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1.
Medicina (Kaunas) ; 55(7)2019 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-31269687

RESUMO

Background and objectives: The etiology of anemia associated with heart failure is not fully understood, but there are data suggesting the involvement of multiple mechanisms, including various drug therapies used in patients with heart failure. Our primary objective was to evaluate the impact of beta blockers, angiotensin-converting enzyme inhibitors, and calcium-channel blockers on iron metabolism in patients with heart failure. Materials and Methods: This was a prospective observational study that included patients diagnosed with heart failure and iron deficiency (defined by ferritin <100 µg/L, or 100-300 µg/L with transferrin saturation <20%). Patients with anemia secondary to a known cause were excluded. Results: We found a statistically significant correlation between beta-blocker treatment and ferritin values (p = 0.02). Iron, hemoglobin, and hematocrit levels were significantly lower in the patients using calcium-channel blockers than those who were not. We also found a statistically significant indirect correlation (p = 0.04) between the use of angiotensin-converting enzyme inhibitors and hematocrit levels. Conclusion: The contribution of our study arises from the additional data regarding the drug-induced etiology of iron deficiency. Practitioners should be aware of the potential impact of therapeutic recommendations and this should imply a close monitoring of the biochemical parameters of iron deficiency in this category of patients.


Assuntos
Anemia/etiologia , Insuficiência Cardíaca/tratamento farmacológico , Distúrbios do Metabolismo do Ferro/etiologia , Antagonistas Adrenérgicos beta/efeitos adversos , Antagonistas Adrenérgicos beta/uso terapêutico , Idoso , Anemia/sangue , Anemia/complicações , Inibidores da Enzima Conversora de Angiotensina/efeitos adversos , Inibidores da Enzima Conversora de Angiotensina/uso terapêutico , Bloqueadores dos Canais de Cálcio/efeitos adversos , Bloqueadores dos Canais de Cálcio/uso terapêutico , Feminino , Insuficiência Cardíaca/sangue , Humanos , Ferro/análise , Ferro/sangue , Distúrbios do Metabolismo do Ferro/sangue , Masculino , Pessoa de Meia-Idade
2.
Materials (Basel) ; 12(4)2019 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-30781782

RESUMO

In the past many research studies have focused on the thiazolidine-4-one scaffold, due to the important biological effects associated with its heterocycle. This scaffold is present in the structure of many synthetic compounds, which showed significant biological effects such as antimicrobial, antifungal, antioxidant, anti-inflammatory, analgesic, antidiabetic effects. It was also identified in natural compounds, such as actithiazic acid, isolated from Streptomyces strains. Starting from this scaffold new xanthine derivatives have been synthetized and evaluated for their antibacterial and antifungal effects. The antibacterial action was investigated against Gram positive (Staphyloccoccus aureus ATCC 25923, Sarcina lutea ATCC 9341) and Gram negative (Escherichia coli ATCC 25922) bacterial strains. The antifungal potential was investigated against Candida spp. (Candida albicans ATCC 10231, Candida glabrata ATCC MYA 2950, Candida parapsilosis ATCC 22019). In order to improve the antimicrobial activity, the most active xanthine derivatives with thiazolidine-4-one scaffold (XTDs: 6c, 6e, 6f, 6k) were included in a chitosan based polymeric matrix (CS). The developed polymeric systems (CS-XTDs) were characterized in terms of morphological (aspect, particle size), physic-chemical properties (swelling degree), antibacterial and antifungal activities, toxicity, and biological functions (bioactive compounds loading, entrapment efficiency). The presence of xanthine-thiazolidine-4-one derivatives into the chitosan matrix was confirmed using Fourier transform infrared (FT-IR) analysis. The size of developed polymeric systems, CS-XTDs, ranged between 614 µm and 855 µm, in a dry state. The XTDs were encapsulated into the chitosan matrix with very good loading efficiency, the highest entrapment efficiency being recorded for CS-6k, which ranged between 87.86 ± 1.25% and 93.91 ± 1.41%, depending of the concentration of 6k. The CS-XTDs systems showed an improved antimicrobial effect with respect to the corresponding XTDs. Good results were obtained for CS-6f, for which the effects on Staphylococcus aureus ATCC 25923 (21.2 ± 0.43 mm) and Sarcina lutea ATCC 9341 (25.1 ± 0.28 mm) were comparable with those of ciprofloxacin (25.1 ± 0.08 mm/25.0 ± 0.1 mm), which were used as the control. The CS-6f showed a notable antifungal effect, especially on Candida parapsilosis ATCC 22019 (18.4 ± 0.42 mm), the effect being comparable to those of nystatin (20.1 ± 0.09 mm), used as the control. Based on the obtained results these polymeric systems, consisting of thiazolidine-4-one derivatives loaded with chitosan microparticles, could have important applications in the food field as multifunctional (antimicrobial, antifungal, antioxidant) packaging materials.

