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1.
Chem Biodivers ; : e202400831, 2024 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-39005105

RESUMEN

5-(Cyanomethyl)-3-((5,5-dimethyl-3-oxocyclohex-1-en-1-yl)amino)-1H-pyrazole-4-carbonitrile (3) is used as a key for the synthesis of arylidenes 5a-fvia its reaction with some aldehydes 4a-f. 5-[(5,5-Dimethyl-3-oxocyclohex-1-en-1-yl)amino]-3-(2-imino-2H-chromen-3-yl)-1H-pyrazole-4-carbonitrile (7) was synthesized via the reaction of compound (3) with 2-hydroxybenzaldehyde in EtOH/piperidine. The target compounds were tested against cotton leafworm larvae in their second and fourth instar. The available data demonstrated that the LC50 values for commercial phenylpyrazole were 3.37 mg/L and 4.55 mg/L for the most affected synthesized compound, 5b. The chemical structure of compound 5b has two cyano moieties, a pyrazole ring and a chlorophenyl, which may be increasing it efficiency. Evaluation of the latent effects of the examined synthesized compounds on various biological parameters, including adult longevity, pupal weight, proportion of normal, deformed pupae, adult emergency, fecundity, and egg hatchability, was done in an additional effort to slightly improve insecticidal compounds. Twelve synthesized compounds were subjected to a molecular docking analysis against glutamate-activated chloride channels. Twelve artificial compounds with the PDB ID of 4COF were subjected to a molecular docking study against the gamma-aminobutyric acid receptor (GABA).

2.
J Agric Food Chem ; 2024 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-39052523

RESUMEN

Ethyl 5-cyano-1,6-dihydro-2-methyl-4-(2'-thienyl)-6-thioxonicotinate (A) was synthesized and reacted with ethyl chloroacetate in the presence of sodium acetate or sodium carbonate to give ethyl 5-cyano-6-((2-ethoxy-2-oxoethyl)thio)-2-methyl-4-(2'-thienyl)nicotinate (1a) or its isomeric thieno[2,3-b]pyridine 2a. 3-Aminothieno[2,3-b]pyridine-2-carboxamide 2b was also synthesized by the reaction of A with 2-chloroacetamide. The reaction of 1a with hydrazine hydrate in boiling ethanol gave acethydrazide 3. Heating ester 1a with hydrazine hydrate under neat conditions afforded 3-amino-1H-pyrazolo[3,4-b]pyridine 10. Compounds 2b, 3, and 10 were used as precursors for synthesizing other new thieno[2,3-b]pyridines and pyrazolo[3,4-b]pyridines containing mainly the ethyl nicotinate scaffold. Structures of all new compounds were confirmed by elemental and spectral analyses. Most of the obtained compounds were evaluated for their insecticidal activity toward the nymphs and adults of Aphis gossypii (Glover,1887). Some compounds such as 4, 9b, and 9c showed promising results. The effect of some sublethal concentrations, less than LC50, of compounds 4, 9b, and 9c on the examined Aphis was subjected to a further study. The results demonstrated that exposure of A. gossypii nymphs to sublethal concentrations of compounds 4, 9b, and 9c had noticeable effects on their biological parameters, i.e., nymphal instar duration, generation time, and adult longevity. The highest concentration C1 of all three compounds increased the nymphal instar duration and generation time and decreased adult longevity and vice versa.

3.
Chem Biodivers ; : e202401310, 2024 Jul 22.
Artículo en Inglés | MEDLINE | ID: mdl-39037938

RESUMEN

In this work, a novel series of N-(arylcarbamothioyl)arylmide) 2-11 were synthesized by treating One-Pot three-multicomponent of Aroyl chloride ammonium isothiocyanate and amine compounds under refluxing conditions. Using spectroscopic methods, the chemical structure of the novelty developed compounds were investigated. After five days, the proposed derivatives' insecticidal bioassay was assessed using the median lethal concentration (LC50) against the second & fourth larvae of Spodoptera frugiperda as toxicity agents. The findings showed that, to varying degrees, every tested substance exerted insecticidal effects on S. frugiperda larvae in both of their instars. Compound 9 was the most poisonous of them all, having an LC50 against larvae in their second and fourth instars of 60.45 and 123.21 mg/L, respectively. Additionally, a few biological and biochemical characteristics of the substances that were generated in a lab setting were also looked at. Furthermore, this work discusses how to discover novel compounds that may one day be employed as insecticidal agents. Finally, all the designed components were monitored for their antibacterial effectiveness toward both Gram-positive & Gram-negative bacteria.

