Curative Activity Research Articles

Luotonin A and Its Derivatives as Novel Antiviral and Antiphytopathogenic Fungus Agents.

Plant diseases caused by viruses and fungi have posed a serious threat to global agricultural production. The discovery of new leads based on natural products is an important way to innovate pesticides. In this work, natural product luotonin A was found to have good antiviral activity against tobacco mosaic virus (TMV) for the first time. A series of luotonin A derivatives were designed, synthesized, and evaluated for their antiviral activities and fungicidal activities systematically. Most compounds displayed better antiviral activities against TMV than commercial ribavirin. Compounds 9k, 12b, and 12d displayed about similar inhibitory effects as ningnanmycin (inhibitory rates of 55, 57, and 59% at 500 μg/mL for inactivation, curative, and protection activities in vivo, respectively), the best antiviral agent at present, and emerged as novel antiviral leads for further research. We selected 9k for further antiviral mechanism research via transmission electron microscopy and molecular docking, which revealed that compound 9k can interact with TMV coat protein through the hydrogen bond, leading to its polymerization, thus preventing virus assembly. Further fungicidal activity tests showed that these compounds also showed broad-spectrum fungicidal activities against 14 kinds of phytopathogenic fungi. Especially, compound 14 with a 100% antifungal effect against Botrytis cinereal emerged as a lead for further research. This work provides a reference for the development of agricultural active ingredients based on Chinese medicine plants.

Green Synthesized ZnO Nanoparticles Mediated by Mentha Spicata Extract Induce Plant Systemic Resistance against Tobacco Mosaic Virus

Globally, plant viral infection is one of the most difficult challenges of food security, where considerable losses in crop production occur. Nanoparticles are an effective control agent against numerous plant pathogens. However, there is limited knowledge concerning their effects against viral infection. In the present study, the green synthesis of zinc oxide nanoparticles (ZnO NPs) using aqueous leaf extract of Mentha spicata was achieved. X-ray diffraction patterns confirmed the crystalline nature of the prepared ZnO NPs. Dynamic light scattering and scanning electron microscopy analyses revealed that the resultant ZnO NPs were spherical in shape with a particle size ranged from 11 to 88 nm. Fourier transmission infrared spectroscopy detected different functional groups, capping and stability agents, and showed Zn-O bond within wavenumber of 487 cm−1. Under greenhouse conditions, the antiviral activity of biological synthesized ZnO NPs (100 µg/mL) against Tobacco mosaic virus (TMV) was evaluated. The double foliar application of the prepared ZnO NPs, 24 h before and 24 h after TMV-inoculation, was the most effective treatment that showed a 90.21% reduction of viral accumulation level and disease severity. Additionally, the transcriptional levels of PAL, PR-1 (salicylic acid marker gene), CHS, and POD genes were induced and up-regulated in all ZnO NPs treated plants. Notably, the results exhibited that aqueous extract of Mentha spicata was an effective reducing agent for the green synthesis of ZnO NPs, which showed significant antiviral activity. Finally, the detected protective and curative activity of ZnO NPs against TMV can encourage us to recommend its application for plant viral disease management. To our knowledge, this is the first study describing the antiviral activity of the green synthesized ZnO NPs.

Conceptualizing Data Curation Activities Within Two Academic Libraries

INTRODUCTION As funders and journals increasingly create policies that require effective data management and data sharing, many institutions have developed research data management (RDM) programs to help researchers meet these mandates. While there is not a standard set of services for these RDM programs, some institutions, particularly those with repositories that accept data deposits, provide data curation services as a way to add value to research data and help make data more accessible and reusable. Stakeholder communities within the field, such as the Data Curation Network (DCN), are also developing guidelines, procedures, and best practices to support and expand data curation practices. DESCRIPTION OF PROJECT This paper examines the data curation activities defined by the DCN, and describes an activity undertaken by library staff at Duke University and the University of North Carolina at Chapel Hill to create a structured model of these tasks to more easily conceptualize and communicate data curation within these two institutional settings. The purpose of this paper is to describe how this model provided a basis for the implementation and expansion of data curation services at each institution and concludes with overall lessons learned. NEXT STEPS As we develop our services, libraries have an opportunity to make the often-invisible work of curation more transparent. This paper aims to provide a point of reference for other libraries as they consider how to scale up their data curation programs as well as contribute to discussions around prioritization of services, program assessment, and communication with stakeholders.

