Stewart Adele, Maity Biswanath, Anderegg Simon P, Allamargot Chantal, Yang Jianqi, Fisher Rory A
Department of Pharmacology and.
Central Microscopy Facility, University of Iowa Carver College of Medicine, Iowa City, IA 52242.
Proc Natl Acad Sci U S A. 2015 Feb 17;112(7):E786-95. doi: 10.1073/pnas.1418795112. Epub 2015 Feb 2.
Alcohol is the most commonly abused drug worldwide, and chronic alcohol consumption is a major etiological factor in the development of multiple pathological sequelae, including alcoholic cardiomyopathy and hepatic cirrhosis. Here, we identify regulator of G protein signaling 6 (RGS6) as a critical regulator of both alcohol-seeking behaviors and the associated cardiac and hepatic morbidities through two mechanistically divergent signaling actions. RGS6(-/-) mice consume less alcohol when given free access and are less susceptible to alcohol-induced reward and withdrawal. Antagonism of GABA(B) receptors or dopamine D2 receptors partially reversed the reduction in alcohol consumption in RGS6(-/-) animals. Strikingly, dopamine transporter inhibition completely restored alcohol seeking in mice lacking RGS6. RGS6 deficiency was associated with alterations in the expression of genes controlling dopamine (DA) homeostasis and a reduction in DA levels in the striatum. Taken together, these data implicate RGS6 as an essential regulator of DA bioavailability. RGS6 deficiency also provided dramatic protection against cardiac hypertrophy and fibrosis, hepatic steatosis, and gastrointestinal barrier dysfunction and endotoxemia when mice were forced to consume alcohol. Although RGS proteins canonically function as G-protein regulators, RGS6-dependent, alcohol-mediated toxicity in the heart, liver, and gastrointestinal tract involves the ability of RGS6 to promote reactive oxygen species-dependent apoptosis, an action independent of its G-protein regulatory capacity. We propose that inhibition of RGS6 might represent a viable means to reduce alcohol cravings and withdrawal in human patients, while simultaneously protecting the heart and liver from further damage upon relapse.
酒精是全球最常被滥用的药物,长期饮酒是多种病理后遗症发生发展的主要病因,包括酒精性心肌病和肝硬化。在此,我们通过两种机制不同的信号传导作用,确定G蛋白信号调节因子6(RGS6)是酒精寻求行为以及相关心脏和肝脏疾病的关键调节因子。RGS6基因敲除小鼠在自由获取酒精时饮酒量较少,且对酒精诱导的奖赏和戒断反应不敏感。拮抗GABA(B)受体或多巴胺D2受体可部分逆转RGS6基因敲除动物酒精摄入量的减少。引人注目的是,抑制多巴胺转运体可完全恢复缺乏RGS6小鼠的酒精寻求行为。RGS6缺乏与控制多巴胺(DA)稳态的基因表达改变以及纹状体中DA水平降低有关。综上所述,这些数据表明RGS6是DA生物利用度的重要调节因子。当小鼠被迫饮酒时,RGS6缺乏还对心脏肥大和纤维化、肝脂肪变性、胃肠道屏障功能障碍和内毒素血症提供了显著的保护作用。尽管RGS蛋白通常作为G蛋白调节剂发挥作用,但RGS6依赖的酒精介导的心脏、肝脏和胃肠道毒性涉及RGS6促进活性氧依赖性细胞凋亡的能力,这一作用独立于其G蛋白调节能力。我们提出,抑制RGS6可能是减少人类患者酒精渴望和戒断反应的一种可行方法,同时保护心脏和肝脏在复发时免受进一步损伤。