ChloroquineV1, Main, Exploration, bibRecord, 000C23

Novel Peroxides as Promising Anticancer Agents with Unexpected Depressed Antimalarial Activity.

Identifieur interne : 000C23 ( Main/Exploration ); précédent : 000C22; suivant : 000C24

Novel Peroxides as Promising Anticancer Agents with Unexpected Depressed Antimalarial Activity.

Auteurs : Paolo Coghi [République populaire de Chine] ; Ivan A. Yaremenko [Russie] ; Parichat Prommana [Thaïlande] ; Peter S. Radulov [Russie] ; Mikhail A. Syroeshkin [Russie] ; Yu Jun Wu [République populaire de Chine] ; Jia Ying Gao [République populaire de Chine] ; Floria M. Gordillo [République populaire de Chine] ; Simon Mok [République populaire de Chine] ; Vincent Kam Wai Wong [République populaire de Chine] ; Chairat Uthaipibull [Thaïlande] ; Alexander O. Terent'Ev [Russie]

Source :

ChemMedChem [ 1860-7187 ] ; 2018.

RBID : pubmed:29469179

Descripteurs français

KwdFr :
- Antinéoplasiques (), Antinéoplasiques (pharmacologie), Antinéoplasiques (synthèse chimique), Antipaludiques (), Antipaludiques (pharmacologie), Antipaludiques (synthèse chimique), Cellules A549, Cellules HepG2, Humains, Lignée cellulaire tumorale, Paludisme (traitement médicamenteux), Peroxydes (), Peroxydes (pharmacologie), Peroxydes (synthèse chimique), Plasmodium falciparum (), Plasmodium falciparum (croissance et développement), Prolifération cellulaire (), Relation dose-effet des médicaments, Relation structure-activité, Structure moléculaire, Survie cellulaire (), Tests de criblage d'agents antitumoraux, Tests de sensibilité parasitaire.
MESH :
- croissance et développement : Plasmodium falciparum.
- pharmacologie : Antinéoplasiques, Antipaludiques, Peroxydes.
- synthèse chimique : Antinéoplasiques, Antipaludiques, Peroxydes.
- traitement médicamenteux : Paludisme.
- Antinéoplasiques, Antipaludiques, Cellules A549, Cellules HepG2, Humains, Lignée cellulaire tumorale, Peroxydes, Plasmodium falciparum, Prolifération cellulaire, Relation dose-effet des médicaments, Relation structure-activité, Structure moléculaire, Survie cellulaire, Tests de criblage d'agents antitumoraux, Tests de sensibilité parasitaire.

English descriptors

KwdEn :
- A549 Cells, Antimalarials (chemical synthesis), Antimalarials (chemistry), Antimalarials (pharmacology), Antineoplastic Agents (chemical synthesis), Antineoplastic Agents (chemistry), Antineoplastic Agents (pharmacology), Cell Line, Tumor, Cell Proliferation (drug effects), Cell Survival (drug effects), Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Hep G2 Cells, Humans, Malaria (drug therapy), Molecular Structure, Parasitic Sensitivity Tests, Peroxides (chemical synthesis), Peroxides (chemistry), Peroxides (pharmacology), Plasmodium falciparum (drug effects), Plasmodium falciparum (growth & development), Structure-Activity Relationship.
MESH :
- chemical , chemical synthesis : Antimalarials, Antineoplastic Agents, Peroxides.
- chemical , chemistry : Antimalarials, Antineoplastic Agents, Peroxides.
- chemical , pharmacology : Antimalarials, Antineoplastic Agents, Peroxides.
- drug effects : Cell Proliferation, Cell Survival, Plasmodium falciparum.
- drug therapy : Malaria.
- growth & development : Plasmodium falciparum.
- A549 Cells, Cell Line, Tumor, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Hep G2 Cells, Humans, Molecular Structure, Parasitic Sensitivity Tests, Structure-Activity Relationship.