3.
Eur J Pharm Sci ; 127: 71-78, 2019 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-30339870

RESUMO

The safety profile of new antidiabetic xanthine derivatives with thiazolidine­4­one scaffold (6, 7) and their new chitosan based formulations (CS-6, CS-7), administrated to diabetic rats, have been evaluated in terms of biochemical markers of liver and kidney function as well as of hematological markers. The effect on lipid profile and clinic parameters (body weight, food and water intake) has been also evaluated. The treatment of diabetic rats with xanthine derivatives (6, 7) and chitosan based formulations (CS-6, CS-7) was associated with lower liver enzymes (AST, ALT, LDH) and bilirubin (direct, total) values compared to the non-treated diabetic rats, that means the tested derivatives/formulations have improved the liver function injured in diabetes mellitus conditions. Also the kidney biochemical markers (creatinine, uric acid, urea) were significantly decreased in diabetic rats treated with 6, 7 and chitosan microparticles (CS-6, CS-7). The values of biochemical markers of liver and kidney functions were even better than the values recorded for pioglitazone, used as standard antidiabetic drug. The improving effect on kidney function was proved by the histopathological study. Moreover, the xanthine derivatives and their chitosan based formulation were associated with improved hematological markers compared to the non-treated diabetic rats which mean the improving of the hemorheological state. These results support the safety profile of new xanthine derivatives with thiazolidine­4­one scaffold (6, 7) and their new chitosan based formulations (CS-6, CS-7) and their potential applications for the treatment of diabetes mellitus syndrome.


Assuntos
Quitosana/administração & dosagem , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Tiazolidinas/administração & dosagem , Xantinas/administração & dosagem , Animais , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Testes Hematológicos , Rim/efeitos dos fármacos , Rim/patologia , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Ratos
4.
J Org Chem ; 82(24): 13700-13707, 2017 12 15.
Artigo em Inglês | MEDLINE | ID: mdl-29131628

RESUMO

This work reports the design of [1,3,4]thiadiazolo[3',2':1,2]imidazo[4,5-c]quinolines using a Pictet-Spengler reaction. The scope of the reaction was achieved from 6-(2-aminophenyl)imidazo[2,1-b][1,3,4]thiadiazole derivatives and available aldehydes. A wide range of aldehydes were employed to examine the scope of the cyclization. In parallel, a mechanism investigation was realized and showed a hydride transfer which led to a dismutation of the intermediate species. To complete this methodological study, a "sequential" oxidation/SNAr procedure was performed to achieve C-2 nucleophilic substitution using several amine types.

