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墨旱莲活性成分对刀豆蛋白A诱导的小鼠肝损伤的作用
引用本文:徐汝明,邓克敏,陆阳. 墨旱莲活性成分对刀豆蛋白A诱导的小鼠肝损伤的作用[J]. 上海交通大学学报(医学版), 2010, 30(1): 50-54
作者姓名:徐汝明  邓克敏  陆阳
作者单位:上海交通大学医学院药学系,上海,200025
基金项目:上海市教委重点学科建设项目(第五期)
摘    要:目的研究中药墨旱莲活性成分对刀豆蛋白A(ConA)诱导的小鼠肝损伤的作用。方法以尾静脉注射ConA(15mg/kg)建立小鼠肝损伤模型,检测墨旱莲提取物对正常小鼠和肝损伤小鼠血清谷丙转氨酶(ALT)的影响,观察肝脏的组织学改变。生物活性跟踪分离得到单体化合物,根据IR谱、^13C—NMR谱、^1H—NMR谱、^1H-^13CHMBC谱和1H-^13CHMQC谱鉴定其结构。结景墨旱莲提取物能降低肝损伤小鼠的血清ALT水平,对抗ConA诱导的小鼠肝细胞凋亡。体外筛选的活性化合物经波谱鉴定为蟛蜞菊内酯,属香豆素类化合物,能选择性抑制ConA诱导的T细胞活化,10μg/mL的蟛蜞菊内酯可完全拮抗ConA的诱导作用。结论中药墨旱莲具有抗ConA诱导的小鼠肝损伤作用,活性成分蟛蜞菊内酯具有较强的抗炎和抗凋亡作用,是一个潜在的抗炎保肝新药的先导化合物。

关 键 词:墨旱莲  蟛蜞菊内酯  刀豆蛋白A  保肝作用  抗炎作用

Protective effect of active component of Eclipta on hepatic injury induced by ConA in mice
XU Ru-ming,DENG Ke-min,LU Yang. Protective effect of active component of Eclipta on hepatic injury induced by ConA in mice[J]. Journal of Shanghai Jiaotong University:Medical Science, 2010, 30(1): 50-54
Authors:XU Ru-ming  DENG Ke-min  LU Yang
Affiliation:Department of Pharmacy, School of Medicine, Shanghai Jiaotong University, Shanghai 200025, China
Abstract:Objecave To explore the protective effect of active component of Eclipta on hepatic injury induced by Concanavalin A(ConA)in mice. Methods Mouse hepatic injury models were established by injection of ConA(15 mg/kg)via tail vein.The effect of Eclipta extracts on serum alanine aminotransferase (ALT) and liver histology in both normal mice and hepatic injury mice was examined.A pure compound was obtained by means of bioactivity-guided isolation,and IR,~(13)C-NMR, ~1H-NMR,~1H-~(13)C HMBC and ~1H-~(13)C HMQC were used for structural identiffcation. Results Eclipta extracts decreased serum ALT in hepatic injury mice induced by ConA.and demonstrated anti-apoptosis effect induced by ConA in hepatoeytes.Wedelolaetone,a eoumarin,was isolated from Eclipta,and its structure was identified on the basis of spectroscopic analysis.Wedelolactone inhibited ConA-induced T cell proliferation selectively,and completely antagonized the effect of ConA at the concentration of 10μg/mL. Conclusion Eclipta herb has hepatoprotective effect.Wedelolactone,the anti-inflammatory and anti-apoptosis active component of Eclipta,might serve as a lead compound for developing new antiinflammatory drugs.
Keywords:Eclipta  Wedelolactone  Concanavalin A  liver protection  anti-inflammatory effect
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