Abstract

Twenty six peroxides belonging to bridged 1,2,4,5-tetraoxanes, bridged 1,2,4-trioxolanes (ozonides), and tricyclic monoperoxides were evaluated for their in vitro antimalarial activity against Plasmodium falciparum (3D7) and for their cytotoxic activities against immortalized human normal fibroblast (CCD19Lu), liver (LO₂ ), and lung (BEAS-2B) cell lines as well as human liver (HepG2) and lung (A549) cancer-cell lines. Synthetic ozonides were shown to have the highest cytotoxicity on HepG2 (IC₅₀ =0.19-0.59 μm), and some of these compounds selectively targeted liver cancer (selectivity index values for compounds 13 a and 14 a are 20 and 28, respectively) at levels that, in some cases, were higher than those of paclitaxel, artemisinin, and artesunic acid. In contrast some ozonides showed only moderate antimalarial activity against the chloroquine-sensitive 3D7 strain of P. falciparum (IC₅₀ from 2.76 to 24.2 μm; 12 b, IC₅₀ =2.76 μm; 13 a, IC₅₀ =20.14 μm; 14 a, IC₅₀ =6.32 μm). These results suggest that these derivatives have divergent mechanisms of action against cancer cells and malaria-infected cells. A cyclic voltammetry study of the peroxides was performed, but most of the compounds did not show direct correlation in oxidative capacity-activity. Our findings offer a new source of antimalarial and anticancer agents through structural modification of peroxide compounds.

DOI: 10.1002/cmdc.201700804
PubMed: 29469179

Affiliations:

Russie, République populaire de Chine, Thaïlande

Le document en format XML

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<author><name sortKey="Gao, Jia Ying" sort="Gao, Jia Ying" uniqKey="Gao J" first="Jia Ying" last="Gao">Jia Ying Gao</name>
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<country xml:lang="fr">République populaire de Chine</country>
<wicri:regionArea>State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau</wicri:regionArea>
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<author><name sortKey="Gordillo, Floria M" sort="Gordillo, Floria M" uniqKey="Gordillo F" first="Floria M" last="Gordillo">Floria M. Gordillo</name>
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<country xml:lang="fr">République populaire de Chine</country>
<wicri:regionArea>State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau</wicri:regionArea>
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<author><name sortKey="Mok, Simon" sort="Mok, Simon" uniqKey="Mok S" first="Simon" last="Mok">Simon Mok</name>
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<country xml:lang="fr">République populaire de Chine</country>
<wicri:regionArea>State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau</wicri:regionArea>
<wicri:noRegion>Macau</wicri:noRegion>
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<author><name sortKey="Wong, Vincent Kam Wai" sort="Wong, Vincent Kam Wai" uniqKey="Wong V" first="Vincent Kam Wai" last="Wong">Vincent Kam Wai Wong</name>
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<country xml:lang="fr">République populaire de Chine</country>
<wicri:regionArea>State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau</wicri:regionArea>
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<author><name sortKey="Uthaipibull, Chairat" sort="Uthaipibull, Chairat" uniqKey="Uthaipibull C" first="Chairat" last="Uthaipibull">Chairat Uthaipibull</name>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>A549 Cells</term>
<term>Antimalarials (chemical synthesis)</term>
<term>Antimalarials (chemistry)</term>
<term>Antimalarials (pharmacology)</term>
<term>Antineoplastic Agents (chemical synthesis)</term>
<term>Antineoplastic Agents (chemistry)</term>
<term>Antineoplastic Agents (pharmacology)</term>
<term>Cell Line, Tumor</term>
<term>Cell Proliferation (drug effects)</term>
<term>Cell Survival (drug effects)</term>
<term>Dose-Response Relationship, Drug</term>
<term>Drug Screening Assays, Antitumor</term>
<term>Hep G2 Cells</term>
<term>Humans</term>
<term>Malaria (drug therapy)</term>
<term>Molecular Structure</term>
<term>Parasitic Sensitivity Tests</term>
<term>Peroxides (chemical synthesis)</term>
<term>Peroxides (chemistry)</term>
<term>Peroxides (pharmacology)</term>
<term>Plasmodium falciparum (drug effects)</term>
<term>Plasmodium falciparum (growth & development)</term>
<term>Structure-Activity Relationship</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr"><term>Antinéoplasiques ()</term>
<term>Antinéoplasiques (pharmacologie)</term>
<term>Antinéoplasiques (synthèse chimique)</term>
<term>Antipaludiques ()</term>
<term>Antipaludiques (pharmacologie)</term>
<term>Antipaludiques (synthèse chimique)</term>
<term>Cellules A549</term>
<term>Cellules HepG2</term>
<term>Humains</term>
<term>Lignée cellulaire tumorale</term>
<term>Paludisme (traitement médicamenteux)</term>
<term>Peroxydes ()</term>
<term>Peroxydes (pharmacologie)</term>
<term>Peroxydes (synthèse chimique)</term>
<term>Plasmodium falciparum ()</term>
<term>Plasmodium falciparum (croissance et développement)</term>
<term>Prolifération cellulaire ()</term>
<term>Relation dose-effet des médicaments</term>
<term>Relation structure-activité</term>
<term>Structure moléculaire</term>
<term>Survie cellulaire ()</term>
<term>Tests de criblage d'agents antitumoraux</term>
<term>Tests de sensibilité parasitaire</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antimalarials</term>
<term>Antineoplastic Agents</term>
<term>Peroxides</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antimalarials</term>
<term>Antineoplastic Agents</term>
<term>Peroxides</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antimalarials</term>
<term>Antineoplastic Agents</term>
<term>Peroxides</term>
</keywords>
<keywords scheme="MESH" qualifier="croissance et développement" xml:lang="fr"><term>Plasmodium falciparum</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Cell Proliferation</term>
<term>Cell Survival</term>
<term>Plasmodium falciparum</term>
</keywords>
<keywords scheme="MESH" qualifier="drug therapy" xml:lang="en"><term>Malaria</term>
</keywords>
<keywords scheme="MESH" qualifier="growth & development" xml:lang="en"><term>Plasmodium falciparum</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antinéoplasiques</term>
<term>Antipaludiques</term>
<term>Peroxydes</term>
</keywords>
<keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antinéoplasiques</term>
<term>Antipaludiques</term>
<term>Peroxydes</term>
</keywords>
<keywords scheme="MESH" qualifier="traitement médicamenteux" xml:lang="fr"><term>Paludisme</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>A549 Cells</term>
<term>Cell Line, Tumor</term>
<term>Dose-Response Relationship, Drug</term>
<term>Drug Screening Assays, Antitumor</term>
<term>Hep G2 Cells</term>
<term>Humans</term>
<term>Molecular Structure</term>
<term>Parasitic Sensitivity Tests</term>
<term>Structure-Activity Relationship</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Antinéoplasiques</term>
<term>Antipaludiques</term>
<term>Cellules A549</term>
<term>Cellules HepG2</term>
<term>Humains</term>
<term>Lignée cellulaire tumorale</term>
<term>Peroxydes</term>
<term>Plasmodium falciparum</term>
<term>Prolifération cellulaire</term>
<term>Relation dose-effet des médicaments</term>
<term>Relation structure-activité</term>
<term>Structure moléculaire</term>
<term>Survie cellulaire</term>
<term>Tests de criblage d'agents antitumoraux</term>
<term>Tests de sensibilité parasitaire</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">Twenty six peroxides belonging to bridged 1,2,4,5-tetraoxanes, bridged 1,2,4-trioxolanes (ozonides), and tricyclic monoperoxides were evaluated for their in vitro antimalarial activity against Plasmodium falciparum (3D7) and for their cytotoxic activities against immortalized human normal fibroblast (CCD19Lu), liver (LO<sub>2</sub>
 ), and lung (BEAS-2B) cell lines as well as human liver (HepG2) and lung (A549) cancer-cell lines. Synthetic ozonides were shown to have the highest cytotoxicity on HepG2 (IC<sub>50</sub>
 =0.19-0.59 μm), and some of these compounds selectively targeted liver cancer (selectivity index values for compounds 13 a and 14 a are 20 and 28, respectively) at levels that, in some cases, were higher than those of paclitaxel, artemisinin, and artesunic acid. In contrast some ozonides showed only moderate antimalarial activity against the chloroquine-sensitive 3D7 strain of P. falciparum (IC<sub>50</sub>
 from 2.76 to 24.2 μm; 12 b, IC<sub>50</sub>
 =2.76 μm; 13 a, IC<sub>50</sub>
 =20.14 μm; 14 a, IC<sub>50</sub>
 =6.32 μm). These results suggest that these derivatives have divergent mechanisms of action against cancer cells and malaria-infected cells. A cyclic voltammetry study of the peroxides was performed, but most of the compounds did not show direct correlation in oxidative capacity-activity. Our findings offer a new source of antimalarial and anticancer agents through structural modification of peroxide compounds.</div>
</front>
</TEI>
<affiliations><list><country><li>Russie</li>
<li>République populaire de Chine</li>
<li>Thaïlande</li>
</country>
</list>
<tree><country name="République populaire de Chine"><noRegion><name sortKey="Coghi, Paolo" sort="Coghi, Paolo" uniqKey="Coghi P" first="Paolo" last="Coghi">Paolo Coghi</name>
</noRegion>
<name sortKey="Gao, Jia Ying" sort="Gao, Jia Ying" uniqKey="Gao J" first="Jia Ying" last="Gao">Jia Ying Gao</name>
<name sortKey="Gordillo, Floria M" sort="Gordillo, Floria M" uniqKey="Gordillo F" first="Floria M" last="Gordillo">Floria M. Gordillo</name>
<name sortKey="Mok, Simon" sort="Mok, Simon" uniqKey="Mok S" first="Simon" last="Mok">Simon Mok</name>
<name sortKey="Wong, Vincent Kam Wai" sort="Wong, Vincent Kam Wai" uniqKey="Wong V" first="Vincent Kam Wai" last="Wong">Vincent Kam Wai Wong</name>
<name sortKey="Wu, Yu Jun" sort="Wu, Yu Jun" uniqKey="Wu Y" first="Yu Jun" last="Wu">Yu Jun Wu</name>
</country>
<country name="Russie"><noRegion><name sortKey="Yaremenko, Ivan A" sort="Yaremenko, Ivan A" uniqKey="Yaremenko I" first="Ivan A" last="Yaremenko">Ivan A. Yaremenko</name>
</noRegion>
<name sortKey="Radulov, Peter S" sort="Radulov, Peter S" uniqKey="Radulov P" first="Peter S" last="Radulov">Peter S. Radulov</name>
<name sortKey="Syroeshkin, Mikhail A" sort="Syroeshkin, Mikhail A" uniqKey="Syroeshkin M" first="Mikhail A" last="Syroeshkin">Mikhail A. Syroeshkin</name>
<name sortKey="Terent Ev, Alexander O" sort="Terent Ev, Alexander O" uniqKey="Terent Ev A" first="Alexander O" last="Terent'Ev">Alexander O. Terent'Ev</name>
</country>
<country name="Thaïlande"><noRegion><name sortKey="Prommana, Parichat" sort="Prommana, Parichat" uniqKey="Prommana P" first="Parichat" last="Prommana">Parichat Prommana</name>
</noRegion>
<name sortKey="Uthaipibull, Chairat" sort="Uthaipibull, Chairat" uniqKey="Uthaipibull C" first="Chairat" last="Uthaipibull">Chairat Uthaipibull</name>
</country>
</tree>
</affiliations>
</record>

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Novel Peroxides as Promising Anticancer Agents with Unexpected Depressed Antimalarial Activity.

Novel Peroxides as Promising Anticancer Agents with Unexpected Depressed Antimalarial Activity.

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