5.
Chem Cent J ; 11: 12, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28203273

RESUMO

BACKGROUND: The xanthine structure has proved to be an important scaffold in the process of developing a wide variety of biologically active molecules such as bronchodilator, hypoglycemiant, anticancer and anti-inflammatory agents. It is known that hyperglycemia generates reactive oxygen species which are involved in the progression of diabetes mellitus and its complications. Therefore, the development of new compounds with antioxidant activity could be an important therapeutic strategy against this metabolic syndrome. RESULTS: New thiazolidine-4-one derivatives with xanthine structure have been synthetized as potential antidiabetic drugs. The structure of the synthesized compounds was confirmed by using spectral methods (FT-IR, 1H-NMR, 13C-NMR, 19F-NMR, HRMS). Their antioxidant activity was evaluated using in vitro assays: DPPH and ABTS radical scavenging ability and phosphomolybdenum reducing antioxidant power assay. The developed compounds showed improved antioxidant effects in comparison to the parent compound, theophylline. In the case of both series, the intermediate (5a-k) and final compounds (6a-k), the aromatic substitution, especially in para position with halogens (fluoro, chloro), methyl and methoxy groups, was associated with an increase of the antioxidant effects. CONCLUSIONS: For several thiazolidine-4-one derivatives the antioxidant effect of was superior to that of their corresponding hydrazone derivatives. The most active compound was 6f which registered the highest radical scavenging activity.Graphical abstractDesign and synthesis of new thiazolidine-4-one derivatives.

6.
Rev Med Chir Soc Med Nat Iasi ; 120(2): 434-8, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27483731

RESUMO

AIM: To synthesize some new azetidin-2-ones of ferulic acid and to evaluate them from physicochemical and spectral point of view. MATERIAL AND METHODS: The synthesis was carried out in several steps: (i) obtaining the ferulic acid chloride; (ii) obtaining the ferulic acid hydrazide with hydrazine hydrate (98%); (iii) condensation of ferulic acid hydrazide with different benzaldehydes (2-hydroxy-/2-nitro-/4-chloro-/4- fluoro-/4-bromo-benzaldehyde) in order to obtain the corresponding hydrazones; (iv) cy- clization of ferulic acid hydrazones with chloroacethyl chloride in freshly distilled toluene medium and in the presence of triethylamine, resulting in the corresponding azetidin-2-ones. RESULTS: Six new azetidin-2-ones of ferulic acid were synthesized. They were characterized in terms of their physicochemical properties and their structure was confirmed by IR and 1H-NMR spectroscopy. CONCLUSIONS: Six new azetidin-2-ones of ferulic acid were synthesized, physicochemically characterized and validated spectrally. A


Assuntos
Antioxidantes/síntese química , Azetidinas/síntese química , Carcinógenos/química , Cloretos/química , Ácidos Cumáricos/química , Hidrazinas/química , Indicadores e Reagentes/química , Benzaldeídos/química , Etilaminas/química , Hidrazonas/química , Solventes/química , Espectrofotometria Infravermelho/métodos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Tolueno/química
7.
Rev Med Chir Soc Med Nat Iasi ; 120(2): 439-44, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27483732

RESUMO

UNLABELLED: L-Arginine is an a-amino acid which plays important roles in different diseases or processes, such as Alzheimer disease, inflammatory process, healing and tissue regeneration and it also could be useful as an anti-atherosclerotic agent. AIM: Considering the large amount of studies on the beneficial effects of different antioxidants, this paper is focused on the evaluation of the antioxidant potential of some imine derivatives, synthesized by the authors and described in a previous article. MATERIAL AND METHODS: The evaluation of the antioxidant power was performed using phosphomolydenum-reducing antioxidant power (PRAP) and ferric reducing antioxidant power (FRAP) assays, tests described in the literature and which are used with some minor modifications. RESULTS: It was found that most of the imine derivatives are more active than the L-Arginine in the PPAP and FRAP assays. The most active derivative was the compound obtained by condensation of L-arginine with 2,3-dihydroxybenzaldehyde (2k) and 2-nitrobenzaldehyde (2g). CONCLUSIONS: Following the described protocol, some imine derivatives of L-arginine were evaluated in terms of antioxidant potential using in vitro methods. The most favorable influence was obtained by the aromatic substitution with nitro and hydroxyl, the corresponding derivatives being the most active derivatives compared to L-arginine.


