论文部分内容阅读
利用人源的白细胞弹性蛋白酶建立了一种快速、微量、灵敏的高通量体外筛选方法。利用该模型从微生物菌种库菌株的次生代谢产物中筛选得到一阳性真菌F02ZA-2554。该菌株发酵液经有机溶剂提取、硅胶柱层析、及HPLC ODS反相柱层析等活性跟踪下的分离纯化,得到活性化合物F02ZA-2554 A,该化合物对白细胞弹性蛋白酶有中等强度的抑制活性,其IC50为32.4μmol/L。通过对该化合物的紫外、质谱、核磁等理化分析,确定该化合物为蒽醌类化合物中的大黄素甲醚(physcion),该化合物的抗炎活性属首次报道。
Using human leukocyte elastase to establish a rapid, trace and sensitive high-throughput in vitro screening method. A positive fungi F02ZA-2554 was screened from the secondary metabolites of the strain of microbial strains using this model. The fermentation broth of the strain was separated and purified by organic solvent extraction, silica gel column chromatography and HPLC ODS reverse phase column chromatography to obtain the active compound F02ZA-2554 A, which has moderate inhibitory activity on leukocyte elastase , The IC50 was 32.4 μmol / L. The compound was identified as physcion in anthraquinones by physico-chemical analysis, such as UV, MS and NMR. The anti-inflammatory activity of the compound was reported for the first time.