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-enyloxy)-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.
- Casimiroa tetrameria
- Solid tumor selectivity
ASJC Scopus subject areas
- Drug Discovery
- Complementary and alternative medicine