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1.
Polymers (Basel) ; 14(18)2022 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-36145960

RESUMO

A novel drug delivery system based on carboxymethyl cellulose containing copper oxide at melamine and zinc oxide at melamine framework (CMC-Cu-MEL and CMC-Zn-MEL) was prepared by the hydrothermal route. Synthesized nanocomposites were characterized by FTIR, SEM, and Raman spectroscopy. In addition, transmission electron microscopy (TEM) and selected area electron diffraction (SAED) images were applied to confirm the particle size and diffraction pattern of the prepared nanocomposites. Furthermore, the crystallinity of the synthesized CMC, CMC-Cu-MEL, and CMC-Zn-MEL materials was studied via X-ray diffraction (XRD). Estimating the transport exponent, which discloses the solvent diffusion and chain relaxation processes, and the Ritger-Peppas kinetic model theory were used to control the TC release mechanism from CMC-Cu-MEL and CMC-Zn-MEL. Additionally, the CMC-Cu-MEL and CMC-Zn-MEL containing TC had the highest activity index percents of 99 and 106% against S. aureus and 93 and 99% against E. coli, respectively. The tailored CMC-Cu-MEL and CMC-Zn-MEL for drug delivery systems are expected to be feasible and efficient.

2.
Polymers (Basel) ; 14(2)2022 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-35054635

RESUMO

In this work, a Zn-benzenetricarboxylic acid (Zn@H3BTC) organic framework coated with a dispersed layer of chitosan (CH/Zn@H3BTC) was synthesized using a solvothermal approach. The synthesized CH/Zn@H3BTC was characterized by Fourier transform infrared spectroscopy (FTIR), field emission scanning electron microscope (FESEM), thermal gravimetric analysis (TGA), and Brunauer, Emmett, and Teller (BET) surface area. The microscopic observation and the analysis of the BET surface area of CH/Zn@H3BTC nanocomposites indicated that chitosan plays an important role in controlling the surface morphology and surface properties of the Zn@H3BTC. The obtained findings showed that the surface area and particle size diameter were in the range of 80 m2 g-1 and 800 nm, respectively. The corrosion protection characteristics of the CH/Zn@H3BTC composite in comparison to pristine chitosan on duplex steel in 2.0 M H2SO4 medium determined by electrochemical (E vs. time, PDP, and EIS) approaches exhibited that the entire charge transfer resistance of the chitosan- and CH/Zn@H3BTC-composite-protected films on the duplex steel substrate was comparatively large, at 252.4 and 364.8 Ω cm2 with protection capacities of 94.1% and 97.8%, respectively, in comparison to the unprotected metal surface (Rp = 20.6 Ω cm2), indicating the films efficiently protected the metal from corrosion. After dipping the uninhabited and protected systems, the surface topographies of the duplex steel were inspected by FESEM. We found the adsorption of the CH/Zn@H3BTC composite on the metal interface obeys the model of the Langmuir isotherm. The CH/Zn@H3BTC composite revealed outstanding adsorption on the metal interface as established by MD simulations and DFT calculations. Consequently, we found that the designed CH/Zn@H3BTC composite shows potential as an applicant inhibitor for steel protection.

3.
Molecules ; 23(5)2018 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-29747479

RESUMO

Small heterocyclic compounds containing nitrogen and sulfur atoms, such as thiazole derivatives, represent a significant class of organic azoles that exhibit promising bioactivities and have a great potential in medicinal and agricultural fields. A convenient and high-yielding synthetic approach for a range of organic molecules is presented. The nuclease-like activities of compounds were studied with the aid of E. coli AB1157 DNA and agarose gel electrophoresis. The antioxidant evaluation of the compounds was carried out with different antioxidant techniques, such as ABTS and NO scavenging efficiency. The antibacterial behavior was evaluated against various bacterial strains, both Gram-positive and -negative, and the minimum inhibitory concentration (MIC) values of these compounds were determined. The antiproliferative activities and IC50 values of the synthesized organic molecules compounds against HEPG-2, MCF-7, and HCT-116 cell lines were evaluated.


