent gossypol acetic acid. VII. Effect of motility stimulated factors on the revival of human spermatozoal motility after gossypol treatment in vitro. Andrologia 1986;18(4):393-397. View abstract.
  • Kanwar, U., Batla, A., Sanyal, S., Minocha, R., Majumdar, S., and Ranga, A. Gossypol inhibition of Ca++ uptake and Ca++-ATPase in human ejaculated spermatozoal plasma membrane vesicles. Contraception 1989;39(4):431-445. View abstract.
  • Keller, P. A., Birch, C., Leach, S. P., Tyssen, D., and Griffith, R. Novel pharmacophore-based methods reveal gossypol as a reverse transcriptase inhibitor. J.Mol.Graph.Model. 2003;21(5):365-373. View abstract.
  • Khomasuridze, A. G. and Marshaniia, Z. S. [Male contraception]. Akush.Ginekol.(Mosk) 1991;(1):64-65. View abstract.
  • Kim, I. C., Waller, D. P., Marcelle, G. B., Cordell, G. A., Fong, H. H., Pirkle, W. H., Pilla, L., and Matlin, S. A. Comparative in vitro spermicidal effects of (+/-)-gossypol, (+)-gossypol, (-)-gossypol and gossypolone. Contraception 1984;30(3):253-259. View abstract.
  • Kim, S. H., Kim, J. H., Alfieri, A. A., He, S. Q., and Young, C. W. Gossypol, a hyperthermic sensitizer of HeLa cells. Cancer Res. 1985;45(12 Pt 1):6338-6340. View abstract.
  • Kjaergaard, N. [Male contraception]. Ugeskr.Laeger 9-8-1986;148(37):2335-2338. View abstract.
  • Konac, E., Ekmekci, A., Yurtcu, E., and Ergun, M. A. An in vitro study of cytotoxic effects of gossypol on human epidermoid larynx carcinoma cell line (HEp-2). Exp.Oncol. 2005;27(1):81-83. View abstract.
  • Kono, H., Lin, Y. C., Yamaguchi, M., Zuspan, F. P., Furuhashi, N., Takayama, K., and Yajima, A. Effects of progesterone and gossypol on monoamine oxidase activity in human term placental explant. Tohoku J.Exp.Med. 1991;163(1):39-45. View abstract.
  • 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. View abstract.
  • Krassnigg, F., Niederhauser, H., Placzek, R., Frick, J., and Schill, W. B. Investigations on the functional role of angiotensin converting enzyme (ACE) in human seminal plasma. Adv.Exp.Med Biol. 1986;198 Pt A:477-485. View abstract.
  • Kulkarni, A. P. and Sajan, M. P. A novel mechanism of glutathione conjugate formation by lipoxygenase: a study with ethacrynic acid. Toxicol.Appl.Pharmacol. 1997;143(1):179-188. View abstract.
  • Labzo, S. S., Novokhatskii, A. S., Kabirov, ShK, and Kniazeva, V. F. [Stimulation of interferon formation by natural and synthetic inducers in cultures of human tonsil cells]. Vopr.Virusol. 1980;(1):81-85. View abstract.
  • Le Blanc, M., Russo, J., Kudelka, A. P., and Smith, J. A. An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines. Pharmacol.Res. 2002;46(6):551-555. View abstract.
  • Lei, H. P. Future research priorities of gossypol in the field of fertility regulation. Proc.Chin Acad.Med.Sci.Peking.Union Med.Coll. 1987;2(2):90-92. View abstract.
  • Levinsky, H., Singer, R., Sagiv, M., Lehrer, N., and Allalouf, D. Inhibition of sialyl transferase activity by gossypol acetic acid in human seminal plasma. Andrologia 1991;23(2):159-161. View abstract.
  • Liang, J. C. and Ye, W. S. Clastogenicity of a male contraceptive, gossypol, in mammalian cell cultures with and without the metabolic activation by S9 mix. Environ.Res. 1985;36(1):138-143. View abstract.
  • Ligueros, M., Jeoung, D., Tang, B., Hochhauser, D., Reidenberg, M. M., and Sonenberg, M. Gossypol inhibition of mitosis, cyclin D1 and Rb protein in human mammary cancer cells and cyclin-D1 transfected human fibrosarcoma cells. Br.J.Cancer 1997;76(1):21-28. View abstract.
  • Lin, T. S., Schinazi, R., Griffith, B. P., August, E. M., Eriksson, B. F., Zheng, D. K., Huang, L. A., and Prusoff, W. H. Selective inhibition of human immunodeficiency virus type 1 replication by the (-) but not the (+) enantiomer of gossypol. Antimicrob.Agents Chemother. 1989;33(12):2149-2151. View abstract.
