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1.
Environ Res ; 246: 118118, 2024 Apr 01.
Article in English | MEDLINE | ID: mdl-38199469

ABSTRACT

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.


Subject(s)
Hydrogen Peroxide , Manure , Animals , Cattle , Fermentation , Whey , Whey Proteins , Carbohydrates , Hydrogen
2.
J Prev Med Hyg ; 60(1): E50-E57, 2019 Mar.
Article in English | MEDLINE | ID: mdl-31041411

ABSTRACT

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.


Subject(s)
Allergens/adverse effects , Cosmetics/chemistry , Odorants , Preservatives, Pharmaceutical/adverse effects , Skin Diseases/chemically induced , Humans
3.
J Environ Manage ; 223: 1078-1085, 2018 Oct 01.
Article in English | MEDLINE | ID: mdl-30096748

ABSTRACT

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 µmol 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 µmol 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.


Subject(s)
Lipids/analysis , Microalgae , Wastewater , Biofuels , Biomass
4.
Environ Sci Pollut Res Int ; 23(15): 15041-52, 2016 Aug.
Article in English | MEDLINE | ID: mdl-27083907

ABSTRACT

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.


Subject(s)
Bacteria/metabolism , Polycyclic Aromatic Hydrocarbons/metabolism , Soil Pollutants/metabolism , Biodegradation, Environmental , Manure/analysis , Nitrogen/metabolism , Sewage/analysis , Soil Microbiology , Temperature
5.
Waste Manag ; 31(12): 2527-35, 2011 Dec.
Article in English | MEDLINE | ID: mdl-21852099

ABSTRACT

A mathematical model has recently been proposed by the authors to simulate the biochemical processes that prevail in a co-digestion reactor fed with sewage sludge and the organic fraction of municipal solid waste. This model is based on the Anaerobic Digestion Model no. 1 of the International Water Association, which has been extended to include the co-digestion processes, using surface-based kinetics to model the organic waste disintegration and conversion to carbohydrates, proteins and lipids. When organic waste solids are present in the reactor influent, the disintegration process is the rate-limiting step of the overall co-digestion process. The main advantage of the proposed modeling approach is that the kinetic constant of such a process does not depend on the waste particle size distribution (PSD) and rather depends only on the nature and composition of the waste particles. The model calibration aimed to assess the kinetic constant of the disintegration process can therefore be conducted using organic waste samples of any PSD, and the resulting value will be suitable for all the organic wastes of the same nature as the investigated samples, independently of their PSD. This assumption was proven in this study by biomethane potential experiments that were conducted on organic waste samples with different particle sizes. The results of these experiments were used to calibrate and validate the mathematical model, resulting in a good agreement between the simulated and observed data for any investigated particle size of the solid waste. This study confirms the strength of the proposed model and calibration procedure, which can thus be used to assess the treatment efficiency and predict the methane production of full-scale digesters.


Subject(s)
Cities , Digestion , Models, Theoretical , Sewage/chemistry , Waste Management/methods , Waste Products/analysis , Hydrogen-Ion Concentration , Kinetics , Methane/biosynthesis , Particle Size , Temperature
6.
Nat Prod Res ; 24(15): 1469-80, 2010 Sep.
Article in English | MEDLINE | ID: mdl-20812134

ABSTRACT

In the present study, a complex of compounds (red orange complex, ROC), obtained from three red orange varieties (Citrus sinensis varieties: Moro, Tarocco and Sanguinello), containing cyanidin glycosides, hydroxycinnamic acids, flavanone glycosides and ascorbic acid, was screened to discover new lead compounds in the suppression of the production of key molecules released during inflammatory events in interleukin-1beta (IL-beta) stimulated human primary chondrocytes. The expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX)-2 and intercellular adhesion molecule-1 (ICAM-1), and the release of nitric oxide, prostaglandin (PG)E(2) and interleukin-8 (IL-8) were determined. Indomethacin was used as an anti-inflammatory drug reference. ROC acts as a potent inhibitor of iNOS and COX-2 gene expression while also suppressing the production of PGE(2) and nitrite in human chondrocytes. In addition, ROC induces a significant decrease in ICAM expression and IL-8 release. These findings suggest that ROC exerts anti-inflammatory effects probably through the suppression of COX-2 and iNOS expression.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Chondrocytes/drug effects , Chondrocytes/metabolism , Citrus sinensis/chemistry , Cyclooxygenase 2/metabolism , Nitric Oxide Synthase Type II/metabolism , Plant Extracts/pharmacology , Anti-Inflammatory Agents/chemistry , Blotting, Western , Cells, Cultured , Humans , Interleukin-8/metabolism , Plant Extracts/chemistry
7.
Water Sci Technol ; 58(7): 1513-9, 2008.
Article in English | MEDLINE | ID: mdl-18957767

ABSTRACT

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.


