WorldWideScience

Sample records for anti-inflammatory steroidal antedrugs

  1. 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)....

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

    Directory of Open Access Journals (Sweden)

    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.

  3. Non-steroidal anti-inflammatory drugs and hypertension.

    Science.gov (United States)

    Zheng, Liuying; Du, Xinping

    2014-06-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are frequently used to alleviate pain of the patients who suffer from inflammatory conditions like rheumatoid arthritis, osteoarthritis, and other painful conditions like gout. This class of drugs works by blocking cyclooxgenases which in turn block the prostaglandin production in the body. Most often, NSAIDs and antihypertensive drugs are used at the same time, and their use increases with increasing age. Moreover, hypertension and arthritis are common in the elderly patients requiring pharmacological managements. An ample amount of studies put forth evidence that NSAIDs reduce the efficiency of antihypertensive drugs plus aggravate pre-existing hypertension or make the individuals prone to develop high blood pressure through renal dysfunction. This review will help doctors to consider the effects and risk factors of concomitant prescription of NSAIDs and hypertensive drugs.

  4. [Non steroidal anti-inflammatory drugs and rheumatic diseases].

    Science.gov (United States)

    Cossermelli, W; Pastor, E H

    1995-01-01

    Nonsteroidal anti-inflammatory drugs (NSAID) comprise an important class of medicaments that reduced the symptoms of inflamation in rheumatic disease. This article emphasizes similarities and class characteristics of the NSAID, mechanisms of action, and drug-interactions.

  5. The non-steroidal anti-inflammatory drug niflumic acid inhibits Candida albicans growth.

    Science.gov (United States)

    Baker, Andrew; Northrop, Frederick D; Miedema, Hendrik; Devine, Gary R; Davies, Julia M

    2002-01-01

    The non-steroidal anti-inflammatory drug niflumic acid was found to inhibit growth of the yeast form of Candida albicans. Niflumic acid inhibited respiratory oxygen uptake and it is hypothesised that this was achieved by cytosolic acidification and block of glycolysis. Inhibitory concentrations are compatible with current practice of topical application.

  6. 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

  7. Non-steroidal anti-inflammatory drugs for chronic low back pain

    NARCIS (Netherlands)

    W.T.M. Enthoven (Wendy); P.D.D.M. Roelofs; R.A. Deyo (Richard); M.W. van Tulder (Maurits); B.W. Koes (Bart)

    2016-01-01

    textabstractBackground: Chronic back pain is an important health problem. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat people with low back pain, especially people with acute back pain. Short term NSAID use is also recommended for pain relief in people with chronic back pa

  8. Effects of Non-Steroidal Anti-Inflammatory Drugs on the Gastrointestinal and Cardiovascular System

    NARCIS (Netherlands)

    G.M.C. Masclee (Gwen)

    2016-01-01

    markdownabstractNon-steroidal anti-inflammatory drugs (NSAIDs) are frequently used for pain relief and antiinflammatory purposes. They are often combined with proton pump inhibitors (PPIs), the most potent blockers of gastric acid secretion to reduce gastroduodenal complications of NSAID use. This t

  9. Non-steroidal Anti-inflammatory Drugs in Raptors

    Science.gov (United States)

    Oaks, J. Lindsay; Meteyer, Carol U.; Miller, R. Eric; Fowler, Murray E.

    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.

  10. Review article : the potential of combinational regimen with non-steroidal anti-inflammatory drugs in the chemoprevention of colorectal cancer

    NARCIS (Netherlands)

    Jalving, M; Koornstra, JJ; De Jong, S; De Vries, EGE; Kleibeuker, JH

    2005-01-01

    Non-steroidal anti-inflammatory drugs are chemopreventive agents in colorectal cancer. Non-steroidal anti-inflammatory drugs do not, however, offer complete protection against adenoma and carcinoma development. There is increasing interest in combining non-steroidal anti-inflammatory drugs with agen

  11. 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.

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

    OpenAIRE

    Brune K; Patrignani P

    2015-01-01

    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 compon...

  13. Non-steroidal anti-inflammatory drugs(NSAIDs and physiotherapy - a selective review

    Directory of Open Access Journals (Sweden)

    P. van der Bijl

    2002-02-01

    Full Text Available This paper presents a selective review on the non-steroidal anti-inflammatory drugs (NSAIDs. These drugs,which form the mainstay of treatment of a variety of musculoskeletal and rheumatic conditions, may facilitate the efficacy of and compliance with physiotherapy treatment.  Their mechanisms of action, adverse effects, various routes of administration, eg systemic versus topical, and the role that these drugs may play in physiotherapy practice  are discussed.

  14. 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.

  15. 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....

  16. Anti-inflammatory activity of aqueous extracts and steroidal sapogenins of Agave americana.

    Science.gov (United States)

    Peana, A T; Moretti, M D; Manconi, V; Desole, G; Pippia, P

    1997-06-01

    Lyophilized aqueous extracts obtained from Agave americana L (Agavaceae) collected in the north of Sardinia were characterized with regard to their steroidal sapogenin content. Extracts of A. americana and genins isolated from them were evaluated for anti-inflammatory properties by testing their effects on carrageenin-induced edema. The effect of orally administered genins on gastric mucous membranes was also assessed. Lyophilized extracts administered by the intraperitoneal route at doses equivalent to 200 and 300 mg/kg of fresh plant starting material, showed good anti-inflammatory activity. Doses of genins (total steroidal sapogenins, hecogenin and tigogenin) equivalent to the amount in the lyophilized extracts produced an antiedentatous effect which was much stronger and more efficacious than that obtained with an i.p. administration of 5 mg/kg of indomethacin or dexamethasone 21-phosphate at a dose equivalent to the molar content of hecogenin administered. At the doses used to evaluate the anti-inflammatory activity, the genins did not have any harmful effect on the gastric mucous membranes. Lesions occurred when significantly higher doses of hecogenin were given, but gastric damage was still less than that caused by the drugs used for comparative purposes.

  17. [Protection by zinc acexamate against gastric lesions induced by non-steroid anti-inflammatory agents].

    Science.gov (United States)

    Navarro, C; Bravo, L; Bulbena, O

    1993-03-01

    The ability of different non-steroidal anti-inflammatory drugs (diclofenac, indomethacin, ketoprofen, naproxen and piroxicam) to inhibit gastric prostaglandin E2 production in the rat was compared with their damaging potential on gastric mucosa. The influence of treatment with zinc acexamate (ZAC) on these two parameters was also determined. ZAC treatment significantly decreased the degree of gastric damage elicited by all the antiinflammatories tested. The experimental data confirm the complexity of the gastrolesive effect exerted by anti-inflammatory drugs and that only part of such effect would be related with their inhibition of prostaglandin synthesis. These results indicate that the gastroprotection of ZAC does not exclusively depend on the effect on the synthesis of prostaglandins by the gastric mucosa, yet it can additionally be exerted through alternative mechanisms.

  18. Non-steroidal Anti-inflammatory Drugs Ranking by Nondeterministic Assessments of Probabilistic Type

    Directory of Open Access Journals (Sweden)

    Madalina luiza MOLDOVEANU

    2012-09-01

    Full Text Available With a number of common therapeutic prescriptions, common mechanisms, common pharmacological effects - analgesic, antipyretic and anti-inflammatory (acetaminophen excepted, common side effects (SE (platelet dysfunction, gastritis and peptic ulcers, renal insufficiency in susceptible patients, water and sodium retention, edemas, nephropathies, and only a few different characteristics – different chemical structures, pharmacokinetics and different therapeutic possibility, different selectivities according to cyclooxygenase pathway 1 and 2, non-steroidal anti-inflammatory drugs (NSAIDs similarities are more apparent than differences. Being known that in a correct treatment benefits would exceed risks, the question “Which anti-inflammatory drug presents the lowest risks for a patient?” is just natural. By the Global Risk Method (GRM and the Maximum Risk Method (MRM we have determined the ranking of fourteen NSAIDs considering the risks presented by each particular NSAID. Nimesulide, Etoricoxib and Celecoxib safety level came superior to the other NSAIDs, whereas Etodolac and Indomethacin present an increased side effects risk.

  19. 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.

  20. Regioselective enzymatic synthesis of non-steroidal anti-inflammatory drugs containing glucose in organic media.

    Science.gov (United States)

    Wang, Na; Liu, Bo Kai; Wu, Qi; Wang, Jun Liang; Lin, Xian Fu

    2005-06-01

    Enzymatic transesterification of glucose with the vinyl ester of non-steroidal anti-inflammatory drugs (NSAIDs) was in organic media performed for synthesis of novel NSAIDs-glucose conjugates. Glucose was regioselectively acylated at the 6-hydroxyl group. The indomethacin-glucose conjugate and ketoprofen-glucose conjugate were produced by the catalysis of alkaline protease from Bacillus subtilis in the respective yields of 42% (over 48 h) and 63% (over 40 h). The etodolac-glucose conjugate was obtained in 26% yield (over 144 h) by lipase from Candida antarctica.

  1. 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.

  2. 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

  3. 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.

  4. 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...... at baseline, during graded 20-min exercise sessions at 25%, 50% and 75% of the maximal oxygen uptake rate, and subsequently during two 1-h recovery periods. Heart rate, arterial blood pressure, cardiac output and plasma catecholamines at rest and during exercise were not altered by indomethacin or nabumetone....... Indomethacin decreased urinary rates of excretion of 6-oxo-prostaglandin F(1alpha) (6-oxo-PGF(1alpha)) and thromboxane B(2) in all study periods. Nabumetone decreased 6-oxo-PGF(1alpha) excretion during and after exercise. Excretion rates for PGE(2) did not change. Neither indomethacin nor nabumetone changed...

  5. 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.

  6. 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.

  7. Cardiovascular pharmacogenetics of anti-thrombotic agents and non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Stitham, J; Vanichakarn, P; Ying, L; Hwa, J

    2014-01-01

    The use of antithrombotic agents, particularly antiplatelet drugs like aspirin and clopidogrel, has been instrumental in decreasing the risk for adverse cardiovascular events across a wide range of patients. However, despite the established benefits, the use of these medications remains suboptimal. There is a high degree of inter-individual variation in response to these treatments, whereby patients experience occlusive thromboembolic events, in spite of maintaining an appropriate treatment regimen. This has lead to the notion of antithrombotic "resistance" or "poor responders", which has been a growing concern amongst clinicians and other healthcare providers. Compounding this matter even further, reports of increased cardiovascular risk associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naproxen, have revealed additional and unforeseen contributors to myocardial infarction and stroke. With all medications, striking a balance between the potential risks and benefits seems more art than science at times. However, given their widespread use and critical cardiovascular implications, further emphasis has been placed on understanding factors influencing antithrombotic and NSAID therapies. A major aim in cardiovascular pharmacogenetics is the discovery of genetic biomarkers that will allow for prospective screening and individualized prediction of drug efficacy and adverse reactions for these medications (both alone and together) within the context of cardiovascular disease.

  8. 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.

  9. Transdermal enhancement effect and mechanism of iontophoresis for non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Zuo, Jing; Du, Lina; Li, Miao; Liu, Boming; Zhu, Weinan; Jin, Yiguang

    2014-05-15

    Iontophoresis is an important approach to improve transdermal drug delivery. However, The transdermal enhancement mechanism of iontophoresis was not well known. The relationship between the physicochemical properties of drugs and the transdermal enhancement effect of iontophoresis was revealed in this study. Non-steroidal anti-inflammatory drugs (NSAIDs) were used as the models, including aspirin, ibuprofen and indomethacin. Their oil-water partition coefficients were measured. The carbomer-based hydrogels of them were prepared. Iontophoresis significantly enhanced in vitro transdermal delivery across the rat skins. Strong lipophilicity could lead to high permeation of drugs. However, the dissociation extent (indicated as pKa) of drugs was the key factor to determine the transdermal enhancement effect of iontophoresis. The more dissociation the drugs were, the higher the transdermal enhancement effect of iontophoresis. The drug-loaded hydrogels combined with iontophoresis improved the treatment of rat raw's inflammatory syndrome. Iontophoresis significantly improved the drugs penetrating into the hypodermis, dermis and epidermis, more deeply than the application of drugs alone according to the experimental result of 5-carboxylfluorescein hydrogels. Iontophoresis led to the unordered arrangement of skin intercellular lipids, the significantly increased flowability and loose stratum corneum structure. Iontophoresis is a promising approach to improve transdermal drug delivery with safety and high efficiency.

  10. 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.

  11. Influence of non-steroidal anti-inflammatory drugs on Drosophila melanogaster longevity.

    Science.gov (United States)

    Danilov, Anton; Shaposhnikov, Mikhail; Shevchenko, Oksana; Zemskaya, Nadezhda; Zhavoronkov, Alex; Moskalev, Alexey

    2015-08-14

    Most age-related diseases and aging itself are associated with chronic inflammation. Thus pharmacological inhibition of inflammatory processes may be effective antiaging strategy. In this study we demonstrated that treatment of Drosophila melanogaster with 10 non-steroidal anti-inflammatory drugs (NSAIDs: CAY10404, aspirin, APHS, SC-560, NS-398, SC-58125, valeroyl salicylate, trans-resveratrol, valdecoxib, licofelone) leads to extension of lifespan, delays age-dependent decline of locomotor activity and increases stress resistance. The effect of the lifespan increase was associated with decrease of fecundity. Depending on the concentration, NSAIDs demonstrated both anti- and pro-oxidant properties in Drosophila tissues. However, we failed to identify clear correlation between antioxidant properties of NSAIDs and their pro-longevity effects. The lifespan extending effects of APHS, SC-58125, valeroyl salicylate, trans-resveratrol, valdecoxib, and licofelone were more pronounced in males, valdecoxib and aspirin - in females. We demonstrated that lifespan extension effect of NSAIDs was abolished in flies with defective genes involved in Pkh2-ypk1-lem3-tat2 pathway.

