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Sample records for anti-inflammatory steroidal antedrugs

  1. In vitro anti-inflammatory activities of new steroidal antedrugs: [16alpha,17alpha-d] Isoxazoline and [16alpha,17alpha-d]-3'-hydroxy-iminoformyl isoxazoline derivatives of prednisolone and 9alpha-fluoroprednisolone.

    Science.gov (United States)

    Park, Kwan-K; Ko, Dong-H; You, Z; Khan, M Omar F; Lee, Henry J

    2006-03-01

    A series of new anti-inflammatory steroidal antedrugs with C-16,17-isoxazoline ring system were synthesized and their pharmacological activities were evaluated. We reported earlier that these compounds are promising antedrugs based on the results of 5-day rat croton oil ear edema assay. In the present study, most of these compounds showed high binding affinities to the glucocorticoid receptor of liver cytosol. 21-acetyloxy-9alpha-fluoro-11beta-hydroxy-3,20-dioxo-1,4-pregnadieno [16alpha,17alpha-d] isoxazoline (FP-ISO-21AC) and 11beta,21-dihydroxy-9alpha-fluoro-3,20-dioxo-1,4-pregnadieno [16alpha,17alpha-d] isoxazoline (FP-ISO-21OH) were found 5.0-, 5.3-fold more potent than prednisolone, respectively. Inhibitory effects of the antedrugs on the nitric oxide (NO) production were assessed using LPS-stimulated RAW 264.7 murine macrophage cells. All these steroidal antedrugs exhibited concentration-dependent inhibition of NO production, but their relative potencies were lower than prednisolone. In vitro metabolism study in rat plasma showed that FP-ISO-21AC and 21-acetyloxy-9alpha-fluoro-11beta-hydroxy-3,20-dioxo-1,4-pregnadieno [16alpha,17alpha-d]-3'-hydroxyiminoformyl isoxazoline (FP-OXIM-21AC) were hydrolyzed rapidly, with the half-lives of 2.1 and 4.2 min, respectively. The half-lives of FP-ISO-21OH and 11beta,21-dihydroxy-9alpha-fluoro-3,20-dioxo-1,4-pregnadieno [16alpha,17alpha-d]-3'-hydroxyiminoformyl isoxazoline (FP-OXIM-21OH) were 92.2 and 110.2 min, respectively. PMID:16309722

  2. Synthesis and pharmacological evaluations of new steroidal anti-inflammatory antedrugs: 9alpha-Fluoro-11beta,17alpha,21-trihydroxy-3,20-dioxo-pregna-1,4-diene-16alpha-carboxylate (FP16CM) and its derivatives.

    Science.gov (United States)

    Park, Kwan-Kyun; Ko, Dong-Hoon; You, Zhengqing; Heiman, Ann S; Lee, Henry Joung

    2006-01-01

    In continuing efforts to develop potent anti-inflammatory steroids without systemic adverse effects, methyl 9alpha-fluoro-11beta,17alpha,21-trihydroxy-3,20-dioxo-pregna-1,4-diene-16alpha-carboxylate (FP16CM) and its 16-alkoxycarbonyl derivatives (FP16CE, FP16CP and FP16CB) were synthesized based on the antedrug concept. The steroids were evaluated for their pharmacological activities and adverse systemic effects. All steroidal antedrugs showed both binding affinity to the glucocorticoid receptor in liver cytosol and inhibitory effect on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophage cell. These compounds also inhibited croton-oil-induced ear edema and showed no systemic effects such as thymus atrophy and suppression of corticosterone level after 5-day treatment. Among those compounds tested, FP16CM showed the highest activities in receptor binding, NO inhibition and ear edema, these activities were comparable to those of prednisolone. Hydrolysis study in plasma showed that FP16CB was hydrolyzed rapidly, with the half-live (T1/2) of 3.2 min and the half-lives of other compounds were between 16.9 and 29.4 min. These results support the antedrug concept, of which the decrease in systemic adverse effects is attributed to fast hydrolysis to inactive metabolite in the systemic circulation. PMID:16280144

  3. Non-steroidal anti-inflammatory drug use and the risk of Parkinson's disease

    DEFF Research Database (Denmark)

    Manthripragada, Angelika D; Schernhammer, Eva S; Qiu, Jiaheng;

    2011-01-01

    Experimental evidence supports a preventative role for non-steroidal anti-inflammatory drugs (NSAIDs) in Parkinson's disease (PD).......Experimental evidence supports a preventative role for non-steroidal anti-inflammatory drugs (NSAIDs) in Parkinson's disease (PD)....

  4. Gastrointestinal Complications of Nnon-Steroidal Anti-Inflammatory Drugs

    OpenAIRE

    MH. Moradi Nejad

    2002-01-01

    Non-steroid anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs in rheumatic disorders. This group of drugs has been associated with various degrees of gastroduodenopathy (GD), which is due to inhibition of prostaglandin (PG) synthesis. There are several differences between their side effect in stomach and in duodenum. But all these drugs have gastrointestinal side effect. Several studies on preventing NSAIDs GD have been performed in Europe and north America. There are se...

  5. Two Anti-inflammatory Steroidal Saponins from Dracaena angustifolia Roxb.

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    Yueh-Hsiung Kuo

    2013-07-01

    Full Text Available Two new steroidal saponins, named drangustosides A–B (1–2, together with eight known compounds 3–10 were isolated and characterized from the MeOH extract of Dracaena angustifolia Roxb. The structures of compounds were assigned based on 1D and 2D NMR spectroscopic analyses, including HMQC, HMBC, and NOESY. Compounds 1 and 2 showed anti-inflammatory activity by superoxide generation and elastase release by human neutrophils in response to fMLP/CB.

  6. Two Anti-inflammatory Steroidal Saponins from Dracaena angustifolia Roxb.

    OpenAIRE

    Yueh-Hsiung Kuo; Chung-Yi Ou; Chi-I Chang; Yao-Haur Kuo; Syh-Yuan Hwang; Tsong-Long Hwang; Hui-Chi Huang; Ming-Kuem Lin

    2013-01-01

    Two new steroidal saponins, named drangustosides A–B (1–2), together with eight known compounds 3–10 were isolated and characterized from the MeOH extract of Dracaena angustifolia Roxb. The structures of compounds were assigned based on 1D and 2D NMR spectroscopic analyses, including HMQC, HMBC, and NOESY. Compounds 1 and 2 showed anti-inflammatory activity by superoxide generation and elastase release by human neutrophils in response to fMLP/CB.

  7. Hypersensitivity to non-steroidal anti-inflammatory drugs (NSAIDs)

    DEFF Research Database (Denmark)

    Nissen, Christoffer V; Bindslev-Jensen, Carsten; Mørtz, Charlotte G

    2015-01-01

    BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are reported to be the second most common cause of drug hypersensitivity. In 2011, experts from the EAACI/ENDA group and GA(2)LEN proposed a new classification system for NSAID hypersensitivity. The aim of this study was to classify....... Medical records were retrospectively investigated with respect to the culprit NSAID(s), underlying diseases and symptoms at the primary reaction and during oral provocation tests (OPTs). Data was supplemented with a questionnaire. Classification according to EAACI guideline was based on these findings...... responders reacted to non-pyrazolone drugs. Only one patient could not be classified according to the EAACI/ENDA system. An overlap between respiratory and cutaneous symptoms was found in 15/39 (38%) of patients. CONCLUSIONS: All but one of our patients could be classified according to the EAACI...

  8. Non-steroidal anti-inflammatory drugs and molecular carcinogenesis of colorectal carcinomas

    NARCIS (Netherlands)

    Huls, G; Koornstra, JJ; Kleibeuker, JH

    2003-01-01

    Context Colorectal cancer is the second most common cause of cancer-related mortality in the west. The high incidence and mortality make effective prevention an important public-health and economic issue. Non-steroidal anti-inflammatory drugs (NSAIDs) can inhibit colorectal-carcinogenesis and are am

  9. Variation in postoperative non-steroidal anti-inflammatory analgesic use after colorectal surgery

    DEFF Research Database (Denmark)

    Pommergaard, Hans-Christian; Klein, Mads; Burcharth, Jakob;

    2014-01-01

    BACKGROUND: Non-steroid anti-inflammatory drugs (NSAIDs) have been proposed as part of a multimodal postoperative analgesia in patients operated for colorectal cancer. However, whether these drugs are prescribed and taken by the patients have not been evaluated. The aim of this study was to...

  10. Non-steroidal Anti-inflammatory Drugs in Raptors

    Science.gov (United States)

    Oaks, J. Lindsay; Meteyer, Carol U.

    2012-01-01

    The use of analgesia has become standard, and appropriate, practice in avian medicine. As in mammals, pain control in avian patients is usually accomplished with opioids and nonsteroidal anti-inflammatory drugs (NSAIDs) used singly or in combination for a multimodal approach. Despite their usefulness, widespread use, and relative safety in clinical use, few controlled studies in birds have been conducted on efficacy, safety, and dosing. The guidelines for the use of NSAIDs in raptors and other birds have mainly been empirical. More recently, NSAIDs in free-living raptors have emerged as a major conservation issue with the discovery that diclofenac sodium was responsible for the population crash of three species of Gyps vultures in southern Asia. In this context, residues of veterinary NSAIDs in domestic animals are now considered environmental contaminants that can be significantly toxic to vultures and possibly other avian scavengers. Ironically, the disaster with Asian vultures has led to a considerable body of research on NSAIDs in raptors to the benefit of clinicians who now have scientific information available to help assess dosing, safety, toxicity, and pharmacokinetics of NSAIDs in their raptor patients.

  11. AMP-activated protein kinase is activated by non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    King, Tanya S; Russe, Otto Quintus; Möser, Christine V; Ferreirós, Nerea; Kynast, Katharina L; Knothe, Claudia; Olbrich, Katrin; Geisslinger, Gerd; Niederberger, Ellen

    2015-09-01

    AMP-activated kinase (AMPK) is a cellular energy sensor, which is activated in stages of increased adenosine triphosphate (ATP) consumption. Its activation has been associated with a number of beneficial effects such as decrease of inflammatory processes and inhibition of disease progression of diabetes and obesity. A recent study suggested that salicylate, the active metabolite of the non-steroidal anti-inflammatory drug (NSAID) acetyl-salicylic acid (aspirin), is able to activate AMPK pharmacologically. This observation raised the question whether or not other NSAIDs might also act as AMPK activators and whether this action might contribute to their cyclooxygenase (COX)-independent anti-inflammatory properties. In this study, we investigated mouse and human neuronal cells and liver tissue of mice after treatment with various NSAIDs. Our results showed that the non-selective acidic NSAIDs ibuprofen and diclofenac induced AMPK activation similar to aspirin while the COX-2 selective drug etoricoxib and the non-opioid analgesic paracetamol, both drugs have no acidic structure, failed to activate AMPK. In conclusion, our results revealed that AMPK can be activated by specific non-steroidal anti-inflammatory drugs such as salicylic acid, ibuprofen or diclofenac possibly depending on the acidic structure of the drugs. AMPK might therefore contribute to their antinociceptive and anti-inflammatory properties. PMID:26049010

  12. Appearance of attenuated intestinal polyposis during chronic non-steroidal anti-inflammatory drugs use

    Institute of Scientific and Technical Information of China (English)

    Hugh; James; Freeman

    2012-01-01

    Aspirin and non-steroidal anti-inflammatory drugs (NSAIDS) may prevent sporadic colonic neoplasia and reduce the polyp burden in familial adenomatous polyposis. A 41-year-old pharmacologist with no family history of intestinal polyps or cancer chronically consumed daily aspirin and other non-steroidal anti-inflammatory drugs for decades despite recurrent and multiple gastric ulcers. A cancerous polyp in the colon was endoscopically resected. Over the next 2 decades, almost 50 adenomatous polyps were removed from the rest of his colon and duodenum, typical of an attenuated form of adenomatous polyposis. Chronic and habitual use of aspirin or NSAIDS may have important significance in delaying the appearance of adenomas. The observations here emphasize the important implications for clinical risk assessment in screening programs designed to detect or prevent colon cancer.

  13. Non-steroidal anti-inflammatory drugs-induced small intestinal injury and probiotic agents

    Institute of Scientific and Technical Information of China (English)

    Mario Guslandi

    2012-01-01

    Intestinal bacteria play a role in the development of non-steroidal anti-inflammatory drugs (NSAID)-induced small intestinal injury.Agents such as probiotics,able t omodify the gut ecology,might theoretically be useful in preventing small intestinal damage induced by NSAIDs.The clinical studies available so far do suggest that some probiotic agents can be effective in this respect.

  14. Non-steroidal anti-inflammatory drugs and ulcer complications: a risk factor analysis for clinical decision-making

    DEFF Research Database (Denmark)

    Hansen, J M; Hallas, J; Lauritsen, Jens;

    1996-01-01

    Use of non-steroidal anti-inflammatory drugs (NSAIDs) is recognized as an important cause of peptic ulcer complications. The aim of this nested case-control study was to identify risk factors for NSAID-related ulcer complications.......Use of non-steroidal anti-inflammatory drugs (NSAIDs) is recognized as an important cause of peptic ulcer complications. The aim of this nested case-control study was to identify risk factors for NSAID-related ulcer complications....

  15. Effect of non-steroidal anti-inflammatory drugs on colon carcinoma Caco-2 cell responsiveness to topoisomerase inhibitor drugs

    OpenAIRE

    Ricchi, P; Matola, T Di; Ruggiero, G; D. Zanzi; Apicella, A; Di Palma, A; M. Pensabene; S. Pignata; Zarrilli, R; Acquaviva, A M

    2002-01-01

    Numerous studies demonstrate that the chemopreventive effect of non-steroidal anti-inflammatory drugs on colon cancer is mediated through inhibition of cell growth and induction of apoptosis. For these effects non-steroidal anti-inflammatory drugs have been recently employed as sensitising agents in chemotherapy. We have shown previously that treatments with aspirin and NS-398, a cyclo-oxygenase-2 selective inhibitor, affect proliferation, differentiation and apoptosis of the human colon aden...

  16. Non-Steroidal Anti-Inflammatory Drugs, Variation in Inflammatory Genes, and Aggressive Prostate Cancer

    Directory of Open Access Journals (Sweden)

    John S. Witte

    2010-10-01

    Full Text Available Increasing evidence suggests that prostatic inflammation plays a key role in the development of prostate cancer. It remains controversial whether non-steroidal anti-inflammatory drugs (NSAIDs reduce the risk of prostate cancer. Here, we investigate how a previously reported inverse association between NSAID use and the risk of aggressive prostate cancer is modulated by variants in several inflammatory genes. We found that NSAIDs may have differential effects on prostate cancer development, depending on one’s genetic makeup. Further study of these inflammatory pathways may clarify the mechanisms through which NSAIDs impact prostate cancer risk.

  17. Role of Non-Steroidal Anti-Inflammatory Drugs in Gynecology

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    Anna Livshits

    2010-07-01

    Full Text Available This review summarizes the current use of non-steroidal anti-inflammatory drugs (NSAIDs in obstetrics, gynecology and infertility. These medications are commonly used in different fields of reproductive medicine, for pain management after operative procedures and to relieve dysmenorrhea. In addition to their analgesic effect, NSAIDs are helpful in the management of menorrhagia by decreasing menstrual blood loss. NSAIDs alleviate pain associated with medical abortion, assist in undertaking natural cycle in-vitro fertilization by preventing follicular rupture and reducing premature ovulation, and serve as tocolytics in preterm labor. New NSAIDs may have a growing role in management of women's health.

  18. Postoperative non-steroidal anti-inflammatory drugs and colorectal anastomotic leakage

    DEFF Research Database (Denmark)

    Klein, Mads; Gögenur, Ismail; Rosenberg, Jacob

    2012-01-01

    Anastomotic leakage (AL) is the most important and one of the most serious complications after colorectal resections with primary anastomosis. Any factors that contribute to increase the risk of AL should be identified and - if possible - eliminated. Non-steroidal anti-inflammatory drugs (NSAIDs....... There were significantly more ALs among the patients receiving diclofenac (7/33 vs. 1/42, p=0.018). In uni- and multivariate logistic regression analyses, diclofenac was the only factor associated with increased AL rate. This study functioned as a hypothesis generating study and laid the ground...

  19. Pain Relief for Acute Urolithiasis: The Case for Non-Steroidal Anti-Inflammatory Drugs.

    Science.gov (United States)

    Steinberg, Peter L; Chang, Steven L

    2016-07-01

    Pain from renal colic is often severe and incapacitating. Many patients require emergent hospitalization and aggressive analgesia to relieve such discomfort. For many years, the optimal analgesic strategy has been sought to manage such severe pain. One of the mainstays of therapy for acute renal colic is with non-steroidal anti-inflammatory drugs (NSAIDs). This paper reviews the mechanism by which NSAIDs allow pain relief in renal colic, the evidence for their use in this condition, and the use of NSAIDs combined with other agents in renal colic. PMID:27286841

  20. Non-steroidal anti-inflammatory drugs and renal response to exercise

    DEFF Research Database (Denmark)

    Olsen, Niels Vidiendal; Jensen, N G; Hansen, J M;

    1999-01-01

    Nabumetone, a newer non-steroidal anti-inflammatory drug (NSAID) which preferentially blocks cyclo-oxygenase-2 activity, may be less nephrotoxic than indomethacin. This study tested whether nabumetone has effects different from those of indomethacin on exercise-induced changes in renal function...... decreased the plasma renin concentration. Thus, during exercise, nabumetone may decrease the excretion of 6-oxo-PGF(1alpha) by inhibition of cyclo-oxygenase-1 or by inhibition of specific exercise-induced activation of cyclo-oxygenase-2, or both. None of the drugs changed the renal response to exercise...

  1. Prescribing non-steroidal anti-inflammatory drugs: a prospective study of patients' preference

    OpenAIRE

    Scott, D L; Low-Beer, T S; Roden, S.; Takavarasha, L.

    1982-01-01

    Thirty-six patients with rheumatoid arthritis were allocated at random to one of 3 groups prescribed 4 different non-steroidal anti-inflammatory drugs (NSAID). Each drug was given for one week over 4 consecutive weeks in a balanced order. The patients were then asked to select one NSAID for continuation therapy and were followed-up 6 months later. The success of the patient selection method was compared with that of physician selection by retrospectively surveying NSAID prescribing in 164 pat...

  2. A short history of anti-rheumatic therapy. III. Non steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    P. Marson

    2011-06-01

    Full Text Available The chemical advances of the 20th century led to the synthesis of non steroidal anti-inflammatory drugs (NSAIDs, beginning from phenylbutazone and indomethacin and continuing with other new drugs, including ibuprofen, diclofenac, naproxen, piroxicam and, more recently, the highly selective COX-2 inhibitors (coxibs. This progress derived from the discovery of the mechanism of action of these drugs: the inhibition of synthesis of prostaglandins due to the cycloxigenase enzyme system, according to the experimental contributions of John R. Vane.

  3. Steroid Injection and Nonsteroidal Anti-inflammatory Agents for Shoulder Pain

    Science.gov (United States)

    Sun, Yaying; Chen, Jiwu; Li, Hong; Jiang, Jia; Chen, Shiyi

    2015-01-01

    Abstract Advantages and possible risks associated with steroid injection compared with nonsteroidal anti-inflammatory drugs (NSAIDs) for shoulder pain are not fully understood. To compare the efficiency and safety of steroid injection versus NSAIDs for patients with shoulder pain. PubMed, Embase, and the Cochrane Library were searched through July 2015. Study eligibility criteria, participants, and interventions: randomized controlled trials (RCTs) that assessed steroid injection versus NSAIDs for patients with shoulder pain. Study appraisal and synthesis methods: predefined primary efficacy outcome was functional improvement; and secondary efficacy outcomes included pain relief and complications. Relative risks (RRs) and standardized mean differences (SMDs) with 95% confidence intervals (CIs) were calculated using a random-effects model accounting for clinical heterogeneity. Eight RCTs involving 465 participants were included in the meta-analysis. Five trials compared steroid injection with oral NSAIDs, and 3 compared steroids injection with NSAIDs injection. Compared with steroid injection, oral NSAIDs were less effective in 4 or 6 weeks for functional improvement (SMD 0.61; 95% CI, 0.08–1.14; P = 0.01), while there was no significant difference in pain relief (SMD 0.45; 95% CI, −0.50–1.40; P shoulder pain were included, detailed intervention protocols were inconsistent across studies, and some estimated data were input into comparison while some data were lost, which could exert an influence on pooled results. Steroid injection, compared with oral NSAIDs, provides slightly more improvement in shoulder function without superiority in pain relief or risk of complications at 4 to 6 weeks. Treatment decision should be made based on diseases. NSAIDs injection might be a treatment method for shoulder pain. PMID:26683932

  4. [Appropriate prescription, adherence and safety of non-steroidal anti-inflammatory drugs].

    Science.gov (United States)

    Sostres, Carlos; Lanas, Ángel

    2016-03-18

    Non-steroidal anti-inflammatory drugs (NSAIDs) are the most numerous category of drugs sharing the same mechanism of action and therapeutic activities (anti-inflammatory, analgesic and anti-pyretic). Despite having similar efficacy for pain relieve, the different available NSAIDs show variability in its safety profile. The risk of gastrointestinal and cardiovascular complications varies depending on the dose of NSAID and also the presence of different risk factors. It is necessary, therefore, an individualized case assessment before establishing the indication of the best NSAID for each patient, taking account of the best gastroprotection strategy. Improved prescription and enhanced treatment adherence are central objectives to reduce NSAID-related complications. A recent consensus of the Spanish Association of Gastroenterology and the Spanish societies of Cardiology and Rheumatology intends to promote the rational use of NSAIDs according to new recent studies. This review provides additional aspects to facilitate the optimal decision-making process in the routine use of these drugs in clinical practice. PMID:26724872

  5. Topical non steroidal anti inflammatory drug (NSAIDs microemulsions: Rationale, review and future prospective

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    Vinod Singh

    2013-01-01

    Full Text Available Microemulsions serve as ideal candidates as potential drug delivery system due to their specialized qualities of improved solubilisation of drug, extended shelf life and ease of method of preparation and administration to patients. The unique features of microemulsions are thermodynamically stable, clear, colloidal dispersion of water and oil that are stabilized by surfactant and cosurfactant. Microemulsion typically has a droplet diameter of approximately 100 nm or less. Microemulsions have numerous applications in pharmaceutics and many other industries. In the present review we shall discuss about the various aspects of microemulsion with respect to the field of non steroidal anti inflammatory drug, along with its preparation, evaluation and research work carried out in microemulsion.

  6. The non-steroidal anti-inflammatory drug diclofenac is readily biodegradable in agricultural soils

    Energy Technology Data Exchange (ETDEWEB)

    Al-Rajab, Abdul Jabbar; Sabourin, Lyne [Agriculture and Agri-Food Canada, London, ON, Canada N5V 4T3 (Canada); Lapen, David R. [Agriculture and Agri-Food Canada, Ottawa ON, Canada K1A 0C6 (Canada); Topp, Edward, E-mail: ed.topp@agr.gc.ca [Agriculture and Agri-Food Canada, London, ON, Canada N5V 4T3 (Canada)

    2010-12-01

    Diclofenac, 2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid, is an important non-steroidal anti-inflammatory drug widely used for human and animals to reduce inflammation and pain. Diclofenac could potentially reach agricultural lands through the application of municipal biosolids or wastewater, and in the absence of any environmental fate data, we evaluated its persistence in agricultural soils incubated in the laboratory. {sup 14}C-Diclofenac was rapidly mineralized without a lag when added to soils varying widely in texture (sandy loam, loam, clay loam). Over a range of temperature and moisture conditions extractable {sup 14}C-diclofenac residues decreased with half lives < 5 days. No extractable transformation products were detectable by HPLC. Diclofenac mineralization in the loam soil was abolished by heat sterilization. Addition of biosolids to sterile or non-sterile soil did not accelerate the dissipation of diclofenac. These findings indicate that diclofenac is readily biodegradable in agricultural soils.

  7. Non-steroidal anti-inflammatory drugs in prevention of gastric cancer

    Institute of Scientific and Technical Information of China (English)

    Yun Dai; Wei-Hong Wang

    2006-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs)including cyclooxygenase 2 (COX-2) selective inhibitors,are potential agents for the chemoprevention of gastric cancer. Epidemiological and experimental studies have shown that NSAID use is associated with a reduced risk of gastric cancer although many questions remain unanswered such as the optimal dose and duration of treatment. The possible mechanisms for the suppressor effect of NSAIDs on carcinogenesis are the ability to induce apoptosis in epithelial cells and regulation of angiogenesis. Both COX-dependent and COX-independent pathways have a role in the biological activity of NSAIDs. Knowledge of how NSAIDs prevent neoplastic growth will greatly aid the design of better chemopreventive drugs and novel treatments for gastric cancer.

  8. Study of Osteoarthritis Treatment with Anti-Inflammatory Drugs: Cyclooxygenase-2 Inhibitor and Steroids

    Directory of Open Access Journals (Sweden)

    Hongsik Cho

    2015-01-01

    Full Text Available Patients with osteoarthritis (OA, a condition characterized by cartilage degradation, are often treated with steroids, nonsteroidal anti-inflammatory drugs (NSAIDs, and cyclooxygenase-2 (COX-2 selective NSAIDs. Due to their inhibition of the inflammatory cascade, the drugs affect the balance of matrix metalloproteinases (MMPs and inflammatory cytokines, resulting in preservation of extracellular matrix (ECM. To compare the effects of these treatments on chondrocyte metabolism, TNF-α was incubated with cultured chondrocytes to mimic a proinflammatory environment with increasing production of MMP-1 and prostaglandin E2 (PGE2. The chondrocytes were then treated with either a steroid (prednisone, a nonspecific COX inhibitor NSAID (piroxicam, or a COX-2 selective NSAID (celecoxib. Both prednisone and celecoxib decreased MMP-1 and PGE-2 production while the nonspecific piroxicam decreased only the latter. Both prednisone and celecoxib decreased gene expression of MMP-1 and increased expression of aggrecan. Increased gene expression of type II collagen was also noted with celecoxib. The nonspecific piroxicam did not show these effects. The efficacy of celecoxib in vivo was investigated using a posttraumatic OA (PTOA mouse model. In vivo, celecoxib increases aggrecan synthesis and suppresses MMP-1. In conclusion, this study demonstrates that celecoxib and steroids exert similar effects on MMP-1 and PGE2 production in vitro and that celecoxib may demonstrate beneficial effects on anabolic metabolism in vivo.

  9. Chiral separation of non-steroidal anti-inflammatory drugs by preparative and simulated moving bed chromatography

    OpenAIRE

    Ribeiro, António E.; Gomes, Pedro Sá; Pais, L.S.; A.E. Rodrigues

    2011-01-01

    The work presents modelling, simulation and experimental results for the chiral separation of non-steroidal anti-inflammatory drugs, particularly, the optimization of mobile phase composition under preparative and simulated moving bed chromatography. The experimental separation of two chiral systems (ketoprofen and flurbiprofen enantiomers) will be presented to show how compounds of the same family can lead to different solutions.

  10. Effects of Non-Steroidal Anti-Inflammatory Drugs onFlexor Tendon Rehabilitation after Repair

    Directory of Open Access Journals (Sweden)

    Alireza Rouhani

    2013-09-01

    Full Text Available   Background: Peritendinous adhesions after repairing an injury to the digital flexor tendons are a major problem in hand surgery. Non-steroidal anti-inflammatory drug therapy may affect tendon healing and the development of peritendinous adhesions. The aim of this study was to evaluate ibuprofen effect in patients function after flexor tendon surgical repair.   Method: Thirty-five patients, who had sharp-edge lacerations of hand-zone II requiring flexor tendons repair, participated in this randomized double-blind clinical trial study. The patients were randomly classified into two parallel and matched groups (21 patients in the intervention group and 14 patients in the control group. The groups were matched considering age, gender, and laceration size. The control group received a placebo with the same appearance and dosage. In the intervention group, ibuprofen was prescribed at a high dosage (2400 mg/day. The range of motion improvement rate of the involved fingers and the patients’ performance after their follow-up period were compared. Results: There was a statistically significant difference between the two groups for range of motion of the involved finger joints (P=0.03. According to the DASH score, there was a statistically significant difference between the final performance of the patients, such that it was 11±2.4 and 18.4±6.3 in the intervention and control groups, respectively (P=0.01. There was not any case of re-tear or need to re-operate in the intervention and control groups. Conclusion: Our findings reveal that ibuprofen with an anti-inflammatory dose was effective in improving the range of motion of the involved fingers joints after flexor tendon injury.

  11. Effects of Non-Steroidal Anti-Inflammatory Drugs onFlexor Tendon Rehabilitation after Repair

    Directory of Open Access Journals (Sweden)

    Alireza Rouhani

    2013-09-01

    Full Text Available Background: Peritendinous adhesions after repairing an injury to the digital flexor tendons are a major problem in hand surgery. Non-steroidal anti-inflammatory drug therapy may affect tendon healing and the development of peritendinous adhesions. The aim of this study was to evaluate ibuprofen effect in patients function after flexor tendon surgical repair.   Method: Thirty-five patients, who had sharp-edge lacerations of hand-zone II requiring flexor tendons repair, participated in this randomized double-blind clinical trial study. The patients were randomly classified into two parallel and matched groups (21 patients in the intervention group and 14 patients in the control group. The groups were matched considering age, gender, and laceration size. The control group received a placebo with the same appearance and dosage. In the intervention group, ibuprofen was prescribed at a high dosage (2400 mg/day. The range of motion improvement rate of the involved fingers and the patients’ performance after their follow-up period were compared. Results: There was a statistically significant difference between the two groups for range of motion of the involved finger joints (P=0.03. According to the DASH score, there was a statistically significant difference between the final performance of the patients, such that it was 11±2.4 and 18.4±6.3 in the intervention and control groups, respectively (P=0.01. There was not any case of re-tear or need to re-operate in the intervention and control groups. Conclusion: Our findings reveal that ibuprofen with an anti-inflammatory dose was effective in improving the range of motion of the involved fingers joints after flexor tendon injury.

  12. Steroids block the anti-inflammatory effects of low level laser therapy

    Science.gov (United States)

    Lopes-Martins, Rodrigo Alvaro B.; Albertini, Regiane; Lopes-Martins, Patricia Sardinha L.; Iversen, Vegard V.; Bjordal, Jan M.

    2006-02-01

    Objective: Concomitant use of multiple therapies is common in musculoskeletal and airway disorders. Low level laser therapy (LLLT) is considered a promising therapy in arthritis, tendinopathies and rhinitis. We designed two animal studies to assess if the expected anti-inflammatory effect LLLT could be affected by resection of the adrenal gland or concomitant use of the cortisol antagonist mifepristone. Methods: Two studies were performed, with 40 male Wistar rats and with 40 Balb C male mice respectively.. In both studies, four groups received carrageenan and one control group received saline. At 1, 2, and 3 hours after injections, LLLT irradiation was performed with a dose of 7.5 J/cm2. In the rat study, two of the carrageenan groups had the adrenal gland dissected. In the mice study, two of the carrageenan-injected groups were in addition pre-treated with orally administered mifepristone. Results: In the rat paw study, LLLT reduced edema significantly compared to the carrageenan only group (1.5 vs 0.9 ml, p< 0.05), but LLLT failed to inhibit edema formation in the group which had the adrenal gland resected. In carrageenan-induced pleurisy, LLLT significantly reduced the number of leukocyte cells ( p<0.0001, Mean 34.5 [95%CI: 32.8 - 36.2] versus 87.7 [95%CI: 81.0 - 94.4]), and that the effect of LLLT could be totally blocked by adding the cortisol antagonist mifepristone ( p<0.0001, Mean 34.5 [95%CI: 32.1 - 36.9] versus 82.9 [95%CI: 70.5 - 95.3]). Conclusion: Steroid therapy should not be used concomitantly with LLLT, as the anti-inflammatory effect of LLLT is lost if cortisol receptors are downregulated.

  13. Non-steroidal anti-inflammatory drugs and statins in relation to colorectal cancer risk

    Institute of Scientific and Technical Information of China (English)

    Mazyar Shadman; Polly A Newcomb; John M Hampton; Karen J Wernli; Amy Trentham-Dietz

    2009-01-01

    AIM: To investigate the association between individual or combined use of non-steroidal anti-inflammatory drugs (NSAIDs) or statins and colorectal cancer risk. METHODS: In a population-based case-control study in women, we examined the association between NSAIDs and statin use and the risk of colorectal cancers. We further investigated whether the use of statins modifies the protective effect of NSAIDs. Female cases ( n = 669)of colorectal cancer aged 50-74 years were identified from a statewide registry in Wisconsin during 1999-2001. Community control women ( n = 1375) were randomly selected from lists of licensed drivers and Medicare beneficiaries. Medication use and risk factor information were gathered during a structured telephone interview. A multivariable logistic regression model was used to calculate odds ratio (OR) and 95% confidence interval (CI). RESULTS: Overall, NSAIDs users had a 30% reduction in risk of colorectal cancer (95% CI: 0.56-0.88). Statin use was not associated with colorectal cancer risk (OR = 1.17, 95% CI: 0.74-1.85), regardless of structural type (lipophilic or hydrophilic), duration of use, or recency. There was no evidence of an interaction between NSAIDs and statins and colorectal cancer risk ( P-interaction = 0.28). CONCLUSION: Although our results confirm the inverse association between NSAIDs use and colorectal cancer risk, they do not support a risk reduction in statin users, or an interaction effect of combined NSAIDs and statin use.

  14. Non-steroidal anti-inflammatory drug prescriptions in hospital inpatients: are we assessing the risks?

    LENUS (Irish Health Repository)

    Kitchen, J

    2012-02-01

    AIM: To determine non-steroidal anti-inflammatory drug (NSAID) prescribing practices in a tertiary referral hospital. METHODS: A single time-point audit of drug kardexes and clinical notes of n = 388 patients on 2 July 2008 was carried out assessing demographics, gastrointestinal and coronary heart disease risk factors, renal function and co-prescribed medications. RESULTS: Fifty-seven of 388 (14.7%) hospital patients were on NSAIDs. Forty-nine were prescribed NSAID after admission. Nineteen (32.2%) were on regular NSAID (11\\/19 on PPI) and 38 patients were on PRN NSAID (12\\/38 on PPI). Seventeen of 49 patients were on other medications associated with gastrointestinal bleeding (10\\/17 were on PPI). Nineteen patients (33.3%) were >60 years. Eight patients had three or four risk factors for gastrointestinal bleeding; six were on PPI. Thirteen patients had two risks; 7 were on PPI. Six of 19 patients with one risk factor were on PPI. 40.3% had stage 2\\/3 chronic kidney disease. 35.1% had ischaemic heart disease. CONCLUSIONS: NSAIDs and PPIs are often prescribed inappropriately.

  15. Helicobacter pylori-negative, non-steroidal anti-inflammatory drug: negative idiopathic ulcers in Asia.

    Science.gov (United States)

    Iijima, Katsunori; Kanno, Takeshi; Koike, Tomoyuki; Shimosegawa, Tooru

    2014-01-21

    Since the discovery of Helicobacter pylori (H. pylori) infection in the stomach, the bacteria infection and non-steroidal anti-inflammatory drugs (NSAIDs) use had been considered to be the 2 main causes of peptic ulcers. However, there have been recent reports of an increase in the proportion of peptic ulcers without these known risk factors; these are termed idiopathic peptic ulcers. Such trend was firstly indicated in 1990s from some reports in North America. In Asia, numerous studies reported that idiopathic ulcers accounted for a small percentage of all ulcers in the 1990s, but in the 2000s, multiple studies reported that the proportion of idiopathic ulcers had reached 10%-30%, indicating that the incidence of idiopathic ulcers in Asia has also been rising in recent years. While a decline in H. pylori infection rates of general population in Asia is seen as the main reason for the increased incidence of idiopathic ulcers, it is also possible that the absolute number of idiopathic ulcer cases has increased. Advanced age, serious systemic complication, and psychological stress are considered to be the potential risk factors for idiopathic ulcers. Management of idiopathic ulcers is challenging, at present, because there is no effective preventative measure against recurrence in contrast with cases of H. pylori-positive ulcers and NSAIDs-induced ulcers. As it is expected that H. pylori infection rates in Asia will decline further in the future, measures to treat idiopathic ulcers will also likely become more important.

  16. Interactions between non-steroidal anti-inflammatory drugs and lipid membranes

    Science.gov (United States)

    Boggara, Mohan; Krishnamoorti, Ramanan

    2008-03-01

    Chronic usage of Non-steroidal anti-inflammatory drugs(NSAIDs) leads to gastrointestinal toxicity and clinical evidences point the cause to direct interactions between NSAIDs and phospholipid membranes. Also, NSAIDs pre-associated with phospholipid vesicles are shown to be safer and therapeutically more effective than unmodified ones. Our initial experiments and simulations on the partitioning of Aspirin and Ibuprofen clearly indicate role played by the drug structure in drug-membrane interactions. Those results motivated systematic molecular dynamics simulations of membranes with NSAIDs of different size, structure and pKa values. Our results suggest high partition coefficients for these NSAIDs in the membrane compared to water and thinning effect on the bilayer. Our small angle neutron scattering and reflectivity studies on DMPC-Ibuprofen systems indicate that the drug affects both ˜5 nm thick bilayer and overall ˜100 nm diameter vesicle, indicating that NSAIDs affect vesicles on various length scales. We will discuss the structural perturbations to membranes due to NSAIDs at clinically relevant molar ratios and their implications on the use of vesicles as delivery vehicles for NSAIDs.

  17. The Comparison of Efficacy of Tricyclic Antidepressant with and without Non Steroidal Anti Inflammatory Drugs in Chronic Low Back Pain

    OpenAIRE

    A.R. Yavarikia

    2007-01-01

    Introduction & Objectives: Low back pain (LBP) is one of common medical problems with several accepted medical modalities such as drugs, physiotherapy, surgery, etc. We studied the efficacy of tricyclic antidepressant (TCA), and tricyclic antidepressant plus non steroidal anti inflammatory drugs (TCA + NSAID) in 200 patients with chronic LBP. Materials & Methods: In an experimental clinical trial study on patients with chronic low back pain without organic findings, patients were divided in t...

  18. Toxicity of non-steroidal anti-inflammatory drugs to Gyps vultures: a new threat from ketoprofen

    OpenAIRE

    Naidoo, Vinny; Wolter, Kerri; Cromarty, Duncan; Diekmann, Maria; Duncan, Neil; Meharg, Andrew A.; Taggart, Mark A.; Venter, Leon; Cuthbert, Richard

    2009-01-01

    Three Gyps vulture species are on the brink of extinction in South Asia owing to the veterinary non-steroidal anti-inflammatory drug (NSAID) diclofenac. Carcasses of domesticated ungulates are the main food source for Asia's vultures and birds die from kidney failure after consuming diclofenac-contaminated tissues. Here, we report on the safety testing of the NSAID ketoprofen, which was not reported to cause mortality in clinical treatment of scavenging birds and is rapidly eliminated from li...

  19. Post-cataract prevention of inflammation and macular edema by steroid and nonsteroidal anti-inflammatory eye drops

    DEFF Research Database (Denmark)

    Kessel, Line; Tendal, Britta; Jørgensen, Karsten Juhl;

    2014-01-01

    PURPOSE: Favorable outcome after cataract surgery depends on proper control of the inflammatory response induced by cataract surgery. Pseudophakic cystoid macular edema is an important cause of visual decline after uncomplicated cataract surgery. DESIGN: We compared the efficacy of topical steroids...... with topical nonsteroidal anti-inflammatory drugs (NSAIDs) in controlling inflammation and preventing pseudophakic cystoid macular edema (PCME) after uncomplicated cataract surgery. PARTICIPANTS: Patients undergoing uncomplicated surgery for age-related cataract. METHODS: We performed a systematic literature...

  20. Duodenal histology, ulceration, and Helicobacter pylori in the presence or absence of non-steroidal anti-inflammatory drugs.

    OpenAIRE

    Taha, A S; Dahill, S; Nakshabendi, I.; Lee, F D; Sturrock, R D; Russell, R I

    1993-01-01

    Duodenitis and gastric metaplasia, which is often colonised by Helicobacter pylori (H pylori), are increasingly recognised for their importance in the pathogenesis of duodenal ulcers. The situation is not clear in patients receiving non-steroidal anti-inflammatory drugs (NSAIDs), who have a higher risk of peptic ulceration. The aim of this study was to identify the duodenal histological abnormalities in the presence or absence of NSAIDs, H pylori, and duodenal ulceration. Endoscopic duodenal ...

  1. The influence of non-steroidal anti-inflammatory drugs on the gut microbiome.

    Science.gov (United States)

    Rogers, M A M; Aronoff, D M

    2016-02-01

    The composition of the gut microbiome with the use of non-steroidal anti-inflammatory drugs (NSAIDs) has not been fully characterized. Drug use within the past 30 days was ascertained in 155 adults, and stool specimens were submitted for analysis. Area under the receiver operating characteristic curve (AUC) was calculated in logit models to distinguish the relative abundance of operational taxonomic units (OTUs) by medication class. The type of medication had a greater influence on the gut microbiome than the number of medications. NSAIDs were particularly associated with distinct microbial populations. Four OTUs (Prevotella species, Bacteroides species, family Ruminococcaceae, and Barnesiella species) discriminated aspirin users from those using no medication (AUC = 0.96; 95% CI 0.84-1.00). The microbiome profile of celecoxib users was similar to that of ibuprofen users, with both showing enrichment of Acidaminococcaceae and Enterobacteriaceae. Bacteria from families Propionibacteriaceae, Pseudomonadaceae, Puniceicoccaceae and Rikenellaceae were more abundant in ibuprofen users than in controls or naproxen users. Bacteroides species and Erysipelotrichaceae species discriminated individuals using NSAIDs plus proton-pump inhibitors from those using NSAIDs alone (AUC = 0.96; 95% CI 0.87-1.00). Bacteroides species and a bacterium of family Ruminococcaceae discriminated individuals using NSAIDs in combination with antidepressants and laxatives from those using NSAIDs alone (AUC = 0.98; 95% CI 0.93-1.00). In conclusion, bacteria in the gastrointestinal tract reflect the combinations of medications that people ingest. The bacterial composition of the gut varied with the type of NSAID ingested. PMID:26482265

  2. Effects of non-steroidal anti-inflammatory drug (NSAID) diclofenac exposure in mussel Mytilus galloprovincialis.

    Science.gov (United States)

    Gonzalez-Rey, Maria; Bebianno, Maria João

    2014-03-01

    In recent years, research studies have increasingly focused on assessing the occurrence of active pharmaceutical ingredients (APIs) in ecosystems. However, much remains unknown concerning the potential effects on APIs on non-target organisms due to the complexity of the mode of action, reactivity and bioconcentration potential for each specific drug. The non-steroidal anti-inflammatory drug (NSAID) diclofenac (DCF) is one of the most frequently detected APIs in surface waters worldwide and has recently been included in the list of priority substances under the European Commission. In this study, mussels (Mytilus galloprovincialis) were exposed to an environmentally relevant nominal concentration of DCF (250 ng L(-1)) over 15 days. The responses of several biomarkers were assessed in the mussel tissues: condition index (CI); superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GR) and phase II glutathione-S-transferase (GST) activities, lipid peroxidation levels (LPO) associated with oxidative stress, acetylcholinesterase (AChE) activity related to neurotoxic effects and vitellogenin-like proteins linked to endocrine disruption. This study demonstrated significant induction of SOD and GR activities in the gills in addition to high CAT activity and LPO levels in the digestive gland. Phase II GST remained unaltered in both tissues, while the up-regulation of the AChE activity was directly related to the vitellogenin-like protein levels in exposed females, indicating an alteration in the estrogenic activity, rather than a breakdown in cholinergic neurotransmission function. This study confirmed that DCF at a concentration often observed in surface water induces tissue-specific biomarker responses. Finally, this study also revealed the importance of a multi-biomarker approach when assessing the potentially deleterious effects in a species that may be vulnerable to the continuously discharge of APIs into the ecosystems; this approach provides crucial new

  3. New insights into the use of currently available non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Brune, Kay; Patrignani, Paola

    2015-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs), which act via inhibition of the cyclooxygenase (COX) isozymes, were discovered more than 100 years ago. They remain a key component of the pharmacological management of acute and chronic pain. The COX-1 and COX-2 isozymes have different biological functions; analgesic activity is primarily (although not exclusively) associated with inhibition of COX-2, while different side effects result from the inhibition of COX-1 and COX-2. All available NSAIDs, including acetaminophen and aspirin, are associated with potential side effects, particularly gastrointestinal and cardiovascular effects, related to their relative selectivity for COX-1 and COX-2. Since all NSAIDs exert their therapeutic activity through inhibition of the COX isozymes, strategies are needed to reduce the risks associated with NSAIDs while achieving sufficient pain relief. A better understanding of the inhibitory activity and COX-1/COX-2 selectivity of an NSAID at therapeutic doses, based on pharmacokinetic and pharmacodynamic properties (eg, inhibitory dose, absorption, plasma versus tissue distribution, and elimination), and the impact on drug tolerability and safety can guide the selection of appropriate NSAIDs for pain management. For example, many NSAIDs with moderate to high selectivity for COX-2 versus COX-1 can be administered at doses that maximize efficacy (~80% inhibition of COX-2) while minimizing COX-1 inhibition and associated side effects, such as gastrointestinal toxicity. Acidic NSAIDs with favorable tissue distribution and short plasma half-lives can additionally be dosed to provide near-constant analgesia while minimizing plasma concentrations to permit recovery of COX-mediated prostaglandin production in the vascular wall and other organs. Each patient's clinical background, including gastrointestinal and cardiovascular risk factors, should be taken into account when selecting appropriate NSAIDs. New methods are emerging to assist

  4. Oxidation of non-steroidal anti-inflammatory drugs with aqueous permanganate.

    Science.gov (United States)

    Rodríguez-Álvarez, Tania; Rodil, Rosario; Quintana, José Benito; Triñanes, Sara; Cela, Rafael

    2013-06-01

    Potassium permanganate is a strong oxidant widely used in drinking water treatment, that can react with organic micropollutants. Thus, the oxidation kinetics and transformation route of seven non-steroidal anti-inflammatory drugs (NSAIDs) upon reaction with potassium permanganate was investigated. A liquid chromatography-quadrupole-time-of-flight-mass spectrometry (LC-Q-TOF-MS) system was used to follow the time course of pharmaceuticals concentrations and for the identification of their by-products. Under strong oxidation conditions (2 mg L(-1) KMnO4, 24 h), only two NSAIDs were significantly degraded: indomethacine and diclofenac. The degradation kinetics of these two drugs was investigated at different concentrations of permanganate, chlorides, phosphates and sample pH by means of a full factorial experimental design. Depending on these factors, half-lives were in the range: 2-270 h for indomethacine and 3-558 h for diclofenac, equivalent to apparent second order constants between 0.65 and 9.5 M(-1) s(-1) and 0.27 and 7.4 M(-1) s(-1), respectively. Permanganate concentration was the most significant factor on NSAIDs oxidation kinetics, but the pH also played a significant role in diclofenac reaction, being faster at acidic pH. In the case of indomethacine, the dose of permanganate seemed also to play an autocatalytic effect. The use of an accurate-mass high resolution LC-Q-TOF-MS system permitted the identification of a total of 13 by-products. The transformation path of these drugs consisted mainly of hydroxylations, decarboxylations and oxidation of aromatic double bonds, with ring opening. The software predicted toxicity of these products indicates that they are expected not to be more toxic than the NSAIDs, with the exception of two indomethacine by-products. Reaction in real samples was slower and/or incomplete for both pharmaceuticals, depending on the organic matter content of the sample. However, still all transformation products could be detected for

  5. New insights into the use of currently available non-steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Brune K

    2015-02-01

    Full Text Available Kay Brune,1 Paola Patrignani2 1Department of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander University Erlangen-Nuremberg, Erlangen, Germany; 2Department of Neuroscience, Imaging and Clinical Sciences, Center of Excellence on Aging, G d’Annunzio University, Chieti, Italy Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs, which act via inhibition of the cyclooxygenase (COX isozymes, were discovered more than 100 years ago. They remain a key component of the pharmacological management of acute and chronic pain. The COX-1 and COX-2 isozymes have different biological functions; analgesic activity is primarily (although not exclusively associated with inhibition of COX-2, while different side effects result from the inhibition of COX-1 and COX-2. All available NSAIDs, including acetaminophen and aspirin, are associated with potential side effects, particularly gastrointestinal and cardiovascular effects, related to their relative selectivity for COX-1 and COX-2. Since all NSAIDs exert their therapeutic activity through inhibition of the COX isozymes, strategies are needed to reduce the risks associated with NSAIDs while achieving sufficient pain relief. A better understanding of the inhibitory activity and COX-1/COX-2 selectivity of an NSAID at therapeutic doses, based on pharmacokinetic and pharmacodynamic properties (eg, inhibitory dose, absorption, plasma versus tissue distribution, and elimination, and the impact on drug tolerability and safety can guide the selection of appropriate NSAIDs for pain management. For example, many NSAIDs with moderate to high selectivity for COX-2 versus COX-1 can be administered at doses that maximize efficacy (~80% inhibition of COX-2 while minimizing COX-1 inhibition and associated side effects, such as gastrointestinal toxicity. Acidic NSAIDs with favorable tissue distribution and short plasma half-lives can additionally be dosed to provide near-constant analgesia while

  6. Evaluation of the analgesic and anti-inflammatory activity of fixed dose combination: Non-steroidal anti-inflammatory drugs in experimental animals

    Directory of Open Access Journals (Sweden)

    Amit Lahoti

    2014-01-01

    Conclusion: Combining paracetamol with ibuprofen enhances analgesic/anti-inflammatory activity over their individual component but potentiation of analgesic activity of diclofenac was not seen when paracetamol was added to it.

  7. Aspirin and non-aspirin non-steroidal anti-inflammatory drug use and risk of lung cancer.

    Science.gov (United States)

    Lim, Wei-Yen; Chuah, Khoon Leong; Eng, Philip; Leong, Swan Swan; Lim, Elaine; Lim, Tow Keang; Ng, Alan; Poh, Wee Teng; Tee, Augustine; Teh, Ming; Salim, Agus; Seow, Adeline

    2012-08-01

    There is evidence that aspirin and non-aspirin non-steroidal anti-inflammatory drug (NSAID) have anti-carcinogenic properties, but their effect on lung cancer, in particular in never-smokers, is unclear. Information on past or current use of anti-inflammatory medication was obtained in 398 Chinese female primary lung cancer cases and 814 controls in a hospital-based study in Singapore. 65% of cases and 88% of controls were never-smokers. Controls were excluded if they had been admitted for conditions associated with aspirin or NSAID use (n=174). Regular aspirin use (twice a week or more, for a month or more) was associated with a reduced risk of lung cancer (adjusted odds ratio [OR] 0.50, 95% confidence intervals [95%CI] 0.31-0.81 in non-smokers; OR 0.38, 95%CI 0.16-0.93 in smokers). Regular use of non-aspirin NSAID, paracetamol, steroid creams and steroid pills was uncommon and no association with lung cancer was detected. Our results suggest that aspirin consumption may reduce lung cancer risk in Asian women and are consistent with current understanding of the role of cyclooxygenase in lung carcinogenesis.

  8. Effects of non-steroidal anti-inflammatory drugs and prostaglandins on alkali secretion by rabbit gastric fundus in vitro

    OpenAIRE

    Rees, W D W; Gibbons, L C; Turnberg, L A

    1983-01-01

    The effects of non-steroidal anti-inflammatory drugs and prostaglandins E2 and F2α on the secretory and electrical activity of isolated rabbit fundic mucosa have been studied. Spontaneous acid secretion was inhibited by serosal side application of sodium thiocyanate (6×10−2M) and the resulting alkali secretion measured by pH stat tiration. Serosal side application of indomethacin (10−5M) or aspirin (3×10−3M) inhibited alkali secretion (0·55±0·06 to 0·12±0·06 μmol/cm2/h, n=6, p

  9. Non-steroidal anti-inflammatory drugs and risk of cardiovascular disease in patients with rheumatoid arthritis

    DEFF Research Database (Denmark)

    Lindhardsen, Jesper; Gislason, Gunnar Hilmar; Jacobsen, Søren;

    2013-01-01

    OBJECTIVE: To examine the risk of major cardiovascular disease associated with non-steroidal anti-inflammatory drugs (NSAIDs) in a large 'real-world' contemporary rheumatoid arthritis (RA) cohort. METHODS: A longitudinal cohort study was conducted with use of Danish nationwide individual......-level registry data on inpatient and outpatient health care provision, pharmacotherapy and income during 1997-2009. 17 320 RA patients were identified and matched with 69 280 controls (4 : 1) by age and sex. NSAID-associated risk of major cardiovascular disease defined as the combined endpoint of myocardial...

  10. Aspirin and other non-steroidal anti-inflammatory drugs and risk of colorectal cancer: A Danish cohort study

    DEFF Research Database (Denmark)

    Friis, Søren; Poulsen, Aslak H; Sørensen, Henrik Toft;

    2009-01-01

    The optimal duration and dose of aspirin and non-aspirin non-steroidal anti-inflammatory drugs (NSAIDs) in the potential prevention of colorectal cancer (CRC) have not been established. We examined this issue in the Danish Diet, Cancer, and Health Study. Self-reported NSAID use at entry (January...... 1995-May 1997) was updated through June 2006, using a nationwide prescription database. CRC incidence was ascertained from nationwide registers. Cox proportional hazards regression was used to compute confounder-adjusted incidence rate ratios (RRs) and 95% confidence intervals (CIs). From 51,053 cohort...

  11. [Mefenamic acid and other non-steroidal anti-inflammatory agents in dental practice. A review of the literature].

    Science.gov (United States)

    Künzel, André Rätzer; Haschke, Manuel; Surber, Christian; Lambrecht, J Thomas

    2007-01-01

    There are no studies verifying that mefenamic acid is more effective than other NSAID (= non-steroidal anti-inflammatory drugs). However, there are several notions in the literature that this drug is less well-tolerated than other NSAID because over a prolonged period of application more lesions of the upper gastro-intestinal tract are induced as well as occasionally renal insufficiency. Compared to other NSAID the systemic toxicity starts already with relatively low doses above the maximal daily dose. Considering current knowledge there is no reason to prefer mefenamic acid to other NSAID. PMID:17330662

  12. The effect of the non-steroidal anti-inflammatory drug diclofenac sodium on thefetuses of albino mice

    Directory of Open Access Journals (Sweden)

    Mohamed A. Shahin, Ramadan A. Ramadan, Samia M. Sakr and Sahar A. Sabry

    2011-07-01

    Full Text Available Introduction: The present study was carried out to evaluate the effect of the non-steroidal anti-inflammatory drug diclofenac sodium (DS on the fetuses of albino mice from the morphological and skeletal points of view. Material and methods: Sixty adult pregnant female mice were used in the present study. They were allocated into 6 groups (10 mice each. The first two groups served as control and were injected intraperitoneally (i.p. with the solvent of the drug, and the 3rd and 5th groups were treated with 1.5 and 3mg/kg body weight of diclofenac sodium for 6 days ( gestation days 1-6 , respectively ; the 4th and 6th groups were treated with 1.5and 3mg/kg body weight of the drug for 8 days ( gestation days 7-14, respectively. Results: The morphological examination of the fetuses of treated groups showed conspicuous decrease in the average body weight and body length in all treated groups. The fetuses maternally treated with the drug showed noticeable external morphological malformations and their skeletons exhibited mild retardation in skeletal elements. In conclusion: The non-steroidal anti-inflammatory drug diclofenac sodium had exerted marked morphological malformations and mild skeletal alterations in mice fetuses maternally treated during different periods of gestation.

  13. Gaultherin, a natural salicylate derivative from Gaultheria yunnanensis: towards a better non-steroidal anti-inflammatory drug.

    Science.gov (United States)

    Zhang, Bin; He, Xiao-Li; Ding, Yi; Du, Guan-Hua

    2006-01-13

    One of the major factors limiting the use of non-steroidal anti-inflammatory drugs is gastrointestinal toxicity. Gaultherin, 2-[(6-O-beta-D-Xylopyranosyl-beta-D-glucopyranosyl)oxy] benzoic acid methyl ester, a natural salicylate derivative extracted from Gaultheria yunnanensis, has been shown to have analgesic and anti-inflammatory effects and lack gastric ulcerogenic effect compared to aspirin in our primary study. The aim of this study was to investigate the mechanism of action of gaultherin, which may rely on its active metabolite, and the mechanism responsible for the non-ulcerogenic property. The results showed that gaultherin (200 mg/kg) significantly inhibited the abdominal contractions in the acetic acid-induced writhing test in mice. The anti-inflammatory effect of gaultherin was demonstrated in the croton oil-induced ear edema model in mice. The results showed that gaultherin and equimolar dose of aspirin produced comparable inhibitory effects. The study of the metabolism characters of gaultherin in mice and rats indicated that gaultherin could be metabolically converted to salicylate, which produced the pharmacological effects, and provided effective concentrations for an extended period. In vitro metabolism experiment showed that gaultherin was metabolized by beta-glycosidase produced by human intestinal bacteria and esterases in intestine, blood and liver successively to release salicylate finally. The study suggested gaultherin did not cause gastric ulcer for the reason that it released salicylate in intestine slowly, not in stomach and it left the cyclooxygenase-1 unaffected, which was the source of cytoprotective prostaglandins in gastric epithelium. PMID:16375889

  14. 非甾体抗炎药与麻醉药的相互作用%Interaction of non-steroidal anti-inflammatory drugs and anesthetics

    Institute of Scientific and Technical Information of China (English)

    刘陆陆; 吕黄伟

    2012-01-01

    非甾体抗炎镇痛药(Non-steroidal anti-inflammatory drugs,NSAIDs)主要用于围手术期超前镇痛.本文对NSAIDs与常用的麻醉药如阿片类药、吸入麻醉药、静脉麻醉药和苯二氮艹卓类药物的相互作用加以综述.%Non-steroidal anti-inflammatory drugs( NSAIDs )is mainly used for perioperative preemptive analgesia. This article summarizes the interaction between NSAIDs and anesthetics such as opioids, inhalation anesthetics, intravenous anesthetics and benzodiazepines.

  15. Breast Cancer Stem Cell Potent Copper(II)-Non-Steroidal Anti-Inflammatory Drug Complexes.

    Science.gov (United States)

    Boodram, Janine N; Mcgregor, Iain J; Bruno, Peter M; Cressey, Paul B; Hemann, Michael T; Suntharalingam, Kogularamanan

    2016-02-18

    The breast cancer stem cell (CSC) potency of a series of copper(II)-phenanthroline complexes containing the nonsteroidal anti-inflammatory drug (NSAID), indomethacin, is reported. The most effective copper(II) complex in this series, 4, selectivity kills breast CSC-enriched HMLER-shEcad cells over breast CSC-depleted HMLER cells. Furthermore, 4 reduces the formation, size, and viability of mammospheres, to a greater extent than salinomycin, a potassium ionophore known to selectively inhibit CSCs. Mechanistic studies revealed that the CSC-specificity observed for 4 arises from its ability to generate intracellular reactive oxygen species (ROS) and inhibit cyclooxygenase-2 (COX-2), an enzyme that is overexpressed in breast CSCs. The former induces DNA damage, activates JNK and p38 pathways, and leads to apoptosis.

  16. Pharmacology and potential therapeutic applications of nitric oxide-releasing non-steroidal anti-inflammatory and related nitric oxide-donating drugs

    Science.gov (United States)

    Keeble, J E; Moore, P K

    2002-01-01

    This review examines the biological significance, therapeutic potential and mechanism(s) of action of a range of nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAID) and related nitric oxide-releasing donating drugs (NODD). The slow release of nitric oxide (NO) from these compounds leads to subtle changes in the profile of pharmacological activity of the parent, non-steroidal anti-inflammatory drugs (NSAID). For example, compared with NSAID, NO-NSAID cause markedly diminished gastrointestinal toxicity and improved anti-inflammatory and anti-nociceptive efficacy. In addition, nitroparacetamol exhibits hepatoprotection as opposed to the hepatotoxic activity of paracetamol. The possibility that NO-NSAID or NODD may be of therapeutic benefit in a wide variety of disease states including pain and inflammation, thrombosis and restenosis, neurodegenerative diseases of the central nervous system, colitis, cancer, urinary incontinence, liver disease, impotence, bronchial asthma and osteoporosis is discussed. PMID:12237248

  17. Ongoing treatment with non-steroidal anti-inflammatory drugs at time of admission is associated with poorer prognosis in patients with first-time acute myocardial infarction

    DEFF Research Database (Denmark)

    Lamberts, M.; Fosbol, E. L.; Olsen, A. M. S.;

    2013-01-01

    Background: Use of non-steroidal anti-inflammatory drugs (NSAIDs) has been associated with increased cardiovascular morbidity and mortality. The purpose of this study was to examine the effect of ongoing NSAID treatment at time of admission for myocardial infarction (MI) on prognosis. Methods: Al...

  18. Expression of pleiotrophin, an important regulator of cell migration, is inhibited in intestinal epithelial cells by treatment with non-steroidal anti-inflammatory drugs

    Science.gov (United States)

    Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely used drugs for the suppression of inflammation and pain. However, the analgesic properties of NSAIDs are also associated with significant negative side effects, most notably in the gastrointestinal (GI) tract. Increasingly, evi...

  19. Exposure to non-steroidal anti-inflammatory drugs during pregnancy and the risk of selected birth defects: a prospective cohort study

    NARCIS (Netherlands)

    Gelder, M.M.H.J. van; Roeleveld, N.; Nordeng, H.

    2011-01-01

    BACKGROUND: Since use of non-steroidal anti-inflammatory drugs (NSAIDs) during pregnancy is common, small increases in the risk of birth defects may have significant implications for public health. Results of human studies on the teratogenic risks of NSAIDs are inconsistent. Therefore, we evaluated

  20. A STUDY OF PRESCRIBING PATTERN OF NON STEROIDAL ANTI INFLAMMATORY DRUGS IN ORTHOPEDIC OUT PATIENT DEPARTMENT AT A TERTIARY CARE HOSPITAL

    OpenAIRE

    Asha Latha; Srinivasu; Ananda Babu Naik; Jaya Chandra

    2015-01-01

    AIM: To determine the pattern of NON STEROIDAL ANTI INFLAMMATORY DRUGS prescribing for arthritic and non - arthritic conditions in orthopedic outpatient department . METHODOLOGY: 100 prescription duplicate collected and analyzed prospectively for the pattern of NSAID prescription for arthritic and non - arthritic conditions; the drug formulation , route , frequency, duration of adm issio n and concomitant medications results. NSAID were...

  1. Impact of proton pump inhibitor treatment on gastrointestinal bleeding associated with non-steroidal anti-inflammatory drug use among post-myocardial infarction patients taking antithrombotics

    DEFF Research Database (Denmark)

    Schjerning Olsen, Anne-Marie; Lindhardsen, Jesper; Gislason, Gunnar H;

    2015-01-01

    STUDY QUESTION: What is the effect of proton pump inhibitors (PPIs) on the risk of gastrointestinal bleeding in post-myocardial infarction patients taking antithrombotics and treated with non-steroidal anti-inflammatory drugs (NSAIDs)? METHODS: This was a nationwide cohort study based on linked...

  2. Analysis of Adverse Reaction of Analgesics, Antipyretics and Non-Steroidal Anti-Inflammatory Drugs Prescribed by Physicians of Health Care Facilities in Podilskyi Region during 2015

    OpenAIRE

    Stepaniuk, N. H.; Hladkykh, F. V.; Basarab, O. V.

    2016-01-01

    The problem of medicines rational use exists all over the world. It concerns particularly analgesics, antipyretics and non-steroidal anti-inflammatory drugs (NSAIDs). In Ukraine the side effects caused by non-steroidal antiphlogistics rank the second place according to the prevalence among all registered cases.The objective of the research was to analyze adverse drug reaction report forms concerning adverse reactions caused by the use of NSAIDs, analgesics, antipyretics, and were submitted du...

  3. The synovial prostaglandin system in chronic inflammatory arthritis: differential effects of steroidal and nonsteroidal anti-inflammatory drugs

    Science.gov (United States)

    Bombardieri, S.; Cattani, P.; Ciabattoni, G.; Di Munno, O.; Pasero, G.; Patrono, C.; Pinca, E.; Pugliese, F.

    1981-01-01

    1 The present study was undertaken to characterize the spectrum of arachidonic acid metabolites present in synovial effusions of patients with rheumatoid or psoriatic arthritis, and to compare changes in their concentration following a short-term treatment with 6α-methyl-prednisolone (6-MeP: 4-8 mg/day) or indoprofen (1.2 g/day), a nonsteroidal anti-inflammatory agent with proven synovial prostaglandin inhibitory effect. 2 Measurements of prostaglandin E2 (PGE2), thromboxane (TX) B2, 6-keto-PGF1α and PGF2α were performed by radioimmunoassay techniques in synovial effusions obtained from 23 patients, and validated by thin-layer chromatographic analysis of the extracted immunoreactivity. 3 PGE2 and TXB2 accounted for more than 60% of the total immunoreactivity in untreated patients. The absence of any constant ratio between the different arachidonic acid metabolites detected in synovial fluid is consistent with a heterogeneous cellular origin of these compounds. 4 Indoprofen treatment was associated with a consistent reduction of synovial prostaglandin and thromboxane concentrations, ranging from 36% in the case of 6-keto-PGF1α to 90% in the case of PGE2. 5 In contrast, 6-MeP caused opposite changes on different metabolites originating via the cyclo-oxygenase pathway. Thus, 6-keto-PGF1α concentrations were reduced by 35%, PGF2α concentrations were increased by 30%, while PGE2 and TXB2 were unchanged following 6-MeP. 6 Although the mechanism(s) underlying the failure of 6-MeP to reduce synovial PGE2 and TXB2 levels are uncertain, the results of the present study clearly indicate that therapeutic doses of steroidal and nonsteroidal anti-inflammatory drugs cause quite distinct changes in arachidonic acid metabolism, which might be relevant to their specific therapeutic actions and side-effects. PMID:6895043

  4. Role of Helicobacter pylori eradication in aspirin or non-steroidal anti-inflammatory drug users

    Institute of Scientific and Technical Information of China (English)

    George V. Papatheodoridis; Athanasios J. Archimandritis

    2005-01-01

    Helicobacter pylori (H pylori) infection and the use of nonsteroidal anti-inflammatory drugs (NSAIDs) including aspirin at any dosage and formulation represent well-established risk factors for the development of uncomplicated and complicated peptic ulcer disease accounting for the majority of such cases. Although the interaction between H pylori and NSAID/aspirin use in the same individuals was questioned in some epidemiological studies, it has now become widely accepted that they are at least independent risk factors for peptic ulcer disease. According to data from randomized intervention trials, naive NSAID users certainly benefit from testing for H pylori infection and, if positive,H pylori eradication therapy prior to the initiation of NSAID. A similar strategy is also suggested for naive aspirin users, although the efficacy of such an approach has not been evaluated yet. Strong data also support that chronic aspirin users with a recent ulcer complication should be tested for H pyloriinfection and, if positive, receive H pylori eradication therapy after ulcer healing, while they appear to benefit from additional long-term therapy with a proton pump inhibitor (PPI).A similar approach is often recommended to chronic aspirin users at a high risk of ulcer complication. H pylori eradication alone does not efficiently protect chronic NSAID users with a recent ulcer complication or those at a high-risk, who certainly should be treated with long-term PPI therapy, but H pylori eradication may be additionally offered even in this setting. In contrast, testing for H pylorior PPI therapy is not recommended for chronic NSAID/aspirin users with no ulcer complications or those at a low risk of complications.

  5. 2-hydroxy arachidonic acid: a new non-steroidal anti-inflammatory drug.

    Directory of Open Access Journals (Sweden)

    Daniel H Lopez

    Full Text Available BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs are a family of COX1 and COX2 inhibitors used to reduce the synthesis of pro-inflammatory mediators. In addition, inflammation often leads to a harmful generation of nitric oxide. Efforts are being done in discovering safer NSAIDs molecules capable of inhibiting the synthesis of pro-inflammatory lipid mediators and nitric oxide to reduce the side effects associated with long term therapies. METHODOLOGY/PRINCIPAL FINDINGS: The analogue of arachidonic acid (AA, 2-hydroxy-arachidonic acid (2OAA, was designed to inhibit the activities of COX1 and COX2 and it was predicted to have similar binding energies as AA for the catalytic sites of COX1 and COX2. The interaction of AA and 2OAA with COX1 and COX2 was investigated calculating the free energy of binding and the Fukui function. Toxicity was determined in mouse microglial BV-2 cells. COX1 and COX2 (PGH2 production activities were measured in vitro. COX1 and COX2 expression in human macrophage-like U937 cells were carried out by Western blot, immunocytochemistry and RT-PCR analysis. NO production (Griess method and iNOS (Western blot were determined in mouse microglial BV-2 cells. The comparative efficacy of 2OAA, ibuprofen and cortisone in lowering TNF-α serum levels was determined in C57BL6/J mice challenged with LPS. We show that the presence of the -OH group reduces the likelihood of 2OAA being subjected to H* abstraction in COX, without altering significantly the free energy of binding. The 2OAA inhibited COX1 and COX2 activities and the expression of COX2 in human U937 derived macrophages challenged with LPS. In addition, 2OAA inhibited iNOS expression and the production of NO in BV-2 microglial cells. Finally, oral administration of 2OAA decreased the plasma TNF-α levels in vivo. CONCLUSION/SIGNIFICANCE: These findings demonstrate the potential of 2OAA as a NSAID.

  6. Selection of non-steroidal anti-inflammatory drug and treatment regimen for sulfur mustard-induced cutaneous lesions.

    Science.gov (United States)

    Plahovinsak, Jennifer L; Buccellato, Matthew A; Reid, Frances M; Graham, John S

    2016-09-01

    The inflammatory process plays an important role in sulfur mustard (HD) injury and HD pathogenesis, suggesting that anti-inflammatory treatments applied as soon as possible following HD injury may reduce tissue damage and accelerate healing. This study used the HD dermal weanling swine model to investigate the efficacy of two non-steroidal anti-inflammatory drugs, capsaicin and diclofenac, when applied in combination with the steroid, clobetasol. The therapeutic regimen was also investigated with respect to initiation of treatment post-exposure, frequency and duration. Yorkshire-cross pigs were randomly assigned to experimental groups, corresponding to all combinations of treatment (capsaicin with clobetasol or diclofenac with clobetasol), onset time (1, 2 or 4 h post-exposure), treatment duration (1, 3 or 5 days) and frequency of applications (2, 3 or 4 per day). For each animal, two sites on the ventral abdomen were exposed to 400 μL of neat HD for 8 min to achieve superficial dermal (SD) lesions and two sites were exposed to 400 μL neat HD for 30 min to achieve deep dermal (DD) lesions. Each treatment regimen was tested against a SD and a DD injury. Untreated SD and DD lesion sites served as within-animal controls. Assessments, up to one week post-challenge, included digital photographs, clinical assessments (lesion size measurements and modified Draize scoring), transepidermal water loss (TEWL), reflectance colorimetry and histopathologic evaluations that included an estimate for depth of injury and wound healing parameters. Diclofenac plus clobetasol treatment resulted in significant reductions in lesion contracture and modified Draize scores, increased barrier function (decreased TEWL), and increased healing as determined by histopathology for both SD and DD injury when compared with untreated sites and sites treated with capsaicin plus clobetasol. An increased duration of treatment from 1 to 5 days was most commonly associated with decreased

  7. Removal of non-steroidal anti-inflammatory drugs ibuprofen and ketoprofen from water by emulsion liquid membrane.

    Science.gov (United States)

    Dâas, Attef; Hamdaoui, Oualid

    2014-02-01

    In this work, the removal of the worldwide non-steroidal anti-inflammatory drugs ibuprofen (IBP) and ketoprofen (KTP) by emulsion liquid membrane (ELM) was carried out. An ELM system is made up of hexane as diluent, Span 80 as the surfactant and sodium carbonate as the inner aqueous solution. Effect of experimental conditions that affect the extraction of IBP such as surfactant concentration, emulsification time, sulfuric acid concentration in external phase, acid type in external phase, internal phase concentration, type of internal phase, stirring speed, volume ratio of internal phase to membrane phase, treatment ratio, IBP initial concentration, diluent type and salt was investigated. The obtained results showed that by appropriate selection of the operational parameters, it was possible to extract nearly all of IBP molecules from the feed solution even in the presence of high concentration of salt. Under optimum operating conditions, the efficiencies of IBP removal from distilled water (99.3 %), natural mineral water (97.3 %) and sea water (94.0 %) were comparable, which shows that the ELM treatment process represents a very interesting advanced separation process for the removal of IBP from complex matrices such as natural and sea waters. Under the optimized experimental conditions, approximately 97.4 % KTP was removed in less than 20 min of contact time. PMID:24037298

  8. Does non-steroidal anti-inflammatory (NSAID) ibuprofen induce antioxidant stress and endocrine disruption in mussel Mytilus galloprovincialis?

    Science.gov (United States)

    Gonzalez-Rey, Maria; Bebianno, Maria João

    2012-03-01

    Ibuprofen (IBU) is one of the most sold over-the-counter non-steroidal anti-inflammatory drugs (NSAID) and widely detected in the aquatic ecosystems. Nevertheless, the information regarding IBU effects in biota is still sparse. The goal of this study was to assess IBU potential effect as oxidative stress and endocrine disruption inducer in mussel Mytilus galloprovincialis applying a battery of biomarkers. Over two weeks of exposure to IBU (250 ngL(-1)), superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GR), phase II glutathione S-transferase (GST) activities and lipid peroxidation (LPO) levels were determined in the digestive gland and alkali-labile phosphates (ALP) were carried out in sex-differentiated mussels' gonads. The results confirm a transitory induction of antioxidant activities responses concomitant to lipid peroxide formation outline and an increase of ALP levels over time, particularly in exposed males which may lead to mussels' reproductive fitness impairment highlighting a higher impact of IBU as an endocrine disruptor than as a short-term reactive oxygen species (ROS)-generator. PMID:22301165

  9. Pregnant women and non-steroidal anti-inflammatory drugs: Knowledge, perception and drug consumption pattern during pregnancy in Ethiopia

    Directory of Open Access Journals (Sweden)

    Chalelgn Kassaw

    2012-01-01

    Full Text Available Background: Non-steroidal anti-inflammatory drugs (NSAIDs are among the widely used drugs and are often used by pregnant women. However, they can have significant teratogenic effects. The aim of the study was to investigate pregnant women′s knowledge about NSAIDs use during pregnancy and their perception and consumption pattern. Materials and Methods: The study was a cross sectional study on women waiting for a consultation in the selected maternity hospitals in Addis Ababa, Ethiopia. The pregnant women were selected randomly and then interviewed by using standardized questionnaires. Result : A total of 224 pregnant women were involved in the study. Out of those, 203 (90.6% of them have taken NSAIDs since the beginning of their pregnancy. About 201 (89.7%, 198 (88.4% and 189 (84.4% of the pregnant women considered that ibuprofen, diclofenac and aspirin are not NSAIDs respectively. Regarding analgesic effect of NSAIDs, 97 (43.3% of the pregnant women believed that NSAIDs are effective for treating pain. Acetaminophen was considered as the most effective treatment for pain by 84 (37.50% of the patients. Conclusion: Acetaminophen is the most common analgesic that was taken by most pregnant women. The knowledge of pregnant women about NSAIDs is poor.

  10. Enhanced Loading and Release of Non-Steroidal Anti-Inflammatory Drugs from Silica-Based Nanoparticle Carriers.

    Science.gov (United States)

    Mohammadzadeh, Mostafa; Nourbakhsh, Mohammad Sadegh; Khodaverdi, Elham; Hadizadeh, Farzin; Omid Malayeri, Sina

    2016-09-01

    Silica nanoparticles can be potentially considered the carriers of controlled drug systems. In this research, non-steroidal anti-inflammatory drugs were used. Diclofenac sodium and piroxicam were loaded on the considered nanosilica using solvent evaporation method. To prove drug encapsulation on the nanosilica and its rate, infrared spectroscopy, X-ray diffraction, and BET were used, and after proving the existence of the drug in the nanosilica matrix and determining the amount of loading, dissolution test was performed in an environment similar to that of stomach and intestine in terms of pH. Drug loading percentage showed that over 90% of drugs were loaded on nanosilica. Dissolution tests in stomach pH environment showed the control samples (drug without SBA-15) released considerable amount of drugs (about 90%) within first 15 min, when it was about 10-20% for the matrixes. Furthermore, release rate of drugs from matrixes has shown slower rate in comparison with control samples. It was indicated nanosilica has the ability of retaining the drugs in acidic pH and prevented their release. Furthermore, the drugs were released in a controlled manner in small intestine, which is the main absorption site. PMID:27062095

  11. Analysis of chiral non-steroidal anti-inflammatory drugs flurbiprofen, ketoprofen and etodolac binding with HSA

    Institute of Scientific and Technical Information of China (English)

    Chang-Chuan Guo; Yi-Hong Tang; Hai-Hong Hu; Lu-Shan Yu; Hui-Di Jiang; Su Zeng

    2011-01-01

    The protein binding of non-steroidal anti-inflammatory drugs flurbiprofen, ketoprofen and etodolac with human serum albumin (HSA) was investigated using indirect chiral high performance liquid chromatography (HPLC) and ultrafiltration techniques. S-(-)-1-(1-naphthyl)- ethylamine (S-NEA) was utilized as chiral derivatization reagent and pre-column derivatization RP-HPLC method was established for the separation and assay of the three pairs of enantiomer. The method had good linear relationship over the investigated concentration range without interference. The average extraction efficiency was higher than 85% in different systems, and the intra-day and inter-day precisions were less than 15%. In serum albumin, the protein binding of etodolac enantiomers showed significant stereoselectivity that the affinity of S-enantiomer was stronger than R-enantiomer, and the stereoselectivity ratio reached 6.06; Flurbiprofen had only weak stereoselectivity in HSA, and ketoprofen had no stereoselectivity at all. Scatchard curves showed that all the three chiral drugs had two types of binding sites in HSA.

