Avaliação do potencial efeito cicatrizante gástrico e antiartrítico da mangiferina, uma xantona glicosilada da Mangifera indica

Rheumatoid arthritis (RA) is a chronic illness with great potential to cause comorbidities resulting from cumulative inflammatory activities, and it contributes with the increase of disabilities and death of patients. It affects 1 to 2% of world population and usually occurs between 30 and 50 years of age. Among existing therapeutic options for the disease non-steroidal anti-inflammatory drugs (NSAIDs) still play an important part in the treatment, being widely used by patients to relieve pain and stiffness. However, this class of drugs causes many adverse gastrointestinal effects, such as dyspepsia, heartburn, nausea and vomit, and its use is one of the most common causes of peptic ulcers. Mangiferin (a glicosilated xanthone extracted mainly from the bark of Mangifera indica L.) is the main compound of an aqueous extract made from the bark stem of the mango tree. Previous studies conducted by our research group prove the anti-inflammatory action of mangiferin on an animal model of periodontitis, and its gastroprotective action has been described before. Considering these informations this study evaluated mangiferin’s potential on the treatment of RA and on gastric ulcer healing in animal models, and analyzed toxicity parameters to assure efficacy and safety of the compound as potential new drug for the treatment of the disease. RA was induced in rats by subcutaneous injection of bovine collagen and Freund’s complete adjuvant. This method presented low incidence of RA in rats, but we were able to induce the disease in 60 to 70% of the animals. Due to the wide use of NSAIDs and its potential to cause peptic ulcers, we induced gastric ulcer on arthritic rats to analyze mangiferin’s gastric healing effect. After 14 days of treatment we noticed small increase of the lesion area of animals treated with mangiferin or ibuprofen, when compared to the animals... (Complete abstract click electronic access below)

Síntese e caracterização do complexo de lantânio (III) e indometacina no estado sólido

In this study, the drug indomethacin, a non-steroidal anti-inflammatory indoleacetic acid derivative and the complex of indomethacin and lanthanum (III) in solid form were synthesized and characterized by Thermogravimetry (TGA), Differential Thermal Analysis (DTA), Differential Scanning Calorimetry (DSC) and powder X-ray diffractometry (XRD), infrared vibrational spectroscopy by diffuse reflectance (FTIR) and complexometric titration with EDTA. With the TG curves it was possible to determine the stoichiometry of the complex as La(Ind)3·3.5H2O where Ind is the drug indomethacin. The result of thermal analyzes provided information on the thermal stability, enthalpy of dehydration and thermal behavior of the compounds. The infrared spectrum and with the aid of theoretical calculations suggests that the indomethacin is coordinated by the carboxylate group in the bidentate mode

Avaliação gastroprotetora da epicatequina e verificação de seus mecanismos de ação

The stomach is an exceptional organ, which functions are sterilize food ingested, form the primitive bolus, digest lipids and proteins, and to store food temporarily in the gastrointestinal tract. Its capacity of digesting food without digesting itself is amazing. This fact occurs due to innumerous protective substances adjacent to the gastric mucosa. When aggressive factors overwhelm the protective factors, a lesion in the gastric mucosa is formed. Lesions that reach the lamina propria are called gastric ulcers, which are classified macroscopically as openings on the gastric wall and; microscopically, as a gastric injury characterized with epithelial desquamation, mucosal hemorrhage, glandular damage and eosinophilic infiltration. The current therapy available is effective, although it causes collateral effects, therefore researching new drugs is necessary. This work aim to evaluate the gastroprotective effect of epicatechin against gastric lesions induced by absolute ethanol and non steroidal anti-inflammatory drugs which are the main causes of this disease currently, yet we aim to study the main mechanisms of action responsible for the gastroprotective effect. The results show that epicatechin has a significant macroscopic and microscopic gastroprotective effect against gastric injuries induced by ethanol and indomethacin, acting locally by augmenting gastric mucus secretion and it also acts via antioxidant system by holding total glutathione levels. Epicatechin’s gastroprotective mechanisms depend on the activation of sulfhydryl compounds and doesn’t depend on the NO-synthase enzyme

