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discovery and structure-activity relationship studies of novel tetrahydro-β-carboline derivatives as apoptosis initiators for treating bacterial infections

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Journal of Integrative Agriculture 2024年第4期23卷 1259-1273页

作者： Shanshan Su Hongwu Liu Junrong Zhang Puying Qi Yue ding Ling Zhang Linli Yang Liwei Liu Xiang Zhou Song Yang National Key laboratory of Green Pesticide/Key laboratory of Green Pesticide and Agricultural Bioengineering Ministry of Education/Center for R&D of Fine ChemicalsGuizhou UniversityGuiyang 550025China

developing and excavating new agrochemicals with highly active and safe is an important tactic for protecting crop health and food *** this paper,to discover the new bactericide candidates,we designed,prepared a new type of1,2,3,4-tetrahydro-β-carboline(THC)derivatives and evaluated the in vitro and in vivo bioactivities against the Xanthomonas oryzae ***(Xoo),Xanthomonas axonopodis ***(Xac),and Pseudomonas syringae ***(Psa).The in vitro bioassay results exhibited that most title molecules possessed good activity toward the three plant pathogenic bacteria,the compound A17 showed the most active against Xoo and Xac with EC50 values of 7.27 and 4.89 mg mL^(-1)respectively,and compound A8 exhibited the best inhibitory activity against Psa with EC50value of 4.87 mg mL^(-1).Pot experiments showed that compound A17 exhibited excellent in vivo antibacterial activities to manage rice bacterial leaf blight and citrus bacterial canker,with protective efficiencies of 52.67 and 79.79%at 200 mgmL^(-1),***,compound A8 showed good control efficiency(84.31%)against kiwifruit bacterial canker at 200 mg mL^(-1).Antibacterial mechanism suggested that these compounds could interfere with the balance of the redox system,damage the cell membrane,and induce the apoptosis of Xoo *** together,our study revealed that tetrahydro-β-carboline derivatives could be a promising candidate model for novel broadspectrum bactericides.

关键词： tetrahydro-β-carboline derivatives antibacterial activity rOS cell apoptosis

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Bactericidal bissulfone B7 targets bacterial pyruvate kinase to impair bacterial biology and pathogenicity in plants

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Science China(Life Sciences) 2024年第2期67卷 391-402页

作者： Awei Zhang Haizhen Zhang ronghua Wang Hongfu He Baoan Song runjiang Song 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

The prevention and control of rice bacterial leaf blight(BLB)disease has not yet been achieved due to the lack of effective agrochemicals and available ***,we develop a series of novel bissulfones and a novel target with a unique mechanism to address this *** developed bissulfones can control Xanthomonas oryzae ***(Xoo),and 2-(bis(methylsulfonyl)methylene)-N-(4-chlorophenyl)hydrazine-1-carboxamide(B_(7))is more effective than the commercial drugs thiodiazole copper(TC)and bismerthiazol(BT).Pyruvate kinase(PYK)in Xoo has been identified for the first time as the target protein of our bissulfone B_(7).PYK modulates bacterial virulence via a CrP-like protein(Clp)/two-component system regulatory protein(reg r)*** elucidation of this pathway facilitates the use of B_(7)to reduce PYK expression at the transcriptional level,block PYK activity at the protein level,and impair the interaction within the PYK-Clp-reg r complex via competitive inhibition,thereby attenuating bacterial biology and *** study offers insights into the molecular and mechanistic aspects underlying anti-Xoo strategies that target *** believe that these valuable discoveries will be used for bacterial disease control in the future.

关键词： 2-bissulfone-N-phenylhydrazine-1-carboxamide derivatives Xoo antibacterial activities pyruvate kinase regulatory mechanism

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Screening and identification of functional bacterial attachment genes in aerobic granular sludge

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Journal of Environmental Sciences 2024年第7期141卷 205-214页

作者： Kai Qiao Tingting Zhao LeiWang Wei Zhang WeiMeng Fan Liu Xu Gao Jianrong Zhu School of Environment Beijing Normal UniversityBeijing 100875China State Key laboratory of Water Simulation Beijing 100875China r&d Centre of Aerobic Granule Technology Beijing 100875China

The screening and identification of attachment genes is important to exploring the formation mechanism of biofilms at the gene *** is helpful to the development of key culture technologies for aerobic granular sludge(AGS).In this study,genome-wide sequencing and gene editing were employed for the first time to investigate the effects and functions of attachment genes in *** the help of whole-genome analysis,ten attachment genes were screened from thirteen genes,and the efficiency of gene screening was greatly ***,two attachment genes were selected as examples to further confirm the gene functions by constructing gene-knockout recombinant mutants of Stenotrophomonas maltophilia;when the two attachment genes were knocked out,the attachment potential was reduced by 50.67%and 43.93%,*** results provide a new theoretical principle and efficient method for the development of AGS from the perspective of attachment genes.

