Das Kaberi P, Wood Carmen R, Lin Mimi T, Starkov Anatoly A, Lau Christopher, Wallace Kendall B, Corton J Christopher, Abbott Barbara D
Toxicity Assessment Division, National Health and Environmental Effects Research Laboratory, US Environmental Protection Agency, 109 TW Alexander Dr., Research Triangle Park, NC 27711, USA.
Department of Biomedical Sciences, University of Minnesota Medical School, Duluth, MN 55812, USA.
Toxicology. 2017 Mar 1;378:37-52. doi: 10.1016/j.tox.2016.12.007. Epub 2016 Dec 31.
Persistent presence of perfluoroalkyl acids (PFAAs) in the environment is due to their extensive use in industrial and consumer products, and their slow decay. Biochemical tests in rodent demonstrated that these chemicals are potent modifiers of lipid metabolism and cause hepatocellular steatosis. However, the molecular mechanism of PFAAs interference with lipid metabolism remains to be elucidated. Currently, two major hypotheses are that PFAAs interfere with mitochondrial beta-oxidation of fatty acids and/or they affect the transcriptional activity of peroxisome proliferator-activated receptor α (PPARα) in liver. To determine the ability of structurally-diverse PFAAs to cause steatosis, as well as to understand the underlying molecular mechanisms, wild-type (WT) and PPARα-null mice were treated with perfluorooctanoic acid (PFOA), perfluorononanoic acid (PFNA), or perfluorohexane sulfonate (PFHxS), by oral gavage for 7days, and their effects were compared to that of PPARα agonist WY-14643 (WY), which does not cause steatosis. Increases in liver weight and cell size, and decreases in DNA content per mg of liver, were observed for all compounds in WT mice, and were also seen in PPARα-null mice for PFOA, PFNA, and PFHxS, but not for WY. In Oil Red O stained sections, WT liver showed increased lipid accumulation in all treatment groups, whereas in PPARα-null livers, accumulation was observed after PFNA and PFHxS treatment, adding to the burden of steatosis observed in control (untreated) PPARα-null mice. Liver triglyceride (TG) levels were elevated in WT mice by all PFAAs and in PPARα-null mice only by PFNA. In vitro β-oxidation of palmitoyl carnitine by isolated rat liver mitochondria was not inhibited by any of the 7 PFAAs tested. Likewise, neither PFOA nor PFOS inhibited palmitate oxidation by HepG2/C3A human liver cell cultures. Microarray analysis of livers from PFAAs-treated mice indicated that the PFAAs induce the expression of the lipid catabolism genes, as well as those involved in fatty acid and triglyceride synthesis, in WT mice and, to a lesser extent, in PPARα-null mice. These results indicate that most of the PFAAs increase liver TG load and promote steatosis in mice We hypothesize that PFAAs increase steatosis because the balance of fatty acid accumulation/synthesis and oxidation is disrupted to favor accumulation.
全氟烷基酸(PFAAs)在环境中的持续存在是由于它们在工业和消费品中的广泛使用以及其缓慢的降解过程。对啮齿动物的生化测试表明,这些化学物质是脂质代谢的强效调节剂,并会导致肝细胞脂肪变性。然而,PFAAs干扰脂质代谢的分子机制仍有待阐明。目前,两个主要假说是PFAAs干扰脂肪酸的线粒体β-氧化和/或它们影响肝脏中过氧化物酶体增殖物激活受体α(PPARα)的转录活性。为了确定结构多样的PFAAs导致脂肪变性的能力,并了解其潜在的分子机制,野生型(WT)和PPARα基因敲除小鼠通过口服灌胃给予全氟辛酸(PFOA)、全氟壬酸(PFNA)或全氟己烷磺酸(PFHxS)7天,并将它们的作用与不会导致脂肪变性的PPARα激动剂WY-14643(WY)进行比较。在WT小鼠中,所有化合物均观察到肝脏重量和细胞大小增加,每毫克肝脏的DNA含量降低,在PPARα基因敲除小鼠中,PFOA、PFNA和PFHxS也观察到了这些现象,但WY没有。在油红O染色切片中,WT肝脏在所有治疗组中均显示脂质积累增加,而在PPARα基因敲除肝脏中,PFNA和PFHxS处理后观察到积累,加重了对照(未处理)PPARα基因敲除小鼠中观察到的脂肪变性负担。所有PFAAs均使WT小鼠肝脏甘油三酯(TG)水平升高,而在PPARα基因敲除小鼠中,仅PFNA使TG水平升高。所测试的7种PFAAs均未抑制离体大鼠肝脏线粒体对棕榈酰肉碱的体外β-氧化。同样,PFOA和PFOS均未抑制HepG2/C3A人肝细胞培养物中棕榈酸的氧化。对PFAAs处理小鼠肝脏的微阵列分析表明,PFAAs在WT小鼠中诱导脂质分解代谢基因以及参与脂肪酸和甘油三酯合成的基因的表达,在PPARα基因敲除小鼠中诱导程度较小。这些结果表明,大多数PFAAs会增加小鼠肝脏TG负荷并促进脂肪变性。我们假设PFAAs会增加脂肪变性,因为脂肪酸积累/合成与氧化之间的平衡被打破,有利于积累。