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。
产品描述
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].
体外活性
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.
体内活性
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.
Cas No.
27060-70-4
分子式
C23H24O3
分子量
348.43
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years