5-Substituted benzylidene 3-acylthiotetronic acids are antifungal.A series of 3-acylthiotetronic acid derivatives with varying substitutions at the 5-position were designed,synthesized,and characterized,based on the b...5-Substituted benzylidene 3-acylthiotetronic acids are antifungal.A series of 3-acylthiotetronic acid derivatives with varying substitutions at the 5-position were designed,synthesized,and characterized,based on the binding pose of 3-acyl thiolactone with the protein C171Q KasA.Fungicidal activities of these compounds were screened against Valsa Mali,Curvularia lunata,Fusarium graminearum,and Fusarium oxysporum f.sp.lycopersici.Most target compounds exhibited excellent fungicidal activities against target fungi at the concentration of 50μg·mL-1.Compounds 11c and 11i displayed the highest activity with a broad spectrum.The median effective concentration(EC50)values of 11c and 11i were 1.9–10.7 and 3.1–7.8μg·mL-1,respectively,against the tested fungi,while the EC50 values of the fungicides azoxystrobin,carbendazim,and fluopyram were respectively 0.30,4.22,and>50μg·mL-1 against V.Mali;6.7,41.7,and 0.18μg·mL-1 against C.lunata;22.4,0.42,and 0.43μg·mL-1 against F.graminearum;and 4.3,0.12,and>50μg·mL-1 against F.oxysporum f.sp.lycopersici.The structures and activities of the target compounds against C.lunata were analyzed to obtain a statistically significant comparative molecular field analysis(CoMFA)model with high prediction abilities(q2=0.9816,r2=0.8060),and its reliability was verified.The different substituents on the benzylidene at the 5-position had significant effects on the activity,while the introduction of a halogen atom at the benzene ring of benzylidene was able to improve the activity against the tested fungi.展开更多
Sparse labeling of neurons contributes to uncovering their morphology, and rapid expression of a fluorescent protein reduces the experiment range. To achieve the goal of rapid and sparse labeling of neurons in vivo, w...Sparse labeling of neurons contributes to uncovering their morphology, and rapid expression of a fluorescent protein reduces the experiment range. To achieve the goal of rapid and sparse labeling of neurons in vivo, we established a rapid method for depicting the fine structure of neurons at 24 h post-infection based on a mutant viruslike particle of Semliki Forest virus. Approximately 0.014 fluorescent focus-forming units of the mutant virus-like particle transferred enhanced green fluorescent protein into neurons in vivo, and its affinity for neurons in vivo was stronger than for neurons in vitro and BHK21(baby hamster kidney) cells. Collectively, the mutant virus-likeparticle provides a robust and convenient way to reveal the fine structure of neurons and is expected to be a helper virus for combining with other tools to determine their connectivity. Our work adds a new tool to the approaches for rapid and sparse labeling of neurons in vivo.展开更多
A newly designed electric assisted micro-electrolysis filter(E-ME) was developed to investigate its degradation efficiency for coking wastewater and correlated characteristics. The performance of the E-ME system was...A newly designed electric assisted micro-electrolysis filter(E-ME) was developed to investigate its degradation efficiency for coking wastewater and correlated characteristics. The performance of the E-ME system was compared with separate electrolysis(SE) and micro-electrolysis(ME) systems. The results showed a prominent synergistic effect on COD removal in E-ME systems. Gas chromatography/mass spectrometry(GC–MS) analysis confirmed that the applied electric field enhanced the degradation of phenolic compounds.Meanwhile, more biodegradable oxygen-bearing compounds were detected. SEM images of granular activated carbon(GAC) showed that inactivation and blocking were inhibited during the E-ME process. The effects of applied voltage and initial p H in E-ME systems were also studied. The best voltage value was 1 V, but synergistic effects existed even with lower applied voltage. E-ME systems exhibited some p H buffering capacity and attained the best efficiency in neutral media, which means that there is no need to adjust p H prior to or during the treatment process. Therefore, E-ME systems were confirmed as a promising technology for treatment of coking wastewater and other refractory wastewater.展开更多
Forster resonance energy transfer(FRET)is a widely used distance measurement method to illustrate protein conformational dynamics.The FRET method relies on the distance between donor and acceptor,as well as the labell...Forster resonance energy transfer(FRET)is a widely used distance measurement method to illustrate protein conformational dynamics.The FRET method relies on the distance between donor and acceptor,as well as the labelling efficiency,the size and the properties of the fluorophores.Here,we labelled a pair of small fluorophores and calculated the energy transferred efficiency through fluorescence lifetime analysis,which can provide more reliable distance measurement than intensity attenuation.The donor fluorophore,7-hydroxycoumarin-4-yl-ethylglycine(HC),was genetically incorporated into specific sites of PYL10,obtaining complete labelling efficiency.The acceptor fluorophore,Alexa488,was labelled through the disulfide bond,whose labelling efficiency was estimated through both absorption peaks and lifetime populations.Fluorescence lifetime and anisotropy analysis showed ABA-induced local conformation changes and dynamics of several HC incorporation sites of PYL10.The lifetime-based FRET distance measurement illustrated the conformation changes of PYL10 with or without ABA application,which is consistent with the previously reported crystal structures.展开更多
