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1.
Actas urol. esp ; 48(3): 204-209, abr. 2024. tab
Artigo em Espanhol | IBECS | ID: ibc-231925

RESUMO

Objetivos Este estudio evalúa el impacto del uso de una vaina de acceso ureteral (VAU) durante la ureteroscopia flexible (URSf) para el tratamiento de la litiasis urinaria, centrándose en resultados como la tasa libre de litiasis, el tiempo quirúrgico y las complicaciones. Métodos Este estudio prospectivo y aleatorizado se llevó a cabo en el Hospital de Badr en la Universidad de Helwan y en los hospitales de la Universidad de Ain Shams, desde agosto de 2021 hasta agosto de 2022. Los pacientes se aleatorizaron sistemáticamente a 2 grupos (URSf con VAU: 33 pacientes y URSf sin VAU: 31 pacientes), y se sometieron a evaluaciones preoperatorias y postoperatorias, incluyendo pruebas de laboratorio y de imagen. Se controlaron los posibles riesgos asociados al procedimiento, como el fracaso en el acceso al cálculo, el dolor, el sangrado y la sepsis. Resultados Se observó que los 2 grupos eran comparables en cuanto a características demográficas o hallazgos preoperatorios de la litiasis (p>0,05 para todos). Sin embargo, el tiempo quirúrgico fue menor en el grupo tratado sin VAU (79,4±15,3 vs. 90,4±16,7min en el grupo tratado con VAU; p=0,008). Las tasas de complicaciones intraoperatorias, incluidos el fracaso del acceso, la interrupción de la operación, las lesiones ureterales y el sangrado, fueron comparables en ambos grupos (p>0,05). No se observaron diferencias significativas en cuanto a la tasa libre de litiasis postoperatoria (78,8 vs. 71,0%; p=0,305) y el tamaño litiásico residual medio (2,7±3,5 vs. 3,1±3,1mm; p=0,687). Conclusiones El presente estudio sugiere que URSf sin VAU puede ofrecer una opción eficiente e igualmente efectiva para el tratamiento de los cálculos renales y de uréter superior. Sin embargo, se necesitan más estudios con muestras de mayor tamaño y periodos de seguimiento más largos para validar estos resultados y establecer indicaciones más precisas para este procedimiento. (AU)


Objectives This study evaluates the impact of using an access sheath (AS) during flexible ureteroscopy (fURS) for urolithiasis treatment, focusing on outcomes such as stone-free rate, operation time, and complications. Methods This prospective, randomized study was carried out at Badr Hospital, Helwan University, and Ain Shams University hospitals from August 2021 to August 2022. Patients were systematically randomized into two groups (fURS with AS: 33 patients and without AS: 31 patients) and underwent preoperative and postoperative assessments, including lab tests and imaging. Possible procedure-associated risks, such as failed stone access, pain, bleeding, and sepsis, were monitored. Results The two groups were found to be comparable in terms of demographic characteristics or preoperative stone findings (P>.05 for all). However, operation duration was shorter in the No Sheath group (79.4±15.3minutes vs. 90.4±16.7minutes in the Sheath group, P=.008). Intraoperative complication rates, including failed access, operation termination, ureteric injury, and bleeding, were comparable in both groups (P>.05). Postoperative stone-free rates (78.8% vs. 71.0%, P=.305) and mean residual stone size (2.7±3.5mm vs. 3.1±3.1mm, P=.687) showed no significant differences. Conclusions The present study suggests that fURS without an access sheath may offer an efficient and equally effective option for managing upper ureteric and renal stones. However, more studies with larger sample sizes and longer follow-up periods are required to validate these findings and to establish more precise indications for this approach. (AU)


Assuntos
Humanos , Masculino , Feminino , Ureteroscopia/instrumentação , Ureteroscopia/métodos , Urolitíase/cirurgia
2.
Biomolecules ; 14(2)2024 Feb 12.
Artigo em Inglês | MEDLINE | ID: mdl-38397453

