Pentagamavunon-1 (PGV-1) is an oral Curcumin analog that effectively induces apoptosis through multiple molecular mechanisms. It primarily targets and inhibits key angiogenic factors, including cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF), which play crucial roles in mediating cell proliferation and survival. Additionally, PGV-1 possesses the ability to inhibit the activation of NF-κB, further enhancing its apoptotic effects. [1]

Pentagamavunon-1 (PGV-1, 1, 2.5, 5, 7.5, 10, 15, and 20 μM) enhances cytotoxic effect of 5-FU on WiDr cells [1]. Pentagamavunon-1 (PGV-1, 1, 2.5, 5, and 10 μM) shows different effects on cell cycle progression and induces G2/M arrest [1]. Cell Viability Assay [1]. Cell Line: Human colon carcinoma WiDr. Concentration: 1, 2.5, 5, 7.5, 10, 15, and 20 μM. Incubation Time: 6, 12, 24, and 48 hours. Result: Significantly enhanced the cytotoxicity of 5-FU on WiDr cells at various concentrations during 6, 12, 24, and 48 h incubation. Cell Cycle Analysis [1]. Cell Line: WiDr cells. Concentration: 1, 2.5, 5, and 10 μM. Incubation Time: 24 h. Result: The non-treated WiDr cells showed cell accumulation in G1, S, and G2/M phase about 50.85%, 36.11% and 13.04%, respectively.

Pentagamavunon-1 (PGV-1, po, 20 mg/kg) exhibits significant anti-tumor activity in PDX model, without obvious toxicity [1]. Animal Model: Human cancer cells in a xenograf mouse model [2]. Dosage: 20mg/kg. Administration: P.O. every 2 days for 20 days. Result: Exhibited little decrease in body weight, nor a decrease in white and red blood cell counts in peripheral blood, nor any other efects in behavior and macroscopic appearance. Thus, PGV-1 was sufciently potent to suppress tumor formation in vivo, but exhibited little or no obvious adverse effects on the normal lineage of cells.