Based on Bloom’s“effective teaching theory,”this paper proposes pre-class activities to improve students’enthusiasm and autonomy in English learning.These include sentence construction,situational dubbing,famous q...Based on Bloom’s“effective teaching theory,”this paper proposes pre-class activities to improve students’enthusiasm and autonomy in English learning.These include sentence construction,situational dubbing,famous quotes,English songs,English games,Chinese stories,regional cultures,and theme debates,which combine life,interest,and inspiration as the main characteristics.The activities can enhance the sense of participation and achievement of all students to achieve the purpose of effective teaching.展开更多
Recently,convolutional neural network(CNN)-based visual inspec-tion has been developed to detect defects on building surfaces automatically.The CNN model demonstrates remarkable accuracy in image data analysis;however...Recently,convolutional neural network(CNN)-based visual inspec-tion has been developed to detect defects on building surfaces automatically.The CNN model demonstrates remarkable accuracy in image data analysis;however,the predicted results have uncertainty in providing accurate informa-tion to users because of the“black box”problem in the deep learning model.Therefore,this study proposes a visual explanation method to overcome the uncertainty limitation of CNN-based defect identification.The visual repre-sentative gradient-weights class activation mapping(Grad-CAM)method is adopted to provide visually explainable information.A visualizing evaluation index is proposed to quantitatively analyze visual representations;this index reflects a rough estimate of the concordance rate between the visualized heat map and intended defects.In addition,an ablation study,adopting three-branch combinations with the VGG16,is implemented to identify perfor-mance variations by visualizing predicted results.Experiments reveal that the proposed model,combined with hybrid pooling,batch normalization,and multi-attention modules,achieves the best performance with an accuracy of 97.77%,corresponding to an improvement of 2.49%compared with the baseline model.Consequently,this study demonstrates that reliable results from an automatic defect classification model can be provided to an inspector through the visual representation of the predicted results using CNN models.展开更多
A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characteriz...A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells.展开更多
New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<s...New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<sub>2</sub>O (1∙2H<sub>2</sub>O), has been synthesized upon reaction of cobalt chloride hexahydrate (Co(Cl)<sub>2</sub>∙6H<sub>2</sub>O) with 3-methyl-1-Phenyl-4-(2-thienoyl)-pyrazol-5-one (referred as HL) in ethanol at room temperature. Single crystal X-ray diffraction (XRD), spectroscopic methods, and microelemental analyses were used to characterize 1∙2H<sub>2</sub>O. Compound 1∙2H<sub>2</sub>O crystallizes in the orthorhombic crystal system with a Pbca space group and with the cobalt atom being pseudo-octahedral coordinated. The broth microdilution technique was used to screen the free ligand (HL) and the complex (1∙2H<sub>2</sub>O) for antimicrobial activities. HL has a low activity (MIC > 100 μg/mL) on all microorganisms, whereas compound 1∙2H<sub>2</sub>O displayed moderate activity (10 ∙2H<sub>2</sub>O exhibited bactericidal and fungicidal activity respectively on all the bacteria and yeasts tested. These findings reveal that the antimicrobial activity of HL was enhanced upon coordination to Co(II) ion against all microorganisms (bacteria and fungus).展开更多
New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<s...New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<sub>2</sub>O (1∙2H<sub>2</sub>O), has been synthesized upon reaction of cobalt chloride hexahydrate (Co(Cl)<sub>2</sub>∙6H<sub>2</sub>O) with 3-methyl-1-Phenyl-4-(2-thienoyl)-pyrazol-5-one (referred as HL) in ethanol at room temperature. Single crystal X-ray diffraction (XRD), spectroscopic methods, and microelemental analyses were used to characterize 1∙2H<sub>2</sub>O. Compound 1∙2H<sub>2</sub>O crystallizes in the orthorhombic crystal system with a Pbca space group and with the cobalt atom being pseudo-octahedral coordinated. The broth microdilution technique was used to screen the free ligand (HL) and the complex (1∙2H<sub>2</sub>O) for antimicrobial activities. HL has a low activity (MIC > 100 μg/mL) on all microorganisms, whereas compound 1∙2H<sub>2</sub>O displayed moderate activity (10 ∙2H<sub>2</sub>O exhibited bactericidal and fungicidal activity respectively on all the bacteria and yeasts tested. These findings reveal that the antimicrobial activity of HL was enhanced upon coordination to Co(II) ion against all microorganisms (bacteria and fungus).展开更多
Education in the new era advocates taking students as the main body and improving students’core literacy on this basis.Subjectivity has also become one of the keys to quality education.Primary school is not only the ...Education in the new era advocates taking students as the main body and improving students’core literacy on this basis.Subjectivity has also become one of the keys to quality education.Primary school is not only the initial stage of life,but also the key period to develop students’subjectivity.At present,there are many problems in class activities,such as the weak concept of taking students as the main body,the lack of subject consciousness among students,the flawed construction system of class activities,the unreasonable evaluation system of class activities,and so on.By establishing the role-playing model under the background of“class activity month,”students can play different roles in class activities and participate in various links,such as theme selection,scheme design,organization,implementation,summary,and evaluation of class activities.Through this process,it does not only improve the quality of class activities,but also cultivate students’subject consciousness and ability in a certain subject,thus highlighting their subject status in class activities.展开更多