  12. 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.

  13. 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

  14. [Cardiovascular side effects of non-steroidal anti-inflammatory drugs in the light of recent recommendations. Diclofenac is not more dangerous].

    Science.gov (United States)

    Horváth, Viktor József; Tabák, Gy Ádám; Szabó, Gergely; Putz, Zsuzsanna; Koós, Csaba Géza; Lakatos, Péter

    2015-03-29

    Among their beneficial effects, non-steroidal anti-inflammatory drugs may also exert several side effects which depend on the dosage and the type of these medications. The most frequent gastrointestinal side effects usually develop shortly after the beginning of their administration, but others such as cardiovascular interactions (which are present much less frequently than gastrointestinal side effects) can also occur after the beginning of drug administration without a latency period. For a long-term treatment, non-steroidal anti-inflammatory drugs are most frequently used in the elderly population where patients typically have high cardiovascular risk and take other medicines, e.g. low dose acetylsalicylic acid that can interact with non-steroidal anti-inflammatory drugs; in this aspect diclofenac may cause less side effects. In this review, the authors briefly review cardiovascular side effects of non-steroidal anti-inflammatory drugs, the processes which potentially influence them, therapeutic consequences and their interaction with acetylsalicylic acid.

  15. Synthesis of modified steroids as a novel class of non-ulcerogenic, anti-inflammatory and anti-nociceptive agents.

    Science.gov (United States)

    Mohareb, Rafat M; Elmegeed, Gamal A; Abdel-Salam, Omar M E; Doss, Senot H; William, Marian G

    2011-01-01

    The identification of compounds able to treat both pain and inflammation with limited side effects is one of the prominent goals in biomedical research. This study aimed at the synthesis of new modified steroids with structures justifying non-ulcerogenic, anti-inflammatory and anti-nociceptive activities. The steroid derivatives were synthesized via straightforward and efficient methods and their structures were established based on the analytical and spectral data. The in vivo anti-inflammatory, anti-nociceptive and anti-ulcerogenic activities of some of these compounds were studied. The newly synthesized compounds 8b, 19b, 24 and 31a showed anti-inflammatory, anti-nociceptive and anti-ulcerogenic activity with various intensities. Oedema was significantly reduced by either dose 25 or 50 mg/kg of all tested compounds at 3 and 4 h post-carrageenan. Compound 19b was the most effective in alleviating thermal pain. The analgesic activity of either dose of the compounds 8b, 24, 31a as well as the high dose 19b was significantly higher than that for indomethacin (IND). Gastric mucosal lesions caused in the rats by the administration of 96% EtOH and IND were inhibited by all tested compounds administered at (50 mg/kg) dose in the study.

  16. 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

  17. Non-steroidal anti-inflammatory drugs affect the methotrexate transport in IEC-6 cells.

    Science.gov (United States)

    Sosogi, Aiko; Gao, Feng; Tomimatsu, Takashi; Hirata, Koji; Horie, Toshiharu

    2003-06-13

    Methotrexate (MTX) is used not only for the cancer chemotherapy but also for the treatment of rheumatic disease, often together with non-steroidal anti-inflammatory drugs (NSAIDs). MTX is actively cotransported with H(+) in the small intestine, mediated by a reduced folate carrier (RFC). The coadministration of some NSAIDs with MTX to rats caused a decrease of MTX absorption through the small intestine. This may be due to the uncoupling effect of oxidative phosphorylation of the NSAIDs. The present study investigated whether flufenamic acid, diclofenac and indomethacin, NSAIDs, decreased ATP content of rat-derived intestinal epithelial cell line IEC-6 cells and affected the MTX transport in IEC-6 cells. The MTX uptake in IEC-6 cells was dependent on medium pH and maximum around pH 4.5-5.5. The MTX uptake was composed of a transport inhibited by 4, 4'-diisothiocyanostilbene-2, 2'-disulfonic acid (DIDS) and a non-saturable one. The DIDS-sensitive component in the MTX uptake showed a saturation kinetics (Michaelis-Menten constant (Km): 3.91 +/- 0.52 microM, Maximum velocity (Vmax): 94.66 +/- 6.56 pmol/mg protein/5 min). The cellular ATP content in IEC-6 cells decreased significantly at 30 min after the cells were started to incubate with the NSAIDs (250 microM flufenamic acid, 500 microM diclofenac and 500 microM indomethacin). The MTX uptake in IEC-6 cells in the presence of the NSAIDs decreased with the reduction of cellular ATP content and showed a good correlation with the ATP content (correlation coefficient: 0.982). Thus it seems likely that the ATP content in IEC-6 cells with the NSAIDs decreased due to the uncoupling effect of oxidative phosphorylation of the NSAIDs, resulting in the inhibition of the secondary active transport of MTX in IEC-6 cells. The present results also suggest that IEC-6 cells are useful to evaluate the drug interaction relating to this carrier system.

  18. 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.

  19. 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.

  20. Mebendazole and a non-steroidal anti-inflammatory combine to reduce tumor initiation in a colon cancer preclinical model.

    Science.gov (United States)

    Williamson, Tara; Bai, Ren-Yuan; Staedtke, Verena; Huso, David; Riggins, Gregory J

    2016-10-18

    Inheritance of a gene mutation leads to the initiation of 5 to 10% of most cancers, including colon cancer cases. We developed a chemoprevention strategy using a novel combination of the non-steroidal anti-inflammatory (NSAID) sulindac plus the anthelminthic benzimidazole, mebendazole. This oral drug combination was effective in the ApcMin/+ mouse model of Familial Adenomatous Polyposis (FAP). Treatment with 35 mg/kg daily mebendazole reduced the number of intestinal adenomas by 56% (P = 0.0002), 160 ppm sulindac by 74% (P cancer patients using mebendazole either alone or in combination. The findings have implications for populations with moderate and above risk for developing cancer.

  1. Randomized trial of switching from prescribed non-selective non-steroidal anti-inflammatory drugs to prescribed celecoxib

    DEFF Research Database (Denmark)

    Macdonald, Thomas M; Hawkey, Chris J; Ford, Ian;

    2016-01-01

    BACKGROUND: Selective cyclooxygenase-2 inhibitors and conventional non-selective non-steroidal anti-inflammatory drugs (nsNSAIDs) have been associated with adverse cardiovascular (CV) effects. We compared the CV safety of switching to celecoxib vs. continuing nsNSAID therapy in a European setting...... primary events per 1000 patient-years exposure. There were only 15 adjudicated secondary upper gastrointestinal complication endpoints (0.078/100 patient-years on celecoxib vs. 0.053 on nsNSAIDs OT, 0.078 vs. 0.053 ITT). More gastrointestinal serious adverse reactions and haematological adverse reactions...

  2. 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...... are more effective in controlling postoperative inflammation after cataract surgery. We found high-quality evidence that topical NSAIDs are more effective than topical steroids in preventing PCME. The use of topical NSAIDs was not associated with an increased events. We recommend using topical NSAIDs...

  3. 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.

  4. Chemopreventive action of non-steroidal anti-inflammatory drugs on the inflammatory pathways in colon cancer.

    Science.gov (United States)

    Ghanghas, Preety; Jain, Shelly; Rana, Chandan; Sanyal, S N

    2016-03-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are emerging as novel chemopreventive agents against a variety of cancers owing to their capability in blocking the tumor development by cellular proliferation and by promoting apoptosis. Inflammation is principal cause of colon carcinogenesis. A missing link between inflammation and cancer could be the activation of NF-κB, which is a hallmark of inflammatory response, and is commonly detected in malignant tumors. Therefore, targeting pro-inflammatory cyclooxygenase enzymes and transcription factors will be profitable as a mechanism to inhibit tumor growth. In the present study, we have studied the role of various pro-inflammatory enzymes and transcription factors in the development of the 1,2-dimethylhydrazine dihydrochloride (DMH)-induced colorectal cancer and also observed the role of three NSAIDs, viz., Celecoxib, Etoricoxib and Diclofenac. Carcinogenic changes were observed in morphological and histopathological studies, whereas protein regulations of various biomolecules were identified by immunofluorescence analysis. Apoptotic studies was done by TUNEL assay and Hoechst/PI co-staining of the isolated colonocytes. It was found that DMH-treated animals were having an over-expression of pro-inflammatory enzymes, aberrant nuclear localization of activated cell survival transcription factor, NF-κB and suppression of anti-inflammatory transcription factor PPAR-γ, thereby suggesting a marked role of inflammation in the tumor progression. However, co-administration of NSAIDs has significantly reduced the inflammatory potential of the growing neoplasm.

  5. 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

    -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......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...... infarction, stroke or cardiovascular mortality was assessed in multivariable survival models. RESULTS: During follow-up (median 4.9 years) 6283 events occurred. The cardiovascular risk associated with overall NSAID use was significantly lower in RA patients than in controls (HR 1.22 (95% CI 1.09 to 1.37) vs...

  6. Sulindac, a non-steroidal anti-inflammatory drug, mediates breast cancer inhibition as an immune modulator.

    Science.gov (United States)

    Yin, Tao; Wang, Guoping; Ye, Tinghong; Wang, Yongsheng

    2016-01-18

    The cooperation of adaptive immunity with pharmacologic therapy influences cancer progression. Though non-steroidal anti-inflammatory drugs (NSAIDs) have a long history of cancer prevention, it is unclear whether adaptive immune system affects the action of those drugs. In present study, we revealed a novel immunological mechanism of sulindac. Our data showed that sulindac had substantial efficacy as a single agent against 4T1 murine breast cancer and prolonged the survival of tumor-bearing mice. However, in the athymic nude mice, sulindac treatment was ineffective. Further in vivo T cell subsets depletion experiments showed that CD8+ T lymphocytes deficiency reversed the anti-tumor effect of sulindac. In addition, sulindac significantly reduced M2 macrophages recruitment, cancer-related inflammation and tumor angiogenesis. Our results advance our understanding of the mechanisms of NSAIDs, and more importantly, this will provide insight into rational drug design or antitumor immunotherapy.

  7. Femtosecond dynamics of a non-steroidal anti-inflammatory drug (piroxicam) in solution: The involvement of twisting motion

    Science.gov (United States)

    Gil, Michał; Douhal, Abderrazzak

    2008-06-01

    In this contribution, we report on fast and ultrafast dynamics of a non-steroidal anti-inflammatory drug, piroxicam (PX), in methyl acetate (MAC) and triacetin (TAC), two solvents of different viscosities. The enol form of PX undergoes a femtosecond (shorter than 100 fs) electronically excited state intramolecular proton-transfer reaction to produce keto tautomers. These structures exhibit an internal twisting motion to generate keto rotamers in ˜2-5 ps, a time being longer in TAC. The transient absorption/emission spectrum is very broad indicating that the potential-energy surface at the electronically excited state is very flat, and reflecting the involvement of several coordinates along which the wavepacket of the fs-produced structures evolve.

  8. 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.

  9. 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...

  10. 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

  11. Molecular dynamics in liquid and glassy states of non-steroidal anti-inflammatory drug: ketoprofen.

    Science.gov (United States)

    Sailaja, U; Shahin Thayyil, M; Krishna Kumar, N S; Govindaraj, G

    2013-05-13

    Ketoprofen is a well known nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects. It acts by inhibiting the body's production of prostaglandin. The molecular mobility of amorphous ketoprofen has been investigated by broadband dielectric spectroscopy (BDS) covering wide temperature and frequency range. Multiple relaxation processes were observed. Besides the primary α-relaxation, one secondary relaxation, γ-have been identified. The γ-process visible in the dielectric spectra at very low temperature is non-JG relaxation, and has an activation energy E=37.91 kJ/mol typical for local mobility. Based on Ngai's coupling model smaller n or a larger Kohlrausch exponent (1-n) of the α-relaxation associated with larger τβ (Tg). In the case of ketoprofen we conclude that the secondary relaxation (β) emerging from intermolecular motions, is hidden under the dominant α-peak. The temperature dependence of the relaxation time of the α-process can be described over the entire measured range by a single Vogel-Fulcher-Tammann (VFT) equation. From VFT fits, the glass transition temperature (Tg) was estimated as 267.07 K, and a fragility or steepness index m=86.57 was calculated, showing that ketoprofen is a fragile glass former. Our differential scanning calorimetry (DSC) study shows that ketoprofen is a non-crystallizing compound. To confirm the hydrogen bond patterns of ketoprofen FTIR spectroscopy was applied in both crystalline and amorphous phases. Solubility test performed at 37 °C proved that amorphous phase is more soluble than the crystalline phase.

  12. 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.

  13. 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.

  14. 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.

  15. Non-steroidal anti-inflammatory drug, nabumetone, prevents indometacin-induced gastric damage via inhibition of neutrophil functions.

    Science.gov (United States)

    Ishiwata, Yoshiro; Okamoto, Masayuki; Yokochi, Shoji; Hashimoto, Hiroyuki; Nakamura, Takashi; Miyachi, Atsushi; Naito, Yuji; Yoshikawa, Toshikazu

    2003-02-01

    Nabumetone is a non-steroidal anti-inflammatory drug (NSAID). It works as a prodrug and is extensively metabolized to an active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). It is well known that neutrophil infiltration and activation are critical in the pathogenesis of NSAID-induced gastric injury, and nabumetone shows less incidence of gastrointestinal irritancy. We examined the effects of nabumetone on neutrophil activation and on indometacin-induced gastric damage. In the indometacin-induced gastric mucosal injury, rats were treated with indometacin and then nabumetone or 6MNA was orally administered. Nabumetone prevented gastric damage accompanied by the reduction of neutrophil infiltration into gastric mucosa, but such an effect was not observed with 6MNA. Nabumetone reduced the formyl methionyl leucyl phenylalanine (fMLP)-induced respiratory burst of human neutrophils to 30% of the control level in-vitro, but 6MNA did not. In addition, nabumetone prevented the fMLP-induced migration of neutrophils. Nabumetone did not inhibit O2- generation in the xanthine-xanthine oxidase system. These results suggest that nabumetone prevents gastric damage induced by the active metabolite, 6MNA, via the suppression of neutrophil activation in gastric mucosa.

  16. Distal bowel selectivity in the chemoprevention of experimental colon carcinogenesis by the non-steroidal anti-inflammatory drug nabumetone.

    Science.gov (United States)

    Roy, H K; Karolski, W J; Ratashak, A

    2001-05-15

    Use of non-steroidal anti-inflammatory drugs (NSAIDs) for chemoprevention of colon cancer has been hindered by their potential gastro-intestinal toxicity. Nabumetone, which is approximately 10 to 36 times safer than conventional NSAIDs, was evaluated in 2 models of experimental colon carcinogenesis. In azoxymethane (AOM)-treated Fisher 344 rats, nabumetone caused dose-dependent inhibition of aberrant crypt foci (ACF), with 750 and 1,500 ppm resulting in 15% and 37% reductions, respectively (p nabumetone, with 900 ppm suppressing approximately half of the intestinal tumors. Interestingly, inhibition of intermediate biomarkers in both models was markedly greater in the distal than the proximal bowel. To mechanistically evaluate this regional selectivity, we assessed cyclo-oxygenase-2 (COX-2) expression in the uninvolved mucosa and demonstrated a 3- to 4-fold excess in the distal relative to the proximal bowel in both MIN mice and AOM-treated rats. We then investigated another putative NSAID target, peroxisome proliferator-activated receptor-delta (PPAR-delta) and demonstrated up-regulation during AOM-induced colonic tumorigenesis. Furthermore, in pre-neoplastic mucosa, there was a 3-fold excess of PPAR-delta in the distal colon. We demonstrate that nabumetone is an effective protective agent in both experimental models of colon carcinogenesis. The striking distal predilection of nabumetone may be, at least partially, explained by distal bowel over-expression of COX-2 and PPAR-delta.

  17. Thermal nociception as a measure of non-steroidal anti-inflammatory drug effectiveness in broiler chickens with articular pain.

    Science.gov (United States)

    Caplen, Gina; Baker, Laurence; Hothersall, Becky; McKeegan, Dorothy E F; Sandilands, Victoria; Sparks, Nick H C; Waterman-Pearson, Avril E; Murrell, Joanna C

    2013-12-01

    Pain associated with poultry lameness is poorly understood. The anti-nociceptive properties of two non-steroidal anti-inflammatory drugs (NSAIDs) were evaluated using threshold testing in combination with an acute inflammatory arthropathy model. Broilers were tested in six groups (n=8 per group). Each group underwent a treatment (saline, meloxicam (3 or 5mg/kg) or carprofen (15 or 25mg/kg)) and a procedure (Induced (arthropathy-induction) or sham (sham-handling)) prior to testing. Induced groups had Freund's complete adjuvant injected intra-articularly into the left intertarsal joint (hock). A ramped thermal stimulus (1°C/s) was applied to the skin of the left metatarsal. Data were analysed using random-intercept multi-level models. Saline-induced birds had a significantly higher skin temperature (± SD) than saline-sham birds (37.6 ± 0.8°C vs. 36.5 ± 0.5°C; Z=-3.47, Pnociception). Quantification of nociceptive responsiveness in a predictable broiler pain model identified thermal anti-hyperalgesic properties of two NSAIDs, which suggested that therapeutically effective treatment was provided at the doses administered. Such validation of analgesic strategies will increase the understanding of pain associated with specific natural broiler lameness types.

  18. Sunlight-driven photocatalytic degradation of non-steroidal anti-inflammatory drug based on TiO₂ quantum dots.

    Science.gov (United States)

    Kaur, Amandeep; Umar, Ahmad; Kansal, Sushil Kumar

    2015-12-01

    This paper reports the facile synthesis, characterization and solar-light driven photocatalytic degradation of TiO2 quantum dots (QDs). The TiO2 QDs were synthesized by a facile ultrasonic-assisted hydrothermal process and characterized in terms of their structural, morphological, optical and photocatalytic properties. The detailed studies confirmed that the prepared QDs are well-crystalline, grown in high density and exhibiting good optical properties. Further, the prepared QDs were efficiently used as effective photocatalyst for the sun-light driven photocatalytic degradation of ketorolac tromethamine, a well-known non-steroidal anti-inflammatory drug (NSAID). To optimize the photocatalytic degradation conditions, various dose-dependent, pH-dependent, and initial drug-concentration dependent experiments were performed. The detailed solar-light driven photocatalytic experiments revealed that ∼99% photodegradation of ketorolac tromethamine drug solution (10 mg L(-1)) was observed with optimized amount of TiO2 QDs and pH (0.5 g L(-1) and 4.4, respectively) under solar-light irradiations. The observed results demonstrate that simply synthesized TiO2 QDs can efficiently be used for the solar-light driven photocatalytic degradation of harmful drugs and chemicals.

  19. Formulation,Optimization and Evaluation of Orally Disintegrating Tablet of Non-Steroidal Anti-inflammatory Drug

    Directory of Open Access Journals (Sweden)

    Patel Minal Arvindbhai

    2012-05-01

    Full Text Available Piroxicam is a non steroidal anti-inflammatory drug with analgesic properties. The purpose of this studywas to develop a taste masked orally disintegrating tablet of poorly soluble Piroxicam by directcompression technique with β-cyclodextrin (ß-CD complexes using various superdisintegrants likesodium starch glycolate, crospovidone XL and croscarmellose sodium. Complex was characterizedusing infrared spectroscopy, differential scanning calorimetry, % drug release study, gustatoryevaluation for taste masking. A 32 full factorial design was applied to systematically optimize the drugdisintegration time. The concentration of Crospovidone (X1 and concentration of Croscarmellose (X2were selected as independent variables. The Disintegration time (Y1 and Wetting time (Y2 wereselected as dependent variables. The prepared tablets were evaluated for hardness, friability,disintegration time, wetting time and In-vitro drug release. FT-IR studies and physical compatibilitystudy were conducted for drug, and drug excipient mixture for interactions if any. The differentformulations showed disintegration time between 12 to 58 sec. The results indicated that concentrationof Crospovidone (X1 and concentration of Croscarmellose (X2 significantly affected theDisintegration time (Y1 and Wetting time (Y2. Regression analysis and numerical optimization wereperformed to identify the best formulation. Formulation F10 prepared with croscarmellose (4.23% &crospovidone (6.74% was found to be the best formulation with disintegration time 16 sec, wetting time21 sec and % drug release in 10 min 94.23%.

  20. Effects of non-steroidal anti-inflammatory drugs on proliferation, differentiation and migration in equine mesenchymal stem cells.

    Science.gov (United States)

    Müller, Maike; Raabe, Oksana; Addicks, Klaus; Wenisch, Sabine; Arnhold, Stefan

    2011-03-01

    In equine medicine, stem cell therapies for orthopaedic diseases are routinely accompanied by application of NSAIDs (non-steroidal anti-inflammatory drugs). Thus, it has to be analysed how NSAIDs actually affect the growth and differentiation potential of MSCs (mesenchymal stem cells) in vitro in order to predict the influence of NSAIDs such as phenylbutazone, meloxicam, celecoxib and flunixin on MSCs after grafting in vivo. The effects of NSAIDs were evaluated regarding cell viability and proliferation. Additionally, the multilineage differentiation capacity and cell migration was analysed. NSAIDs at lower concentrations (0.1-1 μM for celecoxib and meloxicam and 10-50 μM for flunixin) exert a positive effect on cell proliferation and migration, while at higher concentrations (10-200 μM for celecoxib and meloxicam and 100-1000 μM for flunixin and phenylbutazone), there is rather a negative influence. While there is hardly any influence on the adipogenic as well as on the chondrogenic MSC differentiation, the osteogenic differentiation potential, as demonstrated with the von Kossa staining, is significantly disturbed. Thus, it can be concluded that the effects of NSAIDs on MSCs are largely dependent on the concentrations used. Additionally, for some differentiation lineages, also the choice of NSAID is critical.

  1. Charge transfer complex studies between some non-steroidal anti-inflammatory drugs and π-electron acceptors

    Science.gov (United States)

    Duymus, Hulya; Arslan, Mustafa; Kucukislamoglu, Mustafa; Zengin, Mustafa

    2006-12-01

    Charge transfer (CT) complexes of some non-steroidal anti-inflammatory drugs, naproxen and etodolac which are electron donors with some π-acceptors, such as tetracyanoethylene (TCNE), 2,3-dichloro-5,6-dicyano- p-benzoquinone (DDQ), p-chloranil ( p-CHL), have been investigated spectrophotometrically in chloroform at 21 °C. The coloured products are measured spectrophotometrically at different wavelength depending on the electronic transition between donors and acceptors. Beer's law is obeyed and colours were produced in non-aqueous media. All complexes were stable at least 2 h except for etodolac with DDQ stable for 5 min. The equilibrium constants of the CT complexes were determined by the Benesi-Hildebrand equation. The thermodynamic parameters Δ H, Δ S, Δ G° were calculated by Van't Hoff equation. Stochiometries of the complexes formed between donors and acceptors were defined by the Job's method of the continuous variation and found in 1:1 complexation with donor and acceptor at the maximum absorption bands in all cases.

  2. 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.

  3. 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.

  4. Dynamic model of eicosanoid production with special reference to non-steroidal anti-inflammatory drug-triggered hypersensitivity.

    Science.gov (United States)

    Fajmut, Aleš; Emeršič, Tadej; Dobovišek, Andrej; Antić, Nataša; Schäfer, Dirk; Brumen, Milan

    2015-10-01

    The authors developed a mathematical model of arachidonic acid (AA) degradation to prostaglandins (PGs) and leukotrienes (LTs), which are implicated in the processes of inflammation and hypersensitivity to non-steroidal anti-inflammatory drugs (NSAIDs). The model focuses on two PGs (PGE2 and PGD2) and one LT (LTC4), their % increases and their ratios. Results are compared with experimental studies obtained from non-asthmatics (NAs), and asthmatics tolerant (ATA) or intolerant (AIA) to aspirin. Simulations are carried out for predefined model populations NA, ATA and three AIA, based on the differences of two enzymes, PG E synthase and/or LTC4-synthase in two states, that is, no-inflammation and inflammation. Their model reveals that the model population with concomitant malfunctions in both enzymes is the most sensitive to NSAIDs, since the duration and the capacity for bronchoconstriction risk are highest after simulated oral dosing of indomethacin. Furthermore, inflammation prolongs the duration of the bronchoconstriction risk in all AIA model populations, and the sensitivity analysis reveals multiple possible scenarios leading to hypersensitivity, especially if inflammatory processes affect the expression of multiple enzymes of the AA metabolic pathway. Their model estimates the expected fold-changes in enzyme activities and gives valuable information for further targeted transcriptomic/proteomic and metabolomic studies.

  5. 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.

  6. Non-steroidal anti-inflammatory drugs and amyotrophic lateral sclerosis: results from five prospective cohort studies.

    Science.gov (United States)

    Fondell, Elinor; O'Reilly, Éilis J; Fitzgerald, Kathryn C; Falcone, Guido J; McCullough, Marjorie L; Thun, Michael J; Park, Yikyung; Kolonel, Laurence N; Ascherio, Alberto

    2012-10-01

    Animal and pathological studies suggest that inflammation may contribute to amyotrophic lateral sclerosis (ALS) pathology and that non-steroidal anti-inflammatory drugs (NSAIDs) might be protective. However, there are no prospective data on the relation between NSAID use and ALS risk in humans. The relation between NSAID use and ALS risk was explored in five large prospective cohort studies (the Nurses' Health Study, the Health Professionals Follow-up Study, the Cancer Prevention Study II Nutrition Cohort, the Multiethnic Cohort Study, and the National Institutes of Health - AARP Diet and Health Study). Detailed NSAID information was sought from 780,000 participants, 708 of whom developed ALS during follow-up. Cox proportional hazards models were used within each cohort and cohort-specific estimates were pooled with random effects models. Results showed that neither non-aspirin NSAID use, nor aspirin use was associated with ALS risk overall. The multivariable, pooled relative risk was 0.96 (95% CI 0.76-1.22) among non-aspirin NSAID users compared with non-users. Duration of NSAID use in years and frequency of NSAID use were not associated with ALS risk overall. In conclusion, the results do not support an overall effect of NSAIDs on ALS risk, but because NSAIDs have heterogeneous effects, a role of individual compounds cannot be excluded.

  7. 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...... subjects, we identified 615 CRC cases during 1995-2006. Daily aspirin use at entry was associated with a decreased risk of CRC (RR, 0.73; 95% CI, 0.49-1.10). A similar risk reduction was seen among subjects with 10 or more prescriptions for aspirin or non-aspirin NSAIDs and five or more years of follow......-up. Most aspirin prescriptions were for 75-150 mg aspirin tablets. Among non-aspirin NSAID users, only those with body mass index (BMI) above 25 showed risk reductions [RR, 0.69 (0.47-1.03) for 10 or more prescriptions]. Long-term consistent use of aspirin or non-aspirin NSAIDs appears necessary to achieve...

  8. 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.

  9. [Effect of a non-steroidal anti-inflammatory agent, tolmetin sodium on exudative inflammation in experimental animals (author's transl)].

    Science.gov (United States)

    Nakamura, H; Yokoyama, Y; Motoyoshi, S; Ishii, K; Shimizu, M

    1979-07-01

    Effect of tolmetin sodium(Tol) on acute and subacute exudative inflammation was tested in experimental animals. Tol had a potent inhibitory activity (ED50 = 0.75 mg/kg, p.o.) on the increased vascular permeability induced by acetic acid in mice, and the potency was about 0.4 times that of indomethacin (Ind), and 6-93 times that of ibuprofen (Ibu), phenylbutazone(Phe) and aspirin(Asp). The inhibitory activity of Tol(ED50 = 18.2 mg/kg, p.o.) on UV-induced erythema in guinea pigs was about 0.3 times that of Ind. A recovery of the hind paw edema of rats, produced by a mixture of kaolin and carrageenin, was promoted by oral administration of Tol(2.5 approximately 20 mg/kg x 5/2 days). Tol(80 mg/kg/day, p.o.) showed a significant activity in inhibiting the exudation caused by croton oil in rats, and the activity was about 0.025 times that of Ind and greater than that of Ibu, Phe and Asp. Tol(100-800 microgram/ml) inhibited in a dose-dependent manner the phytohemagglutinin-induced blast transformation of cultured lymphocytes from rat thymus, as did salicylic acid. In vitro, Tol showed a potent activity similar to that of Ibu and Phe in preventing the denaturation of bovine serum albumin and the lysis of rat erythrocytes. From these results, it is suggested that Tol has a particularly potent inhibitory activity on acute exudative inflammation, and the mode of action may be attributed to a mechanism similar to that seen with other acidic non-steroidal anti-inflammatory drugs.

  10. 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.

  11. Special diaphragm-like strictures of small bowel unrelated to non-steroidal anti-inflammatory drugs

    Institute of Scientific and Technical Information of China (English)

    Ming-Liang Wang; Fei Miao; Yong-Hua Tang; Xue-Song Zhao; Jie Zhong; Fei Yuan

    2011-01-01

    AIM: To summarize clinical, endoscopic, radiologic and pathologic ffeatures off special diaphragm-like strictures ffound in small bowel, with no patient use off non-steroidal anti-inflammatory drugs (NSAIDs). METHODS: From January 2000 to Ddecember 2009, 5 cases (2 men and 3 women, with a mean age of 41.6 years) were diagnosed as having diaphragm-like strictures off small bowel on imaging,operationand, operationandoperation and pathology. All the patients denied the use of NSAIDs. The clinical, endoscopic, radiologic and pathologic findings in these 5 patients were retrospectively reviewed from the hospital database. Images of capsule endoscopy (CE) and small bowel follow-through (SBFT) obtained in 3 and 3 patients, respectively, and images off double-balloon enteroscopy and computed tomography enterography (CTE) obtained in all 5 patients were available for review. RESULTS: All patients presented with long-term (2-16 years) symptoms of gastrointestinal bleeding and varying degrees of anemia. There was only one stricture in ffour cases and three lesions in one case, and all the lesions were located in the middle or distal segment off ileum. Circumferential stricture was shown in the small bowel in three cases in the CE image, but the capsule was retained in the small bowel of 2 patients. Routine abdomen computed tomography scan showed no other abnormal results except gallstones in one patient. The lesions were shown as circumfferential strictures accompanied by dilated small bowel loops in the small bowel on the images of CTE (in all 5 cases), SBFT (in 2 cases) and double-balloon enteroscopy (in all cases). On microscopy, a chronic infflammatory inffiltrate and circumferential diaphragm were found in all lesions. CONCLUSION: Ddiaphragm-like strictures off small bowel might be a special consequence off unclear damaging insults to the intestine, having similar clinical, endoscopic, radiologic and pathologic features.

  12. Non-steroidal anti-inflammatory drug for pulmonary administration: design and investigation of ketoprofen lysinate fine dry powders.

    Science.gov (United States)

    Stigliani, Mariateresa; Aquino, Rita P; Del Gaudio, Pasquale; Mencherini, Teresa; Sansone, Francesca; Russo, Paola

    2013-05-01

    Pulmonary inflammation is an important therapeutic target in cystic fibrosis (CF) patients, aiming to limit and delay the lung damage. The purpose of the present research was to produce respirable engineered particles of ketoprofen lysinate, a non-steroidal anti-inflammatory drug able to fight lung inflammatory status by direct administration to the site of action. Micronized drug powders containing leucine as dispersibility enhancer were prepared by co-spray drying the active compound and the excipient from water or hydro-alcoholic feeds. Microparticles were fully characterized in terms of process yield, particle size distribution, morphology and drug content. The ability of the drug to reach the deepest airways after aerosolization of spray-dried formulations was evaluated by Andersen cascade impactor, using the monodose DPI as device. In order to investigate the behaviour of the drug once in contact with lung fluid, an artificial CF mucus was prepared. Drug permeation properties were evaluated interposing the mucus layer between the drug and a synthetic membrane mounted in Franz-type diffusion cells. Finally, the effect of the engineered particles on vitality of human airway epithelial cells of patients homozygous for ΔF 508 CF (CuFi1) was studied and compared to that of raw active compound. Results indicated that powders engineering changed the diameter and shape of the particles, making them suitable for inhalation. The mucus layer in the donor compartment of vertical diffusion cells slowed down drug dissolution and permeation, leucine having no influence. Cell proliferation studies evidenced that the spray drying process together with the addition of leucine reduced the cytotoxic effect of ketoprofen lysine salt as raw material, making the ketoprofen lysinate DPI a very promising product for the inflammation control in CF patients.

  13. Non-steroidal anti-inflammatory drugs and renal response to exercise: a comparison of indomethacin and nabumetone.

    Science.gov (United States)

    Olsen, N V; Jensen, N G; Hansen, J M; Christensen, N J; Fogh-Andersen, N; Kanstrup, I L

    1999-10-01

    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 and the renin-aldosterone system. In a randomized fashion, ten subjects were studied after indomethacin (100 mg), nabumetone (1 g) or no medication (control) administered orally at 22.00 hours on the day before each study day, and again at 8.00 hours upon arrival at the laboratory. Renal function was studied at baseline, during graded 20-min exercise sessions at 25%, 50% and 75% of the maximal oxygen uptake rate, and subsequently during two 1-h recovery periods. Heart rate, arterial blood pressure, cardiac output and plasma catecholamines at rest and during exercise were not altered by indomethacin or nabumetone. Indomethacin decreased urinary rates of excretion of 6-oxo-prostaglandin F(1alpha) (6-oxo-PGF(1alpha)) and thromboxane B(2) in all study periods. Nabumetone decreased 6-oxo-PGF(1alpha) excretion during and after exercise. Excretion rates for PGE(2) did not change. Neither indomethacin nor nabumetone changed baseline values or exercise-induced decreases in renal plasma flow or glomerular filtration rate. Indomethacin, but not nabumetone, decreased sodium excretion, urine flow rate and free water clearance. The renal response to exercise, however, remained unchanged. In contrast with nabumatone, indomethacin 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. Inhibition by indomethacin of angiotensin II and thromboxane A(2) synthesis may, during exercise, counterbalance renal vasoconstriction caused by blockade of

  14. 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.

  15. Validation of a micellar liquid chromatographic method for determination of caffeine and non-steroidal anti-inflammatories.

    Science.gov (United States)

    El Sherbiny, Dina; Wahba, Mary E K

    2014-09-01

    An accurate, simple, sensitive and selective micellar liquid chromatographic method has been developed for the simultaneous determination of caffeine (CAF) and two non-steroidal anti-inflammatory drugs, namely ibuprofen (IBU) and ketoprofen (KET). The chemometric approach was applied to the optimization of separation of the studied drugs. To optimize their separation, the effect of six experimental parameters on retention was investigated by means of multivariate analysis. Separation was conducted using an ODS C18 (150 × 4.6 mm i.d.) stainless steel column at ambient temperature with UV detection at 260 nm. A mobile phase composed of 40 mM sodium dodecyl sulphate (SDS), 10% 1-propanol and 0.3% tri-ethylamine in 0.02 M phosphoric acid adjusted to pH 3 has been used at a flow rate of 1 mL/min. Regression models were characterized by both descriptive and predictive ability (R(2) ≥ 97.9% and R(cv)(2) ≥ 96.2%) and allowed the chromatographic separation of the drugs with a good resolution and a total analysis time within 15 min. The calibration curves were rectilinear over the concentration ranges of 2.0-25.0, 1.5-15.0 and 1.0-10.0 µg/mL for IBU, KET and CAF, respectively, with detection limits of 1.2, 1.0 and 0.6 µg/mL, and quantification limits of 1.6, 1.2 and 0.8 µg/mL, respectively. The results obtained were in good agreement with those obtained by the comparison method.

  16. Combinatorial effect of non-steroidal anti-inflammatory drugs and NF-κB inhibitors in ovarian cancer therapy.

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    Luiz F Zerbini

    Full Text Available Several epidemiological studies have correlated the use of non-steroidal anti-inflammatory drugs (NSAID with reduced risk of ovarian cancer, the most lethal gynecological cancer, diagnosed usually in late stages of the disease. We have previously established that the pro-apoptotic cytokine melanoma differentiation associated gene-7/Interleukin-24 (mda-7/IL-24 is a crucial mediator of NSAID-induced apoptosis in prostate, breast, renal and stomach cancer cells. In this report we evaluated various structurally different NSAIDs for their efficacies to induce apoptosis and mda-7/IL-24 expression in ovarian cancer cells. While several NSAIDs induced apoptosis, Sulindac Sulfide and Diclofenac most potently induced apoptosis and reduced tumor growth. A combination of these agents results in a synergistic effect. Furthermore, mda-7/IL-24 induction by NSAIDs is essential for programmed cell death, since inhibition of mda-7/IL-24 by small interfering RNA abrogates apoptosis. mda-7/IL-24 activation leads to upregulation of growth arrest and DNA damage inducible (GADD 45 α and γ and JNK activation. The NF-κB family of transcription factors has been implicated in ovarian cancer development. We previously established NF-κB/IκB signaling as an essential step for cell survival in cancer cells and hypothesized that targeting NF-κB could potentiate NSAID-mediated apoptosis induction in ovarian cancer cells. Indeed, combining NSAID treatment with NF-κB inhibitors led to enhanced apoptosis induction. Our results indicate that inhibition of NF-κB in combination with activation of mda-7/IL-24 expression may lead to a new combinatorial therapy for ovarian cancer.

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

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    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.

  18. The Diamine Oxidase Gene Is Associated with Hypersensitivity Response to Non-Steroidal Anti-Inflammatory Drugs

    Science.gov (United States)

    Agúndez, José A. G.; Ayuso, Pedro; Cornejo-García, José A.; Blanca, Miguel; Torres, María J.; Doña, Inmaculada; Salas, María; Blanca-López, Natalia; Canto, Gabriela; Rondon, Carmen; Campo, Paloma; Laguna, José J.; Fernández, Javier; Martínez, Carmen; García-Martín, Elena

    2012-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are the drugs most frequently involved in hypersensitivity drug reactions. Histamine is released in the allergic response to NSAIDs and is responsible for some of the clinical symptoms. The aim of this study is to analyze clinical association of functional polymorphisms in the genes coding for enzymes involved in histamine homeostasis with hypersensitivity response to NSAIDs. We studied a cohort of 442 unrelated Caucasian patients with hypersensitivity to NSAIDs. Patients who experienced three or more episodes with two or more different NSAIDs were included. If this requirement was not met diagnosis was established by challenge. A total of 414 healthy unrelated controls ethnically matched with patients and from the same geographic area were recruited. Analyses of the SNPs rs17740607, rs2073440, rs1801105, rs2052129, rs10156191, rs1049742 and rs1049793 in the HDC, HNMT and DAO genes were carried out by means of TaqMan assays. The detrimental DAO 16 Met allele (rs10156191), which causes decreased metabolic capacity, is overrepresented among patients with crossed-hypersensitivity to NSAIDs with an OR  = 1.7 (95% CI  = 1.3–2.1; Pc  = 0.0003) with a gene-dose effect (P = 0.0001). The association was replicated in two populations from different geographic areas (Pc  = 0.008 and Pc  = 0.004, respectively). Conclusions and implications The DAO polymorphism rs10156191 which causes impaired metabolism of circulating histamine is associated with the clinical response in crossed-hypersensitivity to NSAIDs and could be used as a biomarker of response. PMID:23152756

  19. Use of non-steroidal anti-inflammatory drugs in pregnancy: impact on the fetus and newborn.

    Science.gov (United States)

    Antonucci, Roberto; Zaffanello, Marco; Puxeddu, Elisabetta; Porcella, Annalisa; Cuzzolin, Laura; Pilloni, Maria Dolores; Fanos, Vassilios

    2012-05-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed in pregnancy to treat fever, pain and inflammation. Indications for chronic use of these agents during pregnancy are inflammatory bowel or chronic rheumatic diseases. Since the seventies, NSAIDs have been used as effective tocolytic agents: indomethacin has been the reference drug, delaying delivery for at least 48 hours and up to 7-10 days. Additionally, self-medication with NSAIDs is practiced by pregnant women. NSAIDs given to pregnant women cross the placenta and may cause embryo-fetal and neonatal adverse effects, depending on the type of agent, the dose and duration of therapy, the period of gestation, and the time elapsed between maternal NSAID administration and delivery. These effects derive from the action mechanisms of NSAIDs (mainly inhibition of prostanoid activity) and from the physiological changes in drug pharmacokinetics occurring during pregnancy. Increased risks of miscarriage and malformations are associated with NSAID use in early pregnancy. Conversely, exposure to NSAIDs after 30 weeks' gestation is associated with an increased risk of premature closure of the fetal ductus arteriosus and oligohydramnios. Fetal and neonatal adverse effects affecting the brain, kidney, lung, skeleton, gastrointestinal tract and cardiovascular system have also been reported after prenatal exposure to NSAIDs. NSAIDs should be given in pregnancy only if the maternal benefits outweigh the potential fetal risks, at the lowest effective dose and for the shortest duration possible. This article discusses in detail the placental transfer and metabolism of NSAIDs, and the adverse impact of prenatal NSAID exposure on the offspring.

  20. Variable Effects of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs on Selected Biochemical Processes Mediated by Soil Microorganisms

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    Mariusz Sebastian Cycoń

    2016-12-01

    Full Text Available Non-steroidal anti-inflammatory drugs (NSAIDs are the most frequently used group of pharmaceuticals. The high consumption and the uncontrolled disposal of unused drugs into municipal waste or their deposit in landfills can result in an increased concentration of these compounds in soils. Moreover, these drugs can affect the microbial activity. However, there is a lack of knowledge about these effects or it is very limited. Therefore, the objective of this study was to compare the impact of selected commercially available NSAIDs, i.e. diclofenac (DCF, naproxen (NPX, ibuprofen (IBF and ketoprofen (KTP, applied at concentrations of 1 and 10 mg/kg soil, on the activity of soil microorganisms during the 90-day experiment. To ascertain this impact, substrate-induced respiration (SIR, soil enzyme activities, i.e. dehydrogenase (DHA, acid and alkaline phosphatases (PHOS-H and PHOS-OH and urease (URE as well as changes in the rates of nitrification and ammonification processes were determined. In addition, the number of culturable bacteria and fungi were enumerated. In general, the obtained data showed a significant stimulatory effect of NSAIDs on the microbial activity. Higher concentrations of NSAIDs caused a greater effect, which was observed for SIR, PHOS-H, PHOS-OH, URE, N-NO3- and N-NH4+, even during the whole incubation period. Moreover, the number of heterotrophic bacteria and fungi increased significantly during the experiment, which was probably a consequence of the evolution of specific microorganisms that were capable of degrading NSAIDs and used them as an additional source of carbon and energy. However, an inhibitory effect of NPX, IBF or KTP for SIR, DHA, on both phosphatases and culturable bacteria and fungi was observed at the beginning of the experiment. At lower concentrations of NSAIDs, in turn, the effects were negligible or transient. In conclusion, the application of NSAIDs altered the biochemical and microbial activity of soil

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

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    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

  2. [Effect of protracted therapy with chondroprotectors and non-steroidal anti-inflammatory drugs on the quality of life in patients with osteoarthrosis].

    Science.gov (United States)

    Maĭko, O Iu; Bagirova, G G

    2009-01-01

    Dynamics of clinical parameters and quality of life (QL) was evaluated in 281 patients with knee and hip osteoarthrosis (OA) during long-term treatment of different duration. The group was dominated by women (71%) aged 41-65 yr with grade I-III OA according to Kellgren. Patients of groups I and II received only non-steroidal anti-inflammatory drugs (diclofenac, nize), those of groups III-IV the same drugs in combination with structum, chondrolon, and zeel T respectively. Clinical parameters were assessed based on VAS at rest and in motion, Leken's indices, and WOMAC, QL from SF-36 questionnaire. Variable clinical course was recorded in patients treated with non-steroidal drugs alone that caused rapid improvement after the very first treatment sessions followed by deterioration of the patients' condition. Addition of structum resulted in marked optimization of clinical and QL parameters within 3 months after the onset of combined therapy. Similar effect was obtained using chondrolon and zeel T, but 2-3 clinical parameters and 3 QL parameters were not significantly different from the initial ones after 12 and 24 months of therapy. It is concluded that structum produced the best therapeutic effect followed by chondrolon and zeel T. Non-steroidal anti-inflammatory drugs had no beneficial action whatever in patients with OA.

  3. 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

  4. Steroid resistance in COPD? : Overlap and differential anti-inflammatory effects in smokers and ex-smokers

    NARCIS (Netherlands)

    Hoonhorst, Susan J. M.; ten Hacken, Nicolaas; Vonk, Judith M.; Timens, Wim; Hiemstra, Pieter S.; Lapperre, Therese S.; Sterk, Peter J.; Postma, Dirkje S.

    2014-01-01

    Background: Inhaled corticosteroids (ICS) reduce exacerbation rates and improve health status but can increase the risk of pneumonia in COPD. The GLUCOLD study, investigating patients with mild-to-moderate COPD, has shown that long-term (2.5-year) ICS therapy induces anti-inflammatory effects. The l

  5. The relationship between non-steroid anti-inflammatory drugs and cardiovascular risk - the myths, the misconceptions, the news, the realities -

    Directory of Open Access Journals (Sweden)

    Mirela-Anca STOIA

    2015-12-01

    Full Text Available While the number of clinical experiments investigating the effects of non-steroid anti-inflammatory drugs (NSAIDs on the cardiovascular (CV events has significantly increased over the last two decades, basic research related to the mechanism by which NSAIDs cause CV dysfunction is limited. High variability in the clinical trials conducted (different populations, dosages, exposure and types of NSAIDs has led to results which are difficult to interpret and compare between studies. Are there some NSAIDs safer than other from the standpoint of CV risk? We have try to answer at some aspects of this question.

  6. Regular use of non-steroidal anti-inflammatory drugs increases the risk of adult-onset asthma: a population-based follow-up study

    DEFF Research Database (Denmark)

    Thomsen, Simon Francis; Kyvik, Kirsten Ohm; Skadhauge, Lars Rauff;

    2009-01-01

    BACKGROUND: Little is known about the relation between regular use of non-steroidal anti-inflammatory drugs (NSAIDs) and the risk of asthma at the population level. The aim of this study was to examine a possible association between intake of NSAIDs and risk of adult-onset asthma. METHODS: Using...... data from two multidisciplinary postal questionnaire surveys concerning health and lifestyle, we prospectively studied 19 349 adult twins enrolled in the nationwide Danish Twin Registry. RESULTS: We found a higher prevalence of new-onset asthma in subjects who used NSAIDs (other than aspirin) regularly...

  7. 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

  8. Steroid resistance in COPD? Overlap and differential anti-inflammatory effects in smokers and ex-smokers.

    Directory of Open Access Journals (Sweden)

    Susan J M Hoonhorst

    Full Text Available BACKGROUND: Inhaled corticosteroids (ICS reduce exacerbation rates and improve health status but can increase the risk of pneumonia in COPD. The GLUCOLD study, investigating patients with mild-to-moderate COPD, has shown that long-term (2.5-year ICS therapy induces anti-inflammatory effects. The literature suggests that cigarette smoking causes ICS insensitivity. The aim of this study is to compare anti-inflammatory effects of ICS in persistent smokers and persistent ex-smokers in a post-hoc analysis of the GLUCOLD study. METHODS: Persistent smokers (n = 41 and persistent ex-smokers (n = 31 from the GLUCOLD cohort were investigated. Effects of ICS treatment compared with placebo were estimated by analysing changes in lung function, hyperresponsiveness, and inflammatory cells in sputum and bronchial biopsies during short-term (0-6 months and long-term (6-30 months treatment using multiple regression analyses. RESULTS: Bronchial mast cells were reduced by short-term and long-term ICS treatment in both smokers and ex-smokers. In contrast, CD3⁺, CD4⁺, and CD8⁺ cells were reduced by short-term ICS treatment in smokers only. In addition, sputum neutrophils and lymphocytes, and bronchial CD8⁺ cells were reduced after long-term treatment in ex-smokers only. No significant interactions existed between smoking and ICS treatment. CONCLUSION: Even in the presence of smoking, long-term ICS treatment may lead to anti-inflammatory effects in the lung. Some anti-inflammatory ICS effects are comparable in smokers and ex-smokers with COPD, other effects are cell-specific. The clinical relevance of these findings, however, are uncertain.

  9. Physicochemical profile and in vitro permeation behavior of a new class of non-steroidal anti-inflammatory drug candidates.

    Science.gov (United States)

    Rolando, Barbara; Lazzarato, Loretta; Di Stilo, Antonella; Fruttero, Roberta; Carrupt, Pierre-Alain; Martel, Sophie; Gasco, Alberto

    2010-06-14

    Recently a new series of nitrooxy-acyl derivatives of salicylic acid (SA) was described presenting similar anti-inflammatory activities but reduced or no gastrotoxicity compared to aspirin. In this work, lipophilicity and permeability profiles of SA derivatives were performed to evaluate their ADME properties related to oral or transdermic delivery. All tested compounds showed potential good passive permeation through gastrointestinal track and also through percutaneous barrier which could be a way to avoid the first hepatic pass.

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

    Directory of Open Access Journals (Sweden)

    Di Pierro F

    2013-04-01

    Full Text Available Francesco Di Pierro,1 Eleonora Di Maio,2 Gaetana Di Paola,3 Raffaele Felice,4 Filippo Murina41Velleja Research, Milan, Italy; 2Molinette Hospital, Turin, Italy; 3ASL TO-3/TO-4, Turin, Italy; 4Outpatient Department of Vulvar Disease, V Buzzi Hospital-ICP, Milan, ItalyAim: 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.Keywords: vulvar dermatitis, lichen simplex chronicus, vulvar itching, Zantogin®, zanthalene

  11. Two non-steroidal anti-inflammatory drugs, niflumic acid and diclofenac, inhibit the human glutamate transporter EAAT1 through different mechanisms.

    Science.gov (United States)

    Takahashi, Kanako; Ishii-Nozawa, Reiko; Takeuchi, Kouichi; Nakazawa, Ken; Sato, Kaoru

    2010-01-01

    We investigated the effects of non-steroidal anti-inflammatory drugs on substrate-induced currents of L-glutamate (L-Glu) transporter EAAT1 expressed in Xenopus laevis oocytes. Niflumic acid (NFA) and diclofenac inhibited L-Glu-induced current through EAAT1 in a non-competitive manner. NFA produced a leftward shift in reversal potential (E(rev)) of L-Glu-induced current and increased current amplitude at the potentials more negative than -100 mV. Diclofenac had no effects on E(rev) and inhibited the current amplitude to the same extent at all negative potentials. These results indicate that NFA and diclofenac inhibit the L-Glu-induced EAAT1 current via different mechanisms.

  12. A sensitive enzyme-linked immunosorbent assay amplified by biotin-streptavidin system for detecting non-steroidal anti-inflammatory drug ketoprofen.

    Science.gov (United States)

    Bu, Dan; Zhuang, Hui S; Yang, Guang X

    2014-01-01

    A sensitive biotin-streptavidin-amplified enzyme-linked immunosorbent assay (BA-ELISA) method was developed for detecting non-steroidal anti-inflammatory drug ketoprofen. Compared with traditional ELISA method, the sensitivity of proposed immunoassay was enhanced by the biotin-streptavidin system. Under the optimal condition, the median inhibitory concentration (IC50) was 0.25 ng mL(-1), with minor cross-reactivity to a number of structural analogs. This developed assay was successfully applied to detect the ketoprofen residues in different fish samples, and good recoveries (72.6-105.5%) were obtained. The results indicated that this immunoassay method could specifically detect trace ketoprofen residues and could be widely used for routine monitoring of food samples.

  13. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  15. 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.

  16. 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.

  17. Low-dose aspirin, non-steroidal anti-inflammatory drugs, selective COX-2 inhibitors and breast cancer recurrence

    DEFF Research Database (Denmark)

    Cronin-Fenton, Deirdre P; Heide-Jørgensen, Uffe; Ahern, Thomas P

    2016-01-01

    BACKGROUND: Aspirin, nonsteroidal anti-inflammatory drugs (NSAIDs), and selective COX-2 inhibitors may improve outcomes in breast cancer patients. We investigated the association of aspirin, NSAIDs, and use of selective COX-2 inhibitors with breast cancer recurrence. METHODS: We identified incident...... stage I-III Danish breast cancer patients in the Danish Breast Cancer Cooperative Group registry, who were diagnosed during 1996-2008. Prescriptions for aspirin (>99% low-dose aspirin), NSAIDs, and selective COX-2 inhibitors were ascertained from the National Prescription Registry. Follow-up began...... on the date of breast cancer primary surgery and continued until the first of recurrence, death, emigration, or 1 January 2013. We used Cox regression models to compute hazard ratios (HR) and corresponding 95% confidence intervals (95% CI) associating prescriptions with recurrence, adjusting for confounders...

  18. 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)

  19. Effects of non-steroidal anti-inflammatory drugs on cyanobacteria and algae in laboratory strains and in natural algal assemblages.

    Science.gov (United States)

    Bácsi, István; B-Béres, Viktória; Kókai, Zsuzsanna; Gonda, Sándor; Novák, Zoltán; Nagy, Sándor Alex; Vasas, Gábor

    2016-05-01

    In recent years measurable concentrations of non-steroidal anti-inflammatory drugs (NSAIDs) have been shown in the aquatic environment as a result of increasing human consumption. Effects of five frequently used non-steroidal anti-inflammatory drugs (diclofenac, diflunisal, ibuprofen, mefenamic acid and piroxicam in 0.1 mg ml(-1) concentration) in batch cultures of cyanobacteria (Synechococcus elongatus, Microcystis aeruginosa, Cylindrospermopsis raciborskii), and eukaryotic algae (Desmodesmus communis, Haematococcus pluvialis, Cryptomonas ovata) were studied. Furthermore, the effects of the same concentrations of NSAIDs were investigated in natural algal assemblages in microcosms. According to the changes of chlorophyll-a content, unicellular cyanobacteria seemed to be more tolerant to NSAIDs than eukaryotic algae in laboratory experiments. Growth of eukaryotic algae was reduced by all drugs, the cryptomonad C. ovata was the most sensitive to NSAIDs, while the flagellated green alga H. pluvialis was more sensitive than the non-motile green alga D. communis. NSAID treatments had weaker impact in the natural assemblages dominated by cyanobacteria than in the ones dominated by eukaryotic algae, confirming the results of laboratory experiments. Diversity and number of functional groups did not change notably in cyanobacteria dominated assemblages, while they decreased significantly in eukaryotic algae dominated ones compared to controls. The results highlight that cyanobacteria (especially unicellular ones) are less sensitive to the studied, mostly hardly degradable NSAIDs, which suggest that their accumulation in water bodies may contribute to the expansion of cyanobacterial mass productions in appropriate environmental circumstances by pushing back eukaryotic algae. Thus, these contaminants require special attention during wastewater treatment and monitoring of surface waters.

  20. 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

  1. 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

  2. Incremental cost effectiveness of proton pump inhibitors for the prevention of non-steroidal anti-inflammatory drug ulcers : a pharmacoeconomic analysis linked to a case-control study

    NARCIS (Netherlands)

    Vonkeman, Harald E.; Braakman-Jansen, Louise M. A.; Klok, Rogier M.; Postma, Maarten J.; Brouwers, Jacobus R. B. J.; van de laar, Mart A. F. J.

    2008-01-01

    Introduction We estimated the cost effectiveness of concomitant proton pump inhibitors (PPIs) in relation to the occurrence of non-steroidal anti-inflammatory drug (NSAID) ulcer complications. Methods This study was linked to a nested case-control study. Patients with NSAID ulcer complications were

  3. Incremental cost effectiveness of proton pump inhibitors for the prevention of non-steroidal anti-inflammatory drug ulcers : a pharmacoeconomic analysis linked to a case-control study

    NARCIS (Netherlands)

    Vonkeman, H.E.; Braakman-Jansen, L.M.A.; Klok, R.M.; Postma, M.J.; Brouwers, J.R.B.J.; van de Laar, M.A.F.J.

    2009-01-01

    Introduction We estimated the cost effectiveness of concomitant proton pump inhibitors (PPIs) in relation to the occurrence of non-steroidal anti-inflammatory drug (NSAID) ulcer complications. Methods This study was linked to a nested case-control study. Patients with NSAID ulcer complications were

  4. 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...

  5. 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.

  6. Proton pump inhibitors are not the key for therapying non-steroidal anti-inflammatory drugs-induced small intestinal injury.

    Science.gov (United States)

    Zhang, Shuo; Chao, Guan-qun; Lu, Bin

    2013-10-01

    The ability of non-steroidal anti-inflammatory drugs (NSAIDs) to injure the small intestine has been well established in humans and animals. Proton pump inhibitors (PPIs) are frequently prescribed to reduce gastric and duodenal injury caused in high-risk patients taking NSAIDs. However, scarce information is available concerning the effects of PPIs on intestinal damage induced by NSAIDs, and the suppression of gastric acid secretion by PPIs is hard to provide any protection against the damage caused by NSAIDs in the small intestine. The present study was designed to examine the effects of intragastric treatment of two PPIs widely used in clinical practice, namely omeprazole and pantoprazole, on the intestinal damage induced by administration of diclofenac in rat. Male SD rats were treated with omeprazole or pantoprazole for 9 days, with concomitant treatment with anti-inflammatory doses of diclofenac on the final 5 days. The anatomical lesion, villous height, the thickness, and the section area of small intestine were quantitatively analyzed. The change of ultrastructural organization was observed. Endotoxin level in blood was measured by photometry. Epidermal growth factor was observed by immunohistochemistry. Omeprazole and pantoprazole didn't decrease the macroscopic and histologic damage induced by diclofenac in the rat's small intestine. In the two PPI groups, villous height was (89.6 ± 11.8 and 92.6 ± 19.3 μm) lower than which of the control group (P thickness became thinning, and the section area became small. LPS levels in the portal blood of omeprazole and pantoprazole were (4.36 ± 1.26 and 4.25 ± 1.17 EU/ml), significantly higher than in controls (P small intestine from the damage induced by diclofenac in the conscious rat. PPIs cannot repair NSAID-induced intestinal damage at least in part because of significant lesion in mechanical barrier function and reduction in epidermal growth factor.

  7. 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.

  8. Non-Steroid Anti-Inflammatory Drugs Are Better than Acetaminophen on Fever Control at Acute Stage of Fracture.

    Directory of Open Access Journals (Sweden)

    Kuang-Ting Yeh

    Full Text Available In addition to adequate surgical fixation and an aggressive rehabilitation program, pain relief is one of the most critical factors in the acute stage of fracture treatment. The most common analgesics are nonsteroid anti-inflammatory drugs and Acetaminophen, both of which relieve pain and reduce body temperature. In clinical experiences, they exhibit effective pain control; however, their influence on body temperature remains controversial. This study is aimed at determining the effects of analgesics at the acute stage of traumatic fracture by performing a clinical retrospective study of patients with fractures and a fracture animal model. The retrospective study revealed that, in the acetaminophen group, the mean value of postmedication body temperature (BT was significantly higher than that of the premedication BT. The change in BT was highly related with the medication rather than other risk factors. Forty eight 12-week-old male Wistar rats were divided into 6 groups: a control group, fracture group, fracture-Acetaminophen group, Acetaminophen group, fracture-Arcoxia group, and Arcoxia group. Fracture rats were prepared by breaking their unilateral tibia and fibula. Their inflammation conditions were evaluated by measuring their serum cytokine level and their physiological status was evaluated by estimating their central temperature, heart rate, and mean blood pressure. The hepatic adverse effects were assessed by measuring the serum levels of aspartate aminotransferase (sGOT and alanine aminotransferase (sGPT. The central temperature in the fracture-Acetaminophen group exceeded that in the groups fed normal saline water or Arcoxia. Accumulated hepatic injury was presented as steadily ascending curves of sGOT and sGPT. Inflammation-related cytokine levels were not higher in the Acetaminophen fracture group and were significantly lower in the fracture-Arcoxia group. Fever appeared to be aggravated by acetaminophen and more related to the

  9. Non-Steroid Anti-Inflammatory Drugs Are Better than Acetaminophen on Fever Control at Acute Stage of Fracture.

    Science.gov (United States)

    Yeh, Kuang-Ting; Wu, Wen-Tien; Subeq, Yi-Maun; Niu, Chi-Chien; Liao, Kuang-Wen; Chen, Ing-Ho; Wang, Jen-Hung; Lee, Ru-Ping

    2015-01-01

    In addition to adequate surgical fixation and an aggressive rehabilitation program, pain relief is one of the most critical factors in the acute stage of fracture treatment. The most common analgesics are nonsteroid anti-inflammatory drugs and Acetaminophen, both of which relieve pain and reduce body temperature. In clinical experiences, they exhibit effective pain control; however, their influence on body temperature remains controversial. This study is aimed at determining the effects of analgesics at the acute stage of traumatic fracture by performing a clinical retrospective study of patients with fractures and a fracture animal model. The retrospective study revealed that, in the acetaminophen group, the mean value of postmedication body temperature (BT) was significantly higher than that of the premedication BT. The change in BT was highly related with the medication rather than other risk factors. Forty eight 12-week-old male Wistar rats were divided into 6 groups: a control group, fracture group, fracture-Acetaminophen group, Acetaminophen group, fracture-Arcoxia group, and Arcoxia group. Fracture rats were prepared by breaking their unilateral tibia and fibula. Their inflammation conditions were evaluated by measuring their serum cytokine level and their physiological status was evaluated by estimating their central temperature, heart rate, and mean blood pressure. The hepatic adverse effects were assessed by measuring the serum levels of aspartate aminotransferase (sGOT) and alanine aminotransferase (sGPT). The central temperature in the fracture-Acetaminophen group exceeded that in the groups fed normal saline water or Arcoxia. Accumulated hepatic injury was presented as steadily ascending curves of sGOT and sGPT. Inflammation-related cytokine levels were not higher in the Acetaminophen fracture group and were significantly lower in the fracture-Arcoxia group. Fever appeared to be aggravated by acetaminophen and more related to the elevation of hepatic

  10. 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.

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

    Directory of Open Access Journals (Sweden)

    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

  12. One-pot three-component synthesis of novel heterocyclic steroids as a central antioxidant and anti-inflammatory agents.

    Science.gov (United States)

    Mohamed, Nadia R; Abdelhalim, Mervat M; Khadrawy, Yasser A; Elmegeed, Gamal A; Abdel-Salam, Omar M E

    2012-11-01

    Oxidative stress and inflammation have been implicated in several neurodegenerative and developmental brain disorders. The present work was devoted to the design and synthesis of novel steroid derivatives bearing promising heterocyclic moiety that would act to reduce neuro-inflammation and oxidative stress in brain. The novel heterocyclic steroids were synthesized and their chemical structures were confirmed by studying their analytical and spectral data. The tested compounds were assayed in the model of neuro-inflammation produced in rats by cerebral lipopolysaccharide injection. The intracerebral administration of bacterial endotoxin resulted in cerebral inflammatory state evidenced by increased malondialdehyde (MDA), decreased reduced glutathione (GSH) level, increased nitric oxide as well as increased acetylcholinesterase (AChE) activity in the brain. Compounds 6, 10, 8b and 13a markedly increased reduced glutathione. Malondialadehyde and nitric oxide levels were reduced to normal values after treatment with all tested compounds. AChE activity was normalized by compound 8b and reduced to below normal values by compounds 10 and 14a. These results are exciting in that these agents might be useful candidates in treatment of cerebral inflammation.

  13. Role of carbonyl reducing enzymes in the phase I biotransformation of the non-steroidal anti-inflammatory drug nabumetone in vitro.

    Science.gov (United States)

    Skarydova, Lucie; Nobilis, Milan; Wsól, Vladimir

    2013-04-01

    1. Nabumetone is a clinically used non-steroidal anti-inflammatory drug, its biotransformation includes major active metabolite 6-methoxy-2-naphtylacetic acid and another three phase I as well as corresponding phase II metabolites which are regarded as inactive. One important biotransformation pathway is carbonyl reduction, which leads to the phase I metabolite, reduced nabumetone. 2. The aim of this study is the determination of the role of a particular human liver subcellular fraction in the nabumetone reduction and the identification of participating carbonyl reducing enzymes along with their stereospecificities. 3. Both subcellular fractions take part in the carbonyl reduction of nabumetone and the reduction is at least in vitro the main biotransformation pathway. The activities of eight cytosolic carbonyl reducing enzymes--CBR1, CBR3, AKR1B1, AKR1B10, AKR1C1-4--toward nabumetone were tested. Except for CBR3, all tested reductases transform nabumetone to its reduced metabolite. AKR1C4 and AKR1C3 have the highest intrinsic clearances. 4. The stereospecificity of the majority of the tested enzymes is shifted to the production of an (+)-enantiomer of reduced nabumetone; only AKR1C1 and AKR1C4 produce predominantly an (-)-enantiomer. This project provides for the first time evidence that seven specific carbonyl reducing enzymes participate in nabumetone metabolism.

  14. 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.

  15. Side-Effects of Non-Steroidal Anti-Inflammatory Drugs on the Liver in Dogs and Hepatoprotective Effect of Plant Remedies

    Directory of Open Access Journals (Sweden)

    Szweda Magdalena

    2014-10-01

    Full Text Available Hepatoprotective effect of plant drugs against hepatic tissue injury induced by non-steroidal anti-inflammatory drugs (NSAIDs was assessed on Beagle dogs. The adverse effects of carprofen and robenacoxib on the hepatic tissue were evaluated on the basis of histopathological examination of liver sections. It was demonstrated that the use of NSAIDs with liquorice and composed plant remedy Pectosol¯ caused a reduction of hepatic adverse effects induced by the administration of NSAIDs. This fact indicates a hepatoprotective effect of the tested plant remedies during the treatment with NSAIDs. However, the results require further studies on a larger group of animals. Liquorice and Pectosol¯ reduce the hepatic side effects, which develop after the treatment with carprofen and, to a lesser extent, robenacoxib in young Beagles. Such studies allow to investigate the negative and positive effects of using robenacoxib and carprofen in dogs and, therefore, help to limit the NSAID-induced side effects on the liver in these animals.

  16. 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.

  17. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  19. Effect of non-steroidal anti-inflammatory drugs on biological properties of Acanthamoeba castellanii belonging to the T4 genotype.

    Science.gov (United States)

    Siddiqui, Ruqaiyyah; Lakhundi, Sahreena; Iqbal, Junaid; Khan, Naveed Ahmed

    2016-09-01

    Non-steroidal anti-inflammatory drug, Diclofenac, targeting COX have shown promise in the treatment of Acanthamoeba keratitis, but the underlying mechanisms remain unknown. Using various NSAIDs, Diclofenac sodium, Indomethacin, and Acetaminophen, here we determined the effects of NSAIDs on the biological properties of Acanthamoeba castellanii belonging to the T4 genotype. Using amoebicidal assays, the results revealed that Diclofenac sodium, and Indomethacin affected growth of A. castellanii. In contrast, none of the compounds tested had any effect on the viability of A. castellanii. Importantly, all NSAIDs tested abolished A. castellanii encystation. This is a significant finding as the ability of amoebae to transform into the dormant cyst form presents a significant challenge in the successful treatment of infection. The NSAIDs inhibit production of cyclo-oxegenase, which regulates the synthesis of prostaglandins suggesting that cyclooxygenases (COX-1 and COX-2) and prostaglandins play significant role(s) in Acanthamoeba biology. As NSAIDs are routinely used in the clinical practice, these findings may help design improved preventative strategies and/or of therapeutic value to improve prognosis, when used in combination with other anti-amoebic drugs.

  20. Practical experience with the treatment of recipient mares with a non-steroidal anti-inflammatory drug in an equine embryo transfer programme.

    Science.gov (United States)

    Koblischke, P; Budik, S; Müller, J; Aurich, C

    2010-12-01

    As part of a commercial embryo transfer programme, 20 embryos were transferred to spontaneously synchronous or synchronized recipient mares. In 14 cases, embryo recipients were treated with non-steroidal anti-inflammatory drugs (NSAID), receiving flunixin meglumine i.v. at the time of transfer and vedaprofen orally twice a day on the 3 days after embryo transfer, while six embryos were transferred to untreated mares that served as controls. Out of the 14 recipient mares treated with NSAID, 11 (79%) were pregnant at 6-8 days after transfer and in 10 mares, the pregnancy was continued. From the six untreated recipients, only one became pregnant but underwent early embryonic death between day 14 and 35 after ovulation. In conclusion, pregnancy rate in NSAID-treated recipients is higher than that in untreated recipients and above reported average values, indicating that treatment of recipient mares with NSAID helps to increase pregnancy rates after transcervical transfer and can be recommended for equine embryo transfer.

  1. Metal-organic frameworks@graphene hybrid aerogels for solid-phase extraction of non-steroidal anti-inflammatory drugs and selective enrichment of proteins.

    Science.gov (United States)

    Zhang, Xiaoqiong; Liang, Qionglin; Han, Qiang; Wan, Wei; Ding, Mingyu

    2016-06-20

    Graphene aerogel (GA)-supported metal-organic framework (MOF) particles with a three-dimensional (3D) architecture were fabricated for the first time via a facile template-free "sol-cryo" method. The prepared MOFs@graphene hybrid aerogels exhibit a 3D interconnected macroporous framework of graphene sheets with uniform dispersion of MOF particles. We also report the first attempt at using the hybrid aerogels as adsorbents for the solid-phase extraction (SPE) of non-steroidal anti-inflammatory drugs (NSAIDs) and the selective enrichment of proteins. The macroporous skeletons of GA provide both low backpressure and rapid mass transfer in SPE application, thus overcoming the obstacle of high backpressure caused by directly packing submicron or micron sized MOF particles into SPE cartridges. Excellent performances including satisfactory recoveries, high sensitivity and good reproducibility were achieved in the extraction of five NSAIDs. The hybrid aerogels also showed an interesting ability for selective enrichment of ribonuclease A (RNase A) and simultaneous exclusion of cytochrome C (Cyt C) and lysozyme (Lyz), which could be attributed to the electrostatic interactions between proteins and the positively charged coordinatively unsaturated metal sites (CUS) in MIL-101. We believe that this work will promote the application of MOFs in adsorption and separation, and our synthetic strategy could be further extended to develop other graphene-based hybrid aerogels.

  2. 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.

  3. 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.

  4. Non-steroidal anti-inflammatory drugs decrease E2F1 expression and inhibit cell growth in ovarian cancer cells.

    Directory of Open Access Journals (Sweden)

    Blanca L Valle

    Full Text Available Epidemiological studies have shown that the regular use of non-steroidal anti-inflammatory (NSAIDs drugs is associated with a reduced risk of various cancers. In addition, in vitro and experiments in mouse models have demonstrated that NSAIDs decrease tumor initiation and/or progression of several cancers. However, there are limited preclinical studies investigating the effects of NSAIDs in ovarian cancer. Here, we have studied the effects of two NSAIDs, diclofenac and indomethacin, in ovarian cancer cell lines and in a xenograft mouse model. Diclofenac and indomethacin treatment decreased cell growth by inducing cell cycle arrest and apoptosis. In addition, diclofenac and indomethacin reduced tumor volume in a xenograft model of ovarian cancer. To identify possible molecular pathways mediating the effects of NSAID treatment in ovarian cancer, we performed microarray analysis of ovarian cancer cells treated with indomethacin or diclofenac. Interestingly, several of the genes found downregulated following diclofenac or indomethacin treatment are transcriptional target genes of E2F1. E2F1 was downregulated at the mRNA and protein level upon treatment with diclofenac and indomethacin, and overexpression of E2F1 rescued cells from the growth inhibitory effects of diclofenac and indomethacin. In conclusion, NSAIDs diclofenac and indomethacin exert an anti-proliferative effect in ovarian cancer in vitro and in vivo and the effects of NSAIDs may be mediated, in part, by downregulation of E2F1.

  5. Gastrotoxic activity and inhibitory effects on gastric mucosal PGE2 production with different non-steroidal anti-inflammatory drugs: modifications induced by pretreatment with zinc acexamate.

    Science.gov (United States)

    Navarro, C; Bravo, M L; Carulla, C; Bulbena, O

    1994-06-01

    Gastrotoxic activities of different non-steroidal anti-inflammatory drugs (NSAIDs) (diclofenac, indomethacin, ketoprofen, naproxen and piroxicam) administered per os were compared with their ability to inhibit gastric prostaglandin E2 (PGE2) synthesis in the rat. In a parallel study, effects of pretreatment with zinc acexamate (ZAC) were also assessed. NSAIDs invariably caused gastric mucosal damage and a decrease of PGE2 levels. A good correlation between the decrease of PGE2 levels and the index of gastric lesion (r = 0.41; p < 0.021) was observed when results obtained with the different NSAIDs were pooled. ZAC pretreatment significantly decreased the overall severity of lesions induced by NSAIDs. However, no correlation between gastric lesion index and depletion of PGE2 gastric levels was observed after treatment with ZAC (r = 0.012; p < 0.948). These data corroborate the hypothesis that preservation of the capability to synthesize endogenous PGs is of critical importance in the maintenance of gastric mucosal integrity. The gastroprotective action observed with ZAC involves alternative mechanisms other than modification of PGE2 levels.

  6. 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.

  7. The effect of sulindac, a non-steroidal anti-inflammatory drug, attenuates inflammation and fibrosis in a mouse model of chronic pancreatitis

    Directory of Open Access Journals (Sweden)

    Bai Han

    2012-08-01

    Full Text Available Abstract Background Chronic pancreatitis is characterized by progressive fibrosis, pain and loss of exocrine and endocrine functions. The long-standing chronic pancreatitis and its associated pancreatic fibrosis are the most common pathogenic events involved in human pancreatic carcinogenesis, but the therapeutic strategies to chronic pancreatitis and the chemoprevention of pancreatic carcinogenesis are very limited. Methods We investigated the effect of sulindac, a non-steroidal anti-inflammatory drug (NSAID, on inhibition of chronic pancreatitis in a caerulein induced chronic pancreatitis mouse model. Results Sulindac significantly reduced the severity of chronic pancreatitis including the extent of acini loss, inflammatory cell infiltration and stromal fibrosis. The protein expression of phosphorylation of MEK/ERK was inhibited in the chronic pancreatic tissues by sulindac treatment as measured by Western blot assay. The levels of inflammatory cytokines including TNF-α and MCP-1 were also significantly decreased with sulindac treatment, as well as the expression of TGF-β, PDGF-β, SHH and Gli in the chronic pancreatic tissue detected by qPCR assay and confirmed by western blot assay. The activation of pancreatic satellet cells was also inhibited by sulindac as measured by the activity of α-smooth muscle actin (α-SMA in the pancreatic tissue of chronic pancreatitis. Conclusions Sulindac is a promising reagent for the treatment of chronic pancreatitis via inhibition of inflammatory cell infiltration and stromal fibrosis, the inhibitory effect of sulindac on chronic pancreatitis may through targeting the activation ERK/MAPK signaling pathway.

  8. In Vitro Interactions between Non-Steroidal Anti-Inflammatory Drugs and Antifungal Agents against Planktonic and Biofilm Forms of Trichosporon asahii.

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    Suteng Yang

    Full Text Available Increasing drug resistance has brought enormous challenges to the management of Trichosporon spp. infections. The in vitro antifungal activities of non-steroidal anti-inflammatory drugs (NSAIDs against Candida spp. and Cryptococcus spp. were recently discovered. In the present study, the in vitro interactions between three NSAIDs (aspirin, ibuprofen and diclofenac sodium and commonly used antifungal agents (fluconazole, itraconazole, voriconazole, caspofungin and amphotericin B against planktonic and biofilm cells of T. asahii were evaluated using the checkerboard microdilution method. The spectrophotometric method and the XTT reduction assay were used to generate data on biofilm cells. The fractional inhibitory concentration index (FICI and the ΔE model were compared to interpret drug interactions. Using the FICI, the highest percentages of synergistic effects against planktonic cells (86.67% and biofilm cells (73.33% were found for amphotericin B/ibuprofen, and caspofungin/ibuprofen showed appreciable percentages (73.33% for planktonic form and 60.00% for biofilm as well. We did not observe antagonism. The ΔE model gave consistent results with FICI (86.67%. Our findings suggest that amphotericin B/ibuprofen and caspofungin/ibuprofen combinations have potential effects against T. asahii. Further in vivo and animal studies to investigate associated mechanisms need to be conducted.

  9. 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.

  10. Evaluation of the anti-inflammatory effects of steroids and arthritis-related biotherapies in an in vitro co-culture model with immune cells and synoviocytes

    Directory of Open Access Journals (Sweden)

    Melissa Noack

    2016-11-01

    Full Text Available Background: During rheumatoid arthritis (RA, steroids and biotherapies are used alone and combined. Efficacy has been established in clinical trials but their differential effects at the cellular level are less documented. The aim was to study these cellular effects using an in vitro model with synoviocytes interacting with peripheral blood mononuclear cells (PBMC to reproduce the interactions in the RA synovium.Methods: Activated-PBMC were co-cultured with RA synoviocytes during 48h. A dose-response of methylprednisolone (MP was tested and different biotherapies (Infliximab, Etanercept, Adalimumab, Tocilizumab, Abatacept and Rituximab were added alone or in combination with MP. Cytokine production (IL-17, IL-6, IL-1β, IFN-γ and IL-10 was measured by ELISA.Results: Addition of MP to co-cultures inhibited the production of all cytokines. The response to the biotherapies alone was treatment-dependent. IL-17 production was inhibited only by Tocilizumab (p=0.004 while IL-6 was decreased only by Infliximab (p≤0.002. IL-1β level was affected in all conditions (p≤0.03. IFN-γ production was mainly decreased by Infliximab (p=0.004, and IL-10 by Infliximab and Tocilizumab (p≤0.004. The combination MP and biotherapy did not induce an additional effect on pro-inflammatory cytokine inhibition. The combination MP and biotherapies induced a higher IL-10 secretion than MP alone, mainly with Rituximab.Conclusion: Steroids inhibited the secretion of all cytokines, and low doses were as potent. The anti-inflammatory effect of biotherapies was dependent on their mechanism of action. MP and biotherapy combination did not enhance the inhibitory effect on pro-inflammatory cytokines but could have a beneficial effect by increasing IL-10 production.

  11. Concentration of Non-Steroidal Anti-Inflammatory Drugs in the Pelvic Floor Muscles: An Experimental Comparative Rat Model

    Science.gov (United States)

    Chin, Hung-Yen; Changchien, Eileen; Lin, Mei-Fung; Chiang, Chi-Hsin

    2014-01-01

    Purpose The aim of this study is to explore non-steroid anti-inflammation drugs (NSAIDs) potency for pelvic floor muscle pain by measuring local concentration in a rat model. Materials and Methods We used nine NSAIDs, including nabumetone, naproxen, ibuprofen, meloxicam, piroxicam, diclofenac potassium, etodolac, indomethacin, and sulindac, and 9 groups of female Wister rats. Each group of rats was fed with one kind of NSAID (2 mg/mL) for three consecutive days. Thereafter, one mL of blood and one gram of pelvic floor muscle were taken to measure drug pharmacokinetics, including partition coefficient, lipophilicity, elimination of half-life (T1/2) and muscle/plasma converting ratio (Css, muscle/Css, plasma). Results Diclofenac potassium had the lowest T1/2 and the highest mean Css, muscle/Css, plasma (1.9 hours and 0.85±0.53, respectively). The mean Css, muscle/Css, plasma of sulindac, naproxen and ibuprofen were lower than other experimental NSAIDs. Conclusion Diclofenac potassium had the highest disposition in pelvic floor muscle in a rat model. The finding implies that diclofenac potassium might be the choice for pain relief in pelvic muscle. PMID:24954342

  12. Acupuncture with non-steroidal anti-inflammatory drugs (NSAIDs) versus acupuncture or NSAIDs alone for the treatment of chronic neck pain: an assessor-blinded randomised controlled pilot study

    OpenAIRE

    2013-01-01

    Objective To investigate the feasibility and sample size required for a full-scale randomised controlled trial of the effectiveness of acupuncture with non-steroidal anti-inflammatory drugs (NSAIDs) for chronic neck pain compared with acupuncture or NSAID treatment alone. Methods A total of 45 patients with chronic neck pain participated in the study. For 3 weeks the acupuncture with NSAIDs treatment group took NSAIDs (zaltoprofen, 80 mg) daily while receiving acupuncture treatment three time...

