27060-70-4

中文名称 Pentagamavunon-1

英文名称 Pentagamavunon-1

CAS 27060-70-4

分子式 C23H24O3

分子量 348.43

MOL 文件 27060-70-4.mol

更新日期 2023/03/20 15:41:23

27060-70-4 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 PENTAGAMAVUNON-1

英文别名

Pentagamavunon-1

物理化学性质

沸点562.1±50.0 °C(Predicted)

密度1.232±0.06 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO: 50 mg/mL (143.50 mM)

酸度系数(pKa)10.12±0.40(Predicted)

形态Solid

颜色Light yellow to yellow

常见问题列表

生物活性

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。

体外研究

Pentagamavunon-1 (PGV-1, 1, 2.5, 5, 7.5, 10, 15, and 20 µM) enhances cytotoxic effect of 5-FU on WiDr cells.
Pentagamavunon-1 (PGV-1, 1, 2.5, 5, and 10 µM) shows different effects on cell cycle progression and induces G2/M arrest.

Cell Viability Assay.

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.

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.

体内研究

Pentagamavunon-1 (PGV-1, po, 20 mg/kg) exhibits significant anti-tumor activity in PDX model, without obvious toxicity.

Animal Model:	Human cancer cells in a xenograf mouse model.
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.