[Objective] This study aimed to analyze the expression, purification and insecticidal activity of Cry1Ac without helix α-1 of domain I in E. coli. [Method] Plasmid of B. thuringiensis HD-1 was used as the template fo...[Objective] This study aimed to analyze the expression, purification and insecticidal activity of Cry1Ac without helix α-1 of domain I in E. coli. [Method] Plasmid of B. thuringiensis HD-1 was used as the template for amplification of Cry1Ac gene, which was linked with pET28a vector to construct the recombinant plasmid. After transformation and IPTG induction, expression of target protein was detected by using SDS-PAGE method. Target protein was extracted and coated on the surface of feed for H. armigera to determine the insecticidal activity. [Result] Cry1Acdela1 gene could normally express the target protein in E. coli. However, the target protein existed in the form of inclusion body. Results of bioassay analysis showed that under the same concentration, fatality rate of activated Cry1Ac toxin reached above 75%, while that of Cry1Acdelα1 was only about 10%. [Conclusion] E. coli-expressed Cry1Acdelα1 had no insecticidal activity against H. armigera.展开更多
Interest is the precondition and motivation for people's accomplishment.However,due to the exam-oriented system,millions of parents and teachers neglect the interests of children,and our children nearly forget the...Interest is the precondition and motivation for people's accomplishment.However,due to the exam-oriented system,millions of parents and teachers neglect the interests of children,and our children nearly forget their interests or hobbies.Based on different interests of children,the thesis analyzes how to apply the goal-setting theory in the second classroom teaching activities of College English,using the example of Lushan College of Guangxi University of Technology.展开更多
One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by ...One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by spectroscopic evi-dences.Compound 1 was initially isolated as an enantiomer,and further separation of 1 by chiral HPLC afforded a pair of enantio-mers,including(-)-5-isopentenyl-cryptoechinuline D(1a)and(+)-5-isopentenyl-cryptoechinuline D(1b).Their absolute configura-tions were elucidated by ECD spectroscopic data.Compounds 1a,5 and 10 could inhibit thioredoxin reductase(TrxR)activity with IC50 values of 6.2,36.3 and 18.6μmol L^(-1),respectively.Surface plasmon resonance(SPR)study also demonsrated the interactions between compounds 6,8 and Niemann-Pick C1 Like 1(NPC1L1)respectively,which indicate that compounds 6 and 8 are potential NPC1L1 inhibitors.展开更多
We examined time allocation by Sichuan snub-nosed monkeys Rhinopithecus roxellana in the montane, temperate and highly seasonal forests of the Shennongjia Nature Reserve in China, in order to improve our understanding...We examined time allocation by Sichuan snub-nosed monkeys Rhinopithecus roxellana in the montane, temperate and highly seasonal forests of the Shennongjia Nature Reserve in China, in order to improve our understanding of the ecological and social influences on monkey behavior. We collected data on activity budgets in relation to food availability in a group of monkeys from July 2003 to September 2004 (except February 2004), using instantaneous scan samples. The monkeys spent 36.21% of daytime moving ( n = 21, 269 records), 24.39% foraging, 9.33% inactive, 11,7% performing social behaviors, and 18.38% performing other behaviors. There were seasonal and annual variations in the proportions of time devoted to some activities. These variations were largely attributed to seasonal or annual fluctuations in the distribution and quality of food resources. Adult males spent more time moving, searching, and displaying other behaviors, but less time feeding and performing social behaviors than adult females. Adults performed other behaviors more often and moving less often than juveniles. These differences in activity budgets may reflect fundamental differences in reproductive biology, parental investment, and development among the different age/sex classes [ Current Zoology 55 (3) : 173 - 179, 2009] .展开更多
This report reviews the characteristics of JS399-19, a novel cyanoacrylate fungicide. JS399-19 strongly inhibits the mycelial growth of the fungal plant pathogens of the genus Fusarium and exhibits great potential in ...This report reviews the characteristics of JS399-19, a novel cyanoacrylate fungicide. JS399-19 strongly inhibits the mycelial growth of the fungal plant pathogens of the genus Fusarium and exhibits great potential in controlling Fusarium head blight (FHB) on wheat and other cereals. The mode of action of JS399-19 is evidently different from that of benzimidazole (for example, carbendazim) and other sort of fungicides, making it a possible replacement for carbendazim in China to manage carbendazim-resistant subpopulations of Fusarium graminearum and F. asiaticum. JS399-t9 has excellent protective and curative activity against these pathogens. Incorrect use of this fungicide, however, is likely to select for resistance. Among JS399-19-resistant mutants of F. asiaticum induced in the laboratory, the resistant level of mutants was high and the phenotype of resistance against JS399-19 was conferred by a major gene by genetic analysis. The fitness of laboratory-induced JS399-19-resistant mutants of F. asiaticum was nearly equal to that of their parents. JS399-19 lacks cross resistance with other sort fungicides. To control FHB with JS399-19 and to delay the development of the fungicide-resistance, farmers should use tank mixtures containing JS399-19 and carbendazim, metconazole, tebuconazole, or prothioconazole.展开更多
