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本文研究了20α-羟基孕酮对土拨鼠肾上腺微粒体P-450催化甾体羟基化的抑制作用。探明了17α-羟基孕酮作底物时,20α-羟基孕酮对P-450_(C_(21))催化的C_(21)羟基化反应及P-450_(17αlyase)催化的C_(17)—C_(20)键断裂的反应均表现出拮抗抑制。抑制常数分别为1.73μmol/L(P-450_(C_(21)))和1.37μmol/L(P-450_(17lyase))。比较了分别以孕酮和17α-羟基孕酮作底物时,20α-羟基孕酮对P-450_(17αlyase)催化C_(17)—C_(20)键断裂的不同影响,由此推论出雄甾烷二酮在肾上腺微粒体中生成的连续反应机理。
In this paper, the inhibitory effect of 20α-hydroxyprogesterone on the hydroxylation of steroidal anti-P-450 adrenal microspheres was studied. The results showed that the effect of 20α-hydroxyprogesterone on C_ (21) hydroxylation catalyzed by P-450_ (C_ (21)) and C_ (17) The reaction of the cleavage of the C_ (20) bond showed antagonistic inhibition. The inhibitory constants were 1.73μmol / L (P-450_ (C_ (21)) and 1.37μmol / L (P-450_ (17lyase)), respectively. The different effects of 20α-hydroxyprogesterone on the cleavage of C_ (17) -C_ (20) bond catalyzed by P-450_ (17αlyase) were compared respectively with progesterone and 17α-hydroxyprogesterone as substrates. Continuous mechanism of formation of steroidal dione in adrenal microsomes.