SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii = 생약소재로부터 퀴논메사이드트리터페노이드 화합물의 사스코로나바이러스 타겟 효소인 3CL억제제 개발

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Title
SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii = 생약소재로부터 퀴논메사이드트리터페노이드 화합물의 사스코로나바이러스 타겟 효소인 3CL억제제 개발
Author(s)
Young Bae RyuSu-Jin Park; Young Min Kim; J Y Lee; W D Seo; Jong Sun Chang; K H Park; Mun Chual RhoWoo Song Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 6, pp. 1873-1876
Publication Year
2010
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.
Keyword
3CLproCelastrolIguesterinQuinone-methideSARS-CoVTripterygium regelii
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2010.01.152
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
Jeonbuk Branch Institute > Immunoregulatory materials Research Center > 1. Journal Articles
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