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目的:研究牛耳枫水提物的化学成分及其抗胆碱脂酶活性。方法:采用硅胶柱色谱,Sephadex LH-20柱色谱,MCI柱色谱和制备液相色谱等方法对牛耳枫的化学成分进行分离纯化,并根据理化性质、核磁共振谱法、质谱法以及参考相关文献鉴定化合物结构;采用UPLC-MS/MS方法测定化合物的抗乙酰胆碱酯酶(ACh E)及丁酰胆碱酯酶(BCh E)活性。结果:从牛耳枫乙酸乙酯部位和正丁醇部位分离得到7个化合物,分别鉴定为5-oxymaltol(1),secodaphniphylline(2),2,6-dimethyl-3-hydroxychromone(3),deoxycalyciphylline B(4),calyciphylline A(5),daphnezzomine M(6),deoxyisocalyciphylline B(7)。其中化合物4和7具有抗ACh E活性,半数抑制浓度(IC50)分别为(128.83±21.41)μmol·L~(-1)和(56.15±11.02)μmol·L~(-1);化合物2,4,5和7具有抗BCh E酶活性,IC50分别为(0.31±0.15),(54.53±3.33),(811.17±22.49)μmol·L~(-1)和(8.13±0.78)μmol·L~(-1)。结论:化合物1和3为首次从该植物中分离获得,化合物2和化合物7具有较强的抗BCh E活性,具有开发为胆碱酯酶抑制剂的潜力。
Objective: To study the chemical constituents and anti-cholinesterase activities of the aqueous extract of Celastrus glaucus. Methods: The constituents of Boswellia serrata were separated and purified by silica gel, Sephadex LH-20, MCI and preparative liquid chromatography (HPLC) The compound structure was identified; the compound was tested for its activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using UPLC-MS / MS method. Results: Seven compounds were isolated from the ethyl acetate fraction and the n-butanol fraction of Celastrus angustifolia and identified as 5-oxymaltol (1), secodaphniphylline (2), 2,6-dimethyl-3-hydroxychromone (3) and deoxycalyciphylline B 4), calyciphylline A (5), daphnezzomine M (6), deoxyisocalyciphylline B (7). Compounds 4 and 7 exhibited anti-ACh E activity with IC50 values of (128.83 ± 21.41) μmol·L -1 and (56.15 ± 11.02) μmol·L -1, respectively. Compounds 2, 4, 5 and 7 had anti-BChE activity with IC50 of (0.31 ± 0.15), (54.53 ± 3.33), (811.17 ± 22.49) μmol·L -1 and (8.13 ± 0.78) μmol·L -1, respectively (-1). CONCLUSION: Compounds 1 and 3 were isolated from this plant for the first time. Compounds 2 and 7 possess strong anti-BCh E activity and potential for developing cholinesterase inhibitors.