Subject(s)
Models, Theoretical , Refuse Disposal/methods , Sewage/chemistry , Anaerobiosis , Bacteria, Anaerobic/growth & development , Bacteria, Anaerobic/metabolism , Biodegradation, Environmental , Hydrogen-Ion Concentration , Kinetics , Sewage/microbiology
8.
Water Sci Technol ; 57(7): 1111-5, 2008.
Article in English | MEDLINE | ID: mdl-18441440

ABSTRACT

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.


Subject(s)
Copper/analysis , Environmental Monitoring , Water Purification/methods , Water/chemistry
9.
Cell Mol Biol (Noisy-le-grand) ; 53 Suppl: OL965-80, 2007.
Article in English | MEDLINE | ID: mdl-17695086

ABSTRACT

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.


Subject(s)
Asbestos, Amphibole/toxicity , Lung/drug effects , Actins/metabolism , Animals , Asbestos, Amphibole/metabolism , Cell Line , Cell Line, Tumor , Cell Movement/drug effects , Cell Survival/drug effects , Cyclooxygenase 2/analysis , Cyclooxygenase 2/metabolism , Dinoprostone/analysis , Epithelial Cells/drug effects , Epithelial Cells/metabolism , Formazans/metabolism , Humans , Immunohistochemistry , In Vitro Techniques , Lung/cytology , Lung/metabolism , Macrophages/drug effects , Macrophages/metabolism , Mesothelioma/metabolism , Mice , Mineral Fibers , Tetrazolium Salts/metabolism , Vascular Endothelial Growth Factor A/biosynthesis , beta Catenin/biosynthesis
10.
J Ethnopharmacol ; 111(2): 315-21, 2007 May 04.
Article in English | MEDLINE | ID: mdl-17196777

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Chondrocytes/drug effects , Hyaluronic Acid/pharmacology , Opuntia/chemistry , Polysaccharides/pharmacology , Anti-Inflammatory Agents/chemistry , Antioxidants/metabolism , Cartilage, Articular/cytology , Cell Culture Techniques , Cell Survival/drug effects , Cells, Cultured , Chondrocytes/cytology , Chondrocytes/metabolism , Culture Media, Conditioned/chemistry , Dinoprostone/analysis , Drug Evaluation, Preclinical , Femoral Neck Fractures/pathology , Femoral Neck Fractures/surgery , Glycosaminoglycans/analysis , Humans , Nitrites/analysis , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Stems/chemistry , Polysaccharides/chemistry , Reactive Oxygen Species/analysis , Reactive Oxygen Species/metabolism , Spectrophotometry/methods
11.
Phytomedicine ; 13(7): 522-6, 2006 Jul.
Article in English | MEDLINE | ID: mdl-16785044

ABSTRACT

The present work was aimed at evaluating the in vitro effects of a lyophilized extract of wine (JW-E) obtained from Jacquez grapes (Vitis aestivalis-cinereaxVitis vinifera grapes) on the production of key molecules released in inflammatory disease utilising interleukin-1beta (IL-1beta) activated chondrocytes. The extract contains large amounts of phenolic components, in particular some flavonoids (flavan-3-ols, also known as catechins) and proanthocyanidins, as hydroxycinnamic acids and anthocyanins, that possess several biological features such as antiinflammatory and antioxidant effects and a "radical scavenger" activity too. In this study, we assayed the effect of JW-E on the production of key molecules released during chronic inflammatory events as nitric oxide (NO), prostaglandins E(2) (PGE(2)) and reactive oxygen species (ROS) in human chondrocytes culture, stimulated with proinflammatory cytokine interleukin-1beta. The JW-E proved to possess good ability against the harmfull effects of IL-1beta. Our data showed the protective effects of JW-E in cartilage alteration, that appears greater than that elicited by indomethacin, a not steroidal antiinflammatory drug (NSAID), commonly employed in joint diseases.


Subject(s)
Chondrocytes/drug effects , Plant Extracts/pharmacology , Vitis , Wine , Cartilage, Articular/cytology , Cells, Cultured , Dinoprostone/metabolism , Fruit , Humans , Inflammation/drug therapy , Interleukin-1/pharmacology , Nitric Oxide/metabolism , Osteochondritis/drug therapy , Plant Extracts/therapeutic use , Reactive Oxygen Species/metabolism
12.
Minerva Endocrinol ; 30(2): 89-94, 2005 Jun.
Article in Italian | MEDLINE | ID: mdl-15988404

ABSTRACT

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.


