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Specific plant terpenoids and lignoids possess potent antiviral activities against severe acute respiratory syndrome coronavirus

Identifieur interne : 003B23 ( Main/Exploration ); précédent : 003B22; suivant : 003B24

Specific plant terpenoids and lignoids possess potent antiviral activities against severe acute respiratory syndrome coronavirus

Auteurs : Chih-Chun Wen [Taïwan] ; Yueh-Hsiung Kuo [Taïwan] ; Jia-Tsrong Jan [Taïwan] ; Po-Huang Liang [Taïwan] ; Sheng-Yang Wang [Taïwan] ; Hong-Gi Liu [Taïwan] ; Ching-Kuo Lee [Taïwan] ; Shang-Tzen Chang [Taïwan] ; Chih-Jung Kuo [Taïwan] ; Shoei-Sheng Lee [Taïwan] ; Chia-Chung Hou [Taïwan] ; Pei-Wen Hsiao [Taïwan] ; Shih-Chang Chien [Taïwan] ; Lie-Fen Shyur [Taïwan] ; Ning-Sun Yang [Taïwan]

Source :

RBID : Pascal:08-0038597

Descripteurs français

English descriptors

Abstract

In this study, 221 phytocompounds were evaluated for activity against anti-severe acute respiratory syndrome associated coronavirus (SARS-CoV) activities using a cell-based assay measuring SARS-CoV-induced cytopathogenic effect on Vero E6 cells. Ten diterpenoids (1-10), two sesquiterpenoids (11 and 12), two triterpenoids (13 and 14), five lignoids (15-19), curcumin (20), and reference controls niclosamide (21) and valinomycin (22) were potent inhibitors at concentrations between 3.3 and 10 μM. The concentrations of the 22 compounds to inhibit 50% of Vero E6 cell proliferation (CC50) and viral replication (EC50) were measured. The selective index values (SI = CC50/EC50) of the most potent compounds 1, 5, 6, 8, 14, and 16 were 58, >510, 111, 193, 180, and >667, respectively. Betulinic acid (13) and savinin (16) were competitive inhibitors of SARS-CoV 3CL protease with Kí values = 8.2 ± 0.7 and 9.1 ± 2.4 μM, respectively. Our findings suggest that specific abietane-type diterpenoids and lignoids exhibit strong anti-SARS-CoV effects.


