Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog.
Identifieur interne : 001037 ( Main/Exploration ); précédent : 001036; suivant : 001038Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog.
Auteurs : Andreia Montoia [Brésil] ; Luiz F. Rocha E Silva [Brésil] ; Zelina E. Torres [Brésil] ; David S. Costa [Brésil] ; Marycleuma C. Henrique [Brésil] ; Emerson S. Lima [Brésil] ; Marne C. Vasconcellos [Brésil] ; Rita C Z. Souza [Brésil] ; Monica R F. Costa [Brésil] ; Andriy Grafov [Finlande] ; Iryna Grafova [Finlande] ; Marcos N. Eberlin [Brésil] ; Wanderli P. Tadei [Brésil] ; Rodrigo C N. Amorim [Brésil] ; Adrian M. Pohlit [Brésil]Source :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2014.
Descripteurs français
- KwdFr :
- Animaux, Antipaludiques (), Antipaludiques (pharmacologie), Antipaludiques (synthèse chimique), Aspidosperma (), Chloroquine (), Chloroquine (pharmacologie), Ellipticines (), Ellipticines (pharmacologie), Ellipticines (synthèse chimique), Fibroblastes (), Humains, Modèles animaux de maladie humaine, Plasmodium falciparum (), Souris, Structure moléculaire, Écorce ().
- MESH :
- pharmacologie : Antipaludiques, Chloroquine, Ellipticines.
- synthèse chimique : Antipaludiques, Ellipticines.
- Animaux, Antipaludiques, Aspidosperma, Chloroquine, Ellipticines, Fibroblastes, Humains, Modèles animaux de maladie humaine, Plasmodium falciparum, Souris, Structure moléculaire, Écorce.
English descriptors
- KwdEn :
- Animals, Antimalarials (chemical synthesis), Antimalarials (chemistry), Antimalarials (pharmacology), Aspidosperma (chemistry), Chloroquine (chemistry), Chloroquine (pharmacology), Disease Models, Animal, Ellipticines (chemical synthesis), Ellipticines (chemistry), Ellipticines (pharmacology), Fibroblasts (drug effects), Humans, Mice, Molecular Structure, Plant Bark (chemistry), Plasmodium falciparum (drug effects).
- MESH :
- chemical , chemical synthesis : Antimalarials, Ellipticines.
- chemical , chemistry : Antimalarials, Chloroquine, Ellipticines.
- chemical , pharmacology : Antimalarials, Chloroquine, Ellipticines.
- chemistry : Aspidosperma, Plant Bark.
- drug effects : Fibroblasts, Plasmodium falciparum.
- Animals, Disease Models, Animal, Humans, Mice, Molecular Structure.
Abstract
Ellipticine has been shown previously to exhibit excellent in vitro antiplasmodial activity and in vivo antimalarial properties that are comparable to those of the control drug chloroquine in a mouse malaria model. Ellipticine derivatives and analogs exhibit antimalarial potential however only a few have been studied to date. Herein, ellipticine and a structural analog were isolated from Aspidosperma vargasii bark. A-ring brominated and nitrated ellipticine derivatives exhibit good in vitro inhibition of Plasmodium falciparum K1 and 3D7 strains. Several of the compounds were found not to be toxic to human fetal lung fibroblasts. 9-Nitroellipticine (IC50=0.55μM) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives.
DOI: 10.1016/j.bmcl.2014.04.070
PubMed: 24813729
Affiliations:
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Rocha E Silva</name><affiliation wicri:level="1"><nlm:affiliation>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil; Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil; Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Torres, Zelina E" sort="Torres, Zelina E" uniqKey="Torres Z" first="Zelina E" last="Torres">Zelina E. Torres</name><affiliation wicri:level="1"><nlm:affiliation>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Costa, David S" sort="Costa, David S" uniqKey="Costa D" first="David S" last="Costa">David S. Costa</name><affiliation wicri:level="1"><nlm:affiliation>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Henrique, Marycleuma C" sort="Henrique, Marycleuma C" uniqKey="Henrique M" first="Marycleuma C" last="Henrique">Marycleuma C. Henrique</name><affiliation wicri:level="1"><nlm:affiliation>Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Lima, Emerson S" sort="Lima, Emerson S" uniqKey="Lima E" first="Emerson S" last="Lima">Emerson S. Lima</name><affiliation wicri:level="1"><nlm:affiliation>Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Vasconcellos, Marne C" sort="Vasconcellos, Marne C" uniqKey="Vasconcellos M" first="Marne C" last="Vasconcellos">Marne C. Vasconcellos</name><affiliation wicri:level="1"><nlm:affiliation>Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Souza, Rita C Z" sort="Souza, Rita C Z" uniqKey="Souza R" first="Rita C Z" last="Souza">Rita C Z. Souza</name><affiliation wicri:level="1"><nlm:affiliation>State