Ezetimibe, an inhibitor of Niemann-Pick C1-like 1 protein, decreases cholesteryl ester transfer protein in type 2 diabetes mellitus.
Ezetimibe, an inhibitor of Niemann-Pick C1-like 1 protein, decreases cholesteryl ester transfer protein in type 2 diabetes mellitus.
复制标题
Ezetimibe 是一种 Niemann-Pick C1-like 1 蛋白抑制剂，可降低 2 型糖尿病中的胆固醇酯转移蛋白。
作者：
H. Yagyu;Shuichi Nagashima;Manabu Takahashi;Michiaki Miyamoto;K. Okada;J. Osuga;S. Ishibashi
为了了解依折麦布对高密度脂蛋白（HDL）代谢的影响，测量了 2 型糖尿病（T2DM）患者的 HDL 亚类、胆固醇酯转移蛋白（CETP）和卵磷脂胆固醇酰基转移酶（LCAT）。 23 名患有 T2DM 的高胆固醇血症患者每天接受 10 mg 依折麦布治疗，持续 12 周。测量血浆总胆固醇(TC)、低密度脂蛋白(LDL)-胆固醇(C)、HDL-C、HDL(2)-C、HDL(3)-C、CETP质量和LCAT活性。依折麦布治疗后，HDL-C 和 HDL(2)-C 分别增加 5% (p<0.05) 和 12% (p<0.01)。在 23 名患者中，21 名 CETP 质量减少，平均减少 20% (p<0.0001)。 LCAT 活性也降低了 6% (p<0.01)。 HDL(2)-C 和 CETP 质量之间较基线的变化呈显着正相关，而 HDL(3)-C 和 CETP 质量之间呈显着负相关。此外，HDL-C的变化与LCAT活性的变化呈正相关。总之，依折麦布可能影响 T2DM 患者的 HDL 代谢并逆转胆固醇转运，尤其是 CETP。这些观察结果可能为了解依折麦布如何预防动脉粥样硬化提供一些见解。
To address the effects of ezetimibe on high-density lipoprotein (HDL) metabolism, the HDL subclasses, cholesteryl ester transfer protein (CETP), and lecithin-cholesterol acyltransferase (LCAT) were measured in patients with type 2 diabetes mellitus (T2DM). Twenty-three hypercholesterolemic patients with T2DM were treated with 10 mg of ezetimibe daily for 12 weeks. Plasma total cholesterol (TC), low-density lipoprotein (LDL)-cholesterol (C), HDL-C, HDL(2)-C, HDL(3)-C, CETP mass, and LCAT activity were measured. HDL-C and HDL(2)-C increased by 5% (p<0.05) and 12% (p<0.01), respectively, in response to ezetimibe. Of the 23 patients, 21 had decreased CETP mass, which led to an average reduction of 20% (p<0.0001). LCAT activity also decreased by 6% (p<0.01). A significant positive correlation was found in the changes from baseline between HDL(2)-C and CETP mass, whereas a significant inverse relationship was observed between HDL(3)-C and CETP mass. Furthermore, the change in HDL-C was positively correlated with the change in LCAT activity. In conclusion, ezetimibe may affect HDL metabolism and reverse cholesterol transport, especially CETP, in T2DM. These observations may provide some insights into how ezetimibe prevents atherosclerosis.