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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| Format: | Article |
| Language: | English |
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Elsevier
2022-03-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S240584402200322X |
| _version_ | 1818309064800600064 |
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| author | Feng-Pai Chou Chia-Chun Liu Huynh Nguyet Huong Giang Sheng-Cih Huang Hsiu-Fu Hsu Tung-Kung Wu |
| author_facet | Feng-Pai Chou Chia-Chun Liu Huynh Nguyet Huong Giang Sheng-Cih Huang Hsiu-Fu Hsu Tung-Kung Wu |
| author_sort | Feng-Pai Chou |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-13T07:24:14Z |
| format | Article |
| id | doaj.art-fe768f36e76b46a1ab5e99ea24055341 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-12-13T07:24:14Z |
| publishDate | 2022-03-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-fe768f36e76b46a1ab5e99ea240553412022-12-21T23:55:21ZengElsevierHeliyon2405-84402022-03-0183e09034Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular dockingFeng-Pai Chou0Chia-Chun Liu1Huynh Nguyet Huong Giang2Sheng-Cih Huang3Hsiu-Fu Hsu4Tung-Kung Wu5Department of Biological Science and Technology, National Yang Ming Chiao Tung University, 1001 Ta-Hsueh Rd., Hsinchu 30010, Taiwan, ROC; Center for Emergent Functional Matter Science, National Yang Ming Chiao Tung University, 1001 Ta-Hsueh Rd., Hsinchu 30010, Taiwan, ROCDepartment of Chemistry, Tamkang University, No.151, Yingzhuan Rd., Tamsui Dist., New Taipei City 251301, Taiwan, ROCDepartment of Material Science, National Yang Ming Chiao Tung University, 1001 Ta-Hsueh Rd., Hsinchu 30010, Taiwan, ROCDepartment of Biological Science and Technology, National Yang Ming Chiao Tung University, 1001 Ta-Hsueh Rd., Hsinchu 30010, Taiwan, ROCDepartment of Chemistry, Tamkang University, No.151, Yingzhuan Rd., Tamsui Dist., New Taipei City 251301, Taiwan, ROC; Corresponding author.Department of Biological Science and Technology, National Yang Ming Chiao Tung University, 1001 Ta-Hsueh Rd., Hsinchu 30010, Taiwan, ROC; Center for Emergent Functional Matter Science, National Yang Ming Chiao Tung University, 1001 Ta-Hsueh Rd., Hsinchu 30010, Taiwan, ROC; Corresponding author.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.http://www.sciencedirect.com/science/article/pii/S240584402200322XSorghumSterolMproGC-376Antiviral drug |
| spellingShingle | Feng-Pai Chou Chia-Chun Liu Huynh Nguyet Huong Giang Sheng-Cih Huang Hsiu-Fu Hsu Tung-Kung Wu Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking Heliyon Sorghum Sterol Mpro GC-376 Antiviral drug |
| title | Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking |
| title_full | Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking |
| title_fullStr | Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking |
| title_full_unstemmed | Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking |
| title_short | Evaluation of RevX solution extract as a potential inhibitor of the main protease of SARS-CoV-2—In vitro study and molecular docking |
| title_sort | evaluation of revx solution extract as a potential inhibitor of the main protease of sars cov 2 in vitro study and molecular docking |
| topic | Sorghum Sterol Mpro GC-376 Antiviral drug |
| url | http://www.sciencedirect.com/science/article/pii/S240584402200322X |
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