期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 35, 期 1, 页码 1045-1049出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2020.1754813
关键词
African swine fever virus protease; antiviral; flavonoid; fret; inhibitory compounds
资金
- National Research Foundation of Korea grant - Ministry of Education, Science and Technology, Republic of Korea (MEST) [2018R1D1A1B07050781, 2018R1D1A1B07050942]
- Brain Korea 21 (BK21) Project
- National Research Foundation of Korea [2018R1D1A1B07050781, 2018R1D1A1B07050942] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
African swine fever (ASF) caused by the ASF virus (ASFV) is the most hazardous swine disease. Since a huge number of pigs have been slaughtered to avoid a pandemic spread, intense studies on the disease should be followed quickly. Recent studies reported that flavonoids have various antiviral activity including ASFV. In this report, ASFV protease was selected as an antiviral target protein to cope with ASF. With a FRET (Fluorescence resonance energy transfer) method, ASFV protease was assayed with a flavonoid library which was composed of sixty-five derivatives classified based on ten different scaffolds. Of these, the flavonols scaffold contains a potential anti-ASFV protease activity. The most prominent flavonol was myricetin with IC50 of 8.4 mu M. Its derivative, myricitrin, with the rhamnoside moiety was also showed the profound inhibitory effect on ASFV protease. These two flavonols apparently provide a way to develop anti-ASFV agents based on their scaffold.
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