RESUMEN
Three different drying methods: hot-air-drying (HAD), dehumidified drying (DD) and freeze drying (FD) were used to dry Indian white button mushrooms (Agaricus bisporus). Dehumidified drying method has been proposed as an alternative technique to improve the quality of dehydrated mushroom. Mushroom powder obtained by DD method had 33.29% protein, 17.21% uronic acid, and 10.93% ash content. It was also a good source of ergosterol (422.18±5.80 mg/100 g dw), which is known as the precursor of Vitamin D2. Ethanolic extract of mushroom powder showed good antioxidant activity with lower DPPH IC50 value (7.16±0.23 mg/mL) and also lower EC50 value of ABTS (4.36±0.04 mg/mL). Mushroom powder is added to ready to cook green gram based chilla mix (vegetable omelette mix) at 10%, 20% and 30% levels. The effect of incorporation of mushroom powder on quality characteristics of the formulation was studied. The results showed that the ready to cook mix containing 20% of mushroom powder had protein: 23.33 g; total dietary fiber: 10.75 g; ergosterol: 79.08 mg and also important minerals like calcium: 99.57 mg; potassium: 1203.49 mg; magnesium: 137.80 mg and zinc: 2.23 mg in 100 g of formulation. The formulated products were shelf-stable at ambient temperature for three months. Supplementary Information: The online version contains supplementary material available at 10.1007/s13197-023-05680-9.
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The SnO2 and SnO2/rGO nanostructures were successfully synthesized using the facile hydrothermal synthesis technique. The prepared nanostructures were well studied using different techniques such as XRD, XPS, UV-DRS, FT-IR, EDX, SEM and HR-TEM analysis. The crystalline nature of SnO2 and SnO2/rGO was confirmed by the XRD technique. The formation of highly pure SnO2 and SnO2/rGO nanostructures was confirmed by EDX analysis. The morphological results show the good agglomeration of several spherical nanoparticles. The optical properties were studied through the UV-DRS technique and the bandgap energies of SnO2 and SnO2/rGO are estimated to be 3.12 eV and 2.71 eV, respectively. The photocatalytic degradation percentage in presence of SnO2 and SnO2/rGO against RhB was found to be 96% and 98%, respectively. The degradation of TTC molecules was estimated as 90% and 88% with SnO2/rGO and SnO2, respectively. The degradation of both RhB and TTC molecules was well suited with the pseudo-first-order kinetics. The results of successive experiments clearly show the enhancement in the photocatalytic properties in the SnO2/rGO nanostructures.
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Contaminantes Ambientales , Nanocompuestos , Catálisis , Grafito , Cinética , Nanocompuestos/química , Preparaciones Farmacéuticas , Espectroscopía Infrarroja por Transformada de Fourier , Compuestos de Estaño/químicaRESUMEN
Arsenic present in water bodies causes devastating effects on aquatic organisms and indirectly poses a hazardous threat to human existence. There is an urgent need to develop potential and convincing technologies to troubleshoot this problem. In the present study, an adsorbent has been prepared using the waste red mud from hazardous aluminium industry and doping it with calcium-alginate beads (ARMCB) for the effective removal of As(III) from wastewater. The concentration of As(III) was reduced from 0.101 mg/L to 0.008 mg/L after adsorption which effectively met the economic and environmental conditions imposed by WHO (>0.01 mg/L). Further, the statistical Response Surface Methodology (RSM) is adopted to analyze the combined effects of four operational parameters namely: pH, sorbent dosage, contact time and initial concentration on the adsorption of As(III) from the synthetic contaminated water samples. A high correlation coefficient (R2) value of 0.9672 projected by ANOVA confirmed the satisfactory regression of the developed model. The maximum adsorption capacity is found to be 1.807 mg/g at optimum operating conditions. The surface characterization of the adsorbent before and after adsorption by SEM, EDX, XRD, and FTIR confirms the potentiality of the adsorbent towards As(III) ions. Thermodynamic, adsorption isotherms and kinetic analysis respectively projected the endothermic Langmuir model adsorption of As(III) and the pseudo-second-order rate kinetics of the sorption mechanism. The current study aids the implementation of the developed robust technique for the successful removal of As(III) from industrial and domestic polluted water samples.
