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Anti-HIV-1 activity and cellular pharmacology of various analogs of gossypol

Tai‐Shun LinComprehensive Cancer Center, Yale University School of Medicine, New Haven, CT 06510 U.S.ARaymond F. SchinaziDepartment of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322 U.S.AJuliang ZhuComprehensive Cancer Center, Yale University School of Medicine, New Haven, CT 06510 U.S.AEvelyn M. BirksDepartment of Pharmacology, Yale University School of Medicine, New Haven, CT 06510 U.S.ARocco CarboneComprehensive Cancer Center, Yale University School of Medicine, New Haven, CT 06510 U.S.ASi YikangInstitute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, ChinaWu KemeiInstitute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, ChinaHuang LiangInstitute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, ChinaWilliam H. PrusoffDepartment of Pharmacology, Yale University School of Medicine, New Haven, CT 06510 U.S.A

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Annotatsiya

We previously reported that the racemic mixture and both enantiomers of gossypol inhibit the replication of human immunodeficiency virus-type 1 (HIV-1) (Lin et al., Antimicrob Agents Chemother 33: 2149-2151, 1989). The present study evaluates the activities of a variety of analogs of gossypol as well as a few non-gossypol analogs. Compounds 2, 3, 10, and 13 were slightly more inhibitory than (-)-gossypol to the replication of HIV-1 in cell culture. Compounds 4 and 8 were cytotoxic to human peripheral blood monocyte (PBM) cells, and compounds 2 and 3 were cytotoxic to Vero cells but not PBM cells. The effects of the two enantiomers of gossypol on the cell volume and migration of H9 cells through the cell cycle were evaluated during 72 hr of incubation. The (-)-enantiomer of gossypol was more toxic to H9 cells than the (+)-enantiomer of gossypol as evidenced by cell destruction. Prior to cell destruction, there appeared to be no significant effect on cell cycle distribution with either enantiomer.

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DOI: 10.1016/0006-2952(93)90411-o

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