期刊
MOLECULES
卷 28, 期 3, 页码 -出版社
MDPI
DOI: 10.3390/molecules28030974
关键词
dengue virus; depside; depsidone; diffractaic acid; drug discovery
This study aimed to identify lichen-derived depsides and depsidones as inhibitors of dengue virus. It was found that barbatic acid, diffractaic acid, and Parmosidone C from lichens were effective in inhibiting dengue virus, with diffractaic acid showing the highest selectivity index and similar efficacy against other related viruses.
Dengue is a mosquito-borne flavivirus that causes 21,000 deaths annually. Depsides and depsidones of lichens have previously been reported to be antimicrobials. In this study, our objective was to identify lichen-derived depsides and depsidones as dengue virus inhibitors. The 18 depsides and depsidones of Usnea baileyi, Usnea aciculifera, Parmotrema dilatatum, and Parmotrema tsavoense were tested against dengue virus serotype 2. Two depsides and one depsidone inhibited dengue virus serotype 2 without any apparent cytotoxicity. Diffractaic acid, barbatic acid, and Parmosidone C were three active compounds further characterized for their efficacies (EC50), cytotoxicities (CC50), and selectivity index (SI; CC50/EC50). Their EC50 (SI) values were 2.43 +/- 0.19 (20.59), 0.91 +/- 0.15 (13.33), and 17.42 +/- 3.21 (8.95) mu M, respectively. Diffractaic acid showed the highest selectivity index, and similar efficacies were also found in dengue serotypes 1-4, Zika, and chikungunya viruses. Cell-based studies revealed that the target was mainly in the late stage with replication and the formation of infectious particles. This report highlights that a lichen-derived diffractaic acid could become a mosquito-borne antiviral lead as its selectivity indices ranged from 8.07 to 20.59 with a proposed target at viral replication.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据