Based on Kohler’s ternary solution model and Miedemaa’s model for calculating the heats of formation-△Hij of binary Systems, the integral equation has ben established for calculating the activity coefficients in te...Based on Kohler’s ternary solution model and Miedemaa’s model for calculating the heats of formation-△Hij of binary Systems, the integral equation has ben established for calculating the activity coefficients in ternarysolution. With the equation, the activity coefficients in Ti-15-3 melt have been calculated. The results show that allof components’ activity coefficients are less than 1, in other wolds, compared with ideal solution, all components takeon a negative deviation. At 2000K, the activity coefficients in Ti-15-3 melt are shown as: about 0.9 for Ti, about0.85 for V, about 0. 1 for Al, aboaut 0.5 for Cr and about 0.23 for Sn. me addition of V lowers the activity coefficient of Ti, but raise the ones of Al, Cr and Sn. These results can be directly used to calculate the evaporation loss ofAl, Cr and Sn during the ISM(Induction Skull Melting) process and at the same time estimate the reactivity betweenTi-15-3 melt and refractory during the cast production.展开更多
In medical diagnosis, the problem of class imbalance is popular. Though there are abundant unlabeled data, it is very difficult and expensive to get labeled ones. In this paper, an ensemble-based active learning algor...In medical diagnosis, the problem of class imbalance is popular. Though there are abundant unlabeled data, it is very difficult and expensive to get labeled ones. In this paper, an ensemble-based active learning algorithm is proposed to address the class imbalance problem. The artificial data are created according to the distribution of the training dataset to make the ensemble diverse, and the random subspace re-sampling method is used to reduce the data dimension. In selecting member classifiers based on misclassification cost estimation, the minority class is assigned with higher weights for misclassification costs, while each testing sample has a variable penalty factor to induce the ensemble to correct current error. In our experiments with UCI disease datasets, instead of classification accuracy, F-value and G-means are used as the evaluation rule. Compared with other ensemble methods, our method shows best performance, and needs less labeled samples.展开更多
The water-soluble part(GS) of Ganoderma sinense Zhao, Xu et Zhang was divided into high molecular(GS-H) and low molecular(GS-L) parts by Cellulose Super Filtration, and GS was also fractionated into four fractio...The water-soluble part(GS) of Ganoderma sinense Zhao, Xu et Zhang was divided into high molecular(GS-H) and low molecular(GS-L) parts by Cellulose Super Filtration, and GS was also fractionated into four fractions, GS-1, 2, 3, and 4 by ethanol precipitation according to their molecular weights. Chemical analysis shows that GS and GS-1, 2, 3, 4 were complexes of polysaccharide and peptide. The fractions with molecular weights over 4000, GS-1, 2, 3, and GS-H show anti-tumor activities, however, the fractions with molecular weights lower than 4000, GS-4, and GS-L have no anti-tumor activity, indicating that the anti-tumor activity of Ganoderma Sinensis was caused by glucopeptides with molecular weight ranging from 4000 to 20000. Two purified glucopeptides, GS-6b and GS-7b were obtained from GS-H by ion-exchange and gel-permeation chromatography. Their molecular weights, glycosidic linkages, and configurations were detected by means of IR spectrum, sugar composition analysis, and methylation analysis. The polysaccharide parts of GS-6b and GS-7b had glucan backbone consisting of β-1→3 Glc, and side chain containing glucosyl, mannosyl, fucosyl, xylosyl, galactosyl, and glucuronic acid residues attached on 1-2, 1-4, 1-6 positions of the backbone of GS-6b, or 1-6, 1-4 positions of the backbone of GS-7b. The peptide parts in GS-6b and GS-7b were composed of 10 kinds of amino acids, including Asp, Ser, Arg, Gly, Thr, Pro, Ala, Val, Met, and Lys.展开更多
The title compound (E)-4-tert-butyl-N-(2,4-dichlorobenzylidene)-5-(1,2,4-triazol-1-yl)-thiazol-2-amine was synthesized by the reaction of 4-tert-butyl-5-(1,2,4-triazol-1-yl)-thiazol-2-amine with 2,4-dichlorobe...The title compound (E)-4-tert-butyl-N-(2,4-dichlorobenzylidene)-5-(1,2,4-triazol-1-yl)-thiazol-2-amine was synthesized by the reaction of 4-tert-butyl-5-(1,2,4-triazol-1-yl)-thiazol-2-amine with 2,4-dichlorobenzaldehyde, and its crystal structure was determined by singlecrystal X-ray diffraction. The crystal belongs to the triclinic system, space group P1 with a = 7.9748(4), b = 10.1803(5), c = 11.4603(6), α = 102.882(1), β = 100.253(1), γ = 104.457(1)°, V = 850.95(7)3, Z = 2, F(000) = 392, C16H15Cl2N5S, Mr = 380.29, Dc = 1.484 g/cm3, S = 1.095, μ = 0.512 mm-1, the final R = 0.0301 and wR = 0.0965 for 3334 observed reflections (I 〉 2σ(I)). The preliminary antitumor activity shows that for the title compound the IC50 of Hela is 0.175 μmol/mL and that of Bel7402 is 0.156 μmol/mL.展开更多
The title compound has been synthesized by the reaction of 4-tert-butyl-5-(1,2,4- triazol-1-yl)-2-aminothiazole with propionic anhydride, and its crystal structure was determined by single-crystal X-ray diffraction....The title compound has been synthesized by the reaction of 4-tert-butyl-5-(1,2,4- triazol-1-yl)-2-aminothiazole with propionic anhydride, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to the orthorhombic system, space group Pbca with α = 18.441(2), b = 8.3284(9), c = 19.257(2) A, Z = 8, V = 2957.5(5) A3, Mr = 279.37, Dc = 1.255 mg/m3, S = 1.033, μ =0.219 mm^-1, F(000) = 1184, the final R = 0.0349 and wR = 0.0876 for 2629 observed reflections (I 〉 2σ(I)). X-ray crystal structure presents the intermolecular N–H···N hydrogen bond, which plays an important role in stabilizing the crystal structure. The preliminary bioassay indicates that the title compound exhibits potent fungicidal activity against R. Solani (25 mg/L) with inhibition rate of 80.0%.展开更多
In recent years, fused heterocycles have been reported to possess important properties in synthesis and pharmacology. Especially, s-triazolo, 3,4-thiadiazole derivatives have been attracting much attention for chemist...In recent years, fused heterocycles have been reported to possess important properties in synthesis and pharmacology. Especially, s-triazolo, 3,4-thiadiazole derivatives have been attracting much attention for chemists and pharmacologists because they show broad spectra of biological activities, such as antifungal, antibacterial, hy-展开更多
