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、^(13)C-NMR谱、~1H-NMR谱、~1H-^(13)C HMBC谱和~1H-^(13)C 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,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。
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 hepatoeytes. Wedelolactone, 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 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.
出处
《上海交通大学学报（医学版）》
CAS
CSCD
北大核心
2010年第1期50-54,共5页
Journal of Shanghai Jiao tong University:Medical Science
基金
上海市教委重点学科建设项目(第五期)(J50201)~~
关键词
墨旱莲
蟛蜞菊内酯
刀豆蛋白A
保肝作用
抗炎作用
Eclipta
Wedelolactone
Concanavalin A
liver protection
anti-inflammatory effect