RESUMO

The purpose of the current investigation was to produce cinammaldehyde-based chalcone derivatives (3a-k) to evaluate their potential effectiveness as antioxidant and inhibitory agents versus human Caco-2 cancer cells. The findings obtained using the DPPH assay showed that compound 3e had the highest effective antioxidant activity with the best IC50 value compared with the other compounds. Moreover, the cytotoxic findings revealed that compound 3e was the best compound for inhibiting Caco-2 development in contrast to all other produced derivatives, with the lowest IC50 concentration (32.19 ± 3.92 µM), and it also had no detrimental effects on healthy human lung cells (wi38 cells). Exposure of Caco-2 cells with this IC50 value of compound 3e resulted in a substantial rise in the number of early and late cells that are apoptotic with a significant comet nucleus when compared with control cells employing the annexin V/PI and comet evaluations, respectively. Furthermore, qRT-PCR and ELISA examinations indicated that compound 3e significantly altered the expression of genes and their relative proteins related to apoptosis in the treated Caco-2 cells, thus significantly inhibiting Caco-2 growth through activating Caspase-3 via an intrinsic apoptotic pathway. As a result, compound 3e could serve as an effective therapy for human colon cancer.


Assuntos
Acroleína/análogos & derivados , Antineoplásicos , Chalcona , Chalconas , Neoplasias do Colo , Humanos , Relação Estrutura-Atividade , Antioxidantes/farmacologia , Chalconas/farmacologia , Linhagem Celular Tumoral , Células CACO-2 , Chalcona/farmacologia , Chalcona/química , Proliferação de Células , Antineoplásicos/química , Neoplasias do Colo/tratamento farmacológico , Apoptose , Estrutura Molecular
3.
Environ Sci Pollut Res Int ; 31(2): 2732-2744, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38066266

RESUMO

The crystalline phase of molybdenum titanium tungsto-phosphate (MoTiWPO4) as an inorganic sorbent material was synthesized via the sol-gel method. The physicochemical characteristics of MoTiWPO4 were evaluated by using Fourier transform infrared (FT-IR), scanning electron microscope (SEM), energy dispersive X-ray (EDX), thermal analysis (TGA-DTA), and X-ray diffraction (XRD). MoTiWPO4 sorbent material exhibits a high chemical resistance to HNO3, HCl, and alkaline media. MoTiWPO4 has good thermal stability as it retained about 75.63% of its saturation capacity upon heating at 500 °C. The sorption studies for several metal ions revealed marked high sorption efficiency of MoTiWPO4 towards Cs+ and Sr2+ ions which reached 99% and 95%, respectively. The saturation capacity of MoTiWPO4 for Cs+ and Sr2+ is 113 and 109 mg/g, respectively. MoTiWPO4 is approved to be successfully eliminating both 137Cs and 85Sr from liquid radioactive waste streams by %eff. of 92.5 and 90.3, respectively, in the presence of competing ions from 60Co(divalent) and 152Eu (trivalent), confirming the batch experiment results for the removal of Cs+ and Sr2+ metal ions. Furthermore, the decontamination factor exceeds 13.3 in the case of 137Cs and 10.3 for 85Sr.


Assuntos
Radioisótopos de Césio , Resíduos Radioativos , Molibdênio , Titânio , Descontaminação , Espectroscopia de Infravermelho com Transformada de Fourier , Adsorção , Íons , Fosfatos
4.
Actas Urol Esp (Engl Ed) ; 48(3): 204-209, 2024 Apr.
Artigo em Inglês, Espanhol | MEDLINE | ID: mdl-37838327

RESUMO

OBJECTIVES: This study evaluates the impact of using an access sheath (AS) during flexible ureteroscopy (fURS) for urolithiasis treatment, focusing on outcomes such as stone-free rate, operation time, and complications. METHODS: This prospective, randomized study was carried out at Badr Hospital, Helwan University, and Ain Shams University hospitals from August 2021 to August 2022. Patients were systematically randomized into two groups (fURS with AS: 33 patients and without AS: 31 patients) and underwent preoperative and postoperative assessments, including lab tests and imaging. Possible procedure-associated risks, such as failed stone access, pain, bleeding, and sepsis, were monitored. RESULTS: The two groups were found to be comparable in terms of demographic characteristics or preoperative stone findings (p > 0.05 for all). However, operation duration was shorter in the No Sheath group (79.4 ±â€¯15.3 min vs. 90.4 ±â€¯16.7 min in the Sheath group, p = 0.008). Intraoperative complication rates, including failed access, operation termination, ureteric injury, and bleeding, were comparable in both groups (p > 0.05). Postoperative stone-free rates (78.8% vs. 71.0%, p = 0.305) and mean residual stone size (2.7 ±â€¯3.5 mm vs. 3.1 ±â€¯3.1 mm, p = 0.687) showed no significant differences. CONCLUSIONS: The present study suggests that fURS without an access sheath may offer an efficient and equally effective option for managing upper ureteric and renal stones. However, more studies with larger sample sizes and longer follow-up periods are required to validate these findings and to establish more precise indications for this approach.


