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Antiinflammatory Agents (antiinflammatory + agent)
Selected AbstractsPseudoporphyria and Nonsteroidal Antiinflammatory Agents in Children with Juvenile Idiopathic ArthritisPEDIATRIC DERMATOLOGY, Issue 6 2000Bernadette De Silva M.R.C.P. Nonsteroidal antiinflammatory drugs (NSAIDs) are implicated in the etiology of this condition. In a 1-year prospective study of children attending the pediatric rheumatology clinic in Edinburgh we found a prevalence of pseudoporphyria of 10.9% in children taking NSAIDs for juvenile idiopathic arthritis. Naproxen was the most commonly implicated NSAID, independent of dosage. Blue/gray eye color was an independent risk factor for the development of pseudoporphyria. We would advise caution in prescribing naproxen in these children to prevent disfiguring facial scarring. [source] ChemInform Abstract: A Facile Regioselective Synthesis of Novel spiro-Thioxanthene and spiro-Xanthene-9,,2-[1,3,4]thiadiazole Derivatives as Potential Analgesic and Antiinflammatory Agents.CHEMINFORM, Issue 1 2009H. N. Hafez Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis and Biological Evaluation of Amide Derivatives of (6-Chloro-2,3-dihydro-1H-inden-1-yl)acetic Acid as Potential Antiinflammatory Agents with Lower Gastrointestinal Toxicity.CHEMINFORM, Issue 43 2008Meenakshi Sharma Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis and Pharmacological Evaluation of Some 3-(4-Methylphenyl)-2-substituted Amino-3H-quinazolin-4-ones as Analgesic and Antiinflammatory Agents.CHEMINFORM, Issue 18 2007Veerachamy Alagarsamy Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Potent hFPRL1 (ALXR) Agonists as Potential Antiinflammatory Agents.CHEMINFORM, Issue 42 2006Roland Buerli Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Studies on Novel 7-Acyl-5-chloro-2-oxo-3H-benzoxazole Derivatives as Potential Analgesic and Antiinflammatory Agents.CHEMINFORM, Issue 49 2003Serdar Uenlue Abstract For Abstract see ChemInform Abstract in Full Text. [source] Isoxazolinyl Derivatives of Anthranilic Acid as Antiinflammatory Agents.CHEMINFORM, Issue 44 2003Preeti Rani Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Novel 4,5-Diaryl-3-hydroxy-2(5H)-furanones as Antioxidants and Antiinflammatory Agents.CHEMINFORM, Issue 34 2002Pascal Coudert Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Inhibition of Neutrophil O2 - Production by Unsymmetrical Methylene Derivatives of Benzopyrans: Their Use as Potential Antiinflammatory Agents.CHEMINFORM, Issue 20 2002Mauro Mazzei Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis of Substituted Benzamides as Antiinflammatory Agents that Inhibit Preferentially Cyclooxygenase 1 but Do Not Cause Gastric Damage.CHEMINFORM, Issue 1 2002Giuseppe Caliendo Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Induction of an antiinflammatory effect and prevention of cartilage damage in rat knee osteoarthritis by CF101 treatmentARTHRITIS & RHEUMATISM, Issue 10 2009S. Bar-Yehuda Objective Studies have suggested that rheumatoid arthritis (RA) and osteoarthritis (OA) share common characteristics. The highly selective A3 adenosine receptor agonist CF101 was recently defined as a potent antiinflammatory agent for the treatment of RA. The purpose of this study was to examine the effects of CF101 on the clinical and pathologic manifestations of OA in an experimental animal model. Methods OA was induced in rats by monosodium iodoacetate, and upon disease onset, oral treatment with CF101 (100 ,g/kg given twice daily) was initiated. The A3 adenosine receptor antagonist MRS1220 (100 ,g/kg given twice daily) was administered orally, 30 minutes before CF101 treatment. The OA clinical score was monitored by knee diameter measurements and by radiographic analyses. Histologic analyses were performed following staining with hematoxylin and eosin, Safranin O,fast green, or toluidine blue, and histologic changes were scored according to a modified Mankin system. Signaling proteins were assayed by Western blotting; apoptosis was detected via immunohistochemistry and TUNEL analyses. Results CF101 induced a marked decrease in knee diameter and improved the changes noted on radiographs. Administration of MRS1220 counteracted the effects of CF101. CF101 prevented cartilage damage, osteoclast/osteophyte