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Anti-SARS coronavirus 3C-like protease effects of Isatis indigotica root and plant-derived phenolic compounds

Identifieur interne : 004E76 ( Main/Exploration ); précédent : 004E75; suivant : 004E77

Anti-SARS coronavirus 3C-like protease effects of Isatis indigotica root and plant-derived phenolic compounds

Auteurs : Cheng-Wen Lin [Taïwan] ; Fuu-Jen Tsai [Taïwan] ; Chang-Hai Tsai [Taïwan] ; Chien-Chen Lai [Taïwan] ; LEI WAN [Taïwan] ; Tin-Yun Ho [Taïwan] ; Chang-Chi Hsieh [Taïwan] ; Pei-Dawn Lee Chao [Taïwan]

Source :

RBID : Pascal:05-0472143

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English descriptors

Abstract

The 3C-like protease (3CLpro) of SARS-coronavirus mediates the proteolytic processing of replicase polypeptides 1a and 1ab into functional proteins, becoming an important target for the drug development. In this study, Isatis indigotica root extract, five major compounds of I. indigotica root, and seven plant-derived phenolic compounds were tested for anti-SARS-CoV 3CLpro effects using cell-free and cell-based cleavage assays. Cleavage assays with the 3CLpro demonstrated that IC50 values were in micromolar ranges for I. indigotica root extract, indigo, sinigrin, aloe emodin and hesperetin. Sinigrin (IC50: 217 μM) was more efficient in blocking the cleavage processing of the 3CLpro than indigo (IC50: 752 μM) and beta-sitosterol (IC50: 1210 μM) in the cell-based assay. Only two phenolic compounds aloe emodin and hesperetin dose-dependently inhibited cleavage activity of the 3CLpro, in which the IC50 was 366 μM for aloe emodin and 8.3 μM for hesperetin in the cell-based assay.


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Le document en format XML

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<name sortKey="Lai, Chien Chen" sort="Lai, Chien Chen" uniqKey="Lai C" first="Chien-Chen" last="Lai">Chien-Chen Lai</name>
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</author>
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<name sortKey="Chao, Pei Dawn Lee" sort="Chao, Pei Dawn Lee" uniqKey="Chao P" first="Pei-Dawn Lee" last="Chao">Pei-Dawn Lee Chao</name>
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<title level="j" type="main">Antiviral research</title>
<title level="j" type="abbreviated">Antivir. res.</title>
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<keywords scheme="KwdEn" xml:lang="en">
<term>Antiviral</term>
<term>Cruciferae</term>
<term>Peptidases</term>
<term>Phenols</term>
<term>Plant origin</term>
<term>Root</term>
<term>Severe acute respiratory syndrome virus</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr">
<term>Virus syndrome respiratoire aigu sévère</term>
<term>Peptidases</term>
<term>Racine</term>
<term>Antiviral</term>
<term>Origine végétale</term>
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<div type="abstract" xml:lang="en">The 3C-like protease (3CL
<sup>pro</sup>
) of SARS-coronavirus mediates the proteolytic processing of replicase polypeptides 1a and 1ab into functional proteins, becoming an important target for the drug development. In this study, Isatis indigotica root extract, five major compounds of I. indigotica root, and seven plant-derived phenolic compounds were tested for anti-SARS-CoV 3CL
<sup>pro</sup>
effects using cell-free and cell-based cleavage assays. Cleavage assays with the 3CL
<sup>pro</sup>
demonstrated that IC
<sub>50</sub>
values were in micromolar ranges for I. indigotica root extract, indigo, sinigrin, aloe emodin and hesperetin. Sinigrin (IC
<sub>50</sub>
: 217 μM) was more efficient in blocking the cleavage processing of the 3CL
<sup>pro</sup>
than indigo (IC
<sub>50</sub>
: 752 μM) and beta-sitosterol (IC
<sub>50</sub>
: 1210 μM) in the cell-based assay. Only two phenolic compounds aloe emodin and hesperetin dose-dependently inhibited cleavage activity of the 3CL
<sup>pro</sup>
, in which the IC
<sub>50</sub>
was 366 μM for aloe emodin and 8.3 μM for hesperetin in the cell-based assay.</div>
</front>
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<name sortKey="Lai, Chien Chen" sort="Lai, Chien Chen" uniqKey="Lai C" first="Chien-Chen" last="Lai">Chien-Chen Lai</name>
<name sortKey="Lei Wan" sort="Lei Wan" uniqKey="Lei Wan" last="Lei Wan">LEI WAN</name>
<name sortKey="Lin, Cheng Wen" sort="Lin, Cheng Wen" uniqKey="Lin C" first="Cheng-Wen" last="Lin">Cheng-Wen Lin</name>
<name sortKey="Tsai, Chang Hai" sort="Tsai, Chang Hai" uniqKey="Tsai C" first="Chang-Hai" last="Tsai">Chang-Hai Tsai</name>
<name sortKey="Tsai, Fuu Jen" sort="Tsai, Fuu Jen" uniqKey="Tsai F" first="Fuu-Jen" last="Tsai">Fuu-Jen Tsai</name>
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