RESUMO
The present paper is focused on enhancing the production of biohydrogen (bioH2) from dairy cow manure (DCM) through dark fermentation (DF). Two enhancement production strategies have been tested: i) the combination of H2O2 with sonification as pretreatment and ii) the co-fermentation with cheese whey as co-substrate. Concerning the pretreatment, the best combination was investigated according to the response surface methodology (RSM) by varying H2O2 dosage between 0.0015 and 0.06 g/gTS and ultrasonic specific energy input (USEI) between 35.48 and 1419.36 J/gTS. The increase of carbohydrates concentration was used as target parameter. Results showed that the combination of 0.06 g/gTS of H2O2 with 1419.36 J/gTS of USEI maximized the concentration of carbohydrates. The optimized conditions were used to pretreat the substrate prior conducting DF tests. The use of pretreatment resulted in obtaining a cumulative bioH2 volume of 51.25 mL/L and enhanced the bioH2 production by 125% compared to the control test conducted using raw DCM. Moreover, the second strategy, i.e. co-fermentation with cheese whey (20% v/v) as co-substrate ended up to enhancing the DF performance as the bioH2 production reached a value of 334.90 mL/L with an increase of 1372% compared to the control DF test. To further improve the process, dark fermentation effluents (DFEs) were valorized via photo fermentation (PF), obtaining an additional hydrogen production aliquot.
Assuntos
Peróxido de Hidrogênio , Esterco , Animais , Bovinos , Fermentação , Soro do Leite , Proteínas do Soro do Leite , Carboidratos , HidrogênioRESUMO
Microalgae cultivation systems fed with wastewater as source of nutrients represents the principal sustainable condition to produce microalgal biomass to be converted conveniently to biofuels. In order to optimize microalgae growth and their lipid content, the effect of light intensity and nutrients load in real wastewater was investigated through batch microalgal cultivation tests. A microalgal polyculture was used as inoculum and grown for 10 days in batch at different conditions of light intensity (i.e. 20, 50 and 100⯵molâ¯s-1m-2) and nutrients concentration in wastewater. Experimental results showed that biomass productivity decreased for rich nutrients conditions and increased for high light intensities. The highest lipid mass content (29%) was found for high light intensity condition (100⯵molâ¯s-1m-2). Furthermore, microalgae settleability tests, conducted at the end of the cultivation time, resulted in the highest biomass recovery efficiency (72%) for low light intensity and nutrients supply conditions.
Assuntos
Lipídeos/análise , Microalgas , Águas Residuárias , Biocombustíveis , BiomassaRESUMO
INTRODUCTION: Cosmetic products contain a wide range of chemicals to which we are exposed every day. The aim of the study was to determine the presence of potential dangerous substances which can cause adverse health effects by examining product labels. MATERIALS AND METHODS: A total of 283 products were collected from various shops in Lecce (Italy) and divided into 3 categories: rinse-off, leave-on and make-up. The label of every product was examined and a list including fragrances, preservatives and other chemicals of concern was created. RESULTS: Fragrances were present in 52.3% of the examined products, mostly limonene (76.9%) and linalool (64.6%) but also citronellol (34.1%), geraniol (31.5%), coumarin (30%) and hexyl cinnamal (29.2%). Preservatives showed a rate of 60% and the most frequently identified were phenoxyethanol (48.7%), sodium benzoate (35.6%), potassium sorbate (22%), methylparaben (15.2%) and MI/MCI (9.9%). The other chemicals of concern were detected in 58% of products; included PEGs (62.3%), acrylate copolymer (34%), petrolatum (17.2%), polysorbates (14,8%), BHT (14.7%), ethylhextyl methoxycinnamate (13.6%), benzophenone-1 (3.7%), benzophenone-3 (4.9%), BHA (1.6%), cocamide DEA and toluene (1.2%). CONCLUSIONS: The use of many of these substances is allowed within certain limits, due to their toxicity at higher concentrations. Other important aspects should be considered as, for instance, the possibility of long-term effects. On the other hand, other substances may induce several acute adverse side-effects, i.e. contact dermatitis and allergic reactions. For these reasons, an enhancement of the criteria used for cosmetics formulation is required since many chemicals used singularly or combined are potentially unsafe.
