上海交通大学学报（医学版）
上海交通大學學報（醫學版）
상해교통대학학보（의학판）
JOURNAL OF SHANGHAI JIAOTONG UNIVERSITY(MEDICAL SCIENCE)
2010年
1期
50-54
,共5页
墨旱莲%蟛蜞菊内酯%刀豆蛋白A%保肝作用%抗炎作用
墨旱蓮%蟛蜞菊內酯%刀豆蛋白A%保肝作用%抗炎作用
묵한련%팽기국내지%도두단백A%보간작용%항염작용
Eclipta%Wedelolactone%Concanavalin A%liver protection%anti-inflammatory effect
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,检测墨早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拈抗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.
目的 研究中藥墨旱蓮活性成分對刀豆蛋白A(ConA)誘導的小鼠肝損傷的作用.方法 以尾靜脈註射ConA(15 mg/kg)建立小鼠肝損傷模型,檢測墨早蓮提取物對正常小鼠和肝損傷小鼠血清穀丙轉氨酶(ALT)的影響,觀察肝髒的組織學改變.生物活性跟蹤分離得到單體化閤物,根據IR譜、~(13)C-NMR譜、~1H-NMR譜、~1H-~(13)C HMBC譜和~1H-~(13)C HMQC譜鑒定其結構.結果 墨旱蓮提取物能降低肝損傷小鼠的血清ALT水平,對抗ConA誘導的小鼠肝細胞凋亡.體外篩選的活性化閤物經波譜鑒定為蟛蜞菊內酯,屬香豆素類化閤物,能選擇性抑製ConA誘導的T細胞活化,10μg/mL的蟛蜞菊內酯可完全拈抗ConA的誘導作用.結論 中藥墨旱蓮具有抗ConA誘導的小鼠肝損傷作用,活性成分蟛蜞菊內酯具有較彊的抗炎和抗凋亡作用,是一箇潛在的抗炎保肝新藥的先導化閤物.
목적 연구중약묵한련활성성분대도두단백A(ConA)유도적소서간손상적작용.방법 이미정맥주사ConA(15 mg/kg)건립소서간손상모형,검측묵조련제취물대정상소서화간손상소서혈청곡병전안매(ALT)적영향,관찰간장적조직학개변.생물활성근종분리득도단체화합물,근거IR보、~(13)C-NMR보、~1H-NMR보、~1H-~(13)C HMBC보화~1H-~(13)C HMQC보감정기결구.결과 묵한련제취물능강저간손상소서적혈청ALT수평,대항ConA유도적소서간세포조망.체외사선적활성화합물경파보감정위팽기국내지,속향두소류화합물,능선택성억제ConA유도적T세포활화,10μg/mL적팽기국내지가완전념항ConA적유도작용.결론 중약묵한련구유항ConA유도적소서간손상작용,활성성분팽기국내지구유교강적항염화항조망작용,시일개잠재적항염보간신약적선도화합물.
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.