Assessment of antiplasmodial activity of Anthocleista grandiflora on Plasmodium berghei infected mice

Medical plants are used traditionally as alternative treatment for malaria. Anthocleista grandiflora (A. grandiflora) is used traditionally for the treatment of malaria.  This study attempt to scientifically validate its traditional use for malaria treatment by evaluating the antiplasmodial activity of its aqueous leaf extract (AAG) in Plasmodium berghei infected mice. P. berghei infected mice were orally treated with AAG (100, 200 and 400 mg/kg) daily in curative, suppressive and prophylactic studies. The untreated parasitized control (UPC) and the (PC) positive control were orally treated with normal saline (0.2mL) and chloroquine (CQ) (10mg/kg) respectively. At the end of treatment, blood samples were analyzed for parasitamia levels, hematological parameter and lipid profile. No morality was observed in acute toxicity evaluation of AAG in mice. AAG showed significant dose-dependent curative, suppressive and prophylactic activities via reductions in parasitamia levels at 100 mg/kg (p<0.05), 200 mg/kg (p<0.01) and 400 mg/kg (p<0.001) when compared to UPC. Mean survival time was increased in a dose-dependent fashion at 100 mg/kg (p<0.05), 200 mg/kg (p<0.01) and 400 mg/kg (p<0.001) when compared to UPC. AAG increased red blood cells, hemoglobin, pack cell volume, high density lipoprotein cholesterol levels, but decreased white blood cells, total cholesterol, triglyceride and low density lipoprotein cholesterol levels  in a dose-dependent fashion at100 mg/kg (p<0.05), 200 mg/kg (p<0.01) and 400 mg/kg (p<0.001) when compared to UPC. Comparatively the effects of AAG (400 mg/kg) were statistically at par with (CQ) 10mg/kg. Based on the observations in this study, AGA seems safe and has antimalaria activity

Streptindole and Its Derivatives as Novel Antiviral and Anti-Phytopathogenic Fungus Agents.

Plant diseases caused by plant viruses and pathogens seriously affect the production and storage of food crops. With the emergence of drug resistance, it is very difficult to control. Natural products are the source of new drug discovery. Here, the natural product streptindole was found to have good antiviral activity against tobacco mosaic virus (TMV) and fungicidal activities against 14 kinds of phytopathogenic fungi. A series of derivatives of streptindole were designed, synthesized, and evaluated for their antiviral and fungicidal activities. Compounds 4, 5, 11, 12c, 12d, 13d, and 13i-13l showed higher anti-TMV activities than ribavirin (inhibitory rate: 38, 37, and 40% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively), among which compound 12d (inhibitory rate: 57, 55, and 53% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively) with excellent antiviral activity was further evaluated for the mode of action. The mechanism research revealed that 12d can break the three-dimensional structure of TMV coat protein (CP) through hydrogen bonds, thus inhibiting the assembly of virus particles. The molecular docking result showed that compound 12d did exhibit strong interaction with TMV CP. The derivatives of streptindole also displayed broad-spectrum fungicidal activities. The current study provided valuable insights into the antiviral and fungicidal activities of streptindole derivatives.

Design, synthesis, anti-tobacco mosaic viral and molecule docking simulations of urea/thiourea derivatives of 2-(piperazine-1-yl)-pyrimidine and 1-(4-Fluoro/4-Chloro phenyl)-piperazine and 1-(4-Chloro phenyl)-piperazine – A study

The objectives of the present work are to design, syhthesize and introduce novel urea/thiourea derivatives of 2-(piperazine-1-yl)-pyrimidine and 1-(4-Fluoro/4-Chloro phenyl)-piperazine molecules as tobacco mosaic virus (TMV) inhibitors. A series of urea/thiourea derivatives containing pyrimidine and piperazine moieties were synthesized, characterized using Fourier-transform infrared (FTIR) mass spectra, nuclear magnetic resonance (NMR) spectroscopy, elemental analysis and evaluated their sustainability using biological experiments. The anti-viral bioassay of the title compounds showed an antiviral activity against TMV. The compounds synthesized, 9j, 6g and 3d, showed highly-potential curative, protective, and inhibitory activities against TMV at 500 mg/mL formulation. All these compounds were allowed to quantum-polarized-ligand (quantum mechanical and molecular mechanical (QM/MM)) docking experiments. The compounds 9j, 6g and 3d structurally exhibited identical higher affinity towards TMV-Helicase and TMV-Coat proteins. The docking interactions proposed had two stage inhibition of TMV virus by binding to coat protein and helicase for inhibition of RNA replication. The long-range molecular dynamics (150 ns) simulations has revealed more consistency by 9j, 6g and 3d. The present study outcomes good binding propensity for active-tunnel of TMV-Hel enzyme, by these thiourea, urea derivatives, 9j, 6g and 3d, to suggest that the designed and synthesized were ideal for proposing as selective novel inhibitors to target for TMV.