The H2S-releasing naproxen derivative, ATB-346, inhibits alveolar bone loss and inflammation in rats with ligature-induced periodontitis

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Efeitos de drogas antiplaquetárias na doença periodontal

The association between platelets, angiogenesis and progression or repair of periodontal disease has been little explored and, consequently, the results are inconclusive. The pathogenic bacteria present in the periodontal pocket release endotoxins that affect the endothelial integrity and are able to induce the production of chemical mediators derived from plasma proteins and blood clotting while altering platelet function. There is great interest in the modulation of platelet activity in vascular disorders, especially cardiovascular diseases. For this reason, antiplatelet drugs, that are commonly used in the prevention of thromboembolic diseases, such as myocardial infarction, ischemic stroke and peripheral arterial disease, have been used. Aspirin is the only non-steroidal antiinflammatory agent with antiplatelet activity. In the periodontium, instead of only reduces levels of inflammatory cytokines, also significantly affects bleeding on probing, suggesting a dose-dependent modulation of periodontitis. In contrast, clopidogrel and ticlopidine are thienopyridine drugs with no known antiinflammatory action, suggesting that this benefit is related to an antiinflammatory effect indirectly correlated to their antiplatelet activity already established. In the literature there is limited information about the effect of these drugs on periodontium and periodontal disease development. Antiplatelet drugs hypothetically can change both the pathogenesis of periodontitis and subsequent periodontal tissue repair by blocking the secretion of chemical mediators which in general are important in modulating inflammation and tissue repair.

Obtenção e caracterização de nanopartículas lipídicas sólidas como sistema de transporte para ibuprofeno

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Evaluation of sodium diclofenac release using natural rubber latex as carrier

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Does clinical treatment with phenylbutazone and meloxicam in the pre-ovulatory period influence the ovulation rate in mares?

The presence of anovulatory haemorrhagic follicles during the oestrous cycle of mares causes financial impacts, slowing conception and increasing the number of services per pregnancy. Non-steroidal anti-inflammatory drugs (NSAIDs) such as meloxicam and phenylbutazone are used in the treatment of several disorders in mares, and these drugs can impair the formation of prostaglandins (PGs) and consequently interfere with reproductive activity. This study aimed to evaluate the effects of treatment with NSAIDs on the development of pre-ovulatory follicles in mares. In total, 11 mares were studied over three consecutive oestrous cycles, and gynaecological and ultrasound examinations were performed every 12 h. When 32-mm-diameter follicles were detected, 1 mg of deslorelin was administered to induce ovulation. The first cycle was used as a control, and the mares received only a dose of deslorelin. In the subsequent cycles, in addition to receiving the same dose of deslorelin, each mare was treated with NSAIDs. In the second cycle, 4.4 mg/kg of phenylbutazone was administered, and in the third cycle, 0.6 mg/kg of meloxicam was administered once a day until ovulation or the beginning of follicular haemorrhage. All of the mares ovulated between 36 and 48 h after the induction in the control cycle. In the meloxicam cycle, 10 mares (92%) did not ovulate, while in the phenylbutazone cycle, nine mares (83%) did not ovulate. In both treatments, intrafollicular hyperechoic spots indicative of haemorrhagic follicles were observed on ultrasound. Thus, our results suggested that treatment with meloxicam and phenylbutazone at therapeutic doses induced intrafollicular haemorrhage and luteinization of anovulatory follicles.

Anaphylactoid reaction caused by sodium ceftriaxone in two horses experimentally infected by Borrelia burgdorferi

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Síntese e caracterização de complexos de lantanídeos pesados e ítrio(III) como o fármaco ibuprofeno no estado sólido

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Pharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-Acyl hydrazone subunit

A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs.

