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SARS-CoV 3CL(pro) inhibitory effects of quinone-methide triterpenes from Tripterygium regeliiopen access
- 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
- Issue Date
- 15-Mar-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- SARS-CoV; 3CL(pro); Tripterygium regelii; Quinone-methide; Celastrol; Iguesterin
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.6, pp 1873 - 1876
- Pages
- 4
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 20
- Number
- 6
- Start Page
- 1873
- End Page
- 1876
- ISSN
- 0960-894X
1464-3405
- 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 3CL(pro) inhibitory activities and showed potent inhibitory activities with IC50 values of 10.3, 5.5, 9.9, and 2.6 mu M, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC50 = 21.7 mu M). 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. (C) 2010 Elsevier Ltd. All rights reserved.
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