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Contaminantes Químicos del Agua , Purificación del Agua , Adsorción , Alginatos , Calcio , Humanos , Concentración de Iones de Hidrógeno , Cinética , AguaRESUMEN
Mayonnaise was prepared by replacing refined sunflower oil with physically refined rice bran oil (RBO), filtered sesame oil (SO) and blends of both RBO:SO. Emulsions were formulated using xanthan gum as a replacer for egg. The effect of replacing xanthan gum on varying oil blends (RBO:SO) on the physicochemical properties such as texture (consistency), stability, viscosity, and bioactives (oryzanol and sesamol content) were also studied. Significant differences were observed in the fat content of the emulsions prepared. Xanthan gum based mayonnaise's had 63-65% fat, whereas control sample with egg had 78% fat. The spreadability ranged between 1.2 and 1.6 N and stability of these spreads was found to be better than that of control. Mayonnaise with the desired colour, optimum spreadability and excellent emulsion stability could be prepared using RBO, and blends of RBO:SO. Significant differences were seen in the instrumental consistency and rheological studies among the mayonnaises prepared. The present study focusses on the preparation of a healthy mayonnaise using rice bran and sesame oil and their blends which have beneficial health effects due to the presence of oryzanol and sesamol.
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We report, based on biophysical studies and molecular mechanical calculations that curcumin binds DNA hairpin in the minor groove adjacent to the loop region forming a stable complex. UV-Vis and fluorescence spectroscopy indicated interaction of curcumin with DNA hairpin. In this novel binding motif, two É£ H of curcumin heptadiene chain are closely positioned to the A16-H8 and A17-H8, while G12-H8 is located in the close proximity of curcumin α H. Molecular dynamics (MD) simulations suggest, the complex is stabilized by noncovalent forces including; π-π stacking, H-bonding and hydrophobic interactions. Nuclear magnetic resonance (NMR) spectroscopy in combination with molecular dynamics simulations indicated curcumin is bound in the minor groove, while circular dichroism (CD) spectra suggested minute enhancement in base stacking and a little change in DNA helicity, without significant conformational change of DNA hairpin structure. The DNA:curcumin complex formed with FdU nucleotides rather than Thymidine, demonstrated enhanced cytotoxicity towards oral cancer cells relative to the only FdU substituted hairpin. Fluorescence co-localization demonstrated stability of the complex in biologically relevant conditions, including its cellular uptake. Acridine orange/EtBr staining further confirmed the enhanced cytotoxic effects of the complex, suggesting apoptosis as mode of cell death. Thus, curcumin can be noncovalently complexed to small DNA hairpin for cellular delivery and the complex showed increased cytotoxicity in combination with FdU nucleotides, demonstrating its potential for advanced cancer therapy.
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Anticarcinógenos/farmacología , Antineoplásicos Fitogénicos/farmacología , Curcumina/farmacología , ADN/efectos de los fármacos , Floxuridina/farmacología , Anticarcinógenos/química , Antineoplásicos Fitogénicos/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Dicroismo Circular , Curcumina/química , Sinergismo Farmacológico , Floxuridina/metabolismo , Humanos , Modelos Moleculares , Simulación de Dinámica Molecular , Resonancia Magnética Nuclear Biomolecular , Conformación de Ácido Nucleico/efectos de los fármacos , Espectrometría de Fluorescencia , Espectrofotometría UltravioletaRESUMEN
Wheat bran, an abundant byproduct of the milling industry, comprises fat-soluble bioactives and fibers. In the present study, two concentrates were prepared from wheat bran oil (WBO) using silicic acid coupled with acetone (WBA) and hexane (WBH). WBA extract had enhanced color and viscosity and was enriched with fat-soluble bioactives (sterols, oryzanol-like compounds, tocopherols, and carotenoids) as evidenced from NMR and other techniques. In in vitro studies, WBA exhibited significant free radical scavenging activity, limited DNA and LDL oxidation, and inhibiting HMG-CoA reductase and lipase activity better than WBH and WBO. Further, an in vivo study with WBA 2 or 3.5% containing high fat diet ameliorated malonaldehyde (MDA) level, lipid profile, and antioxidant enzyme (SOD, catalase, GPx, and GR) activities in liver. A possible reason for this effect is downregulation of HMG-CoA reductase expression with WBA. Thus, WBA has significant potential as an ingredient in health food formulations.
