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All-Trans Retinoic Acid Exhibits Antiviral Effect against SARS-CoV-2 by Inhibiting 3CLpro Activity.
Morita, Takeshi; Miyakawa, Kei; Jeremiah, Sundararaj Stanleyraj; Yamaoka, Yutaro; Sada, Mitsuru; Kuniyoshi, Tomoko; Yang, Jinwei; Kimura, Hirokazu; Ryo, Akihide.
  • Morita T; Department of Microbiology, Yokohama City University Graduate School of Medicine, Yokohama 236-0004, Japan.
  • Miyakawa K; Department of Microbiology, Yokohama City University Graduate School of Medicine, Yokohama 236-0004, Japan.
  • Jeremiah SS; Department of Microbiology, Yokohama City University Graduate School of Medicine, Yokohama 236-0004, Japan.
  • Yamaoka Y; Department of Microbiology, Yokohama City University Graduate School of Medicine, Yokohama 236-0004, Japan.
  • Sada M; Life Science Laboratory, Technology and Development Division, Kanto Chemical Co., Inc., Isehara 259-1146, Japan.
  • Kuniyoshi T; Advanced Medical Science Research Center, Gunma Paz University, Shibukawa 377-0008, Japan.
  • Yang J; R&D Department, TOKIWA Phytochemical Co., Ltd., Sakura, Chiba 285-0801, Japan.
  • Kimura H; R&D Department, TOKIWA Phytochemical Co., Ltd., Sakura, Chiba 285-0801, Japan.
  • Ryo A; Department of Health Science, Gunma Paz University Graduate School, Takasaki 370-0006, Japan.
Viruses ; 13(8)2021 08 23.
Article in English | MEDLINE | ID: covidwho-1524167
ABSTRACT
The pandemic of COVID-19 caused by SARS-CoV-2 continues to spread despite the global efforts taken to control it. The 3C-like protease (3CLpro), the major protease of SARS-CoV-2, is one of the most interesting targets for antiviral drug development because it is highly conserved among SARS-CoVs and plays an important role in viral replication. Herein, we developed high throughput screening for SARS-CoV-2 3CLpro inhibitor based on AlphaScreen. We screened 91 natural product compounds and found that all-trans retinoic acid (ATRA), an FDA-approved drug, inhibited 3CLpro activity. The 3CLpro inhibitory effect of ATRA was confirmed in vitro by both immunoblotting and AlphaScreen with a 50% inhibition concentration (IC50) of 24.7 ± 1.65 µM. ATRA inhibited the replication of SARS-CoV-2 in VeroE6/TMPRSS2 and Calu-3 cells, with IC50 = 2.69 ± 0.09 µM in the former and 0.82 ± 0.01 µM in the latter. Further, we showed the anti-SARS-CoV-2 effect of ATRA on the currently circulating variants of concern (VOC); alpha, beta, gamma, and delta. These results suggest that ATRA may be considered as a potential therapeutic agent against SARS-CoV-2.
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Full text: Available Collection: International databases Database: MEDLINE Document Type: Article Main subject: Antiviral Agents / Tretinoin / Coronavirus 3C Proteases / SARS-CoV-2 Subject: Antiviral Agents / Tretinoin / Coronavirus 3C Proteases / SARS-CoV-2 Language: English Year: 2021

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Full text: Available Collection: International databases Database: MEDLINE Document Type: Article Main subject: Antiviral Agents / Tretinoin / Coronavirus 3C Proteases / SARS-CoV-2 Subject: Antiviral Agents / Tretinoin / Coronavirus 3C Proteases / SARS-CoV-2 Language: English Year: 2021
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