Anti‐African trypanocidal and antimalarial activity of natural flavonoids, dibenzoylmethanes and synthetic analogues
Identifieur interne : 001900 ( Main/Exploration ); précédent : 001899; suivant : 001901Anti‐African trypanocidal and antimalarial activity of natural flavonoids, dibenzoylmethanes and synthetic analogues
Auteurs : Djalma A. P. Dos Santos [Brésil] ; Patricia A. De C. Braga [Brésil] ; M. Fátima Das G. F. Da Silva [Brésil] ; João B. Fernandes [Brésil] ; Paulo C. Vieira [Brésil] ; Aderbal F. Magalhães [Brésil] ; Eva G. Magalhães [Brésil] ; Anita J. Marsaioli [Brésil] ; Valéria R. De S. Moraes [Brésil] ; Lauren Rattray [Royaume-Uni] ; Simon L. Croft [Royaume-Uni]Source :
- Journal of Pharmacy and Pharmacology [ 0022-3573 ] ; 2009-02.
English descriptors
- Teeft :
- Antimalarial, Antimalarial activity, Assay, Brucei, Brucei rhodesiense, Campinas, Campinas state university, Chalcones, Chem, Cruzi, Cytotoxic, Deguelia, Deguelia hatschbachii, Derivative, Dibenzoyl, Dibenzoylmethanes, Falciparum, Flavone, Flavonoid, Herbarium, Lonchocarpus, Lonchocarpus montanus, Magalhaes, Magnifica, Methanol, Murraya paniculata, Neoraputia, Neoraputia paraensis, Petrol, Phytochemistry, Repetitive, Rhodesiense, Selective action, Soxhlet apparatus, Synthetic dibenzoylmethanes, Trypanocidal, Trypanocidal agents, Trypanosoma, Universidade, Universidade estadual, Voucher, Voucher specimen.
Abstract
Objectives The known anti‐protozoal activity of flavonoids has stimulated the testing of other derivatives from natural and synthetic sources. Methods As part of our efforts to find potential lead compounds, a number of flavonoids isolated from Neoraputia paraensis, N. magnifica, Murraya paniculata, (Rutaceae), Lonchocarpus montanus, L. latifolius, L. subglaucescens, L. atropurpureus, L. campestris, Deguelia hatschbachii (Leguminosae), dibenzoylmethanes from L. subglaucescens and synthetic analogues were tested for in‐vitro activity against chloroquine‐sensitive Plasmodium falciparum and Trypanosoma brucei rhodesiense bloodstream form trypomastigotes. An assay withKB cells has been developed inorder tocompare in‐vitro cytotoxicityof flavonoids with a selective action on the parasites. Key findings Thirteen of the compounds tested had IC50 values ranging from 4.6 to 9.9 μM against T. brucei rhodesiense. In contrast, a small number of compounds showed significant activity against P. falciparum; seven of those tested had IC50 values ranging from 2.7 to 9.5 μM. Among the flavones only one had IC50 < 10 μM (7.6 μM), whereas against T. brucei rhodesiense seven had IC50 < 10 μM. Synthetic dibenzoylmethanes were the most active in terms of number (five) of compounds and the IC50 values (2.7–9.5 μM) against P. falciparum. Conclusions Dibenzoylmethanes represent a novel class of compounds tested for the first time as antimalarial and trypanocidal agents.
Url:
DOI: 10.1211/jpp.61.02.0017
Affiliations:
- Brésil, Royaume-Uni
- Angleterre, Grand Londres, État de São Paulo
- Campinas, Londres
- Université d'État de Campinas
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Croft</name><affiliation wicri:level="3"><country xml:lang="fr">Royaume-Uni</country><wicri:regionArea>Department of Infections and Tropical Diseases, London School of Hygiene and Tropical Medicine, London</wicri:regionArea><placeName><settlement type="city">Londres</settlement><region type="country">Angleterre</region><region type="région" nuts="1">Grand Londres</region></placeName></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Pharmacy and Pharmacology</title><title level="j" type="alt">JOURNAL OF PHARMACY AND PHARMACOLOGY</title><idno type="ISSN">0022-3573</idno><idno type="eISSN">2042-7158</idno><imprint><biblScope unit="vol">61</biblScope><biblScope unit="issue">2</biblScope><biblScope unit="page" from="257">257</biblScope><biblScope unit="page" to="266">266</biblScope><biblScope unit="page-count">10</biblScope><publisher>Blackwell Publishing Ltd</publisher><pubPlace>Oxford, UK</pubPlace><date type="published" when="2009-02">2009-02</date></imprint><idno type="ISSN">0022-3573</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-3573</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Antimalarial</term><term>Antimalarial activity</term><term>Assay</term><term>Brucei</term><term>Brucei rhodesiense</term><term>Campinas</term><term>Campinas state university</term><term>Chalcones</term><term>Chem</term><term>Cruzi</term><term>Cytotoxic</term><term>Deguelia</term><term>Deguelia