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Synthesis,Urease Inhibition and Molecular Modelling Studies of Novel Derivatives of the Naturally Occurring b-Amyrenone

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Natural Products and Bioprospecting 2019年第1期9卷 49-59页

作者： Jean J.K.Bankeu Hira Sattar Yannick S.F.Fongang Syeda W.Muhammadi Conrad V.Simoben Fidele Ntie-Kang Guy R.T.Feuya Marthe A.T.Tchuenmogne Mehreen Lateef Bruno N.Lenta Muhammad S.Ali Augustin S.Ngouela Department of Chemistry Faculty of ScienceThe University of BamendaP.O.Box 39BambiliCameroon International center for Chemical and Biological Sciences University of KarachiKarachi 75270Pakistan Department of Chemistry Higher Teacher Training CollegeUniversity of MarouaP.O.Box 55MarouaCameroon Department of Pharmaceutical Chemistry Martin-Luther University of Halle-WittenbergWolfgang-Langenbeck-Str.406120 Halle(Saale)Germany Department of Chemistry Faculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Department of Chemistry Faculty of ScienceScientific and Technical University of MasukuBox 943FrancevilleGabon Department of Chemistry Faculty of ScienceUniversity of Yaounde´IP.O.Box 812Yaounde´Cameroon Multi-Disciplinary research Laboratory(MDRL) Bahria University Medical and Dental CollegeBahria UniversityKarachiPakistan Department of Chemistry Higher Teacher Training CollegeUniversity of Yaounde´IP.O.Box 47Yaounde´Cameroon

Urease enzyme(UE)has been reported to be a potent virulence factor for Helicobacter pylori(HP)bacteria indicated to be responsible for various gastrointestinal ***,the spread of HP,currently regarded by the World Health Organization as a class 1 carcinogen,could be better controlled by targeting *** is in this line that we have synthesized three new derivatives(2–4)of the naturally occurring olean-12-en-3-one(1),which was previously isolated from the figs of Ficus vallis-choudae Delile(Moraceae).Among the synthesized compounds,3 and 4 contain an indole *** structures were unambiguously assigned by spectroscopic and spectrometric techniques(1D-NMR,2D-NMR and MS).The starting material and the synthesized compounds were screened for UE inhibition activity,and showed significant activities with IC50 values ranging from 14.5 to 24.6 lM,with compound(1)being the most potent as compared to the positive control thiourea(IC50=21.6 lM).Amongst the synthetic derivatives,compound 4 was the most potent(IC50-=17.9 lM),while the others showed activities close to that of the *** addition,molecular docking study of target compounds 2–4 was performed in an attempt to explore their binding mode for the design of more potent UE inhibitors.

关键词： Helicobacter pylori Urease inhibition Docking Olean-12-en-3-one derivatives

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ROLE OF SEA SURFACE TEMPERATURE IN MODULATING LIFE CYCLE OF TROPICAL CYCLONES OVER BAY OF BENGAL

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Tropical Cyclone research and Review 2019年第2期8卷 74-89页

作者： Shyama Mohanty Raghu Nadimpalli Krishna K Osuri Sujata Pattanayak U C Mohanty and Sourav Sil School of Earth Ocean and Climate Sciences Indian Institute of Technology BhubaneswarOdishaIndia Department of Earth and Atmospheric Sciences National Institute of Technology RourkelaOdishaIndia National center for Medium Range Weather Forecasting NoidaUttar PradeshIndia

Sea surface temperature(SST) varies significantly in the presence of tropical cyclones(TCs). Using fixed SST throughout the integration of high resolution TC models is general practice in research and operational endeavor over the North Indian Ocean. The present study is to assess the impact of updating realistic SST in TC lifetime on track, intensity and rainfall of TCs. The Hurricane Weather research Forecast(HWRF) model of single domain with 9 km resolution is used. A total of 31 forecast cases are considered from 6 TCs during 2007-16 with unique track and intensity characteristics. A set of two numerical experiments are done without(CNTL) and with 6-hourly SST update(SST) in TC *** track and intensity errors show that there is an improvement of 3–41% in track during 12–120 h forecast length for SST run. The SST runs improve landfall position and time prediction by 20% and 33% respectively. The cross track error of SST run is comparable(44 km) with average errors available for this basin(34 km);and along track errors are improved by 60% as compared to CNTL as well as average errors of the basin. The model is biased to overestimate a weaker TC and underestimate a stronger TC, however, the bias is reduced in SST run by 5–51%. The analyses of wind, enthalpy flux and warm core structures provide insight for realistic intensity prediction of SST run unlike CNTL. Rainfall intensity and radial distribution is also improved in SST run. Thus, this study highlights the significance of ocean coupling with TC models to advance forecast guidance.