Subject(s)
Alendronate/therapeutic use , Antithyroid Agents/therapeutic use , Bone Density/drug effects , Hyperthyroidism/complications , Methimazole/therapeutic use , Osteoporosis/etiology , Aged , Alkaline Phosphatase/blood , Calcium/blood , Case-Control Studies , Drug Therapy, Combination , Humans , Hyperthyroidism/blood , Hyperthyroidism/drug therapy , Male , Osteoporosis/blood , Osteoporosis/drug therapy , Parathyroid Hormone/blood , Phosphorus/blood , Treatment Outcome
13.
Life Sci ; 77(20): 2479-88, 2005 Sep 30.
Article in English | MEDLINE | ID: mdl-15946691

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Capparis/chemistry , Chondrocytes/drug effects , Interleukin-1/toxicity , Cell Survival/drug effects , Cells, Cultured , Chondrocytes/metabolism , Dinoprostone/metabolism , Flowers/chemistry , Glycosaminoglycans/metabolism , Humans , Nitric Oxide/metabolism , Plant Extracts/pharmacology , Reactive Oxygen Species/metabolism
14.
Inflammation ; 29(4-6): 119-28, 2005 Dec.
Article in English | MEDLINE | ID: mdl-17089192

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Cartilage, Articular/physiology , Chondrocytes/physiology , Flurbiprofen/pharmacology , Ketoprofen/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Cartilage, Articular/cytology , Cartilage, Articular/drug effects , Cartilage, Articular/metabolism , Cell Survival , Cells, Cultured , Chondrocytes/drug effects , Chondrocytes/metabolism , Dinoprostone/metabolism , Femur Head , Flurbiprofen/chemistry , Glycosaminoglycans/metabolism , Humans , Interleukin-1beta/pharmacology , Ketoprofen/chemistry , Matrix Metalloproteinase 3/metabolism , Nitrites/metabolism , Reactive Oxygen Species , Stereoisomerism
15.
Inflammation ; 28(4): 231-5, 2004 Aug.
Article in English | MEDLINE | ID: mdl-15673165

ABSTRACT

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.


Subject(s)
Amidines/pharmacology , Cartilage, Articular/drug effects , Cartilage, Articular/immunology , Chondrocytes/drug effects , Interleukin-1/pharmacology , Thiazoles/pharmacology , Amidines/chemistry , Cartilage, Articular/metabolism , Cell Survival/drug effects , Cell Survival/immunology , Cells, Cultured , Chondrocytes/metabolism , Humans , Neuroprotective Agents/pharmacology
16.
Farmaco ; 58(12): 1339-44, 2003 Dec.
Article in English | MEDLINE | ID: mdl-14630249

ABSTRACT

The 2-arylpropionic acid derivatives or 'profens' are an important group of non-steroidal anti-inflammatory drugs that have been used for the symptomatic treatment of various forms of arthritis. These compounds are chiral and the majority of them are still marketed as racemate although it is known that the (S)- form is the principal effective in the cyclooxygenase inhibition. However, recent findings suggest that certain pharmacological effect of 2-arylpropionic acids cannot be attributed exclusively to the (S)-(+) enantiomer. To obtain further insights into the pharmacological effect of profens, the present study investigated the influence of racemic and pure enantiomers of flurbiprofen on the production of nitric oxide and glycosaminoglycans, key molecules involved in cartilage destruction. The culture of human articular cartilage stimulated by interleukin-1beta (IL-1beta), which plays an important role in the degradation of cartilage, has been established, as a profit experimental model, for reproducing the mechanisms involved in the pathophysiology of arthritic diseases. Our results show that mainly (S)-(+)-flurbiprofen decreases, at therapeutically concentrations, the IL-1beta induced cartilage destruction.


Subject(s)
Cartilage, Articular/drug effects , Flurbiprofen/chemistry , Flurbiprofen/pharmacology , Cartilage, Articular/cytology , Cartilage, Articular/metabolism , Cells, Cultured , Flurbiprofen/analogs & derivatives , Glycosaminoglycans/antagonists & inhibitors , Glycosaminoglycans/metabolism , Humans , Interleukin-1/pharmacology , Stereoisomerism
18.
Farmaco ; 57(12): 1009-13, 2002 Dec.
Article in English | MEDLINE | ID: mdl-12564476

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Cartilage/drug effects , Schiff Bases/pharmacology , Thiazoles/pharmacology , Animals , Cartilage/metabolism , Dinoprostone/biosynthesis , Glycosaminoglycans/biosynthesis , In Vitro Techniques , Interleukin-1/toxicity , Nasal Septum/drug effects , Nasal Septum/metabolism , Nitric Oxide/biosynthesis , Swine
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