Lau Patrick, Fitzsimmons Rebecca L, Raichur Suryaprakash, Wang Shu-Ching M, Lechtken Adriane, Muscat George E O
Institute for Molecular Bioscience, University of Queensland, Queensland, Australia.
J Biol Chem. 2008 Jun 27;283(26):18411-21. doi: 10.1074/jbc.M710526200. Epub 2008 Apr 25.
Homozygous staggerer mice (sg/sg) display decreased and dysfunctional retinoic acid receptor-related orphan receptor alpha (RORalpha) expression. We observed decreases in serum (and liver) triglycerides and total and high density lipoprotein serum cholesterol in sg/sg mice. Moreover, the sg/sg mice were characterized by reduced adiposity (associated with decreased fat pad mass and adipocyte size). Candidate-based expression profiling demonstrated that the dyslipidemia in sg/sg mice is associated with decreased hepatic expression of SREBP-1c, and the reverse cholesterol transporters, ABCA1 and ABCG1. This is consistent with the reduced serum lipids. The molecular mechanism did not involve aberrant expression of LXR and/or ChREBP. However, ChIP and transfection analyses revealed that RORalpha is recruited to and regulates the activity of the SREBP-1c promoter. Furthermore, the lean phenotype in sg/sg mice is also characterized by significantly increased expression of PGC-1alpha, PGC-1beta, and lipin1 mRNA in liver and white and brown adipose tissue from sg/sg mice. In addition, we observed a significant 4-fold increase in beta(2)-adrenergic receptor mRNA in brown adipose tissue. Finally, dysfunctional RORalpha expression protects against diet-induced obesity. Following a 10-week high fat diet, wild-type but not sg/sg mice exhibited a approximately 20% weight gain, increased hepatic triglycerides, and notable white and brown adipose tissue accumulation. In summary, these changes in gene expression (that modulate lipid homeostasis) in metabolic tissues are involved in decreased adiposity and resistance to diet-induced obesity in the sg/sg mice, despite hyperphagia. In conclusion, we suggest this orphan nuclear receptor is a key modulator of fat accumulation and that selective ROR modulators may have utility in the treatment of obesity.
纯合子蹒跚小鼠(sg/sg)表现出视黄酸受体相关孤儿受体α(RORα)表达减少且功能失调。我们观察到sg/sg小鼠的血清(和肝脏)甘油三酯以及血清总胆固醇和高密度脂蛋白胆固醇水平降低。此外,sg/sg小鼠的特征是肥胖程度降低(与脂肪垫质量和脂肪细胞大小减小有关)。基于候选基因的表达谱分析表明,sg/sg小鼠的血脂异常与肝脏中固醇调节元件结合蛋白-1c(SREBP-1c)以及逆向胆固醇转运蛋白ABCA1和ABCG1的表达降低有关。这与血清脂质降低一致。分子机制并不涉及肝X受体(LXR)和/或碳水化合物反应元件结合蛋白(ChREBP)的异常表达。然而,染色质免疫沉淀(ChIP)和转染分析显示,RORα被招募到SREBP-1c启动子并调节其活性。此外,sg/sg小鼠的消瘦表型还表现为肝脏以及白色和棕色脂肪组织中过氧化物酶体增殖物激活受体γ辅激活因子-1α(PGC-1α)、PGC-1β和脂素1 mRNA的表达显著增加。此外,我们观察到棕色脂肪组织中β2-肾上腺素能受体mRNA显著增加了4倍。最后,功能失调的RORα表达可预防饮食诱导的肥胖。在进行10周的高脂饮食后,野生型小鼠体重增加了约20%,肝脏甘油三酯增加,白色和棕色脂肪组织明显堆积,而sg/sg小鼠则没有。总之,尽管sg/sg小鼠食欲亢进,但代谢组织中这些调节脂质稳态的基因表达变化与肥胖程度降低和对饮食诱导肥胖的抵抗力有关。总之,我们认为这种孤儿核受体是脂肪积累的关键调节因子,选择性ROR调节剂可能对肥胖治疗有用。