2. Academic Validation
  3. Ginkgolic acid and anacardic acid are specific covalent inhibitors of SARS-CoV-2 cysteine proteases

Ginkgolic acid and anacardic acid are specific covalent inhibitors of SARS-CoV-2 cysteine proteases

  • Cell Biosci. 2021 Feb 28;11(1):45. doi: 10.1186/s13578-021-00564-x.
Zinuo Chen  # 1,  Qinghua Cui  # 1 2 3,  Laura Cooper  # 4,  Pin Zhang 5,  Hyun Lee 6,  Zhaoyu Chen 1,  Yanyan Wang 1,  Xiaoyun Liu 2,  Lijun Rong 7,  Ruikun Du 8 9 10
Affiliations

Affiliations

  • 1 College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China.
  • 2 Experimental Center, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China.
  • 3 Qingdao Academy of Chinese Medicinal Sciences, Shandong University of Traditional Chinese Medicine, Qingdao, 266122, China.
  • 4 Department of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, IL, 60612, USA.
  • 5 Chicago BioSolutions Inc, 2242 W Harrison Street, Chicago, Illinois, 60612, United States.
  • 6 Department of Pharmaceutical Sciences, Center for Biomolecular Sciences, College of Pharmacy, Biophysics Core at Research Resources Center, University of Illinois at Chicago, Chicago, IL, 60607, USA.
  • 7 Department of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, IL, 60612, USA. lijun@uic.edu.
  • 8 College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China. duzi857@163.com.
  • 9 Experimental Center, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China. duzi857@163.com.
  • 10 Qingdao Academy of Chinese Medicinal Sciences, Shandong University of Traditional Chinese Medicine, Qingdao, 266122, China. duzi857@163.com.
  • # Contributed equally.
PMID: 33640032 DOI: 10.1186/s13578-021-00564-x
Abstract

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 (3CLpro) in addition to PLpro. A mechanism of action study using Enzyme kinetics further characterized the two compounds as irreversible inhibitors against both 3CLpro 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.

Keywords

Anacardic acid; Ginkgolic acid; Natural product; Papain‐like protease; SARS-CoV-2.

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