Synthesis and Docking Study of N-(Cinnamoyl)-N'-(substituted)acryloyl Hydrazide Derivatives Containing Pyridinium Moieties as a Novel Class of Filamentous Temperature-Sensitive Protein Z Inhibitors against the Intractable Xanthomonas oryzae pv. oryzae Infections in Rice.

Xanthomonas oryzae pv. oryzae (Xoo) is an offensive phytopathogen that can invade a wide range of plant hosts to develop bacterial diseases, including the well-known rice bacterial leaf blight. However, few agrochemicals have been identified to effectively prevent and eliminate Xoo-induced diseases. Thus, designing novel antibacterial compounds on the basis of the potential targets from Xoo may lead to the discovery of highly efficient and innovative anti-Xoo agents. Filamentous temperature-sensitive protein Z (FtsZ), an important functional protein in the progression of cell division, has been widely reported and exploited as a target for creating antibacterial drugs in the field of medicine. Therefore, the fabrication of innovative frameworks targeting XooFtsZ may be an effective method for managing bacterial leaf blight diseases via blocking the binary division and reproduction of Xoo. As such, a series of novel N-(cinnamoyl)-N'-(substituted)acryloyl hydrazide derivatives containing pyridinium moieties were designed, and the anti-Xoo activity was determined. The bioassay results showed that compound A7 had excellent anti-Xoo activity (EC50 = 0.99 mg L-1) in vitro and distinct curative activity (63.2% at 200 mg L-1) in vivo. Further studies revealed that these designed compounds were XooFtsZ inhibitors, validating by the reduced GTPase activity of recombinant XooFtsZ, the nonfilamentous XooFtsZ assembly observed in the TEM images, and the prolonged Xoo cells from the fluorescence patterns. Computational docking studies showed that compound A7 had strong interactions with ASN34, GLN193, and GLN197 residues located in the α helix regions of XooFtsZ. The present study demonstrates the developed FtsZ inhibitors can serve as agents to control Xoo-induced infections.

Weather factor and chemical management against late leaf spot (LLB) and rust diseases under rainfed groundnut conditions

Groundnut (Arachis hypogaea L.) is most growing under rainfed conditions, the important disease of late leaf spot and rust reduction of yield in rainfed condition. Experiments were conducted 2012, 2013 and 2014. The temperature for three years minimum temperature 23.57 °C temperature 37.54 °C combination of weather conditions during the growing season of groundnut foliar diseases of Late leaf spot and Rust diseases for favourable severe conditions. Among the different chemicals tested for three years the combination of Carbendazim + Mancozeb (SAAF)@1.25Kg/ha recorded the least diseases incidence of Late leaf spot (22.36%) and rust (17.58%) with accounting of diseases reduction for late leaf spot (61.24%) and rust (70.03%) followed by carbendazim and chlorothlonil. The individual application copper hydroxide controlled the rust disease effectively when compared to other treatments also increased yield 1003.67kg/ha. The Carbendazim + Mancozeb (SAAF) @ 1.25kg/ha broad spectrum fungicide for reduced the spraying schedule and no of chemicals used and also protective and curative action with contact and systemic in nature groundnut cultivations under rain fed condition.

Suppressive and curative antiplasmodial properties of Nauclea latifolia root extract and fractions against erythrocytic stage of mice-infective chloroquine-sensitive Plasmodium berghei NK-65

Background: Malaria remains a devastating disease, particularly in the tropics, where it is the highest killer of pregnant women and children under the age of 5 years. Significant efforts and resources have been vested in malaria control and eradication programmes, but the unavailability of malaria vaccine and the emergence of resistance of malaria parasite to existing antimalarial drugs have continued to hamper attempts at controlling or eradicating the disease. This warrants the development of new antimalarial drugs. Nauclea latifolia root is widely applied for malaria treatment in Nigeria. Aim: This study investigated the antimalarial property of N. latifolia roots. Setting: N. latifolia roots were collected from Ikwuano, Umuahia, Abia State, Nigeria. Methods: To extract the bioactive constituents, an aqueous infusion of the plant was prepared and fractionated by solvent-solvent extraction with n -hexane, ethyl acetate and butanol, respectively. Antimalarial property was evaluated using suppressive and curative assays in mice infected with chloroquine-sensitive Plasmodium berghei NK-65 strain. Results: The extract and fractions produced significant suppressive and curative antiplasmodial activities ( p < 0.05). The aqueous extract and n -hexane and butanol fractions gave 85.22%, 84.52% and 91.32% chemosuppression, respectively, which were comparable to that of chloroquine used as positive control. The extract and fractions gave considerable curative effects in the range 52.23% – 77.00%. Conclusion: These findings indicate that N. latifolia roots possess antimalarial property and reflect its ethnomedicinal use for malaria treatment. Thus, N. latifolia roots may be exploited for development of herbal formulations and isolation of novel bioactive compounds for malaria treatment.

Exploring multiple mechanisms of Qingjie Fanggan prescription for prevention and treatment of influenza based on systems pharmacology

Influenza is a type of acute disease characterized by strong contagiousness and short incubation period, which have posed a large potential threat to public health. Traditional Chinese Medicine (TCM) advocates to the aim of combating complex diseases from a holistic view, which has shown effectiveness in anti-influenza. However, the mechanism of TCM prescription remains puzzling. Here, we applied a system pharmacology approach to reveal the underlying molecular mechanisms of Qingjie Fanggan prescription (QFP) in the prevention and treatment of influenza. In this study, we identified 228 potential active compounds by means of absorption, distribution, metabolism, and excretion (ADME) evaluation system and literature research. Then, the targets of the potential active compounds were predicted by using the WES (Weighted Ensemble Similarity) method, and the influenza-related targets were obtained according to some existing gene databases. Next, an herb-component-target network was constructed to further dissect the multi-directional therapeutic approach for QFP. Meanwhile, we also performed gene ontology (GO) enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) annotation analysis on 344 potential targets. Finally, a target-pathway network was constructed to further dissect the core pathways and targets in treatment of influenza for QFP. And the key components and targets were docked by AutoDock Vina to explore their binding mode. All of these demonstrated that QFP had multi-scale curative activity in regulating influenza-related biological processes, which facilitates the application of traditional medicine in modern medicine.

β-Caryophyllene Reduces the Inflammatory Phenotype of Periodontal Cells by Targeting CB2 Receptors.

Human gingival fibroblasts (GF) and human oral mucosa epithelial cells (EC) with an inflammatory phenotype represent a valuable experimental paradigm to explore the curative activity of agents to be used in oral mucositis. The role of cannabinoid receptor 2 (CB2) has not yet been investigated in oral mucositis. The aim of this study was to evaluate the therapeutic potential of β-Caryophyllene (BCP), a CB2 agonist, in an in vitro model of oral mucositis. GF and EC were stimulated with LPS (2 µg/mL) alone or in combination with BCP; a group of LPS challenged GF and EC were treated with BCP and AM630, a CB2 antagonist. LPS increased the inflammatory cytokines TNF-α, IL-1β, IL-6 and IL-17A whereas it decreased the anti-inflammatory cytokine IL-13. The upstream signals were identified in an augmented expression of NF-κB and STAT-3 and in reduced mRNA levels of PPARγ and PGC-1α. BCP blunted the LPS-induced inflammatory phenotype and this effect was reverted by the CB2 antagonist AM630. These results suggest that CB2 receptors are an interesting target to develop innovative strategies for oral mucositis and point out that BCP exerts a marked curative effect in a preclinical model of oral mucositis which deserves to be confirmed in a clinical setting.

Efficacy of Fungicides Applied for Protectant and Curative Activity Against Myrtle Rust.

