Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV.
Identifieur interne : 001071 ( Main/Exploration ); précédent : 001070; suivant : 001072Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV.
Auteurs : Ji-Young Park [Corée du Sud] ; Jin-A Ko [Corée du Sud] ; Dae Wook Kim ; Young Min Kim [Corée du Sud] ; Hyung-Jun Kwon [Corée du Sud] ; Hyung Jae Jeong [Corée du Sud] ; Cha Young Kim [Corée du Sud] ; Ki Hun Park ; Woo Song Lee [Corée du Sud] ; Young Bae Ryu [Corée du Sud]Source :
- Journal of enzyme inhibition and medicinal chemistry [ 1475-6374 ] ; 2016.
Descripteurs français
- KwdFr :
- Angelica (), Antiviraux (), Antiviraux (isolement et purification), Antiviraux (pharmacologie), Chalcones (), Chalcones (isolement et purification), Chalcones (pharmacologie), Cysteine proteases (métabolisme), Inhibiteurs de la cystéine protéinase (), Inhibiteurs de la cystéine protéinase (isolement et purification), Inhibiteurs de la cystéine protéinase (pharmacologie), Relation dose-effet des médicaments, Relation structure-activité, Structure moléculaire, Tests de sensibilité microbienne, Virus du SRAS (), Virus du SRAS (enzymologie).
- MESH :
- enzymologie : Virus du SRAS.
- isolement et purification : Antiviraux, Chalcones, Inhibiteurs de la cystéine protéinase.
- métabolisme : Cysteine proteases.
- pharmacologie : Antiviraux, Chalcones, Inhibiteurs de la cystéine protéinase.
- Angelica, Antiviraux, Chalcones, Inhibiteurs de la cystéine protéinase, Relation dose-effet des médicaments, Relation structure-activité, Structure moléculaire, Tests de sensibilité microbienne, Virus du SRAS.
English descriptors
- KwdEn :
- Angelica (chemistry), Antiviral Agents (chemistry), Antiviral Agents (isolation & purification), Antiviral Agents (pharmacology), Chalcones (chemistry), Chalcones (isolation & purification), Chalcones (pharmacology), Cysteine Proteases (metabolism), Cysteine Proteinase Inhibitors (chemistry), Cysteine Proteinase Inhibitors (isolation & purification), Cysteine Proteinase Inhibitors (pharmacology), Dose-Response Relationship, Drug, Microbial Sensitivity Tests, Molecular Structure, SARS Virus (drug effects), SARS Virus (enzymology), Structure-Activity Relationship.
- MESH :
- chemical , chemistry : Antiviral Agents, Chalcones, Cysteine Proteinase Inhibitors.
- chemistry : Angelica.
- drug effects : SARS Virus.
- enzymology : SARS Virus.
- chemical , isolation & purification : Antiviral Agents, Chalcones, Cysteine Proteinase Inhibitors.
- chemical , metabolism : Cysteine Proteases.
- chemical , pharmacology : Antiviral Agents, Chalcones, Cysteine Proteinase Inhibitors.
- Dose-Response Relationship, Drug, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship.
Abstract
Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) and a papain-like protease (PL(pro)) are attractive targets for the development of anti-SARS drugs. In this study, nine alkylated chalcones (1-9) and four coumarins (10-13) were isolated from Angelica keiskei, and the inhibitory activities of these constituents against SARS-CoV proteases (3CL(pro) and PL(pro)) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PL(pro) inhibitory activity with IC50 values of 11.4 and 1.2 µM. Our detailed protein-inhibitor mechanistic analysis of these species indicated that the chalcones exhibited competitive inhibition characteristics to the SARS-CoV 3CL(pro), whereas noncompetitive inhibition was observed with the SARS-CoV PL(pro).