  12. The Comparison of Efficacy of Tricyclic Antidepressant with and without Non Steroidal Anti Inflammatory Drugs in Chronic Low Back Pain

    Directory of Open Access Journals (Sweden)

    A.R. Yavarikia

    2007-07-01

    Full Text Available Introduction & Objectives: Low back pain (LBP is one of common medical problems with several accepted medical modalities such as drugs, physiotherapy, surgery, etc. We studied the efficacy of tricyclic antidepressant (TCA, and tricyclic antidepressant plus non steroidal anti inflammatory drugs (TCA + NSAID in 200 patients with chronic LBP. Materials & Methods: In an experimental clinical trial study on patients with chronic low back pain without organic findings, patients were divided in two groups of 100 cases. At certain times the response to treatment protocols were collected and compared using VAS system. Patient’s data including age, sex, smoking and response to treatment were recorded and analyzed using chi-square, t-tests, ANOVA and SPSS software. Results: 83 (41.5% of patients were males and 117 (58.5% were females. The age range was 21 to 75 (mean age 43.1 14.1y there was no meaning full statistical difference in demographic characteristics such as age, sex (respectively p=0.66, p=0.78 the ultimate pain was less (p0.05.Conclusion: TCA prescription is an efficient method of treatment of low back pain with or with out NSAIDS. But using NSAID+TCA will be almost more powerful and efficient method in the long term period.

  13. Biophysical study of the non-steroidal anti-inflammatory drugs (NSAID) ibuprofen, naproxen and diclofenac with phosphatidylserine bilayer membranes.

    Science.gov (United States)

    Manrique-Moreno, Marcela; Heinbockel, Lena; Suwalsky, Mario; Garidel, Patrick; Brandenburg, Klaus

    2016-09-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) represent an effective pain treatment option and therefore one of the most sold therapeutic agents worldwide. The study of the molecular interactions responsible for their physiological activity, but also for their side effects, is therefore important. This report presents data on the interaction of the most consumed NSAIDs (ibuprofen, naproxen and diclofenac) with one main phospholipid in eukaryotic cells, dimyristoylphosphatidylserine (DMPS). The applied techniques are Fourier-transform infrared spectroscopy (FTIR), with which in transmission the gel to liquid crystalline phase transition of the acyl chains in the absence and presence of the NSAID are monitored, supplemented by differential scanning calorimetry (DSC) data on the phase transition. FTIR in reflection (ATR, attenuated total reflectance) is applied to record the dependence of the interactions of the NSAID with particular functional groups observed in the DMPS spectrum such as the ester carbonyl and phosphate vibrational bands. With Förster resonance energy transfer (FRET) a possible intercalation of the NSAID into the DMPS liposomes and with isothermal titration calorimetry (ITC) the thermodynamics of the interaction are monitored. The data show that the NSAID react in a particular way with this lipid, but in some parameters the three NSAID clearly differ, with which now a clear picture of the interaction processes is possible. PMID:27316371

  14. Ibuprofen and other widely used non-steroidal anti-inflammatory drugs inhibit antibody production in human cells.

    Science.gov (United States)

    Bancos, Simona; Bernard, Matthew P; Topham, David J; Phipps, Richard P

    2009-01-01

    The widely used non-steroidal anti-inflammatory drugs (NSAIDs) function mainly through inhibition of cyclooxygenases 1 and 2 (Cox-1 and Cox-2). Unlike Cox-1, Cox-2 is considered an inducible and pro-inflammatory enzyme. We previously reported that Cox-2 is upregulated in activated human B lymphocytes and using Cox-2 selective inhibitors that Cox-2 is required for optimal antibody synthesis. It is not known whether commonly used non-prescription and non-Cox-2 selective drugs also influence antibody synthesis. Herein, we tested a variety of Cox-1/Cox-2 non-selective NSAIDs, namely ibuprofen, tylenol, aspirin and naproxen and report that they blunt IgM and IgG synthesis in stimulated human peripheral blood mononuclear cells (PBMC). Ibuprofen had its most profound effects in inhibiting human PBMCs and purified B lymphocyte IgM and IgG synthesis when administered in the first few days after activation. As shown by viability assays, ibuprofen did not kill B cells. The implications of this research are that the use of widely available NSAIDs after infection or vaccination may lower host defense. This may be especially true for the elderly who respond poorly to vaccines and heavily use NSAIDs.

  15. [Induction of NAG-1 gene expression in colon cancer cells by non-steroidal anti-inflammatory drugs].

    Science.gov (United States)

    Wang, Chunhui; Ouyang, Qin; Tang, Chengwei; Liu, Rui; Huang, Minghui

    2007-08-01

    This study was conducted to evaluate the growth and NAG-1 gene expression effected by Non-steroidal anti-inflammatory drug (NSAID) on colon cancer cell lines in vitro. The proliferation of colon cancer cells were determined by MTT assay and COX-2 protein expression were detected by Western blot. Total RNA was isolated from three kinds of colon cancer cell lines; the expressions of NAG-1 mRNA in the cells treated with or without NSAIDs were assessed by semi-quantitative reverse transcription-polymerase chain reaction (RT-PCR) assay. Celecoxib, meloxicam and aspirin were able to inhibit the growth of HT-29, SW480 and LS174-T cells in dose-dependent manner. COX-2 protein expressed in HT-29 and LS174-T, but not in SW480 cells. All of colon cancer cells expressed NAG-1 gene and the level of LS174-T was lower than that of the other two cell lines. NAG-1 expression was increased by treatment with some NSAIDs in all three kinds of colon cancer cells. NSAIDs were able to potentially inhibit the growth of colon cell lines. Induction of NAG-1 gene expression by NSAID was not consistent with COX-2 expression. PMID:17899765

  16. Bacterial microbiota profiling in gastritis without Helicobacter pylori infection or non-steroidal anti-inflammatory drug use.

    Directory of Open Access Journals (Sweden)

    Xiao-Xing Li

    Full Text Available Recent 16S ribosomal RNA gene (rRNA molecular profiling of the stomach mucosa revealed a surprising complexity of microbiota. Helicobacter pylori infection and non-steroidal anti-inflammatory drug (NSAID use are two main contributors to gastritis and peptic ulcer. However, little is known about the association between other members of the stomach microbiota and gastric diseases. In this study, cloning and sequencing of the 16S rRNA was used to profile the stomach microbiota from normal and gastritis patients. One hundred and thirty three phylotypes from eight bacterial phyla were identified. The stomach microbiota was found to be closely adhered to the mucosa. Eleven Streptococcus phylotypes were successfully cultivated from the biopsies. One to two genera represented a majority of clones within any of the identified phyla. We further developed two real-time quantitative PCR assays to quantify the relative abundance of the Firmicutes phylum and the Streptococcus genus. Significantly higher abundance of the Firmicutes phylum and the Streptococcus genus within the Firmicutes phylum was observed in patients with antral gastritis, compared with normal controls. This study suggests that the genus taxon level can largely represent much higher taxa such as the phylum. The clinical relevance and the mechanism underlying the altered microbiota composition in gastritis require further functional studies.

  17. Coordination Polymers Derived from Non-Steroidal Anti-Inflammatory Drugs for Cell Imaging and Drug Delivery.

    Science.gov (United States)

    Paul, Mithun; Dastidar, Parthasarathi

    2016-01-18

    A new series of Mn(II) coordination polymers, namely, [{Mn(L)(H2 O)2 }⋅2 Nap]∞ (CP1), [{Mn(L)(Ibu)2 (H2 O)2 }]∞ (CP2), [{Mn(L)(Flr)2 (H2 O)2 }]∞ (CP3), [{Mn(L)(Ind)2 (H2 O)2 }⋅H2 O]∞ (CP4), [{Mn2 (L)2 (μ-Flu)4 (H2 O)}⋅L]∞ (CP5), [{Mn2 (L)2 (μ-Tol)4 (H2 O)2 }]∞ (CP6) and [{Mn2 (L)2 (μ-Mef)4 (H2 O)2 }]∞ (CP7) (Nap=naproxen, Ibu=ibuprofen, Flr=flurbiprofen, Ind=indometacin, Flu=flufenamic acid, Tol=tolfenamic acid and Mef=mefenamic acid) derived from various non-steroidal anti-inflammatory drugs (NSAIDs) and the organic linker 1,2-bis(4-pyridyl)ethylene (L) have been synthesized with the aim of being used for cell imaging and drug delivery. Single-crystal X-ray diffraction (SXRD) studies revealed that the NSAID molecules were part of the coordination polymeric network either through coordination to the metal center (in the majority of the cases) or through hydrogen bonding. Remarkably, all the Mn(II) coordination polymers were found to be soluble in DMSO, thereby making them particularly suitable for the desired biological applications. Two of the coordination polymers (namely, CP1 and CP3) reported herein, were found to be photoluminescent both in the solid as well as in the solution state. Subsequent experiments (namely, MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide), and PGE2 (prostaglandin E2 ) assays) established their biocompatibility and anti-inflammatory response. In vitro studies by using a macrophage cell line (i.e., RAW 264.7) revealed that both CP1 and CP3 were excellent cell imaging agents. Finally, biodegradability studies under simulated physiological conditions in phosphate-buffered saline (PBS) at pH 7.6 showed that slow and sustained release of the corresponding NSAID was indeed possible from both CP1 and CP3.

  18. Assessment of non-steroidal anti-inflammatory and analgesic pharmaceuticals in seawaters of North of Portugal: Occurrence and environmental risk

    OpenAIRE

    Lolić, Aleksandar; Paíga, Paula; Santos, Lúcia H. M. L. M.; Ramos, Sandra; Correia, Manuela; Delerue-Matos, Cristina

    2015-01-01

    The occurrence of seven pharmaceuticals and two metabolites belonging to non-steroidal anti-inflammatory drugs and analgesics therapeutic classes was studied in seawaters. A total of 101 samples covering fourteen beaches and five cities were evaluated in order to assess the spatial distribution of pharmaceuticals among north Portuguese coast. Seawaters were selected in order to embrace different bathing water quality (excellent, good and sufficient). Acetaminophen, ketoprofen and the metaboli...

  19. Risk factors of adverse drug reaction from non-steroidal anti-inflammatory drugs in Shanghai patients with arthropathy

    Institute of Scientific and Technical Information of China (English)

    Wen SHI; Yong-ming WANG; Shao-li LI; Min YAN; Duan Li; Bin-yah CHEN; Neng-neng CHENG

    2004-01-01

    AIM: The study was to screen the possible risk factors of adverse drug reaction (ADR) induced by non-steroidal anti-inflammatory drugs (NSAIDs) in Shanghai patients with arthropathy. METHODS: The subjects were randomly selected from a database of outpatients with arthropathy from 9 main hospitals in Shanghai. A door to door retrospective epidemiological survey was used to collect demographic information about the patients, both individual and familial. This included data on their medical histories, lifestyle and dietary habits, history of smoking and alcohol consumption, history of drug therapy, quality of life (QOL) prior to NSAIDs intake, history of NSAIDs therapy and its ADR events, etc. Descriptive statistical methods and univariate analysis were also used to identify possible risk factors for ADRs induced by NSAIDs. RESULTS: Of the 1002 patients surveyed, the average length of NSAIDs intake was 2 years. ADR incidence from different NSAIDs was high, in a range from 46.7 %-66.2 %.In general, the candidate risk factors for ADRs were different for each NSAID. Each of the candidate risk factors were defined and studied in order to evaluate its role in the determination of ADRs from NSAIDs. "Family history of ADRs caused by NSAIDs" was found to be a significant risk factor for the four commonly used NSAIDs:meloxicam, diclofenac, nimesulide, and nabumetone. CONCLUSION: A retrospective epidemiological survey was useful in detecting the risk factors for ADRs caused by NSAIDs. The study found that different NSAIDs might have different risk factors and that there is no single risk factor universally applicable to all NSAIDs.

  20. Inhibition of Human Transthyretin Aggregation by Non-Steroidal Anti-Inflammatory Compounds: A Structural and Thermodynamic Analysis

    Directory of Open Access Journals (Sweden)

    Luis Mauricio T. R. Lima

    2013-03-01

    Full Text Available Transthyretin (TTR is a homotetrameric protein that circulates in plasma and cerebral spinal fluid (CSF whose aggregation into amyloid fibrils has been associated with at least two different amyloid diseases: senile systemic amyloidosis (SSA and familial amyloid polyneuropathy (FAP. In SSA aggregates are composed of WT-TTR, while in FAP more than 100 already-described variants have been found in deposits. Until now, TTR-related diseases have been untreatable, although a new drug called Tafamidis has been approved only in Europe to specifically treat V30M patients. Thus, new strategies are still necessary to treat FAP caused by other variants of TTR. TTR has two channels in the dimer interface that bind to the hormone thyroxin and that have been used to accommodate anti-amyloidogenic compounds. These compounds stabilize the tetramers, rendering TTR less amyloidogenic. Here, we investigated the effects of three non-steroidal anti-inflammatory compounds—sulindac (SUL, indomethacin (IND and lumiracoxib (LUM—as tetramer stabilizers and aggregation inhibitors. WT-TTR and the very aggressive TTR variant L55P were used as models. These compounds were able to stabilize TTR against high hydrostatic pressure (HHP, increasing the ΔGf by several kcal. They were also effective in inhibiting WT-TTR and L55P acid- or HHP-induced aggregation; in particular, LUM and IND were very effective, inhibiting almost 100% of the aggregation of both proteins under certain conditions. The species formed when aggregation was performed in the presence of these compounds were much less toxic to cells in culture. The crystal structures of WT-TTR bound to the three compounds were solved at high resolution, allowing the identification of the relevant protein:drug interactions. We discuss here the ligand-binding features of LUM, IND and SUL to TTR, emphasizing the critical interactions that render the protein more stable and less amyloidogenic.

  1. Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Kumar, Raj; Siril, Prem Felix; Javid, Farideh

    2016-12-01

    The non-steroidal anti-inflammatory drugs (NSAIDs) are the most widely used pharmaceuticals worldwide. Interestingly, many of them have significant anticancer properties too. However, the poor water solubility of certain NSAIDs limits their application for cancer treatment. Nanosizing of such drugs can help to improve the solubility and this may result in enhanced anticancer activities too. Moreover, over dosages and the accompanying side effects of NSAIDs can be minimized by improving their solubility and bioavailability. Successful nanoformulation of three NSAIDs: ibuprofen (IBP), ketoprufen (KP) and naproxen (NAP) using a novel evaporation assisted solvent-antisolvent interaction (EASAI) method is reported here. Three water soluble and biocompatible polymers: polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA) and hydroxypropyl methylcellulose (HPMC) were used to stabilize the drug nanoparticles. Particles having spherical morphology with average size below 30nm were thoroughly characterized using dynamic light scattering and field emission scanning electron microscopy (FESEM) imaging. The nanoformulation resulted in ten to fifteen fold improvements in the solubility and significant enhancement in the in-vitro drug release profiles of the NSAIDs. Anticancer screening of the nanoformulated NSAIDs against five different cancer cell lines such as MCF-7 (Human breast cancer cell line), (Human pancreatic cancer cell line) MIA-PA-CA-2, (Human colon cancer cell line) HT-29, (Human leukemia cell line) Jurkat and (human ovarian carcinoma cell line) A2780 was performed. All the nanoformulated samples showed improved anticancer activity against the Leukemia cancer cell line, out of which NAP-PVP showed the highest anti-cancer activity. The anti-Leukemia activity of NAP-PVP was more than twice that of doxorubicin which is a standard anticancer drug. PMID:27612834

  2. Interaction or relationship between Helicobacter pylori and non-steroidal anti-inflammatory drugs in upper gastrointestinal diseases

    Institute of Scientific and Technical Information of China (English)

    Kai-Yu Ji; Fu-Lian Hu

    2006-01-01

    According to a meta-analysis, H pylori and non-steroidal anti-inflammatory drugs (NSAID) independently and significantly increase the risk of gastroduodenal ulcer and ulcer bleeding. Their coincidence is frequent,demonstration of a possible relationship and consequent attitude is of important implications. But unfortunately,no consensus has been approved in the past years and their interactions are still controversial. H pylori and NSAID are known to share a number of pathogenic mechanisms, but there is no evidence for the significant synergic action between these two risk factors. Their relationship is independent, additive, synergistic or antagonistic without considering the influence of other factors because studies on this subject are different in almost all aspects of their methodology, including the definition of a NSAID user as well as the types,doses, duration and their indications for NSAID use,as well as their end-points, definition of dyspepsia and regimes used for eradication of H pylori. These might contribute to the conflicting results and opinions. H pylori infection in humans does not act synergistically with NSAID on ulcer healing, and there is no need to eradicate it. This notion is supported by the finding that the eradication of H pylori does not affect NSAIDinduced gastropathy treated with omeprazole and that H pylori infection induces a strong cyclooxygenase-2(COX-2) expression resulting in excessive biosynthesis of gastroprotective prostaglandin which in turn counteracts NSAID-induced gastropathy and heals the existing ulcer.Other investigators claimed that H pylori infection acts synergistically with NSAID on ulcer development, and H pylori should be eradicated, particularly at the start of long-term NSAID therapy. Eradication of H pylori prior to NSAID treatment does not appear to accelerate ulcer healing or to prevent recurrent ulcers in NSAID users.However, some recommendations can be drawn from the results of clinical trails.

  3. Small Mismatches in Fatty Acyl Tail Lengths Can Effect Non Steroidal Anti-Inflammatory Drug Induced Membrane Fusion.

    Science.gov (United States)

    Majumdar, Anupa; Sarkar, Munna

    2016-06-01

    Biological membranes are made up of a variety of lipids with diverse physicochemical properties. The lipid composition modulates different lipidic parameters, such as hydration, dynamics, lipid packing, curvature strain, etc. Changes in these parameters affect various membrane-mediated processes, such as membrane fusion which is an integral step in many biological processes. Packing defects, which originate either from mismatch in the headgroup region or in the hydrophobic acyl tail region, play a major role in modulating membrane dynamics. In this study, we demonstrate how even a small mismatch in the fatty acyl chain length, achieved by incorporation of low concentrations (up to 30 mol %) of dipalmitoylphosphatidylcholine (DPPC) into dimyristoylphosphatidylcholine (DMPC) small unilamellar vesicles (SUVs), alters several lipidic parameters like packing, dynamics, and headgroup hydration. This in turn affects non steroidal anti-inflammatory drug (NSAID) induced membrane fusion. Dynamic light scattering, differential scanning calorimetry, second-derivative absorption spectrophotometry, and steady-state and time-resolved fluorescence have been used to elucidate the effect of small mismatch in the tails in DMPC/DPPC mixed vesicles and how it modulates membrane fusion induced by the oxicam NSAIDs, meloxicam (Mx), piroxicam (Px), and tenoxicam (Tx). Fusion kinetics was monitored using fluorescence based fusion assays. At low DPPC concentration of 10 mol %, additional fluidization promotes lipid mixing to some extent for Mx, but at higher mol % of DPPC, subsequent increase in rigidity of membrane interior along with increase in headgroup hydration, synergistically inhibits fusion to various extents for the three different drugs, Mx, Px, and Tx. PMID:27153337

  4. Bleeding gastroduodenal ulcers in patients without Helicobacter pylori infection and without exposure to non-steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Smolović Brigita

    2014-01-01

    Full Text Available Background/Aim. A high risk of bleeding in Helicobacter pylori (H.pylori-negative, non-steroidal anti-inflammatory drugs (NSAID-negative ulcers highlights the clinical importance of analysis of the changing trends of peptic ulcer disease. The aim of the study was to investigate the risk factors for ulcer bleeding in patients with non-H. pylori infection, and with no NSAIDs use. Methods. A prospective study included patients with endoscopically diagnosed ulcer disease. The patients were without H. pylori infection (verified by pathohistology and serology and without exposure to NSAIDs and proton pump inhibitors (PPI within 4 weeks before endoscopy. After endoscopy the patients were divided into 2 groups: the study group of 48 patients with bleeding ulcer and the control group of 47 patients with ulcer, but with no bleeding. Prior to endoscopy they had completed a questionnaire about demographics, risk factors and habits. The platelet function, von Willebrand factor (vWF and blood groups were determined. Histopathological analysis of biopsy samples were performed with a modified Sydney system. The influence of bile reflux was analyzed by Bile reflux index (BRI. Results. Age, gender, tobacco and alcohol use did not affect the bleeding rate. The risk of bleeding did not depend on concomitant diseases (p = 0.509 and exposure to stress (p = 0.944. Aspirin was used by 16/48 (33.3% patients with bleeding ulcer, as opposed to 7/47 (14.9% patients who did not bleed (p = 0.036. Abnormal platelet function had 12/48 (25.0% patients who bled, as opposed to 2/47 (4.3% patients who did not bleed (p = 0.004. Patients with BRI < 14 bled in 79.2%, and did not bleed in 57.4% of the cases (p = 0.023. There was no statistical difference between groups in regards to blood groups and range of vWF. Antrum atrophy was found in 14/48 (29.2% patients with bleeding ulcer and in only 5/47 (10.6% patients who had ulcer without bleeding (p = 0.024. Conclusion. Abnormal

  5. Post-steroid management of chronic vulvar itching with a topical formula containing natural anti-itching and anti-inflammatory actives

    Science.gov (United States)

    Di Pierro, Francesco; Di Maio, Eleonora; Di Paola, Gaetana; Felice, Raffaele; Murina, Filippo

    2013-01-01

    Aim To determine whether use of a topical, nonsteroidal, anti-inflammatory, and anti-itching formula was able to preserve the absence of symptoms, mainly itching and burning, induced by an earlier and relatively short treatment with topical steroids in women diagnosed with vulvar dermatitis or lichen simplex. Methods Ninety-six subjects (36 with contact dermatitis, 29 with allergic dermatitis, 31 with lichen simplex) were enrolled in the study. All participants were first treated with topical mometasone furoate (MF) 0.1%. When the symptoms disappeared, they were treated either with Zantogin®, a multicomponent topical formula containing anti-inflammatory and anti-itching natural actives, or a control cream for 60 days. Results The study demonstrated that, in about 85% of the participants treated with Zantogin®, symptoms disappeared completely, and only 15% had to resort to MF as needed, with an average use of about three applications per subject (in total). In the placebo group, approximately 90% of participants had to resort to MF as needed, with an average use per person of more than 16 applications in 60 days. Conclusion Our study demonstrates that, following use of a topical steroid, symptoms such as burning and itching can be validly controlled with subsequent and longer therapy with a herbal topical formula, Zantogin®, which is able to properly counteract itching and inflammation, prevent symptom relapse, and avoid the typical side effects associated with prolonged use of topical steroids. PMID:23637564

  6. Cardiovascular risk with non-steroidal anti-inflammatory drugs: systematic review of population-based controlled observational studies.

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    Patricia McGettigan

    2011-09-01

    Full Text Available BACKGROUND: Randomised trials have highlighted the cardiovascular risks of non-steroidal anti-inflammatory drugs (NSAIDs in high doses and sometimes atypical settings. Here, we provide estimates of the comparative risks with individual NSAIDs at typical doses in community settings. METHODS AND FINDINGS: We performed a systematic review of community-based controlled observational studies. We conducted comprehensive literature searches, extracted adjusted relative risk (RR estimates, and pooled the estimates for major cardiovascular events associated with use of individual NSAIDs, in different doses, and in populations with low and high background risks of cardiovascular events. We also compared individual drugs in pair-wise (within study analyses, generating ratios of RRs (RRRs. Thirty case-control studies included 184,946 cardiovascular events, and 21 cohort studies described outcomes in >2.7 million exposed individuals. Of the extensively studied drugs (ten or more studies, the highest overall risks were seen with rofecoxib, 1.45 (95% CI 1.33, 1.59, and diclofenac, 1.40 (1.27, 1.55, and the lowest with ibuprofen, 1.18 (1.11, 1.25, and naproxen, 1.09 (1.02, 1.16. In a sub-set of studies, risk was elevated with low doses of rofecoxib, 1.37 (1.20, 1.57, celecoxib, 1.26 (1.09, 1.47, and diclofenac, 1.22 (1.12, 1.33, and rose in each case with higher doses. Ibuprofen risk was seen only with higher doses. Naproxen was risk-neutral at all doses. Of the less studied drugs etoricoxib, 2.05 (1.45, 2.88, etodolac, 1.55 (1.28, 1.87, and indomethacin, 1.30 (1.19, 1.41, had the highest risks. In pair-wise comparisons, etoricoxib had a higher RR than ibuprofen, RRR = 1.68 (99% CI 1.14, 2.49, and naproxen, RRR = 1.75 (1.16, 2.64; etodolac was not significantly different from naproxen and ibuprofen. Naproxen had a significantly lower risk than ibuprofen, RRR = 0.92 (0.87, 0.99. RR estimates were constant with different background risks for

  7. INTERACTION BETWEEN ANTI-HYPERTENSIVE AND NON-STEROIDAL ANTI INFLAMMATORY DRUGS: IMPLICATIONS IN MANAGEMENT OF OSTEOARTHRITIS AND OPINION ON A COMPROMISE THERAPY

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    Mr. Adeolu O. Ajala

    2010-01-01

    Full Text Available The premise for this article is that a significant proportion of patients presenting in the clinic with osteoarthritis have hypertension as co-morbidity. A common drug of choice in managing symptoms of osteoarthritis including those affecting the knee joint is the Non-Steroidal Anti-Inflammatory Drugs (NSAIDS groups. It has been reported however that NSAIDs diminish the effects of anti-hypertensive drugs and may lead to an ineffective hypertension therapy. In order to avoid complications in the health of the patient with concomitant hypertension and osteoarthritis and who are on both antihypertensive and NSAIDs, it becomes imperative to consider using non-pharmacologic approaches such as physiotherapy in managing the symptoms of osteoarthritis in this group of patients and thereby maximizing the effects of their antihypertensive therapy. This is more so that information exists on efficacy of physiotherapy in form of therapeutic exercises and electrotherapeutic modalities in management of clinical features of osteoarthritis.

  8. Phenylacetic acids and the structurally related non-steroidal anti-inflammatory drug diclofenac bind to specific gamma-hydroxybutyric acid sites in rat brain

    DEFF Research Database (Denmark)

    Wellendorph, Petrine; Høg, Signe; Skonberg, Christian;

    2009-01-01

    Gamma-Hydroxybutyric acid (GHB) is a proposed neurotransmitter or neuromodulator with a yet unresolved mechanism of action. GHB binds to both specific high-affinity GHB binding sites and to gamma-aminobutyric acid subtype B (GABA(B)) receptors in the brain. To separate specific GHB effects from...... GABA(B) receptor effects, it is imperative to develop GHB selective and potent compounds. We generated the compound, 4-(biphen-4-yl)-4-hydroxybutyric acid, which is the 4-hydroxyl analogue of the non-steroidal anti-inflammatory drug (NSAID) fenbufen (referred to as gamma-hydroxyfenbufen). When measured...... in a rat brain homogenate [(3)H]NCS-382 binding assay, gamma-hydroxyfenbufen inhibited [(3)H]NCS-382 binding with a 10-fold higher affinity than GHB (K(i) 0.44 microM), thus establishing it as a novel lead structure. The active metabolite of fenbufen, 4-biphenylacetic acid inhibited [(3)H]NCS-382 binding...

  9. The effect of non-steroidal anti-inflammatory drugs on the metabolism of /sup 14/C-arachidonic acid by human gingival tissue in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Elattar, T.M.; Lin, H.S.; Tira, D.E.

    1983-09-01

    We investigated the effect of non-steroidal anti-inflammatory drugs on prostaglandins (PGs) and 12-hydroxyeicosatetraenoic acid (12-HETE) formation by inflamed human gingival tissues. Gingival tissue homogenates were incubated with /sup 14/C-arachidonic acid in the presence of indomethacin, piroxicam, or ibuprofen, and the organic solvent extracts were chromatographed on silica gel plates with standards for radiometric assay. There was a significant negative trend between the doses (10(-7)-10(-3) M) of each of indomethacin, piroxicam, and ibuprofen, and the amounts of PGF2 alpha, PGE2, PGD2, and 15-keto-PGE2 produced. All three drugs have a significant inhibitory effect on PGs and 12-HETE production at 10(-3) M when compared with the control. The rank order effectiveness of the drugs, at 10(-3) M, on PG inhibition was indomethacin greater than piroxicam greater than ibuprofen, and on 12-HETE inhibition was indomethacin greater than ibuprofen greater than piroxicam.

  10. Simultaneous determination of non-steroidal anti-inflammatory drugs in pharmaceutical formulations and human serum by reversed phase high performance liquid chromatography

    Directory of Open Access Journals (Sweden)

    Muhammad Nawaz

    2012-01-01

    Full Text Available A rapid and sensitive method using high performance liquid chromatography has been developed and validated for the simultaneous determination of non-steroidal anti-inflammatory drugs (NSAIDs in pharmaceutical formulations and human serum. Six NSAIDs including: naproxen sodium, diclofenac sodium, meloxicam, flurbiprofen, tiaprofenic and mefenamic acid were analyzed simultaneously in presence of ibuprofen as internal standard on Mediterranea C18 (5 µm, 250 x 0.46 mm column. Mobile phase comprised of methanol: acetonitrile: H2O (60:20:20, v/v; pH 3.35 and pumped at a flow rate of 1 mL min-1 using 265 nm UV detection. The method was linear over a concentration range of 0.25-50 µg mL-1 (r² = 0.9999.

  11. Analysis of effect of non-steroidal anti-inflammatory drugs on teeth and oral tissues during orthodontic treatment. Report based on literature review.

    Science.gov (United States)

    Krasny, Marta; Zadurska, Małgorzata; Cessak, Grzegorz; Fiedor, Piotr

    2013-01-01

    In view of high availability and diversity of non-steroidal anti-inflammatory drugs (NSAIDs) on Polish market it is important for orthodontists to be aware of NSAID effect on the range of orthodontic tooth movement as well as the risk of root resorption in the moved teeth and other adverse effects, which might occur within oral cavity. The disadvantages of NSAID non-selective inhibition of COX include common oral inflammatory conditions, gingival bleeding, and disturbances of salivary secretion. Both, the selective and non-selective COX inhibitors, meloxicam excluded, used to alleviate the pain of orthodontic tooth movement, impede the movement of teeth. Paracetamol, explicitly indicated by most authors as the safest NSAID, seems to be the drug of choice in view of no influence on the range of tooth movement, the risk of root resorption or other adverse effects within oral cavity.

  12. Steroidal and phenolic compounds from Sidastrum paniculatum (L. Fryxell and evaluation of cytotoxic and anti-inflammatory activities

    Directory of Open Access Journals (Sweden)

    José Marcílio Sobral Cavalcante

    2010-01-01

    Full Text Available Sidastrum paniculatum (L. Fryxell belongs to the family Malvaceae and is popularly known as "malva roxa" or "malvavisco". The phytochemical study of the hexane, CHCl3 and EtOAc phases from the crude ethanol extract of S. paniculatum led to the isolation of six compounds: a mixture of β-sitosterol and stigmasterol, 4-methoxy-3-hydroxybenzoic acid, 4-methoxy-3-hydroxybenzaldehyde, N-trans-feruloyltyramine and kaempferol-3-O-β-D-(6''-E-p -coumaroyl glucoside. The structural identification of the compounds was made on the basis of spectroscopic methods such as IR, ¹H and 13C NMR with the aid of including two-dimensional techniques, besides comparison with literature data. The β-sitosterol and stigmasterol mixture showed a significant anti-inflammatory activity.

  13. Steroidal and phenolic compounds from Sidastrum paniculatum (L.) Fryxell and evaluation of cytotoxic and anti-inflammatory activities

    Energy Technology Data Exchange (ETDEWEB)

    Cavalcante, Jose Marcilio Sobral; Nogueira, Tiago Bezerra de Sa de Souza; Tomaz, Anna Claudia de Andrade; Antas e Silva, Davi; Agra, Maria de Fatima; Souza, Maria de Fatima Vanderlei de [Universidade Federal da Paraiba (UFPB), Joao Pessoa, PB (Brazil). Lab. de Tecnologia Farmaceutica Prof. Delby Fernandes de Medeiros; Carvalho, Paulo Roberto Cavalcanti; Ramos, Silvia Rafaelli; Nascimento, Silene Carneiro do; Goncalves-Silva, Teresinha [Universidade Federal de Pernambuco (UFPE), Recife, PE (Brazil). Dept. de Antibioticos

    2010-07-01

    Sidastrum paniculatum (L.) Fryxell belongs to the family Malvaceae and is popularly known as 'malva roxa' or 'malvavisco'. The phytochemical study of the hexane, CHCl{sub 3} and EtOAc phases from the crude ethanol extract of S. paniculatum led to the isolation of six compounds: a mixture of {beta}-sitosterol and stigmasterol, 4-methoxy-3-hydroxybenzoic acid, 4-methoxy-3-hydroxybenzaldehyde, N-trans-feruloyltyramine and kaempferol-3-O-{beta}{beta}-D-(6''-E-p-coumaroyl) glucoside. The structural identification of the compounds was made on the basis of spectroscopic methods such as IR, {sup 1}H and {sup 13}C NMR with the aid of including two-dimensional techniques, besides comparison with literature data. The {beta}-sitosterol and stigmasterol mixture showed a significant anti-inflammatory activity. (author)

  14. Effects of paracetamol, non-steroidal anti-inflammatory drugs, acetylsalicylic acid, and opioids on bone mineral density and risk of fracture: results of the Danish Osteoporosis Prevention Study (DOPS)

    DEFF Research Database (Denmark)

    Vestergaard, Peter; Hermann, P; Jensen, J-E B;

    2012-01-01

    Pain medication has been associated with fractures. We found higher weight in paracetamol and non-steroidal anti-inflammatory drugs (NSAID) users and lower vitamin D levels in opioid and acetylsalicylic acid users. None of the pain medications influenced bone mineral density or loss. NSAID were...

  15. Determination of the total concentration of highly protein-bound drugs in plasma by on-line dialysis and column liquid chromatography : application to non-steroidal anti-inflammatory drugs

    NARCIS (Netherlands)

    Herráez-Hernández, R; van de Merbel, N C; Brinkman, U A

    1995-01-01

    The potential of on-line dialysis as a sample preparation procedure for compounds highly bound to plasma proteins is evaluated, using non-steroidal anti-inflammatory drugs as model compounds and column liquid chromatography as the separation technique. Different strategies to reduce the degree of dr

  16. Proton-pump inhibitors are associated with a reduced risk for bleeding and perforated gastroduodenal ulcers attributable to non-steroidal anti-inflammatory drugs : a nested case-control study

    NARCIS (Netherlands)

    Vonkeman, Harald E; Fernandes, Robert W; van der Palen, Job; van Roon, Eric N; van de Laar, Mart A F J

    2007-01-01

    Treatment with non-steroidal anti-inflammatory drugs (NSAIDs) is hampered by gastrointestinal ulcer complications, such as ulcer bleeding and perforation. The efficacy of proton-pump inhibitors in the primary prevention of ulcer complications arising from the use of NSAIDs remains unproven. Selectiv

  17. Apparent tolerance of turkey vultures (Cathartes aura) to the non-steroidal anti-inflammatory drug diclofenac

    Science.gov (United States)

    Rattner, B.A.; Whitehead, M.A.; Gasper, G.; Meteyer, C.U.; Link, W.A.; Taggart, M.A.; Meharg, A.A.; Pattee, O.H.; Pain, D.J.

    2008-01-01

    The nonsteroidal anti-inflammatory drug diclofenac is extremely toxic to Old World Gyps vultures (median lethal dose 0.1?0.2 mg/kg), evoking visceral gout, renal necrosis, and mortality within a few days of exposure. Unintentional secondary poisoning of vultures that fed upon carcasses of diclofenac-treated livestock decimated populations in the Indian subcontinent. Because of the widespread use of diclofenac and other cyclooxygenase-2 inhibiting drugs, a toxicological study was undertaken in turkey vultures (Cathartes aura) as an initial step in examining sensitivity of New World scavenging birds. Two trials were conducted entailing oral gavage of diclofenac at doses ranging from 0.08 to 25 mg/kg body weight. Birds were observed for 7 d, blood samples were collected for plasma chemistry (predose and 12, 24, and 48 h and 7 d postdose), and select individuals were necropsied. Diclofenac failed to evoke overt signs of toxicity, visceral gout, renal necrosis, or elevate plasma uric acid at concentrations greater than 100 times the estimated median lethal dose reported for Gyps vultures. For turkey vultures receiving 8 or 25 mg/kg, the plasma half-life of diclofenac was estimated to be 6 h, and it was apparently cleared after several days as no residues were detectable in liver or kidney at necropsy. Differential sensitivity among avian species is a hallmark of cyclooxygenase-2 inhibitors, and despite the tolerance of turkey vultures to diclofenac, additional studies in related scavenging species seem warranted.

  18. Studies on the protective effect of ebrotidine on experimental ulcers induced by non-steroidal anti-inflammatory drugs in healthy volunteers.

    Science.gov (United States)

    Puscas, I; Puscas, C; Coltau, M; Torres, J; Márquez, M; Herrero, E; Fillat, O; Ortiz, J A

    1997-04-01

    Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]- 4-thiazolyl]methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamid e, CAS 100981-43-9, FI-3542) is a new H2-receptor antagonist providing a new therapy for the prevention and healing of non-steroidal anti-inflammatory drugs-induced gastroduodenal lesions. Carbonic anhydrase is a zinc enzyme, and its isozyme (carbonic anhydrase II) in parietal cells plays a central role in HCl secretion. The effects of ebrotidine on carbonic anhydrase in human subjects are reported. Eighteen healthy volunteers were distributed in 3 equal subgroups and treated for 10 days as follows: ebrotidine 800 mg/d p.o. (Group A); indometacin 4 mg/kg/d p.o. in 3 divided doses (Group B); ebrotidine 800 mg/d p.o. plus indometacin 4 mg/kg/d p.o. (Group C). Assessment of the enzymatic activity of carbonic anhydrase was based on the colorimetric method of changing pH with the stopped-flow technique. In group A, ebrotidine reduced total gastric mucosal carbonic anhydrase activity by 62%; in group B, indometacin increased carbonic anhydrase activity in gastric mucosa by 138%; in group C, the combined treatment with ebrotidine plus indometacin decreased gastric mucosal carbonic anhydrase activity by 38%. The present study shows that, unlike ranitidine, ebrotidine, a competitive H2-receptor antagonist, is also a non-competitive inhibitor of carbonic anhydrase I and II. By antagonizing the activating effects of indometacin on gastric mucosal carbonic anhydrase, ebrotidine prevents mucosal lesions caused by anti-inflammatory drugs.

  19. Analysis of the use and adverse effects of non-steroidal anti-inflammatory drugs: A pilot study

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    Perić Aneta

    2006-01-01

    Full Text Available Background/Aim. The use and adverse effects of nonsteroidal anti-inflammatory drugs (NSAIDs in outpatients with rheumatic diseases has not yet been studied enough. The aim of this study was to evaluate the data about the efficacy and safety of NSAIDs obtained from the questionnaires submitted to the outpatients receiving these drugs. Methods. The patients who had been prescribed any of NSAIDs within the period from June to September, 2004 were included in the study. The answers obtained from the questionnaires were statistically analyzed by means of χ2-test. Results. At the time of the study, 150 patients had been prescribed ibuprofen or some other NSAID. Out of the total number of dispensed questionnaires (n = 150, only 45 (30% were shown to be correctly filled-in. Their analysis showed that 64.4% of the patients had suffered from rheumatic diseases for more than five years, and had regularly used NSAIDs. The average age of these patients was about 70 years, and the number of females was double as high as that of the males. The most frequently used NSAIDs were diclofenac and ibuprofen (46.14%, and 23.24%, respectively. According to the answers given by the patients, the most often adverse reactions were gastric complaints such as nausea (11.1%, and stomach pain (8.9%. Due to this, the majority of the patients (64.4% used some of the antiulcer drugs, most often ranitidine (31.1%. Conclusion. The results of this pilot study revealed that among the outpatients suffering from rheumatic diseases, the number of females was double as high as the number of males, that these patients were of the mean age of 70 years, and that their diseases lasted longer than five years. Gastric complains such as nausea and gastric pain of mild intensity were the most often adverse effects of NSAIDs reported by our patients. It could be the consequence of the predominant use of diclofenac and ibuprofen, NSAIDs with mild to moderate ulcerogenic potential, as well as the

  20. Partitioning of anti-inflammatory steroid drugs into phosphatidylcholine and phosphatidylcholine-cholesterol small unilamellar vesicles as studied by second-derivative spectrophotometry.

    Science.gov (United States)

    Takegami, Shigehiko; Kitamura, Keisuke; Funakoshi, Takako; Kitade, Tatsuya

    2008-05-01

    The partition coefficients (Kps) of six anti-inflammatory steroid drugs, dexamethasone (DMS), betamethasone (BMS), triamcinolone acetonide (TCLA), fluocinolone acetonide (FCLA), betamethasone 17,21-dipropionate (BMSDP), and clobetasole propionate (CBSP), for phosphatidylcholine (PC), and PC-cholesterol small unilamellar vesicles (SUVs) were determined by a second-derivative spectrophotometric method. The Kp values were obtained with a relative standard deviation of below 10% and the following order was observed: BMS< or =DMSsteroid drugs in dermatological treatments depends to some extent on the Kp values of the drug, that is, the affinity of steroid drugs for PC bilayers influences their clinical potency, since potency is related to transdermal absorption.

  1. Cause for concern in the use of non-steroidal anti-inflammatory medications in the community -a population-based study

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    Adams Robert J

    2011-07-01

    Full Text Available Abstract Background Non-steroidal anti-inflammatory (NSAID medications are a common cause of reported adverse drug side-effects. This study describes the prevalence of non-steroidal anti-inflammatory (NSAID use (other than low-dose aspirin and the presence of co-existing relative contraindications to NSAID use and chronic conditions in a representative population sample. Methods Data were analysed from 3,206 adults attending first follow-up of the North West Adelaide Health Study (NWAHS in 2004 - 2006, a longitudinal representative population study. Medications were brought into study clinic visits by participants. Clinical assessment included measured blood pressure, kidney function, serum cholesterol, blood glucose. Questionnaires assessed demographics, lifestyle risk factors, physician-diagnosed chronic conditions. Data were weighted to census measures by region, age group, gender, and probability of selection in the household, to provide population representative estimates. Pearson's Chi-square tests determined significant differences in proportions. Multiple logistic regression was used to examine associations of socio-demographic characteristics with use of NSAIDs. Results Of 3,175 participants, 357 (11.2%, and 16% of those aged > 55 years, reported using either non-specific NSAIDs or COX-2 inhibitors, other than low-dose aspirin. Among people using NSAIDs, 60.8% had hypertension, 30.8% had Stage 3 or higher chronic kidney disease, 17.2% had a history of cardiovascular disease (CVD and 20.7% had a > 15% 10-year CVD risk. The prevalence of NSAID use among people with hypertension was 16%, with kidney disease 15.9%, and a history of CVD 20.0%. Among people taking diuretics, 24.1% were also taking NSAIDs, and of those taking medications for gastro-esophageal reflux, 24.7% were on NSAIDs. Prescription-only COX-2 inhibitors, but not other NSAIDs, were used more by people > 75 years than by 35-54 year olds (OR 3.7, 95% CI 2.0, 6.7, and also were

  2. A STUDY OF PRESCRIBING PATTERN OF NON STEROIDAL ANTI INFLAMMATORY DRUGS IN ORTHOPEDIC OUT PATIENT DEPARTMENT AT A TERTIARY CARE HOSPITAL

    Directory of Open Access Journals (Sweden)

    Asha Latha

    2015-01-01

    Full Text Available AIM: To determine the pattern of NON STEROIDAL ANTI INFLAMMATORY DRUGS prescribing for arthritic and non - arthritic conditions in orthopedic outpatient department . METHODOLOGY: 100 prescription duplicate collected and analyzed prospectively for the pattern of NSAID prescription for arthritic and non - arthritic conditions; the drug formulation , route , frequency, duration of adm issio n and concomitant medications results. NSAID were prescribed for non - traumatic musculo skeletal 35% pain, 25% post traumatic pain, 20% osteoarthritis, 10% post - operative pain, 3% ankylosing spondylitis, 6% degenerativ e disease of spine, 1% neuralgia. The NSAIDs commonly prescribed were Aceclofenac 45%, Etodolac 20%, Diclofenac 24%, and Ibuprofen 11%. Fixed dose combination of NSAIDs with adjuvante was prescribed in. The adjuvants, included are paracetamol 55.6%, serrat opeptidase 32.8%, chlorzoxazone 9.1%, Thiocolchichoside 2.5%. oral formulations of NSAIDs were prescribed in all patients, supplemented by Topical formulations as gel/cream in 15% of subjects. The dosing frequency was BID (65%, OD (25%, TID (2%, SOS (8% . Duration of administration ranged from 5 - 15 days . other classes of drugs used concomitantly were proton pump inhibitors , calcium supplements, Multivitamins, Anti microbials, Immuno suppressants, and Glucosamine. CONCLUSION: NSAIDs were prescribed empiric all y for various arthritic and Non - arthritic conditions, frequently as fixed dose combinations [FDC]s with various adjuvants as per the standard guide lines. However patient information was inadequate in most of the prescriptions. Proper patient Assessment deemed necessary for individualizing NSAIDs.

  3. Tolerance effects of non-steroidal anti-inflammatory drugs microinjected into central amygdala, periaqueductal grey, and nucleus raphe Possible cellular mechanism

    Institute of Scientific and Technical Information of China (English)

    Merab G. Tsagareli; Nana Tsiklauri; Ivliane Nozadze; Gulnaz Gurtskaia

    2012-01-01

    Pain is a sensation related to potential or actual damage in some tissue of the body. The mainstay of medical pain therapy remains drugs that have been around for decades, like non-steroidal anti-inflammatory drugs (NSAIDs), or opiates. However, adverse effects of opiates, particularly tolerance, limit their clinical use. Several lines of investigations have shown that systemic (intraperitoneal) administration of NSAIDs induces antinociception with some effects of tolerance. In this review, we report that repeated microinjection of NSAIDs analgin, clodifen, ketorolac and xefocam into the central nucleus of amygdala, the midbrain periaqueductal grey matter and nucleus raphe magnus in the following 4 days result in progressively less antinociception compared to the saline control testing in the tail-flick reflex and hot plate latency tests. Hence, tolerance develops to these drugs and cross-tolerance to morphine in male rats. These findings strongly support the suggestion of endogenous opioid involvement in NSAIDs antinociception and tolerance in the descending pain-control system. Moreover, the periaqueductal grey-rostral ventro-medial part of medulla circuit should be viewed as a pain-modulation system. These data are important for human medicine. In particular, cross-tolerance between non-opioid and opioid analgesics should be important in the clinical setting.

  4. Biological evaluation of bismuth non-steroidal anti-inflammatory drugs (BiNSAIDs): stability, toxicity and uptake in HCT-8 colon cancer cells.

    Science.gov (United States)

    Hawksworth, Emma L; Andrews, Philip C; Lie, Wilford; Lai, Barry; Dillon, Carolyn T

    2014-06-01

    Recent studies showed that the metal-coordinated non-steroidal anti-inflammatory drug (NSAID), copper indomethacin, reduced aberrant crypt formation in the rodent colon cancer model, while also exhibiting gastrointestinal sparing properties. In the present study, the stability and biological activity of three BiNSAIDs of the general formula [Bi(L)3]n, where L=diflunisal (difl), mefenamate (mef) or tolfenamate (tolf) were examined. NMR spectroscopy of high concentrations of BiNSAIDs (24h in cell medium, 37°C) indicated that their structural stability and interactions with cell medium components were NSAID specific. Assessment of cell viability using the [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium]bromide (MTT) assay showed that the toxicity ranking of the BiNSAIDs paralleled those of the respective free NSAIDs: diflHXRF imaging showed that the intracellular fate of bismuth was independent of the specific BiNSAID treatment whereby all BiNSAID-treated cells showed bismuth accumulation in the cytoplasm within 24-h exposure. The size and location of the hot spots (0.3-5.8μm(2)), were consistent with cellular organelles such as lysosomes. PMID:24650572

  5. Use of non-steroidal anti-inflammatory drugs and prostate cancer risk: a population-based nested case-control study.

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    Salaheddin M Mahmud

    Full Text Available BACKGROUND: Despite strong laboratory evidence that non-steroidal anti-inflammatory drugs (NSAIDs could prevent prostate cancer, epidemiological studies have so far reported conflicting results. Most studies were limited by lack of information on dosage and duration of use of the different classes of NSAIDs. METHODS: We conducted a nested case-control study using data from Saskatchewan Prescription Drug Plan (SPDP and Cancer Registry to examine the effects of dose and duration of use of five classes of NSAIDs on prostate cancer risk. Cases (N = 9,007 were men aged ≥40 years diagnosed with prostatic carcinoma between 1985 and 2000, and were matched to four controls on age and duration of SPDP membership. Detailed histories of exposure to prescription NSAIDs and other drugs were obtained from the SPDP. RESULTS: Any use of propionates (e.g., ibuprofen, naproxen was associated with a modest reduction in prostate cancer risk (Odds ratio = 0.90; 95%CI 0.84-0.95, whereas use of other NSAIDs was not. In particular, we did not observe the hypothesized inverse association with aspirin use (1.01; 0.95-1.07. There was no clear evidence of dose-response or duration-response relationships for any of the examined NSAID classes. CONCLUSIONS: Our findings suggest modest benefits of at least some NSAIDs in reducing prostate cancer risk.

  6. Enantioselective analysis of non-steroidal anti-inflammatory drugs in freshwater fish based on microextraction with a supramolecular liquid and chiral liquid chromatography-tandem mass spectrometry.

    Science.gov (United States)

    Caballo, Carmen; Sicilia, Maria Dolores; Rubio, Soledad

    2015-06-01

    Toxicity of pharmaceuticals to aquatic biota is still largely unknown, and no research on the stereoselective toxicity of chiral drugs to these organisms has been undertaken to date. Because of the lack of analytical methods available for this purpose, this manuscript deals, for the first time, with the enantioselective analysis of the non-steroidal anti-inflammatory drugs (NSAIDs) ibuprofen, naproxen and ketoprofen in freshwater fish. The method was based on the microextraction of NSAIDs from fish muscle with a supramolecular liquid made up of inverted hexagonal aggregates of decanoic acid, their enantiomeric separation by liquid chromatography onto a (R)-1-naphthylglycine and 3,5-dinitrobenzoic acid stationary phase and quantification by tandem mass spectrometry. Limits of quantitation (LOQs) for NSAID enantiomers were in the range 1.7-3.3 ng g(-1). Absolute recoveries were from 97 to 104 %, which indicated the high extraction efficiency of the supramolecular solvent. Extraction equilibrium conditions were reached after 10 min which permitted fast sample treatment. Relative standard deviations for enantiomers in fish muscle were always below 6 %. Isotopically labelled internal standards were used to compensate for matrix interferences. The method in-house validation was carried out with the Oncorhynchus mykiss species, and it was applied to the determination of NSAID enantiomers in different fortified freshwater fish species (Alburnus alburnus, Lepomis gibbosus, Micropterus salmoides, O. mykiss and Cyprinus carpio). PMID:25869485

  7. Structural Mechanism of the Interaction of Alzheimer Disease Aβ Fibrils with the Non-steroidal Anti-inflammatory Drug (NSAID) Sulindac Sulfide.

    Science.gov (United States)

    Prade, Elke; Bittner, Heiko J; Sarkar, Riddhiman; Lopez Del Amo, Juan Miguel; Althoff-Ospelt, Gerhard; Multhaup, Gerd; Hildebrand, Peter W; Reif, Bernd

    2015-11-27

    Alzheimer disease is the most severe neurodegenerative disease worldwide. In the past years, a plethora of small molecules interfering with amyloid-β (Aβ) aggregation has been reported. However, their mode of interaction with amyloid fibers is not understood. Non-steroidal anti-inflammatory drugs (NSAIDs) are known γ-secretase modulators; they influence Aβ populations. It has been suggested that NSAIDs are pleiotrophic and can interact with more than one pathomechanism. Here we present a magic angle spinning solid-state NMR study demonstrating that the NSAID sulindac sulfide interacts specifically with Alzheimer disease Aβ fibrils. We find that sulindac sulfide does not induce drastic architectural changes in the fibrillar structure but intercalates between the two β-strands of the amyloid fibril and binds to hydrophobic cavities, which are found consistently in all analyzed structures. The characteristic Asp(23)-Lys(28) salt bridge is not affected upon interacting with sulindac sulfide. The primary binding site is located in the vicinity of residue Gly(33), a residue involved in Met(35) oxidation. The results presented here will assist the search for pharmacologically active molecules that can potentially be employed as lead structures to guide the design of small molecules for the treatment of Alzheimer disease.

  8. Click chemistry-based synthesis of water-dispersible hydrophobic magnetic nanoparticles for use in solid phase extraction of non-steroidal anti-inflammatory drugs

    International Nuclear Information System (INIS)

    Magnetic nanoparticles (MNPs), prepared via thiol-ene click chemistry and containing both diol and octadecyl groups, are shown to possess both hydrophobic and hydrophilic functionalities. They display excellent dispersibility in water and also are capable of extracting non-steroidal anti-inflammatory drugs (NSAIDs) from water samples. The MNPs can be magnetically separated, and the NSAIDs eluted with acetonitrile-water (9:1, v:v) and submitted to high performance liquid chromatographic analysis. Extraction variables, such as the kind of ion-pairing reagents, amount of MNPs, pH of sample solution, extraction and desorption time, volume of desorption solvent and salt addition, were optimized. Under optimum conditions, the method has a wide analytical range (from 5 to 800 ng∙mL-1), good reproducibility with intra-day and inter-day relative standard deviations of <19.2 % (for n = 6), and low detection limits of 0.32 to 1.44 ng∙mL-1 for water samples. The results demonstrate that the material possesses good water compatibility, thus warranting ease of operation and good reproducibility. (author)

  9. Ecotoxicological potential of non-steroidal anti-inflammatory drugs (NSAIDs) in marine organisms: Bioavailability, biomarkers and natural occurrence in Mytilus galloprovincialis.

    Science.gov (United States)

    Mezzelani, M; Gorbi, S; Da Ros, Z; Fattorini, D; d'Errico, G; Milan, M; Bargelloni, L; Regoli, F

    2016-10-01

    Pharmaceuticals represent a major environmental concern since the knowledge on their occurrence, distribution and ecotoxicological potential is still limited particularly in coastal areas. In this study, bioaccumulation and cellular effects of various non steroidal anti-inflammatory drugs (NSAIDs) were investigated in mussels Mytilus galloprovincialis to reveal whether common molecules belonging to the same therapeutic class might cause different effects on non target organisms. Organisms exposed to environmental concentrations of acetaminophen (AMP), diclofenac (DIC), ibuprofen (IBU), ketoprofen (KET) and nimesulide (NIM) revealed a significant accumulation of DIC, IBU and NIM, while AMP and KET were always below detection limit. Nonetheless, for all tested NSAIDs, measurement of a large panel of ecotoxicological biomarkers highlighted impairment of immunological parameters, onset of genotoxicity and modulation of lipid metabolism, oxidative and neurotoxic effects. Laboratory results were integrated with a field study which provided the first evidence on the occurrence of DIC, IBU and NIM in tissues of wild mussels sampled during summer months from an unpolluted, touristic area of Central Adriatic Sea. Overall results demonstrated M. galloprovincialis as a good sentinel species for monitoring presence and ecotoxicological hazard of pharmaceuticals in the Mediterranean.

  10. Synthesis, crystal structure and spectroscopy of bioactive Cd(II) polymeric complex of the non-steroidal anti-inflammatory drug diclofenac sodium: Antiproliferative and biological activity

    Science.gov (United States)

    Tabrizi, Leila; Chiniforoshan, Hossein; McArdle, Patrick

    2015-02-01

    The interaction of Cd(II) with the non-steroidal anti-inflammatory drug diclofenac sodium (Dic) leads to the formation of the complex [Cd2(L)41.5(MeOH)2(H2O)]n(L = Dic), 1, which has been isolated and structurally characterized by X-ray crystallography. Diclofenac sodium and its metal complex 1 have also been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The results of cytotoxic activity in vitro expressed as IC50 values indicated the diclofenac sodium and cadmium chloride are non active or less active than the metal complex of diclofenac (1). Complex 1 was also found to be a more potent cytotoxic agent against T-24 and MCF-7 cancer cell lines than the prevalent benchmark metallodrug, cisplatin, under the same experimental conditions. The superoxide dismutase activity was measured by Fridovich test which showed that complex 1 shows a low value in comparison with Cu complexes. The binding properties of this complex to biomolecules, bovine or human serum albumin, are presented and evaluated. Antibacterial and growth inhibitory activity is also higher than that of the parent ligand compound.

  11. Prevalence of Helicobacter Pylori-Negative, Non-Steroidal Anti-Inflammatory Drug Related Peptic Ulcer Disease in Patients Referred to Afzalipour Hospital.

    Science.gov (United States)

    Seyed Mirzaei, Seyed Mahdi; Zahedi, Mohammad Javad; Shafiei Pour, Sara

    2015-10-01

    BACKGROUND Although Helicobacter pylori and non-steroidal anti-inflammatory drugs (NSAIDs) are the main causes of peptic ulcers disease (PUD), recently the prevalence of idiopathic peptic ulcer (IPU) is increasing in most parts of the world. The aim of this study was to assess the prevalence of IPU in Kerman, the center of largest province in south-east Iran. METHODS We included 215 patients with peptic ulcer in our study. Combined methods rapid urease test (RUT), histology, and real time polymerase chain reaction (PCR) was performed on endoscopic samples of peptic ulcers. NSAID use was determined by medical history. SPSS software version 16 was used for data analysis. p valueulcer, four (1.8%) had H.pylorinegative and NSAID-negative PUD. There were not significant differences between patients with IPU and patients with peptic ulcer associated with H.pylori or NSAIDs regarding the sex, age, cigarette smoking, and opioid abuse. CONCLUSION Our study showed that in contrast to other reports from western and some Asian countries, the prevalence of IPU is low in Kerman and H.pylori infection is still the major cause of PUD. We recommend a large and multi-central study to determine the prevalence of IPU in Iran.

  12. Development of high-throughput multi-residue method for non-steroidal anti-inflammatory drugs monitoring in swine muscle by LC-MS/MS.

    Science.gov (United States)

    Castilhos, Tamara S; Barreto, Fabiano; Meneghini, Leonardo; Bergold, Ana Maria

    2016-07-01

    A reliable and simple method for the detection and quantification of residues of 14 non-steroidal anti-inflammatory drugs and a metamizole metabolite in swine muscle was developed using liquid chromatography-electrospray ionisation-tandem mass spectrometry (LC-ESI-MS/MS). The samples were extracted with acetonitrile (ACN) in solid-liquid extraction followed by a low-temperature partitioning (LLE-LTP) process at -20 ± 2°C. After evaporation to dryness, the residue was reconstituted with hexane and a mixture of water:acetonitrile (1:1). LC separation was achieved on a reversed-phase (RP18) column with gradient elution using water (phase A) and ACN (phase B) both containing 1 mmol l(-)(1) ammonium acetate (NH4COO) with 0.025% acetic acid. Analysis was carried out on a triple-quadrupole tandem mass spectrometer (LC-MS/MS) in multiple reaction monitoring mode using an electrospray interface in negative and positive mode in a single run. Method validation was performed according to the criteria of Commission Decision No. 2002/657/EC. The matrix effect and linearity were evaluated. Decision limit (CCα), detection capability (CCβ), accuracy and repeatability of the method are also reported. The proposed method proved to be simple, easy and adequate for high-throughput analysis and was applied to routine analysis by the Brazilian Ministry of Agriculture, Livestock and Food Supply. PMID:27268755

  13. Crystal structures of three classes of non-steroidal anti-inflammatory drugs in complex with aldo-keto reductase 1C3.

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    Jack U Flanagan

    Full Text Available Aldo-keto reductase 1C3 (AKR1C3 catalyses the NADPH dependent reduction of carbonyl groups in a number of important steroid and prostanoid molecules. The enzyme is also over-expressed in prostate and breast cancer and its expression is correlated with the aggressiveness of the disease. The steroid products of AKR1C3 catalysis are important in proliferative signalling of hormone-responsive cells, while the prostanoid products promote prostaglandin-dependent proliferative pathways. In these ways, AKR1C3 contributes to tumour development and maintenance, and suggest that inhibition of AKR1C3 activity is an attractive target for the development of new anti-cancer therapies. Non-steroidal anti-inflammatory drugs (NSAIDs are one well-known class of compounds that inhibits AKR1C3, yet crystal structures have only been determined for this enzyme with flufenamic acid, indomethacin, and closely related analogues bound. While the flufenamic acid and indomethacin structures have been used to design novel inhibitors, they provide only limited coverage of the NSAIDs that inhibit AKR1C3 and that may be used for the development of new AKR1C3 targeted drugs. To understand how other NSAIDs bind to AKR1C3, we have determined ten crystal structures of AKR1C3 complexes that cover three different classes of NSAID, N-phenylanthranilic acids (meclofenamic acid, mefenamic acid, arylpropionic acids (flurbiprofen, ibuprofen, naproxen, and indomethacin analogues (indomethacin, sulindac, zomepirac. The N-phenylanthranilic and arylpropionic acids bind to common sites including the enzyme catalytic centre and a constitutive active site pocket, with the arylpropionic acids probing the constitutive pocket more effectively. By contrast, indomethacin and the indomethacin analogues sulindac and zomepirac, display three distinctly different binding modes that explain their relative inhibition of the AKR1C family members. This new data from ten crystal structures greatly broadens

  14. Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index.

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    Marie-José C van Lierop

    Full Text Available Glucocorticoids (GCs such as prednisolone are potent immunosuppressive drugs but suffer from severe adverse effects, including the induction of insulin resistance. Therefore, development of so-called Selective Glucocorticoid Receptor Modulators (SGRM is highly desirable. Here we describe a non-steroidal Glucocorticoid Receptor (GR-selective compound (Org 214007-0 with a binding affinity to GR similar to that of prednisolone. Structural modelling of the GR-Org 214007-0 binding site shows disturbance of the loop between helix 11 and helix 12 of GR, confirmed by partial recruitment of the TIF2-3 peptide. Using various cell lines and primary human cells, we show here that Org 214007-0 acts as a partial GC agonist, since it repressed inflammatory genes and was less effective in induction of metabolic genes. More importantly, in vivo studies in mice indicated that Org 214007-0 retained full efficacy in acute inflammation models as well as in a chronic collagen-induced arthritis (CIA model. Gene expression profiling of muscle tissue derived from arthritic mice showed a partial activity of Org 214007-0 at an equi-efficacious dosage of prednisolone, with an increased ratio in repression versus induction of genes. Finally, in mice Org 214007-0 did not induce elevated fasting glucose nor the shift in glucose/glycogen balance in the liver seen with an equi-efficacious dose of prednisolone. All together, our data demonstrate that Org 214007-0 is a novel SGRMs with an improved therapeutic index compared to prednisolone. This class of SGRMs can contribute to effective anti-inflammatory therapy with a lower risk for metabolic side effects.

  15. COMPARATIVE EVALUATION OF TRANSCUTANEOUS ELECTRICAL NERVE STIMULATION (TENS V/S NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDS FOR POSTOPERATIVE PAIN MANAGEMENT IN OPEN CHOLECYSTECTOMY

    Directory of Open Access Journals (Sweden)

    Hans Raj

    2016-06-01

    Full Text Available Pain is not only an unpleasant sensation but also increases morbidity of any operation like atelectasis, ileus, requirement of intensive care and increase in hospital stay. By neuro-modulation based on the gate control theory, we can achieve the similar results as with pharmaceutics without their side effects. Aim of this study was to compare the Non-Steroidal Anti-Inflammatory Drug (NSAID with Transcutaneous Nerve Stimulation (TENS in terms of postoperative pain and duration of pain relief by using a visual analogue scale. MATERIAL AND METHODS Our study included open cholecystectomy patients, 25 patients in each group (Groups I with NSAID, group II with TENS use. The lower limit of age was 20 years. All patients who underwent open cholecystectomy and above 20 years of age without any comorbidities were included in the study. Data was analysed by using SPSS software version 16. RESULTS In TENS therapy group, patient’s acceptance was 84%. Patients in group I had a higher VAS score and less duration of pain relief than group II at 24 and 48 hours (VAS = 4 v/s 2, duration of pain relief = 8.0 and 8.8 hours v/s 10.8 and 11.2 hours. Average numbers of application for the group I was higher than group II (3 v/s 2.1. Both showed no complications of pain equal physiologic parameters like pulse and blood pressure, so both modalities were effective in controlling pain. CONCLUSION TENS can be used without analgesic for the postoperative pain of cholecystectomy with good patient acceptance and effectiveness.

  16. Effect of therapeutic plasma concentrations of non-steroidal anti-inflammatory drugs on the production of reactive oxygen species by activated rat neutrophils

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    Paino I.M.M.

    2005-01-01

    Full Text Available The release of reactive oxygen specie (ROS by activated neutrophil is involved in both the antimicrobial and deleterious effects in chronic inflammation. The objective of the present investigation was to determine the effect of therapeutic plasma concentrations of non-steroidal anti-inflammatory drugs (NSAIDs on the production of ROS by stimulated rat neutrophils. Diclofenac (3.6 µM, indomethacin (12 µM, naproxen (160 µM, piroxicam (13 µM, and tenoxicam (30 µM were incubated at 37ºC in PBS (10 mM, pH 7.4, for 30 min with rat neutrophils (1 x 10(6 cells/ml stimulated by phorbol-12-myristate-13-acetate (100 nM. The ROS production was measured by luminol and lucigenin-dependent chemiluminescence. Except for naproxen, NSAIDs reduced ROS production: 58 ± 2% diclofenac, 90 ± 2% indomethacin, 33 ± 3% piroxicam, and 45 ± 6% tenoxicam (N = 6. For the lucigenin assay, naproxen, piroxicam and tenoxicam were ineffective. For indomethacin the inhibition was 52 ± 5% and diclofenac showed amplification in the light emission of 181 ± 60% (N = 6. Using the myeloperoxidase (MPO/H2O2/luminol system, the effects of NSAIDs on MPO activity were also screened. We found that NSAIDs inhibited both the peroxidation and chlorinating activity of MPO as follows: diclofenac (36 ± 10, 45 ± 3%, indomethacin (97 ± 2, 100 ± 1%, naproxen (56 ± 8, 76 ± 3%, piroxicam (77 ± 5, 99 ± 1%, and tenoxicam (90 ± 2, 100 ± 1%, respectively (N = 3. These results show that therapeutic levels of NSAIDs are able to suppress the oxygen-dependent antimicrobial or oxidative functions of neutrophils by inhibiting the generation of hypochlorous acid.

  17. Laboratory monitoring of patients treated with antihypertensive drugs and newly exposed to non steroidal anti-inflammatory drugs: a cohort study.

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    Jean-Pascal Fournier

    Full Text Available BACKGROUND: Drug-Drug Interactions between Non Steroidal Anti-Inflammatory Drugs (NSAIDs and Angiotensin Converting Enzyme Inhibitors (ACEIs, Angiotensin Receptor Blocker (ARBs or diuretics can lead to renal failure and hyperkalemia. Thus, monitoring of serum creatinine and potassium is recommended when a first dispensing of NSAID occur in patients treated with these drugs. METHODS: We conducted a pharmacoepidemiological retrospective cohort study using data from the French Health Insurance Reimbursement Database to evaluate the proportion of serum creatinine and potassium laboratory monitoring in patients treated with ACEI, ARB or diuretic and receiving a first dispensing of NSAID. We described the first dispensing of NSAID among 3,500 patients of a 4-year cohort (6,633 patients treated with antihypertensive drugs and analyzed serum creatinine and potassium laboratory monitoring within the 3 weeks after the first NSAID dispensing. RESULTS: General Practitioners were the most frequent prescribers of NSAIDs (85.5%, 95% CI: 84.3-86.6. The more commonly prescribed NSAIDs were ibuprofen (20%, ketoprofen (15%, diclofenac (15% and piroxicam (12%. Serum creatinine and potassium monitoring was 10.7% (95% CI: 9.5-11.8 in patients treated by ACEIs, ARBs or diuretics. Overall, monitoring was more frequently performed to women aged over 60, treated with digoxin or glucose lowering drugs, but not to patients treated with ACEIs, ARBs or diuretics. Monitoring was more frequent when NSAIDs' prescribers were cardiologists or anesthesiologists. CONCLUSION: Monitoring of serum creatinine and potassium of patients treated with ACEIs, ARBs or diuretics and receiving a first NSAID dispensing is insufficiently performed and needs to be reinforced through specific interventions.

  18. Non-steroidal anti-inflammatory drugs use is associated with reduced risk of inflammation-associated cancers: NIH-AARP study.

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    Fatma M Shebl

    Full Text Available BACKGROUND: Chronic inflammation has been linked to cancers, and use of non-steroidal anti-inflammatory drugs (NSAIDs has been associated with reduced risk of several cancers. To further refine the magnitude of NSAID-related associations, in particular for cancers related to inflammation, such as alcohol-, infection-, obesity-, and smoking-related cancers, as well as for less common cancers, we evaluated the use of NSAIDs and cancer risk in a very large cohort. We used propensity scores to account for potential selection bias and hypothesized that NSAID use is associated with decreased cancer incidence. METHODS: We conducted a prospective study among 314,522 participants in the NIH-AARP Diet and Health Study. Individuals who completed the lifestyle questionnaire, which included NSAID use, in 1996-1997 were followed through 2006. Information on cancer incidence was ascertained by linking to cancer registries and vital status databases. FINDINGS: During 2,715,994 person-years of follow-up (median 10.1 person-years, there were 51,894 incident cancers. Compared with non-users of NSAIDs, individuals who reported use in the 12 months prior to interview had a significantly lower risk of all inflammation-related cancer, alcohol-related, infection-related, obesity-related, and smoking-related cancers [hazard ratio (HR (95% CI 0.90 (0.87-0.93, 0.80 (0.74-0.85, 0.82 (0.78-0.87, 0.88 (0.84-0.92, and 0.88 (0.85-0.92 respectively]. CONCLUSIONS: After accounting for potential selection bias, our data showed an inverse association between NSAID use and alcohol-related, infection-related, obesity-related, and smoking-related cancers and support the hypothesis that inflammation is related to an increased risk of certain cancers.

  19. Non-steroidal anti-inflammatory drugs, Cyclooxygenase-2 inhibitors and paracetamol use in Queensland and in the whole of Australia

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    Tett Susan E

    2008-09-01

    Full Text Available Abstract Background Cross national drug utilization studies can provide information about different influences on physician prescribing. This is important for medicines with issues around safety and quality of use, like non selective non-steroidal anti-inflammatory drugs (ns-NSAIDs and cyclo-oxygenase-2 (COX-2 inhibitors. To enable comparison of prescription medicine use across different jurisdictions with a range of population sizes, data first need to be compared within Australia to understand whether use in a smaller sub-population may be considered as representative of the total use within Australia. The aim of this study was to compare the utilization of non selective NSAID, COX-2 inhibitors and paracetamol between Queensland and Australia. Method Dispensing data were obtained for concession beneficiaries for Australia for ns-NSAIDs, COX-2 inhibitors and paracetamol subsidized by the PBS over the period 1997–2003. The same data were purchased for Queensland. Data were converted to Defined Daily Dose (DDD/1000 beneficiaries/day (World Health Organization anatomical therapeutic chemical classification, 2005. Results Total NSAID and paracetamol consumption were similar in Australia and Queensland. Ns-NSAID use decreased sharply with the introduction of COX-2 inhibitors (from approximately 80 to 40 DDD/1000 beneficiaries/day. Paracetamol was constant (approximately 45 DDD/1000 beneficiaries/day. COX-2 inhibitors consumption was initially higher in Queensland than in the whole of Australia. Conclusion Despite initial divergence in celecoxib use between Queensland and Australia, the use of ns-NSAIDs, COX-2 inhibitors and paracetamol overall, in concession beneficiaries, was comparable in Australia and Queensland.

  20. P-glycoprotein modulates morphine uptake into the CNS: a role for the non-steroidal anti-inflammatory drug diclofenac.

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    Lucy Sanchez-Covarrubias

    Full Text Available Our laboratory has previously demonstrated that peripheral inflammatory pain (PIP, induced by subcutaneous plantar injection of λ-carrageenan, results in increased expression and activity of the ATP-dependent efflux transporter P-glycoprotein (P-gp that is endogenously expressed at the blood-brain barrier (BBB. The result of increased P-gp functional expression was a significant reduction in CNS uptake of morphine and, subsequently, reduced morphine analgesic efficacy. A major concern in the treatment of acute pain/inflammation is the potential for drug-drug interactions resulting from P-gp induction by therapeutic agents co-administered with opioids. Such effects on P-gp activity can profoundly modulate CNS distribution of opioid analgesics and alter analgesic efficacy. In this study, we examined the ability of diclofenac, a non-steroidal anti-inflammatory drug (NSAID that is commonly administered in conjunction with the opioids during pain therapy, to alter BBB transport of morphine via P-gp and whether such changes in P-gp morphine transport could alter morphine analgesic efficacy. Administration of diclofenac reduced paw edema and thermal hyperalgesia in rats subjected to PIP, which is consistent with the known mechanism of action of this NSAID. Western blot analysis demonstrated an increase in P-gp expression in rat brain microvessels not only following PIP induction but also after diclofenac treatment alone. Additionally, in situ brain perfusion studies showed that both PIP and diclofenac treatment alone increased P-gp efflux activity resulting in decreased morphine brain uptake. Critically, morphine analgesia was significantly reduced in animals pretreated with diclofenac (3 h, as compared to animals administered diclofenac and morphine concurrently. These novel findings suggest that administration of diclofenac and P-gp substrate opioids during pain pharmacotherapy may result in a clinically significant drug-drug interaction.

  1. Non-steroidal anti-inflammatory drug use, hormone receptor status, and breast cancer-specific mortality in the Carolina Breast Cancer Study.

    Science.gov (United States)

    Allott, E H; Tse, C-K; Olshan, A F; Carey, L A; Moorman, P G; Troester, M A

    2014-09-01

    Epidemiologic studies report a protective association between non-steroidal anti-inflammatory drug (NSAID) use and hormone receptor-positive breast cancer risk, a finding consistent with NSAID-mediated suppression of aromatase-driven estrogen biosynthesis. However, the association between NSAID use and breast cancer-specific mortality is uncertain and it is unknown whether this relationship differs by hormone receptor status. This study comprised 935 invasive breast cancer cases, of which 490 were estrogen receptor (ER)-positive, enrolled between 1996 and 2001 in the Carolina Breast Cancer Study. Self-reported NSAID use in the decade prior to diagnosis was categorized by duration and regularity of use. Differences in tumor size, stage, node, and receptor status by NSAID use were examined using Chi-square tests. Associations between NSAID use and breast cancer-specific mortality were examined using age- and race-adjusted Cox proportional hazards analysis. Tumor characteristics did not differ by NSAID use. Increased duration and regularity of NSAID use was associated with reduced breast cancer-specific mortality in women with ER-positive tumors (long-term regular use (≥8 days/month for ≥ 3 years) versus no use; hazard ratio (HR) 0.48; 95 % confidence interval (CI) 0.23-0.98), with a statistically significant trend with increasing duration and regularity (p-trend = 0.036). There was no association for ER-negative cases (HR 1.19; 95 %CI 0.50-2.81; p-trend = 0.891). Long-term, regular NSAID use in the decade prior to breast cancer diagnosis was associated with reduced breast cancer-specific mortality in ER-positive cases. If confirmed, these findings support the hypothesis that potential chemopreventive properties of NSAIDs are mediated, at least in part, through suppression of estrogen biosynthesis. PMID:25151293

  2. Effects of non-steroidal anti-inflammatory drugs on cancer sites other than the colon and rectum: a meta-analysis

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    García Rodríguez Luis A

    2003-10-01

    Full Text Available Abstract Background Observational studies have consistently shown that aspirin and non-steroidal anti-inflammatory drug (NSAID use is associated with a close to 50% reduced risk of colorectal cancer. Studies assessing the effects of NSAIDs on other cancers have shown conflicting results. Therefore, we conducted a meta-analysis to evaluate the relationship between NSAID use and cancer other than colorectal. Methods We performed a search in Medline (from 1966 to 2002 and identified a total of 47 articles (13 cohort and 34 case-control studies. Overall estimates of the relative risk (RR were calculated for each cancer site using random effects models. Results Aspirin use was associated with a reduced risk of cancer of the esophagus and the stomach (RR, 0.51; 95%CI (0.38–0.69, and 0.73; 95%CI (0.63–0.84. Use of NSAIDs was similarly associated with a lower risk of esophageal and gastric cancers (RR,0.65; 95% CI(0.46–0.92 and RR,0.54; 95%CI (0.39–0.75. Among other cancers, only the results obtained for breast cancer were fairly consistent in showing a slight reduced risk among NSAID and aspirin users (RR, 0.77; 95%CI (0.66–0.88, and RR, 0.77; 95%CI (0.69–0.86 respectively. Conclusions The results of this meta-analysis show that the potential chemopreventive role of NSAIDs in colorectal cancer might be extended to other gastrointestinal cancers such as esophagus and stomach. Further research is required to evaluate the role of NSAIDs at other cancers sites.

  3. Long-term frequent use of non-steroidal anti-inflammatory drugs might protect patients with ankylosing spondylitis from cardiovascular diseases: a nationwide case-control study.

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    Wen-Chan Tsai

    Full Text Available The objective of this case-control study was to investigate the risk of cardiovascular disease (CVD following non-steroidal anti-inflammatory drug (NSAID use in patients with ankylosing spondylitis (AS. A total of 10,763 new AS patients were identified from the National Taiwan Health Insurance claims database during the period from 1997 to 2008. In all, 421 AS patients with CVD were recruited as cases, and up to 2-fold as many sex- and age-matched controls were selected. Logistic regression models were used to estimate the odds ratio (OR between NSAID use and CVD incidence. The medication possession rate (MPR was used to evaluate NSAID exposure during the study period. AS patients had increased risk of CVD (OR, 1.68; 95% confidence interval (CI, 1.57 to 1.80. Among frequent (MPR≥80% COX II users, the risks for all types of CVD were ten times lower than those among non-users at 24 months (OR, 0.08; 95% CI, 0.01 to 0.92. Among frequent NSAID users, the risks of major adverse cardiac event (MACE were significantly lower at 12 months (OR, 0.23; 95% CI, 0.07 to 0.76--a trend showing that longer exposure correlated with lower risk. Regarding non-frequent NSAID users (MPR<80%, short-term exposure did carry higher risk (for 6 months: OR, 1.41; 95% CI, 1.07 to 1.86, but after 12 months, the risk no longer existed. We conclude that long-term frequent use of NSAIDs might protect AS patients from CVD; however, NSAIDs still carried higher short-term risk in the non-frequent users.

