Crabb David W, Galli Andrea, Fischer Monika, You Min
Department of Medicine, Indiana University, Emerson Hall, Room 317, 545 Barnhill Drive, Indianapolis, IN 46202, USA.
Alcohol. 2004 Aug;34(1):35-8. doi: 10.1016/j.alcohol.2004.07.005.
Normal function of the peroxisome proliferator-activated receptor alpha (PPARalpha) is crucial for the regulation of hepatic fatty acid metabolism. Fatty acids serve as ligands for PPARalpha, and when fatty acid levels increase, activation of PPARalpha induces a battery of fatty acid-metabolizing enzymes to restore fatty acid levels to normal. Hepatic fatty acid levels are increased during ethanol consumption. However, results of in vitro work showed that ethanol metabolism inhibited the ability of PPARalpha to bind DNA and activate reporter genes. This observation has been further studied in mice. Four weeks of ethanol feeding of C57BL/6J mice also impairs fatty acid catabolism in liver by blocking PPARalpha-mediated responses. Ethanol feeding decreased the level of retinoid X receptor alpha (RXRalpha) as well as the ability of PPARalpha/RXR in liver nuclear extracts to bind its consensus sequence, and the levels of mRNAs for several PPARalpha-regulated genes were reduced [long-chain acyl coenzyme A (acyl-CoA) dehydrogenase and medium-chain acyl-CoA dehydrogenase] or failed to be induced (acyl-CoA dehydrogenase, liver carnitine palmitoyl-CoA transferase I, very long-chain acyl-CoA synthetase, very long-chain acyl-CoA dehydrogenase) in livers of the ethanol-fed animals. Consistent with this finding, ethanol feeding did not induce the rate of fatty acid beta-oxidation, as assayed in liver homogenates. Inclusion of WY14,643, a PPARalpha agonist, in the diet restored the DNA-binding activity of PPARalpha/RXR, induced mRNA levels of several PPARalpha target genes, stimulated the rate of fatty acid beta-oxidation in liver homogenates, and prevented fatty liver in ethanol-fed animals. Blockade of PPARalpha function during ethanol consumption contributes to the development of alcoholic fatty liver, which can be overcome by WY14,643.
过氧化物酶体增殖物激活受体α(PPARα)的正常功能对于肝脏脂肪酸代谢的调节至关重要。脂肪酸作为PPARα的配体,当脂肪酸水平升高时,PPARα的激活会诱导一系列脂肪酸代谢酶,使脂肪酸水平恢复正常。乙醇摄入期间肝脏脂肪酸水平会升高。然而,体外实验结果表明,乙醇代谢会抑制PPARα与DNA结合并激活报告基因的能力。这一观察结果已在小鼠中得到进一步研究。对C57BL/6J小鼠进行四周的乙醇喂养,也会通过阻断PPARα介导的反应损害肝脏中的脂肪酸分解代谢。乙醇喂养降低了视黄醇X受体α(RXRα)的水平以及肝核提取物中PPARα/RXR结合其共有序列的能力,并且几种PPARα调节基因的mRNA水平在乙醇喂养动物的肝脏中降低[长链酰基辅酶A(酰基辅酶A)脱氢酶和中链酰基辅酶A脱氢酶]或未能被诱导(酰基辅酶A脱氢酶、肝脏肉碱棕榈酰辅酶A转移酶I、极长链酰基辅酶A合成酶、极长链酰基辅酶A脱氢酶)。与这一发现一致,如在肝脏匀浆中检测到的,乙醇喂养并未诱导脂肪酸β氧化速率。在饮食中添加PPARα激动剂WY14,643可恢复PPARα/RXR的DNA结合活性,诱导几种PPARα靶基因的mRNA水平,刺激肝脏匀浆中的脂肪酸β氧化速率,并预防乙醇喂养动物的脂肪肝。乙醇摄入期间PPARα功能的阻断有助于酒精性脂肪肝的发展,而WY14,643可以克服这一问题。