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Biotechnol Lett. 2017 Mar;39(3):415-421. doi: 10.1007/s10529-016-2261-6. Epub 2016 Nov 24.

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

Author information

1
Graduate School of International Agricultural Technology and Institute of Food Industrialization, Institutes of Green Bioscience & Technology, Seoul National University, Pyeongchang-gun, Gangwon-do, 25354, South Korea.
2
Section of Neurobiology, Department of Biological Sciences, University of Southern California, Los Angeles, CA, 90089, USA.
3
Skin Research Institute, Amorepacific Corporation R&D Center, Yongin, 17074, South Korea.
4
Graduate School of International Agricultural Technology and Institute of Food Industrialization, Institutes of Green Bioscience & Technology, Seoul National University, Pyeongchang-gun, Gangwon-do, 25354, South Korea. kimdm@snu.ac.kr.

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.

KEYWORDS:

Flavanoids; Myricetin; Polyphenols; Protease; Zika virus

PMID:
27885509
DOI:
10.1007/s10529-016-2261-6
[Indexed for MEDLINE]

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