147444-03-9
147444-03-9 结构式
基本信息
pyripyropene A
2H,11H-Naphtho[2,1-b]pyrano[3,4-e]pyran-11-one, 3,6-bis(acetyloxy)-4-[(acetyloxy)methyl]-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-12-hydroxy-4,6a,12b-trimethyl-9-(3-pyridinyl)-, (3S,4R,4aR,6S,6aS,12R,12aS,12bS)-
物理化学性质
常见问题列表
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 |