SARS-CoV 3CL super(pro) inhibitory effects of quinone-methide triterpenes from Tripterygium regelii

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-Co...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 6; pp. 1873 - 1876
Main Authors Ryu, Young Bae, Park, Su-Jin, Kim, Young Min, Lee, Ju-Yeon, Seo, Woo Duck, Chang, Jong Sun, Park, Ki Hun, Rho, Mun-Chual, Lee, Woo Song
Format Journal Article
LanguageEnglish
Published 15.03.2010
Subjects
SARS coronavirus
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Summary: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 3CL super(pro) inhibitory activities and showed potent inhibitory activities with IC sub(50) values of 10.3, 5.5, 9.9, and 2.6 kM, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC sub(50) = 21.7 kM). 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. AB:
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.01.152