  • Liu, G. Z. and Lyle, K. C. Clinical trial of gossypol as a male contraceptive drug. Part II. Hypokalemia study. Fertil.Steril. 1987;48(3):462-465. View abstract.
  • Liu, G. Z. Clinical study of gossypol as a male contraceptive. Reproduccion. 1981;5(3):189-193. View abstract.
  • Liu, G. Z., Ch'iu-Hinton, K., Cao, J. A., Zhu, C. X., and Li, B. Y. Effects of K salt or a potassium blocker on gossypol-related hypokalemia. Contraception 1988;37(2):111-117. View abstract.
  • Liu, G. Z., Lyle, K. C., and Cao, J. Clinical trial of gossypol as a male contraceptive drug. Part I. Efficacy study. Fertil.Steril. 1987;48(3):459-461. View abstract.
  • Liu, G. Z., Lyle, K. C., and Cao, J. Experiences with gossypol as a male pill. Am.J.Obstet.Gynecol. 1987;157(4 Pt 2):1079-1081. View abstract.
  • Liu, S., Kulp, S. K., Sugimoto, Y., Jiang, J., Chang, H. L., Dowd, M. K., Wan, P., and Lin, Y. C. The (-)-enantiomer of gossypol possesses higher anticancer potency than racemic gossypol in human breast cancer. Anticancer Res. 2002;22(1A):33-38. View abstract.
  • Liu, Y. Endometrium implantation and ectopic pregnancy. Sci China C.Life Sci 2004;47(4):293-302. View abstract.
  • Lopez, L. M., Grimes, D. A., and Schulz, K. F. Nonhormonal drugs for contraception in men: a systematic review. Obstet.Gynecol.Surv. 2005;60(11):746-752. View abstract.
  • Luukkainen, T. [Health benefits of contraception]. Duodecim 1992;108(23-24):2083-2087. View abstract.
  • Massfelder, T., Stewart, A. F., Endlich, K., Soifer, N., Judes, C., and Helwig, J. J. Parathyroid hormone-related protein detection and interaction with NO and cyclic AMP in the renovascular system. Kidney Int 1996;50(5):1591-1603. View abstract.
  • Matsuo, M. Preference of female students for "tempe" preparations composed of glandless cottonseed and defatted soybean or corn at various ratios. J Nutr Sci Vitaminol.(Tokyo) 2000;46(4):210-213. View abstract.
  • Meade, V. Contraceptive development lags in U.S. Am.Pharm. 1990;NS30(5):22-23. View abstract.
  • Mego, M. Telomerase inhibitors in anticancer therapy: gossypol as a potential telomerase inhibitor. Bratisl.Lek.Listy 2002;103(10):378-381. View abstract.
  • Meng, G. D., Zhu, J. C., Chen, Z. W., Wong, L. T., Zhang, G. Y., Hu, Y. Z., Ding, J. H., Wang, X. H., Qian, S. Z., Wang, C., and . Follow-up of men in the recovery period immediately after the cessation of gossypol treatment. Contraception 1988;37(2):119-128. View abstract.
  • Meng, G. D., Zhu, J. C., Chen, Z. W., Wong, L. T., Zhang, G. Y., Hu, Y. Z., Ding, J. H., Wang, X. H., Qian, S. Z., Wang, C., and . Recovery of sperm production following the cessation of gossypol treatment: a two-centre study in China. Int.J.Androl 1988;11(1):1-11. View abstract.
  • Moh, P. P., Li, P. K., Darby, M. V., Brueggemeier, R. W., and Lin, Y. C. Characteristics of covalent gossypol binding to microsomal proteins. Res.Commun.Chem.Pathol.Pharmacol. 1992;76(3):305-322. View abstract.
  • Mohammad, R. M., Wang, S., Banerjee, S., Wu, X., Chen, J., and Sarkar, F. H. Nonpeptidic small-molecule inhibitor of Bcl-2 and Bcl-XL, (-)-Gossypol, enhances biological effect of genistein against BxPC-3 human pancreatic cancer cell line. Pancreas 2005;31(4):317-324. View abstract.
  • Montero, M., Garcia-Sancho, J., and Alvarez, J. Comparative effects of cytochrome P-450 inhibitors on Ca2+ and Mn2+ entry induced by agonists or by emptying the Ca2+ stores of human neutrophils. Biochim.Biophys.Acta 6-6-1993;1177(2):127-133. View abstract.
