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Andrographolide and its fluorescent derivative inhibit the main proteases of 2019-nCoV and SARS-CoV through covalent linkage.
Shi, Tzu-Hau; Huang, Yi-Long; Chen, Chiao-Che; Pi, Wen-Chieh; Hsu, Yu-Ling; Lo, Lee-Chiang; Chen, Wei-Yi; Fu, Shu-Ling; Lin, Chao-Hsiung.
Affiliation
  • Shi TH; Department of Life Sciences and Institute of Genome Sciences, National Yang-Ming University, Taipei, 112, Taiwan; Biomedical Industry Ph.D. Program, National Yang-Ming University, Taipei, 112, Taiwan.
  • Huang YL; Aging and Health Research Center, National Yang-Ming University, Taipei, 112, Taiwan.
  • Chen CC; Department of Life Sciences and Institute of Genome Sciences, National Yang-Ming University, Taipei, 112, Taiwan.
  • Pi WC; Institute of Biochemistry and Molecular Biology, National Yang-Ming University, Taipei, 112, Taiwan.
  • Hsu YL; Department of Chemistry, National Taiwan University, Taipei, 106, Taiwan.
  • Lo LC; Department of Chemistry, National Taiwan University, Taipei, 106, Taiwan.
  • Chen WY; Institute of Biochemistry and Molecular Biology, National Yang-Ming University, Taipei, 112, Taiwan.
  • Fu SL; Institute of Traditional Medicine, National Yang-Ming University, Taipei, 112, Taiwan. Electronic address: slfu@ym.edu.tw.
  • Lin CH; Department of Life Sciences and Institute of Genome Sciences, National Yang-Ming University, Taipei, 112, Taiwan; Aging and Health Research Center, National Yang-Ming University, Taipei, 112, Taiwan; Institute of Biopharmaceutical Sciences, National Yang-Ming University, Taipei, 112, Taiwan. Electro
Biochem Biophys Res Commun ; 533(3): 467-473, 2020 Dec 10.
Article in En | MEDLINE | ID: mdl-32977949
ABSTRACT
The coronavirus disease 2019 (COVID-19) pandemic caused by 2019 novel coronavirus (2019-nCoV) has been a crisis of global health, whereas the effective vaccines against 2019-nCoV are still under development. Alternatively, utilization of old drugs or available medicine that can suppress the viral activity or replication may provide an urgent solution to suppress the rapid spread of 2019-nCoV. Andrographolide is a highly abundant natural product of the medicinal plant, Andrographis paniculata, which has been clinically used for inflammatory diseases and anti-viral therapy. We herein demonstrate that both andrographolide and its fluorescent derivative, the nitrobenzoxadiazole-conjugated andrographolide (Andro- NBD), suppressed the main protease (Mpro) activities of 2019-nCoV and severe acute respiratory syndrome coronavirus (SARS-CoV). Moreover, Andro-NBD was shown to covalently link its fluorescence to these proteases. Further mass spectrometry (MS) analysis suggests that andrographolide formed a covalent bond with the active site Cys145 of either 2019-nCoV Mpro or SARS-CoV Mpro. Consistently, molecular modeling analysis supported the docking of andrographolide within the catalytic pockets of both viral Mpros. Considering that andrographolide is used in clinical practice with acceptable safety and its diverse pharmacological activities that could be beneficial for attenuating COVID-19 symptoms, extensive investigation of andrographolide on the suppression of 2019-nCoV as well as its application in COVID-19 therapy is suggested.
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Full text: 1 Database: MEDLINE Main subject: Protease Inhibitors / Cysteine Endopeptidases / Viral Nonstructural Proteins / Diterpenes Language: En Journal: Biochem Biophys Res Commun Year: 2020 Type: Article Affiliation country: Taiwan

Full text: 1 Database: MEDLINE Main subject: Protease Inhibitors / Cysteine Endopeptidases / Viral Nonstructural Proteins / Diterpenes Language: En Journal: Biochem Biophys Res Commun Year: 2020 Type: Article Affiliation country: Taiwan