Herbal Research Laboratory, CSIR-Indian Institute of Toxicology Research (CSIR-IITR), Vishvigyan Bhawan, 31, Post Box No. 80, Mahatma Gandhi Marg, Lucknow-226001, India.
Food Funct. 2021 Jan 21;12(2):892-909. doi: 10.1039/d0fo02501a. Epub 2021 Jan 7.
Non-alcoholic fatty liver disease (NAFLD), a chronic metabolic disorder is concomitant with oxidative stress and inflammation. This study aimed to assess the effects of berbamine (BBM), a natural bisbenzylisoquinoline alkaloid with manifold biological activities and pharmacological effects on lipid, cholesterol and glucose metabolism in a rat model of NAFLD, and to explicate the potential mechanisms underlying its activity. BBM administration alleviated the increase in the body weight and liver index of HFD rats. The aberrations in liver function, serum parameters, and microscopic changes in the liver structure of HFD fed rats were significantly improved upon BBM administration. BBM also significantly attenuated oxidative damage and inhibited triglyceride and cholesterol synthesis. The SIRT1 deacetylase activity was also enhanced by BBM through liver kinase B1 and activated AMP-activated protein kinase. Activation of the SIRT1/LKB1/AMPK pathway prevented the downstream target ACC (acetyl-CoA carboxylase) and elevation in the expression of FAS (fatty acid synthase) and SCD1 (steroyl CoA desaturase). BBM also modulated the expression of PPARs maintaining the fatty acid homeostasis regulation. The assessment of berbamine induced ultrastructural changes by TEM analysis and the expression of autophagic markers LC3a/b, Beclin 1 and p62 revealed the induction of autophagy to alleviate fatty liver conditions. These results show novel findings that BBM induced protection against hepatic lipid metabolic disorders is achieved by regulating the SIRT1/LKB1/AMPK pathway, and thus it emerges as an effective phyoconstituent for the management of NAFLD.
非酒精性脂肪性肝病 (NAFLD) 是一种慢性代谢紊乱疾病,伴有氧化应激和炎症。本研究旨在评估小檗胺 (BBM) 对 NAFLD 大鼠模型脂质、胆固醇和葡萄糖代谢的影响,并阐明其活性的潜在机制。BBM 给药可减轻 HFD 大鼠体重和肝指数的增加。BBM 给药可显著改善 HFD 喂养大鼠的肝功能、血清参数和肝组织结构的微观变化。BBM 还可显著减轻氧化损伤,并抑制甘油三酯和胆固醇的合成。BBM 通过肝激酶 B1 和激活 AMP 激活的蛋白激酶增强 SIRT1 脱乙酰酶活性。SIRT1/LKB1/AMPK 通路的激活可防止下游靶标 ACC(乙酰辅酶 A 羧化酶)和 FAS(脂肪酸合酶)和 SCD1(硬脂酰辅酶 A 去饱和酶)的表达升高。BBM 还调节 PPARs 的表达,维持脂肪酸稳态调节。通过 TEM 分析评估 BBM 诱导的超微结构变化以及自噬标记物 LC3a/b、Beclin 1 和 p62 的表达,表明自噬的诱导可减轻脂肪肝状况。这些结果表明,BBM 通过调节 SIRT1/LKB1/AMPK 通路诱导对肝脂质代谢紊乱的保护作用,因此它成为 NAFLD 管理的有效植物成分。