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Antioxidantes/química , Fibras de la Dieta/análisis , Hiperlipidemias/tratamiento farmacológico , Hipolipemiantes/química , Aceites de Plantas/química , Triticum/química , Animales , Antioxidantes/administración & dosificación , Antioxidantes/aislamiento & purificación , Catalasa/genética , Catalasa/metabolismo , LDL-Colesterol/metabolismo , Humanos , Hidroximetilglutaril-CoA Reductasas/genética , Hidroximetilglutaril-CoA Reductasas/metabolismo , Hiperlipidemias/enzimología , Hiperlipidemias/genética , Hiperlipidemias/metabolismo , Hipolipemiantes/administración & dosificación , Hipolipemiantes/aislamiento & purificación , Lipasa/genética , Lipasa/metabolismo , Hígado/enzimología , Hígado/metabolismo , Masculino , Malondialdehído/metabolismo , Aceites de Plantas/administración & dosificación , Aceites de Plantas/aislamiento & purificación , Superóxido Dismutasa/genética , Superóxido Dismutasa/metabolismoRESUMEN
AIM: To evaluate the application of extended nasolabial flap versus buccal fat pad graft in the surgical management of oral submucous fibrosis. SETTINGS AND DESIGN: This prospective study was carried out in the Department of Oral and Maxillofacial Surgery, Tamil Nadu Government Dental College and Hospital, Chennai. MATERIAL AND METHODS: A total of 8 patients (6 men and 2 women) with age range from 21 to 65 years were selected for study. These 8 patients were randomly divided into two groups of four namely group 1 and group 2. In group 1 patients, reconstruction was planned with extended nasolabial flaps and in group 2 patients, reconstruction was planned with buccal fat pad graft respectively. STATISTICAL ANALYSIS USED: Paired t test, Independent sample t test, ANOVA test. RESULTS: The mean preoperative mouth opening in group 1 was 8.5 mm and in group 2 was 11.75 mm. The mean increase in group 1 after one year of postoperative period was 21.50 mm and in group 2 was 24.75 mm. CONCLUSIONS: In the present study, buccal fat pad graft proved to give better results as the interposition material as it has good patient acceptance, rapid epithelization, minimal donor site morbidity and minimal intra and postoperative complications.
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In present work, the influence of reservoir pH conditions on dynamics of microbial enhanced oil recovery (MEOR) processes using Pseudomonas putida was analysed numerically from the developed mathematical model for MEOR processes. Further, a new strategy to improve the MEOR performance has also been proposed. It is concluded from present study that by reversing the reservoir pH from highly acidic to low alkaline condition (pH 5-8), flow and mobility of displaced oil, displacement efficiency, and original oil in place (OOIP) recovered gets significantly enhanced, resulting from improved interfacial tension (IFT) reduction by biosurfactants. At pH 8, maximum of 26.1% of OOIP was recovered with higher displacement efficiency. The present study introduces a new strategy to increase the recovery efficiency of MEOR technique by characterizing the biosurfactants for IFTmin/IFTmax values for different pH conditions and subsequently, reversing the reservoir pH conditions at which the IFTmin/IFTmax value is minimum.
