Inhibitory Effect and Interaction of Stanozolol with Pig Testicular Cytochrome P-450 (17α-Hydroxylase/C_<17,20>-Lyase)

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The inhibitory effect of an anabolic steroid, stanozolol, on testicular microsomal cytochrome P-450 (17α-hydroxylase/C_<17,20>-lyase)(P-450_<17α/lyase>) and the nature of the interaction were compared with those of other anabolic steroids, furazabol and mestanolone. Stanozolol markedly inhibited Δ^<16>-C_<19>-steroid synthesizing activity, 17α-hydroxylase and C_<17,20>-lyase activities, which were mediated by oxygenase activities of testicular microsomal cytochrome P-450_<17α/lyase>. In addition, stanozolol was a competitive inhibitor of 17α-hydroxylase (K_i=6.31 μM) and C_<17,20>-lyase (K_i=1.30 μM) activities in the reconstituted enzyme system.The interaction of cytochrome P-450_<17α/lyase> with stanozolol induced a type I difference spectrum (peak at 387 nm and trough at 418 nm) with a dissociation constant (K_s) of 1.47 μM.
公益社団法人日本薬学会の論文
1989-07-25