Assuntos
Alérgenos/efeitos adversos , Cosméticos/química , Odorantes , Conservantes Farmacêuticos/efeitos adversos , Dermatopatias/induzido quimicamente , HumanosRESUMO
A new procedure, recently proposed for on-line monitoring of copper released from metal pipes in household plumbing system for drinking water distribution during the development of corrosion processes, is tested experimentally. Experiments were carried out in laboratory controlled conditions, using synthetic water and varying the water alkalinity. The possibility of using the corrosion potential as a surrogate measure of copper concentration in stagnating water is shown, verifying, in the meantime, the effect of alkalinity on the development of passivation phenomena, which tend to protect the pipe from corrosion processes. Experimental data are discussed, highlighting the potentiality of the procedure, and recognizing its limitations.
Assuntos
Cobre/análise , Monitoramento Ambiental , Purificação da Água/métodos , Água/químicaRESUMO
This paper presents a mathematical model able to simulate under dynamic conditions the physical, chemical and biological processes prevailing in a OFMSW and sewage sludge anaerobic digestion system. The model proposed is based on differential mass balance equations for substrates, products and bacterial groups involved in the co-digestion process and includes the biochemical reactions of the substrate conversion and the kinetics of microbial growth and decay. The main peculiarity of the model is the surface based kinetic description of the OFMSW disintegration process, whereas the pH determination is based on a nine-order polynomial equation derived by acid-base equilibria. The model can be applied to simulate the co-digestion process for several purposes, such as the evaluation of the optimal process conditions in terms of OFMSW/sewage sludge ratio, temperature, OFMSW particle size, solid mixture retention time, reactor stirring rate, etc. Biogas production and composition can also be evaluated to estimate the potential energy production under different process conditions. In particular, model simulations reported in this paper show the model capability to predict the OFMSW amount which can be treated in the digester of an existing MWWTP and to assess the OFMSW particle size diminution pre-treatment required to increase the rate of the disintegration process, which otherwise can highly limit the co-digestion system.
Assuntos
Modelos Teóricos , Eliminação de Resíduos/métodos , Esgotos/química , Anaerobiose , Bactérias Anaeróbias/crescimento & desenvolvimento , Bactérias Anaeróbias/metabolismo , Biodegradação Ambiental , Concentração de Íons de Hidrogênio , Cinética , Esgotos/microbiologiaRESUMO
The in vitro biological response to fluoro-edenite (FE) fibres, an asbestos-like amphibole, was evaluated in lung alveolar epithelial A549, mesothelial MeT-5A and monocyte-macrophage J774 cell lines. The mineral has been found in the vicinity of the town of Biancavilla (Catania, Sicily), where an abnormal incidence of mesothelioma has been documented. Cell motility, distribution of polymerized actin, and synthesis of vascular endothelial growth factor (VEGF) and of beta-catenin, critical parameters for tumour development, progression and survival, were investigated in A549 and MeT-5A cells exposed to 50 microg/ml FE fibres for 24 hr and 48 hr. The levels of cyclooxygenase (COX-2) and prostaglandin (PGE2), two molecules involved in cancer pathogenesis by affecting mitogenesis, cell adhesion, immune surveillance and apoptosis, were measured in J774 cells treated with FE fibres under the same experimental conditions. Finally, FE fibres were studied by SEM and EDS analysis to investigate their chemical composition. Exposure of A549 and MeT-5A cells to FE fibres affected differentially phalloidin-stained cytoplasmic F-actin networks, cell motility and VEGF and beta-catenin expression according to the different sensitivity of the two cell lines. In J774 cells it induced a significant increase in COX-2 expression, as assessed by Western blot analysis, and in the concentration of PGE2, measured in culture media by ELISA. SEM-EDS investigations demonstrated two types of FE fibres, edenite and fluoro-edenite, differing in chemical composition and both recognizable as calcic amphiboles. Fibre width ranged from less than 1 microm (prevalently 0.5 microm) to 2-3 microm (edenite) up to several microm (fluoro-edenite); length ranged from about 6 to 80 microm (edenite) up to some hundred microm (fluoro-edenite). Results provide convincing evidence that FE fibres are capable of inducing in vitro functional modifications in a number of parameters with crucial roles in cancer development and progression. Inhaled FE fibres have the potential to induce mesothelioma, even though their ability to penetrate lung alveoli depends on their aerodynamic diameter.