Assuntos
Tiazóis/síntese química , Tiazóis/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , DNA/metabolismo , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Óxido Nítrico/metabolismo , Tiazóis/química
4.
Eur J Med Chem ; 139: 107-113, 2017 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-28800451

RESUMO

Two series of fused tricyclic sultams (carboxylates, 3a, b and 5a, f, g and anilides 5b-e) were synthesized from saccharin and their chemical structures were confirmed by spectroscopic tools. Then, their antibacterial activities and MIC were evaluated against two strains of gram positive and gram-negative bacteria. The MIC values of the tested compounds are in the of range 8-33 µg/ml. In addition, their DNA cleavage ability, binding affinity and their anticancer activities against hepatic cancer cell were tested. And their antioxidant activities were also measured. Four carboxylate derivatives (3a, 5a, 5f and 5g) and one anilide (5d) of the tested compounds proved to be the highest activity all over the study.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Sacarina/química , Sulfonamidas/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Clivagem do DNA/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Escherichia coli/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química
5.
Chin J Physiol ; 60(1): 54-61, 2017 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-28052646

RESUMO

Lead is one of the oldest environmental and occupational toxins. Health hazards from increased lead exposure as a result of industrial and environmental pollution are recognized. The aim of the present study was to investigate the protective effects of quercetin as a model of an antioxidant drug against the toxic effects of lead acetate on the blood and the testis of rats. The lead concentrations were determined in blood and the testis. Testosterone (T), luteinizing hormone (LH) and follicle stimulating hormone (FSH) were assessed in serum. Hemoglobin (Hb) content, packed cell volume (PCV), white blood cell (WBC) and red blood cell (RBC) counts were evaluated in the whole blood. Our results showed that administration of lead acetate was associated with an increased lead levels in blood as well as in the testis. Lead acetate administration also caused a decrease in testicular function, Hb content, PCV and RBC count in comparison to the respective mean values of the control. In addition, lead acetate increased WBC count and induced alterations in sperm count, sperm motility and sperm abnormality and histopathology. In the contrary, administration of lead acetate along with quercetin partially restored the studied parameters to normal values. In conclusion, the treatment with quercetin may provide a partial protection against the toxic effects induced by lead acetate in blood and the testis of rats.


Assuntos
Antioxidantes/uso terapêutico , Intoxicação por Chumbo/prevenção & controle , Quercetina/uso terapêutico , Doenças Testiculares/prevenção & controle , Animais , Antioxidantes/farmacologia , Chumbo/toxicidade , Masculino , Quercetina/farmacologia , Distribuição Aleatória , Ratos , Espermatozoides/efeitos dos fármacos , Testículo/efeitos dos fármacos
6.
Biomed Mater Eng ; 27(1): 87-99, 2016 May 12.
Artigo em Inglês | MEDLINE | ID: mdl-27175470

RESUMO

Biocompatible metals have been suggested as revolutionary biomaterials for bone-grafting therapies. Although metals and their alloys are widely and successfully used in producing biomedical implants due to their good mechanical properties and corrosion resistance, they have a lack in bioactivity. Therefore coating of the metal surface with calcium phosphates (CaP) is a benign way to achieve well bioactivity and get controlled corrosion properties. The biocompatibility and bioactivity calcium phosphates (CaP) in bone growth were guided them to biomedical treatment of bone defects and fractures. Many techniques have been used for fabrication of CaP coatings on metal substrates such as magnesium and titanium. The present review will focus on the synthesis of CaP and their relative forms using different techniques especially electrochemical techniques. The latter has always been known of its unique way of optimizing the process parameters that led to a control in the structure and characteristics of the produced materials.


Assuntos
Substitutos Ósseos/química , Fosfatos de Cálcio/química , Materiais Revestidos Biocompatíveis/química , Metais/química , Animais , Biomimética/métodos , Substitutos Ósseos/síntese química , Fosfatos de Cálcio/síntese química , Materiais Revestidos Biocompatíveis/síntese química , Técnicas Eletroquímicas/métodos , Humanos , Magnésio/química , Metais/síntese química , Ortopedia/métodos , Próteses e Implantes , Propriedades de Superfície
7.
PLoS One ; 10(12): e0144509, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26659465

