| Summary: | The antiproliferative effect and mediation of apoptosis in human hepatoma HepG2 cells induced by djulis husk and its bioactive compounds was investigated. The ethanolic extracts of djulis husk (EEDH) at 50, 250, and 500 µg/mL induced remarkable cytotoxicity on HepG2 cells. By flow cytometry analysis, EEDH slowed down the cell cycle at the Sub-G0 phase after 24 h of incubation. Moreover, all EEDH treatment induced an apoptotic response in HepG2 cells. EEDH-induced apoptosis was associated with the attenuation of mitochondrial transmembrane potentials (ΔΨ<sub>m</sub>), an increase in Bax/Bcl-2 ratio, activation of caspase-3, and poly(ADP-ribose)polymerase (PARP) cleavage, as well as an increase in reactive oxygen species (ROS) generation. According to the HPLC-DAD and HPLC-MS/MS analysis, quercetin and kaempferol derivatives and another sixteen compounds were present in EEDH. Quercetin and kaempferol at 25–150 μM showed antiproliferative action and induced apoptosis on HepG2 cells, which may in part account for the anticancer activity of EEDH. Overall, EEDH may be a potent chemopreventive agent due to apoptosis in HepG2 cells.
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