Diarylheptanoids from Alnus japonica Inhibit Papain-Like Protease of Severe Acute Respiratory Syndrome Coronavirus

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  • Park Ji-Young
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology School of Biological Science and Biotechnology, Chonnam National University Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB) School of Biological Science and Biotechnology, Chonnam National University
  • Jae Jeong Hyung
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)
  • Hoon Kim Jang
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)
  • Min Kim Young
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)
  • Park Su-Jin
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)
  • Kim Doman
    School of Biological Science and Biotechnology, Chonnam National University School of Biological Science and Biotechnology, Chonnam National University
  • Hun Park Ki
    Division of Applied Life Science (BK 21 Program, IALS), Graduate School of Gyeongsang National University Division of Applied Life Science (BK 21 Program, IALS), Graduate School of Gyeongsang National University
  • Song Lee Woo
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)
  • Bae Ryu Young
    Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)

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  • Diarylheptanoids from <i>Alnus japonica</i> Inhibit Papain-Like Protease of Severe Acute Respiratory Syndrome Coronavirus

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The papain-like protease (PLpro), which controls replication of the severe acute respiratory syndrome coronavirus (SARS-CoV), has been identified as a potential drug target for the treatment of SARS. An intensive hunt for effective anti-SARS drugs has been undertaken by screening for natural product inhibitors that target SARS-CoV PLpro. In this study, diarylheptanoids 1–9 were isolated from Alnus japonica, and the inhibitory activities of these compounds against PLpro were determined. Of the isolated diarylheptanoids, hirsutenone (2) showed the most potent PLpro inhibitory activity, with an inhibitory concentration (IC50) value of 4.1 µM. Structure–activity analysis showed that catechol and α,β-unsaturated carbonyl moiety in the molecule were the key requirement for SARS-CoV cysteine protease inhibition.

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