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马体内合成代谢类固醇代谢的相关研究:去势马体内19-去甲睾酮的I期和II期生物转化

Studies related to the metabolism of anabolic steroids in the horse: the phase I and phase II biotransformation of 19-nortestosterone in the equine castrate.

作者信息

Dumasia M C, Houghton E

出版信息

Xenobiotica. 1984 Aug;14(8):647-55. doi: 10.3109/00498258409151462.

Abstract

The metabolism of 19-nor[4-14C]testosterone has been studied in the equine castrate. Following XAD-2 extraction of aliquots of the 0-24 h urine samples, the glucuronic acid and sulphate conjugates were separated by Sephadex LH-20 column chromatography. After hydrolysis of the conjugates, the neutral phase I metabolites of 19-nortestosterone were extracted, purified and identified by g.l.c.-mass spectrometry. In phase I metabolism stereospecificity was observed in the reduction of the A-ring with the formation of the 5 alpha, 3 beta-isomers of estranediol. Epimerization at C-17 and hydroxylation at C-16 were the other major pathways. In phase II metabolism the C-17 alpha steroid epimers were predominantly conjugated with glucuronic acid and the C-17 beta epimers with sulphuric acid. One animal showed a slight variation in metabolism with a tendency towards the formation of polar metabolites.

摘要

已在去势马中研究了19-去甲[4-¹⁴C]睾酮的代谢情况。对0至24小时尿液样本的等分试样进行XAD-2萃取后,通过葡聚糖凝胶LH-20柱色谱法分离葡萄糖醛酸和硫酸盐缀合物。缀合物水解后,提取、纯化19-去甲睾酮的中性I相代谢物,并通过气相色谱-质谱联用仪进行鉴定。在I相代谢中,观察到A环还原时具有立体特异性,形成了雌烷二醇的5α, 3β-异构体。C-17位的差向异构化和C-16位的羟基化是其他主要途径。在II相代谢中,C-17α甾体差向异构体主要与葡萄糖醛酸结合,C-17β差向异构体则与硫酸结合。有一只动物的代谢情况略有不同,有形成极性代谢物的倾向。

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