Assuntos
Amiantos Anfibólicos/toxicidade , Pulmão/efeitos dos fármacos , Actinas/metabolismo , Animais , Amiantos Anfibólicos/metabolismo , Linhagem Celular , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/análise , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/análise , Células Epiteliais/efeitos dos fármacos , Células Epiteliais/metabolismo , Formazans/metabolismo , Humanos , Imuno-Histoquímica , Técnicas In Vitro , Pulmão/citologia , Pulmão/metabolismo , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Mesotelioma/metabolismo , Camundongos , Fibras Minerais , Sais de Tetrazólio/metabolismo , Fator A de Crescimento do Endotélio Vascular/biossíntese , beta Catenina/biossínteseRESUMO
Conventional medications in articular disease are often effective for symptom relief, but they can also cause significant side effects and do not slow the progression of the disease. Several natural substances have been shown to be effective as non-steroidal anti-inflammatory drugs at relieving the symptoms of osteoarthritis (OA), and preliminary evidence suggests that some of these compounds may exert a favourable influence on the course of the disease. In this study, we assay the anti-inflammatory/chondroprotective effect of some lyophilised extracts obtained from Opuntia ficus indica (L.) cladodes and of hyaluronic acid (HA) on the production of key molecules released during chronic inflammatory events such as nitric oxide (NO), glycosaminoglycans (GAGs), prostaglandins (PGE(2)) and reactive oxygen species (ROS) in human chondrocyte culture, stimulated with proinflammatory cytokine interleukin-1 beta (IL-1 beta). Further the antioxidant effect of these extracts was evaluated in vitro employing the bleaching of the stable 1,1-diphenyl-2-picrylhydrazyl radical (DPPH test). All the extracts tested in this study showed an interesting profile in active compounds. Particularly some of these extracts were characterized by polyphenolic and polysaccharidic species. In vitro results pointed out that the extracts of Opuntia ficus indica cladodes were able to contrast the harmful effects of IL-1 beta. Our data showed the protective effect of the extracts of Opuntia ficus indica cladodes in cartilage alteration, which appears greater than that elicited by hyaluronic acid (HA) commonly employed as visco-supplementation in the treatment of joint diseases.
Assuntos
Anti-Inflamatórios/farmacologia , Condrócitos/efeitos dos fármacos , Ácido Hialurônico/farmacologia , Opuntia/química , Polissacarídeos/farmacologia , Anti-Inflamatórios/química , Antioxidantes/metabolismo , Cartilagem Articular/citologia , Técnicas de Cultura de Células , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Condrócitos/citologia , Condrócitos/metabolismo , Meios de Cultivo Condicionados/química , Dinoprostona/análise , Avaliação Pré-Clínica de Medicamentos , Fraturas do Colo Femoral/patologia , Fraturas do Colo Femoral/cirurgia , Glicosaminoglicanos/análise , Humanos , Nitritos/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Caules de Planta/química , Polissacarídeos/química , Espécies Reativas de Oxigênio/análise , Espécies Reativas de Oxigênio/metabolismo , Espectrofotometria/métodosRESUMO
This study investigates the importance of the organic matter characteristics of several organic amendments (i.e., buffalo manure, food and kitchen waste, fruit and vegetables waste, and activated sewage sludge) and their influence in the bioremediation of a polycyclic aromatic hydrocarbons (PAH)-contaminated soil. The removal of low molecular weights (LMW) and high molecular weights (HMW) PAHs was monitored in four bioremediation reactors and used as an indicator of the role of organic amendments in contaminant removal. The total initial concentration of LMW PAHs was 234 mg kg(-1) soil (dry weight), while the amount for HMW PAHs was 422 mg kg(-1) soil (dry weight). Monitoring of operational parameters and chemical analysis was performed during 20 weeks. The concentrations of LMW PAH residues in soil were significantly lower in reactors that displayed a mesophilic phase, i.e., 11 and 15 %, compared to reactors that displayed a thermophilic phase, i.e., 29 and 31 %. Residual HMW PAHs were up to five times higher compared to residual LMW PAHs, depending on the reactor. This demonstrated that the amount of added organic matter and macronutrients such as nitrogen and phosphorus, the biochemical organic compound classes (mostly soluble fraction and proteins), and the operational temperature are important factors affecting the overall efficiency of bioremediation. On that basis, this study shows that characterization of biochemical families could contribute to a better understanding of the effects of organic amendments and clarify their different efficiency during a bioremediation process of PAH-contaminated soil.
