Biflavonoids of Dacrydium balansae with Potent Inhibitory Activity on Dengue 2 NS5 Polymerase
Identifieur interne : 000186 ( France/Analysis ); précédent : 000185; suivant : 000187Biflavonoids of Dacrydium balansae with Potent Inhibitory Activity on Dengue 2 NS5 Polymerase
Auteurs : Paul Coulerie [France] ; Cécilia Eydoux [France] ; Edouard Hnawia [France] ; Laetttia Stuhl [France] ; Alexandre Maciuk [France] ; Nicolas Lebouvier [France] ; Bruno Canard [France] ; Bruno Figadere [France] ; Jean-Claude Guillemot [France] ; Mohammed Nour [France]Source :
- Planta medica [ 0032-0943 ] ; 2012.
Descripteurs français
- Pascal (Inist)
- Wicri :
- topic : Plante médicinale.
English descriptors
- KwdEn :
Abstract
In order to find new molecules for antiviral drug design, we screened 102 ethyl acetate extracts from New-Caledonian flora for antiviral activity against the dengue 2 virus RNA-dependant RNA polymerase (DV-NS5 RdRp). The leaf extract of Dacrydium balansae, which strongly inhibited the DV-NS5, was submitted to bioguided fractionation. Four biflavonoids (1-4), three sterols (5-7), and two stilbene derivatives (8-9) were identified and evaluated for their antiviral potential on the DV-NS5 RdRp. Biflavonoids appeared to be potent inhibitors of DV-NS5 RdRp with IC50s between 0.26 and 3.12 uM. Inhibitory activity evaluations against the RNA polymerase from other Flaviviridae viruses allowed us to conclude that these compounds are specific inhibitors of the DV RNA polymerase. The strongest inhibitions were observed with hinokiflavone (4), but podocarpusflavone A (2) is the strongest noncytotoxic inhibitor of the DV-NS5 and it also displayed polymerase inhibitory activity in a DV replicon. A preliminary structure-activity relationship study (SARs) revealed the necessity of the biflavonoid skeleton, the influence of number and position of methoxylations, and the importance of a free rotation of the linkage between the two apigenin monomers of the biflavonoids. To the best of our knowledge, podocarpusflavone A (2) is the strongest noncytotoxic non-nucleotide molecule exhibiting a specific inhibitory activity against the RNA polymerase domain of DV-NS5 and thus is promising for chemotherapy development against dengue fever.
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream PascalFrancis, to step Corpus: 000063
- to stream PascalFrancis, to step Curation: 000924
- to stream PascalFrancis, to step Checkpoint: 000068
- to stream Main, to step Merge: 002019
- to stream Main, to step Curation: 001F93
- to stream Main, to step Exploration: 001F93
- to stream France, to step Extraction: 000186
Links to Exploration step
Pascal:12-0212137Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en" level="a">Biflavonoids of Dacrydium balansae with Potent Inhibitory Activity on Dengue 2 NS5 Polymerase</title>
<author><name sortKey="Coulerie, Paul" sort="Coulerie, Paul" uniqKey="Coulerie P" first="Paul" last="Coulerie">Paul Coulerie</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Eydoux, Cecilia" sort="Eydoux, Cecilia" uniqKey="Eydoux C" first="Cécilia" last="Eydoux">Cécilia Eydoux</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Hnawia, Edouard" sort="Hnawia, Edouard" uniqKey="Hnawia E" first="Edouard" last="Hnawia">Edouard Hnawia</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Stuhl, Laetttia" sort="Stuhl, Laetttia" uniqKey="Stuhl L" first="Laetttia" last="Stuhl">Laetttia Stuhl</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Maciuk, Alexandre" sort="Maciuk, Alexandre" uniqKey="Maciuk A" first="Alexandre" last="Maciuk">Alexandre Maciuk</name>
<affiliation wicri:level="1"><inist:fA14 i1="03"><s1>Laboratoire de Pharmacognosie-Chimie des substances naturelles et chimiothérapies antiparasitaires, UMR CNRS 8076 BioCIS, Université Paris-Sud XI, Clément</s1>
<s2>Châtenay-Malabry</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>8 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
<wicri:noRegion>Clément</wicri:noRegion>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Lebouvier, Nicolas" sort="Lebouvier, Nicolas" uniqKey="Lebouvier N" first="Nicolas" last="Lebouvier">Nicolas Lebouvier</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Canard, Bruno" sort="Canard, Bruno" uniqKey="Canard B" first="Bruno" last="Canard">Bruno Canard</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Figadere, Bruno" sort="Figadere, Bruno" uniqKey="Figadere B" first="Bruno" last="Figadere">Bruno Figadere</name>
<affiliation wicri:level="1"><inist:fA14 i1="03"><s1>Laboratoire de Pharmacognosie-Chimie des substances naturelles et chimiothérapies antiparasitaires, UMR CNRS 8076 BioCIS, Université Paris-Sud XI, Clément</s1>
