里查酮 A

Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC ₅₀ 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. 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. 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.

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.