Pentagamavunon-1 (PGV-1) 是Curcumin 的类似物，具有口服活性，通过多个机制诱导凋亡信号，如抑制COX-2 和 VEGF。Pentagamavunon-1 (PGV-1) 可抑制 NF-κB 的激活。
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].
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.
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].
[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.
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