Department of Occupational and Environmental Health, Nagoya University Graduate School of Medicine, Showa-ku, Aichi, Japan.
Arch Toxicol. 2012 Jan;86(1):63-74. doi: 10.1007/s00204-011-0704-3. Epub 2011 Apr 17.
Perfluorooctanoic acid is a ligand for peroxisome proliferator-activated receptor (PPARα). Ammonium perfluorooctanoate (APFO) at 0.1 and 0.3 mg/kg doses activated mouse PPARα, but not human PPARα. This study aimed to clarify whether milligram-order APFO can activate human PPARα, and the receptor is involved in APFO-induced chronic hepatic damage. Male Sv/129 wild-type (mPPARα), Pparα-null, and humanized PPARα (hPPARα) mice (8 weeks old) were divided into three groups. The first was treated with water and the other two with 1.0 and 5.0 mg/kg APFO for 6 weeks, orally, respectively. Both doses activated mouse and human PPARα to a similar or lower degree in the latter. APFO dose dependently increased hepatic triglyceride levels in Pparα-null and hPPARα mice, but conversely decreased those in mPPARα ones. APFO-induced hepatic damage differed markedly among the three genotyped groups: single-cell necrosis was observed in all genotyped mice; inflammatory cells and macrovesicular steatosis only in Pparα-null mice; and microvesicular steatosis and hydropic degenerations in hPPARα and Pparα-null mice. The molecular mechanism underlying these differences may be attributable to those of gene expressions involved in lipid homeostasis (PPARα, β- and ω-oxidation enzymes, and diacylglycerol acyltransferases) and uncoupling protein 2. Thus, milligram-order APFO activated both mouse and human PPARα in a different manner, which may reflect histopathologically different types of hepatic damage.
全氟辛酸是过氧化物酶体增殖物激活受体(PPARα)的配体。 0.1 和 0.3mg/kg 剂量的全氟辛基铵(APFO)激活了小鼠的 PPARα,但不激活人 PPARα。本研究旨在阐明毫克级 APFO 是否可以激活人 PPARα,以及该受体是否参与 APFO 诱导的慢性肝损伤。雄性 Sv/129 野生型(mPPARα)、Pparα 基因敲除和人源化 PPARα(hPPARα)小鼠(8 周龄)分为三组。第一组用饮用水处理,另外两组分别用 1.0 和 5.0mg/kg APFO 经口处理 6 周。后两者以相似或更低的程度激活了鼠和人 PPARα。APFO 剂量依赖性地增加了 Pparα 基因敲除和 hPPARα 小鼠的肝甘油三酯水平,但相反降低了 mPPARα 小鼠的肝甘油三酯水平。APFO 诱导的肝损伤在三种基因型组中差异明显:所有基因型小鼠均观察到单个细胞坏死;Pparα 基因敲除小鼠仅观察到炎症细胞和大泡性脂肪变性;hPPARα 和 Pparα 基因敲除小鼠仅观察到微泡性脂肪变性和水样变性。这些差异的分子机制可能归因于涉及脂质稳态(PPARα、β-和ω-氧化酶和二酰基甘油酰基转移酶)和解偶联蛋白 2 的基因表达的差异。因此,毫克级 APFO 以不同的方式激活了鼠和人 PPARα,这可能反映了肝损伤的组织病理学不同类型。