<s2>Châtenay-Malabry</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>8 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
<wicri:noRegion>Clément</wicri:noRegion>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Guillemot, Jean Claude" sort="Guillemot, Jean Claude" uniqKey="Guillemot J" first="Jean-Claude" last="Guillemot">Jean-Claude Guillemot</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Nour, Mohammed" sort="Nour, Mohammed" uniqKey="Nour M" first="Mohammed" last="Nour">Mohammed Nour</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">INIST</idno>
<idno type="inist">12-0212137</idno>
<date when="2012">2012</date>
<idno type="stanalyst">PASCAL 12-0212137 INIST</idno>
<idno type="RBID">Pascal:12-0212137</idno>
<idno type="wicri:Area/PascalFrancis/Corpus">000063</idno>
<idno type="wicri:Area/PascalFrancis/Curation">000924</idno>
<idno type="wicri:Area/PascalFrancis/Checkpoint">000068</idno>
<idno type="wicri:explorRef" wicri:stream="PascalFrancis" wicri:step="Checkpoint">000068</idno>
<idno type="wicri:doubleKey">0032-0943:2012:Coulerie P:biflavonoids:of:dacrydium</idno>
<idno type="wicri:Area/Main/Merge">002019</idno>
<idno type="wicri:Area/Main/Curation">001F93</idno>
<idno type="wicri:Area/Main/Exploration">001F93</idno>
<idno type="wicri:Area/France/Extraction">000186</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a">Biflavonoids of Dacrydium balansae with Potent Inhibitory Activity on Dengue 2 NS5 Polymerase</title>
<author><name sortKey="Coulerie, Paul" sort="Coulerie, Paul" uniqKey="Coulerie P" first="Paul" last="Coulerie">Paul Coulerie</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Eydoux, Cecilia" sort="Eydoux, Cecilia" uniqKey="Eydoux C" first="Cécilia" last="Eydoux">Cécilia Eydoux</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Hnawia, Edouard" sort="Hnawia, Edouard" uniqKey="Hnawia E" first="Edouard" last="Hnawia">Edouard Hnawia</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Stuhl, Laetttia" sort="Stuhl, Laetttia" uniqKey="Stuhl L" first="Laetttia" last="Stuhl">Laetttia Stuhl</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Maciuk, Alexandre" sort="Maciuk, Alexandre" uniqKey="Maciuk A" first="Alexandre" last="Maciuk">Alexandre Maciuk</name>
<affiliation wicri:level="1"><inist:fA14 i1="03"><s1>Laboratoire de Pharmacognosie-Chimie des substances naturelles et chimiothérapies antiparasitaires, UMR CNRS 8076 BioCIS, Université Paris-Sud XI, Clément</s1>
<s2>Châtenay-Malabry</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>8 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
<wicri:noRegion>Clément</wicri:noRegion>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Lebouvier, Nicolas" sort="Lebouvier, Nicolas" uniqKey="Lebouvier N" first="Nicolas" last="Lebouvier">Nicolas Lebouvier</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Canard, Bruno" sort="Canard, Bruno" uniqKey="Canard B" first="Bruno" last="Canard">Bruno Canard</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Figadere, Bruno" sort="Figadere, Bruno" uniqKey="Figadere B" first="Bruno" last="Figadere">Bruno Figadere</name>
<affiliation wicri:level="1"><inist:fA14 i1="03"><s1>Laboratoire de Pharmacognosie-Chimie des substances naturelles et chimiothérapies antiparasitaires, UMR CNRS 8076 BioCIS, Université Paris-Sud XI, Clément</s1>
<s2>Châtenay-Malabry</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>8 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
<wicri:noRegion>Clément</wicri:noRegion>
<wicri:noRegion>Châtenay-Malabry</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Guillemot, Jean Claude" sort="Guillemot, Jean Claude" uniqKey="Guillemot J" first="Jean-Claude" last="Guillemot">Jean-Claude Guillemot</name>
<affiliation wicri:level="4"><inist:fA14 i1="02"><s1>AFMB, UMR 6098, Aix-Marseille Université, Campus de Luminy</s1>
<s2>Marseille</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Provence-Alpes-Côte d'Azur</region>
<region type="old region">Provence-Alpes-Côte d'Azur</region>
<settlement type="city">Marseille</settlement>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
</affiliation>
</author>
<author><name sortKey="Nour, Mohammed" sort="Nour, Mohammed" uniqKey="Nour M" first="Mohammed" last="Nour">Mohammed Nour</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>France</country>
<wicri:noRegion>Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
<wicri:noRegion>Laboratoire Insulaire du Vivant et de l'Environnement, Université de la Nouvelle-Caledonie, Nouméa Cedex- Nouvelle-Calédonie</wicri:noRegion>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">Planta medica</title>
