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Inhibitory effect of flavonoids against NS2B-NS3 protease of ZIKA virus and their structure activity relationship.
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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.
SUBMITTER: Lim HJ
PROVIDER: S-EPMC7088272 | biostudies-literature | 2017 Mar
REPOSITORIES: biostudies-literature
Publications
Inhibitory effect of flavonoids against NS2B-NS3 protease of ZIKA virus and their structure activity relationship.
Biotechnology letters 20161124 3
<h4>Objectives</h4>To determine the inhibitory activities of flavonoids against NS2B-NS3 protease of ZIKA virus (ZIKV NS2B-NS3<sup>pro</sup>) expressed in Escherichia coli BL21 (DE3) and their structure activity relationship.<h4>Results</h4>ZIKV NS2B-NS3<sup>pro</sup> was expressed in E. coli BL21(DE3) as a 35 kDa protein. It had a K <sub>m</sub> of 26 µM with the fluorogenic peptide Dabcyl-KTSAVLQSGFRKME-Edan. The purified ZIKV NS2B-NS3<sup>pro</sup> was used for inhibition and kinetic assays t ...[more]