具有聚集诱导发光特性的天然药源荧光探针黄连素的诊疗作用  

Theragnostic effect of berberine-a natural herb resourced fluorescent probe with aggregation-induced emission property

作　　者：苏会芳 孙新志[1] 寇红伟[1] 尚国伟[1] 陈松峰 尚春风 燕淼恒 赵楠 李龙域 刘宏建[1] Su Huifang;Sun Xinzhi;Kou Hongwei;Shang Guowei;Chen Songfeng;Shang Chunfeng;Yan Miaoheng;Zhao Nan;Li Longyu;Liu Hongjian(Department of Orthopedics,the First Affiliated Hospital of Zhengzhou University,Zhengzhou 450052,China)

机构地区：[1]郑州大学第一附属医院骨科,450052

出　　处：《中华实验外科杂志》2021年第5期897-900,共4页Chinese Journal of Experimental Surgery

基　　金：国家自然科学基金(81902356、81972523、82072581);河南省省部共建项目(SB201901029、SB201901017);河南省医学科技攻关计划联合共建基金(2018020025)。

摘　　要：目的探讨黄连素(BBR)的聚集诱导发光(AIE)性质,细胞器靶向性及双光子成像效果,以及光动力治疗效果。方法采用HeLa细胞作为模型细胞,探讨其生物相容性,以商业线粒体染料为比较对象,探讨其亚细胞水平的靶向区域和靶向能力,并将斑马鱼作为模式动物,探讨BBR对其组织渗透性和双光子成像性能,最终应用白光光源辐照,探讨其对肿瘤细胞的潜在的光动力治疗效果。结果BBR具有良好的生物相容性,其对线粒体的靶向性能与商用线粒体染料具有94%的共染率,且其对斑马鱼胚胎具有良好的渗透性能,在840 nm的双光子激发下能够良好的激发其进行整体斑马鱼的成像;采用低能量白光辐照下,其光动力治疗杀伤效果显示,在较低的浓度下,肿瘤细胞可被大比例杀伤(杀伤率>90%)。结论BBR具有良好的聚集诱导发光性能,可以在聚集状态下发光更加明亮,且其是一种良好的线粒体染料,其具有良好的双光子吸收、发射性能和光动力治疗效果。Objective To investigate the Aggregation-Induced Emission(AIE)property,cell organelle targeting and two-photon imaging abilities of berberine(BBR)and its potential application in photodynamic therapy.Methods HeLa cell line was used as a cell model,and the biocompatibility of BBR was studied.MitoTracker™Red FM,which is targeting mitochondria,was as a comparison probe,then we investigated its subcellular level targeting region and targeting ability.Zebrafish was used as a model animal,we tested the tissue permeability and two-photon imaging performance of BBR,finally its potential application of photodynamic therapy under white light irradiation was explored.Results BBR has good biocompatibility.The targeting property(colocalization coefficient rate)of BBR to MitoTracker™Red FM is 94%,and it owned good penetration property in whole zebrafish embryo,in which BBR in the tissue could be stimulated by 840 nm two-photon excitation to perform whole good zebrafish imaging.While under low energy white light irradiation,the photodynamic therapy effect of BBR showed that the HeLa tumor cells could be killed by a large proportion(killing rate>90%)at a low concentration.Conclusion BBR owns good AIE property,which endowed it the potential of emitting much brighter in the aggregation state,and it can be used as a good mitochondrial probe with good two-photon absorption and emission properties,and an efficient sensitizer in photodynamic therapy effect as well.

关 键 词：光动力治疗 黄连素 线粒体 双光子成像 

分 类 号：R285[医药卫生—中药学]