formation, and bone destruction. In addition, CF101 markedly reduced pannus formation and lymphocyte infiltration. Mechanistically, CF101 induced deregulation of the NF-,B signaling pathway, resulting in down-regulation of tumor necrosis factor ,. Consequently, CF101 induced apoptosis of inflammatory cells that had infiltrated the knee joints; however, it prevented apoptosis of chondrocytes. Conclusion CF101 deregulated the NF-,B signaling pathway involved in the pathogenesis of OA. CF101 induced apoptosis of inflammatory cells and acted as a cartilage protective agent, which suggests that it would be a suitable candidate drug for the treatment of OA. [source] Inhibition of adjuvant-induced arthritis by systemic tissue inhibitor of metalloproteinases 4 gene deliveryARTHRITIS & RHEUMATISM, Issue 12 2002Mahmut Y. Çeliker Objective An imbalance in the matrix metalloproteinase:tissue inhibitor of metalloproteinases (MMP:TIMP) ratio in favor of MMP appears to be an important determinant of tissue damage in arthritis. We undertook this study to explore whether reversal of this imbalance in favor of TIMP would alter this process and to examine the mechanism of this alteration. Methods We administered human TIMP-4 by electroporation-mediated intramuscular injection of naked DNA using the rat adjuvant-induced arthritis (AIA) model. Results Intramuscular naked TIMP-4 gene administration resulted in high circulating TIMP-4 levels and completely abolished arthritis development in the rat AIA model. This inhibition was associated with significantly decreased MMP activity in the joint tissue as well as with significantly decreased serum and tissue tumor necrosis factor , levels and serum interleukin-1, levels compared with animals with arthritis. The mutation of cysteine at position 1 of TIMP-4 failed to block the development of AIA. Conclusion Our data indicate that TIMP-4 is a potent antiinflammatory agent, and that its antiarthritis function may be mediated by MMPs. Arthritis-inhibiting effects of TIMP-4 may suggest a unique application of this gene therapy method for arthritis. [source] New and emerging treatments in dermatology: acneDERMATOLOGIC THERAPY, Issue 2 2008A. Katsambas ABSTRACT:, Topical retinoids, benzoyl peroxide, azelaic acid, and topical and oral antibiotics remain the milestone of treatment for mild to moderate acne vulgaris. Oral isotretinoin is useful for the treatment of severe nodular acne, treatment-resistant acne, and acne with a risk of physical or psychological scarring. Hormonal treatment in female acne is useful in resistant or late-onset acne. With increasing concerns regarding teratogenicity of isotretinoin and increasing antibiotic resistance, there is a clear need for therapeutic alternatives to these long-used treatments. Research in the pathogenesis of acne has allowed for new therapies and future perspectives regarding acne to evolve. They include low-dose long-term isotretinoin regimens, insulin-sensitizing agents, 5,-reductase type 1 inhibitors, topical photodynamic therapy, new combination formulations, dietary interventions, and antiinflammatory agents such as lipoxygenase inhibitors. [source] Effects of furocoumarins from Cachrys trifida on some macrophage functionsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2001M. J. Abad Phytochemical and biological studies aimed at the discovery and development of novel antiinflammatory agents from natural sources have been conducted in our laboratory for a number of years. In this communication, three naturally occurring furocoumarins (imperatorin, isoimperatorin and prantschimgin) were evaluated as potential inhibitors of some macrophage functions involved in the inflammatory process. These furocoumarins have been tested in two experimental systems: ionophore-stimulated mouse peritoneal macrophages serve as a source of cyclooxygenase-1 and 5-lipoxygenase, and mouse peritoneal macrophages stimulated with E. coli lipopolysaccharide are the means of testing for anti-cyclooxygenase-2 and nitric-oxide-synthase activity. All above-mentioned furocoumarins showed significant effect on 5-lipoxygenase (leukotriene C4) with IC50 values of < 15 ,M. Imperatorin and isoimperatorin exhibited strong-to-medium inhibition on cyclooxygenase-1- and cyclooxygenase-2-catalysed prostaglandin E2 release, with