上海交通大学学报（医学版）

›› 2010, Vol. 30 ›› Issue (1): 50-.

• 论著（基础研究） • 上一篇    下一篇

墨旱莲活性成分对刀豆蛋白A诱导的小鼠肝损伤的作用

徐汝明, 邓克敏, 陆 阳   

  1. 上海交通大学医学院 药学系, 上海 200025
  • 出版日期:2010-01-26 发布日期:2010-01-26
  • 通讯作者: 陆 阳, 电子信箱: huaxue@shsmu.edu.cn。
  • 作者简介:徐汝明（1965—）, 女, 满族, 副教授, 博士；电子信箱: jyxurm@shsmu.edu.cn。
  • 基金资助:

    上海市教委重点学科建设项目(第五期)（J50201）

Protective effect of active component of Eclipta on hepatic injury induced by ConA in mice

XU Ru-ming, DENG Ke-min, LU Yang   

  1. Department of Pharmacy, School of Medicine, Shanghai Jiaotong University, Shanghai 200025, China
  • Online:2010-01-26 Published:2010-01-26
  • Supported by:

    Shanghai Education Committee Foundation, J50201

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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（15 mg/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-13C HMBC谱和1H-13C HMQC谱鉴定其结构。结果 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，10 μg/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

Abstract:

Objective 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, 13C-NMR, 1H-NMR, 1H-13C HMBC and 1H-13C HMQC were used for structural identification. Results Eclipta extracts decreased serum ALT in hepatic injury mice induced by ConA, and demonstrated anti-apoptosis effect induced by ConA in hepatocytes. Wedelolactone, a coumarin, 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 10 μg/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.

Key words: Eclipta, Wedelolactone, Concanavalin A, liver protection, anti-inflammatory effect