Assuntos
Antioxidantes/farmacologia , Arginina/síntese química , Benzaldeídos/síntese química , Catecóis/síntese química , Avaliação Pré-Clínica de Medicamentos , Iminas/farmacologia , Antioxidantes/síntese química , Avaliação Pré-Clínica de Medicamentos/métodos , Iminas/síntese química , Técnicas In Vitro
8.
Molecules ; 21(7)2016 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-27367664

RESUMO

The present paper focuses on solid lipid particles (SLPs), described in the literature as the most effective lipid drug delivery systems that have been introduced in the last decades, as they actually combine the advantages of polymeric particles, hydrophilic/lipophilic emulsions and liposomes. In the current study, we present our most recent advances in the preparation of alendronate (AL)-loaded SLPs prepared by hot homogenization and ultrasonication using various ratios of a self-emulsifying lipidic mixture of Compritol 888, Gelucire 44/14, and Cremophor A 25. The prepared AL-loaded SLPs were investigated for their physicochemical, morphological and structural characteristics by dynamic light scattering, differential scanning calorimetry, thermogravimetric and powder X-ray diffraction analysis, infrared spectroscopy, optical and scanning electron microscopy. Entrapment efficacy and actual drug content were assessed by a validated HPLC method. In vitro dissolution tests performed in simulated gastro-intestinal fluids and phosphate buffer solution pH 7.4 revealed a prolonged release of AL of 70 h. Additionally, release kinetics analysis showed that both in simulated gastrointestinal fluids and in phosphate buffer solution, AL is released from SLPs based on equal ratios of lipid excipients following zero-order kinetics, which characterizes prolonged-release drug systems.


Assuntos
Alendronato/administração & dosagem , Conservadores da Densidade Óssea/administração & dosagem , Sistemas de Liberação de Medicamentos , Lipossomos , Administração Oral , Administração Tópica , Varredura Diferencial de Calorimetria , Portadores de Fármacos , Liberação Controlada de Fármacos , Lipídeos/química , Lipossomos/química , Lipossomos/ultraestrutura , Análise Espectral , Difração de Raios X
9.
Chem Cent J ; 10: 6, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26855668

RESUMO

BACKGROUND: l-Arginine is a semi-essential aminoacid with important role in regulation of physiological processes in humans. It serves as precursor for the synthesis of proteins and is also substrate for different enzymes such as nitric oxide synthase. This amino-acid act as free radical scavenger, inhibits the activity of pro-oxidant enzymes and thus acts as an antioxidant and has also bactericidal effect against a broad spectrum of bacteria. RESULTS: New thiazolidine-4-one derivatives of nitro-l-arginine methyl ester (NO2-Arg-OMe) have been synthesized and biologically evaluated in terms of antioxidant and antibacterial/antifungal activity. The structures of the synthesized compounds were confirmed by (1)H, (13)C NMR, Mass and IR spectral data. The antioxidant potential was investigated using in vitro methods based on ferric/phosphomolybdenum reducing antioxidant power and DPPH/ABTS radical scavenging assay. The antibacterial effect was investigated against Gram positive (Staphylococcus aureus ATCC 25923, Sarcina lutea ATCC 9341) and Gram negative (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853) bacterial strains. The antifungal activity was also investigated against Candida spp. (Candida albicans ATCC 10231, Candida glabrata ATCC MYA 2950, Candida parapsilosis ATCC 22019). CONCLUSIONS: Synthesized compounds showed a good antioxidant activity in comparison with the NO2-Arg-OMe. The antimicrobial results support the selectivity of tested compounds especially on P. aeruginosa as bacterial strain and C. parapsilosis as fungal strain. The most proper compounds were 6g (R = 3-OCH3) and 6h (R = 2-OCH3) which showed a high free radical (DPPH, ABTS) scavenging ability and 6j (R = 2-NO2) that was the most active on both bacterial and fungal strains and also it showed the highest ABTS radical scavenging ability.Graphical abstract1: ethyl 3-aminopropionate hydrochloride, 2a-j: aromatic aldehydes, 3: thioglycolic acid, 4a-j: thiazolidine-propionic acid derivatives , 5: Nω-nitro-L-arginine methyl ester hydrochloride, 6a-j: thiazolidine-propionyl-nitro-L-arginine methyl ester derivatives.