Assuntos
Bactérias/metabolismo , Hidrocarbonetos Policíclicos Aromáticos/metabolismo , Poluentes do Solo/metabolismo , Biodegradação Ambiental , Esterco/análise , Nitrogênio/metabolismo , Esgotos/análise , Microbiologia do Solo , TemperaturaRESUMO
The aim of the present study was to evaluate the in vitro chondroprotective effects of the lyophilised methanolic extract from flowering buds of Capparis Spinosa L (LECS). This plant, common to the Mediterranean basin, has been used by the traditional medicine for its diuretic and antihypertensive effects and also in certain pathological conditions related to uncontrolled lipid peroxidation. The extract contains many constituents, in particular some flavonoids (kaempferol and quercetin derivatives) and hydrocinammic acids with several known biological effects such as the anti-inflammatory and the antioxidant ones. In this study, we assayed the effect of LECS on human chondrocytes cultures stimulated by proinflammatory cytokine interleukin-1beta (IL-1beta) and we determined the production of key molecules released during chronic inflammatory events (nitric oxide, glycosaminoglycans, prostaglandins and reactive oxygen species). We observed that LECS was able to counteract the harmful effects induced by IL-1beta. This protection appeared to be greater than that elicited by indomethacin, which is usually employed in joint diseases. Since LECS possess a chondroprotective effect, it might be used in the management of cartilage damage during the inflammatory processes.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Capparis/química , Condrócitos/efeitos dos fármacos , Interleucina-1/toxicidade , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Condrócitos/metabolismo , Dinoprostona/metabolismo , Flores/química , Glicosaminoglicanos/metabolismo , Humanos , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismoRESUMO
An important group of non steroidal antinflammatory drugs (NSAIDs), which have been used for the symptomatic treatment of various forms of arthritis, are the 2-arylpropionic acid derivatives, 'profens'. By virtue of a chiral carbon atom on the propionic acid side chain, they exist as enantiomeric pairs. Whereas the S (+) enantiomer could be represented as an effective, but unselective COX inhibitor, the R (-) enantiomer could be much less active in this respect. However, recent findings suggest that certain pharmacological effects of profens cannot be attributed exclusively to the S (+) enantiomer. To obtain further insights into the pharmacological effects of profens, this study investigated the influence of pure enantiomers (S), (R), and racemic flurbiprofen and ketoprofen on the production of NO, MMP-3, PGE(2), ROS and GAGs, key molecules involved in cartilage destruction. Our results show that (S) flurbiprofen and ketoprofen decrease, at 1- and 10-microM concentrations, the interleukin-1beta induced cartilage destruction.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Cartilagem Articular/fisiologia , Condrócitos/fisiologia , Flurbiprofeno/farmacologia , Cetoprofeno/farmacologia , Anti-Inflamatórios não Esteroides/química , Cartilagem Articular/citologia , Cartilagem Articular/efeitos dos fármacos , Cartilagem Articular/metabolismo , Sobrevivência Celular , Células Cultivadas , Condrócitos/efeitos dos fármacos , Condrócitos/metabolismo , Dinoprostona/metabolismo , Cabeça do Fêmur , Flurbiprofeno/química , Glicosaminoglicanos/metabolismo , Humanos , Interleucina-1beta/farmacologia , Cetoprofeno/química , Metaloproteinase 3 da Matriz/metabolismo , Nitritos/metabolismo , Espécies Reativas de Oxigênio , EstereoisomerismoRESUMO
AIM: It is well-know that hyperthyroidism is one of the key causes of secondary osteoporosis. High values of thyroid hormones increase the bone mineral turnover speed by promoting osteoclastic and osteoblastic activities. The aim of our study is to evaluate the increase of bone mineral density (BMD) in osteoporotic and hyperthyroid patients treated with only antithyroid drugs versus patients treated with antithyroid drugs and diphosphonates. METHODS: Twenty-six elderly male patients, 65-75 years, were selected. In all these patients, thyroid function (FT3, FT4, TSH, Tg, AbTg, AbTPO) was evaluated at baseline and after 6 and 12 months from the start of medical treatment; the following were evaluated: BMD, calcium serum, phosphorus serum, alkaline phosphatase, PTH and 24 hours urinary calcium, phosphorus and hydroxyprolin. Thirteen patients (group 1) were treated with antithyroid drugs (methimazole 5-20 mg/die/os) and diphosphonates (alendronate 10 mg/die/os). The control group of 13 patients (group 2) was treated with antithyroid drugs only. RESULTS: After 6 months of treatment, the patients of group 1 showed a mean increase of 2.5% in lumbar spine BMD compared with a mean increase of 0.3% in group 2 (p<0.01). After 12 months, group 1 showed a mean increase of 6.2% in lumbar spine BMD, compared with a mean increase of 2% in group (p<0.001). CONCLUSIONS: The combination of antithyroid and diphosphonates drugs appears to be more efficacious than antithyroid therapy alone for the treatment of osteoporosis in male hyperthyroid patients.
