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Antimalarial activity of extract and norbergenin derivatives from the stem bark of Diospyros sanza‐minika A. Chevalier (Ebenaceae)

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Antimalarial activity of extract and norbergenin derivatives from the stem bark of Diospyros sanza‐minika A. Chevalier (Ebenaceae)

Auteurs : Jean Gustave Tangmouo [Cameroun, Suisse] ; Raimana Ho [Suisse] ; An Matheeussen [Belgique] ; Alain Meli Lannang [Cameroun] ; Justin Komguem [Cameroun] ; Bernadette Biloa Messi [Cameroun, Suisse] ; Louis Maes [Belgique] ; Kurt Hostettmann [Suisse]

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RBID : ISTEX:B747D3A0175ACC2032904783D144162550E52739

Abstract

The methanol extract from the stem bark of Diospyros sanza‐minika as well as five norbergenin derivatives isolated from this crude extract were evaluated for their in vitro activity against Plasmodium falciparum K1 and cytotoxicity on MRC‐5 cells. 4‐O‐(3′‐methylgalloyl)norbergenin was found to be the most potent compound (IC50 0.6 μg/mL; CC50 24.7 μg/mL), followed by 4‐O‐galloylnorbergenin (IC50 3.9 μg/mL; CC50 > 64 μg/mL) and 11‐O‐p‐hydroxy‐benzoyl‐norbergenin (IC50 4.9 μg/mL; CC50 > 64 μg/mL). Norbergenin and 4‐O‐syringoylnorbergenin were inactive (IC50 > 32 μg/mL; CC50 > 64 μg/mL). The antimalarial activity of the pure constituents and of the methanol extract from the stem bark of Diospyros sanza‐minika is reported for the first time. The results provide interesting baseline information for the potential use of the crude extract well as some of the isolated compounds in the search for novel antimalarial compounds. Copyright © 2010 John Wiley & Sons, Ltd.

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DOI: 10.1002/ptr.3192

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ISTEX:B747D3A0175ACC2032904783D144162550E52739

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<div type="abstract" xml:lang="en">The methanol extract from the stem bark of Diospyros sanza‐minika as well as five norbergenin derivatives isolated from this crude extract were evaluated for their in vitro activity against Plasmodium falciparum K1 and cytotoxicity on MRC‐5 cells. 4‐O‐(3′‐methylgalloyl)norbergenin was found to be the most potent compound (IC50 0.6 μg/mL; CC50 24.7 μg/mL), followed by 4‐O‐galloylnorbergenin (IC50 3.9 μg/mL; CC50 > 64 μg/mL) and 11‐O‐p‐hydroxy‐benzoyl‐norbergenin (IC50 4.9 μg/mL; CC50 > 64 μg/mL). Norbergenin and 4‐O‐syringoylnorbergenin were inactive (IC50 > 32 μg/mL; CC50 > 64 μg/mL). The antimalarial activity of the pure constituents and of the methanol extract from the stem bark of Diospyros sanza‐minika is reported for the first time. The results provide interesting baseline information for the potential use of the crude extract well as some of the isolated compounds in the search for novel antimalarial compounds. Copyright © 2010 John Wiley & Sons, Ltd.</div>
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