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Modelos Teóricos , Aceites , Pseudomonas putida/metabolismo , Tensoactivos/química , Yacimiento de Petróleo y Gas , Petróleo , Tensión SuperficialRESUMEN
The extent of dissolution of petroleum hydrocarbon fuels into groundwater depends greatly on fuel composition. Petroleum fuels can consist of thousands of compounds creating different interactions within the non-aqueous phase liquid (NAPL), thereby affecting the relative dissolution of the components and hence a groundwater plume's composition over long periods. Laboratory experiments were conducted to study the variability in the effective solubilities and activity coefficients for common constituents of gasoline fuels (benzene, toluene, p-xylene and 1,2,4-trimethylbenzene) (BTX) in matrices with an extreme range of molar volumes and chemical affinities. Four synthetic mixtures were investigated comprising BTX with the bulk of the NAPL mixtures made up of either, ethylbenzene (an aromatic like BTX with similar molar volume); 1,3,5-trimethylbenzene (an aromatic with a greater molar volume); n-hexane (an aliphatic with a low molar volume); and n-decane (an aliphatic with a high molar volume). Equilibrium solubility values for the constituents were under-predicted by Raoult's law by up to 30% (higher experimental concentrations) for the mixture with n-hexane as a filler and over-predicted by up to 12% (lower experimental concentrations) for the aromatic mixtures with ethylbenzene and 1,3,5-trimethylbenzene as fillers. Application of PP-LFER (poly-parameter linear free energy relationship) model for non-ideal mixtures also resulted in poor correlation between experimentally measured and predicted concentrations, indicating that differences in chemical affinities can be the major cause of deviation from ideal behavior. Synthetic mixtures were compared with the dissolution behavior of fresh and naturally weathered unleaded gasoline. The presence of lighter aliphatic components in the gasoline had a profound effect on estimating effective solubility due to chemical affinity differences (estimated at 0.0055 per percentage increase in the molar proportion of aliphatic) as well as reduced molar volumes (estimated at -0.0091 in the activity coefficient per unit increase in molar volume, mL/mol). Previously measured changes in activity coefficients due to natural weathering of 0.25 compares well to 0.27 calculated here based on changes in the chemical affinity and molar volumes. The study suggests that the initial estimation of the composition of a fuel is crucial in evaluating dissolution processes due to ideal and non-ideal dissolution, and in predicting long term dissolution trends and the longevity of NAPL petroleum plume risks.
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Gasolina , Contaminantes Químicos del Agua/química , Benceno/química , Derivados del Benceno/química , Gasolina/análisis , Agua Subterránea , Hexanos/química , Solubilidad , Tolueno/química , Contaminantes Químicos del Agua/análisis , Xilenos/químicaRESUMEN
pH and resident time of injected slug plays a critical role in characterizing the reservoir for potential microbial enhanced oil recovery (MEOR) application. To investigate MEOR processes, a multispecies (microbes-nutrients) reactive transport model in porous media was developed by coupling kinetic and transport model. The present work differs from earlier works by explicitly determining parametric values required for kinetic model by experimental investigations using Pseudomonas putida at different pH conditions and subsequently performing sensitivity analysis of pH, resident time and water saturation on concentrations of microbes, nutrients and biosurfactant within reservoir. The results suggest that nutrient utilization and biosurfactant production are found to be maximum at pH 8 and 7.5 respectively. It is also found that the sucrose and biosurfactant concentrations are highly sensitive to pH rather than reservoir microbial concentration, while at larger resident time and water saturation, the microbial and nutrient concentrations were lesser due to enhanced dispersion.
