青霉素G酰化酶的近红外荧光探针及其活体成像  

In vivo imaging of penicillin G acylase in mice via a near-infrared fluorescent probe

作　　者：贺新元[1] 张昊琳 李晓花[1] 史文[1] 马会民[1] 

机构地区：[1]中国科学院化学研究所，活体分析化学重点实验室，北京分子科学国家实验室,北京100190

出　　处：《中国科学：化学》2017年第8期994-999,共6页SCIENTIA SINICA Chimica

基　　金：国家自然科学基金(编号:91432101,21621062);国家重大科学研究计划(编号:2015CB932001);北京分子科学国家实验室开放课题资助项目

摘　　要：青霉素G酰化酶(PGA)是一种酰胺键水解酶,是半合成青霉素工业化生产中重要的催化剂.基于PGA能选择性水解苯乙酸衍生物的性质,设计合成了一种以氨基半菁为荧光母体、苯乙酰基为识别单元的新型PGA近红外荧光探针.该探针与PGA反应20 min后,在705 nm处产生明显的荧光发射,荧光强度较探针本身增强了82倍.该荧光响应还呈现出良好的线性范围和很低的检测限.借助多功能活体成像系统,该探针已初步用于小鼠中PGA的活性检测,并在生物样品中PGA的检测方面具有很大的潜力.Penicillin G acylase （PGA） is a hydrolytic enzyme, which is also industrially employed in the preparation of semisynthetic penicillin. Abuse of PGA might occur in milk products to decompose the possible excessive antibiotics.Detection of PGA, including in vivo imaging of PGA, is necessary to understand the potential function of this enzyme in living biosystems; however, a near-infrared（NIR） fluorescent probe for PGA is still lacking. On the basis of amino hemicyanine as well as the ability of PGA to hydrolyze phenylacetamide, in this work we have developed a new selective and sensitive NIR fluorescent probe for such a purpose.Combined with in vivo fluorescence imaging system, the probe has been preliminarily used to image the change of the PGA activity in mice. In addition, the NIR feature of our probe makes it of potential use in studying the function of PGA in vivo.

关 键 词：青霉素G酰化酶 近红外荧光探针 活体成像 氨基半菁 

分 类 号：O657.3[理学—分析化学] Q55[理学—化学]