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Troglitazone, an Antidiabetic Agent, Inhibits Cholesterol Biosynthesis Through a Mechanism Independent of Peroxisome Proliferator-Activated Receptor-γ

机译:曲格列酮是一种抗糖尿病药,通过过氧化物酶体增殖物激活的受体-γ独立的机制抑制胆固醇的生物合成。

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摘要

Troglitazone is an antidiabetic agent of the thiazo- lidinedione family. It is generally believed that thiazo- lidinediones exert their insulin-sensitizing activity through activation of peroxisome proliferator-activated receptor-γ (PPAR-γ), a member of the steroid nuclear receptor superfamily. In the present study, we examined the effect of troglitazone on cholesterol biosynthesis in cultured Chinese hamster ovary (CHO) cell. Troglita- zone inhibited biosynthesis of cholesterol, but not that of total sterols, in a dose-dependent manner, with a half- maximal concentration (IC_50) value of 8 μmol/1.
机译:曲格列酮是噻唑烷二酮家族的抗糖尿病药。一般认为,噻唑烷二酮通过类固醇核受体超家族成员过氧化物酶体增殖物激活受体-γ(PPAR-γ)的活化而发挥其胰岛素敏感性。在本研究中,我们检查了曲格列酮对培养的中国仓鼠卵巢(CHO)细胞中胆固醇生物合成的影响。曲格列酮区以剂量依赖性方式抑制胆固醇的生物合成,但不抑制总固醇的生物合成,半数最大浓度(IC_50)值为8μmol/ 1。

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