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Julolidinyl aza-BODIPYs as NIR-Ⅱ fluorophores for the bioimaging of nanocarriers

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Acta Pharmaceutica Sinica B 2024年第7期14卷 3155-3168页

作者： Chang Liu Yifan Cai Zichen Zhang Yi Lu Quangang Zhu Haisheng He Zhongjian Chen Weili Zhao Wei Wu Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China department of MediChinal chemistry School of PharmacyFudan UniversityShanghai 201203China

The aggregation-caused quenching(ACQ)rationale has been employed to improve the fluorescence imaging accuracy of nanocarriers by precluding free probe-derived ***,its usefulness is undermined by limited penetration and low spatiotemporal resolution of NIR-Ⅰ(700-900 nm)bioimaging owing to absorption and diffraction by biological tissues and tissue-derived *** study aimed to develop ACQ-based NIR-Ⅱ(1000-1700 nm)probes to further improve the imaging resolution and *** strategy employed is to install highly planar and electron-rich julolidine into the 3,5-position of aza-BODIPY based on the larger substituent *** newly developed probes displayed remarkable photophysical properties,with intense absorption centered at approximately 850 nm and bright emission in the 950-1300 nm *** with the NIR-Ⅰ counterpart P2,the NIR-Ⅱ probes demonstrated superior water sensitivity and quenching ***1 and ACQ6 exhibited more promising ACQ effects with absolute fluorescence quenching at water fractions above 40% and higher quenching stability with less than 2.0% fluorescence reillumination in plasma after 24 h of *** calculations verified that molecular planarity is more important than hydrophobicity for ACQ ***,in vivo and ex vivo reillumination studies revealed less than 2.5% signal interference from prequenched ACQ1,in contrast to 15% for P2.

关键词： 3,5-Julolidinyl Aza-BODIPY Nanocarriers Near-infraredⅡ Fluorescence imaging Aggregation-caused quenching Polymeric micelles Polymeric nanoparticles

Spin chiral anisotropy of diamagnetic chiral mesostructured In_(2)O_(3) films

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维普期刊数据库

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Nano Research 2024年第8期17卷 7756-7761页

作者： Ting Ji Quanzheng Deng Hao Chen Lu Han Zhibei Qu Shunai Che Yingying Duan Frontiers Science Center for Transformative Molecules State Key Laboratory of Metal Matrix CompositesShanghai Key Laboratory for Molecular Engineering of Chiral DrugsSchool of Chemistry and Chemical EngineeringShanghai Jiao Tong UniversityShanghai 200240China school of Chemical Science and Engineering Tongji UniversityShanghai 200092China department of medicinal chemistry School of PharmacyFudan UniversityShanghai 201203China

Spin chiral anisotropy(SChA)refers to the occurrence of different spin polarization in antipodal chiral ***,we report the SChA in diamagnetic chiral mesostructured In2O3 films(CMIFs)with manifestation of chirality-dependent magnetic circular dichroism(MCD)*** were grown on fluorine-doped tin dioxide conductive glass(FTO)substrates,which were synthesized via a hydrothermal route,with malic acid used as the symmetry-breaking *** levels of chirality have been identified in CMIFs:primary nanoflakes with atomically twisted crystal lattices and secondary helical stacking of the *** exhibit chirality-dependent asymmetric MCD signals due to the different interactions of chirality-induced effective magnetic field and external magnetic field,which distinguish from the commonly observed external magnetic fielddependent symmetric MCD *** findings provide insights into spin manipulation of spin-paired diamagnets.

关键词： chiral inorganics mesostructure diamagnet spin chiral anisotropy(SChA) magnetic circular dichroism(MCD)

1,6-Conjugate addition of para-quinone methides using gem-diborylcarbanions: Practical access to gem-diborylalkanes bearing vicinal tertiary/quaternary stereocenters

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Green Synthesis and Catalysis 2024年第1期5卷 68-72页

作者： Pu-Zhang Zi Xing-Bang Liu Quan-Hong Zhao Min He Yuan Huang department of medicinal chemistry School of PharmacyXi'an Jiaotong UniversityXi'an710061China

A novel,efficient and pragmatic method to prepare gem-diboron products with vicinal tertiary/quaternary stereocenters using LiTMP-mediated 1,6-conjugate addition of gem-diborylalkanes to para-quinone methides was described for the first *** results showed that various gem-diboron products with vicinal tertiary and quaternary stereocenters could be formed within 15 min at ambient *** simple protocol has also been applied for the efficient synthesis of the analogue of Bedaquiline.