10.
Carbohydr Polym ; 141: 28-40, 2016 May 05.
Artigo em Inglês | MEDLINE | ID: mdl-26876993

RESUMO

Chitosan is a non-toxic, biocompatible, biodegradable natural cationic polymer known for its low imunogenicity, antimicrobial, antioxidant effects and wound-healing activity. To improve its therapeutic potential, new chitosan-sulfonamide derivatives have been designed to develop new wound dressing biomaterials. The structural, morphological and physico-chemical properties of synthesized chitosan derivatives were analyzed by FT-IR, (1)H NMR spectroscopy, scanning electron microscopy, swelling ability and porosity. Antimicrobial, in vivo testing and biodegradation behavior have been also performed. The chitosan derivative membranes showed improved swelling and biodegradation rate, which are important characteristics required for the wound healing process. The antimicrobial assay evidenced that chitosan-based sulfadiazine, sulfadimethoxine and sulfamethoxazole derivatives were the most active. The MTT assay showed that some of chitosan derivatives are nontoxic. Furthermore, the in vivo study on burn wound model induced in Wistar rats demonstrated an improved healing effect and enhanced epithelialization of chitosan-sulfonamide derivatives compared to neat chitosan. The obtained results strongly recommend the use of some of the newly developed chitosan derivatives as antimicrobial wound dressing biomaterials.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bandagens , Quitosana/análogos & derivados , Cicatrização/efeitos dos fármacos , Animais , Antibacterianos/química , Antifúngicos/química , Porosidade , Ratos , Ratos Wistar , Molhabilidade
11.
Nanomaterials (Basel) ; 6(11)2016 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-28335334

RESUMO

Chitosan (CH) nanofibrous structures containing sulfadiazine (SDZ) or sulfadiazine modified chitosan (SCH) in the form of functional nanoparticles attached to nanofibers (hybrid nanostructures) were obtained by mono-axial and coaxial electrospinning. The mono-axial design consisted of a SDZ/CH mixture solution fed through a single nozzle while the coaxial design consisted of SCH and CH solutions separately supplied to the inner and outer nozzle (or in reverse order). The CH ability to form nanofibers assured the formation of a nanofiber mesh, while SDZ and SCH, both in form of suspensions in the electrospun solution, assured the formation of active nanoparticles which remained attached to the CH nanofiber mesh after the electrospinning process. The obtained nanostructures were morphologically characterized by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The SDZ release profiles and kinetics were analyzed. The SDZ or SCH nanoparticles loosely attached at the surface of the nanofibers, provide a burst release in the first 20 min, which is important to stop the possible initial infection in a wound, while the SDZ and SCH from the nanoparticles which are better confined (or even encapsulated) into the CH nanofibers would be slowly released with the erosion/disruption of the CH nanofiber mesh.

12.
Rev Med Chir Soc Med Nat Iasi ; 120(3): 727-31, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-30152662

RESUMO

Aim: The in vitro antioxidant potential of new thiazolidin-4-one derivatives of ferulic acid was evaluated according to the total antioxidant activity and ferric reducing power assays. Material and Methods: The ferric reducing power assay was based on the reduction of ferricyanide to ferrocyanide, which form in the presence of ferric chloride a Perl Prussian blue color complex. The total antioxidant activity assay was assessed using phosphomolybdenum method. The results were expressed as effective concentration (EC50) values and ascorbic acid was used as positive control. All determinations were performed in triplicate. Results: It was found that the activity of the tested compounds is influenced by the substituents on phenyl ring of the thiazolidine-4-one moiety. The most active compound was 1i, which contains 2,3-diOH as substituent on phenyl ring. Conclusions: A total of 10 new thiazolidin-4-one derivatives of ferulic acid were investigated for their in vitro antioxidant activity. The most active compound 1i (R=2,3-diOH) proved to be about 4 times more active than ferulic acid and comparable to ascorbic acid in both antioxidant assays.