4.
Anal Biochem ; 694: 115624, 2024 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-39029643

RESUMEN

Nitro fatty acids (NO2-FAs) are biologically active compounds produced from the reaction of unsaturated fatty acids with reactive nitrogen species (RNS). Due to their electrophilic nature, these endogenously produced metabolites can react with nucleophilic targets, producing a spectrum of modulatory and protective effects. Determination of NO2-FAs in biological samples is challenging due to their low nanomolar to picomolar endogenous concentrations, indistinct metabolism, and distribution in many tissues and biofluids. Several attempts have been made to develop precise, standardized, and efficient methodologies for assessing physiological and pathophysiological processes to overcome the difficulties associated with their measurement. This review discusses those approaches utilizing liquid chromatography tandem mass spectrometry (LC‒MS/MS) and gas chromatography tandem mass spectrometry (GC‒MS/MS) for the quantification of NO2-FAs, in addition to a summary of their laboratory synthesis and extraction from biological samples. Clinical associations with different pathological conditions, including hyperlipidaemia, cardiac ischemia and herpes simplex type 2 viral infection (HSV-2), are also discussed.

5.
Heliyon ; 10(11): e31086, 2024 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-38832266

RESUMEN

The success of industrial operations depends on the effective identification, appraisal, and mitigation of possible hazards and associated environmental concerns. This report provides a complete review of environmental management techniques at the Sukari Gold Mine (SGM), located in the southeastern desert of Egypt. Extensive environmental measurements were taken to assess air and water quality, identify hazards, and analyze risks on the SGM premises. Air quality and noise intensity levels were measured at 39 places around the mine's working region. The findings found noncompliance with the Egyptian Environmental Law's (EEL4/94) noise exposure limitations, with the Power Generator House having the maximum noise levels at 107 dB. Remedial measures such as personal protective equipment (PPE) and exposure limit reduction strategies are being considered to address elevated noise levels. Measurements of particulate matter (PM10) and noxious gases (e.g., CO, SO2, NO2, HCN, and NH3) were conducted in workplace and ambient environments. Elevated PM10 concentrations were particularly concerning in underground regions, forcing the deployment of water depression techniques and improved PPE measures. While gas emissions from most activities remained under regulatory limits, select zones showed hydrogen cyanide (HCN) levels that exceeded permitted thresholds, necessitating specific control actions. Using hazard index (HI) and risk rating assessments, this study found different risk profiles across SGM's workplaces, focusing on high-risk regions for focused intervention. Additionally, a water assessment near a Tailing Storage Facility (TSF) was conducted to monitor the impact of mining activities on groundwater quality. The study revealed that groundwater in the region belongs to the Na-K-Cl-SO4 and Ca-Mg-Cl-SO4 water classes, with potential degradation attributed to high mineralization processes induced by aquifer materials and seawater intrusion. The findings underscore the importance of ongoing monitoring, control measures, and implementation of programs to ensure environmental sustainability and minimize risks associated with mining activities in the Sukari Gold Mines. This research highlights the imperative of continuous monitoring, proactive control measures, and the implementation of environmental initiatives to ensure the sustainability of mining operations within the Sukari Gold Mines.

6.
Chem Biodivers ; : e202400948, 2024 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-38899798

RESUMEN

Due to its severe damage, Spodoptera frugiperda is receiving attention as one of the biggest dangers to world food security. Although there are numerous insecticides that are widely and successfully used to control S. frugiperda, they do not have an immediate effect. In our work focusing for synthesized twelve novel benzamide derivatives and examined their insecticidal effectiveness against S. frugiperda larvae in their second & fourth larvae instars, with the aim of further improving the insecticidal activity based on combination principles. Several spectroscopic methods, including elemental analysis, NMR & infrared spectroscopy, were employed for confirming the structure of the newly designed products. It has been discovered that most compounds show good of promising efficacy. With an LC50 of 24.8 mg/L for larvae in the second instar & 56.2 mg/L for larvae in the fourth instar, compound 23 was the most active. Among all compounds 11, 22 and 20 exhibited excellent results. Furthermore, a number of biological and histopathological properties of the demonstration compounds of the produced goods under laboratory conditions were also examined. This work further demonstrates the anti-proliferation of S. frugiperda and offers fresh ideas for the manufacture of benzamide derivatives.