DOI: 10.3109/14756366.2014.1003215
PubMed: 25683083
Affiliations:
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Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author><author><name sortKey="Ko, Jin A" sort="Ko, Jin A" uniqKey="Ko J" first="Jin-A" last="Ko">Jin-A Ko</name><affiliation wicri:level="1"><nlm:affiliation>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author><author><name sortKey="Kim, Dae Wook" 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Jun" uniqKey="Kwon H" first="Hyung-Jun" last="Kwon">Hyung-Jun Kwon</name><affiliation wicri:level="1"><nlm:affiliation>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author><author><name sortKey="Jeong, Hyung Jae" sort="Jeong, Hyung Jae" uniqKey="Jeong H" first="Hyung Jae" last="Jeong">Hyung Jae Jeong</name><affiliation wicri:level="1"><nlm:affiliation>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author><author><name sortKey="Kim, Cha Young" sort="Kim, Cha Young" uniqKey="Kim C" first="Cha Young" last="Kim">Cha Young Kim</name><affiliation wicri:level="1"><nlm:affiliation>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author><author><name sortKey="Park, Ki Hun" sort="Park, Ki Hun" uniqKey="Park K" first="Ki Hun" last="Park">Ki Hun Park</name><affiliation><nlm:affiliation>b Division of Applied Life Science (BK21 program, IALS) , Graduate School of Gyeongsang National University , Jinju , Republic of Korea , and.</nlm:affiliation><wicri:noCountry code="subField">and</wicri:noCountry></affiliation></author><author><name sortKey="Lee, Woo Song" sort="Lee, Woo Song" uniqKey="Lee W" first="Woo Song" last="Lee">Woo Song Lee</name><affiliation wicri:level="1"><nlm:affiliation>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author><author><name sortKey="Ryu, Young Bae" sort="Ryu, Young Bae" uniqKey="Ryu Y" first="Young Bae" last="Ryu">Young Bae Ryu</name><affiliation wicri:level="1"><nlm:affiliation>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup </wicri:regionArea><wicri:noRegion>Jeongeup </wicri:noRegion></affiliation></author></analytic><series><title level="j">Journal of enzyme inhibition and medicinal chemistry</title><idno type="eISSN">1475-6374</idno><imprint><date when="2016" type="published">2016</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Angelica (chemistry)</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (isolation & purification)</term><term>Antiviral Agents (pharmacology)</term><term>Chalcones (chemistry)</term><term>Chalcones (isolation & purification)</term><term>Chalcones (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>Dose-Response Relationship, Drug</term><term>Microbial Sensitivity Tests</term><term>Molecular Structure</term><term>SARS Virus (drug effects)</term><term>SARS Virus (enzymology)</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Angelica ()</term><term>Antiviraux ()</term><term>Antiviraux (isolement et purification)</term><term>Antiviraux (pharmacologie)</term><term>Chalcones ()</term><term>Chalcones (isolement et purification)</term><term>Chalcones (pharmacologie)</term><term>Cysteine proteases (métabolisme)</term><term>Inhibiteurs de la cystéine protéinase ()</term><term>Inhibiteurs de la cystéine protéinase (isolement et purification)</term><term>Inhibiteurs de la cystéine protéinase (pharmacologie)</term><term>Relation dose-effet des médicaments</term><term>Relation structure-activité</term><term>Structure moléculaire</term><term>Tests de sensibilité microbienne</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>Chalcones</term><term>Cysteine Proteinase Inhibitors</term></keywords><keywords scheme="MESH" qualifier="chemistry" xml:lang="en"><term>Angelica</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><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" type="chemical" qualifier="isolation & purification" xml:lang="en"><term>Antiviral Agents</term><term>Chalcones</term><term>Cysteine Proteinase Inhibitors</term></keywords><keywords scheme="MESH" qualifier="isolement et purification" xml:lang="fr"><term>Antiviraux</term><term>Chalcones</term><term>Inhibiteurs de la cystéine protéinase</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Cysteine Proteases</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>Chalcones</term><term>Inhibiteurs de la cystéine protéinase</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term><term>Chalcones</term><term>Cysteine Proteinase Inhibitors</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Dose-Response Relationship, Drug</term><term>Microbial Sensitivity Tests</term><term>Molecular Structure</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Angelica</term><term>Antiviraux</term><term>Chalcones</term><term>Inhibiteurs de la cystéine protéinase</term><term>Relation dose-effet des médicaments</term><term>Relation structure-activité</term><term>Structure moléculaire</term><term>Tests de sensibilité microbienne</term><term>Virus du SRAS</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) and a papain-like protease (PL(pro)) are attractive targets for the development of anti-SARS drugs. In this study, nine alkylated chalcones (1-9) and four coumarins (10-13) were isolated from Angelica keiskei, and the inhibitory activities of these constituents against SARS-CoV proteases (3CL(pro) and PL(pro)) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PL(pro) inhibitory activity with IC50 values of 11.4 and 1.2 µM. Our detailed protein-inhibitor mechanistic analysis of these species indicated that the chalcones exhibited competitive inhibition characteristics to the SARS-CoV 3CL(pro), whereas noncompetitive inhibition was observed with the SARS-CoV PL(pro). </div></front></TEI><affiliations><list><country><li>Corée du Sud</li></country></list><tree><noCountry><name sortKey="Kim, Dae Wook" sort="Kim, Dae Wook" uniqKey="Kim D" first="Dae Wook" last="Kim">Dae Wook Kim</name><name sortKey="Park, Ki Hun" sort="Park, Ki Hun" uniqKey="Park K" first="Ki Hun" last="Park">Ki Hun Park</name></noCountry><country name="Corée du Sud"><noRegion><name sortKey="Park, Ji Young" sort="Park, Ji Young" uniqKey="Park J" first="Ji-Young" last="Park">Ji-Young Park</name></noRegion><name sortKey="Jeong, Hyung Jae" sort="Jeong, Hyung Jae" uniqKey="Jeong H" first="Hyung Jae" last="Jeong">Hyung Jae Jeong</name><name sortKey="Kim, Cha Young" sort="Kim, Cha Young" uniqKey="Kim C" first="Cha Young" last="Kim">Cha Young 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="Ko, Jin A" sort="Ko, Jin A" uniqKey="Ko J" first="Jin-A" last="Ko">Jin-A Ko</name><name sortKey="Kwon, Hyung Jun" sort="Kwon, Hyung Jun" uniqKey="Kwon H" first="Hyung-Jun" last="Kwon">Hyung-Jun Kwon</name><name sortKey="Lee, Woo Song" sort="Lee, Woo Song" uniqKey="Lee W" first="Woo Song" last="Lee">Woo Song Lee</name><name sortKey="Ryu, Young Bae" sort="Ryu, Young Bae" uniqKey="Ryu Y" first="Young Bae" last="Ryu">Young Bae Ryu</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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