Inhibition potential of UDP-glucuronosyltransferases (UGTs) 1A isoforms by the analogue of resveratrol, bakuchiol

	Inhibition potential of UDP-glucuronosyltransferases (UGTs) 1A isoforms by the analogue of resveratrol, bakuchiol
	Dong, De-Gang 1; Zhang, Yao 2; Zhang, Shu-Lan 2; Lv, Jing 3; Guo, En-Mian 3; Fang, Zhong-Ze 4; Cao, Yun-Feng 4
刊名	pharmazie
	2014
卷号	69 期号:1 页码:60-63
英文摘要	bakuchiol is a promising anti-tumor candidate with resveratrol-like structure. the present study aims to evaluate the inhibition potential of bakuchiol towards udp-glucuronosyltransferases (ugt) 1a isoforms. an in vitro incubation system using 4-methylumbelliferone (4-mu) glucuronidation was used to evaluate the inhibition capability of bakuchiol towards ugt1a1, 1a3, 1a6, 1a7, 1a8, 1a9 and 1a10. the glucuronidation of trifluoperazine (tfp) was employed as the probe reaction to determine bakuchiol's inhibition towards ugt1a4. at 1 mu m and 10 mu m of bakuchiol, no or weak inhibition was observed for all the tested ugt1a isoforms. at 100 mu m of bakuchiol, the activity of ugt1a1, 1a3, 1a4, 1a6, 1a7, 1a8, 1a9 and 1a10 was inhibited by -46.2%, 74.7%, 17.8%, 98.7%, 70.4%, 99.2%, 75.8%, and 93.3%, respectively. further inhibition kinetic behaviour was determined for ugt1a6, 1a8, and 1a10. both dixon plot and lineweaver-burk plot showed the noncompetitive inhibition of bakuchiol towards all these three ugt isoforms. the inhibition kinetic parameters (k-i)were calculated to be 5.3, 1.8, and 92.6 mu m for ugt1a6, 1a8, and 1a10, respectively. in combination with the in vivo exposure of bakuchiol, the high possibility of in vivo inhibition of ugt1a6 and 1a8 was predicted. however, relatively low possibility of in vivo inhibition towards ugt1a10 was predicted due to lower in vivo concentration of bakuchiol than its inhibition parameter (k-i). all these information will be helpful for the r&d of bakuchiol as a promising anti-tumor drug.
WOS标题词	science & technology ; life sciences & biomedicine ; physical sciences
类目[WOS]	chemistry, medicinal ; chemistry, multidisciplinary ; pharmacology & pharmacy
研究领域[WOS]	pharmacology & pharmacy ; chemistry
关键词[WOS]	psoralea-corylifolia ; in-vitro ; glucuronidation ; identification ; metabolism ; acid
收录类别	SCI
语种	英语
WOS记录号	WOS:000334259500012
公开日期	2016-05-09
内容类型	期刊论文
源URL	[http://cas-ir.dicp.ac.cn/handle/321008/145510]
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.Dalian Med Univ, Hosp 2, Dalian, Liaoning, Peoples R China 2.China Med Univ, Shengjing Hosp, Shenyang, Liaoning, Peoples R China 3.Liaoning Univ Chinese Tradit Med, Affiliated Hosp, Liaoning, Peoples R China 4.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian, Peoples R China 5.Liaoning Med Univ, Affiliated Hosp 1, Dalian, Peoples R China
推荐引用方式 GB/T 7714	Dong, De-Gang,Zhang, Yao,Zhang, Shu-Lan,et al. Inhibition potential of UDP-glucuronosyltransferases (UGTs) 1A isoforms by the analogue of resveratrol, bakuchiol[J]. pharmazie,2014,69(1):60-63.
APA	Dong, De-Gang.,Zhang, Yao.,Zhang, Shu-Lan.,Lv, Jing.,Guo, En-Mian.,...&Cao, Yun-Feng.(2014).Inhibition potential of UDP-glucuronosyltransferases (UGTs) 1A isoforms by the analogue of resveratrol, bakuchiol.pharmazie,69(1),60-63.
MLA	Dong, De-Gang,et al."Inhibition potential of UDP-glucuronosyltransferases (UGTs) 1A isoforms by the analogue of resveratrol, bakuchiol".pharmazie 69.1(2014):60-63.