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Antiplasmodial Phenolic Compounds from Piptadenia pervillei

Identifieur interne : 000304 ( France/Analysis ); précédent : 000303; suivant : 000305

Antiplasmodial Phenolic Compounds from Piptadenia pervillei

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

Source :

RBID : Pascal:08-0207828

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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 FcBl of Plasmodium falciparum with ICso values of 1.2 pM and 1.0 pM, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC50 values >75μM). Five analogues (5-9) of (+)-catechin 5-gallate (2) were synthesized and evaluated for their antiplasmodial activity.

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Pascal:08-0207828

Le document en format XML

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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 FcBl of Plasmodium falciparum with IC
<sub>so</sub>
values of 1.2 pM and 1.0 pM, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC
<sub>50</sub>
values >75μM). Five analogues (5-9) of (+)-catechin 5-gallate (2) were synthesized and evaluated for their antiplasmodial activity.</div>
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<name sortKey="Ramanandraibe, Voahangy" sort="Ramanandraibe, Voahangy" uniqKey="Ramanandraibe V" first="Voahangy" last="Ramanandraibe">Voahangy Ramanandraibe</name>
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<name sortKey="Ramanitrahasimbola, David" sort="Ramanitrahasimbola, David" uniqKey="Ramanitrahasimbola D" first="David" last="Ramanitrahasimbola">David Ramanitrahasimbola</name>
<name sortKey="Rasoanaivo, Philippe" sort="Rasoanaivo, Philippe" uniqKey="Rasoanaivo P" first="Philippe" last="Rasoanaivo">Philippe Rasoanaivo</name>
</country>
<country name="France">
<region name="Île-de-France">
<name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name>
</region>
<name sortKey="Deville, Alexandre" sort="Deville, Alexandre" uniqKey="Deville A" first="Alexandre" last="Deville">Alexandre Deville</name>
<name sortKey="Joyeau, Roger" sort="Joyeau, Roger" uniqKey="Joyeau R" first="Roger" last="Joyeau">Roger Joyeau</name>
<name sortKey="Mambu, Lengo" sort="Mambu, Lengo" uniqKey="Mambu L" first="Lengo" last="Mambu">Lengo Mambu</name>
<name sortKey="Martin, Marie Therese" sort="Martin, Marie Therese" uniqKey="Martin M" first="Marie-Thérèse" last="Martin">Marie-Thérèse Martin</name>
<name sortKey="Mouray, Elisabeth" sort="Mouray, Elisabeth" uniqKey="Mouray E" first="Elisabeth" last="Mouray">Elisabeth Mouray</name>
</country>
</tree>
</affiliations>
</record>

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