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Title 

Dieckol, a SARS-CoV 3CLpro inhibitor, isolated from the edible brown algae Ecklonia cava

 

감태로부터 분리한 dieckol의 사스 코로나 3CLpro 저해활성

Authors 

Ji-Young ParkJang Hoon KimJung Min KwonHyung Jun KwonHyung Jae JeongYoung-Min KimD KimWoo Song LeeYoung Bae Ryu

Publisher 

Elsevier

Issue Date 

2013

Citation 

Bioorganic & Medicinal Chemistry, vol. 21, no. 13, pp. 3730-3737

Keywords 

DieckolEcklonia cavaEckolPhlorotanninSARS-CoV

Abstract 

SARS-CoV 3CLpro 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 3CLpro 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 3CLpro trans/cis-cleavage inhibitory effects (IC50s = 2.7 and 68.1 μM, respectively). This is the first report of a (8) phlorotannin chemotype significantly blocking the cleavage of SARS-CoV 3CLpro 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 3CLpro.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2013.04.026

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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