The title compound was synthesized by the reaction of 4-tert-butyl-5-(4-chlorobenzyl)-2-aminothiazole with 2,6-difluorobenzoic acid. The crystal structure of the title compound, C21H19ClF2N2OS, was determined by sin...The title compound was synthesized by the reaction of 4-tert-butyl-5-(4-chlorobenzyl)-2-aminothiazole with 2,6-difluorobenzoic acid. The crystal structure of the title compound, C21H19ClF2N2OS, was determined by single-crystal X-ray diffraction. The crystal belongs to the triclinic system, space group Pbca with a = 12.6479(13), b = 13.1204(13), c = 14.1341(15), Z = 4, V = 2011.5(4)3, Mr = 420.89, Dc = 1.390 g/cm3, S = 1.023, μ = 0.326 mm-1, F(000) = 872, the final R = 0.0365 and wR = 0.0880 for 6101 observed reflections(I 〉 2σ(I)), and R = 0.0507, wR = 0.0978 for 7779 independent reflections. X-ray crystal structure displays that the hydrogen bonding interactions observed link the molecules to form a dimeric unit. The preliminary biological test of the title compound shows good antitumor activity, with IC50 of 0.046 μmol/mL against the Hela cell line.展开更多
BACKGROUND Gastric cancer(GC)is one of the most common cancer types worldwide,and its prevention and treatment methods have garnered much attention.As the active ingredient of licorice,18β-glycyrrhetinic acid(18β-GR...BACKGROUND Gastric cancer(GC)is one of the most common cancer types worldwide,and its prevention and treatment methods have garnered much attention.As the active ingredient of licorice,18β-glycyrrhetinic acid(18β-GRA)has a variety of pharmacological effects.The aim of this study was to explore the effective target of 18β-GRA in the treatment of GC,in order to provide effective ideas for the clinical prevention and treatment of GC.AIM To investigate the mechanism of 18β-GRA in inhibiting cell proliferation and promoting autophagy flux in GC cells.METHODS Whole transcriptomic analyses were used to analyze and screen differentially expressed microRNAs(miRNAs)in GC cells after 18β-GRA intervention.Lentivirus-transfected GC cells and the Cell Counting Kit-8 were used to detect cell proliferation ability,cell colony formation ability was detected by the clone formation assay,and flow cytometry was used to detect the cell cycle and apoptosis.A nude mouse transplantation tumor model of GC cells was constructed to verify the effect of miR-328-3p overexpression on the tumorigenicity of GC cells.Tumor tissue morphology was observed by hematoxylin and eosin staining,and microtubule-associated protein light chain 3(LC3)expression was detected by immunohistochemistry.TransmiR,STRING,and miRWalk databases were used to predict the relationship between miR-328-3p and signal transducer and activator of transcription 3(STAT3)-related information.Expression of STAT3 mRNA and miR-328-3p was detected by quantitative polymerase chain reaction(qPCR)and the expression levels of STAT3,phosphorylated STAT3(p-STAT3),and LC3 were detected by western blot analysis.The targeted relationship between miR-328-3p and STAT3 was detected using the dual-luciferase reporter gene system.AGS cells were infected with monomeric red fluorescent protein-green fluorescent protein-LC3 adenovirus double label.LC3 was labeled and autophagy flow was observed under a confocal laser microscope.RESULTS The expression of miR-328-3p was significantly upregulated after 18β-GRA intervention in AGS cells(P=4.51E-06).Overexpression of miR-328-3p inhibited GC cell proliferation and colony formation ability,arrested the cell cycle in the G0/G1 phase,promoted cell apoptosis,and inhibited the growth of subcutaneous tumors in BALB/c nude mice(P<0.01).No obvious necrosis was observed in the tumor tissue in the negative control group(no drug intervention or lentivirus transfection)and vector group(the blank vector for lentivirus transfection),and more cells were loose and necrotic in the miR-328-3p group.Bioinformatics tools predicted that miR-328-3p has a targeting relationship with STAT3,and STAT3 was closely related to autophagy markers such as p62.After overexpressing miR-328-3p,the expression level of STAT3 mRNA was significantly decreased(P<0.01)and p-STAT3 was downregulated(P<0.05).The dual-luciferase reporter gene assay showed that the luciferase activity of miR-328-3p and STAT33’untranslated regions of the wild-type reporter vector group was significantly decreased(P<0.001).Overexpressed miR-328-3p combined with bafilomycin A1(Baf A1)was used to detect the expression of LC3 II.Compared with the vector group,the expression level of LC3 II in the overexpressed miR-328-3p group was downregulated(P<0.05),and compared with the Baf A1 group,the expression level of LC3 II in the overexpressed miR-328-3p+Baf A1 group was upregulated(P<0.01).The expression of LC3 II was detected after intervention of 18β-GRA in GC cells,and the results were consistent with the results of miR-328-3p overexpression(P<0.05).Additional studies showed that 18β-GRA promoted autophagy flow by promoting autophagosome synthesis(P<0.001).qPCR showed that the expression of STAT3 mRNA was downregulated after drug intervention(P<0.05).Western blot analysis showed that the expression levels of STAT3 and p-STAT3 were significantly downregulated after drug intervention(P<0.05).CONCLUSION 18β-GRA promotes the synthesis of autophagosomes and inhibits GC cell proliferation by regulating the miR-328-3p/STAT3 signaling pathway.展开更多
文摘Based on Bloom’s“effective teaching theory,”this paper proposes pre-class activities to improve students’enthusiasm and autonomy in English learning.These include sentence construction,situational dubbing,famous quotes,English songs,English games,Chinese stories,regional cultures,and theme debates,which combine life,interest,and inspiration as the main characteristics.The activities can enhance the sense of participation and achievement of all students to achieve the purpose of effective teaching.