关键词： Attachment gene Genome-wide sequence Gene-knockout Attachment potential Aerobic granular sludge biofilm

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Microstructure evolution and phase transformation of the mushy zone in a quenchedβ-solidifying TiAl alloy

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Journal of Materials Science & Technology 2024年第2期169卷 28-41页

作者： Fuqiang Zhang Xianfei ding Leming Xu Xin Feng Hai Nan Jianping He Yongfeng Liang Junpin Lin State Key laboratory for Advanced Metals and Materials University of Science and Technology BeijingBeijing 100083China Cast Titanium Alloy r&d Center Beijing Institute of Aeronautical MaterialsBeijing 100095China

This study investigates the phase constitutions and transformations that occur in the mushy zone and in the adjacent phase fields of a directionally solidified Ti-44Al-8Nb-1Cr alloy via quenching *** results indicate that the mushy zone consists of unmeltedβdendrites and interdendritic liquid,whose formation can be attributed to the difference in melting point aroused by local heterogeneity in ***βdendrite is composed of numerous subgrains with various *** quenching,theβdendrite transforms into Widmanstättenαvia a precipitation reaction,owing to the decreasing cooling rate caused by heat transfer from the surrounding ***,after quenching,the interdendritic liquid is transformed intoγ*** the singleβphase field and the lower part of the mushy zone,a massive transformation ofβtoγ***,in theβ+αphase field,bothβandαphases are retained to ambient *** the heating process,the transformation ofα→βgives rise to the formation ofβvariants,which affects the orientation ofβdendrites in the mushy *** growth kinematics of theα→βtransformation was elucidated,revealing the preferential growth directions of111and112forβ***,this study presents an illustration of the formation process of the mushy zone and the microstructural evolution during the heating and quenching process.

关键词： Titanium aluminides Mushy zone Quenching Electron backscattering diffraction Phase transformation

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Thickening progression mechanism of silica fume-oil well cement composite system at high temperatures

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Petroleum Science 2024年第4期21卷 2793-2805页

作者： Hang Zhang Miao-Miao Hu Peng-Peng Li Guo-Qing Liu Qing-Lu Chang Jie Cao Ming Liu Wen-Hua Xu Xiu-Jian Xia Jin-Tang Guo School of Chemical Engineering and Technology Tianjin University Zhejiang Institute of Tianjin University Haihe laboratory of Sustainable Chemical Transformations CNPC Engineering Technology r&d Company Limited

This work studied the thickening progression mechanism of the silica fume-oil well cement composite system at high temperatures(110-180.C) in order to provide a theoretical guidance for the rational application of silica fume in the cementing engineering. results showed that silica fume seldom affected the thickening progression of oil well cement slurry at 110-120.C, but when temperature reached above130.C, it would aggravate the bulging degree of thickening curves and significantly extend the thickening time, meanwhile causing the abnormal “temperature-based thickening time reversal” and“dosage-based thickening time reversal” phenomena in the range of 130-160.C and 170-180.C respectively. At 130-160.C, the thickening time of oil well cement slurry was mainly associated with the generation rate of calcium hydroxide(CH) crystal. The introduced silica fume would be attracted to the cement minerals' surface that were hydrating to produce CH and agglomerate together to form an“adsorptive barrier” to hinder further hydration of the inner cement minerals. This “adsorptive barrier”effect strengthened with the rising temperature which extended the thickening time and caused the occurrence of the “temperature-based thickening time reversal” phenomenon. At 170-180.C, the pozzolanic activity of silica fume significantly enhanced and considerable amount of C-S-H was generated, thus the “temperature-based thickening time reversal” vanished and the “dosage-based thickening time reversal” was presented.

