Dataset Information

Near-Infrared Aggregation-Induced Emission-Active Probe Enables in situ and Long-Term Tracking of Endogenous ?-Galactosidase Activity.

ABSTRACT: High-fidelity tracking of specific enzyme activities is critical for the early diagnosis of diseases such as cancers. However, most of the available fluorescent probes are difficult to obtain in situ information because of tending to facile diffusion or inevitably suffering from 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 the NIR wavelength, and a hydrophilic ?-galactosidase (?-gal) triggered unit for improving miscibility and guaranteeing its non-emission in aqueous media. This probe is virtually activated by ?-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 the AIE-active process, making on-site the detection of endogenous ?-gal activity in living cells. By virtue of the NIR AIE-active performance of enzyme-catalyzed nanoaggregates, QM-HBT-?gal is capable of affording a localizable fluorescence signal and long-term tracking of endogenous ?-gal activity. All results demonstrate that the probe QM-HBT-?gal has potential to be a powerful molecular tool to evaluate the biological activity of ?-gal, attaining high-fidelity information in preclinical applications.

SUBMITTER: Fu W

PROVIDER: S-EPMC6527754 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Publications

Near-Infrared Aggregation-Induced Emission-Active Probe Enables <i>in situ</i> and Long-Term Tracking of Endogenous β-Galactosidase Activity.

Fu Wei W Yan Chenxu C Zhang Yutao Y Ma Yiyu Y Guo Zhiqian Z Zhu Wei-Hong WH

Frontiers in chemistry 20190514

High-fidelity tracking of specific enzyme activities is critical for the early diagnosis of diseases such as cancers. However, most of the available fluorescent probes are difficult to obtain <i>in situ</i> information because of tending to facile diffusion or inevitably suffering from 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-hydroxyp ...[more]

PMID: 31139612

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Project description:Photodynamic therapy (PDT) has been widely applied in the clinic for the treatment of various types of cancer due to its precise controllability, minimally invasive approach and high spatiotemporal accuracy as compared with conventional chemotherapy. However, the porphyrin-based photosensitizers (PSs) used in clinics generally suffer from aggregation-caused reductions in the generation of reactive oxygen species (ROS) and limited tissue penetration because of visible light activation, which greatly hampers their applications for the treatment of deep-seated tumors. Methods: We present a facile strategy for constructing a NIR-regulated cancer theranostic nanoplatform by encapsulating upconversion nanoparticles (UCNPs) and a luminogen (2-(2,6-bis((E)-4-(phenyl(40-(1,2,2-triphenylvinyl)-[1,10-biphenyl]-4-yl)amino)styryl)-4H-pyran-4-ylidene)malononitrile, TTD) with aggregation-induced emission (AIEgen) characteristics using an amphiphilic polymer, and further conjugating cyclic arginine-glycine-aspartic acid (cRGD) peptide to yield UCNP@TTD-cRGD NPs. We then evaluated the bioimaging and anti-tumor capability of the UCNP@TTD-cRGD NPs under NIR light illumination in an in vitro three-dimensional (3D) cancer spheroid and in a murine tumor model, respectively. Results: With a close match between the UCNP emission and absorption of the AIEgen, the synthesized NPs could efficiently generate ROS, even under excitation through thick tissues. The NIR-regulated UCNP@TTD-cRGD NPs that were developed could selectively light up the targeted cancer cells and significantly inhibit tumor growth during the NIR-regulated PDT treatment as compared with the cells under white light excitation. Conclusion: In summary, the synthesized UCNP@TTD-cRGD NPs showed great potential in NIR light-regulated photodynamic therapy of deep-seated tumors. Our study will inspire further exploration of novel theranostic nanoplatforms that combine UCNPs and various AIEgen PSs for the advancement of deep-seated tumor treatments with potential clinical translations.

Dataset Information

Near-Infrared Aggregation-Induced Emission-Active Probe Enables in situ and Long-Term Tracking of Endogenous ?-Galactosidase Activity.

Publications

Near-Infrared Aggregation-Induced Emission-Active Probe Enables <i>in situ</i> and Long-Term Tracking of Endogenous β-Galactosidase Activity.

Similar Datasets

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