In recent years,crowd counting has increasingly drawn attention due to its widespread applications in the field of computer vision.Most of the existing methods rely on datasets with scarce labeled images to train netw...In recent years,crowd counting has increasingly drawn attention due to its widespread applications in the field of computer vision.Most of the existing methods rely on datasets with scarce labeled images to train networks.They are prone to suffer from the over-fitting problem.Further,these existing datasets usually just give manually labeled annotations related to the head center position.This kind of annotation provides limited information.In this paper,we propose to exploit virtual synthetic crowd scenes to improve the performance of the counting network in the real world.Since we can obtain people masks easily in a synthetic dataset,we first learn to distinguish people from the background via a segmentation network using the synthetic data.Then we transfer the learned segmentation priors from synthetic data to real-world data.Finally,we train a density estimation network on real-world data by utilizing the obtained people masks.Our experiments on two crowd counting datasets demonstrate the effectiveness of the proposed method.展开更多
Trajectory prediction is a fundamental and challenging task for numerous applications,such as autonomous driving and intelligent robots.Current works typically treat pedestrian trajectories as a series of 2D point coo...Trajectory prediction is a fundamental and challenging task for numerous applications,such as autonomous driving and intelligent robots.Current works typically treat pedestrian trajectories as a series of 2D point coordinates.However,in real scenarios,the trajectory often exhibits randomness,and has its own probability distribution.Inspired by this observation and other movement characteristics of pedestrians,we propose a simple and intuitive movement description called a trajectory distribution,which maps the coordinates of the pedestrian trajectory to a 2D Gaussian distribution in space.Based on this novel description,we develop a new trajectory prediction method,which we call the social probability method.The method combines trajectory distributions and powerful convolutional recurrent neural networks.Both the input and output of our method are trajectory distributions,which provide the recurrent neural network with sufficient spatial and random information about moving pedestrians.Furthermore,the social probability method extracts spatio-temporal features directly from the new movement description to generate robust and accurate predictions.Experiments on public benchmark datasets show the effectiveness of the proposed method.展开更多
基金This work was financially supported in part by the National Natural Science Foundation of China(31901906)the Opening Project of Shanghai Key Laboratory of Chemical Biology,the Natural Science Foundation of Anhui Province,China(1808085QC71)+1 种基金the Natural Science Foundation of Anhui Education Department(KJ2016A834)the US Department of Agriculture(USDA:HAW5032-R).
文摘5-Substituted benzylidene 3-acylthiotetronic acids are antifungal.A series of 3-acylthiotetronic acid derivatives with varying substitutions at the 5-position were designed,synthesized,and characterized,based on the binding pose of 3-acyl thiolactone with the protein C171Q KasA.Fungicidal activities of these compounds were screened against Valsa Mali,Curvularia lunata,Fusarium graminearum,and Fusarium oxysporum f.sp.lycopersici.Most target compounds exhibited excellent fungicidal activities against target fungi at the concentration of 50μg·mL-1.Compounds 11c and 11i displayed the highest activity with a broad spectrum.The median effective concentration(EC50)values of 11c and 11i were 1.9–10.7 and 3.1–7.8μg·mL-1,respectively,against the tested fungi,while the EC50 values of the fungicides azoxystrobin,carbendazim,and fluopyram were respectively 0.30,4.22,and>50μg·mL-1 against V.Mali;6.7,41.7,and 0.18μg·mL-1 against C.lunata;22.4,0.42,and 0.43μg·mL-1 against F.graminearum;and 4.3,0.12,and>50μg·mL-1 against F.oxysporum f.sp.lycopersici.The structures and activities of the target compounds against C.lunata were analyzed to obtain a statistically significant comparative molecular field analysis(CoMFA)model with high prediction abilities(q2=0.9816,r2=0.8060),and its reliability was verified.The different substituents on the benzylidene at the 5-position had significant effects on the activity,while the introduction of a halogen atom at the benzene ring of benzylidene was able to improve the activity against the tested fungi.
基金supported by the National Natural Science Foundation of China(31771197,31830035 and 91732304)the National Basic Research Development Program(973 Program)of China(2015CB755600)+2 种基金the Strategic Priority Research Program(B)Chinese Academy of Sciences,China(XDBS01030200)the Major Research Plan of the National Natural Science Foundation of China(91632303)
文摘Sparse labeling of neurons contributes to uncovering their morphology, and rapid expression of a fluorescent protein reduces the experiment range. To achieve the goal of rapid and sparse labeling of neurons in vivo, we established a rapid method for depicting the fine structure of neurons at 24 h post-infection based on a mutant viruslike particle of Semliki Forest virus. Approximately 0.014 fluorescent focus-forming units of the mutant virus-like particle transferred enhanced green fluorescent protein into neurons in vivo, and its affinity for neurons in vivo was stronger than for neurons in vitro and BHK21(baby hamster kidney) cells. Collectively, the mutant virus-likeparticle provides a robust and convenient way to reveal the fine structure of neurons and is expected to be a helper virus for combining with other tools to determine their connectivity. Our work adds a new tool to the approaches for rapid and sparse labeling of neurons in vivo.
