Yoo Yeong-Min, Nam Jung-Hwan, Kim Min-Young, Choi Jongwon, Park Hee-Juhn
Department of Pharmaceutical Engineering, Sangji University, 660 Woosan-dong, Wonju 220-702, Kangwon-Do, South Korea.
Biol Pharm Bull. 2008 Apr;31(4):760-4. doi: 10.1248/bpb.31.760.
To identify the hepatoprotective component from the leaves of Cirsium setidens (Compositae), the methanolic extract was divided into two fractions, chloroform and butanol fractions, and their hepatoprotective efficacy was evaluated in a rat model of hepatic injury caused by D-galactosamine (GalN). Hepatoprotective activity was measured by the activity of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), and lactate dehydrogenase (LDH). Glutathione metabolism was measured via biochemical parameters such as glutathione (GSH), glutathione reductase (GR), gamma-glutamylcysteine synthetase (GCS), glutathione S-transferase (GST), and superoxide dismutase (SOD) levels. We subjected the butanol fraction, which had higher activity, to column chromatography to yield pectolinarin, which was further hydrolyzed to yield pectolinarigenin. Administration (10, 20 mg/kg, p.o.) of the main flavonoid glycoside component, pectolinarin, and its aglycone, pectolinarigenin, for 2 weeks significantly decreased the activity levels of AST, ALT, ALP and LDH, indicating that the two compounds have hepatoprotective activity. Pectolinarin and pectolinarigenin also increased activity levels of GSH, GR, GCS, and GST, as well as SOD. The significant effect was only seen in SOD activity. This suggests that the two components exhibit hepatoprotective activity mainly via SOD antioxidant mechanism.
为了从大蓟(菊科)叶中鉴定出具有肝脏保护作用的成分,将甲醇提取物分为氯仿和正丁醇两个馏分,并在D-半乳糖胺(GalN)诱导的肝损伤大鼠模型中评估它们的肝脏保护功效。通过血清天冬氨酸转氨酶(AST)、丙氨酸转氨酶(ALT)、碱性磷酸酶(ALP)和乳酸脱氢酶(LDH)的活性来测定肝脏保护活性。通过谷胱甘肽(GSH)、谷胱甘肽还原酶(GR)、γ-谷氨酰半胱氨酸合成酶(GCS)、谷胱甘肽S-转移酶(GST)和超氧化物歧化酶(SOD)水平等生化参数来测定谷胱甘肽代谢。我们对活性较高的正丁醇馏分进行柱色谱分离,得到橙皮苷,橙皮苷进一步水解得到橙皮素。主要黄酮苷成分橙皮苷及其苷元橙皮素以10、20 mg/kg的剂量口服给药2周,显著降低了AST、ALT、ALP和LDH的活性水平,表明这两种化合物具有肝脏保护活性。橙皮苷和橙皮素还提高了GSH、GR、GCS和GST以及SOD的活性水平。显著效果仅在SOD活性中观察到。这表明这两种成分主要通过SOD抗氧化机制发挥肝脏保护活性。