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使用[1,2-³H]底物研究人胎盘对15α和16α羟基化雄激素的芳香化作用。

Aromatization of 15 alpha and 16 alpha hydroxylated androgens in the human placental using [1,2-3H]-substrates.

作者信息

Cantineau R, Kremers P, De Graeve J, Gielen J E, Lambotte R

出版信息

J Steroid Biochem. 1982 Feb;16(2):157-63. doi: 10.1016/0022-4731(82)90162-5.

Abstract

This in vitro study reports data on the aromatization of [1,2-3H]-C19 steroids in the human term placenta [androstenedione (III), testosterone (IV), 15 alpha-hydroxy-androstenedione (V), 15 alpha-hydroxy-testosterone (VI), 16 alpha-hydroxy-androstenedione (VII)]. The hydroxylated androgens were microbiologically synthesized from commercially radiolabelled [1,2-3H]-androstenedione and testosterone. Androstenedione and testosterone were good substrates for the human placental aromatase (low Km values, high Vmax); they strongly inhibited the 15 and 16 hydroxylated androgens aromatizations. On the other hand, these hydroxylated compounds acted as poor substrates and were only non-competitive inhibitors of the androstenedione and testosterone aromatizations. However, 15 alpha-hydroxy-androstenedione could not be disregarded as a potential precursor of 15 alpha-hydroxylated estrogens in the human placenta.

摘要

这项体外研究报告了人足月胎盘(雄烯二酮(III)、睾酮(IV)、15α-羟基雄烯二酮(V)、15α-羟基睾酮(VI)、16α-羟基雄烯二酮(VII))中[1,2-³H]-C19类固醇芳构化的数据。羟基化雄激素由市售放射性标记的[1,2-³H]-雄烯二酮和睾酮经微生物合成。雄烯二酮和睾酮是人胎盘芳香化酶的良好底物(低Km值,高Vmax);它们强烈抑制15和16羟基化雄激素的芳构化。另一方面,这些羟基化化合物是较差的底物,并且只是雄烯二酮和睾酮芳构化的非竞争性抑制剂。然而,15α-羟基雄烯二酮不能被忽视作为人胎盘中15α-羟基化雌激素的潜在前体。

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