Journal
PHYTOCHEMISTRY
Volume 68, Issue 9, Pages 1312-1320Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2007.02.006
Keywords
Piper hostmanniantun var. berbicense; Piperaceae; dihydrochalcones; flavanones; antiplasmodial activity; Plasimodium falciparum
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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 mu M, respectively against both chloroquine-sensitive and resistant strains of Plasmodium falciparum (F32, FcBl). 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. (c) 2007 Elsevier Ltd. All rights reserved.
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