Assuntos
Antioxidantes/química , Ácidos Cumáricos/química , Tiazolidinas/química , Antioxidantes/síntese química , Ácido Ascórbico , Tiazolidinas/síntese química
13.
Int J Mol Sci ; 16(12): 29843-55, 2015 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-26694354

RESUMO

The objective of this study was to develop new films based on chitosan functionalized with sulfonamide drugs (sulfametoxydiazine, sulfadiazine, sulfadimetho-xine, sulfamethoxazol, sulfamerazine, sulfizoxazol) in order to enhance the biological effects of chitosan. The morphology and physical properties of functionalized chitosan films as well the antioxidant effects of sulfonamide-chitosan derivatives were investigated. The chitosan-derivative films showed a rough surface and hydrophilic properties, which are very important features for their use as a wound dressing. The film based on chitosan-sulfisoxazol (CS-S6) showed the highest swelling ratio (197%) and the highest biodegradation rate (63.04%) in comparison to chitosan film for which the swelling ratio was 190% and biodegradation rate was only 10%. Referring to the antioxidant effects the most active was chitosan-sulfamerazine (CS-S5) which was 8.3 times more active than chitosan related to DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging ability. This compound showed also a good ferric reducing power and improved total antioxidant capacity.


Assuntos
Bandagens , Quitosana/farmacologia , Sulfonamidas/farmacologia , Cicatrização/efeitos dos fármacos , Antioxidantes/farmacologia , Compostos de Bifenilo/química , Depuradores de Radicais Livres/química , Processamento de Imagem Assistida por Computador , Testes de Sensibilidade Microbiana , Microscopia de Força Atômica , Oxirredução , Picratos/química , Propriedades de Superfície , Água/química
14.
Rev Med Chir Soc Med Nat Iasi ; 119(2): 579-84, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26204670

RESUMO

Diabetes mellitus is a major health problem due to its increasing prevalence and life-threatening complications. Antidiabetic sulfonylureas represent the first-line drugs in type 2 diabetes even though the most common associated risk is pharmacologically-induced hypoglycemia. In the development of this side effect are involved several factors including the pharmacokinetic and pharmacodynamic profile of the drug, patient age and behavior, hepatic or renal dysfunctions, or other drugs associated with a high risk of interactions. If all these are controlled, the risk-benefit balance can be equal to other oral antidiabetic drugs.


Assuntos
Diabetes Mellitus Tipo 2 , Hipoglicemia/induzido quimicamente , Hipoglicemiantes/efeitos adversos , Compostos de Sulfonilureia/efeitos adversos , Clorpropamida/efeitos adversos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Gliclazida/efeitos adversos , Glipizida/efeitos adversos , Glibureto/efeitos adversos , Humanos , Hipoglicemiantes/administração & dosagem , Fatores de Risco , Compostos de Sulfonilureia/administração & dosagem , Tolbutamida/efeitos adversos
15.
Eur J Pharm Sci ; 77: 122-34, 2015 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-26079402

RESUMO

New xanthine derivatives as antidiabetic agents were synthesized and new chitosan formulations have been developed in order to improve their biological and pharmacokinetic profile. Their physicochemical properties in terms of particle size, morphology, swelling degree, crystalline state, the loading efficiency as well as in vitro release and biodegradation rate were evaluated. According to the results the optimized formulations have a high drug loading efficiency (more than 70%), small particle size, a good release profile in the simulated biological fluids (the percentage of cumulative release being more than 55%) and improved biodegradation rate in reference with chitosan microparticles. The presence of xanthine derivatives (6, 7) in chitosan microparticles was demonstrated by means of FTIR analysis. The X-ray diffraction (XRD) proved that xanthine derivatives present a crystalline state. The biological evaluation assays confirmed the antioxidant and antidiabetic effects of the xanthine derivatives (6, 7) and their chitosan formulations (CS-6, CS-7). Xanthine derivative 6 showed a high antiradical scavenging effect (DPPH remaining=41.78%). It also reduced the glucose blood level with 59.30% and recorded level of glycosylated hemoglobin was 4.53%. The effect of its chitosan formulation (CS-6) on the level of blood glucose (114.5mg/dl) was even more intense than the one recorded by pioglitazone (148.5mg/dl) when used as standard antidiabetic drug. These results demonstrated the potential application of xanthine derivative 6 and its chitosan formulation (CS-6) in the treatment of the diabetes mellitus syndrome.