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Biocombustibles , Modelos Teóricos , Pseudomonas putida/metabolismo , Medios de Cultivo , Concentración de Iones de Hidrógeno , Cinética , Pseudomonas putida/crecimiento & desarrollo , Sacarosa/metabolismo , Tensoactivos/químicaRESUMEN
Knowledge about distribution of dissolved plumes and their influencing factors is essential for risk assessment and remediation of light non-aqueous phase liquid contamination in groundwater. Present study deals with the applicability of numerical model for simulating various hydro-geological scenarios considering non-uniform source distribution at a petroleum contaminated site in Chennai, India. The complexity associated with the hydrogeology of the site has limited scope for on-site quantification of petroleum pipeline spillage. The change in fuel composition under mass-transfer limited conditions was predicted by simultaneously comparing deviations in aqueous concentrations and activity coefficients (between Raoult's law and analytical approaches). The effects of source migration and weathering on the dissolution of major soluble fractions of petroleum fuel were also studied in relation to the apparent change in their activity coefficients and molar fractions. The model results were compared with field observations and found that field conditions were favourable for biodegradation, especially for the aromatic fraction (benzene and toluene (nearly 95% removal), polycyclic aromatic hydrocarbons (up to 65% removal) and xylene (nearly 45% removal). The results help to differentiate the effect of compositional non-ideality from rate-limited dissolution towards tailing of less soluble compounds (alkanes and trimethylbenzene). Although the effect of non-ideality decreased with distance from the source, the assumption of spatially varying residual saturation could effectively illustrate post-spill scenario by estimating the consequent decrease in mass transfer rate.
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Agua Subterránea/química , Modelos Teóricos , Petróleo/análisis , Hidrocarburos Policíclicos Aromáticos/química , Contaminantes Químicos del Agua/química , Biodegradación Ambiental , Contaminación Ambiental/análisis , India , Movimientos del Agua , Contaminantes Químicos del Agua/análisisRESUMEN
The proximate composition and bioactive components were screened in eight wheat bran cultivars such as UAS (304, 415, 428), DWR (162, 185, 1006) and DDK (1025, 1029). The results showed that carbohydrate content ranged from 62.3 to 73.9%, protein 11-21%, fat 2.4-5.6%, ash content 5-6.5% among the wheat bran genotypes and dietary fiber content was found to be between 21 and 52%. Mineral content vary viz., Fe (0.7-2.45), Mg (4.78-8.36), K (16.47-44.58), Zn (0.78-1.44), Cu (3.35-15.79), Na (1.22-7.14) and Mn (21.77-70.09) µg/gm, highest being in UAS-428 variety, except for Ca content. Linoleic acid was the major fatty acid present to the extent of 47-53%. The antioxidant capacity of wheat bran extract through free radical scavenging showed the IC50 values (mg/mL) of 9.4 for UAS 428 and 10.55 for UAS 415 indicating higher activity. The steryl ferulates, total tocopherols and carotenoids were estimated as fat soluble nutraceuticals. Higher content of steryl ferulate was observed in DWR 185 (477 mg/100 g) followed by DDK 1025 (465 mg/100 g) and the least in UAS 415 (119 mg/100 g) variety. In conclusion genotypic wheat bran is an important source of dietary micronutrients like minerals especially in UAS variety with a potential free radical reducing ability. These varieties have health protective properties and can be incorporated in various food formulations for improved lifestyles.
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Two organic cocrystals namely, 1,10-phenanthroline-5,6-dione:2-naphthoxyacetic acid [(phendione)(2-naa)] (1) and 1,10-phenanthroline-5,6-dione:2-formylphenoxyacetic acid [(phendione)(2-fpaa)] (2) were synthesized and studied by single crystal XRD, FT-IR, NMR, thermogravimetric, and powder X-ray diffraction analysis. The molecular properties of cocrystals were studied using density functional theory (DFT), basis set B3LYP/6-31G(d,p). Both cocrystals are stabilized through intermolecular hydrogen bonding (OHâ¯N). The total electron density and molecular electrostatic potential surfaces of the cocrystals were constructed by NBO analysis using B3LYP/6-31G(d,p) method to display the electrostatic potential (electron+nuclei) distribution. The energy gap between HOMO and LUMO was measured for both cocrystals.
