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Anticoronaviral Activity of the Natural Phloroglucinols, Dryocrassin ABBA and Filixic Acid ABA from the Rhizome of Dryopteris crassirhizoma by Targeting the Main Protease of SARS-CoV-2.
Jin, Young-Hee; Jeon, Sangeun; Lee, Jihye; Kim, Seungtaek; Jang, Min Seong; Park, Chul Min; Song, Jong Hwan; Kim, Hyoung Rae; Kwon, Sunoh.
  • Jin YH; KM Application Center, Korea Institute of Oriental Medicine, Daegu 41062, Korea.
  • Jeon S; Center for Convergent Research of Emerging Virus Infection, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
  • Lee J; Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam 13488, Korea.
  • Kim S; Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam 13488, Korea.
  • Jang MS; Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam 13488, Korea.
  • Park CM; Center for Convergent Research of Emerging Virus Infection, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
  • Song JH; Department of Non-Clinical Studies, Korea Institute of Toxicology, Daejeon 34114, Korea.
  • Kim HR; Center for Convergent Research of Emerging Virus Infection, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
  • Kwon S; Center for Convergent Research of Emerging Virus Infection, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
Pharmaceutics ; 14(2)2022 Feb 08.
Article in English | MEDLINE | ID: covidwho-1674760
ABSTRACT
The rhizome of Dryopteris crassirhizoma Nakai. (Dryopteridaceae) has been used in traditional medicine in East Asia and has recently been reported to have anticancer, anti-inflammation, and antibacterial activity as well as antiviral activity. Natural phloroglucinols from D. crassirhizoma, dryocrassin ABBA and filixic acid ABA were reported to inhibit influenza virus infection with an inhibitory activity on neuraminidase. In this study, we found that dryocrassin ABBA and filixic acid ABA have an inhibitory activity against the main protease of SARS-CoV-2. Therefore, dryocrassin ABBA and filixic acid ABA exhibited inhibitory activity against SARS-CoV-2 infection in Vero cells dose-dependently using the immunofluorescence-based antiviral assays. Moreover, these compounds inhibited SARS-CoV and MERS-CoV infection, suggesting their broad-spectrum anticoronaviral activity. In addition, a 5-day repeated-dose toxicity study of dryocrassin ABBA and filixic acid ABA suggested that an approximately lethal dose of these compounds in mice was >10 mg/kg. Pharmacokinetic studies of dryocrassin ABBA showed good microsomal stability, low hERG inhibition, and low CYP450 inhibition. In vivo pharmacokinetic properties of dryocrassin ABBA showed a long half-life (5.5-12.6 h) and high plasma exposure (AUC 19.3-65 µg·h/mL). Therefore, dryocrassin ABBA has therapeutic potential against emerging coronavirus infections, including COVID-19.
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Full text: Available Collection: International databases Database: MEDLINE Topics: Traditional medicine Language: English Year: 2022 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Topics: Traditional medicine Language: English Year: 2022 Document Type: Article