Myrtle rust, caused by the pathogen Austropuccinia psidii, affects species of the Myrtaceae, many of which are endemic to Australia and New Zealand. Originating from South America, A. psidii is now present in both countries, necessitating effective chemical control for disease management. Using an artificial inoculation protocol, the efficacy of eight fungicides (tebuconazole/trifloxystrobin, cyproconazole/azoxystrobin, fosetyl aluminum, triforine, triadimenol, oxycarboxin, copper, and tebuconazole) applied as curative or protectant treatments was tested on two native New Zealand species (Lophomyrtus × ralphii and Metrosideros excelsa). The impacts of rate (×2), frequency (single or double), and timing (pre- or postinfection) of fungicide application were investigated. Overall, the most effective fungicides tested across both species were those that included a demethylation inhibitor and strobilurin mix, notably tebuconazole/trifloxystrobin (Scorpio) and cyproconazole/azoxystrobin (Amistar Xtra). These fungicides significantly reduced infection of host plants relative to the water control. Timing of application significantly affected bioefficacy, with applications made 7 days before inoculation or 7 days after inoculation being generally the most effective. The rate of fungicide application was not significant for both host species, with few interaction terms showing overall significance. Key findings from this study will set the foundation for further fungicide bioefficacy research conducted to evaluate formulations and adjuvant mixtures, determine suitable application methods for enhanced retention and coverage, and derive optimum application time for effective protection of native and exotic Myrtaceae species in New Zealand.

Design, Synthesis, and Bioactivity of α-Ketoamide Derivatives Bearing a Vanillin Skeleton for Crop Diseases.

A series of novel α-ketoamide derivatives bearing a vanillin skeleton were designed and synthesized. Bioactivity tests on virus and bacteria were performed. The results indicated that some compounds exhibited excellent antitobacco mosaic virus (TMV) activities, such as compound 34 exhibited an inactivation activity of 90.1% and curative activity of 51.8% and compound 28 exhibited a curative activity of 54.8% at 500 μg mL-1, which is equivalent to that of the commercial ningnanmycin (inactivation of 91.9% and curative of 51.9%). Moreover, the in vitro antibacterial activity test illustrated that compounds 2, 22, and 33 showed much higher activities than commercial thiodiazole copper, which could be used as lead compounds or potential candidates. The findings of transmission electron microscopy and molecular docking indicated that the synthesized compounds exhibited strong and significant binding affinity to the TMV coat protein and could obstruct the self-assembly and increment of TMV particles. This study revealed that α-ketoamide derivatives bearing a vanillin skeleton could be used as a novel potential pesticide for controlling the plant diseases.

HUKUM DAN KEKERASAN DI SEKOLAH: OPTIMALISASI PERAN KONSELOR SEKOLAH

Violence in the school environment is still a problem that requires multi-sectoral solutions. The school is an organization as a place to gather for a long time. Interactions in schools are multistrata interactions such as differences in the social backgrounds of students, teachers, and education personnel. The method used in this article is literature review. The results of the study in this study are school counselors have an important role in developing social attitudes of school residents with programmatic counseling activities. The counseling program is implemented to provide rights and obligations for school residents. By having a social attitude, conflicts between school members can be prevented. Counseling activities are organized as preventive and curative activities from violence in schools.

Control of major citrus postharvest diseases by sulfur-containing food additives

Sodium metabisulfite (SMBS), potassium metabisulfite (PMBS), aluminum sulfate (AlS) and aluminum potassium sulfate (AlPS), common sulfur-containing salts used as food additives, were evaluated for their antifungal activity against Penicillium digitatum, Penicillium italicum and Geotrichum citri-aurantii, the most economically important pathogens causing postharvest diseases of citrus fruits. In vitro radial mycelial growth was measured on potato dextrose agar (PDA) Petri dishes amended with five different concentrations of the salts (10, 20, 30, 50, 100 mM) after 7 d of incubation at 25 °C. SMBS and PMBS at all concentrations, and AIS and AIPS above 20 mM, completely inhibited the growth of these fungi. The curative antifungal activity of the four salts to control citrus green (GM) and blue (BM) molds and sour rot (SR) was evaluated on ‘Valencia’ oranges artificially inoculated in rind wounds with P. digitatum, P. italicum and G. citri-aurantii, respectively. In vivo primary screenings showed no significant antifungal activity of AlS and AlPS to control the three diseases at any dose tested, but SMBS and PMBS reduced the incidence and severity of GM, BM and SR at various concentrations. Effective salts and concentrations were selected for in vivo dip treatments in small-scale trials. Dips at room temperature (20 °C) in SMBS and PMBS at 20 and 50 mM for 60 or 120 s significantly reduced the incidence and severity of GM and BM, with PMBS at 50 mM for 120 s the most effective treatment. Conversely, dips in SMBS and PMBS at 50 mM for 60 or 120 s did not reduce SR incidence and severity. SMBS and PMBS treatments are potentially new tools to be included in reduced-risk non-polluting strategies to control Penicillium diseases, but not SR, on citrus fruits.

