Journal of Natural Products · 1993 · 261 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyChemotherapyDrug DiscoverySynthetic Medicinal ChemistryAntiparasitic PharmacologyEnzyme InhibitionMalariaMedicinal PlantsStructure-activity Relationship AnalysisAntimalarial AgentsAntimalarial ChemotherapyAntimalarial Drug DevelopmentMolecular Structure DeterminationPlant AlkaloidsPlasmodium FalciparumQuinoline AlkaloidsSelectivity
(+)-2-N-Methyltelobine [1], a new alkaloid, together with twelve known bisbenzylisoquinolines, was isolated from the tubers of Stephania erecta. The structure determination and the complete 1H- and unambiguous 13C-nmr assignments of 1 were obtained through extensive use of several 1D and 2D nmr techniques. All alkaloids inhibited the growth of cultured Plasmodium falciparum strains D-6 and W-2 and displayed nonselective cytotoxicity with a battery of cultured mammalian cells. These data were used for the calculation of selectivity indices. Relative to known antimalarial agents, these bisbenzylisoquinoline alkaloids do not appear to be promising clinical candidates at the present time.