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Summary. Concentrations of (+) and (−) gossypol were measured by high performance liquid chromatography after they were incubated with plasma proteins in vitro. The concentration of (−) gossypol decreased more than the concentration of (+) gossypol. A similar decrease in free gossypol concentrations in the blood plasma of rats was observed after intravenous infusion of gossypol enantiomers. The concentration of (−) gossypol was also found to be lower than the concentration of (+) gossypol at the blood–testis barrier. The biological effect of (−) gossypol probably results from its stereospecific binding to extra- and intracellular proteins in vivo and inhibition of the biological activity of some proteins.
Keywords: gossypol enantiomers; HPLC; protein binding; blood–testis barrier; rat
