SrasV1, Main, Exploration, bibRecord, 001960

Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.

Identifieur interne : 001960 ( Main/Exploration ); précédent : 001959; suivant : 001961

Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.

Auteurs : Ji-Young Park [Corée du Sud] ; Jang Hoon Kim ; Jung Min Kwon ; Hyung-Jun Kwon ; Hyung Jae Jeong ; Young Min Kim ; Doman Kim ; Woo Song Lee ; Young Bae Ryu

Source :

Bioorganic & medicinal chemistry [ 1464-3391 ] ; 2013.

RBID : pubmed:23647823

Descripteurs français

KwdFr :
- Antiviraux (), Antiviraux (isolement et purification), Antiviraux (pharmacologie), Benzofuranes (), Benzofuranes (isolement et purification), Benzofuranes (pharmacologie), Cysteine proteases (métabolisme), Humains, Inhibiteurs de la cystéine protéinase (), Inhibiteurs de la cystéine protéinase (isolement et purification), Inhibiteurs de la cystéine protéinase (pharmacologie), Phaeophyta (), Relation quantitative structure-activité, Simulation de docking moléculaire, Syndrome respiratoire aigu sévère (traitement médicamenteux), Virus du SRAS (), Virus du SRAS (enzymologie).
MESH :
- enzymologie : Virus du SRAS.
- isolement et purification : Antiviraux, Benzofuranes, Inhibiteurs de la cystéine protéinase.
- métabolisme : Cysteine proteases.
- pharmacologie : Antiviraux, Benzofuranes, Inhibiteurs de la cystéine protéinase.
- traitement médicamenteux : Syndrome respiratoire aigu sévère.
- Antiviraux, Benzofuranes, Humains, Inhibiteurs de la cystéine protéinase, Phaeophyta, Relation quantitative structure-activité, Simulation de docking moléculaire, Virus du SRAS.

English descriptors

KwdEn :
- Antiviral Agents (chemistry), Antiviral Agents (isolation & purification), Antiviral Agents (pharmacology), Benzofurans (chemistry), Benzofurans (isolation & purification), Benzofurans (pharmacology), Cysteine Proteases (metabolism), Cysteine Proteinase Inhibitors (chemistry), Cysteine Proteinase Inhibitors (isolation & purification), Cysteine Proteinase Inhibitors (pharmacology), Humans, Molecular Docking Simulation, Phaeophyta (chemistry), Quantitative Structure-Activity Relationship, SARS Virus (drug effects), SARS Virus (enzymology), Severe Acute Respiratory Syndrome (drug therapy).
MESH :
- chemical , chemistry : Antiviral Agents, Benzofurans, Cysteine Proteinase Inhibitors.
- chemical , isolation & purification : Antiviral Agents, Benzofurans, Cysteine Proteinase Inhibitors.
- chemical , metabolism : Cysteine Proteases.
- chemical , pharmacology : Antiviral Agents, Benzofurans, Cysteine Proteinase Inhibitors.
- chemistry : Phaeophyta.
- drug effects : SARS Virus.
- drug therapy : Severe Acute Respiratory Syndrome.
- enzymology : SARS Virus.
- Humans, Molecular Docking Simulation, Quantitative Structure-Activity Relationship.

Abstract

SARS-CoV 3CL(pro) plays an important role in viral replication. In this study, we performed a biological evaluation on nine phlorotannins isolated from the edible brown algae Ecklonia cava. The nine isolated phlorotannins (1-9), except phloroglucinol (1), possessed SARS-CoV 3CL(pro) inhibitory activities in a dose-dependently and competitive manner. Of these phlorotannins (1-9), two eckol groups with a diphenyl ether linked dieckol (8) showed the most potent SARS-CoV 3CL(pro) trans/cis-cleavage inhibitory effects (IC(50)s = 2.7 and 68.1 μM, respectively). This is the first report of a (8) phlorotannin chemotype significantly blocking the cleavage of SARS-CoV 3CL(pro) in a cell-based assay with no toxicity. Furthermore, dieckol (8) exhibited a high association rate in the SPR sensorgram and formed extremely strong hydrogen bonds to the catalytic dyad (Cys145 and His41) of the SARS-CoV 3CL(pro).

DOI: 10.1016/j.bmc.2013.04.026
PubMed: 23647823

Affiliations:

