Pentagamavunon-1

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[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> COX

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

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.

[1]. Edy Meiyanto, et al. Curcumin Analog Pentagamavunon-1 (PGV-1) Sensitizes Widr Cells to 5-Fluorouracil Through Inhibition of NF-κB Activation. Asian Pac J Cancer Prev. 2018 Jan 27;19(1):49-56.

[2]. Beni Lestari, et al. Pentagamavunon-1 (PGV-1) Inhibits ROS Metabolic Enzymes and Suppresses Tumor Cell Growth by Inducing M Phase (Prometaphase) Arrest and Cell Senescence. Sci Rep . 2019 Oct 16;9(1):14867.