Assuntos
Alendronato/uso terapêutico , Antitireóideos/uso terapêutico , Densidade Óssea/efeitos dos fármacos , Hipertireoidismo/complicações , Metimazol/uso terapêutico , Osteoporose/etiologia , Idoso , Fosfatase Alcalina/sangue , Cálcio/sangue , Estudos de Casos e Controles , Quimioterapia Combinada , Humanos , Hipertireoidismo/sangue , Hipertireoidismo/tratamento farmacológico , Masculino , Osteoporose/sangue , Osteoporose/tratamento farmacológico , Hormônio Paratireóideo/sangue , Fósforo/sangue , Resultado do TratamentoRESUMO
The behavioral responses of the rat to an extract of Cannabis sativa were examined after IP injection of 5, 15 and 30 mg/kg (expressed as delta 9 tetrahydrocannabinol). The lowest dose of the extract induced stereotyped behavior (rhythmic head movements, intermittent gnawing and sniffing) together with hypersensitivity to stimuli and hyperthermia. The administration of higher doses of the extract resulted, initially, in similar behavioral effects but of greater intensity, followed by a cataleptic state alternating with atonic muscular prostration; rectal temperature was decreased. Pre-treatment with 6-hydoxydopamine (6-OHDA, which produces degeneration of catecholamine-containing nerve terminals)or pimozide (blocker of dopamine receptors) significantly reduced both stereotype and hyperreactivity. Thermic effects were also antagonized by 6-OHDA pre-treatment. Cannabis-induced catalepsy was enhanced by pimozide but reduced by atropine (3 mg/kg SC). These results support the hypothesis that catecholamines play an important role in the complex behavioral effects of cannabis.
Assuntos
Comportamento Animal/efeitos dos fármacos , Canabinoides/farmacologia , Cannabis , Animais , Regulação da Temperatura Corporal/efeitos dos fármacos , Catalepsia/induzido quimicamente , Humanos , Hidroxidopaminas/farmacologia , Masculino , Oxidopamina , Ratos , Ratos Endogâmicos , Receptores Dopaminérgicos/efeitos dos fármacos , Comportamento Estereotipado/efeitos dos fármacosRESUMO
A thermophilic aerobic microorganism, able to produce two exocellular polysaccharides (EPS1 and EPS2), was isolated from a shallow hydrothermal vent at Vulcano island (Eolian Islands, Italy). EPS1 and EPS2 were based on mannose and glucose although in a different ratio. EPS2 possessed a trisaccharide repeating unit with a manno-pyranoside configuration. New isolate phenotype was studied by physiological and morphological observations, including biochemical and antimicrobial susceptibility tests (134). Previous analyses carried out on 87 field isolates and 8 thermophilic reference bacilli displayed low phenotypic similarity level (S(SM) = 65%) with Bacillus thermodenitrificans DSM 465. Optimal growth occurs at 65 degrees C and pH 7.0. Oxidase and catalase are negative. The guanine-plus-cytosine (G+C) content of DNA is 52.7%. Genotypic investigations demonstrated the diversity of the isolate with fifteen selected thermophilic Bacillus spp. when we compared the restriction patterns of the amplified 16S rDNA. The membrane lipids are based on fatty acids mainly belonging to the iso-family.