关键词： tropical cyclone HWRF SST Bay of Bengal

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Polyplex interaction strength as a driver of potency during cancer immunotherapy

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Nano research 2018年第10期11卷 5642-5656页

作者： Shannon d. Tsai James I. Andorko Xiangbin Zeng Joshua M. Gammon Christopher M. dewell Fischell Department of Bioengineering University of Marylond 8278 Paint Branch Drive College Park MD 20742 USA Robert E. Fischell Institute for Biomedicol Devices University of Maryland 8278 Paint Branch Drive College Park MD 20742 USA United States Department of Veterans Affairs Maryland VA Health Care System 10 North Greene Street Baltimore MD 21201 USA Deportment of Microbiology and Immunology University of Maryland Medical School 685 West Baltimore Street Baltimore MD 21201 USA Marlene and Stewart Greenebaum Cancer center 22 South Greene Street Baltimore MD 21201 USA

Many experimental cancer vaccines are exploring toll-like receptor agonists （TLRas） such as CpG, a DNA motif that agonizes toll-like receptor 9 （TLR9）, to trigger immune responses that are potent and molecularly-specific. The ability to tune the immune response is especially important in the immunosuppressive microenvironments of tumors. Because TLR9 is located intracellularly, CpG must be internalized by immune cells for functionality. Polyplexes can be self- assembled through electrostatics using DNA （anionic） condensed by a positively charged carrier. These structures improve cell delivery and have been widely explored for gene therapy. In contrast, here we use cationic poly （^-amino esters）（PBAEs） to assemble polyplexes from CpG as an adjuvant to target and improve immune stimulation in cells and mouse models. Polyplexes were formed over a range of PBAE：CpG ratios, resulting in a library of complexes with increasingly positive charge and stronger binding as PBAE：CpG ratio increased. Although higher PBAE：CpG ratios exhibited improved CpG uptake, lower ratios of PBAE：CpG--which condensed CpG more weakly, activated DCs and tumorspecific T cells more effectively. In a mouse melanoma model, polyplexes with lower binding affinities improved survival more effectively compared with higher binding affinities. These data demonstrate that altering the polyplex interaction strength impacts accessibility of CpG to TLRs in immune cells. Thus, physiochemical properties, particularly the interplay between charge, uptake, and affinity, play a key role in determining the nature and efficacy of the immune response generated. This insight identifies new design considerations that must be balanced for engineering effective immunotherapies and vaccines.

关键词： cancer immunotherapy nanoparticle vaccine polyplex

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U-Net-based deep learning for tracking and quantitative analysis of intracellular vesicles in time-lapse microscopy images

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Journal of Innovative Optical Health Sciences 2022年第5期15卷 63-73页

作者： Zhichao Liu Heng Zhang Luhong Jin Jincheng Chen Alexander Nedzved Sergey Ablameyko Qing Ma Jiahui Yu Yingke Xu Department of Biomedical Engineering MOE Key Laboratory of Biomedical Engineering State Key Laboratory of Modern Optical Instrumentation Zhejiang Provincial Key Laboratory of Cardio-Cerebral Vascular Detection Technology and Medicinal Effectiveness Appraisal Zhejiang University Hangzhou 310027P.R.China Alibaba-Zhejiang University Joint research center of Future Digital Healthcare Hangzhou 310027P.R.China National Academy of Sciences United Institute of Informatics Problems Belarusian State University Minsk 220012Republic of Belarus§Hangzhou Dowell Photonics Measurement Company Limited Hangzhou 310000P.R.China Binjiang Institute of Zhejiang University Hangzhou 310053 P.R.China Department of Endocrinology Children's Hospital of Zhejiang University School of Medicine National Clinical research center for Children's Health Hangzhou 310051 China

