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Antiplasmodial phenolic compounds from Piptadenia pervillei.

Identifieur interne : 000111 ( Ncbi/Checkpoint ); précédent : 000110; suivant : 000112

Antiplasmodial phenolic compounds from Piptadenia pervillei.

Auteurs : Voahangy Ramanandraibe [Madagascar] ; Philippe Grellier ; Marie-Thérèse Martin ; Alexandre Deville ; Roger Joyeau ; David Ramanitrahasimbola ; Elisabeth Mouray ; Philippe Rasoanaivo ; Lengo Mambu

Source :

RBID : pubmed:18484535

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English descriptors

Abstract

Piptadenia pervillei Vatke (Fabaceae) was selected from a screening programme devoted to the search of naturally-occuring antimalarial compounds from plants of Madagascar. Bioassay-guided fractionation of the ethyl acetate extract of the leaves led to the isolation of four phenolic compounds, (+)-catechin ( 1), (+)-catechin 5-gallate ( 2), (+)-catechin 3-gallate ( 3) and ethyl gallate ( 4). Structures were determined by NMR and mass spectroscopy. Compounds 2 and 3 displayed the highest in vitro activity against the chloroquine-resistant strain FcB1 of Plasmodium falciparum with IC (50) values of 1.2 microM and 1.0 microM, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC (50) values > 75 microM). Five analogues ( 5 - 9) of (+)-catechin 5-gallate ( 2) were synthesized and evaluated for their antiplasmodial activity.

DOI: 10.1055/s-2008-1034328
PubMed: 18484535


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pubmed:18484535

Le document en format XML

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<name sortKey="Ramanitrahasimbola, David" sort="Ramanitrahasimbola, David" uniqKey="Ramanitrahasimbola D" first="David" last="Ramanitrahasimbola">David Ramanitrahasimbola</name>
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<term>Antineoplastic Agents, Phytogenic (pharmacology)</term>
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<div type="abstract" xml:lang="en">Piptadenia pervillei Vatke (Fabaceae) was selected from a screening programme devoted to the search of naturally-occuring antimalarial compounds from plants of Madagascar. Bioassay-guided fractionation of the ethyl acetate extract of the leaves led to the isolation of four phenolic compounds, (+)-catechin ( 1), (+)-catechin 5-gallate ( 2), (+)-catechin 3-gallate ( 3) and ethyl gallate ( 4). Structures were determined by NMR and mass spectroscopy. Compounds 2 and 3 displayed the highest in vitro activity against the chloroquine-resistant strain FcB1 of Plasmodium falciparum with IC (50) values of 1.2 microM and 1.0 microM, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC (50) values > 75 microM). Five analogues ( 5 - 9) of (+)-catechin 5-gallate ( 2) were synthesized and evaluated for their antiplasmodial activity.</div>
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<name sortKey="Joyeau, Roger" sort="Joyeau, Roger" uniqKey="Joyeau R" first="Roger" last="Joyeau">Roger Joyeau</name>
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