A New Fluorometric Turn-on Assay for Carboxylesterase and Inhibitor Screening Based on Aggregation Induced Emission Behavior of Tetraphenylethylene Molecules
文献类型：期刊论文
| 作者 | Yang Yang1,2; Huang Yanyan1,2; Zhang Guanxin1; Zhao Rui1,2; Zhang Deqing1,2 |
| 刊名 | ACTA CHIMICA SINICA
 |
| 出版日期 | 2016-11-15 |
| 卷号 | 74期号:11页码:871-876 |
| 关键词 | Aggregation Induced Emission Tetraphenylethylene Fluorescence Sensor Carboxylesterase |
| 英文摘要 | It is known that carboxylesterase (CaE) are a group of isoenzymes commonly distributed in mammalian organs, and they can catalyze the hydrolysis of carboxyl ester. As a result, they play an important role in detoxification of narcotics or chemical toxin clearance. Moreover, they serve as important drug candidates for protein-based therapeutics or drug targets for chemotherapeutic prodrug activation. It is reported recently that human plasma carboxylesterase can be a novel biomarker candidate for hepatocellular carcinoma. Therefore, establishing a reliable fluorescent system for detecting carboxylesterase is of great importance in terms of biochemical studies as well as clinical applications. Herein, we report a new fluorometric turn-on assay for carboxylesterase activity and inhibitor screening with compound 1 by utilizing the aggregation-induced emission (AIE) feature of tetraphenylethylene (TPE) molecules. The sensing mechanism is illustrated in Figure 1 and explains as follows: (i) the pyridinium moiety may render compound 1 water-soluble. As a result it is anticipated that compound 1 is weakly emissive in aqueous solutions according to previous studies; (ii) the incubation of carboxylesterase with compound 1 can result in cleaving the carboxylic ester bond, followed by hydrolysis and 1,6-elimination of p-quinonemethide to yield the p-pyridine substituted TPE (TPE-Py). TPE-Py is not soluble in aqueous solutions, thus aggregation will occur and turn on the fluorescence of TPE moiety based on the ATE feature of TPE compounds. In this way, compound 1 can be employed for the fluorescence turn-on assay for carboxylesterase activity. The results reveal that the buffer solution of compound 1 emitted very weakly. However, the green fluorescence emission was switched on after addition of carboxylesterase. Carboxylesterase at concentrations as low as 5.67 X 10(-5) U/mL can be assayed with compound 1. Further results clearly indicate that compound 1 can be utilized not only for carboxylesterase activity assay but also for the corresponding inhibitor screening. More importantly, this probe can be applied for detection of carboxylesterases in living cells. |
| 语种 | 英语 |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/38042]  |
| 专题 | 化学研究所_有机固体实验室 |
| 作者单位 | 1.Chinese Acad Sci, Inst Chem, CAS Key Labs Organ Solids & Analyt Chem Living Bi, Beijing 100190, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang Yang,Huang Yanyan,Zhang Guanxin,et al. A New Fluorometric Turn-on Assay for Carboxylesterase and Inhibitor Screening Based on Aggregation Induced Emission Behavior of Tetraphenylethylene Molecules[J]. ACTA CHIMICA SINICA,2016,74(11):871-876. |
| APA | Yang Yang,Huang Yanyan,Zhang Guanxin,Zhao Rui,&Zhang Deqing.(2016).A New Fluorometric Turn-on Assay for Carboxylesterase and Inhibitor Screening Based on Aggregation Induced Emission Behavior of Tetraphenylethylene Molecules.ACTA CHIMICA SINICA,74(11),871-876. |
| MLA | Yang Yang,et al."A New Fluorometric Turn-on Assay for Carboxylesterase and Inhibitor Screening Based on Aggregation Induced Emission Behavior of Tetraphenylethylene Molecules".ACTA CHIMICA SINICA 74.11(2016):871-876. |
入库方式： OAI收割
来源：化学研究所
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