Fluorescence microscopy has become an essential tool for biologists,to visualize the dynamics of intracellular structures with specific *** measuring the dynamics of moving objects inside the cell is pivotal for understanding of the underlying regulatory ***-containing vesicles are involved in various biological processes such as material transportation,organelle interaction,and hormonal regulation,whose dynamic characteristics are signi¯cant to disease diagnosis and drug *** some algorithms have been developed for vesicle tracking,most of them have limited performance when dealing with images with low resolution,poor signal-to-noise ratio(SNR)and complicated ***,we proposed a novel deep learning-based method for intracellular vesicle *** trained the U-Net for vesicle localization and motion classification,with demonstrates great performance in both simulated datasets and real biological *** combination with fan-shaped tracker(FsT)we have previously developed,this hybrid new algorithm significantly improved the performance of particle tracking with the function of subsequently automated vesicle motion ***,its performance was further demonstrated in analyzing with vesicle dynamics in different temperature,which achieved reasonable ***,we anticipate that this novel method would have vast applications in analyzing the vesicle dynamics in living cells.

关键词： Deep learning image processing vesicle tracking fluorescence microscopy U-Net.

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Inpatient bed allocation policy under uncertain capacity

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Journal of Management Science and Engineering 2019年第4期4卷 228-251页

作者： Xing Liu Youhua Chen Li Luo Ting Zhu Wenwu Shen TAIWO Enayon Sunday Noah’s Ark Laboratory Huawei TechnologiesShenzhen250012China Business School City University of Hong KongHong KongChina Business School Sichuan UniversitySichuan610064China West China Biomedical Big Data center West China Hospital/West China School of MedicineSichuan UniversitySichaun610041China Outpatient Department West China HospitalSichuan UniversitySichuan610041China

This paper concerns the problem of inpatient bed allocation for two classes of patients(scheduled and non-scheduled)when there is uncertainty about daily available *** the afternoon of each day,patients from the scheduled class,also called backlogged elective admissions,are selected from a waiting list,for the admission on the next *** non-scheduled class,also called emergent admissions,are new requests that arise randomly each day with emergent *** capacity of available beds for a medical specialty to provide hospitalization services is uncertain when backlogged elective pa-tients are *** too many of elective patients may result in exceeding a day’s capacity,which can potentially necessitate"overflowing"or"postponing"some emergent requests that should be performed as soon as ***,the problem faced by the medical specialty facility at the decision-making point of each day is how many of the backlogged elective patients can be *** formulate this problem as a Markov decision process(MDP)and study the structural properties of the model to characterize the nature of the optimal *** propose easy-to-implement policies(the fixed quota policy and the best fixed quota policy),which perform well under fitted *** reporting numerical analyses using real data from a Chinese public hospital,we finally compare the improvements that our proposed solutions could bring to the hospital with the existing practices under several different cost structures.

关键词： Bed allocation Markov decision process Emergency reservation Healthcare management

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Specific features of SH-waves propagation in structures with prestressed inhomogeneous coating made of piezoceramics based on LiNbO_(3)

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Journal of Advanced Dielectrics 2021年第5期11卷 15-24页

作者： T.I.Belyankova E.I.Vorovichy V.V.Kalinchuk O.M.Tukodovay Department of Mechanics Mathematics and Nanotechnology Southern Scientific center of RAS 41 Chekhov Avenue 344006 Rostov-on-DonRussia Department of Applied Mathematics Don State Technical University 1 Gagarin Square 344010 Rostov-on-DonRussia

Within the framework of the linearized theory of electroelastic wave propagation,a model of a piezoelectric structure with a prestressed functionally graded coating made of piezoceramics of a trigonal system with a symmetry class of 3m is *** ferroelectric LiNbO_(3) is used as the main material of the *** initial deformed state of the coating material is homogeneous,induced by the action of initial mechanical stresses and an external electrostatic field,the properties of the coating continuously change in *** the example of the problem of the propagation of SH-waves from a remote source for structures with an inhomogeneous prestressed coating in the case of an electrically free and short-circuited surface,the influence of the nature and localization of the inhomogeneity of the coating on the features of SAW propagation is *** separate and combined effects of initial actions on changes in the physical properties of the structure,the transformation of the surface wave field,and the change in the SAW velocities in a wide frequency range is *** results obtained in this work are useful for understanding the dynamic processes in prestressed piezoelectric structures,in the optimization and design of new structures and devices on SAW with high performance characteristics.

