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利用大茎点霉进行去氢表雄酮的生物转化及转化产物的β-葡萄糖醛酸苷酶抑制活性。

Biotransformation of dehydroepiandrosterone with Macrophomina phaseolina and β-glucuronidase inhibitory activity of transformed products.

机构信息

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.

出版信息

J Enzyme Inhib Med Chem. 2012 Jun;27(3):348-55. doi: 10.3109/14756366.2011.590804. Epub 2011 Jul 21.

DOI:10.3109/14756366.2011.590804
PMID:21774747
Abstract

The biotransformation of dehydroepiandrosterone (1) with Macrophomina phaseolina was investigated. A total of eight metabolites were obtained which were characterized as androstane-3,17-dione (2), androst-4-ene-3,17-dione (3), androst-4-ene-17β-ol-3-one (4), androst-4,6-diene-17β-ol-3-one (5), androst-5-ene-3β,17β-diol (6), androst-4-ene-3β-ol-6,17-dione (7), androst-4-ene-3β,7β,17β-triol (8), and androst-5-ene-3β,7α,17β-triol (9). All the transformed products were screened for enzyme inhibition, among which four were found to inhibit the β-glucuronidase enzyme, while none inhibited the α-chymotrypsin enzyme.

摘要

用木霉(Macrophomina phaseolina)对脱氢表雄甾酮(1)进行了生物转化研究。共得到 8 种代谢产物,分别鉴定为雄烷-3,17-二酮(2)、雄甾-4-烯-3,17-二酮(3)、雄甾-4-烯-17β-醇-3-酮(4)、雄甾-4,6-二烯-17β-醇-3-酮(5)、雄甾-5-烯-3β,17β-二醇(6)、雄甾-4-烯-3β-醇-6,17-二酮(7)、雄甾-4-烯-3β,7β,17β-三醇(8)和雄甾-5-烯-3β,7α,17β-三醇(9)。所有转化产物均进行了酶抑制筛选,其中 4 种对β-葡萄糖醛酸酶有抑制作用,而对α-糜蛋白酶无抑制作用。

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