内溶酶体和胆固醇在阿尔茨海默病发病机制中的作用:他汀类药物可能无法提供临床益处的原因

Xuesong Chen, Liang Hui, Jonathan D Geiger
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引用次数: 0

摘要

胆固醇稳态的改变和低密度脂蛋白(LDL)胆固醇水平的升高是散发性阿尔茨海默病(AD)发病的一个重要危险因素。正因为如此,他汀类药物家族被广泛用于降低胆固醇水平,试图预防和/或减轻阿尔茨海默病的神经发病机制。不幸的是,迄今为止积累的证据不足以支持继续使用他汀类药物作为抗AD的可行药物治疗方法。为了理解这些复杂且相互关联的问题,重要的是回顾胆固醇稳态改变是如何导致AD发病的,以及为什么他汀类药物对AD没有临床疗效。载脂蛋白对各种脂质和控制胆固醇摄取的受体具有不同的亲和力,可导致胆固醇在神经元内运输和分布的巨大差异。apoE4的存在或血浆LDL胆固醇水平升高可导致一系列类似于在尼曼-皮克C型病中观察到的溶酶体脂质储存障碍的情况,如胆固醇返回内质网(ER)、高尔基体和质膜的再循环受损,质膜胆固醇缺乏,以及内溶酶体胆固醇积累增加导致内溶酶体功能障碍。因此,使用他汀类药物阻断内质网胆固醇合成不仅可能进一步降低质膜胆固醇水平,从而扰乱突触完整性,还可能增加内溶酶体的胆固醇负荷,从而加重内溶酶体功能障碍。因此,与他汀类药物一起使用降胆固醇策略并没有给AD患者带来临床益处也就不足为奇了。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Role of endolysosomes and cholesterol in the pathogenesis of Alzheimer's disease: Insights into why statins might not provide clinical benefit.

Role of endolysosomes and cholesterol in the pathogenesis of Alzheimer's disease: Insights into why statins might not provide clinical benefit.

Altered cholesterol homeostasis in general and increased levels of low-density lipoprotein (LDL) cholesterol specifically is a robust risk factor for the pathogenesis of sporadic Alzheimer's disease (AD). Because of this, the family of drugs known as statins have been tried extensively to lower cholesterol levels in attempting to prevent and/or lessen the neuropathogenesis of AD. Unfortunately, evidence accumulated to date is insufficient to support the continued use of statins as a viable pharmacotherapeutic approach against AD. To understand these complex and inter-related issues it is important to review how altered cholesterol homeostasis contributes to AD pathogenesis and why statins have not provided clinical benefit against AD. Apolipoproteins with their different affinities for various lipids and the receptors that control cholesterol uptake can result in drastic differences in cholesterol trafficking into and its distribution within neurons. The presence of the apoE4 or elevated plasma levels of LDL cholesterol can lead to a set of conditions that resembles lysosomal lipid storage disorders observed in Niemann-Pick type C disease such as impaired recycling of cholesterol back to the endoplasmic reticulum (ER), Golgi and plasma membranes, cholesterol deficiencies in plasma membranes, and increased cholesterol accumulation in endolysosomes resulting in endolysosome dysfunction. Consequently, the use of statins to block cholesterol synthesis in ER might not only decrease further plasma membrane cholesterol levels thus disturbing synaptic integrity, but also could also increase cholesterol burden in endolysosomes thus worsening endolysosome dysfunction. Therefore, it is not surprising that the use of cholesterol-lowering strategies with statins has not resulted in clinical benefit for patients living with AD.

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