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还原响应荧光探针的研制
引用本文:赵泽恺,王璐,薛敬伟,张灿. 还原响应荧光探针的研制[J]. 中国药科大学学报, 2014, 45(5): 535-539
作者姓名:赵泽恺  王璐  薛敬伟  张灿
作者单位:中国药科大学新药研究中心;中国药科大学新药研究中心;中国药科大学新药研究中心;中国药科大学新药研究中心
基金项目:国家自然科学基金资助项目(No.81273468)
摘    要:基于荧光共振能量转移(FRET)原理和胞质中的还原环境,对载体在细胞胞质中的稳定性进行了表征。首次合成了同时具有FRET效应和还原响应性的新型荧光探针偶联物:3-羧酸-7-羟基-香豆素-硫-硫-异硫氰酸荧光素(CHC-SS-FITC)。以脂质体为模型载体,制备了荷载荧光探针偶联物的脂质体,并评价了探针偶联物的荧光共振能量转移效应和还原响应性。以巨噬细胞为模型细胞,通过激光共聚焦显微技术考察了载药纳米脂质体在巨噬细胞中稳定性。结果表明,本研究设计的新型荧光探针偶联物CHC-SS-FITC,由于同时具备FRET效应的高灵敏度和还原环境触发式响应的强抗干扰能力,克服了传统表征手段的不足,为纳米载体在细胞胞质中的稳定性表征开辟了新的道路。

关 键 词:探针偶联物;荧光共振能量转移;还原响应性;稳定性;细胞质

Development of reduction response probes
ZHAO Zekai,WANG Lu,XUE Jingwei and ZHANG Can. Development of reduction response probes[J]. Journal of China Pharmaceutical University, 2014, 45(5): 535-539
Authors:ZHAO Zekai  WANG Lu  XUE Jingwei  ZHANG Can
Abstract:Based on fluorescence resonance energy transfer(FRET)principle and the reductive environment in the cytoplasm, this study attempted to characterize the stability of the carrier in cells. A new probe conjugation with FRET and reduction responsibility simultaneously, (3-COOH-7-OH-coumarin)-(sulfur-sulfur)-(fluorescein isothiocyanate)(CHC-SS-FITC), was first synthesized. With liposome being used as model carrier, (CHC-SS-FITC)-liposome was prepared and the FRET effect and reduction responsibility of CHC-SS-FITC were assessed. The stability of drug-loading liposome in macrophages was investigated by laser scan confocal microscopy. Results showed that the reduction response FRET probes(CHC-SS-FITC)could be used to characterize the stability of nano-carrier in cytoplasm, due to the high sensitivity and strong counter-interference of the carrier.
Keywords:probe conjugation   fluorescence resonance energy transfer   reduction responsibility   stability   cytoplasm
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