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Journal of Asian Natural Products Research Volume 14, 2012 - Issue 10
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Original Articles

Biotransformation products of phellopterin by rat liver microsomes and the inhibition on NO production in LPS-activated RAW264.7 cells

Ai-Hong Zhao State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing, 100191, China
,
Xin-Bao Yang Beijing University of Chinese Medicine, Beijing, 100029, China; Research Center, Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing, 100091, China
,
Xiu-Wei Yang State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing, 100191, ChinaCorrespondence[email protected]
,
You-Bo Zhang State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing, 100191, China
,
Wei Xu State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing, 100191, China
&
Jian-Xun Liu Beijing University of Chinese Medicine, Beijing, 100029, China; Research Center, Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing, 100091, ChinaCorrespondence[email protected]
Pages 956-965 | Received 06 Jul 2012, Accepted 10 Sep 2012, Published online: 10 Oct 2012
 
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Abstract

Four new coumarins (2′,3′-dihydroxyphellopterin, E-5-methoxytrichoclin acetate, Z-5-methoxytrichoclin acetate, and E-5-methoxytrichoclin) and three known coumarins (byakangelicol, byakangelicin, and Z-5-methoxytrichoclin) were produced by liver microsomes from rats pre-treated with sodium phenobarbital. The chemical structures were elucidated on the basis of their spectroscopic data. The inhibitory activities of nitric oxide (NO) production in lipopolysaccharide-activated macrophage-like cell line RAW264.7 were tested. The main biotransformation product, byakangelicin, showed inhibitory activities of NO production with the IC50 value of 217.83 μM, whereas the parent compound phellopterin showed cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM.

Acknowledgment

This research was partly supported by the National Key Technology R&D Program of China (2012BAI29B02, 2011BAI07B08, 2006BAI 06A01-02).

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