  4. Systematic review and meta-analysis on the prophylacticrole of non-steroidal anti-inflammatory drugs to preventpost-endoscopic retrograde cholangiopancreatographypancreatitis

    Institute of Scientific and Technical Information of China (English)

    2015-01-01

    AIM To critically appraise the published randomized,controlled trials on the prophylactic effectiveness ofthe non-steroidal anti-inflammatory drugs (NSAIDs),in reducing the risk of post-endoscopic retrogradecholangiopancreatography (ERCP) pancreatitis.METHODS: A systematic literature search (MEDLINE,Embase and the Cochrane Library, from inception of thedatabases until May 2015) was conducted to identifyrandomized, clinical trials investigating the role ofNSAIDs in reducing the risk of post-ERCP pancreatitis.Random effects model of the meta-analysis was carriedout, and results were presented as odds ratios (OR)with corresponding 95%CI.RESULTS: Thirteen randomized controlled trials on3378 patients were included in the final meta-analysis.There were 1718 patients in the NSAIDs group and 1660patients in non-NSAIDs group undergoing ERCP. Theuse of NSAIDs (through rectal route or intramuscularroute) was associated with the reduced risk of post-ERCPpancreatitis [OR, 0.52 (0.38-0.72), P = 0.0001]. Theuse of pre-procedure NSAIDs was effective in reducingapproximately 48% incidence of post-ERCP pancreatitis,number needed to treat were 16 with absolute riskreduction of 0.05. But the risk of post-ERCP pancreattiswas reduced by 55% if NSAIDs were administered afterprocedure. Similarly, diclofenac was more effective (55%)prophylactic agent compared to indomethacin (41%).CONCLUSION: NSAIDs seem to have clinically provenadvantage of reducing the risk of post-ERCP pancreatitis.

  5. Long-term use of non-steroidal anti-inflammatory drugs and the risk of myocardial infarction in the general population

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    González-Pérez Antonio

    2005-11-01

    Full Text Available Abstract Background Recent data indicate that chronic use of coxibs leads to an increased occurrence of thrombotic cardiovascular events. This raises the question as to whether traditional non-steroidal anti-inflammatory drugs (tNSAIDs might also produce similar hazards. Our aim has been to evaluate the association between the chronic use of tNSAIDs and the risk of myocardial infarction (MI in patients. Methods We performed a nested case-control analysis with 4,975 cases of acute MI and 20,000 controls, frequency matched to cases by age, sex, and calendar year. Results Overall, current use of tNSAID was not associated with an increased risk of MI (RR:1.07;95%CI: 0.95–1.21. However, we found that the relative risk (RR of MI for durations of tNSAID treatment of >1 year was 1.21 (95% CI, 1.00–1.48. The corresponding RR was 1.34 (95% CI, 1.06–1.70 for non-fatal MI. The effect was independent from dose. The small risk associated with long-term use of tNSAIDs was observed among patients not taking low-dose aspirin (RR: 1.29; 95% CI, 1.01–1.65. The effect of long-term use for individual tNSAIDs ranged from a RR of 0.87 (95% CI, 0.47–1.62 with naproxen to 1.38 (95% CI, 1.00–1.90 with diclofenac. Conclusion This study adds support to the hypothesis that chronic treatment with some tNSAIDs is associated with a small increased risk of non-fatal MI. Our data are consistent with a substantial variability in cardiovascular risks between individual tNSAIDs.

  6. Exposure to non-steroidal anti-inflammatory drugs during pregnancy and the risk of selected birth defects: a prospective cohort study.

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    Marleen M H J van Gelder

    Full Text Available BACKGROUND: Since use of non-steroidal anti-inflammatory drugs (NSAIDs during pregnancy is common, small increases in the risk of birth defects may have significant implications for public health. Results of human studies on the teratogenic risks of NSAIDs are inconsistent. Therefore, we evaluated the risk of selected birth defects after prenatal exposure to prescribed and over-the-counter NSAIDs. METHODS AND FINDINGS: We used data on 69,929 women enrolled in the Norwegian Mother and Child Cohort Study between 1999 and 2006. Data on NSAID exposure were available from a self-administered questionnaire completed around gestational week 17. Information on pregnancy outcome was obtained from the Medical Birth Registry of Norway. Only birth defects suspected to be associated with NSAID exposure based upon proposed teratogenic mechanisms and previous studies were included in the multivariable logistic regression analyses. A total of 3,023 women used NSAIDs in gestational weeks 0-12 and 64,074 women did not report NSAID use in early pregnancy. No associations were observed between overall exposure to NSAIDs during pregnancy and the selected birth defects separately or as a group (adjusted odds ratio 0.7, 95% confidence interval 0.4-1.1. Associations between maternal use of specific types of NSAIDs and the selected birth defects were not found either, although an increased risk was seen for septal defects and exposure to multiple NSAIDs based on small numbers (2 exposed cases; crude odds ratio 3.9, 95% confidence interval 0.9-15.7. CONCLUSIONS: Exposure to NSAIDs during the first 12 weeks of gestation does not seem to be associated with an increased risk of the selected birth defects. However, due to the small numbers of NSAID-exposed infants for the individual birth defect categories, increases in the risks of specific birth defects could not be excluded.

  7. The role of activated carbon and disinfection on the removal of endocrine disrupting chemicals and non-steroidal anti-inflammatory drugs from wastewater.

    Science.gov (United States)

    Noutsopoulos, Constantinos; Mamais, Daniel; Mpouras, Thanasis; Kokkinidou, Despina; Samaras, Vasilios; Antoniou, Korina; Gioldasi, Marianna

    2014-01-01

    Endocrine disrupting chemicals and non-steroidal anti-inflammatory drugs are two important groups of emerging pollutants due to their toxicological and chemical characteristics and their persistent detection in the aquatic environment. Wastewater treatment plants are a significant pathway for their transfer to the water courses. It is well evidenced that these chemicals are only partially removed through biological treatment of wastewater and therefore being detected in secondary effluents. This work focuses on the evaluation of the efficiency of two well-established disinfection technologies (chlorination and UV irradiation) along with UV/H2O2 and powdered activated carbon (PAC) to remove these chemicals from biologically treated wastewater. Based on the results it is shown that appreciable removal efficiencies due to chlorination should be expected for most of the target compounds, whereas this was not the case for ibuprofen and ketoprofen. With the exemption of diclofenac and ketoprofen direct UV irradiation did not efficiently removed target compounds for UV doses usually applied for disinfection purposes. The application of advanced UV treatment through the addition of H2O2 although resulted in increased removal of the target compounds is not sufficient at moderate UV and H2O2 doses to achieve satisfactory removal efficiencies. PAC use resulted in sufficient removal of target compounds although high PAC doses were required for some chemicals. Comparison of Freundlich isotherms of this study with those of other studies, derived employing water samples, suggested that the water matrix along with the target compounds concentration range can significantly affect the outcome of the experiments. PMID:24645450

  8. Non steroidal anti-inflammatory drugs modulate the physicochemical properties of plasma membrane in experimental colorectal cancer: a fluorescence spectroscopic study.

    Science.gov (United States)

    Vaish, Vivek; Sanyal, Sankar Nath

    2011-12-01

    According to "fluid-mosaic model," plasma membrane is a bilayer constituted by phospholipids which regulates the various cellular activities governed by many proteins and enzymes. Any chemical, biochemical, or physical factor has to interact with the bilayer in order to regulate the cellular metabolism where various physicochemical properties of membrane, i.e., polarization, fluidity, electrostatic potential, and phase state may get affected. In this study, we have observed the in vivo effects of a pro-carcinogen 1,2-dimethylhydrazine dihydrochloride (DMH) and the two non steroidal anti-inflammatory drugs (NSAIDs); sulindac and celecoxib on various properties of the plasma membrane of colonocytes, i.e., electric potential, fluidity, anisotropy, microviscosity, lateral diffusion, and phase state in the experimentally induced colorectal cancer. A number of fluorescence probes were utilized like membrane fluidity and anisotropy by 1,6-diphenyl-1,3,5-hexatriene, membrane microviscosity by Pyrene, membrane electric potential by merocyanine 540, lateral diffusion by N-NBD-PE, and phase state by Laurdan. It is observed that membrane phospholipids are less densely packed and therefore, the membrane is more fluid in case of carcinogenesis produced by DMH than control. But NSAIDs are effective in reverting back the membrane toward normal state when co-administered with DMH. The membrane becomes less fluid, composed of low electric potential phospholipids whose lateral diffusion is being prohibited and the membrane stays mostly in relative gel phase. It may be stated that sulindac and celecoxib, the two NSAIDs may exert their anti-neoplastic role in colorectal cancer via modifying the physicochemical properties of the membranes. PMID:21725642

  9. Crystal structure of a mixed-ligand silver(I) complex of the non-steroidal anti-inflammatory drug diclofenac and pyrimidine

    Science.gov (United States)

    Hamamci Alisir, Sevim; Dege, Necmi

    2016-01-01

    In the title mixed-ligand silver(I) coordination polymeric complex with the non-steroidal anti-inflammatory drug diclofenac (C14H11Cl2NO2) (diclH) and pyrimidine (pym), namely poly[{μ2-2-[2-(2,6-di­chloro­anilino)phen­yl]acetato-κ2 O:O′}(μ2-pyrimidine-κ2 N 1:N 3)silver(I)], [Ag(C14H10Cl2NO2)(C4H4N2)]n or [Ag(μ-dicl)(μ-pym)]n, the very distorted tetra­hedral AgN2O2 coordination centres comprise two N-atom donors from bridging pym ligands [Ag—N = 2.381 (3) and 2.412 (3) Å] and two carboxyl­ate O-atom donors from dicl ligands [Ag—O = 2.279 (2) and 2.280 (2) Å], which bridge Ag atoms, giving a centrosymmetric dinuclear units with a short Ag⋯Ag separation [2.8931 (5) Å]. Within the units are short intra­ligand C—Cl⋯π(pym) inter­actions [3.6409 (15) Å]. The units are linked through the bridging N atoms of the pym ligand into a two-dimensional sheet–polymer structure lying parallel to (100) and stabilized by inter-ring π–π inter­actions between the pym ligands [Cg⋯Cg = 3.4199 (17) Å]. Additional inter-unit C—H⋯O and C—H⋯Cg hydrogen-bonding inter­actions between the sheets give an overall three-dimensional structure. PMID:27746945

  10. Determination of non-steroidal anti-inflammatory drugs and their metabolites in milk by liquid chromatography-tandem mass spectrometry.

    Science.gov (United States)

    Jedziniak, Piotr; Szprengier-Juszkiewicz, Teresa; Pietruk, Konrad; Sledzińska, Edyta; Zmudzki, Jan

    2012-07-01

    Non-steroidal anti-inflammatory drugs are widely used for treatment of animals. According to Council Directive 96/23/EC, residues of these drugs must be monitored because of the potential risk they pose to the consumers' health. For this reason an LC-MS-MS method was developed for detection of wide range of NSAIDs, including both "acidic" NSAIDs (carprofen, diclofenac, flunixin, meloxicam, phenylbutazone, oxyphenbutazone, tolfenamic acid, mefenamic acid, naproxen, ketoprofen, ibuprofen, firocoxib, rofecoxib, and celecoxib) and "basic" NSAIDs (four metamizole metabolites). Analytes were extracted from milk samples with acetonitrile in the presence of ammonium acetate. One portion of the extract was directly analyzed for the presence of metamizole metabolites; a second portion was cleaned with an amino cartridge. All NSAIDs were separated on a Phenomenex Luna C8(2) column and analyzed by LC-MS-MS in negative (acidic NSAIDs) and positive (metamizole metabolites) ion modes. The method was validated in accordance with the requirements of Commission Decision 2002/657/EC. Within-laboratory reproducibility was in the range 7-28%, and accuracy was in the range 71-116%. The method enabled detection of all the analytes with the expected sensitivity, below the recommended concentrations. The method fulfills the criteria for confirmatory methods and, because of its efficiency, may also be used for screening purposes. The procedure was also successfully verified in the proficiency test organized by EU-RL in 2010. As far as the authors are aware, this is one of the first methods capable of detecting diclofenac residues below the MRL in milk (0.1 μg kg(-1)). An additional advantage is the possibility of simultaneous determination of "acidic" NSAIDs and metamizole metabolites. PMID:22395450

  11. ASTHMA AND RHINITIS INDUCED BY SELECTIVE IMMEDIATE REACTIONS TO PARACETAMOL AND NON-STEROIDAL ANTI-INFLAMMATORY DRUGS IN ASPIRIN TOLERANT SUBJECTS

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    Diana Pérez-Alzate

    2016-07-01

    Full Text Available In subjects with non-steroidal anti-inflammatory drugs (NSAIDs- exacerbated respiratory disease (NERD symptoms are triggered by acetyl salicylic acid (ASA and other strong COX-1 inhibitors, and in some cases by weak COX-1 or by selective COX-2 inhibitors. The mechanism involved is related to prostaglandin pathway inhibition and leukotriene release. Subjects who react to a single NSAID and tolerate others are considered selective responders, and often present urticaria and/or angioedema and anaphylaxis (SNIUAA. An immunological mechanism is implicated in these reactions. However, anecdotal evidence suggests that selective responders who present respiratory airway symptoms may also exist.Our objective was to determine if subjects might develop selective responses to NSAIDs/paracetamol that manifest as upper/lower airways respiratory symptoms. For this purpose we studied patients reporting asthma and/or rhinitis induced by paracetamol or a single NSAID that tolerated ASA. An allergological evaluation plus controlled challenge with ASA was carried out. If ASA tolerance was found, we proceeded with an oral challenge with the culprit drug. The appearance of symptoms was monitored by a clinical questionnaire and by measuring FEV1 and/or nasal airways volume changes pre and post challenge. From a total of 21 initial cases, we confirmed the appearance of nasal and/or bronchial manifestations in ten, characterised by a significant decrease in FEV1% and/or a decrease in nasal volume cavity after drug administration. All cases tolerated ASA.This shows that ASA tolerant subjects with asthma and/or rhinitis induced by paracetamol or a single NSAID without skin/systemic manifestations exist. Whether these patients represent a new clinical phenotype to be included within the current classification of hypersensitivity reactions to NSAIDs requires further investigation.

  12. Asthma and Rhinitis Induced by Selective Immediate Reactions to Paracetamol and Non-steroidal Anti-inflammatory Drugs in Aspirin Tolerant Subjects

    Science.gov (United States)

    Pérez-Alzate, Diana; Blanca-López, Natalia; Doña, Inmaculada; Agúndez, José A.; García-Martín, Elena; Cornejo-García, José A.; Perkins, James R.; Blanca, Miguel; Canto, Gabriela

    2016-01-01

    In subjects with non-steroidal anti-inflammatory drugs (NSAIDs)- exacerbated respiratory disease (NERD) symptoms are triggered by acetyl salicylic acid (ASA) and other strong COX-1 inhibitors, and in some cases by weak COX-1 or by selective COX-2 inhibitors. The mechanism involved is related to prostaglandin pathway inhibition and leukotriene release. Subjects who react to a single NSAID and tolerate others are considered selective responders, and often present urticaria and/or angioedema and anaphylaxis (SNIUAA). An immunological mechanism is implicated in these reactions. However, anecdotal evidence suggests that selective responders who present respiratory airway symptoms may also exist. Our objective was to determine if subjects might develop selective responses to NSAIDs/paracetamol that manifest as upper/lower airways respiratory symptoms. For this purpose, we studied patients reporting asthma and/or rhinitis induced by paracetamol or a single NSAID that tolerated ASA. An allergological evaluation plus controlled challenge with ASA was carried out. If ASA tolerance was found, we proceeded with an oral challenge with the culprit drug. The appearance of symptoms was monitored by a clinical questionnaire and by measuring FEV1 and/or nasal airways volume changes pre and post challenge. From a total of 21 initial cases, we confirmed the appearance of nasal and/or bronchial manifestations in ten, characterized by a significant decrease in FEV1% and/or a decrease in nasal volume cavity after drug administration. All cases tolerated ASA. This shows that ASA tolerant subjects with asthma and/or rhinitis induced by paracetamol or a single NSAID without skin/systemic manifestations exist. Whether these patients represent a new clinical phenotype to be included within the current classification of hypersensitivity reactions to NSAIDs requires further investigation. PMID:27489545

  13. Effect of increase in orientational order of lipid chains and head group spacing on non steroidal anti-inflammatory drug induced membrane fusion.

    Science.gov (United States)

    Roy, Sutapa Mondal; Bansode, Amol S; Sarkar, Munna

    2010-12-21

    Membrane fusion is a key event in many biological processes. The fusion process, both in vivo and in vitro, is induced by different agents which include mainly proteins and peptides. For protein- and peptide-mediated membrane fusion, conformational reorganization serves as a driving force. Small drug molecules do not share this advantage; hence, drug induced membrane fusion occurring in absence of any other fusogenic agent and at physiologically relevant concentration of the drugs is a very rare event. To date, only three drugs, namely, meloxicam (Mx), piroxicam (Px), and tenoxicam (Tx), belonging to the oxicam group of non steroidal anti-inflammatory drugs (NSAIDs), have been shown by us to induce fusion at very low drug to lipid ratio without the aid of any other fusogenic agent. In our continued effort to understand the interplay of different physical and chemical parameters of both the participating drugs and the membrane on the mechanism of this drug induced membrane fusion, we present here the effect of increase in orientational order of the lipid chains and increase in head group spacing. This is achieved by studying the effect of low concentration cholesterol (gel to fluid transition temperature, is mainly known to increase orientational order of the lipid chains and increase head group spacing. To isolate the effect of these parameters, small unilameller vesicles (SUVs) formed by dimyristoylphosphatidylcholine (DMPC) with an average diameter of 50-60 nm were used as simple model membranes. Fluorescence assays were used to probe the time dependence of lipid mixing, content mixing, and leakage and also used to determine the partitioning of the drugs in the membrane bilayer. Differential scanning calorimetry (DSC) was used to study the effect of drugs in the presence of cholesterol on the chain-melting temperature which reflects the fluidization effect of the hydrophobic tail region of the bilayer. Our results show contradictory effect of low concentration

  14. Non-steroidal anti-inflammatory high digestive bleeding hospital income / Ingresos hospitalarios por hemorragia digestiva alta por antiinflamatorios no esteroidicos

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    Valls MD

    2004-12-01

    Full Text Available From year 1997 the Requena Hospital Pharmacy Service maintain a program of detection and prevention of drugs-related problems hospital income (DRPI. The program is coordinated with the Primary Care Pharmacy Service for the establishment of the preventive measures. The DRPI program establishes feedback, collective and/or individualized, on the agents of health of the Health Area and on the population in general, according to the cases, as it bases for the prevention of DRPIs. Methods: The detection of IDRP is made by means of revision of the diagnoses gathered in the admission book of the Emergency Department and the HIGIA database. Clinical records of the patients are retrospectively analyzed. Medical criteria, specifically gathered in clinical history, are accepted for the imputability establishment. Results: In period 1997-2003, 195 drug-related high digestive hemorrhage hospital income (HDH have been detected: 188 by non-steroidal anti-inflammatory drugs (NSAID, in two cases the NSAID could not settle down cause, 3 by ticlopidine, 3 by metamizole and 1 by clopidogrel. In 45 cases (23% the involved medicine was over the counter (OTC, 58 cases were related to low doses aspirin (AAS, 15 cases related to the association of NSAIDs or NSAIDs with low doses AAS and 70 cases were produced by non-aspirin-NSAIDs or non-OTC-AAS to doses of 500mg. 80% of the cases of HDH by AAS to low doses took place in patients of 69 years old or older. In 85% of the cases of HDH by non-aspirin- NSAID or non-OTC-AAS of 500mg with gastro-protection criteria this had not been used. In the three cases of HDH by metamizole patients were older than 80 years and with HDH antecedents. Conclusions: The low use of gastroprotection between the affected population of HDH by NSAIDs in spite of the existence of clear factors of risk concludes. Gastroprotection in patients dealt with low doses AAS and equal or greater age about 69 years although the age were the only factor of risk

  15. PRESCRIBING PATTERN OF NON - STEROIDAL ANTI - INFLAMMATORY DRUGS IN OUT PATIENTS OF ORTHOPEDIC DEPARTMENTS OF SECONDARY AND TERTIARY HEALTH CARE SETTINGS

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    Sanalkumar

    2015-08-01

    Full Text Available BACKGROUND: Non - steroidal anti - inflammatory drugs (NSAIDs make up one of the largest groups of pharmaceutical agents used worldwide . Though NSAIDs are beneficial , they are not without adverse reactions , of which , gastrointestinal toxicity is the most relevant . Hence cautious and rational use of this group of drug is indicated to avoid a major catastrophe . This study has been designed to evaluate the use of NSAIDs and the profile of their utilization . OBJECTIVES: 1 . To Study the Pattern of NSAIDs prescription in the secondary and tertiary health centers . 2 . To Study the proportions having Co - prescription with gastro protective agents . METHODOLOGY: A cross sectional study done in orthopedic outpatient departments of tertiary and secondary health centers of Thiruvananthapuram which includes totally 769 patients . Study was conducted from June 1 st to September 30 , 2006 after ethical clearance from the ethical committee , Government Medical College , Thiruvananthapuram . RESULTS: 769 patients were studied from three health care facilities in Thiruvananthapuram District . Diclofenac was the most commonly used drug in the District Hospital and Medical College Hospital (MCH , 62% and 46 . 6% respectively; whereas Ibuprofen was the most commonly used drug in Taluk hospital (45 . 9% . In General hospital , 247 cases received NSA ID out of which 95 cases only received gastro protective agents , the lowest % among the three centers . Out of 262 cases in the MCH 249 cases received NSAIDs . Among 249 cases only 193 cases received gastro protective agents that is about 77 . 5% . Out of 257 cases in the Taluk Hospital 256 cases received NSAIDs and among 256 cases 248 cases received gastro protective agents , about 96 . 8 % , highest % of gastro protective agents . Conclusion: Diclofenac was the most commonly used drug in the District Hospital and Medical College Hospital , 62% and 46 . 6% respectively; whereas Ibuprofen was the most commonly

  16. Non-steroidal anti-inflammatory drugs for the treatment of pain and immobility-associated osteoarthritis: consensus guidance for primary care

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    Adebajo Ade

    2012-03-01

    Full Text Available Abstract Background Osteoarthritis is a common presentation in primary care, and non-selective non-steroidal anti-inflammatory drugs (sometimes also referred to as traditional NSAIDs or tNSAIDs and selective cyclo-oxygenase 2 inhibitors (COX-2 inhibitors are commonly used to treat it. The UK's National Institute for Health and Clinical Excellence (NICE recommends taking patient risk factors into account when selecting a tNSAID or a COX-2 inhibitor, but GPs have lacked practical guidance on assessing patient risk. Methods A multi-disciplinary group that included primary care professionals (PCPs developed an evidence-based consensus statement with an accompanying flowchart that aimed at providing concise and specific guidance on NSAID use in osteoarthritis treatment. An open invitation to meet and discuss the issue was made to relevant healthcare professionals in South Yorkshire. A round table meeting was held that used a modified nominal group technique, aimed at generating opinions and ideas from all stakeholders in the consensus process. A draft developed from this meeting went through successive revisions until a consensus was achieved. Results Four statements on the use of tNSAIDs and COX-2 inhibitors (and an attached category of evidence were agreed: 1 tNSAIDs are effective drugs in relieving pain and immobility associated with osteoarthritis. COX-2 inhibitors are equally effective; 2 tNSAIDs and COX-2 inhibitors vary in their potential gastrointestinal, liver, and cardio-renal toxicity. This risk varies between individual treatments within both groups and is increased with dose and duration of treatment; 3 COX-2 inhibitors are associated with a significantly lower gastrointestinal toxicity compared to tNSAIDs. Co-prescribing of aspirin reduces this advantage; 4 PPIs should always be considered with a tNSAID and with a COX-2 inhibitor in higher GI risk patients. An accompanying flowchart to guide management was also agreed. Conclusions

  17. Primary treatment for temporomandibular joint osteoarthritis. Combination therapy with two consecutive arthrocenteses (steroid injection) followed by mouth-opening exercises and non-steroidal anti-inflammatory drug administration

    International Nuclear Information System (INIS)

    Arthrocentesis is the surgical treatment of choice for temporomandibular joint (TMJ) disorders. Many studies of arthrocentesis have been performed, with excellent clinical outcomes. No previous study has used multiple arthrocenteses to treat the dysfunctional TMJ. This study evaluated the efficacy of two consecutive arthrocenteses (steroid injection) followed by mouth-opening exercises during non-steroidal anti-inflammatory drug (NSAID) administration as a primary treatment for TMJ osteoarthritis. Subjects in this study were selected from a consecutive series of new patients with unilateral moderate to severe TMJ dysfunction at TMD Clinic, Aichi-Gakuin University Hospital during a year. Twenty-eight patients with MRI documentation of osteoarthritis underwent two consecutive arthrocenteses with steroid injection at a 2-week interval followed by mouth-opening exercises and treatment with the NSAID, Etodolac. The patients were postoperatively examined every 2 weeks for 12 weeks. The patients were clinically evaluated on the basis of visual analog scales (0-100) and the range of motion. Factors that affected the clinical outcome of TMJ function were assessed. Of the 28 patients who underwent two consecutive arthrocenteses, 21 (75%) showed substantial improvement on follow-up at 12 weeks. The range of motion (median) increased from 28 mm to 41 mm. Visual analog scale pain-scores on mouth opening and chewing significantly decreased from 50 and 60 to 24 and 22, respectively. The disturbance score for activities of daily life also decreased from 55 to 18. A longer duration of TMJ symptoms before the procedure was found to affect outcome. (author)

  18. Synthesis and assignment of absolute configuration of (-)-oleocanthal: a potent, naturally occurring non-steroidal anti-inflammatory and anti-oxidant agent derived from extra virgin olive oils.

    Science.gov (United States)

    Smith, Amos B; Han, Qiang; Breslin, Paul A S; Beauchamp, Gary K

    2005-10-27

    [structure: see text] Effective total syntheses and the assignment of absolute configurations of both the (+)- and (-)-enantiomers of oleocanthal 1 (a.k.a. deacetoxy ligstroside aglycon), the latter derived from extra virgin olive oils and known to be responsible for the back of the throat irritant properties of olive oils, have been achieved. The absolute and relative stereochemistry of the naturally occurring enantiomer (-)-1 proved to be 3S,4E. Both syntheses begin with d-(-)-ribose, proceed in 12 steps, and are achieved with an overall yield of 7%. Both enantiomers proved to be non-steroidal anti-inflammatory and anti-oxidant agents. PMID:16235961

  19. On the absorption and emission properties of three new non-steroidal anti-inflammatory drugs-β-cyclodextrin host-guest inclusion complexes: differentiated sensitivity to the microenvironment upon light excitation

    OpenAIRE

    MONTI S; Salemi, M. G.; S. Giuffrida; De Fazio, S; Guidi, G.; Sortino, S.

    1999-01-01

    The effects of β-cyclodextrin (β-CD) complexation on the absorption and emission properties of the non-steroidal anti-inflammatory drugs tolmetin (TM), diflunisal (DF), and fenbufen (FB) have been investigated. The absorption spectra of all these compounds are only slightly affected by the addition of ��-CD. In contrast, the emission properties were markedly influenced by CD complexation and in a different manner for the three compounds due to a differentiated sensitivity of the exci...

  20. Novel anti-inflammatory agents in COPD

    DEFF Research Database (Denmark)

    Loukides, Stelios; Bartziokas, Konstantinos; Vestbo, Jørgen;

    2013-01-01

    Inflammation plays a central role in chronic obstructive pulmonary disease (COPD). COPD related inflammation is less responsive to inhaled steroids compared to asthma. There are three major novel anti-inflammatory approaches to the management of COPD. The first approach is phosphodiesterase...

  1. Therapeutic potential of a non-steroidal bifunctional anti-inflammatory and anti-cholinergic agent against skin injury induced by sulfur mustard

    International Nuclear Information System (INIS)

    Sulfur mustard (bis(2-chloroethyl) sulfide, SM) is a highly reactive bifunctional alkylating agent inducing edema, inflammation, and the formation of fluid-filled blisters in the skin. Medical countermeasures against SM-induced cutaneous injury have yet to be established. In the present studies, we tested a novel, bifunctional anti-inflammatory prodrug (NDH 4338) designed to target cyclooxygenase 2 (COX2), an enzyme that generates inflammatory eicosanoids, and acetylcholinesterase, an enzyme mediating activation of cholinergic inflammatory pathways in a model of SM-induced skin injury. Adult SKH-1 hairless male mice were exposed to SM using a dorsal skin vapor cup model. NDH 4338 was applied topically to the skin 24, 48, and 72 h post-SM exposure. After 96 h, SM was found to induce skin injury characterized by edema, epidermal hyperplasia, loss of the differentiation marker, keratin 10 (K10), upregulation of the skin wound marker keratin 6 (K6), disruption of the basement membrane anchoring protein laminin 322, and increased expression of epidermal COX2. NDH 4338 post-treatment reduced SM-induced dermal edema and enhanced skin re-epithelialization. This was associated with a reduction in COX2 expression, increased K10 expression in the suprabasal epidermis, and reduced expression of K6. NDH 4338 also restored basement membrane integrity, as evidenced by continuous expression of laminin 332 at the dermal–epidermal junction. Taken together, these data indicate that a bifunctional anti-inflammatory prodrug stimulates repair of SM induced skin injury and may be useful as a medical countermeasure. - Highlights: • Bifunctional anti-inflammatory prodrug (NDH4338) tested on SM exposed mouse skin • The prodrug NDH4338 was designed to target COX2 and acetylcholinesterase. • The application of NDH4338 improved cutaneous wound repair after SM induced injury. • NDH4338 treatment demonstrated a reduction in COX2 expression on SM injured skin. • Changes of skin repair

  2. Therapeutic potential of a non-steroidal bifunctional anti-inflammatory and anti-cholinergic agent against skin injury induced by sulfur mustard

    Energy Technology Data Exchange (ETDEWEB)

    Chang, Yoke-Chen; Wang, James D.; Hahn, Rita A.; Gordon, Marion K.; Joseph, Laurie B. [Department of Pharmacology and Toxicology, Rutgers University, Piscataway, NJ (United States); Heck, Diane E. [Department of Environmental Science, New York Medical College, Valhalla, NY (United States); Heindel, Ned D. [Department of Chemistry, Lehigh University, Bethlehem, PA (United States); Young, Sherri C. [Department of Chemistry, Muhlenberg College, Allentown, PA (United States); Sinko, Patrick J. [Department of Pharmaceutics, Rutgers University, Piscataway, NJ (United States); Casillas, Robert P. [MRIGlobal, Kansas City, MO (United States); Laskin, Jeffrey D. [Environmental and Occupational Medicine, Robert Wood Johnson Medical School, Rutgers University, Piscataway, NJ (United States); Laskin, Debra L. [Department of Pharmacology and Toxicology, Rutgers University, Piscataway, NJ (United States); Gerecke, Donald R., E-mail: gerecke@eohsi.rutgers.edu [Department of Pharmacology and Toxicology, Rutgers University, Piscataway, NJ (United States)

    2014-10-15

    Sulfur mustard (bis(2-chloroethyl) sulfide, SM) is a highly reactive bifunctional alkylating agent inducing edema, inflammation, and the formation of fluid-filled blisters in the skin. Medical countermeasures against SM-induced cutaneous injury have yet to be established. In the present studies, we tested a novel, bifunctional anti-inflammatory prodrug (NDH 4338) designed to target cyclooxygenase 2 (COX2), an enzyme that generates inflammatory eicosanoids, and acetylcholinesterase, an enzyme mediating activation of cholinergic inflammatory pathways in a model of SM-induced skin injury. Adult SKH-1 hairless male mice were exposed to SM using a dorsal skin vapor cup model. NDH 4338 was applied topically to the skin 24, 48, and 72 h post-SM exposure. After 96 h, SM was found to induce skin injury characterized by edema, epidermal hyperplasia, loss of the differentiation marker, keratin 10 (K10), upregulation of the skin wound marker keratin 6 (K6), disruption of the basement membrane anchoring protein laminin 322, and increased expression of epidermal COX2. NDH 4338 post-treatment reduced SM-induced dermal edema and enhanced skin re-epithelialization. This was associated with a reduction in COX2 expression, increased K10 expression in the suprabasal epidermis, and reduced expression of K6. NDH 4338 also restored basement membrane integrity, as evidenced by continuous expression of laminin 332 at the dermal–epidermal junction. Taken together, these data indicate that a bifunctional anti-inflammatory prodrug stimulates repair of SM induced skin injury and may be useful as a medical countermeasure. - Highlights: • Bifunctional anti-inflammatory prodrug (NDH4338) tested on SM exposed mouse skin • The prodrug NDH4338 was designed to target COX2 and acetylcholinesterase. • The application of NDH4338 improved cutaneous wound repair after SM induced injury. • NDH4338 treatment demonstrated a reduction in COX2 expression on SM injured skin. • Changes of skin repair

  3. Influenza-induced tachypnea is prevented in immune cotton rats, but cannot be treated with an anti-inflammatory steroid or a neuraminidase inhibitor

    International Nuclear Information System (INIS)

    Influenza viruses are one of the leading causes of morbidity and mortality during winter months. Increased respiratory rate (tachypnea) is a sign of increasing lower respiratory disease during influenza infection and is frequently observed in hospitalized patients. We investigated this clinical sign in influenza virus-infected cotton rats (Sigmodon hispidus) and the efficacy of antiviral and anti-inflammatory therapy in reducing symptomatic disease. Cotton rats infected intranasally with A/Wuhan/359/95 (H3N2) had increased respiratory rates from 1 to 4 days postinfection that correlated with the dose of virus used to inoculate the animal but not the amount of virus recovered from the lung. In addition, evaluation of sequential lung tissue pathology revealed that extensive epithelial cell destruction of small airways correlated with tachypnea. Increased respiratory rate was not observed in immune animals, supporting results that demonstrated a requirement for exposure to, and infection by, large amounts of live virus for induction of tachypnea. A variety of therapeutic approaches proved ineffective in reducing tachypnea, including anti-inflammatory therapy with systemic triamcinolone acetonide, bronchodilatory therapy with levalbuterol, or antiviral therapy with zanamivir. These results, together with the pathologic observations, suggest that early disruption of the lower respiratory tract epithelium is a major component of the pathophysiology of influenza infection. Therapeutic approaches need to be tailored to clear airway obstruction and restore an intact epithelium

  4. Research Progress of Non-steroidal Anti-inflammatory Drugs on Ankylosing Spondylitis%非甾体抗炎药治疗强直性脊柱炎研究进展

    Institute of Scientific and Technical Information of China (English)

    杨瑾; 于锋

    2012-01-01

    Non -steroidal anti -Inflammatory drugs (NSAIDs) always play an important role in the treatment of ankylosing spondylitis, but people still have questions about how to properly use them. In this paper, a review of studies about the effect of NSAIDs on ankylosing spondylitis is presented in details, in order to offer references for their rational applications.%非甾体抗炎药在强直性脊柱炎的治疗中一直占有重要位置,但人们对于其合理使用还一直存在疑问,本文将近几年国内外非甾体抗炎药治疗强直性脊柱炎的研究文献进行分析、总结,以期为临床的合理使用提供参考.

  5. Analytical strategy for the confirmatory analysis of the non-steroidal anti-inflammatory drugs firocoxib, propyphenazone, ramifenazone and piroxicam in bovine plasma by liquid chromatography tandem mass spectrometry.

    Science.gov (United States)

    Dowling, Geraldine; Malone, Edward

    2011-09-10

    A sensitive and selective method for the simultaneous determination of non-steroidal anti-inflammatory drugs in bovine plasma was developed. Confirmatory analysis was carried out by liquid chromatography coupled with an electrospray ionisation tandem mass spectrometer (LC-ESI-MS/MS). Target compounds were acidified in plasma and extracted with acetonitrile. Sodium chloride was added to assist separation of the plasma and acetonitrile mixture. The acetonitrile extract is then subjected to liquid-liquid purification by the addition of hexane. Accuracy of the methods in plasma was between 93 and 102%. The precision of the method for the basic NSAIDs in plasma expressed as % RSD, for the within-laboratory reproducibility was less than 10%. Decision limit (CCα values) and detection capability (CCβ) values were established. The methods were validated according to Commission Decision 2002/657/EC. PMID:21684706

  6. Prescription Nonsteroidal Anti-Inflammatory Medicines

    Science.gov (United States)

    MENU Return to Web version Prescription Nonsteroidal Anti-Inflammatory Medicines Prescription Nonsteroidal Anti-Inflammatory Medicines How do prescription nonsteroidal anti-inflammatory drugs work? Nonsteroidal anti-inflammatory drugs (also called NSAIDs) stop cyclooxygenase ...

  7. Anti-inflammatory Activity.

    Science.gov (United States)

    2016-01-01

    Inflammation is the body's first response to infection or injury and is critical for both innate and adaptive immunity. It can be considered as part of the complex biological response of vascular tissues to harmful stimuli such as pathogens, damaged cells, or irritants. The search for natural compounds and phytoconstituents that are able to interfere with these mechanisms by preventing a prolonged inflammation could be useful for human health. Here, the anti-inflammatory properties of plant-based drugs are put together with both in vitro and acute (carrageenan, egg albumin and croton oil) and chronic (cotton pellet) in vivo models. PMID:26939273

  8. Molecular interactions between some non-steroidal anti-inflammatory drugs (NSAID's) and bovine (BSA) or human (HSA) serum albumin estimated by means of isothermal titration calorimetry (ITC) and frontal analysis capillary electrophoresis (FA/CE).

    Science.gov (United States)

    Ràfols, Clara; Zarza, Sílvia; Bosch, Elisabeth

    2014-12-01

    The interactions between some non-steroidal anti-inflammatory drugs, NSAIDs, (naproxen, ibuprofen and flurbiprofen) and bovine (BSA) or human (HSA) serum albumin have been examined by means of two complementary techniques, isothermal titration calorimetry (ITC) and frontal analysis/capillary electrophoresis (FA/CE). It can be concluded that ITC is able to measure with high precision the strongest drug-albumin interactions but the higher order interactions can be better determined by means of FA/CE. Then, the combination of both techniques leads to a complete evaluation of the binding profiles between the selected NSAIDs and both kind of albumin proteins. When BSA is the binding protein, the NSAIDs show a strong primary interaction (binding constants: 1.5 × 10(7), 8 × 10(5) and 2 × 10(6) M(-1) for naproxen, ibuprofen and flurbiprofen, respectively), and also lower affinity interactions of the same order for the three anti-inflammatories (about 1.7 × 10(4) M(-1)). By contrast, when HSA is the binding protein two consecutive interactions can be observed by ITC for naproxen (9 × 10(5) and 7 × 10(4) M(-1)) and flurbiprofen (5 × 10(6) and 6 × 10(4) M(-1)) whereas only one is shown for ibuprofen (9 × 10(5) M(-1)). Measurements by FA/CE show a single interaction for each drug being the ones of naproxen and flurbiprofen the same that those evaluated by ITC as the second interaction events. Then, the ability of both techniques as suitable complementary tools to establish the whole interaction NSAIDs-albumin profile is experimentally demonstrated and allows foreseeing suitable strategies to establish the complete drug-protein binding profile. In addition, for the interactions analyzed by means of ITC, the thermodynamic signature is established and the relative contributions of the enthalpic and entropic terms discussed.

  9. Aging Enables Ca2+ Overload and Apoptosis Induced by Amyloid-β Oligomers in Rat Hippocampal Neurons: Neuroprotection by Non-Steroidal Anti-Inflammatory Drugs and R-Flurbiprofen in Aging Neurons.

    Science.gov (United States)

    Calvo-Rodríguez, María; García-Durillo, Mónica; Villalobos, Carlos; Núñez, Lucía

    2016-07-22

    The most important risk factor for Alzheimer's disease (AD) is aging. Neurotoxicity in AD has been linked to dyshomeostasis of intracellular Ca2+ induced by small aggregates of the amyloid-β peptide 1-42 (Aβ42 oligomers). However, how aging influences susceptibility to neurotoxicity induced by Aβ42 oligomers is unknown. In this study, we used long-term cultures of rat hippocampal neurons, a model of neuronal in vitro aging, to investigate the contribution of aging to Ca2+ dishomeostasis and neuron cell death induced by Aβ42 oligomers. In addition, we tested whether non-steroidal anti-inflammatory drugs (NSAIDs) and R-flurbiprofen prevent apoptosis acting on subcellular Ca2+ in aged neurons. We found that Aβ42 oligomers have no effect on young hippocampal neurons cultured for 2 days in vitro (2 DIV). However, they promoted apoptosis modestly in mature neurons (8 DIV) and these effects increased dramatically after 13 DIV, when neurons display many hallmarks of in vivo aging. Consistently, cytosolic and mitochondrial Ca2+ responses induced by Aβ42 oligomers increased dramatically with culture age. At low concentrations, NSAIDs and the enantiomer R-flurbiprofen lacking anti-inflammatory activity prevent Ca2+ overload and neuron cell death induced by Aβ42 oligomers in aged neurons. However, at high concentrations R-flurbiprofen induces apoptosis. Thus, Aβ42 oligomers promote Ca2+ overload and neuron cell death only in aged rat hippocampal neurons. These effects are prevented by low concentrations of NSAIDs and R-flurbiprofen acting on mitochondrial Ca2+ overload.

  10. Efficacy of triple therapy and sequential therapy in the eradication of Helicobacter pylor in patients receiving long-term non-steroidal anti-inflammatory drugs treatnent

    Institute of Scientific and Technical Information of China (English)

    黄鑫薪

    2013-01-01

    Objective To explore the efficacy of triple therapy and sequential therapy in the eradication of Helicobacter pylori(Hp) in patients receiving long-term non-steroidal antiinflammatorv drugs(NSAID) treatment. Methods Patients receiving long-term NSAID treatment were enrolled

  11. Analysis of non-steroidal anti-inflammatory drugs in milk using QuEChERS and liquid chromatography coupled to mass spectrometry: triple quadrupole versus Q-Orbitrap mass analyzers.

    Science.gov (United States)

    Rúbies, Antoni; Guo, Lili; Centrich, Francesc; Granados, Mercè

    2016-08-01

    We developed a Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS) method for the high throughput determination of 10 non-steroidal anti-inflammatory drugs (NSAIDs) in milk samples using high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) with a triple quadrupole (QqQ) instrument and an electrospray ionization (ESI) source. The new extraction procedure is highly efficient, and we obtained absolute recoveries in the range 78.1-97.1 % for the extraction and clean-up steps. Chromatographic separation is performed in the gradient mode with a biphenyl column and acidic mobile phases consisting of water and acetonitrile containing formic acid. The chromatographic run time was about 12 min, and NSAID peaks showed a good symmetry factor. For MS/MS detection, we used multiple reaction monitoring (MRM) mode, using ESI in both positive and negative modes. Our method has been validated in compliance with the European Commission Decision 657/2002/EC, and we obtained very satisfactory results in inter-laboratory testing. Furthermore, we explored the use of a hybrid high resolution mass spectrometer, combining a quadrupole and an Orbitrap mass analyzer, for high resolution (HR) MS/MS detection of NSAIDs. We achieved lower NSAID quantification limits with Q-Orbitrap high resolution mass spectrometry (HRMS/MS) detection than those achieved with the QqQ instrument; however, its main feature is its very high selectivity, which makes HRMS/MS particularly suitable for confirmatory analysis. PMID:27325465

  12. 非甾体类抗炎药物对骨折愈合影响的研究进展%The Effect of Non-Steroidal Anti-Inflammatory Drugs on the Bone Fracture Healing Progress

    Institute of Scientific and Technical Information of China (English)

    陈坚; 李义凯; 张佩

    2014-01-01

    Non-steroidal anti-inflammatory drugs(NSAIDs)are widely used in clinical,especial y selective cyclo-oxygenase-2(COX-2) inhibitors,having less gastrointestinal adverse effects.However,recently some studies showing the drugs may delay the bone frature healing progress have raised concerns.Use of NSAIDs in the treatment of pain, heterotopic ossification,ankylosing spondylitis should be cautious,keeping in mind its benefits and adverse.The purpose of the present review article is thorough review and analysis the animal studies and clinical trials.%非甾体类抗炎药物在临床上广泛应用,特别是对胃肠道副作用小的环氧化酶-2(COX-2)抑制剂,但近年一些研究显示,其可能会延缓骨折的愈合过程,引起了临床医生的注意,镇痛、异位骨化、强直性脊柱炎的治疗策略可能会发生改变。本文通过文献回顾,就目前可获得动物或者临床观察数据结果作一综述。

  13. The pharmacology and activity of non-steroidal anti-inflammatory drugs (NSAIDs: a review of their use as an adjuvant treatment in patients with HBV and HCV chronic hepatitis

    Directory of Open Access Journals (Sweden)

    Sirio Fiorino

    2013-03-01

    Full Text Available Introduction: Different DNA and RNA viruses exploit common strategies to support their persistence and replication in infected individuals. In particular, the hepatitis B virus (HBV and the hepatitis C virus (HCV cause major health problems worldwide. These pathogens exert an immunosuppressive role by inducing the persistent activation of cyclooxygenase-2 (COX-2 and an increased synthesis of prostaglandin E2 (PGE2. The suppression of this proinflammatory network by non-steroidal anti-inflammatory drugs (NSAIDs has been proposed as a therapeutic approach to decrease viral replication. Materials and methods: In this review, the role of inflammation in the support of viral replication and NSAIDs and ketoprofen pharmacology are briefly discussed. In addition, studies that have investigated the use of NSAIDs for the treatment of HBV and HCV chronic hepatitis, which were identified by a systematic literature search of PubMed and MEDLINE, are reported. Results: To date, pegylated-interferon (PEG-IFN and/or nucleot(side analogues and PEG-IFN and ribavirin remain the standard therapy for HBV and HCV chronic hepatitis, respectively. Discussion: The use of NSAIDs in patients with chronic viral hepatitis has only a ‘‘historical’’ interest. Nevertheless, the possible usefulness of ketoprofen with PEG-IFN and ribavirin for HCVinfected patients, non-responders to standard therapy or with genotype 1, should be evaluated in future clinical studies.

  14. Anti-inflammatory management for tendon injuries - friends or foes?

    Directory of Open Access Journals (Sweden)

    Chan Kai-Ming

    2009-10-01

    Full Text Available Abstract Acute and chronic tendon injuries are very common among athletes and in sedentary population. Most physicians prescribe anti-inflammatory managements to relieve the worst symptoms of swelling and pain, including non-steroidal anti-inflammatory drugs, corticosteroids and physical therapies. However, experimental research shows that pro-inflammatory mediators such as prostaglandins may play important regulatory roles in tendon healing. Noticeably nearly all cases of chronic tendon injuries we treat as specialists have received non-steroidal anti-inflammatory drugs by their physician, suggesting that there might be a potential interaction in some of these cases turning a mild inflammatory tendon injury into chronic tendinopathy in predisposed individuals. We are aware of the fact that non-steroidal anti-inflammatory drugs and corticosteroids may well have a positive effect on the pain control in the clinical situation whilst negatively affect the structural healing. It follows that a comprehensive evaluation of anti-inflammatory management for tendon injuries is needed and any such data would have profound clinical and health economic importance.

  15. Altered membrane lipid dynamics and chemoprevention by non-steroidal anti inflammatory drugs during colon carcinogenesis Alteración de la dinámica de los lípidos de membrana y quimioprevención mediante los fármacos antiinflamatorios no esteroideos en la carcinogénesis de colon

    OpenAIRE

    S. Singh Kanwar; V. Vaish; S. Nath Sanya

    2011-01-01

    The present work focuses on the anti-neoplastic role of non steroidal anti-inflammatory drugs (NSAIDs) in modulating the biophysical parameters of the colonic membranes in 1,2-dimethylhydrazine dihydrochloride (DMH) induced carcinogenesis. The steady-state fluorescence polarization technique was applied to assess membrane fluidity, membrane polarity and lipid phase states. The decline in cholesterol content, biosynthesis and cholesterol: phospholipids ratio with DMH treatment indicates more f...

  16. A cluster randomised stepped wedge trial to evaluate the effectiveness of a multifaceted information technology-based intervention in reducing high-risk prescribing of non-steroidal anti-inflammatory drugs and antiplatelets in primary medical care: the DQIP study protocol

    OpenAIRE

    Dreischulte Tobias; Grant Aileen; Donnan Peter; McCowan Colin; Davey Peter; Petrie Dennis; Treweek Shaun; Guthrie Bruce

    2012-01-01

    Abstract Background High-risk prescribing of non-steroidal anti-inflammatory drugs (NSAIDs) and antiplatelet agents accounts for a significant proportion of hospital admissions due to preventable adverse drug events. The recently completed PINCER trial has demonstrated that a one-off pharmacist-led information technology (IT)-based intervention can significantly reduce high-risk prescribing in primary care, but there is evidence that effects decrease over time and employing additional pharmac...

  17. Lansoprazole prevents experimental gastric injury induced by non-steroidal anti-inflammatory drugs through a reduction of mucosal oxidative damage

    Institute of Scientific and Technical Information of China (English)

    Corrado Blandizzi; Matteo Fornai; Rocchina Colucci; Gianfranco Natale; Valter Lubrano; Cristina Vassalle; Luca Antonioli; Gloria Lazzeri; Mario Del Tacca

    2005-01-01

    AIM: This study investigated the mechanisms of protection afforded by the proton pump inhibitor lansoprazole against gastric injury induced by different non-steroidal antiinflammatory drugs (NSAIDs) in rats.METHODS: Male Sprague-Dawley rats were orally treated with indomethacin (100 μmol/kg), diclofenac (60 μmol/kg),piroxicam (150 μmol/kg) or ketoprofen (150 μmol/kg).Thirty minutes before NSAIDs, animals were orally treated with lansoprazole 18 or 90 μmol/kg. Four hours after the end of treatments, the following parameters were assessed: gastric mucosal PGE2, malondialdehyde (MDA), myeloperoxidase (MPO) or non-proteic sulfhydryl compounds (GSH) levels; reverse transcription-polymerase chain reaction (RT-PCR) of mucosal COX-2 mRNA; gastric acid secretion in pylorus-ligated animals; in vitro effects of lansoprazole (1-300 μmol/L) on the oxidation of low density lipoproteins (LDLs) induced by copper sulphate.RESULTS: All NSAIDs elicited mucosal necrotic lesions which were associated with neutrophil infiltration and reduction of PGE2 levels. Increments of MPO and MDA contents, as well as a decrease in GSH levels were detected in the gastric mucosa of indomethacin- or piroxicam-treated animals. Indomethacin enhanced mucosal cyclooxygenase-2 expression, while not affecting cyclooxygenase-1. At the oral dose of 18 μmol/kg lansoprazole partly counteracted diclofenac-induced mucosal damage, whereas at 90 μmol/kg it markedly prevented injuries evoked by all test NSAIDs. Lansoprazole at 90 μmol/kg reversed also the effects of NSAIDs on MPO, MDA and GSH mucosal contents, without interfering with the decrease in PGE2 levels or indomethacin-induced cyclooxygenase-2 expression. However, both lansoprazole doses markedly inhibited acid secretion in pylorus-ligated rats. Lansoprazole concentration-dependently reduced the oxidation of LDLs in vitro.CONCLUSION: These results suggest that, besides the inhibition of acid secretion, lansoprazole protection against NSAID

  18. Gas chromatography-flame ionization determination of benzaldehyde in non-steroidal anti-inflammatory drug injectable formulations using new ultrasound-assisted dispersive liquid-liquid micro extraction

    International Nuclear Information System (INIS)

    Summary: In this study, simple and efficient ultrasound-assisted dispersive liquid-liquid micro extraction combined with gas chromatography (GC) was developed for the preconcentration and determination of benzaldehyde in injectable formulations of the non-steroidal anti-inflammatory drugs, diclofenac, Vitamin B-complex and Voltaren injection solutions. Fourteen microliters of toluene was injected slowly into 10 mL home-designed centrifuge glass vial containing an aqueous sample without salt addition that was located inside the ultrasonic water bath. The formed emulsion was centrifuged and 2 macro L of separated toluene was injected into a gas chromatographic system equipped with a flame ionization detector (GC-FID) for analysis. Several factors influencing the extraction efficiency as the nature and volume of organic solvent, extraction temperature, ionic strength and centrifugation time were investigated and optimized. Using optimum extraction conditions a detection limit of 0.3 macro g L/sup -1/ and a good linearity in a calibration range of 2.0-1000 macro g L/sup -1/ were achieved for analyte. This proposed method was successfully applied to the analysis of benzaldehyde in three injection formulations and relative standard deviation (RSD) of analysis (n=3), before spiking with standard benzaldehyde were 3.3, 2.0 and 1.3% for Na-diclofenac, vitamin B-complex and voltaren, respectively and after spiking of standard benzaldehyde (0.3 mg L/sup -1/), the RSD were 6.5, 3.6 and 2.8% for Na-diclofenac, vitamin B-complex and voltaren, respectively. (author)

  19. Demographic, medical, and behavioral characteristics associated with over the counter non-steroidal anti-inflammatory drug use in a population based cohort: results from the Multi-Ethnic Study of Atherosclerosis

    Science.gov (United States)

    Delaney, Joseph A C; Biggs, Mary L.; Kronmal, Richard A; Psaty, Bruce M

    2010-01-01

    Background Three types of non-steroidal anti-inflammatory drugs (NSAIDs) can be obtained both over the counter (OTC) and by prescription in the United States. OTC NSAID use is not recorded in prescription claims databases; this might lead to differential misclassification of NSAID exposure status in studies that use computerized pharmacy databases to study NSAID use. Objective To evaluate characteristics of OTC versus prescription NSAID users Methods This analysis is set within the Multi-Ethnic Study of Atherosclerosis (MESA) study; a prospective cohort study of 6,814 adults from 4 ethnic groups (European descent, Asian, African-American and Hispanic) with a mean age of 62 years. The cohort was restricted to those who initiated NSAID use (aspirin, ibuprofen or naproxen) during follow-up. We compared information about age, sex, ethnicity, body mass index, smoking, diabetes, medication use, education, income, health insurance status and exercisebetween groups. Results OTC NSAID use was prevalent at baseline (25% Aspirin, 9% Ibuprofen, 2% Naproxen). Compared to prescribed NSAID use, OTC NSAID use was lower for users of non-European descent for all classes: aspirin (p<0.0001), ibuprofen (p<0.0001) and naproxen (p=0.0094). For aspirin, differences were seen for male gender (Relative Risk (RR):0.92; 95%(Confidence interval) CI:0.86–0.98), use of lipid lowering drugs (RR:0.88; 95% CI: 0.80–0.96), low income (RR:0.89; 95%CI:0.81–0.97), and participants one standard deviation above average in intentional exercise (RR:1.03; 95%CI:1.01–1.05). Conclusions OTC NSAID use is prevalent in an older multi-ethnic population and OTC users differ from prescription NSAID users. Caution should be exercised when using prescribed NSAIDs as a proxy for NSAID use. PMID:21182156

  20. Concurrent use of diuretics, angiotensin converting enzyme inhibitors, and angiotensin receptor blockers with non-steroidal anti-inflammatory drugs and risk of acute kidney injury: nested case-control study

    Science.gov (United States)

    Lapi, Francesco; Azoulay, Laurent; Yin, Hui; Nessim, Sharon J

    2013-01-01

    Objectives To assess whether a double therapy combination consisting of diuretics, angiotensin converting enzyme inhibitors, or angiotensin receptor blockers with addition of non-steroidal anti-inflammatory drugs (NSAIDs) and the triple therapy combination of two of the aforementioned antihypertensive drugs to which NSAIDs are added are associated with an increased risk of acute kidney injury. Design Retrospective cohort study using nested case-control analysis. Setting General practices contributing data to the UK Clinical Practice Research Datalink linked to the Hospital Episodes Statistics database. Participants A cohort of 487 372 users of antihypertensive drugs. Main outcome measures Rate ratios with 95% confidence intervals of acute kidney injury associated with current use of double and triple therapy combinations of antihypertensive drugs with NSAIDs. Results During a mean follow-up of 5.9 (SD 3.4) years, 2215 cases of acute kidney injury were identified (incidence rate 7/10 000 person years). Overall, current use of a double therapy combination containing either diuretics or angiotensin converting enzyme inhibitors or angiotensin receptor blockers with NSAIDs was not associated with an increased rate of acute kidney injury. In contrast, current use of a triple therapy combination was associated with an increased rate of acute kidney injury (rate ratio 1.31, 95% confidence interval 1.12 to 1.53). In secondary analyses, the highest risk was observed in the first 30 days of use (rate ratio 1.82, 1.35 to 2.46). Conclusions A triple therapy combination consisting of diuretics with angiotensin converting enzyme inhibitors or angiotensin receptor blockers and NSAIDs was associated with an increased risk of acute kidney injury. The risk was greatest at the start of treatment. Although antihypertensive drugs have cardiovascular benefits, vigilance may be warranted when they are used concurrently with NSAIDs. PMID:23299844

  1. Screening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation.

    Science.gov (United States)

    Maurer, H H; Tauvel, F X; Kraemer, T

    2001-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used as analgesic and anti-rheumatic drugs, and they are often misused. A gas chromatographic-mass spectrometric (GC-MS) screening procedure was developed for their detection in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons after extractive methylation. The compounds were separated by capillary GC and identified by computerized MS in the full-scan mode. Using mass chromatography with the ions m/z 119, 135, 139, 152, 165, 229, 244, 266, 272, and 326, the possible presence of NSAIDs and their metabolites could be indicated. The identity of positive signals in such mass chromatograms was confirmed by comparison of the peaks underlying full mass spectra with the reference spectra recorded during this study. This method allowed the detection of therapeutic concentrations of acemetacin, acetaminophen (paracetamol), acetylsalicylic acid, diclofenac, diflunisal, etodolac, fenbufen, fenoprofen, flufenamic acid, flurbiprofen, ibuprofen, indometacin, kebuzone, ketoprofen, lonazolac, meclofenamic acid, mefenamic acid, mofebutazone, naproxen, niflumic acid, phenylbutazone, suxibuzone, tiaprofenic acid, tolfenamic acid, and tolmetin in urine samples. The overall recoveries of the different NSAIDs ranged between 50 and 80% with coefficients of variation of less than 15% (n = 5), and the limits of detection of the different NSAIDs were between 10 and 50 ng/mL (S/N = 3) in the full-scan mode. Extractive methylation has proved to be a versatile method for STA of various acidic drugs, poisons, and their metabolites in urine. It has also successfully been used for plasma analysis.

  2. Use of non-steroidal anti-inflammatory drugs that elevate cardiovascular risk: an examination of sales and essential medicines lists in low-, middle-, and high-income countries.

    Directory of Open Access Journals (Sweden)

    Patricia McGettigan

    Full Text Available BACKGROUND: Certain non-steroidal anti-inflammatory drugs (NSAIDs (e.g., rofecoxib [Vioxx] increase the risk of heart attack and stroke and should be avoided in patients at high risk of cardiovascular events. Rates of cardiovascular disease are high and rising in many low- and middle-income countries. We studied the extent to which evidence on cardiovascular risk with NSAIDs has translated into guidance and sales in 15 countries. METHODS AND FINDINGS: Data on the relative risk (RR of cardiovascular events with individual NSAIDs were derived from meta-analyses of randomised trials and controlled observational studies. Listing of individual NSAIDs on Essential Medicines Lists (EMLs was obtained from the World Health Organization. NSAID sales or prescription data for 15 low-, middle-, and high-income countries were obtained from Intercontinental Medical Statistics Health (IMS Health or national prescription pricing audit (in the case of England and Canada. Three drugs (rofecoxib, diclofenac, etoricoxib ranked consistently highest in terms of cardiovascular risk compared with nonuse. Naproxen was associated with a low risk. Diclofenac was listed on 74 national EMLs, naproxen on just 27. Rofecoxib use was not documented in any country. Diclofenac and etoricoxib accounted for one-third of total NSAID usage across the 15 countries (median 33.2%, range 14.7-58.7%. This proportion did not vary between low- and high-income countries. Diclofenac was by far the most commonly used NSAID, with a market share close to that of the next three most popular drugs combined. Naproxen had an average market share of less than 10%. CONCLUSIONS: Listing of NSAIDs on national EMLs should take account of cardiovascular risk, with preference given to low risk drugs. Diclofenac has a risk very similar to rofecoxib, which was withdrawn from worldwide markets owing to cardiovascular toxicity. Diclofenac should be removed from EMLs.

  3. COMPARATIVE STUDY OF ANTI-INFLAMMATORY ACTIVITY OF NEWER MACROLIDES WITH ETORICOXIB

    Directory of Open Access Journals (Sweden)

    Gajendra Naidu

    2014-03-01

    Full Text Available The present study was designed to investigate the anti-inflammatory activity of macrolides and to compare with standard non- steroidal anti-inflammatory drug (NSAID etoricoxib. This study was conducted in male wistar albino rats by inducing edema with 1% carrageenan. Animals were divided into 5 groups with 6 in each and paw edema volume was measured by digital plethysmograph before and 3hrs after 1% carrageenan administration. Percentage of inhibition of paw edema was calculated. Results showed macrolides having significant anti-inflammatory activity & the anti-inflammatory activity of roxithromycin was almost equally comparable with etoricoxib

  4. Enhancement of antinociception by coadminstration of minocycline and a non-steroidal anti-inflammatory drug indomethacin in naïve mice and murine models of LPS-induced thermal hyperalgesia and monoarthritis

    Directory of Open Access Journals (Sweden)

    Masocha Willias

    2010-12-01

    Full Text Available Abstract Background Minocycline and a non-steroidal anti-inflammatory drug (NSAID indomethacin, have anti-inflammatory activities and are both used in the management of rheumatoid arthritis. However, there are no reports on whether coadministration of these drugs could potentiate each other's activities in alleviating pain and weight bearing deficits during arthritis. Methods LPS was injected to BALB/c mice intraperitoneally (i.p. to induce thermal hyperalgesia. The hot plate test was used to study thermal nociception in naïve BALB/c and C57BL/6 mice and BALB/c mice with LPS-induced thermal hyperalgesia and to evaluate antinociceptive effects of drugs administered i.p. Monoarthritis was induced by injection of LPS intra-articularly into the right hind (RH limb ankle joint of C57BL/6 mice. Weight bearing changes and the effect of i.p. drug administration were analyzed in freely moving mice using the video-based CatWalk gait analysis system. Results In naïve mice indomethacin (5 to 50 mg/kg had no significant activity, minocycline (25 to 100 mg/kg produced hyperalgesia to thermal nociception, however, coadministration of minocycline 50 mg/kg with indomethacin 5 or 10 mg/kg produced significant antinociceptive effects in the hot plate test. A selective inhibitor of COX-1, FR122047 (10 mg/kg and a selective COX-2 inhibitor, CAY10404 (10 mg/kg had no significant antinociceptive activities to thermal nociception in naïve mice, however, coadministration of minocycline, with CAY10404 but not FR122047 produced significant antinociceptive effects. In mice with LPS-induced hyperalgesia vehicle, indomethacin (10 mg/kg or minocycline (50 mg/kg did not produce significant changes, however, coadministration of minocycline plus indomethacin resulted in antinociceptive activity. LPS-induced RH limb monoarthritis resulted in weight bearing (RH/left hind (LH limb paw pressure ratios and RH/LH print area ratios deficits. Treatment with indomethacin (1 mg/kg or

  5. Nonsteroid Anti-inflammatory Drugs and Kidney

    Directory of Open Access Journals (Sweden)

    Yaşar Yıldırım1

    2016-03-01

    Full Text Available Non-steroidal anti-inflammatory drugs (NSAIDs are often used in the treatment of chronic and acute pain and inflammation as an analgesic and anti-inflammatory agent. They inhibit the synthesis of prostaglandins which have influence on glomerular capillaries, vasa recta and tubular functions. They lead to significant complications such as hyperkalemia, hyponatremia, edema and hypertension. Usage of NSAIDs is a risk factor for acute kidney injury in some conditions such as advanced age, dehydration, vomiting, diuretics, ACE/ARB therapy, heart failure, nephrotic syndrome, cirrhosis and chronic kidney disease. Acute interstitial nephritis is not dependent on the drug dose and it is characterized by immunological inflammatory reaction and a decrease in creatinine clearance. Besides the classical findings, glomerules can be involved and minimal change disease or membranous glomerulonephritis can develop. Analgesic nephropathy is characterized by interstitial nephritis and papillary necrosis. Metabolites of NSAIDs are accumulated in renal medulla which has lowest oxygen pressure in kidney and they disrupt the renal parencymal perfusion by vasoconstriction. Respectively, papillar necrosis, glomerular sclerosis, interstitial fibrosis and cortical atrophy can develop insidiously.

  6. Simultaneous analysis of non-steroidal anti-inflammatory drugs and estrogenic hormones in water and wastewater samples using gas chromatography-mass spectrometry and gas chromatography with electron capture detection

    Energy Technology Data Exchange (ETDEWEB)

    Migowska, Natalia; Caban, Magda; Stepnowski, Piotr; Kumirska, Jolanta, E-mail: kumirska@chem.univ.gda.pl

    2012-12-15

    Non-steroidal anti-inflammatory drugs are the group of pharmaceuticals that is most often found in the environment, whereas estrogenic hormones are considered to be potent endocrine disruptors. However, the fate and persistence of these compounds in the environment are still unclear. In this study we propose two approaches for determining these compounds in environmental water samples: GC-MS using time windows and operating in selected ion-monitoring mode (SIM) and, for the first time, gas chromatography with electron capture detection (GC-ECD). The identification criteria of both methods fulfilled the requirements of Directive 2002/657/EC. The use of time windows improved the sensitivity of GC-MS measurements. In GC-MS analysis the pharmaceuticals were determined as trimethylsilyl, in GC-ECD as pentafluoropropionyl derivatives. The influence of such parameters as the type of reagent, type of solvent, reaction time, reaction temperature and microwave irradiation in a household microwave oven on the efficacy of silylation was investigated. Derivatization using N,O-bis(trimethylsilyl)trifluoroacetamide (BSTFA) and 1% trimethylchlorosilane (TMCS) in pyridine (1:1, v/v) for 30 min in 60 Degree-Sign C was found to be optimal. Optimization of the solid phase extraction procedure (SPE) confirmed that the application of Oasis HLB cartridges, the acidification of loading samples to pH 2 and the use of methanol as eluent gave the best absolute recoveries (ARs) of the target compounds. The following ARs of all the compounds were achieved: 58.2-106.8% in influent wastewater, 77.8-103.4% in effluent wastewater and 81.2-101.9% in surface water samples. Validation of the SPE-GC-MS method enables 13 pharmaceuticals to be determined with MDLs between 3.3 and 343.6 ng/L, depending on the analytes and matrices. GC-ECD analysis enables the determination of 6 pharmaceuticals in surface water samples with MDLs between 0.7 and 5.4 ng/L. The proposed methods were successfully used for

  7. 非甾体类抗炎药与消化道肿瘤的化学预防%Non-steroidal Anti-inflammatory Drugs and Chemoprevention of Digestive Cancer

    Institute of Scientific and Technical Information of China (English)

    魏文强; 乔友林

    2001-01-01

    Recent epidemiology and laboratory studies indicate that regular taking of aspirin and other non-steroidal anti-inflammatory drugs(NSAIDs) may reduce the risk of colorectal, esophageal, stomach and pancreatic cancers and other digestive cancers. Thus, aspirin and other NSAIDs may be an effective chemoprevention agent for digestive cancers. On the other hand, this protection effort may be benefitial to the course of the intervention, regression and prevention of cancer lesions. The possible mechanism of NSAIDs chemoprevention may be: (1)reducing the synthesis of prostaglandin(PG) and inhibiting cyclo-oxygenase(COX) activity; (2) inducing apoptosis in epithelial cells of the gastro-intestinal origin; (3)obstructing signaling transduction pathways of COX and PG. Now, chemoprevention of NSAIDs has become focus of research on cancer secondary prevention, as its protective effects of chemoprevention of digesrive cancer have been determined. NSAIDs, especially selective COX-2 inhibitor may be a novel useful chemoprevention agents for digestive cancer and their precursor lesions in future.%近年来,流行病学及实验室研究表明,长期使用阿斯匹林或其它非甾体类抗炎药(NSAIDs),可降低结、直肠癌、食管癌、胃癌、胰腺癌等消化道肿瘤的发病危险性,提示NSAIDs可能对消化道肿瘤具有一定的化学预防作用。同时,这一保护作用也很有可能在肿瘤的前期病变过程中发挥有益的阻断、逆转或预防作用。NSAIDs化学预防作用的可能机制:(1)抑制前列腺素(PG)合成和细胞环氧化酶(COX)活性;(2)诱导胃肠道来源的上皮细胞凋亡;(3)引起PG和COX调节通路的障碍。目前,NSAIDs的化学预防作用已经成为肿瘤二级预防领域的研究热点并已基本肯定了它在消化道肿瘤预防中的作用。NSAIDs,尤其是特异性环氧化酶-2抑制剂,有望成为肿瘤以及癌前病变新的化学预防的药物。

  8. Simultaneous analysis of non-steroidal anti-inflammatory drugs and estrogenic hormones in water and wastewater samples using gas chromatography–mass spectrometry and gas chromatography with electron capture detection

    International Nuclear Information System (INIS)

    Non-steroidal anti-inflammatory drugs are the group of pharmaceuticals that is most often found in the environment, whereas estrogenic hormones are considered to be potent endocrine disruptors. However, the fate and persistence of these compounds in the environment are still unclear. In this study we propose two approaches for determining these compounds in environmental water samples: GC–MS using time windows and operating in selected ion-monitoring mode (SIM) and, for the first time, gas chromatography with electron capture detection (GC–ECD). The identification criteria of both methods fulfilled the requirements of Directive 2002/657/EC. The use of time windows improved the sensitivity of GC–MS measurements. In GC–MS analysis the pharmaceuticals were determined as trimethylsilyl, in GC–ECD as pentafluoropropionyl derivatives. The influence of such parameters as the type of reagent, type of solvent, reaction time, reaction temperature and microwave irradiation in a household microwave oven on the efficacy of silylation was investigated. Derivatization using N,O-bis(trimethylsilyl)trifluoroacetamide (BSTFA) and 1% trimethylchlorosilane (TMCS) in pyridine (1:1, v/v) for 30 min in 60 °C was found to be optimal. Optimization of the solid phase extraction procedure (SPE) confirmed that the application of Oasis HLB cartridges, the acidification of loading samples to pH 2 and the use of methanol as eluent gave the best absolute recoveries (ARs) of the target compounds. The following ARs of all the compounds were achieved: 58.2–106.8% in influent wastewater, 77.8–103.4% in effluent wastewater and 81.2–101.9% in surface water samples. Validation of the SPE–GC–MS method enables 13 pharmaceuticals to be determined with MDLs between 3.3 and 343.6 ng/L, depending on the analytes and matrices. GC–ECD analysis enables the determination of 6 pharmaceuticals in surface water samples with MDLs between 0.7 and 5.4 ng/L. The proposed methods were successfully

  9. The attitudes of owners and veterinary professionals in the United Kingdom to the risk of adverse events associated with using non-steroidal anti-inflammatory drugs (NSAIDs) to treat dogs with osteoarthritis.

    Science.gov (United States)

    Belshaw, Zoe; Asher, Lucy; Dean, Rachel S

    2016-09-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed by veterinary surgeons for the treatment of canine osteoarthritis, and affected dogs may receive these drugs for long periods of time. Whilst short term administration of NSAIDs to dogs is linked to adverse events such as gastrointestinal haemorrhage and renal injury, reports of adverse events associated with their long-term administration are limited in the veterinary literature. This study aimed to investigate the attitudes towards the long term use of NSAIDs for canine osteoarthritis held by three groups who manage osteoarthritic dogs in the United Kingdom: dog owners, veterinary surgeons and veterinary nurses. A qualitative methodology was adopted, using semi-structured interviews and focus groups. Thematic analysis of these data identified three themes: awareness of potential risks; recognition of adverse events; and influence of risk perception on the use of NSAIDs. Awareness of, and concern about, the risk of adverse events associated with NSAID administration to dogs with osteoarthritis was high in all groups, with veterinary surgeons being one of a variety of information sources used by owners to acquire this knowledge. Veterinary surgeons described difficulty in recognising, managing and avoiding adverse events associated with NSAIDs. When adverse events occurred, a wide range of management approaches were adopted ranging from a brief drug respite to permanent cessation of administration of any NSAIDs to that dog. Commonly employed approaches to minimise risk included dose reduction and screening blood tests. This study describes a high level of concern about the risks associated with long term NSAID administration to dogs with osteoarthritis and highlights a diverse range of strategies employed to minimise these risks. The evidence base for these strategies is poor, and this may present a risk to animal welfare if the affected dogs are not receiving adequate analgesia. In order to

  10. 非甾体类抗炎药在牙周病治疗中的作用%Effect of non-steroidal anti-inflammatory drugs in the treatment of periodontal diseases

    Institute of Scientific and Technical Information of China (English)

    孙小娜; 宋爱梅; 杨丕山

    2014-01-01

    地诺前列酮是牙槽骨吸收最有力的刺激因子,既可刺激破骨细胞引起破骨性骨吸收,破坏牙周组织;还可提高缓激肽和组胺水平,引起疼痛的感觉。地诺前列酮与血栓素A2间失衡,会影响血管生成和组织愈合。非甾体类抗炎药(NSAID)可抑制人体内的环加氧酶活性,减少地诺前列酮的生成,从而降低牙周炎症,缓解疼痛;可引起内皮细胞通透性降低,影响急性期多种细胞的迁移;可抑制透明质酸的形成,从而影响细胞增殖。布洛芬缓释凝胶和米诺环素-布洛芬缓释凝胶均能有效地改善慢性牙周炎的临床症状,控制牙周炎症,减少组织破坏。NSAID用于牙周组织再生术治疗,对骨移植后的骨再生有明显的促进作用。NSAID对于牙周炎的治疗既有优势,也有不可忽视的缺点。NSAID会抑制血栓素A2的生成,减少血小板的聚集,从而增加患者血肿和持续出血的风险。牙周手术与此类药物怎样结合应用才能收到最佳效果,NSAID能否在牙周再生手术中起到促进作用仍需进一步探讨。%Dinoprostone is a powerful stimulating factor for alveolar bone resorption. It can destroy periodontal tissues by activating osteoclasts and cause pain by increasing the level of bradykinin and histamine. The imbalance between Dinoprostone and thromboxane A2 may influence angiogenesis and tissue healing. Non-steroidal anti-inflammatory drugs(NSAID) can reduce the production of Dinoprostone by inhibiting the clyco-oxygenase activity, thus decreasing the periodontal inflammation and relieving pain. It can also reduce the permeability of endothelial cells and influence cell migration during the acute inflammation period. It can inhibit the formation of hyaluronic acid and affect cell proliferation. Ibuprofen gel and minocycline-ibuprofen gel can improve the clinical symptoms of chronic periodontitis effectively and reduce tissue destruction

  11. Analysis of the Use of Non Steroidal Anti-inflammatory Drugs in 2011-2013%2011-2013年非甾体消炎药使用情况分析

    Institute of Scientific and Technical Information of China (English)

    左拥军; 李永兵

    2015-01-01

    目的:探讨2011—2013年非甾体消炎药(NSAIDs)的使用情况。方法收集2011年1月至2013年12月濮阳市人民医院信息系统(HIS)NSAIDs数据,包括药物名称、规格剂型、年销售量、销售金额等,统计NSAIDs的用药频度、日均费用。结果2011—2013年NSAIDs销售金额排序前3名的均为氨酚麻美干混悬剂、阿司匹林肠溶片、塞来昔布胶囊;2011—2013年NSAIDs DDDs排序前3位的均为阿司匹林肠溶片(进口)、阿司匹林肠溶片(国产)、塞来昔布胶囊;塞来昔布胶囊的DDC最高,其次为感冒灵颗粒;2011—2013年COX-1选择性抑制剂、非选择性COX抑制剂的销售金额、DDDs逐年增高;选择性COX-2抑制剂的销售金额、DDDs及DDC比较稳定。结论 NSAIDs使用基本合理,传统NSAIDs仍处于主导地位,特异性COX-2抑制剂等新型NSAIDs已广泛使用于临床治疗中,具有良好的应用前景。%Objective To investigate the use of non steroidal anti-inflammatory drugs (NSAIDs) in 2011-2013. Methods Col ect January 2011 to December 2013 Puyang People's Hospital information system (HIS) NSAIDs drug data,including drug name,specifications,annual sales,sales amount,etc,statistics NSAIDs drug use frequency,average daily cost.Results Before three sort of 2011—2013 NSAIDs drug sales amount are paracetamol and pseudoephe-drine dry suspension,aspirin and celecoxib capsules;2011—2013 NSAIDs DDDs of the both aspirin enteric coated tablets (imports),aspirin enteric coated tablets (made in China),celecoxib celecoxib capsules;celecoxib capsules DDC was the highest,fol owed by Ganmaoling granules;2011—2013 COX-1 selective inhibitor,non selective COX inhibitors of sales amount, DDDs increased year by year;selective COX-2 inhibitor of the consumption sum,DDDs and DDC value is stable. Conclusion NSAIDs drug use is basical y rational,traditional NSAIDs is stil in a dominant position,the specific COX-2 inhibitor and other new

  12. Application of quality control circle in reducing the adverse reaction of non-steroidal anti-inflammatory drugs in rheumatology department%品管圈在降低风湿科非甾体类抗炎药不良反应中的应用

    Institute of Scientific and Technical Information of China (English)

    蒋楠; 李晓兰; 刘秋玉; 冯子芸; 黄霞霞; 邓小虎

    2014-01-01

    Objective:To evaluate the effect of quality control circle activities in reducing the adverse reaction of non-steroidal anti-inflammatory drugs in rheumatology department. Methods: Quality control circle was set up and PDCA method was applied to analyze the cause of adverse reactions induced by non-steroidal anti-inflammatory drugs, and the corresponding improvement measures were formulated. Reducing adverse reactions associated with non-steroidal anti-inflammatory drugs in rheumatology department was set as the primary goal. Results:By improving the form and content of health education, admission assessment, offering physical and mental support, the occurrence rate of adverse reactions induced by non-steroidal anti-inlfammatory drug decreased from prior 17.1%to now 6.9%. Conclusion:Quality control circle activities reduced the occurrence rate of non-steroidal anti-inlfammatory drugs adverse reactions in rheumatology department and improved the medical security. Meanwhile, teamwork among colleagues was established in the process of data collecting and explaining, overall nursing care was applied well in clinic.%目的:探讨品管圈活动对降低风湿科非甾体类抗炎药不良反应的效果。方法:成立品管圈,运用PDCA法,以降低“风湿科非甾体类抗炎药不良反应”为主题,对发生不良反应的原因进行统计、分析,制定相应的改进措施。结果:通过观察并总结风湿科非甾体类抗炎药不良反应发生的原因,从健康教育的形式、内容、入院评估、身心并护等方面入手,使风湿科非甾体类抗炎药不良反应的发生率从活动前的17.1%降低至活动后的6.9%。结论:品管圈活动降低了风湿科非甾体类抗炎药不良反应的发生率,提高了用药安全性,培养了同事间的团队精神,使责任制整体护理更好的运用于临床工作中。

  13. Topical diclofenac versus dexamethasone after strabismus surgery: A double-blind randomized clinical trial of anti-inflammatory effect and ocular hypertensive response

    OpenAIRE

    Khan Hayat; Amitava Abadan

    2007-01-01

    Background: Compared to steroids non-steroidal anti-inflammatory drugs offer comparable anti-inflammatory action without ocular side-effects. Aim: To compare the anti-inflammatory effect and effect on IOP (Goldmann) of topical diclofenac 0.1% with dexamethasone 0.1% after strabismus surgery. Design: Prospective, randomized, double-blind, single-center, clinical trial. Materials and Methods: Forty-three cases of constant horizontal strabismus, qualifying for standard un...