基金supported by a Korea Agency for Infrastructure Technology Advancement(KAIA)grant funded by the Ministry of Land,Infrastructure,and Transport(Grant 22CTAP-C163951-02).
文摘Recently,convolutional neural network(CNN)-based visual inspec-tion has been developed to detect defects on building surfaces automatically.The CNN model demonstrates remarkable accuracy in image data analysis;however,the predicted results have uncertainty in providing accurate informa-tion to users because of the“black box”problem in the deep learning model.Therefore,this study proposes a visual explanation method to overcome the uncertainty limitation of CNN-based defect identification.The visual repre-sentative gradient-weights class activation mapping(Grad-CAM)method is adopted to provide visually explainable information.A visualizing evaluation index is proposed to quantitatively analyze visual representations;this index reflects a rough estimate of the concordance rate between the visualized heat map and intended defects.In addition,an ablation study,adopting three-branch combinations with the VGG16,is implemented to identify perfor-mance variations by visualizing predicted results.Experiments reveal that the proposed model,combined with hybrid pooling,batch normalization,and multi-attention modules,achieves the best performance with an accuracy of 97.77%,corresponding to an improvement of 2.49%compared with the baseline model.Consequently,this study demonstrates that reliable results from an automatic defect classification model can be provided to an inspector through the visual representation of the predicted results using CNN models.
文摘A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells.
文摘New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<sub>2</sub>O (1∙2H<sub>2</sub>O), has been synthesized upon reaction of cobalt chloride hexahydrate (Co(Cl)<sub>2</sub>∙6H<sub>2</sub>O) with 3-methyl-1-Phenyl-4-(2-thienoyl)-pyrazol-5-one (referred as HL) in ethanol at room temperature. Single crystal X-ray diffraction (XRD), spectroscopic methods, and microelemental analyses were used to characterize 1∙2H<sub>2</sub>O. Compound 1∙2H<sub>2</sub>O crystallizes in the orthorhombic crystal system with a Pbca space group and with the cobalt atom being pseudo-octahedral coordinated. The broth microdilution technique was used to screen the free ligand (HL) and the complex (1∙2H<sub>2</sub>O) for antimicrobial activities. HL has a low activity (MIC > 100 μg/mL) on all microorganisms, whereas compound 1∙2H<sub>2</sub>O displayed moderate activity (10 ∙2H<sub>2</sub>O exhibited bactericidal and fungicidal activity respectively on all the bacteria and yeasts tested. These findings reveal that the antimicrobial activity of HL was enhanced upon coordination to Co(II) ion against all microorganisms (bacteria and fungus).
文摘New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<sub>2</sub>O (1∙2H<sub>2</sub>O), has been synthesized upon reaction of cobalt chloride hexahydrate (Co(Cl)<sub>2</sub>∙6H<sub>2</sub>O) with 3-methyl-1-Phenyl-4-(2-thienoyl)-pyrazol-5-one (referred as HL) in ethanol at room temperature. Single crystal X-ray diffraction (XRD), spectroscopic methods, and microelemental analyses were used to characterize 1∙2H<sub>2</sub>O. Compound 1∙2H<sub>2</sub>O crystallizes in the orthorhombic crystal system with a Pbca space group and with the cobalt atom being pseudo-octahedral coordinated. The broth microdilution technique was used to screen the free ligand (HL) and the complex (1∙2H<sub>2</sub>O) for antimicrobial activities. HL has a low activity (MIC > 100 μg/mL) on all microorganisms, whereas compound 1∙2H<sub>2</sub>O displayed moderate activity (10 ∙2H<sub>2</sub>O exhibited bactericidal and fungicidal activity respectively on all the bacteria and yeasts tested. These findings reveal that the antimicrobial activity of HL was enhanced upon coordination to Co(II) ion against all microorganisms (bacteria and fungus).
文摘Education in the new era advocates taking students as the main body and improving students’core literacy on this basis.Subjectivity has also become one of the keys to quality education.Primary school is not only the initial stage of life,but also the key period to develop students’subjectivity.At present,there are many problems in class activities,such as the weak concept of taking students as the main body,the lack of subject consciousness among students,the flawed construction system of class activities,the unreasonable evaluation system of class activities,and so on.By establishing the role-playing model under the background of“class activity month,”students can play different roles in class activities and participate in various links,such as theme selection,scheme design,organization,implementation,summary,and evaluation of class activities.Through this process,it does not only improve the quality of class activities,but also cultivate students’subject consciousness and ability in a certain subject,thus highlighting their subject status in class activities.