<title level="j" type="abbreviated">Planta med.</title>
<idno type="ISSN">0032-0943</idno>
<imprint><date when="2012">2012</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><title level="j" type="main">Planta medica</title>
<title level="j" type="abbreviated">Planta med.</title>
<idno type="ISSN">0032-0943</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Coniferales</term>
<term>Dengue 2</term>
<term>Dengue virus</term>
<term>Flavonoid</term>
<term>Medicinal plant</term>
<term>Pharmacognosy</term>
<term>Plant origin</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Flavonoïde</term>
<term>Dengue 2</term>
<term>Coniferales</term>
<term>Virus dengue</term>
<term>Pharmacognosie</term>
<term>Plante médicinale</term>
<term>Origine végétale</term>
<term>Podocarpaceae</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 order to find new molecules for antiviral drug design, we screened 102 ethyl acetate extracts from New-Caledonian flora for antiviral activity against the dengue 2 virus RNA-dependant RNA polymerase (DV-NS5 RdRp). The leaf extract of Dacrydium balansae, which strongly inhibited the DV-NS5, was submitted to bioguided fractionation. Four biflavonoids (1-4), three sterols (5-7), and two stilbene derivatives (8-9) were identified and evaluated for their antiviral potential on the DV-NS5 RdRp. Biflavonoids appeared to be potent inhibitors of DV-NS5 RdRp with IC<sub>50</sub>
s between 0.26 and 3.12 uM. Inhibitory activity evaluations against the RNA polymerase from other Flaviviridae viruses allowed us to conclude that these compounds are specific inhibitors of the DV RNA polymerase. The strongest inhibitions were observed with hinokiflavone (4), but podocarpusflavone A (2) is the strongest noncytotoxic inhibitor of the DV-NS5 and it also displayed polymerase inhibitory activity in a DV replicon. A preliminary structure-activity relationship study (SARs) revealed the necessity of the biflavonoid skeleton, the influence of number and position of methoxylations, and the importance of a free rotation of the linkage between the two apigenin monomers of the biflavonoids. To the best of our knowledge, podocarpusflavone A (2) is the strongest noncytotoxic non-nucleotide molecule exhibiting a specific inhibitory activity against the RNA polymerase domain of DV-NS5 and thus is promising for chemotherapy development against dengue fever.</div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
</country>
<region><li>Provence-Alpes-Côte d'Azur</li>
</region>
<settlement><li>Marseille</li>
</settlement>
<orgName><li>Université d'Aix-Marseille</li>
</orgName>
</list>
<tree><country name="France"><noRegion><name sortKey="Coulerie, Paul" sort="Coulerie, Paul" uniqKey="Coulerie P" first="Paul" last="Coulerie">Paul Coulerie</name>
</noRegion>
<name sortKey="Canard, Bruno" sort="Canard, Bruno" uniqKey="Canard B" first="Bruno" last="Canard">Bruno Canard</name>
<name sortKey="Eydoux, Cecilia" sort="Eydoux, Cecilia" uniqKey="Eydoux C" first="Cécilia" last="Eydoux">Cécilia Eydoux</name>
<name sortKey="Figadere, Bruno" sort="Figadere, Bruno" uniqKey="Figadere B" first="Bruno" last="Figadere">Bruno Figadere</name>
<name sortKey="Guillemot, Jean Claude" sort="Guillemot, Jean Claude" uniqKey="Guillemot J" first="Jean-Claude" last="Guillemot">Jean-Claude Guillemot</name>
<name sortKey="Hnawia, Edouard" sort="Hnawia, Edouard" uniqKey="Hnawia E" first="Edouard" last="Hnawia">Edouard Hnawia</name>
<name sortKey="Lebouvier, Nicolas" sort="Lebouvier, Nicolas" uniqKey="Lebouvier N" first="Nicolas" last="Lebouvier">Nicolas Lebouvier</name>
<name sortKey="Maciuk, Alexandre" sort="Maciuk, Alexandre" uniqKey="Maciuk A" first="Alexandre" last="Maciuk">Alexandre Maciuk</name>
<name sortKey="Nour, Mohammed" sort="Nour, Mohammed" uniqKey="Nour M" first="Mohammed" last="Nour">Mohammed Nour</name>
<name sortKey="Stuhl, Laetttia" sort="Stuhl, Laetttia" uniqKey="Stuhl L" first="Laetttia" last="Stuhl">Laetttia Stuhl</name>
</country>
</tree>
</affiliations>
</record>
Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/SrasV1/Data/France/Analysis
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000186 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/France/Analysis/biblio.hfd -nk 000186 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien |wiki= Sante |area= SrasV1 |flux= France |étape= Analysis |type= RBID |clé= Pascal:12-0212137 |texte= Biflavonoids of Dacrydium balansae with Potent Inhibitory Activity on Dengue 2 NS5 Polymerase }}
This area was generated with Dilib version V0.6.33. |