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首页> 外文期刊>Life sciences >Effects of FR145237, an acyl-CoA:cholesterol acyltransferase inhibitor, on diet-induced hypercholesterolemia in diabetic rats.
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Effects of FR145237, an acyl-CoA:cholesterol acyltransferase inhibitor, on diet-induced hypercholesterolemia in diabetic rats.

机译：酰基辅酶A：胆固醇酰基转移酶抑制剂FR145237对饮食诱导的糖尿病大鼠高胆固醇血症的影响。

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摘要

Recent studies have shown that acyl-CoA:cholesterol acyltransferase (ACAT) plays an important role in the initiation of diabetes-associated hypercholesterolemia. To confirm this hypothesis, effects of a potent ACAT inhibitor, FR145237, on diet-induced hypercholesterolemia were examined in streptozotocin (STZ)-induced diabetic rats. One-week feeding of 1% cholesterol and 0.5% cholic acid to normal rats and STZ-induced diabetic rats increased plasma cholesterol levels in both groups, and the response was more remarkable in the STZ rats than in the normal ones (1266 +/- 476 mg/dl and 146 +/- 7 mg/dl, respectively). FR145237 dose-dependently reduced the rise in plasma cholesterol levels in the STZ rats and the levels were almost normalized by treatment with 1 mg/kg/day of the compound. These results suggest that hyperresponse to dietary cholesterol was induced in the STZ rats and that ACAT is involved in the hyperresponse. The effects of FR145237 on other plasma lipids such as high density lipoprotein (HDL) cholesterol and triglyceride (TG) levels were also examined.
机译：最近的研究表明，酰基辅酶A：胆固醇酰基转移酶（ACAT）在引发糖尿病相关的高胆固醇血症中起重要作用。为了证实这一假设，在链脲佐菌素（STZ）诱导的糖尿病大鼠中检查了有效的ACAT抑制剂FR145237对饮食诱导的高胆固醇血症的影响。正常大鼠和STZ诱导的糖尿病大鼠每周喂食1％胆固醇和0.5％胆酸会增加两组的血浆胆固醇水平，STZ大鼠的反应比正常大鼠更为显着（1266 +/-分别为476 mg / dl和146 +/- 7 mg / dl）。 FR145237剂量依赖性地降低了STZ大鼠血浆胆固醇水平的升高，并且通过用1 mg / kg /天的化合物治疗，该水平几乎得以标准化。这些结果表明在STZ大鼠中诱导了对饮食胆固醇的过度反应，并且ACAT参与了过度反应。还检查了FR145237对其他血浆脂质（如高密度脂蛋白（HDL）胆固醇和甘油三酸酯（TG））的影响。

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