Assuntos
Bacillus/metabolismo , Polissacarídeos Bacterianos/metabolismo , Bacillus/classificação , Bacillus/isolamento & purificação , Técnicas de Tipagem Bacteriana , Composição de Bases , DNA Bacteriano , Geografia , Fenômenos Geológicos , Geologia , Temperatura Alta , Itália , Polimorfismo de Fragmento de Restrição , Polissacarídeos Bacterianos/química , Microbiologia da ÁguaRESUMO
The in vitro effects on human articular chondrocytes were evaluated for a series of N-benzo[d]isothiazol-3-yl-amidines, bearing as pharmacophoric moiety the nonacidic isosteric nitrogen analogue of the carboxylic group. The aim was to verify their effectiveness in articular diseases, such as arthritis. Human chondrocytes were treated with IL-1beta in the presence of a series of N-benzo[d]isothiazol-3-yl-amidines at a concentration of 100 microg/mL. After 120 h, the amount of glycosaminoglycans (GAGs), the production of nitric oxide (NO) and the inhibition of metalloproteinases (MMP-3) and prostaglandin (PGE2) were measured. Nitrite production induced by inflammatory IL-1beta on cultured chondrocytes was inhibited by the N-benzo[d]isothiazol-3-yl-amidines tested, in particular by N-benzo[d]isothiazol-3-yl-benzamidine, which was the most active. Concerning the effects on GAGs, all the tested benzisothiazolylamidines, and in particular N-benzo[d]isothiazol-3-yl-acetamidine, prevented the depletion of proteoglycan induced by IL-1beta. Inhibitory effects of the tested compounds on MMP-3 activity and on PGE2 production were also observed.
Assuntos
Amidinas/farmacologia , Cartilagem Articular/efeitos dos fármacos , Cartilagem Articular/imunologia , Condrócitos/efeitos dos fármacos , Interleucina-1/farmacologia , Tiazóis/farmacologia , Amidinas/química , Cartilagem Articular/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/imunologia , Células Cultivadas , Condrócitos/metabolismo , Humanos , Fármacos Neuroprotetores/farmacologiaRESUMO
The potential of liposomes as an in-vivo ophthalmic drug delivery system for acyclovir was investigated. The drug-membrane interaction was evaluated by means of differential scanning calorimetry analysis. These experiments showed that acyclovir is able to interact with both positively and negatively charged membranes via electrostatic or hydrogen bonds. No interaction was observed with neutral membranes made up of dipalmitoylphosphatidylcholine. Different liposome preparation procedures were carried out to encapsulate acyclovir. The drug encapsulation mainly depends on the amount of water which the liposome system is able to entrap. In the case of multilamellar vesicles, charged systems showed the highest encapsulation efficiency. No particular difference in the encapsulation efficiency was observed for oligolamellar vesicles prepared with the reverse-phase evaporation technique. Oligolamellar liposomes showed the highest acyclovir encapsulation parameters and had release profiles similar to those of multilamellar liposomes. In-vivo experiments using male New Zealand albino rabbits were carried out to evaluate the aqueous humour concentration of acyclovir bioavailability. The most suitable ophthalmic drug delivery system was oligolamellar systems made up of dipalmitoylphosphatidylcholine-cholesterol-dimethyldioctadecyl glycerole bromide (7:4:1 molar ratio), which presented the highest encapsulation capacity and were able to deliver greater amounts of the drug into the aqueous humour than a saline acyclovir solution or a physical liposome/drug blend.
Assuntos
Aciclovir/farmacocinética , Córnea/metabolismo , Absorção , Animais , Antivirais/farmacocinética , Membrana Celular/metabolismo , Permeabilidade da Membrana Celular , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Lipossomos , Masculino , Fenômenos Fisiológicos Oculares , CoelhosRESUMO
4-Biphenylacetic acid, a potent non-steroidal anti-inflammatory agent forms a solid inclusion complex with beta-cyclodextrin in a 1:1 molar ratio, which exhibits better solubility and dissolution characteristics than the uncomplexed drug. Following oral administration of the complex to rats, quicker and higher drug plasma concentrations can be achieved than with the drug alone. Parallel studies, using the carrageenan paw oedema test, demonstrate a greater anti-inflammatory activity of the complex (ED50 of 2.9 mg kg-1 for the complex and of 6.2 mg kg-1 for the free drug). The complex displayed a better gastric tolerability in the rat than drug alone.
