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A nir fluorescent probe for Vanin-1 and its applications in imaging, kidney injury diagnosis,and the development of inhibitor

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Acta Pharmaceutica Sinica B 2022年第1期12卷 316-325页

作者： Zhenhao Tian Fei Yan Xiangge Tian Lei Feng Jingnan Cui Sa Deng Baojing Zhang Tian Xie Shanshan Huang Xiaochi Ma Dalian Key Laboratory of Metabolic Target Characterization and Traditional Chinese Medicine Intervention The Second Affiliated HospitalCollege of Integrative MedicineCollege of PharmacyDalian Medical UniversityDalian 116044China Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy Xuzhou Medical UniversityXuzhou 221004China School of Life Sciences Northwestern Polytechnical UniversityXi'an 710072China School of Chemistry and Chemical Engineering Henan Normal UniversityXinxiang 453007China State Key Laboratory of Fine Chemicals Dalian University of TechnologyDalian 116024China College of Pharmacy Key Laboratory of Elemene Class Anti-Cancer Chinese MedicinesHangzhou Normal UniversityHangzhou 311121China

Vanin-1 is an amidohydrolase that catalyses the conversion of pantetheine into the aminothiol cysteamine and pantothenic acid(coenzyme A precursor), which plays a vital role in multiple physiological and pathological processes. In this study, an enzyme-activated near-infrared(nir) fluorescent probe(DDAV) has been constructed for sensitively detecting Vanin-1 activity in complicated biosamples on the basis of its catalytic characteristics. DDAV exhibited a high selectivity and sensitivity toward Vanin-1 and was successfully applied to the early diagnosis of kidney injury in cisplatin-induced kidney injury model. In addition, DDAV could serve as a visual tool for in situ imaging endogenous Vanin-1 in vivo. More importantly, Enterococcus faecalis 20247 which possessed high expression of Vanin-1 was screened out from intestinal bacteria using DDAV, provided useful guidance for the rational use of NSAIDs in clinic. Finally, oleuropein as a potent natural inhibitor for Vanin-1 was discovered fromherbal medicines library using a high-throughput screening method using DDAV, which held great promise for clinical therapy of inflammatory bowel disease.

关键词： Vanin-1 nir fluorescent probe Kidney injury diagnosis Fluorescence imaging Oleuropein

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Highly selective nir fluorescent probe for acetylcholinesterase and its application in pesticide residues detection

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Chinese Chemical Letters 2022年第9期33卷 4233-4237页

作者： Shengui He Shufang Zhang Xin Zhao Xinyue Zhu Lisen Chen Jingnan Cui State Key Laboratory of Fine Chemicals Dalian University of Technology Dalian 116024China

A series of near-infrared(nir)fluorescent substrates(NDRO-1∼8)derived from fluorophore NDRH with different volumes of ester bond as the recognition group were designed and synthesized for the detection of acetylcholinesterase(AChE),among which NDRO-1 with the smallest acetate group displayed the highest activity toward AChE.The detection limit of NDRO-1 for sensing AChE was 0.32μg/mL,and K_(m )was 6.40μmol/L,indicating ultra-sensitivity and good affinity of NDRO-1 toward AChE.NDRO-1 was used to detect the inhibitory of four kinds of pesticides including methamidophos,dichlorvos,and the detection limit was lower than 50μg/L,which was further used in pesticide residues detection.

关键词： nir fluorescent probe Acetylcholinesterase Enzyme-activated Pesticide residue detection

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Lighting up plants with near-infrared fluorescence probes

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Science China Chemistry 2024年第3期67卷 774-787页

作者： Yida Pang Mengjiao Lu Hyeonji Rha Wenchao Yang Amit Sharma Yao Sun Jong Seung Kim National Key Laboratory of Green Pesticide Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationCenter for R&D of Fine Chemicals of Guizhou UniversityGuiyang 550025China National Key Laboratory of Green Pesticide College of ChemistryCentral China Normal UniversityWuhan 430079China Department of Chemistry Korea UniversitySeoul 02841Korea CSIR-Central Scientific Instruments Organisation Sector-30CChandigarh160030India TheranoChem Incorporation Seongbuk-guSeoul02856Korea

Fluorescence imaging is a non-invasive and highly sensitive bioimaging technique that has shown remarkable strides in plant science. It enables real-time monitoring and analysis of biological and pathological processes in plants by labeling specific molecular or cellular structures with fluorescent probes. However, tissue scattering and phytochrome interference have been obstacles for conventional fluorescence imaging of plants in the ultraviolet and visible spectrum, resulting in unsatisfactory imaging quality. Fortunately, advances in near-infrared(nir) fluorescence imaging technology(650-900 nm) offer superior spatial-temporal resolution and reduced tissue scattering, which is sure to improve plant imaging quality. In this review, we summarize recent progress in the development of nir fluorescence imaging probes and their applications for in vivo plant imaging and the identification of plant-related biomolecules. We hope this review provides a new perspective for plant science research and highlights nir fluorescence imaging as a powerful tool for analyzing plant physiology, adaptive mechanisms, and coping with environmental stress in the near future.

