北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学药学院  > 期刊论文
学科主题: 药学
题名:
Acitretin exhibits inhibitory effects towards UDP-glucuronosyltransferase (UGT)1A9-mediated 4-methylumbelliferone (4-MU) and propofol glucuronidation reaction
作者: Yu, Ming-Lian1; Yang, Yue2; Wang, Cong-Min3; Zhang, Meng-Meng4; Bai, Miao-Chun5; Guo, Yue-Ling1
刊名: PHARMAZIE
发表日期: 2013-06-01
DOI: 10.1691/ph.2013.2816
卷: 68, 期:6, 页:449-452
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: DRUG GLUCURONIDATION ; PHARMACOKINETICS ; UGT ; METABOLITE ; ACID
英文摘要:

The present study aimed to evaluate the potential risk of drug-drug interactions associated with acitretin which is a drug for therapy of psoriasis approved by the Food and Drug Administration (FDA). The initial screening of acitretin′s inhibition towards 4-methylumbelliferone (4-MU) glucuronidation catalyzed by important UDP-glucuronosyltransferase (UGT) isoforms in the liver showed that UGT1A9 activity was strongly inhibited by acitretin with other UGT isoforms negligibly influenced. The inhibition type is best fit to competitive inhibition, and the inhibition kinetic parameter (KO was determined to be 3.5 mu M,The inhibition behaviour of acitretin towards UGT1A9 activity did not exhibit probe substrate-dependent behaviour when selecting human liver microsomes (HLMs)-catalyzed propofol-O-glucuronidation as probe reaction of UGT1A9. The same inhibition type and similar inhibition parameters (K-i=3.21 mu M) were obtained. Using the maximum plasma exposure dose of acitretin (C-max), the C-max/K-i values were calculated to be 0.23 and 0.25 when selecting 4-MU and propofol as probe substrates, respectively. All these results indicate a potential clinical drug-drug interaction between acitretin and 4-MU or propofol.

语种: 英语
WOS记录号: WOS:000334260200012
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66141
Appears in Collections:北京大学药学院_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: 1.Mil Gen Hosp Beijing PLA, Dept Pharm, Beijing, Peoples R China
2.Mil Gen Hosp Beijing PLA, Outpatient Serv Unit, Beijing, Peoples R China
3.Shenyang Pharmaceut Univ, Fac Business Adm, Shenyang 110016, Peoples R China
4.Mil Gen Hosp Beijing PLA Beijing, Dept Dermatol, Beijing, Peoples R China
5.Peking Univ, Sch Pharm, Dept Pharm Adm & Clin Pharm, Beijing 100871, Peoples R China

Recommended Citation:
Yu, Ming-Lian,Yang, Yue,Wang, Cong-Min,et al. Acitretin exhibits inhibitory effects towards UDP-glucuronosyltransferase (UGT)1A9-mediated 4-methylumbelliferone (4-MU) and propofol glucuronidation reaction[J]. PHARMAZIE,2013,68(6):449-452.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Yu, Ming-Lian]'s Articles
[Yang, Yue]'s Articles
[Wang, Cong-Min]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Yu, Ming-Lian]‘s Articles
[Yang, Yue]‘s Articles
[Wang, Cong-Min]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace