Inactivation of human immunodeficiency virus in vitro by gossypol.

Gossypol, a polyphenolic aldehyde extracted from cottonseed, is a male anti-fertility agent which has been reported to have anti-viral activity. In this paper we report that gossypol inactivates human immunodeficiency virus (HIV) in an in vitro system. Following exposure of cell-free incubates of HIV to 100 uM gossypol, ultracentrifugation and inoculation of the washed pellet onto H9 cells, there is no evidence of elevated reverse transcriptase activity over 21 days. Treatment with lower concentrations of gossypol reduces the peak and lengthens the time to maximal reverse transcriptase activity compared with control cultures. These observations suggest that gossypol could be used as a vaginal spermicidal/virucidal agent. The mechanism of the in vitro anti-viral action as well as the effect of orally administered gossypol on the infectivity of semen of HIV-seropositive men warrant further study.