关键词： gem-Diborylalkanes Quaternary stereocenter Conjugate addition para-Quinone methides Organoboron compounds

Screening COVID-19 from chest X-ray images by an optical diffractive neural network with the optimized F number

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Photonics Research 2024年第7期12卷 1410-1426页

作者： JIALONG WANG SHOUYU CHAI WENTING GU BOYI LI XUE JIANG YUNXIANG ZHANG HONGEN LIAO XIN LIU DEAN TA Academy for Engineering and Technology Fudan UniversityShanghai 200433China Center for Biomedical Engineering Fudan UniversityShanghai 200433China department of chemistry Fudan UniversityShanghai 200433China department of Biomedical Engineering School of MedicineTsinghua UniversityBeijing 100084China

The COVID-19 pandemic continues to significantly impact people's lives worldwide, emphasizing the critical need for effective detection methods. Many existing deep learning-based approaches for COVID-19 detection offer high accuracy but demand substantial computing resources, time, and energy. In this study, we introduce an optical diffractive neural network(ODNN-COVID), which is characterized by low power consumption, efficient parallelization, and fast computing speed for COVID-19 detection. In addition, we explore how the physical parameters of ODNN-COVID affect its diagnostic performance. We identify the F number as a key parameter for evaluating the overall detection capabilities. Through an assessment of the connectivity of the diffractive network, we established an optimized range of F number, offering guidance for constructing optical diffractive neural networks. In the numerical simulations, a three-layer system achieves an impressive overall accuracy of 92.64% and 88.89% in binary-and threeclassification diagnostic tasks. For a single-layer system, the simulation accuracy of 84.17% and the experimental accuracy of 80.83% can be obtained with the same configuration for the binary-classification task, and the simulation accuracy is 80.19% and the experimental accuracy is 74.44% for the three-classification task. Both simulations and experiments validate that the proposed optical diffractive neural network serves as a passive optical processor for effective COVID-19 diagnosis, featuring low power consumption, high parallelization, and fast computing capabilities. Furthermore, ODNN-COVID exhibits versatility, making it adaptable to various image analysis and object classification tasks related to medical fields owing to its general architecture.

关键词： neural network offering

Granting strength to aerogel fibers through encapsulation

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Science China Materials 2024年第4期67卷 1365-1366页

作者： Wenhui Xu department of Basic chemistry School of PharmacyJiangxi University of Chinese MedicineNanchang 330004China

Aerogel fibers, distinguished by their lightweight nature, pronounced porosity, large surface area, and superior thermal insulation properties, have diversified applications in thermal management, energy devices, and environmental remediation[1]. However, compared with monolithic ones, these fibershaped aerogels exhibit limited mechanical strength and resilience due to their one-dimensional small size.

关键词： strength fibers thermal

mIgM-mediated splenic marginal zone B cells targeting of folic acid for immunological evasion

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Acta Pharmaceutica Sinica B 2024年第2期14卷 808-820页

作者： Huan Wang Zhuxuan Jiang Zhiwei Guo Gan Luo Tianhao Ding Changyou Zhan department of Pharmacology School of Basic Medical Sciences&Department of PharmacyShanghai Pudong HospitalFudan UniversityShanghai 200032China department of Pharmaceutical Sciences School of PharmacyNaval Medical UniversityShanghai 200433China Shanghai Engineering Research Center for Synthetic Immunology Fudan UniversityShanghai 200032China

Folic acid is a fully oxidized synthetic folate with high bioavailability and stability which has been extensively prescribed to prevent congenital *** we revealed the immunosuppressive effect of folic acid by targeting splenic marginal zone B(MZB)*** acid demonstrates avid binding with the Fc domain of immunoglobulin M(IgM),targeting IgM positive MZB cells in vivo to destabilize IgM-B cell receptor(BCR)complex and block immune *** induced anergy of MZB cells by folic acid provides an immunological escaping window for *** conjugation of folic acid with therapeutic proteins and antibodies induces immunological evasion to mitigate the production of anti-drug antibodies,which is a major obstacle to the long-term treatment of biologics by reducing curative effects and/or causing adverse *** acid acts as a safe and effective immunosuppressant via IgM-mediated MZB cells targeting to boost the clinical outcomes of biologics by inhibiting the production of anti-drug antibodies,and also holds the potential to treat other indications that adverse immune responses need to be transiently shut off.

