Abstract
A CHCl 3-soluble fraction of 70% EtOH extract of the flower of Kayea assamica from Myanmar exhibited 100% preferential cytotoxicity (PC 100) against human pancreatic cancer PANC-1 cells under nutrient-deprived conditions at 1 μg/mL. Bioassay-guided fractionation and isolation afforded nine new coumarins, kayeassamins A ( 8), B ( 9), and C−I ( 1−7), together with nine known coumarins ( 10−18). The structures of these compounds were identified by extensive spectroscopic techniques as well as by comparison with published data. Absolute configuration at C-1′ of 1 was established as S-configuration by the modified Mosher method. All the isolates were evaluated for their in vitro preferential cytotoxicity using novel anti-austerity strategy. Among them, the novel coumarins, kayeassamins A ( 8), B ( 9), D ( 2), E ( 3), and G ( 5) exhibited the most potent preferential cytotoxicity (PC 100 1 μM) in a concentration- and time- dependent manner and induced apoptosis-like morphological changes of PANC-1 cells within 24 h of treatment. Based on the observed cytotoxicity, structure-activity relationships have been established.
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