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Folic Acid Modified Polymeric Micelles for Intravesical Instilled Chemotherapy

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Chinese Journal of Polymer Science 2018年第4期36卷 479-487页

作者： Dan-Hua Zhou Guan Zhang qing-song yu Zhi-Hua Gan National University of Singapore Environmental Research Institute(NERI) National University of SingaporeSingapore 117576Singapore Beijing Advanced Innovation Center for Soft Matter Science and Engineering State Key Laboratory of Organic-inorganic Composite MaterialsCollege of Life Science and TechnologyBeijing University of Chemical TechnologyBeijing 100029China Department of Urology China-Japan Friendship HospitalBeijing 100029China

In this study, a targeting micellar drug delivery system was developed for intravesical instilled chemotherapy of bladder cancer. The amphiphilic diblock copolymer poly（？-caprolactone）-block-poly（ethylene glycol）（PCL-b-PEO） with functional amino group（NH2） at the end of PEO block was synthesized. Then the copolymer was conjugated with folic acid（FA） and fluorescein isothiocyannate（FITC） via the PEO-NH2 terminus, and then assembled into micelles with the target moiety and fluorescence labeling. In addition, drug loaded micelles were also fabricated with anticancer drug doxorubicin（DOX） encapsulated in the hydrophobic core. The micelles were characterized in terms of size, drug loaded efficiency and critical micellization concentration（CMC） by means of DLS, UV and fluorescence spectra. In vitro cellular uptake and cytotoxicity studies showed that FA modified PCL-b-PEO-FA micelles have a greater targeting efficiency to human bladder cancer cell（T-24 cell） compared to PCL-b-PEO-NH2 micelles due to the conjugation of FA on the surface, while no targeting effect to normal tissue originated human embryonic kidney 293（HEK-293） cells was observed, enabling the micelles a promising drug carrier for intravesical instilled chemotherapy of bladder cancer.

关键词： Targeted drug delivery Superficial bladder cancer Intravesical instilled chemotherapy Folic acid Micelles

Comb-like Poly(N-(2-hydroxypropyl) methacrylamide) Doxorubicin Conjugates: The Influence of Polymer Architecture and Composition on the Biological Properties

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Chinese Journal of Polymer Science 2018年第11期36卷 1225-1238页

作者： Hao Tang Jin Tang Yi Shen Wen-Xuan Guo Min Zhou Rui-Hua Wang Ni Jiang Zhi-Hua Gan qing-song yu The State Key Laboratory of Organic-inorganic Composites Beijing Laboratory of Biomedical Materials Beijing University of Chemical Technology College of Life Science and Technology Beijing University of Chemical Technology Beijing Advanced Innovation Center for Soft Matter Science and Engineering Beijing University of Chemical Technology

The synthesis and structure-property correlation of poly（N-（2-hydroxypropyl） methacrylamide）（PHPMA） conjugates with various architectures including random, block, branched or star-like structures and compositions have been thoroughly explored. However, related synthesis and structure-property data are still lacking for comb-like PHPMA. In this work, we report the synthesis of comb-like PHPMA copolymer-doxorubicin （DOX） conjugates with different backbone/side-chain lengths and location of drug moieties. Well-defined comb-like PHPMA-DOX conjugates are obtained via the combination of controlled radical polymerization and fractional precipitation techniques. The influences of structural factors on the biological properties such as cellular uptake, blood circulation and tumor accumulation have been investigated. Long blood circulation and efficient tumor accumulation can be achieved by proper control of the comb number, length and location of drug moieties. These facile comb-like structures possess great potentials in future theranostics for brachytherapy or surgical navigation.

