Kaempferol derivatives as antiviral drugs against the 3a channel protein of coronavirus.
Identifieur interne : 001625 ( Main/Exploration ); précédent : 001624; suivant : 001626Kaempferol derivatives as antiviral drugs against the 3a channel protein of coronavirus.
Auteurs : Silvia Schwarz [République populaire de Chine] ; Daniel Sauter [République populaire de Chine] ; Kai Wang [République populaire de Chine] ; Ronghua Zhang [République populaire de Chine] ; Bing Sun [République populaire de Chine] ; Anastasia Karioti [Italie] ; Anna Rita Bilia [Italie] ; Thomas Efferth [Allemagne] ; Wolfgang Schwarz [République populaire de Chine]Source :
- Planta medica [ 1439-0221 ] ; 2014.
Descripteurs français
- KwdFr :
- MESH :
- antagonistes et inhibiteurs : Protéines virales.
- métabolisme : Protéines virales.
- pharmacologie : Antiviraux, Kaempférols.
- Animaux, Antiviraux, Kaempférols, Protéines virales, Techniques de patch-clamp, Virus du SRAS, Xenopus.
English descriptors
- KwdEn :
- MESH :
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemistry : Antiviral Agents, Kaempferols, Viral Proteins.
- chemical , metabolism : Viral Proteins.
- chemical , pharmacology : Antiviral Agents, Kaempferols.
- Animals, Patch-Clamp Techniques, SARS Virus, Xenopus.
Abstract
The protein coded by the open-reading-frame 3a of SARS coronavirus has been demonstrated to form a cation-selective channel that may become expressed in the infected cell. The activity of the channel is involved in the mechanism of virus release. Drugs that inhibit the ion channel can, therefore, inhibit virus release, and they could be a source for development of novel therapeutic antiviral agents. Various drugs found in Chinese herbs that are well known as anticancer agents also have an antiviral potency. Here we tested the flavonols kaempferol, kaempferol glycosides, and acylated kaempferol glucoside derivatives with respect to their potency to block the 3a channel. We used the Xenopus oocyte with a heterologously expressed 3a protein as a model system to test the efficacy of the flavonols. Some of these drugs turned out to be potent inhibitors of the 3a channel. The most effective one was the glycoside juglanin (carrying an arabinose residue) with an IC50 value of 2.3 µM for inhibition of the 3a-mediated current. Kaempferol derivatives with rhamnose residue also seem to be quite effective. We suggest that viral ion channels, in general, may be a good target for the development of antiviral agents, and that, in particular, kaempferol glycosides are good candidates for 3a channel proteins of coronaviruses.
DOI: 10.1055/s-0033-1360277
PubMed: 24458263
Affiliations:
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type="city">Mayence</settlement></placeName></affiliation></author><author><name sortKey="Schwarz, Wolfgang" sort="Schwarz, Wolfgang" uniqKey="Schwarz W" first="Wolfgang" last="Schwarz">Wolfgang Schwarz</name><affiliation wicri:level="1"><nlm:affiliation>Shanghai Research Center for Acupuncture & Meridians, Shanghai, China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Shanghai Research Center for Acupuncture & Meridians, Shanghai</wicri:regionArea><wicri:noRegion>Shanghai</wicri:noRegion></affiliation></author></analytic><series><title level="j">Planta medica</title><idno type="eISSN">1439-0221</idno><imprint><date when="2014" type="published">2014</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (pharmacology)</term><term>Kaempferols (chemistry)</term><term>Kaempferols 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type="chemical" qualifier="metabolism" xml:lang="en"><term>Viral Proteins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term><term>Kaempferols</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Protéines virales</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Protéines virales</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term><term>Kaempférols</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Patch-Clamp Techniques</term><term>SARS Virus</term><term>Xenopus</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Antiviraux</term><term>Kaempférols</term><term>Protéines virales</term><term>Techniques de patch-clamp</term><term>Virus du SRAS</term><term>Xenopus</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The protein coded by the open-reading-frame 3a of SARS coronavirus has been demonstrated to form a cation-selective channel that may become expressed in the infected cell. The activity of the channel is involved in the mechanism of virus release. Drugs that inhibit the ion channel can, therefore, inhibit virus release, and they could be a source for development of novel therapeutic antiviral agents. Various drugs found in Chinese herbs that are well known as anticancer agents also have an antiviral potency. Here we tested the flavonols kaempferol, kaempferol glycosides, and acylated kaempferol glucoside derivatives with respect to their potency to block the 3a channel. We used the Xenopus oocyte with a heterologously expressed 3a protein as a model system to test the efficacy of the flavonols. Some of these drugs turned out to be potent inhibitors of the 3a channel. The most effective one was the glycoside juglanin (carrying an arabinose residue) with an IC50 value of 2.3 µM for inhibition of the 3a-mediated current. Kaempferol derivatives with rhamnose residue also seem to be quite effective. We suggest that viral ion channels, in general, may be a good target for the development of antiviral agents, and that, in particular, kaempferol glycosides are good candidates for 3a channel proteins of coronaviruses. </div></front></TEI><affiliations><list><country><li>Allemagne</li><li>Italie</li><li>République populaire de Chine</li></country><region><li>Rhénanie-Palatinat</li></region><settlement><li>Mayence</li></settlement></list><tree><country name="République populaire de Chine"><noRegion><name sortKey="Schwarz, Silvia" sort="Schwarz, Silvia" uniqKey="Schwarz S" first="Silvia" last="Schwarz">Silvia Schwarz</name></noRegion><name sortKey="Sauter, Daniel" sort="Sauter, Daniel" uniqKey="Sauter D" first="Daniel" last="Sauter">Daniel Sauter</name><name sortKey="Schwarz, Wolfgang" sort="Schwarz, Wolfgang" uniqKey="Schwarz W" first="Wolfgang" last="Schwarz">Wolfgang Schwarz</name><name sortKey="Sun, Bing" sort="Sun, Bing" uniqKey="Sun B" first="Bing" last="Sun">Bing Sun</name><name sortKey="Wang, Kai" sort="Wang, Kai" uniqKey="Wang K" first="Kai" last="Wang">Kai Wang</name><name sortKey="Zhang, Ronghua" sort="Zhang, Ronghua" uniqKey="Zhang R" first="Ronghua" last="Zhang">Ronghua Zhang</name></country><country name="Italie"><noRegion><name sortKey="Karioti, Anastasia" sort="Karioti, Anastasia" uniqKey="Karioti A" first="Anastasia" last="Karioti">Anastasia Karioti</name></noRegion><name sortKey="Bilia, Anna Rita" sort="Bilia, Anna Rita" uniqKey="Bilia A" first="Anna Rita" last="Bilia">Anna Rita Bilia</name></country><country name="Allemagne"><region name="Rhénanie-Palatinat"><name sortKey="Efferth, Thomas" sort="Efferth, Thomas" uniqKey="Efferth T" first="Thomas" last="Efferth">Thomas Efferth</name></region></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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