关键词： Piezoelectric structure lithium niobate(LiNbO_(3)) functionally graded piezoelectric material(FGPM) surface acoustic waves(SAW) Bluestein-Gulyaev wave(WBG) initial deformed state(IDS)

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Intelligent Energy Consumption For Smart Homes Using Fused Machine-Learning Technique

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Computers, materials & Continua 2023年第1期74卷 2261-2278页

作者： Hanadi AlZaabi Khaled Shaalan Taher M.Ghazal Muhammad A.Khan Sagheer Abbas Beenu Mago Mohsen A.A.Tomh Munir Ahmad Faculty of Engineering and IT The British University in DubaiUnited Arab Emirates center for Cyber Security Faculty of Information Science and TechnologyUniversity Kebangsaan Malaysia(UKM)Bangi43600SelangorMalaysia School of Information Technology Skyline University CollegeUniversity City SharjahSharjah1797United Arab Emirates Riphah School of Computing&Innovation Faculty of ComputingRiphah International University Lahore CampusLahore54000Pakistan Pattern Recognition and Machine Learning Lab. Department of SoftwareGachon UniversitySeongnamGyeonggido13120Korea Faculty of Computer Science NCBA&ELahore54660Pakistan

Energy is essential to practically all exercises and is imperative for the development of personal ***,valuable energy has been in great demand for many years,especially for using smart homes and structures,as individuals quickly improve their way of life depending on current ***,there is a shortage of energy,as the energy required is higher than that *** new plans are being designed to meet the consumer’s energy *** many regions,energy utilization in the housing area is 30%–40%.The growth of smart homes has raised the requirement for intelligence in applications such as asset management,energy-efficient automation,security,and healthcare monitoring to learn about residents’actions and forecast their future *** overcome the challenges of energy consumption optimization,in this study,we apply an energy management *** fusion has recently attracted much energy efficiency in buildings,where numerous types of information are *** proposed research developed a data fusion model to predict energy consumption for accuracy and miss *** results of the proposed approach are compared with those of the previously published techniques and found that the prediction accuracy of the proposed method is 92%,which is higher than the previously published approaches.

关键词： Energy consumption intelligent machine learning technique smart homes prediction

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Diversity, novelty, antimicrobial activity, and new antibiotics of cultivable endophytic actinobacteria isolated from psammophytes collected from Taklamakan Desert

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Journal of Pharmaceutical Analysis 2021年第2期11卷 241-250页

作者： Ting Wang Feina Li Qinpei Lu Gang Wu Zhongke Jiang Shaowei Liu Xugela Habden Elizaveta A.Razumova Ilya A.Osterman Petr V.Sergiev Olga A.Dontsova Xinxin Hu Xuefu You Chenghang Sun Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing100050China Beijing Key Laboratory of Antimicrobial Agents Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing100050China College of Life Science Xinjiang Normal UniversityUrumchi830054China Lomonosov Moscow State University Moscow119992Russia center of Life Sciences Skolkovo Institute of Science and TechnologyMoscow143025Russia Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of SciencesMoscow119992Russia

Three hundred and twenty endophytic actinobacterial strains were isolated from psammophytes collected from Taklamakan Desert and identified. Among them, three strains already had been identified as new species of two genera and sixteen isolates showed relatively low 16 S rRNA similarities new *** the strategy of integrating genetics-based discovery program and MS/MS-based molecular networking, two new streptogramin-type antibiotics, i.e., acetyl-griseoviridin and desulphurizing griseoviridin, along with known griseoviridin, were isolated from the culture broth of strain 8P21H-1. Their chemical structures were determined by HR-MS, and 1D and 2D NMR. Desulphurizing griseoviridin and griseoviridin exhibited antibacterial activities by inhibiting translation.

