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Simultaneous Screening and Analysis of Anti-inflammatory and Antiproliferative Compounds from Euphorbia maculata Combining Bio-affinity Ultrafiltration with Multiple Drug Targets

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Journal of Analysis and Testing 2022年第2期6卷 98-110页

作者： Tojofaniry Fabien Rakotondrabe min-xia fan Yong-Li Zhang ming-Quan Guo CAS Key Laboratory of Plant Germplasm Enhancement and Specialty Agriculture Wuhan Botanical GardenChinese Academy of SciencesWuhan 430074China University of Chinese Academy of Sciences Beijing 100049China Sino-Africa Joint Research Center Chinese Academy of SciencesWuhan 430074China Innovation Academy for Drug Discovery and Development Chinese Academy of SciencesShanghai 201203China

Euphorbia maculata has long been used for managing different impairments in Asian ***,its antioxidant,anti-inflammatory and antiproliferative potentialities,along with its potential bioactive compounds remain *** this context,a bio-a ffinity ultrafiltration strategy was developed to fish out ligand candidates against Cycloxygenase-2(COX-2),Topoisomerase I(Topo I),and TopoisomeraseⅡ(TopoⅡ).Thereafter,lead compounds activities were assessed in silico and in vitro for ascertaining the screening results and forecasting its corresponding *** a result,the *** ethyl acetate(EMEA)fraction showed interesting COX-2 inhibition activity with an IC 50 value of 0.67±0.09μg/mL,as well as good growth inhibitions for three malignant cell *** chemical fingerprinting was also conducted to enable a tentative identification of 17 compounds,among which,11 were assessed as ligand candidates to COX-2,8 compounds to Topo I,and 10 compounds to TopoⅡ.Dihydromyricetin and quercetin-3-O-arabinoside were revealed to be multipotent compounds which exerted good a ffinity to the three targeted enzymes,and also supported with their molecular docking simulations and in vitro assay *** interrelationship between ***’s associated activities(antioxidant,anti-inflammatory and antiproliferative)was revealed with the corresponding multipotent phytochemical active components from this *** also provided a useful direction for its empirical traditional use and further explorations in the near future.

关键词： Euphorbia maculata Antioxidant Anti-infl ammatory Antiproliferative UF-UPLC-QTOF-MS/MS Multipotent compounds

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Establishment of human cerebral organoid systems to model early neural development and assess the central neurotoxicity of environmental toxins

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Neural Regeneration Research 2025年第1期20卷 242-252页

作者： Daiyu Hu Yuanqing Cao Chenglin Cai Guangming Wang min Zhou Luying Peng Yantao fan Qiong Lai Zhengliang Gao Fundamental Research Center Shanghai Yangzhi Rehabilitation Hospital(Shanghai Sunshine Rehabilitation Center)School of MedicineTongji UniversityShanghaiChina Institute of Geriatrics(Shanghai University) Affiliated Nantong Hospital of Shanghai University(The Sixth People’s Hospital of Nantong)Shanghai University School of MedicineNantongJiangsu ProvinceChina Shanghai Engineering Research Center of Organ Repair Shanghai University School of MedicineShanghaiChina Key Laboratory of Arrhythmias Ministry of EducationShanghai East HospitalSchool of MedicineTongji UniversityShanghaiChina

