Liver cancer has become one of the major types of
cancer with high mortality and
liver cancer is not responsive to the current
cytotoxic agents used in
chemotherapy. The purpose of this study was to examine the in vitro cytotoxicity of
goniothalamin on human
hepatoblastoma HepG2 cells and normal liver Chang cells. The cytotoxicity of
goniothalamin against HepG2 and liver Chang cell was tested using MTT cell viability assay, LDH leakage assay, cell cycle flow cytometry PI analysis,
BrdU proliferation ELISA assay and
trypan blue dye exclusion assay.
Goniothalamin selectively inhibited HepG2 cells [IC₅₀ = 4.6 (±0.23) µM in the MTT assay; IC₅₀ = 5.20 (±0.01) µM for LDH assay at 72 hours], with less sensitivity in Chang cells [IC₅₀ = 35.0 (±0.09) µM for MTT assay; IC₅₀ = 32.5 (±0.04) µM for LDH assay at 72 hours]. In the
trypan blue dye exclusion assay, the Viability Indexes were 52 ± 1.73% for HepG2 cells and 62 ± 4.36% for Chang cells at IC₅₀ after 72 hours. Cytotoxicity of
goniothalamin was related to inhibition of
DNA synthesis, as revealed by the reduction of
BrdU incorporation. At 72 hours, the lowest concentration of
goniothalamin (2.3 µL) retained 97.6% of normal liver Chang cells proliferation while it reduced HepG2 cell proliferation to 19.8% as compared to control. Besides,
goniothalamin caused accumulation of hypodiploid apoptosis and different degree of G2/M arrested as shown in cell cycle analysis by flow cytometry.
Goniothalamin selectively killed
liver cancer cell through suppression of proliferation and induction of apoptosis. These results suggest that
goniothalamin shows potential cytotoxicity against
hepatoblastoma HepG2 cells.