RESUMO

The present study aims to investigate the hepatoprotective effect of taurine (TAU) alone or in combination with silymarin (SIL) on CCl4-induced liver damage. Twenty five male rats were randomized into 5 groups: normal control (vehicle treated), toxin control (CCl4 treated), CCl4+TAU, CCl4+SIL and CCl4+TAU+SIL. CCl4 provoked significant increases in the levels of hepatic TBARS, NO and NOS compared to control group, but the levels of endogenous antioxidants such as SOD, GPx, GR, GST and GSH were significantly decreased. Serum pro-inflammatory and fibrogenic cytokines including TNF-α, TGF-ß1, IL-6, leptin and resistin were increased while the anti-inflammatory (adiponectin) cytokine was decreased in all treated rats. Our results also showed that CCl4 induced an increase in liver injury parameters like serum ALT, AST, ALP, GGT and bilirubin. In addition, a significant increase in liver tissue hydroxyproline (a major component of collagen) was detected in rats exposed to CCl4. Moreover, the concentrations of serum TG, TC, HDL-C, LDL-C, VLDL-C and FFA were significantly increased by CCl4. Both TAU and SIL (i.e., antioxidants) post-treatments were effectively able to relieve most of the above mentioned imbalances. However, the combination therapy was more effective than single applications in reducing TBARS levels, NO production, hydroxyproline content in fibrotic liver and the activity of serum GGT. Combined treatment (but not TAU- or SIL-alone) was also able to effectively prevent CCl4-induced decrease in adiponectin serum levels. Of note, the combined post-treatment with TAU+SIL (but not monotherapy) normalized serum FFA in CCl4-treated rats. The biochemical results were confirmed by histological and ultrastructural changes as compared to CCl4-poisoned rats. Therefore, on the basis of our work, TAU may be used in combination with SIL as an additional adjunct therapy to cure liver diseases such as fibrosis, cirrhosis and viral hepatitis.


Assuntos
Anti-Inflamatórios/uso terapêutico , Sequestradores de Radicais Livres/uso terapêutico , Cirrose Hepática/tratamento farmacológico , Fígado/patologia , Substâncias Protetoras/uso terapêutico , Silimarina/uso terapêutico , Taurina/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/metabolismo , Biomarcadores/metabolismo , Tetracloreto de Carbono , Citocinas/sangue , Sequestradores de Radicais Livres/farmacologia , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Hepatócitos/ultraestrutura , Lipídeos/sangue , Fígado/efeitos dos fármacos , Fígado/ultraestrutura , Cirrose Hepática/sangue , Masculino , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase/metabolismo , Substâncias Protetoras/farmacologia , Ratos Wistar , Silimarina/farmacologia , Taurina/farmacologia
8.
Molecules ; 20(2): 2591-610, 2015 Feb 02.
Artigo em Inglês | MEDLINE | ID: mdl-25648599

RESUMO

An expedient synthesis of novel triazoles, tetrazine and thiadiazoles, using conveniently accessible and commercially available starting materials has been achieved. The synthesized compounds were characterized by spectroscopic and elemental analyses, and screened for their antibacterial activities against four different strains, namely E. coli, P. aeruginosa, S. aureus and B. megaterium. In particular, the compounds 5, 24 and 26h exhibited excellent antibacterial activities compared to the reference antibiotic. To get further insight about their behavior, these compounds were tested for their antioxidant activities via SOD-like activity, DPPH free radical scavenging activity, ABST and NO, which showed promising results. Furthermore, these compounds effectively promoted the cleavage of genomic DNA as well, in the absence of any external additives.


Assuntos
Antibacterianos/síntese química , Compostos Heterocíclicos com 1 Anel/síntese química , Tiadiazóis/síntese química , Triazóis/síntese química , Antibacterianos/farmacologia , Bacillus megaterium/efeitos dos fármacos , Clivagem do DNA , Escherichia coli/efeitos dos fármacos , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/farmacologia , Compostos Heterocíclicos com 1 Anel/farmacologia , Testes de Sensibilidade Microbiana , Óxido Nítrico/química , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Tiadiazóis/farmacologia , Triazóis/farmacologia
9.
Nat Prod Res ; 21(2): 156-60, 2007 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-17365703

RESUMO

A new germacranolide-type sesquiterpene lactone, 1alpha-hydroxy-3-oxo-7alpha,11betaH-germacra-4Z,9Z-dien-12,6alpha-olide (1), was isolated from the CH2Cl2--MeOH extract of the aerial parts of Tanacetum santolinoides. Its structure was determined by spectroscopic techniques including, IR, high-resolution-EIMS, and extensive 400 MHz one- and two-dimensional NMR-analysis (1H, 13C-NMR, DEPT, 1H--1H COSY, HMQC, HMBC, and NOE experiments).


Assuntos
Sesquiterpenos de Germacrano/química , Sesquiterpenos/química , Tanacetum/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Sesquiterpenos/isolamento & purificação , Sesquiterpenos de Germacrano/isolamento & purificação , Solventes/química
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