五叶山小桔中光活化DNA结合性和抗微生物活性的生物碱研究(英文)  

Photo-activated DNA binding and antimicrobial activities of alkaloids from Glycosmis pentaphylla

作　　者：陈玉[1] 杨博[2] 徐婧[2] 郑桐[2] 范华[2] 杨光忠[2] 

机构地区：[1]中南民族大学化学与材料科学学院,湖北武汉430074 [2]中南民族大学药学院,湖北武汉430074

出　　处：《药学学报》2012年第12期1646-1652,共7页Acta Pharmaceutica Sinica

基　　金：supported by the Special Fund for Basic Scientific Research of Central Colleges,South-Central University for Nationalities(ZZY10003)

摘　　要：为了寻找天然来源的光敏剂,通过色谱技术,从五叶山小桔中分离出4个生物碱,它们的结构通过波谱数据分别鉴定为glycoborinine(1)、glybomine B(2)、carbalexin A(3)和N-p-coumaroyltyramine(4)。通过薄层色谱自显影技术,评价了4个生物碱对金葡菌和枯草芽孢杆菌的光活化抗微生物的活性,化合物1和4显示出一定的活性。以质粒pET-28为模板,通过PCR反应获得1.8 kb的DNA片段,通过凝胶电泳的方法,研究了4个生物碱类化合物与DNA的结合性,研究表明,化合物1经UVA照射处理能够插入到含有5'-TpA和5'-ApT的DNA序列中,从而对Nde Ⅰ、Nco Ⅰ、Xba Ⅰ和Bcl Ⅰ四种酶对其识别位点的切割显示出一定的抑制活性,与8-甲氧基补骨脂素显示出同样的抑制模式。然而,其他3个化合物对任何限制性内切酶都没有表现出抑制活性。In our screening for photosensitizers from natural resources, four alkaloids were isolated from Glycosmis pentaphylla by various chromatography techniques. Their structures were identified as glycoborinine （1）, glybomine B （2）, carbalexin A （3） and N-p-coumaroyltyramine （4） by spectral analysis. Their photo- activated antimicrobial activities were evaluated by thin-layer chromatography （TLC） agar overlay assay against Staphylococcus aureus and Bacillus subtilis. It was found that compounds 1 and 4 showed photo-activated antimicrobial activities. Meantime, photo-activated DNA binding activities of these compounds were also assessed by using a specially prepared 1.8 kb DNA fragment and restriction enzymes. Under UVA irradiation, compound 1 showed moderate inhibition on Nde I, Xba I, Nco I and Bcl I which have either 5＇-TpA or 5＇-APT and trace or no inhibition on other restriction enzymes. It showed a similar inhibition pattern with the reference 8-methoxypsoralen. However, compounds 2-4 showed no inhibition against any of the restriction enzymes.

关 键 词：五叶山小桔 光敏剂 光活化DNA结合性 

分 类 号：R284[医药卫生—中药学]