Corée du Sud

Le document en format XML

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<affiliation wicri:level="1"><nlm:affiliation>Infection Control Research Center, Korea Research Institute of Bioscience and Biotechnology, Jeongeup 580-185, Republic of Korea.</nlm:affiliation>
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<author><name sortKey="Kim, Jang Hoon" sort="Kim, Jang Hoon" uniqKey="Kim J" first="Jang Hoon" last="Kim">Jang Hoon Kim</name>
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<author><name sortKey="Kwon, Jung Min" sort="Kwon, Jung Min" uniqKey="Kwon J" first="Jung Min" last="Kwon">Jung Min Kwon</name>
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<author><name sortKey="Kwon, Hyung Jun" sort="Kwon, Hyung Jun" uniqKey="Kwon H" first="Hyung-Jun" last="Kwon">Hyung-Jun Kwon</name>
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<author><name sortKey="Jeong, Hyung Jae" sort="Jeong, Hyung Jae" uniqKey="Jeong H" first="Hyung Jae" last="Jeong">Hyung Jae Jeong</name>
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<author><name sortKey="Kim, Young Min" sort="Kim, Young Min" uniqKey="Kim Y" first="Young Min" last="Kim">Young Min Kim</name>
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<author><name sortKey="Kim, Doman" sort="Kim, Doman" uniqKey="Kim D" first="Doman" last="Kim">Doman Kim</name>
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<author><name sortKey="Lee, Woo Song" sort="Lee, Woo Song" uniqKey="Lee W" first="Woo Song" last="Lee">Woo Song Lee</name>
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<author><name sortKey="Ryu, Young Bae" sort="Ryu, Young Bae" uniqKey="Ryu Y" first="Young Bae" last="Ryu">Young Bae Ryu</name>
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<author><name sortKey="Kim, Doman" sort="Kim, Doman" uniqKey="Kim D" first="Doman" last="Kim">Doman Kim</name>
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<author><name sortKey="Lee, Woo Song" sort="Lee, Woo Song" uniqKey="Lee W" first="Woo Song" last="Lee">Woo Song Lee</name>
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<term>Antiviral Agents (isolation & purification)</term>
<term>Antiviral Agents (pharmacology)</term>
<term>Benzofurans (chemistry)</term>
<term>Benzofurans (isolation & purification)</term>
<term>Benzofurans (pharmacology)</term>
<term>Cysteine Proteases (metabolism)</term>
<term>Cysteine Proteinase Inhibitors (chemistry)</term>
<term>Cysteine Proteinase Inhibitors (isolation & purification)</term>
<term>Cysteine Proteinase Inhibitors (pharmacology)</term>
<term>Humans</term>
<term>Molecular Docking Simulation</term>
<term>Phaeophyta (chemistry)</term>
<term>Quantitative Structure-Activity Relationship</term>
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<term>SARS Virus (enzymology)</term>
<term>Severe Acute Respiratory Syndrome (drug therapy)</term>
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<term>Antiviraux (pharmacologie)</term>
<term>Benzofuranes ()</term>
<term>Benzofuranes (isolement et purification)</term>
<term>Benzofuranes (pharmacologie)</term>
<term>Cysteine proteases (métabolisme)</term>
<term>Humains</term>
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<term>Inhibiteurs de la cystéine protéinase (isolement et purification)</term>
<term>Inhibiteurs de la cystéine protéinase (pharmacologie)</term>
<term>Phaeophyta ()</term>
<term>Relation quantitative structure-activité</term>
<term>Simulation de docking moléculaire</term>
<term>Syndrome respiratoire aigu sévère (traitement médicamenteux)</term>
<term>Virus du SRAS ()</term>
<term>Virus du SRAS (enzymologie)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antiviral Agents</term>
<term>Benzofurans</term>
<term>Cysteine Proteinase Inhibitors</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="isolation & purification" xml:lang="en"><term>Antiviral Agents</term>
<term>Benzofurans</term>
<term>Cysteine Proteinase Inhibitors</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Cysteine Proteases</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term>
<term>Benzofurans</term>
<term>Cysteine Proteinase Inhibitors</term>
</keywords>
<keywords scheme="MESH" qualifier="chemistry" xml:lang="en"><term>Phaeophyta</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>SARS Virus</term>
</keywords>
<keywords scheme="MESH" qualifier="drug therapy" xml:lang="en"><term>Severe Acute Respiratory Syndrome</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="isolement et purification" xml:lang="fr"><term>Antiviraux</term>
<term>Benzofuranes</term>
<term>Inhibiteurs de la cystéine protéinase</term>
</keywords>
<keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Cysteine proteases</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term>
<term>Benzofuranes</term>
<term>Inhibiteurs de la cystéine protéinase</term>
</keywords>
<keywords scheme="MESH" qualifier="traitement médicamenteux" xml:lang="fr"><term>Syndrome respiratoire aigu sévère</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Humans</term>
<term>Molecular Docking Simulation</term>
<term>Quantitative Structure-Activity Relationship</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Antiviraux</term>
<term>Benzofuranes</term>
<term>Humains</term>
<term>Inhibiteurs de la cystéine protéinase</term>
<term>Phaeophyta</term>
<term>Relation quantitative structure-activité</term>
<term>Simulation de docking moléculaire</term>
<term>Virus du SRAS</term>
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<front><div type="abstract" xml:lang="en">SARS-CoV 3CL(pro) plays an important role in viral replication. In this study, we performed a biological evaluation on nine phlorotannins isolated from the edible brown algae Ecklonia cava. The nine isolated phlorotannins (1-9), except phloroglucinol (1), possessed SARS-CoV 3CL(pro) inhibitory activities in a dose-dependently and competitive manner. Of these phlorotannins (1-9), two eckol groups with a diphenyl ether linked dieckol (8) showed the most potent SARS-CoV 3CL(pro) trans/cis-cleavage inhibitory effects (IC(50)s = 2.7 and 68.1 μM, respectively). This is the first report of a (8) phlorotannin chemotype significantly blocking the cleavage of SARS-CoV 3CL(pro) in a cell-based assay with no toxicity. Furthermore, dieckol (8) exhibited a high association rate in the SPR sensorgram and formed extremely strong hydrogen bonds to the catalytic dyad (Cys145 and His41) of the SARS-CoV 3CL(pro).</div>
</front>
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<name sortKey="Kim, Jang Hoon" sort="Kim, Jang Hoon" uniqKey="Kim J" first="Jang Hoon" last="Kim">Jang Hoon Kim</name>
<name sortKey="Kim, Young Min" sort="Kim, Young Min" uniqKey="Kim Y" first="Young Min" last="Kim">Young Min Kim</name>
<name sortKey="Kwon, Hyung Jun" sort="Kwon, Hyung Jun" uniqKey="Kwon H" first="Hyung-Jun" last="Kwon">Hyung-Jun Kwon</name>
<name sortKey="Kwon, Jung Min" sort="Kwon, Jung Min" uniqKey="Kwon J" first="Jung Min" last="Kwon">Jung Min Kwon</name>
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Serveur d'exploration SRAS

Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.

Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri

Pour générer des pages wiki

	Serveur d'exploration SRAS
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