Assuntos
Cálculos Renais , Ureter , Urolitíase , Humanos , Ureteroscopia/métodos , Ureteroscópios , Ureter/cirurgia , Cálculos Renais/cirurgia , Urolitíase/cirurgia , Urolitíase/complicações
5.
RSC Adv ; 13(51): 35911-35919, 2023 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-38090085

RESUMO

Zinc coating is one of the oldest types of coating for mild steel. The main drawback of zinc coating is that the steel loses its zinc ion after being exposed to environmental factors, leaving mild steel vulnerable to corrosion. Researchers have been working hard to create a zinc-based coating using co-deposition with agricultural waste. The outcome of this co-deposition is increased wear resistance, increased hardness, improved oxidation stability, and improved corrosion resistance. This work aims to enhance the oxidation, wear, and corrosion resistance of mild steel by co-deposition of zinc and maize cob ash nanoparticles. 0, 5, 10, and 15 wt% maize cob ash nanoparticles were used in the production of the coating. Scanning electron microscopy was used to characterize the materials' microstructure. The resulting coated samples' hardness, wear, oxidation, and corrosion properties were examined. The hardness parameters increased by 74.89% and the protection against corrosion by 76.6%. It has been shown that mild steel may have its corrosion, wear, and oxidation resistance increased by using 15 wt% maize cob ash particles.

6.
Endocrinol Diabetes Nutr (Engl Ed) ; 70(10): 619-627, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38065627

RESUMO

BACKGROUND AND AIMS: Neuregulin 1 (NRG-1) is one of the members of the epidermal growth factors proteins. The present study provides novel insights into the relationship between serum levels of NRG-1 and insulin resistance, subclinical atherosclerosis and cardiac dysfunction that occur in type 2 diabetes (T2D). METHODS: The study included 50 patients with T2D and 40 healthy age- and gender-matched controls. Serum NRG-1 was measured using ELISA. Glycemic parameters, lipid profile and insulin resistance were assessed. Trans-thoracic echocardiography and carotid intima media thickness (CIMT) were studied for all study subjects. RESULTS: T2D patients had significantly lower serum NRG-1 levels than controls. Serum NRG-1 was negatively correlated with age, fasting blood glucose, HbA1c, insulin resistance, blood urea, serum creatinine and LDL-C, and positively correlated with HDL-C, eGFR and CIMT. Regarding echocardiographic variables, serum NRG-1 was found to correlate positively with left ventricular global longitudinal strain and negatively with E/Ea ratio. NRG-1 was found to predict subclinical atherosclerosis in type 2 diabetes patients at a cut-off value<108.5pg/ml with 78% sensitivity and 80% specificity. CONCLUSIONS: A robust relationship was found between serum NRG-1 levels and hyperglycemia, insulin resistance, subclinical atherosclerosis, and cardiac dysfunction in patients with type 2 diabetes. These results shed light on a possible role of NRG-1 as a potential noninvasive biomarker for detection of cardiometabolic risk in T2D.


Assuntos
Aterosclerose , Diabetes Mellitus Tipo 2 , Cardiopatias , Resistência à Insulina , Neuregulina-1 , Humanos , Aterosclerose/etiologia , Aterosclerose/diagnóstico , Espessura Intima-Media Carotídea , Diabetes Mellitus Tipo 2/complicações , Neuregulina-1/sangue , Neuregulina-1/química , Neuregulina-1/metabolismo , Fatores de Risco , Função Ventricular
7.
Sci Rep ; 13(1): 21554, 2023 Dec 06.
Artigo em Inglês | MEDLINE | ID: mdl-38057351

