三颗针抗菌活性成分研究  

Analysis of Antimicrobial Activity Constituents of “San Ke Zhen”

作　　者：徐婵[1] 吴潇潇[1] 万定荣[1] 王强[2] 吕静南 黄密[1] 杨新洲[1,3] 

机构地区：[1]中南民族大学药学院,武汉430074 [2]武汉科技大学医学院,武汉430081 [3]中国科学院上海药物研究所新药研究国家重点实验室,上海201201

出　　处：《华中科技大学学报（医学版）》2015年第5期556-562,共7页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

基　　金：新药研究国家重点实验室开放基金(No.SIMM1403KF-07);国家科技支撑计划项目(No.2012BAI27B06);中南民族大学"十二五"民族药学国家级实验教学示范中心资助;湖北省教育厅重点项目(No.D20131103)

摘　　要：目的系统地研究三颗针的抗菌活性成分,并比较不同来源三颗针提取物的高效液相色谱分析的稳定性和重现性。方法运用制备高效液相色谱法结合凝胶过滤和重结晶法分离纯化化学成分,利用现代波谱技术鉴定所分离化合物的结构,采用HPLC-PDA法分析不同来源的8个三棵针样品甲醇提取物,采用肉汤稀释法测试上述8个甲醇提取物和单体生物碱成分的抗菌活性。结果从湖北小檗甲醇提取物中分离得到7个单体化合物,鉴定为异紫堇定碱（1）、小檗胺（2）、药根碱（3）、巴马汀（4）、小檗碱（5）、4-羟基苯甲酸（6）、β-谷甾醇（7）,化合物1~7为首次从该植物中分得。8个甲醇提取物与化合物2~5对革兰阳性菌金黄色葡萄球菌及表皮葡萄球菌显抗菌活性,MIC值范围为12.5~50.0μg/mL。结论三颗针中所含的异喹啉生物碱显示出良好的抗菌活性,不同来源的三颗针甲醇提取物高效液相色谱分析具有良好的稳定性和重现性,这些研究为三颗针进一步的开发奠定了基础。Objective To systematically investigate the antimicrobial activity constituents of Chinese medicine＂San Ke Zhen＂and compare the stability and reproducibility of HPLC-PDA analysis of methanolic extracts of＂San Ke Zhen＂of different origins.Methods The isolation and purification of chemical constituents were performed with preparative HPLC,Sephadex LH-20 gel column chromatography and recrystallization.Structures of isolated pure compounds were identified by modern spectrum analysis.The HPLC-PDA method was performed to analyze eight methanolic extracts from different regions.Antimicrobial activities of the eight methanolic extracts and the monomeric alkaloids were evaluated by using the broth dilution method.Results Seven monomeric compounds were obtained from methanolic extracts,and after identification,they were found to be（1）isocorydine,（2）berbamine,（3）jatrorrhizine,（4）palmatine,（5）berberine,（6）4-hydroxybenzoic acid and（7）β-sitosterol.Compounds 1-7were firstly isolated from this plant.The in vitro results showed that all eight methanolic extracts and compounds 2-5displayed antimicrobial activities against staphylococcus aureus and staphylococcus epidermidis,with MIC values ranging from 12.5to 50.0μg/mL.Conclusion Isoquinoline alkaloids isolated from＂San Ke Zhen＂exhibit good antimicrobial activities.HPLC-PDA analysis of methanolic extracts of different origins is of good stability and reproducibility,which lays a foundation for further studies on＂San Ke Zhen＂.

关 键 词：三颗针 湖北小檗 抗微生物活性 生物碱 制备型高效液相 

分 类 号：R284.1[医药卫生—中药学] R284.2[医药卫生—中医学]