  14. Topical ketorolac has no antinociceptive or anti-inflammatory effect in thermal injury

    DEFF Research Database (Denmark)

    Møiniche, S; Pedersen, J L; Kehlet, H

    1994-01-01

    This study investigated the antinociceptive and anti-inflammatory effect of a topical non-steroidal anti-inflammatory drug in human thermal injury. Twelve healthy unmedicated volunteers had identical burn injuries produced on the medial side of both calves with a 49 degrees C 15 x 25 mm thermode...... and MPDT, an increase in EI and development of mechanical hyperalgesia (P < 0.05). Ketorolac gel had no effect on any of the nociceptive or inflammatory variables studies (P > 0.2)....

  15. Chemopreventive response of diclofenac, a non-steroidal anti-inflammatory drug in experimental carcinogenesis Respuesta quimiopreventiva del diclofenaco, un fármaco antiinflamatorio no esteroideo en la carcinogénesis de colon experimental

    OpenAIRE

    M. Kaur Saini; J Kaur; Sharma, P.; S. Nath Sanyal

    2009-01-01

    The chemopreventive response was evaluated of nonsteroidal anti-inflammatory drug, Diclofenac, a preferential cyclooxygenase-2 (COX-2) inhibitor in 1,2-dimethyhydrazine (DMH)-induced colon cancer in rat model. The signs of neoplasm were evident in the animals receiving 30mg of DMH per kg body weight in a weekly s.c injection for six weeks. The putative biomarker of carcinogenesis was visible in the form of multiple plaque lesions in DMH treatment and then regression seen in those animals whic...

  16. Evaluation of anti-inflammatory activity of Strobilanthus callosus Nees and Strobilanthus ixiocephala Benth

    Directory of Open Access Journals (Sweden)

    Rupali Vitthal Sarpate

    2012-01-01

    Full Text Available Context: Strobilanthus callosus Nees and Strobilanthus ixiocephala Benth belongs to family Acanthaceae. The plants have been the subject of scientific research which confirms its use in folk medicine as anti-inflammatory drugs showing potent anti-rheumatic effects. Previous research claims the anti-inflammatory and anti-arthritic activities of Lupeol and 19α-H Lupeol isolated from Strobilanthus callosus and Strobilanthus ixiocephala roots. Based on the literature cited, the unexplored parts stems and leaves of the two species were selected for the present study. Aim: The present study is designed to isolate steroidal and alkaloidal components from the two species Strobilanthus callosus and Strobilanthus ixiocephala using the unexplored parts viz. stems and leaves and to investigate its anti-inflammatory effect. Settings and Design: The anti-inflammatory effect was investigated employing subacute anti-inflammatory models namely cotton pellet granuloma and carrageenan-induced rat paw edema. Materials and Methods: Anti-inflammatory activity was carried out using isolated test components RVS-A (Lupeol, RVS-C (Doctriacantone and standard drug Diclofenac sodium (10 mg/kg. Results: The present study has dealt up with isolation of two phytoconstituents Lupeol and Dotriacontane which gave marked anti-inflammatory activity at the dose 20 mg/kg in both the models Carrageenan induced rat paw edema and Cotton pellet granuloma. Conclusion: The results confirm that the mechanism of the anti-inflammatory effect of RVS-A (Lupeol and RVS-C (Doctriacantone involves reduction of prostaglandins through inhibition of cyclooxygenase and suppression of proliferative phase of sub acute inflammation. Thus the steroidal and alkaloidal components Lupeol and Doctriacantone isolated from Strobilanthus callosus Nees and Strobilanthus ixiocephala Benth shows marked anti-inflammatory activity.

  17. Anti-Inflammatories and Corticosteroids

    Science.gov (United States)

    ... with anabolic steroids and have often feared their use. Anabolic steroids are testosterone, or the male sex hormone. This hormone is also secreted by the adrenal cortex. This hormone is androgenic, ... mass. The medical use of this hormone includes stimulation of red blood ...

  18. 加巴喷丁联合非甾体消炎药治疗腰椎管狭窄症的疗效评价%CLINICAL EFFICACY OF COMBINATION OF GABAPENTIN AND NON-STEROIDAL ANTI-INFLAMMATORY DRUGS FOR PATIENTS WITH LUMBAR SPINAL STENOSIS

    Institute of Scientific and Technical Information of China (English)

    王昕辉; 易红蕾; 李红霞; 王谦; 孙海燕

    2012-01-01

    Objective: To evaluate the efficacy and safety of the combination of gabapentin and non-steroidal anti-inflammatory drugs in the treatment of patients with mild to moderate lumbar spinal stenosis. Methods: In this prospective nonrandomized control study, 54 patients with mild to moderate lumbar spinal stenosis were divided into the control group (n = 30) administered with non-steroidal anti-inflammatory drugs only, and the experimental group (n = 24) administered with gabapentin and non-steroidal anti-inflammatory drugs. The dose of gabapentin was titrated from 300 mg/d to 1800 mg/d. The visual analogue scale (VAS) of low back and leg pain, walking distance and side effects were measured every month. Results: All the patients were followed up for 12 weeks. Compared with the control group, the walking distance of the experimental group increased (P < 0.01), low back and leg pain VAS scores decreased (P < 0.05) and sensory deficit improved (P < 0.05). Three patients taking gabapentin had side effects, such as drowsiness, dizziness and ataxia. However, the symptoms relieved or disappeared after rest. Conclusion: Combination of gabapentin and non-steroidal anti-inflammatory drugs can improve the symptoms of lumbar spinal stenosis safely and effectively, its short-term efficacy and safety is reliable.%目的:观察加巴喷丁联合非甾体消炎药治疗轻至中度腰椎管狭窄症患者的有效性和安全性.方法:采用前瞻性对照研究,选择轻至中度症状的腰椎管狭窄症患者54例为研究对象,其中对照组30例仅口服非甾体消炎药;试验组24例,口服加巴喷丁+非甾体消炎药物.加巴喷丁剂量从300 mg/d逐步滴定至1800 mg/d.随访期间,每月分别统计腰腿痛评分、行走距离、副作用等.结果:所有病例随访12周.与对照组比较,试验组治疗后步行距离增加(P<0.01),腰腿痛评分下降(P<0.05),感觉功能障碍恢复(P<0.05).试验组3人出现嗜睡、头晕、共济失调

  19. Rehabilitation of muscle after injury - the role of anti-inflammatory drugs

    DEFF Research Database (Denmark)

    Mackey, Abigail; Mikkelsen, U R; Magnusson, S P;

    2012-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely consumed among athletes worldwide in relation to muscle injury and soreness. This review aims to provide an overview of studies investigating their effects on skeletal muscle, in particular the repair processes in injured muscle. Muscle...

  20. Clinical Study of Non-steroidal Anti-inflammatory Drugs Combined Glucosamine in the Treatment of Osteoarthritis of Knee Joint%非甾体抗炎药物联合氨基葡萄糖治疗膝骨性关节炎的临床研究

    Institute of Scientific and Technical Information of China (English)

    甘祝梅; 黄珠砂

    2013-01-01

      目的观察非甾体抗炎药物联合氨基葡萄糖治疗膝骨性关节炎的疗效及患者不良反应,探讨治疗骨性关节炎临床用药。方法选取本院80例临床诊断为膝骨性关节炎患者,按照随机分配原则分为非选择性非甾体抗炎药治疗组20例;COX-2非甾体抗炎药治疗组20例;非选择性非甾体抗炎药联合氨基葡萄糖治疗组20例;COX-2非甾体抗炎药联合氨基葡萄糖治疗组20例。分别于治疗6周后进行临床疗效评定并观察其不良反应,确定最佳用药方案。结果药物治疗6周后,四组患者的疗效经多组间检验差异有统计学意义(P<0.05),联合氨基葡萄糖治疗组患者疗效优于非联合氨基葡萄糖;COX-2非甾体抗炎药联合氨基葡萄糖治疗组临床缓解比率与非选择性非甾体抗炎药联合氨基葡萄糖治疗组比较差异有统计学意义(P<0.05)。COX-2非甾体抗炎药联合氨基葡萄糖治疗组不良反应率与其它三组比较,差异有统计学意义(P<0.05)。结论膝骨性关节炎使用 COX-2非甾体抗炎药联合氨基葡萄糖治疗,能够显著缓解骨性关节炎患者的症状,疗效确切,不良反应少,患者耐受性好,避免了短期内复发的可能。%Objective To observe the ef icacy of Non-steroidal anti-inflammatory drugs combined glucosamine in the treatment of osteoarthritis of knee joint, and respectively joint analysis of two kinds of mode of administrationglucosamine capsules clinical studies on the of osteoarthritis ef icacy and adverse reactions, to explore the clinical use of drugs to treat osteoarthritis. Methods By selecting a hospital clinical y patients diagnosed with osteoarthritis of the knee, 80 cases was divided into four groups of 20 cases in accordance with the principle of random al ocation. Respectively, after 6 weeks, the patients have been clinical ef icacy evaluation and observed the adverse reactions,in order to

  1. Metabolomic analysis of glycerophospholipid signatures of inflammation treated with non-steroidal anti-inflammatory drugs-induced-RAW264.7 cells using (1)H NMR and U-HPLC/Q-TOF-MS.

    Science.gov (United States)

    Wu, Xia; Cao, Han; Zhao, Lifang; Song, Jianao; She, Yuqi; Feng, Yifan

    2016-08-15

    Non-destructive proton nuclear magnetic resonance ((1)H NMR) spectroscopy and highly sensitive ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (U-HPLC/Q-TOF-MS) coupled to data processing methods were applied to analyze the metabolic profiling changes of glycerophospholipids (GPLs) in RAW264.7 cells from inflammation to prognosis. Analysis of (1)H NMR was shown that the models were grouped successfully, illustrating that all of them had significant differences. Based on the highly simple, accurate, non-targeted and non-destructively advantages of (1)H NMR, it could be used as a new screening tool of anti-inflammatory drugs in the metabolic profiling of GPLs. 58 GPLs were identified by U-HPLC/Q-TOF-MS, and 19 components were firstly identified in this study compared with our previous results. In addition, ten potential biomarkers were proved, of which phosphatidylcholine (PC) (16:0/18:1) and (18:0/18:1) changed consistently in three drug-induced groups and might be the important biomarkers. Compared with (1)H NMR, U-HPLC/Q-TOF-MS showed higher sensitivity and specificity and was more suitable for the determination of biomarkers apart from the deficiency of time-consuming sample preparation steps and unambiguous metabolite identification. Therefore, it is feasible to analyze the changes of GPLs during inflammation by combining (1)H NMR spectroscopy with U-HPLC/Q-TOF-MS. The metabolic profiling of GPLs provides valuable evidence for inflammation diagnosis and prognosis, and might unravel the mechanisms involved in inflammation progression. PMID:27371817

  2. Pseudoceramide stimulates peroxisome proliferator-activated receptor-α expression in a murine model of atopic dermatitis: molecular basis underlying the anti-inflammatory effect and the preventive effect against steroid-induced barrier impairment.

    Science.gov (United States)

    Lee, Sang Eun; Jung, Min Kyung; Oh, Seung Joon; Jeong, Se Kyoo; Lee, Seung Hun

    2015-11-01

    Topical pseudoceramides are successfully used in skin barrier repair therapy for atopic dermatitis (AD) and demonstrated to reduce the adverse effects of topical glucocorticoids (GC). However, the molecular mechanisms involved are not fully understood. We investigated whether PC-9S (myristoyl/palmitoyloxostearamide/arachamide MEA, Neopharm, Daejeon, Korea), one of the synthetic pseudoceramides, could stimulate peroxisome proliferator-activated receptor (PPAR)α expression in a hapten [oxazolone (oxa)]-induced AD murine model (oxa-AD mice) and subsequently improved permeability barrier, reduced inflammation, and increased antimicrobial peptides (AMPs) expression. Normal hairless mice and oxa-AD mice were topically treated twice daily with either PC-9S-containing physiologic lipid mixture (PLM), vehicle (PLM), or PPARα agonist for 4 days. Topical PC-9S significantly increased PPARα expression in mouse epidermis in vivo and in oxa-AD mice skin comparable with PPARα agonist. Topical PC-9S-containing PLM significantly reduced basal trans-epidermal water loss (TEWL), surface pH, and mast cell infiltrates and prevented the decline of AMPs expression in oxa-AD mice, which were abrogated by PPARα antagonist. Then, oxa-AD mice were treated with super-potent topical GC twice daily for 4 days with or without PC-9S co-applications. Co-treatment with PC-9S-containing PLM suppressed GC-induced increase in basal TEWL, epidermal thinning, reduced loricrin expression, and impaired barrier recovery and these effects were attenuated by PPARα antagonist. Collectively, our findings suggest that pseudoceramide PC-9S-induced stimulation of PPARα expression provides a new mechanism by which pseudoceramides show anti-inflammatory property, improve the permeability and antimicrobial barrier function, and prevent the negative effects of topical GC.

  3. A cluster randomised stepped wedge trial to evaluate the effectiveness of a multifaceted information technology-based intervention in reducing high-risk prescribing of non-steroidal anti-inflammatory drugs and antiplatelets in primary medical care: The DQIP study protocol

    Directory of Open Access Journals (Sweden)

    Dreischulte Tobias

    2012-03-01

    Full Text Available Abstract Background High-risk prescribing of non-steroidal anti-inflammatory drugs (NSAIDs and antiplatelet agents accounts for a significant proportion of hospital admissions due to preventable adverse drug events. The recently completed PINCER trial has demonstrated that a one-off pharmacist-led information technology (IT-based intervention can significantly reduce high-risk prescribing in primary care, but there is evidence that effects decrease over time and employing additional pharmacists to facilitate change may not be sustainable. Methods/design We will conduct a cluster randomised controlled with a stepped wedge design in 40 volunteer general practices in two Scottish health boards. Eligible practices are those that are using the INPS Vision clinical IT system, and have agreed to have relevant medication-related data to be automatically extracted from their electronic medical records. All practices (clusters that agree to take part will receive the data-driven quality improvement in primary care (DQIP intervention, but will be randomised to one of 10 start dates. The DQIP intervention has three components: a web-based informatics tool that provides weekly updated feedback of targeted prescribing at practice level, prompts the review of individual patients affected, and summarises each patient's relevant risk factors and prescribing; an outreach visit providing education on targeted prescribing and training in the use of the informatics tool; and a fixed payment of 350 GBP (560 USD; 403 EUR up front and a small payment of 15 GBP (24 USD; 17 EUR for each patient reviewed in the 12 months of the intervention. We hypothesise that the DQIP intervention will reduce a composite of nine previously validated measures of high-risk prescribing. Due to the nature of the intervention, it is not possible to blind practices, the core research team, or the data analyst. However, outcome assessment is entirely objective and automated. There will

  4. Marine soft corals as source of lead compounds for anti-inflammatories

    Directory of Open Access Journals (Sweden)

    Masteria Yunovilsa Putra

    2016-01-01

    Full Text Available Marine soft corals are known to produce a wide array of secondary metabolites, particularly diterpenoids and steroids, and often characterized by uncommon structural features and potent bioactivities. The remarkable abundance and diversity of bioactive small molecule which have been isolated from soft corals have made these organisms an important source of new drug candidates for human diseases, particularly for their anti-inflammatory activity. In this paper, the authors reported anti-inflammatory marine natural products isolated from diverse species of soft corals determined in vitro by their inhibition of lipopolysaccharide-induced expression of inducible NO synthase and cyclooxygenase-2 in murine macrophage cells (RAW 264.7.

  5. Steroids

    Science.gov (United States)

    ... steroids (say: STARE-oydz), they often mean illegal anabolic steroids. Anabolic steroids are artificially produced hormones that are the same ... these is testosterone (say: tes-TOSS-tuh-rone). Anabolic steroids can be taken in the form of pills, ...

  6. Chemopreventive response of diclofenac, a non-steroidal anti-inflammatory drug in experimental carcinogenesis Respuesta quimiopreventiva del diclofenaco, un fármaco antiinflamatorio no esteroideo en la carcinogénesis de colon experimental

    Directory of Open Access Journals (Sweden)

    M. Kaur Saini

    2009-12-01

    Full Text Available The chemopreventive response was evaluated of nonsteroidal anti-inflammatory drug, Diclofenac, a preferential cyclooxygenase-2 (COX-2 inhibitor in 1,2-dimethyhydrazine (DMH-induced colon cancer in rat model. The signs of neoplasm were evident in the animals receiving 30mg of DMH per kg body weight in a weekly s.c injection for six weeks. The putative biomarker of carcinogenesis was visible in the form of multiple plaque lesions in DMH treatment and then regression seen in those animals which also received an oral dose of Diclofenac, 8 mg/kg body weight whereas no such macroscopic neoplastic lesions were seen in the animals receiving Diclofenac only or the control animals receiving the vehicle of the drug. Histopathological results showed the presence of early aberrant changes in the form of severe dysplasia and also numerous crypt fissions in the apical surface of the colonic mucosa. A very high expression of COX-2 was seen in the colonic epithelium of DMH-treated rats, as analyzed by immunohistochemistry. Also, the apoptotic events were assessed by terminal deoxynucleotidyl dUTP nick end labeling (TUNEL assay, where the DMH group shows few number of TUNEL positive cells which dramatically increased in the Diclofenac treatment. The results suggest that Diclofenac could be an effective chemopreventive agent in colon cancer, where perhaps apoptosis plays a very dominant end effect in cancer cell killings.Se evaluó la respuesta quimiopreventiva del fármaco antiinflamatorio no esteroideo, diclofenaco, un inhibidor preferente de la ciclooxigenasa-2 (Cox-2, en el cáncer de colon inducido por 1,2-dimetilhidracina (DMH en un modelo de rata. Los signos de neoplasia fueron evidentes en los animales que recibieron 30 mg de DMH por kg de peso corporal mediante inyecciones s.c. semanales durante 6 semanas. El biomarcador putativo de la carcinogénesis fue visible en la forma de múltiples lesiones en placas con el tratamiento de DMH y la posterior regresi

  7. Anti-inflammatory Agents: Present and Future.

    NARCIS (Netherlands)

    Dinarello, C.A.

    2010-01-01

    Inflammation involving the innate and adaptive immune systems is a normal response to infection. However, when allowed to continue unchecked, inflammation may result in autoimmune or autoinflammatory disorders, neurodegenerative disease, or cancer. A variety of safe and effective anti-inflammatory a

  8. Medicinal plants with anti-inflammatory activities.

    Science.gov (United States)

    Maione, Francesco; Russo, Rosa; Khan, Haroon; Mascolo, Nicola

    2016-06-01

    Medicinal plants have been the main remedy to treat various ailments for a long time and nowadays, many drugs have been developed from traditional medicine. This paper reviews some medicinal plants and their main constituents which possess anti-inflammatory activities useful for curing joint inflammation, inflammatory skin disorders, cardiovascular inflammation and other inflammatory diseases. Here, we provide a brief overview of quick and easy reading on the role of medicinal plants and their main constituents in these inflammatory diseases. We hope that this overview will shed some light on the function of these natural anti-inflammatory compounds and attract the interest of investigators aiming at the design of novel therapeutic approaches for the treatment of various inflammatory conditions.

  9. Anti-inflammatory actions of acupuncture

    Directory of Open Access Journals (Sweden)

    Freek J. Zijlstra

    2003-01-01

    Full Text Available Acupuncture has a beneficial effect when treating many diseases and painful conditions, and therefore is thought to be useful as a complementary therapy or to replace generally accepted pharmacological intervention. The attributive effect of acupuncture has been investigated in inflammatory diseases, including asthma, rhinitis, inflammatory bowel disease, rheumatoid arthritis, epicondylitis, complex regional pain syndrome type 1 and vasculitis. Large randomised trials demonstrating the immediate and sustained effect of acupuncture are missing. Mechanisms underlying the ascribed immunosuppressive actions of acupuncture are reviewed in this communication. The acupuncture-controlled release of neuropeptides from nerve endings and subsequent vasodilative and anti-inflammatory effects through calcitonine gene-related peptide is hypothesised. The complex interactions with substance P, the analgesic contribution of β-endorphin and the balance between cell-specific pro-inflammatory and anti-inflammatory cytokines tumour necrosis factor-α and interleukin-10 are discussed.

  10. Anti-Inflammatory Effect of Allium ursinum

    Directory of Open Access Journals (Sweden)

    Alina Elena PÂRVU

    2014-03-01

    Full Text Available The aim of the present study was to evaluate Allium ursinum leaves and flowers extract anti-inflammatory effect. Plant extract 1:1 (w:v was prepared from A. ursinum leaves by a modified Squibb repercolation method. The in vivo anti-inflammatory effects were evaluated on a rat turpentine oil-induced inflammation (i.m. 6 mL/kg BW. The animals were randomly assigned to nine groups (n=8: negative control, inflammation, A. ursinum flower extract (AUF, A. ursinum leaves extract (AUL, indomethacin (INDO (20 mg/kg BW, aminoguanidine (AG (50 mg/kg b.w./d i.p. as a selective NOS2 inhibitor, NG-nitro L-arginine methyl ester (NAME (5 mg/kg b.w./d i.p. as a nonselective NOS inhibitor, L-arginine (ARG (100 mg/kg b.w./d i.p., NO synthesis substrate, and Trolox (20 mg/kg b.w./d i.p as an antioxidant. At 24h from inflammation induction total oxidative status (TOS, oxidative stress index (OSI, nitric oxide (NOx and in vitro phagocytosis test were reduced and the total antioxidative reactivity (TAR was increased by the testes plant extracts. AUF had a better inhibitory effect than AUL. In conclusion, we provided evidence for the hypothesis that A. ursinum leaves and flowers extract exerts anti-inflammatory activity by inhibiting the phagocytosis through the reduction of the nitro-oxidative stress.

  11. Intestinal toxicity of non-steroideal anti-inflammatory drugs with differential cyclooxigenase inhibition selectivity Toxicidad intestinal de los fármacos antiinflamatorios no esteroideos con una selectividad diferenciada en la inhibición de la ciclooxigenasa

    Directory of Open Access Journals (Sweden)

    S. Chopra

    2007-10-01

    Full Text Available The present study was designed to investigate the gastrointestinal side effects of cycloxygenase (COX inhibitor with varying selectivity, called the non-steroidal antiinflammatory drugs (NSAIDs viz., non-selective COX-1 & 2 inhibitor -aspirin, prefentially selective COX-2 inhibitor- nimesulide and highly selective COX-2 inhibitor- celecoxib. Treatment with NSAIDs exhibited a decrease in the activity of rat intestinal brush border membrane associated enzymes such as sucrase, lactase, maltase and alkaline phosphatase as compared to the control in the duodenum, jejunum and ileum. The uptake of D-glucose and L-histidine in the everted intestinal sac was found to be decreased. Also the decease of glucose and histidine uptake was found to be dependent on the substrate concentration, temperature and the time interval of incubation. The physical state and composition of brush border membrane was found to be altered as evident in the FTIR spectrum, by appearance of new peaks while disappearance of certain peaks occurred which were characteristics of the control membrane. The changes in wave number as well as peaks height were also noticed. Alterations in protein profile of the membrane were demonstrated using SDS-PAGE analysis where disappearance of few bands and change in the relative intensities of the bands were noticed and correlated with the alterations that have taken place at the molecular level. Histological studies have depicted a marked decrease in the absorption surface area such as the villi height of the intestinal segment. In addition, crypt number also deceased in the treated animals, an indication that such changes also correlate well with the changes in the transport of the end product nutrients.Se diseñó este estudio para investigar los efectos adversos gastrointestinales de los inhibidores de la ciclooxigenasa (COX con selectividad variable, denominados fármacos antiinflamatorios no esteroideos (AINE, inhibidores no selectivos de la

  12. 非甾体类抗炎药对种植体周围骨愈合和骨改建的影响%Effect of non-steroidal anti-inflammatory drug on healing and remolding of peri-implant bones

    Institute of Scientific and Technical Information of China (English)

    郑小菲; 游智惟; 莫安春

    2015-01-01

    The success of dental implants depends on optimal osseointegration, which is affected by many factors, such as systemic drug administration. In clinical practice, non-steroidal anti-inflammatory drugs(NSAID) are prescribed to deal with chronic inflammation or pain caused by some joint disorders or fractures and to control discomfort after implant surgery. NSAID can inhibit the activity of cyclo-oxygenase, resulting in decreased production of dinoprost, which plays avitalroleinbonemetabolism.Hence,administrationofNSAIDmayinfluencebonehealingofperi-implantsduringosseointegration. This article aims to review available data regarding the effects of NSAID on implant osseointegration, as well as on healing or remolding of peri-implant bones.%牙种植的成功首先取决于种植体的骨整合,而良好的骨整合受诸多因素的影响。非甾体类抗炎药(NSAID)除用来治疗骨关节系统的慢性炎症性疾病之外,还常用于控制种植手术后的疼痛不适。NSAID通过抑制环加氧酶的活性来减少地诺前列酮的合成,进而影响种植体骨整合和骨改建过程中新骨的形成。本文就NSAID对成骨细胞、骨愈合和种植体周围成骨的作用等研究进展作一综述。

  13. Upper gastrointestinal hemorrhage caused by non-steroidal anti-inflammatory drugs in young and middle aged patients%非甾体抗炎药致中青年患者上消化道出血临床分析(附81例)

    Institute of Scientific and Technical Information of China (English)

    谭仲华; 黎蓉; 石少燕; 李信健; 李志明

    2013-01-01

    目的 探讨非甾体抗炎药(NSAIDs)致中青年患者上消化道出血的临床特点.方法 回顾分析81例非甾体抗炎药中青年患者的临床资料.结果 本组81患者2周内均有服用NSAIDs病史,都经大便潜血及纤维胃镜确诊.伴有腹部疼痛症状18例占22.2%(18/81);有嗜咖啡或酸辣饮食习惯53例(占65.4%);有吸烟史48例(占59.3%).结论 中青年人群服用NSAIDs引起的上消化道出血起病隐匿、临床症状轻和体征不明显的特点,应引起临床医师和药师的警惕.%Objective To explore the clinical features of upper gastrointestinal hemorrhage caused by non-steroidal anti-inflammatory drugs(NSAIDs)in young and middle-aged patients.Methods The clinical data of 81 young and middle-aged patients with upper gastrointestinal hemorrhage caused by NSAIDs were retrospectively analyzed.Results All patients,taking NSAIDs within two weeks,diagnosed by fecal occult blood and fiber gastroscope.18 cases(22.2%)complicated with abdominal pain.53 cases (65.4%)addicted to coffee or sour-spicy food.48 cases(59.3%)smoked.Conclusions Upper gastrointestinal hemorrhage caused by NSAIDs in young and middle-aged people is occult onset and has mild clinical symptoms and unobvious signs.Clinicians and pharmacists should pay attention to it.

  14. 非甾体类抗炎药对结肠癌细胞NAG-1 基因表达的诱导%Induction of NAG-1 Gene Expression in Colon Cancer Cells by Non-steroidal Anti-inflammatory Drugs

    Institute of Scientific and Technical Information of China (English)

    王春晖; 欧阳钦; 唐承薇; 刘瑞; 黄明慧

    2007-01-01

    研究非甾体类抗炎药(Non-steroidal anti-inflammatory drug, NSAID)对结肠癌细胞生长的影响及NSAID活化基因-1(NAG-1)的诱导作用.体外培养HT-29、SW480及LS174-T三种结肠癌细胞,分别加入不同浓度的aspirin、celecoxib及meloxicam作用于HT-29及SW480细胞,采用MTT法检测结肠癌细胞增殖;蛋白质印迹技术检测三种结肠癌细胞COX-2的表达;采用半定量RT-PCR技术分析NSAID对三种结肠癌细胞NAG-1基因表达的影响.aspirin、celecoxib及meloxicam均能有效抑制体外培养的HT-29、SW480结肠癌细胞生长,并具有良好的量-效关系.Western blot 表明,HT-29细胞表达COX-2,而SW480细胞不表达COX-2.三种结肠癌细胞均表达 NAG-1基因mRNA,其中LS174-T细胞NAG-1基础水平较低;NSAID能不同程度上调结肠癌细胞NAG-1基因表达.NSAID能有效抑制结肠癌细胞生长,这种作用可能部分通过诱导结肠癌细胞NAG-1基因表达实现,NAG-1基因表达不受肿瘤细胞是否表达COX-2的影响.

  15. COX-Independent Mechanisms of Cancer Chemoprevention by Anti-Inflammatory Drugs

    OpenAIRE

    Gurpinar, Evrim; Grizzle, William E.; Piazza, Gary A.

    2013-01-01

    Epidemiological and clinical studies suggest that non-steroidal anti-inflammatory drugs (NSAIDs), including cyclooxygenase (COX)-2 selective inhibitors, reduce the risk of developing cancer. Experimental studies in human cancer cell lines and rodent models of carcinogenesis support these observations by providing strong evidence for the antineoplastic properties of NSAIDs. The involvement of COX-2 in tumorigenesis and its overexpression in various cancer tissues suggest that inhibition of COX...

  16. COX-independent mechanisms of cancer chemoprevention by anti-inflammatory drugs

    OpenAIRE

    Evrim eGurpinar; Grizzle, William E.; Piazza, Gary A.

    2013-01-01

    Epidemiological and clinical studies suggest that non-steroidal anti-inflammatory drugs (NSAIDs), including cyclooxygenase (COX)-2 selective inhibitors, reduce the risk of developing cancer. Experimental studies in human cancer cell lines and rodent models of carcinogenesis support these observations by providing strong evidence for the antineoplastic properties of NSAIDs. The involvement of COX-2 in tumorigenesis and its overexpression in various cancer tissues suggest that inhibition of COX...

  17. Preparation of controlled release microspheres using supercritical fluid technology for delivery of anti-inflammatory drugs

    OpenAIRE

    Duarte, Ana Rita C.; Costa, M. S.; Simplicio, A. L.; Cardoso, M. Margarida; Duarte, Catarina M. M.

    2006-01-01

    Ethylcellulose/methylcellulose blends were produced using different precipitation techniques and impregnated with naproxen, a non-steroidal anti-inflammatory drug (NSAID). Solvent-evaporation technique was used not only for the preparation of ethylcellulose/methylcellulose microspheres but also to encapsulate naproxen. Supercritical fluid (SCF) impregnation was also performed to prepare naproxen loaded microspheres. The microspheres, impregnated by the SCF technique, were prepared bo...

  18. Marine soft corals as source of lead compounds for anti-inflammatories

    OpenAIRE

    Masteria Yunovilsa Putra; Tutik Murniasih

    2016-01-01

    Marine soft corals are known to produce a wide array of secondary metabolites, particularly diterpenoids and steroids, and often characterized by uncommon structural features and potent bioactivities. The remarkable abundance and diversity of bioactive small molecule which have been isolated from soft corals have made these organisms an important source of new drug candidates for human diseases, particularly for their anti-inflammatory activity. In this paper, the authors repor...

  19. Chemotherapeutic properties of phospho-nonsteroidal anti-inflammatory drugs, a new class of anticancer compounds

    OpenAIRE

    Huang, Liqun; Mackenzie, Gerardo G; Sun, Yu; Ouyang, Nengtai; Xie, Gang; Vrankova, Kvetoslava; Komninou, Despina; Rigas, Basil

    2011-01-01

    Non-steroidal anti-Inflammatory drugs (NSAIDs) exhibit antineoplastic properties, but conventional NSAIDs do not fully meet safety and efficacy criteria for use as anti-cancer agents. In this study, we evaluated the chemotherapeutic efficacy of five novel phospho-NSAIDs, each of which includes in addition to the NSAID moiety a diethylphosphate linked through a butane moiety. All five compounds inhibited the growth of human breast, colon and pancreatic cancer cell lines with micromolar potency...

  20. Molecular mechanisms of inflammation. Anti-inflammatory benefits of virgin olive oil and the phenolic compound oleocanthal.

    Science.gov (United States)

    Lucas, Lisa; Russell, Aaron; Keast, Russell

    2011-01-01

    Chronic inflammation is a critical factor in the pathogenesis of many inflammatory disease states including cardiovascular disease, cancer, diabetes, degenerative joint diseases and neurodegenerative diseases. Chronic inflammatory states are poorly understood, however it is known that dietary habits can evoke or attenuate inflammatory responses. Popular methods to deal with inflammation and its associated symptoms involve the use of non steroidal anti-inflammatory drugs, however the use of these drugs are associated with severe side effects. Therefore, investigations concerned with natural methods of inflammatory control are warranted. A traditional Mediterranean diet has been shown to confer some protection against the pathology of chronic diseases through the attenuation of pro-inflammatory mediators and this has been partially attributed to the high intake of virgin olive oil accompanying this dietary regime. Virgin olive oil contains numerous phenolic compounds that exert potent anti-inflammatory actions. Of interest to this paper is the recently discovered phenolic compound oleocanthal. Oleocanthal is contained in virgin olive oil and possesses similar anti-inflammatory properties to ibuprofen. This pharmacological similarity has provoked interest in oleocanthal and the few studies conducted thus far have verified its anti-inflammatory and potential therapeutic actions. A review of the health benefits of the Mediterranean diet and anti-inflammatory properties of virgin olive oil is presented with the additional emphasis on the pharmacological and anti-inflammatory properties of the phenolic compound oleocanthal. PMID:21443487

  1. Erdosteine: antitussive and anti-inflammatory effects.

    Science.gov (United States)

    Dal Negro, Roberto W

    2008-01-01

    Erdosteine is a multifactorial drug currently used in COPD for its rheologic activity on bronchial secretions and its positive effects on bacterial adhesiveness. Erdosteine produces an active metabolite (Met 1) which was shown to produce antioxidant effects during the respiratory burst of human PMNs, due to the presence of an SH group. The substantial antitussive effects of erdosteine were first documented in clinical trials even though mucolytic agents are regarded as not consistently effective in ameliorating cough in patients with bronchitis, although they may be of benefit to this population in other ways. Actually, a mucolytic drug could exert antitussive effects if it also affects mucus consistency and enhances ciliary function. In the last decade, data from several studies on animal models pointed to the possible antitussive and anti-inflammatory properties of erdosteine and an indirect anti-inflammatory mechanism of action was suggested. Recently, data from some controlled versus placebo studies documented the antioxidant properties of erdosteine in humans and in current smokers with COPD. The mechanism of action was described as related to erdosteine's ability to inhibit some inflammatory mediators and some pro-inflammatory cytokines that are specifically involved in oxidative stress. As oxidative stress is also presumed to impair beta-adrenoceptor function and contribute to airway obstruction, specific controlled studies recently investigated the effect of antioxidant intervention on short-term airway response to salbutamol in nonreversible COPD, according to a double-blind design versus placebo and NAC. Only erdosteine consistently restored a significant short-term reversibility in COPD subjects, previously unresponsive to beta(2) adrenergics. This peculiar activity of erdosteine (to our knowledge never previously assessed) proved related to the ROS scavenging activity (which actually proved equal to that of N), and its significant inhibiting effect on

  2. Erdosteine: antitussive and anti-inflammatory effects.

    Science.gov (United States)

    Dal Negro, Roberto W

    2008-01-01

    Erdosteine is a multifactorial drug currently used in COPD for its rheologic activity on bronchial secretions and its positive effects on bacterial adhesiveness. Erdosteine produces an active metabolite (Met 1) which was shown to produce antioxidant effects during the respiratory burst of human PMNs, due to the presence of an SH group. The substantial antitussive effects of erdosteine were first documented in clinical trials even though mucolytic agents are regarded as not consistently effective in ameliorating cough in patients with bronchitis, although they may be of benefit to this population in other ways. Actually, a mucolytic drug could exert antitussive effects if it also affects mucus consistency and enhances ciliary function. In the last decade, data from several studies on animal models pointed to the possible antitussive and anti-inflammatory properties of erdosteine and an indirect anti-inflammatory mechanism of action was suggested. Recently, data from some controlled versus placebo studies documented the antioxidant properties of erdosteine in humans and in current smokers with COPD. The mechanism of action was described as related to erdosteine's ability to inhibit some inflammatory mediators and some pro-inflammatory cytokines that are specifically involved in oxidative stress. As oxidative stress is also presumed to impair beta-adrenoceptor function and contribute to airway obstruction, specific controlled studies recently investigated the effect of antioxidant intervention on short-term airway response to salbutamol in nonreversible COPD, according to a double-blind design versus placebo and NAC. Only erdosteine consistently restored a significant short-term reversibility in COPD subjects, previously unresponsive to beta(2) adrenergics. This peculiar activity of erdosteine (to our knowledge never previously assessed) proved related to the ROS scavenging activity (which actually proved equal to that of N), and its significant inhibiting effect on

  3. Optimization and pharmacological validation of a leukocyte migration assay in zebrafish larvae for the rapid in vivo bioactivity analysis of anti-inflammatory secondary metabolites.

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    María Lorena Cordero-Maldonado

    Full Text Available Over the past decade, zebrafish (Danio rerio have emerged as an attractive model for in vivo drug discovery. In this study, we explore the suitability of zebrafish larvae to rapidly evaluate the anti-inflammatory activity of natural products (NPs and medicinal plants used in traditional medicine for the treatment of inflammatory disorders. First, we optimized a zebrafish assay for leukocyte migration. Inflammation was induced in four days post-fertilization (dpf zebrafish larvae by tail transection and co-incubation with bacterial lipopolysaccharides (LPS, resulting in a robust recruitment of leukocytes to the zone of injury. Migrating zebrafish leukocytes were detected in situ by myeloperoxidase (MPO staining, and anti-inflammatory activity was semi-quantitatively scored using a standardized scale of relative leukocyte migration (RLM. Pharmacological validation of this optimized assay was performed with a panel of anti-inflammatory drugs, demonstrating a concentration-responsive inhibition of leukocyte migration for both steroidal and non-steroidal anti-inflammatory drugs (SAIDs and NSAIDs. Subsequently, we evaluated the bioactivity of structurally diverse NPs with well-documented anti-inflammatory properties. Finally, we further used this zebrafish-based assay to quantify the anti-inflammatory activity in the aqueous and methanolic extracts of several medicinal plants. Our results indicate the suitability of this LPS-enhanced leukocyte migration assay in zebrafish larvae as a front-line screening platform in NP discovery, including for the bioassay-guided isolation of anti-inflammatory secondary metabolites from complex NP extracts.

  4. 重视变态反应性结膜炎治疗中非甾体抗炎药物的应用%Consideration of application of non-steroidal anti-inflammatory drugs in the treatment of allergic conjunctivitis

    Institute of Scientific and Technical Information of China (English)

    李莹

    2014-01-01

    近年来随着工业化进程的加快,变态反应性结膜炎的发生率逐渐升高.目前,变态反应性结膜炎的治疗以眼局部治疗为主,主要目的在于针对病因,减轻症状和预防并发症.变态反应性结膜炎的治疗药物包括抗组胺药、肥大细胞稳定剂、双效作用药物(稳定肥大细胞/抗组胺)、非甾体抗炎药(NSAIDs)、糖皮质激素及免疫抑制剂六大类.抗组胺药、肥大细胞稳定剂、双效作用药物的主要作用是减轻眼部瘙痒、结膜充血等症状和体征,也可用于急性变态反应性结膜炎患者,而NSAIDs、糖皮质激素及免疫抑制剂则用于症状严重患者或慢性病例.糖皮质激素类药物治疗变态反应性结膜炎效果显著,可作用于过敏反应的多个环节,但是长期应用可能会导致眼压升高、视力障碍、视野缺损和后囊下白内障,有角膜溃疡的患者更应谨慎使用.免疫抑制剂具有抑制免疫的作用,可抑制局部或机体异常的免疫反应,但由于价格较高及局部刺激性强等不良反应,故也不宜长期应用.NSAIDs具有良好的抗炎效果,作用温和,刺激性小,目前在眼表变态反应性结膜炎中广泛应用.%Allergic conjunctivitis is a very common pathology and its incidence has increased in developing countries with the development of industrialization.At present,the therapy of allergic conjunctivitis is mainly the use of topical eyedrops to eliminate causative factors,relieve symptoms and prevent complications.The drugs used in allergic conjunctivitis have 6 groups,including antihistamine,mastocyte stabilizer,drugs with dual effects (antihistamine and mastocyte stabilizer),non-steroidal anti-inflammatory drugs (NSAIDs),glucocorticoids and immunosuppressors.The goals of topical use of antihistamine,mastocyte stabilizer and drugs of dual effects are to remove the itching and hyperaemia of eye or to treat the patients with acute allergic conjunctivitis; while NSAIDs

  5. In vivo anti-inflammatory activity of some naturally occurring O- and N-prenyl secondary metabolites.

    Science.gov (United States)

    Epifano, Francesco; Genovese, Salvatore; Fiorito, Serena; della Loggia, Roberto; Tubaro, Aurelia; Sosa, Silvio

    2014-01-01

    A series of O- and N-prenyl secondary metabolites of insect, fungal, and plant origin have been evaluated for their topical anti-inflammatory activity using the Croton oil ear test in mice as a model of acute inflammation. Some of the tested compounds revealed an effect (ID50 = 0.31 divided by 0.56 micromol/cm2) comparable with that of the reference non-steroidal anti-inflammatory drug indomethacin (ID50 = 0.23 micromol/cm2). PMID:24660470

  6. Design, synthesis, and local anti-inflammatory activity of 17β-carboxamide derivatives of glucocorticoids.

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    Dobričić, Vladimir; Marković, Bojan; Milenković, Nikola; Savić, Vladimir; Jaćević, Vesna; Rančić, Nemanja; Vladimirov, Sote; Cudina, Olivera

    2014-11-01

    Molecular docking studies were performed on 18 17β-carboxamide steroids in order to select compounds with potential local anti-inflammatory activity. These derivatives are amides of cortienic acids (obtained from hydrocortisone, prednisolone, and methylprednisolone) with methyl or ethyl esters of six amino acids. Interactions with the glucocorticoid receptor (GR), binding energies and ligand efficiency values of these compounds were compared with dexamethasone and cortienic acid obtained from prednisolone (inactive metabolite). On the basis of molecular docking studies, seven compounds were selected and their binding affinities for the GR were predicted by use of the exponential model created in this study. Subsequently, selected compounds were synthesized in good yields by use of modified N,N'-dicyclohexylcarbodiimide (DCC)/1-hydroxybenzotriazole (HOBt) coupling procedure. Finally, the local anti-inflammatory activity of the synthesized compounds was examined by use of the croton oil-induced ear edema test. In vivo evaluation of systemic side effects as well as in silico prediction of metabolism were performed on the derivative with the best local anti-inflammatory activity. The combination of molecular docking studies and the exponential model for the GR binding affinity prediction could be used as an in silico tool for the rational design of novel 17β-carboxamide steroids with potentially better biological profile than dexamethasone. PMID:25159891

  7. Smoking status and anti-inflammatory macrophages in bronchoalveolar lavage and induced sputum in COPD

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    Rabe Klaus F

    2011-03-01

    Full Text Available Abstract Background Macrophages have been implicated in the pathogenesis of COPD. M1 and M2 macrophages constitute subpopulations displaying pro- and anti-inflammatory properties. We hypothesized that smoking cessation affects macrophage heterogeneity in the lung of patients with COPD. Our aim was to study macrophage heterogeneity using the M2-marker CD163 and selected pro- and anti-inflammatory mediators in bronchoalveolar lavage (BAL fluid and induced sputum from current smokers and ex-smokers with COPD. Methods 114 COPD patients (72 current smokers; 42 ex-smokers, median smoking cessation 3.5 years were studied cross-sectionally and underwent sputum induction (M/F 99/15, age 62 ± 8 [mean ± SD] years, 42 (31-55 [median (range] packyears, post-bronchodilator FEV1 63 ± 9% predicted, no steroids past 6 months. BAL was collected from 71 patients. CD163+ macrophages were quantified in BAL and sputum cytospins. Pro- and anti-inflammatory mediators were measured in BAL and sputum supernatants. Results Ex-smokers with COPD had a higher percentage, but lower number of CD163+ macrophages in BAL than current smokers (83.5% and 68.0%, p = 0.04; 5.6 and 20.1 ×104/ml, p = 0.001 respectively. The percentage CD163+ M2 macrophages was higher in BAL compared to sputum (74.0% and 30.3%, p + BAL macrophages (Rs = 0.38, p = 0.003. No significant differences were found between smokers and ex-smokers in the levels of pro-inflammatory (IL-6 and IL-8, and anti-inflammatory (elafin, and Secretory Leukocyte Protease Inhibitor [SLPI] mediators in BAL and sputum. Conclusions Our data suggest that smoking cessation partially changes the macrophage polarization in vivo in the periphery of the lung towards an anti-inflammatory phenotype, which is not accompanied by a decrease in inflammatory parameters.

  8. Innovative combination of QuEChERS extraction with on-line solid-phase extract purification and pre-concentration, followed by liquid chromatography-tandem mass spectrometry for the determination of non-steroidal anti-inflammatory drugs and their metabolites in sewage sludge.

    Science.gov (United States)

    Rossini, D; Ciofi, L; Ancillotti, C; Checchini, L; Bruzzoniti, M C; Rivoira, L; Fibbi, D; Orlandini, S; Del Bubba, M

    2016-09-01

    For the first time QuEChERS extraction of sewage sludge was combined with the automatic solid-phase pre-concentration and purification of the extract (following indicated as SPE) and LC-MS/MS analysis, for the determination of the non-steroidal anti-inflammatory drugs acetylsalicylic acid (ASA), diclofenac (DIC), fenbufen (FEN), flurbiprofen (FLU), ketoprofen (KET), ibuprofen (IBU) and naproxen (NAP), and their metabolites salicylic acid (SAL), 4'-hydroxydiclofenac (4'-HYDIC), 1-hydroxyibuprofen (1-HYIBU), 2-hydroxyibuprofen (2-HYIBU), 3-hydroxyibuprofen (3-HYIBU) and o-desmethylnaproxen (O-DMNAP). Various commercial pellicular stationary phases (i.e. silica gel functionalized with octadecyl, biphenyl, phenylhexyl and pentafluorophenyl groups) were preliminarily investigated for the resolution of target analytes and different sorbent phases (i.e. octyl or octadecyl functionalized silica gel and a polymeric phase functionalized with N-benzylpyrrolidone groups) were tested for the SPE phase. The optimized method involves the QuEChERS extraction of 1 g of freeze-dried sludge with 15 mL of water/acetonitrile 1/2 (v/v), the SPE of the extract with the N-benzylpyrrolidone polymeric phase and the water/acetonitrile gradient elution on the pentafluorophenyl stationary phase at room temperature. Matrix effect was always suppressive and in most cases low, being it ≤20% for ASA, DIC, FLU, KET, IBU, 1-HYIBU, 2-HYIBU, 3-HYIBU, NAP and O-DMNAP, and included in the range of 35-47% for the other analytes. Recoveries were evaluated at three spiking levels, evidencing almost quantitative values for HYIBUs and O-DMNAP; for ASA, SAL and KET the recoveries were included in between 50 and 76%, whereas for the other compounds they ranged from 36% to 55%. The proposed method showed better analytical performances than those so far published, being suitable for target compound determination in real samples from tens of pg g(-1) to ng g(-1) of freeze-dried sludge, with a total analysis

  9. Review of Anti-Inflammatory Herbal Medicines.

    Science.gov (United States)

    Ghasemian, Mona; Owlia, Sina; Owlia, Mohammad Bagher

    2016-01-01

    Medicinal plants and their secondary metabolites are progressively used in the treatment of diseases as a complementary medicine. Inflammation is a pathologic condition that includes a wide range of diseases such as rheumatic and immune-mediated conditions, diabetes, cardiovascular accident, and etcetera. We introduce some herbs which their anti-inflammatory effects have been evaluated in clinical and experimental studies. Curcuma longa, Zingiber officinale, Rosmarinus officinalis, Borago officinalis, evening primrose, and Devil's claw are some of the introduced medicinal herbs in this review. Since the treatment of inflammation is not a one-dimensional remedy, this review tries to reach a multidimensional therapeutic approach to inflammation with the help of herbal medicine and modification in lifestyle. PMID:27247570

  10. Review of Anti-Inflammatory Herbal Medicines

    Directory of Open Access Journals (Sweden)

    Mona Ghasemian

    2016-01-01

    Full Text Available Medicinal plants and their secondary metabolites are progressively used in the treatment of diseases as a complementary medicine. Inflammation is a pathologic condition that includes a wide range of diseases such as rheumatic and immune-mediated conditions, diabetes, cardiovascular accident, and etcetera. We introduce some herbs which their anti-inflammatory effects have been evaluated in clinical and experimental studies. Curcuma longa, Zingiber officinale, Rosmarinus officinalis, Borago officinalis, evening primrose, and Devil’s claw are some of the introduced medicinal herbs in this review. Since the treatment of inflammation is not a one-dimensional remedy, this review tries to reach a multidimensional therapeutic approach to inflammation with the help of herbal medicine and modification in lifestyle.

  11. The role of chronic inflammation in the development of gastrointestinal cancers: reviewing cancer prevention with natural anti-inflammatory intervention.

    Science.gov (United States)

    Lee, Ho-Jae; Park, Jong-Min; Han, Young Min; Gil, Hong Kwon; Kim, Jinhyung; Chang, Ji Young; Jeong, Migyeong; Go, Eun-Jin; Hahm, Ki Baik

    2016-01-01

    Inflammatory mediators alter the local environment of tumors, known as the tumor microenvironment. Mechanistically, chronic inflammation induces DNA damage, but understanding this hazard may help in the search for new chemopreventive agents for gastrointestinal (GI) cancer which attenuate inflammation. In the clinic, GI cancer still remains a major cause of cancer-associated mortality, chemoprevention with anti-inflammatory agents is thought to be a realistic approach to reduce GI cancer. Proton pump inhibitors, monoclonal antibodies targeting tumor necrosis factor-alpha, anti-sense targeted smad7 and non-steroidal anti-inflammatory agents have been investigated for their potential to prevent inflammation-based GI cancer. Besides these, a wide variety of natural products have also shown potential for the prevention of GI cancer. In this review, the authors will provide insights to explain the mechanistic connection between inflammation and GI cancer, as well as describe a feasible cancer prevention strategy based on anti-inflammatory treatments.

  12. Endoscopical appearances of nonsteroidal anti inflammatory drug (NSAID- enteropathy

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    Marcellus Simadibrata

    2005-12-01

    Full Text Available Non Steroidal Anti Inflammatory Drugs (NSAID have been associated with a sudden and sustained rise in the incidence of gastrointestinal ulcer complications. The aim of the study was to reveal the endoscopical abnormalities found in the duodenum & proximal jejunum due to NSAID. Thirty eight patients taking NSAID for their arthritis or rheumatism were included in this study. Gastro-duodeno-jejunoscopy was done with Olympus PCF-10. The endoscopical appearances of NSAID entero gastropathy were evaluated with a scoring system. The NSAID-entero-gastropathy appearances were endoscopically seen as hyperemia, erosion and ulcer. From all patient recruited, 7.9% complaint of diarrhea and 71.1% complaint of dyspepsia. Endoscopically, in the duodenal bulb we found 79% cases of hyperemia, 39.5% cases of erosion and 7.9% cases of ulcer. In the second part (descending part of the duodenum we found 28.9% cases of hyperemia, 15.8% cases of erosion and 2.6% case of ulcer. In the jejunum, we found 7.9% cases of hyperemia, 2.6% case of erosion and no ulcer. It is concluded that the most frequent abnormal endoscopical appearances in NSAID- enteropathy was hyperemia. The most frequent site of NSAID-enteropathy abnormal findings was in the duodenal bulb. (Med J Indones 2005; 14: 225-9Keywords: NSAID-enteropathy, endoscopical appearances.

  13. Anti-Inflammatory Components from the Root of Solanum erianthum

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    Yueh-Hsiung Kuo

    2013-06-01

    Full Text Available Two new norsesquiterpenoids, solanerianones A and B (1–2, together with nine known compounds, including four sesquiterpenoids, (−-solavetivone (3, (+-anhydro-β-rotunol (4, solafuranone (5, lycifuranone A (6; one alkaloid, N-trans-feruloyltyramine (7; one fatty acid, palmitic acid (8; one phenylalkanoid, acetovanillone (9, and two steroids, β-sitosterol (10 and stigmasterol (11 were isolated from the n-hexane-soluble part of the roots of Solanum erianthum. Their structures were elucidated on the basis of physical and spectroscopic data analyses. The anti-inflammatory activity of these isolates was monitored by nitric oxide (NO production in lipopolysaccharide (LPS-activated murine macrophage RAW264.7 cells. The cytotoxicity towards human lung squamous carcinoma (CH27, human hepatocellular carcinoma (Hep 3B, human oral squamous carcinoma (HSC-3 and human melanoma (M21 cell lines was also screened by using an MTT assay. Of the compounds tested, 3 exhibited the strongest NO inhibition with the average maximum inhibition (Emax at 100 μM and median inhibitory concentration (IC50 values of 98.23% ± 0.08% and 65.54 ± 0.18 μM, respectively. None of compounds (1–9 was found to possess cytotoxic activity against human cancer cell lines at concentrations up to 30 μM.

  14. Study of anti-inflammatory effect of simvastatin in rats

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    Ranga Satya Venkatesh

    2016-08-01

    Results: At a dose of 40 mg Simvastatin showed anti-inflammatory effect which is statically highly significant. Conclusions: However, the above preclinical experiments only give us an idea about the anti-inflammatory activity, but large scale clinical trials are necessary for final assessment. [Int J Basic Clin Pharmacol 2016; 5(4.000: 1520-1523

  15. Anti-inflammatory and immunomodulatory properties of Carica papaya.

    Science.gov (United States)

    Pandey, Saurabh; Cabot, Peter J; Shaw, P Nicholas; Hewavitharana, Amitha K

    2016-07-01

    Chronic inflammation is linked with the generation and progression of various diseases such as cancer, diabetes and atherosclerosis, and anti-inflammatory drugs therefore have the potential to assist in the treatment of these conditions. Carica papaya is a tropical plant that is traditionally used in the treatment of various ailments including inflammatory conditions. A literature search was conducted by using the keywords "papaya", "anti-inflammatory and inflammation" and "immunomodulation and immune" along with cross-referencing. Both in vitro and in vivo investigation studies were included. This is a review of all studies published since 2000 on the anti-inflammatory activity of papaya extracts and their effects on various immune-inflammatory mediators. Studies on the anti-inflammatory activities of recognized phytochemicals present in papaya are also included. Although in vitro and in vivo studies have shown that papaya extracts and papaya-associated phytochemicals possess anti-inflammatory and immunomodulatory properties, clinical studies are lacking.

  16. Anti-Inflammatory Activity of Different Agave Plants and the Compound Cantalasaponin-1

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    Jaime Tortoriello

    2013-07-01

    Full Text Available Species of the agave genus, such as Agave tequilana, Agave angustifolia and Agave americana are used in Mexican traditional medicine to treat inflammation-associated conditions. These plants’ leaves contain saponin compounds which show anti-inflammatory properties in different models. The goal of this investigation was to evaluate the anti-inflammatory capacity of these plants, identify which is the most active, and isolate the active compound by a bio-directed fractionation using the ear edema induced in mice with 12-O-tetradecanoylphorbol-13-acetate (TPA technique. A dose of 6 mg/ear of acetone extract from the three agave species induced anti-inflammatory effects, however, the one from A. americana proved to be the most active. Different fractions of this species showed biological activity. Finally the F5 fraction at 2.0 mg/ear induced an inhibition of 85.6%. We identified one compound in this fraction as (25R-5α-spirostan-3β,6α,23α-triol-3,6-di-O-β-D-glucopyranoside (cantalasaponin-1 through 1H- and 13C-NMR spectral analysis and two dimensional experiments like DEPT NMR, COSY, HSQC and HMBC. This steroidal glycoside showed a dose dependent effect of up to 90% of ear edema inhibition at the highest dose of 1.5 mg/ear.

  17. Immunoadjuvant and anti-inflammatory plant saponins: characteristics and biotechnological approaches towards sustainable production.

    Science.gov (United States)

    de Costa, F; Yendo, A C A; Fleck, J D; Gosmann, G; Fett-Neto, A G

    2011-09-01

    Saponins can be classified as triterpenoid (C30) or steroidal (C27), based on their carbon nucleus (aglycone). Sugar residues are linked to the aglycone, conferring an amphiphilic nature on these molecules, which is relevant for their biological activities. Saponins include a large variety of molecules that find several applications in pharmacology. Saponins have been shown to display immunoadjuvant, anti-inflammatory, antiplatelet, hypocholesterolemic, antitumoral, anti-HIV, antibacterial, insecticide, fungicide and anti-leishmanial activities. Anti-inflammatory medicines are increasingly demanded to treat various forms of arthritis in aging and obese populations and to help reduce the doses and duration of conventional corticotherapy with less side effects and without immunosuppression. The vaccine market for both human and veterinary uses is close to US$ 15 billion, progressively inflated by the recurrent threat of global pandemics.This paper provides an overview of recent advances (main focus on the last five years) on plant saponins that show anti-inflammatory and/or immunoadjuvant activities: source plants, isolation procedures, mechanism of action and biotechnological approaches towards sustainable production of bioactive saponins. Special attention is given to ginseng and Quillaja saponins. Strategies based on plant cultivation, cell and tissue culture, elicitation, and metabolic engineering for improved production of saponins are described. Future directions for research in the field and strategies to overcome bottlenecks are also discussed. PMID:21762102

  18. Topical anti-inflammatory constituents of lipophilic leaf fractions of Alchornea floribunda and Alchornea cordifolia.

    Science.gov (United States)

    Okoye, F B C; Osadebe, P O; Nworu, C S; Okoye, N N; Omeje, E O; Esimone, C O

    2011-12-01

    The leaves of Alchornea floribunda and Alchornea cordifolia are used traditionally as topical anti-inflammatory agents. In this study, two highly lipophilic fractions AFLF and ACLF isolated from A. floribunda and A. cordifolia leaves respectively were investigated for topical anti-inflammatory effects using xylene-induced mice ear oedema as a model of inflammation. AFLF and ACLF at 5 mg per ear showed significant (p eugenol (21.26%) and cadinol (4.76%), and other constituents like, nanocosaine (36.86%) and steroid derivatives, ethyl iso-allocholate (4.59%) and 3-acetoxy-7,8-epoxylanostan-1-ol (15.86%). Analysis of the volatile oil (ACV) extracted from the fresh leaves of A. cordifolia revealed the presence of high concentrations of eugenol (41.7%), cadinol (2.46%), Caryophylene (1.04%), Linalool (30.59%) and (E)-α-bergamotene (4.54%). These compounds could be contributing to the topical anti-inflammatory effects of A. floribunda and A. cordifolia leaf extracts.

  19. Anti-inflammatory drugs for Duchenne muscular dystrophy: focus on skeletal muscle-releasing factors.

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    Miyatake, Shouta; Shimizu-Motohashi, Yuko; Takeda, Shin'ichi; Aoki, Yoshitsugu

    2016-01-01

    Duchenne muscular dystrophy (DMD), an incurable and a progressive muscle wasting disease, is caused by the absence of dystrophin protein, leading to recurrent muscle fiber damage during contraction. The inflammatory response to fiber damage is a compelling candidate mechanism for disease exacerbation. The only established pharmacological treatment for DMD is corticosteroids to suppress muscle inflammation, however this treatment is limited by its insufficient therapeutic efficacy and considerable side effects. Recent reports show the therapeutic potential of inhibiting or enhancing pro- or anti-inflammatory factors released from DMD skeletal muscles, resulting in significant recovery from muscle atrophy and dysfunction. We discuss and review the recent findings of DMD inflammation and opportunities for drug development targeting specific releasing factors from skeletal muscles. It has been speculated that nonsteroidal anti-inflammatory drugs targeting specific inflammatory factors are more effective and have less side effects for DMD compared with steroidal drugs. For example, calcium channels, reactive oxygen species, and nuclear factor-κB signaling factors are the most promising targets as master regulators of inflammatory response in DMD skeletal muscles. If they are combined with an oligonucleotide-based exon skipping therapy to restore dystrophin expression, the anti-inflammatory drug therapies may address the present therapeutic limitation of low efficiency for DMD.

  20. Evolución del consumo y gasto farmacéutico público de anti-inflamatorios no esteroideos (aines en el período 2001 - 2005 Evolution of public consumption and spending on non-steroidal anti-inflammatory drugs (nsaids during the period 2001 to 2005

    Directory of Open Access Journals (Sweden)

    Patricia Barber Pérez

    2007-12-01

    Full Text Available Este estudio observacional retrospectivo analizó el consumo y gasto farmacéutico de AINEs (antiinflamatorios no esteroideos clásicos en Costa Rica en el periodo 2001-2005. Su objetivo es contribuir al conocimiento de la estructura de gasto y perfil de utilización y consumo farmacológico de este grupo de medicamentos con el fin de abordar con mayores garantías la gestión del irremediable proceso de aparición y previsible financiación pública de los AINEs de nueva generación en el país. Los AINEs son un grupo de fármacos asociados de forma especial a los nuevos estilos de vida cuyo nivel de consumo crece de forma ininterrumpida y cuya participación en el gasto farmacéutico es cada vez más relevante. En la actualidad, constituyen el cuarto grupo en gasto farmacéutico público con un incremento del 15% en términos reales en el periodo 2001-2004. El consumo de AINEs para 2005 en Costa Rica es de 21,02 DHD (dosis diaria por habitante y día y en el periodo 2000-2005 su consumo se ha incrementado un 48%. Respecto al consumo en 2005 de los principios activos que forman este grupo farmacológico destaca la Indometacina con un 6,36 DHD, Sulindaco con 6,06 DHD y el Ibuprofeno con 4,36 DHD y el Tenoxican con 3,25 DHD. El CTD (Coste de Tratamiento Diario varía entre 2 céntimos de dólar para el Ibuprofeno y 1,49 dólares para el Tenoxican.This observational, retrospective study analyzed the pharmaceutical consumption and expense of classic NSAIDs (non-steroidal anti-inflammatory drugs in Costa Rica during the period 2001 to 2005. Its objective was to contribute to knowledge regarding the expense structure as well as the pattern of use and pharmacological consumption of this group of medicines with the purpose of providing better support to the inexorable process of the appearance and foreseeable public financing of new-generation NSAIDs in our country. NSAIDs are a group of medicines associated in a special fashion to the new lifestyles

  1. Altered membrane lipid dynamics and chemoprevention by non-steroidal anti inflammatory drugs during colon carcinogenesis Alteración de la dinámica de los lípidos de membrana y quimioprevención mediante los fármacos antiinflamatorios no esteroideos en la carcinogénesis de colon

    Directory of Open Access Journals (Sweden)

    S. Singh Kanwar

    2011-10-01

    Full Text Available The present work focuses on the anti-neoplastic role of non steroidal anti-inflammatory drugs (NSAIDs in modulating the biophysical parameters of the colonic membranes in 1,2-dimethylhydrazine dihydrochloride (DMH induced carcinogenesis. The steady-state fluorescence polarization technique was applied to assess membrane fluidity, membrane polarity and lipid phase states. The decline in cholesterol content, biosynthesis and cholesterol: phospholipids ratio with DMH treatment indicates more fluidity associated with carcinogenesis. The DMH group had shown lower order parameter indicating more fluidity whereas NSAIDs resulted in increasing the membrane lipid order. The converging effects of these changes were more in membrane phase separations and membrane phase state. In DMH treatment membrane shows lesser phase separation or high polarity, and more liquid crystalline state while for NSAID groups membranes have higher phase separations or low polarity, and more of the gel phase. Further, NSAIDs induced anti-proliferative effects were evidently observed by apoptosis in the colonocytes by using acridine orange-ethidium bromide fluorescent staining and Terminal de-oxynucleotidyl transferase dUTP nick end labeling (TUNEL assay. The results suggest that NSAIDs induced alteration in the membrane biophysical parameters may be an important initiating event for the chemopreventive action.Este trabajo se centra en el papel antineoplásico de los fármacos antiinflamatorios no esteroideos (AINE en la modulación de los parámetros biofísicos de las membranas colónicas en la carcinogénesis inducida por 1,2-dihidrocloruro de dimetilhidracina (DMH. Se aplicó la técnica de polarización de la fluorescencia en estado de equilibrio para evaluar la fluidez de la membrana, su polaridad y los estados de fase lipídica. El declive del contenido de colesterol, la biosíntesis y el cociente colesterol: fosfolípidos con el tratamiento con DMH indica más fluidez

  2. Effect of non-steroidal anti-inflammatory drugs and the pro-carcinogen 1, 2 dimethylhydrazine on the rat intestinal membrane structure and function Efecto de los fármacos antiinflmatorios no esteroideos y del procarcinógeno 1,2-dimetilhidracina sobre la estructura y función de la membrana intestinal de la rata

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    N. Mittal

    2008-10-01

    Full Text Available The present study was designed to evaluate the effects of three non-steroidal anti-inflammatory drugs (NSAIDs with varying cycloxygenase selectivities on the small intestinal biochemical composition, function and histology during 1, 2-dimethylhydrazine (DMH administration. Sprague Dawley male rats were divided into five different groups viz: Group 1 (control, vehicle treated, Group 2 (DMH-treated, 30 mg/kg body weight/week in 1 mM EDTA-saline, subcutaneously, Group 3 (DMH + aspirin-60 mg/kg body weight, Group 4 (DMH + celecoxib-6 mg/kg body weight, Group 5 (DMH + etoricoxib-0.64 mg/kg body weight. After six weeks of treatment, brush border membrane was isolated from the jejunum segment of all the groups and changes in the associated enzymes such as sucrase, lactase, maltase, alkaline phosphatase, membrane lipid composition, fluorescence polarizations of diphenylhexatriene, pyrene excimer formation, histological changes and surface characteristics were studied. The results indicated a significant alteration in the enzyme activity as well as changes in the structure and function of the intestine in the presence of the pro-carcinogen, DMH, which suggests the possible chemopreventive efficacy of NSAIDs against the intestinal cancer.El presente estudio se diseñó para evaluar los efectos de tres fármacos antiinflamatorios no esteroideos (AINE con diferente selectividad por la ciclooxigenasa sobre la composición bioquímica, la función y la histología del intestino delgado durante la administración de 1,2-dimetilhidracina (DMH. Se distribuyó a ratas macho Sprague Dawley en grupos distintos: Grupo 1 (control, tratado con vehículo, Grupo 2 (tratado con DMH, 30 mg/kg de peso /semana en 1 mM de EDTA-salino, subcutáneo, Grupo 3 (DMH + aspirina-60 mg/kg de peso, Grupo 4 (DMH + celecoxib-6 mg/kg de peso, Grupo 5 (DMH + etoricoxib-0,64 mg/kg de peso. Tras seis semanas de tratamiento, se aisló la membrana en cepillo de un segmento del yeyuno en todos

  3. A case-control study on non-steroidal anti-inflammatory drugs(NSAIDs)induced and NSAIDs unrelated peptic ulcer with upper gastrointestinal bleeding%NSAIDs相关性消化性溃疡出血与非NSAIDs消化性溃疡出血的临床对照研究

    Institute of Scientific and Technical Information of China (English)

    宗晔; 赵海英; 王青釭; 吴咏冬; 张澍田

    2012-01-01

    目的 探讨非甾体类抗炎药(NSAIDs)相关性溃疡出血与非NSAIDs消化性溃疡出血的差异.方法 通过临床对照研究,比较46例NSAIDs相关性溃疡出血与88例非NSAIDs消化性溃疡出血的临床资料.结果 NSAIDs组年龄显著高于非NSAIDs组,女性患者比率高于非NSAIDs组;NSAIDs组具有心脑血管和/或风湿免疫性疾病的患者多于非NSAIDs组,而既往具有消化性溃疡病史的患者低于非NSAIDs组;NSAIDs组上腹痛症状显著低于非NSAIDs组;NSAIDs组发病时血糖高于非NSAIDs组;NSAIDs组胃溃疡比率显著高于非NSAIDs组.以上差异均有统计学意义(P<0.05).结论 NSAIDs相关性溃疡出血发病年龄、性别、临床表现及溃疡的发生部位与非NSAIDs溃疡患者均有差异,熟悉NSAIDs相关性溃疡出血的特点有利于临床诊治.%Objective To explore the difference in clinical characteristics between non - steroidal anti - inflammatory drugs ( NSAIDs ) induced and NSAIDs unrelated peptic ulcer with upper gastrointestinal bleeding. Methods The case - control study was used to analyze the clinical data of forty - six patients with NSAIDs induced and eighty - eight patients with NSAIDs unrelated peptic ulcer with upper gastrointestinal bleeding. Results The age range of patients in NSAIDs induced group was older than that of NSAIDs unrelated group. Female patients in NSAIDs induced group were more than those in NSAIDs unrelated group. More patients in NSAIDs induced group had the history of cardio - cerebral - vascular diseases or rheumatic diseases, fewer patients in NSAIDs induced group had the history of peptic ulcer and epigastric pain. The level of blood sugar in NSAIDs induced group was higher than that of NSAIDs unrelated group. The number of patients with gastric ulcer in NSAIDs induced group was more than that of NSAIDs unrelated group. Their difference was significant( P < 0. 05 ). Conclusion There was significant difference between NSAIDs induced group and

  4. Association studies of Helicobacter pylori and non-steroidal anti-inflammatory drugs in patients with bleeding peptic ulcer%幽门螺杆菌感染及非甾体抗炎药致消化性溃疡并出血的相关性研究

    Institute of Scientific and Technical Information of China (English)

    王莹; 王秀英; 王敏琴

    2011-01-01

    OBJECTIVE To explore the association studies of Helicobacter pylori and non-steroidal anti-inflammatory drug in patients with bleeding peptic ulcer. METHODS The clinical dates of 188 cases of peptic ulcer were reviewed retrospectively. Each parameters were evaluated with univariate and multivariate analysis.RESULTS Univariate analysis identified 4 statistically significant variables, including aged ≥60 years, the history of peptic ulcer, cardio cerebral vascular diseases and NSAIDs use(P<0.05). Logistic regression analysis showed that aged 60 years, the history of peptic ulcer, bleeding peptic ulcer and cardio cerebral vascular diseases, H. pylori infection alone, NSAIDs alone and combined H. pylori infection and NSAIDs were the risk factors of bleeding peptic ulcer(P<0. 01). CONCLUSION H. pylori infection is not a risk factor for bleeding peptic ulcer, but combination of aged 60 years, H. pylori, the history of peptic ulcer, bleeding peptic ulcer and cardio cerebral vascular diseases increases in risk factors of bleeding peptic ulcer.%目的 探讨服用非甾体抗炎药及幽门螺杆菌感染与消化性溃疡并出血的相关性.方法 对188例消化性溃疡患者的临床资料进行回顾性分析,将其所有的危险因素行单因素和多因素分析.结果 在单因素分析中,出血组中年龄≥60岁、既往有消化道出血史、心脑血管史、口服非甾体抗炎药所占比例高于未出血组,两组比较差异有统计学意义(P<0.05);进一步行多因素logistic回归分析,发现年龄≥60岁、既往有消化性溃疡史、消化道出血史、心脑血管病史、单纯Hp感染、单纯服用非甾体抗炎药及Hp感染+服用非甾体抗炎药均为消化性溃疡并出血的危险因素(P<0.01).结论 单纯Hp感染并不能增加消化性溃疡并出血的危险性,但若与年龄≥60岁、服用非甾体抗炎药、既往有消化性溃疡史、消化道出血史、心脑血管史等因素同时出现可增加其危险性.

  5. Efeito do uso profilático do anti-inflamatório não-esteroide ibuprofeno sobre o desempenho em uma sessão de treino de força Effects of prophylactic anti-inflammatory non-steroidal ibuprofen on performance in a session of strength training

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    Cleiton Silva Correa

    2013-04-01

    Full Text Available INTRODUÇÃO: Medicamentos anti-inflamatórios não esteroides, como o ibuprofeno, têm sido utilizados por atletas de várias modalidades com o intuito de aumentar desempenho esportivo. OBJETIVO: Verificar o efeito do uso profilático de ibuprofeno sobre desempenho em uma sessão de treino de força. MÉTODOS: Um ensaio clínico, cruzado, randomizado, duplo-cego e placebo-controlado foi desenvolvido com 12 praticantes regulares de treino de força do sexo masculino, os quais realizaram uma sessão de treino após a ingestão de ibuprofeno (1,2 g e uma outra após a ingestão de placebo. Seis séries dos exercícios supino e agachamento foram realizadas em cada sessão de treino com uma carga constante correspondente a 65% da 1RM de cada exercício. O desempenho no treinamento foi mensurado através do número de repetições que os voluntários conseguiram realizar em cada série de exercício a cada sessão de treino de força. RESULTADOS: Não foram verificadas diferenças significativas de desempenho no treino de força com a administração prévia de placebo ou ibuprofeno (p > 0,05. CONCLUSÃO: A ingestão de ibuprofeno nos parâmetros de administração adotados pelo presente estudo não promove qualquer tipo de alteração na tolerância ao exercício em uma sessão isolada de treino de força, o que contraria a indicação dessa substância para fins ergogênicos no treino de força.INTRODUCTION: Non-steroidal anti-inflammatory drugs, such as ibuprofen, have been used by athletes of several sports modalities in order to increase athletic performance. OBJECTIVE: To verify the effect of the prophylactic use of ibuprofen on performance in a strength training session. METHODS: A crossover, randomized, double-blind and placebo-controlled clinical assay was developed with twelve male regular practitioners of strength training who performed one strength training session after ibuprofen (1.2 g ingestion and another session after placebo

  6. EVALUATION OF ANTI-INFLAMMATORY AND ANALGESIC ACTIVITY OF PUNICA GRANATUM LINN LEAVES

    OpenAIRE

    Nain Parminder; Saini Mamta; Malik Manisha

    2011-01-01

    The methanolic extract of dried leaves of Punica granatum linn was studied for the anti-inflammatory activity in rat using carrageenan induced paw edema with plethysmometer and analgesic activity on mice by Eddy’s hot plate & tail immersion method. A preliminary phytochemical screening of leaves extract revealed the presence of alkaloids, tannins, flavonoids, and steroids. Among all the doses (200mg/kg, 400mg/kg, 600mg/kg, 800mg/kg) of methanolic extract 600mg/kg orally showed maximum signifi...

  7. Nonsteroidal Anti-Inflammatory Agents in the Treatment of Asthma in Children

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    Pierre Gaudreault

    1995-01-01

    Full Text Available The increasing scientific information clearly demonstrates the important role of inflammation in asthma. This evidence has led physicians to focus their treatment on the elimination of inflammation instead of working solely against bronchoconstriction. Steroids and nonsteroidal agents are currently used to prevent this inflammatory component. This paper focuses only on nonstcroidal anti-inflammatory agents such as sodium cromoglycate, nedocromil sodium and ketotifen and their use in pediatric asthma. The discussion on each medication addresses its mechanism of action, the evidence concerning its efficacy in pediatrics (ie, clinical pharmacology, acute bronchial challenge, late asthmatic response, bronchial hyperrcactivity, clinical efficacy and the pediatric dose.

  8. Anti-inflammatory, anticoagulant and antioxidant effects of aqueous extracts from Moroccan thyme varieties

    Institute of Scientific and Technical Information of China (English)

    Tarik; Khouya; Mhamed; Ramchoun; Abdelbassat; Hmidani; Souliman; Amrani; Hicham; Harnafi; Mohamed; Benlyas; Younes; Filali; Zegzouti; Chakib; Alem

    2015-01-01

    Objective: To evaluate the anti-inflammatory, anticoagulant and antioxidant effects of aqueous extracts of thyme varieties from Moroccan.Methods: The aqueous extracts of tree medicinal plants [Thymus atlanticus(T. atlanticus), Thymus satureioides and Thymus zygis(T. zygis)] were screened for their antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl radical-scavenging, ferric reducing antioxidant power assay, radical scavenging activity method, the inhibition of 2,2’-azobis(2-amidinopropane) dihydrochloride that induces oxidative erythrocyte hemolysis and thiobarbituric acid reactive substances assay. The anti-inflammatory activity of aqueous extracts was evaluated in vivo using croton oil-induced ear edema and carrageenan-induced paw edema in mice and rats, respectively. This extracts were evaluated in vitro for their anticoagulant activity at the different concentrations by partial thromboplastin time and prothrombin time activated. Results: All thyme varieties were found to possess considerable antioxidant activity and potent anti-inflammatory activity in the croton oil-induced edema. Administration of aqueous extracts of two varieties(50 mg/kg)(T. zygis and T. atlanticus) reduced significantly the carrageenaninduced paw edema similar to non-steroidal anti-inflammatory drug(indomethacin, 10 mg/kg). In partial thromboplastin time and prothrombin time tests, T. atlanticus and T. zygis extracts showed the strongest anticoagulant activity. In contrast, Thymus satureioides did not show the anticoagulant activity in these tests. Conclusions: All aqueous extracts possess considerable antioxidant activity and are rich in total polyphenol and flavonoid but they act differently in the process of inflammatory and coagulation studied. This study shows great variability of biological activities in thyme varieties.

