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Flavonoid-mediated Inhibition of SARS Coronavirus 3C-like Protease Expressed in Pichia Pastoris

Flavonoid-mediated Inhibition of SARS Coronavirus 3C-like Protease Expressed in Pichia Pastoris

Thi Thanh Hanh Nguyen, Hye-Jin Woo, Hee-Kyoung Kang, Van Dao Nguyen, Young-Min Kim, Do-Won Kim, Sul-Ah Ahn, Yongmei Xia, Doman Kim

Biotechnol Lett. 2012 May;34(5):831-8.

PMID: 22350287

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP4233969	(−)-Gallocatechin gallate		4233-96-9	Price

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