  • Morris, I. D., Higgins, C., and Matlin, S. A. Inhibition of testicular LDH-X from laboratory animals and man by gossypol and its isomers. J.Reprod.Fertil. 1986;77(2):607-612. View abstract.
  • Mushtaq, M., Kulp, S., Chang, W., and Lin, Y. C. Gossypol inhibits human chorionic gonadotropin-stimulated testosterone production by cultured canine testicular interstitial cells. Res.Commun.Mol.Pathol.Pharmacol. 1996;91(3):259-272. View abstract.
  • Nakamura, M., Ikeda, M., Komukai, M., Suyemitsu, T., Okinaga, S., and Arai, K. Presence of a 16 kd protein in human seminal plasma counteracts the effects of the anti-fertility agent, gossypol. Hum.Reprod. 1991;6(5):714-721. View abstract.
  • Nordenskjold, M. and Lambert, B. Gossypol induces DNA strand breaks in human fibroblasts and sister chromatid exchanges in human lymphocytes in vitro. J.Med.Genet. 1984;21(2):129-132. View abstract.
  • Oliver, C. L., Bauer, J. A., Wolter, K. G., Ubell, M. L., Narayan, A., O'Connell, K. M., Fisher, S. G., Wang, S., Wu, X., Ji, M., Carey, T. E., and Bradford, C. R. In vitro effects of the BH3 mimetic, (-)-gossypol, on head and neck squamous cell carcinoma cells. Clin.Cancer Res. 11-15-2004;10(22):7757-7763. View abstract.
  • Oliver, C. L., Miranda, M. B., Shangary, S., Land, S., Wang, S., and Johnson, D. E. (-)-Gossypol acts directly on the mitochondria to overcome Bcl-2- and Bcl-X(L)-mediated apoptosis resistance. Mol.Cancer Ther 2005;4(1):23-31. View abstract.
  • Orhan, G., Ekmekci, A., and Menevse, S. The effect of the male contraceptive agent gossypol acetic acid on mouse bone marrow cells in vivo: micronuclei and mitotic index. Contraception 1993;47(4):377-385. View abstract.
  • Parodi, P. W. Cows' milk fat components as potential anticarcinogenic agents. J Nutr 1997;127(6):1055-1060. View abstract.
  • Pathak, V. N., Chaturvedi, R. K., Sharma, S., Jain, M., and Joshi, K. C. Non-steroidal antifertility agents. Pharmazie 1993;48(5):323-339. View abstract.
  • Patton, C. S., Legendre, A. M., Gompf, R. E., and Walker, M. A. Heart failure caused by gossypol poisoning in two dogs. J.Am.Vet.Med.Assoc. 9-15-1985;187(6):625-627. View abstract.
  • Pei-Gen, X. and Nai-Gong, W. Can ethnopharmacology contribute to the development of anti-fertility drugs? J Ethnopharmacol. 1991;32(1-3):167-177. View abstract.
  • Penningroth, S. M. Pharmacological basis of therapeutics: gossypol, an oral male contraceptive? J.Med.Soc.N.J. 1984;81(8):663-665. View abstract.
  • Placzek, R., Krassnigg, F., and Schill, W. B. Effect of ace-inhibitors, calmodulin antagonists, acetylcholine receptor blocking, and alpha receptor blocking agents on motility of human sperm. Arch.Androl 1988;21(1):1-10. View abstract.
  • Porat, O. Effects of gossypol on the motility of mammalian sperm. Mol.Reprod.Dev. 1990;25(4):400-408. View abstract.
  • Poso, H., Wichmann, K., Janne, J., and Luukkainen, T. Gossypol, a powerful inhibitor of human spermatozoal metabolism. Lancet 4-19-1980;1(8173):885-886. View abstract.
  • Prasad, M. R. and Diczfalusy, E. New contraceptives for men. What are the prospects? Int J Androl 1983;6(4):305-309. View abstract.
  • Prusoff, W., Lin, T. S., Pivazyan, A., Sun, A. S., and Birks, E. Empirical and rational approaches for development of inhibitors of the human immunodeficiency virus--HIV-1. Pharmacol.Ther 1993;60(2):315-329. View abstract.
  • Qian, S. Z. and Wang, Z. G. Gossypol: a potential antifertility agent for males. Annu.Rev.Pharmacol.Toxicol. 1984;24:329-360. View abstract.
  • Fu, Y. F., Zhang, S. L., Lu, Z. M., and Wang, W. Effects of gossypol on the activity of kidney (Na+ + K+)-ATPase and the functions of erythrocyte membrane. Contraception 1988;37(2):179-184. View abstract.