  9. Nonsteroidal Anti-Inflammatory Drugs: Adverse Effects and Their Prevention

    NARCIS (Netherlands)

    Vonkeman, Harald E.; Laar, van de Mart A.F.J.

    2010-01-01

    Objectives: To discuss nonsteroidal anti-inflammatory drugs (NSAIDs), their history, development, mode of action, toxicities, strategies for the prevention of toxicity, and future developments. - Methods: Medline search for articles published up to 2007, using the keywords acetylsalicylic acid, asp

  10. Anti-inflammatory and analgesic activities of Melanthera scandens

    Institute of Scientific and Technical Information of China (English)

    Jude E Okokon; Anwanga E Udoh; Samuel G Frank; Louis U Amazu

    2012-01-01

    Objective: To evaluate the anti-inflammatory and analgesic activities of leaf extract of Melanthera scandens (M. scandens). Methods: The crude leaf extract (39-111 mg/kg) of M. scandens was investigated for anti-inflammatory and analgesic activities using various experimental models. The anti-inflammatory activity was investigated using carragenin, egg-albumin induced oedema models, while acetic acid, formalin-induced paw licking and thermal-induced pain models were used to evaluate the antinociceptive property. Results: The extract caused a significant (P<0.05 - 0.001) dose-dependent reduction of inflammation and pains induced by different agents used. Conclusions: The leaf extract possesses anti-inflammatory and analgesic effects which may be mediated through the phytochemical constituents of the plant.

  11. Topical anti-inflammatory activity of yacon leaf extracts

    OpenAIRE

    Rejane B. Oliveira; Daniela A. Chagas-Paula; Adriana Secatto; Thaís H. Gasparoto; Faccioli, Lúcia H.; Campanelli, Ana P.; Fernando B. Da Costa

    2013-01-01

    Smallanthus sonchifolius (Poepp.) H. Rob. , Asteraceae, known as yacon, is an herb that is traditionally used for the treatment of diabetes in folk medicine. However, recent studies have demonstrated that this plant has other interesting properties such as anti-microbial and anti-inflammatory actions. Thus, the purpose of this study was to evaluate the topical anti-inflammatory property of different extracts prepared from yacon leaves and analyze the role of different chemical classes in this...

  12. Synthesis and anti-inflammatory activity of chalcone derivatives.

    Science.gov (United States)

    Herencia, F; Ferrándiz, M L; Ubeda, A; Domínguez, J N; Charris, J E; Lobo, G M; Alcaraz, M J

    1998-05-19

    Chalcones and their derivatives were synthesized and evaluated for their anti-inflammatory activity. In vitro, chalcones 2, 4, 8, 10 and 13 inhibited degranulation and 5-lipoxygenase in human neutrophils, whereas 11 behaved as scavenger of superoxide. Only four compounds (4-7) inhibited cyclo-oxygenase-2 activity. The majority of these samples showed anti-inflammatory effects in the mouse air pouch model.

  13. Anti-inflammatory Effects and M echmdsms of Usnic Acid

    Institute of Scientific and Technical Information of China (English)

    HUANG Zhijun; ZHENG Guohua; TAO Junyan; RUAN Jinlan

    2011-01-01

    The anti-inflammatory effect and mechanism of Usnic acid (UA) were explored on lipopolysaccharide (LPS)-stimulated RAW264.7 cell line.The effects of UA on pro-inflammatory cytokines including tumor necrosis factor-alfa (TNF-a),interleukin-6 (IL-6) and interleukin-I beta (IL-lβ),pro-inflammatory mediators such as nitric oxide (NO),inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2)were studied by sandwich ELISA,real-time PCR and western blot analyses.Similarly,the effect of UA on anti-inflammatory cytokine interleukin- 10 (IL- 10) and anti-inflammatory mediator heme oxygenase- l (HO- 1)were also studied following the same methods.Furthermore,nuclear factor-kB (NF-kB) was assayed by immunocytochemistry.The results showed that UA has anti-inflammatory effect by down-regulatinng iNOS,COX-2,IL-lβ,IL-6 and TNF-a,COX-2 gene expression through the suppression of NF-kB activation and increasing anti-inflammatory cytokine IL-10 and anti-inflammatory mediator HO-1 production.

  14. Repositioning of 2,4-dichlorophenoxy acetic acid as a potential anti-inflammatory agent: in silico and pharmaceutical formulation study.

    Science.gov (United States)

    Khedr, Mohammed A; Shehata, Tamer M; Mohamed, Maged E

    2014-12-18

    2,4-Dichlorophenoxy acetic acid (2,4-D) is a well-known plant auxin which is widely used in plant tissue culture experiments as well as a weed killer and a herbicide. In this study, 2,4-D was rediscovered as a new anti-inflammatory agent through an in silico molecular modeling and docking studies along with drug formulation and in vivo anti-inflammatory inspection. The molecular modeling and docking studies indicated high affinity of 2,4-D toward COX-2 enzyme in a way similar to Ibuprofen, suggesting a higher anti-inflammatory activity. Molecular docking by both MOE 2013.08 and Leadit 2.1.2 revealed excellent binding pattern compared to some of well-known non-steroidal anti-inflammatory drugs. 2,4-D was formulated in different gel bases. In vitro drug release experiments were used to examine the best 2,4-D formula for in vivo studies. In vivo carrageenan-induced hind paw edema inflammatory model in rats was used to test the in silico finding. 2,4-D showed potential in vivo anti-inflammatory activity and significantly reduced the concentration of prostaglandin E2 in hind paw tissues in a way similar to Ibuprofen. These results may open the door to introduce a new anti-inflammatory molecule; especially that 2,4-D is a well-investigated regarding its toxicity and side effect. PMID:25245006

  15. N-Acetylcysteine enhances the action of anti-inflammatory drugs as suppressors of prostaglandin production in monocytes

    Directory of Open Access Journals (Sweden)

    Erica Hoffer

    2002-01-01

    Full Text Available The anti-inflammatory effect of non-steroidal anti-inflammatory drugs (NSAIDs is associated with inhibition of cyclooxygenase (COX, the rate-limiting enzyme responsible for the synthesis of prostaglandins. Since oxygen free radicals can act as second cellular messengers, especially to modulate the metabolism of arachidonic acid and the prostaglandin tract, it seems plausible that antioxidants might affect the production of prostaglandin by activated cells. This research is focused on the effect of the antioxidant N-acetylcysteine (NAC on the inhibition of prostaglandin E2 formation in activated monocytes by specific and non-specific COX inhibitors. We found that lipopolysaccharide-induced prostaglandin E2 formation was significantly reduced by rofecoxib and by diclofenac, two NSAIDs. Addition of NAC to each of these drugs enhanced the effect of the NSAIDs. These results suggest that one might expect either a potentiation of the anti-inflammatory effect of COX inhibitors by their simultaneous administration with NAC, or obtaining the same anti-inflammatory at lower drug levels.

  16. Anti-Inflammatory and Anti-Pyretic Activity of the Leaf, Root and Saponin Fraction from Vernonia amygdalina

    Directory of Open Access Journals (Sweden)

    P.C. Adiukwu

    2013-04-01

    Full Text Available Studies have shown that Vernonia amygdalina possess saponin as one of the bitter phyto-constituents. This study was aimed at determining the anti-inflammatory and antipyretic activity of the aqueous extract of the leaf, root and saponin fraction from the herb. Standard procedures using ear thickness measurement in xylene induced inflammation and anal temperature readings in Saccharomyces cerevisiae induced pyrexia in rats were followed. Data indicated significant (p≤0.05 inhibitory activity for all the dose levels of the extracts in the anti-inflammatory and antipyretic evaluations. Saponin fraction at the dose of 100 and 200 mg/kg with 10.5 and 19.6% inhibition respectively, showed significant (p≤0.05 anti-inflammatory activity. The antipyretic evaluation of the saponin fraction showed no anal temperature reduction at 50 mg/kg dose level. Finding suggests the antipyretic and non-steroid like anti-inflammatory activity of the saponin fraction. This may partly explain the observed activity of the herbal extract which has found use traditionally as remedy for similar ailments.

  17. Anti-inflammatory activity of Bromelia hieronymi: comparison with bromelain.

    Science.gov (United States)

    Errasti, María E; Caffini, Néstor O; Pelzer, Lilian E; Rotelli, Alejandra E

    2013-03-01

    Some plant proteases (e. g., papain, bromelain, ficin) have been used as anti-inflammatory agents for some years, and especially bromelain is still being used as alternative and/or complementary therapy to glucocorticoids, nonsteroidal antirheumatics, and immunomodulators. Bromelain is an extract rich in cysteine endopeptidases obtained from Ananas comosus. In this study the anti-inflammatory action of a partially purified extract of Bromelia hieronymi fruits, whose main components are cysteine endopeptidases, is presented. Different doses of a partially purified extract of B. hieronymi were assayed on carrageenan-induced and serotonine-induced rat paw edema, as well as in cotton pellet granuloma model. Doses with equal proteolytic activity of the partially purified extract and bromelain showed significantly similar anti-inflammatory responses. Treatment of the partially purified extract and bromelain with E-64 provoked loss of anti-inflammatory activity on carrageenan-induced paw edema, a fact which is consistent with the hypothesis that the proteolytic activity would be responsible for the anti-inflammatory action.

  18. Anti-inflammatory activity of root of Alpinia galanga willd

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    Asim Kumar Ghosh

    2011-01-01

    Full Text Available Objective: The objective of the study is to evaluate the acute and chronic anti-inflammatory activities of root extract of Alpinia galanga in rodents. Materials and Methods: The study was carried out using albino rats of either sex (150-200 g. An extract of the root of A. galanga was prepared using absolute alcohol and distillation in a Soxhlet apparatus. The acute anti-inflammatory effects of this extract were evaluated using carrageenan-, bradykinin-, and 5-HT-induced rat paw edema. The chronic anti-inflammatory effects were evaluated using formaldehyde-induced rat paw edema. Results and Analysis: Inhibition of inflammation was seen to be 32.22% in carrageenan-induced, 37.70% in 5-HT-induced, and 35.21% in bradykinin-induced anti-inflammatory models. In chronic inflammatory model, a progressive inhibition of 34.73% (3 rd day, 37.50% (5 th day, 38.83% (7 th day, 44.66% (9 th day, 49.59% (11 th day, and 55.75% (13 th day was observed with study compound. The efficacy was comparable with the standard drugs. Conclusion: It can be thus concluded that A. galanga has anti-inflammatory properties and probably acts by blocking histaminic and serotonin pathways. It may be an effective alternative to NASAIDs and corticosteroid in inflammatory disorders.

  19. Anti-inflammatory activity of Syzygium cumini bark.

    Science.gov (United States)

    Muruganandan, S; Srinivasan, K; Chandra, S; Tandan, S K; Lal, J; Raviprakash, V

    2001-05-01

    The ethanolic extract of the bark of Syzygium cumini was investigated for its anti-inflammatory activity in animal models. The extract did not show any sign of toxicity up to a dose of 10.125 g/kg, p.o. in mice. Significant anti-inflammatory activity was observed in carrageenin (acute), kaolin-carrageenin (subacute), formaldehyde (subacute)-induced paw oedema and cotton pellet granuloma (chronic) tests in rats. The extract did not induce any gastric lesion in both acute and chronic ulcerogenic tests in rats. Thus, the present study demonstrated that S. cumini bark extract has a potent anti-inflammatory action against different phases of inflammation without any side effect on gastric mucosa. PMID:11395258

  20. IL-35 is a novel responsive anti-inflammatory cytokine--a new system of categorizing anti-inflammatory cytokines.

    Science.gov (United States)

    Li, Xinyuan; Mai, Jietang; Virtue, Anthony; Yin, Ying; Gong, Ren; Sha, Xiaojin; Gutchigian, Stefanie; Frisch, Andrew; Hodge, Imani; Jiang, Xiaohua; Wang, Hong; Yang, Xiao-Feng

    2012-01-01

    It remains unknown whether newly identified anti-inflammatory/immunosuppressive cytokine interleukin-35 (IL-35) is different from other anti-inflammatory cytokines such as IL-10 and transforming growth factor (TGF)-β in terms of inhibition of inflammation initiation and suppression of full-blown inflammation. Using experimental database mining and statistical analysis methods we developed, we examined the tissue expression profiles and regulatory mechanisms of IL-35 in comparison to other anti-inflammatory cytokines. Our results suggest that in contrast to TGF-β, IL-35 is not constitutively expressed in human tissues but it is inducible in response to inflammatory stimuli. We also provide structural evidence that AU-rich element (ARE) binding proteins and microRNAs target IL-35 subunit transcripts, by which IL-35 may achieve non-constitutive expression status. Furthermore, we propose a new system to categorize anti-inflammatory cytokines into two groups: (1) the house-keeping cytokines, such as TGF-β, inhibit the initiation of inflammation whereas (2) the responsive cytokines including IL-35 suppress inflammation in full-blown stage. Our in-depth analyses of molecular events that regulate the production of IL-35 as well as the new categorization system of anti-inflammatory cytokines are important for the design of new strategies of immune therapies.

  1. Anti-inflammatory new coumarin from the Ammi majus L.

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    Selim, Yasser Abdelaal; Ouf, Nabil Hassan

    2012-01-12

    Investigation of the aerial parts of the Egyptian medicinal plant Ammi majus L. led to isolation of new coumarin, 6-hydroxy-7-methoxy-4 methyl coumarin (2) and 6-hydroxy-7-methoxy coumarin (3); this is the first time they have been isolated from this plant. The structures of the compounds (2 &3) were elucidated by spectroscopic data interpretation and showed anti-inflammatory and anti-viral activity. GRAPHICAL An efficient, one-new coumarin (2) was isolated from the aerial parts of the A. Majus L. was evaluated for their anti-viral and anti-inflammatory activities.

  2. Anti-inflammatory drugs for Duchenne muscular dystrophy: focus on skeletal muscle-releasing factors

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    Miyatake S

    2016-08-01

    Full Text Available Shouta Miyatake,1 Yuko Shimizu-Motohashi,2 Shin’ichi Takeda,1 Yoshitsugu Aoki1 1Department of Molecular Therapy, National Institute of Neuroscience, National Center of Neurology and Psychiatry, Kodaira, Tokyo, Japan; 2Department of Child Neurology, National Center Hospital, National Center of Neurology and Psychiatry, Kodaira, Tokyo, Japan Abstract: Duchenne muscular dystrophy (DMD, an incurable and a progressive muscle wasting disease, is caused by the absence of dystrophin protein, leading to recurrent muscle fiber damage during contraction. The inflammatory response to fiber damage is a compelling candidate mechanism for disease exacerbation. The only established pharmacological treatment for DMD is corticosteroids to suppress muscle inflammation, however this treatment is limited by its insufficient therapeutic efficacy and considerable side effects. Recent reports show the therapeutic potential of inhibiting or enhancing pro- or anti-inflammatory factors released from DMD skeletal muscles, resulting in significant recovery from muscle atrophy and dysfunction. We discuss and review the recent findings of DMD inflammation and opportunities for drug development targeting specific releasing factors from skeletal muscles. It has been speculated that nonsteroidal anti-inflammatory drugs targeting specific inflammatory factors are more effective and have less side effects for DMD compared with steroidal drugs. For example, calcium channels, reactive oxygen species, and nuclear factor-κB signaling factors are the most promising targets as master regulators of inflammatory response in DMD skeletal muscles. If they are combined with an oligonucleotide-based exon skipping therapy to restore dystrophin expression, the anti-inflammatory drug therapies may address the present therapeutic limitation of low efficiency for DMD. Keywords: calcium channels, ryanodine receptor 1, exon skipping, NF-κB, myokine, ROS

  3. Salvia macrosiphon seeds and seed oil: pharmacognostic, anti-inflammatory and analgesic properties

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    A. Hamedi

    2016-10-01

    Full Text Available Background and objectives:Wild Sage(Salvia macrosiphon Boiss. known as “Marvak” in Persian is one of the polymorphic and abundant plants of Lamiaceae. The plants whole seeds usually soaked or boiled in hot water are widely used for inflammatory ailments in folk medicine. Documents have shown that there is scant information on the chemical constituents of this plant seeds. The current study was carried out to assess the phytochemical constituents of Salvia macrosiphon seeds as well as anti-inflammatory activities. Methods: The seed oil extracted via a Soxhlet extractor was subjected to pharmacognostic assays using High Performance Thin Layer Chromatography (HPTLC, Gas chromatography/mass spectrometry (GC/MS analysis of fatty acids and sterols as well as evaluation of the possible anti-inflammatory activities in rats. Results: Total ash, acid insoluble and water soluble ash values were determined as 51.67±7.53, 10.00±0.02 and 30.01±5.01 mg/g, respectively. HPTLC assessment revealed the presence of different steroids, triterpenes and fatty acids. Amount of sterols in oil was found 2.44, 24.92 and 4.60 mg/g for esterified β-sitosterol, free β-sitosterol and free stigmasterol, respectively. The α-linolenic acid (77.69±6.10% was the principal fatty acid. Regarding the anti-inflammatory activity, the seed oil showed low activity in the early phase of formalin test; however, could not significantly inhibit the neutrophil-induced damage by reducing MPO activity in the paws of the rat. Conclusion: The seed oil did not exhibit satisfactory effects on acute inflammation in this study but considering the rich phytosterols content, the seed and its oil can be introduced as useful dietary supplements.

  4. Antibiotic and anti-inflammatory use and the risk of prostate cancer

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    Bent Stephen

    2009-04-01

    Full Text Available Abstract Background Prostate inflammation or infection may increase the risk of prostate cancer. Antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs are used to treat prostatitis and urinary tract infections (UTIs. The objective of our study was to assess whether their use decreases the risk of prostate cancer. Methods We conducted a case-control study among men with incident prostate cancer (N = 65 cases and without prostate cancer (N = 195 controls at the San Francisco Veteran Affairs medical center (VAMC between June 1996 and June 2006. Cases were all patients who had prostate biopsies positive for cancer. We matched controls to cases on age group and race at a 3:1 ratio, and each matched pair was given an identical index date. Total antibiotic, aspirin, and NSAID use (number of prescriptions was computed for each participant by drug type and was restricted to a fill date at least 1 year before the index date. Logistic regression was used for analysis. We adjusted for the matching variables (age group and race and potential confounders (years of VAMC enrollment and number of clinic visits. Results Neither total antibiotic use nor total anti-inflammatory use reduces the risk of prostate cancer (P > 0.05. Conclusion Our analysis did not reveal a relation between use of antibiotics, aspirin, or NSAIDs and the risk of prostate cancer.

  5. Consumption and awareness of students about nonsteroidal anti-inflammatory drugs

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    Wawryk-Gawda Ewelina

    2014-09-01

    Full Text Available Nonsteroidal anti-inflammatory drugs (NSAIDs are used by millions of people worldwide to neutralize pain that is of different origin, as well as to treat fever and inflammation. However, NSAIDs misuse/overuse can induce many adverse effects and some potentially serious complications. The aim of the our study was to ascertain young people’s knowledge about non-steroidal anti-inflammatory drugs. The research tool was a questionnaire. This study was carried out among students of the Medical University in Lublin, and it involved 236 persons of an average age of 20 years. The questions were intended to assess the frequency of NSAIDs use and the general knowledge that is held with respect to them. The results of this work show that more than 77% of the respondents confirmed that they use NSAIDs. Our results revealed no statistical correlation between the place of living or origin and the use of this drug. Hence, it can be said that while young adults quite often use NSAIDs, their knowledge about the dangers associated with the use of NSAIDs is low. Therefore, it is necessary to more intensively disseminate knowledge on the potential adverse effects of NSAID utilization.

  6. Topical anti-inflammatory activity of yacon leaf extracts

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    Rejane B. Oliveira

    2013-06-01

    Full Text Available Smallanthus sonchifolius (Poepp. H. Rob. , Asteraceae, known as yacon, is an herb that is traditionally used for the treatment of diabetes in folk medicine. However, recent studies have demonstrated that this plant has other interesting properties such as anti-microbial and anti-inflammatory actions. Thus, the purpose of this study was to evaluate the topical anti-inflammatory property of different extracts prepared from yacon leaves and analyze the role of different chemical classes in this activity. Three yacon leaf extracts were obtained: aqueous extract, where chlorogenic acid derivatives and sesquiterpene lactones were detected; leaf rinse extract, rich in sesquiterpene lactones; and polar extract, rich in chlorogenic acid derivatives. All the extracts exhibited anti-edematogenic activity in vivo (aqueous extract: 25.9% edema inhibition at 0.50 mg/ear; polar extract: 42.7% inhibition at 0.25 mg/ear; and leaf rinse extract: 44.1% inhibition at 0.25 mg/ear. The leaf rinse extract furnished the best results regarding neutrophil migration inhibition, and NO, TNF-α and PGE2 inhibition. These data indicate that both sesquiterpene lactones and chlorogenic acid derivatives contribute to the anti-inflammatory action, although sesquiterpene lactones seem to have more pronounced effects. In conclusion, yacon leaf extracts, particularly the sesquiterpene lactone-rich extract, has potential use as topical anti-inflammatory agent.

  7. Marine Diterpenoids as Potential Anti-Inflammatory Agents

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    González, Yisett; Torres-Mendoza, Daniel; Jones, Gillian E.; Fernandez, Patricia L.

    2015-01-01

    The inflammatory response is a highly regulated process, and its dysregulation can lead to the establishment of chronic inflammation and, in some cases, to death. Inflammation is the cause of several diseases, including rheumatoid arthritis, inflammatory bowel diseases, multiple sclerosis, and asthma. The search for agents inhibiting inflammation is a great challenge as the inflammatory response plays an important role in the defense of the host to infections. Marine invertebrates are exceptional sources of new natural products, and among those diterpenoids secondary metabolites exhibit notable anti-inflammatory properties. Novel anti-inflammatory diterpenoids, exclusively produced by marine organisms, have been identified and synthetic molecules based on those structures have been obtained. The anti-inflammatory activity of marine diterpenoids has been attributed to the inhibition of Nuclear Factor-κB activation and to the modulation of arachidonic acid metabolism. However, more research is necessary to describe the mechanisms of action of these secondary metabolites. This review is a compilation of marine diterpenoids, mainly isolated from corals, which have been described as potential anti-inflammatory molecules. PMID:26538822

  8. Anti-inflammatory activity of some traditional medicinal plants.

    Science.gov (United States)

    Singh, R K; Joshi, V K; Gambhir, S S

    1998-10-01

    The ethanol extract of roots, fruits and roots of solanum indicum and saccharum munja respectively and water soluble resin of commiphora myrrha were studied for antiinflammatory activity against carrageenin induced oedema in rats, the significant antiinflammatory activity were found in former two plants will slight anti inflammatory activity was observed in latter plant.

  9. Anti-Inflammatory Activity of N-(3-Florophenylethylcaffeamide in Mice

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    Yueh-Hsiung Kuo

    2013-07-01

    Full Text Available In this study, we evaluated the anti-inflammatory activity of one synthetic product, N-(3-Florophenylethylcaffeamide (abbrev. FECA, by using animal model of λ-carrageenan-induced paw edema in mice. The anti-inflammatory mechanism of FECA was determined by measuring the levels of cyclooxygenase-2 (COX-2, nitric oxide (NO, tumor necrosis factor (TNF-α, interleukin-1β (IL-1β, and malondialdehyde (MDA in the edema paw tissue, and the activities of superoxide dismutase (SOD, glutathione peroxidase (GPx, and glutathione reductase (GRd in the liver. The results showed that FECA reduced the paw edema at three, four and five hours after λ-carrageenan administration. The levels of COX-2, NO, TNF-α, and MDA in the λ-carrageenan-induced edema paws were reduced and the activities of SOD, GPx, and GRd in liver tissues were raised by FECA. These results suggested that FECA possessed anti-inflammatory activities and the anti-inflammatory mechanisms might be related to the decrease of the levels of COX-2, NO, and TNF-α in inflamed tissues and the increase in the MDA level by increasing the activities of SOD, GPx, and GRd.

  10. Nonsteroidal Anti-Inflammatory Drug Hypersensitivity in Preschool Children

    OpenAIRE

    Kidon Mona; Kang Liew; Chin Chiang; Hoon Lim; Hugo,, Argentiniensis, (ca. 1210-ca. 1270)

    2007-01-01

    Although extensively studied in adults, nonsteroidal anti-inflammatory drug (NSAID) hypersensitivity in children, especially in young children, remains poorly defined. Pediatricians, prescribing antipyretics for children, rarely encounter significant problems, but the few epidemiologic studies performed show conflicting results. Although it is clear that some patients with acetylsalicylic acid (ASA)-sensitive asthma have their clinical onset of disease in childhood and bronchoconstriction af...

  11. Anti-inflammatory defense mechanisms of Entamoeba histolytica.

    Science.gov (United States)

    Silva-García, Raúl; Rico-Rosillo, Guadalupe

    2011-02-01

    The monocyte locomotion inhibitory factor (MLIF), a heat-stable oligopeptide found in the supernatant fluid of Entamoeba histolytica axenic cultures, may contribute to the delayed inflammation observed in amoebic hepatic abscess. This factor was isolated by ultra-filtration and high powered liquid chromatography, obtaining a primary Met-Gln-Cys-Asn-Ser structure, identified afterwards as the carboxyl-terminal (…Cys-Asn-Ser) active site. The selective anti-inflammatory effects of the pentapeptide have been observed in both in vitro and in vivo models, using a synthetic pentapeptide to maintain the same anti-inflammatory conditions during the experimental assays. Anti-inflammatory effects observed include inhibition of human monocyte locomotion and the respiratory burst in monocytes and neutrophils, increasing expression of anti-inflammatory cytokines and inhibiting expression of the adhesion molecules VLA-4 and VCAM, among others. In this review, we will describe the effects of MLIF detected so far and how it might be used as a therapeutical agent against inflammatory diseases.

  12. Glycosaminoglycan analogs as a novel anti-inflammatory strategy

    Science.gov (United States)

    Severin, India C.; Soares, Adriano; Hantson, Jennifer; Teixeira, Mauro; Sachs, Daniela; Valognes, Delphine; Scheer, Alexander; Schwarz, Matthias K.; Wells, Timothy N. C.; Proudfoot, Amanda E. I.; Shaw, Jeffrey

    2012-01-01

    Heparin, a glycosaminoglycan (GAG), has both anti-inflammatory and anti-coagulant properties. The clinical use of heparin against inflammation, however, has been limited by concerns about increased bleeding. While the anti-coagulant activity of heparin is well understood, its anti-inflammatory properties are less so. Heparin is known to bind to certain cytokines, including chemokines, small proteins which mediate inflammation through their control of leukocyte migration and activation. Molecules which can interrupt the chemokine-GAG interaction without inhibiting coagulation could therefore, represent a new class of anti-inflammatory agents. In the present study, two approaches were undertaken, both focusing on the heparin-chemokine relationship. In the first, a structure based strategy was used: after an initial screening of potential small molecule binders using protein NMR on a target chemokine, binding molecules were optimized through structure-based design. In the second approach, commercially available short oligosaccharides were polysulfated. In vitro, these molecules prevented chemokine-GAG binding and chemokine receptor activation without disrupting coagulation. However, in vivo, these compounds caused variable results in a murine peritoneal recruitment assay, with a general increase of cell recruitment. In more disease specific models, such as antigen-induced arthritis and delayed-type hypersensitivity, an overall decrease in inflammation was noted, suggesting that the primary anti-inflammatory effect may also involve factors beyond the chemokine system. PMID:23087686

  13. The Use of Nonsteroidal Anti-Inflammatory Drugs in Sports.

    Science.gov (United States)

    Calabrese, Leonard H.; Rooney, Theodore W.

    1986-01-01

    Recent advances in the understanding of the mechanism of action and clinical pharmacology of the new nonsteroidal anti-inflammatory drugs (NSAIDs) can help practitioners decide which to use and how to administer them. Indications for and effects of NSAIDs are described. (MT)

  14. Anti-Inflammatory Activity of Compounds Isolated from Plants

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    R.M. Perez G.

    2001-01-01

    Full Text Available This review shows over 300 compounds isolated and identified from plants that previously demonstrated anti-inflammatory activity. They have been classified in appropriate chemical groups and data are reported on their pharmacological effects, mechanisms of action, and other properties.

  15. Salivary gland derived peptides as a new class of anti-inflammatory agents: review of preclinical pharmacology of C-terminal peptides of SMR1 protein

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    Befus A Dean

    2010-09-01

    Full Text Available Abstract The limitations of steroidal and non steroidal anti-inflammatory drugs have prompted investigation into other biologically based therapeutics, and identification of immune selective anti-inflammatory agents of salivary origin. The traditional view of salivary glands as accessory digestive structures is changing as their importance as sources of systemically active immunoregulatory and anti-inflammatory factors is recognized. Salivary gland involvement in maintenance of whole body homeostasis is regulated by the nervous system and thus constitutes a "neuroendocrine axis". The potent anti-inflammatory activities, both in vivo and in vitro, of the tripeptide Phe-Glu-Gly (FEG are reviewed. FEG is a carboxyl terminal peptide of the prohormone SMR1 identified in the rat submandibular salivary gland, The D-isomeric form (feG mimics the activity of its L-isomer FEG. Macropharmacologically, feG attenuates the cardiovascular and inflammatory effects of endotoxemia and anaphylaxis, by inhibition of hypotension, leukocyte migration, vascular leak, and disruption of pulmonary function and intestinal motility. Mechanistically, feG affects activated inflammatory cells, especially neutrophils, by regulating integrins and inhibiting intracellular production of reactive oxygen species. Pharmacodynamically, feG is active at low doses (100 μg/kg and has a long (9-12 hour biological half life. As a therapeutic agent, feG shows promise in diseases characterized by over exuberant inflammatory responses such as systemic inflammatory response syndrome and other acute inflammatory diseases. Arthritis, sepsis, acute pancreatitis, asthma, acute respiratory inflammation, inflammatory bowel disease, and equine laminitis are potential targets for this promising therapeutic peptide. The term "Immune Selective Anti-Inflammatory Derivatives" (ImSAIDs is proposed for salivary-derived peptides to distinguish this class of agents from corticosteroids and nonsteroidal anti-inflammatory

  16. Antinociceptive and Anti-inflammatory Activities of a Chinese Herbal Recipe (DJW in Animal Models

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    P Kunanusorn

    2009-03-01

    Full Text Available Summary: Since in our previous study, Duhuo Jisheng Wan (DJW, which means pill of pubescent angelica root and mulberry mistletoe combination, demonstrates clinically comparable efficacy to diclofenac in the symptomatic treatment of osteoarthritis (OA of the knee after 4 weeks of treatment.  Therefore, in order to verify its mechanisms of action, this study was performed to investigate the antinociceptive and anti-inflammatory activities of DJW in various animal models.  The antinociceptive activity of DJW was investigated by using the formalin test in mice model.  The acute inflammatory model using the carrageenin-induced hind paw edema in rats and the chronic inflammatory model using the cotton pellet-induced granuloma formation in rats were utilized.  Results showed that DJW possessed a marked antinociceptive activity in both phases of the formalin test in mice.  However, in the carrageenin-induced hind paw edema model, which is known to be sensitive to cyclooxygenase (COX inhibitors, DJW showed an insignificant anti-inflammatory effect, and in the cotton pellet-induced granuloma model, it had no antigranuloma formation and showed no effect on the transudate weight.  In addition, DJW showed no suppressive effects on weight gain and the thymus weight of the rats.  In conclusion, the overall results demonstrate that DJW possess both central and peripheral antinociceptive activities.  However, its anti-inflammatory activity, if any, could not be demonstrated in these two inflammatory models in the present study and remains to be elucidate.   Industrial relevance: Since drug therapy in OA patients, such as paracetamol, non-steroidal anti-inflammatory drugs (NSAIDs, and topical analgesics may prove ineffective in some patients, and long-term therapy with NSAIDs often have been associated with serious adverse effects.  Such patients are turning increasingly to herbal medicines and DJW may be an alternative since it demonstrates clinically

  17. Anti-inflammatory drug delivery from hyaluronic acid hydrogels.

    Science.gov (United States)

    Hahn, Sei K; Jelacic, Sandra; Maier, Ronald V; Stayton, Patrick S; Hoffman, Allan S

    2004-01-01

    Two different types of hyaluronic acid (HA) hydrogels were synthesized by crosslinking HA with divinyl sulfone (DVS) and poly(ethylene glycol)-divinyl sulfone (VS-PEG-VS). Vitamin E succinate (VES), an anti-inflammatory drug, and bovine serum albumin (BSA), a model of anti-inflammatory protein drugs, were loaded into the gels and their release kinetics were measured in vitro. VES and BSA released with a burst from both HA hydrogels during the first few hours, and release continued gradually for several days. The rate of release from HA-VS-PEG-VS-HA hydrogels was faster than that from HA-DVS-HA hydrogels, presumably due to the lower crosslink density in the former. The anti-inflammatory action of released VES was tested by incubating peripheral blood mononuclear cells (PBMC) on HA hydrogels with and without VES in the gel. The number of cells adhering on HA hydrogels was very low compared to that on tissue culture polystyrene (TCPS), which might be one of the important advantages of using HA hydrogels for implant coatings or tissue engineering applications. ELISA test results showed that the tumor necrosis factor-alpha (TNF-alpha) concentration was very low in the supernatant of the wells containing the HA hydrogel with VES in contact with the activated macrophages compared to that without VES. This is probably the effect of the released VES reducing the production of anti-inflammatory cytokine, TNF-alpha. HA hydrogels containing anti-inflammatory drugs may have potential for use in tissue engineering and also as biocompatible coatings of implants. PMID:15503629

  18. Bioengineered Colorectal Cancer Drugs: Orally Delivered Anti-Inflammatory Agents.

    Science.gov (United States)

    Urbanska, Aleksandra Malgorzata; Zhang, Xiaoying; Prakash, Satya

    2015-07-01

    Intestinal inflammation is one of the major factors that increase colorectal cancer (CRC) incidence worldwide. Inflammation in the gastrointestinal tract is directly linked to tumor development at the early stages of the disease, thus a key issue toward the prevention and the treatment of colonic neoplasia. Thus, the use of anti-inflammatory drugs has emerged first as a strategy to reduce chronic inflammation in case of many inflammatory bowel diseases (IBD), but it has proven its efficacy by reducing the risk of colonic neoplasia. This comprehensive review highlights the role of chronic inflammation, mainly in IBD, in the development of CRC including molecular and immune mechanisms that have tumorigenic effects. Multiple lines of evidence indicate that several bioactive and phytochemical compounds used as anti-inflammatory drugs have also antitumoral attributes. The uses of orally delivered cytokines and small molecules, as well as key dietary supplementation as anti-inflammatory therapeutics are discussed. In addition, comprehensive knowledge about CRC and intestinal inflammation, and the importance of the intestinal mucosal wall as a mucosal immunological barrier that comes into play during interactions with gut microbiota (pathogens and commensal), luminal secretions (bile acids, and bacterial and epithelial metabolites), and ingested chemicals (food components, high fat content, heterocyclic amines, and low intake of dietary fiber) are underscored. The multifunctionality of several anti-inflammatory drugs opens a line for their application in the treatment and prevention not only in IBD but also in CRC. Current bioengineering approaches for oral delivery of anti-inflammatory agents including cytokines, genetically modified bacteria, or small molecule inhibitors of inflammation directly contribute to the early management of CRC. Limitations of the current therapeutics, which stem from the lack of complete understanding of the complex molecular interactions

  19. Use of nonsteroidal anti-inflammatory drugs in patients with vertebral osteoporotic fractures

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    R. Bortolotti

    2011-09-01

    Full Text Available Objective: The aim of the study was to assess the use of Non Steroidal Anti-Inflammatory Drugs (NSAIDs in patients with a history of osteoporotic vertebral fractures. Methods: We investigated 119 patients with postmenopausal osteoporosis complicated by one or more non recent vertebral fractures. Results: More than 60% of the patients took at least one dose of NSAID weekly. The most prescribed NSAID was nimesulide, at a dose with an exclusively antalgic effect. Patients with wedge fracture and those with a documented vertebral fracture in the last 12 months were those taking NSAIDs more frequently. 77% of the patients that used NSAIDs had concomitant features of osteoarthritis, mainly at the spine or at the knee. The use of NSAIDs was negatively related to the use of specific therapy for osteoporosis, particularly for oral daily tablets. Conclusions: This study highlights the significant use of NSAIDs in patients with osteoporotic vertebral fractures and the overlap between osteoporosis, osteoarthritis and related treatments.

  20. [Longterm effects of steroid therapy].

    Science.gov (United States)

    Kuna, P

    1998-01-01

    Asthma is a chronic inflammatory disease of the airways play. Anti-inflammatory drugs the fundamental role in the treatment of asthma and among them steroids are the most important. However, oral steroids may cause many serious side effects. A major breakthrough in the treatment of asthma was introducing inhaled steroids. Inhaled steroids have much less side effects than oral steroids, although they have the same anti-inflammatory activity. Long term effect of inhaled steroids can be divided into wanted and unwanted outcome. The desirable anti-inflammatory effect of steroids is reflected by lowering of bronchial hyperresponsiveness and a better control of asthma symptoms. Inhaled corticosteroid may have systemic side effects similar to those observed with oral steroids such as 1) adrenal suppression, 2) effect on bone metabolism, 3) growth suppression in children, 4) impaired skin collagen synthesis, 5) cataract, 6) metabolic disturbances, 7) effect on central nervous system. Topical side effects of inhaled corticosteroid such as oral candidiasis, dysphonia and cough effect about 10 to 30% of patients taking those drugs. Summing up it is advisable to use inhaled corticosteroid in the lower effective dose. PMID:9610231

  1. Use of anti-inflammatory and analgesic drugs in dogs and cats.

    Science.gov (United States)

    Watson, A D; Nicholson, A; Church, D B; Pearson, M R

    1996-09-01

    Responses (486) were collared from a survey of 5054 Australian veterinarians on their use of anti-inflammatory and analgesic drugs in dogs and cats. Almost all respondents used glucocorticoids (usually prednisolone) to treat allergic, pruritic dermatoses in dogs, while two-thirds also gave fatty acid supplements and one-half used antihistamines. Almost 60% of respondents initially injected a glucocorticoid (frequently a long-acting preparation) when treating inflammatory skin diseases in dogs. More than 90% of respondents used glucocorticoids to treat immune-mediated haemolytic anaemia or thrombocytopenia, and about one-third also gave cytotoxic drugs. Administration of prednisolone on alternate days was generally favoured for long-term enteral steroid therapy. Phenylbutazone was the most preferred treatment for painful or inflammatory musculoskeletal disorders of dogs, but aspirin and pentosan polysulphate were also used widely. Regarding the use of analgesics drugs generally, both narcotic analgesics and non-steroidal anti-inflammatory drugs (NSAIDs) were used more widely in dogs than in cats, but alpha-2 agonists were used similarly in both species. The most commonly used narcotic analgesics were pethidine and buprenorphine in both species, while the NSAIDs used most often were flunixin and dipyrone in dogs and ketoprofen in cats. More than 80% of respondents generally used analgesic drugs with potentially painful surgical procedures, with doses given usually before anaesthetic recovery. Analgesic use rates varied with the condition, ranging from 94% for patients with acute severe trauma, through 60% for cruciate ligament repair and 29% for perineal herniorrahphy, to about 5% for ovariohysterectomy and dog castration. The three clinical signs most frequently nominated as indicators of pain in dogs and cats were (in descending order) vocalisation, response to handling or palpating the affected area, and mental depression. Other items mentioned frequently were

  2. Spasmolytic and anti-inflammatory effects of Aloysia triphylla and citral, in vitro and in vivo studies.

    Science.gov (United States)

    Ponce-Monter, Héctor; Fernández-Martínez, Eduardo; Ortiz, Mario I; Ramírez-Montiel, Martha L; Cruz-Elizalde, Delia; Pérez-Hernández, Nury; Cariño-Cortés, Raquel

    2010-01-01

    Aloysia triphylla is traditionally utilized for the treatment of menstrual colic (primary dysmenorrhea) in Mexico. Citral is the main chemical component found in Aloysia triphylla leaves extract. Primary dysmenorrhea is a very frequent gynecological disorder in menstruating women, affecting 30-60% of them. It is usually treated with non-steroidal anti-inflammatory drugs (NSAIDs); although their effect is rapid, they possess many side effects. Due to these shortcomings, Mexican folk therapy is considered as a feasible alternative. The effects of the hexane extract of Aloysia triphylla and citral on uterine contractions were evaluated in vitro as well as their anti-inflammatory properties and gastric wound capabilities were assessed in vivo. The inhibitory effects on the contractions were analyzed using isolated uterus strips from estrogen primed rats. Contractions were induced by KCl 60 mM, oxytocin 10 mIU/mL, charbacol 10 µM and PGF(2α) 5 µM. The anti-inflammatory effect was assessed on carrageenan-induced rat hind paw edema model. The inhibitory concentration-50 (IC(50)) of the hexane extract of Aloysia triphylla upon each contractile response was for KCl 44.73 ± 2.48 µg/mL, oxytocin 42.16 ± 3.81 µg/mL, charbacol 41.87 ± 1.73 µg/mL and PGF(2α) 28.70 ± 2.40 µg/mL in a concentration-dependent way. The extract of Aloysia triphylla produced a significant inhibitory effect on PGF(2α)-induced contraction compared to its inhibitory actions on the others. Citral exhibited the same inhibitory effect on the contraction induced by PGF(2α). The oral administration of the extract (100-800 mg/kg) and citral (100-800 mg/kg) showed anti-inflammatory activity; furthermore, the maximal dose utilized did not produce gastric injury. These results were compared with anti-inflammatory effects and gastric damage produced by 30 mg/kg of indomethacin p.o. The spasmolytic and anti-inflammatory effects support the traditional use of Aloysia triphylla leaves in the treatment of

  3. Chemical constituents of Machaerium hirtum Vell. (Fabaceae) leaves and branches and its anti-inflammatory activity evaluation.

    Science.gov (United States)

    Ignoato, Marlene C; Fabrão, Rodrigo M; Schuquel, Ivânia T A; Botelho, Marcos F P; Bannwart, Geanderson; Pomini, Armando M; Arruda, Laura L M; Bersani-Amado, Ciomar A; Santin, Silvana M O

    2013-01-01

    Leaves and branches of Machaerium hirtum Vell. (Fabaceae), native to South America, were subjected to phytopharmacological investigation in order to identify its major chemical constituents and evaluate its extracts, fractions and isolated compounds in assays for anti-inflammatory activities. These were performed using mouse ear edema model, pleurisy and myeloperoxidase activity assays. Six compounds were isolated and identified as the flavanones swertisin and isovitexin, the alkaloid 4-hydroxy-N-methylproline, the triterpenes friedelin and lupeol, and the steroids sitosterol and stigmasterol. These compounds were identified by nuclear magnetic resonance of (1)H and (13)C data, in comparison with literature. PMID:23126578

  4. Anti-inflammatory and antipyretic effects of boldine.

    Science.gov (United States)

    Backhouse, N; Delporte, C; Givernau, M; Cassels, B K; Valenzuela, A; Speisky, H

    1994-10-01

    Boldine, an antioxidant alkaloid isolated from Peumus boldus, exhibits a dose-dependent anti-inflammatory activity in the carrageenan-induced guinea pig paw edema test with an oral ED50 of 34 mg/kg. Boldine also reduces bacterial pyrogen-induced hyperthermia in rabbits to an extent which varied between 51% and 98% at a dose of 60 mg/kg p.o. In vitro studies carried out in rat aortal rings revealed that boldine is an effective inhibitor of prostaglandin biosynthesis, promoting 53% inhibition at 75 microM. The latter in vitro effect may be mechanistically linked to the anti-inflammatory and antipyretic effects of boldine exerted in vivo. PMID:7879695

  5. Novel anti-inflammatory therapies for the treatment of atherosclerosis.

    Science.gov (United States)

    Khan, Razi; Spagnoli, Vincent; Tardif, Jean-Claude; L'Allier, Philippe L

    2015-06-01

    The underlying role of inflammation in atherosclerosis has been characterized. However, current treatment of coronary artery disease (CAD) predominantly consists of targeted reductions in serum lipoprotein levels rather than combating the deleterious effects of acute and chronic inflammation. Vascular inflammation acts by a number of different molecular and cellular pathways to contribute to atherogenesis. Over the last decades, both basic studies and clinical trials have provided evidence for the potential benefits of treatment of inflammation in CAD. During this period, development of pharmacotherapies directed towards inflammation in atherosclerosis has accelerated quickly. This review will highlight specific therapies targeting interleukin-1β (IL-1β), P-selectin and 5-lipoxygenase (5-LO). It will also aim to examine the anti-inflammatory effects of serpin administration, colchicine and intravenous HDL-directed treatment of CAD. We summarize the mechanistic rationale and evidence for these novel anti-inflammatory treatments at both the experimental and clinical levels.

  6. Proteomic analysis of the anti-inflammatory action of minocycline

    OpenAIRE

    Dunston, Christopher R; Helen R Griffiths; Lambert, Peter A; Staddon, Susan; Vernallis, Ann B

    2010-01-01

    Minocycline possesses anti-inflammatory properties independently of its antibiotic activity although the underlying molecular mechanisms are unclear. Lipopolysaccharide (LPS)-induced cytokines and pro-inflammatory protein expression are reduced by minocycline in cultured macrophages. Here, we tested a range of clinically important tetracycline compounds (oxytetracycline, doxycycline, minocycline and tigecycline) and showed that they all inhibited LPS-induced nitric oxide production. We made t...

  7. Anti-inflammatory cyclohexenyl chalcone derivatives in Boesenbergia pandurata.

    Science.gov (United States)

    Tuchinda, Patoomratana; Reutrakul, Vichai; Claeson, Per; Pongprayoon, Ubonwan; Sematong, Tuanta; Santisuk, Thawatchai; Taylor, Walter C

    2002-01-01

    The cyclohexenyl chalcone derivative [(-)-hydroxypanduratin A], together with the previously known panduratin A, sakuranetin, pinostrobin, pinocembrin, and dihydro-5,6-dehydrokawain were isolated from the chloroform extract of the red rhizome variety of Boesenbergia pandurata (Robx.) Schltr. [currently known as Boesenbergia rotunda (L.) Mansf., Kulturpfl.]. Their structures were assigned on the basis of their spectroscopic data. (-)-Hydroxypanduratin A and (-)-panduratin A showed significant topical anti-inflammatory activity in the assay of TPA-induced ear edema in rats. PMID:11809452

  8. Gastrointestinal and Cardiovascular Risk of Nonsteroidal Anti-inflammatory Drugs

    OpenAIRE

    Abdulwahed Al-Saeed

    2011-01-01

     Nonsteroidal anti-inflammatory drugs (NSAIDs) confer a gastrointestinal (GI) side effect profile and concerns regarding adverse cardiovascular effects have emerged associated with considerable morbidity and mortality. NSAIDs are highly effective in treating pain and inflammation, but it is well recognized that these agents are associated with substantial gastrointestinal toxicity. Cyclo-oxygenase-2 inhibitors may also reduce the risk for gastrointestinal events, although they may increase ca...

  9. Hepatoprotective and anti-inflammatory activities of Plantago major L.

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    Turel Idris

    2009-01-01

    Full Text Available Objective: The aim of this study was to investigate anti-inflammatory and hepatoprotective activities of Plantago major L. (PM. Materials and Methods: Anti-inflammatory activity: Control and reference groups were administered isotonic saline solution (ISS and indomethacin, respectively. Plantago major groups were injected PM in doses of 5 mg/kg (PM-I, 10 mg/kg (PM-II, 20 mg/kg (PM-III and 25 mg/kg (PM-IV. Before and three hours after the injections, the volume of right hind-paw of rats was measured using a plethysmometer. Hepatoprotective Activity: The hepatotoxicity was induced by carbon tetrachloride (CCl4 administration. Control, CCl4 and reference groups received isotonic saline solution, CCl4 and silibinin, respectively. Plantago major groups received CCl4 (0.8 ml/kg and PM in doses of 10, 20 and 25 mg/kg, respectively for seven days. Blood samples and liver were collected on the 8th day after the animals were killed. Results: Plantago major had an anti-inflammatory effect matching to that of control group at doses of 20 and 25 mg/kg. It was found that reduction in the inflammation was 90.01% with indomethacin, 3.10% with PM-I, 41.56% with PM-II, 45.87% with PM-III and 49.76% with PM-IV. Median effective dose (ED50 value of PM was found to be 7.507 mg/kg. Plantago major (25 mg/kg significantly reduced the serum alanine aminotransferase (ALT and aspartate aminotransferase (AST levels when compared to the CCl4 group. The histopathological findings showed a significant difference between the PM (25 mg/kg and CCl4 groups. Conclusion: The results showed that PM had a considerable anti-inflammatory and hepatoprotective activities.

  10. Anti-inflammatory and antimicrobial activities of novel pyrazole analogues.

    Science.gov (United States)

    Surendra Kumar, R; Arif, Ibrahim A; Ahamed, Anis; Idhayadhulla, Akbar

    2016-09-01

    A new sequence of pyrazole derivatives (1-6) was synthesized from condensation technique under utilizing ultrasound irradiation. Synthesized compounds were characterized from IR, (1)H NMR, (13)C NMR, Mass and elemental analysis. Synthesized compounds (1-6) were screened for antimicrobial activity. Among the compounds 3 (MIC: 0.25 μg/mL) was exceedingly antibacterially active against gram negative bacteria of Escherichia coli and compound 4 (MIC: 0.25 μg/mL) was highly active against gram positive bacteria of Streptococcus epidermidis compared with standard Ciprofloxacin. Compound 2 (MIC: 1 μg/mL) was highly antifungal active against Aspergillus niger proportionate to Clotrimazole. Synthesized compounds (1-6) were screened for anti-inflammatory activity and the compound 2-((5-hydroxy-3-methyl-1H-pyrazol-4-yl)(4-nitrophenyl)methyl)hydrazinecarboxamide (4) was better activity against anti-inflammatory when compared with standard drugs (Diclofenac sodium). Compounds (2, 3 and 4) are the most important molecules and hence the need to develop new drugs of antibacterial, antifungal and anti-inflammatory agents. PMID:27579011

  11. Anti-Inflammatory Activity and Composition of Senecio salignus Kunth

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    Cuauhtemoc Pérez González

    2013-01-01

    Full Text Available We investigated the anti-inflammatory activity of Senecio salignus. This medicinal plant is often used in Mexico for the treatment of fever and rheumatism. Chloroform and methanol extracts of the plant were tested on 12-O-tetradecanoylphorbol-13-acetate- (TPA- induced edema in mice ears. The methanol extract of the plant inhibited edema by 36±4.4% compared with the control, while the chloroform extract exhibited an even greater level of inhibition (64.1%. The chloroform extract was then fractionated, and the composition of the active fraction was determined by GC-MS. The anti-inflammatory activity of this fraction was then tested on TPA-induced ear edema in mice, and we found that the active fraction could inhibit edema by 46.9%. The anti-inflammatory effect of the fraction was also tested on carrageenan-induced paw edema in rats at doses of 100 mg/kg; a 58.9±2.8% reduction of the edema was observed 4 h after administration of carrageenan, and the effect was maintained for 5 h.

  12. Anti-inflammatory activity and composition of Senecio salignus Kunth.

    Science.gov (United States)

    González, Cuauhtemoc Pérez; Vega, Roberto Serrano; González-Chávez, Marco; Sánchez, Miguel Angel Zavala; Gutiérrez, Salud Pérez

    2013-01-01

    We investigated the anti-inflammatory activity of Senecio salignus. This medicinal plant is often used in Mexico for the treatment of fever and rheumatism. Chloroform and methanol extracts of the plant were tested on 12-O-tetradecanoylphorbol-13-acetate- (TPA-) induced edema in mice ears. The methanol extract of the plant inhibited edema by 36 ± 4.4% compared with the control, while the chloroform extract exhibited an even greater level of inhibition (64.1%). The chloroform extract was then fractionated, and the composition of the active fraction was determined by GC-MS. The anti-inflammatory activity of this fraction was then tested on TPA-induced ear edema in mice, and we found that the active fraction could inhibit edema by 46.9%. The anti-inflammatory effect of the fraction was also tested on carrageenan-induced paw edema in rats at doses of 100 mg/kg; a 58.9 ± 2.8% reduction of the edema was observed 4 h after administration of carrageenan, and the effect was maintained for 5 h. PMID:23691512

  13. Anti-inflammatory activity in selected Antarctic benthic organisms

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    Juan eMoles

    2014-07-01

    Full Text Available Antarctic benthos was prospected in search for anti-inflammatory activity in polar benthic invertebrates, in two different geographical areas: deep-bottoms of the Eastern Weddell Sea and shallow-waters of the South Shetland Islands. A total of 36 benthic algae and invertebrate species were selected to perform solubility tests in order to test them for anti-inflammatory activity. From these, ethanol extracts of ten species from five different phyla resulted suitable to be studied in cell macrophage cultures (RAW 264.7. Cytotoxicity (MTT method and production of inflammatory mediators (prostaglandin E2, leukotriene B4, interleukin-1 were determined at three extract concentrations (50, 125, 250 g/mL. Bioassays resulted in four different species showing anti-inflammatory activity corresponding to three sponges: Mycale (Oxymycale acerata, Isodictya erinacea, and I. toxophila; and one hemichordate: Cephalodiscus sp. These results show that Antarctic sessile invertebrates may have great value as a source of lead compounds with potential pharmaceutical applications.

  14. Anti-inflammatory activities of selected synthetic homoisoflavanones.

    Science.gov (United States)

    Shaikh, Mahidansha M; Kruger, Hendrik G; Bodenstein, Johannes; Smith, Peter; du Toit, Karen

    2012-01-01

    Four homoisoflavanones of the 3-benzylidene-4-chromanone type, some of which were previously isolated from Caesalpinia pulcherrima, were synthesised to determine their anti-inflammatory activity and cytotoxicity. A range of four different homoisoflavanones (compounds 4a-4d) were synthesised from the corresponding substituted phenols. ¹H- and ¹³C-NMR data together with high-resolution mass spectroscopy data were employed to elucidate the structures. Anti-inflammatory activity was determined in mice with acute croton oil-induced auricular dermatitis. In vitro cytotoxicity was tested against a Chinese hamster ovarian cell line using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide (MTT) assay. Compound 4a exhibited a tendency to inhibit oedema in a dose-dependent manner after 3 and 6 h of treatment. Compounds 4b-4d also inhibited oedema, although a clear dose-response relationship was not observed. Compounds 4a-4c were found to be less cytotoxic than compound 4d. Compound 4b was the least cytotoxic. Compounds 4a-4d exhibited anti-inflammatory activity and varying levels of cytotoxicity. PMID:21950651

  15. Anti-Inflammatory and Antimicrobial activity of Flacourtia Ramontchi Leaves

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    Sulbha Lalsare

    2011-06-01

    Full Text Available The literature survey revealed that a very merge amount of pharmacological work has been carried out on Flacourtia ramontchi. Also it was observed from the Ayurvedic literature and Ethnobotanical studies that the plant is very useful in treating inflammation and infectious diseases but no scientific investigation has been done in such direction. Very merge work has been done regarding phytochemical and pharmacological effectiveness on this plant. Successive extraction of the leaves with solvents of increasing polarity; preliminary phytochemical studies of different extracts; screening of chloroform, methanol and hydromethanolic extracts for anti-inflammatory (by Carrageenan induced rat paw model and antimicrobial activity (by Cup and plate method and thin layer chromatographic studies of active extracts using mobile phase i.e. chloroform and methanol. The results clearly indicate that all three extracts i.e. chloroform, methanol and hydromethanolic, of the leaves having anti-inflammatory activity. But the chloroform and methano extract showed promising results and even chloroform extract at the dose 150mg/kg exhibits equipotent anti-inflammatory activity as that of the standard Indomethacin. Methanol extract possess broad-spectrum antimicrobial activity at concentration 10000 mg/ml whereas hydromethanolic and chloroform extracts having more or less antimicrobial activity.

  16. Anti-inflammatory activity and chemical profile of Galphimia glauca.

    Science.gov (United States)

    González-Cortazar, Manasés; Herrera-Ruiz, Maribel; Zamilpa, Alejandro; Jiménez-Ferrer, Enrique; Marquina, Silvia; Alvarez, Laura; Tortoriello, Jaime

    2014-01-01

    Galphimia glauca, commonly known as "flor de estrella", is a plant species used in Mexican traditional medicine for the treatment of different diseases that have an acute or chronic inflammatory process in common. Aerial parts of this plant contain nor-seco-triterpenoids with anxiolytic properties, which have been denominated galphimines. Other compounds identified in the plant are tetragalloyl-quinic acid, gallic acid, and quercetin, which are able to inhibit the bronchial obstruction induced by platelet-activating factor. The objective of this work was to evaluate the anti-inflammatory effect of crude extracts from G. glauca and, by means of bioguided chemical separation, to identify the compounds responsible for this pharmacological activity. n-Hexane, ethyl acetate, dichloromethane, and methanol extracts showed an important anti-inflammatory effect. Chemical separation of the active methanol extract allowed us to identify the nor-seco-triterpenes galphimine-A (1) and galphimine-E (3) as the anti-inflammatory principles. Analysis of structure-activity relationships evidenced that the presence of an oxygenated function in C6 is absolutely necessary to show activity. In this work, the isolation and structural elucidation of two new nor-seco-triterpenes denominated as galphimine-K (4) and galphimine-L (5), together with different alkanes, fatty acids, as well as three flavonoids (17-19), are described, to our knowledge for the first time, from Galphimia glauca.

  17. Anti-inflammatory effect of thalidomide dithiocarbamate and dithioate analogs.

    Science.gov (United States)

    Talaat, Roba; El-Sayed, Waheba; Agwa, Hussein S; Gamal-Eldeen, Amira M; Moawia, Shaden; Zahran, Magdy A H

    2015-08-01

    Thalidomide has anti-inflammatory, immunomodulatory, and anti-angiogenic properties. It has been used to treat a variety of cancers and autoimmune diseases. This study aimed to characterize anti-inflammatory activities of novel thalidomide analogs by exploring their effects on splenocytes proliferation and macrophage functions and their antioxidant activity. MTT assay was used to assess the cytotoxic effect of thalidomide analogs against splenocytes. Tumor necrosis factor (TNF-α) and nuclear factor kappa B (NF-κB-P65) were determined by enzyme-linked immunosorbent assay (ELISA). Nitric oxide (NO) was estimated by colorimetric assay. Antioxidant activity was examined by ORAC assay. Our results demonstrated that thalidomide dithioate analog 2 and thalidomide dithiocarbamate analog 4 produced a slight increase in splenocyte proliferation compared with thalidomide. Thalidomide dithiocarbamate analog 1 is a potent inhibitor of TNF-α production, whereas thalidomide dithiocarbamate analog 5 is a potent inhibitor of both TNF-α and NO. Analog 2 has a pronounced inhibitory effect on NF-κB-P65 production level. All thalidomide analogs showed prooxidant activity against hydroxyl (OH) radical. Analog 1 and thalidomide dithioate analog 3 have prooxidant activity against peroxyl (ROO) radical in relation to thalidomide. On the other hand, analog 4 has a potent scavenging capacity against peroxyl (ROO) radical compared with thalidomide. Taken together, the results of this study suggest that thalidomide analogs might have valuable anti-inflammatory activities with more pronounced effect than thalidomide itself.

  18. Association of terpinolene and diclofenac presents antinociceptive and anti-inflammatory synergistic effects in a model of chronic inflammation

    Directory of Open Access Journals (Sweden)

    E.M.A. Macedo

    2016-01-01

    Full Text Available Pharmacological treatment of inflammatory pain is usually done by administration of non-steroidal anti-inflammatory drugs (NSAIDs. These drugs present high efficacy, although side effects are common, especially gastrointestinal lesions. One of the pharmacological strategies to minimize such effects is the combination of drugs and natural products with synergistic analgesic effect. The monoterpene terpinolene (TPL is a chemical constituent of essential oils present in many plant species, which have pharmacological activities, such as analgesic and anti-inflammatory. The association of ineffective doses of TPL and diclofenac (DCF (3.125 and 1.25 mg/kg po, respectively presented antinociceptive and anti-inflammatory effects in the acute (0, 1, 2, 3, 4, 5 and 6 h, after treatment and chronic (10 days inflammatory hyperalgesia induced by Freund's complete adjuvant (CFA in the right hind paw of female Wistar rats (170-230 g, n=6-8. The mechanical hyperalgesia was assessed by the Randall Selitto paw pressure test, which determines the paw withdrawal thresholds. The development of edema was quantified by measuring the volume of the hind paw by plethismography. The TPL/DCF association reduced neutrophils, macrophages and lymphocytes in the histological analysis of the paw, following a standard staining protocol with hematoxylin and eosin and the counts were performed with the aid of optical microscopy after chronic oral administration of these drugs. Moreover, the TPL/DCF association did not induce macroscopic gastric lesions. A possible mechanism of action of the analgesic effect is the involvement of 5-HT2A serotonin receptors, because ketanserin completely reversed the antinociceptive effect of the TPL/DCF association. These results suggest that the TPL/DCF association had a synergistic anti-inflammatory and analgesic effect without causing apparent gastric injury, and that the serotonergic system may be involved in the antinociceptive effect of this

  19. Intralesional steroid induced histological changes in the skin

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    Kaur S

    2003-05-01

    Full Text Available Intralesional steroids are commonly used in dermatology. Besides their strong anti-inflammatory effects, the long acting steroids and other preservative agents may induce interesting histopatholoical changes, which may simulate focal mucinosis or a granulomatous pathology. A variety of histopathological changes induced by Intralesional injection of steroid in a lesion of keloid are being described.

  20. Acute anti-inflammatory activity of ethanolic extract of leaves of Leucas indica by carrageenan induced paw oedema in wistar albino rats

    Directory of Open Access Journals (Sweden)

    Chandrashekar R.

    2013-06-01

    Full Text Available Background: Inflammation is basically a defense phenomenon but can lead to serious pathological conditions. It is treated by various agents with good to moderate success because of both considerable toxicity and side effects. There are various mediators to cause an inflammatory reaction that can contribute to the associated symptoms and tissue injury. Even though non steroidal anti-inflammatory drugs are the most commonly prescribed drugs in the world, their use as anti-inflammatory agents continues to be principally limited by their undesired side effects. Hence, the traditional medical practitioners and scientists are turning towards Indian System of Medicine (ISM. Methods: Dried powdered leaves of Leucas indica were subjected to solvent extraction by using 90 % ethanol. Based on acute oral toxicity study according to Organization for Economic Cooperation and Development (OECD guidelines No. 423, three doses of the test drug 75, 150 & 300mg/kg were selected and subjected to preclinical anti-inflammatory screening by carrageenin induced paw oedema in Wistar Albino rats. Results : Oral administration of Ethanolic Extract Of Leaves of Leucas Indica (EELLI at doses of 150 mg/kg and 300mg/kg showed significant anti-inflammatory activity 52.58% (p<0.01 and 36.87% (p<0.05 respectively compared to control. Conclusion: Even though oral administration of EELLI has shown significant anti-inflammatory activity, further studies are required to evaluate its comprehensive analysis including quantitative / semi quantitative analysis, characterize its chemical structure and assess its pharmacotherapeutic activities with exact mechanism of action as an anti-inflammatory agent. [Int J Basic Clin Pharmacol 2013; 2(3.000: 302-305

  1. Influence of Hydrothermal Treatment on Physicochemical Properties and Drug Release of Anti-Inflammatory Drugs of Intercalated Layered Double Hydroxide Nanoparticles

    OpenAIRE

    Zi Gu; Aihua Wu; Li Li; Zhi Ping (Gordon) Xu

    2014-01-01

    The synthesis method of layered double hydroxides (LDHs) determines nanoparticles’ performance in biomedical applications. In this study, hydrothermal treatment as an important synthesis technique has been examined for its influence on the physicochemical properties and the drug release rate from drug-containing LDHs. We synthesised MgAl–LDHs intercalated with non-steroidal anti-inflammatory drugs (i.e., naproxen, diclofenac and ibuprofen) using a co-precipitation method with or without hy...

  2. Ibuprofen versus steroids: risk and benefit, efficacy and safety

    Directory of Open Access Journals (Sweden)

    M. Giovannini

    2013-10-01

    Full Text Available In the last few years we have observed an upward trend in the employment of ibuprofen as anti-inflammatory and antipyretic therapy. Therefore the pediatrician has often a precious option in the anti-inflammatory and antipyretic treatment in children instead of using steroids and paracetamol. In clinical practice ibuprofen can be used in the treatment of headache, toothache, otalgy, dysmenorrhea, neuralgia, arthralgia, myalgia, abdominal pain and fever: it is the first choice for these common diseases. However, the use of steroids is a routine, even if non-corticosteroid anti-inflammatory molecules could be useful. Certainly steroids are powerful anti-inflammatory, indicated for the treatment of chronic inflammatory disorders and in acute respiratory and allergic diseases. Beside, thanks to their chemical and pharmacological profile, they also provide patients with an antipyretic effect. However, the use of steroids must be reserved to cases in which other classical antipyretics such as non-steroidal anti-inflammatory drugs are not effective. The possible side effects and risks associated with stepping down steroids must be considered. Although “steroids-phobia” should be discouraged, steroids are to be reserved only as the first indication. In all other cases the pediatrician can use ibuprofen, whose efficacy and safety are widely demonstrated by now.

  3. Topical diclofenac versus dexamethasone after strabismus surgery: A double-blind randomized clinical trial of anti-inflammatory effect and ocular hypertensive response

    Directory of Open Access Journals (Sweden)

    Khan Hayat

    2007-01-01

    Full Text Available Background: Compared to steroids non-steroidal anti-inflammatory drugs offer comparable anti-inflammatory action without ocular side-effects. Aim: To compare the anti-inflammatory effect and effect on IOP (Goldmann of topical diclofenac 0.1% with dexamethasone 0.1% after strabismus surgery. Design: Prospective, randomized, double-blind, single-center, clinical trial. Materials and Methods: Forty-three cases of constant horizontal strabismus, qualifying for standard uniocular recession-resection surgery on two horizontal rectus muscles were randomized to either the dexamethasone or diclofenac group. They were excluded if they had previous ocular surgery, recently used anti-inflammatory drugs and had a neurological, systemic or an ocular inflammatory condition. In addition all received ciprofloxacin 0.3% four times daily. Assessment was done on the first postoperative day and at two and four weeks. The inflammatory characteristics graded from nil (0 to severe (3 were: discomfort, chemosis, injection, discharge and drop-intolerance. Their sum provided the total inflammatory score (TIS. Results: Dexamethasone group (n=21 was comparable in age, gender, preoperative IOP, strabismus, anesthesia administered and baseline IOP, to diclofenac (n=22. There were no significant differences in the inflammatory characteristics and TIS. The dexamethasone group had IOP significantly higher at two weeks (95% CI 0.17 to 3.25 and four weeks (95% CI 1.09 to 4.24 compared to diclofenac group and the net change of IOP at four weeks (95% CI 0.60 to 3.14. Compared to the baseline IOP. Conclusion: Topical diclofenac is comparable to dexamethasone in providing anti-inflammatory and analgesic effect with the advantage of significantly lesser IOP rise and should be preferred after strabismus surgery.

  4. Nonsteroidal anti-inflammatory drugs in the treatment of low back pain

    Directory of Open Access Journals (Sweden)

    Kuritzky L

    2012-11-01

    .Keywords: low back pain, non-steroidal anti-inflammatory drugs, cyclo-oxygenase 2

  5. [Place of anti-inflammatory agents in the prevention of deep phlebitis].

    Science.gov (United States)

    Guilmet, C

    1975-01-01

    The inflammatory reaction includes, after an initial tissue lesion, a catabolic phase with proteolysis, an exudative reaction phase, and finally an anabolic phase with the formation of an inflammatory granuloma. The reaction should be considered, however, as an initial inflammation, rapid and limited to the affected tissues, and a secondary inflammation induced at a distance by a humoral mechanism with the appearance of pathological globulins. Only certain anti-inflammatory agents act at these two levels : steroids and non-steroids. Corticosteroids can be used effectively in small doses. Courses of salicylates are difficult to manage and are not standardized. Fenamates and indometacine lead to psychiatric disorders. The only useful drugs are phenylbutazone and hydroxyphenylbutazone. These two drugs can be used alone, or in combination, or eventually being superseded by anti-coagulants. As they are derived from pyrazolidine, they are above all preventive. Their absorption in the digestive tract is rapid and almost complete ; the maximum plasma concentration occurs 2-4 h. after injection. Delayed accidents occur 7-15 days after the last dose. Suppotanderil and suppophenylbutazone are used at the dose of 250ml, 2 or 3 times a day. They may be combined with AVK depending on the clinical signs and the prothrombin and Howell's time. These drugs are contraindicated in patients with ulcers, with haematological diseases, and with severe cirrhosis. They should always be replaced straight away by anti-coagulants in patients with valve prostheses or with severe rhythm disorders.

  6. Anti-Inflammatory and Antinociceptive Activities of Bufalin in Rodents

    Directory of Open Access Journals (Sweden)

    Lili Wen

    2014-01-01

    Full Text Available The aims of this study were to evaluate the anti-inflammatory and analgesic effects of bufalin, a major component of “Chan-su.” We used a carrageenan-induced paw edema model to assess the anti-inflammatory activity of this compound, and Western blot analysis detected NF-κB signaling during this effect. The antinociceptive activities were evaluated by acetic acid-induced writhing, formalin, and hot-plate tests; open-field test investigated effects on the central nervous system. Our data showed that bufalin (0.3 and 0.6 mg/kg, i.p. potently decreased carrageenan-induced paw edema. Bufalin down regulated the expression levels of nitric oxide synthase (iNOS, cyclooxygenase-2 (COX-2, interleukin-1β (IL-1β, interleukin-6 (IL-6, and tumor necrosis factor-α (TNF-α during these treatments. Further studies demonstrated that bufalin significantly inhibited the activation of NF-κB signaling. Bufalin also reduced acetic acid-induced writhing and the licking time in the formalin test and increased hot-plate reaction latencies. Naloxone pretreatment (2 mg/kg, i.p. in the early phases of the formalin test and hot-plate test significantly attenuated the bufalin-induced antinociception effects, which suggests the involvement of the opioid system. A reduction in locomotion was not observed in the open-field test after bufalin administration. Taken together, bufalin treatment resulted in in vivo anti-inflammatory and analgesic effects, and bufalin may be a novel, potential drug for the treatment of inflammatory diseases.

  7. Antinociceptive and anti-inflammatory potential of Rhododendron arboreum bark.

    Science.gov (United States)

    Nisar, Muhammad; Ali, Sajid; Muhammad, Naveed; Gillani, Syed N; Shah, Muhmmad R; Khan, Haroon; Maione, Francesco

    2016-07-01

    Rhododendron arboreum Smith. (Ericaceae), an evergreen small tree, is one of the 1000 species that belongs to genus Rhododendron distributed worldwide. In folk medicine, as various parts of this plant exhibit medicinal properties, it is used in the treatment of different ailments.The present study was designed to evaluate the potential anti-inflammatory and antinociceptive effects of methanolic extract of R. arboreum bark, followed by activity-guided fractionation of n-hexane, n-butanol, chloroform, ethyl acetate and aqueous fractions.The ethyl acetate fraction (200 mg/kg i.p.) showed the maximum analgesic effect (82%) in acetic acid-induced writhing, followed, to a less extent, by crude extract and chloroform fraction both at a dose of 200 mg/kg i.p. (65.09% and 67.89%, respectively). In carrageenan-induced mouse paw oedema, the crude extract and its related fractions displayed in a dose-dependent manner (50-200 mg/kg i.p.) an anti-inflammatory activity for all time-courses (1-5 hrs). For the active extract/fractions (200 mg/kg i.p.), the maximum effect was observed 5 h after carrageenan injection. These evidences were also supported by in vitro lipoxygenase inhibitory properties. In conclusion, R. arboreum crude methanolic extract and its fractions exhibited anti-inflammatory and antinociceptive effects. For these reasons, this plant could be a promising source of new compounds for the management of pain and inflammatory diseases. PMID:25501256

  8. Anti-inflammatory activity of Abutilon indicum extract.

    Science.gov (United States)

    Tripathi, Priyanka; Chauhan, N S; Patel, J R

    2012-01-01

    Abutilon indicum Linn. had been broadly used for its reported biological activities in indigenous system of medicine. The ethanolic extract of the whole plant of A. indicum Linn. was evaluated for its anti-inflammatory activity at doses 250, 500 and 750 mg kg⁻¹ using the carrageenan-induced paw oedema in healthy Wistar albino rats. Results of in vivo activity led to the conclusion that the ethanolic extract of A. indicum showed predominantly significant activity in a dose-dependent manner, which is comparable to the reference standard ibuprofen. The results prove the traditional use of plant in the treatment of inflammation. PMID:21999427

  9. Anti-inflammatory agents in the treatment of bipolar depression

    DEFF Research Database (Denmark)

    Rosenblat, Joshua D; Kakar, Ron; Berk, Michael;

    2016-01-01

    OBJECTIVE: Inflammation has been implicated in the risk, pathophysiology, and progression of mood disorders and, as such, has become a target of interest in the treatment of bipolar disorder (BD). Therefore, the objective of the current qualitative and quantitative review was to determine...... or significant treatment-emergent adverse events were reported. CONCLUSIONS: Overall, a moderate antidepressant effect was observed for adjunctive anti-inflammatory agents compared with conventional therapy alone in the treatment of bipolar depression. The small number of studies, diversity of agents, and small...... sample sizes limited interpretation of the current analysis....

  10. Anti-Inflammatory Mechanism of Total Glycosides of Acanthopanax Giraldii

    Institute of Scientific and Technical Information of China (English)

    袁芳; 陈杰; 许国敏; 郑加嘉; 龙启才

    2009-01-01

    Objective:To study the anti-inflammatory mechanisms of total glycosides of Acanthopanax Giraldii (TGA).Methods:The changes of prostaglandin E_2(PGE_2),tumor necrosis factor(TNF-α),nitric oxide(NO), and expressions of COX-1 mRNA and COX-2 mRNA in BALB/c mouse macrophages were observed by the radioimmunoassay,ELISA and nitric acid reduction and RT-PCR in the presence or absence of TGA.Results: (1) TGA could significantly decrease the production of PGE_2 and NO in mouse peritoneal macrophages.The inhibitory...

  11. Paracetamol. Ny viden om virkningsmekanismer samt smertelindrende og antiinflammatorisk effekt sammenlignet med ikke-steroide antiinflammatorika

    DEFF Research Database (Denmark)

    Handberg, G

    2000-01-01

    Paracetamol is usually termed a peripheral analgesic from the common belief that its site of action is near the injury. In this review a possible central action is summarised. Furthermore the analgesic effect of paracetamol is compared to non-steroidal anti-inflammatory drugs and the possible anti......-inflammatory effect of paracetamol is discussed....

  12. The Anti-Inflammatory Activity of Eugenia Caryophllata Essential Oil: An animal model of anti-inflammatory activity

    OpenAIRE

    2005-01-01

    Aim: The aim of this study is gas chromatographic analysis of Eugenia caryaphyllata (clove) essential oil and investigation of its anti-inflammatory effects. Methods: The study involved eight groups; Serum physiologic, ethyl alcohol, indomethacin (3 mg/kg), etodolac (50 mg/kg), cardamom (0.05 mL/kg), EC-I (0.025 mL/kg), EC-II (0.050 mL/kg), EC-III (0.100 mL/kg) and EC-IV (0.200mL/kg). After measuring the volumes of right hind-paws of rats using a plethysmometer, drugs were injected intraperit...

  13. Anti-inflammatory strategies in the treatment of schizophrenia.

    Science.gov (United States)

    Andrade, Chittaranjan

    2016-01-01

    Schizophrenia is a major mental illness with a lifetime prevalence of about 1%. Antipsychotic drugs, with a primary mechanism of action that involves dopamine receptor blockade, are the mainstay in the treatment of the disorder. However, despite optimum antipsychotic treatment, few patients return to pre-morbid levels; the treatment deficit includes refractory positive symptoms, negative symptoms, mood impairments, cognitive impairments, social impairments, and/or a variety of medication-related adverse effects, including extrapyramidal symptoms, metabolic disturbances, hyperprolactinemia, and others. To address these, antipsychotic treatment has been augmented with psychosocial interventions, cognitive rehabilitation, different kinds of electrical and magnetic brain stimulation, and a large range of drugs from the neuropsychiatric as well as, surprise, the general medical pharmacopeia. The pleomorphic pathophysiology of schizophrenia includes abnormalities in immunological and inflammatory pathways, and so it is not surprising that anti-inflammatory drugs have also been trialed as augmentation agents in schizophrenia. This article critically examines the outcomes after augmentation with conventional anti-inflammatory interventions; results from randomized controlled trials do not encourage the use of either aspirin (1000 mg/day) or celecoxib (400 mg/day), both of which have been studied for this indication during the past decade and a half.

