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目的:内生菌作为一种良好的生物资源,已产生许多结构新颖、活性多样的代谢产物,在进行药用植物内生菌的研究中,分离得到了一株踝节菌属真菌,该属真菌是一个产多样代谢产物的真菌,从该内生菌中分离鉴定环肽类成分,并研究其乙酰胆碱酯酶抑制活性。方法:利用柱色谱法,包括硅胶柱色谱、大孔树脂柱色谱和小孔树脂(MCI)凝胶柱色谱等分离化合物;利用波谱方法,包括氢核磁共振、碳核磁共振、电喷雾质谱等鉴定化合物结构;采用改良的Ellman法测定化合物的乙酰胆碱酯酶抑制活性。结果:分离鉴定了4个环肽,它们分别鉴定为discarine-M(1),fumitremorgin C(2),fructigenine B(3),spirotryprostatin A(4),化合物1显示了中等强度的抗乙酰胆碱酯酶活性,其半抑制浓度(IC50)56μmol·L-1。结论:分离的4个化合物均为从踝节菌属(Talaromyces)真菌中首次分得。
Objective: Endophyte as a good biological resources, has produced many novel and diverse metabolites, active in the study of medicinal plant endophytes, isolated from a strain of Talaromyces fungi, the genus Fungus is a fungus that produces a variety of metabolites. From this endophytic fungus, the components of cyclic peptides were isolated and their acetylcholinesterase inhibitory activities were studied. Methods: The compounds were isolated by column chromatography, including silica gel column chromatography, macroporous resin column chromatography and MCI gel column chromatography. Their structures were identified by spectral methods including 1HNMR, carbon nuclear magnetic resonance and electrospray ionization mass spectrometry Compound structure; Compounds were tested for their acetylcholinesterase inhibitory activity using a modified Ellman method. RESULTS: Four cyclic peptides were isolated and identified as discarine-M (1), fumitremorgin C (2), fructigenine B (3) and spirotryprostatin A (4) respectively. Compound 1 showed moderate-intensity anti-acetylcholinesterase Activity, its half inhibitory concentration (IC50) 56μmol·L-1. Conclusion: The four compounds isolated were isolated from the fungus Talaromyces for the first time.