RESUMO
The reaction between ninhydrin-malononitrile adduct [2-(1,3-dioxo-1,3-dihydro-2H-inden-2-ylidene)malononitrile] and ethyl 2-(alkylamino)-4-aryl-4-oxo-but-2-enoates (prepared from ethyl 2,4-dioxo-4-arylbutanoate and alkylamines) in the presence of Et3N in MeCN at room temperature afforded 3-alkylamino-2-aryloyl-1',3',4-trioxo-1',3'-dihydrospiro[cyclopentane-1,2'-inden]-2-ene-5,5-dicarbonitriles in 78-95% yields. Five derivatives of these NH-acidic compounds are used to intercept the reactive zwitterionic intermediates generated from dimethyl acetylenedicarboxylate and Ph3P to produce dimethyl 4,4-dicyano-6-aryloyl-1-alkyl-1',3'-dioxo-1',2,3',4-tetrahydro-1H-spiro[cyclopenta[b]pyrrole-5,2'-indene]-2,3-dicarboxylates. Radical scavenging activity of four derivatives was investigated by radical trapping of diphenylpicrylhydrazine and ferric reduction power experiments. The antibacterial activities of six derivatives were studied by disk diffusion test on Gram-positive and Gram-negative bacteria.
Assuntos
Antibacterianos , Indenos , Antibacterianos/farmacologia , Pirróis , Bactérias Gram-Negativas , Bactérias Gram-PositivasRESUMO
[Cd(C7H3NO4)(H2O)1.5]n or [Cd(2,6-pydc)(H2O)1.5]n, (1) (2,6-pydc = pyridine-2,6-dicarboxylate) was obtained from the reaction of pyridine-2,6-dicarboxylic acid and 4-hydroxypyridine-2,6-dicarboxylic acid with cadmium(II) nitrate tetrahydrate in the presence of piperazine and characterized by elemental analysis, IR spectra and X-ray single crystal diffraction. Complex (1) is a novel carboxylate-bridged one-dimensional pincer-shaped helical chain of cadmium(II) polymer. Each Cd atom is seven-coordinate and exhibits an approximately pentagonal-bipyramidal CdNO6 coordination geometry. The metal fragments are linked via the central four-membered Cd2O2 ring and the structural analysis showed that 4-hydroxypyridine-2,6-dicarboxylic acid and piperazine do not appear in the structure.
RESUMO
Selection of biodegradable chitosan as a raw material is a smart technique due to its easy modifiability and high renewability. Herein, taking advantage of these functional characteristics, an ionic biopolymer support is produced from copolymerization of allylated chitosan (with 48 % degree of substitution) and polymerizable ionic liquid ([MEVIm]Br). Next, palladium nanoparticles are successfully stabilized in this designed support through a facile manner based on interconnected porous network, ionic nature and rich functional groups. Then, the Pd@CS-PIL structure was utilized as a heterogeneous catalyst for regioselective synthesis of pyrazole-fused heterocycles. The as-synthesized Pd@CS-PIL was characterized by various techniques such as XRD, EDX, FESEM, elemental mapping, TEM, BET, ICP, TGA, and FT-IR to better determine the structure, morphology, purity and physical properties. The obtained results revealed that the proposed nanostructure provides favorable porosity with significant specific surface area (139.2 m2.g-1), Pd nanoparticles with high dispersion (mean diameter â¼ 22.8 nm) and crosslinked nature with good thermal stability (50 % weight loss about 600 °C). Therefore, Pd@CS-PIL nanostructure showed the key features of a super-active catalyst, and pharmaceutical pyrazole-fused scaffolds were produced in favorable yields (86-96 %) under ultrasound conditions.
Assuntos
Quitosana , Nanopartículas Metálicas , Quitosana/química , Nanopartículas Metálicas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Paládio/química , Íons , Catálise , PirazóisRESUMO
As a common metabolic disorder, hyperglycemia (HG) affects and disrupts the physiology of various systems in the body. Transplantation of mesenchymal stem cells (MSCs) has been used to control the complications of disease. Most of the therapeutic properties of MSCs are attributed to their secretome. This study aimed to investigate the effects of conditioned media extracted from sole or caffeine pre-treated bone-marrow-derived MSCs on hyperglycemia-induced detrimental impact on some aspects of reproduction. The HG was induced by intraperitoneally injection of streptozotocin (65 mg/kg) and nicotinamide (110 mg/kg). Twenty-four male Wistar rats (190 ± 20 g) were divided into control, HG, and the hyperglycemic groups receiving conditioned media of proliferated MSCs solely (CM) or MSCs pre-treated with caffeine (CCM). During the 49-day treatment, body weight and blood glucose were measured weekly. Finally, HbA1c, spermatogenesis development, sperm count, morphology, viability, motility, chromatin condensation, and DNA integrity were examined. Also, testicular total antioxidant capacity (TAC), malondialdehyde, sperm fertilization potential, and pre-implantation embryo development were evaluated. A one-way ANOVA and Tukey's post-hoc tests were used to analyze the quantitative data. The p < 0.05 was considered statistically significant. The CM and with a higher efficiency, the CCM remarkably (p < 0.05) improved body weight and HG-suppressed spermatogenesis, enhanced sperm parameters, chromatin condensation, DNA integrity, and TAC, reduced HbA1c, sperm abnormalities, and malondialdehyde, and significantly improved pre-implantation embryo development versus HG group. The conditioned media of MSCs solely (CM) and more effectively after pre-treatment of MSCs with caffeine (CCM) could improve spermatogenesis development, sperm quality, pre-implantation embryo development, and testicular global antioxidant potential during hyperglycemia.