University of Campinas, Campus Universitário Zeferino Vaz SN, 13083-970 Campinas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>State University of Campinas, Campus Universitário Zeferino Vaz SN, 13083-970 Campinas</wicri:regionArea><wicri:noRegion>13083-970 Campinas</wicri:noRegion></affiliation></author><author><name sortKey="Costa, Monica R F" sort="Costa, Monica R F" uniqKey="Costa M" first="Monica R F" last="Costa">Monica R F. Costa</name><affiliation wicri:level="1"><nlm:affiliation>Heitor Vieira Dourado Tropical Medicine Foundation, Avenida Pedro Teixeira, 25, 69040-000 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>Heitor Vieira Dourado Tropical Medicine Foundation, Avenida Pedro Teixeira, 25, 69040-000 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Grafov, Andriy" sort="Grafov, Andriy" uniqKey="Grafov A" first="Andriy" last="Grafov">Andriy Grafov</name><affiliation wicri:level="4"><nlm:affiliation>University of Helsinki, A.I. Virtasen aukio 1, PL 55, FI-00014 Helsinki, Finland.</nlm:affiliation><country xml:lang="fr">Finlande</country><wicri:regionArea>University of Helsinki, A.I. Virtasen aukio 1, PL 55, FI-00014 Helsinki</wicri:regionArea><orgName type="university">Université d'Helsinki</orgName><placeName><settlement type="city">Helsinki</settlement><region type="région" nuts="2">Uusimaa</region></placeName></affiliation></author><author><name sortKey="Grafova, Iryna" sort="Grafova, Iryna" uniqKey="Grafova I" first="Iryna" last="Grafova">Iryna Grafova</name><affiliation wicri:level="4"><nlm:affiliation>University of Helsinki, A.I. Virtasen aukio 1, PL 55, FI-00014 Helsinki, Finland.</nlm:affiliation><country xml:lang="fr">Finlande</country><wicri:regionArea>University of Helsinki, A.I. Virtasen aukio 1, PL 55, FI-00014 Helsinki</wicri:regionArea><orgName type="university">Université d'Helsinki</orgName><placeName><settlement type="city">Helsinki</settlement><region type="région" nuts="2">Uusimaa</region></placeName></affiliation></author><author><name sortKey="Eberlin, Marcos N" sort="Eberlin, Marcos N" uniqKey="Eberlin M" first="Marcos N" last="Eberlin">Marcos N. Eberlin</name><affiliation wicri:level="1"><nlm:affiliation>State University of Campinas, Campus Universitário Zeferino Vaz SN, 13083-970 Campinas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>State University of Campinas, Campus Universitário Zeferino Vaz SN, 13083-970 Campinas</wicri:regionArea><wicri:noRegion>13083-970 Campinas</wicri:noRegion></affiliation></author><author><name sortKey="Tadei, Wanderli P" sort="Tadei, Wanderli P" uniqKey="Tadei W" first="Wanderli P" last="Tadei">Wanderli P. Tadei</name><affiliation wicri:level="1"><nlm:affiliation>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Amorim, Rodrigo C N" sort="Amorim, Rodrigo C N" uniqKey="Amorim R" first="Rodrigo C N" last="Amorim">Rodrigo C N. Amorim</name><affiliation wicri:level="1"><nlm:affiliation>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author><author><name sortKey="Pohlit, Adrian M" sort="Pohlit, Adrian M" uniqKey="Pohlit A" first="Adrian M" last="Pohlit">Adrian M. Pohlit</name><affiliation wicri:level="1"><nlm:affiliation>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil. Electronic address: ampohlit@inpa.gov.br.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas</wicri:regionArea><wicri:noRegion>Amazonas</wicri:noRegion></affiliation></author></analytic><series><title level="j">Bioorganic & medicinal chemistry letters</title><idno type="eISSN">1464-3405</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>Antimalarials (chemical synthesis)</term><term>Antimalarials (chemistry)</term><term>Antimalarials (pharmacology)</term><term>Aspidosperma (chemistry)</term><term>Chloroquine (chemistry)</term><term>Chloroquine (pharmacology)</term><term>Disease Models, Animal</term><term>Ellipticines (chemical synthesis)</term><term>Ellipticines (chemistry)</term><term>Ellipticines (pharmacology)</term><term>Fibroblasts (drug effects)</term><term>Humans</term><term>Mice</term><term>Molecular Structure</term><term>Plant Bark (chemistry)</term><term>Plasmodium falciparum (drug effects)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Antipaludiques ()</term><term>Antipaludiques (pharmacologie)</term><term>Antipaludiques (synthèse chimique)</term><term>Aspidosperma ()</term><term>Chloroquine ()</term><term>Chloroquine (pharmacologie)</term><term>Ellipticines ()</term><term>Ellipticines (pharmacologie)</term><term>Ellipticines (synthèse chimique)</term><term>Fibroblastes ()</term><term>Humains</term><term>Modèles animaux de