RESUMO

Azo dyes are widely used for dyeing polyester fabrics but require optimization of properties like color strength and fastness. Fourteen novel disperse azo dyes were synthesized from 2,3-naphthalenediol and aniline derivatives to examine their potential for polyester dyeing. The dyes were prepared via diazotization and coupling reactions and characterized using FT-IR, UV-Vis, 1H NMR, 13C NMR, and elemental analysis. Furthermore, several techniques were employed to study the azo-hydrazone tautomerism, including UV-Vis spectroscopy, NMR spectroscopy, and computational methods. DFT computations revealed hydrazone tautomers were more stable than azo tautomers. The prepared azo dyes were applied on polyester fabrics at 2% depth using a high temperature pressure technique in water utilizing DYEWELL-002 as a dispersing agent. The color shading of dyed polyester samples ranged from peach amber to apple of my eye, depending on the coupler moieties. The fastness properties, assessed using a grey scale of dyed polyester fabrics, indicated very good to excellent grades for most dyes. Additionally, measurements of color strength (K/S), dye exhaustion (%E), as well as colorimetric colors CILAB of dyed polyester fabrics values, were measured and discussed in terms of the effect of substituents. The findings provide new insights into structure-performance relationships to design optimized disperse dyes for polyester coloration. Overall, the synthesized aryldiazenyl dyes are promising candidates for dyeing polyester fabrics across a spectrum of shades with good fastness properties.

8.
Sex Med ; 11(5): qfad058, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-38028732

RESUMO

Background: Injection of adipose-derived stem cells (ADSCs) into the injured tunica albuginea (TA) may prevent fibrosis, restore the balance between pro- and antifibrotic pathways, and potentially mitigate erectile dysfunction caused by abnormal TA healing. Aim: To assess the potential role of ADSC injection on structural, ultrastructural, functional, and molecular changes in surgically induced trauma of the rat's TA. Methods: Forty adult male albino Wistar rats were divided into 5 groups of 8 rats each: group 1, sham; group 2, injury to TA without treatment; group 3, injury to TA and suture repair; group 4, injury to TA and injection of ADSCs without suture repair; group 5, injury to TA followed by injection of ADSCs and suture repair. Outcomes: After 6 weeks, all groups were subjected to functional, histologic, and ultrastructural examination and molecular expression of healing growth factors. Results: The intracavernous pressure (ICP; mean ± SD) was 114 ± 2, 32 ± 2, 65 ± 2, 68 ± 2, and 111 ± 2 mm Hg in groups 1 to 5, respectively. There were significant differences in ICP between each of groups 3 to 5 and group 2 (P < .05), and groups 3 and 4 each had significant differences with group 1 (P < .05). No significant difference in ICP occurred between groups 3 and 4 (P > .05). There were significant histologic and ultrastructural alterations in tunical tissues from group 2; however, these changes were markedly less in group 5 in terms of lower levels of fibrotic changes, elastosis, and superior overall neuroendothelial expression. Groups 3 and 4 showed improved structural and ultrastructural parameters when compared with group 2. Group 5 demonstrated lower levels of transforming growth factor ß1 and basic fibroblast growth factor expression. Clinical Implications: This experimental model may encourage administration of ADSCs to prevent the deleterious effects of trauma to the TA. Strengths and Limitations: Injecting ADSCs can improve the healing process and erectile dysfunction in a rat model following TA injury, and combining ADSC injection with surgical suturing resulted in superior outcomes. The main limitation was the absence of long-term ICP measurements and a longer follow-up period that may provide further insight into the chronic phase of the healing process. Conclusion: ADSC injection may prevent structural, ultrastructural, functional, and molecular alterations in surgically induced trauma of the rat's TA and enhance the effect of tunical suturing after trauma.

9.
Molecules ; 28(17)2023 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-37687250

RESUMO

The goal of the current study was to prepare two new homologous series of N,N'-diarylurea and N,N'-diarylthiourea derivatives to investigate the therapeutic effects of these derivatives on the methodologies of inhibition directed on human MCF-7 cancer cells. The molecular structures of the prepared derivatives were successfully revealed through elemental analyses, 1H-NMR, 13C-NMR and FT-IR spectroscopy. The cytotoxic results showed that Diarylthiourea (compound 4) was the most effective in suppressing MCF-7 cell growth when compared to all other prepared derivatives, with the most effective IC50 value (338.33 ± 1.52 µM) after an incubation period of 24 h and no cytotoxic effects on normal human lung cells (wi38 cells). Using the annexin V/PI and comet tests, respectively, treated MCF-7 cells with this IC50 value of the Diarylthiourea 4 compound displayed a considerable increase in early and late apoptotic cells, as well as an intense comet nucleus in comparison to control cells. An arrest of the cell cycle in the S phase was observed via flow cytometry in MCF-7 cells treated with the Diarylthiourea 4 compound, suggesting the onset of apoptosis. Additionally, ELISA research showed that caspase-3 was upregulated in MCF-7 cells treated with compound 4 compared to control cells, suggesting that DNA damage induced by compound 4 may initiate an intrinsic apoptotic pathway and activate caspase-3. These results contributed to recognizing that the successfully prepared Diarylthiourea 4 compound inhibited the proliferation of MCF-7 cancer cells by arresting the S cell cycle and caspase-3 activation via an intrinsic apoptotic route. These results, however, need to be verified through in vivo studies utilizing an animal model.


