3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂对酰基辅酶A：胆固醇酰基转移酶的抑制作用
Inhibition of acyl coenzyme A: cholesterol acyltransferase by 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors.
作者信息
Ishida F, Sato A, Iizuka Y, Kamei T
出版信息
Chem Pharm Bull (Tokyo). 1989 Jun;37(6):1635-6. doi: 10.1248/cpb.37.1635.
Relatively high concentrations of MK-733 (simvastatin) and MK-803 (lovastatin, mevinolin), which are 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, were found to inhibit acyl coenzyme A: cholesterol acyltransferase (ACAT) of rabbit intestinal microsomes with IC50's of 2.0 x 10(-5) and 3.6 x 10(-5) M, respectively. Dihydroxy acid forms of both MK-733 and MK-803 did not inhibit ACAT activity. A kinetic analysis using a Lineweaver-Burk plot indicated that MK-733 is a competitive inhibitor of ACAT, with a Ki value of 1.2 x 10(-5) M.
相对高浓度的MK - 733（辛伐他汀）和MK - 803（洛伐他汀，美伐他汀），它们是3 - 羟基 - 3 - 甲基戊二酰辅酶A（HMG - CoA）还原酶抑制剂，被发现能抑制兔肠道微粒体的酰基辅酶A：胆固醇酰基转移酶（ACAT），其半数抑制浓度（IC50）分别为2.0×10⁻⁵和3.6×10⁻⁵ M。MK - 733和MK - 803的二羟基酸形式均不抑制ACAT活性。使用Lineweaver - Burk图进行的动力学分析表明，MK - 733是ACAT的竞争性抑制剂，其抑制常数（Ki）值为1.2×10⁻⁵ M。
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