关键词： Poly（N-（2-hydroxypropyl） methacrylamide） Comb-like copolymer Anticancer drug delivery Synthesis Structure-property correlation

Chalcone derivatives as novel,potent and selective inhibitors against human Notum:Structure–activity relationships and biological evaluations

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Chinese Chemical Letters 2024年第3期35卷 321-325页

作者： Jin-Hui Shi Bei Zhao Li-Lin song yu-qing song Meng-Ru Sun Tian Tian Hong-yu Chen yun-qing song Jian-Ming Sun Guang-Bo Ge Shanghai Frontiers Science Center of TCM Chemical Biology Institute of Interdisciplinary Integrative Medicine Research Shanghai University of Traditional Chinese MedicineShanghai 201203China Dalian Engineering Research Center for Carbohydrate Agricultural Preparations Liaoning Provincial Key Laboratory of CarbohydratesDalian Institute of Chemical PhysicsChinese Academy of SciencesDalian 116023China Seventh People's Hospital of Shanghai University of Traditional Chinese Medicine Shanghai 200137China

Human Notum(hNotum)inhibitors could be used for treating Wnt signalling-associated diseases including colorectal cancer.Herein,two series of chalcone derivatives were designed and synthesized aiming to find selective and potent hNotum inhibitors.Structure–activity relationship(SAR)studies showed that 2-methoxyl and 5-bromine substitutions on A-ring significantly enhanced anti-hNotum effect,while 4’-ethoxyl and 3’-alkyl substitutions on B-ring were beneficial for hNotum inhibition.Among all tested chalcones,B11 displayed the most potent anti-Notum effect(IC_(50)=3.6 nmol/L),good selectivity,excellent chemical stability and suitable metabolic stability.Further investigations showed that B11 acted as a competitive inhibitor of hNotum,while this agent(5μmol/L)significantly weaken the migration abilities of colorectal cancer cells.Collectively,this study deciphers the SARs of chalcones as hNotum inhibitors and reports a novel and potent hNotum inhibitor with the anti-migration effect on colorectal cancer cells,which offers a promising lead compound to develop novel anti-cancer agents.

关键词： Human notum(hNotum) Chalcone Computer-assisted drug discovery Structure–activity relationship(SAR) Anti-colorectal cancer agent

Effects of Diesel Concentration on the Thermal Conductivity,Specific Heat Capacity and Thermal Diffusivity of Diesel-Contaminated Soil

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Journal of Thermal Science 2024年第2期33卷 696-709页

作者： WU yuhao WU yuefei LUO Gubai ZHANG Teng WANG qing FAN Liwu song Xin yu Zitao Key Laboratory of Clean Energy and Carbon Neutrality of Zhejiang Province Zhejiang UniversityHangzhou310027China State Key Laboratory of Clean Energy Utilization Zhejiang UniversityHangzhou310027China Institute of Thermal Science and Power Systems School of Energy EngineeringZhejiang UniversityHangzhou310027China Center Environmental Protection Technology Company Limited Beijing100176China Institute of Soil Science Chinese Academy of SciencesNanjing210008China

High energy consumption is a serious issue associated with in situ thermal desorption(TD)remediation of sites contaminated by petroleum hydrocarbons(PHs).The knowledge on the thermophysical properties of contaminated soil can help predict accurately the transient temperature distribution in a remediation site,for the purpose of energy conservation.However,such data are rarely reported for PH-contaminated soil.In this study,by taking diesel as a representative example for PHs,soil samples with constant dry bulk density but different diesel mass concentrations ranging from 0% to 20% were prepared,and the variations of their thermal conductivity,specific heat capacity and thermal diffusivity were measured and analyzed over a wide temperature range between 0℃ and 120℃.It was found that the effect of diesel concentration on the thermal conductivity of soil is negligible when it is below 1%.When diesel concentration is below 10%,the thermal conductivity of soil increases with raising the temperature.However,when diesel concentration becomes above 10%,the change of the thermal conductivity of soil with temperature exhibits the opposite trend.This is mainly due to the competition between soil minerals and diesel,because the thermal conductivity of minerals increases with temperature,whereas the thermal conductivity of diesel decreases with temperature.The analysis results showed that,compared with temperature,the diesel concentration has more significant effects on soil thermal conductivity.Regardless of the diesel concentration,with the increase of temperature,the specific heat capacity of soil increases,while the thermal diffusivity of soil decreases.In addition,the results of a control experiment exhibited that the relative differences of the thermal conductivity of the soil samples containing the same concentration of both diesel and a pure alkane are all below 10%,indicating that the results obtained with diesel in this study can be extended to the family of PHs.A theoretical prediction model was proposed based on c

