期刊
CELL AND BIOSCIENCE
卷 11, 期 1, 页码 -出版社
BMC
DOI: 10.1186/s13578-021-00564-x
关键词
SARS-CoV-2; Natural product; Ginkgolic acid; Anacardic acid; Papain‐ like protease
资金
- Key Technology Research and Development Program of Shandong, China [2020CXGC010505]
- Natural Science Foundation of Shandong Province, China [ZR2020MH383]
The study identified two natural products, ginkgolic acid and anacardic acid, as inhibitors of SARS-CoV-2, with dual inhibition effects on both the papain-like protease (PLpro) and the 3-chymotrypsin-like protease (3CL(pro)). These compounds were characterized as irreversible inhibitors against both 3CL(pro) and PLpro, and were found to inhibit SARS-CoV-2 replication in vitro at nontoxic concentrations, showing promise as potential antivirals against SARS-CoV-2.
Background In the urgent campaign to develop therapeutics against SARS-CoV-2, natural products have been an important source of new lead compounds. Results We herein identified two natural products, ginkgolic acid and anacardic acid, as inhibitors using a high-throughput screen targeting the SARS-CoV-2 papain-like protease (PLpro). Moreover, our study demonstrated that the two hit compounds are dual inhibitors targeting the SARS-CoV-2 3-chymotrypsin-like protease (3CL(pro)) in addition to PLpro. A mechanism of action study using enzyme kinetics further characterized the two compounds as irreversible inhibitors against both 3CL(pro) and PLpro. Significantly, both identified compounds inhibit SARS-CoV-2 replication in vitro at nontoxic concentrations. Conclusions Our finding provides two novel natural products as promising SARS-CoV-2 antivirals.
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