Naganuma H, Sasano N, Ojima M
Nihon Naibunpi Gakkai Zasshi. 1986 Mar 20;62(3):149-57. doi: 10.1507/endocrine1927.62.3_149.
The effects of canrenone K (Soldactone) on 3 beta-hydroxysteroid dehydrogenase, 11 beta-hydroxylase and 18-hydroxylase activities were determined in vitro using isolated mitochondrial and microsomal fractions of the bovine adrenal glands. There was dose-related inhibition of 3 beta-hydroxysteroid dehydrogenation in the concentration between 10(-8) M and 10(-3) M, and 11 beta-hydroxylation and 18-hydroxylation in the concentration between 10(-7) M and 10(-3) M, respectively. The concentration of 50% inhibition of 3 beta-hydroxysteroid dehydrogenase activity was 8.5 X 10(-7) M and those of 11 beta-hydroxylase and 18-hydroxylase activities were 5 X 10(-5) M and 6 X 10(-6) M, respectively. NADPH added to a mitochondrial fraction or NAD to a microsomal fraction had no effect on the inhibition of conversion in the presence of canrenone K. The results indicate that canrenone K inhibited 3 beta-hydroxysteroid dehydrogenase in the pharmacological dose, 11 beta-hydroxylase and 18-hydroxylase in a higher concentration, and with the exception of NADPH or NAD, it may inhibit the generating system directly.
使用牛肾上腺分离的线粒体和微粒体部分,在体外测定了坎利酮K(索体舒通)对3β-羟类固醇脱氢酶、11β-羟化酶和18-羟化酶活性的影响。在10^(-8)M至10^(-3)M的浓度范围内,3β-羟类固醇脱氢反应存在剂量相关抑制,在10^(-7)M至10^(-3)M的浓度范围内,11β-羟化反应和18-羟化反应分别存在剂量相关抑制。3β-羟类固醇脱氢酶活性50%抑制浓度为8.5×10^(-7)M,11β-羟化酶和18-羟化酶活性的50%抑制浓度分别为5×10^(-5)M和6×10^(-6)M。添加到线粒体部分的NADPH或添加到微粒体部分的NAD对坎利酮K存在时的转化抑制无影响。结果表明,坎利酮K在药理剂量下抑制3β-羟类固醇脱氢酶,在较高浓度下抑制11β-羟化酶和18-羟化酶,且除NADPH或NAD外,它可能直接抑制生成系统。