Dieckol, a SARS-CoV 3CLpro inhibitor, isolated from the edible brown algae Ecklonia cava = 감태로부터 분리한 dieckol의 사스 코로나 3CLpro 저해활성

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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
Author(s)
Ji Young Park; Jang Hoon Kim; Jung Min Kwon; Hyung Jun KwonHyung Jae Jeong; Young-Min Kim; D Kim; Woo Song LeeYoung Bae Ryu
Bibliographic Citation
Bioorganic & Medicinal Chemistry, vol. 21, no. 13, pp. 3730-3737
Publication Year
2013
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.
Keyword
DieckolEcklonia cavaEckolPhlorotanninSARS-CoV
ISSN
0968-0896
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmc.2013.04.026
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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