Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.In Vitro: Pentagamavunon-1 (PGV-1, 1, 2.5, 5, 7.5, 10, 15, and 20 μM) enhances cytotoxic effect of 5-FU on WiDr cells.
Pentagamavunon-1 (PGV-1, 1, 2.5, 5, and 10 μM) shows different effects on cell cycle progression and induces G2/M arrest.
In Vivo: Pentagamavunon-1 (PGV-1, po, 20 mg/kg) exhibits significant anti-tumor activity in PDX model, without obvious toxicity.