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Insect Science 2024年第3期31卷 792-802页

作者： Yuzhe Du Shane Scheibener Yucheng Zhu Maribel Portilla Mingling Zhang USDA-ARS Southern Insect Management Research UnitStonevilleUSA USDA-ARS Pollinator Health in Southern Crop Ecosystem Research UnitStonevilleUSA

Due to rapidly developed resistance,pest management relies less on pyrethroids to control economically damaging infestations of the tarnished plant bug(TPB),Lygus lineolaris(Palisot de Beauvois)in cotton fields of ***,pyrethroid resistance remains prevalent in TPB *** study assessed the resistance levels in adult TPB to six common pyrethroids and *** TBPs were collected from wild host plants in late October after harvest in the Mississippi Delta region of the united *** on LCso values,the field-resistant TPBs displayed higher resistance to permethrin,esfenvalerate,and bifenthrin(approximately 30 fold)and moderate resistance toα-cyhalothrin,β-cyfluthrin,5-cypermethrin,and acephate(approximately 15 fold).Further investigations showed that the inhibitors of three detoxification enzyme,triphenyl phosphate(TPP),diethyl maleate(DEM),and piperonyl butoxide(PBO)had synergistic effects on permethrin,γ-cyhalothrin,and bifenthrin in resistant ***,elevated esterase,GST,and P450 activities were significantly expressed in fieldresistant ***,GST and esterase were reduced after 48 h exposure to certain pyrethroids at LCso *** synergistic and biochemical assays consistently indicated that P450 and esterase were involved in pyrethroid detoxification in *** study provides valuable information for the continued use of pyrethroids and acephate in controlling TPBs in cotton fields in the Mississippi Delta region of the united States.

关键词： cytochrome P450-monooxygenases(P450) detoxification enzyme activities esterase Lygus lineolaris pyrethroids and organophosphate resistance tarnished plant bug

Characterisation of the granular dynamics at the interface between a pipe and a granular flow in a rotating drum

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Particuology 2024年第3期86卷 117-125页

作者： Francois Rioual Paule Emmanuelle Eva Gbehe research unit FRISE National Research Institute for Agriculture Food and the Environment1 Rue Pierre Gilles De Gennes92160AntonyFrance

A new mobile bed heat exchanger is presented in this work which is composed of a flowing granular material in a rotating drum and a cylindrical pipe with potential interest in different energy applications as cooling,heating or heat recovery *** optimal design of the device requires a characterisation of the phenomena involved at the interface between the granular flow and the *** process is modelled by the discrete element method and a global classification of the flow patterns around the pipe is presented with respect to the three main control parameters of the problem:the Froude number,the diameter ratio and the relative filling height of the *** second part is devoted to the characterisation of the structure of the flow at the interface(velocity field,density field)in particular in a so-called Biflow regime where granular motion occurs above as well as below the pipe which is favourable to transfer by convection.A typical behavior at the interface with the pipe consists of a zone I with high velocities of particles at the top of the pipe,a second zone with quasistatic particles or low velocity particles at the front and at the bottom of the pipe and a last zone ll of depletion of particles at the back of the *** Froude number has a limited effect on the features of this structure on the first layer in the range of Froude numbers considered whereas the relative height is a more determinant parameter to control the relative magnitude of velocities in zone I and zone Il as well as the extent of the depletion *** first hydrodynamical characterisation can shed light on the dynamical regimes with improved transfer between the particles and the pipe boundary.

关键词： Granular flow Transfer Heat exchange Mobile bed Boundary condition

Design and optimization of piperidinesubstituted thiophene[3,2-d]pyrimidine-based HIV-1 NNRTIs with improved drug resistance and pharmacokinetic profiles

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Acta Pharmaceutica Sinica B 2024年第7期14卷 3110-3124页

作者： Yanying Sun Zhenzhen Zhou Zhongling Shi Fabao Zhao Minghui Xie Zongji Zhuo Erik De Clercq Christophe Pannecouqueb Dongwei Kang Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesShandong UniversityJinan 250012China Rega Institute for Medical research Laboratory of Virology and ChemotherapyK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative research Center for Innovative antiviral Drugs of Shandong Province Jinan 250012China

