Pyripyropene A is a potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC₅₀ of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo^[4].

Pyripyropene A (0-100 µM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC₅₀ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Hayashi A, et al. Pyripyropenes, fungal sesquiterpenes conjugated with alpha-pyrone and pyridine moieties, exhibits anti-angiogenic activity against human umbilical vein endothelial cells. Biol Pharm Bull. 2009 Jul;32(7):1261-5.  [Content Brief]

  . Ohtawa M, et al. Design and Synthesis of A-Ring Simplified Pyripyropene A Analogues as Potent and Selective Synthetic SOAT2 Inhibitors. ChemMedChem. 2018 Mar 6;13(5):411-421.  [Content Brief]

  . Ohshiro T, et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15.  [Content Brief]

  [4]. Lee KR , et al. Determination of Penicillium griseofulvum-oriented pyripyropene A, a selective inhibitor of acyl-coenzyme A:cholesterol acyltransferase 2, in mouse plasma using liquid chromatography-tandem mass spectrometry and its application to pharmaco  [Content Brief]