作者
Ji-Young Park, Jang Hoon Kim, Jung Min Kwon, Hyung-Jun Kwon, Hyung Jae Jeong, Young Min Kim, Doman Kim, Woo Song Lee, Young Bae Ryu
发表日期
2013/7/1
期刊
Bioorganic & medicinal chemistry
卷号
21
期号
13
页码范围
3730-3737
出版商
Pergamon
简介
SARS-CoV 3CL pro plays an important role in viral replication. In this study, we performed a biological evaluation on nine phlorotannins isolated from the edible brown algae Ecklonia cava. The nine isolated phlorotannins (1–9), except phloroglucinol (1), possessed SARS-CoV 3CL pro inhibitory activities in a dose-dependently and competitive manner. Of these phlorotannins (1–9), two eckol groups with a diphenyl ether linked dieckol (8) showed the most potent SARS-CoV 3CL pro trans/cis-cleavage inhibitory effects (IC 50 s= 2.7 and 68.1 μM, respectively). This is the first report of a (8) phlorotannin chemotype significantly blocking the cleavage of SARS-CoV 3CL pro in a cell-based assay with no toxicity. Furthermore, dieckol (8) exhibited a high association rate in the SPR sensorgram and formed extremely strong hydrogen bonds to the catalytic dyad (Cys145 and His41) of the SARS-CoV 3CL pro.
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