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作 者:黄德盈 Shiro Kominami Shigeki Takemori
机构地区:[1]Department of Chemistry, South Central Institute for National Minorities, Wuhan 430074, PRC [2]Faculty of Integrated Arts and Sciences, Hiroshima University
出 处:《Science China Chemistry》1993年第4期411-419,共9页中国科学(化学英文版)
摘 要:Using guinea pig andrenal microsomes, we studied the inhibitory effects of 20α-hydroxyprogesterone on steroid hydroxylation reactions catalyzed by cytochromes P-450. When 17α-hydroxyprogesterone was used as a substrate, 20α-hydroxyprogesterone functioned as a competitive inhibitor on the C_(17)—C_(20) bond cleavage reaction of P-450_(17α lyase). The inhibition constant, K_i was 1.37 μmol/L. 20α-hydroxyprogesterone also competitively inhibited the convertion of 17α-bydroxyprogesterone to 11-deoxycortisol by the action of P-450_(c21). The value of K_i was 1.73μmol/L. When progesterone was used as a substrate, 20α-hydroxyprogesterone inhibited neither the 21-hydroxylation of P-450_(c21). the C_(17)—C_(20) bond cleavage, nor 17α-hydroxylation of P-450_(17α lyase). Based on the seresults, we can deduce that the production of androstenedione from progesterone by the action of P-450_(17α lyase) proceeds through a successive monooxygenase reaction.Using guinea pig andrenal microsomes, we studied the inhibitory effects of 20α-hydroxyprogesterone on steroid hydroxylation reactions catalyzed by cytochromes P-450. When 17α-hydroxyprogesterone was used as a substrate, 20α-hydroxyprogesterone functioned as a competitive inhibitor on the C<sub>17</sub>—C<sub>20</sub> bond cleavage reaction of P-450<sub>17α lyase</sub>. The inhibition constant, K<sub>i</sub> was 1.37 μmol/L. 20α-hydroxyprogesterone also competitively inhibited the convertion of 17α-bydroxyprogesterone to 11-deoxycortisol by the action of P-450<sub>c21</sub>. The value of K<sub>i</sub> was 1.73μmol/L. When progesterone was used as a substrate, 20α-hydroxyprogesterone inhibited neither the 21-hydroxylation of P-450<sub>c21</sub>. the C<sub>17</sub>—C<sub>20</sub> bond cleavage, nor 17α-hydroxylation of P-450<sub>17α lyase</sub>. Based on the seresults, we can deduce that the production of androstenedione from progesterone by the action of P-450<sub>17α lyase</sub> proceeds through a successive monooxygenase reaction.
关 键 词:cytochrome P-450_(c21) cytochrome P-450_(17α lyase ) 20α-hydroxyprogesterone adrenal microsome steroidogenesis.
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