关键词： contaminated soil diesel concentration thermal conductivity specific heat capacity thermal diffusivity thermal desorption fractal model

Effect of an Airbag-selective Portal Vein Blood Arrester on the Liver after Hepatectomy:A New Technique for Selective Clamping of the Portal Vein

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Current Medical Science 2024年第2期44卷 380-390页

作者： Ce-xiong FU Xiao-ri QIN Jin-song CHEN Jie ZHONG yu-xu XIE Bi-dan LI qing-qing FU Fang LI Jin-fang ZHENG Department of Hepatobiliary and Pancreatic Surgery Hainan General HospitalHainan Affiliated Hospital of Hainan Medical UniversityHaikou 57031lChina University of South China Hengyang 421001China Department of Gastroenterology Gastroenterology Endoscopy CenterHainan General HospitalHainan Affiliated Hospital of Hainan Medical UniversityHaikou 57031lChina Center of Clinical Laboratory Hainan General HospitalHainan Afiliated Hospital of Hainan Medical UniversityHaikou 570311China Department of Radiology Hainan General HospitalHainan Afiliated Hospital of Hainan Medical UniversityHaikou 570311China

Objective:A novel technique was explored using an airbag-selective portal vein blood arrester that circumvents the need for an intraoperative assessment of anatomical variations in patients with complex intrahepatic space-occupying lesions.Methods:Rabbits undergoing hepatectomy were randomly assigned to 4 groups:intermittent portal triad clamping(PTC),intermittent portal vein clamping(PVC),intermittent portal vein blocker with an airbag-selective portal vein blood arrester(APC),and without portal blood occlusion(control).Hepatic ischemia and reperfusion injury were assessed by measuring the 7-day survival rate,blood loss,liver function,hepatic pathology,hepatic inflammatory cytokine infiltration,hepatic malondialdehyde levels,and proliferating cell nuclear antigen levels.Results:Liver damage was substantially reduced in the APC and PVC groups.The APC animals exhibited transaminase levels similar to or less oxidative stress damage and inflammatory hepatocellular injury compared to those exhibited by the PVC animals.Bleeding was significantly higher in the control group than in the other groups.The APC group had less bleeding than the PVC group because of the avoidance of portal vein skeletonization during hepatectomy.Thus,more operative time was saved in the APC group than in the PVC group.Moreover,the total 7-day survival rate in the APC group was higher than that in the PTC group.Conclusion:Airbag-selective portal vein blood arresters may help protect against hepatic ischemia and reperfusion injury in rabbits undergoing partial hepatectomy.This technique may also help prevent liver damage in patients requiring hepatectomy.

关键词： hepatectomy portal vein hepatic damage selective clamping

Development of a scintillating-fiber-based beam monitor for the coherent muon-to-electron transition experiment

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Nuclear Science and Techniques 2024年第4期35卷 156-164页

作者： yu Xu yun-song Ning Zhi-Zhen Qin Yao Teng Chang-qing Feng Jian Tang yu Chen Yoshinori Fukao Satoshi Mihara Kou Oishi School of Physics Sun Yat-sen UniversityGuangzhou 510275China State Key Laboratory of Particle Detection and Electronics University of Science and Technology of ChinaHefei 230026China Department of Modern Physics University of Science and Technology of ChinaHefei 230026China High Energy Accelerator Research Organization(KEK) Ibaraki 305‑0801Japan Department of Physics Imperial College LondonLondon SW72AZUK

The coherent muon-to-electron transition(COMET)experiment is a leading experiment for the coherent conversion of μ^(-)N→e^(-)N using a high-intensity pulsed muon beamline,produced using innovative slow-extraction techniques.Therefore,it is critical to measure the muon beam characteristics.We set up a muon beam monitor(MBM),where scintillating fibers woven in a cross shape were coupled to silicon photomultipliers to measure the spatial profile and timing structure of the extracted muon beam for the COMET.The MBM detector was tested successfully with a proton beamline at the China Spallation Neutron Source and took data with good performance in the commissioning run.The development of the MBM,including its mechanical structure,electronic readout,and beam measurement results,are discussed.

