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Near-Infrared AIE-Active Probe Enable in Situ and Long-Term Tracking of Endogenous β-Galactosidase Activity

机译:近红外AIE活性探针可对内源性β-半乳糖苷酶活性进行原位和长期跟踪

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High-fidelity tracking specific enzyme activities is critical for the early diagnosis of diseases such as cancers. However, most of available fluorescent probes are difficult to obtain in situ information because of tending to facilely diffusion or inevitably suffering from the aggregation-caused quenching (ACQ) effect. In this work, we developed an elaborated near-infrared (NIR) aggregation-induced emission (AIE)-active fluorescent probe, which is composed of a hydrophobic 2-(2-hydroxyphenyl) benzothiazole (HBT) moiety for extending into NIR wavelength, and a hydrophilic β-galactosidase (β-gal) triggered unit for improving miscibility and guaranteeing its non-emissive in aqueous media. This probe is virtually activated by β-gal, and then specific enzymatic turnover would liberate hydrophobic AIE luminogen (AIEgen) QM-HBT-OH. Simultaneously, brightness NIR fluorescent nanoaggregates are in situ generated as a result of AIE-active process, making on-site the detection of endogenous β-gal activity in living cells. By virtue of NIR AIE-active performance of enzyme-catalyzed nanoaggregates, QM-HBT-βgal is capable of affording a localizable fluorescence signal and long-term tracking of endogenous β-gal activity. All results demonstrate that the probe QM-HBT-βgal is a powerful molecular tool to better understand the biological roles of β-gal activity, attaining high-fidelity information in preclinical applications.
机译:高保真跟踪特定酶的活性对于诸如癌症等疾病的早期诊断至关重要。然而,由于趋于容易扩散或不可避免地遭受聚集引起的猝灭(ACQ)效应,大多数可用的荧光探针难以原位获得信息。在这项工作中,我们开发了一种精细的近红外(NIR)聚集诱导发射(AIE)活性荧光探针,该探针由疏水的2-(2-羟苯基)苯并噻唑(HBT)部分组成,可扩展到NIR波长,亲水性β-半乳糖苷酶(β-gal)触发单元,可改善混溶性并确保其在水性介质中不散发。该探针实际上被β-gal激活,然后特定的酶转化将释放疏水性AIE发光剂(AIEgen)QM-HBT-OH。同时,由于AIE活性过程的结果,原位生成了亮度NIR荧光纳米聚集体,可现场检测活细胞中的内源性β-gal活性。凭借酶催化的纳米聚集体的NIR AIE活性,QM-HBT-βgal能够提供可定位的荧光信号并长期跟踪内源性β-gal活性。所有结果表明,探针QM-HBT-βgal是一种强大的分子工具,可以更好地了解β-gal活性的生物学作用,从而在临床前应用中获得高保真信息。

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