Assuntos
Núcleo Celular , Neoplasias , Animais , Humanos , Caspase 3 , Espectroscopia de Infravermelho com Transformada de Fourier , Proteólise , Células MCF-7
10.
Cancers (Basel) ; 15(18)2023 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-37760496

RESUMO

Lung cancer (LC) is the second-most prevalent tumor worldwide. According to the most recent GLOBOCAN data, over 2.2 million LC cases were reported in 2020, with an estimated new death incident of 1,796,144 lung cancer cases. Genetic, lifestyle, and environmental exposure play an important role as risk factors for LC. E-cigarette, or vaping, products (EVPs) use has been dramatically increasing world-wide. There is growing concern that EVPs consumption may increase the risk of LC because EVPs contain several proven carcinogenic compounds. However, the relationship between EVPs and LC is not well established. E-cigarette contains nicotine derivatives (e.g., nitrosnornicotine, nitrosamine ketone), heavy metals (including organometal compounds), polycyclic aromatic hydrocarbons, and flavorings (aldehydes and complex organics). Several environmental toxicants have been proven to contribute to LC. Proven and plausible environmental carcinogens could be physical (ionizing and non-ionizing radiation), chemicals (such as asbestos, formaldehyde, and dioxins), and heavy metals (such as cobalt, arsenic, cadmium, chromium, and nickel). Air pollution, especially particulate matter (PM) emitted from vehicles and industrial exhausts, is linked with LC. Although extensive environmental exposure prevention policies and smoking reduction strategies have been adopted globally, the dangers remain. Combined, both EVPs and toxic environmental exposures may demonstrate significant synergistic oncogenicity. This review aims to analyze the current publications on the importance of the relationship between EVPs consumption and environmental toxicants in the pathogenesis of LC.

11.
Molecules ; 28(9)2023 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-37175214

RESUMO

The effect of the terminal benzyloxy group on the mesomorphic properties of liquid crystalline materials developed from rod-like Schiff base has been described. For this objective, a novel Schiff base liquid crystal family, specifically new series of Schiff base liquid crystals, namely, (E)-4-(alkyloxy)-N-(4-(benzyloxy)benzylidene)aniline, In, are prepared and investigated in detail. The length of the terminal alkyloxy chain (n) varies amongst the compounds in the series. Where n varies between 6, 8 and 16 carbons. At the other end of the compounds, benzyloxy moiety was attached. The molecular structures of all synthesized compounds were established using different spectroscopic techniques. The molecular self-assembly was explored using differential scanning calorimetry (DSC) and polarized optical microscope (POM). Depending on the length of the terminal alkyloxy chain, only one type of SmA phase with different stability was observed. The previously reported para-substituted systems and the present investigated compounds were compared and discussed. The calculated quantum chemical parameters were computationally correlated using the DFT method via the B3LYP 6-311G(d,p) basis set. The theoretical computations revealed that the length of the alkyl side chain influences the zero-point energy, reactivity and other estimated thermodynamic parameters of benzoyloxy/azomethine derivatives. Furthermore, the FMO energy analysis shows that molecule I16 have higher HOMO energies than the other compounds, and I6 has a much lower LUMO level than the rest.

