Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV.
J Enzyme Inhib Med Chem
; 31(1): 23-30, 2016.
Article
em En
| MEDLINE
| ID: mdl-25683083
ABSTRACT
Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) and a papain-like protease (PL(pro)) are attractive targets for the development of anti-SARS drugs. In this study, nine alkylated chalcones (1-9) and four coumarins (10-13) were isolated from Angelica keiskei, and the inhibitory activities of these constituents against SARS-CoV proteases (3CL(pro) and PL(pro)) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PL(pro) inhibitory activity with IC50 values of 11.4 and 1.2 µM. Our detailed protein-inhibitor mechanistic analysis of these species indicated that the chalcones exhibited competitive inhibition characteristics to the SARS-CoV 3CL(pro), whereas noncompetitive inhibition was observed with the SARS-CoV PL(pro).
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
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Inibidores de Cisteína Proteinase
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Angelica
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Coronavírus Relacionado à Síndrome Respiratória Aguda Grave
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Chalconas
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Cisteína Proteases
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article