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目的:对黄芩苷进行化学修饰得到8-(N,N-二甲基-胺甲基)-黄芩苷,对其结构进行初步分析并探讨其抑菌作用,为拓展其应用范围进行初步研究。方法:通过Mannich反应制备8-(N,N-二甲基-胺甲基)-黄芩苷,采用HPLC检测其纯度,质谱碳谱对其结构进行初步分析。选用8种标准菌株和其中2种细菌的临床菌株为受试菌株,以8-(N,N-二甲基-胺甲基)-黄芩苷为实验组,黄芩苷为对照组,检测8-(N,N-二甲基-胺甲基)-黄芩苷和黄芩苷对受试菌株的最低抑菌浓度(MIC)、MIC50、MIC90和最低杀菌浓度(MBC)。结果:HPLC检测8-(N,N-二甲基-胺甲基)-黄芩苷的纯度为91.4%,质谱鉴定其相对分子质量为504.1501,并经碳谱检测对其结构进行了初步确认。抑菌实验结果显示,8-(N,N-二甲基-胺甲基)-黄芩苷和黄芩苷对受试菌株均有一定的抑菌效果。8-(N,N-二甲基-胺甲基)-黄芩苷对大肠埃希氏菌、肺炎克雷伯氏菌、福氏志贺氏菌、铜绿假单胞菌标准菌株的MIC、MIC50、MIC90、MBC明显小于黄芩苷,有显著性差异(P<0.05)。结论:8-(N,N-二甲基-胺甲基)-黄芩苷对大肠埃希氏菌、肺炎克雷伯氏菌、福氏志贺氏菌、铜绿假单胞菌标准菌株的抑菌效果优于黄芩苷。
OBJECTIVE: The chemical modification of baicalin to give 8- (N, N-dimethyl-aminomethyl) -baiarin glycosides is carried out. The structure of baicalin is preliminary analyzed and the antibacterial activity is explored. Methods: 8- (N, N-dimethyl-aminomethyl) -baicin was prepared by Mannich reaction. The purity of the product was determined by HPLC. The structure of the product was analyzed by mass spectrum. Eight clinical isolates and two kinds of bacterial strains were selected as the tested strains. 8- (N, N-dimethyl-aminomethyl) -baicin as experimental group and baicalin as control group, The minimum inhibitory concentration (MIC), MIC50, MIC90 and minimum bactericidal concentration (MBC) of (N, N - dimethyl - aminomethyl) - baicalin and baicalin against the tested strains were determined. Results: The purity of 8- (N, N-dimethyl-aminomethyl) -baicinalin was 91.4% by HPLC. The relative molecular mass was identified as 504.1501 by mass spectrometry. The structure of the purified product was initially confirmed by carbon spectrum. Bacteriostasis test results showed that 8- (N, N-dimethyl-aminomethyl) -baiarin and baicalin had a certain antibacterial effect on the tested strains. The MICs of 8- (N, N-dimethyl-aminomethyl) -baicinalin against Escherichia coli, Klebsiella pneumoniae, Shigella flexneri and Pseudomonas aeruginosa standard strains, MIC50 , MIC90, MBC were significantly less than baicalin, there was a significant difference (P <0.05). Conclusion: The inhibitory effect of 8- (N, N-dimethyl-aminomethyl) -calcium baicalensisin on Escherichia coli, Klebsiella pneumoniae, Shigella flexneri and Pseudomonas aeruginosa Bacteria better than baicalin.