12.
Sci Rep ; 13(1): 7826, 2023 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-37188698

RESUMO

Benzidine was coupled with ethyl cyanoacetate, and malononitrile, to give azo-hydrazo products which in turn were cyclized by using hydrazine and phenyl hydrazine to give 4,4'-([1,1'-biphenyl]-4,4'-diylbis(hydrazin-2-yl-1-ylidene))bis pyrazole derivatives 5-7. These compounds were identified by various spectral analysis. The examination of 0.1 M NaOH and 0.1 M HCl in DMF revealed that the λmax of the synthesized dyes are quite sensitive to pH variation and slightly affected by the coupler moieties. Utilizing the dispersion agent DYEWELL-002, polyester fabric (PE-F) was dyed in water. The color strength (K/S), its summation (K/Ssum), dye exhaustion (%E) and reflectance values were measured and discussed. The DFT method estimates the chemical descriptor parameters of the titled dyes, using B3LYP/6-31G(d,p) level to investigate the performance of dyes as well as to postulate a mechanism of dyeing process.

13.
Heliyon ; 9(4): e14871, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37025900

RESUMO

New organic derivatives named, (E)-3(or4) -(alkyloxy)-N-{(trifluoromethyl)benzylidene}aniline, 1a-f, were synthesized and examined their liquid crystalline behaviors. FT-IR, 1H NMR, 13C NMR, 19F NMR, elemental analyses and GCMS were used to validate the prepared compounds' chemical structures. We used differential scanning calorimetry (DSC) and polarized optical microscopy (POM) to investigate the mesomorphic characteristics of the formed Schiff bases. All tested compounds of series 1a-c have mesomorphic behaviour of nematogenic temperature ranges while the group 1d-f show non-mesomorphic properties. Moreover, it was found that the enantiotropic N phases included all of the homologue 1a-c. Computational studies using DFT (density functional theory) validated the experimental mesomorphic behavior results. All the analyzed compounds had their dipole moments, polarizability, and reactivity characteristics explained. Theoretical simulations showed that as the length of the terminal chain is increased, the polarizability of the stuided compounds increases. Consequently, compounds 1a and 1d have the least polarizability.

14.
Genes (Basel) ; 14(2)2023 01 30.
Artigo em Inglês | MEDLINE | ID: mdl-36833281

RESUMO

Heat shock proteins (HSPs) are cytoprotective against stressful conditions, as in the case of cancer cell metabolism. Scientists proposed that HSP70 might be implicated in increased cancer cell survival. This study aimed to investigate the HSP70 (HSPA4) gene expression signature in patients with renal cell carcinoma (RCC) in correlation to cancer subtype, stage, grade, and recurrence, combining both clinicopathological and in silico analysis approaches. One hundred and thirty archived formalin-fixed paraffin-embedded samples, including 65 RCC tissue specimens and their paired non-cancerous tissues, were included in the study. Total RNA was extracted from each sample and analyzed using TaqMan quantitative Real-Time Polymerase Chain Reaction. Correlation and validation to the available clinicopathological data and results were executed. Upregulated HSP70 (HSPA4) gene expression was evident in RCC compared to non-cancer tissues in the studied cohort and was validated by in silico analysis. Furthermore, HSP70 expression levels showed significant positive correlations with cancer size, grade, and capsule infiltration, as well as recurrence in RCC patients. The expression levels negatively correlated with the overall survival (r = -0.87, p < 0.001). Kaplan-Meier curves showed lower survival rates in high HSP70 expressor group compared to the low expressors. In conclusion, the HSP70 expression levels are associated with poor RCC prognosis in terms of advanced grade, capsule infiltration, recurrence, and short survival.


Assuntos
Carcinoma de Células Renais , Proteínas de Choque Térmico HSP70 , Neoplasias Renais , Humanos , Carcinoma de Células Renais/genética , Proteínas de Choque Térmico HSP70/genética , Neoplasias Renais/genética , Prognóstico
15.
Eur J Med Chem ; 247: 115040, 2023 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-36584632