  • Fu, Y. F., Zhang, S. L., Lu, Z. M., and Wang, W. Effects of gossypol on the activity of rabbit kidney Na,K-ATPase and the functions of human erythrocyte membrane. Prog.Clin.Biol.Res. 1988;268B:385-392. View abstract.
  • Gao, H., Yang, Z. S., and Jin, S. X. [Primary observations on distal renal tubule acidosis in 177 cases caused by gossypol intoxication]. Zhonghua Nei Ke.Za Zhi. 1985;24(7):419-21, 447. View abstract.
  • Glander, H. J. [Gossypol and other nonhormonal substances for the inhibition of male fertility]. Zentralbl.Gynakol. 1988;110(12):772-777. View abstract.
  • Goldsmith, K. C. and Hogarty, M. D. Targeting programmed cell death pathways with experimental therapeutics: opportunities in high-risk neuroblastoma. Cancer Lett. 10-18-2005;228(1-2):133-141. View abstract.
  • Gombe, S. A review of the current status in male contraceptive studies. East Afr.Med J 1983;60(4):203-211. View abstract.
  • Gottlieb, C. and Aanesen, A. [A male contraceptive injection can be available within 5 years]. Lakartidningen 9-22-1999;96(38):4039-4044. View abstract.
  • Greydanus, D. E. and Lonchamp, D. Contraception in the adolescent. Preparation for the 1990s. Med Clin.North Am. 1990;74(5):1205-1224. View abstract.
  • Grimes, D. A., Lopez, L. M., Gallo, M. F., Halpern, V., Nanda, K., and Schulz, K. F. Steroid hormones for contraception in men. Cochrane Database Syst Rev 2007;(2):CD004316. View abstract.
  • Grimes, D., Gallo, M., Grigorieva, V., Nanda, K., and Schulz, K. Steroid hormones for contraception in men. Cochrane Database Syst Rev 2004;(3):CD004316. View abstract.
  • Gu, Z. P., Mao, B. Y., Wang, Y. X., Zhang, R. A., Tan, Y. Z., Chen, Z. X., Cao, L., You, G. D., and Segal, S. J. Low dose gossypol for male contraception. Asian J.Androl 2000;2(4):283-287. View abstract.
  • Gu, Z. P., Wang, Y. X., Sang, G. W., Wang, W. C., Chen, Z. X., Zhao, X. J., Shao, Q. X., and Jiang, Y. Relationship between hormone profiles and the restoration of spermatogenesis in men treated with gossypol. Int.J.Androl 1990;13(4):253-257. View abstract.
  • Gui-Yuan, Z., Meng-Chun, J., Jin-Lai, C., and Wen-Qing, Y. The effect of long-term treatment with crude cotton seed oil on pituitary and testicular function in men. Int J Androl 1989;12(6):404-410. View abstract.
  • Han, H. L. [Gossypol treatment for menopausal functional bleeding, myoma of uterus and endometriosis--preliminary report (author's transl)]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1980;2(3):167-170. View abstract.
  • Han, M. L. [Clinical observation of the gossypol treatment of endometriosis and uterine myoma and the location of the pharmacological action]. Zhong.Xi.Yi.Jie.He.Za Zhi. 1982;2(3):159-161. View abstract.
  • Han, M. L., Wang, Y. F., Tang, M. Y., Ge, Q. S., Zhou, L. F., Zhu, P. D., and Sun, Y. T. Gossypol in the treatment of endometriosis and uterine myoma. Contrib.Gynecol.Obstet. 1987;16:268-270. View abstract.
  • Haspel, H. C., Corin, R. E., and Sonenberg, M. Effect of gossypol on erythrocyte membrane function: specific inhibition of inorganic anion exchange and interaction with band 3. J.Pharmacol.Exp.Ther. 1985;234(3):575-583. View abstract.
  • Heiser, V., Scherzinger, E., Boeddrich, A., Nordhoff, E., Lurz, R., Schugardt, N., Lehrach, H., and Wanker, E. E. Inhibition of huntingtin fibrillogenesis by specific antibodies and small molecules: implications for Huntington's disease therapy. Proc.Natl.Acad.Sci U.S.A 6-6-2000;97(12):6739-6744. View abstract.
  • Hoffer, A. P., Agarwal, A., Meltzer, P., Herlihy, P., Naqvi, R. H., Lindberg, M. C., and Matlin, S. A. Ultrastructural, fertility, and spermicidal studies with isomers and derivatives of gossypol in male hamsters. Biol.Reprod. 1987;37(4):909-924. View abstract.