关键词： Silica fume Oil well cement Thickening time reversal Pozzolanic reaction Adsorptive barrier CH and C−S−H

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Friction and wear performance of polyether ether ketone(PEEK)polymers in three lubrication regimes

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Friction 2024年第4期12卷 670-682页

作者： davide MASSOCCHI Nora LECIS Marco LATTUAdA davide SCAGLIA Steven CHATTErTON Paolo PENNACCHI department of Mechanical Engineering Politecnico di MilanoMilan 20156Italy Eni SpA Downstream product R&DLombardia 20097Italy Eurobearings S.r.L. Lombardia 29016Italy

This experimental study investigates the friction and wear of three coatings commonly used in industrial applications,particularly in hydrodynamic *** three materials under investigation were Babbitt,polyether ether ketone(PEEK)reinforced with 15%carbon fibers,and PEEK reinforced with 20%carbon *** first polymer material was extruded,while the other was produced by fused deposition modelling(FdM).The materials were subjected to sliding tests in a pin-on-disc configuration,with a steel ball serving as the counter *** tests were conducted at room temperature,with a load of 10 N and under three different lubrication conditions:dry,grease,and *** linear speed was set at 0.3 m/s for the dry and semi-solid lubrication tests,while for the oil tests,the speed was set at 0.25 m/*** greases used had consistency grades of NGLI 000 and NGLI *** ISO VG 68 circulation oil was used for the oil lubrication ***,thermodynamic analyses were performed under the most severe conditions(i.e.,dry)to investigate the steel-Babbitt and steel-PEEK contact.

关键词： hydrodynamic bearings polyether ether ketone(PEEK)polymers additive manufacturing grease lubrication sliding oil lubrication ball-on-disk tribology

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A creep model for ultra-deep salt rock considering thermal-mechanical damage under triaxial stress conditions

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Journal of rock Mechanics and Geotechnical Engineering 2024年第2期16卷 588-596页

作者： Chao Liang Jianfeng Liu Jianxiong Yang Huining Xu Zhaowei Chen Lina ran College of Water resource and Hydropower Sichuan UniversityChengdu610065China CNPC Key laboratory of Oil and Gas Underground Storage Engineering Langfang065007China CNPC Engineering Technology r&d Company Limited Beijing102206China

To investigate the specific creep behavior of ultra-deep buried salt during oil and gas exploitation,a set of triaxial creep experiments was conducted at elevated temperatures with constant axial pressure and unloading confining pressure *** results show that the salt sample deforms more significantly with the increase of applied temperature and deviatoric *** accelerated creep phase is not occurring until the applied temperature reaches 130℃,and higher temperature is beneficial to the occurrence of accelerated *** describe the specific creep behavior,a novel three-dimensional(3d)creep constitutive model is developed that incorporates the thermal and mechanical variables into mechanical ***,the standard particle swarm optimization(SPSO)method is adopted to fit the experimental data,and the sensibility of key model parameters is analyzed to further illustrate the model *** a result,the model can accurately predict the creep behavior of salt under the coupled thermo-mechanical effect in deep-buried *** on the research results,the creep mechanical behavior of wellbore shrinkage is predicted in deep drilling projects crossing salt layer,which has practical implications for deep rock mechanics problems.

关键词： Creep experiments Creep model Thermal and mechanical damage Fractional derivative

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Cytoplasmic FKBPs are involved in molting and metamorphosis through regulating the nuclear localization of Ecr

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Insect Science 2024年第3期31卷 759-772页

作者： Xian Zhang Qiao-ran Wang Qian Wu Jun Gu Li-Hua Huang Guangdong Provincial Key laboratory of Insect developmental Biology and Applied Technology School of Life SciencesSouth China Normal UniversityGuangzhouChina Guangmeiyuan r&d Center Guangdong Provincial Key Laboratory of Insect Developmental Biology and Applied TechnologySouth China Normal UniversityMeizhouChina