RESUMO

Antibiotic-resistant bacteria represent a serious threat to modern medicine and human life. Only a minority of antibacterial agents are active against Gram-negative bacteria. Hence, the development of novel antimicrobial agents will always be a vital need. In an effort to discover new therapeutics against Gram-negative bacteria, we previously reported a structure-activity-relationship (SAR) study on 1,2-disubstituted benzimidazole derivatives. Compound III showed a potent activity against tolC-mutant Escherichia coli with an MIC value of 2 µg/mL, representing a promising lead for further optimization. Building upon this study, herein, 49 novel benzimidazole compounds were synthesized to investigate their antibacterial activity against Gram-negative bacteria. Our design focused on three main goals, to address the low permeability of our compounds and improve their cellular accumulation, to expand the SAR study to the unexplored ring C, and to optimize the lead compound (III) by modification of the methanesulfonamide moiety. Compounds (25a-d, 25f-h, 25k, 25l, 25p, 25r, 25s, and 26b) exhibited potent activity against tolC-mutant E. coli with MIC values ranging from 0.125 to 4 µg/mL, with compound 25d displaying the highest potency among the tested compounds with an MIC value of 0.125 µg/mL. As its predecessor, III, compound 25d exhibited an excellent safety profile without any significant cytotoxicity to mammalian cells. Time-kill kinetics assay indicated that 25d exhibited a bacteriostatic activity and significantly reduced E. coli JW55031 burden as compared to DMSO. Additionally, combination of 25d with colistin partially restored its antibacterial activity against Gram-negative bacterial strains (MIC values ranging from 4 to 16 µg/mL against E. coli BW25113, K. pneumoniae, A. baumannii, and P. aeruginosa). Furthermore, formulation of III and 25d as lipidic nanoparticles (nanocapsules) resulted in moderate enhancement of their antibacterial activity against Gram-negative bacterial strains (A. Baumannii, N. gonorrhoeae) and compound 25d demonstrated superior activity to the lead compound III. These findings establish compound 25d as a promising candidate for treatment of Gram-negative bacterial infections and emphasize the potential of nano-formulations in overcoming poor cellular accumulation in Gram-negative bacteria where further optimization and investigation are warranted to improve the potency and broaden the spectrum of our compounds.


Assuntos
Anti-Infecciosos , Escherichia coli , Animais , Humanos , Antibacterianos/farmacologia , Bactérias Gram-Negativas , Benzimidazóis/farmacologia , Pseudomonas aeruginosa , Testes de Sensibilidade Microbiana , Bactérias Gram-Positivas , Mamíferos
16.
Osteoarthr Cartil Open ; 4(3): 100271, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36474949

RESUMO

Objective: To understand patient perceived acceptability of participating in a telehealth delivered group-based education and exercise-therapy program for knee osteoarthritis. Design: This qualitative study involved semi-structured, one-on-one interviews with knee osteoarthritis patients who have completed the Good Living with osteoArthritis from Denmark (GLA:D®) program via telehealth or in-person. Interviews were recorded, transcribed verbatim, coded, and analysed using an inductive content analysis approach, focusing on themes related to telehealth. Results: Nineteen participants [12 (63%) female, mean aged 62 years, range 49-72 years] were included. Eleven (58%) received GLA:D® via telehealth and 8 (42%) attended in-person sessions. Two overarching themes (6 sub-themes) related to telehealth perceived acceptability were identified: 1) Perceptions of telehealth acceptability was highly influenced by exposure. Individuals who had received telehealth considered it easy, convenient, and flexible, whereas telehealth was perceived to be inferior and misunderstood by those without exposure. 2) Telehealth participants reported similar program benefits to in-person participants, including reduced fear of pain and joint damage, changed beliefs in value of exercise, and stated improvements in pain and function. Conclusions: Telehealth delivery of group-based education and exercise-therapy for knee osteoarthritis was acceptable for people who had experienced it and provides similar benefits as in-person care for pain and beliefs about the safety and value of exercise. Wider implementation of telehealth group-based education and exercise-therapy may improve access to high value care for people with knee osteoarthritis.

17.
Sci Rep ; 12(1): 22251, 2022 12 23.
Artigo em Inglês | MEDLINE | ID: mdl-36564523

RESUMO

Phosphoric acid is the core material for the fertilizer industry; however, it is incredibly corrosive to manufacturing plants' structures, mainly steel. Corrosion is one of the most severe problems encountered during phosphate fertilizer manufacturing. Recently, plant extracts have been commonly used as corrosion inhibitors because they are cheap and environmentally friendly. Steel corrosion in a 20% aqueous phosphoric acid solution in the absence and presence of fenugreek seed (Fen) or cape gooseberry leaf (CgL) extracts was investigated using the electrochemical impedance spectroscopy technique, potentiodynamic polarization measurement, scanning electron microscope, and quantum chemical calculations. Fourier Transform Infrared, FTIR, was used to identify the functional groups in Fen and CgL extracts. The inhibition efficiency for steel in 20% aqueous phosphoric acid was roughly equal to 80% for 0.4 g/L CgL and 1.2 g/L Fen extracts. A scanning electron microscope showed that the chemical constituents of extracts block the surface roughness of steel, decreasing the corrosion rate. The activation parameters indicated the effectiveness of the extracts at a higher temperature. Measurements of the potential of zero charges showed that the steel surface is positively charged in the phosphoric acid solution. Quantum chemical computations were also employed to examine the corrosion inhibition mechanisms of the natural extracts.


