Pyripyropene A 是一种高效、选择性的SOAT2/ACAT2抑制剂,其IC50值为 0.07 μM。Pyripyropene A 在体内能减轻高胆固醇血症和动脉粥样硬化。
生物活性 | Pyripyropene A is a potent and selectivesterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterolacyltransferase2 (ACAT2)inhibitor, with anIC50of 0.07 μM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo[1][2][3][4]. |
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体外研究 (In Vitro) | Pyripyropene A (0-100 μM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC50value of 1.8 μM[1]. Pyripyropene A (10 μM ; 24 hours) inhibits VEGF (20 ng/ml)-induced migration and tubular formation of HUVECs in dose-dependent fashion[1]. Pyripyropene A do not show growth inhibitory effects against KB3-1, K562 and Neuro2A cells[1].
Cell Proliferation Assay[1] Cell Line: | HUVECs | Concentration: | 0-100 μM | Incubation Time: | 72 hours | Result: | Exhibited anti-proliferative activity against HUVECs with an IC50value of 1.8 μM. |
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体内研究 (In Vivo) | 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[3]. Pyripyropene A inhibits the hepatic e acyl–coenzyme A:cholesterol acyltransferase 2 (ACAT2) activity in vivo[3]. Pyripyropene A displays a half-life (t1/2) of 0.693/λ, where λ represented the terminal slope of the log-linear portion of concentration time profile[4].
Animal Model: | Male C57BL/6 mice[2] | 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)[4] | Dosage: | 5 mg/kg ,10 mg/kg | Administration: | Oral administration | Result: | t1/2= 0.693/λ |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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