7.
Microvasc Res ; 154: 104695, 2024 07.
Artículo en Inglés | MEDLINE | ID: mdl-38723843

RESUMEN

Exosomes are nanosized vesicles that have been reported as cargo-delivering vehicles between cells. Müller cells play a crucial role in the pathogenesis of diabetic retinopathy (DR). Activated Müller cells in the diabetic retina mediate disruption of barrier integrity and neovascularization. Endothelial cells constitute the inner blood-retinal barrier (BRB). Herein, we aim to evaluate the effect of Müller cell-derived exosomes on endothelial cell viability and barrier function under normal and hyperglycemic conditions. Müller cell-derived exosomes were isolated and characterized using Western blotting, nanoparticle tracking, and electron microscopy. The uptake of Müller cells-derived exosomes by the human retinal endothelial cells (HRECs) was monitored by labeling exosomes with PKH67. Endothelial cell vitality after treatment by exosomes under normo- and hypoglycemic conditions was checked by MTT assay and Western blot for apoptotic proteins. The barrier function of HRECs was evaluated by analysis of ZO-1 and transcellular electrical resistance (TER) using ECIS. Additionally, intracellular Ca+2 in HRECs was assessed by spectrofluorimetry. Analysis of the isolated exosomes showed a non-significant change in the number of exosomes isolated from both normal and hyperglycemic condition media, however, the average size of exosomes isolated from the hyperglycemic group showed a significant rise when compared to that of the normoglycemic group. Müller cells derived exosomes from hyperglycemic condition media markedly reduced HRECs cell count, increased caspase-3 and Annexin V, decreased ZO-1 levels and TER, and increased intracellular Ca+ when compared to other groups. However, treatment of HRECs under hyperglycemia with normo-glycemic Müller cells-derived exosomes significantly decreased cell death, preserved cellular integrity and barrier function, and reduced intracellular Ca+2. Collectively, Müller cell-derived exosomes play a remarkable role in the pathological changes associated with hyperglycemia-induced inner barrier dysfunction in DR. Further in vivo research will help in understanding the role of exosomes as therapeutic targets and/or delivery systems for DR.


Asunto(s)
Apoptosis , Barrera Hematorretinal , Supervivencia Celular , Retinopatía Diabética , Células Endoteliales , Células Ependimogliales , Exosomas , Exosomas/metabolismo , Retinopatía Diabética/metabolismo , Retinopatía Diabética/patología , Retinopatía Diabética/fisiopatología , Células Ependimogliales/metabolismo , Células Ependimogliales/patología , Humanos , Células Endoteliales/metabolismo , Células Endoteliales/patología , Barrera Hematorretinal/metabolismo , Barrera Hematorretinal/patología , Células Cultivadas , Proteína de la Zonula Occludens-1/metabolismo , Permeabilidad Capilar , Señalización del Calcio , Línea Celular , Vasos Retinianos/metabolismo , Vasos Retinianos/patología , Vasos Retinianos/fisiopatología
8.
J Agric Food Chem ; 72(20): 11369-11380, 2024 May 22.
Artículo en Inglés | MEDLINE | ID: mdl-38727083

