Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris.

Biotechnology Letters
Thi Thanh Hanh NguyenDoman Kim

Abstract

The 3C-like protease (3CL(pro)) of severe acute respiratory syndrome associated coronavirus (SARS-CoV) is vital for SARS-CoV replication and is a promising drug target. Recombinant 3CL(pro) was expressed in Pichia pastoris GS115 as a 42 kDa protein that displayed a K ( m ) of 15 ± 2 μM with Dabcyl-KTSAVLQSGFRKME-Edans as substrate. Purified 3CL(pro) was used for inhibition and kinetic assays with seven flavonoid compounds. The IC(50) of six flavonoid compounds were 47-381 μM. Quercetin, epigallocatechin gallate and gallocatechin gallate (GCG) displayed good inhibition toward 3CL(pro) with IC(50) values of 73, 73 and 47 μM, respectively. GCG showed a competitive inhibition pattern with K ( i ) value of 25 ± 1.7 μM. In molecular docking experiments, GCG displayed a binding energy of -14 kcal mol(-1) to the active site of 3CL(pro) and the galloyl moiety at 3-OH position was required for 3CL(pro) inhibition activity.

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Citations

Dec 20, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Thi Thanh Hanh NguyenDoman Kim
Aug 2, 2018·Virology Journal·Chenguang YaoYanhong Wei
Nov 15, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Seri JoMi-Sun Kim
Jan 1, 2019·Biotechnology and Bioprocess Engineering : BBE·Jeesoo KimDoman Kim
Aug 15, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Shogo NakanoSohei Ito
Jun 20, 2020·Journal of Evidence-based Integrative Medicine·Hanan Polansky, Gillad Lori
Aug 29, 2020·Oxidative Medicine and Cellular Longevity·Lúcio Ricardo Leite DinizDamião Pergentino de Sousa
Sep 29, 2020·Phytochemistry Reviews : Proceedings of the Phytochemical Society of Europe·Julia Solnier, Johannes-Paul Fladerer
May 28, 2020·International Journal of Molecular Sciences·André FischerMarkus A Lill
Sep 5, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Muchtaridi MuchtaridiHabibah A Wahab
Aug 28, 2020·Frontiers in Pharmacology·Bachir Benarba, Atanasio Pandiella
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Sep 12, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Simona PiccolellaSeverina Pacifico
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Methods Mentioned

BETA
PCR
electrophoresis
fluorescence
FRET
glycosylation

Software Mentioned

SigmaPlot
AutoDockTools
Ligplot
AutoDock

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