Muscle lesion treatment in Brazilian soccer players: theory vs. practice

Background: In this study we evaluated the rehabilitation profile of Brazilian soccer players which underwent lower limb muscle lesions. Methods: This is a descriptive investigation. We evaluated 139 professional soccer players (1724 years old). We evaluated the following variables: muscle lesion diagnosis, symptoms, non steroidal anti-inflammatory used, physiotherapy treatment, which physiotherapy recourses was used if treated and train adaptation. Results: In great part of the athletes muscle lesion remained between 2 weeks and 1 month. Around 54% were diagnosed by a physician; the other part was diagnosed by a physical therapist. Non steroidal anti-inflammatory were prescribed by physicians in 42% of the cases; in 7% the physical therapist prescribed the medication while in 49% of the cases the masseur prescribed the drug. More than 1/4 of the athletes received physiotherapy treatement between 48 hours and 5 days. Isometric exercise therapy was applied in 15% of the cases. 63% were not accompanied by the physiotherapist on their return to the field. 48% received massages immediately after injury. Conclusion: We presented discrepancy between the recommended theory described by several researches and the practice. We indicate the necessity of recycling in a general context the rehabilitation of muscle injuries.

DETERMINATION OF DICLOFENAC SODIUM IN RABBIT PLASMA BY HPLC/UV: EVALUATION AND CHARACTERIZATION OF ITS CRYSTALLINE FORMS, ANHYDROUS AND HYDRATE, ON THE ANTIPYRETIC EFFECT

Diclofenac sodium (DS) is a non-steroidal anti-inflammatory drug that is widely prescribed for the treatment of rheumatoid arthritis and post-surgery analgesia. The active pharmaceutical ingredient is the anhydrous form; however, it can also exist in hydrate form. In this context, knowing the properties of the solid state is important and relevant in the pharmaceutical area because they have a significant impact on the solubility, bioavailability, and chemical stability of the drugs. In the present study, data from XRPD, FTIR spectroscopy, and thermal analysis were used for the identification and characterization of DS forms (anhydrous and hydrate). An HPLC method was optimized to evaluate the plasma concentration of DS in rabbits. The optimized method exhibited good linearity over the range 0.1-60 mu g/mL with correlation coefficients of >0.9991. The mean recovery was 100%. Precision and accuracy were determined within acceptable limits. Finally, to compare the pharmacological properties of anhydrous and hydrate DS forms, we investigated their effects in the febrile response induced by lipopolysaccharide from E. coli in rabbits. The results show that the antipyretic effect of anhydrous and hydrate DS forms are similar.

Synthesis and characterization of a diruthenium(II,III)-ketoprofen compound and study of the in vitro effects on CRC cells in comparison to the naproxen and ibuprofen derivatives

A new diruthenium(II,III) complex, of formula [Ru2Cl(ket)(4)], Ruket, containing the non-steroidal anti-inflammatory drug ketoprofen was synthesized and mainly characterized by electrospray ionization mass spectrometry (ESI-MS), UV-Vis-IR electronic spectroscopy and FTIR and Raman vibrational spectroscopies. The four drug-carboxylato bridging ligands stabilize a Ru-2(II,III) mixed valent core in a paddlewheel type structure as confirmed by ESI mass spectra, electronic and vibrational spectroscopies and magnetic measurements. Ruket and the analogous compounds containing ibuprofen, Ruibp, and naproxen, Runpx, were tested for the biological effects in the human colon carcinoma cells HT-29 and Caco-2 expressing high and low levels of COX-2 respectively. All compounds only weakly affected the proliferation of the colorectal cancer cells HT-29 and Caco-2, and similarly only partially inhibited the production/activity of MMP-2 and MMP-9 by HT-29 cells, suggesting that COX-2 inhibition by these drugs can only partially be involved in the pharmacological effects of these derivatives. (c) 2012 Elsevier Ltd. All rights reserved.

Infection and immune-mediated meningococcal-associated arthritis: combination features in the same patient

We present a case of a 16-year-old male patient with sudden-onset, rash, arthritis and meningitis by Neisseria meningitidis one week after an acute upper respiratory infection. On the 10th day of treatment followed by neurological and arthritis clinical improvement, he presented once again a tender and swollen left knee with a moderate effusion, and active and passive range of motion was severely limited secondary to pain, and when he was submitted to surgical drainage and synovial fluid analysis he showed inflammatory characteristics. A non-steroidal anti-inflammatory drug was taken for five days with complete improvement of symptoms. The case is notable for its combination of features of septic and immune-mediated arthritis, which has rarely been reported in the same patient.