Assuntos
Cafeína , Meios de Cultivo Condicionados , Fertilização , Hiperglicemia , Células-Tronco Mesenquimais , Espermatogênese , Cafeína/farmacologia , Células-Tronco Mesenquimais/efeitos dos fármacos , Meios de Cultivo Condicionados/farmacologia , Hiperglicemia/fisiopatologia , Fertilização/efeitos dos fármacos , Masculino , Animais , Ratos , Modelos Animais de Doenças , Peso Corporal/efeitos dos fármacos , Glicemia/efeitos dos fármacos , Hemoglobinas Glicadas , Espermatogênese/efeitos dos fármacos , Contagem de Espermatozoides , Testículo/efeitos dos fármacos , Testículo/metabolismo , Espermatozoides/anormalidades , Espermatozoides/efeitos dos fármacosRESUMO
A novel supported molybdenum complex on cross-linked poly (1-Aminopropyl-3-vinylimidazolium bromide) entrapped cobalt oxide nanoparticles has been successfully fabricated through two different procedures, i.e. ultrasound (US) irradiations (100 W, 40 kHz) and reflux. The efficiency of the two different methods was comparatively investigated on the fundamental properties of proposed catalyst using diverse characterization techniques. Based on the obtained results, the ultrasonication method provides controlled polymerization process; as a result, well connected polymeric network is formed. In addition, the use of ultrasound waves turned out to be able to increase the particles uniformity, specific surface area (from 79.19 to 223.83 m2/g), and the onset thermal degradation temperature (Td) value (from 248 to 400 °C) of the prepared catalyst which intensifies the catalytic efficiency. Besides, US-treated catalyst demonstrated high chemical stability and maintained its cross-linked network after eight cycles recovery, while the cross-linked network of catalyst obtained under silent condition was completely disrupted. Furthermore, the ultrafast multi-step fabrication procedure was performed in less than 6 h under ultrasonic condition while a similar process promoted by a mechanical stirring method came to a conclusion after 5-6 days. Accordingly, the utility of the ultrasound irradiation was proved, and US-treated catalyst was applied for improved synthetic methodology of spiro 1,4-dihydropyridines and spiro pyranopyrazoles through different acidic active sites. Due to the significant synergistic influence between the proposed catalyst and US irradiation, a variety of novel and recognized mono-spiro compounds were fabricated at room temperature in high regioselectivity.
Assuntos
Complexos de Coordenação/química , Engenharia , Líquidos Iônicos/química , Molibdênio/química , Compostos de Espiro/química , Compostos de Espiro/síntese química , Ondas Ultrassônicas , Técnicas de Química Sintética , Concentração de Íons de Hidrogênio , Pirazóis/química , Estereoisomerismo , TemperaturaRESUMO
Although poly (ionic liquids) (PILs) have attracted great research interest owing to their various applications, the performance of nanoporous PILs has been rarely developed in the catalysis field. To this end, a micro-mesoporous PIL with acid-base bifunctional active sites was designed and fabricated by two different polymerization protocols including hydrothermal and classical precipitation polymerization in this paper. Based on our observations, hydrothermal conditions (high temperature and pressure) enabled the proposed sonocatalyst to possess a great porous structure with a high specific surface area (S BET: 315 m2 g-1) and thermal stability (around 450 °C for 45% weight loss) through strengthening cross-linking. In a comparative study, the preferred nanoporous PIL was selected and utilized as the sonocatalyst in a multicomponent reaction of isatins, primary amines, and thioglycolic acid. In the following, a variety of new and known pharmaceutical spiro-4-thiazolidinone derivatives were synthesized at room temperature and obtained excellent yields (>90%) within short reaction times (4-12 min) owing to the substantial synergistic effect between ultrasound irradiation and magnetically separable catalyst.
RESUMO
Leptin, the 16-kDa product of the obese (ob) gene, primarily secreted from adipose tissue, has been implicated to play an important role in the regulation of food intake and energy expenditure. This study investigated protective effect of leptin on trichostatin A-induced apoptotic on in vitro maturation ratio of buffalo oocytes. Ovaries were collected from abattoir and were transported immediately to the laboratory by a thermos flask containing sterile normal saline with antibiotics. Oocytes were aspirated from 2 to 8 mm visible follicles. Oocytes were placed in a culture plate and then incubated at 38.5 ËC with 5% CO2 in air for 24 hr. The maturation of oocytes was evaluated under a stereomicroscope. The FITC-Annexin V and propidium iodide staining method was used to detect oocyte apoptosis. In leptin treated groups with 0, 10, 50 and 100 ng mL(-1) and groups that apoptosis was induced, the percentage of oocytes maturation was 77.03, 86.12, 85.08, and 79.89% and 59.96, 56.93 and 51.98, respectively, while the percentage of apoptosis was 8.83, 7.90, 8.58, and 9.39%, and 10.37, 11.57 and 12.03, respectively. Our findings showed that addition of 10 and 50 ng mL(-1) leptin to IVM medium of buffalo oocytes could increase oocyte nuclear maturation, and could decrease oocyte apoptosis when trichostatin A added for inducing apoptosis.