基金supported by the National Major Project for Water Pollution Control and Scientific Management (No. 2014ZX07105-001)the Major Special Science and Technology Project of Yunnan Province for New Energy (No. 2012ZB005)the National Natural Science Foundation of China (No. 21377048)
文摘A newly designed electric assisted micro-electrolysis filter(E-ME) was developed to investigate its degradation efficiency for coking wastewater and correlated characteristics. The performance of the E-ME system was compared with separate electrolysis(SE) and micro-electrolysis(ME) systems. The results showed a prominent synergistic effect on COD removal in E-ME systems. Gas chromatography/mass spectrometry(GC–MS) analysis confirmed that the applied electric field enhanced the degradation of phenolic compounds.Meanwhile, more biodegradable oxygen-bearing compounds were detected. SEM images of granular activated carbon(GAC) showed that inactivation and blocking were inhibited during the E-ME process. The effects of applied voltage and initial p H in E-ME systems were also studied. The best voltage value was 1 V, but synergistic effects existed even with lower applied voltage. E-ME systems exhibited some p H buffering capacity and attained the best efficiency in neutral media, which means that there is no need to adjust p H prior to or during the treatment process. Therefore, E-ME systems were confirmed as a promising technology for treatment of coking wastewater and other refractory wastewater.
基金supported by National Key R&D Program of China(Nos.2017YFA0505300,2016YFA0400900)the Instrument Developing Project of the Chinese Academy of Sciences(No.YZ201564)the National Natural Science Foundation of China(Nos.U1832181,31670776,31500611)
文摘Forster resonance energy transfer(FRET)is a widely used distance measurement method to illustrate protein conformational dynamics.The FRET method relies on the distance between donor and acceptor,as well as the labelling efficiency,the size and the properties of the fluorophores.Here,we labelled a pair of small fluorophores and calculated the energy transferred efficiency through fluorescence lifetime analysis,which can provide more reliable distance measurement than intensity attenuation.The donor fluorophore,7-hydroxycoumarin-4-yl-ethylglycine(HC),was genetically incorporated into specific sites of PYL10,obtaining complete labelling efficiency.The acceptor fluorophore,Alexa488,was labelled through the disulfide bond,whose labelling efficiency was estimated through both absorption peaks and lifetime populations.Fluorescence lifetime and anisotropy analysis showed ABA-induced local conformation changes and dynamics of several HC incorporation sites of PYL10.The lifetime-based FRET distance measurement illustrated the conformation changes of PYL10 with or without ABA application,which is consistent with the previously reported crystal structures.
基金This work was supported in part by the National Natural Science Foundation of China(Grant Nos.61802351,61822701,61872324,61772474,62036010)in part by China Postdoctoral Science Foundation(2018M632802)in part by Key R&D and Promotion Projects in Henan Province(192102310258).
文摘In recent years,crowd counting has increasingly drawn attention due to its widespread applications in the field of computer vision.Most of the existing methods rely on datasets with scarce labeled images to train networks.They are prone to suffer from the over-fitting problem.Further,these existing datasets usually just give manually labeled annotations related to the head center position.This kind of annotation provides limited information.In this paper,we propose to exploit virtual synthetic crowd scenes to improve the performance of the counting network in the real world.Since we can obtain people masks easily in a synthetic dataset,we first learn to distinguish people from the background via a segmentation network using the synthetic data.Then we transfer the learned segmentation priors from synthetic data to real-world data.Finally,we train a density estimation network on real-world data by utilizing the obtained people masks.Our experiments on two crowd counting datasets demonstrate the effectiveness of the proposed method.
基金supported in part by the National Natural Science Foundation of China under Grant Nos.61772474,61802351,61822701,and 61872324in part by the Program for Science and Technology Innovation Talents in Universities of Henan Province under Grant No.20HASTIT021.
文摘Trajectory prediction is a fundamental and challenging task for numerous applications,such as autonomous driving and intelligent robots.Current works typically treat pedestrian trajectories as a series of 2D point coordinates.However,in real scenarios,the trajectory often exhibits randomness,and has its own probability distribution.Inspired by this observation and other movement characteristics of pedestrians,we propose a simple and intuitive movement description called a trajectory distribution,which maps the coordinates of the pedestrian trajectory to a 2D Gaussian distribution in space.Based on this novel description,we develop a new trajectory prediction method,which we call the social probability method.The method combines trajectory distributions and powerful convolutional recurrent neural networks.Both the input and output of our method are trajectory distributions,which provide the recurrent neural network with sufficient spatial and random information about moving pedestrians.Furthermore,the social probability method extracts spatio-temporal features directly from the new movement description to generate robust and accurate predictions.Experiments on public benchmark datasets show the effectiveness of the proposed method.