摘要
目的为深入了解小檗碱与生物大分子核酸的作用关系,探讨小檗碱类化合物的分子药理机制方法采用荧光分析技术观察小檗碱及其8-烷基修饰物与质粒DNA作用后的荧光光谱变化规律。结果与小檗碱比较,短链烷基(乙基、丁基、己基和辛基)修饰后的小檗碱衍生物与质粒DNA作用后的荧光强度增强,其中8-丁基小檗碱表现出最强作用,长链烷基(十二烷基、十六烷基)则相反。同时发现,所有小檗碱烷基修饰物与细菌质粒DNA的最佳作用浓度与小檗碱一样,均为6.25×10-5mol.L-1。结论短链烷基的接入有利于小檗碱与质粒DNA的作用强度,烷基修饰并没有改变药物分子与DNA的作用位点数,只是增强了相互之间的作用强度。
Objective To understand the interaction between berberine and DNA,and the pharmacological mechanism of berberine derivatives.Methods The fluorescence spectrum was observed while 8-alkylberberine was acting with plasmid DNA.Results Berberine and its 8-alkyl derivatives all enhanced the fluorescence intensity of plasmid DNA.Compared with berberine,the 8-alkylberberine with shorter alkyl groups 8-ethyl-berberine,8-butyl-berberine,8-hexyl-berberine and 8-octyl-berberine showed strong fluorescence increasing effect;however,8-dodecyl-berberine and 8-cetyl-berberine showed weak effect,and 8-butyl-berberine showed the strongest fluorescence increasing effect among all experiment compounds.All experiment compounds showed the strongest fluorescence increasing effect at 6.25×10-5 mol·L-1.Conclusion Modification with shorter alkyl group benefits the binding effect.Alkyl group only changes the bending strength,but not the number of binding site.between 8-alklberberine and plasmid DNA.
出处
《中南药学》
CAS
2012年第11期806-808,共3页
Central South Pharmacy
基金
湖南省科技厅立项项目(No.2011FJ3038)
关键词
小檗碱
烷基修饰
质粒DNA
荧光分析
berberine
modification with alkyl group
plasmid DNA
fluorescence analysis