HIV-1 reverse transcriptase(RT)has received great attention as an attractive therapeutic target for acquired immune deficiency syndrome(AIDS),but the inevitable drug resistance and side effects have always been major challenges faced by non-nucleoside reverse transcriptase inhibitors(NNRTIs).This work aimed to identify novel chemotypes of anti-HIV-1 agents with improved drugresistance profiles,reduced toxicity,and excellent druggability.A series of diarylpyrimidine(DAPY)derivatives were prepared via structural modifications of the leads K-5a2 and *** them,15a with dimethylphosphine oxide moiety showed the most prominent antiviral potency against all of the tested viral panel,being 1.6-fold(WT,EC_(50) Z 1.75 nmol/L),3.0-fold(L100I,EC_(50) Z 2.84 nmol/L),2.4-fold(K103N,EC_(50) Z 1.27 nmol/L),3.3-fold(Y181C,EC50 Z 5.38 nmol/L),2.9-fold(Y188L,EC_(50) Z 7.96 nmol/L),2.5-fold(E138K,EC_(50) Z 4.28 nmol/L),4.8-fold(F227L/V106A,EC_(50) Z 3.76 nmol/L)and 5.3-fold(RES056,EC_(50) Z 15.8 nmol/L)more effective than that of the marketed drug *** docking results illustrated the detailed interactions formed by compound 15a and WT,F227L/V106A,and RES056 ***,15a-HCl carried outstanding pharmacokinetic(t1/2 Z 1.32 h,F Z 40.8%)and safety profiles(LD_(50)>2000 mg/kg),which demonstrated that 15a HCl is a potential anti-HIV-1 drug candidate.

关键词： HIV-1 NNRTIs NNIBP Structural alert Anti-HIV-1 drug candidate

Rhodium-catalyzed enantioselective in situ C(sp^(3))-H heteroarylation by a desymmetrization approach

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Chinese Chemical Letters 2024年第10期35卷 218-222页

作者： Yujia Shi Yan Qiao Pengfei Xie Miaomiao Tian Xingwei Li Junbiao Chang Bingxian Liu State Key Laboratory of antiviral Drugs NMPA Key Laboratory for Research and Evaluation of Innovative DrugSchool of Chemistry and Chemical EngineeringHenan Normal UniversityPingyuan LaboratoryXinxiang 453007China Department of Pathophysiology School of Basic Medical SciencesZhengzhou UniversityZhengzhou 450001China

A rhodium-catalyzed desymmetrization reaction for enantioselective methyl C-H arylation is achieved by utilizing an in situ arylating reagent via nucleophilic cyclization of o-aminoaryl *** reaction results in chiral indoles containing all-carbon quaternary stereocenters under atmospheric conditions,with a wide range of substrates exhibiting good enantioselectivity(44 examples).Mechnism and DFT studies show that the stereocontrol is reasonably achieved through the collaborative control of a large silicon substituted chiral ligand and C-H···π,LP···πinteractions between aryl rings of the carboxylate group and the *** experiments demonstrate that Rh-aryl bond formation via in situ nucleophilic cyclization is more critical for reaction efficiency than via C-H activation of the nucleophilic cyclization byproduct.

关键词： Heteroarylation C(sp^(3))-H activation Enantioselective Desymmetrization πInteractions

Structure-based design and optimization lead to the identification of novel dihydrothiopyrano[3,2-d]pyrimidine derivatives as potent HIV-1 inhibitors against drug-resistant variants

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Acta Pharmaceutica Sinica B 2024年第3期14卷 1257-1282页

作者： Zhao Wang Heng Zhang Zhen Gao Zihao Sang Erik De Clercq Christophe Pannecouque Dongwei Kang Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJinan 250012China Rega Institute for Medical research Laboratory of Virology and ChemotherapyK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative research Center for Innovative antiviral Drugs of Shandong Province Jinan 250012China Suzhou research Institute Shandong UniversitySuzhou 215123China

With our continuous endeavors in seeking potent anti-HIV-1 agents,we reported here the discovery,biological characterization,and druggability evaluation of a class of nonnucleoside reverse transcriptase *** fully explore the chemical space of the NNRTI-binding pocket,novel series of dihydrothiopyrano[3,2-d]pyrimidines were developed by employing the structure-based design *** of the derivatives were endowed with prominent antiviral activities against HIV-1 wild-type and resistant strains at nanomolar *** them,compound 23h featuring the aminopiperidine moiety was identified as the most potent inhibitor,with EC50values ranging from 3.43 to 21.4 nmol/***,for the challenging double-mutants F227L+V106A and K103N+Y181C,23h exhibited 2.3-to 14.5-fold more potent activity than the first-line drugs efavirenz and ***,the resistance profiles of 23h achieved remarkable improvement compared to efavirenz and *** binding target of 23h was further confirmed to be HIV-1 reverse *** modeling studies were also performed to elucidate the biological evaluation results and give guidance for the optimization ***,no apparent inhibition of the major CYP450 enzymes and hERG channel was observed for *** importantly,23h was characterized by good pharmacokinetic properties and excellent safety in ***,23h holds great promise as a potential candidate for its effective antiviral efficacy and favorable drug-like profiles.