RESUMEN

In keeping with our investigation, a simple and practical synthesis of novel heterocyclic compounds with a sulfamoyl moiety that can be employed as insecticidal agents was reported. The compound 2-hydrazinyl-N-(4-sulfamoylphenyl)-2-thioxoacetamide 1 was coupled smoothly with triethylorthoformate or a variety of halo compounds, namely phenacyl chloride, chloroacetyl chloride, chloroacetaldehyde, chloroacetone, 1,3-dichloropropane, 1,2-dichloroethane, ethyl chloroformate, 2,3-dichloro-1,4-naphthoquinone, and chloroanil respectively, which afforded the 1,3,4-thiadiazole and 1,3,4-thiadiazine derivatives. The new products structure was determined using elemental and spectral analysis. Under laboratory conditions, the biological and toxicological effects of the synthetic compounds were also evaluated as insecticides against Spodoptera littoralis (Boisd.). Compounds 3 and 5 had LC50 values of 6.42 and 6.90 mg/L, respectively. The investigated compounds (from 2 to 11) had been undergoing molecular docking investigation for prediction of the optimal arrangement and strength of binding between the ligand (herein, the investigated compounds (from 2 to 11)) and a receptor (herein, the 2CH5) molecule. The binding affinity within docking score (S, kcal/mol) ranged between -8.23 (for compound 5), -8.12 (for compound 3) and -8.03 (for compound 9) to -6.01 (for compound 8). These compounds were shown to have a variety of binding interactions within the 2CH5 active site, as evidenced by protein-ligand docking configurations. This study gives evidence that those compounds have 2CH5-inhibitory capabilities and hence may be used for 2CH5-targeting development. Furthermore, the three top-ranked compounds (5, 3, and 9) and the standard buprofezin were subjected to density functional theory (DFT) analysis. The highest occupied molecular orbital-lowest unoccupied molecular orbital (HOMO-LUMO) energy difference (ΔE) of compounds 5, 3, and 9 was found to be comparable to that of buprofezin. These findings highlighted the potential and relevance of charge transfer at the molecular level.


Asunto(s)
Diseño de Fármacos , Insecticidas , Simulación del Acoplamiento Molecular , Spodoptera , Tiadiazinas , Tiadiazoles , Animales , Insecticidas/química , Insecticidas/síntesis química , Insecticidas/farmacología , Spodoptera/efectos de los fármacos , Tiadiazoles/química , Tiadiazoles/farmacología , Tiadiazoles/síntesis química , Tiadiazinas/química , Tiadiazinas/farmacología , Tiadiazinas/síntesis química , Relación Estructura-Actividad , Sulfonamidas/química , Sulfonamidas/farmacología , Sulfonamidas/síntesis química , Proteínas de Insectos/química , Bencenosulfonamidas , Estructura Molecular , Anhidrasa Carbónica II/antagonistas & inhibidores , Anhidrasa Carbónica II/metabolismo , Anhidrasa Carbónica II/química
9.
Cancer Cell Int ; 24(1): 136, 2024 Apr 16.
Artículo en Inglés | MEDLINE | ID: mdl-38627665

RESUMEN

BACKGROUND: Hydrogen sulfide (H2S) is a significant endogenous mediator that has been implicated in the progression of various forms of cancer including breast cancer (BC). Cystathionine-ß-synthase (CBS), cystathionine-γ-lyase (CSE), and 3-mercaptopyruvate sulfurtransferase (3MST) are the three principal mammalian enzymes responsible for H2S production. Overexpression of CBS, CSE and 3MST was found to be associated with poor prognosis of BC patients. Moreover, H2S was linked to an immune-suppressive tumor microenvironment in BC. Recently it was observed that BC cells, in response to single or dual inhibition of H2S synthesizing enzymes, develop an escape mechanism by overexpressing alternative sources of H2S generation. Thus, the aim of this work is to escape the H2S compensatory mechanism by pan repressing the three enzymes using microRNAs (miRNAs) and to investigate their impact on the oncogenic and immunogenic profile of BC cells. METHODS: BC female patients (n = 25) were recruited. In-silico analysis was used to identify miRNAs targeting CBS, CSE, and 3MST. MDA-MB-231 cells were cultured and transfected using oligonucleotides. Total RNA was extracted using Biazol, reverse transcribed and quantified using qRT-PCR. H2S levels were measured using AzMc assay. BC hallmarks were assessed using trans-well migration, wound healing, MTT, and colony forming assays. RESULTS: miR-193a and miR-548c were validated by eight different bioinformatics software to simultaneously target CBS, CSE and 3MST. MiR-193a and miR-548c were significantly downregulated in BC tissues compared to their non-cancerous counterparts. Ectopic expression of miR-193a and miR-548c in MDA-MB-231 TNBC cells resulted in a marked repression of CBS, CSE, and 3MST transcript and protein levels, a significant decrease in H2S levels, reduction in cellular viability, inhibition of migration and colony forming ability, repression of immune-suppressor proteins GAL3 GAL9, and CD155 and upregulation of the immunostimulatory MICA and MICB proteins. CONCLUSION: This study sheds the light onto miR-193a and miR-548c as potential pan-repressors of the H2S synthesizing enzymes. and identifies them as novel tumor suppressor and immunomodulatory miRNAs in TNBC.