Assuntos
Quitosana/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/química , Xantinas/química , Animais , Portadores de Fármacos , Avaliação Pré-Clínica de Medicamentos , Hipoglicemiantes/uso terapêutico , Espectroscopia de Ressonância Magnética , Camundongos , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X , Xantinas/uso terapêutico
16.
Rev Med Chir Soc Med Nat Iasi ; 119(4): 1189-94, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26793868

RESUMO

AIM: To develop sustained release matrix tablets based on xanthan as highly water-soluble, cost-effective, non-toxic, easily available, and suitable hydrophilic systems. MATERIAL AND METHODS: Xanthan and lignin epoxy-modified resin (LER) mixture were crosslinked using epichlorohydrin as crosslinking agent leading to superabsorbent hydrogels with high swelling rate in aqueous mediums. RESULTS AND CONCLUSIONS: These hydrogels were tested as carries by the loading/delivery behaviour of bisoprolol fumarate in physiological conditions and based on the obtained results these hydrogels may show interest for application in medical and pharmaceutical areas. The amount of drug loaded in polymer networks was found to be ranging between 14.4% and 19.2%. Drug release was retarded and the release mechanism of the active principle was found to depend on matrix composition.


Assuntos
Anti-Hipertensivos/farmacocinética , Bisoprolol/farmacocinética , Portadores de Fármacos/química , Hidrogéis/química , Lignina/química , Polissacarídeos Bacterianos/química , Anti-Hipertensivos/síntese química , Anti-Hipertensivos/química , Bisoprolol/síntese química , Bisoprolol/química , Química Farmacêutica , Preparações de Ação Retardada/química , Liberação Controlada de Fármacos , Técnicas In Vitro
17.
Materials (Basel) ; 8(1): 317-338, 2015 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-28787940

RESUMO

In the present study polyelectrolyte complexes (PECs) based on new sulfadiazine-chitosan conjugates with sodium hyaluronate have been developed with potential use in treatment of burn wounds. The PECs were chemically characterized using Fourier Transform-Infrared Spectroscopy, Scanning Electon Microscopy and Near Infrared Chemical Imaging Technique. The swelling behavior and in vitro sulfadiazine release were also investigated. The antimicrobial activity was evaluated towards three bacterial strains: Escherichia coli, Listeria monocytogenes and Salmonella thyphymurium. The developed PECs demonstrated their antimicrobial efficiency against tested bacterial strains, the PECs containing sulfadiazine-modified chitosan being more active than PECs containing unmodified chitosan.

18.
Molecules ; 19(9): 15005-25, 2014 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-25237755

RESUMO

New thiazolidine-4-one derivatives of 2-(4-isobutylphenyl)propionic acid (ibuprofen) have been synthesized as potential anti-inflammatory drugs. The structure of the new compounds was proved using spectral methods (FR-IR, 1H-NMR, 13C-NMR, MS). The in vitro antioxidant potential of the synthesized compounds was evaluated according to the total antioxidant activity, the DPPH and ABTS radical scavenging assays. Reactive oxygen species (ROS) and free radicals are considered to be involved in many pathological events like diabetes mellitus, neurodegenerative diseases, cancer, infections and more recently, in inflammation. It is known that overproduction of free radicals may initiate and amplify the inflammatory process via upregulation of genes involved in the production of proinflammatory cytokines and adhesion molecules. The chemical modulation of acyl hydrazones of ibuprofen 3a-l through cyclization to the corresponding thiazolidine-4-ones 4a-n led to increased antioxidant potential, as all thiazolidine-4-ones were more active than their parent acyl hydrazones and also ibuprofen. The most active compounds are the thiazolidine-4-ones 4e, m, which showed the highest DPPH radical scavenging ability, their activity being comparable with vitamin E.