关键词： Membrane-bound IgM Anti-drugantibodies Bcell anergy Folic acid Marginal zoneBcells Bcell receptor Biologics Targeting

A multi-parameter-induced activation of gas therapeutic platform to remarkably amplify photodynamic therapy efficacy

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Science China chemistry 2024年第7期67卷 2403-2411页

作者： Jie Sun Ziwen Zhang Hongyu Wu Xuemei Dong Chengjun Dong Lixin Sun Zhiqian Guo Yingchao Liu Xianfeng Gu Chunchang Zhao Key Laboratory for Advanced Materials and Feringa Nobel Prize Scientist Joint Research Center Institute of Fine ChemicalsSchool of Chemistry and Molecular EngineeringEast China University of Science and TechnologyShanghai 200237China department of medicinal chemistry School of PharmacyFudan UniversityShanghai 201203China Shandong Provincial Hospital Affiliated to Shandong First Medical university Shandong First Medical University&Shandong Academy of Medical ScienceJinan 250021China

Gas therapy(GT)combined with photodynamic therapy(PDT)is an effective strategy to compensate for the PDT limitation caused by the hypoxic tumor microenvironment,which can greatly improve PDT *** uncontrolled leakage of gas molecules during delivery seriously hinders its practical biological ***,we report a multifunction nanomedicine that enables precise gas therapy(including carbon monoxide(CO)release and H_(2)S depletion)using a multi-parameter-induced activation gas release strategy,enlarging the PDT *** nanomedicine uses a disulfide bond to covalently link a photosensitizer with the CO donor 3-hydroxyflavone(3-HF).The disulfide bond can be specifically consumed in H_(2)S-rich tumor areas,releasing the CO donor(3-HF),and also depleting H_(2)*** importantly,the photo-controlled production of^(1)O_(2)can induce 3-HF precise release of CO in the tumor *** H_(2)S,light,and^(1)O_(2)multi-parameter-induced activation of gas release strategy ensures the accuracy of GT to amplify PDT *** expected,in vitro and in vivo investigations show that GT makes up for the PDT limitation,exhibiting the highest tumor therapeutic *** multi-parameter-activated design strategy provides a new way to improve the precision and efficacy of multimodal synergistic therapy of tumors.

关键词： gas therapy precision gas release hydrogen sulfide depletion photodynamic therapy multimodal synergistic therapy

Hydrophobic tagging-induced degradation of NAMPT in leukemia cells

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Chinese Chemical Letters 2024年第9期35卷 214-218页

作者： Menglu Guo Ying-Qi Song Junfei Cheng Guoqiang Dong Xun Sun Chunquan Sheng department of Natural Medicine School of PharmacyFudan UniversityShanghai 201203China school of Pharmaceutical Sciences Hainan UniversityHaikou 570228China school of pharmacy Second Military Medical UniversityShanghai 200433China

Nicotinamide phosphoribosyl transferase(NAMPT)is considered as a promising target for cancer therapy to its crucial role in cancer *** the therapeutic potential of NAMPT enzymatic inhibitors,their effectiveness is limited by dose-related toxicity and the inability to suppress nonenzymatic functions of extracellular NAMPT(e NAMPT).Herein,we designed and synthesized the first hydrophobic tagging NAMPT *** them,compound NH-11 selectively degraded NAMPT in leukemia cells through the ubiquitin-proteasome *** NH-11 effectively induced apoptosis and showed low toxicity to normal cells,representing a promising anti-leukemia lead compound.?2024 Published by Elsevier *** behalf of Chinese Chemical Society and Institute of Materia Medica,Chinese Academy of Medical Sciences.

关键词： NAMPT Hydrophobic tagging Leukemia Degradation Anti-cancer

Nickel-Catalyzed Regio-and Stereoselective Defluorinative Arylation of gem-Difluorinated Cyclopropanes

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Chinese Journal of chemistry 2024年第8期42卷 823-828页

作者： Shutao Qi Yunkai Hua Liangkai Pan Junfeng Yang Junliang Zhang department of chemistry Fudan University2005 Songhu RoadShanghai200438 China fudan Zhangjiang Institute Shanghai201203 China school of chemistry and Chemical Engineering Henan Normal UniversityXinxiangHenan 453007China

Comprehensive Summary,Herein,we report nickel-catalyzed cross-coupling of gem-difluorinated cyclopropanes with boronic acids,providing the corresponding arylated 2-fluoroallylic *** approach used commercially available phosphine ligand Xantphos to obtain monofluorinated alkenes with high regioselectivity and *** studies proposed a Ni(II)-fluoroallyl pathway and excluded the radical pathway.

关键词： Nickel Monofluoroolefin Cyclopropane Regioselectivity Stereoselectivity C-C coupling Cross-coupling Synthetic methods