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Activity-guided Isolation of Antiplasmodial Dihydrochalcones and Flavanones From Piper Hostmannianum Var. Berbicense

Activity-guided Isolation of Antiplasmodial Dihydrochalcones and Flavanones From Piper Hostmannianum Var. Berbicense

Bénédicte Portet, Nicolas Fabre, Vincent Roumy, Heinz Gornitzka, Geneviève Bourdy, Séverine Chevalley, Michel Sauvain, Alexis Valentin, Claude Moulis

Phytochemistry. 2007 May;68(9):1312-20.

PMID: 17397884

Abstract:

The bioassay-guided purification of an n-hexane extract from the leaves of Piper hostmannianum var. berbicense led to the isolation of four monoterpene or prenyl-substituted dihydrochalcones (1a, 1b, 2, 3) as well as the known compounds 2',6'-dihydroxy-4'-methoxydihydrochalcone (4), linderatone (5), strobopinin (6), adunctin E (7) and (-)-methyllinderatin (8). Their structures were established on the basis of NMR and X-ray analysis. (-)-Methyllinderatin, linderatone and 2',6'-dihydroxy-4'-methoxydihydrochalcone exhibited the most potent antiplasmodial activity with IC50 values of 5.64, 10.33 and 12.69 microM, respectively against both chloroquine-sensitive and resistant strains of Plasmodium falciparum (F32,FcB1). The activity of (-)-methyllinderatin was confirmed in vivo against Plasmodium vinckei petteri in mice (80% of reduction of parasitemia) at a dose of 20 mg/kg/day.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP35241555	2′,6′-Dihydroxy 4′-methoxydihydrochalcone		35241-55-5	Price

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