10.
Chem Biodivers ; 21(6): e202400451, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38556464

RESUMEN

Five types of heterocyclic compounds containing trifloromethylpyridine scaffold namely; 3-cyano-2-(N-phenyl)carbamoylmethylthio-6-(thiophen-2-yl)-4-trifluoromethyl-pyridine (6a), thieno[2,3-b]pyridines 3-5 and 7a-c, pyrido[3',2':4,5]thieno[3,2-d] pyrimidines 8-13 and 15a-c, pyrido[3',2':4,5]thieno[3,2-d][1,2,3]triazines 16a,b, and 9-(thiophen-2-yl)-7-(trifluoromethyl) pyrido [3',2':4,5]thieno[2,3-e][1,2,4]triazolo[1,5-c]pyrimidine (14) were synthesized in excellent yields and very pure state. The structures of these compounds were confirmed by elemental and spectral analyses. Most of the synthesized compounds were evaluated as insecticidal agents toward Aphis gossypii insects and promising results obtained. Among all tested compounds, only 6, 7a, 7c and 15c being the most potent compounds against nymphs and adults of Aphis gossypii and their activities are nearly to that of acetamiprid as a reference. The effect of 6a compounds 7a, 7c and 15c on the Aphis digestive system from histological point of view was also included.


Asunto(s)
Áfidos , Compuestos Heterocíclicos , Insecticidas , Piridinas , Animales , Insecticidas/química , Insecticidas/farmacología , Insecticidas/síntesis química , Piridinas/química , Piridinas/síntesis química , Compuestos Heterocíclicos/química , Compuestos Heterocíclicos/síntesis química , Compuestos Heterocíclicos/farmacología , Áfidos/efectos de los fármacos , Relación Estructura-Actividad , Estructura Molecular
11.
JAMA Neurol ; 2024 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-38436973

RESUMEN

Importance: Stroke is a leading cause of death and disability in the US. Accurate and updated measures of stroke burden are needed to guide public health policies. Objective: To present burden estimates of ischemic and hemorrhagic stroke in the US in 2019 and describe trends from 1990 to 2019 by age, sex, and geographic location. Design, Setting, and Participants: An in-depth cross-sectional analysis of the 2019 Global Burden of Disease study was conducted. The setting included the time period of 1990 to 2019 in the US. The study encompassed estimates for various types of strokes, including all strokes, ischemic strokes, intracerebral hemorrhages (ICHs), and subarachnoid hemorrhages (SAHs). The 2019 Global Burden of Disease results were released on October 20, 2020. Exposures: In this study, no particular exposure was specifically targeted. Main Outcomes and Measures: The primary focus of this analysis centered on both overall and age-standardized estimates, stroke incidence, prevalence, mortality, and DALYs per 100 000 individuals. Results: In 2019, the US recorded 7.09 million prevalent strokes (4.07 million women [57.4%]; 3.02 million men [42.6%]), with 5.87 million being ischemic strokes (82.7%). Prevalence also included 0.66 million ICHs and 0.85 million SAHs. Although the absolute numbers of stroke cases, mortality, and DALYs surged from 1990 to 2019, the age-standardized rates either declined or remained steady. Notably, hemorrhagic strokes manifested a substantial increase, especially in mortality, compared with ischemic strokes (incidence of ischemic stroke increased by 13% [95% uncertainty interval (UI), 14.2%-11.9%]; incidence of ICH increased by 39.8% [95% UI, 38.9%-39.7%]; incidence of SAH increased by 50.9% [95% UI, 49.2%-52.6%]). The downturn in stroke mortality plateaued in the recent decade. There was a discernible heterogeneity in stroke burden trends, with older adults (50-74 years) experiencing a decrease in incidence in coastal areas (decreases up to 3.9% in Vermont), in contrast to an uptick observed in younger demographics (15-49 years) in the South and Midwest US (with increases up to 8.4% in Minnesota). Conclusions and Relevance: In this cross-sectional study, the declining age-standardized stroke rates over the past 3 decades suggest progress in managing stroke-related outcomes. However, the increasing absolute burden of stroke, coupled with a notable rise in hemorrhagic stroke, suggests an evolving and substantial public health challenge in the US. Moreover, the significant disparities in stroke burden trends across different age groups and geographic locations underscore the necessity for region- and demography-specific interventions and policies to effectively mitigate the multifaceted and escalating burden of stroke in the country.