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Le document en format XML

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<sZ>11 aut.</sZ>
<sZ>12 aut.</sZ>
<sZ>13 aut.</sZ>
<sZ>14 aut.</sZ>
<sZ>15 aut.</sZ>
</inist:fA14>
<country>Taïwan</country>
<wicri:noRegion>Taipei 115</wicri:noRegion>
</affiliation>
</author>
<author>
<name sortKey="Shyur, Lie Fen" sort="Shyur, Lie Fen" uniqKey="Shyur L" first="Lie-Fen" last="Shyur">Lie-Fen Shyur</name>
<affiliation wicri:level="1">
<inist:fA14 i1="01">
<s1>Agricultural Biotechnology Research Center, Academia Sinica</s1>
<s2>Taipei 115</s2>
<s3>TWN</s3>
<sZ>1 aut.</sZ>
<sZ>11 aut.</sZ>
<sZ>12 aut.</sZ>
<sZ>13 aut.</sZ>
<sZ>14 aut.</sZ>
<sZ>15 aut.</sZ>
</inist:fA14>
<country>Taïwan</country>
<wicri:noRegion>Taipei 115</wicri:noRegion>
</affiliation>
</author>
<author>
<name sortKey="Yang, Ning Sun" sort="Yang, Ning Sun" uniqKey="Yang N" first="Ning-Sun" last="Yang">Ning-Sun Yang</name>
<affiliation wicri:level="1">
<inist:fA14 i1="01">
<s1>Agricultural Biotechnology Research Center, Academia Sinica</s1>
<s2>Taipei 115</s2>
<s3>TWN</s3>
<sZ>1 aut.</sZ>
<sZ>11 aut.</sZ>
<sZ>12 aut.</sZ>
<sZ>13 aut.</sZ>
<sZ>14 aut.</sZ>
<sZ>15 aut.</sZ>
</inist:fA14>
<country>Taïwan</country>
<wicri:noRegion>Taipei 115</wicri:noRegion>
</affiliation>
</author>
</analytic>
<series>
<title level="j" type="main">Journal of medicinal chemistry : (Print)</title>
<title level="j" type="abbreviated">J. med. chem. : (Print)</title>
<idno type="ISSN">0022-2623</idno>
<imprint>
<date when="2007">2007</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt>
<title level="j" type="main">Journal of medicinal chemistry : (Print)</title>
<title level="j" type="abbreviated">J. med. chem. : (Print)</title>
<idno type="ISSN">0022-2623</idno>
</seriesStmt>
</fileDesc>
<profileDesc>
<textClass>
<keywords scheme="KwdEn" xml:lang="en">
<term>Animals</term>
<term>Antiviral</term>
<term>Cell Proliferation (drug effects)</term>
<term>Chlorocebus aethiops</term>
<term>Cysteine Endopeptidases (chemistry)</term>
<term>Enzyme inhibitor</term>
<term>In vitro</term>
<term>Inhibitor enzyme complex</term>
<term>Lignan</term>
<term>Lignans (chemistry)</term>
<term>Medicinal plant</term>
<term>Modeling</term>
<term>Models, Molecular</term>
<term>Molecular model</term>
<term>Natural compound</term>
<term>Peptidases</term>
<term>Pharmacognosy</term>
<term>Plant origin</term>
<term>Plants, Medicinal</term>
<term>Protease inhibitor</term>
<term>SARS Virus (drug effects)</term>
<term>SARS Virus (enzymology)</term>
<term>Severe acute respiratory syndrome virus</term>
<term>Structure activity relation</term>
<term>Structure-Activity Relationship</term>
<term>Terpenes (chemistry)</term>
<term>Terpenes (pharmacology)</term>
<term>Terpenoid</term>
<term>Triterpenes (chemistry)</term>
<term>Vero Cells</term>
<term>Viral Proteins (antagonists & inhibitors)</term>
<term>Viral Proteins (chemistry)</term>
<term>Virus Replication</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr">
<term>Animaux</term>
<term>Cellules Vero</term>
<term>Cysteine endopeptidases ()</term>
<term>Lignanes ()</term>
<term>Modèles moléculaires</term>
<term>Plantes médicinales</term>
<term>Prolifération cellulaire ()</term>
<term>Protéines virales ()</term>
<term>Protéines virales (antagonistes et inhibiteurs)</term>
<term>Relation structure-activité</term>
<term>Réplication virale</term>
<term>Terpènes ()</term>
<term>Terpènes (pharmacologie)</term>
<term>Triterpènes ()</term>
<term>Virus du SRAS ()</term>
<term>Virus du SRAS (enzymologie)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en">
<term>Viral Proteins</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en">
<term>Cysteine Endopeptidases</term>
<term>Lignans</term>
<term>Terpenes</term>
<term>Triterpenes</term>
<term>Viral Proteins</term>
</keywords>
<keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr">
<term>Protéines virales</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en">
<term>Cell Proliferation</term>
<term>SARS Virus</term>
</keywords>
<keywords scheme="MESH" qualifier="enzymologie" xml:lang="fr">
<term>Virus du SRAS</term>
</keywords>
<keywords scheme="MESH" qualifier="enzymology" xml:lang="en">
<term>SARS Virus</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr">
<term>Terpènes</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en">
<term>Terpenes</term>
</keywords>
<keywords scheme="MESH" xml:lang="en">
<term>Animals</term>
<term>Chlorocebus aethiops</term>
<term>Models, Molecular</term>
<term>Plants, Medicinal</term>
<term>Structure-Activity Relationship</term>
