4-O-(2',3',4'-tri-O-methyl-β-D-xylopyranosyl) diphyllin (M3) is a cytotoxic compound that was first isolated from the aerial parts of Phyllanthus taxodiifolius. The current study demonstrated that M3, a lignan xyloside, exhibits anticancer effects in a number of cancer cell lines by MTT test, including HCT116 cells. An association was identified between M3 treatment and the reduced proliferation of cancer cells; the half maximal inhibitory concentration (IC50) value of M3 ranged from 0.08 to 1.12 µM. Furthermore, M3 was revealed to exhibit a stronger antiproliferative effect by Annexin-V-FLUOS test compared with VP-16, another natural lignan used in cancer treatment. Notably, the IC50 value of M3 with MTT test in HCT116 cells was 0.08 µM. In addition, it was revealed that M3 could induce apoptosis in HCT116 cells in a caspase-3-dependent manner at a lower concentration compared with VP-16. Further analysis identified that the antiproliferation effect of M3 was associated with the promotion of microtubule depolymerization by CytoDYNAMIX Screen 03 Tubulin Polymerization assay. In summary, the current study demonstrated that M3 could inhibit proliferation and induce apoptosis in HCT116 cells, which supports a potential therapeutic application of M3 in cancer treatment, particularly in colon cancer.
Keywords: antiproliferation; lignan xyloside; mechanism; microtubule; pro-apoptosis.