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Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking

The main protease (Mpro) of SARS-CoV-2 is a protease necessary for viral polyprotein processing and maturation. Mpro cleaves the polypeptide sequence after the glutamine residues. There is no known cellular protease with this substrate specificity in humans; therefore, it is considered an attractive...

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Published in:Heliyon 2022-03, Vol.8 (3), p.e09034-e09034, Article e09034
Main Authors: Chou, Feng-Pai, Liu, Chia-Chun, Huong Giang, Huynh Nguyet, Huang, Sheng-Cih, Hsu, Hsiu-Fu, Wu, Tung-Kung
Format: Article
Language:English
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Summary:The main protease (Mpro) of SARS-CoV-2 is a protease necessary for viral polyprotein processing and maturation. Mpro cleaves the polypeptide sequence after the glutamine residues. There is no known cellular protease with this substrate specificity in humans; therefore, it is considered an attractive drug target. Previously, fermented sorghum extract RevX (trademark of Revolutrx INC.) solution significantly alleviated physical decline and complications in a patient with lung adenocarcinoma, suggesting the role of bioactive components in RevX solution. To further explore whether the bioactive components in RevX solution exhibit other biological activities, such as antiviral effects, we investigated its inhibitory effect on the Mpro of SARS-CoV-2 virus. We report herein that the solid extract of the RevX solution exhibits an efficacious Mpro inhibitory activity, with IC50 of 2.07 ± 0.38 μg/mL. Molecular docking of sterol-like components in the RevX extracts identified by MS shows that the three sterol-like molecules can bind to the active region of the GC376-Mpro complex, supporting the structure-function relationship. Combined with its ability to significantly alleviate the body's immunity decline and to inhibit the activity of SARS-CoV-2 Mpro, RevX solution may provide a possible alternative supportive treatment for patients with COVID-19. •The unique substrate specificity of SARS-CoV-2 Mpro makes it a potential target for drug design.•Fermented sorghum extract RevX solution enhances adjuvant therapy of lung adenocarcinoma, suggesting the role of bioactive components in RevX solution.•The solid extract of RevX showed potent Mpro inhibitory activity with IC50 of 2.07 ± 0.38 μg/mL.•The three sterol-like structures of RevX extract showed a similar binding cavity to Mpro-GC376, suggesting its putative inhibitory activity. Sorghum; Sterol; Mpro; GC-376; Antiviral drug.
ISSN:2405-8440
2405-8440
DOI:10.1016/j.heliyon.2022.e09034