8-(N,N-二甲基-胺甲基)-黄芩苷的结构修饰与抑菌作用研究

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: To obtain 8-(N, N-dimethyl-amine methyl)-baicalin by chemical modification of baicalin, make a preliminary analysis of the structure and discuss the bacteriostasis of 8-(N, N-dimethyl-amine methyl)-baicalin, so as to expand the field of application of 8-(N, N-dimethyl-amine methyl)-baicalin. Methods: 8-(N, N-dimethyl-amine methyl)-baicalin was prepared by Mannich reaction, its purity was detected by HPLC and a preliminary analysis of the structure was detected by mass spectrometric detection and carbon spectrum detection.Eight standard strains and two clinical isolated strains were selected as the tested strains to detect the minimal inhibitory concentrations(MIC), MIC₅₀, MIC₉₀ and the minimum bactericidal concentration(MBC)of 8-(N, N-dimethyl-amine methyl)-baicalin, and the matched data of baicalin as the control group were detected. Results: The purity of 8-(N, N-dimethyl-amine methyl)-baicalin detected by HPLC was 91.4% and the relative molecular mass detected by mass spectrometric detection was 504.1501.The structure of 8-(N, N-dimethyl-amine methyl)-baicalin was preliminarily confirmed by carbon spectrum detection.The results of the antibacterial experiment showed that 8-(N, N-dimethyl-amine methyl)-baicalin and baicalin were found to have certain bacteriostatic effects on the tested strains.The MIC, MIC₅₀, MIC₉₀ and MBC of 8-(N, N-dimethyl-amine methyl)-baicalin were significantly lower than those of baicalin on the standard strains of Escherichia coli, Klebsiella pneumonia, Shigella flexneri and Pseudomonas aeruginosa(P<0.05). Conclusion: The antibacterial effect of 8-(N, N-dimethyl-amine methyl)-baicalin is obviously better than that of baicalin on the standard strains of Escherichia coli, Klebsiella pneumonia, Shigella flexneri and Pseudomonas aeruginosa.