Assuntos
Ciclodextrinas/farmacologia , Fenilacetatos/farmacocinética , beta-Ciclodextrinas , Administração Oral , Animais , Disponibilidade Biológica , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Masculino , Fenilacetatos/administração & dosagem , Ratos , Ratos Endogâmicos , Úlcera Gástrica/induzido quimicamenteRESUMO
A series of anti-inflammatory agents known as Schiff bases, combining thiazolyl and benzothiazolyl ring and vanillin moieties in the same molecule, was synthesized and evaluated for screening anti-degenerative activity on nasal pig cartilage cultures treated with interleukin 1beta, (IL-1beta). The amount of glycosaminoglycans (GAGs), the production of nitric oxide (NO) and prostaglandin E2 (PGE2), released into the culture medium, were detected. The tested Schiff bases decreased, dose-dependently, the NO and PGE2 production and the GAGs release with respect to samples treated with IL-1beta alone, showing a different behavior correlated to their structure. These results suggest that thiazolyl and benzothiazolyl Schiff bases in general, and particularly the Schiff base with bromine and methoxyl group in position three would protect cartilage matrix from degenerative factors induced by IL-1beta.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Cartilagem/efeitos dos fármacos , Bases de Schiff/farmacologia , Tiazóis/farmacologia , Animais , Cartilagem/metabolismo , Dinoprostona/biossíntese , Glicosaminoglicanos/biossíntese , Técnicas In Vitro , Interleucina-1/toxicidade , Septo Nasal/efeitos dos fármacos , Septo Nasal/metabolismo , Óxido Nítrico/biossíntese , SuínosRESUMO
We prepared some series of 2-(alkylaminoacyl) derivatives of 2-amino-1,3,4-thiadiazoles. Most terms were subjected to a biological screening showing a local anesthetic activity both in infiltration and trunkular tests. For some of the assayed derivatives, the activity was comparable to that of lidocaine, taken as the reference molecule. From the obtained results an acceptable relationship between some structural features and activity was drawn.
Assuntos
Anestésicos Locais/síntese química , Anestésicos Locais/farmacologia , Tiadiazóis/síntese química , Tiadiazóis/farmacologia , Anestésicos Locais/química , Animais , Feminino , Masculino , Ratos , Ratos Wistar , Tiadiazóis/químicaRESUMO
Some carboxymethyl- and carboxy-derivatives of 7H- and 5H-1,2,4-triazolo [3,4-b][1,3,4] thiadiazine were prepared. Their structure are discussed on the basis of IR, NMR and mass spectra. The synthesized compounds were subjected to a preliminary pharmacological screening for antiinflammatory-analgesic activity and to microbiological test on various species of mycetes and bacteria.
Assuntos
Analgésicos/síntese química , Antibacterianos/síntese química , Anti-Inflamatórios não Esteroides/síntese química , Tiadiazinas/síntese química , Tiazinas/síntese química , Triazóis/síntese química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Bactérias/efeitos dos fármacos , Comportamento Animal/efeitos dos fármacos , Ácidos Carboxílicos/síntese química , Ácidos Carboxílicos/farmacologia , Fenômenos Químicos , Química , Camundongos , Testes de Sensibilidade Microbiana , Ratos , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/fisiopatologia , Tiadiazinas/farmacologia , Triazóis/farmacologiaRESUMO
3-Carboxyalkylthio derivatives of 5-alkoxyphenyl-1,2,4-triazole were prepared, performing some substitutions both on carboxyalkyl chain, by lengthening it or introducing substituents with increasing molecular weight in alpha- at the carboxy group, and on N-4 atom in the triazole ring, by introducing an amino or methyl group, so that to vary steric conformation along with the lipophilicity of molecules. The corresponding bicyclic thiazolo-triazolone and triazolo-thiazinone derivatives, which represent the rigid models of carboxymethylthio- and carboxyethylthio- open structures, were also obtained. All the compounds show "in vivo" antiinflammatory activity, while only carboxyalkylthio derivatives of 4-amino- and 4-methyltriazole display an appreciable analgesic one. From the relief of some data on substituent present in the synthesized compounds, a structure-activity relationship is also suggested.