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学科主题: 药学
题名:
Biotransformation of columbianadin by rat hepatic microsomes and inhibition of biotransformation products on NO production in RAW 264.7 cells in vitro
作者: Zhang, You-Bo; Li, Wei; Yang, Xiu-Wei
关键词: Angelica pubescens f. biserrata ; Umbelliferae ; Biotransformation ; Columbianadin ; Columbianadiratimetins A-H ; Nitric oxide
刊名: PHYTOCHEMISTRY
发表日期: 2012-09-01
DOI: 10.1016/j.phytochem.2012.06.015
卷: 81, 页:109-116
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Plant Sciences
研究领域[WOS]: Biochemistry & Molecular Biology ; Plant Sciences
关键词[WOS]: MECHANISM-BASED INACTIVATION ; HUMAN LIVER ; UMBELLIFEROUS PLANTS ; CYTOCHROME-P450 2A6 ; PEUCEDANUM-PALUSTRE ; COUMARIN ; METABOLISM ; CARBOXYLESTERASES ; CONSTITUENTS ; MYRISLIGNAN
英文摘要:

Columbianadin (CBN, 1), 1-[(8S)-8,9-dihydro-2-oxo-2H-furo[2,3-h]-1-benzopyran-8-yl]-1-methylethyl-[(2Z)-2-methyl-2-butenoic acid jester is a coumarin-type compound and one of the main bioactive constituents of the underground part of Angelica pubescens Maxim. f. biserrata Shan et Yuan. Although numerous investigations have been undertaken to study the biological activities of CBN, such as analgesic, anti-inflammatory, calcium-channel blocking, and platelet aggregation inhibiting functions, little attention has been paid to its metabolism and/or biotransformation. Biotransformation of CBN by rat liver microsomes in vitro was studied, and thirteen biotransformation products including eight hitherto unknown compounds [columbianadiratimetins A-H (3-10)] and five known compounds [columbianadin oxide (2), (+)-2,3-dihydro-4-hydroxy-2-(1-hydroxy-1-methylethyl)-5-benzofurancarboxaldehyde (11), oroselol (12), columbianetin (13), and vaginol (14)] were produced by liver microsomes from rats pre-treated with sodium phenobarbital. The structures of these compounds were elucidated on the basis of extensive spectroscopic analyses which included IR, UV, EIMS, HRESIMS, 1D NMR and 2D NMR, respectively. The inhibition of CBN and its main biotransformation products on nitric oxide production induced by lipopolysaccharide was assayed in RAW 264.7 cells at concentrations ranging from 10 to 200 mu M to evaluate the biological significance of biotransformation. (C) 2012 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 2011BAI07B08 ; 30672609 ; 2009ZX09301-010 ; Z0004105040311
项目资助者: National Key Technology R&amp ; D Program of China ; National Natural Science Foundation of China ; "Major New Medicine Project" in Mega-projects of Science Research of China ; Beijing Municipal Special-purpose Science Foundation of China
WOS记录号: WOS:000308121000012
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内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67206
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Dept Nat Med,State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Zhang, You-Bo,Li, Wei,Yang, Xiu-Wei. Biotransformation of columbianadin by rat hepatic microsomes and inhibition of biotransformation products on NO production in RAW 264.7 cells in vitro[J]. PHYTOCHEMISTRY,2012,81:109-116.
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