IR@PKUHSC  > 北京大学药学院
学科主题药学
Acitretin exhibits inhibitory effects towards UDP-glucuronosyltransferase (UGT)1A9-mediated 4-methylumbelliferone (4-MU) and propofol glucuronidation reaction
Yu, Ming-Lian1; Yang, Yue2; Wang, Cong-Min3; Zhang, Meng-Meng4; Bai, Miao-Chun5; Guo, Yue-Ling1
刊名PHARMAZIE
2013-06-01
DOI10.1691/ph.2013.2816
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
引用统计
被引频次:10[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/66141
专题北京大学药学院
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
推荐引用方式
GB/T 7714
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.
APA Yu, Ming-Lian,Yang, Yue,Wang, Cong-Min,Zhang, Meng-Meng,Bai, Miao-Chun,&Guo, Yue-Ling.(2013).Acitretin exhibits inhibitory effects towards UDP-glucuronosyltransferase (UGT)1A9-mediated 4-methylumbelliferone (4-MU) and propofol glucuronidation reaction.PHARMAZIE,68(6),449-452.
MLA Yu, Ming-Lian,et al."Acitretin exhibits inhibitory effects towards UDP-glucuronosyltransferase (UGT)1A9-mediated 4-methylumbelliferone (4-MU) and propofol glucuronidation reaction".PHARMAZIE 68.6(2013):449-452.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Yu, Ming-Lian]的文章
[Yang, Yue]的文章
[Wang, Cong-Min]的文章
百度学术
百度学术中相似的文章
[Yu, Ming-Lian]的文章
[Yang, Yue]的文章
[Wang, Cong-Min]的文章
必应学术
必应学术中相似的文章
[Yu, Ming-Lian]的文章
[Yang, Yue]的文章
[Wang, Cong-Min]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。