Inhibitory effect of flavonoids against NS2B-NS3 protease of ZIKA virus and their structure activity relationship.
Biotechnol Lett
; 39(3): 415-421, 2017 Mar.
Article
em En
| MEDLINE
| ID: mdl-27885509
ABSTRACT
OBJECTIVES:
To determine the inhibitory activities of flavonoids against NS2B-NS3 protease of ZIKA virus (ZIKV NS2B-NS3pro) expressed in Escherichia coli BL21 (DE3) and their structure activity relationship.RESULTS:
ZIKV NS2B-NS3pro was expressed in E. coli BL21(DE3) as a 35 kDa protein. It had a K m of 26 µM with the fluorogenic peptide Dabcyl-KTSAVLQSGFRKME-Edan. The purified ZIKV NS2B-NS3pro was used for inhibition and kinetic assays to determine the activities of 22 polyphenol compounds. These polyphenol compounds at 100 µM inhibited the activity of ZIKV NS2B-NS3pro by 6.2-88%. Seven polyphenol compounds had IC50 ranging from 22 ± 0.2 to 112 ± 5.5 µM. Myricetin showed a mixed type inhibitory pattern against ZIKV NS2B-NS3pro protease. Its IC50 value was 22 ± 0.2 µM with a K i value of 8.9 ± 1.9 µM.CONCLUSION:
The chemical structure of a polyphenol compound and its inhibitory activity against ZIKV NS2B-NS3pro can be explored to develop highly selective inhibitors against ZIKV NS2B-NS3pro.Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Flavonoides
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Proteínas não Estruturais Virais
/
Zika virus
Idioma:
En
Revista:
Biotechnol Lett
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Coréia do Sul