Human brain development is a complex process,and animal models often have significant *** address this,researchers have developed pluripotent stem cell-derived three-dimensional structures,known as brain-like organoids,to more accurately model early human brain development and *** enable more consistent and intuitive reproduction of early brain development,in this study,we incorporated forebrain organoid culture technology into the traditional unguided method of brain organoid *** involved embedding organoids in matrigel for only 7 days during the rapid expansion phase of the neural epithelium and then removing them from the matrigel for further cultivation,resulting in a new type of human brain organoid *** cerebral organoid system replicated the temporospatial characteristics of early human brain development,including neuroepithelium derivation,neural progenitor cell production and maintenance,neuron differentiation and migration,and cortical layer patterning and formation,providing more consistent and reproducible organoids for developmental modeling and toxicology *** a proof of concept,we applied the heavy metal cadmium to this newly improved organoid system to test whether it could be used to evaluate the neurotoxicity of environmental *** organoids exposed to cadmium for 7 or 14 days manifested severe damage and abnormalities in their neurodevelopmental patterns,including bursts of cortical cell death and premature *** exposure caused progressive depletion of neural progenitor cells and loss of organoid integrity,accompanied by compensatory cell proliferation at ectopic *** convenience,flexibility,and controllability of this newly developed organoid platform make it a powerful and affordable alternative to animal models for use in neurodevelopmental,neurological,and neurotoxicological studies.

关键词： cadmium cell death cell proliferation cortical development environmental toxins neural progenitor cells neurogenesis neurotoxicology organoids stem cells

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Tackling the microlensing wave effects of strong lensing gravitational waves with TAAH

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Science China(Physics,Mechanics & Astronomy) 2025年第1期Mechanics & Astronomy) .卷 257-258页

作者： Zuhui fan South-Western Institute for Astronomy Research Yunnan University

The rapid development of gravitational wave（GW） observations since their first detection in 2015 [1] has opened a completely new window for exploring the Universe. Consequently, astronomical research has entered the multimessenger era, allowing us to use different tracers to view the cosmos from various perspectives. Among others, the appealing application of gravitational wave events from compact binary mergers is that they can act as standard sirens to determine absolute cosmic distances entirely independent of standard candles. This approach is one of the most promising means to solve the current H0tension problem.

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Soluble epoxide hydrolase:a next-generation drug target for Alzheimer's disease and related dementias

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Neural Regeneration Research 2025年第9期20卷 2585-2586页

作者： Andrew Gregory Chengyun Tang fan fan Department of Physiology Medical College of GeorgiaAugusta UniversityAugustaGAUSA

Alzheimer's disease(AD)and Alzheimer's diseaserelated dementias(ADRD)represent a significant public health challenge,with projections indicating a substantial increase in affected individuals due to the aging global *** the World Health Organization,AD/ADRD has affected more than 55 million individuals worldwide,with an additional 10 million cases diagnosed each year.

关键词： Alzheimer population drug

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Synthetic control of chiral pore surfaces in covalent organic frameworks for enantioselective separation of chiral drugs

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Science China Chemistry 2025年

作者： Shiguo Fu xiaofeng Zhang Kaixuan Wang Linfeng Chen fan xia Yong Cui Yan Liu School of Chemistry and Chemical Engineering Frontiers Science Center for Transformative Molecules and State Key Laboratory of Metal Matrix Composites Shanghai Jiao Tong University Faculty of Materials Science and Chemistry China University of Geosciences

Enantioselective separations of racemates using porous materials are highly attractive and significant in both fundamental research and technological applications. However, achieving controlled chiral pore surfaces to create the necessary driving force for enantiomer discrimination poses a fundamental challenge. Herein, we demonstrate that chiral covalent organic frameworks(COFs) possess the essential characteristics for effective enantioseparations through synthetic control over pore surfaces. We synthesized three 3D chiral COFs (CCOFs) featuring abundant chiral recognition sites on the pore walls via the condensation of enantiopure dialdehyde of 2,2′-dihydroxy-1,1′-binaphthyl and tetraamine. All CCOFs with high stability exhibit an 11-fold interpenetrated framework with tubular open channels, decorated with dihydroxyl or diethoxyl groups. The CCOFs with dihydroxyl groups serve as solid adsorbents for the adsorptive separation and solid-phase extraction of various chiral 1-phenylethanol-derived enantiomers, particularly racemic drugs, achieving up to 98%enantiomeric excess. In contrast, the CCOF with diethoxy groups is unable to resolve the racemates. These CCOF materials can be recycled and reused without any apparent loss of performance. Density functional theory (DFT) calculations reveal that the enantiospecific recognition arises from the well-organized chiral inner sphere and multiple chiral host-guest interactions.

