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ANALYTICAL CHEMISTRY · 2014 · IF 5.825

Discovery of Bioluminogenic Probes for Aminopeptidase N Imaging

Jing Li,Laizhong Chen,Wenxiao Wu,Wei Zhang,Zhao Ma,Yanna Cheng,Lupei Du,Minyong Li

To find an approach that can image the hydrolysis activity of aminopeptidase N (APN) both in vitro and in vivo, three bioluminescent probes have been well designed and synthesized herein. All of them can be recognized and hydrolyzed by APN to produce bioluminescence emission in the presence of firefly luciferase. To the best of our knowledge, they are the first bioluminescent probes for imaging APN in deep tissues and living animals.

CAS / MDL: 9001-05-2 56-65-5

研究领域: 生物化学 · 分子影像学 · 医学

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DYES AND PIGMENTS · 2025 · IF 4.2

Enzyme-activatable hemicyanine-based probe for spatiotemporal detection of aminopeptidase N in colitis

Xin-Ke Shao,Lu Fan,Jie-Li Zhou,Kai Wang

The development of novel molecular probes for real-time monitoring of aminopeptidase N (APN) activity is crucial for understanding inflammatory bowel disease (IBD) progression. Here, we present a new probe, HDAPN, a near-infrared (NIR) activatable fluorescent probe based on a hemicyanine scaffold, designed for selective APN detection. Structural characterization confirmed the molecular integrity of the probe, while spectroscopic studies demonstrated its exceptional photostability and response. HDAPN exhibits a remarkable "turn-on" response (720 nm emission) upon APN-mediated cleavage, with outstanding sensitivity (LOD = 0.82 ng/mL) and linearity under physiological conditions. The probe showed minimal cross-reactivity with interferents (e.g., ROS, metal ions, and other enzymes) and successfully detected LPS-induced APN upregulation in RAW264.7 macrophages. In DSS-induced colitis models, HDAPN enabled non-invasive visualization of APN activity, with fluorescence intensity correlating with disease severity (2-fold increase in severe colitis). Comprehensive toxicity evaluations confirmed its biosafety in vitro and in vivo . These findings highlight the potential of HDAPN as a robust tool for studying APN-associated pathophysiology and therapeutic development.

研究领域: 生物化学 · 分子成像 · 炎症性肠病 · 荧光探针 · 酶学 · 生物医学光学

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Discovery of Bioluminogenic Probes for Aminopeptidase N Imaging

Enzyme-activatable hemicyanine-based probe for spatiotemporal detection of aminopeptidase N in colitis