Assuntos
Ribes , Aço , Aço/química , Corrosão , Fertilizantes , Extratos Vegetais/química
18.
Molecules ; 27(15)2022 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-35956864

RESUMO

A variety of structurally different pyrimidines were synthesized. Elemental analysis, FT-IR, 1H NMR, and 13C NMR spectroscopy were used to confirm the chemical structures of all prepared compounds. The synthesized pyrimidines were screened against the growth of five human cancer cell lines (prostate carcinoma PC3, liver carcinoma HepG-2, human colon cancer HCT-116, human breast cancer MCF-7, human lung cancer A-549), and normal human lung fibroblasts (MRC-5) using MTT assay. Most of the screened pyrimidines have anti-proliferative activity on the growth of the PC3 cell line. Compounds 3b and 3d were more potent than the reference vinblastine sulfate (~2 to 3 × fold) and they can be considered promising leads for treating prostate cancer disease. Moreover, the screened compounds 3b, 3f, 3g, 3h, and 5 were assessed according to the values of their selectivity index (SI) and were found to be more selective and safer than vinblastine sulfate. Furthermore, using in silico computational tools, the physicochemical properties of all pyrimidine ligands were assessed, and the synthesized compounds fall within the criteria of RO5, thus having the potential to be orally bioavailable.


Assuntos
Antineoplásicos , Carcinoma , Compostos Heterocíclicos , Antineoplásicos/química , Proliferação de Células , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Compostos Heterocíclicos/química , Compostos Heterocíclicos/farmacologia , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Pirimidinas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-Atividade , Vimblastina/farmacologia
19.
Molecules ; 27(12)2022 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-35744824

RESUMO

A new N,N'-disubstituted piperazine conjugated with 1,3,4-thiadiazole and 1,2,4-triazole was prepared and the chemical structures were identified by IR, NMR and elemental analysis. All the prepared compounds were tested for their antimicrobial activity. The antimicrobial results indicated that the tested compounds showed significant antibacterial activity against gram-negative strains, especially E. coli, relative to gram-positive bacteria. Docking analysis was performed to support the biological results; binding modes with the active site of enoyl reductase amino acids from E. coli showed very good scores, ranging from -6.1090 to -9.6184 kcal/mol. Correlation analysis was performed for the inhibition zone (nm) and the docking score.


Assuntos
Anti-Infecciosos , Escherichia coli , Antibacterianos/química , Anti-Infecciosos/química , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Oxirredutases , Piperazinas/química , Tiadiazóis
20.
Braz J Biol ; 82: e261785, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35703635

RESUMO

Phytoremediation is an ecofriendly technique to clean heavy metals from contaminated soil by the use of high biomass producing plant species. Chelators can help to improve this biological technique by increasing metal solubility. Therefore, a pot experiment was conducted to determine the effect of the chelators EDTA and citric acid (CA) in phytoremediation of Ni contaminated soil by using Brassica napus (canola). Two cultivars of B. napus, Con-II (tolerant) and Oscar (sensitive), were selected after screening and exposed to NiSO4 at 30 ppm at the time of sowing. CA (10 mM) and EDTA (1.5 mM) were applied either alone or in combination with each other after two weeks of Ni treatments. Different parameters like morpho-physiological and biochemical data were recorded after 15 days of chelate application. The results highlighted the successful use of chelating agents (CA and EDTA) not only to ameliorate Ni stress but also to enhance Ni accumulation which is prerequisite for phytoremediation. The basal application of 10 mMCA and 1.5 mM EDTA concentration proved to be effective for the growth of plants. The combination of chelating agents failed to show any synergistic effects.


Assuntos
Brassica napus , Metais Pesados , Poluentes do Solo , Biodegradação Ambiental , Quelantes/farmacologia , Ácido Cítrico/farmacologia , Ácido Edético/farmacologia , Solo , Poluentes do Solo/análise , Poluentes do Solo/farmacologia
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