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Effect of a Carbon Fibre-steel Fibre-graphite Conductive Filler on the Electrothermal Properties of Cementitious Materials

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Journal of Wuhan University of Technology(Materials Science) 2025年第1期40卷 141-151页

作者： fan Yanan WEI Hong ZHENG Hongyong DU Hongxiu Department of Architecture and Environmental Engineering Taiyuan UniversityTaiyuan 030032China College of Civil Engineering Taiyuan University of TechnologyTaiyuan 030032China

Carbon fibre,steel fibre and graphite were used as conductive fillers to prepare cementitious materials with excellent electrothermal *** electrically conductive cementitious materials with different volume dosages were analysed through compressive and flexural strength,electrochemical impedance spectroscopy and temperature rise *** equivalent circuit model was established to study the electrically conductive heat generation mechanism in the electrically conductive cementitious *** results indicate that the mechanical properties of cementitious composite materials with a ternary conductive phase are better than those of pristine cementitious materials because the fibrous filler improves their mechanical ***,the incorporation of graphite in the material reduces its *** fibrous and point-like conductive phase materials into the cementitious material enhances the overall conductive pathway and considerably reduces the electrical resistance of the cementitious material,enhancing its conductive *** volume ratios of carbon fibre,steel fibre and graphite that achieve an optimal complex doping in the cementitious material were 0.35%,0.6%and 6%,*** was determined using the mutation point of each circuit element parameter as the percolation *** addition,at a certain safety voltage,there is a uniform change between the internal and surface temperatures of the conductive cementitious material,and the heating effect in this materialis is considerably better than that in the pristine cementitious material.

关键词： cementitious composites conductive fillers electrothermal properties electrochemical impedance spectroscopy

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Endoscopy-assisted lightweight diagnosis system based on transformers for colon polyp detection

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Optoelectronics Letters 2025年第1期21卷 57-64页

作者： fan Weiming YU Jiahui JU Zhaojie School of Automation and Electrical Engineering Shenyang Ligong University Department of Biomedical Engineering Zhejiang University School of Computing University of Portsmouth

The integration of endoscopy has significantly propelled the diagnosis and treatment of gastrointestinal diseases, with colonoscopy establishing itself as the primary method for early diagnosis and preventive care in colorectal cancer(CRC). Although deep learning holds promise in mitigating missed polyp rates, modern endoscopy examinations pose additional challenges, such as image blurring and atomizing. This study explores lightweight yet powerful attention mechanisms, introducing the spatial-channel transformer(SCT), an innovative approach that leverages spatial channel relationships for attention weight calculation. The method utilizes rotation operations for inter-dimensional dependencies, followed by residual transformation, encoding inter-channel and spatial information with minimal computational overhead. Extensive experiments on the CVC-Clinic DB polyp detection dataset, addressing endoscopy pitfalls, underscore the superiority of our SCT over other state-of-the-art methods. The proposed model maintains high performance, even in challenging scenarios.

关键词： Endoscopy

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Visualization of the protective role of estrogen against female liver fibrosis via an ER viscosity NIR fluorescent probe

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Science China Chemistry 2025年第1期 360-368页

作者： Zheng Liu Changyu Zhang Zipeng Li Wanying Ma Jia Liu xiang xia Ning Xu Wen Sun Jianjun Du Jiangli fan xiaojun Peng State Key Laboratory of Fine Chemicals Dalian University of Technology Ningbo Institute of Dalian University of Technology