inhibition percentages similar to those of the reference drugs, indometacin and nimesulide, respectively. Of the three furocoumarins, only imperatorin caused a significant reduction of nitric oxide generation. Imperatorin and isoimperatorin can be classified as dual inhibitors, since it was evident that both cyclooxygenase and lipoxygenase pathways of arachidonate metabolism were inhibited by these compounds. However, selective inhibition of the 5-lipoxygenase pathway is suggested to be the primary target of action of prantschimgin. [source] Effects of some pharmacological agents on the survival of unipedicled venous flaps: an experimental studyMICROSURGERY, Issue 8 2001Ibrahim Askar M.D. Clinical and experimental studies have been conducted to improve the survival of venous flaps. As a result of these studies, although various survival mechanisms were raised, none obtained satisfactory information. Venous stasis, and the resultant venous thrombosis, is a factor that decreases the survival of venous flaps. In this study, we evaluated the effects of two antiinflammatory agents, etodolac and etofenamate, on the survival of unipedicled venous flaps. In this study, 35 male New Zealand white rabbits (3,500,4,000 g) (70 ears) were used. Perichondrocutaneous flaps, 3 × 4.5 cm in size, were designed and raised, keeping the central veins intact in the middle of venous flap. Central arteries and nerves were ligated and transected both proximally and distally, to prepare unipedicled venous flaps. A silicone sheet was placed between the cartilage tissue and flap, to prevent blood flow and revascularization beneath. The subjects were divided into seven groups, consisting of five rabbits (10 ears). In the negative control group (group I), the single vascular pedicle of venous flaps, central veins were ligated and flaps sutured into their own place as the composite graft. In the positive control group (group II), after venous flaps were prepared, normal saline, 0.2 mL, was given subcutaneously. In the first of five experimental groups (group III), unfractionated heparin (100 U/day) was given subcutaneously. In the second experimental group (group IV), etodolac (5 mg/kg/day) was given subcutaneously. In the third experimental group (group V), etophenamate (5 mg/kg/day) was given orally through a feeding tube. In the fourth experimental group (group VI), parnaparin (5 anti-Xa U/kg/day) was given subcutaneously. In the fifth experimental group (group VII), nadroparin (5 anti-Xa U/kg/day) was given subcutaneously, about 7 days postoperatively. At the eighth postoperative day, surviving areas of venous flaps were measured, and the results were evaluated by Kruskal-Wallis ANOVA and Mann-Whitney U-test (P < 0.05). Biopsies were also taken from the flaps for histological evaluation of border of necrotic tissue. Surviving areas of unipedicled venous flaps were larger in experimental groups than those in negative and positive control group (P < 0.05). However, comparison of the experimental groups demonstrated no statistically significant difference (P > 0.05). We concluded that all pharmacological agents used in the experimental groups succeeded in increasing the survival of unipedicled venous flaps. Survival of the unipedicled venous flap was higher in venous flaps than that of composite graft, clearly showing the importance of the venous pedicle. © 2001 Wiley-Liss Inc. MICROSURGERY 21:350--356, 2001 [source] Antiinflammatory activities of flavonoids and a triterpene caffeate isolated from Bauhinia variegataPHYTOTHERAPY RESEARCH, Issue 7 2008Yerra Koteswara Rao Abstract In the continuing search for novel antiinflammatory agents, six flavonoids, namely kaempferol (1), ombuin (2), kaempferol 7,4,-dimethyl ether 3- O - , - d -glucopyranoside (3), kaempferol 3- O - , - d -glucopyranoside (4), isorhamnetin 3- O - , - d -glucopyranoside (5) and hesperidin (6), together with one triterpene caffeate, 3, - trans -(3,4-dihydroxycinnamoyloxy)olean-12-en-28-oic acid (7) were isolated from the non-woody aerial parts of Bauhinia variegata. Compounds 1,7 were evaluated as inhibitors of some macrophage functions involved in the inflammatory process. These seven compounds significantly and dose dependently inhibited lipopolysaccharide (LPS) and interferon (IFN)- , induced nitric oxide (NO), and cytokines [tumor necrosis factor (TNF)- , and interleukin (IL)-12]. The concentration causing a 50% inhibition (IC50) of NO, TNF- , and IL-12 production by compounds 1, 2 and 7 was approximately 30, 50 and 10 µM, respectively, while at 50, 200 and 40 µM compounds 3, 4, and 5, 6 showed 15,30% inhibition, respectively. On the other hand, compounds 3 and 7 showed no inhibitory effect, while compounds 1, 4,6 reduced by around 10,30% the synthesis of NO by macrophages, when inducible NO synthase was already expressed with LPS/IFN- , for 24 h. These experimental findings lend pharmacological support to the suggested folkloric uses of the plant B. variegata in the management of inflammatory conditions. Copyright © 2008 John Wiley & Sons, Ltd. [source] Phytochemical and antioedematogenic studies of commercial copaiba oils available in BrazilPHYTOTHERAPY RESEARCH, Issue 6 2001Valdir F. Veiga Jr Abstract The composition of eight samples of commercial copaiba oils, used in the Amazonian region as antiinflammatory agents and available in popular markets, were analysed by gas chromatography/mass spectrometry (HRGC-MS). Major differences were observed in their chemical composition and some adulterations were pointed out. When tested in vivo oils 1 and 3, and to a lesser extent oil 6, significantly inhibited bradykinin-induced oedema formation. The other tested oils had no effect. When assessed in carrageenan-induced oedema formation, oils 1, 2 and 6, but not oil 3, significantly attenuated the oedema formation. The other tested oils failed to affect carrageenan-induced paw oedema. Oils 1 and 6 were further fractionated and several sesquiterpenes and diterpenes were detected. It is suggested that the naturally occurring sesquiterpenes present in the copaiba oils seem to be responsible for the antiinflammatory action reported in the folk medicine. Furthermore, our results clearly show an adulteration in copaiba oils available in Brazil. Copyright © 2001 John Wiley & Sons, Ltd. [source] Organotin(IV) tryptophanylglycinates: potential non-steroidal antiinflammatory agents; crystal structure of dibutyltin(IV) tryptophanylglycinateAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 9 2009Mala Nath Abstract Diorganotin(IV) derivatives of tryptophanylglycine (H2Trp,Gly) with general formula R2Sn(Trp,Gly), where R = Me, n -Bu, Ph and n -Oct, and triorganotin(IV) derivatives R,3 Sn(HTrp,Gly) where R, = Me, n -Bu and Ph, have been synthesized and structurally characterized in the ,solid state as well as in solution on the basis of various spectroscopic techniques, viz. FT-IR, multinuclear 1H, 13C and 119Sn NMR, 119Sn Mössbauer and single crystal X-ray diffraction. These investigations suggest that tryptophanylglycine in R2Sn(Trp,Gly) acts as dianionic tridentate coordinating through carboxylate oxygen [C(O)O,], amino nitrogen (NH2) and N,peptide, while in the case of R,3 Sn(HTrp,Gly), the ligand acts as monoanionic bidentate coordinating through C(O)O, and NH2. This is further confirmed by the single-crystal X-ray structure of n -Bu2Sn(Trp,Gly) which shows that two butyl groups and peptide nitrogen (N,peptide) are in the equatorial positions, while the two axial positions are occupied by the carboxylic oxygen [C(O)O,] and the amino nitrogen (NH2) atom from the same ligand molecule in the distorted trigonal,bipyramidal geometry around tin. The anti-inflammatory (using the carrageenan-induced paw edema bioassay in rats), cardiovascular activities and acute toxicity (LD50) of some of these compounds have been examined. All of the studied R2Sn(Trp,Gly) and Ph3Sn(HTrp,Gly) exhibit very high anti-inflammatory activities comparable to that of phenylbutazone along with high safety margin (LD50 > 400 mg kg,1) with no side effects on the cardiovascular system. Copyright © 2009 John Wiley & Sons, Ltd. [source] Efficacy of traditional and biologic agents in different clinical phenotypes of adult-onset Still's diseaseARTHRITIS & RHEUMATISM, Issue 8 2010Stefano Franchini Objective To evaluate the efficacy of antiinflammatory agents, steroids, immunosuppressants, and biologic agents in patients with adult-onset Still's disease (AOSD) who have either chronic articular disease or nonchronic disease. Methods Forty-five patients with AOSD were seen and followed up for at least 2 years at our institution, from 