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题名: Comparison of Inhibition Capability of Scutellarein and Scutellarin Towards Important Liver UDP-Glucuronosyltransferase (UGT) Isoforms
作者: Ma, Guang-You1;  Cao, Yun-Feng2, 3;  Hu, Cui-Min1, 2, 3;  Fang, Zhong-Ze1, 2, 3, 4;  Sun, Xiao-Yu2, 3;  Hong, Mo2, 3;  Zhu, Zhi-Tu1
关键词: enzyme inhibition ;  UDP-glucuronosyltransferase (UGT) ;  scutellarin ;  scutellarein
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2014-03-01
DOI: 10.1002/ptr.4990
卷: 28, 期:3, 页:382-386
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Scutellarin is an important bioactive flavonoid extracted from Erigeron breviscapus (Vant.) Hand-Mazz, and scutellarein is the corresponding aglycone of scutellarin. The present study aims to compare the inhibition potential of scutellarin and scutellarein towards several important UDP-glucuronosyltransferase (UGT) isoforms, including UGT1A1, UGT1A6, UGT1A9 and UGT2B7. It was demonstrated that scutellarein exerted stronger inhibition towards the tested UGT isoforms than scutellarin. Furthermore, the inhibition kinetic type and parameters (K-i) were determined for the scutellarein's inhibition towards these UGT isoforms. Competitive inhibition of scutellarein towards all these UGT isoforms was demonstrated, and the K-i values were calculated to be 0.02, 5.0, 5.8 and 35.9 mu M for UGT1A1, 1A6, 1A9 and 2B7, respectively. Using in vivo maximum plasma concentration of scutellarein in rat, the in vitro-in vivo extrapolation was performed to predict in vivo situation, indicating the most possible in vivo adverse effects due to the inhibition of scutellarein towards UGT1A1. All these results remind us to monitor the utilization of scutellarin and scutellarein, and the herbs containing these two components. Copyright (c) 2013 John Wiley & Sons, Ltd.
关键词[WOS]: HERB-DRUG INTERACTIONS ;  IDENTIFICATION ;  METABOLISM ;  BIOACTIVATION ;  1A3
语种: 英语
WOS记录号: WOS:000332988100006
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/145445
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou 121001, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian 116023, Peoples R China
3.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China
4.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA

Recommended Citation:
Ma, Guang-You,Cao, Yun-Feng,Hu, Cui-Min,et al. Comparison of Inhibition Capability of Scutellarein and Scutellarin Towards Important Liver UDP-Glucuronosyltransferase (UGT) Isoforms[J]. PHYTOTHERAPY RESEARCH,2014,28(3):382-386.
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