Department of Pathology, University of Pittsburgh School of Medicine, Pittsburgh, PA, United States.
J Hepatol. 2013 May;58(5):993-9. doi: 10.1016/j.jhep.2013.01.011. Epub 2013 Jan 20.
BACKGROUND & AIMS: Pharmacological approaches can potentially improve fatty liver condition in alcoholic and non-alcoholic fatty liver diseases. The salutary effects of reducing lipid synthesis or promoting lipid oxidation have been well reported, but the benefits of increasing lipid degradation have yet to be well explored. Macroautophagy is a cellular degradation process that can remove subcellular organelles including lipid droplets. We thus investigated whether pharmacological modulation of macroautophagy could be an effective approach to alleviate fatty liver condition and liver injury.
C57BL/6 mice were given ethanol via intraperitoneal injection (acute) or by a 4-week oral feeding regime (chronic), or high fat diet for 12 weeks. An autophagy enhancer, carbamazepine or rapamycin, or an autophagy inhibitor, chloroquine, was given before sacrifice. Activation of autophagy, level of hepatic steatosis, and blood levels of triglycerides, liver enzyme, glucose and insulin were measured.
In both acute and chronic ethanol condition, macroautophagy was activated. Carbamazepine, as well as rapamycin, enhanced ethanol-induced macroautophagy in hepatocytes in vitro and in vivo. Hepatic steatosis and liver injury were exacerbated by chloroquine, but alleviated by carbamazepine. The protective effects of carbamazepine and rapamycin in reducing steatosis and in improving insulin sensitivity were also demonstrated in high fat diet-induced non-alcoholic fatty liver condition.
These findings indicate that pharmacological modulation of macroautophagy in the liver can be an effective strategy for reducing fatty liver condition and liver injury.
药理学方法可能有助于改善酒精性和非酒精性脂肪性肝病中的脂肪肝状况。减少脂质合成或促进脂质氧化的有益作用已有相关报道,但增加脂质降解的益处尚未得到充分探索。巨自噬是一种细胞降解过程,可以去除包括脂滴在内的亚细胞细胞器。因此,我们研究了药理学调节巨自噬是否可以作为一种有效方法来减轻脂肪肝状况和肝损伤。
通过腹腔注射(急性)或 4 周口服喂养(慢性)给予 C57BL/6 小鼠乙醇,或给予高脂肪饮食 12 周。在处死前给予自噬增强剂卡马西平或雷帕霉素,或自噬抑制剂氯喹。测量自噬的激活、肝脂肪变性的程度以及甘油三酯、肝酶、血糖和胰岛素的血液水平。
在急性和慢性乙醇条件下,巨自噬均被激活。卡马西平以及雷帕霉素增强了乙醇诱导的肝细胞内巨自噬的体外和体内作用。氯喹加剧了肝脂肪变性和肝损伤,但卡马西平减轻了这种损伤。卡马西平和雷帕霉素在改善胰岛素敏感性的同时,还减轻了高脂肪饮食诱导的非酒精性脂肪性肝病中的脂肪变性。
这些发现表明,肝脏巨自噬的药理学调节可能是减轻脂肪肝状况和肝损伤的有效策略。