  • Hong, C. Y. [Application of a trans-membrane migration method in the study of human sperm motility: a review]. Zhonghua Yi.Xue.Za Zhi.(Taipei) 1991;48(3):163-170. View abstract.
  • Hong, C. Y., Huang, J. J., and Wu, P. The inhibitory effect of gossypol on human sperm motility: relationship with time, temperature and concentration. Hum.Toxicol. 1989;8(1):49-51. View abstract.
  • Duo, X., Cai, W. J., Zhu, B. H., Dong, C. J., Zheng, Z. C., and Gao, Z. Q. Clinical safety of long-term administration of gossypol in 32 cases. Contraception 1988;37(2):129-135. View abstract.
  • Eliasson, R. and Virji, N. Effects of gossypol acetic acid on the activity of LDH-C4 from human and rabbit spermatozoa. Int.J.Androl 1983;6(1):109-112. View abstract.
  • Ergun, M. A., Konac, E., Erbas, D., and Ekmekci, A. Apoptosis and nitric oxide release induced by thalidomide, gossypol and dexamethasone in cultured human chronic myelogenous leukemic K-562 cells. Cell Biol.Int. 2004;28(3):237-242. View abstract.
  • Fan, L. P., Ren, C. Q., and Hou, T. X. [Emergency treatment and care of hypokalemia paralysis due to gossypol poisoning]. Zhonghua Hu Li Za Zhi. 9-5-1995;30(9):522-525. View abstract.
  • 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. View abstract.
  • Flack, M. R., Pyle, R. G., Mullen, N. M., Lorenzo, B., Wu, Y. W., Knazek, R. A., Nisula, B. C., and Reidenberg, M. M. Oral gossypol in the treatment of metastatic adrenal cancer. J.Clin.Endocrinol.Metab 1993;76(4):1019-1024. View abstract.
  • Forstermann, U. Properties and mechanisms of production and action of endothelium-derived relaxing factor. J Cardiovasc.Pharmacol. 1986;8 Suppl 10:S45-S51. View abstract.
  • Forstermann, U., Alheid, U., Frolich, J. C., and Mulsch, A. Mechanisms of action of lipoxygenase and cytochrome P-450-mono-oxygenase inhibitors in blocking endothelium-dependent vasodilatation. Br.J Pharmacol. 1988;93(3):569-578. View abstract.
  • Forstermann, U., Mugge, A., Alheid, U., Bode, S. M., and Frolich, J. C. Endothelium-derived relaxing factor (EDRF): a defence mechanism against platelet aggregation and vasospasm in human coronary arteries. Eur.Heart J 1989;10 Suppl F:36-43. View abstract.
  • Forstermann, U., Mugge, A., Bode, S. M., and Frolich, J. C. Response of human coronary arteries to aggregating platelets: importance of endothelium-derived relaxing factor and prostanoids. Circ.Res. 1988;63(2):306-312. View abstract.
  • Forstermann, U., Warmuth, G., Dudel, C., and Alheid, U. Formation and functional importance of endothelium-derived relaxing factor (EDRF) and prostaglandins in the microcirculation. Z.Kardiol. 1989;78 Suppl 6:85-91. View abstract.
  • Franco-Cereceda, A. and Rudehill, A. Capsaicin-induced vasodilatation of human coronary arteries in vitro is mediated by calcitonin gene-related peptide rather than substance P or neurokinin A. Acta Physiol Scand. 1989;136(4):575-580. View abstract.
  • Frick, J. and Aulitzky, W. Male contraception. Hum.Reprod. 1988;3(2):147-151. View abstract.
  • Frick, J., Aulitzky, W., and Kalla, N. R. Clinical microdose study of gossypol: effect on sperm motility and renal function. Contraception 1988;37(2):153-162. View abstract.
  • Demery, A. [Male contraception]. Soins.Gynecol.Obstet.Pueric.Pediatr. 1987;(72):33-38. View abstract.
  • Demoulin, A. [Male contraception]. Rev Med Liege 4-1-1984;39(7):266-272. View abstract.
  • Diczfalusy, E. [Contraception in the eighties: a theme with variations]. Lakartidningen 1-16-1980;77(3):98-105. View abstract.
  • Dodou, K., Anderson, R. J., Small, D. A., and Groundwater, P. W. Investigations on gossypol: past and present developments. Expert.Opin.Investig.Drugs 2005;14(11):1419-1434. View abstract.
  • Dogliotti, L., Berruti, A., Pia, A., Paccotti, P., Ali, A., and Angeli, A. Cytotoxic chemotherapy for adrenocortical carcinoma. Minerva Endocrinol. 1995;20(1):105-109. View abstract.