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Ácido Acético/química , Modelos Moleculares , Fenantrolinas/química , Espectroscopía de Resonancia Magnética con Carbono-13 , Cristalografía por Rayos X , Electrones , Enlace de Hidrógeno , Conformación Molecular , Polvos , Espectroscopía de Protones por Resonancia Magnética , Espectroscopía Infrarroja por Transformada de Fourier , TermogravimetríaRESUMEN
The inclusion complexation behavior of phenoxyaliphatic acid derivatives of 3,3'-bis(indolyl)methane (BIMs 1-5) with ß-cyclodextrin (ß-CD) were investigated in both solution and solid state by means of UV-Visible, fluorescence spectroscopy, FT-IR and (1)H NMR techniques. The nature of the host-guest inclusion complex between BIMs and ß-CD has been elucidated. The experimental results confirmed the existence of 1:1 inclusion complex of BIMs with ß-CD. The binding constants describing the extent of formation of the complexes have been determined using Benesi-Hildebrand plots using UV-Vis and fluorescence spectroscopy. BIMs exhibited an affinity for ß-CD. The spectral studies suggested the phenyl ring along with alkyl substitutions of BIMs is present inside of ß-CD cavity.
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Ácidos Grasos/química , Indoles/química , Fenoles/química , beta-Ciclodextrinas/química , Ácidos Grasos/metabolismo , Concentración de Iones de Hidrógeno , Indoles/metabolismo , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Fenoles/metabolismo , Espectrometría de Fluorescencia , Espectrofotometría Ultravioleta , Espectroscopía Infrarroja por Transformada de Fourier , beta-Ciclodextrinas/metabolismoRESUMEN
A series of novel aryl-3,3'-bis(indolyl)methanes (BIMs) were synthesized using indole and formylphenoxyaliphatic acid(s) in water in the absence of any catalyst. The formylphenoxyaliphatic acid behaves as an in situ Bronsted-Lowry acid catalyst in water. UV-Visible and fluorescence spectra of the compounds were recorded in selected solvents. The gas phase geometry optimization of the compounds were achieved using DFT calculations at B3LYP/3-21G((*)) level of theory. The electronic properties, such as HOMO-LUMO energies were calculated using the above method based on the optimized structure. Compounds have better DPPH radical scavenging activity and reduction of oxidative damage of DNA.
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ADN/metabolismo , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Indoles/química , Indoles/farmacología , Animales , Compuestos de Bifenilo/metabolismo , Bovinos , Cristalografía por Rayos X , Depuradores de Radicales Libres/síntesis química , Indoles/síntesis química , Modelos Moleculares , Picratos/metabolismoRESUMEN
A series of novel clubbed Isopropylthiazole derivatives triazolothiadiazines 2a-g, dihydro triazolothiadiazoles 3a-g, thioxotriazoles 4a-d, triazolothiadiazole 5, arylideneamino triazolethiones 7a-h and oxadiazolethiones 11a-b were synthesized and characterized by IR, (1)H NMR, (13)C NMR, elemental and mass spectral analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by broth dilution assay method. All the compounds exhibited moderate to significant antibacterial and antifungal activities. Results of the antitubercular screening against M. tuberculosis H(37)Rv showed compounds 7c and 7d exhibited good antitubercular activity (MIC 4 and 8 µg/mL) respectively, when compared with first line drug such as isoniazid (0.25 µg/mL).
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Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Antituberculosos/síntesis química , Antituberculosos/farmacología , Tiazoles/síntesis química , Tiazoles/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Espectrofotometría InfrarrojaRESUMEN
In the present study a series of 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazole derivatives have been synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral analysis. Synthesized compounds were evaluated for their preliminary cytotoxicity, antimicrobial and antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Antimycobacterial activity tested against M. tuberculosis indicated that compounds 4b and 6g exhibited twofold enhanced potency than parent compound 1 and the results indicate that some of them exhibited promising activities and they deserve more consideration as potential antitubercular agents. Compound 3c, 4b and 6c exhibited good or moderate antibacterial inhibition and compounds 3h and 7c showed excellent antifungal activity.