  14. HU-444, a Novel, Potent Anti-Inflammatory, Nonpsychotropic Cannabinoid.

    Science.gov (United States)

    Haj, Christeene G; Sumariwalla, Percy F; Hanuš, Lumír; Kogan, Natalya M; Yektin, Zhana; Mechoulam, Raphael; Feldmann, Mark; Gallily, Ruth

    2015-10-01

    Cannabidiol (CBD) is a component of cannabis, which does not cause the typical marijuana-type effects, but has a high potential for use in several therapeutic areas. In contrast to Δ(9)-tetrahydrocannabinol (Δ(9)-THC), it binds very weakly to the CB1 and CB2 cannabinoid receptors. It has potent activity in both in vitro and in vivo anti-inflammatory assays. Thus, it lowers the formation of tumor necrosis factor (TNF)-α, a proinflammatory cytokine, and was found to be an oral antiarthritic therapeutic in murine collagen-induced arthritis in vivo. However, in acidic media, it can cyclize to the psychoactive Δ(9)-THC. We report the synthesis of a novel CBD derivative, HU-444, which cannot be converted by acid cyclization into a Δ(9)-THC-like compound. In vitro HU-444 had anti-inflammatory activity (decrease of reactive oxygen intermediates and inhibition of TNF-α production by macrophages); in vivo it led to suppression of production of TNF-α and amelioration of liver damage as well as lowering of mouse collagen-induced arthritis. HU-444 did not cause Δ(9)-THC-like effects in mice. We believe that HU-444 represents a potential novel drug for rheumatoid arthritis and other inflammatory diseases. PMID:26272937

  15. Develop Anti-Inflammatory Nanotherapies to Treat Cardiovascular Disease

    Science.gov (United States)

    Tang, Jun

    Cardiovascular disease (CVD) is the leading cause of disease-related death in the world, accounting for 30 % global mortality. The majority of CVD is caused by atherosclerosis, a chronic inflammatory disease of major arteries featured by the deposition of lipids and cholesterol. Inflammation of atherosclerosis is mainly promoted by the pathological macrophages and monocytes, and modulating their functions has been proposed as a promising therapeutic target. This dissertation first presents the development of a novel simvastatin-loaded high-density lipoprotein (HDL) based nanoparticle ([S]-rHDL), which was able to deliver anti-inflammatory simvastatin preferentially to inflammatory monocytes in the blood and to macrophages in advanced atherosclerotic plaques, leading to the reduced inflammation in the tissue. Second, extensive in vivo characterization of [S]-rHDL in a mouse atherosclerosis model revealed that the anti-inflammatory capability of [S]-rHDL derived from its effects on blood monocytes, endothelial layer, monocyte recruitment, and plaque macrophage function. Third, a translational study that integrated the use of [S]-rHDL into oral statin treatment demonstrated a great potential for this nanomedicine as an attractive addition to the current high-dose oral statin standard-of-care for acute coronary syndrome. Finally, preliminary results suggested potential applications of the rHDL platform to other macrophage-implicated diseases.

  16. A Novel Anti-Inflammatory Effect for High Density Lipoprotein.

    Directory of Open Access Journals (Sweden)

    Scott J Cameron

    Full Text Available High density lipoprotein has anti-inflammatory effects in addition to mediating reverse cholesterol transport. While many of the chronic anti-inflammatory effects of high density lipoprotein (HDL are attributed to changes in cell adhesion molecules, little is known about acute signal transduction events elicited by HDL in endothelial cells. We now show that high density lipoprotein decreases endothelial cell exocytosis, the first step in leukocyte trafficking. ApoA-I, a major apolipoprotein of HDL, mediates inhibition of endothelial cell exocytosis by interacting with endothelial scavenger receptor-BI which triggers an intracellular protective signaling cascade involving protein kinase C (PKC. Other apolipoproteins within the HDL particle have only modest effects upon endothelial exocytosis. Using a human primary culture of endothelial cells and murine apo-AI knockout mice, we show that apo-AI prevents endothelial cell exocytosis which limits leukocyte recruitment. These data suggest that high density lipoprotein may inhibit diseases associated with vascular inflammation in part by blocking endothelial exocytosis.

  17. Anti-inflammatory Cerebrosides from Cultivated Cordyceps militaris.

    Science.gov (United States)

    Chiu, Ching-Peng; Liu, Shan-Chi; Tang, Chih-Hsin; Chan, You; El-Shazly, Mohamed; Lee, Chia-Lin; Du, Ying-Chi; Wu, Tung-Ying; Chang, Fang-Rong; Wu, Yang-Chang

    2016-02-24

    Cordyceps militaris (bei-chong-chaw, northern worm grass) is a precious and edible entomopathogenic fungus, which is widely used in traditional Chinese medicine (TCM) as a general booster for the nervous system, metabolism, and immunity. Saccharides, nucleosides, mannitol, and sterols were isolated from this fungus. The biological activity of C. militaris was attributed to the saccharide and nucleoside contents. In this study, the aqueous methanolic fraction of C. militaris fruiting bodies exhibited a significant anti-inflammatory activity. Bioactivity-guided fractionation of the active fraction led to the isolation of eight compounds, including one new and two known cerebrosides (ceramide derivatives), two nucleosides, and three sterols. Cordycerebroside A (1), the new cerebroside, along with soyacerebroside I (2) and glucocerebroside (3) inhibited the accumulation of pro-inflammatory iNOS protein and reduced the expression of COX-2 protein in LPS-stimulated RAW264.7 macrophages. This is the first study on the isolation of cerebrosides with anti-inflammatory activity from this TCM. PMID:26853111

  18. Anti-inflammatory strategies in the treatment of schizophrenia.

    Science.gov (United States)

    Andrade, Chittaranjan

    2016-01-01

    Schizophrenia is a major mental illness with a lifetime prevalence of about 1%. Antipsychotic drugs, with a primary mechanism of action that involves dopamine receptor blockade, are the mainstay in the treatment of the disorder. However, despite optimum antipsychotic treatment, few patients return to pre-morbid levels; the treatment deficit includes refractory positive symptoms, negative symptoms, mood impairments, cognitive impairments, social impairments, and/or a variety of medication-related adverse effects, including extrapyramidal symptoms, metabolic disturbances, hyperprolactinemia, and others. To address these, antipsychotic treatment has been augmented with psychosocial interventions, cognitive rehabilitation, different kinds of electrical and magnetic brain stimulation, and a large range of drugs from the neuropsychiatric as well as, surprise, the general medical pharmacopeia. The pleomorphic pathophysiology of schizophrenia includes abnormalities in immunological and inflammatory pathways, and so it is not surprising that anti-inflammatory drugs have also been trialed as augmentation agents in schizophrenia. This article critically examines the outcomes after augmentation with conventional anti-inflammatory interventions; results from randomized controlled trials do not encourage the use of either aspirin (1000 mg/day) or celecoxib (400 mg/day), both of which have been studied for this indication during the past decade and a half. PMID:26427750

  19. Analgesic and Anti-inflammatory Effects of Ginger Oil

    Institute of Scientific and Technical Information of China (English)

    JIA Yong-liang; XIE Qiang-min; ZHAO Jun-ming; ZHANG Lin-hui; SUN Bao-shan; BAO Meng-jing; LI Fen-fen; SHEN Jian; SHEN Hui-jun; ZHAO Yu-qing

    2011-01-01

    Objective Ginger (Zingiber officinale) is widely used as a spice in cooking and as a medicinal herb in traditional herbal medicine. The present study was to investigate the analgesic and anti-inflammatory activities of ginger oil in experimental animal models. Methods The analgesic effect of the oils was evaluated by the "acetic acid" and "hot-plate" test models of pain in mice. The anti-inflammatory effect of the oil was investigated in rats, using rat paw edema induced by carrageenan, adjuvant arthritis, and vascular permeability induced by bradykinin, arachidonic acid, and histamine. Indomethacin (1 mg/kg), Aspirin (0.5 g/kg) and Dexamethasone (2.5 mg/kg) were used respectively as reference drugs for comparison. Results The ginger oil (0.25-1.0 g/kg) produced significant analgesic effect against chemically- and thermally-induced nociceptive pain stimuli in mice (P < 0.05, 0.01). And the ginger oil (0.25-1.0 g/kg) also significantly inhibited carrageenan-induced paw edema, adjuvant arthritis, and inflammatory mediators-induced vascular permeability in rats (P < 0.05, 0.001). Conclusion These findings confirm that the ginger oil can be used to treat pain and chronic inflammation such as rheumatic arthritis.

  20. Topical anti-inflammatory activity of Solanum corymbiflorum leaves.

    Science.gov (United States)

    Piana, Mariana; Camponogara, Camila; Boligon, Aline Augusti; Machado, Michel Mansur; de Brum, Thiele Faccim; Oliveira, Sara Marchesan; de Freitas Bauermann, Liliane

    2016-02-17

    Solanum corymbiflorum is popularly known as "baga-de-veado" and its leaves are applied on inflamed legs, scabies, tick bite, boils, mastitis, low back pain and otitis. The aim of this study was evaluate anti-inflammatory in vivo activity and relate this activity with antioxidant compounds present in the extract of S. corymbiflorum leaves. The extract from S. corymbiflorum leaves topically applied was able to reduce the croton oil-induced ear edema and myeloperoxidase (MPO) activity with maximum inhibition of 87±3% and 45±7%, rescpectively in the dose of 1mg/ear. Similar results were found for positive control dexamethasone, which presented inhibitions of ear edema and MPO activity of 89±3% and 50±3%, respectively in a dose of 0.1mg/ear. These findings are due, at least in part, the presence of polyphenols (195.28mg GAE/g) and flavonoids, as chlorogenic acid (59.27mg/g), rutin (12.72mg/g), rosmarinic acid, caffeic acid and gallic acid found by high performance liquid chromatography (HPLC) analysis. This species showed potencial antioxidant by 1,1-diphenyl-2-picrylhydrazyl (DPPH), and carbonyl groups in proteins methods which may be related with the presence of this compounds. This species possess anti-inflammatory activity confirming their popular use for the local treatment of skin inflammatory disorders. PMID:26721215

  1. ANTI INFLAMMATORY ACTIVITY OF ALPINIA GALANGA IN EXPERIMENTAL ANIMALS

    Directory of Open Access Journals (Sweden)

    Venuturumilli Lakshmi

    2015-03-01

    Full Text Available In the present study the anti - inflammatory activity of Alpinia galanga is evaluated using rat paw edema, in comparison with Indomethacin using digital Plethysmometer. Male Wistar rats were grouped into 3 of 6 each. Test group given 250mg/kg Alpinia galang a suspended in 2% gum acacia, Standard group 20mg/kg Indomethacin orally. Hind paw edema was produced by sub plantar injection of 0.1ml of 1% carrageenin and the paw edema was measured at 0 and 3 hrs after injection using digital plethysmometer. Mean incre ase in paw volume and percentage inhibition were calculated. Data were represented as percentage inhibition of paw volume and Mean±S.E.M. Statistical analysis was done using student ‘t’ test. P values < 0.05 were considered significant. CONCLUSION: Alpinia galanga showed a 52.5% percentage of inhibition in comparison with Indomethacin which showed 68.75%. The test compound Alpinia galanga showed anti - inflammatory activity with a p value of <0.05 in comparison with Indomethacin with a p value of <0.001

  2. Anti-inflammatory and analgesic potential of Caesalpinia ferrea

    Directory of Open Access Journals (Sweden)

    Sandrine Maria A. Lima

    2012-02-01

    Full Text Available Caesalpinia ferrea Mart. belongs to the family Fabaceae. Known as pau-ferro and jucá, it is used in folk medicine to treat diabetes, as antipyretic and antirheumatic. This study aimed to evaluate the anti-inflammatory and antinociceptive activities of the ethanol extract of the fruits of C. ferrea (EECf. In the evaluation of anti-inflammatory activity, EECf (50 mg/kg produced significantly inhibition of ear edema by 66.6% compared to control. Indomethacin (10 mg/kg showed inhibition of 83.9% compared to control. EECf (50 mg/kg inhibited of vascular permeability induced by acetic acid and was also able to reduce of cell migration to the peritoneal cavity induced by thioglycolate. In the writhing test induced by acid acetic, EECf (12.5, 25 and 50 mg/kg significantly reduced the number of contortions by 24.9, 46.9 and 74.2%, respectively. In the formalin test, EECf presented effects only in the second phase. The results provided experimental evidence for the effectiveness of the traditional use of C. ferrea in treating various diseases associated with inflammation and pain.

  3. Nanoliposomal Nitroglycerin Exerts Potent Anti-Inflammatory Effects

    Science.gov (United States)

    Ardekani, Soroush; Scott, Harry A.; Gupta, Sharad; Eum, Shane; Yang, Xiao; Brunelle, Alexander R.; Wilson, Sean M.; Mohideen, Umar; Ghosh, Kaustabh

    2015-11-01

    Nitroglycerin (NTG) markedly enhances nitric oxide (NO) bioavailability. However, its ability to mimic the anti-inflammatory properties of NO remains unknown. Here, we examined whether NTG can suppress endothelial cell (EC) activation during inflammation and developed NTG nanoformulation to simultaneously amplify its anti-inflammatory effects and ameliorate adverse effects associated with high-dose NTG administration. Our findings reveal that NTG significantly inhibits human U937 cell adhesion to NO-deficient human microvascular ECs in vitro through an increase in endothelial NO and decrease in endothelial ICAM-1 clustering, as determined by NO analyzer, microfluorimetry, and immunofluorescence staining. Nanoliposomal NTG (NTG-NL) was formulated by encapsulating NTG within unilamellar lipid vesicles (DPhPC, POPC, Cholesterol, DHPE-Texas Red at molar ratio of 6:2:2:0.2) that were ~155 nm in diameter and readily uptaken by ECs, as determined by dynamic light scattering and quantitative fluorescence microscopy, respectively. More importantly, NTG-NL produced a 70-fold increase in NTG therapeutic efficacy when compared with free NTG while preventing excessive mitochondrial superoxide production associated with high NTG doses. Thus, these findings, which are the first to reveal the superior therapeutic effects of an NTG nanoformulation, provide the rationale for their detailed investigation for potentially superior vascular normalization therapies.

  4. Anti-inflammatory effects ofMorninga oleifera lam extract in rats

    Institute of Scientific and Technical Information of China (English)

    Georgewill OA; Georgewill UO; Nwankwoala RNP

    2010-01-01

    Objective:To investigate the acute and delayed anti-inflammatory effects ofMorning oleifera lam (MOL) crude methanolic extract.Methods: Compared the anti-inflammatory effects of MOL with that of standard anti-inflammatory agents like indomethacin and hydrocortisone using Air Pouch Model.Results: In both acute and delayed inflammation, the MOL extract produced dose dependent anti-inflammatory effect [acute IC50= (399.30 ±5.43) mg/kg; delayed IC50= (510.26±4.53) mg/kg]. The order of anti-inflammatory potency for the three drugs was hydrocortisone> indomethacin > MOL.Conclusions: These observations indicate that MOL possesses potential anti-inflammatory property.

  5. Anti-inflammatory drugs and uterine cervical cancer cells: Antineoplastic effect of meclofenamic acid

    OpenAIRE

    Soriano-Hernandez, Alejandro D; MADRIGAL-PÉREZ, DANIELA; GALVAN-SALAZAR, HECTOR R.; Martinez-Fierro, Margarita L; Laura L. Valdez-Velazquez; Espinoza-Gómez, Francisco; VAZQUEZ-VUELVAS, OSCAR F.; OLMEDO-BUENROSTRO, BERTHA A.; Guzman-Esquivel, Jose; Rodriguez-Sanchez, Iram P.; LARA-ESQUEDA, AGUSTIN; MONTES-GALINDO, DANIEL A.; Delgado-Enciso, Ivan

    2015-01-01

    Uterine cervical cancer (UCC) is one of the main causes of cancer-associated mortality in women. Inflammation has been identified as an important component of this neoplasia; in this context, anti-inflammatory drugs represent possible prophylactic and/or therapeutic alternatives that require further investigation. Anti-inflammatory drugs are common and each one may exhibit a different antineoplastic effect. As a result, the present study investigated different anti-inflammatory models of UCC ...

  6. ANTI-INFLAMMATORY AND MAST CELL PROTECTIVE EFFECT OF FICUS RELIGIOSA

    OpenAIRE

    Viswanathan, S; Thirugnanasambantham, P; Reddy, M. Kannappa; Narasimhan, S.; Subramaniam, G. Anantha

    1990-01-01

    The aqueous extract of bark of Ficus religiosa was prepared and investigated for its anti-inflammatory effect and for its protective effect on mast cells against degranulation. A significant anti-inflammatory effect was observed in both acute and chronic models of inflammation. The extract also protected mast cells from degranulation induced by various degranulatiors. The observed anti-inflammatory and mast cell protective effect may be responsible for the beneficial effect of Ficus religiosa...

  7. ANTI-INFLAMMATORY AND DIURETIC EFFECT OF PLANT EXTRACTS OF PSEUDARTHRIA VISCIDA (L) WEIGHT & ARN.

    OpenAIRE

    Saravanan C.; Shantha kumar S.; Anandan R.; Narayanaswamy V.B.; Varunraj S.

    2010-01-01

    The ethanolic extracts prepared from aerial parts of Pseudarthria viscida was studied for anti-inflammatory and diuretic activities in albino rats. The results obtained were compared with that of standard drug indomethacin and frusemide for their anti-inflammatory and diuretic activities respectively. The present study demonstrated the diuretic effect of P.viscida by increasing the excretion of Na+, K+ and Cl- ions in the urine. The extract also showed significant anti-inflammatory effect by ...

  8. Há uma associação entre anti-inflamatórios não-esteroides e nefropatia induzida por contraste? ¿Hay una asociación entre antiinflamatorios no esteroides y nefropatía inducida por contraste? Is there an association between non-steroidal anti-inflammatory drugs and contrast nephropathy?

    Directory of Open Access Journals (Sweden)

    Luciano Passamani Diogo

    2010-12-01

    uso de AINEs y su asociación con desarrollo de NIC, a través de la alteración de los niveles de creatinina sérica o tasa de filtrado glomerular en 48 o 72 horas. RESULTADOS: En el período de julio de 2005 a julio de 2006, 236 pacientes fueron incluidos en el estudio, de los cuales 29 fueron posteriormente excluidos. La incidencia de NIC fue 10,37% (20 de 207 y 42% de los pacientes estaban recibiendo AINEs hasta el momento de la evaluación. No hubo asociación entre el uso de AINEs y el desarrollo de NIC con OR de 1,293; IC95% (0,46-4,2. El estudio detectó factores de riesgo conocidos para el desarrollo de NIC, tales como diabetes, con OR de 2,77; IC95% (1,05-7,47 e insuficiencia renal crónica con OR de 3,48; IC95% (1,1-11,07 y también sugirió una acción protectora de la hidratación con solución salina con OR de 0,166; IC95% (0,03-0,92. CONCLUSIÓN: Con base en los datos obtenidos, concluimos que no hubo asociación entre NIC y uso previo de AINEs, por lo menos con un OR > 2,85, el cual nuestra muestra detectó.BACKGROUND: The association between the use of nonsteroidal anti-inflammatory drugs (NSAIDs and acute or chronic renal failure is well documented, but evidence of such association between NSAIDs and Contrast-Induced Nephropathies (CIN is not found in the indexed literature. OBJECTIVE: To evaluate the possible association between NSAIDs and CIN. METHODS: In a cohort study, through clinical interviews of patients that underwent cardiac catheterization, we analyzed the use of NSAIDs and its association with the development of CIN, through alterations in serum creatinine or glomerular filtration rate in 48 or 72 hours. RESULTS: From July 2005 to July 2006, 236 patients were enrolled in the study, of which 29 were later excluded. The incidence of CIN was 10.37% (20 of 207 and 42% of the patients were using NSAIDs until the moment of the evaluation. There was no association between the use of NSAIDs and the development of CIN with OR of 1.293 95% CI (0

  9. Anti-Inflammatory Effects of Metformin Irrespective of Diabetes Status

    Science.gov (United States)

    Cameron, Amy R.; Morrison, Vicky L.; Levin, Daniel; Mohan, Mohapradeep; Forteath, Calum; Beall, Craig; McNeilly, Alison D.; Balfour, David J.K.; Savinko, Terhi; Wong, Aaron K.F.; Viollet, Benoit; Sakamoto, Kei; Fagerholm, Susanna C.; Foretz, Marc

    2016-01-01

    Rationale: The diabetes mellitus drug metformin is under investigation in cardiovascular disease, but the molecular mechanisms underlying possible benefits are poorly understood. Objective: Here, we have studied anti-inflammatory effects of the drug and their relationship to antihyperglycemic properties. Methods and Results: In primary hepatocytes from healthy animals, metformin and the IKKβ (inhibitor of kappa B kinase) inhibitor BI605906 both inhibited tumor necrosis factor-α–dependent IκB degradation and expression of proinflammatory mediators interleukin-6, interleukin-1β, and CXCL1/2 (C-X-C motif ligand 1/2). Metformin suppressed IKKα/β activation, an effect that could be separated from some metabolic actions, in that BI605906 did not mimic effects of metformin on lipogenic gene expression, glucose production, and AMP-activated protein kinase activation. Equally AMP-activated protein kinase was not required either for mitochondrial suppression of IκB degradation. Consistent with discrete anti-inflammatory actions, in macrophages, metformin specifically blunted secretion of proinflammatory cytokines, without inhibiting M1/M2 differentiation or activation. In a large treatment naive diabetes mellitus population cohort, we observed differences in the systemic inflammation marker, neutrophil to lymphocyte ratio, after incident treatment with either metformin or sulfonylurea monotherapy. Compared with sulfonylurea exposure, metformin reduced the mean log-transformed neutrophil to lymphocyte ratio after 8 to 16 months by 0.09 U (95% confidence interval, 0.02–0.17; P=0.013) and increased the likelihood that neutrophil to lymphocyte ratio would be lower than baseline after 8 to 16 months (odds ratio, 1.83; 95% confidence interval, 1.22–2.75; P=0.00364). Following up these findings in a double-blind placebo controlled trial in nondiabetic heart failure (trial registration: NCT00473876), metformin suppressed plasma cytokines including the aging

  10. Anti-inflammatory and antifibrotic effects of methyl palmitate

    International Nuclear Information System (INIS)

    Methyl palmitate (MP) has been shown earlier to inhibit Kupffer cells and rat peritoneal macrophages. To evaluate the potential of MP to inhibit the activation of other macrophages, RAW cells (macrophages of alveolar origin) were treated with varying concentrations of MP (0.25, 0.5, 1 mM). Assessment of cytotoxicity using MTT assay revealed that 0.25 and 0.5 mM are not toxic to RAW cells. MP was able to inhibit the phagocytic function of RAW cells. Treatment of cells with MP 24 hours prior to LPS stimulation significantly decreased nitric oxide release and altered the pattern of cytokines release; there was a significant decrease in TNF-α and a significant increase in IL-10 compared to the controls. However, there is a non-significant change in IL-6 level. Furthermore, phosphorylation of inhibitory kappa B (IκBα) protein was significantly decreased in RAW cells treated with 0.5 mM MP after LPS stimulation. Based upon the in-vitro results, it was examined whether MP treatment will be effective in preventing bleomycin-induced lung inflammation and fibrosis in-vivo. Bleomycin given by itself caused destruction of the lung architecture characterized by pulmonary fibrosis with collapse of air alveoli and emphysematous. Bleomycin induced a significant increase in hydroxyproline level and activated NF-κB, p65 expression in the lung. MP co-treatment significantly ameliorated bleomycin effects. These results suggest that MP has a potential of inhibiting macrophages in general. The present study demonstrated for the first time that MP has anti-inflammatory and antifibrotic effect that could be through NF-kB inhibition. Thus MP like molecule could be a promising anti-inflammatory and antifibrotic drug. - Research highlights: →Methyl palmitate is a universal macrophage inhibitor. →It could be a promising nucleus of anti-inflammatory and antifibrotic drugs. →The underlying mechanism of these effects could be through NF-kB inhibition.

  11. Studies on the mechanisms of anti-inflammatory activity of the extracts and fractions of Alchornea floribunda leaves

    Institute of Scientific and Technical Information of China (English)

    Festus BC.Okoye; Patience O.Osadebe

    2009-01-01

    Objective:Alchornea floribunda leaves are widely used in ethnomedicinal management of inflammatory disor-ders.The present work is aimed at investigating this folkloric use.Methods:The anti-inflammatory effect of the leaf extracts and fractions was investigated in experimental animal models of acute and chronic inflamma-tion.The possible mechanisms by which the two most active fractions,hexane (HE)and ethyl acetate (EF) exert their effects were also investigated.Results:The crude extract (200 mg/kg)showed moderate inhibition of egg albumen-induced edema in rats (% edema inhibition =54.69)at 4 h.HE and EF showed very high activity (% edema inhibition of 81.25 and 67.19 respectively at 200 mg/kg)at 4h as compared to the con-trol.Both fractions ameliorated arthritis induced by formaldehyde in rats.At 400 mg/kg,HE evoked a signifi-cant irritation of gastric mucosa in rats.EF (200 mg/kg,p.o.)significantly inhibited leucocytes (% inhibi-tion =36.79)migration in vivo,but could not stabilize heat and hypotonicity-induced lysis of human erythro-cyte at 200 and 400 μg/mL in vitro.Phytochemical investigation revealed the presence of terpenoids and ster-oids in HE and flavonoids,tannins and saponins in EF.Conclusion:These results suggest that the leaves of Alchornea floribunda possess anti-inflammatory activity in acute and chronic inflammation.The activity may de-rive from a combination of inhibition of prostaglandin synthesis and leucocytes migration.The phytochemical constituents detected in HE and EF may account for the anti-inflammatory activity.

  12. [Anti-inflammatory and anti-allergic oral vaccines?].

    Science.gov (United States)

    Lomholt, H B; Kilian, M

    1996-09-16

    Recent data suggest clinical efficacy of specific antigens delivered at mucosal sites in the treatment of certain organ specific autoimmune diseases. This approach appears non-toxic and has no side effects. Phase I/II human trials on multiple sclerosis and rheumatoid arthritis show positive outcomes. Furthermore, animal studies point to beneficial effects on uveitis, diabetes mellitus, transplantation reactions and allergic diseases. The immunological mechanism is oral tolerance, a well known principle for induction of a systemic hyporesponse to specific antigens. The tolerance is most pronounced on delayed type hypersensibility and IgE-mediated reactions. At least three different mechanisms mediate the tolerance. Low doses of antigen induce active suppression, intermediate doses induce clonal T-cell anergy, and high doses induce clonal T-cell deletion. The recent improvements in the understanding of the mechanisms of oral tolerance have fueled an interest in manipulating this principle to develop anti-inflammatory vaccines. PMID:8966773

  13. Immunomodulatory and anti-inflammatory properties of macrolides

    Directory of Open Access Journals (Sweden)

    Bulska Magdalena

    2014-06-01

    Full Text Available Macrolides are a group of antibiotics whose activity is ascribable to the presence of the macrolide ring, to which one or more deoxy sugars may be attached. Two properties are inherent in this group of antibiotics, the immunomodulatory and the anti-inflammatory actions, ensuring great efficacy in a wide spectrum of infections. Macrolides demonstrate several immunomodulatory activities both in vitro and in vivo. They can down-regulate prolonged inflammation, increase mucus clearance, prevent the formation of bacterial biofilm and either enhance or reduce activation of the immune system. According to given properties and exceptional effects on bacterial phatogens, the macrolide antimicrobial agents have been found to serve a unique role in the management of chronic airway disorders, including diffuse panbronchiolitis, cystic fibrosis and chronic obstructive pulmonary disease. Use of macrolides can result in clinical improvement in patients with severe, chronic inflammatory airway diseases, improving their spirometry indicators, gas exchange and overall quality of life.

  14. Further studies on the anti-inflammatory effect of insulin.

    Science.gov (United States)

    Ottlecz, A; Koltai, M; Gecse, A

    1977-10-01

    Experiments performed on rats showed that insulin, when applied i.v. or s.c., inhibited the foot edema induced by carrageenin, thermic effect of 45.7 degrees C, compound 48/80 and 5-HT, but moderately increased the paw swelling evoked by kallikrein, a kinin-forming enzyme. The increased vascular permeability elicited by intradermal injection of histamine, 5-HT, bradykinin, PGE1, carrageenin and compound 48/80 was also suppressed. The anti-inflammatory effect was not significantly altered by propranolol and adrenalectomy on the thermal and carrageenin edema, it was variably inhibited on the skin test, and was completely abolished on the paw swelling induced by 5-HT and compound 48/80. Since insulin had little or no effect on the vascular response when given topically together with the vasoactive agents, its complex effect on the acute inflammation appears to be brought about via indirect mechanisms. PMID:930760

  15. Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata.

    Science.gov (United States)

    Li, Yi-Jie; Xu, Cheng-Ting; Lin, Dan-Dan; Qin, Jiang-Ke; Ye, Gao-Jie; Deng, Qing-Hua

    2016-08-01

    A new bergenin derivative, bergenin-11-O-α-d-galactopyranoside (compound 1), together with seven known polyphenolic compounds, were isolated from the stem of Cissus pteroclada Hayata. The structures of the 8 compounds were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Moreover, the in vitro anti-inflammatory effects of compounds (1-8) in LPS-stimulated murine macrophage RAW 264.7 cells were also investigated. Our results revealed that compound 1 inhibited the production of pro-inflammatory mediators NO and PGE2 and the expression of NF-κB, TNF-α, IL-1β, iNOS and COX-2. PMID:27374242

  16. Cutaneous reactions to analgesic-antipyretics and nonsteroidal anti-inflammatory drugs. Analysis of reports to the spontaneous reporting system of the Gruppo Italiano Studi Epidemiologici in Dermatologia.

    Science.gov (United States)

    1993-01-01

    We analyzed the cutaneous reactions to systemic analgesic-antipyretics and non-steroidal anti-inflammatory drugs reported to the spontaneous reporting system of the Gruppo Italiano Studi Epidemiologici in Dermatologia (GISED). The system has been active since 1988, with periodic intensive surveillance exercises, and 202 dermatologists have collaborated. Up to December 1991, 2,137 reactions had been collected, of which 713 were reactions to systemic analgesic-antipyretics and nonsteroidal anti-inflammatory drugs. A general profile of the reactions was identifiable. It included, in order of frequency, urticaria/angioedema, fixed eruptions, exanthemas, erythema multiforme and Stevens Johnson syndrome. Fixed eruptions and Stevens Johnson syndrome were reported with exceedingly high frequency in association with feprazone. Our system also revealed previously unreported reactions, including fixed eruption to nimesulide, fixed eruption to piroxicam and fixed eruption to flurbiprofen.

  17. Effect of anti-inflammatory treatment on depression, depressive symptoms and side effects: A systematic review and meta-analysis of randomized clinical trials

    DEFF Research Database (Denmark)

    Köhler, Karl Ole

    2014-01-01

    of anti-inflammatory interventions. Data Sources: Trials published prior to December, 31st 2013, were identified searching CENTRAL, PubMed, EMBASE, Psychinfo, Clinicaltrials.gov, and relevant review articles. Study Selection: Randomized, placebo-controlled trials assessing efficacy and side effects...... Outcome Measures: Depression scores after treatment and side effects. Results: 10 publications covering 14 trials (n=6,262) were included: 10 on non-steroidal anti-inflammatory drugs (NSAIDs) (n=4,258) and four on cytokine-inhibitors (n=2,004). The pooled effect estimate suggested that anti...... heterogeneity of the studies was not explained by differences in inclusion of clinical depression versus depressive symptoms or NSAIDs versus cytokine inhibitors. Sub-analyses particularly emphasized antidepressant properties for the selective COX-2 inhibitor celecoxib in general (SMD=-0.29; 95%-CI: -0.49 to -0...

  18. Anti-inflammatory and antinociceptive activities of azadirachtin in mice.

    Science.gov (United States)

    Soares, Darly G; Godin, Adriana M; Menezes, Raquel R; Nogueira, Rafaela D; Brito, Ana Mercy S; Melo, Ivo S F; Coura, Giovanna Maria E; Souza, Danielle G; Amaral, Flávio A; Paulino, Tony P; Coelho, Márcio M; Machado, Renes R

    2014-06-01

    Azadirachta indica (Meliaceae) extracts have been reported to exhibit anti-inflammatory and antinociceptive properties. However, the activities of azadirachtin, a limonoid and the major bioactive compound found in the extracts, have been poorly investigated in animal models. In the present study, we investigated the effects induced by azadirachtin in experimental models of pain and inflammation in mice. Carrageenan-induced paw edema and fibrovascular tissue growth induced by subcutaneous cotton pellet implantation were used to investigate the anti-inflammatory activity of azadirachtin in mice. Zymosan-induced writhing and hot plate tests were employed to evaluate the antinociceptive activity. To explore putative mechanisms of action, the level of tumor necrosis factor-α in inflammatory tissue was measured and the effect induced by opioidergic and serotonergic antagonists was evaluated. Previous per os (p. o.) administration of azadirachtin (120 mg/kg) significantly reduced the acute paw edema induced by carrageenan. However, the concomitant increase of the paw concentration of tumor necrosis factor-α induced by this inflammatory stimulus was not reduced by azadirachtin. In addition to inhibiting the acute paw edema induced by carrageenan, azadirachtin (6, 60, and 120 mg/kg) inhibited the proliferative phase of the inflammatory response, as demonstrated by the reduced formation of fibrovascular tissue growth. Azadirachtin (120 mg/kg) also inhibited the nociceptive response in models of nociceptive (hot plate) and inflammatory (writhing induced by zymosan) pain. The activity of azadirachtin (120 mg/kg) in the model of nociceptive pain was attenuated by a nonselective opioid antagonist, naltrexone (10 mg/kg, i. p.), but not by a nonselective serotonergic antagonist, cyproheptadine. In conclusion, this study demonstrates the activity of azadirachtin in experimental models of nociceptive and inflammatory pain, and also in models of acute and chronic inflammation

  19. ANTI-INFLAMMATORY EFFECTS OF MAGNOLIAE FARGESII VOLATILE OIL

    Institute of Scientific and Technical Information of China (English)

    WANG Feng; CHEN Zhi-dong; XING Tao; WANG Nian-song

    2009-01-01

    Objective To explore the anti-inflammatory effects of magnoliae fargesii volatile oil.Methods Human umbilical vein endothelial cells (HUVECs) were stimulated by TNF-α to express the adhesion molecules. Then the anti-adhesion effects of magnoliae fargesii volatile oil between HUVECs and human peripheral neutrophils were observed. The ischemia-reperfusion animal models were established by 60min renal ischemia followed by 1, 3, 6 and 24h reperfusion. Rats were randomly divided into the following groups: the sham-operation controls, ischemic group only treated with normal saline, and treated group infused magnoliae fargesii volatile oil before reperfusion. Then the renal injury of rats was detected. Results High rate of cell adhesion between HUVECs and neutrophils was observed. Magnoliae fargesii volatile oil could inhibit the adhesion process at the concentration of 0.5μL/mL (191.6±8.6), 1.0μL/mL (158.2±9.0) and 2.0μL/mL (155.2±9.7) (P<0.05). The anti-adhesion effects were strengthened with the increase of volatile oil concentration. Blood urea nitrogen and creatinine levels of the animal models were significantly increased after 24h reperfusion while the increase was remarkably attenuated by the treatment with magnoliae fargesii volatile oil. The renal injury was severe after 1h reperfusion, which was significantly attenuated by the treatment of magnoliae fargesii volatile oil. Conclusion Magnoliae fargesii volatile oil has anti-inflammatory effects.

  20. The Anti-inflammatory mechanisms of Hsp70

    Directory of Open Access Journals (Sweden)

    Thiago J Borges

    2012-05-01

    Full Text Available Immune responses to heat shock proteins (Hsp develop in virtually all inflammatory diseases; however, the significance of such responses is only now becoming clear. In experimental disease models, Hsp administration can prevent or arrest inflammatory damage, and in initial clinical trials in patients with chronic inflammatory diseases, Hsp peptides have been shown to promote the production of anti-inflammatory cytokines, indicating immunoregulatory potential of Hsp. Therefore, the presence of immune responses to Hsp in inflammatory diseases can be seen as an attempt of the immune system to correct the inflammatory condition. Hsp70 can modulate inflammatory responses in models of arthritis, colitis and graft rejection, and the mechanisms underlying this effect are now being elucidated. Incubation with microbial Hsp70 was seen to induce tolerogenic DCs and to promote a suppressive phenotype in myeloid-derived suppressor cells and monocytes. These DC could induce regulatory T cells (Tregs, independently of the antigens they presented. Some Hsp70 family members are associated with autophagy, leading to a preferential uploading of Hsp70 peptides in MHC class II molecules of stressed cells. Henceforth, conserved Hsp70 peptides may be presented in these situations and constitute targets of Tregs, contributing to downregulation of inflammation. Finally, an interfering effect in multiple intracellular inflammatory signaling pathways is also known for Hsp70. Altogether it seems attractive to use Hsp70, or its derivative peptides, for modulation of inflammation. This is a physiological immunotherapy approach, without the immediate necessity of defining disease specific auto-antigens. In this article, we present the evidence on anti-inflammatory effects of Hsp70 and discuss the need for experiments that will be crucial for the further exploration of the immuno-suppressive potential of this protein.

  1. COX-independent mechanisms of cancer chemoprevention by anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Evrim eGurpinar

    2013-07-01

    Full Text Available Epidemiological and clinical studies suggest that non-steroidal anti-inflammatory drugs (NSAIDs, including cyclooxygenase (COX-2 selective inhibitors, reduce the risk of developing cancer. Experimental studies in human cancer cell lines and rodent models of carcinogenesis support these observations by providing strong evidence for the antineoplastic properties of NSAIDs. The involvement of COX-2 in tumorigenesis and its overexpression in various cancer tissues suggest that inhibition of COX-2 is responsible for the chemopreventive efficacy of these agents. However, the precise mechanisms by which NSAIDs exert their antiproliferative effects are still a matter of debate. Numerous other studies have shown that NSAIDs can act through COX-independent mechanisms. This review provides a detailed description of the major COX-independent molecular targets of NSAIDs and discusses how these targets may be involved in their anticancer effects. Toxicities resulting from COX inhibition and the suppression of prostaglandin synthesis preclude the long-term use of NSAIDs for cancer chemoprevention. Furthermore, chemopreventive efficacy is incomplete and treatment often leads to the development of resistance. Identification of alternative NSAID targets and elucidation of the biochemical processes by which they inhibit tumor growth could lead to the development of safer and more efficacious drugs for cancer chemoprevention.

  2. Psoriatic arthritis: treatment strategies using anti-inflammatory drugs and classical DMARDs

    Directory of Open Access Journals (Sweden)

    E. Lubrano

    2012-06-01

    Full Text Available Psoriatic Arthritis (PsA is a chronic inflammatory disease typically characterized by arthritis and psoriasis variably associated with other extra-articular manifestations. PsA has been considered a milder and less disabling disease compared with rheumatoid arthritis (RA, even if some studies showed that PsA had joint erosions and damage. In addition, about 20-40% of PsA patients have axial skeleton involvement that may lead to functional limitation and deformity. The treatment of PsA ranged from initial treatment with non-steroidal anti-inflammatory drugs (NSAIDs to one or more disease-modifying anti-rheumatic agents (DMARDs for the suppression of inflammation in patients with recalcitrant peripheral joint disease. In clinical practice, the most widely used DMARDs are methotrexate (level of evidence B, sulfasalazine (level of evidence A, leflunomide (level of evidence A, and ciclosporin (level of evidence B. However, the efficacy of these agents in inhibiting joint erosions has not been assessed in controlled studies. Finally, the effectiveness of DMARDs in treating enthesitis and dactylitis is controversial. The present paper revised the evidence-based results on treatment with “conventional” therapy for PsA. The revision was based on all the subsets of the diseases, namely the various manifestations of the articular involvement (peripheral, axial, enthesitis, dactylitis as well as the skin and nail involvement.

  3. Adverse respiratory reactions to aspirin and nonsteroidal anti-inflammatory drugs.

    Science.gov (United States)

    Simon, Ronald A

    2004-01-01

    Aspirin-exacerbated respiratory disease (AERD) is an adult-onset condition that manifests as asthma, rhinosinusitis/nasal polyps, and sensitivity to aspirin and other cyclooxygenase-1 (COX-1)-inhibitor nonsteroidal anti-inflammatory drugs (NSAIDs). There is no cross-sensitivity to highly selective COX-2 inhibitors. AERD is chronic and does not improve with avoidance of COX-1 inhibitors. The diagnosis of AERD is made through provocative challenge testing. Following a positive aspirin challenge, patients can be desensitized to aspirin and NSAIDs. The desensitized state can be maintained indefinitely with continued daily administration. After desensitization, there is an approximately 48-hour refractory period to adverse effects from aspirin. The pathogenesis of AERD remains unknown, but these patients have been shown to have multiple abnormalities in arachidonic acid metabolism and in cysteinyl leukotriene 1 receptors. AERD patients can take up to 650 mg of acetaminophen for analgesic or antipyretic relief. Patients can also use weak COX-1 inhibitors, such as sodium salicylate or choline magnesium trisalicylate. Treatment of AERD patients with antileukotriene medications has been helpful but not preferential when compared with non-AERD patients. An alternative treatment for many AERD patients is aspirin desensitization. This is particularly effective in reducing upper-airway mucosal congestion, nasal polyp formation, and systemic steroids. PMID:14680616

  4. Computational Structure-Based De Novo Design of Hypothetical Inhibitors against the Anti- Inflammatory Target COX-2.

    Directory of Open Access Journals (Sweden)

    Jaspreet Kaur Dhanjal

    Full Text Available Cyclooxygenase-2 (COX-2 produces prostaglandins in inflamed tissues and hence has been considered as an important target for the development of anti-inflammatory drugs since long. Administration of traditional non-steroidal anti-inflammatory drugs (NSAIDs and other COX-2 selective inhibitors (COXIBS for the treat of inflammation has been found to be associated with side effects, which mainly includes gastro-intestinal (GI toxicity. The present study involves developing a virtual library of novel molecules with high druglikeliness using structure-based de novo drug designing and 2D fingerprinting approach. A library of 2657 drug like molecules was generated. 2D fingerprinting based screening of the designed library gave a unique set of compounds. Molecular docking approach was then used to identify two compounds highly specific for COX-2 isoform. Molecular dynamics simulations of protein-ligand complexes revealed that the candidate ligands were dynamically stable within the cyclooxygenase binding site of COX-2. The ligands were further analyzed for their druglikeliness, ADMET properties and synthetic accessibility using knowledge based set of rules. The results revealed that the molecules are predicted to selectively bind to COX-2 enzyme thereby potentially overcoming the limitations posed by the drugs in clinical use.

  5. Preventative oral methylthioadenosine is anti-inflammatory and reduces DSS-induced colitis in mice

    Science.gov (United States)

    Methylthioadenosine (MTA) is a precursor of the methionine salvage pathway and has been shown to have anti-inflammatory properties in various models of acute and chronic inflammation. However, the anti-inflammatory properties of MTA in models of intestinal inflammation are not defined. We hypothesiz...

  6. In-vitro anti- inflammatory activity of aqueous extract of leaves of Plectranthus amboinicus (Lour.) Spreng

    OpenAIRE

    Ravikumar, V.R.; Dhanamani, M.; Sudhamani, T.

    2009-01-01

    Aqueous extract of leaves of Plectranthus amboinicus (lour.) Spreng, which is traditionally used in the treatment of cough and cold was screened for its anti- inflammatory activity by HRBC membrane stabilisation model. Aqueous extract (500 mcg/ml) showed significant anti-inflammatory activity as compared to that of hydrocortisone sodium.

  7. In-vitro anti- inflammatory activity of aqueous extract of leaves of Plectranthus amboinicus (Lour.) Spreng.

    Science.gov (United States)

    Ravikumar, V R; Dhanamani, M; Sudhamani, T

    2009-04-01

    Aqueous extract of leaves of Plectranthus amboinicus (lour.) Spreng, which is traditionally used in the treatment of cough and cold was screened for its anti- inflammatory activity by HRBC membrane stabilisation model. Aqueous extract (500 mcg/ml) showed significant anti-inflammatory activity as compared to that of hydrocortisone sodium. PMID:22557324

  8. ANTI-INFLAMMATORY AND ANTIOXIDANT COMPOUND, RUTIN IN CARDIOSPERMUM HALICACABUM LEAVES

    OpenAIRE

    Babu, K.C. Venkatesh; Krishnakumari, S.

    2005-01-01

    C.halicacabum is wide spread in tropical and sub-tropical Asia and Africa. Our laboratory results showed crude ethanolic extract of this plant exerted anti-inflammatory activity in chronic inflammatory models. In this present study, we tried to investigate the presence of anti-inflammatory compound in this extract.

  9. Anti-inflammatory properties of a novel peptide interleukin 1 receptor antagonist

    DEFF Research Database (Denmark)

    Klementiev, Boris; Li, Shizhong; Korshunova, Irina;

    2014-01-01

    Interleukin 1 (IL-1) is implicated in neuroinflammation, an essential component of neurodegeneration. We evaluated the potential anti-inflammatory effect of a novel peptide antagonist of IL-1 signaling, Ilantide.......Interleukin 1 (IL-1) is implicated in neuroinflammation, an essential component of neurodegeneration. We evaluated the potential anti-inflammatory effect of a novel peptide antagonist of IL-1 signaling, Ilantide....

  10. DMPD: Molecular mechanisms of the anti-inflammatory functions of interferons. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 18086388 Molecular mechanisms of the anti-inflammatory functions of interferons. Ko...varik P, Sauer I, Schaljo B. Immunobiology. 2007;212(9-10):895-901. Epub 2007 Nov 8. (.png) (.svg) (.html) (.csml) Show Molecular... mechanisms of the anti-inflammatory functions of interferons. PubmedID 18086388 Title Molecular

  11. Anti-inflammatory effect of interleukin-10 in rabbit immune complex-induced colitis

    NARCIS (Netherlands)

    Grool, TA; Van Dullemen, H; Meenan, J; Koster, F; Ten Kate, FJW; Lebeaut, A; Tytgat, GNJ; Van Deventer, SJH

    1998-01-01

    Background: Interleukin-10 (IL-10) is an anti-inflammatory cytokine that downregulates the secretion of pro-inflammatory cytokines and additionally induces the secretion of anti-inflammatory cytokines, thus possibly leading to reduction of chronic inflammation in inflammatory bowel disease. In this

  12. The Toxicity of Nonsteroidal Anti-inflammatory Eye Drops against Human Corneal Epithelial Cells in Vitro.

    Science.gov (United States)

    Lee, Jong Soo; Kim, Young Hi; Park, Young Min

    2015-12-01

    This study investigated the toxicity of commercial non-steroid anti-inflammatory drug (NSAID) eye solutions against corneal epithelial cells in vitro. The biologic effects of 1/100-, 1/50-, and 1/10-diluted bromfenac sodium, pranoprofen, diclofenac sodium, and the fluorometholone on corneal epithelial cells were evaluated after 1-, 4-, 12-, and 24-hr of exposure compared to corneal epithelial cell treated with balanced salt solution as control. Cellular metabolic activity, cellular damage, and morphology were assessed. Corneal epithelial cell migration was quantified by the scratch-wound assay. Compared to bromfenac and pranoprofen, the cellular metabolic activity of diclofenac and fluorometholone significantly decreased after 12-hr exposure, which was maintained for 24-hr compared to control. Especially, at 1/10-diluted eye solution for 24-hr exposure, the LDH titers of fluorometholone and diclofenac sodium markedly increased more than those of bromfenac and pranoprofen. In diclofenac sodium, the Na(+) concentration was lower and amount of preservatives was higher than other NSAIDs eye solutions tested. However, the K(+) and Cl(-) concentration, pH, and osmolarity were similar for all NSAIDs eye solutions. Bromfenac and pranoprofen significantly promoted cell migration, and restored wound gap after 48-hr exposure, compared with that of diclofenac or fluorometholone. At 1/50-diluted eye solution for 48-hr exposure, the corneal epithelial cellular morphology of diclofenac and fluorometholone induced more damage than that of bromfenac or pranoprofen. Overall, the corneal epithelial cells in bromfenac and pranoprofen NSAID eye solutions are less damaged compared to those in diclofenac, included fluorometholone as steroid eye solution.

  13. Anti-inflammatory effects of progesterone in lipopolysaccharide-stimulated BV-2 microglia.

    Directory of Open Access Journals (Sweden)

    Beilei Lei

    Full Text Available Female sex is associated with improved outcome in experimental brain injury models, such as traumatic brain injury, ischemic stroke, and intracerebral hemorrhage. This implies female gonadal steroids may be neuroprotective. A mechanism for this may involve modulation of post-injury neuroinflammation. As the resident immunomodulatory cells in central nervous system, microglia are activated during acute brain injury and produce inflammatory mediators which contribute to secondary injury including proinflammatory cytokines, and nitric oxide (NO and prostaglandin E2 (PGE2, mediated by inducible NO synthase (iNOS and cyclooxygenase-2 (COX-2, respectively. We hypothesized that female gonadal steroids reduce microglia mediated neuroinflammation. In this study, the progesterone's effects on tumor necrosis factor alpha (TNF-α, iNOS, and COX-2 expression were investigated in lipopolysaccharide (LPS-stimulated BV-2 microglia. Further, investigation included nuclear factor kappa B (NF-κB and mitogen activated protein kinase (MAPK pathways. LPS (30 ng/ml upregulated TNF-α, iNOS, and COX-2 protein expression in BV-2 cells. Progesterone pretreatment attenuated LPS-stimulated TNF-α, iNOS, and COX-2 expression in a dose-dependent fashion. Progesterone suppressed LPS-induced NF-κB activation by decreasing inhibitory κBα and NF-κB p65 phosphorylation and p65 nuclear translocation. Progesterone decreased LPS-mediated phosphorylation of p38, c-Jun N-terminal kinase and extracellular regulated kinase MAPKs. These progesterone effects were inhibited by its antagonist mifepristone. In conclusion, progesterone exhibits pleiotropic anti-inflammatory effects in LPS-stimulated BV-2 microglia by down-regulating proinflammatory mediators corresponding to suppression of NF-κB and MAPK activation. This suggests progesterone may be used as a potential neurotherapeutic to treat inflammatory components of acute brain injury.

  14. Anti-inflammatory and analgesic activities of the water extract from the fruit of Phyllanthus emblica Linn.

    Directory of Open Access Journals (Sweden)

    K Jaijoy

    2010-06-01

    Full Text Available Abstract: The fresh or dry fruit of Phyllanthus emblica Linn. is used in traditional medicines for the treatment of diarrhea, jaundice and inflammatory disorder. In the present study, we investigated the anti-inflammatory and analgesic activities of the standardized water extract from the fruit of Phyllanthus emblica was prepared according to the Thai Herbal Pharmacopoeia (THP. P. emblica water extract was evaluated for its anti-inflammatory activity in rats using ethyl phenylpropiolate (EPP-induced and arachidonic acid (AA-induced ear edema, carrageenan-induced paw edema as well as cotton pellet-induced granuloma models, and its analgesic activity in mice using formalin test. The extract at 1 mg/ear exhibited anti-inflammatory effect on EPP-induced ear edema, but not on AA-induced ear edema. Oral administration of P. emblica at the doses of 150, 300 and 600 mg/kg caused dose-dependent inhibition of carrageenan-induced rat paw edema. P. emblica at 600 mg/kg did reduce neither transudative and proliferative phases nor body weight gain and thymus weight in cotton pellet-induced granuloma formation. The extract at the doses of 150, 300 and 600 mg/kg elicited a significant analgesic activity in a dose-dependent manner on both the early and late phase of formalin test. The anti-inflammatory and analgesic mechanism of activity of the standardized water extract of P. emblica seems to be similar to NSAIDs rather than to steroidal drugs. Inhibitory effect on the synthesis and/or release of inflammatory or pain mediators may be the main mechanisms of action of P. emblica water extract.   Industrial relevance: Medicinal plants have long been recognized as an important source of therapeutically effective treatment for inflammatory diseases. Many patients are turning to herbal medicine as their primary, complementary or alternative therapies because of the adverse effects of the pharmaceutical drugs. P. emblica fruit has been used in traditional management

  15. Anti-inflammatory Hydrolyzable Tannins from Myricaria bracteata.

    Science.gov (United States)

    Liu, Jia-Bao; Ding, Ya-Si; Zhang, Ying; Chen, Jia-Bao; Cui, Bao-Song; Bai, Jin-Ye; Lin, Ming-Bao; Hou, Qi; Zhang, Pei-Cheng; Li, Shuai

    2015-05-22

    Twelve hydrolyzable tannins were obtained from the twigs of Myricaria bracteata, including two new hellinoyl-type dimers, bracteatinins D1 (1) and D2 (2); a new hellinoyl-type trimer, bracteatinin T1 (3); two known monomers, nilotinin M4 (4) and 1,3-di-O-galloyl-4,6-O-(aS)-hexahydroxydiphenoyl-β-d-glucose (5); six known dimers, tamarixinin A (6), nilotinin D8 (7), hirtellins A (10), B (9), and E (8), and isohirtellin C (11); and a known trimer, hirtellin T3 (12). The structures of the tannins were elucidated by spectroscopic data analysis and comparisons to known tannins. All compounds were evaluated as free radical scavengers using 1,1-diphenyl-2-picrylhydrazyl and hydroxy radicals and compared to the activity of BHT and Trolox. Compound 6 showed a significant anti-inflammatory effect on croton oil-induced ear edema in mice (200 mg/kg, inhibition rate 69.8%) and on collagen-induced arthritis in DBA/1 mice (20 mg/kg, inhibition rate 46.0% at day 57). PMID:25918997

  16. Anti-Inflammatory Dimethylfumarate: A Potential New Therapy for Asthma?

    Directory of Open Access Journals (Sweden)

    Petra Seidel

    2013-01-01

    Full Text Available Asthma is a chronic inflammatory disease of the airways, which results from the deregulated interaction of inflammatory cells and tissue forming cells. Beside the derangement of the epithelial cell layer, the most prominent tissue pathology of the asthmatic lung is the hypertrophy and hyperplasia of the airway smooth muscle cell (ASMC bundles, which actively contributes to airway inflammation and remodeling. ASMCs of asthma patients secrete proinflammatory chemokines CXCL10, CCL11, and RANTES which attract immune cells into the airways and may thereby initiate inflammation. None of the available asthma drugs cures the disease—only symptoms are controlled. Dimethylfumarate (DMF is used as an anti-inflammatory drug in psoriasis and showed promising results in phase III clinical studies in multiple sclerosis patients. In regard to asthma therapy, DMF has been anecdotally reported to reduce asthma symptoms in patients with psoriasis and asthma. Here we discuss the potential use of DMF as a novel therapy in asthma on the basis of in vitro studies of its inhibitory effect on ASMC proliferation and cytokine secretion in ASMCs.

  17. Incorporation of anti-inflammatory agent into mesoporous silica

    Science.gov (United States)

    Rodrigues Braz, Wilson; Lamec Rocha, Natállia; de Faria, Emerson H.; Silva, Márcio L. A. e.; Ciuffi, Katia J.; Tavares, Denise C.; Furtado, Ricardo Andrade; Rocha, Lucas A.; Nassar, Eduardo J.

    2016-09-01

    The unique properties of macroporous, mesoporous, and microporous systems, including their ability to accommodate molecules of different sizes inside their pores and to act as drug delivery systems, have been the object of extensive studies. In this work, mesoporous silica with hexagonal structure was obtained by template synthesis via the sol-gel process. The resulting material was used as support to accommodate the anti-inflammatory agent indomethacin. The alkaline route was used to prepare the mesoporous silica; cetyltrimethylammonium bromide was employed as porogenic agent. The silica particles were functionalized with 3-aminopropyltriethoxysilane alkoxide (APTES) by the sol-gel post-synthesis method. Indomethacin was incorporated into the silica functionalized with APTES and into non-functionalized silica. The resulting systems were characterized by x-ray diffraction (XRD), specific area, infrared spectroscopy, and thermal analyses (TGA). XRD attested to formation of mesoporous silica with hexagonal structure. This structure remained after silica functionalization with APTES and incorporation of indomethacin. Typical infrared spectroscopy vibrations and organic material decomposition during TGA confirmed silica functionalization and drug incorporation. The specific surface area and pore volume of the functionalized material incorporated with indomethacin decreased as compared with the specific surface area and pore volume of the non-functionalized silica containing no drug, suggesting both the functionalizing agent and the drug were present in the silica. Cytotoxicity tests conducted on normal fibroblasts (GM0479A) cells attested that the silica matrix containing indomethacin was less toxic than the free drug.

  18. Nonsteroidal Anti-Inflammatory Drug Hypersensitivity in Preschool Children

    Directory of Open Access Journals (Sweden)

    Kidon Mona

    2007-12-01

    Full Text Available Although extensively studied in adults, nonsteroidal anti-inflammatory drug (NSAID hypersensitivity in children, especially in young children, remains poorly defined. Pediatricians, prescribing antipyretics for children, rarely encounter significant problems, but the few epidemiologic studies performed show conflicting results. Although it is clear that some patients with acetylsalicylic acid (ASA-sensitive asthma have their clinical onset of disease in childhood and bronchoconstriction after ASA challenge is seen in 0 to 22% of asthmatic children so challenged, ibuprofen at antipyretic doses may cause acute respiratory problems only in a very small number of mild to moderate asthmatics. The recently elucidated mechanism of action of acetaminophen may explain some occurrences of adverse reactions in patients with cross-reactive NSAID hypersensitivity on the basis of its inhibitory activity on the newly described enzyme, cyclooxygenase (COX-3. This nonspecific sensitivity to inhibition of COX is most likely genetically determined and shows a remarkable association with atopic disease even in the very young age group and possibly an increased predilection in specific ethnic groups. This review summarizes state-of-the-art published data on NSAID hypersensitivity in preschool children.

  19. Anti-inflammatory properties of drugs from saffron crocus.

    Science.gov (United States)

    Poma, Anna; Fontecchio, Gabriella; Carlucci, Giuseppe; Chichiriccò, Giuseppe

    2012-01-01

    The medicinal uses of saffron (Crocus sativus Linnaeus) have a long history beginning in Asian countries since the Late Bronze Age. Recent studies have validated its potential to lower the risk of several diseases. Some metabolites derived from saffron stigmas exert numerous therapeutic effects due to hypolipidemic, antitussive, antioxidant, antidiabetic activities and many others. Water and ethanol extracts of Crocus sativus L. are cardioprotective and counteract neurodegenerative disorders. Many of these medicinal properties of saffron can be attributed to a number of its compounds such as crocetin, crocins and other substances having strong antioxidant and radical scavenger properties against a variety of radical oxygen species and pro-inflammatory cytokines. Botany, worldwide spreading of cultivars, biochemical pathways, active constituents and chemical detection methods are reviewed. Therapeutic uses of saffron principles with particular regard to those exhibiting antioxidant and thus anti-inflammatory features are discussed. To date, very few adverse health effects of saffron have been demonstrated. At high doses (more than 5 g/die day), it should be avoided in pregnancy owing to its uterine stimulation activity.

  20. A novel anti-inflammatory oligopeptide produced by Entamoeba histolytica.

    Science.gov (United States)

    Kretschmer, R R; Rico, G; Giménez, J A

    2001-02-01

    The monocyte locomotion inhibitory factor (MLIF), a heat-stable oligopeptide found in the supernatant fluid of Entamoeba histolytica axenic cultures was isolated by ultra-filtration, gel-sieve chromatography and high powered liquid chromatography (HPLC), and its primary structure (Met-Gln-Cys-Asn-Ser) established by Edman sequencing and mass-spectrometry (MS). A synthetic peptide had the same selective anti-inflammatory features as the native material in comparable concentrations: in vitro inhibition of the locomotion in human peripheral blood monocytes, and of the respiratory burst in the same cells and in human neutrophil polymorphonuclear leucocytes; and in vivo depression of delayed hypersensitivity skin reactions to dinitrochlorobenzene in guinea pigs. This oligopeptide is apparently synthesized by the ameba as suggested by [(35)S]-Cys and Met incorporation, probably as part of a larger molecule, from which it is cleaved by proteolysis. The full sequence was not found in the 431 available E. histolytica protein sequences. The factor may contribute to the unexpected paucity of the late inflammatory reaction found in advanced invasive amebiasis and, perhaps in consequence, to the regeneration without scarring (restitutio ad integrum) of the affected organs that is observed following successful treatment of this disease

  1. ANTI-INFLAMMATORY EVALUATION OF LEAF EXTRACT OF MORINGA OLEIFERA

    Directory of Open Access Journals (Sweden)

    Gurvinder Pal Singh

    2012-02-01

    Full Text Available Moringa oleifera Lam. Is a small or medium-sized tree, about 10m high, found wild in the sub-Himalayan tract. The leaves are rich in vitamin A and C and are considered useful in scurvy and catarrhal affections. The leaves are rich in ascorbic acids, amino acids, sterols, isoquercetin glucoside, carotenes, rhamnetin, kaempferol and kaempferitrin. Flowers are traditionally used as tonic, diuretic and abortifacient considered as anthelmintic and also used to cure inflammation, muscle disease, tumors and enlargement of the spleen. All part of this plant is used for the treatment of ascites, rheumatism. Venomous bites and for enhancing cardiac function. In present study, the anti-inflammatory activity was investigated by employing main model Carrageenan induced paw odema (Winter et al., 1962. The results showed a dose dependent decrease in size of odema when observed at 0hr, 1hr, 2hr, 3hr, and 4hr. This effect corresponded with the maximum effect of test dose at 2 hr (Carrageenan-induced paw. The p value<0.0001 was considered to be statistically significant.

  2. Anti-inflammatory and anti-oxidant properties of Curcuma longa (turmeric) versus Zingiber officinale (ginger) rhizomes in rat adjuvant-induced arthritis.

    Science.gov (United States)

    Ramadan, Gamal; Al-Kahtani, Mohammed Ali; El-Sayed, Wael Mohamed

    2011-08-01

    Turmeric (rich in curcuminoids) and ginger (rich in gingerols and shogaols) rhizomes have been widely used as dietary spices and to treat different diseases in Ayurveda/Chinese medicine since antiquity. Here, we compared the anti-inflammatory/anti-oxidant activity of these two plants in rat adjuvant-induced arthritis (AIA). Both plants (at dose 200 mg/kg body weight) significantly suppressed (but with different degrees) the incidence and severity of arthritis by increasing/decreasing the production of anti-inflammatory/pro-inflammatory cytokines, respectively, and activating the anti-oxidant defence system. The anti-arthritic activity of turmeric exceeded that of ginger and indomethacin (a non-steroidal anti-inflammatory drug), especially when the treatment started from the day of arthritis induction. The percentage of disease recovery was 4.6-8.3% and 10.2% more in turmeric compared with ginger and indomethacin (P turmeric over ginger and indomethacin, which may have beneficial effects against rheumatoid arthritis onset/progression as shown in AIA rat model.

  3. DMPD: Mechanisms for the anti-inflammatory effects of adiponectin in macrophages. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 18336664 Mechanisms for the anti-inflammatory effects of adiponectin in macrophages...(.html) (.csml) Show Mechanisms for the anti-inflammatory effects of adiponectin in macrophages. PubmedID 18...336664 Title Mechanisms for the anti-inflammatory effects of adiponectin in macro

  4. DMPD: Anti-inflammatory actions of PPAR ligands: new insights on cellular andmolecular mechanisms. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 17981503 Anti-inflammatory actions of PPAR ligands: new insights on cellular andmol...) (.html) (.csml) Show Anti-inflammatory actions of PPAR ligands: new insights on cellular andmolecular mech...anisms. PubmedID 17981503 Title Anti-inflammatory actions of PPAR ligands: new in

  5. Assessment of anti-inflammatory potential of Sesbania bispinosa Linn. leaf extracts and fractions by acute and

    Directory of Open Access Journals (Sweden)

    Ganesh D. Boddawar

    2016-09-01

    Conclusion: The results of the present study suggest that leaves of S. bispinosa possess significant level of anti-inflammatory activity and ethyl acetate fraction may be further explored as an anti-inflammatory remedy as it was found to possess higher anti-inflammatory activity among all extracts and fractions as demonstrated in both acute and chronic models.

  6. Potential analgesic, anti-inflammatory and antioxidant activities of hydroalcoholic extract of Areca catechu L. nut.

    Science.gov (United States)

    Bhandare, Amol M; Kshirsagar, Ajay D; Vyawahare, Neeraj S; Hadambar, Avinash A; Thorve, Vrushali S

    2010-12-01

    The hydroalcoholic extract of Areca catechu L. (ANE) nut was screened for its analgesic, anti-inflammatory and in vitro antioxidant potential. Three doses of ANE (250, 500 and 1000 mg/kg orally) were tested for analgesic and anti-inflammatory activities. Evaluation of analgesic activity of ANE was performed using hot plate and formalin test in mice. ANE showed maximum increase in hot plate reaction time (56.27%, pAreca catechu could be considered as a potential analgesic, anti-inflammatory and antioxidant agent. PMID:20849907

  7. Anti-inflammatory and mast cell protective effect of ficus religiosa.

    Science.gov (United States)

    Viswanathan, S; Thirugnanasambantham, P; Reddy, M K; Narasimhan, S; Subramaniam, G A

    1990-10-01

    The aqueous extract of bark of Ficus religiosa was prepared and investigated for its anti-inflammatory effect and for its protective effect on mast cells against degranulation. A significant anti-inflammatory effect was observed in both acute and chronic models of inflammation. The extract also protected mast cells from degranulation induced by various degranulatiors. The observed anti-inflammatory and mast cell protective effect may be responsible for the beneficial effect of Ficus religiosa in kumkum dermatitis and other inflammatory conditions. PMID:22556521

  8. Antioxidant and Anti-Inflammatory Activities of Essential Oils: A Short Review

    Directory of Open Access Journals (Sweden)

    Maria Graça Miguel

    2010-12-01

    Full Text Available Essential oils are complex mixtures isolated from aromatic plants which may possess antioxidant and anti-inflammatory activities of interest in thye food and cosmetic industries as well as in the human health field. In this work, a review was done on the most recent publications concerning their antioxidant and anti-inflammatory activities. At the same time a survey of the methods generally used for the evaluation of antioxidant activity and some of the mechanisms involved in the anti-inflammatory activities of essential oils are also reported.

  9. 信息动态%Anti-inflammatory and analgesic effects of granule to pelvic inflammation

    Institute of Scientific and Technical Information of China (English)

    2011-01-01

    Objective To study anti-inflammatory and analgesic effects of granucle to pelvic inflammation. Methods The anti-inflammatory effects were studied by dimethylbenzene-induced swelling oar in mouse, carrageenin induced paw edema and tampon-induced proliferation in rats. The analgesic effects were studied by acetic acid-induced writhing and optothermal-induced pain in mice. Results Granule to pelvic inflammation significantly reduced swelling oar in mouse, paw edema and proliferation in rats;prolonged latency of writhing test, reduced the writhing number and improved optothermal-induced analgesia percentage. Conclusion Granule to pelvic inflammation has anti-inflammatory and analgesic effects.

  10. The Epidemiology of Nonsteroidal Anti-Inflammatory Drugs

    Directory of Open Access Journals (Sweden)

    Jerry Tenenbaum

    1999-01-01

    Full Text Available Nonsteroidal anti-inflammatory drug (NSAID use has increased dramatically in the past two decades. A large proportion of the elderly population (more than 65 years of age holds a current or recent NSAID prescription, accounting for approximately 90% of all NSAID prescriptions. Despite studies that advise finding alternatives for NSAIDs for the management of osteoarthritis, physicians often prescribe NSAIDs first for such common musculoskeletal conditions. Despite being identified as risk factors for gastrointestinal complications, the simultaneous use of two NSAIDs and the coadministration of NSAIDs with corticosteroids and with coumadin continue to occur. The point prevalence of NSAID-induced ulcers is 10% to 30%, and 15% to 35% of all peptic ulcer complications are caused by NSAIDs. The increased risk of gastrointestinal complications when NSAIDs are used is 3% to 5%. This risk increases with other identified risk factors (eg, older age, previous gastrointestinal history, comorbid diseases and poor health. Gastrointestinal causes of hospitalization (eg, gastrointestinal hemorrhage and perforation and death have increased in parallel to increased NSAID use. ‘Antiulcer’ agents are prescribed twice as often in NSAID users, and the economic impact (eg, diagnostic tests and hospitalization is that about one-third of the arthritis budget has been dedicated to deal with gastrointestinal side effects of NSAIDs. Misoprostol and omeprazole have been shown to be cytoprotective for the gastroduodenal mucosa when NSAIDs are used, and misoprostol has been shown to reduce the risk of gastroduodenal ulcer complications. Economic evaluations have suggested that these agents are a cost effective means of dealing with such NSAID-associated problems. Although no NSAID is totally safe, a number of studies have demonstrated that NSAIDs may be ranked according to relative gastrointestinal toxicity. The role of Helicobacter pylori in NSAID-associated problems

  11. Determination of Teloschistes flavicans (sw norm anti-inflammatory activity

    Directory of Open Access Journals (Sweden)

    Eugênia C Pereira

    2010-01-01

    Full Text Available Background: Lichens produce a variety of substances that possesses pharmacological actions. However, rare products are submitted to rigorous scientific tests or have the risk potential or side effects evaluated. The lack of medical and sanitary control, absence of accurate botanical identification or purity certification, founded in diverse natural products, may represent great danger to population health. This work aimed to evaluate toxic effects and anti-inflammatory action in vivo of Teloschistes flavicans (Sw. Norm. (TFN unrefined extracts, as well as determinate its main constituents. Methods: The carrageenan induced paw edema and cotton pellet implant induced granuloma methods were utilized, besides a classic acute toxicity test. TFN acetone extract inhibited carrageenan paw edema on 60, 120, and 180 min (inhibition percentiles of 45.03%, 60.59% and 41.72%. Results: TFN ethereal (inhibition percentiles of 23.95% and 29.01% and chloroform (inhibition percentiles of 28.8% and 22.04% extracts inhibited edema on 120 and 180 min. None of the extract inhibited the granuloma development. None of the extract caused death or other acute toxicity signs. Vicanicine (60.26% in ethereal extract and 51.17% in acetone extract, parietine (9.60% in ethereal extract and 15.38% on second, falacinol (0.78% in ether and 14.95% in acetone and very low concentration of falacinal (0.15% in ethereal extract and 3.32% in acetone extract were detected in the medicine. Conclusions: The tested extracts have antiedematogenic activity, but are not effective on subchronic inflammation. The extracts do not present toxic effects in administered doses.

  12. Inflammatory and anti-inflammatory effects of soybean agglutinin

    Directory of Open Access Journals (Sweden)

    Benjamin C.F.

    1997-01-01

    Full Text Available Soybean agglutinin (SBA lectin, a protein present in raw soybean meals, can bind to and be extensively endocytosed by intestinal epithelial cells, being nutritionally toxic for most animals. In the present study we show that SBA (5-200 µg/cavity injected into different cavities of rats induced a typical inflammatory response characterized by dose-dependent exudation and neutrophil migration 4 h after injection. This effect was blocked by pretreatment with glucocorticoid (0.5 mg/kg or by co-injection of N-acetyl-galactosamine (100 x [M] lectin, but not of other sugars (100 x [M] lectin, suggesting an inflammatory response related to the lectin activity. Neutrophil accumulation was not dependent on a direct effect of SBA on the macrophage population since the effect was not altered when the number of peritoneal cells was increased or decreased in vivo. On the other hand, SBA showed chemotactic activity for human neutrophils in vitro. A slight increase in mononuclear cells was observed 48 h after ip injection of SBA. Phenotypic analysis of these cells showed an increase in the CD4+/CD8- lymphocyte population that returned to control levels after 15 days, suggesting the development of an immune response. SBA-stimulated macrophages presented an increase in the expression of CD11/CD18 surface molecules and showed some characteristics of activated cells. After intravenous administration, SBA increased the number of circulating neutrophils and inhibited in a dose-dependent manner the neutrophil migration induced by ip injection of carrageenan into peritoneal cavities. The co-injection of N-acetyl-galactosamine or mannose, but not glucose or fucose, inhibited these effects. The data indicate that soybean lectin is able to induce a local inflammatory reaction but has an anti-inflammatory effect when present in circulating blood

  13. Anti-inflammatory effect of Momordica charantia in sepsis mice.

    Science.gov (United States)

    Chao, Che-Yi; Sung, Ping-Jyun; Wang, Wei-Hsien; Kuo, Yueh-Hsiung

    2014-01-01

    Wild bitter gourd (Momordica charantia L. var. abbreviate Seringe), a common vegetable in Asia, is used in traditional medicine to treat various diseases, including inflammation. Extant literature indicates that wild bitter gourds have components that activate PPARα and PPARγ. This research probed the influence of adding wild bitter gourd to diets on inflammation responses in mice with sepsis induced by intraperitoneal injection of LPS. Male BALB/c mice were divided normal, sepsis, positive control, and three experimental groups. The latter ate diets with low (1%), moderate (2%), and high (10%) ratios of wild bitter gourd lyophilized powder. Before mice were sacrificed, with the exception of the normal group, intraperitoneal injection of LPS induced sepsis in each group; positive control group was injected with LPS after PDTC. This experiment revealed starkly lower weights in groups with added wild bitter gourd than those of the remaining groups. Blood lipids (TG, cholesterol, and NEFA) were also lower in comparison to the sepsis group, and blood glucose concentrations recovered and approached normal levels. Blood biochemistry values related to inflammation reactions indicated GOT, GPT, C-RP, and NO concentrations of groups with added wild bitter gourd were all lower than those of the sepsis group. Secretion levels of the spleen pro-inflammatory cytokines IL-1, IL-6, and TNF-α tallied significantly lower in comparison to the sepsis group, whereas secretion levels of IL-10 anti-inflammatory cytokine increased. Expression level of proteins NF-κB, iNOS, and COX-2 were significantly inhibited. Results indicate wild bitter gourd in diets promoted lipid metabolism, reducing fat accumulation, and improving low blood glucose in sepsis. Addition of wild bitter gourd can reduce inflammation biochemical markers or indicators and pro-inflammatory cytokines in the body, hence improving the inflammation responses in mice with sepsis. PMID:25153878

  14. Anti-inflammatory and antiviral effects of Glossogyne tenuifolia.

    Science.gov (United States)

    Wu, Ming-Jiuan; Weng, Ching-Yi; Ding, Hsiou-Yu; Wu, Pei-Jong

    2005-01-21

    Glossogyne tenuifolia (Hsiang-Ju) is a traditional antipyretic and hepatoprotective herb used in Chinese medicine. The aim of this research is to investigate the pharmacological activities and potent components of the ethanol extract of Glossogyne tenuifolia (GT) in human primary cells and cell line. We found that GT (0.1 approximately 0.25 mg/ml) exerted dose-dependent inhibitions on the release of TNF-alpha and IL-6 in LPS-activated human whole blood and peripheral blood mononuclear cells (PBMC), and IFN-gamma in PHA-stimulated human whole blood. The lack of cytotoxicity indicated that the inhibitory effects of GT on cytokine production were not due to cell death. Luteolin, the deglycosylated derivative of one of the major compositions, luteolin-7-glucoside, exerted inhibitory effects on TNF-alpha, IL-6 and IFN-gamma production in activated human whole blood with estimated IC(50)s of 42.73 microM, 44.86 microM and 3.34 microM, respectively. Furthermore, GT had potent anti-hepatitis B virus (HBV) effects on the human hepatocellular carcinoma cell line, PLC/PRF/5. GT exhibited a dose-dependent inhibition on the release of hepatitis B surface antigen (HBsAg) by repressing the expression of HBsAg with IC(50) of 0.093 mg/ml. We concluded that GT exerted combinatorial anti-inflammatory and antiviral effects, and the multiple actions may underlie its traditional hepatoprotective function. PMID:15620577

  15. Development of poly(glycerol adipate) nanoparticles loaded with non-steroidal anti-inflammatory drugs.

    NARCIS (Netherlands)

    Wahab, A.; Favretto, M.E.; Onyeagor, N.D.; Khan, G.M.; Douroumis, D.; Casely-Hayford, M.A.; Kallinteri, P.

    2012-01-01

    The aim of this study was to assess acylated and non-acylated poly(glycerol adipate) polymers (PGA) as suitable nanoparticulate systems for encapsulation and release of ibuprofen, ibuprofen sodium salt (IBU-Na) and ketoprofen as model drugs. Drug encapsulated nanoparticles were prepared using the in

  16. Cardiovascular risks associated with non-aspirin non-steroidal anti-inflammatory drug use

    DEFF Research Database (Denmark)

    Schmidt, Morten

    2015-01-01

    whether use of non-aspirin NSAIDs was associated with risk of major adverse cardiovascular events (MACE) after coronary stent implantation (study I), risk of venous thromboembolism (study II), risk of atrial fibrillation (study III), and 30-day stroke mortality (study IV). We conducted two cohort studies...... coronary intervention with stent implantation in Western Denmark. Compared with non-users of NSAIDs, the adjusted incidence rate ratio (IRR) for MACE was 1.04 (95% CI: 0.83-1.31) for users of nonselective NSAIDs and 1.00 (95% CI: 0.81-1.25) for users of COX-2 inhibitors. Consistently, current use of non-aspirin...... COX-2 inhibitors, the MRR was driven by new use of older traditional COX-2 inhibitors (1.30, 95% CI: 1.12-1.52), being 1.51 (95% CI: 1.16-1.98) for etodolac and 1.21 (95% CI: 1.01-1.45) for diclofenac. Mortality from hemorrhagic strokes was not associated with preadmission use of non-aspirin NSAIDs...

  17. Topical non steroidal anti inflammatory drug (NSAIDs microemulsions: Rationale, review and future prospective

    OpenAIRE

    Vinod Singh; Hitesh Sharma; Ram Veerma; Athar Javed; Mamta Singh

    2013-01-01

    Microemulsions serve as ideal candidates as potential drug delivery system due to their specialized qualities of improved solubilisation of drug, extended shelf life and ease of method of preparation and administration to patients. The unique features of microemulsions are thermodynamically stable, clear, colloidal dispersion of water and oil that are stabilized by surfactant and cosurfactant. Microemulsion typically has a droplet diameter of approximately 100 nm or less. Microemulsions have ...

  18. [Survey of consumer demand for non-steroidal anti-inflammatory preparations].

    Science.gov (United States)

    Khmelidze, M G; Ernashvili, V M; Abuladze, N B; Dugashvili, N G

    2007-01-01

    Subject of marketing research may represent medical means as well as consumers which are characterizing the market. The significant and spread out methods of segmentation is group method with one or some signs, also structural and statistical analysis methods. In the grouping process the geographical, demographic, social-economic and sociological principles are frequently used. Segmentation is the method to represent the difference on the basis of defined principles. 107 persons were participated in the interviews, among them 93 women and 14 men. Their age from 20-up to 60, among them 43 participants were with high education, 22 with technical and 20 with secondary education. The majority of population (51,4%) gets the information about new medicines by advertisements. The sources of getting information are equally from doctors (23,37%) and the chemists (23,37%); from other means this index is very low (1,86%). The population gives the priority to import insteroidic antiphlogistic medical means (45, 78%); less to native medicines (24,3%) and 29,9 % of participants can't give the answer on this question. The population mostly use tablets (78,5%), ampoules (11,21%); capsules (5,6%), ointment (3,75%) and candles (9,94%). Our study showed, that population more often use aspirin, diklophenak, indometacin, ibuprophen, ketoprofen. The main factors on the choosing the medicines are quality and price, producing firm's country prestige. PMID:17327636

  19. Steroid Anti-Inflammatory Effects Did Not Improve Organ Quality in Brain-Dead Rats

    NARCIS (Netherlands)

    Rebolledo, Rolando A.; Liu, Bo; Akhtar, Mohammed Z.; Ottens, Petra J.; Zhang, Jian-ning; Ploeg, Rutger J.; Leuvenink, Henri G. D.

