Institute of Liver Diseases, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Zhangheng Road, Pudong District, Shanghai, 201203, People's Republic of China.
J Pharmacol Exp Ther. 2013 Mar;344(3):646-54. doi: 10.1124/jpet.112.201137. Epub 2012 Dec 31.
Puerarin, an isoflavone component extracted from Kudzu (Pueraria lobata), has been demonstrated to alleviate alcohol-related disorders. Our study examined whether puerarin ameliorates chronic alcoholic liver injury through inhibition of endotoxin gut leakage, the subsequent Kupffer cell activation, and endotoxin receptors expression. Rats were provided with the Liber-DeCarli liquid diet for 8 weeks. Puerarin (90 mg/kg or 180 mg/kg daily) was orally administered from the beginning of the third week until the end of the experiment. Chronic alcohol intake caused increased serum alanine aminotransferase, aspartate aminotransferase, hepatic gamma-glutamyl transpeptidase, and triglyceride levels as well as fatty liver and neutrophil infiltration in hepatic lobules as determined by biochemical and histologic assays. A significant increase of liver tumor necrosis factor α was detected by enzyme-linked immunosorbent assay. These pathologic effects correlated with increased endotoxin level in portal vein and upregulated protein expression of hepatic CD68, lipopolysaccharide-binding protein, CD14, Toll-like receptor 2, and Toll-like receptor 4. Meanwhile, the intestinal microvilli were observed to be sparse, shortened, and irregularity in distribution under the transmission electron microscope in conjunction with the downregulated intestinal zonula occludens-1 protein expression. These hepatic pathologic changes were significantly inhibited in puerarin-treated animals as were the endotoxin levels and hepatic CD68 and endotoxin receptors. Moreover, the pathologic changes in intestinal microvillus and the decreased intestinal zonula occludens-1 were also ameliorated with puerarin treatment. These results thus demonstrate that puerarin inhibition of endotoxin gut leakage, Kupffer cell activation, and endotoxin receptors expression is involved in the alleviation of chronic alcoholic liver injury in rats.
葛根素是从野葛(Pueraria lobata)中提取的一种异黄酮成分,已被证明可缓解与酒精相关的疾病。我们的研究旨在探讨葛根素是否通过抑制内毒素肠道渗漏、随后的枯否细胞激活和内毒素受体表达来改善慢性酒精性肝损伤。大鼠给予 Liber-DeCarli 液体饮食 8 周。从第三周开始,每天给予葛根素(90mg/kg 或 180mg/kg)口服,直至实验结束。慢性酒精摄入导致血清丙氨酸氨基转移酶、天冬氨酸氨基转移酶、肝γ-谷氨酰转肽酶和三酰甘油水平升高,肝小叶脂肪变性和中性粒细胞浸润增加,生化和组织学检测结果显示。酶联免疫吸附试验检测到肝肿瘤坏死因子α显著增加。这些病理效应与门静脉内毒素水平升高以及肝 CD68、脂多糖结合蛋白、CD14、Toll 样受体 2 和 Toll 样受体 4 蛋白表达上调相关。同时,电镜下观察到肠微绒毛稀疏、缩短、分布不规则,同时肠紧密连接蛋白-1 表达下调。这些肝病理变化在葛根素治疗动物中明显受到抑制,内毒素水平和肝 CD68 及内毒素受体也受到抑制。此外,葛根素治疗还改善了肠微绒毛的病理变化和下调的肠紧密连接蛋白-1。这些结果表明,葛根素抑制内毒素肠道渗漏、枯否细胞激活和内毒素受体表达,参与了大鼠慢性酒精性肝损伤的缓解。