Department of Pharmacy, Anhui Medical University, Hefei bHefei XinFeng Co. Ltd, Hefei, Anhui 230032, China.
J Pharm Pharmacol. 2011 Apr;63(4):587-93. doi: 10.1111/j.2042-7158.2011.01256.x. Epub 2011 Mar 3.
Nonalcoholic steatohepatitis (NASH), a metabolic disorder of the liver, may gradually evolve into fibrosis or cirrhosis. Recent studies have suggested that geniposide can effectively inhibit experimental liver fibrosis. Therefore, the aim of this study was to determine whether geniposide can influence the early phase of fibrogenesis in an animal model of NASH.
Male Sprague-Dawley rats were given a high fat diet alone or the same diet combined with geniposide at doses of 25, 50 or 100 mg/kg for six weeks. Ten rats received corresponding solvent as a normal control.
Treatment with geniposide could improve liver histology through reducing the elevated liver index (liver weight/body weight), serum alanine aminotransferase and aspartate aminotransferase. Total cholesterol, triglycerides and free fatty acids in serum and liver decreased in geniposide-treated rats. Furthermore, geniposide increased serum insulin levels but reduced serum tumour necrosis factor-α level in high-fat diet rats. In addition, geniposide suppressed expression of CYP2E1 and increased peroxisome proliferator-activated receptor-α (PPARα) expression. These benefits may be associated with increased superoxide dismutase and decreased malondialdehyde in liver.
Geniposide exerts protective effects against hepatic steatosis in rats fed with a high fat diet; the underlying mechanism may be associated with its antioxidant actions or regulation of adipocytokine release and expression of PPARα.
非酒精性脂肪性肝炎(NASH)是一种肝脏代谢紊乱,可能逐渐发展为纤维化或肝硬化。最近的研究表明,京尼平苷能有效抑制实验性肝纤维化。因此,本研究旨在确定京尼平苷是否能影响 NASH 动物模型中肝纤维化的早期阶段。
雄性 Sprague-Dawley 大鼠单独给予高脂肪饮食或相同饮食联合京尼平苷 25、50 或 100mg/kg 治疗 6 周。10 只大鼠给予相应溶剂作为正常对照。
京尼平苷治疗可通过降低升高的肝指数(肝重/体重)、血清丙氨酸氨基转移酶和天冬氨酸氨基转移酶来改善肝组织学。京尼平苷治疗大鼠血清和肝脏总胆固醇、甘油三酯和游离脂肪酸降低。此外,京尼平苷增加了高脂肪饮食大鼠的血清胰岛素水平,但降低了血清肿瘤坏死因子-α水平。此外,京尼平苷抑制 CYP2E1 的表达,增加过氧化物酶体增殖物激活受体-α(PPARα)的表达。这些益处可能与肝脏中超氧化物歧化酶的增加和丙二醛的减少有关。
京尼平苷对高脂肪饮食喂养的大鼠肝脂肪变性具有保护作用;其作用机制可能与其抗氧化作用或调节脂肪细胞因子释放和 PPARα 的表达有关。