    2015-01-01

    Effect of glucocorticoid administration on improving the outcomes of kidney and liver allografts has not been clearly elucidated. This study investigated the effect of prednisolone administration after onset of brain death (BD) on kidney and liver in a controlled rat model of BD. BD was induced in r

  20. The Role of Non-Steroidal Anti-Inflammatory Drugs in Renal Colic

    Directory of Open Access Journals (Sweden)

    Elizabeth Waine

    2010-04-01

    Full Text Available NSAIDs provide optimal analgesia in renal colic due to the reduction in glomerular filtration and renal pelvic pressure, ureteric peristalsis and ureteric oedema. Prevention of glomerular afferent arteriolar vasodilatation renders these patients at risk of renal impairment. NSAIDs have the additional benefit of reducing the number of new colic episodes and preventing subsequent readmission to hospital. Despite recent work promoting the use of pharmacological agents to improve stone passage rates, NSAIDs do not appear to reduce the time to stone passage or increase the likelihood of stone passage in renal colic.

  1. The Role of Non-Steroidal Anti-Inflammatory Drugs in Renal Colic

    OpenAIRE

    Elizabeth Waine; Kim Davenport

    2010-01-01

    NSAIDs provide optimal analgesia in renal colic due to the reduction in glomerular filtration and renal pelvic pressure, ureteric peristalsis and ureteric oedema. Prevention of glomerular afferent arteriolar vasodilatation renders these patients at risk of renal impairment. NSAIDs have the additional benefit of reducing the number of new colic episodes and preventing subsequent readmission to hospital. Despite recent work promoting the use of pharmacological agents to improve stone passage ra...

  2. Fulminant hepatic failure in woman with iron and non-steroidal anti-inflammatory drug intoxication.

    Science.gov (United States)

    Magdalan, Jan; Zawadzki, Marcin; Sozanski, Tomasz

    2011-08-01

    A 17-year-old, previously healthy female ingested 16,000 mg iron sulphate (96.15 mg of iron ions per kg of b.wt.) with a suicidal intent. The patient was admitted to a toxicology unit 10 hours after the drug ingestion. Serum iron concentration at admission was 2351 μg% (421.0 μmol/L). In the course of the intoxication, hemorrhagic gastritis, renal insufficiency and increasing signs of fulminant hepatic failure complicated with coagulopathy and encephalopathy were observed. Treatment with deferoxamine was started immediately after admission to the hospital and continued for 15 hours until the serum concentration of iron decreased to 145 μg% (25.9 μmol/L). Patient was qualified for liver transplant, therefore albumin dialysis as a bridge to liver transplantation was performed. In spite of two procedures of albumin dialysis using the Prometheus system, deep coma, shock and respiratory insufficiency developed. The patient died 80 hours after iron ingestion. In the presented case, the ingestion of a very high dose of iron and late introduction of deferoxamine treatment contributed to fulminant liver failure and fatal outcome of the intoxication. PMID:20952452

  3. Cardiovascular safety of non-steroidal anti-inflammatory drugs among healthy individuals

    DEFF Research Database (Denmark)

    Fosbøl, Emil Loldrup; Køber, Lars; Torp-Pedersen, Christian;

    2010-01-01

    Studies have raised concern on the cardiovascular safety of NSAIDs. We studied safety of NSAID therapy in a nationwide cohort of healthy individuals.......Studies have raised concern on the cardiovascular safety of NSAIDs. We studied safety of NSAID therapy in a nationwide cohort of healthy individuals....

  4. Anti-inflammatory Agents in the Treatment of Diabetes and Its Vascular Complications.

    Science.gov (United States)

    Pollack, Rena M; Donath, Marc Y; LeRoith, Derek; Leibowitz, Gil

    2016-08-01

    The association between hyperglycemia and inflammation and vascular complications in diabetes is now well established. Antidiabetes drugs may alleviate inflammation by reducing hyperglycemia; however, the anti-inflammatory effects of these medications are inconsistent and it is unknown whether their beneficial metabolic effects are mediated via modulation of chronic inflammation. Recent data suggest that immunomodulatory treatments may have beneficial effects on glycemia, β-cell function, and insulin resistance. However, the mechanisms underlying their beneficial metabolic effects are not always clear, and there are concerns regarding the specificity, safety, and efficacy of immune-based therapies. Herein, we review the anti-inflammatory and metabolic effects of current antidiabetes drugs and of anti-inflammatory therapies that were studied in patients with type 2 diabetes. We discuss the potential benefit of using anti-inflammatory treatments in diabetes and important issues that should be addressed prior to implementation of such therapeutic approaches. PMID:27440839

  5. Analgesic and anti-inflammatory activity of root bark of Grewia asiatica Linn. in rodents

    Directory of Open Access Journals (Sweden)

    Udaybhan Singh Paviaya

    2013-01-01

    Conclusions: The present study indicates that root bark of G. asiatica exhibits peripheral and central analgesic effect and anti-inflammatory activity, which may be attributed to the various phytochemicals present in root bark of G. asiatica.

  6. Anti-inflammatory and gastroprotective properties of Hypericum richeri oil extracts.

    Science.gov (United States)

    Zdunić, Gordana; Godevac, Dejan; Milenković, Marina; Savikin, Katarina; Menković, Nebojsa; Petrović, Silvana

    2010-08-01

    Oil extracts of flowering tops of Hypericum richeri Vill. prepared in three different ways were evaluated for chemical composition, and anti-inflammatory and gastroprotective activities. An HPLC method was developed for determination of two dominant flavonoids, quercetin and I3,II8-biapigenin. The carrageenan-induced rat paw edema test was used for screening the anti-inflammatory activity, while indomethacin-induced rat gastric mucosa damage test was used for evaluation of gastroprotective activity. The oil extract prepared by maceration with 96% ethanol, followed by extraction with sunflower oil by heating on a water bath, exhibited the highest anti-inflammatory (38.4%) and gastroprotective activities (gastric damage score of 0.9). The same oil extract had the highest content of quercetin (49 microg/mL) and I3,II8-biapigenin (60 microg/mL). These results approve the usage of oil extracts of H. richeri as an anti-inflammatory and gastroprotective agent.

  7. IN VITRO ANTI-INFLAMMATORY ACTIVITY OF PTEROCARPUS MARSUPIUM ROXB. STEM BARK ON ALBINO RATS

    Directory of Open Access Journals (Sweden)

    Mohammed Rageeb Mohammed Usman

    2012-04-01

    Full Text Available Natural products are believed to be an important source of new chemical substance with potential therapeutic applicability. Several plant species traditionally used as anti-inflammatory.This research work is carryout for the anti-inflammatory activity of Pterocarpus marsupium roxb. Stem bark extracts using Carrageenan induced rat paw oedema method. Ibuprofen 60mg/kg p.o. was kept as standard. The research was carried out in Wister strain weighing 150-200gm. The Methanol (100mg/Kg and Aqueous extract (100mg/Kg has exhibited anti-inflammatory activity in carrageenan induced rat paw oedema method. Flavonoids present in stem bark may be responsible for anti-inflammatory activity. However, it needs isolation, structural elucidation and screening of above active principles to pin point activity of drug.

  8. Analgesic and anti-inflammatory activities ofPassiflora foetida L

    Institute of Scientific and Technical Information of China (English)

    Sasikala V; Saravanan S; Parimelazhagan T

    2011-01-01

    Objective:To investigate the analgesic and anti-inflammatory activities of ethanol extract of Passiflora foetida (P. foetida) leaves.Methods:Ethanol extract ofP. foetida leaf was evaluated for analgesic action by acetic acid-induced writhing and hot plate method in albino mice. The anti-inflammatory property of ethanolic leaf extract was tested by carrageenan induced acute paw edema and histamine induced acute paw edema in rats.Results:The dose200 mg/kg ofP. foetida leaf extract exhibited highest significant analgesic activity [(13.50±0.43) min] at a reaction time of20 min in hot plate method in mice. The ethanol extract of leaf dose 100 mg/kg produced a highly significant anti inflammatory effect [(1.302±0.079)mL] in rats.Conclusions: It is very clear thatP. foetidaalso has analgesic and anti-inflammatory activities for the pharmaceuticals.

  9. Anti-inflammatory potential of Agaricus in carrageenan-induced model of local inflammation in rats

    Directory of Open Access Journals (Sweden)

    Abdelrazzag A. Elmajdoub

    2015-06-01

    Conclusions: These data may indicate that Agaricus extract has the potential of anti-inflammatory activity that could be applied in acute inflammatory disorders. [Int J Basic Clin Pharmacol 2015; 4(3.000: 497-502

  10. INVESTIGATION OF ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY OF CURCUMA LONGA

    Directory of Open Access Journals (Sweden)

    Mohammad Basir Khan , Md. Atai Rabby , Md Hasmat Ullah and Chowdhury Faiz Hossain*

    2013-03-01

    Full Text Available ABSTRACT: Turmeric (Curcuma longa is a rhizomatous herbaceous perennial plant used as a food additive. It has been reported that rhizome of this plant have antibacterial, antifungal, anti-inflammatory, antioxidant and antitumor property. Methanol extract of Rhizome of Curcuma longa was investigated here to see the antimicrobial actions and anti-inflammatory effect. During the extraction process a purified single compound (D1 was isolated and investigated for its antimicrobial activity. Significant antimicrobial activity than penicillin were found for 500µg C. longa extract. Anti-inflammatory action of C. longa was also assessed using mice models. The purified compound D1 fraction showed antimicrobial action in 50µg concentration. Our study reveal that C. longa has antimicrobial activity against various gram positive and gram negative bacteria where curcumin may not be the only compound that is responsible for the antimicrobial activity. On the other hand, C. longa extract had shown significant anti-inflammatory action.

  11. Phenolic composition, anitproliferative and anti-inflammatory properties of conventional and organic cinnamon and peppermint

    Science.gov (United States)

    Conventional and organic cinnamon and peppermint were investigated for their phenolic profile, antiproliferative, anti-inflammatory, and antioxidant properties. Accelerated solvent extraction (ASE) with 75% acetone was a better method than Soxhlet and overnight extraction for phenolic content and a...

  12. Screening of Ficus religiosa leaves fractions for analgesic and anti-inflammatory activities

    OpenAIRE

    Vishal Gulecha; Sivakumar, T.; Aman Upaganlawar; Manoj Mahajan; Chandrashekhar Upasani

    2011-01-01

    Objective : To evaluate the different fractions of dried leaves of Ficus religiosa Linn for analgesic and anti-inflammatory activity using different models of pain and inflammation Materials and Methods : The analgesic activity of F. religiosa carried out using acetic acid-induced writhing in mice and tail flick test in rats. The anti-inflammatory activity was evaluated using carrageenan-induced rat paw edema and cotton pellet-granuloma formation in rats. Five different fractions (FRI, FR...

  13. Does prolonged anti-inflammatory therapy reduce number of unnecessary repeat saturation prostate biopsy?

    OpenAIRE

    Giuseppe Candiano; Pietro Pepe; Francesco Pietropaolo; Francesco Aragona

    2013-01-01

    Introduction. The effect of a prolonged oral anti-inflammatory therapy on PSA values in patients with persistent abnormal PSA values after negative prostate biopsy (PBx) was evaluated. Material and methods. From September 2011 to September 2012, 70 patients (medi- an age 62 years), with persistent abnormal PSA values after negative extended PBx, were given an herbal extract with anti-inflammatory activity for 3 months (Lenidase®; 1 tablet daily constituted of baicalina, bromelina and esci...

  14. Role of Prooxidants and Antioxidants in the Anti-Inflammatory and Apoptotic Effects of Curcumin (Diferuloylmethane)

    OpenAIRE

    Sandur, Santosh K.; Ichikawa, Haruyo; Pandey, Manoj K.; Kunnumakkara, Ajaikumar B.; Sung, Bokyung; Sethi, Gautam; Aggarwal, Bharat B.

    2007-01-01

    Extensive research within last half a century has indicated that curcumin (diferuloylmethane), a yellow pigment in curry powder, exhibits antioxidant, anti-inflammatory and proapoptotic activities. Whether anti-inflammatory and proapoptotic activities assigned to curcumin, are mediated through its antioxidant mechanism was investigated. We found that TNF-mediated NF-κB activation was inhibited by curcumin; and glutathione reversed the inhibition. Similarly, suppression of TNF-induced AKT acti...

  15. AP-1/IRF-3 Targeted Anti-Inflammatory Activity of Andrographolide Isolated from Andrographis paniculata

    OpenAIRE

    Ting Shen; Woo Seok Yang; Young-Su Yi; Gi-Ho Sung; Man Hee Rhee; Haryoung Poo; Mi-Yeon Kim; Kyung-Woon Kim; Jong Heon Kim; Jae Youl Cho

    2013-01-01

    Andrographolide (AG) is an abundant component of plants of the genus Andrographis and has a number of beneficial properties including neuroprotective, anticancer, anti-inflammatory, and antidiabetic effects. Despite numerous pharmacological studies, the precise mechanism of AG is still ambiguous. Thus, in the present study, we investigated the molecular mechanisms of AG and its target proteins as they pertain to anti-inflammatory responses. AG suppressed the production of nitric oxide (NO) an...

  16. ANTI-INFLAMMATORY ACTIVITIES OF SOME SPECIES OF ANDROGRAPHIS WALL. (ACANTHACEAE)

    OpenAIRE

    Balu, S.; Alagesaboopathi, C.

    1993-01-01

    The anti – inflammatory activities of the alcoholic extracts of three species of Andrographis Wall. were assayed at a dose of 500 mg/kg body weight in Male albino rats using carrageenin induced rat paw edema. All the extracts were screened for their anti-inflammatory activities in Carrageenin induced inflammation in rats. The maximal anti-inflammatory activity was found with the alcoholic extract of Andrographis alata Nees.

  17. The marine plant thalassia testudinum possesses anti-inflammatory and analgesic properties

    OpenAIRE

    Llanio, M.; Fernández, M.D.; Cabrera, B.; Bermejo, P.; Abad, M.J.; Payá, M; Alcaraz, M. J.

    2006-01-01

    The natural marine compounds represent a source of new chemical structures and of pharmacological substances with anti-inflammatory activity that will allow to deep in the knowledge of the inflammatory process and in novel mechanisms of action of therapeutic agents. In this work we carry out the study of a extract of a marine plant present in the Cuban coast, Thalassia testudinum (Tt) with the objective of detecting anti-inflammatory and analgesic effects by carrageena...

  18. ANTI-INFLAMMATORY ACTIVITY OF WHOLE PLANT OF POLYGALA ROSMARINIFOLIA WIGHT & ARN (POLYGALACEAE

    Directory of Open Access Journals (Sweden)

    V.R. Mohan et al

    2012-10-01

    Full Text Available In the present study, Polygala rosmarinifolia whole plant was extracted with ethanol and evaluated for anti-inflammatory activity in rats using a carrageenan induced paw edema method. Ethanol extract exhibits potent anti-inflammatory activity at 200mg/kg at 3rd hr after administration is compared with reference standard drug, Indomethacin. Observed pharmacological activity in the present study provides scientific validation of ethnomedicinal use of this plant in treating acute inflammation.

  19. Genetically Engineered Immunomodulatory Streptococcus thermophilus Strains Producing Antioxidant Enzymes Exhibit Enhanced Anti-Inflammatory Activities

    OpenAIRE

    del Carmen, Silvina; de Moreno de LeBlanc, Alejandra; Martin, Rebeca; Chain, Florian; Langella, Philippe; Bermúdez-Humarán, Luis G; LeBlanc, Jean Guy

    2014-01-01

    The aims of this study were to develop strains of lactic acid bacteria (LAB) having both immunomodulatory and antioxidant properties and to evaluate their anti-inflammatory effects both in vitro, in different cellular models, and in vivo, in a mouse model of colitis. Different Lactobacillus delbrueckii subsp. bulgaricus and Streptococcus thermophilus strains were cocultured with primary cultures of mononuclear cells. Analysis of the pro- and anti-inflammatory cytokines secreted by these cells...

  20. Anti-inflammatory and anti-cancer activity of mulberry (Morus alba L.) root bark

    OpenAIRE

    Eo, Hyun Ji; Park, Jae Ho; Park, Gwang Hun; Lee, Man Hyo; Lee, Jeong Rak; Koo, Jin Suk; Jeong, Jin Boo

    2014-01-01

    Background Root bark of mulberry (Morus alba L.) has been used in herbal medicine as anti-phlogistic, liver protective, kidney protective, hypotensive, diuretic, anti-cough and analgesic agent. However, the anti-cancer activity and the potential anti-cancer mechanisms of mulberry root bark have not been elucidated. We performed in vitro study to investigate whether mulberry root bark extract (MRBE) shows anti-inflammatory and anti-cancer activity. Methods In anti-inflammatory activity, NO was...

  1. ANTI-INFLAMMATORY ACTIVITY OF ETHANOLIC STEM EXTRACTS OF RUBIA CORDIFOLIA LINN. IN RATS

    OpenAIRE

    Tailor Chandra Shekhar; Bahuguna Y M; Singh Vijender

    2010-01-01

    In the present Study of Ethanolic extract of Stem of Rubia cordifolia Linn.(Rubiaceae) was screened for anti-inflammatory activity in carrageenan induced paw oedema rats. The effect was assessed by Difference in paw oedema volume, before & after the low & high dose administration of the extract in Rats. Ethanolic extract of Rubia cordifolia stem (20 & 40 mg./kg./ml.) were administered orally. Anti-inflammatory effects were compared with Standard drug- Indomethacin (10mg./kg/ml.). These observ...

  2. Anti-inflammatory and antinociceptive activities of Bauhinia monandra leaf lectin

    OpenAIRE

    Campos, Janaína K. L.; Araújo, Chrisjacele S. F.; Araújo, Tiago F. S.; Santos, Andréa F. S.; Teixeira, J.A.; Vera L M Lima; Coelho, Luana C. B. B.

    2016-01-01

    A galactose-specific lectin from Bauhinia monandra leaves (BmoLL) have been purified through ammonium sulphate fractionation followed by guar gel affinity chromatography column. This study aimed to evaluate the potential anti-inflammatory and antinociceptive activity of pure BmoLL in mice. Anti-inflammatory activity was evaluated by 1% carrageenan-induced inflammation in mice treated with BmoLL. Acetic acid-induced abdominal writhing and hot plate methods evaluated antinociceptive activity. B...

  3. Exercise-induced hippocampal anti-inflammatory response in aged rats

    OpenAIRE

    Gomes da Silva, Sérgio; Simões, Priscila Santos Rodrigues; Mortara, Renato Arruda; Scorza, Fulvio Alexandre; Cavalheiro, Esper Abrão; da Graça Naffah-Mazzacoratti, Maria; Arida, Ricardo Mario

    2013-01-01

    Aging is often accompanied by cognitive decline, memory impairment and an increased susceptibility to neurodegenerative disorders. Most of these age-related alterations have been associated with deleterious processes such as changes in the expression of inflammatory cytokines. Indeed, higher levels of pro-inflammatory cytokines and lower levels of anti-inflammatory cytokines are found in the aged brain. This perturbation in pro- and anti-inflammatory balance can represent one of the mechanism...

  4. Antioxidant, Anti-Inflammatory, and Cytotoxic Activities of Garcinia nervosa (Clusiaceae)

    OpenAIRE

    N. M. U. Seruji; H. Y. Khong; C. J. Kutoi

    2013-01-01

    In our continuing interest on Sarawak Garcinia species, we carried out the evaluation of antioxidant, anti-inflammatory and cytotoxic activities on the methanolic extracts of Garcinia nervosa. The extracts were prepared from its air-dried grounded leaves and barks. The evaluation of antioxidant activities was done using the (2,2-diphenyl-1-picrylhydrazyl) DPPH radical scavenging assay and the result showed high radical scavenging activities. Meanwhile, the anti-inflammatory evaluation was per...

  5. Systems Pharmacology Dissection of the Anti-Inflammatory Mechanism for the Medicinal Herb Folium Eriobotryae

    OpenAIRE

    Jingxiao Zhang; Yan Li; Su-Shing Chen; Lilei Zhang; Jinghui Wang; Yinfeng Yang; Shuwei Zhang; Yanqiu Pan; Yonghua Wang; Ling Yang

    2015-01-01

    Inflammation is a hallmark of many diseases like diabetes, cancers, atherosclerosis and arthritis. Thus, lots of concerns have been raised toward developing novel anti-inflammatory agents. Many alternative herbal medicines possess excellent anti-inflammatory properties, yet their precise mechanisms of action are yet to be elucidated. Here, a novel systems pharmacology approach based on a large number of chemical, biological and pharmacological data was developed and exemplified by a probe her...

  6. Antimicrobial, Antiparasitic, Anti-Inflammatory, and Cytotoxic Activities of Lopezia racemosa

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    Carla Cruz Paredes

    2013-01-01

    Full Text Available The present study investigates the potential benefits of the Mexican medicinal plant Lopezia racemosa (Onagraceae. Extracts and fractions from aerial parts of this plant were assessed to determine their antibacterial, antifungal, antiparasitic, anti-inflammatory and cytotoxic activities in vitro. Aerial parts of the plant were extracted with various solvents and fractionated accordingly. Extracts and fractions were tested against a panel of nine bacterial and four fungal species. The antiparasitic activity was tested against Leishmania donovani, whereas the anti-inflammatory activity of the compounds was determined by measuring the secretion of interleukin-6 from human-derived macrophages. The same macrophage cell line was used to investigate the cytotoxicity of the compounds. Various extracts and fractions showed antibacterial, antifungal, antiparasitic, and anti-inflammatory activities. The hexanic fraction HF 11-14b was the most interesting fraction with antimicrobial, and anti-inflammatory activities. The benefit of L. racemosa as a traditional medicinal plant was confirmed as shown by its antibacterial, antifungal and anti-inflammatory activities. To the best of our knowledge, this is the first study reporting the biological activities of L. racemosa, including antiparasitic and anti-inflammatory activities.

  7. [In vitro anti-inflammatory and free radical scavenging activities of flavans from Ilex centrochinensis].

    Science.gov (United States)

    Li, Lu-jun; Yu, Li-juan; Li, Yan-ci; Liu, Meng-yuan; Wu, Zheng-zhi

    2015-04-01

    This study was carried out to evaluate the anti-inflammatory and free radical scavenging activities of flavans from flex centrochinensis S. Y. Hu in vitro and their structure-activity relationship. LPS-stimulated RAW 264.7 macrophage was used as inflammatory model. MTT assay for cell availability, Griess reaction for nitric oxide (NO) production, the content of TNF-alpha, IL-1beta, IL-6 and PGE, were detected with ELISA kits; DPPH, superoxide anion and hydroxyl free radicals scavenging activities were also investigated. According to the result, all flavans tested exhibited anti-inflammatory effect in different levels. Among them, compounds 1, 3, 4 and 6 showed potent anti-inflammatory effect through the inhibition of NO, TNF-alpha, IL-lp and IL-6, of which 1 was the most effective inhibitor, however, 2 and 5 were relatively weak or inactive. The order of free radical scavenging activities was similar to that of anti-inflammatory activities. Therefore, these results suggest that 3, 4 and 6, especially of 1, were,in part responsible for the anti-inflammatory and free radical scavenging activity of Ilex centrochinensis. Hydroxyl group at 4'-position of B-ring plays an important role in the anti-inflammatory and free radical scavenging capacities. PMID:26281592

  8. Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs

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    Cristina Theoduloz

    2015-06-01

    Full Text Available The aim of the study was to assess changes in the activity of anti-inflammatory terpenes from Chilean medicinal plants after the formation of derivatives incorporating synthetic anti-inflammatory agents. Ten new hybrid molecules were synthesized combining terpenes (ferruginol (1, imbricatolic acid (2 and oleanolic acid (3 with ibuprofen (4 or naproxen (5. The topical anti-inflammatory activity of the compounds was assessed in mice by the arachidonic acid (AA and 12-O-tetradecanoyl phorbol 13-acetate (TPA induced ear edema assays. Basal cytotoxicity was determined towards human lung fibroblasts, gastric epithelial cells and hepatocytes. At 1.4 µmol/mouse, a strong anti-inflammatory effect in the TPA assay was observed for oleanoyl ibuprofenate 12 (79.9% and oleanoyl ibuprofenate methyl ester 15 (80.0%. In the AA assay, the best activity was observed for 12 at 3.2 µmol/mouse, with 56.8% reduction of inflammation, in the same range as nimesulide (48.9%. All the terpenyl-synthetic anti-inflammatory hybrids showed better effects in the TPA assay, with best activity for 6, 12 and 15. The cytotoxicity of the compounds 8 and 10 with a free COOH, was higher than that of 2. The derivatives from 3 were less toxic than the triterpene. Several of the new compounds presented better anti-inflammatory effect and lower cytotoxicity than the parent terpenes.

  9. In vitro antioxidant capacity and anti-inflammatory activity of seven common oats.

    Science.gov (United States)

    Chu, Yi-Fang; Wise, Mitchell L; Gulvady, Apeksha A; Chang, Tony; Kendra, David F; Jan-Willem van Klinken, B; Shi, Yuhui; O'Shea, Marianne

    2013-08-15

    Oats are gaining increasing scientific and public interest for their purported antioxidant-associated health benefits. Most reported studies focused on specific oat extracts or particular oat components, such as β-glucans, tocols (vitamin E), or avenanthramides. Studies on whole oats with respect to antioxidant and anti-inflammatory activities are still lacking. Here the antioxidant and anti-inflammatory activities from whole oat groats of seven common varieties were evaluated. All oat varieties had very similar oxygen radical absorption capacity compared with other whole grains. In an anti-inflammatory assay, oat variety CDC Dancer inhibited tumor necrosis factor-α induced nuclear factor-kappa B activation by 27.5% at 2 mg/ml, whereas variety Deiter showed 13.7% inhibition at a comparable dose. Avenanthramide levels did not correlate with the observed antioxidant and anti-inflammatory activities. Further investigations are needed to pinpoint the specific antioxidant and anti-inflammatory compounds, and potential synergistic and/or matrix effects that may help explain the mechanisms of oat's anti-inflammatory actions.

  10. Evaluation of anti-inflammatory activity of selected medicinal plants of Khyber Pakhtunkhwa, Pakistan.

    Science.gov (United States)

    Khuda, Fazli; Iqbal, Zafar; Khan, Ayub; Zakiullah; Shah, Yasar; Ahmad, Lateef; Nasir, Fazli; Hassan, Muhammad; Ismail; Shah, Waheed Ali

    2014-03-01

    In present study, the anti-inflammatory potential of three medicinal plants, Xanthium strumarium, Achyranthes aspera and Duchesnea indica were evaluated, using both in vitro and in vivo assays. Carrageenan induced hind paw edema model was used to carry out the in vivo anti-inflammatory activity, while for in vitro screening lipoxygenase inhibition assay was used. Crude extract of all the selected plants depicted significant (plt;0.001) anti-inflammatory activity, at late phase of inflammation. Achyranthes aspera also showed considerable anti-inflammatory activity (47%) at relatively lower concentration (200 mg/ml), at the initial phase of inflammation. Similarly the ethyl acetate fraction of all the selected plants showed significant lipoxygenase inhibition activity when compared with the standard drug (Baicalein). The results obtained from both in vitro and in vivo anti-inflammatory activity suggest that the ethyl acetate fraction of the crude extract of all the selected plants can be used for the isolation of new lead compounds with better anti-inflammatory activity. PMID:24577927

  11. Rose geranium essential oil as a source of new and safe anti-inflammatory drugs

    Science.gov (United States)

    Boukhatem, Mohamed Nadjib; Kameli, Abdelkrim; Ferhat, Mohamed Amine; Saidi, Fairouz; Mekarnia, Maamar

    2013-01-01

    Background Since the available anti-inflammatory drugs exert an extensive variety of side effects, the search for new anti-inflammatory agents has been a priority of pharmaceutical industries. Aims The aim of the present study was to assess the anti-inflammatory activities of the essential oil of rose geranium (RGEO). Methods The chemical composition of the RGEO was investigated by gas chromatography. The major components were citronellol (29.13%), geraniol (12.62%), and citronellyl formate (8.06%). In the carrageenan-induced paw edema, five different groups were established and RGEO was administered orally in three different doses. Results RGEO (100 mg/kg) was able to significantly reduce the paw edema with a comparable effect to that observed with diclofenac, the positive control. In addition, RGEO showed a potent anti-inflammatory activity by topical treatment in the method of croton oil-induced ear edema. When the dose was 5 or 10 µl of RGEO per ear, the inflammation was reduced by 73 and 88%, respectively. This is the first report to demonstrate a significant anti-inflammatory activity of Algerian RGEO. In addition, histological analysis confirmed that RGEO inhibited the inflammatory responses in the skin. Conclusion Our results indicate that RGEO may have significant potential for the development of novel anti-inflammatory drugs with improved safety profile. PMID:24103319

  12. Objective assessment of topical anti-inflammatory drug activity on experimentally induced nickel contact dermatitis: comparison between visual scoring, colorimetry, laser Doppler velocimetry and transepidermal water loss.

    Science.gov (United States)

    Queille-Roussel, C; Duteil, L; Padilla, J M; Poncet, M; Czernielewski, J

    1990-01-01

    Four topical anti-inflammatory drugs were investigated for their effect on allergic contact dermatitis. Nickel dermatitis was chosen for its high incidence in European healthy volunteers. Experimental lesions were treated twice daily with two steroids, two non-steroidal anti-inflammatory drugs and a blank base for 4.5 days without occlusion. The influence of treatments was assessed by daily visual grading and one site was left untreated for comparison over the same period. To quantify drug activities objectively, skin colour (colorimetry), skin blood flow (laser Doppler velocimetry) and transepidermal water loss (evaporimetry) were measured before drugs were first applied, then 6 hr after the last application. As expected, only Dermoval cream significantly improved the spontaneous clinical evolution in comparison with the other creams (Hydrocortisone Aster à 1%. Parfenac, indomethacin 2.5% and Skinbase) and the untreated site. Colorimetric parameter a* (redness) and L* (luminance) showed more differences between treatments than the other criteria and a close relationship was obtained between these two parameters and skin blood flow, all three being highly correlated to visual grading. Transepidermal water loss appeared less related to clinical improvement but this parameter could prove helpful for detecting compounds which could be irritant to diseased skin.

  13. EVALUATION OF ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF METHANOLIC EXTRACT OF COCCULUS HIRSUTUS LEAVES

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    G. Sarvankumar

    2011-12-01

    Full Text Available Inflammation and pain are the most common health problems treated with traditional remedies which mainly comprise medicinal plants. A number of natural products are used in the traditional medical systems in many countries. An alternative medicine for the treatment of various diseases is getting more popular. Many medicinal plants provide relief of symptoms comparable to that of obtained from allopathic medicines. Therefore agents of natural origin with very little side effects are required as substitute chemicals therapeutics. The methanolic leaf extract of Cocculus hirsutus (100& 200mg/kg Linn (Menispermaceae was investigated for its analgesic and anti-inflammatory effects in laboratory animals. The analgesic activity of the methanolic leaf extract of Cocculus hirsutus was investigated by eddy’s hot plate model and acetic acid induced writhing in mice. Anti-inflammatory activity of Cocculus hirsutus was studied by both in-vitro and in vivo models. Human red blood cells membrane stabilization method was adopted for the in-vitro anti-inflammatory activity and for in-vivo, Carrageenan induced paw edema and cotton pellet induced granuloma in rats was employed. In eddy’s hot plate analgesic study, both the doses of Cocculus hirsutus showed significant (p<0.05 and p<0.01 respectively analgesic activity. In acetic acid induced writhing model, the onset of writhing was delayed and duration of writhing was shortened by the methanolic extract of Cocculus hirsutus.In-vitro anti-inflammatory activity of the methanolic leaf extract of Cocculus hirsutus showed significant anti inflammatory activity in a concentration dependent manner. Cocculus hirsutus showed significant anti-inflammatory activity on both carrgeenan as well as cotton pellet induced granuloma models in rats. From the results, it was concluded that the methanolic leaf extract of Cocculus hirsutus possess analgesic and anti-inflammatory.

  14. Steroid ulcers:Any news?

    Institute of Scientific and Technical Information of China (English)

    Mario; Guslandi

    2013-01-01

    Steroid ulcers,although a common feature in experimental studies,seldom develop in clinical practice,as observed by the meta-analyses carried out in the 90s.Corticosteroids alone become ulcerogenic only if treatment lasts longer than one month and the total administered dose exceeds 1000 mg.On the other hand concomitant intake of non-steroidal anti-inflammatory drugs results in a synergistic,highly damaging effect on the gastroduodenal mucosa.Thus,despite the survival of the steroid ulcer myth in the medical culture,pharmacological protection against steroid-induced peptic ulcers is a rare necessity while the best prophylactic strategy still remains to be determined.

  15. Anti-inflammatory and antinociceptive activities of methanolic extract from red seaweed Dichotomaria obtusata

    Directory of Open Access Journals (Sweden)

    Neivys García Delgado

    2013-03-01

    Full Text Available The aim of the present work was to investigate the anti-inflammatory and antinociceptive effects of methanolic extract from D. obtusata using classic models in mice (croton oil-induced ear edema and acetic acid-induced writhing and a phospholipase A2 activity test. Qualitative analysis of the chemical composition of seaweed was also determined by extraction with solvents of increasing polarity and precipitation and color tests. Results of qualitative chemical study showed the presence of lactonic and phenolic compounds, reduced carbohydrates, other sugars, flavonoids, fatty compounds, triterpenes and steroids. The extract inhibited mouse ear edema in a dose-dependent manner with an efficacy higher than 90% and a mean effective dose of 4.87µg/ear, while intraperitoneal administration presented a moderate activity. The extract did not inhibit phospholipase A2 activity. In the writhing test, the intraperitoneal administration of the extract showed a strong antinociceptive activity (80.2%, while the oral route showed a lower efficacy. In conclusion, this study demonstrated the anti-inflammatory and antinociceptive effects of methanol extract of D. obtusata in experimental models, suggesting its therapeutic potential in the treatment of peripheral painful and/or inflammatory pathologies.O objetivo do presente trabalho foi investigar os efeitos antiinflamatórios e antinociceptivos de um extrato metanólico de D. obtusata, utilizando modelos clássicos em ratos (teste do edema de orelha induzido por óleo de cróton e teste de contorções induzidas por ácido acético e um teste de atividade de fosfolipase A2. A análise qualitativa da composição química das algas foi também determinada através de extração com solventes de polaridade crescente e testes de precipitação e cor. Os resultados do estudo de química qualitativa mostraram a presença de compostos lactônicos e fenólicos, hidratos de carbono reduzidos e outros a

  16. Enhancement of Anti-Inflammatory Activity of Curcumin Using Phosphatidylserine-Containing Nanoparticles in Cultured Macrophages

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    Ji Wang

    2016-06-01

    Full Text Available Macrophages are one kind of innate immune cells, and produce a variety of inflammatory cytokines in response to various stimuli, such as oxidized low density lipoprotein found in the pathogenesis of atherosclerosis. In this study, the effect of phosphatidylserine on anti-inflammatory activity of curcumin-loaded nanostructured lipid carriers was investigated using macrophage cultures. Different amounts of phosphatidylserine were used in the preparation of curcumin nanoparticles, their physicochemical properties and biocompatibilities were then compared. Cellular uptake of the nanoparticles was investigated using a confocal laser scanning microscope and flow cytometry analysis in order to determine the optimal phosphatidylserine concentration. In vitro anti-inflammatory activities were evaluated in macrophages to test whether curcumin and phosphatidylserine have interactive effects on macrophage lipid uptake behavior and anti-inflammatory responses. Here, we showed that macrophage uptake of phosphatidylserine-containing nanostructured lipid carriers increased with increasing amount of phosphatidylserine in the range of 0%–8%, and decreased when the phosphatidylserine molar ratio reached over 12%. curcumin-loaded nanostructured lipid carriers significantly inhibited lipid accumulation and pro-inflammatory factor production in cultured macrophages, and evidently promoted release of anti-inflammatory cytokines, when compared with curcumin or phosphatidylserine alone. These results suggest that the delivery system using PS-based nanoparticles has great potential for efficient delivery of drugs such as curcumin, specifically targeting macrophages and modulation of their anti-inflammatory functions.

  17. Pro- and Anti-Inflammatory Cytokines Release in Mice Injected with Crotalus durissus terrificus Venom

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    A. Hernández Cruz

    2008-01-01

    Full Text Available The effects of Crotalus durissus terrificus venom (Cdt were analyzed with respect to the susceptibility and the inflammatory mediators in an experimental model of severe envenomation. BALB/c female mice injected intraperitoneally presented sensibility to Cdt, with changes in specific signs, blood biochemical and inflammatory mediators. The venom induced reduction of glucose and urea levels and an increment of creatinine levels in serum from mice. Significant differences were observed in the time-course of mediator levels in sera from mice injected with Cdt. The maximum levels of IL-6, NO, IL-5, TNF, IL-4 and IL-10 were observed 15 min, 30 min, 1, 2 and 4 hours post-injection, respectively. No difference was observed for levels of IFN-γ. Taken together, these data indicate that the envenomation by Cdt is regulated both pro- and anti-inflammatory cytokine responses at time-dependent manner. In serum from mice injected with Cdt at the two first hours revealed of pro-inflammatory dominance. However, with an increment of time an increase of anti-inflammatory cytokines was observed and the balance toward to anti-inflammatory dominance. In conclusion, the observation that Cdt affects the production of pro- and anti-inflammatory cytokines provides further evidence for the role played by Cdt in modulating pro/anti-inflammatory cytokine balance.

  18. A Systematic Review for Anti-Inflammatory Property of Clusiaceae Family: A Preclinical Approach

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    Mônica Santos de Melo

    2014-01-01

    Full Text Available Background. Clusiaceae family (sensu lato is extensively used in ethnomedicine for treating a number of disease conditions which include cancer, inflammation, and infection. The aim of this review is to report the pharmacological potential of plants of Clusiaceae family with the anti-inflammatory activity in animal experiments. Methods. A systematic review about experiments investigating anti-inflammatory activity of Clusiaceae family was carried out by searching bibliographic databases such as Medline, Scopus and Embase. In this update, the search terms were “anti-inflammatory agents,” “Clusiaceae,” and “animals, laboratory.” Results. A total of 255 publications with plants this family were identified. From the initial 255 studies, a total of 21 studies were selected for the final analysis. Studies with genera Allanblackia, Clusia, Garcinia or Rheedia, and Hypericum showed significant anti-inflammatory activity. The findings include a decrease of total leukocytes, a number of neutrophils, total protein concentration, granuloma formation, and paw or ear edema formation. Other interesting findings included decreased of the MPO activity, and inflammatory mediators such as NF-κB and iNOS expression, PGE2 and Il-1β levels and a decrease in chronic inflammation. Conclusion. The data reported suggests the anti-inflammatory effect potential of Clusiaceae family in animal experiments.

  19. Evaluation of anti-inflammatory activity of some Libyan medicinal plants in experimental animals

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    Nahar Lutfun

    2012-01-01

    Full Text Available Ballota pseudodictamnus (L. Benth. (Lamiaceae, Salvia fruticosa Mill. (Lamiaceae and Thapsia garganica L. (Apiaceae are three well-known medicinal plants from the Libyan flora, which have long been used for the treatment of inflammations. The aim of the present study was to investigate, for the first time, the anti-inflammatory property of the methanol (MeOH extracts of the aerial parts of these plants. Shade-dried and ground aerial parts of B. pseudodictamnus, S. fruticosa and T. garganica were Soxhlet-extracted with MeOH. The extracts were concentrated by evaporation under reduced pressure at 40°C. The anti-inflammatory activity of the extracts was evaluated using the carrageenan-induced mice paw edema model. The administration of the extracts at a dose of 500 mg/kg body weight produced statistically significant inhibition (p < 0.05 of edema within 3 h of carrageenan administration. The results demonstrated significant anti-inflammatory properties of the test extracts. Among the extracts, the S. fruticosa extract exhibited the most significant inhibition of inflammation after 3 h (62.1%. Thus, S. fruticosa could be a potential source for the discovery and development of newer anti-inflammatory ‘leads’ for drug development. The anti-inflammatory activity of B. pseudodictamnus and S. fruticosa could be assumed to be related to high levels of phenolic compounds, e.g., flavonoids, present in these plants.

  20. Anti-inflammatory and analgesic activities of acetophenone semicarbazone and benzophenone semicarbazone

    Institute of Scientific and Technical Information of China (English)

    Shaikh M Mohsin Ali; Mele Jesmin; M Abul Kalam Azad; M Khairul Islam; Ronok Zahan

    2012-01-01

    Objective: To study anti-inflammatory and analgesic activities in swiss albino mice, two schiff bases namely acetophenone semicarbazone (ASC) and benzophenone semicarbazone (BSC) were synthesized and characterized. Methods: Two doses of the test compounds 25 and 50 mg/kg (p.o) for each were selected throughout the research work. The anti-inflammatory activity of the test compounds was determined by ‘carragenan induced mice paw edema inhibition’ method. The analgesic activity was determined by both, ‘acetic acid induced writhing’ and ‘tail immersion' methods. All such data were compared with standard drugs at the dose of 10 mg/kg (p.o.). Results:Both ASC and BSC have showed positive effects as anti-inflammatory and analgesic agents. Anti-inflammatory and analgesic activities of the test compounds at 50 mg/kg (p.o.) were quite comparable to those of standard drugs at 10 mg/kg (p.o.). Conclusion: Both ASC and BSC can be considered as potent anti-inflammatory and analgesic agents.

  1. Anti-Inflammatory Properties and Chemical Characterization of the Essential Oils of Four Citrus Species.

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    Jorge Luis Amorim

    Full Text Available Citrus fruits have potential health-promoting properties and their essential oils have long been used in several applications. Due to biological effects described to some citrus species in this study our objectives were to analyze and compare the phytochemical composition and evaluate the anti-inflammatory effect of essential oils (EO obtained from four different Citrus species. Mice were treated with EO obtained from C. limon, C. latifolia, C. aurantifolia or C. limonia (10 to 100 mg/kg, p.o. and their anti-inflammatory effects were evaluated in chemical induced inflammation (formalin-induced licking response and carrageenan-induced inflammation in the subcutaneous air pouch model. A possible antinociceptive effect was evaluated in the hot plate model. Phytochemical analyses indicated the presence of geranial, limonene, γ-terpinene and others. EOs from C. limon, C. aurantifolia and C. limonia exhibited anti-inflammatory effects by reducing cell migration, cytokine production and protein extravasation induced by carrageenan. These effects were also obtained with similar amounts of pure limonene. It was also observed that C. aurantifolia induced myelotoxicity in mice. Anti-inflammatory effect of C. limon and C. limonia is probably due to their large quantities of limonene, while the myelotoxicity observed with C. aurantifolia is most likely due to the high concentration of citral. Our results indicate that these EOs from C. limon, C. aurantifolia and C. limonia have a significant anti-inflammatory effect; however, care should be taken with C. aurantifolia.

  2. Anti-Inflammatory Properties and Chemical Characterization of the Essential Oils of Four Citrus Species.

    Science.gov (United States)

    Amorim, Jorge Luis; Simas, Daniel Luiz Reis; Pinheiro, Mariana Martins Gomes; Moreno, Daniela Sales Alviano; Alviano, Celuta Sales; da Silva, Antonio Jorge Ribeiro; Fernandes, Patricia Dias

    2016-01-01

    Citrus fruits have potential health-promoting properties and their essential oils have long been used in several applications. Due to biological effects described to some citrus species in this study our objectives were to analyze and compare the phytochemical composition and evaluate the anti-inflammatory effect of essential oils (EO) obtained from four different Citrus species. Mice were treated with EO obtained from C. limon, C. latifolia, C. aurantifolia or C. limonia (10 to 100 mg/kg, p.o.) and their anti-inflammatory effects were evaluated in chemical induced inflammation (formalin-induced licking response) and carrageenan-induced inflammation in the subcutaneous air pouch model. A possible antinociceptive effect was evaluated in the hot plate model. Phytochemical analyses indicated the presence of geranial, limonene, γ-terpinene and others. EOs from C. limon, C. aurantifolia and C. limonia exhibited anti-inflammatory effects by reducing cell migration, cytokine production and protein extravasation induced by carrageenan. These effects were also obtained with similar amounts of pure limonene. It was also observed that C. aurantifolia induced myelotoxicity in mice. Anti-inflammatory effect of C. limon and C. limonia is probably due to their large quantities of limonene, while the myelotoxicity observed with C. aurantifolia is most likely due to the high concentration of citral. Our results indicate that these EOs from C. limon, C. aurantifolia and C. limonia have a significant anti-inflammatory effect; however, care should be taken with C. aurantifolia.

  3. Anti-Inflammatory and Antioxidant Activities of Salvia fruticosa: An HPLC Determination of Phenolic Contents.

    Science.gov (United States)

    Boukhary, Rima; Raafat, Karim; Ghoneim, Asser I; Aboul-Ela, Maha; El-Lakany, Abdalla

    2016-01-01

    Objectives. Salvia fruticosa Mill. (S. fruticosa) is widely used in folk medicine. Accordingly, the present study was designed to evaluate the antioxidant and anti-inflammatory activities of S. fruticosa, and to determine the phenolic constituents of its extracts. Methods. The antioxidant activity was determined using 2,2-diphenylpicrylhydrazyl assay. Total phenolic contents were estimated using Folin-Ciocalteu reagent, and high-performance liquid chromatography was performed to identify phenolic constituents. To evaluate the anti-inflammatory activity, carrageenan-induced mouse paw edema was determined plethysmographically. Key Findings. Different plant extracts demonstrated strong radical scavenging activity, where the ethyl acetate extract had the highest value in the roots and the lowest in the aerial parts. This antioxidant activity was correlated to the total phenolic content of different extracts, where rutin and luteolin were the most abundant constituents. Interestingly, both the roots and aerial parts revealed a significant anti-inflammatory activity comparable to diclofenac. Conclusions. This study is the first to demonstrate pharmacologic evidence of the potential anti-inflammatory activity of S. fruticosa. This activity may partly be due to the radical scavenging effects of its polyphenolic contents. These findings warrant the popular use of the East Mediterranean sage and highlight the potential of its active constituents in the development of new anti-inflammatory drugs.

  4. Systems pharmacology dissection of the anti-inflammatory mechanism for the medicinal herb Folium eriobotryae.

    Science.gov (United States)

    Zhang, Jingxiao; Li, Yan; Chen, Su-Shing; Zhang, Lilei; Wang, Jinghui; Yang, Yinfeng; Zhang, Shuwei; Pan, Yanqiu; Wang, Yonghua; Yang, Ling

    2015-01-28

    Inflammation is a hallmark of many diseases like diabetes, cancers, atherosclerosis and arthritis. Thus, lots of concerns have been raised toward developing novel anti-inflammatory agents. Many alternative herbal medicines possess excellent anti-inflammatory properties, yet their precise mechanisms of action are yet to be elucidated. Here, a novel systems pharmacology approach based on a large number of chemical, biological and pharmacological data was developed and exemplified by a probe herb Folium Eriobotryae, a widely used clinical anti-inflammatory botanic drug. The results show that 11 ingredients of this herb with favorable pharmacokinetic properties are predicted as active compounds for anti-inflammatory treatment. In addition, via systematic network analyses, their targets are identified to be 43 inflammation-associated proteins including especially COX2, ALOX5, PPARG, TNF and RELA that are mainly involved in the mitogen-activated protein kinase (MAPK) signaling pathway, the rheumatoid arthritis pathway and NF-κB signaling pathway. All these demonstrate that the integrated systems pharmacology method provides not only an effective tool to illustrate the anti-inflammatory mechanisms of herbs, but also a new systems-based approach for drug discovery from, but not limited to, herbs, especially when combined with further experimental validations.

  5. Systems Pharmacology Dissection of the Anti-Inflammatory Mechanism for the Medicinal Herb Folium Eriobotryae

    Directory of Open Access Journals (Sweden)

    Jingxiao Zhang

    2015-01-01

    Full Text Available Inflammation is a hallmark of many diseases like diabetes, cancers, atherosclerosis and arthritis. Thus, lots of concerns have been raised toward developing novel anti-inflammatory agents. Many alternative herbal medicines possess excellent anti-inflammatory properties, yet their precise mechanisms of action are yet to be elucidated. Here, a novel systems pharmacology approach based on a large number of chemical, biological and pharmacological data was developed and exemplified by a probe herb Folium Eriobotryae, a widely used clinical anti-inflammatory botanic drug. The results show that 11 ingredients of this herb with favorable pharmacokinetic properties are predicted as active compounds for anti-inflammatory treatment. In addition, via systematic network analyses, their targets are identified to be 43 inflammation-associated proteins including especially COX2, ALOX5, PPARG, TNF and RELA that are mainly involved in the mitogen-activated protein kinase (MAPK signaling pathway, the rheumatoid arthritis pathway and NF-κB signaling pathway. All these demonstrate that the integrated systems pharmacology method provides not only an effective tool to illustrate the anti-inflammatory mechanisms of herbs, but also a new systems-based approach for drug discovery from, but not limited to, herbs, especially when combined with further experimental validations.

  6. Systems pharmacology dissection of the anti-inflammatory mechanism for the medicinal herb Folium eriobotryae.

    Science.gov (United States)

    Zhang, Jingxiao; Li, Yan; Chen, Su-Shing; Zhang, Lilei; Wang, Jinghui; Yang, Yinfeng; Zhang, Shuwei; Pan, Yanqiu; Wang, Yonghua; Yang, Ling

    2015-01-01

    Inflammation is a hallmark of many diseases like diabetes, cancers, atherosclerosis and arthritis. Thus, lots of concerns have been raised toward developing novel anti-inflammatory agents. Many alternative herbal medicines possess excellent anti-inflammatory properties, yet their precise mechanisms of action are yet to be elucidated. Here, a novel systems pharmacology approach based on a large number of chemical, biological and pharmacological data was developed and exemplified by a probe herb Folium Eriobotryae, a widely used clinical anti-inflammatory botanic drug. The results show that 11 ingredients of this herb with favorable pharmacokinetic properties are predicted as active compounds for anti-inflammatory treatment. In addition, via systematic network analyses, their targets are identified to be 43 inflammation-associated proteins including especially COX2, ALOX5, PPARG, TNF and RELA that are mainly involved in the mitogen-activated protein kinase (MAPK) signaling pathway, the rheumatoid arthritis pathway and NF-κB signaling pathway. All these demonstrate that the integrated systems pharmacology method provides not only an effective tool to illustrate the anti-inflammatory mechanisms of herbs, but also a new systems-based approach for drug discovery from, but not limited to, herbs, especially when combined with further experimental validations. PMID:25636035

  7. Anti-inflammatory effects of five commercially available mushroom species determined in lipopolysaccharide and interferon-γ activated murine macrophages.

    Science.gov (United States)

    Gunawardena, Dhanushka; Bennett, Louise; Shanmugam, Kirubakaran; King, Kerryn; Williams, Roderick; Zabaras, Dimitrios; Head, Richard; Ooi, Lezanne; Gyengesi, Erika; Münch, Gerald

    2014-04-01

    Inflammation is a well-known contributing factor to many age-related chronic diseases. One of the possible strategies to suppress inflammation is the employment of functional foods with anti-inflammatory properties. Edible mushrooms are attracting more and more attention as functional foods since they are rich in bioactive compounds, but their anti-inflammatory properties and the effect of food processing steps on this activity has not been systematically investigated. In the present study, White Button and Honey Brown (both Agaricus bisporus), Shiitake (Lentinus edodes), Enoki (Flammulina velutipes) and Oyster mushroom (Pleurotus ostreatus) preparations were tested for their anti-inflammatory activity in lipopolysaccharide (LPS) and interferon-γ (IFN-γ) activated murine RAW 264.7 macrophages. Potent anti-inflammatory activity (IC₅₀portion of the anti-inflammatory activity was lost suggesting that the anti-inflammatory compounds might be susceptible to heating or prone to evaporation. PMID:24262531

  8. HE3286, an oral synthetic steroid, treats lung inflammation in mice without immune suppression.

    NARCIS (Netherlands)

    Conrad, D.; Wang, A.; Pieters, R.; Nicoletti, F.; Mangano, K.; van Heeckeren, A.; White, S.K.; Frincke, J.; Reading, C.L.; Stickney, D.; Auci, D.L.

    2010-01-01

    ABSTRACT: BACKGROUND: 17α-Ethynyl-5-androsten-3β, 7β, 17β-triol (HE3286) is a synthetic derivative of an endogenous steroid androstenetriol (β-AET), a metabolite of the abundant adrenal steroid deyhdroepiandrosterone (DHEA), with broad anti-inflammatory activities. We tested the ability of this nove

  9. Screening for anti-inflammatory components from Corydalis bungeana Turcz. based on macrophage binding combined with HPLC

    OpenAIRE

    Dong, Zi-Bo; Zhang, Yong-Hong; Zhao, Bing-Jie; Li, Chao; Tian, Gang; Niu, Ben; Qi, Hong; Feng, Liang; Shao, Jian-Guo

    2015-01-01

    Background Corydalis bungeana Turcz. (CB; family: Corydalis DC.) is an anti-inflammatory medicinal herb used widely in traditional Chinese medicine (TCM) for upper respiratory tract infection, etc., but its anti-inflammatory active molecules are unknown. This study was designed to screen for the anti-inflammatory components from CB based on macrophage binding combined with HPLC. Methods Xylene-induced ear edema in mouse and carrageenan-induced hind-paw edema in rats were used to evaluate the ...

  10. Inhaled Steroids

    Science.gov (United States)

    ... Medications > Long-Term Control Medications > Inhaled Steroids Inhaled Steroids What are some common inhaled steroids? How are ... more about steroids? What are some common inhaled steroids? Common inhaled steroids include: Asmanex ® (mometasone) Alvesco ® (ciclesonide) ...

  11. Anti Bacterial and Anti Inflammatory efficacy of Zingiber officinale and Decalepis hamiltonii ? In Vitro Study

    Directory of Open Access Journals (Sweden)

    Arun kumar M

    2014-09-01

    Full Text Available Aim: To evaluate the in vitro anti bacterial and anti inflammatory potential of Zingiber Officinale and Decalepis Hamiltonii against E. faecalis. Materials and Methods: Ethanolic extract of Zingiber and Decalepis was subjected to microbiological assay to determine its Maximum zone of inhibition using Agar disk diffusion test, minimum inhibitory concentration using serial broth dilution method and anti inflammatory potential using protein denaturation assay against E. faecalis. Results: Ethanolic extract of Zingiber and Decalepis showed: (a Maximum zone of inhibition of 20 mm and 24 mm respectively, (b MIC of 5% and 2.5%respectively, (C Protein denaturation assay value (IC50 of 115 and 80 respectively. Conclusion: Ethanolic extract of Zingiber and Decalepis was found to possess both anti bacterial and anti-inflammatory potential against E. faecalis.

  12. Optimization on Extraction Engineering of the Anti - inflammatory Bioactive Materials from Ainsliaea Fragrans Champ

    Directory of Open Access Journals (Sweden)

    Yang Jie

    2016-01-01

    Full Text Available Ainsliaea fragrans Champ.(A.fragrans is a traditional Chinese herbal, phenolic compounds was the major anti - inflammatory bioactive constituents. To improve the bioavailability and enhanced the curative effect of A.fragrans, the anti - inflammatory effect of phenolic acids and the “non-active” group of control vectors constitute a new biomedical material, which is of great significance to the treatment of diseases inflammation. Hence, in this thesis, regarding the total phenolic acid transfer rate as the indicator, L9(34 orthogonal design was used to optimize the extraction process of total Phenolic acid from A.fragrans by reflux extraction method on solvent dosage, extraction times and extraction time.The optimal extraction technology was as follows: 15 times of water volume, reflux extraction 3 times, extraction time 60 min. The result of pharmacological activity indicated anti-inflammatory effect: 95% ethanol extraction > water extraction > 30% ethanol extraction > 60% ethanol extraction.

  13. Effect of Anti-inflammatory Treatment on Depression, Depressive Symptoms, and Adverse Effects

    DEFF Research Database (Denmark)

    Köhler, Ole; Benros, Michael E; Nordentoft, Merete;

    2014-01-01

    IMPORTANCE: Several studies have reported antidepressant effects of anti-inflammatory treatment; however, the results have been conflicting and detrimental adverse effects may contraindicate the use of anti-inflammatory agents. OBJECTIVE: To systematically review the antidepressant and possible......) and odds ratios (ORs) were calculated. MAIN OUTCOMES AND MEASURES: Depression scores after treatment and adverse effects. RESULTS: Ten publications reporting on 14 trials (6262 participants) were included: 10 trials evaluated the use of nonsteroidal anti-inflammatory drugs (NSAIDs) (n=4,258) and 4...... properties of the selective cyclooxygenase 2 inhibitor celecoxib (SMD, -0.29; 95% CI, -0.49 to -0.08; I2=73%) on remission (OR, 7.89; 95% CI, 2.94 to 21.17; I2=0%) and response (OR, 6.59; 95% CI, 2.24 to 19.42; I2=0%). Among the 6 studies reporting on adverse effects, we found no evidence of an increased...

  14. Intravital Microscopic Methods to Evaluate Anti-inflammatory Effects and Signaling Mechanisms Evoked by Hydrogen Sulfide

    Science.gov (United States)

    Zuidema, Mozow Y.; Korthuis, Ronald J.

    2016-01-01

    Hydrogen sulfide (H2S) is an endogenous gaseous signaling molecule with potent anti-inflammatory properties. Exogenous application of H2S donors, administered either acutely during an inflammatory response or as an antecedent preconditioning intervention that invokes the activation of anti-inflammatory cell survival programs, effectively limits leukocyte rolling, adhesion and emigration, generation of reactive oxygen species, chemokine and cell adhesion molecule expression, endothelial barrier disruption,capillary perfusion deficits, and parenchymal cell dysfunction and injury. This chapter focuses on intravital microscopic methods that can be used to assess the anti-inflammatory effects exerted by H2S, as well as to explore the cellular signaling mechanisms by which this gaseous molecule limits the aforementioned inflammatory responses. Recent advances include use of intravital multiphoton microscopy and optical biosensor technology to explore signaling mechanisms in vivo. PMID:25747477

  15. Anti-inflammatory, analgesic, and antipyretic activities of virgin coconut oil.

    Science.gov (United States)

    Intahphuak, S; Khonsung, P; Panthong, A

    2010-02-01

    This study investigated some pharmacological properties of virgin coconut oil (VCO), the natural pure oil from coconut [Cocos nucifera Linn (Palmae)] milk, which was prepared without using chemical or high-heat treatment. The anti-inflammatory, analgesic, and antipyretic effects of VCO were assessed. In acute inflammatory models, VCO showed moderate anti-inflammatory effects on ethyl phenylpropiolate-induced ear edema in rats, and carrageenin- and arachidonic acid-induced paw edema. VCO exhibited an inhibitory effect on chronic inflammation by reducing the transudative weight, granuloma formation, and serum alkaline phosphatase activity. VCO also showed a moderate analgesic effect on the acetic acid-induced writhing response as well as an antipyretic effect in yeast-induced hyperthermia. The results obtained suggest anti-inflammatory, analgesic, and antipyretic properties of VCO.

  16. Synthesis and anti-inflammatory activity of some potential cyclic phenothiazines.

    Science.gov (United States)

    Kumar, A; Ram, T; Tyagi, R; Goel, B; Bansal, E; Srivastava, V K

    1998-05-01

    Some new schiff's bases (IVa-IVe), thiazolidinones (Va-Ve), delta 2-triazolines (VIa-VIe) and formazans (VIIa-VIIe) of 2-chlorophenothiazine have been synthesized and screened against Carrageenin induced oedema in albino rats. Some compounds of the series have shown promising activity. The most active compound is 2-chloro-10[5-(2-fluorophenyl-2-oxo-4 thiazolidin-1-yl)-amino acetyl] phenothiazine was found to be most potent. This compound (Vb) was further evaluated in detail and compared with phenylbutazone for its relative anti inflammatory potency (ED50), ulcerogenic liabilities (UD50) and acute toxicity (ALD50). It was found to be almost comparable to phenylbutazone as regards anti-inflammatory activity was concerned but and minimum ulcerogenic liability and cardiovascular effects. Hence, it seems promising as an anti-inflammatory agent in our preliminary studies. PMID:9689901

  17. Phytochemical analysis, antioxidant and anti-inflammatory activity of calyces from Physalis peruviana.

    Science.gov (United States)

    Toro, Reina M; Aragón, Diana M; Ospina, Luis F; Ramos, Freddy A; Castellanos, Leonardo

    2014-11-01

    Physalis peruviana calyces are used extensively in folk medicine. The crude ethanolic extract and some fractions of calyces were evaluated in order to explore antioxidant and anti-inflammatory activities. The anti-inflammatory activity was evaluated by the TPA-induced ear edema model. The antioxidant in vitro activity was measured by means of the superoxide and nitric oxide scavenging activity of the extracts and fractions. The butanolic fraction was found to be promising due to its anti-inflammatory and antioxidant activities. Therefore, a bio-assay guided approach was employed to isolate and identify rutin (1) and nicotoflorin (2) from their NMR spectroscopic and MS data. The identification of rutin in calyces of P. peruviana supports the possible use of this waste material for phytotherapeutic, nutraceutical and cosmetic preparations. PMID:25532284

  18. Study of Analgesic and Anti-inflammatory Effects of Lappaconitine Gelata

    Institute of Scientific and Technical Information of China (English)

    WANG Ying-zi; XIAO YONG-qing; ZHANG Chao; SUN Xiu-mei

    2009-01-01

    Objective:To explore the analgesic and anti-inflammatory effects of lappaconitine gelata (LA). Methods:The writhing response induced by acetic acid, the pain response induced by formaldehyde and hot plate method in the mouse, and the paw edema induced by egg albumen in the rat and the ear edema induced by xylene in the mouse were used for investigation on the analgesic and anti-inflammatory effects of LA.Results: The writhing response induced by acetic acid, the pain response induced by formaldehyde and hot plate methods was significantly inhibited by LA. In addition, the paw edema induced by egg albumen in the rat and the ear edema induced by xylene in the mouse were all significantly suppressed by LA. Conclusion:LA has the analgesic and anti-inflammatory effects.

  19. Anti-inflammatory activity of the apolar extract from the seaweed Galaxaura marginata (Rhodophyta, Nemaliales

    Directory of Open Access Journals (Sweden)

    E. Rozas

    2007-01-01

    Full Text Available The red seaweed Galaxaura marginata (Ellis & Solander Lamouroux, well known by the antibacterial activity of its polar extract and the cytotoxic activity of its oxygenated desmosterol, showed anti-inflammatory action in its apolar fraction. Topical anti-inflammatory activity was observed in samples collected at São Sebastião channel, northern littoral of São Paulo State, Brazil. The apolar extract and its fractions obtained through Thin-Layer Chromatography (TLC reduced the topical inflammation produced by croton oil in mouse ear. Such data indicated that the apolar extract from the marine red alga G. marginata displayed anti-inflammatory activity (since 1mg/ear extract reduced 95±0.5% inflammation, which could be the result of the synergic activity of the four fractions present in the apolar extract.

  20. Use of nonsteroidal anti-inflammatory drugs among healthy people and specific cerebrovascular safety

    DEFF Research Database (Denmark)

    Fosbøl, Emil L; Olsen, Anne-Marie Schjerning; Olesen, Jonas Bjerring;

    2014-01-01

    stroke). RESULTS: We selected 1,028,437 healthy individuals (median age 39 years). At least one nonsteroidal anti-inflammatory drug was claimed by 44·7% of the study population, and the drugs were generally used for a short period of time and in low doses. High-dose ibuprofen and diclofenac were......BACKGROUND: Nonsteroidal anti-inflammatory drugs can increase bleeding and thrombosis, but little is known about the cerebrovascular safety of these drugs, especially among healthy people. AIMS: The aim of this study was to examine the risk of ischemic and hemorrhagic stroke associated with the use...... of nonsteroidal anti-inflammatory drugs in healthy people. METHODS: By individual-level linkage of nationwide administrative registers in Denmark, information on hospital admissions, prescription claims, vital status, and cause of death were obtained. A cohort of healthy people without hospital admissions...

  1. EVALUATION OF ANTI INFLAMMATORY ACTIVITY OF GARCINIA INDICA FRUIT RIND EXTRACTS IN WISTAR RATS

    Directory of Open Access Journals (Sweden)

    Khatib N.A

    2010-12-01

    Full Text Available Garcinia indica choisy (Kokum is known for its food, medicinal and commercial values. The present study was carried out to evaluate the effect of aqueous and ethanolic extract of Garcinia indica fruit rind (GIFR for its anti inflammatory activity in rats. The inflammation was induced by carrageenan induced paw odema. The serum enzymes like Acid phoshatase(ACP and Alkaline Phosphatase(ALP were estimated. Both extracts at dose (200 & 400 mg/kg p.o single dose shows significant (P<0.001 anti inflammatory activity in (Carrageenan induced paw odema acute inflammation. The extracts treatment also showed significant (p<0.001 reduction in the levels of serum enzymes ACP & ALP. Similar results were obtained from aspirin (200mg/kg treated group. The result obtained from the present study indicates both aqueous and ethanolic extracts possessing anti inflammatory activity and further study required to establish its mechanism of action.

  2. Exploitation of the nicotinic anti-inflammatory pathway for the treatment of epithelial inflammatory diseases

    Institute of Scientific and Technical Information of China (English)

    David A Scott; Michael Martin

    2006-01-01

    Discoveries in the first few years of the 21st century have led to an understanding of important interactions between the nervous system and the inflammatory response at the molecular level, most notably the acetylcholine (ACh)-triggered, α7-nicotinic acetylcholine receptor (α7nAChR)-dependent nicotinic anti-inflammatory pathway. Studies using the α7nAChR agonist, nicotine, for the treatment of mucosal inflammation have been undertaken but the efficacy of nicotine as a treatment for inflammatory bowel diseases remains debatable. Further understanding of the nicotinic anti-inflammatory pathway and other endogenous anti-inflammatory mechanisms is required in order to develop refined and specific therapeutic strategies for the treatment of a number of inflammatory diseases and conditions, including periodontitis, psoriasis,sarcoidosis, and ulcerative colitis.

  3. Anti-Inflammatory Effects of GLP-1-Based Therapies beyond Glucose Control

    Directory of Open Access Journals (Sweden)

    Young-Sun Lee

    2016-01-01

    Full Text Available Glucagon-like peptide-1 (GLP-1 is an incretin hormone mainly secreted from intestinal L cells in response to nutrient ingestion. GLP-1 has beneficial effects for glucose homeostasis by stimulating insulin secretion from pancreatic beta-cells, delaying gastric emptying, decreasing plasma glucagon, reducing food intake, and stimulating glucose disposal. Therefore, GLP-1-based therapies such as GLP-1 receptor agonists and inhibitors of dipeptidyl peptidase-4, which is a GLP-1 inactivating enzyme, have been developed for treatment of type 2 diabetes. In addition to glucose-lowering effects, emerging data suggests that GLP-1-based therapies also show anti-inflammatory effects in chronic inflammatory diseases including type 1 and 2 diabetes, atherosclerosis, neurodegenerative disorders, nonalcoholic steatohepatitis, diabetic nephropathy, asthma, and psoriasis. This review outlines the anti-inflammatory actions of GLP-1-based therapies on diseases associated with chronic inflammation in vivo and in vitro, and their molecular mechanisms of anti-inflammatory action.

  4. Synthesis and anti-inflammatory activity of 1-acylaminoalkyl-3,4-dialkoxybenzene derivatives.

    Science.gov (United States)

    Labanauskas, L; Brukstus, A; Udrenaite, E; Bucinskaite, V; Susvilo, I; Urbelis, G

    2005-03-01

    New 1-acylaminoalkyl-3,4-dialkoxybenzene derivatives 17-31 were synthesized by the acylation of amines 9-16 with acyl chlorides. Amines 9-16 were obtained from aryl ketones 1-8. Aryl ketones 1-8 were synthesized by the acylation of corresponding aromatic compounds. As it was preliminary predicted by PASS (Prediction of Activity Spectra for Substance) program, all 1-acylaminoalkyl-3,4-dimethoxy- and 3,4-diethoxybenzene derivatives possess anti-inflammatory activity. Activity of compounds 18, 19, 21, 24, 26, 27, 28, 29 was similar to that of acetylsalicylic acid or ibuprofen however their acute toxicity was less than that of mentioned anti-inflammatory drugs. A series of 1-acylaminoalkyl-3,4-dimethoxybenzene, 1-acylaminoalkyl-3,4-diethoxybenzene and 6-acylaminoalkyl-2,3-dihydro-1,4-benzodioxine derivatives have been synthesized. These compounds possess moderate or strong anti-inflammatory activity and low toxicity.

  5. DIURETIC AND ANTI-INFLAMMATORY ACTIVITY OF AQUEOUS EXTRACT OF AERVA SANGUINOLENTA (L. BLUME

    Directory of Open Access Journals (Sweden)

    Srinivas Reddy K

    2011-07-01

    Full Text Available The study was designed to evaluate the diuretic and anti-inflammatory potency of aqueous extract of whole plant of Aerva sanguinolenta in wistar albino rats. Different parameters viz. total urine volume, urine concentration of electrolytes such as sodium; potassium and chloride have been evaluated for assessment of diuretic activity. Anti-inflammatory was performed against carrageenan induced paw oedema method by using indomethacin as standard.The results revealed that the aqueous extract showed significant diuretic activity at a dose of 400 mg/kg body weigh by increasing the total volume of urine and concentration of sodium, potassium and chloride ions in urine and also extract showed significant anti-inflammatory activity.

  6. Inflammation in Depression and the Potential for Anti-Inflammatory Treatment

    DEFF Research Database (Denmark)

    Köhler, Karl Ole; Krogh, Jesper; Mors, Ole;

    2016-01-01

    the association between inflammation and depression together with the current evidence on use of anti-inflammatory treatment in depression. Based on this, we address the questions and challenges that seem most important and relevant to future studies, such as timing, most effective treatment lengths......Accumulating evidence supports an association between depression and inflammatory processes, a connection that seems to be bidirectional. Clinical trials have indicated antidepressant treatment effects for anti-inflammatory agents, both as add-on treatment and as monotherapy. In particular......, nonsteroidal anti-inflammatory drugs (NSAIDs) and cytokine-inhibitors have shown antidepressant treatment effects compared to placebo, but also statins, poly-unsaturated fatty acids, pioglitazone, minocycline, modafinil, and corticosteroids may yield antidepressant treatment effects. However, the complexity...

  7. Inflammation in Depression and the Potential for Anti-Inflammatory Treatment

    DEFF Research Database (Denmark)

    Köhler, Ole; Krogh, Jesper; Mors, Ole;

    2016-01-01

    Accumulating evidence supports an association between depression and inflammatory processes, a connection that seems to be bidirectional. Clinical trials have indicated antidepressant treatment effects for anti-inflammatory agents, both as add-on treatment and as monotherapy. In particular......, nonsteroidal anti-inflammatory drugs (NSAIDs) and cytokine-inhibitors have shown antidepressant treatment effects compared to placebo, but also statins, poly-unsaturated fatty acids, pioglitazone, minocycline, modafinil, and corticosteroids may yield antidepressant treatment effects. However, the complexity of...... the inflammatory cascade, limited clinical evidence, and the risk for side effects stress cautiousness before clinical application. Thus, despite proof-of-concept studies of anti-inflammatory treatment effects in depression, important challenges remain to be investigated. Within this paper, we review...

  8. Evaluation of anti-inflammatory potential of leaf extracts of Skimmia anquetilia

    Institute of Scientific and Technical Information of China (English)

    Vijender Kumar; Zulfiqar Ali Bhat; Dinesh Kumar; NA Khan; IA Chashoo

    2012-01-01

    Objective: To evaluate anti-inflammatory potential of leaf extract of Skimmia anquetilia by in-vitro and in-vivo anti-inflammatory models. Methods: Acute toxicity study was carried out to determine the toxicity level of different extract using acute toxic class method as described in Organization of Economic Co-operation and Development Guidelines No.423. Carrageenan (1%w/w) was administered and inflammation was induced in rat paw. The leaf extracts of Skimmiaanquetilia were evaluated for anti-inflammatory activity by in-vitro human red blood cell (HRBC) membrane stabilization method and in-vivo carrangeenan-induced rat paw edema method.Results:The in-vitro membrane stabilizing test showed petroleum ether (PE), chloroform (CE), ethyl acetate (EE), methanol (ME) and aqueous extracts (AE) showed 49.44%, 59.39%, 60.15%, 68.40%and 52.18 % protection, respectively as compared to control groups. The in-vivo results of CE, EE and ME showed 58.20%, 60.17% and 67.53% inhibition of inflammation after 6h administration of test drugs in albino rats. The potency of the leaf extracts of Skimmia anquetilia were compared with standard diclofenac (10 mg/kg) which showed 74.18% protection in in-vitro HRBC membrane stabilization test and 71.64% inhibition in in-vivo carrangeenan-induced rat paw edema model. The ME showed a dose dependent significant (P< 0.01) anti-inflammatory activity in human red blood cell membrane stabilization test and reduction of edema in carrageenan induced rat paw edema. Conclusions: The present investigation has confirmed the anti-inflammatory activity ofSkimmia anquetilia due to presence of bioactive phytoconstitutes for the first time and provide the pharmacological evidence in favor of traditional claim of Skimmia anquetilia as an anti-inflammatory agent.

  9. Genetically engineered immunomodulatory Streptococcus thermophilus strains producing antioxidant enzymes exhibit enhanced anti-inflammatory activities.

    Science.gov (United States)

    Del Carmen, Silvina; de Moreno de LeBlanc, Alejandra; Martin, Rebeca; Chain, Florian; Langella, Philippe; Bermúdez-Humarán, Luis G; LeBlanc, Jean Guy

    2014-02-01

    The aims of this study were to develop strains of lactic acid bacteria (LAB) having both immunomodulatory and antioxidant properties and to evaluate their anti-inflammatory effects both in vitro, in different cellular models, and in vivo, in a mouse model of colitis. Different Lactobacillus delbrueckii subsp. bulgaricus and Streptococcus thermophilus strains were cocultured with primary cultures of mononuclear cells. Analysis of the pro- and anti-inflammatory cytokines secreted by these cells after coincubation with candidate bacteria revealed that L. delbrueckii subsp. bulgaricus CRL 864 and S. thermophilus CRL 807 display the highest anti-inflammatory profiles in vitro. Moreover, these results were confirmed in vivo by the determination of the cytokine profiles in large intestine samples of mice fed with these strains. S. thermophilus CRL 807 was then transformed with two different plasmids harboring the genes encoding catalase (CAT) or superoxide dismutase (SOD) antioxidant enzymes, and the anti-inflammatory effects of recombinant streptococci were evaluated in a mouse model of colitis induced by trinitrobenzenesulfonic acid (TNBS). Our results showed a decrease in weight loss, lower liver microbial translocation, lower macroscopic and microscopic damage scores, and modulation of the cytokine production in the large intestines of mice treated with either CAT- or SOD-producing streptococci compared to those in mice treated with the wild-type strain or control mice without any treatment. Furthermore, the greatest anti-inflammatory activity was observed in mice receiving a mixture of both CAT- and SOD-producing streptococci. The addition of L. delbrueckii subsp. bulgaricus CRL 864 to this mixture did not improve their beneficial effects. These findings show that genetically engineering a candidate bacterium (e.g., S. thermophilus CRL 807) with intrinsic immunomodulatory properties by introducing a gene expressing an antioxidant enzyme enhances its anti-inflammatory

  10. New isorhamnetin derivatives from Salsola imbricata Forssk. leaves with distinct anti-inflammatory activity

    Directory of Open Access Journals (Sweden)

    Samir M Osman

    2016-01-01

    Full Text Available Background: Salsola imbricata Forssk. is a shrub widely growing in Egypt, used as a camel food, traditionally, used as anti-inflammatory agent. Literature survey showed no report about the anti-inflammatory activity of S. imbricata. Aim of the Study: This work was designed to study the phenolic constituents and to provide evidence for the traditional use of S. imbricata as an anti-inflammatory agent. Materials and Methods: The in vitro anti-inflammatory activity of the total aqueous methanol extract and some isolated compounds were investigated in RAW 264.7 macrophage cells using nitric oxide assay. All chemical structures were identified on the basis of electrospray ionization-mass spectrometry, one- and two-dimension nuclear magnetic resonance. Results: Nine phenolic compounds, among them two new natural products; isorhamnetin-3-O-β-D-glucuronyl (1'''→4'' glucuronide (1 and its dimethyl ester; isorhamnetin-3-O-β-D-di glucuronate dimethyl ester (2, two isorhamnetin glycosides: Isorhamnetin-3-O-β-D-galactopyranoside (3, isorhamnetin-3-O-β-D-glucopyranoside (4, and isorhamnetin (5. In addition, an alkaloidal phenolic; trans N-feruloyl tyramine (6, three phenolic acids: Isovanillic acid (7, ferulic acid (8, and p-hydroxy benzoic acid (9 were isolated from salsola imbricata leaves. All compounds were isolated and identified for the first time from this plant except compound (6. The extract and the tested compounds showed distintict anti-inflammatory activities with no toxicity on RAW 264.7 macrophage cells. Conclusion: The extract and the tested compounds showed distintict anti-inflammatory activities with no toxicity on RAW 264.7 macrophage cells.

  11. Variation in antibacterial and anti-inflammatory activity of different growth forms of Malva parviflora and evidence for synergism of the anti-inflammatory compounds.

    Science.gov (United States)

    Shale, T L; Stirk, W A; van Staden, J

    2005-01-01

    Malva parviflora leaves and roots were collected from five sites within the Qacha's Nek District in Lesotho. These plants had two distinct growth forms--upright and prostrate. Hexane, methanol and water extracts were made from the plant material and tested for antibacterial and anti-inflammatory activity using the disc diffusion and cyclooxygenase-1 (Cox-1) bioassays, respectively. Hexane, methanol and water extracts made from Malva parviflora with a prostrate growth form inhibited the growth of Gram-positive and Gram-negative bacteria, while extracts made from plants with an upright growth form inhibited the growth of Gram-positive bacteria only. Cox-1 anti-inflammatory activity of hexane, methanol and water extracts did not show any variation between the two growth forms. The hexane extracts of both the leaves and roots were the most inhibitory. The water extracts had the least inhibitory activity. Bioassay-guided fractionation of the root dichloromethane extract showed that Cox-1 anti-inflammatory activity was caused by at least two compounds that acted synergistically to produce the biological effect.