Curative Fungicide Activity Against Calonectria pseudonaviculata, the Boxwood Blight Pathogen1

Abstract Azoxystrobin, azoxystrobin plus benzovindiflupyr, kresoxim-methyl, propiconazole, pyraclostrobin, pyraclostrobin plus fluxapyroxad, tebuconazole, tetraconazole, thiophanate-methyl, and triflumizole fungicides were evaluated for curative and anti-sporulant activity against boxwood blight caused by Calonectria pseudonaviculata on detached leaves and whole boxwood plants (Buxus spp.). Pretreating detached leaves with 30 or 300 ppm a.i. 24 h prior to inoculation reduced disease compared to the untreated control for all fungicides. Fungicides were also applied 24 to 96 h post-inoculation. Only propiconazole reduced diseased leaf incidence to at least half of the control. When leaves were treated post-infection with 300 ppm propiconazole, tetraconazole, tebuconazole, or triflumizole, the pathogen did not sporulate over 2 wks. Propiconazole also reduced the percent of leaf area diseased; lesions were nearly 80% smaller with 300 ppm applied 48 h after inoculation. ‘True Dwarf' boxwood plants treated with 450 ppm thiophanate-methyl, 120 ppm pyraclostrobin or 150 ppm propiconazole 48 h after inoculation demonstrated that only propiconazole reduced the number of diseased leaves, blight lesions and the frequency of pathogen re-isolation. Experiments with ‘Green Mound' and ‘Green Mountain' boxwood cultivars and additional fungicides applied 48 h after inoculation demonstrated that propiconazole at 300 ppm, pyraclostrobin plus fluxapyroxad (150 ppm each) and azoxystrobin (135 ppm) plus benzovindiflupyr (67.5 ppm) reduced disease. Index words: fungicide management, Buxus, chemical disease management Chemicals used in this study: azoxystrobin (Heritage 50 WG), azoxystrobin plus benzovindiflupyr (Mural 30, 50 WG), kresoxim-methyl (Cygnus 50 WG), propiconazole (ProCon-Z 14.3 L), pyraclostrobin (Insignia 20 WG), pyraclostrobin plus fluxapyroxad (Orkestra Intrinsic 21.26 SC), tebuconazole (Torque 38.7 SC), tetraconazole (Minerva 11.6 SC), thiophanate-methyl (3336 50% WP), triflumizole (Procure 480 SC). Species used in this study: boxwood (Buxus L.), boxwood blight (Calonectria pseudonaviculata (Crous, J.Z. Groenew. &amp; C.F. Hill) L. Lombard, M. J. Wingf. &amp; Crous.

Social Curation Experience: Towards Authentic Learning in Preservice Teacher Training

The purpose of this research was to characterize the curation activity of preservice teachers practicing digital curation by constructing “knowledge exhibitions” in an academic course. Our database included 64 knowledge exhibitions on the Scoop.it platform. Factor analysis of curator’s activities resulted in 3 factors, contributing 57.63% of the total variance explained: the social factor, the personal content factor and the personal process factor. Narratives of curators’ reflections were analyzed using content analysis, resulting in 3 additional categories: relevance, curator activities and products. When combining the qualitative and quantitative categories, a two-dimensional conceptual model was constructed. The model illustrates a taxonomy of components that are included in the curation process, which portrays authentic learning. We conclude that curation contributes to the improvement of students’ knowledge and 21st skills as curators. Curation requires personal and social skills, e.g., cognitive and meta-cognitive skills from an individual and social perspective, social skills on social media and affective skills. Hence, while focusing on personal skills in constructing an ontology, curation is also social in nature. Using social curation transforms learning, but surprisingly is uncommon in educational settings, and research is consequently meager. This highlights the need for incorporating curation as authentic learning in teacher training.

The relationship between features enabling SDHI fungicide binding to the Sc-Sdh complex and its inhibitory activity against Sclerotinia sclerotiorum.