关键词： Beam instrumentation Profile monitor Scintillating fiber Silicon photomultipliers

Comparative Study on the Immunogenicity and Efficacy of Different Post-exposure Intramuscular Rabies Vaccination Regimens in China

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Biomedical and Environmental Sciences 2024年第2期37卷 178-186页

作者： song yun HE Ying LU Xue Xin ZHANG Xiao Mei JIANG XIAO Lin song qing HUANG Xue Yong MA Hong Xia yu Peng Cheng ZHU Wu Yang Henan Provincial Center for Disease Control and Prevention Infectious Disease Prevention and Control InstituteHenan Provincial Key Laboratory of Infectious Disease PathogensZhengzhou 450000HenanChina National Institute for Viral Disease Control and Prevention China CDCKey Laboratory of BiosafetyNational Health CommissionBeijing 102206China Shandong Provincial Center for Disease Control and Prevention Jinan 250014ShandongChina qingdao Chengyang District Center for Disease Control and Prevention Qingdao 266108ShandongChina

Objective This study aimed to compare the current Essen rabies post-exposure immunization schedule(0-3-7-14-28)in China and the simple 4-dose schedule(0-3-7-14)newly recommended by the World Health Organization in terms of their safety,efficacy,and protection.Methods Mice were vaccinated according to different immunization schedules,and blood was collected for detection of rabies virus neutralizing antibodies(RVNAs)on days 14,21,28,35,and 120after the first immunization.Additionally,different groups of mice were injected with lethal doses of the CVS-11 virus on day 0,subjected to different rabies immunization schedules,and assessed for morbidity and death status.In a clinical trial,185 rabies-exposed individuals were selected for post-exposure vaccination according to the Essen schedule,and blood was collected for RVNAs detection on days 28and 42 after the first immunization.Results A statistically significant difference in RVNAs between mice in the Essen and 0-3-7-14 schedule groups was observed on the 35th day(P0.05)in RVNAs levels at any time point.The post-exposure immune protective test showed that the survival rate of mice in the control group was 20%,whereas that in the immunization groups was 40%.In the clinical trial,the RVNAs positive conversion rates on days 28(14 days after 4 doses)and 42(14 days after 5 doses)were both 100%,and no significant difference in RVNAs levels was observed(P>0.05).Conclusion The simple 4-dose schedule can produce sufficient RVNAs levels,with no significant effect of a delayed fourth vaccine dose(14–28 d)on the immunization potential.

关键词： Rabies Post-exposure immunization Essen regimen RVNAs

Molecular surface functionalization of In_(2)O_(3) to tune interfacial microenvironment for enhanced catalytic performance of CO_(2) electroreduction

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Nano Research 2024年第3期17卷 1242-1250页

作者： Suwen WangQiang GaoCui Xu Shuai Jiang Mengyang Zhang Xianjun Yin Hui-qing Peng Bin Liu yu-Fei song State Key Laboratory of Chemical Resource Engineering Beijing Advanced Innovation Center for Soft Matter Science and EngineeringCollege of ChemistryBeijing University of Chemical TechnologyBeijing 100029China

Indium-based materials(e.g.,In_(2)O_(3))are a class of promising non-noble metal-based catalysts for electroreduction of carbon dioxide(CO_(2)).However,competitive hydrogen reduction reaction(HER)on indium-based catalysts hampers CO_(2) reduction reaction(CO_(2)RR)process.We herein tune the interfacial microenvironment of In_(2)O_(3) through chemical graft of alkyl phosphoric acid molecules using a facile solution-processed strategy for the first time,which is distinguished from other researches that tailor intrinsic activity of In_(2)O_(3) themselves.The surface functionalization of alkyl phosphoric acids over In_(2)O_(3) is demonstrated to remarkably boost CO_(2) conversion.For example,octadecylphosphonic acid modified In_(2)O_(3) exhibits Faraday efficiency for H_(2) H_(2) H_(2)(FE)of as low as 6.6%and FEHCOOH of 86.5%at-0.67 V vs.RHE,which are far superior to parent In_(2)O_(3) counterparts(FE of 24.0%and FEHCOOH of 63.1%).Moreover,the enhancing effect of alkyl phosphoric acid functionalization is found to be closely related to the length of alkyl chains.By virtue of comprehensive experimental characterizations and molecular dynamics simulations,it is revealed that the modification of alkyl phosphoric acids significantly alters the interface microenvironment of the electrocatalyst,which changes the electrocatalyst surface from hydrophilic and aerophobic to hydrophobic and aerophilic.In this case,the water molecules are pushed away and more CO_(2) molecules are trapped,increasing local CO_(2) concentration at In_(2)O_(3) active sites,thus leading to the significantly enhanced CO_(2)RR and suppressed HER.This work highlights the importance of regulating the interfacial microenvironment of inorganic catalysts by molecular surface functionalization as a means for promoting the electrochemical performance in electrosynthesis and beyond.

