Inhibition of African swine fever virus protease by myricetin and myricitrin
Inhibition of African swine fever virus protease by myricetin and myricitrin
复制标题
DOI：
10.1080/14756366.2020.1754813
复制
发表时间：
2020-01-01
影响因子：
5.6
通讯作者：
Kim, Mi-Sun
中科院分区：
文献类型：
--
作者：
Jo, Seri;Kim, Suwon;Kim, Mi-Sun
非洲猪瘟（African Swine Fever，ASF）是由非洲猪瘟病毒（African Swine Fever Virus，ASFV）引起的一种危害性最大的猪病。由于大量的猪被屠宰以避免大流行的传播，因此对这种疾病的深入研究应该迅速进行。近年来研究发现黄酮类化合物具有多种抗病毒活性，包括抗ASFV。本研究选择ASFV蛋白酶作为科普ASF病毒的靶蛋白。利用FRET（Fluorescence resonance energy transfer）方法，对ASFV蛋白酶活性进行了检测。其中，黄酮醇支架含有潜在的抗ASFV蛋白酶活性。最突出的黄酮醇是杨梅苷，IC 50为8.4 μ M。其衍生物杨梅苷与鼠李糖苷部分，也显示出深刻的抑制作用ASFV蛋白酶。这两种黄酮醇显然提供了一种基于其支架开发抗ASFV药物的方法。
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.