基金Supported by Beijing Natural Science Foundation(50920075112009)~~
文摘[Objective] This study aimed to analyze the expression, purification and insecticidal activity of Cry1Ac without helix α-1 of domain I in E. coli. [Method] Plasmid of B. thuringiensis HD-1 was used as the template for amplification of Cry1Ac gene, which was linked with pET28a vector to construct the recombinant plasmid. After transformation and IPTG induction, expression of target protein was detected by using SDS-PAGE method. Target protein was extracted and coated on the surface of feed for H. armigera to determine the insecticidal activity. [Result] Cry1Acdela1 gene could normally express the target protein in E. coli. However, the target protein existed in the form of inclusion body. Results of bioassay analysis showed that under the same concentration, fatality rate of activated Cry1Ac toxin reached above 75%, while that of Cry1Acdelα1 was only about 10%. [Conclusion] E. coli-expressed Cry1Acdelα1 had no insecticidal activity against H. armigera.
文摘Interest is the precondition and motivation for people's accomplishment.However,due to the exam-oriented system,millions of parents and teachers neglect the interests of children,and our children nearly forget their interests or hobbies.Based on different interests of children,the thesis analyzes how to apply the goal-setting theory in the second classroom teaching activities of College English,using the example of Lushan College of Guangxi University of Technology.
基金supported by the National Natural Science Foundation of China(No.82204276)the Guangxi Natural Science Foundation(No.2021GXNSFBA075036)+4 种基金the Specific Research Project of Guangxi for Research Bases and Talents(Nos.AD22035018,AD20297036)the 2021 University-Level Scientific Research Projects of Guangxi Minzu University(No.2021MDKJ003)the Talent Scientific Research Initiation Project of Guangxi Minzu University(No.2021KJQD09)the Xiangsi Lake Youth Innovation Team Project of Guangxi Minzu University(No.2021 RSCXSHQN01)the Guangxi Scholarship Fund of Guangxi Education Department.
文摘One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by spectroscopic evi-dences.Compound 1 was initially isolated as an enantiomer,and further separation of 1 by chiral HPLC afforded a pair of enantio-mers,including(-)-5-isopentenyl-cryptoechinuline D(1a)and(+)-5-isopentenyl-cryptoechinuline D(1b).Their absolute configura-tions were elucidated by ECD spectroscopic data.Compounds 1a,5 and 10 could inhibit thioredoxin reductase(TrxR)activity with IC50 values of 6.2,36.3 and 18.6μmol L^(-1),respectively.Surface plasmon resonance(SPR)study also demonsrated the interactions between compounds 6,8 and Niemann-Pick C1 Like 1(NPC1L1)respectively,which indicate that compounds 6 and 8 are potential NPC1L1 inhibitors.
基金supported by grants from the"973"program(code:2007CB411600)the National Science Foundation(code:30670354)
文摘We examined time allocation by Sichuan snub-nosed monkeys Rhinopithecus roxellana in the montane, temperate and highly seasonal forests of the Shennongjia Nature Reserve in China, in order to improve our understanding of the ecological and social influences on monkey behavior. We collected data on activity budgets in relation to food availability in a group of monkeys from July 2003 to September 2004 (except February 2004), using instantaneous scan samples. The monkeys spent 36.21% of daytime moving ( n = 21, 269 records), 24.39% foraging, 9.33% inactive, 11,7% performing social behaviors, and 18.38% performing other behaviors. There were seasonal and annual variations in the proportions of time devoted to some activities. These variations were largely attributed to seasonal or annual fluctuations in the distribution and quality of food resources. Adult males spent more time moving, searching, and displaying other behaviors, but less time feeding and performing social behaviors than adult females. Adults performed other behaviors more often and moving less often than juveniles. These differences in activity budgets may reflect fundamental differences in reproductive biology, parental investment, and development among the different age/sex classes [ Current Zoology 55 (3) : 173 - 179, 2009] .
基金sponsored by the National Natural Science Foundation of China (30971891)the Natural Science Foundation of Jiangsu Province, China(BK2008337)the Anhui Provincial Natural Sci-ence Foundation,China (10040606Q26)
文摘This report reviews the characteristics of JS399-19, a novel cyanoacrylate fungicide. JS399-19 strongly inhibits the mycelial growth of the fungal plant pathogens of the genus Fusarium and exhibits great potential in controlling Fusarium head blight (FHB) on wheat and other cereals. The mode of action of JS399-19 is evidently different from that of benzimidazole (for example, carbendazim) and other sort of fungicides, making it a possible replacement for carbendazim in China to manage carbendazim-resistant subpopulations of Fusarium graminearum and F. asiaticum. JS399-t9 has excellent protective and curative activity against these pathogens. Incorrect use of this fungicide, however, is likely to select for resistance. Among JS399-19-resistant mutants of F. asiaticum induced in the laboratory, the resistant level of mutants was high and the phenotype of resistance against JS399-19 was conferred by a major gene by genetic analysis. The fitness of laboratory-induced JS399-19-resistant mutants of F. asiaticum was nearly equal to that of their parents. JS399-19 lacks cross resistance with other sort fungicides. To control FHB with JS399-19 and to delay the development of the fungicide-resistance, farmers should use tank mixtures containing JS399-19 and carbendazim, metconazole, tebuconazole, or prothioconazole.