12.
PLOS Glob Public Health ; 4(3): e0001904, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38470940

RESUMEN

Diabetes remains one of the four major causes of morbidity and mortality globally among non-communicable diseases (NCDs. It is predicted to increase in sub-Saharan Africa by over 50% by 2045. The aim of this study is to identify, map and estimate the burden of diabetes in Ghana, which is essential for optimising NCD country policy and understanding existing knowledge gaps to guide future research in this area. We followed the Arksey and O'Malley framework for scoping reviews. We searched electronic databases including Medline, Embase, Web of Science, Scopus, Cochrane and African Index Medicus following a systematic search strategy. The Preferred Reporting Items for Systematic Reviews and Meta-Analyses Extension for Scoping Reviews was followed when reporting the results. A total of 36 studies were found to fulfil the inclusion criteria. The reported prevalence of diabetes at national level in Ghana ranged between 2.80%- 3.95%. At the regional level, the Western region reported the highest prevalence of diabetes: 39.80%, followed by Ashanti region (25.20%) and Central region at 24.60%. The prevalence of diabetes was generally higher in women in comparison to men. Urban areas were found to have a higher prevalence of diabetes than rural areas. The mean annual financial cost of managing one diabetic case at the outpatient clinic was estimated at GHS 540.35 (2021 US $194.09). There was a paucity of evidence on the overall economic burden and the regional prevalence burden. Ghana is faced with a considerable burden of diabetes which varies by region and setting (urban/rural). There is an urgent need for effective and efficient interventions to prevent the anticipated elevation in burden of disease through the utilisation of existing evidence and proven priority-setting tools like Health Technology Assessment (HTA).

13.
Sci Rep ; 14(1): 5769, 2024 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-38459064

RESUMEN

This paper introduces a planar antipodal meander line antenna fabricated using RO3003 substrate. The proposed antenna is designed to radiate in the end-fire direction, achieving a maximum measured gain of 10.43 dBi within its working bandwidth, which ranges from 2.24 GHz to 2.7 GHz, covering long-range WLAN/WiMAX applications. A systematic procedure is adopted in the design process to prove its tunability to cover other application requirements in terms of gain and bandwidth. The proposed design steps show that the bandwidth and the gain can independently be controlled by adjusting specific design parameters such as the number of radiators and the scaling factor. The antenna is fine-tuned using sensitivity analysis and parametric study to guarantee optimum operation at the desired bandwidth. Experimental measurements of the fabricated design demonstrate a high degree of correlation with simulations conducted using CST and HFSS. In comparison to other end-fire antennas presented in the literature, the proposed design manifests its capability to provide high gain for WLAN/WiMAX nodes connectivity. The measurements show that the proposed traveling wave antenna exhibits a high radiation efficiency with maximum value of 99.8% at 2.35 GHz. The measured side lobe level is found to be below - 18 dB and - 20 dB at 2.45 GHz along the E - and H -planes, respectively. Apart from its excellent radiation performance, the antenna is characterized by its low profile and fabrication simplicity.

14.
Chem Biodivers ; 21(4): e202400218, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38381590

RESUMEN

Certain 2-amino-6-alkoxy-4-arylpyridine-3,5-dicyanide 1a-e were prepared via a straightforward process using microwave technology rather than conventional methods. This involved reaction of arylidenemalononitrile thru propanedinitrile in the occurrence of sodium alkoxide under MW. While, their positional isomer 4-amino-6-alkoxy-2-arylpyridine-3,5-dicyanide 3a-j have been separated from the reaction of aryl aldehydes with 2-aminoprop-1-ene-1,1,3-tricarbonitrile 2 in the presence of sodium alkoxide using microwave technic. Furthermore, the insecticidal properties of all synthesized compounds were observed with respect to Cotton aphid nymphs and adults. Neonicotinoid pesticides are indicated as the most effective pesticides toward aphids and many other pests. Many insecticides are discovered as novelties. As a result, several pyridine compounds were chemical method synthesized to serve as equivalents of neonicotinoids, a broad class of insecticides. With LC50 value of 0.03 mg/L, components 3g exhibit the highest insecticidal bioactivity. This work discusses how to find new chemicals that could be used as insecticidal agents in the future.