  • Drayer, D. E. and Reidenberg, M. M. Gossypol and Na+, K+ ATPase from human erythrocytes. Contraception 1988;38(5):579-583. View abstract.
  • Drife, J. O. The effects of drugs on sperm. Drugs 1987;33(6):610-622. View abstract.
  • Cao, J. and Liu, G. Z. [Reversibility of azoospermia following gossypol withdrawal]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1983;5(4):227-230. View abstract.
  • Cao, J., Fei, R., Zhao, Y., Chen, H., Jin, W., and Chen, S. [Effect of low dose gossypol treatment on male sperm nuclear basic protein]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 2000;22(3):220-222. View abstract.
  • Chang, J. S., Hsu, Y. L., Kuo, P. L., Chiang, L. C., and Lin, C. C. Upregulation of Fas/Fas ligand-mediated apoptosis by gossypol in an immortalized human alveolar lung cancer cell line. Clin.Exp.Pharmacol.Physiol 2004;31(10):716-722. View abstract.
  • Chang, M. C., Gu, Z., and Saksena, S. K. Effects of Gossypol on the fertility of male rats, hamsters and rabbits. Contraception 1980;21(5):461-469. View abstract.
  • Chen, X. M., Li, H. Y., and Xue, S. P. [Effects of gossypol on lactate dehydrogenase isoenzyme-X in human spermatozoa]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1983;5(4):223-226. View abstract.
  • Chen, Y., Sten, M., Nordenskjold, M., Lambert, B., Matlin, S. A., and Zhou, R. H. The effect of gossypol on the frequency of DNA-strand breaks in human leukocytes in vitro. Mutat.Res. 1986;164(1):71-78. View abstract.
  • Cheng, J. S., Liu, C. P., Lo, Y. K., Chou, K. J., Lin, M. C., Su, W., Law, Y. P., Chou, K. J., Wang, J. L., Chen, W. C., and Jan, C. R. Gossypol, a component in cottonseed, induced increases in cytosolic Ca2+ levels in Chang liver cells. Toxicon 2002;40(7):851-856. View abstract.
  • Cheng, J. S., Lo, Y. K., Yeh, J. H., Cheng, H. H., Liu, C. P., Chen, W. C., and Jan, C. R. Effect of gossypol on intracellular Ca2+ regulation in human hepatoma cells. Chin J.Physiol 9-30-2003;46(3):117-122. View abstract.
  • Cheng, K. F., Wu, W. Y., Tang, M. Y., and Chu, P. T. Endometrial changes after administration of gossypol for menorrhagia. Am.J.Obstet.Gynecol. 12-15-1980;138(8):1227-1229. View abstract.
  • Chongthammakun, S., Ekavipat, C., Sanitwongse, B., and Pavasuthipaisit, K. Effects of gossypol on human and monkey sperm motility in vitro. Contraception 1986;34(3):323-331. View abstract.
  • Clarke, C. A. Medicine in China. Ceylon Med J 1979;24(3-4):51-54. View abstract.
  • Comhaire, F. H. Male contraception: hormonal, mechanical and other. Hum.Reprod. 1994;9(4):586-590. View abstract.
  • Coutinho, E. M. and Melo, J. F. Clinical experience with gossypol in non-Chinese men: a follow-up. Contraception 1988;37(2):137-151. View abstract.
  • Coutinho, E. M. Latin America's contributions to contraceptive development. Fertil.Steril. 1993;60(2):227-230. View abstract.
  • Coutinho, E. M., Melo, J. F., Barbosa, I., and Segal, S. J. Antispermatogenic action of gossypol in men. Fertil.Steril. 1984;42(3):424-430. View abstract.
  • Cowart, C. L., London, S. N., Vernon, M. W., and Pedigo, N. G. The effects of cyclic adenosine monophosphate, forskolin, and theophylline on motility parameters in gossypol-treated human sperm. Fertil.Steril. 1994;61(5):929-934. View abstract.
  • Dando, C., Schroeder, E. R., Hunsaker, L. A., Deck, L. M., Royer, R. E., Zhou, X., Parmley, S. F., and Vander Jagt, D. L. The kinetic properties and sensitivities to inhibitors of lactate dehydrogenases (LDH1 and LDH2) from Toxoplasma gondii: comparisons with pLDH from Plasmodium falciparum. Mol.Biochem.Parasitol. 2001;118(1):23-32. View abstract.
