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) at concentrations ranging from 1 to 20 μM significantly enhances the cytotoxic effect of 5-fluorouracil (5-FU) on WiDr human colon carcinoma cells, as demonstrated through various incubation periods of 6, 12, 24, and 48 hours, thus suggesting a potentiated anti-cancer effect. Additionally, at lower concentrations (1, 2.5, 5, and 10 μM), PGV-1 distinctly influences cell cycle progression, leading to G2/M phase arrest after 24 hours of treatment. This indicates PGV-1’s dual mechanism of action: enhancing 5-FU cytotoxicity and altering cell cycle dynamics.

Pentagamavunon-1 (PGV-1, po, 20 mg/kg) exhibited significant anti-tumor effects in a Patient-Derived Xenograft (PDX) model without apparent toxicity. Administered orally at 20 mg/kg every two days for 20 days, PGV-1 inhibited tumor growth in a human cancer cell xenograft mouse model, showing negligible impact on body weight, white and red blood cell counts, behavior, and macroscopic appearance.