关键词： HIV-1 Reverse transcriptase Dihydrothiopyrano[3,2-d]pyrimidine antiviral agent

What is the effect of Tribulus terrestris on testicular morphology and sperm production?An experimental study in the rat model

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Asian Journal of Andrology 2024年第1期26卷 67-70页

作者： Marcello Henrique Araujo Da Silva Gabriela Faria Buys-Goncalves Joao Henrique Duque Reis Estrada Francisco Jose Barcellos Sampaio Diogo Benchimol de Souza Urogenital research unit Rio de Janeiro State UniversityRio de Janeiro 20551-030RJBrazil

The objective of this study was to investigate whether treatment with Tribulus terrestris(Tt)has any impact on the testicular morphology and function in a rodent *** male rats were divided into a control group and a group receiving 100 mg kg^(-1) body weight of Tt *** 4o days of experiment,the animals were submitted to euthanasia;epididymal tail spermatozoa were collected;and spermatozoa concentration,motility,and viability were *** addition,testicles were collected and processed for histomorphometrical *** were compared using the Student's t-test and considered significant when P<*** concentration,motility,and viability showed no difference between the ***,testicular weight and volume,seminiferous tubule diameter,tunica propria surface density,seminiferous epithelium surface density,and intertubular compartment surface density were statistically similar between the ***,seminiferous epithelium height and tubular lumen surface density were augmented in animals treated with *** with Tt does not cause a major impact on testicular morphology,promoting only subtle *** difference on spermatozoa parameters was observed.

关键词： morphometry testicle Tribulus terrestris

Evaluation of the efficiency of urban solid waste management in Brazil by data envelopment analysis and possible variables of influence

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Waste Disposal and Sustainable Energy 2024年第2期6卷 283-295页

作者： Isabel das Merces Costa Marta Ferreira Dias Margarita Robaina GOvCOPP-research unit on Governance Competitiveness and Public Policies and Analyst of UniversidadeEstadual de Feira de SantanaUniversidade de AveiroAveiroPortugal GOvCOPP-research unit on Governance Competitiveness and Public PoliciesDEGEIT-Department of EconomicsManagementIndustrial Engineering and TourismUniversidade de AveiroAveiroPortugal

This article has the general objective of estimating the efficiency of urban solid waste management in 940 Brazilian munici-palities through Data Envelopment Analysis(DEA)technique and has specific objectives:(i)to estimate efficiency scores;(ii)to compare the performance between different groups of municipalities;and(ii)to analyze the profile of efficient munici-palities from the perspective of the guidelines of Law 12,305/2010 and socio-economic and environmental *** technique used was DEA with output-oriented and variable scale to return *** results showed higher efficiency scores in the municipalities with populations above 500,000 *** score variation ranged from 0.5(municipalities with populations<10,000 inhabitants)to 0.9(municipalities with more than 500,000 inhabitants).Of the sample set,only 12.34%of the municipalities were considered efficient,and when analyzing the efficient group,it was found that adherence to legislation was not a major factor in achieving efficiency.

关键词： Urban solid waste management Data envelopment analysis Efficiency Brazil Municipalities

Catalytic Effect of Transition Metal Complexes of Triaminoguanidine on the Thermolysis of Energetic NC/DEGDN Composite

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火炸药学报 2024年第3期47卷 209-219,I0003页

作者： Mohammed Dourari Ahmed Fouzi Tarchoun Djalal Trache Amir Abdelaziz Roufaida Tiliouine Tessnim Barkat Weiqiang Pang Energetic Materials Laboratory(EMLab) Teaching and Research Unit of Energetic ProcessesEcole Militaire PolytechniqueBP 17Bordj El-Bahri16046AlgiersAlgeria Xi′an Modern Chemistry research Institute Xi′an 710065China