1991 to 2008. The majority of patients were treated with several therapeutic regimens; a total of 152 efficacy trials were administered. Data regarding the type of medication, the dosage used, and the outcome of these trials were collected and analyzed. Results Our data showed that the efficacy of monotherapy with a nonsteroidal antiinflammatory drug was very low (16%) and confirmed good efficacy of steroid therapy (63%), particularly in patients without chronic articular disease (78%). Patients whose disease did not respond to steroid therapy at the time of disease onset were at risk of the subsequent development of chronic arthritis. Disease-modifying antirheumatic drug (DMARD) monotherapy was successful in controlling steroid-resistant or steroid-dependent disease in 60% of patients. Methotrexate and cyclosporine showed the best response rates. The combination of high-dose steroids and cyclosporine was administered to successfully control some acute life-threatening complications. Only 6 patients had disease that was both steroid resistant and DMARD resistant. Treatment with biologic agents eventually led to satisfactory control of disease manifestations in 5 (83%) of these 6 patients. Conclusion Steroids were less effective in patients with chronic articular disease than in those with nonchronic disease. The administration of DMARDs early after disease onset could be beneficial in patients with steroid-resistant disease who are at risk of the development of chronic articular disease. Biologic agents proved to be highly effective in both steroid-resistant and DMARD-resistant AOSD. [source] ECL Cell Histamine Mobilization Studied byGastric Submucosal Microdialysis in Awake Rats:Methodological ConsiderationsBASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 2 2003Peter Ericsson They secrete histamine in response to circulating gastrin. Gastric submucosal microdialysis has been used to study ECL-cell histamine mobilization in awake rats. In the present study we assess the usefulness and limitations of the technique. Microdialysis probes were implanted in the gastric submucosa. Histological analysis of the stomach wall around the probe revealed a moderate, local inflammatory reaction 1,2 days after implantation; the inflammation persisted for at least 10 days. Experiments were conducted 3 days after the implantation. The "true" submucosal histamine concentration was determined by perfusing at different rates (the zero flow method) or with different concentrations of histamine at a constant rate (the no-net-flux method): in fasted rats it was calculated to be 87±5 (means±S.E.M.) nmol/l and 76±9 nmol/l, respectively. The corresponding histamine concentrations in fed rats were 93±5 and 102±8 nmol/l, respectively. With a perfusion rate of 74 ,l/hr the recovery of submucosal histamine was 49%, at 34 ,l/hr the recovery increased to 83%. At a perfusion rate below 20 ,l/hr the microdialysate histamine concentration was close to the actual concentration in the submucosa. The ECL-cell histamine mobilization was independent of the concentrations of Ca2+ in the perfusion medium (0,3.4 mmol/l Ca2+). In one experiment, histamine mobilization in response to gastrin (10 nmol/kg/hr subcutaneously) was monitored in rats pretreated with prednisolone (60 mg/kg) or indomethacin (15 mg/kg). The two antiinflammatory agents failed to affect the concentration of histamine in the microdialysate either before or during the gastrin challenge, which was in accord with the observation that the inflammatory reaction was modest and that inflammatory cells were relatively few around the probe and in the wall of the probe. In another experiment, rats were given aminoguanidine (10 mg/kg) or metoprine (10 mg/kg) 4 hr before the start of gastrin infusion (5 nmol/kg/hr intravenously). Metoprine (inhibitor of histamine N-methyl transferase) did not affect the microdialysate histamine concentration, while aminoguanidine (inhibitor of diamine oxidase) raised both basal and gastrin-stimulated histamine concentrations. We conclude that microdialysis can be used to monitor changes in the concentration of histamine in the submucosa of the stomach, and that the inflammatory reaction to the probe is moderate and does not affect the submucosal histamine mobilization. [source] | |||||||||||||||||||||||||