Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent[1]. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways[2].
Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC50 values are 6.9 μg/ml, 3.4 μg/ml and 2.8 μg/ml in cells with 24-, 48- and 72-hours treatment, respectively[1].Leachianone A (10-30 μg/ml; 48 hours) indicates that at low concentration of LA (10 μg/ml), a substantial amount of cells is primarily in the early phase of apoptosis, at higher concentrations, induces a shift of the cell population to late apoptotic/ necrotic stage[1].Leachianone A (10-30 μg/ml; 48 hours) decreases the precursor of caspase-3 in a dose-dependent manner, reduces the protein level of the pro-forms of upstream initiator caspases, caspases-8 and -9, decreases two downstream substrates, namely inhibitor of caspase-activated DNase(ICAD) and poly-ADP-ribose polymerase (PARP) in HepG2 cells[1]. Cell Viability Assay[1] Cell Line: HepG2 cells
Leachianone A (intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days) significantly diminishes the tumor volume by 17-54% in LA-treated nude mice, when compared with those solely given the vehicle[1]. Animal Model: Male nude mice with human hepatoma HepG2 cells[1]
[1]. Jeong GS, et al. Lavandulyl flavanones from Sophora flavescens protect mouse hippocampal cells against glutamate-induced neurotoxicity via the induction of heme oxygenase-1. Biol Pharm Bull. 2008 Oct;31(10):1964-7. [2]. Cheung CS, et al. Leachianone A as a potential anti-cancer drug by induction of apoptosis in human hepatoma HepG2 cells. Cancer Lett. 2007 Aug 18;253(2):224-35. Epub 2007 Mar 26.