AIM:To isolate and characterize solid tumor inhibitory and other constituents from a bioactive extract of Casimiroa tetrameria((Rutaceae).METHODS:A crude extract of C.tetrameria obtained from the US National Cancer In...AIM:To isolate and characterize solid tumor inhibitory and other constituents from a bioactive extract of Casimiroa tetrameria((Rutaceae).METHODS:A crude extract of C.tetrameria obtained from the US National Cancer Institute Natural Product Repository and found to exhibit selective toxicity to solid tumor cells was subjected bioactivity-guided fractionation involving solvent-solvent partitioning,gel filtration,and chromatography.The structures of all isolated compounds were elucidated by spectroscopic analysis(NMR and MS) and/or by comparison with the reported data.Compounds 1 and 4-9 were evaluated for their solid tumor selective cytotoxicity.RESULTS:Nine metabolites,including a new furanocoumarin,5-methoxy-8-(4'-acetoxy-3'-methylbut-2-eny-loxy)-psoralen(1),and the previously known compounds 2-9 were encountered.Of these the flavonoid zapotin(6),and N-benzoyltyramide derivatives 7 and 8 were found to be the active constituents.CONCLUSION:Zapotin(6) is the most potent constituent of C.tetrameria with solid tumor selectivity.展开更多
基金supported by the US National Institutes of Health research grant CA092143 awarded by National Cancer Institute
文摘AIM:To isolate and characterize solid tumor inhibitory and other constituents from a bioactive extract of Casimiroa tetrameria((Rutaceae).METHODS:A crude extract of C.tetrameria obtained from the US National Cancer Institute Natural Product Repository and found to exhibit selective toxicity to solid tumor cells was subjected bioactivity-guided fractionation involving solvent-solvent partitioning,gel filtration,and chromatography.The structures of all isolated compounds were elucidated by spectroscopic analysis(NMR and MS) and/or by comparison with the reported data.Compounds 1 and 4-9 were evaluated for their solid tumor selective cytotoxicity.RESULTS:Nine metabolites,including a new furanocoumarin,5-methoxy-8-(4'-acetoxy-3'-methylbut-2-eny-loxy)-psoralen(1),and the previously known compounds 2-9 were encountered.Of these the flavonoid zapotin(6),and N-benzoyltyramide derivatives 7 and 8 were found to be the active constituents.CONCLUSION:Zapotin(6) is the most potent constituent of C.tetrameria with solid tumor selectivity.
