A phenolic acid.
Potential treatment - pre-clinical evidence
Anacardic acid is a bioactive phenolic acid (Hemshekhar et al., 2011). It was suggested to act as an irreversible covalent inhibitor of SARS-CoV-2 Papain-like and 3C-like proteases (Chen et al. 2021).
2-Hydroxy-6-pentadecylbenzoic acid; Ginkgolic acid C15:0
Ginkgolic acid and anacardic acid are specific covalent inhibitors of SARS-CoV-2 cysteine proteases
3CLpro PapainLpro Small molecule Enzyme assay In vitro In silico
|in silico; in vitro enzyme assay; Vero E6 cells; SARS-CoV-2 isolate USA-WA1/2020
Dose-dependently inhibited SARS-CoV-2 Papain-like protease and 3C-like protease with IC50s of ca. 17.8 μM and 2.07 μM, respectively, in vitro. The compound also blocked SARS-CoV-2 replication with an EC50 of ca. 9 μM in Vero E6 cells (at sub-cytotoxic concentrations (CC50 of 25.48 μM)).
Discovery of naturally occurring inhibitors against SARS-CoV-2 3CLpro from Ginkgo biloba leaves via large-scale screening
3CLpro Enzyme assay In vitro In silico
|in silico; in vitro enzyme assay
The compound inhibited SARS-CoV-2 3C-like protease with an IC50 of ca. 0.7 μM. It was also computationally modelled to bind a druggable site of the protease.