Endoplasmic reticulum(ER) viscosity has emerged as a new potential biomarker for hepatic fibrosis(HF). Herein, we report the first ER-targeting viscosity-responsive near-infrared(NIR) fluorescent probe HBT-PP for investigations of HF *** twisted intramolecular charge transfer(TICT) and the excited state intramolecular proton transfer(ESIPT) are combined to endow HBT-PP with the selective response towards viscosity(～62-fold) and a super large stokes shift(～320 nm). HBT-PP mainly targets organelle ER and is able to image the drug-or alcohol-induced viscosity elevation in living cells. Significantly,HBT-PP was successfully applied to visualize the gender difference in HF and the protective role of estrogen in restraining HF progression. Of note, after 10 min of stain with HBT-PP, HF lesions showed a stage-based response, indicating the potential of this probe in fast and early diagnosis of HF. These results clearly demonstrated the promising application of HBT-PP as a new tool for exploring ER viscosity-involved physiological and pathological processes.

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Engineering high-performance chemiluminescent probes via enzymatic pocket targeting: high-throughput screening for ultralong afterglow imaging of orthotopic hepatocellular carcinoma

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Science China Chemistry 2025年

作者： Shuai Huang Shuaige Bai Ting Luo Bin Feng min Liu fan Zheng Shuang Huang Yanpeng fang Dan Ding Wenbin Zeng xiangya School of Pharmaceutical Sciences Central South University College of Life Sciences Nankai University

Hepatocellular carcinoma （HCC） is a highly aggressive liver malignancy and the main form of liver cancer. Early diagnosis and treatment of HCC can effectively reduce mortality. Carboxylesterase （CE）-specific detection and imaging can be used for early diagnosis and image-guided surgical of HCC. However, traditional optical probes suffer from poor selectivity and low imaging signal-to-noise ratio. Here, we have constructed a series of chemiluminescent probes for carboxylesterase detection based on the strategy of enzymatic pocket-oriented steric tailoring techniques. The probes with different unique and excellent properties have been obtained through the structure-based steric hindrance adjustment on the recognition site. Here, CE-2 has been successfully used for high-throughput screening of rapid carboxylesterase inhibitors due to its extremely low detection limit (2.5×10-4U mL-1) and fast recognition ability. CE-3 has been successfully used for image-guided surgery of orthotopic hepatocellular carcinoma due to its ultra-long chemiluminescence imaging （over 12 h） of hepatocellular carcinoma. This study may promote advances in the rapid detection and screening of inhibitory drugs for CE and the field of surgical navigation in HCC.

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Macro-mechanics and Microstructure of Nanomaterial-modified Geopolymer Concrete: A Comprehensive Review

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Journal of Wuhan University of Technology(Materials Science) 2025年第1期40卷 204-214页

作者： WANG Tao fan xiangqian GAO Changsheng QU Chiyu The National Key Laboratory of Water Disaster Prevention Nanjing Hydraulic Research InstituteNanjing 210024China Southern Marine Science and Engineering Guangdong Laboratory(Guangzhou) Guangzhou 511458China School of Water Conservancy and Transportation Zhengzhou UniversityZhengzhou 450001China

We have described in detail the effects of nano-SiO_(2),nano-CaCO_(3),carbon nanotubes,and nano-Al_(2)O_(3) on geopolymer concrete from the perspectives of macro mechanics and *** existing research results show that the mechanism of nano-materials on geopolymer concrete mainly includes the filling effect,nucleation effect,and bridging effect,the appropriate amount of nano-materials can be used as fillers to reduce the porosity of geopolymer concrete,and can also react with Ca(OH)2 to produce C-S-H gel,thereby improving the mechanical properties of geopolymer *** optimum content of nano-SiO_(2) is between 1.0%and 2.0%.The optimum content of nano-CaCO_(3) is between 2.0%and 3.0%.The optimum content of carbon nanotubes is between 0.1%and 0.2%.The optimum content of nano-Al_(2)O_(3) is between 1.0%and 2.0%.The main problems existing in the research and application of nanomaterial-modified geopolymer concrete are summarized,which lays a foundation for the further application of nanomaterial in geopolymer concrete.

关键词： nanomaterials low carbon geopolymer concrete macro-mechanics microstructure

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