The effects of (+)-Gossypol on 11β-HSD and the concentration of corticosterone and dehydrocorticosterone in mice serum and tissues

11β-hydroxysteroid dehydrogenase (11β-HSD) plays an important part in mediating glucocorticoid action, catalyzing the interconversion of corticosterone (B) and dehydrocorticosterone (A) in rodents. The aim of our study is to investigate the effects of (+)-gossypol (G+) on 11β-HSD. Adult ICR mice were given B and B + (G+) by intraperitoneal injection. The activity of 11β-HSD was evaluated by measuring the ratio of A and B, meanwhile the effects of (+)-gossypol on the conversion rate of B to A was determined with HPLC. Serum A/B levels of the B+(G+) group decreased by 2.42, 7.32, 17.85, 31.39, and 40.02 % compared to the B group at each measured time interval. A/B levels at 1 h for the B + (G+) group decreased by 43.78, 21.29 and 34.47% in liver, kidney and adrenal glands, respectively, in comparison to the B group. However, (+)-gossypol had no effect on brain and testis. (+)-Gossypol was an inhibitor of 11β-HSD.Colegio de Farmacéuticos de la Provincia de Buenos Aire