Asunto(s)
Alcoholes , Áfidos , Insecticidas , Animales , Insecticidas/química , Microondas , Neonicotinoides/farmacología , Sodio/farmacología
15.
Water Sci Technol ; 89(4): 841-858, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38423604

RESUMEN

The most important information required to successfully issue a flood warning is the quantitative precipitation forecasts (QPFs). This is important to run subsequent rainfall-runoff simulations. A rainfall-runoff simulation derives its accuracy mainly from the accuracy of the input QPFs. The dynamically based global numerical weather prediction models (NWPMs) are strong candidate sources of QPFs. A main problem is the real-time selection of which NWPM should be used to provide the QPFs for flood warning simulations. This paper develops an automated technique to solve this problem. The technique performs real-time comparisons with measured rainfall fields using a novel 'tolerant' hydrologic approach. The 'tolerant' approach performs the comparison on the basin scale and allows for timing shifts in the forecasts. This is because QPFs can be good but only a few hours early or late. Two events are used for illustration, and the proposed real-time application in flood warning is presented. The developed technique, employing the tolerant approach, could eliminate the effects of the timing shifts and, accordingly, succeeded to select the QPFs to be used. A Python package was developed for automation. The developed technique is expected to also be useful for offline assessments of historical performances of NWPMs.


Asunto(s)
Inundaciones , Lluvia , Tiempo (Meteorología) , Simulación por Computador , Hidrología
16.
Saudi J Biol Sci ; 31(2): 103894, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38205263

RESUMEN

Because of its high degree of biodegradability, chitosan is widely used as a component in food packaging. However, its poor physical properties, such as permeability, limit its applicability. Consequently, applying nano chitosan is regarded as the most effective solution to this issue. In the current study, we studied the effect of using different materials in the coating process on the quality of "Murcott" mandarin during cold storage. We used different concentrations of nano chitosan (50 and 100 ppm) without wax and 100 ppm nano chitosan with wax. We investigated the impact of these compounds on the chemical composition and quality of fruits. The most successful treatment for preventing weight loss from discarded fresh fruit was a combination of wax and 100 ppm nano chitosan. This combination also prevented the deterioration of vitamin C, maintained the fruit pulp, and preserved the fruit's superior taste during cold storage and shelf life. It also maintains a better total soluble solids and total acidity level than other treatments. In addition, the activity of antioxidant enzymes and the total number of antioxidants indicates no degradation of plant tissues compared to those not coated with nano chitosan. It also reduces the microbial load on the coated fruits. Consequently, this coating combination could suggest prolonging post-harvest life and increasing the marketing period of mandarin fruits.

17.
Noncoding RNA ; 10(1)2024 Jan 18.
Artículo en Inglés | MEDLINE | ID: mdl-38250807

RESUMEN

Recently, myriad studies have defined the versatile abilities of gasotransmitters and their synthesizing enzymes to play a "Maestro" role in orchestrating several oncological and non-oncological circuits and, thus, nominated them as possible therapeutic targets. Although a significant amount of work has been conducted on the role of nitric oxide (NO) and carbon monoxide (CO) and their inter-relationship in the field of oncology, research about hydrogen sulfide (H2S) remains in its infancy. Recently, non-coding RNAs (ncRNAs) have been reported to play a dominating role in the regulation of the endogenous machinery system of H2S in several pathological contexts. A growing list of microRNAs (miRNAs) and long non-coding RNAs (lncRNAs) are leading the way as upstream regulators for H2S biosynthesis in different mammalian cells during the development and progression of human diseases; therefore, their targeting can be of great therapeutic benefit. In the current review, the authors shed the light onto the biosynthetic pathways of H2S and their regulation by miRNAs and lncRNAs in various oncological and non-oncological disorders.

