Skip to main content
Log in

A preliminary clinical study of gossypol in advanced human cancer

  • Short Communication
  • Gossypol, Advanced Human Cancer
  • Published:
Cancer Chemotherapy and Pharmacology Aims and scope Submit manuscript

Summary

A total of 34 patients with advanced cancer were given weekly or daily escalating doses of oral gossypol, a cottonseed-oil constituent showing evidence of antineoplastic activity in pre-clinical studies. No major adverse events occurred and there was no evidence of haematological or biochemical disturbance. As determined by dose escalation in 17 patients, the dose-limiting toxicity was emessis in 16 patients. There was no evidence of tumour regression in any of the 20 patients assessed for response. We conclude that gossypol is safe but unlikely to be clinically useful in patients with advanced cancer.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

References

  1. Abou-Donia MB, Dieckert JW (1974) Gossypol: uncoupling of respiratory chain and oxidative phosphorylation. Life Sci 14: 1955

    Google Scholar 

  2. Adlakha RC, Aschorn CL, Chan D, Zwelling LA (1989) Modulation of 4′-(9-acridinylamino)methanesulfon-m-anisidide-induced, topoisomerase II-mediated DNA cleavage by gossypol. Cancer Res 49: 2052

    Google Scholar 

  3. Band V, Hoffer AP, Band H, Rhinehardt AE, Knapp RC, Matlin SA, Anderson DJ (1989) Antiproliferative effect of gossypol and its optical isomers on human reproductive cancer cell lines. Gynecol Oncol 32: 273

    Google Scholar 

  4. Benz C, Keniry M, Goldberg H (1988) Selective toxicity of gossypol against epithelial tumors and its detection by magnetic resonance spectroscopy. Contraception 37: 221

    Google Scholar 

  5. Flack MR, Wu YW, Reidenburg MA, Pyle RG, Mullens NM, Nisula BC, Loriaux DL (1990) Treatment of adrenocortical carcinoma with gossypol. Proc Am Assoc Cancer Res 31: 198

    Google Scholar 

  6. Haspel H, Ren YF, Watanabe KA, Sonenberg M, Corin RE (1984) Cytocidal effect of gossypol on cultured murine erythroleukemia cells is prevented by serum protein. J Pharmacol Exp Ther 229: 218

    Google Scholar 

  7. Joseph AEA, Matlin SA, Knox P (1986) Cytotoxicity of enantiomers of gossypol. Br J Cancer 54: 511

    Google Scholar 

  8. Keniry MA, Hollander C, Benz CC (1989) The effect of gossypol and 6-aminonicotinamide on tumor cell metabolism: a31P-magnetic resonance spectroscopic study. Biochem Biophys Res Commun 164: 947

    Google Scholar 

  9. Lee CYG, Moon YS, Yuan JH, Chen AF (1982) Enzyme inactivation and inhibition by gossypol. Mol Cell Biochem 47: 65

    Google Scholar 

  10. Matlin SA, Belenguer A, Vince PA, Stein RC (1990) Analysis of gossypol enantiomers in human serum. J Liquid Chromatogr 13: 2261

    Google Scholar 

  11. Miller AB, Hoogstraten B, Straquet M, Winkler A (1981) Reporting results of cancer treatment. Cancer 47: 207

    Google Scholar 

  12. Rao PN, Wang YC, Lotzova E, Khan AA, Rao SP, Stephens LC (1985) Antitumor effects of gossypol on murine tumors. Cancer Chemother Pharmacol 15: 20

    Google Scholar 

  13. Rosenberg LJ, Adlakha RC, Desai DM, Rao PN (1986) Inhibition of DNA polymerase alpha by gossypol. Biochim Biophys Acta 866: 258

    Google Scholar 

  14. Tso WW (1984) Gossypol inhibits Ehrlich ascites tumor cell proliferation. Cancer Lett 24: 257

    Google Scholar 

  15. Tso WW, Lee CS (1982) Gossypol uncoupling of respiratory chain and oxidative phosphorylation in ejaculated boar spermatozoa. Contraception 25: 649

    Google Scholar 

  16. Tuszynski GP, Cossu G (1984) Differential cytotoxic effect of gossypol on human melanoma, colon carcinoma, and other tissue culture cell lines. Cancer Res 44: 768

    Google Scholar 

  17. Ueno H, Sahni MK, Segal SJ, Koide SS (1988) Interaction of gossypol with sperm macromolecules and enzymes. Contraception 37: 333

    Google Scholar 

  18. Wang YC, Rao PN (1984) Effect of gossypol on DNA synthesis and cell cycle progression of mammalian cells in vitro. Cancer Res 44: 35

    Google Scholar 

  19. Wu DF (1989) An overview of the clinical pharmacology and therapeutic potential of gossypol as a male contraceptive agent and in gynaecological disease. Drugs 38: 333

    Google Scholar 

  20. Wu DF, Yu YW, Tang ZM, Wang MZ (1986) Pharmacokinetics of (+/−), (+), (−) gossypol in humans and dogs. Clin Pharmacol Ther 39: 613

    Google Scholar 

  21. Wu DF, Reidenberg MM, Drayer DE (1988) Determination of gossypol enantiomers in plasma after administration of racemate using high-performance liquid chromatography with precolumn chemical derivatisation. J Chromatogr 433: 141

    Google Scholar 

  22. Wu YW, Chik CL, Knazek RA (1989) An in vitro and in vivo study of antitumour effects of gossypol on human SW-13 adrenocortical carcinoma. Cancer Res 49: 3754

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Stein, R.C., Joseph, A.E.A., Matlin, S.A. et al. A preliminary clinical study of gossypol in advanced human cancer. Cancer Chemother. Pharmacol. 30, 480–482 (1992). https://doi.org/10.1007/BF00685601

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00685601

Keywords

Navigation