Inhibitory effect and interaction of stanozolol with pig testicular cytochrome P-450 (17 alpha-hydroxylase/C17,20-lyase). 1989

S Nakajin, and K Takahashi, and M Shinoda

The inhibitory effect of an anabolic steroid, stanozolol, on testicular microsomal cytochrome P-450 (17 alpha-hydroxylase/C17,20-lyase) (P-450(17 alpha/lyase] and the nature of the interaction were compared with those of other anabolic steroids, furazabol and mestanolone. Stanozolol markedly inhibited delta 16-C19-steroid synthesizing activity, 17 alpha-hydroxylase and C17,20-lyase activities, which were mediated by oxygenase activities of testicular microsomal cytochrome P-450(17 alpha/lyase). In addition, stanozolol was a competitive inhibitor of 17 alpha-hydroxylase (Ki = 6.31 microM) and C17,20-lyase (Ki = 1.30 microM) activities in the reconstituted enzyme system. The interaction of cytochrome P-450&17 alpha/lyase) with stanozolol induced a type I difference spectrum (peak at 387 nm and trough at 418 nm) with a dissociation constant (Ks) of 1.47 microM.

UI MeSH Term Description Entries
D008297 Male Males
D008861 Microsomes Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed) Microsome
D003577 Cytochrome P-450 Enzyme System A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism. Cytochrome P-450,Cytochrome P-450 Enzyme,Cytochrome P-450-Dependent Monooxygenase,P-450 Enzyme,P450 Enzyme,CYP450 Family,CYP450 Superfamily,Cytochrome P-450 Enzymes,Cytochrome P-450 Families,Cytochrome P-450 Monooxygenase,Cytochrome P-450 Oxygenase,Cytochrome P-450 Superfamily,Cytochrome P450,Cytochrome P450 Superfamily,Cytochrome p450 Families,P-450 Enzymes,P450 Enzymes,Cytochrome P 450,Cytochrome P 450 Dependent Monooxygenase,Cytochrome P 450 Enzyme,Cytochrome P 450 Enzyme System,Cytochrome P 450 Enzymes,Cytochrome P 450 Families,Cytochrome P 450 Monooxygenase,Cytochrome P 450 Oxygenase,Cytochrome P 450 Superfamily,Enzyme, Cytochrome P-450,Enzyme, P-450,Enzyme, P450,Enzymes, Cytochrome P-450,Enzymes, P-450,Enzymes, P450,Monooxygenase, Cytochrome P-450,Monooxygenase, Cytochrome P-450-Dependent,P 450 Enzyme,P 450 Enzymes,P-450 Enzyme, Cytochrome,P-450 Enzymes, Cytochrome,Superfamily, CYP450,Superfamily, Cytochrome P-450,Superfamily, Cytochrome P450
D000732 Androstanols Androstanes and androstane derivatives which are substituted in any position with one or more hydroxyl groups. Hydroxyandrostanes
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013196 Dihydrotestosterone A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. 5 alpha-Dihydrotestosterone,Androstanolone,Stanolone,17 beta-Hydroxy-5 beta-Androstan-3-One,17beta-Hydroxy-5alpha-Androstan-3-One,5 beta-Dihydrotestosterone,5-alpha Dihydrotestosterone,5-alpha-DHT,Anaprotin,Andractim,Dihydroepitestosterone,Gelovit,17 beta Hydroxy 5 beta Androstan 3 One,17beta Hydroxy 5alpha Androstan 3 One,5 alpha DHT,5 alpha Dihydrotestosterone,5 beta Dihydrotestosterone,Dihydrotestosterone, 5-alpha,beta-Hydroxy-5 beta-Androstan-3-One, 17
D013197 Stanozolol A synthetic steroid that has anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1194) Androstanazol,Methylstanazol,Stanazolol,Stromba,Winstrol
D013552 Swine Any of various animals that constitute the family Suidae and comprise stout-bodied, short-legged omnivorous mammals with thick skin, usually covered with coarse bristles, a rather long mobile snout, and small tail. Included are the genera Babyrousa, Phacochoerus (wart hogs), and Sus, the latter containing the domestic pig (see SUS SCROFA). Phacochoerus,Pigs,Suidae,Warthogs,Wart Hogs,Hog, Wart,Hogs, Wart,Wart Hog
D013737 Testis The male gonad containing two functional parts: the SEMINIFEROUS TUBULES for the production and transport of male germ cells (SPERMATOGENESIS) and the interstitial compartment containing LEYDIG CELLS that produce ANDROGENS. Testicles,Testes,Testicle
D065607 Cytochrome P-450 Enzyme Inhibitors Drugs and compounds which inhibit or antagonize the biosynthesis or actions of CYTOCHROME P-450 ENZYMES. Cytochrome P-450 Inhibitors,Cytochrome P-450 Monooxygenase Inhibitors,Cytochrome P-450 Oxygenase Inhibitors,Cytochrome P-450-Dependent Monooxygenase Inhibitors,P-450 Enzyme Inhibitors,P450 Enzyme Inhibitors,Cytochrome P 450 Dependent Monooxygenase Inhibitors,Cytochrome P 450 Enzyme Inhibitors,Cytochrome P 450 Inhibitors,Cytochrome P 450 Monooxygenase Inhibitors,Cytochrome P 450 Oxygenase Inhibitors,Enzyme Inhibitors, P-450,Enzyme Inhibitors, P450,Inhibitors, Cytochrome P-450,Inhibitors, P-450 Enzyme,Inhibitors, P450 Enzyme,P 450 Enzyme Inhibitors,P-450 Inhibitors, Cytochrome

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