Assuntos
Propionatos/síntese química , Propionatos/farmacologia , Antioxidantes/farmacologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Propionatos/química , Espectroscopia de Infravermelho com Transformada de Fourier
19.
Molecules ; 19(9): 13824-47, 2014 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-25255761

RESUMO

New thiazolidine-4-one derivatives based on the 4-aminophenazone (4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one) scaffold have been synthesized as potential anti-inflammatory drugs. The pyrazoline derivatives are known especially for their antipyretic, analgesic and anti-inflammatory effects, but recently there were synthesized new compounds with important antioxidant, antiproliferative, anticancer and antidiabetic activities. The beneficial effects of these compounds are explained by nonselective inhibition of cyclooxygenase izoenzymes, but also by their potential scavenging ability for reactive oxygen and nitrogen species. The structure of the new compounds was proved using spectroscopic methods (FR-IR, 1H-NMR, 13C-NMR, MS). The in vitro antioxidant potential of the synthesized compounds was evaluated according to the ferric reducing antioxidant power, phosphomolydenum reducing antioxidant power, DPPH and ABTS radical scavenging assays. The chemical modulation of 4-aminophenazone (6) through linkage to thiazolidine-propanoic acid derivatives 5a-l led to improved antioxidant potential, all derivatives 7a-l being more active than phenazone. The most active compounds are the derivatives 7e, and 7k, which showed the higher antioxidant effect depending on the antioxidant assay considered.


Assuntos
Desenho de Drogas , Avaliação Pré-Clínica de Medicamentos , Pirazóis/química , Tiazolidinas/química , Tiazolidinas/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Espectroscopia de Ressonância Magnética , Tiazolidinas/síntese química
20.
Rev Med Chir Soc Med Nat Iasi ; 118(1): 213-8, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24741803

RESUMO

AIM: To design new thiazolidin-4-ones derivatives and to evaluate their potential antioxidant effects using in vitro methods. MATERIAL AND METHODS: New ethyl esters of the 2-(R-phenyl)-4-oxo-thiazolidin-3-yl propionic acid were synthesized using "one step reaction" between different aromatic aldehydes, thioglycolic acid and beta-alanine ethyl ester hydrochloride. The antioxidant potential of the synthesized compounds was evaluated using the DPPH radical scavenging assay and phosphomolybdenum method. RESULTS: Eight thiazolidine-4-one derivatives were obtained in good yields and high purity. The structure of the synthesized compounds was confirmed using IR spectroscopy. The evaluation of antioxidant activity showed that 2-[(4-NO2)-phenyl]-4-oxo-thiazolidin-3-yl propionic acid ethyl ester (compound 16) was the most active compound. For this derivative the DPPH radical scavenger activity (I% = 91.63% +/- 0.77) and the total antioxidant capacity (absorbance = 1.0691 +/- 0.0763) were similar with that of ascorbic acid used as standard antioxidant. CONCLUSIONS: The antioxidant activity of the thiazolidine-4-one derivatives depends on the nature of the phenyl ring substituents, the NO2 and OH radicals having the most significant influence.


Assuntos
Antioxidantes/síntese química , Antioxidantes/farmacologia , Tiazolidinas/síntese química , Tiazolidinas/farmacologia , Aldeídos/síntese química , Antioxidantes/química , Cloretos/síntese química , Ésteres/síntese química , Depuradores de Radicais Livres , Espectroscopia de Infravermelho com Transformada de Fourier , Tiazolidinas/química , Tioglicolatos/síntese química , beta-Alanina/síntese química
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