关键词： Taklamakan desert Endophytic actinobacteria Novelty Diversity Streptogramin-type antibiotic

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自上而下和自下而上相结合提高大规模生态修复规划的实用性和效率——来自社会生态系统的启示（英文）

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Engineering 2023年第12期 50-58页

作者： Zhaowei Ding Hua Zheng Jun Wang Patrick O'Connor Cong Li Xiaodong Chen Ruonan Li Zhiyun Ouyang State Key Laboratory of Urban and Regional Ecology Research Center for Eco-Environmental Sciences Chinese Academy of Sciences College of Resources and Environment University of Chinese Academy of Sciences Key Laboratory of Land Consolidation and Rehabilitation Land Consolidation and Rehabilitation Center Ministry of Natural Resources Centre for Global Food and Resources University of Adelaide School of Economics and Finance Xi’an Jiaotong University

Ecological restoration policies and their implementation are influenced by ecological and socioeconomic drivers. Top-down approach-based spatial planning, emphasizing hierarchical control within government structures, and without a comprehensive consideration of social–ecological interactions may result in implementation failure and low efficiency. Although many researchers have indicated the necessity to engage social–ecological interactions between stakeholders in effective planning processes,socioeconomic drivers of ecological restoration on a large scale are difficult to quantify because of data scarcity and knowledge limitations. Here, we established a new ecological restoration planning approach linking a social–ecological system framework to large-scale ecological restoration planning. The new spatial planning approach integrates bottom-up approaches targeting stakeholder interests and provides social considerations for stakeholder behavior analysis. Based on this approach, a meta-analysis is introduced to recognize key socioeconomic and social–ecological factors influencing large-scale ecological restoration implementation, and a stochastic model is constructed to analyze the impact of socioeconomic drivers on the behavior of authorities and participants on a large scale. We used the Yangtze River Basin-based Conversion of Cropland to Forest Program(CCFP), one of the largest payments for ecosystem service programs worldwide, to quantify the socioeconomic impacts of large-scale ecological restoration programs. Current CCFP planning without socioeconomic considerations failed to achieve large-scale program goals and showed low investment efficiency, with 19.71% of the implemented area reconverting to cropland after contract expiry. In contrast, spatial matching between planned and actual restoration increased from 61.55% to 81.86% when socioeconomic drivers were included. In addition, compared to that with the current CCFP implementation, the cost effectivenes

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Polymeric coating lubricates nanocontainers to escape macrophage uptake for bioreceptor recognition

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Bioactive materials 2022年第8期7卷 120-133页

作者： Yulong Sun Yanxin Han Yannong Dou Xinqi Gong Haimang Wang Xiaoyu Yu Qiang Wang Yixin Wang Yue Dai Fangfu Ye Wei Jin Hongyu Zhang State Key Laboratory of Tribology Department of Mechanical EngineeringTsinghua UniversityBeijing100084China Department of Cardiovascular Medicine Heart Failure CenterRuijin HospitalShanghai Jiao Tong University School of MedicineShanghai200025China Department of Pharmacology of Chinese Materia Medica China Pharmaceutical UniversityNanjing210009China Institute for Mathematical Sciences Renmin University of ChinaBeijing100872China Lab of Soft Matter and Biological Physics Institute of PhysicsChinese Academy of SciencesBeijing100190China Institute of Wenzhou University of Chinese Academy of SciencesWenzhou325001China

Accurate drug delivery to the lesion has been deliberated for several decades,but one important phenomenon is usually neglected that the immune system can prevent smooth transportation of *** injection would reduce first-pass effect,macrophages in the blood can still recognize and phagocytose *** we show that a lubricated nanocontainer,which is prepared based on polyelectrolytes and mesoporous silica nanoparticles,can accurately target muscarinic bioreceptor while escaping from the identification of *** in vitro and in vivo studies,this nanocontainer,combining both immune escape and bioreceptor targeting,has greatly improved the drug ***,this nanocontainer shows good biocompatibility,and the targeted heart tissues and other important metabolic organs,such as liver and kidney,keep physiological structures and functions without the detection of side ***,the mechanism of immune escape for the developed nanocontainer has been investigated by lubrication test and molecular *** anticipate that our study will establish a new perspective on the achievement of immune escape-based targeted drug delivery,which can provide a fundamental approach for the design of related biomaterials.

关键词： Mesoporous silica nanoparticles Polyelectrolytes Lubrication Macrophage escape Drug delivery

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