摘要
为了建立一种荧光衍生试剂丹磺酰氯DNS-Cl对含氮药物进行荧光标记与分析的方法,进行了DNS-Cl对一系列含氮物质的荧光衍生反应。通过紫外、荧光等光学检测手段分析荧光标记产物的光学性质,以间隔取样监测标记产物荧光强度随时间的稳定性,进行体外活细胞环境的细胞毒性评价与细胞荧光成像标记,评价荧光衍生产物在活细胞环境的适用性。结果显示,DNS-Cl与含氮药物或化合物的衍生反应条件温和、标记迅速、适用性广,且表现出荧光标记的稳定性及低毒性。DNS-Cl不仅可以实现药物分子半衰期内或代谢期内的荧光稳定标记,而且可以实现细胞水平、分子水平的药物作用代谢示踪等,荧光标记产物在体外活细胞环境中安全有效,反应检测直观可视。
In order to establish a fluorescent labeling and analytical method of nitrogen-containing drugs by fluorescent reagent DNS-Cl,the DNS-Cl fluorescent derivative reactions with a series of nitrogen-containing compounds were carried out.The optical properties of fluorescent labeled products were analyzed by UV-Vis and FS,fluorescent stability-time curve was realized by interval sampling,cytotoxicity and fluorescence imaging were evaluated by in vitro experiment ofliving cells,giving an evaluation on further application of fluorescent derivative in living cell environment.The results indicated that DNS-Cl derivative reaction with nitrogen-containing drugs or compounds was mild,rapid and applicable,demonstrating fluorescence stability and low toxicity.In the half-life or metabolic periods of drugs,as a safe labeling and visible detection methodin living cells,it can not only be realized to label the drug molecules,but also trace drug action and metabolism at the cellular and molecular level.
作者
成昭
周磊
苗延青
梁飞
CHENG Zhao;ZHOU Lei;MIAO Yanqing;LIANG Fei(School of Pharmaceutical Sciences/Institute of Medicine,Xi′an Medical University,Xi′an 710021,China)
出处
《西北大学学报(自然科学版)》
CAS
CSCD
北大核心
2018年第5期686-692,共7页
Journal of Northwest University(Natural Science Edition)
基金
陕西省科技厅社会发展科技攻关基金资助项目(2017SF-174)
陕西省教育厅自然科学基金资助项目(17JK0664)
西安医学院科研基金资助项目(2015DOC16
2017GJFY04)
西安医学院大学生创新创业训练计划基金资助项目(2017DC-71)
关键词
荧光衍生
光稳定性
细胞毒性:丹磺酰氯
含氮药物
fluorescence derivatization
photostability
cytotoxicity
sulfonyl chloride
nitrogen-containing drugs