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中华根霉对20(R)-人参二醇的生物转化

Biotransformation of 20(R)-panaxadiol by the fungus Rhizopus chinensis.

作者信息

Lin Xiong-Hao, Cao Ming-Nan, He Wen-Ni, Yu Si-Wang, Guo De-An, Ye Min

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.

出版信息

Phytochemistry. 2014 Sep;105:129-34. doi: 10.1016/j.phytochem.2014.06.001. Epub 2014 Jun 30.

Abstract

Microbial transformation of 20(R)-panaxadiol by the fungus Rhizopus chinensis CICC 3043 yielded seven metabolites. Their structures were elucidated on the basis of extensive spectroscopic analyses. R. chinensis could catalyze hydroxylation and further dehydrogenation at C-24 of 20(R)-panaxadiol, as well as hydroxylation at C-7, C-15, C-16, and C-29. Three of these compounds at 10μM could moderately inhibit growth of HepG2 human hepatocellular carcinoma cells with an inhibition rate of about 40%. Three compounds (also at 10μM) showed approximately 30% inhibition on NF-κB transcriptional activity in SW480 human colon carcinoma cells stably transfected with NF-κB luciferase reporter and induced by LPS.

摘要

华根霉CICC 3043对20(R)-人参二醇的微生物转化产生了七种代谢产物。通过广泛的光谱分析阐明了它们的结构。华根霉可催化20(R)-人参二醇C-24位的羟基化和进一步脱氢反应,以及C-7、C-15、C-16和C-29位的羟基化反应。其中三种化合物在10μM时可适度抑制HepG2人肝癌细胞的生长,抑制率约为40%。三种化合物(同样在10μM时)对稳定转染了NF-κB荧光素酶报告基因并由LPS诱导的SW480人结肠癌细胞中的NF-κB转录活性显示出约30%的抑制作用。

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