apigenin + vorinostat

**apigenin + vorinostat** is an experimental combination drug that merges the plant-derived flavonoid apigenin with the histone deacetylase inhibitor vorinostat, either as a physical mixture or as a novel conjugated small molecule (APIGENIN–VORINOSTAT-CONJUGATE, AVC)[1][3][5][7]. Apigenin exerts anticancer effects through inhibition of cell migration, modulation of epigenetic regulators, induction of cell cycle arrest, and activation of pro-apoptotic markers. Vorinostat inhibits HDAC enzymes altering histone acetylation and gene expression, thereby suppressing tumor cell proliferation and inducing apoptosis. The conjugate (AVC) exhibits synergistic activity, markedly inhibiting proliferation in leukemic (AML)[1][3] and triple-negative breast cancer (TNBC) cells[5][7]. Mechanistically, AVC antagonizes HDAC family members (notably HDAC1, HDAC2, HDAC3, and HDAC6), upregulates p21CIP1 protein and acetylated-histone H3, and suppresses survival/proliferative signaling by targeting c-Kit and PI3K and ATP-binding site occupancy by apigenin. Preclinical studies demonstrate potent anti-leukemic and anti-TNBC properties with relatively low toxicity toward normal tissues[1][3][5][7].

Other names

apigenin + vorinostatapigenin-vorinostat conjugateAVC