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题名: Inhibition potential of UDP-glucuronosyltransferases (UGTs) 1A isoforms by the analogue of resveratrol, bakuchiol
作者: Dong, De-Gang1;  Zhang, Yao2;  Zhang, Shu-Lan2;  Lv, Jing3;  Guo, En-Mian3;  Fang, Zhong-Ze4;  Cao, Yun-Feng4
刊名: PHARMAZIE
发表日期: 2014
DOI: 10.1691/ph.2014.3717
卷: 69, 期:1, 页:60-63
收录类别: SCI
文章类型: Article
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
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.
关键词[WOS]: PSORALEA-CORYLIFOLIA ;  IN-VITRO ;  GLUCURONIDATION ;  IDENTIFICATION ;  METABOLISM ;  ACID
语种: 英语
WOS记录号: WOS:000334259500012
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/145510
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.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

Recommended Citation:
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.
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