  12. Anti-Inflammatory and Antinociceptive Activities of a Hydroethanolic Extract of Tamarindus indica Leaves.

    Science.gov (United States)

    Bhadoriya, Santosh Singh; Mishra, Vijay; Raut, Sushil; Ganeshpurkar, Aditya; Jain, Sunil K

    2012-09-01

    The present study aimed to investigate the anti-inflammatory and anti-nociceptive potential of a hydroethanolic extract of Tamarindus indica L. leaves (HTI) along with its possible mode of action. The anti-inflammatory activity of HTI was estimated by carrageenan-induced hind paw oedema in male Wistar albino rats. Furthermore, HTI was assessed to determine its effects on membrane stabilization. The antinociceptive action was determined by acetic acid-induced writhing, tail-flick, and the hot plate model. Oral administration of HTI at the dose of 500, 750, and 1000 mg/kg body weight produced significant (Pindica as were mentioned in Indian traditional and folklore practices.

  13. In-silico Design, Synthesis, Anti-inflammatory and Anticancer Evaluation of Pyrazoline Analogues of Vanillin

    Directory of Open Access Journals (Sweden)

    M. J. Neethu

    2014-04-01

    Full Text Available A series of novel pyrazoline derivatives of vanillin were synthesized. The hydroxyl group in vanillin was masked by converting into methyl vanillin. The methyl vanillin was allowed to condense with different acetophenone derivatives gave chalcone derivatives and finally cyclized with thiosemicarbazide to form the pyrazoline derivatives of vanillin. Docking studies were carried out against anti-inflammatory cyclooxygenase receptor and anticancer farnesyl transferase receptor. Majority of the synthesized compounds showed good fitting with the active site of all the docked targets. The synthesized compounds had shown significant anti inflammatory and anticancer activities.

  14. Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines.

    Science.gov (United States)

    Balakumar, C; Lamba, P; Kishore, D Pran; Narayana, B Lakshmi; Rao, K Venkat; Rajwinder, K; Rao, A Raghuram; Shireesha, B; Narsaiah, B

    2010-11-01

    A series of novel 8/10-trifluoromethyl-substituted-imidazo[1,2-c] quinazolines have been synthesized and evaluated in vivo (rat paw edema) for their anti-inflammatory activity and in silico (docking studies) to recognize the hypothetical binding motif of the title compounds with the cyclooxygenase isoenzymes (COX-1 and COX-2) employing GOLD (CCDC, 4.0.1 version) software. The compounds, 9b and 10b, were found to have good anti-inflammatory activity [around 80% of the standard: indomethacin]. The binding mode of the title compounds has been proposed based on the docking studies.

  15. Cardiovascular disease event rates in patients with severe psoriasis treated with systemic anti-inflammatory drugs

    DEFF Research Database (Denmark)

    Ahlehoff, O; Skov, L; Gislason, G;

    2013-01-01

    disease events. We therefore examined the rate of cardiovascular disease events in patients with severe psoriasis treated with systemic anti-inflammatory drugs. DESIGN, SETTING AND PARTICIPANTS: Individual-level linkage of nationwide administrative databases was used to assess the event rates associated......OBJECTIVES: Psoriasis is a chronic inflammatory disorder associated with cardiovascular morbidity and mortality. Systemic anti-inflammatory drugs, including biological agents, are widely used in the treatment of patients with moderate to severe psoriasis and may attenuate the risk of cardiovascular...... cardiovascular disease event rates compared to patients treated with other anti-psoriatic therapies....

  16. Enhancement of anti-inflammatory activity of bromelain by its encapsulation in katira gum nanoparticles.

    Science.gov (United States)

    Bernela, Manju; Ahuja, Munish; Thakur, Rajesh

    2016-06-01

    Bromelain-loaded katira gum nanoparticles were synthesized using 3 level optimization process and desirability approach. Nanoparticles of the optimized batch were characterized using particle size analysis, zeta potential, transmission electron microscopy and Fourier-transform infrared spectroscopy. Investigation of their in vivo anti-inflammatory activity by employing carrageenan induced rat-paw oedema method showed that encapsulation of bromelain in katira gum nanoparticles substantially enhanced its anti-inflammatory potential. This may be attributed to enhanced absorption owing to reduced particle size or to protection of bromelain from acid proteases. PMID:27083339

  17. ANTI INFLAMMATORY, ANALGESIC AND PHYTOCHEMICAL STUDIES OF CLITORIA TERNATEA LINN FLOWER EXTRACT

    Directory of Open Access Journals (Sweden)

    Shyamkumar

    2012-03-01

    Full Text Available Clitoria ternatea Linn is a well known bio active plant in the Ayurvedic medicine. The present study evaluates the analgesic and anti-inflammatory activity of Clitoria ternatea Linn flower extract. The petroleum ether (60-80◦C extract poses significant anti inflammatory, analgesic properties. The extract is found to be safe even at the dose of 2000 mg/kg body weight by acute toxicity studies. Phytochemical investigation carried out on Petroleum ether(60-80◦C extract reveals the presence of Taraxerol, a pentacyclic triterpenoid which may impart the pharmacological activity of the extract.

  18. ANTI INFLAMMATORY, ANALGESIC AND PHYTOCHEMICAL STUDIES OF CLITORIA TERNATEA LINN FLOWER EXTRACT

    OpenAIRE

    Shyamkumar; Bhat Ishwar

    2012-01-01

    Clitoria ternatea Linn is a well known bio active plant in the Ayurvedic medicine. The present study evaluates the analgesic and anti-inflammatory activity of Clitoria ternatea Linn flower extract. The petroleum ether (60-80◦C) extract poses significant anti inflammatory, analgesic properties. The extract is found to be safe even at the dose of 2000 mg/kg body weight by acute toxicity studies. Phytochemical investigation carried out on Petroleum ether(60-80◦C) extract reveals the presence of...

  19. Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines.

    Science.gov (United States)

    Balakumar, C; Lamba, P; Kishore, D Pran; Narayana, B Lakshmi; Rao, K Venkat; Rajwinder, K; Rao, A Raghuram; Shireesha, B; Narsaiah, B

    2010-11-01

    A series of novel 8/10-trifluoromethyl-substituted-imidazo[1,2-c] quinazolines have been synthesized and evaluated in vivo (rat paw edema) for their anti-inflammatory activity and in silico (docking studies) to recognize the hypothetical binding motif of the title compounds with the cyclooxygenase isoenzymes (COX-1 and COX-2) employing GOLD (CCDC, 4.0.1 version) software. The compounds, 9b and 10b, were found to have good anti-inflammatory activity [around 80% of the standard: indomethacin]. The binding mode of the title compounds has been proposed based on the docking studies. PMID:20800934

  20. [Role of anti-inflammatory drugs in the treatment of acute coronary syndromes. From athero-inflammation to athero-thrombosis].

    Science.gov (United States)

    Altman, Raúl; Scazziota, Alejandra

    2003-01-01

    Coronary thrombosis is the most important cause of morbidity and mortality and the most severe manifestation of atherosclerosis. Knowledge of the pathophysiology of atheroma formation and the causes of atheroma accidents have allowed the development of new therapeutic measures for reducing thrombotic events after a coronary episode. Treating the thrombosis after plaque rupture is useful, but a late measure once coronary flow is disturbed. Therefore, treatment at an earlier stage, which we call athero-inflammation, a central event in atheroma progression leading to atherothrombosis, seems wise. There is evidence of an inflammatory component in the pathogenesis of atheroma rupture in acute coronary events. Earlier studies of anti-inflammatory medication have not demonstrated a reduction in thrombotic complications after an acute coronary episode. However, there are pathophysiological arguments and clinical findings that suggest that it would be advisable to include anti-inflammatory medications, especially those that inhibit preferentially COX-2, in the therapeutic arsenal for this pathology. We postulated that blocking athero-inflammation could prevent thrombosis. A pilot study was carried out in 120 patients with acute coronary syndrome without ST-segment elevation in which 60 patients were treated with meloxicam, a preferential COX-2 inhibitor. All patients received heparin and aspirin. During the stay in the coronary care unit, as well as after 90 days, meloxicam lowered composite outcomes (myocardial infarction, death and revascularization procedures) compared with the control group. These results and available pathophysiological and clinical evidence support the hypothesis of potential benefits of non-steroidal anti-inflammatory drugs with preferential inhibitory activity on COX-2 in patients with acute coronary syndromes. More trials are needed to confirm their preventive effect. PMID:12549993

  1. Use of low-dose aspirin and non-aspirin nonsteroidal anti-inflammatory drugs and risk of glioma

    DEFF Research Database (Denmark)

    Gaist, David; García-Rodríguez, L A; Sørensen, H T;

    2013-01-01

    Background:Few studies have examined the association between use of aspirin or other non-steroidal anti-inflammatory drugs (NSAIDs) and risk of glioma and the results have been equivocal. We therefore investigated the influence of NSAID use on glioma risk in a nationwide setting.Methods:We used...... exposure to low-dose aspirin or non-aspirin (NA) NSAIDs into ever use or long-term use, defined as continuous use for 5 years. Conditional logistic regression was used to compute odds ratios (ORs), with 95% confidence intervals (CIs), for glioma associated with NSAID use, adjusted for potential...... confounders.Results:A total of 2688 glioma cases and 18 848 population controls were included in the study. Ever use of low-dose aspirin (OR=0.90; 95% CI: 0.77-1.04) or NA-NSAIDs (OR=1.05; 95% CI: 0.96-1.14) was not associated with glioma risk. Compared with never use, long-term use of low-dose aspirin or of...

  2. Acetylsalicylic Acid Reduces the Severity of Dextran Sodium Sulfate-Induced Colitis and Increases the Formation of Anti-Inflammatory Lipid Mediators

    Directory of Open Access Journals (Sweden)

    Thomas Köhnke

    2013-01-01

    Full Text Available The role of non-steroidal anti-inflammatory drugs in inflammatory bowel disease is controversial, as they have been implicated in disease aggravation. Different from other cyclooxygenase inhibitors, acetylsalicylic acid (ASA enhances the formation of anti-inflammatory and proresolution lipoxins derived from arachidonic acid as well as resolvins from omega-3 polyunsaturated fatty acids such as docosahexaenoic acid (DHA. In this study, we examined the effect of ASA on murine dextran sodium sulfate colitis. A mouse magnetic resonance imaging (MRI protocol and post mortem assessment were used to assess disease severity, and lipid metabolites were measured using liquid chromatography-coupled tandem mass spectrometry. Decreased colitis activity was demonstrated by phenotype and MRI assessment in mice treated with ASA, and confirmed in postmortem analysis. Analysis of lipid mediators showed sustained formation of lipoxin A4 and an increase of DHA-derived 17-hydroxydocosahexaenoic acid (17-HDHA after treatment with ASA. Furthermore, in vitro experiments in RAW264.7 murine macrophages demonstrated significantly increased phagocytosis activity after incubation with 17-HDHA, supporting its proresolution effect. These results show a protective effect of ASA in a murine colitis model and could give a rationale for a careful reassessment of ASA therapy in patients with inflammatory bowel disease and particularly ulcerative colitis, possibly combined with DHA supplementation.

  3. Anti-inflammatory drugs interacting with Zn (II) metal ion based on thiocyanate and azide ligands: Synthesis, spectroscopic studies, DFT calculations and antibacterial assays

    Science.gov (United States)

    Chiniforoshan, Hossein; Tabrizi, Leila; Hadizade, Morteza; Sabzalian, Mohammad R.; Chermahini, Alireza Najafi; Rezapour, Mehdi

    2014-07-01

    Zinc (II) complexes with non-steroidal anti-inflammatory drugs (NSAIDs) naproxen (nap) and ibuprofen (ibu) were synthesized in the presence of nitrogen donor ligands (thiocyanate or azide). The complexes were characterized by elemental analysis, FT-IR, 1H NMR and UV-Vis spectroscopes. The binding modes of the ligands in complexes were established by means of molecular modeling of the complexes, and calculation of their IR, NMR and absorption spectra at DFT (TDDFT)/B3LYP level were studied. The experimental and calculated data verified monodentate binding through the carboxylic oxygen atoms of anti-inflammatory drugs in the zinc complexes. The calculated 1H, FT-IR and UV-Vis data are in better agreement with the experimental results, and confirm the predicted tetrahedral structures for the Zn (II) complexes. In addition to DFT calculations of complexes, natural bond orbital (NBO) was performed at B3LYP/6-31+G(d,p) level of theory. Biological studies showed the antibacterial activity of zinc complexes against Gram-positive and Gram-negative bacterial strains.

  4. Auraptene Acts as an Anti-Inflammatory Agent in the Mouse Brain

    Directory of Open Access Journals (Sweden)

    Satoshi Okuyama

    2015-11-01

    Full Text Available The anti-inflammatory activity of auraptene (AUR, a citrus coumarin, in peripheral tissues is well-known, and we previously demonstrated that AUR exerts anti-inflammatory effects in the ischemic brain; the treatment of mice with AUR for eight days immediately after ischemic surgery suppressed demise and neuronal cell death in the hippocampus, possibly through its anti-inflammatory effects in the brain. We suggested that these effects were at least partly mediated by the suppression of inflammatory mediators derived from astrocytes. The present study showed that (1 AUR, as a pretreatment for five days before and another three days after ischemic surgery, suppressed microglial activation, cyclooxygenase (COX-2 expression in astrocytes, and COX-2 mRNA expression in the hippocampus; (2 AUR suppressed the lipopolysaccharide-induced expression of COX-2 mRNA and the mRNA of pro-inflammatory cytokines in cultured astrocytes; (3 AUR was still detectable in the brain 60 min after its intraperitoneal administration. These results support our previous suggestion that AUR directly exerts anti-inflammatory effects on the brain.

  5. General unknown screening, antioxidant and anti-inflammatory potential of Dendrobium macrostachyum Lindl.

    Directory of Open Access Journals (Sweden)

    Nimisha Pulikkal Sukumaran

    2016-01-01

    Conclusions: The results showed a relatively high concentration of phenolics, high scavenger activity and high anti-inflammatory activity of the stem extract compared to the leaf extract. The results indicate that the plant can be a potential source of bioactive compounds.

  6. Antimicrobial and anti-inflammatory activities of leaf extract of Valeriana wallichii DC.

    Science.gov (United States)

    Khuda, Fazli; Iqbal, Zafar; Zakiullah; Khan, Ayub; Nasir, Fazli

    2012-10-01

    Valeriana wallichii DC (Valerianaceae) is one of the most widely used traditional remedies for various complications associated with nervous system and digestion. No antimicrobial and anti-inflammatory studies have so far been carried out on the aerial parts of the plant. The present work was focused to evaluate the antimicrobial (antifungal and antibacterial) and anti-inflammatory properties of V. wallichii using reported methods. Chloroform fraction (VW-2) and hexane fraction (VW-3) exhibited significant activity against S. aureus and B. subtilus, respectively. The chloroform fraction (VW-2) showed significant activity against S. aureus with 0.27 mg/ml MIC, where 0.31 mg/ml MIC was deduced for VW-3 fraction against B. subtilus. VW-3 fraction was also found to be the most potent inhibitor of M. canis, showing 70% inhibition with an MIC value of 0.19 mg/ml. Considerable inhibitory activity was also observed for VW-2 and water fraction (VW-6) against M. canis and A. flavus. A remarkable anti-inflammatory like activity was observed for the crude extract at a dose of 200 mg/kg at all observed durations. Other doses of the sample also showed excellent activity. Looking to these results it may be concluded that V. wallichii may be a potential source for activity guided isolation of natural products with antimicrobial and anti-inflammatory-like properties. PMID:23009985

  7. Anti-inflammatory mechanisms of bioactive milk proteins in the intestine of newborns

    DEFF Research Database (Denmark)

    Chatterton, Dereck E W; Nguyen, Duc Ninh; Bering, Stine Brandt;

    2013-01-01

    of proteins with anti-inflammatory properties and in this review we gather together some recent significant advances regarding the isolation and proteomic identification of these minor constituents of both human and bovine milk. We introduce the process of inflammation, with a focus on the immature gut...

  8. Pharmacological potential of Populus nigra extract as antioxidant, anti-inflammatory, cardiovascular and hepatoprotective agent

    Directory of Open Access Journals (Sweden)

    Nadjet Debbache-Benaida

    2013-09-01

    Conclusions: The extract exerted significant anti-inflammatory, hepatoprotective and vasorelaxant activities, the latter being endothelium-independent believed to be mediated mainly by the ability of components present in the extract to exert antioxidant properties, probably related to an inhibition of Ca2+ influx.

  9. Pharmacological potential of Populus nigra extract as antioxidant, anti-inflammatory, cardiovascular and hepatoprotective agent

    Institute of Scientific and Technical Information of China (English)

    Nadjet Debbache-Benaida; Dina Atmani-Kilani; Valrie Barbara Schini-Keirth; Nouredine Djebbli; Djebbar Atmani

    2013-01-01

    Objective: To evaluate antioxidant, anti-inflammatory, hepatoprotective and vasorelaxant activities of Populus nigra flower buds ethanolic extract. Methods: Antioxidant and anti-inflammatory activities of the extract were assessed using respectively the ABTS test and the animal model of carrageenan-induced paw edema. Protection from hepatic toxicity caused by aluminum was examined by histopathologic analysis of liver sections. Vasorelaxant effect was estimated in endothelium-intact and-rubbed rings of porcine coronary arteries precontracted with high concentration of U46619. Results:The results showed a moderate antioxidant activity (40%), but potent anti-inflammatory activity (49.9%) on carrageenan-induced mice paw edema, and also as revealed by histopathologic examination, complete protection against AlCl3-induced hepatic toxicity. Relaxant effects of the same extract on vascular preparation from porcine aorta precontracted with high concentration of U46619 were considerable at 10-1 g/L, and comparable (P>0.05) between endothelium-intact (67.74%, IC50=0.04 mg/mL) and-rubbed (72.72%, IC50=0.075 mg/mL) aortic rings. Conclusions: The extract exerted significant anti-inflammatory, hepatoprotective and vasorelaxant activities, the latter being endothelium-independent believed to be mediated mainly by the ability of components present in the extract to exert antioxidant properties, probably related to an inhibition of Ca2+influx.

  10. Synthesis and anti-inflammatory activity of imidazo [1,2-a] pyrimidine derivatives

    Institute of Scientific and Technical Information of China (English)

    Jin Pei Zhou; Yi Wei Ding; Hui Bin Zhang; Lian Xu; Yue Dai

    2008-01-01

    A series of imidazo [1,2-a] pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests suggested that these compounds have antiinflammatory activities with COX-2 selectivity to some extent.

  11. Anti-Inflammatory and Immunomodulatory Mechanism of Tanshinone IIA for Atherosclerosis

    Directory of Open Access Journals (Sweden)

    Zhuo Chen

    2014-01-01

    Full Text Available Tanshinone IIA (Tan II A is widely used in the treatment of cardiovascular diseases as an active component of Salvia miltiorrhiza Bunge. It has been demonstrated to have pleiotropic effects for atherosclerosis. From the anti-inflammatory and immunomodulatory mechanism perspective, this paper reviewed major progresses of Tan IIA in antiatherosclerosis research, including immune cells, antigens, cytokines, and cell signaling pathways.

  12. Bioassay-guided evaluation of anti-inflammatory and antinociceptive activities of pistachio, Pistacia vera L.

    Science.gov (United States)

    Orhan, I; Küpeli, E; Aslan, M; Kartal, M; Yesilada, E

    2006-04-21

    The ethanolic and aqueous extracts prepared from different parts of Pistacia vera L. (Anacardiaceae) as well as its oleoresin were evaluated for their in vivo anti-inflammatory and antinociceptive activities. Among the extracts screened, only the oleoresin was shown to possess a marked anti-inflammatory activity against carrageenan-induced hind paw edema model in mice without inducing any gastric damage at both 250 and 500 mg/kg doses whereas the rest of the extracts were totally inactive. While the oleoresin was found to display significant antinociceptive activity at 500 mg/kg dose, the ethanolic and aqueous extracts belonging to fruit, leaf, branch and peduncle of Pistacia vera did not exhibit any noticeable antinociception in p-benzoquinone-induced abdominal contractions in mice. Fractionation of the oleoresin indicated the n-hexane fraction to be active, which further led to recognition of some monoterpenes, mainly alpha-pinene (77.5%) by capillary gas chromatography-mass spectrometry (GC-MS) as well as the oleoresin itself. alpha-Pinene was also assessed for its antinociceptive and anti-inflammatory activities in the same manner and exerted a moderate anti-inflammatory effect at 500 mg/kg dose.

  13. Endogenous stress proteins as targets for anti-inflammatory T cells

    NARCIS (Netherlands)

    Wieten, L.

    2009-01-01

    Stress proteins such as heat shock proteins (Hsp) are important controllers of both cellular and immune homeostasis. Enhanced Hsp expression can be observed in virtually every inflammatory condition and has been proposed by us and others to lead to local activation of Hsp-specific anti-inflammatory

  14. AP-1/IRF-3 Targeted Anti-Inflammatory Activity of Andrographolide Isolated from Andrographis paniculata

    Directory of Open Access Journals (Sweden)

    Ting Shen

    2013-01-01

    Full Text Available Andrographolide (AG is an abundant component of plants of the genus Andrographis and has a number of beneficial properties including neuroprotective, anticancer, anti-inflammatory, and antidiabetic effects. Despite numerous pharmacological studies, the precise mechanism of AG is still ambiguous. Thus, in the present study, we investigated the molecular mechanisms of AG and its target proteins as they pertain to anti-inflammatory responses. AG suppressed the production of nitric oxide (NO and prostaglandin E2 (PGE2, as well as the mRNA abundance of inducible NO synthase (iNOS, tumor necrosis factor-alpha (TNF-α, cyclooxygenase (COX-2, and interferon-beta (IFN-β in a dose-dependent manner in both lipopolysaccharide- (LPS- activated RAW264.7 cells and peritoneal macrophages. AG also substantially ameliorated the symptoms of LPS-induced hepatitis and EtOH/HCl-induced gastritis in mice. Based on the results of luciferase reporter gene assays, kinase assays, and measurement of nuclear levels of transcription factors, the anti-inflammatory effects of AG were found to be clearly mediated by inhibition of both (1 extracellular signal-regulated kinase (ERK/activator protein (AP-1 and (2 IκB kinase ε (IKKε/interferon regulatory factor (IRF-3 pathways. In conclusion, we detected a novel molecular signaling pathway by which AG can suppress inflammatory responses. Thus, AG is a promising anti-inflammatory drug with two pharmacological targets.

  15. Structural investigation of chitosan-based microspheres with some anti-inflammatory drugs

    Science.gov (United States)

    Dreve, Simina; Kacso, Iren; Popa, Adriana; Raita, Oana; Dragan, Felicia; Bende, A.; Borodi, Gh.; Bratu, I.

    2011-06-01

    The use of chitosan as an excipient in oral formulations, as a drug delivery vehicle for ulcerogenic anti-inflammatory drugs and as base in polyelectrolyte complex systems, to prepare solid release systems as sponges was investigated. The preparation by double emulsification of chitosan hydrogels carrying diclofenac, acetyl-salycilic acid and hydrocortisone acetate as anti-inflammatory drugs is reported. The concentration of anti-inflammatory drug in the chitosan hydrogel generating the sponges was 0.08 mmol. Chitosan-drug loaded sponges with anti-inflammatory drugs were prepared by freeze-drying at -60 °C and 0.009 atm. Structural investigations of the solid formulations were done by Fourier-transformed infrared and ultraviolet-visible spectroscopy, spectrofluorimetry, differential scanning calorimetry and X-ray diffractometry. The results indicated that the drug molecules are forming temporary chelates in chitosan hydrogels and sponges. Electron paramagnetic resonance demonstrates the presence of free radicals in a wide range and the antioxidant activity for chitosan-drug supramolecular cross-linked assemblies.

  16. Anti-Tumor Effect and Anti-Inflammatory Activity of Boschniakia rossica

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Objective: To investigate the anti-tumor effect and anti-inflammatory activity of Boschniakia rossica (BR). Methods: The expression of tumor marker, GST-P, p53 and p21ras proteins in promotion stage of rat chemical hepatocarcinogenesis were examined by immunohistochemical technique ABC method. Anti-tumor effect of BR was investigated by inhibitory test on Sarcoma180. Anti-inflammatory activity of BR was tested by xylene-induced mouse ear swelling method. Results: BR-H2O extract (the H2O extract fractionated from BR-Methanol extract with CH2Cl2 and H2O) 500 mg/kg has inhibitory effect on the formation of diethylnitrosamine (DEN)-induced glutathione S-transferase placental form (GST-P) positive foci in rat liver with the expression of mutant p53 and p21ras proteins lower than those of non-treated hepatic preneoplastic lesions. BR extract showed inhibitory effect on Sarcoma180 and anti-inflammatory effect in mice by xylene-induced mouse ear swelling tests. Conclusion: BR- H2O extract exerted inhibitory effect on DEN-induced preneoplastic hepatic foci in promotion stage of rat chemical hepatocarcinogenesis and might suppress the growth of solid Sarcoma180 in mice. Both CH2Cl2 and H2O extract from BR exerted anti-inflammatory effect in mice.

  17. Antioxidant, analgesic and anti-inflammatory effects of lavender essential oil.

    Science.gov (United States)

    Silva, Gabriela L da; Luft, Carolina; Lunardelli, Adroaldo; Amaral, Robson H; Melo, Denizar A da Silva; Donadio, Márcio V F; Nunes, Fernanda B; de Azambuja, Marcos S; Santana, João C; Moraes, Cristina M B; Mello, Ricardo O; Cassel, Eduardo; Pereira, Marcos Aurélio de Almeida; de Oliveira, Jarbas R

    2015-08-01

    Several studies have investigated the antinociceptive, immunomodulatory and anti-inflammatory properties of compounds found in the lavender essential oil (LEO), however to date, there is still lack of substantial data. The objective of this study was to assess the antioxidant, anti-inflammatory and antinociceptive effects of lavender essential oil. The 1,1-diphenyl-2-picrylhydrazyl radical decolorization assay was used for antioxidant activity evaluation. The anti-inflammatory activity was tested using two models of acute inflammation: carrageenan-induced pleurisy and croton oil-induced ear edema. The antinociceptive activity was tested using the pain model induced by formalin. LEO has antioxidant activity, which is dose-dependent response. The inflammatory response evoked by carrageenan and by croton oil was reduced through the pre-treatment of animals with LEO. In the pleurisy model, the drug used as positive control, dexamethasone, was more efficacious. However, in the ear swelling, the antiedematogenic effect of the oil was similar to that observed for dexamethasone. In the formalin test, LEO consistently inhibited spontaneous nociception and presented a similar effect to that of tramadol. The results of this study reveal (in vivo) the analgesic and anti-inflammatory activities of LEO and demonstrates its important therapeutic potential. PMID:26247152

  18. Doxycycline Is Anti-Inflammatory and Inhibits Staphylococcal Exotoxin-Induced Cytokines and Chemokines

    OpenAIRE

    Krakauer, Teresa; Buckley, Marilyn

    2003-01-01

    Proinflammatory cytokines mediate the toxic effect of superantigenic staphylococcal exotoxins (SE). Doxycycline inhibited SE-stimulated T-cell proliferation and production of cytokines and chemokines by human peripheral blood mononuclear cells. These results suggest that the antibiotic doxycycline has anti-inflammatory effects and is therapeutically useful for mitigating the pathogenic effects of SE.

  19. Anti-Inflammatory and Antiarthritic Activity of Anthraquinone Derivatives in Rodents

    Directory of Open Access Journals (Sweden)

    Ajay D. Kshirsagar

    2014-01-01

    Full Text Available Aloe emodin is isolated compound of aloe vera which is used traditionally as an anti-inflammatory agent. In vitro pharmacokinetic data suggest that glucuronosyl or sulfated forms of aloe emodin may provide some limitations in its absorption capacity. Aloe emodin was reported to have in vitro anti-inflammatory activity due to inhibition of inducible nitric oxide (iNO and prostaglandin E2, via its action on murine macrophages. However, present work evidenced that molecular docking of aloe emodin modulates the anti-inflammatory activity, as well as expression of COX-2 (cyclooxygenase-2 in rodent. The AEC (4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2 carboxylic acid was synthesized using aloe emodin as starting material. The study was planned for evaluation of possible anti-inflammatory and antiarthritic activity in carrageenan rat induced paw oedema and complete Freund’s adjuvant induced arthritis in rats. The AE (aloe emodin and AEC significantly P<0.001 reduced carrageenan induced paw edema at 50 and 75 mg/kg. Complete Freund’s adjuvant induced arthritis model showed significant P<0.001 decrease in injected and noninjected paw volume, arthritic score. AE and AEC showed significant effect on various biochemical, antioxidant, and hematological parameters. Diclofenac sodium 10 mg/kg showed significant P<0.001 inhibition in inflammation and arthritis.

  20. Anti-inflammatory and immune-regulatory mechanisms prevent contact hypersensitivity to Arnica montana L.

    Science.gov (United States)

    Lass, Christian; Vocanson, Marc; Wagner, Steffen; Schempp, Christoph M; Nicolas, Jean-Francois; Merfort, Irmgard; Martin, Stefan F

    2008-10-01

    Sesquiterpene lactones (SL), secondary plant metabolites from flowerheads of Arnica, exert anti-inflammatory effects mainly by preventing nuclear factor (NF)-kappaB activation because of alkylation of the p65 subunit. Despite its known immunosuppressive action, Arnica has been classified as a plant with strong potency to induce allergic contact dermatitis. Here we examined the dual role of SL as anti-inflammatory compounds and contact allergens in vitro and in vivo. We tested the anti-inflammatory and allergenic potential of SL in the mouse contact hypersensitivity model. We also used dendritic cells to study the activation of NF-kappaB and the secretion of interleukin (IL)-12 in the presence of different doses of SL in vitro. Arnica tinctures and SL potently suppressed NF-kappaB activation and IL-12 production in dendritic cells at high concentrations, but had immunostimulatory effects at low concentrations. Contact hypersensitivity could not be induced in the mouse model, even when Arnica tinctures or SL were applied undiluted to inflamed skin. In contrast, Arnica tinctures suppressed contact hypersensitivity to the strong contact sensitizer trinitrochlorobenzene and activation of dendritic cells. However, contact hypersensitivity to Arnica tincture could be induced in acutely CD4-depleted MHC II knockout mice. These results suggest that induction of contact hypersensitivity by Arnica is prevented by its anti-inflammatory effect and immunosuppression as a result of immune regulation in immunocompetent mice.

  1. Nonsteroidal anti-inflammatory drugs for low back pain - An updated Cochrane review

    NARCIS (Netherlands)

    Roelofs, Pepijn D. D. M.; Deyo, Rick A.; Koes, Bart W.; Scholten, Rob J. P. M.; van Tulder, Maurits W.

    2008-01-01

    Study Design. A systematic review of randomized controlled trials. Objectives. To assess the effects of nonsteroidal anti-inflammatory drugs (NSAIDs) and COX-2 inhibitors in the treatment of nonspecific low back pain and to assess which type of NSAID is most effective. Summary of Background Data. NS

  2. Antinociceptive and Anti-inflammatory Effects of Pistacia vera LeafExtract in Mice.

    Science.gov (United States)

    Hosseinzadeh, Hossein; Behravan, Effat; M Soleimani, Mohammad

    2011-01-01

    Pistacia vera L., a member of Anacardiaceae family, has been used for sedation and analgesia in traditional medicine. In this study, the antinociceptive and anti-inflammatory effects as well as acute toxicity of the aqueous and ethanolic extracts of P. vera leaves were investigated in mice. The antinociceptive activity was studied using hot plate and writhing tests. The effect of the extracts against acute inflammation was determined using xylene-induced ear edema and the activity of the extracts, against chronic inflammation, was assessed using the cotton pellet test. The LD50 values of the infusion and maceration extracts were 0.8 g/Kg and 0.79 g/Kg, respectively. The aqueous and ethanolic maceration extracts of the P. vera leaves at the doses of 0.4 g/Kg and 0.5 g/Kg (IP), respectively, showed antinociceptive effects. The pretreatment of naloxone (2 mg/Kg, SC) inhibited the activities of extracts in hot plate test, but naloxone at the same dose could not inhibit the antinociceptive activity in writhing test. The extracts also showed anti-inflammatory effects in acute and chronic anti-inflammatory tests. The ethanolic extract was as effective as diclofenac in both inflammatory tests. The aqueous and ethanolic extracts of P. vera leaves demonstrated central and peripheral antinociceptive activities dose-dependently and the central effect may be mediated by opioid system. The extracts also demonstrated anti-inflammatory effects against acute and chronic inflammation. PMID:24250418

  3. Bioassay-guided evaluation of anti-inflammatory and antinociceptive activities of pistachio, Pistacia vera L.

    Science.gov (United States)

    Orhan, I; Küpeli, E; Aslan, M; Kartal, M; Yesilada, E

    2006-04-21

    The ethanolic and aqueous extracts prepared from different parts of Pistacia vera L. (Anacardiaceae) as well as its oleoresin were evaluated for their in vivo anti-inflammatory and antinociceptive activities. Among the extracts screened, only the oleoresin was shown to possess a marked anti-inflammatory activity against carrageenan-induced hind paw edema model in mice without inducing any gastric damage at both 250 and 500 mg/kg doses whereas the rest of the extracts were totally inactive. While the oleoresin was found to display significant antinociceptive activity at 500 mg/kg dose, the ethanolic and aqueous extracts belonging to fruit, leaf, branch and peduncle of Pistacia vera did not exhibit any noticeable antinociception in p-benzoquinone-induced abdominal contractions in mice. Fractionation of the oleoresin indicated the n-hexane fraction to be active, which further led to recognition of some monoterpenes, mainly alpha-pinene (77.5%) by capillary gas chromatography-mass spectrometry (GC-MS) as well as the oleoresin itself. alpha-Pinene was also assessed for its antinociceptive and anti-inflammatory activities in the same manner and exerted a moderate anti-inflammatory effect at 500 mg/kg dose. PMID:16337351

  4. In vitro anti-inflammatory, mutagenic and antimutagenic activities of ethanolic extract of Clerodendrum paniculatum root

    Directory of Open Access Journals (Sweden)

    Pravaree Phuneerub

    2015-01-01

    Full Text Available Clerodendrum paniculatum L. (Family Verbenaceae has been used as an antipyretic and anti-inflammatory drug in traditional Thai medicine. This present study investigated the in vitro anti-inflammatory, mutagenic and antimutagenic activities of the ethanolic extract of C. paniculatum (CPE dried root collected from Sa Kaeo Province of Thailand. Murine macrophage J774A.1 cells were stimulated by lipopolysaccharide (LPS to evaluate nitric oxide (NO, tumor necrosis factor-α (TNF-α and prostaglandin E 2 (PGE 2 production in the anti-inflammatory test while the mutagenic and antimutagenic potential was performed by the Ames test. The outcome of this study displayed that the CPE root significantly inhibited LPS-induced NO, TNF-α, and PGE 2 production in macrophage cell line. In addition, the CPE root was not mutagenic toward Salmonella typhimurium strain TA98 and TA100 with and without nitrite treatment. Moreover, it inhibited the mutagenicity of nitrite treated 1-aminopyrene on both strains. The findings suggested the anti-inflammatory and antimutagenic potentials of CPE root.

  5. Amauroderma rugosum (Blume & T. Nees Torrend: Nutritional Composition and Antioxidant and Potential Anti-Inflammatory Properties

    Directory of Open Access Journals (Sweden)

    Pui-Mun Chan

    2013-01-01

    Full Text Available Amauroderma rugosum is a wild mushroom that is worn as a necklace by the indigenous communities in Malaysia to prevent fits and incessant crying by babies. The aim of this study was to investigate the nutritive composition and antioxidant potential and anti-inflammatory effects of A. rugosum extracts on LPS-stimulated RAW264.7 cells. Nutritional analysis of freeze-dried mycelia of A. rugosum (KUM 61131 from submerged culture indicated a predominant presence of carbohydrates, proteins, dietary fibre, phosphorus, potassium, and sodium. The ethanol crude extract (EE, its hexane (HF, ethyl acetate (EAF, and aqueous (AF fractions of mycelia of A. rugosum grown in submerged culture were evaluated for antioxidant potential and anti-inflammatory effects. EAF exhibited the highest total phenolic content and the strongest antioxidant activity based on 2,2-diphenyl-1-picrylhydrazyl (DPPH and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS assays. HF showed dose-dependent inhibition of NO production in LPS-stimulated RAW264.7 cells and NO radical scavenging activity. Gas chromatographic analysis of HF revealed the presence of ethyl linoleate and ergosterol, compounds with known anti-inflammatory properties. In conclusion, the nutritive compositions and significant antioxidant potential and anti-inflammatory effects of mycelia extracts of A. rugosum have the potential to serve as a therapeutic agent or adjuvant in the management of inflammatory disorders.

  6. Study of anti-inflammatory activities of α-D-glucosylated eugenol.

    Science.gov (United States)

    Zhang, Peng; Zhang, Erli; Xiao, Min; Chen, Chang; Xu, Weijian

    2013-01-01

    Inflammation is an immune response against a variety of noxious stimuli, such as infection, chemicals, and physical injury. Eugenol, a natural phenolic extract, has drawn much attention for its various desirable pharmacological functions and is, therefore, broadly used in our daily life and medical practice. However, further usage of eugenol is greatly limited due to its unwanted properties, such as physicochemical instability, poor solubility, and high-dose cytotoxicity. In hopes of extending its applicability through glycosylation, we previously reported a novel, efficient, and high throughput way to biosynthesize α-D-glucosylated eugenol (α-EG). In this study, we further explored the potential superior properties of α-EG to its parent eugenol in terms of anti-inflammatory activities. We demonstrated that α-EG was an effective anti-inflammatory mediator in both non-cellular and cellular environments. In addition, the non-cellular inhibitory effect of α-EG could be amplified by α-glucosidase, which ubiquitously exists in cytoplasm. Furthermore, α-EG exhibited a superior anti-inflammatory effect to its parent eugenol in a cellular environment. In words, our findings collectively suggest that α-EG is a stronger anti-inflammatory mediator and may thereby serve as a desirable substitute for eugenol and a potential therapeutic prodrug in treating inflammatory diseases in the future.

  7. Feijoa sellowiana Berg fruit juice: anti-inflammatory effect and activity on superoxide anion generation.

    Science.gov (United States)

    Monforte, Maria T; Fimiani, Vincenzo; Lanuzza, Francesco; Naccari, Clara; Restuccia, Salvatore; Galati, Enza M

    2014-04-01

    Feijoa sellowiana Berg var. coolidge fruit juice was studied in vivo for the anti-inflammatory activity by carrageenin-induced paw edema test and in vitro for the effects on superoxide anion release from neutrophils in human whole blood. The fruit juice was analyzed by the high-performance liquid chromatography method, and quercetin, ellagic acid, catechin, rutin, eriodictyol, gallic acid, pyrocatechol, syringic acid, and eriocitrin were identified. The results showed a significant anti-inflammatory activity of F. sellowiana fruit juice, sustained also by an effective antioxidant activity observed in preliminary studies on 1,1-diphenyl-2-picrylhydrazyl (DPPH) test. In particular, the anti-inflammatory activity edema inhibition is significant since the first hour (44.11%) and persists until the fifth hour (44.12%) of the treatment. The effect on superoxide anion release was studied in human whole blood, in the presence of activators affecting neutrophils by different mechanisms. The juice showed an inhibiting response on neutrophils basal activity in all experimental conditions. In stimulated neutrophils, the higher inhibition of superoxide anion generation was observed at concentration of 10(-4) and 10(-2) mg/mL in whole blood stimulate with phorbol-myristate-13-acetate (PMA; 20% and 40%) and with N-formyl-methionyl-leucyl-phenylalanine (FMLP; 15% and 48%). The significant reduction of edema and the inhibition of O2(-) production, occurring mainly through interaction with protein-kinase C pathway, confirm the anti-inflammatory effect of F. sellowiana fruit juice. PMID:24433073

  8. Antinociceptive anti-inflammatory effect of Monotropein isolated from the root of Morinda officinalis.

    Science.gov (United States)

    Choi, Jongwon; Lee, Kyung-Tae; Choi, Moo-Young; Nam, Jung-Hwan; Jung, Hyun-Ju; Park, Sun-Kyu; Park, Hee-Juhn

    2005-10-01

    The root of Morinda officinalis (Rubiaceae) is used to treat rheumatoid arthritis and impotence in the traditional Oriental medicine. To identify the antinociceptive anti-inflammatory components of this crude drug, we adopted an activity-directed fractionation approach. The active fraction of the BuOH extract of M. officinalis root was subjected to silica gel and ODS column chromatography to yield two diterpenes, compounds 1 and 2 and these were identified as monotropein and deacetylasperulosidic acid, respectively. The iridoid glycoside, monotropein, was tested for its anti-inflammatory antinociceptive effects using hot plate- and writhing antinociceptive assays and by using carrageenan-induced anti-inflammatory assays in mice and rats. Pretreatment with monotropein (at 20, 30 mg/kg/d, p.o.) significantly reduced stretching episodes and prolonged action time in mice. It also significantly reduced acute paw edema by carrageenan in rats. These results indicate that monotropein contributes to the antinociceptive and anti-inflammatory action of Morinda officinalis root. PMID:16204945

  9. New Concept of Neural Stem Cell Transplantation: Anti-inflammatory Role

    OpenAIRE

    Lee, Soon-Tae; Chu, Kon; Park, Hee-Kwon; Jung, Keun-Hwa; Kim, Manho; Lee, Sang Kun; Roh, Jae-Kyu

    2008-01-01

    Neural stem cells (NSCs) transplantation has been studied as a promising tool for replacing damaged neurons in various neurological disorders. However, recent growing data showed new therapeutic benefits of NSCs, which is that transplanted NSCs can modulate cerebral inflammation and protect the brain from further degeneration. We review recent discoveries regarding to the anti-inflammatory effects of NSCs and their future perspectives.

  10. Novel coumarin-benzimidazole derivatives as antioxidants and safer anti-inflammatory agents.

    Science.gov (United States)

    Arora, Radha Krishan; Kaur, Navneet; Bansal, Yogita; Bansal, Gulshan

    2014-10-01

    Inspired from occurrence of anti-inflammatory activity of 3-substituted coumarins and antiulcer activity of various 2-substituted benzimidazoles, novel compounds have been designed by coupling coumarin derivatives at 3-position directly or through amide linkage with benzimidazole nucleus at 2-position. The resultant compounds are expected to exhibit both anti-inflammatory and antioxidant activities along with less gastric toxicity profile. Two series of coumarin-benzimidazole derivatives (4a-e and 5a-e) were synthesized and evaluated for anti-inflammatory activity and antioxidant activity. Compounds 4c, 4d and 5a displayed good anti-inflammatory (45.45%, 46.75% and 42.85% inhibition, respectively, versus 54.54% inhibition by indomethacin) and antioxidant (IC50 of 19.7, 13.9 and 1.2 µmol/L, respectively, versus 23.4 µmol/L for butylatedhydroxytoluene) activities. Evaluation of ulcer index and in vivo biochemical estimations for oxidative stress revealed that compounds 4d and 5a remain safe on gastric mucosa and did not induce oxidative stress in tissues. Calculation of various molecular properties suggests the compounds to be sufficiently bioavailable. PMID:26579406

  11. Anti-inflammatory activity of aqueous extract of Mirabilis jalapa Linn. leaves

    Directory of Open Access Journals (Sweden)

    Manjit Singh

    2010-01-01

    Full Text Available Background: The objective of the present study was to evaluate the anti-inflammatory activity of aqueous extract of Mirabilis jalapa Linn. (MJL (Nyctaginaceae leaves for scientific validation of the folklore claim of the plant. The leaves are used as traditional folk medicine in the south of Brazil to treat inflammatory and painful diseases. Cosmetic or dermo-pharmaceutical compositions containing MJL are claimed to be useful against inflammation and dry skin. Methods: Aqueous extract of the leaves was prepared by cold maceration. Results: The anti-inflammatory activity was evaluated using carrageenan and formalin-induced paw edema models in Wistar albino rats. The anti-inflammatory activity was found to be dose dependent in carrageenan-induced paw edema model. The aqueous extract has shown significant (P < 0.05 inhibition of paw oedema, 37.5% and 54.0% on 4 th hour at the doses of 200 and 400 mg/kg, respectively. Similar pattern of paw edema inhibition was seen in formalin-induced paw edema model. The maximum percentage inhibition in paw edema was 32.9% and 43.0% on 4 th day at the doses of 200 and 400 mg/kg, respectively. Conclusion: The results of present study demonstrate that aqueous extract of the leaves possess significant (P < 0.05 anti-inflammatory potential.

  12. Anti-inflammatory Effect of Sodium Valproate on Carrageenan-Induced Paw Edema in Male Rat

    Directory of Open Access Journals (Sweden)

    mj Khoshnood

    2008-12-01

    Full Text Available ABESTRACT: Introduction & objective: Inflammation is a body defensive response to the endogenous and exogenous stimulators such as chemical, radiation, trauma and invasive microorganism, which result pain and tissue necrosis. There are many natural and synthetic drugs for treatment of inflammation and lot of them are under investigation. Sodium valporate is an antiepileptic drug used particularly in the treatment of primary generalized seizure notably absence, myocolonic seizure, acute manic phase of bipolar disorder and prophylaxis of migraine. The previous observations showed sodium valporate increases level of gamma amino butyric acid (GABA in the central and peripheral nervous system. In acute inflammation, GABA showed a significant attenuation of paw edema and nociception. The aim of this study was evaluation of anti-inflammatory effect of sodium valporate. Materials & Methods: In order to evaluated the anti-inflammatory and antiexudative of sodium valporate doses of 200,400 and 600 mg/kg were investigated on rat paw edema that induced by carrageenan. In addition, the plasma leakage in the inflamed tissue was evaluated by application of trypan blue as intravenous injection. Dexamethason was used as positive control. Results: Results showed sodium valporate doses of 400 and 600 mg/kg decreased inflammatory and exudative effect as compared to control group. Conclusion: Although the anti-inflammatory mechanisms of this drug were not evident but we can say sodium valporate in addition to already proved effects has anti-inflammatory effect.

  13. Anti-inflammatory effect of the methanol extract from Anthocephalus cadamba stem bark in animal models

    Directory of Open Access Journals (Sweden)

    Kodangala Subraya Chandrashekar

    2010-02-01

    Full Text Available Background: Anthocephalus cadamba (ReboxMiq. (Rubiaceae is widely distributed throughout the greater part of India, especially at low levels in wet place. Traditionally the bark is used as tonic, febrifuge and to reduce the pain and inflammation. The anti-inflammatory effect of methanol extract obtained from  Anthocephalus cadamba  aerial parts, MEAC, were investigated in this study. Design and methods: The effects of MEAC on the acute and chronic phases of inflammation were studied in carrageenan, dextran and mediators (histamine and serotonin induced paw edema and cotton pallet-induced granuloma, respectively. The anti-edema effect of MEAC was compared with 10 mg/kg of indomethacin orally. Results: The results suggested that MEAC possess potent anti-inflammatory activity. The acute inflammatory model showed that all the doses of MEAC effectively suppressed the edema produced by histamine, so it may be suggested that its anti-inflammatory activity is possibly backed by its antihistaminic activity. In chronic inflammatory model the effect may be due to the cellular migration to injured sites and accumulation of collagen and mucopolysaccharide. Conclusions: On the basis of these findings, it may be inferred that  Anthocephalus cadamba  is an anti-inflammatory agent and the results are in agreement with its traditional use.

  14. Phytol: A chlorophyll component with anti-inflammatory and metabolic properties

    DEFF Research Database (Denmark)

    Olofsson, Peter; Hultqvist, Malin; Hellgren, Lars I.;

    2014-01-01

    The naturally occurring dipterpene molecule Phytol is an alcohol that can be extracted from the chlorophyll of green plants. Phytol has been studied for decades and has been suggested to have both metabolic properties as well as potent anti-inflammatory effects. Phytol represents a molecule derived...

  15. Anti-inflammatory activities of the hydroalcoholic extracts from Erythrina velutina and E. mulungu in mice

    Directory of Open Access Journals (Sweden)

    Silvânia M. M. Vasconcelos

    2011-12-01

    Full Text Available This work studied the anti-inflammatory activities of the hydroalcoholic extracts (HAEs from Erythrina velutina Willd. (Ev and E. mulungu Mart. ex Benth. (Em in the carrageenan- and dextran-induced mice hind paw edema models. These medicinal plants belonging to the Fabaceae family are used in some Brazilian communities to treat pain, inflammation, insomnia and disorders of the central nervous system. In the present work, the extracts were administered orally in male mice at the doses of 200 or 400 mg/kg. In the carrageenan-induced test, only Em showed anti-inflammatory activity, decreasing the paw edema, at the doses of 200 and 400 mg/kg. No effect was observed with Ev in this model. On the other hand, in the dextran model, Ev demonstrated anti-inflammatory effect, showing decrease of the paw edema at the 1, 2, 3, 4 and 24th h. Em (200 or 400 mg/kg presented anti-inflammatory effect at the 2, 3 and 4th h after administration of dextran, as compared to control. In conclusion, the work showed that Ev and Em present anti-edematous actions, which possibly occurs by distinct mechanisms. While Ev seems to interfere especially in inflammatory processes in which mast cells have an important role, Em exerts greater activity in the inflammatory process that depends mainly on polymorphonuclear leucocytes. However, further studies are needed to determine the exact mechanism of action of the species investigated.

  16. Smoking status and anti-inflammatory macrophages in induced sputum and bronchoalveolar lavage in COPD

    NARCIS (Netherlands)

    L.I. Kunz; T.S. Lapperre; J.B. Snoeck-Stroband; S.E. Budulac; W. Timens; S. van Wijngaarden; J.A. Schrumpf; K.F. Rabe; D.S. Postma; P.J. Sterk; P.S. Hiemstra

    2011-01-01

    ABSTRACT: BACKGROUND: Macrophages have been implicated in the pathogenesis of COPD. M1 and M2 macrophages constitute subpopulations displaying pro- and anti-inflammatory properties. We hypothesized that smoking cessation affects macrophage heterogeneity in the lung of patients with COPD. Our aim was

  17. Smoking status and anti-inflammatory macrophages in bronchoalveolar lavage and induced sputum in COPD

    NARCIS (Netherlands)

    Kunz, Lisette I Z; Lapperre, Thérèse S; Snoeck-Stroband, Jiska B; Budulac, Simona E; Timens, Wim; van Wijngaarden, Simone; Schrumpf, Jasmijn A; Rabe, Klaus F; Postma, Dirkje S; Sterk, Peter J; Hiemstra, Pieter S

    2011-01-01

    Background: Macrophages have been implicated in the pathogenesis of COPD. M1 and M2 macrophages constitute subpopulations displaying pro-and anti-inflammatory properties. We hypothesized that smoking cessation affects macrophage heterogeneity in the lung of patients with COPD. Our aim was to study m

  18. Neutrophilia and an Anti-Inflammatory Drug as Markers of Inflammation in Delayed Muscle Soreness.

    Science.gov (United States)

    Smith, Lucille L.; And Others

    This study reexamined the concept that delayed muscle soreness (DMS) is a form of inflammatory pain. This was accomplished by having 32 male volunteers perform exercise known to induce DMS and then assess the total and differential white blood cell changes. In addition, an anti-inflammatory drug, idomethacin, was administered to determine whether…

  19. Nonsteroidal anti-inflammatory drugs for low back pain - An updated Cochrane review

    NARCIS (Netherlands)

    Roelofs, Pepijn D. D. M.; Deyo, Rick A.; Koes, Bart W.; Scholten, Rob J. P. M.; van Tulder, Maurits W.

    2008-01-01

    Study Design. A systematic review of randomized controlled trials. Objectives. To assess the effects of nonsteroidal anti-inflammatory drugs (NSAIDs) and COX-2 inhibitors in the treatment of nonspecific low back pain and to assess which type of NSAID is most effective. Summary of Background Data. NS

  20. Comparative Evaluation of Anti-Inflammatory Activity of Curcuminoids, Turmerones, and Aqueous Extract of Curcuma longa

    Directory of Open Access Journals (Sweden)

    Ashish Subhash Bagad

    2013-01-01

    Full Text Available Curcuma longa is widely known for its anti-inflammatory activity in traditional system of medicine for centuries and has been scientifically validated extensively. The present study was conducted to evaluate the anti-inflammatory activity of curcuminoids and oil-free aqueous extract (COFAE of C. longa and compare it with that of curcuminoids and turmerones (volatile oil, the bioactive components of C. longa that are proven for the anti-inflammatory potential. The activity against inflammation was evaluated in xylene-induced ear edema, cotton pellet granuloma models in albino Swiss mice and albino Wistar rats, respectively. The results showed that COFAE of C. longa at three dose levels significantly (P≤0.05 inhibited inflammation in both models, as evidenced by reduction in ear weight and decrease in wet as well as dry weights of cotton pellets, when compared to the vehicle control. The COFAE of C. longa showed considerable anti-inflammatory effects against acute and chronic inflammation and the effects were comparable to those of curcuminoids and turmerones.

  1. Tissue Distribution and Anti-inflammatory Activity of DexamethasoneAcetate Incorporated In Lipid Emulsion

    Institute of Scientific and Technical Information of China (English)

    QuanDongqin; CuiGuanghua; DongHuajin; RuanJinxiu

    2001-01-01

    Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenousemulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection andLimethasone(Jepanese product) given intravenously were evaluated by using the preformed carrageenan granulomapouch method in rats. Results: The anti-inflammatory activity of dexamethasone acetate emulsion at low dose of 0.05mg.kg1 was as potent as dexamethasone sodium phosphate solution at high dose of 0.3 mg.kg1. The distributionpatterns in mice tissues of [3H]dexamethasone acetate emulsion and [3H]dexamethasone sodium phosphate solution inmice were markedly different. Dexamethasone acetate emulsion showed a much higher concentration in the liver,spleen, lung, and inflamed tissues, whereas dexamethasone sodium phosphate had a high concenti,mon in themuscles of vastus lateralis. These results may indicate that dexamethasone incoporated in lipid emulsion was taken upby the reticuloendothelial system and inflammatory cells much more than dexamethasone sodium phosphate solution.Conclusion: When dexamethasone acetate was incorporated in emulsion, the distribution patterns in tissues werechanged and they had a stronger anti-inflammatory activity.

  2. Pharmacognostic study and anti-inflammatory activity of Callistemon lanceolatus leaf

    Institute of Scientific and Technical Information of China (English)

    Kumar S; Kumar V; Prakash OM

    2011-01-01

    Objective: To study detail pharmacognosy and anti-inflammatory activity of Callistemonlanceolatus (C. lanceolatus) leaf. Methods: Leaf sample was studied by organoleptic, macroscopical, microscopical, phytochemical and other WHO recommended methods for standardizations. The methanolic leaf extract of the plant was also screened for anti-inflammatory activity on carrageenan-induced paw edema in rat at doses of 200 and 400 mg/kg, orally. The detail pharmacognostic study of the C. lanceolatus leaf was carried out to lay down the standards which could be useful in future experimental studies. Results: C. lanceolatus methanolic leaf extract showed significant (P<0.05) anti-inflammatory activity at doses of 200 mg/kg and 400 mg/kg. This significant anti-inflammatory of C. lanceolatus methanolic leaf extract at the dose of 400 mg/kg was comparable with diclofenac sodium. Conclusions: The pharmacognostic profile of the C. lanceolatus leaf is helpful in standardization for quality, purity and sample identification. The methanolic extract at a dose of 400 mg/kg shows a significant activity in comparison with the standard drug diclofenac sodium (50 mg/kg).

  3. A Novel Liposomal Dexamethasone Palmitate Formulation and Anti-inflammatory Effects on Mice

    Institute of Scientific and Technical Information of China (English)

    LI, Ji; YANG, Jing; WANG, Wenxin; YU, Jichen; FU, Jingguo; WANG, Xiaolai

    2009-01-01

    A novel dexamethasone palmitate liposomal long-circulating (DPL long-circulating) drug delivery system was established. The DPL long-circulating and DPL (dexamethasone palmitate liposomal) systems were prepared by film-distributed extrusion with phospholipid and cholesterol. The formulation stability of DPL long-circulating and DPL were investigated. The anti-inflammatory activity and acute toxicity of DPL long-circulating, DPL and dexa- methasone sodium phosphate injection (DSP) were evaluated with mice. The DPL long-circulating systems were successfully prepared by film-distributed extrusion methods. The experimental results showed that the DPL long-circulating had uniform particle size and stable property. The DPL long-circulating and DPL showed stronger anti-inflammatory effect than DSP in an anti-inflammatory test. Acute toxicity tests showed that DSP injection had lower toxicity than the DPL long-circulating and DPL, which suggested that DPL long-circulating and DPL had higher bioavailability with passive targeting efficacy of liposomes. The DPL long-circulating formulation product can meet quality requirement. This formulation had stronger anti-inflammatory effect and higher acute toxicity.

  4. Antioxidant and in vitro anti-inflammatory activities of Mimusops elengi leaves

    Institute of Scientific and Technical Information of China (English)

    Biswakanth Kar; RB Suresh Kumar; Indrajit Karmakar; Narayan Dolai; Asis Bala; Upal K Mazumder; Pallab K Haldar

    2012-01-01

    Objective: To assess the antioxidant and in vitro anti-inflammatory activities of the alcoholic extract of Mimusops elengi L (M. elengi) leaves. Methods: In vitro antioxidant activity was evaluated for peroxynitrite, superoxide and hypochlorous acid scavenging activity. Total phenolic content also determined. Inhibition of protein denaturation and HRBC (Human Red Blood Cell) membrane stabilization method was evaluated for anti-inflammatory activity. Results: The leave extract of M. elengi exhibited dose dependent free radical scavenging property in peroxynitrite, superoxide and hypochlorous acid models and the IC50 value were found to be (205.53 ± 2.30), (60.5±2.3), (202.4±5.3) μg/mL respectively. Total phenolic content was found to be 97.3 μg/mg of extract. The maximum membrane stabilization of M. elengi L was found to be (73.85±0.80)% at a dose of 1 000 μg/0.5 mL and that of protein denaturation was found to be 86.23% at a dose of 250 μg/mL with regards to standards in the anti-inflammatory activity. Conclusion: From the result it can conclude that M. elengi extract show good antioxidant and in vitro anti -inflammatory activities.

  5. Do nonsteroidal anti-inflammatory drugs decrease the risk for Alzheimer's disease?

    DEFF Research Database (Denmark)

    Andersen, K; Launer, L J; Ott, A;

    1995-01-01

    Based on reports that the use of nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the risk for Alzheimer's disease (AD), we studied the cross-sectional relation between NSAID use and the risk for AD in a population-based study of disease and disability in older people. After controlling...

  6. Anti-inflammatory effects of nicotine in obesity and ulcerative colitis

    Directory of Open Access Journals (Sweden)

    Kirchgessner Annette

    2011-08-01

    Full Text Available Abstract Cigarette smoke is a major risk factor for a number of diseases including lung cancer and respiratory infections. Paradoxically, it also contains nicotine, an anti-inflammatory alkaloid. There is increasing evidence that smokers have a lower incidence of some inflammatory diseases, including ulcerative colitis, and the protective effect involves the activation of a cholinergic anti-inflammatory pathway that requires the α7 nicotinic acetylcholine receptor (α7nAChR on immune cells. Obesity is characterized by chronic low-grade inflammation, which contributes to insulin resistance. Nicotine significantly improves glucose homeostasis and insulin sensitivity in genetically obese and diet-induced obese mice, which is associated with suppressed adipose tissue inflammation. Inflammation that results in disruption of the epithelial barrier is a hallmark of inflammatory bowel disease, and nicotine is protective in ulcerative colitis. This article summarizes current evidence for the anti-inflammatory effects of nicotine in obesity and ulcerative colitis. Selective agonists for the α7nAChR could represent a promising pharmacological strategy for the treatment of inflammation in obesity and ulcerative colitis. Nevertheless, we should keep in mind that the anti-inflammatory effects of nicotine could be mediated via the expression of several nAChRs on a particular target cell.

  7. DMPD: Endogenous anti-inflammatory substances, inter-alpha-inhibitor and bikunin. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 17132099 Endogenous anti-inflammatory substances, inter-alpha-inhibitor and bikunin.... Kobayashi H. Biol Chem. 2006 Dec;387(12):1545-9. (.png) (.svg) (.html) (.csml) Show Endogenous anti-inflam...matory substances, inter-alpha-inhibitor and bikunin. PubmedID 17132099 Title Endogenous anti-inflammatory s

  8. Anti-inflammatory activity of some extracts and isolates from leonotis nepetaefolia on TPA-induced edema model

    OpenAIRE

    Hortensia Parra Delgado; Gabriela García Ruiz; Antonio Nieto Camacho; Mariano Martínez Vázquez

    2004-01-01

    Several extracts of aerial parts of Leonotis nepetaefolia showed anti-inflammatory activity on TPA-induced edema model. The chromatography of the extracts led to the isolation of stigmasterol and leonotinin. Although the presence of leonotinin is in agreement with previous phytochemical studies of this species, this is the first time that its anti-inflammatory activity is determined.

  9. Cardioprotective and anti-inflammatory effects of treatment with Adenocaine/Mg2+ in a porcine model of endotoxemia

    DEFF Research Database (Denmark)

    Granfeldt, Asger

    Cardioprotective and anti-inflammatory effects of treatment with Adenocaine/Mg2+ in a porcine model of endotoxemia American Heart Scientific sessions Resuscitation Science symposium 16-20 November......Cardioprotective and anti-inflammatory effects of treatment with Adenocaine/Mg2+ in a porcine model of endotoxemia American Heart Scientific sessions Resuscitation Science symposium 16-20 November...

  10. DMPD: Molecular aspects of anti-inflammatory action of G-CSF. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 12005202 Molecular aspects of anti-inflammatory action of G-CSF. Boneberg EM, Hartu...ng T. Inflamm Res. 2002 Mar;51(3):119-28. (.png) (.svg) (.html) (.csml) Show Molecular aspects of anti-infla...mmatory action of G-CSF. PubmedID 12005202 Title Molecular aspects of anti-inflammatory action of G-CSF. Aut

  11. New Isorhamnetin Derivatives from Salsola imbricata Forssk. Leaves with Distinct Anti-inflammatory Activity

    Science.gov (United States)

    Osman, Samir M.; El Kashak, Walaa A.; Wink, Michael; El Raey, Mohamed A.

    2016-01-01

    Background: Salsola imbricata Forssk. is a shrub widely growing in Egypt, used as a camel food, traditionally, used as anti-inflammatory agent. Literature survey showed no report about the anti-inflammatory activity of S. imbricata. Aim of the Study: This work was designed to study the phenolic constituents and to provide evidence for the traditional use of S. imbricata as an anti-inflammatory agent. Materials and Methods: The in vitro anti-inflammatory activity of the total aqueous methanol extract and some isolated compounds were investigated in RAW 264.7 macrophage cells using nitric oxide assay. All chemical structures were identified on the basis of electrospray ionization-mass spectrometry, one- and two-dimension nuclear magnetic resonance. Results: Nine phenolic compounds, among them two new natural products; isorhamnetin-3-O-β-D-glucuronyl (1’’’→4’’) glucuronide (1) and its dimethyl ester; isorhamnetin-3-O-β-D-di glucuronate dimethyl ester (2), two isorhamnetin glycosides: Isorhamnetin-3-O-β-D-galactopyranoside (3), isorhamnetin-3-O-β-D-glucopyranoside (4), and isorhamnetin (5). In addition, an alkaloidal phenolic; trans N-feruloyl tyramine (6), three phenolic acids: Isovanillic acid (7), ferulic acid (8), and p-hydroxy benzoic acid (9) were isolated from salsola imbricata leaves. All compounds were isolated and identified for the first time from this plant except compound (6). The extract and the tested compounds showed distintict anti-inflammatory activities with no toxicity on RAW 264.7 macrophage cells. Conclusion: The extract and the tested compounds showed distintict anti-inflammatory activities with no toxicity on RAW 264.7 macrophage cells. SUMMARY Investigation of the chemical constituents of the leaves of Salsola imbricata led to isolation of two new isorhamnetin derivatives: isorhamnetin.3-O-β-D.glucuronyl (1’“→”) glucuronide (1) and its dimethyl ester (2), together with seven known phenolic compounds. The extract and the

  12. Sucrose esters from Physalis peruviana calyces with anti-inflammatory activity.

    Science.gov (United States)

    Franco, Luis A; Ocampo, Yanet C; Gómez, Harold A; De la Puerta, Rocío; Espartero, José L; Ospina, Luis F

    2014-11-01

    Physalis peruviana is a native plant from the South American Andes and is widely used in traditional Colombian medicine of as an anti-inflammatory medicinal plant, specifically the leaves, calyces, and small stems in poultice form. Previous studies performed by our group on P. peruviana calyces showed potent anti-inflammatory activity in an enriched fraction obtained from an ether total extract. The objective of the present study was to obtain and elucidate the active compounds from this fraction and evaluate their anti-inflammatory activity in vivo and in vitro. The enriched fraction of P. peruviana was purified by several chromatographic methods to obtain an inseparable mixture of two new sucrose esters named peruviose A (1) and peruviose B (2). Structures of the new compounds were elucidated using spectroscopic methods and chemical transformations. The anti-inflammatory activity of the peruvioses mixture was evaluated using λ-carrageenan-induced paw edema in rats and lipopolysaccharide-activated peritoneal macrophages. Results showed that the peruvioses did not produce side effects on the liver and kidneys and significantly attenuated the inflammation induced by λ-carrageenan in a dosage-dependent manner, probably due to an inhibition of nitric oxide and prostaglandin E2, which was demonstrated in vitro. To our knowledge, this is the first report of the presence of sucrose esters in P. peruviana that showed a potent anti-inflammatory effect. These results suggest the potential of sucrose esters from the Physalis genus as a novel natural alternative to treat inflammatory diseases. PMID:25338213

  13. Development and mechanism investigation of a new piperlongumine derivative as a potent anti-inflammatory agent.

    Science.gov (United States)

    Sun, Lan-Di; Wang, Fu; Dai, Fang; Wang, Yi-Hua; Lin, Dong; Zhou, Bo

    2015-06-01

    Inflammation, especially chronic inflammation, is directly involvement in the pathogenesis of many diseases including cancer. An effective approach for managing inflammation is to employ chemicals to block activation of nuclear factor-κB (NF-κB), a key regulator for inflammatory processes. Piperlongumine (piplartine, PL), an electrophilic molecule isolated from Piper longum L., possesses excellent anti-cancer and anti-inflammatory properties. In this study, a new PL analogue (PL-0N) was designed by replacing nitrogen atom of lactam in PL with carbon atom to increase its electrophilicity and thus anti-inflammatory activity. It was found that PL-0N is more potent than the parent compound in suppressing lipopolysaccharide (LPS)-induced secretion of nitric oxide and prostaglandin E2 as well as expression of inducible nitric oxide synthase and cyclooxygenase-2 in RAW264.7 macrophages. Mechanistic investigation implies that PL-0N exerts anti-inflammatory activity through inhibition of LPS-induced NF-κB transduction pathway, down-regulation of LPS-induced MAPKs activation and impairment of proteasomal activity, but also enhancement of LPS-induced autophagy; the inhibition of NF-κB by PL-0N is achieved at various stages by: (i) preventing phosphorylation of IKKα/β, (ii) stabilizing the suppressor protein IκBα, (iii) interfering with the nuclear translocation of NF-κB, and (iv) inhibiting the DNA-binding of NF-κB. These data indicate that nitrogen-atom-lacking pattern is a successful strategy to improve anti-inflammatory property of PL, and that the novel molecule, PL-0N may be served as a promising lead for developing natural product-directed anti-inflammatory agents. PMID:25850000

  14. Novel 2,5-disubstituted-1,3,4-oxadiazoles as anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Ega Durgashivaprasad

    2014-01-01

    Full Text Available Objective: 1,3,4-oxadiazole ring is a versatile moiety with a wide range of pharmacological properties. The present work deals with the synthesis and evaluation of the anti-inflammatory activity of two novel 2,5-disubstituted-1,3,4-oxadiazoles (OSD and OPD. Materials and Methods: Carrageenan-induced rat hind paw edema was employed as an acute model of inflammation. For evaluating sub-acute anti-inflammatory activity, carrageenan-induced inflammation in rat air pouch was employed. Complete Freund′s adjuvant-induced arthritis in rats was used as a model of chronic inflammation. To evaluate in vitro anti-inflammatory activity, lipopolysaccharide (LPS-stimulated RAW264.7 cells were used. Results: OSD (100 mg/kg reduced carrageen-induced paw edema by 60%, and OPD (100 mg/kg produced a modest 32.5% reduction. OSD also reduced leukocyte influx and myeloperoxidase in carrageenan-induced rat air pouch model. In complete Freund′s adjuvant-induced arthritis model, both OSD and OPD (200 mg/kg for 14 days reduced paw edema and NO levels. In LPS-stimulated RAW264.7 cells, OSD and OPD inhibited formation of nitric oxide and reactive oxygen species, with OPD showing a better activity in comparison to OSD. Conclusions: OSD was the better of the two compounds in in vivo models of inflammation. The o-phenol substitution at position 2 of oxadiazole ring in OSD may be responsible for its better in vivo anti-inflammatory activity. The ability of the compounds to inhibit LPS-induced pro-inflammatory mediator release suggests an anti-inflammatory mechanism targeting LPS-TLR4-NF-κB signalling pathway, which needs to be explored in detail. The disparate efficacy in vitro and in vivo also requires in-depth evaluation of the pharmacokinetics of these novel oxadiazoles.

  15. Phytochemical study and evaluation of anti-inflammatory activity of Aeschynomene fluminensis Vell. (Fabaceae); Estudo fitoquimico e avaliacao da atividade anti-inflamatoria de Aeschynomene fluminensis Vell. (Fabaceae)

    Energy Technology Data Exchange (ETDEWEB)

    Ignoato, Marlene Capelin; Fabrao, Rodrigo Monteiro; Schuquel, Ivania Teresinha Albrecht; Botelho, Marcos Felipe Pinatto; Santin, Silvana Maria de Oliveira [Universidade Estadual de Maringa (UEM) PR (Brazil). Dept. de Quimica; Arruda, Laura Licia Milani de; Bersani-Amado, Ciomar Aparecida [Universidade Estadual de Maringa (UEM) PR (Brazil). Dept. de Farmacologia e Terapeutica; Souza, Maria Conceicao de, E-mail: smoliveira@uem.br [Universidade Estadual de Maringa (UEM) PR (Brazil). Dept. de Biologia

    2012-07-01

    Phytochemical investigation of Aeschynomene fluminensis leaves and branches led to isolation of the flavonoid glycosides kaempferol 3,7-di-O-{alpha}-L-rhamnopyranoside, kaempferol 7-O-{alpha}-L-rhamnopyranoside, kaempferol 3-O-apiofuranosil-7-O- rhamnopyranoside, quercetin 3-O-{alpha}-L-rhamnopyranoside, quercetin 3-O-arabinofuranoside, 8-{beta}-D-glucopyranosyl 4',5,7-trihydroxyflavanone, the isoflavonoid 4',7-di-hydroxy-isoflavone, the dimer epicatechin-(2{beta} ->7, 4{beta} ->8)- epicatechin, the polyol 3-O-methyl-chiro-inositol and two steroids in sitosterol and stigmasterol mixture. These compounds were identified by NMR {sup 1}H and {sup 13}C and compared with literature data. Anti-inflammatory activity of the crude methanolic extract and its fractions was evaluated (author)

  16. Inflammatory Kinetics and Efficacy of Anti-inflammatory Treatments on Human Nucleus Pulposus Cells

    Science.gov (United States)

    Walter, Benjamin A; Purmessur, Devina; Likhitpanichkul, Morakot; Weinberg, Alan; Cho, Samuel K.; Qureshi, Sheeraz A.; Hecht, Andrew C.; Iatridis, James C.

    2015-01-01

    Study Design Human nucleus pulposus (NP) cell culture study investigating response to tumor necrosis factor-α (TNFα), effectiveness of clinically available anti-inflammatory drugs, and interactions between pro-inflammatory cytokines. Objective To characterize the kinetic response of pro-inflammatory cytokines released by human NP cells to TNFα stimulation and the effectiveness of multiple anti-inflammatories with 3 sub-studies: Timecourse, Same-time blocking, Delayed blocking. Summary of Background Data Chronic inflammation is a key component of painful intervertebral disc (IVD) degeneration. Improved efficacy of anti-inflammatories requires better understanding of how quickly NP cells produce pro-inflammatory cytokines and which pro-inflammatory mediators are most therapeutically advantageous to target. Methods Degenerated human NP cells (n=10) were cultured in alginate with or without TNFα (10ng/mL). Cells were incubated with one of four anti-inflammatories (anti-IL-6 receptor/atlizumab, IL-1 receptor anatagonist, anti-TNFα/infliximab and sodium pentosan polysulfate/PPS) in two blocking-studies designed to determine how intervention timing influences drug efficacy. Cell viability, protein and gene expression for IL-1β, IL-6 & IL-8 were assessed. Results Timecourse: TNFα substantially increased the amount of IL-6, IL-8 & IL-1β, with IL-1β and IL-8 reaching equilibrium within ~72 hours (IL-1β: 111±40pg/mL, IL-8: 8478±957pg/mL), and IL-6 not reaching steady state after 144 hours (1570±435 pg/mL). Anti-TNFα treatment was most effective at reducing the expression of all cytokines measured when added at the same time as TNFα stimulation. Similar trends were observed when drugs were added 72 hours after TNFα stimulation, however, no anti-inflammatories significantly reduced cytokine levels compared to TNF control. Conclusion IL-1β, IL-6 and IL-8 were expressed at different rates and magnitudes suggesting different roles for these cytokines in disease

  17. Anti-inflammatory activity of aqueous leaf extract of Chromolaena odorata.

    Science.gov (United States)

    Owoyele, Victor B; Adediji, Joseph O; Soladoye, Ayodele O

    2005-01-01

    The anti-inflammatory activity of the aqueous extract of Chromolaena odorata was investigated in rats using the carrageenan-induced oedema, cotton pellet granuloma and formalin-induced oedema methods. The extract was administered orally at doses of 25, 50, 100 and 200 mg/kg. In the carrageenan method the paw oedema was significantly reduced by all the doses of the extract administered, with the 200 mg/kg dose producing the highest oedema inhibition (80.5%). In the cotton pellet method, granuloma weight was significantly reduced from 14 +/- 0.1 to 9.0 +/- 0.1 mg, while in the formaldehyde induced arthritis the extract inhibited the oedema during the 10-day period. In conclusion, this study has established the anti-inflammatory activity of C. odorata and, thus, justifies the traditional uses of the plant in the treatment of wounds and inflammation. PMID:16280100

  18. Hepatoprotective and anti-inflammatory effects of a traditional medicinal plant of Chile, Peumus boldus.

    Science.gov (United States)

    Lanhers, M C; Joyeux, M; Soulimani, R; Fleurentin, J; Sayag, M; Mortier, F; Younos, C; Pelt, J M

    1991-04-01

    Dried hydro-alcoholic extract of Peumus boldus (Monimiaceae) has been evaluated for hepatoprotective, choleretic and anti-inflammatory effects in mice and rats, in order to validate or to invalidate traditional therapeutic indications. This extract exerted a significant hepatoprotection of tert-butyl hydroperoxide-induced hepatotoxicity in isolated rat hepatocytes (in vitro technique) by reducing the lipid peroxidation and the enzymatic leakage of LDH; this in vitro efficacy was reinforced by a significant hepatoprotection on CCl4-induced hepatotoxicity in mice (in vivo technique), the plant extract reducing the enzymatic leakage of ALAT. Boldine, the main alkaloid of P. boldus appears to be implicated in this hepatoprotective activity. Choleretic effects, often mentioned in traditional indications, have not been confirmed in rats. Finally, significant and dose-dependent anti-inflammatory effects were obtained on an acute inflammatory process (carrageenan-induced edema test in rats). Boldine does not appear to be involved in such properties. PMID:1891491

  19. Anti-inflammatory effects of hyaluronan in arthritis therapy: Not just for viscosity

    Directory of Open Access Journals (Sweden)

    Kayo Masuko

    2009-04-01

    Full Text Available Kayo Masuko1, Minako Murata2, Kazuo Yudoh2, Tomohiro Kato1, Hiroshi Nakamura31Department of Biochemistry; 2Institute of Medical Science, St. Marianna University School of Medicine, Kawasaki-shi, Kanagawa, Japan; 3Department of Joint Disease and Rheumatism, Nippon Medical School, Bunkyo-ku, Tokyo, JapanAbstract: Hyaluronic acid (HA has been widely used for viscosupplementation of diseased or aged articular joints. However, recent investigations have revealed the active anti-inflammatory or chondroprotective effect of HA, suggesting its potential role in attenuation of joint damage. In particular, interactions between HA and other inflammatory mediators are attracting interest. This review summarizes several aspects of recent investigations of the anti-inflammatory effects of HA in arthritis.Keywords: hyaluronan, inflammation, chondroprotection

  20. A novel anti-inflammatory role of NCAM-derived mimetic peptide, FGL

    DEFF Research Database (Denmark)

    Downer, Eric J; Cowley, Thelma R; Lyons, Anthony;

    2010-01-01

    novel anti-inflammatory agent. Administration of FGL to aged rats attenuated the increased expression of markers of activated microglia, the increase in pro-inflammatory interleukin-1beta (IL-1beta) and the impairment in long-term potentiation (LTP). We report that the age-related increase in microglial......Age-related cognitive deficits in hippocampus are correlated with neuroinflammatory changes, typified by increased pro-inflammatory cytokine production and microglial activation. We provide evidence that the neural cell adhesion molecule (NCAM)-derived mimetic peptide, FG loop (FGL), acts as a...... CD200 in vitro. We provide evidence that the increase in CD200 is reliant on IL-4-induced extracellular signal-regulated kinase (ERK) signal transduction. These findings provide the first evidence of a role for FGL as an anti-inflammatory agent and identify a mechanism by which FGL controls...