상세 정보

underline
Metadata Downloads : dc(xml) or Excel
Cited 0 time in scopus ci

Title 

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii

 

생약소재로부터 퀴논메사이드트리터페노이드 화합물의 사스코로나바이러스 타겟 효소인 3CL억제제 개발

Authors 

Young Bae RyuSu-Jin ParkYoung Min KimJ Y LeeW D SeoJong Sun ChangK H ParkMun Chual RhoWoo Song Lee

Publisher 

Elsevier

Issue Date 

2010

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 6, pp. 1873-1876

Keywords 

3CLproCelastrolIguesterinQuinone-methideSARS-CoVTripterygium regelii

Abstract 

Quinone-methide triterpenes, celastrol (1), pristimerin (2), tingenone (3), and iguesterin (4) were isolated from Triterygium regelii and dihydrocelastrol (5) was synthesized by hydrogenation under palladium catalyst. Isolated quinone-methide triterpenes (1-4) and 5 were evaluated for SARS-CoV 3CLpro inhibitory activities and showed potent inhibitory activities with IC50 values of 10.3, 5.5, 9.9, and 2.6 μM, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC50 = 21.7 μM). As a result, quinone-methide moiety in A-ring and more hydrophobic E-ring assist to exhibit potent activity. Also, all quinone-methide triterpenes 1-4 have proven to be competitive by the kinetic analysis.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2010.01.152

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


There are no files associated with this item.
qrcode

FusionCharts.
DSpace Software Coptright(c) 2010 MIT and Hewleft-Packard  /  KRIBB-REPOSITORY ( Email:jakim@kribb.re.kr)