  • Dao, V. T., Dowd, M. K., Gaspard, C., Martin, M. T., Hemez, J., Laprevote, O., Mayer, M., and Michelot, R. J. New thioderivatives of gossypol and gossypolone, as prodrugs of cytotoxic agents. Bioorg.Med.Chem. 5-1-2003;11(9):2001-2006. View abstract.
  • Dao, V. T., Dowd, M. K., Martin, M. T., Gaspard, C., Mayer, M., and Michelot, R. J. Cytotoxicity of enantiomers of gossypol Schiff's bases and optical stability of gossypolone. Eur.J Med Chem. 2004;39(7):619-624. View abstract.
  • Dao, V. T., Gaspard, C., Mayer, M., Werner, G. H., Nguyen, S. N., and Michelot, R. J. Synthesis and cytotoxicity of gossypol related compounds. Eur.J.Med.Chem. 2000;35(9):805-813. View abstract.
  • Datta, K. and Kulkarni, A. P. Co-oxidation of all-trans retinol acetate by human term placental lipoxygenase and soybean lipoxygenase. Reprod.Toxicol. 1996;10(2):105-112. View abstract.
  • Datta, K. and Kulkarni, A. P. Oxidative metabolism of aflatoxin B1 by lipoxygenase purified from human term placenta and intrauterine conceptal tissues. Teratology 1994;50(4):311-317. View abstract.
  • Datta, K., Sherblom, P. M., and Kulkarni, A. P. Co-oxidative metabolism of 4-aminobiphenyl by lipoxygenase from soybean and human term placenta. Drug Metab Dispos. 1997;25(2):196-205. View abstract.
  • de Peyster, A., Quintanilha, A., Packer, L., and Smith, M. T. Oxygen radical formation induced by gossypol in rat liver microsomes and human sperm. Biochem.Biophys.Res.Commun. 1-30-1984;118(2):573-579. View abstract.
  • DeBonis, S., Skoufias, D. A., Lebeau, L., Lopez, R., Robin, G., Margolis, R. L., Wade, R. H., and Kozielski, F. In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities. Mol.Cancer Ther 2004;3(9):1079-1090. View abstract.
  • Deck, L. M., Chamblee, B. B., Royer, R. E., Hunsaker, L. A., and Vander Jagt, D. L. Inhibition of aldose reductase by gossypol and gossypol-related compounds. Adv.Exp.Med.Biol. 1999;463:487-492. View abstract.
  • Deck, L. M., Vander Jagt, D. L., and Royer, R. E. Gossypol and derivatives: a new class of aldose reductase inhibitors. J.Med.Chem. 1991;34(11):3301-3305. View abstract.
  • Aitken, J. Future developments in contraception. Practitioner 1988;232(1441):46-52. View abstract.
  • Aitken, R. J. New techniques in contraception: gossypol, vaccines and GnRH analogues. Proc.Annu.Symp.Eugen.Soc. 1983;19:1-18. View abstract.
  • Aitken, R. J., Liu, J., Best, F. S., and Richardson, D. W. An analysis of the direct effects of gossypol on human spermatozoa. Int.J.Androl 1983;6(2):157-167. View abstract.
  • Badawy, S. Z., Souid, A. K., Cuenca, V., Montalto, N., and Shue, F. Gossypol inhibits proliferation of endometrioma cells in culture. Asian J Androl 2007;9(3):388-393. View abstract.
  • Balci, A., Sahin, F. I., and Ekmekci, A. Gossypol induced apoptosis in the human promyelocytic leukemia cell line HL 60. Tohoku J.Exp.Med. 1999;189(1):51-57. View abstract.
  • Band, V., Hoffer, A. P., Band, H., Rhinehardt, A. E., Knapp, R. C., Matlin, S. A., and Anderson, D. J. Antiproliferative effect of gossypol and its optical isomers on human reproductive cancer cell lines. Gynecol.Oncol. 1989;32(3):273-277. View abstract.
  • Bauer, J. A., Trask, D. K., Kumar, B., Los, G., Castro, J., Lee, J. S., Chen, J., Wang, S., Bradford, C. R., and Carey, T. E. Reversal of cisplatin resistance with a BH3 mimetic, (-)-gossypol, in head and neck cancer cells: role of wild-type p53 and Bcl-xL. Mol.Cancer Ther 2005;4(7):1096-1104. View abstract.
  • Baumgrass, R., Weiwad, M., Erdmann, F., Liu, J. O., Wunderlich, D., Grabley, S., and Fischer, G. Reversible inhibition of calcineurin by the polyphenolic aldehyde gossypol. J.Biol.Chem. 12-21-2001;276(51):47914-47921. View abstract.
