Ardisiacrispin A (Deglucocyclamin) has cytotoxic activity toward HepG2 cancer cell with the GI(50) value of 1.56μM, it could inhibit the proliferation of Bel-7402 cells by inducing apoptosis and disassembling microtubule.Ardisiacrispin(A+B) exhibit prominent abilities to inhibit the proliferation of HL-60 cells by blocking the cell cycle at S phase and inducing apoptosis.

Ardisiacrispin A+Ardisiacrispin B is a mixture of Ardisiacrispin A and ardisiacrispin B, derived from Ardisia crenata with a fixed proportion (2:1). METHODS AND RESULTS:The present study was conducted to investigate its anticancer activity on human cancer cells and its underlying mechanism of action. The (IC50)s of Ardisiacrispin A+Ardisiacrispin B on proliferation of several human cancer cell lines were in the range of 0.9-6.5 microg/ml by sulphorhodamine B-based colorimetric assay, in which Bel-7402 was the most sensitive cell line. Moreover, Ardisiacrispin A+Ardisiacrispin B induced dose-dependent apoptosis in Bel-7402 cells at doses of 1-10 microg/ml by flow cytometry, and resulted in the changes of the mitochondrial membrane depolarization, membrane permeability enhancement, and nuclear condensation in a dose-dependent manner through high-content screening analysis. Furthermore, Ardisiacrispin A+Ardisiacrispin B could disassemble microtubule in Bel-7402 cells; the fluorescence intensity of microtubules decreased at the concentration of 5-20 microg/ml. CONCLUSIONS: These findings suggest that Ardisiacrispin A+Ardisiacrispin B could inhibit the proliferation of Bel-7402 cells by inducing apoptosis and disassembling microtubule.