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Antibacterianos/farmacología , Antineoplásicos/farmacología , Antituberculosos/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Tiazoles/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Antineoplásicos/síntesis química , Antineoplásicos/química , Antituberculosos/síntesis química , Antituberculosos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Oxadiazoles/química , Estereoisomerismo , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiazoles/química , Triazoles/químicaRESUMEN
Chemical investigation of the stem bark of Oroxylum indicum resulted in the isolation and characterization of two new flavonoid glycosides (1, 2), along with seven known compounds (3-9). Their structures were established on the basis of extensive spectroscopic (IR, MS, 2D NMR) data analysis and by the comparison with spectroscopic data reported in the literature. In addition, all the compounds were tested for their ulcer protective effects against various gastric ulceritis inducing models in rats.
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Antiulcerosos/química , Bignoniaceae/química , Flavanonas/química , Flavonas/química , Flavonoides/química , Animales , Antiulcerosos/aislamiento & purificación , Antiulcerosos/farmacología , Modelos Animales de Enfermedad , Flavanonas/aislamiento & purificación , Flavanonas/farmacología , Flavonas/aislamiento & purificación , Flavonas/farmacología , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Espectroscopía de Resonancia Magnética , Corteza de la Planta/química , Tallos de la Planta/química , RatasRESUMEN
Interaction of the protoberberine alkaloids berberine, palmatine, and coralyne with the two double-stranded RNA homopolymers of cytidine-guanosine (CG) and inosine-cytidine (IC) sequences in the protonated conformation was investigated using various biophysical techniques. All the three alkaloids bound polyC(+)G in a cooperative way. The binding of coralyne to both the polyribonucleotides was stronger than that of berberine and palmatine. Evidence for the intercalative binding of coralyne was revealed from fluorescence quenching studies. Isothermal titration calorimetry results suggested that the binding of berberine to both the polymers and palmatine to polyIC(+) was very weak while that of palmatine and coralyne to polyC(+)G and polyIC(+) was predominantly entropy driven. Circular dichroic results provided evidence for the perturbation of the RNA conformation with the bound coralyne in a more deeply intercalated position compared to berberine and palmatine as revealed by induced circular dichroism peaks. Taken together, the present study suggests that planarity of coralyne results in a more favorable and stronger binding to the double-stranded RNA conformations compared to berberine and palmatine that may potentiate its use in RNA-targeted drug design.
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Alcaloides de Berberina/metabolismo , Berberina/metabolismo , Protones , ARN/química , ARN/metabolismo , Berberina/farmacología , Alcaloides de Berberina/farmacología , Productos Biológicos/metabolismo , Productos Biológicos/farmacología , Calorimetría , Concentración de Iones de Hidrógeno , Conformación de Ácido Nucleico/efectos de los fármacos , Poli I-C , Análisis Espectral , TermodinámicaRESUMEN
In the present study a series of 4-isopropylthiazole-2-carbohydrazide analogs, derived clubbed oxadiazole-thiazole and triazole-thiazole derivatives have been synthesized and characterized by IR, (1)H NMR, (13)C NMR, elemental and mass spectral analyses. The synthesized compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by broth dilution assay method. The synthesized compounds 7a, 7b, 7d and 4 showed an antitubercular efficacy considerably greater than that of the parent 4-isopropyl-1,3-thiazole-2-carbohydrazide 1, suggesting that the substituted 4-isopropylthiazole-2-carbohydrazide moiety plays an important role in enhancing the antitubercular properties of this class of compounds. Compounds 2c, 3, 4, 6d, 7a and 7b exhibited good or moderate antibacterial and antifungal activity. Compounds 4 and 7b showed appreciable cytotoxicity at a concentration of 250muM.