Inhibition of SARS-CoV 3C-like protease activity by theaflavin-3,3′- digallate (TF3)

Chia Nan Chen; Coney P.C. Lin; Kuo Kuei Huang; Wei Cheng Chen; Hsin Pang Hsieh; Po Huang Liang; John T.A. Hsu

doi:10.1093/ecam/neh081

Inhibition of SARS-CoV 3C-like protease activity by theaflavin-3,3′- digallate (TF3)

Chia Nan Chen, Coney P.C. Lin, Kuo Kuei Huang, Wei Cheng Chen, Hsin Pang Hsieh, Po Huang Liang, John T.A. Hsu

Center of Applied Nanomedicine

Research output: Contribution to journal › Article › peer-review

171 Citations (Scopus)

Abstract

SARS-CoV is the causative agent of severe acute respiratory syndrome (SARS). The virally encoded 3C-like protease (3CL^Pro) has been presumed critical for the viral replication of SARS-CoV in infected host cells. In this study, we screened a natural product library consisting of 720 compounds for inhibitory activity against 3CL^Pro. Two compounds in the library were found to be inhibitive: tannic acid (IC₅₀ = 3 μM) and 3-isotheaflavin-3-gallate (TF2B) (IC₅₀ = 7 μM). These two compounds belong to a group of natural polyphenols found in tea. We further investigated the 3CL^Pro-inhibitory activity of extracts from several different types of teas, including green tea, oolong tea, Puer tea and black tea. Our results indicated that extracts from Puer and black tea were more potent than that from green or oolong teas in their inhibitory activities against 3CL^Pro. Several other known compositions in teas were also evaluated for their activities in inhibiting 3CL^Pro. We found that caffeine, (-)-epigallocatechin gallte (EGCg), epicatechin (EC), theophylline (TP), catechin (C), epicatechin gallate (ECg) and epigallocatechin (EGC) did not inhibit 3CL^Pro activity. Only theaflavin-3,3′-digallate (TF3) was found to be a 3CL^Pro inhibitor. This study has resulted in the identification of new compounds that are effective 3CL^Pro inhibitors.

Original language	English
Pages (from-to)	209-215
Number of pages	7
Journal	Evidence-based Complementary and Alternative Medicine
Volume	2
Issue number	2
DOIs	https://doi.org/10.1093/ecam/neh081
Publication status	Published - 2005 Jun

All Science Journal Classification (ASJC) codes

Complementary and alternative medicine

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10.1093/ecam/neh081

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title = "Inhibition of SARS-CoV 3C-like protease activity by theaflavin-3,3′- digallate (TF3)",

abstract = "SARS-CoV is the causative agent of severe acute respiratory syndrome (SARS). The virally encoded 3C-like protease (3CLPro) has been presumed critical for the viral replication of SARS-CoV in infected host cells. In this study, we screened a natural product library consisting of 720 compounds for inhibitory activity against 3CLPro. Two compounds in the library were found to be inhibitive: tannic acid (IC50 = 3 μM) and 3-isotheaflavin-3-gallate (TF2B) (IC50 = 7 μM). These two compounds belong to a group of natural polyphenols found in tea. We further investigated the 3CLPro-inhibitory activity of extracts from several different types of teas, including green tea, oolong tea, Puer tea and black tea. Our results indicated that extracts from Puer and black tea were more potent than that from green or oolong teas in their inhibitory activities against 3CLPro. Several other known compositions in teas were also evaluated for their activities in inhibiting 3CLPro. We found that caffeine, (-)-epigallocatechin gallte (EGCg), epicatechin (EC), theophylline (TP), catechin (C), epicatechin gallate (ECg) and epigallocatechin (EGC) did not inhibit 3CLPro activity. Only theaflavin-3,3′-digallate (TF3) was found to be a 3CLPro inhibitor. This study has resulted in the identification of new compounds that are effective 3CLPro inhibitors.",

author = "Chen, {Chia Nan} and Lin, {Coney P.C.} and Huang, {Kuo Kuei} and Chen, {Wei Cheng} and Hsieh, {Hsin Pang} and Liang, {Po Huang} and Hsu, {John T.A.}",

year = "2005",

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doi = "10.1093/ecam/neh081",

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AU - Chen, Chia Nan

AU - Lin, Coney P.C.

AU - Huang, Kuo Kuei

AU - Chen, Wei Cheng

AU - Hsieh, Hsin Pang

AU - Liang, Po Huang

AU - Hsu, John T.A.

PY - 2005/6

Y1 - 2005/6

N2 - SARS-CoV is the causative agent of severe acute respiratory syndrome (SARS). The virally encoded 3C-like protease (3CLPro) has been presumed critical for the viral replication of SARS-CoV in infected host cells. In this study, we screened a natural product library consisting of 720 compounds for inhibitory activity against 3CLPro. Two compounds in the library were found to be inhibitive: tannic acid (IC50 = 3 μM) and 3-isotheaflavin-3-gallate (TF2B) (IC50 = 7 μM). These two compounds belong to a group of natural polyphenols found in tea. We further investigated the 3CLPro-inhibitory activity of extracts from several different types of teas, including green tea, oolong tea, Puer tea and black tea. Our results indicated that extracts from Puer and black tea were more potent than that from green or oolong teas in their inhibitory activities against 3CLPro. Several other known compositions in teas were also evaluated for their activities in inhibiting 3CLPro. We found that caffeine, (-)-epigallocatechin gallte (EGCg), epicatechin (EC), theophylline (TP), catechin (C), epicatechin gallate (ECg) and epigallocatechin (EGC) did not inhibit 3CLPro activity. Only theaflavin-3,3′-digallate (TF3) was found to be a 3CLPro inhibitor. This study has resulted in the identification of new compounds that are effective 3CLPro inhibitors.

AB - SARS-CoV is the causative agent of severe acute respiratory syndrome (SARS). The virally encoded 3C-like protease (3CLPro) has been presumed critical for the viral replication of SARS-CoV in infected host cells. In this study, we screened a natural product library consisting of 720 compounds for inhibitory activity against 3CLPro. Two compounds in the library were found to be inhibitive: tannic acid (IC50 = 3 μM) and 3-isotheaflavin-3-gallate (TF2B) (IC50 = 7 μM). These two compounds belong to a group of natural polyphenols found in tea. We further investigated the 3CLPro-inhibitory activity of extracts from several different types of teas, including green tea, oolong tea, Puer tea and black tea. Our results indicated that extracts from Puer and black tea were more potent than that from green or oolong teas in their inhibitory activities against 3CLPro. Several other known compositions in teas were also evaluated for their activities in inhibiting 3CLPro. We found that caffeine, (-)-epigallocatechin gallte (EGCg), epicatechin (EC), theophylline (TP), catechin (C), epicatechin gallate (ECg) and epigallocatechin (EGC) did not inhibit 3CLPro activity. Only theaflavin-3,3′-digallate (TF3) was found to be a 3CLPro inhibitor. This study has resulted in the identification of new compounds that are effective 3CLPro inhibitors.

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Inhibition of SARS-CoV 3C-like protease activity by theaflavin-3,3′- digallate (TF3)

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