Influenza virus neuraminidase inhibitory activity of phlorotannins from the edible brown alga Ecklonia cava = 갈조류 감태로부터 분리한 플로로탄닌계 화합물의 인플루엔자 뉴라미니데이즈 저해활성

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Title
Influenza virus neuraminidase inhibitory activity of phlorotannins from the edible brown alga Ecklonia cava = 갈조류 감태로부터 분리한 플로로탄닌계 화합물의 인플루엔자 뉴라미니데이즈 저해활성
Author(s)
Young Bae RyuHyung Jae Jung; So Young Yoon; Ji Young Park; Young Min Kim; Su-Jin ParkMun Chual Rho; S J Kim; Woo Song Lee
Bibliographic Citation
Journal of Agricultural and Food Chemistry, vol. 59, no. 12, pp. 6467-6473
Publication Year
2011
Abstract
Influenza A virus infections continue to pose a major threat to humans and several animal species. Neuraminidase (NA) is one of the most promising targets for the development of drugs against influenza viruses because of its critical role in the viral life cycle. During the course of a search for NA inhibitors from edible natural sources, we found that the ethyl acetate layer of ethanol extracts of Ecklonia cava showed extremely high NA-inhibitory activity (72.1% inhibition at 30 μg/mL). Bioactivity-guided fractionation of the ethyl acetate layer yielded five phlorotannins, identified as phloroglucinol (1), eckol (2), 7-phloroeckol (3), phlorofucofuroeckol (4), and dieckol (5). The inhibitory activities of these compounds (1-5) against NAs from group-1 (A/Bervig-Mission/1/18 [H1N1], A/PR/8/34 [H1N1]) and group-2 (A/Hong Kong/8/68 [H3N2], A/Chicken/Korea/MS96/96 [H9N2]) influenza A were evaluated to determine potencies and kinetic behavior. Analyses using various in vitro influenza A virus NA assays showed that all five phlorotannin derivatives were selective NA inhibitors. Of the phlorotannins, phlorofucofuroeckol (4) exhibited the most potent inhibitory activities toward group-1 NAs (IC50 values, 4.5 and 14.7 μM), whereas dieckol (5) potently inhibited group-2 NAs. Kinetic analyses indicated that compounds 1-5 were all noncompetitive. Notably, these noncompetitive inhibitors synergized with oseltamivir to enhance the NA-inhibitory effects of oseltamivir.
Keyword
Ecklonia cavaInfluenza virusneuraminidasephlorotannin
ISSN
0021-8561
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/jf2007248
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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