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设计并合成一种偶氮还原酶响应性黄酮醇-吲哚美辛杂合体，用于结肠炎的诊断和治疗。

Design and Synthesis of an Azo Reductase Responsive Flavonol-Indomethacin Hybrid Used for the Diagnosis and Treatment of Colitis.

机构信息

School of Pharmacy, Jiangsu Vocational College of Medicine, Yancheng 224005, China.

School of Pharmacy, Nantong University, Nantong 226019, China.

出版信息

Molecules. 2024 Sep 6;29(17):4244. doi: 10.3390/molecules29174244.

DOI:10.3390/molecules29174244
PMID:39275092
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11397019/
Abstract

Human intestinal bacteria are the primary producers of azo reductase, and the content of azo reductase is closely associated with various intestinal diseases, including ulcerative colitis (UC). The rapid detection of changes in azo reductase levels is crucial for diagnosing and promptly intervening in UC. In this study, a therapeutic agent, , specifically targeting UC, was designed and synthesized. This agent was developed by linking the anti-inflammatory drug indomethacin to flavonols with antioxidant activity via an azo bond (off-on). Breakage of the azo bond breaks results in the release of both fluorophores and drugs, achieving targeted tracing and integrated treatment effects. In vivo and in vitro fluorescence imaging experiments were used to demonstrate the potential of in the diagnosis of UC, together with synergistic therapeutic effects through the release of both fluorophores and anti-inflammatory agents. Therefore, this diagnostic agent shows promise as a potential tool for diagnosing and treating UC.

摘要

人类肠道细菌是偶氮还原酶的主要产生者，偶氮还原酶的含量与各种肠道疾病密切相关，包括溃疡性结肠炎（UC）。快速检测偶氮还原酶水平的变化对于 UC 的诊断和及时干预至关重要。在本研究中，设计并合成了一种针对 UC 的治疗剂 。该试剂通过偶氮键（开-关）将具有抗炎作用的吲哚美辛与具有抗氧化活性的类黄酮连接起来。偶氮键的断裂导致荧光团和药物的释放，实现了靶向追踪和综合治疗效果。体内和体外荧光成像实验证明了 在 UC 诊断中的应用潜力，以及通过释放荧光团和抗炎剂的协同治疗效果。因此，这种诊断试剂有望成为诊断和治疗 UC 的一种潜在工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/18ab0f7372b7/molecules-29-04244-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/2ddf8d6d6625/molecules-29-04244-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/2083fc8988c5/molecules-29-04244-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/0aa4d5a62d87/molecules-29-04244-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/18aa1ff14503/molecules-29-04244-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/27790caf66c6/molecules-29-04244-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/cc4ff8c2911f/molecules-29-04244-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/e79c8ad975d0/molecules-29-04244-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/493c0ab63444/molecules-29-04244-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/f7ee5b1fa80c/molecules-29-04244-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/18ab0f7372b7/molecules-29-04244-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/2ddf8d6d6625/molecules-29-04244-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/2083fc8988c5/molecules-29-04244-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/0aa4d5a62d87/molecules-29-04244-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/18aa1ff14503/molecules-29-04244-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/27790caf66c6/molecules-29-04244-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/cc4ff8c2911f/molecules-29-04244-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/e79c8ad975d0/molecules-29-04244-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/493c0ab63444/molecules-29-04244-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/f7ee5b1fa80c/molecules-29-04244-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c419/11397019/18ab0f7372b7/molecules-29-04244-g008.jpg

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