文摘Based on Kohler’s ternary solution model and Miedemaa’s model for calculating the heats of formation-△Hij of binary Systems, the integral equation has ben established for calculating the activity coefficients in ternarysolution. With the equation, the activity coefficients in Ti-15-3 melt have been calculated. The results show that allof components’ activity coefficients are less than 1, in other wolds, compared with ideal solution, all components takeon a negative deviation. At 2000K, the activity coefficients in Ti-15-3 melt are shown as: about 0.9 for Ti, about0.85 for V, about 0. 1 for Al, aboaut 0.5 for Cr and about 0.23 for Sn. me addition of V lowers the activity coefficient of Ti, but raise the ones of Al, Cr and Sn. These results can be directly used to calculate the evaporation loss ofAl, Cr and Sn during the ISM(Induction Skull Melting) process and at the same time estimate the reactivity betweenTi-15-3 melt and refractory during the cast production.
文摘In medical diagnosis, the problem of class imbalance is popular. Though there are abundant unlabeled data, it is very difficult and expensive to get labeled ones. In this paper, an ensemble-based active learning algorithm is proposed to address the class imbalance problem. The artificial data are created according to the distribution of the training dataset to make the ensemble diverse, and the random subspace re-sampling method is used to reduce the data dimension. In selecting member classifiers based on misclassification cost estimation, the minority class is assigned with higher weights for misclassification costs, while each testing sample has a variable penalty factor to induce the ensemble to correct current error. In our experiments with UCI disease datasets, instead of classification accuracy, F-value and G-means are used as the evaluation rule. Compared with other ensemble methods, our method shows best performance, and needs less labeled samples.
文摘The water-soluble part(GS) of Ganoderma sinense Zhao, Xu et Zhang was divided into high molecular(GS-H) and low molecular(GS-L) parts by Cellulose Super Filtration, and GS was also fractionated into four fractions, GS-1, 2, 3, and 4 by ethanol precipitation according to their molecular weights. Chemical analysis shows that GS and GS-1, 2, 3, 4 were complexes of polysaccharide and peptide. The fractions with molecular weights over 4000, GS-1, 2, 3, and GS-H show anti-tumor activities, however, the fractions with molecular weights lower than 4000, GS-4, and GS-L have no anti-tumor activity, indicating that the anti-tumor activity of Ganoderma Sinensis was caused by glucopeptides with molecular weight ranging from 4000 to 20000. Two purified glucopeptides, GS-6b and GS-7b were obtained from GS-H by ion-exchange and gel-permeation chromatography. Their molecular weights, glycosidic linkages, and configurations were detected by means of IR spectrum, sugar composition analysis, and methylation analysis. The polysaccharide parts of GS-6b and GS-7b had glucan backbone consisting of β-1→3 Glc, and side chain containing glucosyl, mannosyl, fucosyl, xylosyl, galactosyl, and glucuronic acid residues attached on 1-2, 1-4, 1-6 positions of the backbone of GS-6b, or 1-6, 1-4 positions of the backbone of GS-7b. The peptide parts in GS-6b and GS-7b were composed of 10 kinds of amino acids, including Asp, Ser, Arg, Gly, Thr, Pro, Ala, Val, Met, and Lys.
基金Supported by the Natural Science Foundation of Hunan Province (No. 07JJ302)
文摘The title compound (E)-4-tert-butyl-N-(2,4-dichlorobenzylidene)-5-(1,2,4-triazol-1-yl)-thiazol-2-amine was synthesized by the reaction of 4-tert-butyl-5-(1,2,4-triazol-1-yl)-thiazol-2-amine with 2,4-dichlorobenzaldehyde, and its crystal structure was determined by singlecrystal X-ray diffraction. The crystal belongs to the triclinic system, space group P1 with a = 7.9748(4), b = 10.1803(5), c = 11.4603(6), α = 102.882(1), β = 100.253(1), γ = 104.457(1)°, V = 850.95(7)3, Z = 2, F(000) = 392, C16H15Cl2N5S, Mr = 380.29, Dc = 1.484 g/cm3, S = 1.095, μ = 0.512 mm-1, the final R = 0.0301 and wR = 0.0965 for 3334 observed reflections (I 〉 2σ(I)). The preliminary antitumor activity shows that for the title compound the IC50 of Hela is 0.175 μmol/mL and that of Bel7402 is 0.156 μmol/mL.
基金supported by the Natural Science Foundation of Hunan Province(No.12jj3012)
文摘The title compound has been synthesized by the reaction of 4-tert-butyl-5-(1,2,4- triazol-1-yl)-2-aminothiazole with propionic anhydride, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to the orthorhombic system, space group Pbca with α = 18.441(2), b = 8.3284(9), c = 19.257(2) A, Z = 8, V = 2957.5(5) A3, Mr = 279.37, Dc = 1.255 mg/m3, S = 1.033, μ =0.219 mm^-1, F(000) = 1184, the final R = 0.0349 and wR = 0.0876 for 2629 observed reflections (I 〉 2σ(I)). X-ray crystal structure presents the intermolecular N–H···N hydrogen bond, which plays an important role in stabilizing the crystal structure. The preliminary bioassay indicates that the title compound exhibits potent fungicidal activity against R. Solani (25 mg/L) with inhibition rate of 80.0%.
