通过微生物氧化制备螺内酯的代谢产物。

Preparation of metabolites of spironolactone by microbial oxygenation.

作者信息

Marsheck W J, Karim A

出版信息

Appl Microbiol. 1973 Apr;25(4):647-9. doi: 10.1128/am.25.4.647-649.1973.

DOI:10.1128/am.25.4.647-649.1973

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC380879/

Abstract

It has been postulated that 3-(3-oxo-7alpha-methylthio-4-androsten-17alpha-yl)propionic acid gamma-lactone (I) is a key intermediate in the metabolism of the anti-aldosterone agent, spironolactone (3-[3-oxo-7alpha-acetylthio-17beta-hydroxy-4-androsten-17alpha-yl] propionic acid gamma-lactone). In the present study it was found that microbial oxygenation of I by Chaetomium cochloides QM 624 gave three metabolites which retained sulfur in their molecules and were found to be identical to the human metabolites of spironolactone.

摘要

据推测，3-(3-氧代-7α-甲硫基-4-雄甾烯-17α-基)丙酸γ-内酯（I）是抗醛固酮剂螺内酯（3-[3-氧代-7α-乙酰硫基-17β-羟基-4-雄甾烯-17α-基]丙酸γ-内酯）代谢过程中的关键中间体。在本研究中发现，球毛壳菌QM 624对I进行微生物氧化产生了三种分子中保留硫的代谢产物，并且发现它们与螺内酯的人体代谢产物相同。

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引用本文的文献

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Pharmacokinetics of spironolactone in man.螺内酯在人体中的药代动力学。

Naunyn Schmiedebergs Arch Pharmacol. 1976 Dec;296(1):37-45. doi: 10.1007/BF00498838.

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Effect of entekohepatic circulation on the pharmacokinetics of spironolactone in man.肝肠循环对螺内酯在人体内药代动力学的影响。

Naunyn Schmiedebergs Arch Pharmacol. 1977 Nov;300(3):281-7. doi: 10.1007/BF00500971.

本文引用的文献

1

Isolation and identification of novel sulfur-containing metabolites of spironolactone (Aldactone).螺内酯（安体舒通）新型含硫代谢物的分离与鉴定。

Steroids. 1972 Jul;20(1):41-62. doi: 10.1016/0039-128x(72)90117-1.

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