Species-Associated Differences in the Inhibition of Propofol Glucuronidation by Magnolol
Yang, Lu1; Zhu, Liangliang2; Ge, Guangbo4; Xiao, Ling3; Wu, Yan2; Liang, Sicheng4; Cao, Yunfeng4; Yang, Ling4; Wang, Dong1
刊名journal of the american association for laboratory animal science
2014-07-01
卷号53期号:4页码:408-411
英文摘要magnolol, a major active constituent in herbal medicine, potently inhibits propofol glucuronidation in human liver microsomes, with inhibition constants in the nanomolar range. this study was conducted to investigate magnolol-induced inhibition of propofol glucuronidation in liver microsomes from swiss-hauschka mice, sprague-dawley rats, chinese bama pigs, and cynomolgus macaques. results indicated that magnolol (10 mu m) inhibited propofol glucuronidation in liver microsomes from bama pigs and cynomolgus macaques but not in those from mice or rats. data from liver microsomes from bama pigs indicated a competitive inhibition mechanism, with a k-i of 1.7 mu m. in contrast to that of pig liver microsomes, the inhibition of microsomes from cynomolgus macaques followed a noncompetitive mechanism, with a k-i of 3.4 mu m. in summary, this study indicates that magnolol-induced inhibition of propofol glucuronidation varies substantially among species, and the k-i values determined by using liver microsomes from various experimental animal species far exceed that for human liver microsomes. the inhibition of propofol glucuronidation by magnolol in liver microsomes from all animal species tested was significantly lower than the inhibition previously demonstrated in human liver microsomes. hepatic microsomes from swiss-hauschka mice, sprague-dawley rats, chinese bama pigs, and cynomolgus macaques are not effective models of the inhibition of glucuronidation induced by magnolol in humans.
WOS标题词science & technology ; life sciences & biomedicine
类目[WOS]veterinary sciences ; zoology
研究领域[WOS]veterinary sciences ; zoology
关键词[WOS]messenger-rna expression ; udp-glucuronosyltransferases ; microsomes ; metabolism ; isoforms ; liver ; mice
收录类别SCI
语种英语
WOS记录号WOS:000339231600012
公开日期2016-05-09
内容类型期刊论文
源URL[http://cas-ir.dicp.ac.cn/handle/321008/145697]  
专题大连化学物理研究所_中国科学院大连化学物理研究所
作者单位1.Liaoning Univ Tradit Chinese Med, Sch Pharm, Dalian, Peoples R China
2.Anqing Normal Univ, Sch Life Sci, Anqing, Peoples R China
3.Anqing Normal Univ, Sch Resources & Environm, Anqing, Peoples R China
4.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian, Peoples R China
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GB/T 7714
Yang, Lu,Zhu, Liangliang,Ge, Guangbo,et al. Species-Associated Differences in the Inhibition of Propofol Glucuronidation by Magnolol[J]. journal of the american association for laboratory animal science,2014,53(4):408-411.
APA Yang, Lu.,Zhu, Liangliang.,Ge, Guangbo.,Xiao, Ling.,Wu, Yan.,...&Wang, Dong.(2014).Species-Associated Differences in the Inhibition of Propofol Glucuronidation by Magnolol.journal of the american association for laboratory animal science,53(4),408-411.
MLA Yang, Lu,et al."Species-Associated Differences in the Inhibition of Propofol Glucuronidation by Magnolol".journal of the american association for laboratory animal science 53.4(2014):408-411.
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