Inhibitory effect of flavonoids against NS2B-NS3 protease of ZIKA virus and their structure activity relationship.

ABSTRACT:

Objectives

To determine the inhibitory activities of flavonoids against NS2B-NS3 protease of ZIKA virus (ZIKV NS2B-NS3^pro) expressed in Escherichia coli BL21 (DE3) and their structure activity relationship.

Results

ZIKV NS2B-NS3^pro 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-NS3^pro 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-NS3^pro 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

SUBMITTER: Lim HJ 

PROVIDER: S-EPMC7088272 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature