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本研究分别以丁酰硫代胆碱和二硫二硝基苯甲酸为底物和显色剂 ,建立了一种准确、快速的高通量筛选微生物代谢产物来源的抑制剂的体外筛选模型。利用此方法从 2 14 1株放线菌中筛选到一株阳性菌株N98 10 2 1,该菌株的发酵液经有机溶剂提取、ODS柱层析及HPLC制备分离 ,得到一个活性化合物N98 10 2 1A ,该化合物对乙酰胆碱酯酶的IC50 为 2 0 μmol/L ,经酶抑制动力学分析 ,该化合物为乙酰胆碱酯酶的非竞争性可逆抑制剂。通过对该化合物的紫外、红外、质谱、核磁等理化分析 ,得知该化合物与terferol结构相同。但该化合物对乙酰胆碱脂酶的抑制活性至今未见报道。
In this study, butyrylthiocholine and dithiobisnitrobenzoic acid were used as substrate and chromogenic reagent respectively to establish an accurate and rapid in vitro screening model for high-throughput screening of inhibitors of microbial metabolites. A positive strain of N98 10 2 1 was screened from 2 14 1 strains of actinomycetes using this method. The fermentation broth of this strain was separated by organic solvent extraction, ODS column chromatography and HPLC. An active compound N98 10 2 1A The compound has an IC50 of 20 μmol / L for acetylcholinesterase, which is a noncompetitive reversible inhibitor of acetylcholinesterase by enzymatic inhibition kinetics. The physico-chemical analysis of the compound by UV, IR, MS and NMR showed that the compound has the same structure as terferol. However, the inhibitory activity of the compound on acetylcholinesterase has not been reported.