27060-70-4
中文名稱
Pentagamavunon-1
英文名稱
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 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)562.1±50.0 °C(Predicted)
密度1.232±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 50 mg/mL (143.50 mM)
酸度系數(shù)(pKa)10.12±0.40(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
Pentagamavunon-1 (PGV-1) 是Curcumin 的類似物，具有口服活性，通過(guò)多個(gè)機(jī)制誘導(dǎo)凋亡信號(hào)，如抑制COX-2 和 VEGF。Pentagamavunon-1 (PGV-1) 可抑制 NF-κB 的激活。體外研究
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. |
體內(nèi)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. |