文摘In recent years, fused heterocycles have been reported to possess important properties in synthesis and pharmacology. Especially, s-triazolo, 3,4-thiadiazole derivatives have been attracting much attention for chemists and pharmacologists because they show broad spectra of biological activities, such as antifungal, antibacterial, hy-
基金Project supported by the National Technology R&D Program(No.2011 BAE06B01)
文摘The title compound was synthesized by the reaction of 4-tert-butyl-5-(4-chlorobenzyl)-2-aminothiazole with 2,6-difluorobenzoic acid. The crystal structure of the title compound, C21H19ClF2N2OS, was determined by single-crystal X-ray diffraction. The crystal belongs to the triclinic system, space group Pbca with a = 12.6479(13), b = 13.1204(13), c = 14.1341(15), Z = 4, V = 2011.5(4)3, Mr = 420.89, Dc = 1.390 g/cm3, S = 1.023, μ = 0.326 mm-1, F(000) = 872, the final R = 0.0365 and wR = 0.0880 for 6101 observed reflections(I 〉 2σ(I)), and R = 0.0507, wR = 0.0978 for 7779 independent reflections. X-ray crystal structure displays that the hydrogen bonding interactions observed link the molecules to form a dimeric unit. The preliminary biological test of the title compound shows good antitumor activity, with IC50 of 0.046 μmol/mL against the Hela cell line.
基金Ningxia Medical University Project,No. XZ2021005Ningxia Natural Science Foundation,Nos. 2022AAC03144 and 2022AAC02039National Natural Science Foundation of China,No. 82260879
文摘BACKGROUND Gastric cancer(GC)is one of the most common cancer types worldwide,and its prevention and treatment methods have garnered much attention.As the active ingredient of licorice,18β-glycyrrhetinic acid(18β-GRA)has a variety of pharmacological effects.The aim of this study was to explore the effective target of 18β-GRA in the treatment of GC,in order to provide effective ideas for the clinical prevention and treatment of GC.AIM To investigate the mechanism of 18β-GRA in inhibiting cell proliferation and promoting autophagy flux in GC cells.METHODS Whole transcriptomic analyses were used to analyze and screen differentially expressed microRNAs(miRNAs)in GC cells after 18β-GRA intervention.Lentivirus-transfected GC cells and the Cell Counting Kit-8 were used to detect cell proliferation ability,cell colony formation ability was detected by the clone formation assay,and flow cytometry was used to detect the cell cycle and apoptosis.A nude mouse transplantation tumor model of GC cells was constructed to verify the effect of miR-328-3p overexpression on the tumorigenicity of GC cells.Tumor tissue morphology was observed by hematoxylin and eosin staining,and microtubule-associated protein light chain 3(LC3)expression was detected by immunohistochemistry.TransmiR,STRING,and miRWalk databases were used to predict the relationship between miR-328-3p and signal transducer and activator of transcription 3(STAT3)-related information.Expression of STAT3 mRNA and miR-328-3p was detected by quantitative polymerase chain reaction(qPCR)and the expression levels of STAT3,phosphorylated STAT3(p-STAT3),and LC3 were detected by western blot analysis.The targeted relationship between miR-328-3p and STAT3 was detected using the dual-luciferase reporter gene system.AGS cells were infected with monomeric red fluorescent protein-green fluorescent protein-LC3 adenovirus double label.LC3 was labeled and autophagy flow was observed under a confocal laser microscope.RESULTS The expression of miR-328-3p was significantly upregulated after 18β-GRA intervention in AGS cells(P=4.51E-06).Overexpression of miR-328-3p inhibited GC cell proliferation and colony formation ability,arrested the cell cycle in the G0/G1 phase,promoted cell apoptosis,and inhibited the growth of subcutaneous tumors in BALB/c nude mice(P<0.01).No obvious necrosis was observed in the tumor tissue in the negative control group(no drug intervention or lentivirus transfection)and vector group(the blank vector for lentivirus transfection),and more cells were loose and necrotic in the miR-328-3p group.Bioinformatics tools predicted that miR-328-3p has a targeting relationship with STAT3,and STAT3 was closely related to autophagy markers such as p62.After overexpressing miR-328-3p,the expression level of STAT3 mRNA was significantly decreased(P<0.01)and p-STAT3 was downregulated(P<0.05).The dual-luciferase reporter gene assay showed that the luciferase activity of miR-328-3p and STAT33’untranslated regions of the wild-type reporter vector group was significantly decreased(P<0.001).Overexpressed miR-328-3p combined with bafilomycin A1(Baf A1)was used to detect the expression of LC3 II.Compared with the vector group,the expression level of LC3 II in the overexpressed miR-328-3p group was downregulated(P<0.05),and compared with the Baf A1 group,the expression level of LC3 II in the overexpressed miR-328-3p+Baf A1 group was upregulated(P<0.01).The expression of LC3 II was detected after intervention of 18β-GRA in GC cells,and the results were consistent with the results of miR-328-3p overexpression(P<0.05).Additional studies showed that 18β-GRA promoted autophagy flow by promoting autophagosome synthesis(P<0.001).qPCR showed that the expression of STAT3 mRNA was downregulated after drug intervention(P<0.05).Western blot analysis showed that the expression levels of STAT3 and p-STAT3 were significantly downregulated after drug intervention(P<0.05).CONCLUSION 18β-GRA promotes the synthesis of autophagosomes and inhibits GC cell proliferation by regulating the miR-328-3p/STAT3 signaling pathway.