Molting and metamorphosis are important physiological processes in insects that are tightly controlled by ecdysone receptor(Ecr)through the 20-hydroxyecdysone(20E)signaling *** is a steroid nuclear receptor(Sr).Several FK506-binding proteins(FKBPs)have been identified from the mammal Sr complex,and are thought to be involved in the subcellular trafficking of ***,their roles in insects are poorly *** explore whether FKBPs are involved in insect molting or metamorphosis,we injected an FKBP inhibitor(FK506)into a lepidopteran insect,Spodoptera litura,and found that molting was inhibited in 61.11%of the larvae,and that the time for larvae to pupate was significantly extended.A total of 10 FKBP genes were identified from the genome of *** and were clustered into 2 distinct groups,according to their subcellular localization,with FKBP13 and FKBP14 belonging to the endoplasmic reticulum(Er)group and with the other members belonging to the cytoplasmic(Cy)*** the CyFKBPs were significantly upregulated in the prepupal or pupal stages,with the opposite being observed for the Er group ***506 completely blocked the transfer of Ecr to the nucleus under 20E induction,and significantly downregulated the transcriptional expression of many 20E signaling genes.A similar phenomenon was observed after rNA interference of2 CyFKBPs(FKBP45 and FKBP12b),but not for *** together,our data indicate that the cytoplasmic FKBPs,especially FKBP45 and FKBP12b,mediate the nuclear localization of Ecr,thereby regulating the 20E signaling and ultimately affecting molting and metamorphosis in insects.

关键词： Ecr FKBP metamorphosis molting rNAi subcellular localization

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Improving lipid production by rhodotorula glutinis for renewable fuel production based on machine learning

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Frontiers of Chemical Science and Engineering 2024年第5期18卷 23-35页

作者： Lihe Zhang Changwei Zhang Xi Zhao Changliu He Xu Zhang National Energy r&d Center for Biorefinery Beijing University of Chemical TechnologyBeijing 100029China Collage of Life Science and Technology Beijing University of Chemical TechnologyBeijing 100029China Beijing Key laboratory of Bioprocess Beijing University of Chemical TechnologyBeijing 10029China

Microbial lipid fermentation encompasses intricate complex cell growth processes and heavily relies on expert experience for optimal *** modeling of the fermentation process assists researchers in making intelligent decisions,employing logical reasoning and strategic planning to optimize lipid *** this study,the effects of medium components and concen-trations on lipid fermentation were investigated,*** then,leveraging the collated data,a variety of machine learning algorithms were used to model and optimize the lipid fermentation *** models,based on artificial neural networks and support vector machines,achieved r?values all higher than 0.93,ensuring accurate predictions of the fermentation *** linear regression was used to evaluate the respective target parameter,which were affected by the medium components of lipid ***,single and multi-objective optimiza-tion were conducted for lipid fermentation using the genetic *** results demonstrated the maximum biomass of 50.3 g·L^(-1) and maximum lipid concentration of 14.1 g:L^(-1) with the error between the experimental and predicted values less than 5%.The results of the multi-objective optimization reveal the synergistic and competitive relationship between biomass,lipid concentration,and conversion rate,which lay a basis for in-depth optimization and amplification.

关键词： microbial lipid machine learning artificial neural network support vector machine genetic algorithm

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dynamic Location Method for Shallow Ocean Bottom Nodes Using the Levenberg-Marquart Algorithm

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Journal of Ocean University of China 2024年第4期23卷 953-960页

作者： TONG Siyou LI Junjie XU Xiugang FANG Yunfen WANG Zhongcheng Key laboratory of Submarine Geosciences and Prospecting Techniques MOEOcean University of ChinaQingdao 266100China laboratory for Marine Mineral resources Qingdao Marine Science and Technology CenterQingdao 266237China r&d Center of BGP CNPCZhuozhou 072751China Insitute of Shengli Oilfield SINOPECDongying 257022China

Ocean bottom node(OBN)data acquisition is the main development direction of marine seismic exploration;it is widely promoted,especially in shallow sea ***,the OBN receivers may move several times because they are easily affected by tides,currents,and other factors in the shallow sea environment during long-term *** uncorrected,then the imaging quality of subsequent processing will be *** conventional secondary positioning does not consider the case of multiple movements of the receivers,and the accuracy of secondary positioning is *** first arrival wave of OBN seismic data in shallow ocean mainly comprises refracted *** this study,a nonlinear model is established in accordance with the propagation mechanism of a refracted wave and its relationship with the time interval curve to realize the accurate location of multiple receiver *** addition,the Levenberg-Marquart algorithm is used to reduce the influence of the first arrival pickup error and to automatically detect the receiver movements,identifying the accurate dynamic relocation of the *** simulation and field data show that the proposed method can realize the dynamic location of multiple receiver movements,thereby improving the accuracy of seismic imaging and achieving high practical value.

关键词： OBN dynamic location method Levenberg-Marquart algorithm seismic exploration of shallow sea

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