Pharmacol Res. 2002 Dec; 46(6): 551-5.

An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines.

Le Blanc M, Russo J, Kudelka AP, Smith JA.

University of Houston College of Pharmacy, Houston, TX, USA.

Gossypol, a cottonseed extract, has been shown to have antiproliferative activity in a variety of cancer cell lines. The objective of this study was to determine the inhibitory effects of gossypol on cell proliferation. Five human carcinoma cell lines were evaluated including endometrial (RL95-2), ovarian (SKOV-3), medullary thyroid (TT), and adrenocortical (NCI-H295R and SW-13). Gossypol and the metabolite, apogossypol hexaacetate, were examined at concentrations up to 500 microg ml(-1) and the IC(50) was determined using the MTT assay. Gossypol and apogossypol hexaacetate produced a dose-dependent growth inhibition in all cellular lines examined. The IC(50) for gossypol ranged from 1.3 to 18.9 microM while the IC(50) for apogossypol hexaacetate ranged from 5.2 to 9.0 microM. The results indicate that gossypol possesses antiproliferative action toward human carcinoma cells in vitro. These investigations suggest that gossypol may have therapeutic potential for the treatment of cancer.