A new generation of succinate dehydrogenase inhibitors (SDHIs) with high efficiency and broad-spectrum antifungal activity has been frequently used in crop production. Sclerotinia stem rot is a major disease of various plants and crops caused by Sclerotinia sclerotiorum. Although benzovindiflupyr and isopyrazam reportedly have high activity against S. sclerotiorum, little is known about the bioactivity of different SDHIs classes against S. sclerotiorum or the mechanism of their differential antifungal activity. The in vitro tests revealed that the pyrazole-4-carboxamides of SDHIs (benzovindiflupyr, isopyrazam, fluxapyroxad, pydiflumetofen) had the highest activity against S. sclerotiorum followed by pyridine carboxamides (boscalid), pyridinyl-ethyl benzamides (fluopyram) and thiazole carboxamides (thifluzamide), and of these thifluzamide showed poor antifungal activity with EC50 values greater than 6.01 mg L-1 . The pyrazole-4-carboxamides of SDHIs showed satisfactory protective and curative activity against Sclerotinia stem rot. After treatment with the pyrazole-4-carboxamides of SDHIs, mitochondrial function in S. sclerotiorum decreased significantly. The enzyme activity assays revealed a lower affinity between thifluzamide and the Sc-Sdh complex than was observed for the other six fungicides, with IC50 values ranging from 0.0036 to 1.2088 μmol L-1 . Additionally, the docking positions of fungicides were similar, yet binding energies were different in the docking study with the Sdh complex. The correspondingly weaker hydrogen bonds may be responsible for the poor activity of thifluzamide against S. sclerotiorum. Understanding different binding features of various SDHIs classes with the Sc-Sdh complex might be beneficial for the design and development of highly effective broad-spectrum fungicides to ensure high yield and quality in crops by reducing fungicide use. © 2020 Society of Chemical Industry.

Discovery of novel bis-sulfoxide derivatives bearing acylhydrazone and benzothiazole moieties as potential antibacterial agents

On the basis of the active substructure combination principle, 24 novel synthesis of novel bis-sulfoxide derivatives bearing acylhydrazone and benzothiazole moieties as potential antibacterial agents were designed and synthesized. The bioactivity assay results showed that many compounds had significant in vitro inhibitory effects against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas citri pv. citri (Xac). Notably, compound 4b had the best in vitro antibacterial activity against Xoo at an half-maximal effective concentration value of 11.4 μg/mL, which was superior to those of thiodiazole copper (TDC) and bismerthiazol (BMT). Compared with TDC and BMT, compound 4b was more effective in vivo controlling rice bacterial leaf blight with curative and protection activities of 42.5% and 40.3%, respectively. In addition, compound 4b can influence biofilm formation, inhibit extracellular polysaccharide production, and ultimately reduce the pathogenicity of Xoo. All the results indicated that bis-sulfoxide derivatives bearing acylhydrazone and benzothiazole moieties can be used for the development of small-molecule pesticides with high antibacterial activity.

Novel sulfone derivatives containing a 1,3,4-oxadiazole moiety: design and synthesis based on the 3D-QSAR model as potential antibacterial agent.

The rice bacterial leaf blight (BLB) is one of the most serious bacterial diseases caused by Xanthomonas oryzae pv. oryzae (Xoo), which can cause yield loss of rice up to 50%. The three-dimensional quantitative structure-activity relationship (3D-QSAR) is an important auxiliary method to find potential high-efficient pesticides active structures. A series of novel 1,3,4-oxadiazole compounds were designed and synthesized based on the 3D-QSAR model, and their antibacterial activities in vitro against Xoo were evaluated. The results indicated that all the target compounds showed excellent in vitro antibacterial activities. For example, the compounds 6, 12, 13, 20, 21, and 23 exhibited excellent antibacterial activities against Xoo, with half-maximal effective concentration (EC50 ) values of 0.24, 0.31, 0.36, 0.29, 0.19, and 0.31 mg/L, respectively, which were superior to the antibacterial agents thiodiazole copper (127.44 mg/L) and bismerthiazol (91.08 mg/L). Meanwhile, compound 21 showed good antibacterial activity in vivo against BLB, with curative and protective activities of 46.7% and 56.4%, respectively, which were superior to thiodiazole copper (28.5% and 32.5%) and bismerthiazol (37.6% and 38.4%). Compound 21 can significantly reduce the extracellular polysaccharides production of Xoo, increase the permeability of the cell membranes, and also can cause cell surface wrinkles, deformation and dryness. The 3D-QSAR model can be used to find sulfone compounds containing a 1,3,4-oxadiazole moiety with higher antibacterial activity, and compound 21 can be used as a potential antibacterial agent in the future. © 2020 Society of Chemical Industry.