<term>Vero Cells</term>
<term>Virus Replication</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr">
<term>Animaux</term>
<term>Cellules Vero</term>
<term>Cysteine endopeptidases</term>
<term>Lignanes</term>
<term>Modèles moléculaires</term>
<term>Origine végétale</term>
<term>Plantes médicinales</term>
<term>Prolifération cellulaire</term>
<term>Protéines virales</term>
<term>Relation structure-activité</term>
<term>Réplication virale</term>
<term>Terpènes</term>
<term>Terpénoïde</term>
<term>Antiviral</term>
<term>Relation structure activité</term>
<term>Triterpènes</term>
<term>Virus du SRAS</term>
<term>Virus syndrome respiratoire aigu sévère</term>
<term>Lignane</term>
<term>Composé naturel</term>
<term>Plante médicinale</term>
<term>Pharmacognosie</term>
<term>Inhibiteur protease</term>
<term>In vitro</term>
<term>Modèle moléculaire</term>
<term>Complexe enzyme inhibiteur</term>
<term>Inhibiteur enzyme</term>
<term>Peptidases</term>
<term>Modélisation</term>
</keywords>
<keywords scheme="Wicri" type="topic" xml:lang="fr">
<term>Plante médicinale</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front>
<div type="abstract" xml:lang="en">In this study, 221 phytocompounds were evaluated for activity against anti-severe acute respiratory syndrome associated coronavirus (SARS-CoV) activities using a cell-based assay measuring SARS-CoV-induced cytopathogenic effect on Vero E6 cells. Ten diterpenoids (1-10), two sesquiterpenoids (11 and 12), two triterpenoids (13 and 14), five lignoids (15-19), curcumin (20), and reference controls niclosamide (21) and valinomycin (22) were potent inhibitors at concentrations between 3.3 and 10 μM. The concentrations of the 22 compounds to inhibit 50% of Vero E6 cell proliferation (CC
<sub>50</sub>
) and viral replication (EC
<sub>50</sub>
) were measured. The selective index values (SI = CC
<sub>50</sub>
/EC
<sub>50</sub>
) of the most potent compounds 1, 5, 6, 8, 14, and 16 were 58, >510, 111, 193, 180, and >667, respectively. Betulinic acid (13) and savinin (16) were competitive inhibitors of SARS-CoV 3CL protease with K
<sub>í</sub>
values = 8.2 ± 0.7 and 9.1 ± 2.4 μM, respectively. Our findings suggest that specific abietane-type diterpenoids and lignoids exhibit strong anti-SARS-CoV effects.</div>
</front>
</TEI>
<affiliations>
<list>
<country>
<li>Taïwan</li>
</country>
</list>
<tree>
<country name="Taïwan">
<noRegion>
<name sortKey="Wen, Chih Chun" sort="Wen, Chih Chun" uniqKey="Wen C" first="Chih-Chun" last="Wen">Chih-Chun Wen</name>
</noRegion>
<name sortKey="Chang, Shang Tzen" sort="Chang, Shang Tzen" uniqKey="Chang S" first="Shang-Tzen" last="Chang">Shang-Tzen Chang</name>
<name sortKey="Chien, Shih Chang" sort="Chien, Shih Chang" uniqKey="Chien S" first="Shih-Chang" last="Chien">Shih-Chang Chien</name>
<name sortKey="Hou, Chia Chung" sort="Hou, Chia Chung" uniqKey="Hou C" first="Chia-Chung" last="Hou">Chia-Chung Hou</name>
<name sortKey="Hsiao, Pei Wen" sort="Hsiao, Pei Wen" uniqKey="Hsiao P" first="Pei-Wen" last="Hsiao">Pei-Wen Hsiao</name>
<name sortKey="Jan, Jia Tsrong" sort="Jan, Jia Tsrong" uniqKey="Jan J" first="Jia-Tsrong" last="Jan">Jia-Tsrong Jan</name>
<name sortKey="Kuo, Chih Jung" sort="Kuo, Chih Jung" uniqKey="Kuo C" first="Chih-Jung" last="Kuo">Chih-Jung Kuo</name>
<name sortKey="Kuo, Yueh Hsiung" sort="Kuo, Yueh Hsiung" uniqKey="Kuo Y" first="Yueh-Hsiung" last="Kuo">Yueh-Hsiung Kuo</name>
<name sortKey="Kuo, Yueh Hsiung" sort="Kuo, Yueh Hsiung" uniqKey="Kuo Y" first="Yueh-Hsiung" last="Kuo">Yueh-Hsiung Kuo</name>
<name sortKey="Lee, Ching Kuo" sort="Lee, Ching Kuo" uniqKey="Lee C" first="Ching-Kuo" last="Lee">Ching-Kuo Lee</name>
<name sortKey="Lee, Shoei Sheng" sort="Lee, Shoei Sheng" uniqKey="Lee S" first="Shoei-Sheng" last="Lee">Shoei-Sheng Lee</name>
<name sortKey="Liang, Po Huang" sort="Liang, Po Huang" uniqKey="Liang P" first="Po-Huang" last="Liang">Po-Huang Liang</name>
<name sortKey="Liu, Hong Gi" sort="Liu, Hong Gi" uniqKey="Liu H" first="Hong-Gi" last="Liu">Hong-Gi Liu</name>
<name sortKey="Shyur, Lie Fen" sort="Shyur, Lie Fen" uniqKey="Shyur L" first="Lie-Fen" last="Shyur">Lie-Fen Shyur</name>
<name sortKey="Wang, Sheng Yang" sort="Wang, Sheng Yang" uniqKey="Wang S" first="Sheng-Yang" last="Wang">Sheng-Yang Wang</name>
<name sortKey="Wen, Chih Chun" sort="Wen, Chih Chun" uniqKey="Wen C" first="Chih-Chun" last="Wen">Chih-Chun Wen</name>
<name sortKey="Yang, Ning Sun" sort="Yang, Ning Sun" uniqKey="Yang N" first="Ning-Sun" last="Yang">Ning-Sun Yang</name>
</country>
</tree>
</affiliations>
</record>

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