啶南平 A
啶南平 A 性质
| 熔点 | 153-154℃ |
|---|---|
| 沸点 | 690.8±55.0 °C(Predicted) |
| 密度 | 1.33±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| 溶解度 | DMSO：可溶；甲醇：可溶 |
| 酸度系数(pKa) | 11.72±0.70(Predicted) |
| 形态 | 白色至棕色粉末。 |
| 颜色 | 淡粉色至铁锈棕色 |
啶南平 A 用途与合成方法
IC50: 0.07 µM (ACAT2)
Pyripyropene A (0-100 µM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC
50
value of 1.8 µM.
Pyripyropene A (10 µM ; 24 hours) inhibits VEGF (20 ng/ml)-induced migration and tubular formation of HUVECs in dose-dependent fashion.
Pyripyropene A do not show growth inhibitory effects against KB3-1, K562 and Neuro2A cells.
Cell Proliferation Assay
| Cell Line: | HUVECs |
| Concentration: | 0-100 µM |
| Incubation Time: | 72 hours |
| Result: | Exhibited anti-proliferative activity against HUVECs with an IC 50 value of 1.8 µM. |
Pyripyropene A (10-50 mg/kg per day; p.o; 12 weeks) reduces the levels of plasma cholesterol, very-low-density lipoprotein (VLDL), and low-density lipoprotein (LDL) and hepatic cholesterol content in apolipoprotein E-knockout mice. And Pyripyropene A-treated mice display reduction of atherogenic lesion areas in the aortae and heart.
Pyripyropene A inhibits the hepatic e acyl–coenzyme A:cholesterol acyltransferase 2 (ACAT2) activity in vivo.
Pyripyropene A displays a half-life (t
1/2
) of 0.693/λ, where λ represented the terminal slope of the log-linear portion of concentration time profile.
| Animal Model: | Male C57BL/6 mice |
| Dosage: | 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg |
| Administration: | Oral administration; daily; for 12 weeks |
| Result: | Reduced atherogenic lesion areas in the aortae and heart. |
| Animal Model: | 9-week old male ICR mice (pharmacokinetic analysis) |
| Dosage: | 5 mg/kg ,10 mg/kg |
| Administration: | Oral administration |
| Result: | t 1/2 = 0.693/λ |
