Journal
MOLECULES
Volume 23, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules23081849
Keywords
Asarum sieboldii; (-)-asarinin; cytotoxicity; ovarian cancer cells; apoptosis; caspase
Funding
- Bio-Synergy Research Project of the Ministry of Science, ICT and Future Planning through National Research Foundation of Korea (NRF) [NRF-2015M3A9C4070483]
- Basic Science Research Program through NRF - Ministry of Education [NRF-2016R1D1A1B03930222]
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Two tetrahydrofurofurano lignans (1 and 2), four phenylpropanoids (3-6), and two alkamides (7 and 8) were isolated from the EtOAc-soluble fraction of the roots of Asarum sieboldii. The chemical structures of the isolates were identified by analysis of spectroscopic data measurements, and by a comparison of their data with published values. The isolates (1, 2, 4-8) were evaluated for their cytotoxicity against human ovarian cancer cells (A2780 and SKOV3) and immortalized ovarian surface epithelial cells (IOSE80PC) using a MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide) assay. Of the isolates, (-)-asarinin (1) exhibited the most potent cytotoxicity to both A2780 and SKOV3 cells. A propidium iodide/annexin V-fluorescein isothiocyanate (V-FITC) double staining assay showed that (-)-asarinin (1) induces apoptotic cell death in ovarian cancer cells. In addition, (-)-asarinin (1) increased the activation of caspase-3, caspase-8, and caspase-9 in ovarian cancer cells. Pretreatment with caspase inhibitors attenuated the cell death induced by (-)-asarinin (1). In conclusion, our findings show that (-)-asarinin (1) from the roots of A. sieboldii may induce caspase-dependent apoptotic cell death in human cancer cells.
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