Department of Metabolic Regulation, Shinshu University School of Medicine, 3-1-1 Asahi, Matsumoto, Nagano, 390-8621, Japan.
Department of Nephrology, Shinshu University School of Medicine, 3-1-1 Asahi, Matsumoto, Nagano, 390-8621, Japan.
Arch Toxicol. 2019 Jan;93(1):149-161. doi: 10.1007/s00204-018-2335-4. Epub 2018 Oct 19.
Peroxisome proliferator-activated receptor α (PPARα) is involved in the regulation of fatty acid and cholesterol metabolism. A high-cholesterol (HC) diet increases the risk of developing cardiovascular diseases (CVD); however, it is unclear whether the toxic effects of cholesterol involve changes in thrombotic factor expression, and whether PPARα is necessary for such effects. To investigate this possibility, we fed a HC diet to wild-type (WT) and Ppara-null mice and measured cholesterol and triglyceride contents, liver histology, serum/plasma levels of coagulation factors, hepatic expression of the coagulation factors, liver/serum sulfatide levels, hepatic sulfatide metabolism, hepatic expression of lipid transporters, and hepatic oxidative stress and its relating enzymes. In Ppara-null mice, the HC diet caused triglyceride accumulation and exacerbated inflammation and oxidative stress in liver, increased levels of coagulation factors, including tissue factor, plasminogen activator inhibitor-1 and carboxypeptidase B2 in blood and liver, and decreased levels of anti-thrombotic sulfatides in serum and liver. These changes were much less marked in WT mice. These findings imply that cholesterol overload exerts its toxic effects at least in part by enhancing thrombosis, secondary to abnormal hepatic lipid metabolism, inflammation, and oxidative stress. Moreover, we reveal for the first time that PPARα can attenuate these toxic effects by transcriptional regulation of coagulation factors and sulfatides, in addition to its known effects of controlling lipid homeostasis and suppressing inflammation and oxidative stress. Therapies aimed at activating PPARα might prevent HC diet-induced CVD through modulating various pro- and anti-thrombotic factors.
过氧化物酶体增殖物激活受体 α(PPARα)参与脂肪酸和胆固醇代谢的调节。高胆固醇(HC)饮食会增加患心血管疾病(CVD)的风险;然而,胆固醇的毒性作用是否涉及血栓形成因子表达的变化,以及 PPARα 是否是这种作用所必需的,目前尚不清楚。为了研究这种可能性,我们用 HC 饮食喂养野生型(WT)和 Ppara 基因敲除(KO)小鼠,并测量胆固醇和甘油三酯含量、肝组织学、血清/血浆凝血因子水平、肝脏凝血因子表达、肝/血清硫酸酯水平、肝硫酸酯代谢、肝脂质转运蛋白表达以及肝氧化应激及其相关酶。在 Ppara 基因敲除(KO)小鼠中,HC 饮食导致甘油三酯积累,并加剧肝脏炎症和氧化应激,增加血液和肝脏中包括组织因子、纤溶酶原激活物抑制剂-1 和羧肽酶 B2 在内的凝血因子水平,并降低血清和肝脏中抗血栓形成的硫酸酯水平。在 WT 小鼠中,这些变化则不那么明显。这些发现表明,胆固醇过载至少部分通过增强血栓形成发挥其毒性作用,这是由于肝脏脂质代谢、炎症和氧化应激异常所致。此外,我们首次揭示 PPARα 可以通过转录调节凝血因子和硫酸酯来减轻这些毒性作用,除了其已知的控制脂质稳态、抑制炎症和氧化应激的作用。通过调节各种促血栓形成和抗血栓形成因子,激活 PPARα 的治疗方法可能预防 HC 饮食引起的 CVD。