关键词： carbon dioxide(CO_(2))electroreduction interfacial microenvironment molecular surface functionalization In_(2)O_(3)catalyst water and CO_(2)diffusion

Compound extreme inundation risk of coastal wetlands caused by climate change and anthropogenic activities in the Yellow River Delta,China

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Advances in Climate Change Research 2024年第1期15卷 134-147页

作者： Xiao-Li WANG Ai-qing FENG Xi-Yong HOU qing-Chen CHAO Bai-yuan song yu-Bin LIU Qi-Guang WANG He XU yu-Xin ZHANG Dong Li Li-Jie DONG yu GUO CAS Key Laboratory of Coastal Environmental Processes and Ecological Remediation Yantai Institute of Coastal Zone ResearchChinese Academy of SciencesYantai 264003China Shandong Key Laboratory of Coastal Environmental Processes Yantai 264003China China Meteorological Administration Key Laboratory for Climate Prediction Studies National Climate CentreBeijing 100081China Tongji Urban Planning Design Research Institute Shanghai 200092China School of Geography and Tourism Qilu Normal UniversityJinan 250200China China Meteorological Administration Training Centre China Meteorological AdministrationBeijing 10008China University of Chinese Academy of Sciences Beijing 100049China Marine Science and Technology College Zhejiang Ocean UniversityZhoushan 316022China

The coastal wetlands of the Yellow River Delta(YRD)in China are crucial for their valuable resources,environmental significance,and economic contributions.However,these wetlands are also vulnerable to the dual threats of climate change and human disturbances.Despite substantial attention to the historical shifts in YRD's coastal wetlands,uncertainties remain regarding their future trajectory in the face of compound risks from climate change and anthropogenic activities.Based on a range of remote sensing data sources,this study undertakes a comprehensive investigation into the evolution of YRD's coastal wetlands between 2000 and 2020.Subsequently,the potential fate of coastal wetlands is thoroughly analyzed through the Land Use/Cover Change(LUCC)simulation using System Dynamic-Future Land Use Simulation(SD-FLUS)model and the extreme water levels projection integrated future sea-level rise,storm surge,and astronomical high tide in 2030,2050,and 2100 under scenarios of SSP1-2.6,SSP2-4.5,and SSP5-8.5.Results revealed that YRD's coastal wetlands underwent a marked reduction,shrinking by 1688.72 km²from 2000 to 2020.This decline was mostly attributed to the substantial expansion in the areas of artificial wetlands(increasing by 823.78 km2),construction land(increasing by 767.71 km²),and shallow water(increasing by 274.58 km²).Looking ahead to 2030-2100,the fate of coastal wetlands appears to diverge based on different scenarios.Under the SSP1-2.6 scenario,the area of coastal wetland is projected to experience considerable growth.In contrast,the SSP5-8.5 scenario anticipates a notable decrease in coastal wetlands.Relative to the inundated area suffered from the current extreme water levels,the study projects a decrease of 6.8%-10.6%in submerged coastal wetlands by 2030 and 9.4%-18.2%by 2050 across all scenarios.In 2100,these percentages are projected to decrease by 0.4%(SSP2-4.5)and 27.1%(SSP5-8.5),but increase by 35.7%(SSP1-2.6).Results suggest that coastal wetlands in the YRD will face a serious compound risk from cli

关键词： Climate change Anthropogenic activities Compound extreme risk Coastal wetlands Yellow River Delta