DICP OpenIR
Cryptotanshinone and dihydrotanshinone I exhibit strong inhibition towards human liver microsome (HLM)-catalyzed propofol glucuronidation
Cong, Ming1; Hu, Cui-Min5; Cao, Yun-Feng2,3; Fang, Zhong-Ze2,3,5; Tang, Shu-Hong4; Wang, Jia-Rui4; Luo, Jun-Sheng1
KeywordDanshen Udp-glucuronosyltransferases (Ugts) Herb-drug Interaction
Source PublicationFITOTERAPIA
2013-03-01
DOI10.1016/j.fitote.2013.01.002
Volume85Pages:109-113
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectChemistry, Medicinal ; Pharmacology & Pharmacy
WOS Research AreaPharmacology & Pharmacy
WOS KeywordUDP-GLUCURONOSYLTRANSFERASE ISOFORMS ; SALVIA-MILTIORRHIZA ; SUPRAVENTRICULAR TACHYCARDIA ; TANSHINONE IIA ; IDENTIFICATION ; CONSTITUENTS ; CHEMISTRY
AbstractDanshen is one of the most famous herbs in the world, and more and more danshen-prescribed drugs interactions have been reported in recent years. Evaluation of inhibition potential of danshen's major ingredients towards UDP-glucuronosyltransferases (UGTs) will be helpful for understanding detailed mechanisms for danshen-drugs interaction. Therefore, the aim of the present study is to investigate the inhibitory situation of cryptotanshinone and dihydrotanshinone I towards UGT enzyme-catalyzed propofol glucuronidation. In vitro the human liver microsome (HLM) incubation system was used, and the results showed that cryptotanshinone and dihydrotanshinone I exhibited dose-dependent inhibition towards HLM-catalyzed propofol glucuronidation. Dixon plot and Lineweaver-Burk plot showed that the inhibition type was best fit to competitive inhibition type for both cryptotanshinone and dihydrotanshinone I. The second plot using the slopes from the Lineweaver-Burk plot versus the concentrations of cryptotanshinone or dihydrotanshinone I was employed to calculate the inhibition parameters (K-1) to be 0.4 and 1.7 mu M, respectively. Using the reported maximum plasma concentration (C-max), the altered in vivo exposure of propofol increased by 10% and 8.2% for the co-administration of dihydrotanshinone I and cryptotanshinone, respectively. All these results indicated the possible danshen-propofol interaction due to the inhibition of dihydrotanshinone I and cryptotanshinone towards the glucuronidation reaction of propofol. (C) 2013 Elsevier B.V. All rights reserved.
Language英语
WOS IDWOS:000317172000016
Citation statistics
Cited Times:17[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/137738
Collection中国科学院大连化学物理研究所
Affiliation1.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou 121001, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian 116023, Peoples R China
3.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China
4.Fifth Hosp Dalian, Dept Oncol, Dalian 116021, Peoples R China
5.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA
Recommended Citation
GB/T 7714
Cong, Ming,Hu, Cui-Min,Cao, Yun-Feng,et al. Cryptotanshinone and dihydrotanshinone I exhibit strong inhibition towards human liver microsome (HLM)-catalyzed propofol glucuronidation[J]. FITOTERAPIA,2013,85:109-113.
APA Cong, Ming.,Hu, Cui-Min.,Cao, Yun-Feng.,Fang, Zhong-Ze.,Tang, Shu-Hong.,...&Luo, Jun-Sheng.(2013).Cryptotanshinone and dihydrotanshinone I exhibit strong inhibition towards human liver microsome (HLM)-catalyzed propofol glucuronidation.FITOTERAPIA,85,109-113.
MLA Cong, Ming,et al."Cryptotanshinone and dihydrotanshinone I exhibit strong inhibition towards human liver microsome (HLM)-catalyzed propofol glucuronidation".FITOTERAPIA 85(2013):109-113.
Files in This Item:
There are no files associated with this item.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Cong, Ming]'s Articles
[Hu, Cui-Min]'s Articles
[Cao, Yun-Feng]'s Articles
Baidu academic
Similar articles in Baidu academic
[Cong, Ming]'s Articles
[Hu, Cui-Min]'s Articles
[Cao, Yun-Feng]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Cong, Ming]'s Articles
[Hu, Cui-Min]'s Articles
[Cao, Yun-Feng]'s Articles
Terms of Use
No data!
Social Bookmark/Share
All comments (0)
No comment.
 

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