18.
Chem Biodivers ; 21(2): e202301390, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38179826

RESUMEN

Overcoming or reducing the majority of difficulties caused by the use of common pesticides requires the use of developed, secure, unique and selective organic compounds. Due to their clear mechanism of action on pests and lower poisonousness towards vertebrates than conventional insecticides, juvenile hormone analogues as an example of insect growth regulators appear promising. Thus, a unique set of pure insect growth regulators has been synthesized. The structure of these synthesized compounds, which were related to the most well-known insect growth regulator insecticides, was confirmed by elemental and contemporary spectroscopic investigations (IR, UV, 1 H-NMR, 13 C NMR, and Dept 135 spectrum). Under laboratory conditions, the effectiveness of a chemically newly synthesized products was tested against the cotton mealybug, Phenacoccus solenopsis, and compared with Fenoxycarb as a reference insecticide. Compound 7 was discovered to be more effective than the other synthetic compounds, with LC50 values of 0.907 mg/L for adult female P. solenopsis and 0.377 mg/L for third instar nymphs. Furthermore, this results concluded that the adult female's stage of P. solenopsis was less sensitive to the checked treatments as matched to the third instar nymphs.


Asunto(s)
Hormigas , Hemípteros , Insecticidas , Animales , Femenino , Insecticidas/farmacología
19.
J Pept Sci ; 30(4): e3550, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37853814

RESUMEN

Antimicrobial peptides (AMPs) are promising alternatives to conventional antibiotics and chemotherapy in the treatment of multidrug-resistant pathogens and drug-resistant cancers. Clinical application of AMPs is limited due to low stability and inefficient transport. Encapsulation in nanocarriers may improve their therapeutic potential. Chitosan nanoparticles (CS-NPs) are efficient carriers for proteins and peptides, improving the treatment of microbial infections and targeted drug delivery. We examined toxicity against cancer cell lines and antibacterial activities of the pleurocidin-like AMP NRC-07 upon encapsulation in CS-NPs by ionotropic gelation. The biological activities of various formulations of free and encapsulated NRC-07 and free nanoparticles were evaluated against Pseudomonas aeruginosa and breast cancer cells, using assays for cell viability and lactate dehydrogenase cytolysis with non-cancer cell lines as controls. NRC-07-containing nanoparticles decreased the bacterial and cancer cell viability in a concentration-dependent manner. Activities of encapsulated peptide were >2-fold higher than those of free NRC-07 peptide. Unloaded CS-NPs and free peptide were not cytotoxic against control cells. Encapsulation of NRC-07 into CS-NPs enhanced the antibacterial and selective cytotoxicity of the peptide, possibly enhancing anticancer activities. Encapsulation presents a promising tool for the development of efficient drug delivery systems.


Asunto(s)
Quitosano , Nanopartículas , Neoplasias , Humanos , Quitosano/farmacología , Péptidos Antimicrobianos , Antibacterianos/farmacología , Péptidos/farmacología
20.
Chem Biodivers ; 21(1): e202301284, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38036947

RESUMEN

Unintentional environmental effects brought on by insecticides encourage the creation of safer substitutes. A very polyphagous migrating lepidopteran pest species in Africa called S. Frugiperda causes terrible damage. In the current paper, treatment of 4-acetylphenyl 4-methylbenzenesulfonate with different aromatic aldehydes in the presence of NaOH afforded benzylideneacetophenones. The structure of the newly prepared compounds were proved by different spectroscopic techniques such as IR, 1 H-NMR, 13 C NMR, and elemental analysis. We looked at the association between contact with S. frugiperda and stricture reaction to examine their harmful effect. Additionally, S. frugiperda was used for testing the newly created compounds for their ability to kill insects. The majority of substances have been proven to be effective and promising. It has been found that 4-[3-(4-Methylphenyl)prop-2-enoyl]phenyl-4-methyl benzenesulfonate (4) was the most active with an LC50 =3.46 mg/L of 2nd instar larvae and LC50 =9.45 mg/L of 4th instar larvae. Moreover, some of biological and histopathological aspects of the synthesized products were investigated under laboratory conditions.


Asunto(s)
Chalcona , Insecticidas , Animales , Insecticidas/farmacología , Spodoptera , Larva , Dosificación Letal Mediana
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