4'-O-Methylglabridin

4'-O-Methylglabridin is an apoptosis (apoptosis) inducer with antioxidant, cell cycle interference, and anticancer cytotoxic properties. It effectively inhibits various cancer cell lines, including liver, breast, and colorectal cancers. This compound promotes cell accumulation in subG1 and G2/M phases by reducing phosphorylation of Rb (Ser807/811) and p21 protein expression. It triggers caspase-dependent apoptosis through cytochrome C release and Caspase-9 activation. Additionally, 4'-O-Methylglabridin exhibits antioxidant effects by inhibiting lipid peroxidation levels and decreasing β-carotene consumption, thereby preventing LDL oxidation. It is useful in research related to various cancers and atherosclerotic diseases.

4'-O-Methylglabridin effectively inhibits the proliferation of Huh7, MCF7, and HCT116 cancer cell lines in vitro at concentrations ranging from 2.5 to 40 μM over 72 hours, with the strongest activity observed in Huh7 cells (IC 50 = 9.6 μM). It shows a time-dependent inhibition of Huh7 cell proliferation (IC 50; 24 h, 48 h, 72 h), as the IC 50 value increases from 7.31 μM at 24 hours to 11.4 μM at 72 hours. When Huh7 cells are treated with 10 μM of 4'-O-Methylglabridin for 48 hours, apoptotic nuclear changes occur, accompanied by subG1 phase accumulation and G2/M phase arrest. The compound induces caspase-dependent apoptosis in Huh7 cells by increasing cytochrome C release and activating caspase-9, while also reducing phosphorylation levels of Rb, p53, Mdm2, and p21, thereby disrupting cell cycle regulation. In a cell-free β-carotene-linoleic acid assay, 4'-O-Methylglabridin (50 μM; 90 min; 50°C) inhibits 78% of β-carotene consumption. Additionally, it potently inhibits AAPH-induced oxidation of human LDL in vitro (30 μM; 2 h; 37°C).