maladie humaine</term><term>Plasmodium falciparum ()</term><term>Souris</term><term>Structure moléculaire</term><term>Écorce ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antimalarials</term><term>Ellipticines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antimalarials</term><term>Chloroquine</term><term>Ellipticines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antimalarials</term><term>Chloroquine</term><term>Ellipticines</term></keywords><keywords scheme="MESH" qualifier="chemistry" xml:lang="en"><term>Aspidosperma</term><term>Plant Bark</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Fibroblasts</term><term>Plasmodium falciparum</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antipaludiques</term><term>Chloroquine</term><term>Ellipticines</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antipaludiques</term><term>Ellipticines</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Disease Models, Animal</term><term>Humans</term><term>Mice</term><term>Molecular Structure</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Antipaludiques</term><term>Aspidosperma</term><term>Chloroquine</term><term>Ellipticines</term><term>Fibroblastes</term><term>Humains</term><term>Modèles animaux de maladie humaine</term><term>Plasmodium falciparum</term><term>Souris</term><term>Structure moléculaire</term><term>Écorce</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Ellipticine has been shown previously to exhibit excellent in vitro antiplasmodial activity and in vivo antimalarial properties that are comparable to those of the control drug chloroquine in a mouse malaria model. Ellipticine derivatives and analogs exhibit antimalarial potential however only a few have been studied to date. Herein, ellipticine and a structural analog were isolated from Aspidosperma vargasii bark. A-ring brominated and nitrated ellipticine derivatives exhibit good in vitro inhibition of Plasmodium falciparum K1 and 3D7 strains. Several of the compounds were found not to be toxic to human fetal lung fibroblasts. 9-Nitroellipticine (IC50=0.55μM) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives. </div></front></TEI><affiliations><list><country><li>Brésil</li><li>Finlande</li></country><region><li>Uusimaa</li></region><settlement><li>Helsinki</li></settlement><orgName><li>Université d'Helsinki</li></orgName></list><tree><country name="Brésil"><noRegion><name sortKey="Montoia, Andreia" sort="Montoia, Andreia" uniqKey="Montoia A" first="Andreia" last="Montoia">Andreia Montoia</name></noRegion><name sortKey="Amorim, Rodrigo C N" sort="Amorim, Rodrigo C N" uniqKey="Amorim R" first="Rodrigo C N" last="Amorim">Rodrigo C N. Amorim</name><name sortKey="Costa, David S" sort="Costa, David S" uniqKey="Costa D" first="David S" last="Costa">David S. Costa</name><name sortKey="Costa, Monica R F" sort="Costa, Monica R F" uniqKey="Costa M" first="Monica R F" last="Costa">Monica R F. Costa</name><name sortKey="Eberlin, Marcos N" sort="Eberlin, Marcos N" uniqKey="Eberlin M" first="Marcos N" last="Eberlin">Marcos N. Eberlin</name><name sortKey="Henrique, Marycleuma C" sort="Henrique, Marycleuma C" uniqKey="Henrique M" first="Marycleuma C" last="Henrique">Marycleuma C. Henrique</name><name sortKey="Lima, Emerson S" sort="Lima, Emerson S" uniqKey="Lima E" first="Emerson S" last="Lima">Emerson S. Lima</name><name sortKey="Pohlit, Adrian M" sort="Pohlit, Adrian M" uniqKey="Pohlit A" first="Adrian M" last="Pohlit">Adrian M. Pohlit</name><name sortKey="Rocha E Silva, Luiz F" sort="Rocha E Silva, Luiz F" uniqKey="Rocha E Silva L" first="Luiz F" last="Rocha E Silva">Luiz F. Rocha E Silva</name><name sortKey="Souza, Rita C Z" sort="Souza, Rita C Z" uniqKey="Souza R" first="Rita C Z" last="Souza">Rita C Z. Souza</name><name sortKey="Tadei, Wanderli P" sort="Tadei, Wanderli P" uniqKey="Tadei W" first="Wanderli P" last="Tadei">Wanderli P. Tadei</name><name sortKey="Torres, Zelina E" sort="Torres, Zelina E" uniqKey="Torres Z" first="Zelina E" last="Torres">Zelina E. Torres</name><name sortKey="Vasconcellos, Marne C" sort="Vasconcellos, Marne C" uniqKey="Vasconcellos M" first="Marne C" last="Vasconcellos">Marne C. Vasconcellos</name></country><country name="Finlande"><region name="Uusimaa"><name sortKey="Grafov, Andriy" sort="Grafov, Andriy" uniqKey="Grafov A" first="Andriy" last="Grafov">Andriy Grafov</name></region><name sortKey="Grafova, Iryna" sort="Grafova, Iryna" uniqKey="Grafova I" first="Iryna" last="Grafova">Iryna Grafova</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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