The transition metal complexes of triaminoguanidine(TAG-M,where M=Cobalt(Co)or Iron(Fe))have been *** catalytic effect of these complexes on the thermolysis of energetic composite based on nitrocellulose and diethylene glycol dinitrate,has been *** characterization of the resulting energetic composites was carried out using scanning electron microscopy(SEM),X-ray diffraction(XRD),Fourier transform infrared spectroscopy(FTIR),and differential scanning calorimetry(DSC).Isoconversional kinetic analysis was performed to determine the Arrhenius parameters associated with the thermolysis of the elaborated energetic *** is found that TAG-M complexes have strong catalytic effect on the thermo-kinetic decomposition of NC/DEGDN by decreasing the apparent activation energy and significantly increased the total heat *** models that govern the decomposition processes are also studied,and it is revealed that different reaction processes are accomplished by introduction metal complexes of ***,this study serves as a valuable reference for future research focused on the investigation of catalytic combustion features of solid propellants.

关键词： triaminoguanidine transition metal complexes nitrocellulose diethylene glycol dinitrate catalytic effect

Improving the structural efficiency of textured threedimensional concrete printing wall by architectural design

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Frontiers of Structural and Civil Engineering 2024年第5期18卷 699-715页

作者： Wannapol SADAKORN Santirak PRASERTSUK Lapyote PRASITTISOPIN Architectural Technology research unit Department of ArchitectureFaculty of ArchitectureChulalongkorn UniversityBangkok 10330Thailand Faculty of Architecture and Planning Thammasat UniversityPathumthani 12121Thailand

Three-dimensional concrete printing(3DCP)technology begins to be adopted into construction application *** studies have focused on producing a higher concrete quality and offering a user-friendly construction ***,the 3DCP construction cost is unlikely to be lower than that of conventional construction,which is especially important for projects where the cost is *** broaden the 3DCP construction applications,reduction of the quantity of 3DCP material usage is *** work aims to perform structural analysis of several patterns of geometric textured 3DCP shell wall structures.21 different cantilevered textured patterns of 3DCP shell wall structures were architecturally designed and then subjected to structural analysis by a finite element method(FEM).The results indicated that by designing appropriate patterns,the structural performance to weight ratio could be improved up to 300%.The study therefore offers an innovative design process for constructing 3DCP housing and suggests preconstruction analysis methods for 3DCP shell wall structures.

关键词： 3D printing concrete architectural design shell wall finite element method

Approaching the Sarcopenic Patient with Nonalcoholic Steatohepatitis-related Cirrhosis

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Journal of Clinical and Translational Hepatology 2024年第3期12卷 278-286页

作者： Paolo Gallo Valentina Flagiello Andrea Falcomatà Giulia Di Pasquale Giorgio D’Avanzo Francesca Terracciani Antonio Picardi Umberto Vespasiani-Gentilucci Operative research unit of Clinical Medicine and Hepatology Fondazione Policlinico Universitario Campus Bio-MedicoVia Alvaro del PortilloRomaItaly research unit of Hepatology Department of Medicine and SurgeryUniversitàCampus Bio-Medico di RomaVia Alvaro del PortilloRomaItaly

Sarcopenia is a well-known complication of chronic liver disease(CLD),and it is almost always observed in patients with cirrhosis,at least in those with decompensated *** nonalcoholic fatty liver disease(NAFLD),recently renamed metabolic dysfunction-associated steatotic liver disease(MASLD),is becoming the leading cause of end-stage liver disease,a new scenario characterized by the frequent coexistence of NAFLD,obesity,and sarcopenia is *** it is not yet resolved whether the bidirectional relationship between sarcopenia and NAFLD subtends causal determinants,it is clear that the interaction of these two conditions is associated with an increased risk of poor ***,during the course of CLD,deregulation of the liver-muscle-adipose tissue axis has been ***,owing to the lack of properly designed studies,specific therapeutic guidelines for patients with sarcopenia in the context of NAFLD-related CLD have not yet been *** aimed to induce the loss of fat mass together with the maintenance of lean body mass seem most *** can be achieved by properly designed diets integrated with specific nutritional supplementations and accompanied by adequate physical *** studies aiming to add to the knowledge of the correct assessment and approach to sarcopenia in the context of NAFLD-related CLD are eagerly awaited.

关键词： NAFLD MASLD Cirrhosis Sarcopenia Sarcopenic obesity