  • Becattini, B., Kitada, S., Leone, M., Monosov, E., Chandler, S., Zhai, D., Kipps, T. J., Reed, J. C., and Pellecchia, M. Rational design and real time, in-cell detection of the proapoptotic activity of a novel compound targeting Bcl-X(L). Chem.Biol. 2004;11(3):389-395. View abstract.
  • Benditt, J. M. Current contraceptive research. Fam.Plann.Perspect. 1980;12(3):149-155. View abstract.
  • Benhaim, P., Mathes, S. J., Hunt, T. K., Scheuenstuhl, H., and Benz, C. C. Induction of neutrophil Mac-1 integrin expression and superoxide production by the medicinal plant extract gossypol. Inflammation 1994;18(5):443-458. View abstract.
  • Benz, C. C., Keniry, M. A., Ford, J. M., Townsend, A. J., Cox, F. W., Palayoor, S., Matlin, S. A., Hait, W. N., and Cowan, K. H. Biochemical correlates of the antitumor and antimitochondrial properties of gossypol enantiomers. Mol.Pharmacol. 1990;37(6):840-847. View abstract.
  • Benz, C., Hollander, C., Keniry, M., James, T. L., and Mitchell, M. Lactic dehydrogenase isozymes, 31P magnetic resonance spectroscopy, and in vitro antimitochondrial tumor toxicity with gossypol and rhodamine-123. J.Clin.Invest 1987;79(2):517-523. View abstract.
  • Benz, C., Keniry, M., and Goldberg, H. Selective toxicity of gossypol against epithelial tumors and its detection by magnetic resonance spectroscopy. Contraception 1988;37(3):221-228. View abstract.
  • Best, R. G. and McKenzie, W. H. Variable sister-chromatid exchange response in human lymphocytes exposed in vitro to gossypol acetic acid. Mutat.Res. 1988;206(2):227-233. View abstract.
  • Bi, X. F., Ye, Y. X., Yang, H. F., and Zhang, Z. R. [Preliminary study on gossypol in causing hypokalemia (author's transl)]. Zhongguo Yi.Xue.Ke.Xue.Yuan Xue.Bao. 1981;3(3):175-178. View abstract.
  • Bi, X. F., Zheng, Y. J., Yang, H. F., and Zhang, Z. R. The effect of gossypol on ATPase activity of the kidney. Sci.Sin. 1981;24(4):573-580. View abstract.
  • Blackstaffe, L., Shelley, M. D., and Fish, R. G. Cytotoxicity of gossypol enantiomers and its quinone metabolite gossypolone in melanoma cell lines. Melanoma Res. 1997;7(5):364-372. View abstract.
  • Burgos, C., Gerez de Burgos, N. M., Rovai, L. E., and Blanco, A. In vitro inhibition by gossypol of oxidoreductases from human tissues. Biochem.Pharmacol. 3-1-1986;35(5):801-804. View abstract.
  • Bushunow, P., Reidenberg, M. M., Wasenko, J., Winfield, J., Lorenzo, B., Lemke, S., Himpler, B., Corona, R., and Coyle, T. Gossypol treatment of recurrent adult malignant gliomas. J.Neurooncol. 1999;43(1):79-86. View abstract.
  • Cameron, S. M., Waller, D. P., and Zaneveld, L. J. Vaginal spermicidal activity of gossypol in the Macaca arctoides. Fertil.Steril. 1982;37(2):273-274. View abstract.
  • Adekunle, A. O., Arowojolu, A. O., Adejuwon, C. A., Okpara, N. C., and Ladipo, O. A. Seminal plasma zinc level in users of gossypol. Afr.J.Med.Med.Sci. 1999;28(1-2):1-4. View abstract.
  • Adlakha, R. C., Ashorn, C. L., Chan, D., and Zwelling, L. A. Modulation of 4'-(9-acridinylamino)methanesulfon-m-anisidide-induced, topoisomerase II-mediated DNA cleavage by gossypol. Cancer Res. 4-15-1989;49(8):2052-2058. View abstract.
  • Taylor GT, Griffin MG, Bardgett M. Search for a male contraceptive: the effect of gossypol on sexual motivation and epididymal sperm. J Med 1991;22:29-44. View abstract.
  • Teng CS. Reversible changes in the content of cellular and microtubular tubulin in spermatogenic cells after gossypol treatment. Contraception 1997;55:183-8. View abstract.
  • Wu D. An overview of the clinical pharmacology and therapeutic potential of gossypol as a male contraceptive agent and in gynaecological disease. Drugs 1989;38:333-41. View abstract.

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