hatschbachii</term><term>Derivative</term><term>Dibenzoyl</term><term>Dibenzoylmethanes</term><term>Falciparum</term><term>Flavone</term><term>Flavonoid</term><term>Herbarium</term><term>Lonchocarpus</term><term>Lonchocarpus montanus</term><term>Magalhaes</term><term>Magnifica</term><term>Methanol</term><term>Murraya paniculata</term><term>Neoraputia</term><term>Neoraputia paraensis</term><term>Petrol</term><term>Phytochemistry</term><term>Repetitive</term><term>Rhodesiense</term><term>Selective action</term><term>Soxhlet apparatus</term><term>Synthetic dibenzoylmethanes</term><term>Trypanocidal</term><term>Trypanocidal agents</term><term>Trypanosoma</term><term>Universidade</term><term>Universidade estadual</term><term>Voucher</term><term>Voucher specimen</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Objectives The known anti‐protozoal activity of flavonoids has stimulated the testing of other derivatives from natural and synthetic sources. Methods As part of our efforts to find potential lead compounds, a number of flavonoids isolated from Neoraputia paraensis, N. magnifica, Murraya paniculata, (Rutaceae), Lonchocarpus montanus, L. latifolius, L. subglaucescens, L. atropurpureus, L. campestris, Deguelia hatschbachii (Leguminosae), dibenzoylmethanes from L. subglaucescens and synthetic analogues were tested for in‐vitro activity against chloroquine‐sensitive Plasmodium falciparum and Trypanosoma brucei rhodesiense bloodstream form trypomastigotes. An assay withKB cells has been developed inorder tocompare in‐vitro cytotoxicityof flavonoids with a selective action on the parasites. Key findings Thirteen of the compounds tested had IC50 values ranging from 4.6 to 9.9 μM against T. brucei rhodesiense. In contrast, a small number of compounds showed significant activity against P. falciparum; seven of those tested had IC50 values ranging from 2.7 to 9.5 μM. Among the flavones only one had IC50 < 10 μM (7.6 μM), whereas against T. brucei rhodesiense seven had IC50 < 10 μM. Synthetic dibenzoylmethanes were the most active in terms of number (five) of compounds and the IC50 values (2.7–9.5 μM) against P. falciparum. Conclusions Dibenzoylmethanes represent a novel class of compounds tested for the first time as antimalarial and trypanocidal agents.</div></front></TEI><affiliations><list><country><li>Brésil</li><li>Royaume-Uni</li></country><region><li>Angleterre</li><li>Grand Londres</li><li>État de São Paulo</li></region><settlement><li>Campinas</li><li>Londres</li></settlement><orgName><li>Université d'État de Campinas</li></orgName></list><tree><country name="Brésil"><noRegion><name sortKey="Dos Santos, Djalma A P" sort="Dos Santos, Djalma A P" uniqKey="Dos Santos D" first="Djalma A. P." last="Dos Santos">Djalma A. P. Dos Santos</name></noRegion><name sortKey="Braga, Patricia A De C" sort="Braga, Patricia A De C" uniqKey="Braga P" first="Patricia A. De C." last="Braga">Patricia A. De C. Braga</name><name sortKey="Da Silva, M Fatima Das G F" sort="Da Silva, M Fatima Das G F" uniqKey="Da Silva M" first="M. Fátima Das G. F." last="Da Silva">M. Fátima Das G. F. Da Silva</name><name sortKey="Da Silva, M Fatima Das G F" sort="Da Silva, M Fatima Das G F" uniqKey="Da Silva M" first="M. Fátima Das G. F." last="Da Silva">M. Fátima Das G. F. Da Silva</name><name sortKey="Fernandes, Joao B" sort="Fernandes, Joao B" uniqKey="Fernandes J" first="João B." last="Fernandes">João B. Fernandes</name><name sortKey="Magalhaes, Aderbal F" sort="Magalhaes, Aderbal F" uniqKey="Magalhaes A" first="Aderbal F." last="Magalhães">Aderbal F. Magalhães</name><name sortKey="Magalhaes, Eva G" sort="Magalhaes, Eva G" uniqKey="Magalhaes E" first="Eva G." last="Magalhães">Eva G. Magalhães</name><name sortKey="Marsaioli, Anita J" sort="Marsaioli, Anita J" uniqKey="Marsaioli A" first="Anita J." last="Marsaioli">Anita J. Marsaioli</name><name sortKey="Moraes, Valeria R De S" sort="Moraes, Valeria R De S" uniqKey="Moraes V" first="Valéria R. De S." last="Moraes">Valéria R. De S. Moraes</name><name sortKey="Vieira, Paulo C" sort="Vieira, Paulo C" uniqKey="Vieira P" first="Paulo C." last="Vieira">Paulo C. Vieira</name></country><country name="Royaume-Uni"><region name="Angleterre"><name sortKey="Rattray, Lauren" sort="Rattray, Lauren" uniqKey="Rattray L" first="Lauren" last="Rattray">Lauren Rattray</name></region><name sortKey="Croft, Simon L" sort="Croft, Simon L" uniqKey="Croft S" first="Simon L." last="Croft">Simon L. Croft</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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