关键词： nir fluorescent probe plant imaging biologic application

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High-throughput fluorescent screening of thioredoxin reductase inhibitors to inhibit Mycobacterium tuberculosis

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Chinese Chemical Letters 2024年第3期35卷 358-362页

作者： Fei Yan Xin Zhao Ruibo Li Xiuyan Han Qiulong Yan Lei Feng Xiulan Xin Jingnan Cui Xiaochi Ma Second Affiliated Hospital Dalian Medical UniversityDalian 116044China State Key Laboratory of Fine Chemicals Dalian University of TechnologyDalian 116024China Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy Xuzhou Medical UniversityXuzhou 221004China School of Chemistry and Chemical Engineering Henan Normal UniversityXinxiang 453007China College of Bioengineering Beijing PolytechnicBeijing 100029China

Tuberculosis(TB)is a chronic infectious disease,which is caused by the pathogen Mycobacterium tuberculosis(Mtb)and reemerged as a global health risk with a significant proportion of multi-drug resistant and extensively drug resistant TB cases.It is very urgent to find some novel high-confidence drug targets in Mtb for discovering the effective anti-TB agents.Thioredoxin reductase(TrxR)has been identified to be a highly viable target for anti-TB drugs for its important role in protecting the pathogen from thiol-specific oxidizing stress,regulating intracellular dithiol/disulfide homeostasis and DNA replication and repair.In the present work,a near-infrared(nir)fluorescent probe DDAT was developed for the detection of TrxR activity and used to high-throughput screen the TrxR inhibitors from natural products.Two screened TrxR inhibitors from Sappan Lignum and microbial metabolites that were further used to inhibit Mycobacterium tuberculosis.All the results indicate that DDAT is a practical fluorescent molecular tool for the discovery of potential anti-TB drugs.

关键词： Thioredoxin reductase nir fluorescent probe Fluorescence imaging High-throughput screening inhibitors Inhibit Mycobacterium tuberculosis

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Hypoxia-activatable nano-prodrug for fluorescently tracking drug release in mice

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Science China Chemistry 2021年第3期64卷 499-508页

作者： Haidong Li Qichao Yao Zhongji Pu Jeewon Chung Haoying Ge Chao Shi Ning Xu Feng Xu Wen Sun Jianjun Du Jiangli Fan Jingyun Wang Juyoung Yoon Xiaojun Peng State Key Laboratory of Fine Chemicals Dalian University of TechnologyDalian 116024China Department of Chemistry and Nanoscience Ewha Womans UniversitySeoul 03760Korea Ningbo Institute of Dalian University of Technology Ningbo 315016China School of Bioengineering Dalian University of TechnologyDalian 116024China

Chemotherapy is one of the commonly used methods to treat various types of cancers in clinic by virtue of its high efficiency and universality. However, strong side effects and low concentration of conventional drugs at the tumor site have always been important factors that plague the chemotherapy effects of patients, further precluding their practical applications. Thereof, to solve the above dilemma, by integration of anticancer drug(nitrogen mustard, NM) into an nir fluorophore(a dicyanoisophorone derivative), an intelligent prodrug nir-NM was developed via molecular engineering strategy. Prodrug nir-NM stimulated in hypoxia condition exhibits significantly higher toxicity to cancer cells than normal cells, essentially reducing the collateral damage to healthy cells and tissues of nitrogen mustard. More importantly, the nanoparticle prodrug FA-lip@nir-NM showed the advantages of the high accumulation of drug at tumor site and long-circulation capacity in vivo, which endowed it the ability to track the release of the active chemotherapeutic drug and further treat solid tumors.

关键词： nir fluorescent probe activatable hypoxia prodrug imaging

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A highly selective colorimetric and ratiometric fluorescent probe for cysteine with enhanced near-infrared fluorescence and its application in living cells

A highly selective colorimetric and ratiometric fluorescent ...

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第十届全国化学生物学学术会议

作者： Shumin Feng Yang Fang Weiyong Feng Qingfeng Xia Guoqiang Feng Key Laboratory of Pesticide and Chemical Biology of Ministry of Education College of ChemistryCentral China Normal University

A new ratiometric near-infrared（nir） fluorescent probe with significant nir fluorescent turn-on changes was reported for rapid, colorimetric and ratiometric fluorescent detection of cysteine（Cys）. This probe is able to detect Cys in aqueous solution under mild conditions, showing high selectivity and sensitivity for Cys over various analytes including the similar structured homocysteine（Hcy） and glutathione（GSH）. The detection limit of this probe for Cys was found to be as low as 0.2 μM, which is far below the normal content of Cys（30-200 μM） in cells. Bioimaging experiments showed that this probe can be applied to image intracellular Cys in living cells with low cytotoxicity, indicating this probe holds great potential for biological applications.

关键词： cysteine colorimetric nir fluorescent probe ratiometric bioimaging

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