  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. Nonsteroid Anti-inflammatory Drugs and Kidney

    OpenAIRE

    Yaşar Yıldırım; Zülfükar Yılmaz; A. Veysel Kara1; et al.,

    2016-01-01

    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, dehydr...

  15. Variants of CEP68 gene are associated with acute urticaria/angioedema induced by multiple non-steroidal anti-inflammatory drugs.

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    José Antonio Cornejo-García

    Full Text Available Non-steroidal anti-inflammatory drugs (NSAIDs are the most consumed drugs worldwide because of their efficacy and utility in the treatment of pain and inflammatory diseases. However, they are also responsible for an important number of adverse effects including hypersensitivity reactions. The most important group of these reactions is triggered by non-immunological, pharmacological mechanisms catalogued under the denomination of cross-intolerance (CRI, with acute urticaria/angioedema induced by multiple NSAIDs (MNSAID-UA the most frequently associated clinical entity. A recent genome-wide association study identified the gene encoding the centrosomal protein of 68 KDa (CEP68 as the major locus associated with aspirin intolerance susceptibility in asthmatics. In this study, we aimed to assess the role of this locus in susceptibility to CRI to NSAIDs by examining 53 common gene variants in a total of 635 patients that were classified as MNSAID-UA (n = 399, airway exacerbations (n = 110 or blended pattern (n = 126, and 425 controls. We found in the MNSAID-UA group a number of variants (17 associated (lowest p-value = 1.13 × 10(-6, including the non-synonymous Gly74Ser variant (rs7572857 previously associated with aspirin intolerance susceptibility in asthmatics. Although not being significant in the context of multiple testing, eight of these variants were also associated with exacerbated respiratory disease or blended reactions. Our results suggest that CEP68 gene variants may play an important role in MNSAID-UA susceptibility and, despite the different regulatory mechanisms involved depending on the specific affected organ, in the development of hypersensitivity reactions to NSAIDs.

  16. Variants of CEP68 gene are associated with acute urticaria/angioedema induced by multiple non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Cornejo-García, José Antonio; Flores, Carlos; Plaza-Serón, María C; Acosta-Herrera, Marialbert; Blanca-López, Natalia; Doña, Inmaculada; Torres, María J; Mayorga, Cristobalina; Guéant-Rodríguez, Rosa M; Ayuso, Pedro; Fernández, Javier; Laguna, José J; Agúndez, José A G; García-Martín, Elena; Guéant, Jean-Louis; Canto, Gabriela; Blanca, Miguel

    2014-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are the most consumed drugs worldwide because of their efficacy and utility in the treatment of pain and inflammatory diseases. However, they are also responsible for an important number of adverse effects including hypersensitivity reactions. The most important group of these reactions is triggered by non-immunological, pharmacological mechanisms catalogued under the denomination of cross-intolerance (CRI), with acute urticaria/angioedema induced by multiple NSAIDs (MNSAID-UA) the most frequently associated clinical entity. A recent genome-wide association study identified the gene encoding the centrosomal protein of 68 KDa (CEP68) as the major locus associated with aspirin intolerance susceptibility in asthmatics. In this study, we aimed to assess the role of this locus in susceptibility to CRI to NSAIDs by examining 53 common gene variants in a total of 635 patients that were classified as MNSAID-UA (n = 399), airway exacerbations (n = 110) or blended pattern (n = 126), and 425 controls. We found in the MNSAID-UA group a number of variants (17) associated (lowest p-value = 1.13 × 10(-6)), including the non-synonymous Gly74Ser variant (rs7572857) previously associated with aspirin intolerance susceptibility in asthmatics. Although not being significant in the context of multiple testing, eight of these variants were also associated with exacerbated respiratory disease or blended reactions. Our results suggest that CEP68 gene variants may play an important role in MNSAID-UA susceptibility and, despite the different regulatory mechanisms involved depending on the specific affected organ, in the development of hypersensitivity reactions to NSAIDs.

  17. 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.

  18. 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.

  19. 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.

  20. Molecular modeling and simulation studies of recombinant laccase from Yersinia enterocolitica suggests significant role in the biotransformation of non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Singh, Deepti; Rawat, Surender; Waseem, Mohd; Gupta, Sunita; Lynn, Andrew; Nitin, Mukesh; Ramchiary, Nirala; Sharma, Krishna Kant

    2016-01-08

    The YacK gene from Yersinia enterocolitica strain 7, cloned in pET28a vector and expressed in Escherichia coli BL21 (DE3), showed laccase activity when oxidized with 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and guaiacol. The recombinant laccase protein was purified and characterized biochemically with a molecular mass of ≈58 KDa on SDS-PAGE and showed positive zymogram with ABTS. The protein was highly robust with optimum pH 9.0 and stable at 70 °C upto 12 h with residual activity of 70%. Kinetic constants, Km values, for ABTS and guaiacol were 675 μM and 2070 μM, respectively, with corresponding Vmax values of 0.125 μmol/ml/min and 6500 μmol/ml/min. It also possess antioxidative property against BSA and Cu(2+)/H2O2 model system. Constant pH MD simulation studies at different protonation states of the system showed ABTS to be most stable at acidic pH, whereas, diclofenac at neutral pH. Interestingly, aspirin drifted out of the binding pocket at acidic and neutral pH, but showed stable binding at alkaline pH. The biotransformation of diclofenac and aspirin by laccase also corroborated the in silico results. This is the first report on biotransformation of non-steroidal anti-inflammatory drugs (NSAIDs) using recombinant laccase from gut bacteria, supported by in silico simulation studies.

  1. Occurrence and behavior of non-steroidal anti-inflammatory drugs and lipid regulators in wastewater and urban river water of the Pearl River Delta, South China.

    Science.gov (United States)

    Huang, Qiuxin; Yu, Yiyi; Tang, Caiming; Zhang, Kun; Cui, Jianlan; Peng, Xianzhi

    2011-04-01

    Occurrence of five non-steroidal anti-inflammatory drugs (salicylic acid, ibuprofen, naproxen, indomethacin and diclofenac) and three lipid regulators (bezafibrate, clofibric acid and gemfibrozil) was investigated in wastewater, sewage sludge, and river water of the urban section of the Pearl River at Guangzhou in South China. Behavior and fate of the pharmaceuticals during treatment in two sewage treatment plants (STPs) were also studied in depth by determining concentrations in the influents and effluents at major treatment units and the sewage sludge. Concentrations of the pharmaceuticals in the raw wastewater were mostly at ng L(-1) levels except salicylic acid whose concentrations ranged from 9.6 to 23.3 μg L(-1). No significant amount of the pharmaceuticals was detected in the suspended particulate matter of wastewater and sewage sludge. Salicylic acid, indomethacin, and naproxen were almost completely removed (≥ 99%); gemfibrozil, ibuprofen and bezafibrate were significantly removed (>75%), whereas diclofenac and clofibric acid were removed by 60-70% during treatment in the STPs. Generally, biodegradation was the governing process for elimination of the investigated pharmaceuticals. Anaerobic biodegradation was responsible for most of the removal of diclofenac whereas aerobic biodegradation also played an important role in elimination of the other pharmaceuticals except SA, which was nearly completely removed after the anoxic process. In the Pearl River, the pharmaceuticals were widely detected. Both the concentrations and detection frequency were higher in March 2008 than those in the other seasons, which may be ascribed mainly to less dilution caused by lower precipitation. Besides the STPs, urban canals directly connected with the Pearl River may also be important contributors to the pharmaceutical contamination in the river.

  2. 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.

  3. Association of individual non-steroidal anti-inflammatory drugs and chronic kidney disease: a population-based case control study.

    Directory of Open Access Journals (Sweden)

    Ylenia Ingrasciotta

    Full Text Available Non-steroidal anti-inflammatory agents (NSAIDs are known to be associated with renal damage. No clear evidence exists regarding differential risk of chronic kidney disease (CKD, specifically, across various NSAIDs.The aim of this population-based case-control study was to evaluate the association between use of individual NSAIDs and risk of CKD in a general population of Southern Italy.A nested case-control study was carried out using the general practice Arianna database, identifying incident CKD patients as cases and matched controls from 2006 to 2011. The date of first CKD diagnosis was defined as the index date (ID. Conditional logistic regressions were performed to estimate the risk of CKD associated with NSAIDs by class and individual drugs as compared to non-use during different time windows (within one year, six or three months prior to ID, with the latter being defined as current users. Among current users, the effect of cumulative exposure to these drugs was evaluated.Overall, 1,989 CKD cases and 7,906 matched controls were identified. A statistically significant increase in the risk of CKD was found for current users of oxicams (adjusted OR: 1.68; 95% CI: 1.15-2.44 and concerning individual compounds, for ketorolac (adj. OR: 2.54; 95% CI: 1.45-4.44, meloxicam (adj. OR: 1.98; 95% CI: 1.01-3.87 and piroxicam (adj. OR: 1.95; 95% CI: 1.19-3.21.The risk of CKD varies across individual NSAIDs. Increased risk has been found for ketorolac, which may precipitate subclinical CKD through acute renal damage, and long-term exposure to oxicams, especially meloxicam and piroxicam.

  4. Non-steroidal anti-inflammatory drugs and paracetamol in self-therapy of various disorders in students of different fields of study.

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    Wiliński, Jerzy; Lechowicz, Marta; Kameczura, Tomasz; Głowacki, Mikołaj; Kameczura, Anna; Chrapusta, Anna; Wiliński, Bogdan

    2015-01-01

    Over-the-counter non-steroidal anti-inflammatory drugs (NSAIDs) and paracetamol are most commonly the first-line pharmacotherapy in combating different pain and inflammatory disorders and fever. Unfortunately, those drugs might have serious side effects, especially when they are used in an inappropriate way. The aim of the study was to explore various aspects of NSAIDs and paracetamol use in the self-therapy of miscellaneous disorders in young adults. The questionnaire-based survey comprised 250 consecutive students aged 22.1 ± 1.9 years (189 women) of diverse fields of study. The drugs were applied in clinical conditions in which they should be avoided including asthma attack (1.2%), vomiting (2.4%), malaise and depression (3.6%), in autumn and winter as a preventive measure against infections (14.0%), heart-burn (2.0%) and during food poisoning (16.0%). As many as 6.0% of the students claimed that studied medications are ultimately free of adverse reactions. Men more frequently than women used NSAIDs and paracetamol during alcohol consumption (49.2% vs 30.7%, p = 0.009, respectively) but less often were aware that there are maximum doses of medications which should not be exceeded (57.4% vs 76.7%, p = 0.003, respectively). The students of medical-related degree courses (n = 82) compared with individuals of other subjects (n = 168) declared they more often have the custom of always reading medications' leaflets (46.3% vs 31.0%, p = 0.017, respectively). Side effects of medicines were reported by 65 participants - 26.0%. In conclusion, students' knowledge about NSAIDs and paracetamol is low. Participants do not search for information on drug related endangerments, the medication group choice for the given disorder is often inappropriate and the drugs are applied in conditions in which they are contraindicated.

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

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    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.

  6. Fabrication of aluminum terephthalate metal-organic framework incorporated polymer monolith for the microextraction of non-steroidal anti-inflammatory drugs in water and urine samples.

    Science.gov (United States)

    Lyu, Dan-Ya; Yang, Cheng-Xiong; Yan, Xiu-Ping

    2015-05-08

    Polymer monolith microextraction (PMME) based on capillary monolithic column is an effective and useful technique to preconcentrate trace analytes from environmental and biological samples. Here, we report the fabrication of a novel aluminum terephthalate metal-organic framework (MIL-53(Al)) incorporated capillary monolithic column via in situ polymerization for the PMME of non-steroidal anti-inflammatory drugs (NSAIDs) (ketoprofen, fenbufen and ibuprofen) in water and urine samples. The fabricated MIL-53(Al) incorporated monolith was characterized by X-ray powder diffractometry, scanning electron microscopy, Fourier transform infrared spectrometry, and nitrogen adsorption experiment. The MIL-53(Al) incorporated monolith gave larger surface area than the neat polymer monolith. A 2-cm long MIL-53(Al) incorporated capillary monolith was applied for PMME coupled with high-performance liquid chromatography for the determination of the NSAIDs. Potential factors affecting the PMME were studied in detail. Under the optimized conditions, the developed method gave the enhancement factors of 46-51, the linear range of 0.40-200μgL(-1), the detection limits (S/N=3) of 0.12-0.24μgL(-1), and the quantification limits (S/N=10) of 0.40-0.85μgL(-1). The recoveries for spiked NSAIDs (20μgL(-1)) in water and urine samples were in the range of 77.3-104%. Besides, the MIL-53(Al) incorporated monolith was stable enough for 120 extraction cycles without significant loss of extraction efficiency. The developed method was successfully applied to the determination of NSAIDs in water and urine samples.

  7. Variants of CEP68 Gene Are Associated with Acute Urticaria/Angioedema Induced by Multiple Non-Steroidal Anti-Inflammatory Drugs

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    Cornejo-García, José Antonio; Flores, Carlos; Plaza-Serón, María C.; Acosta-Herrera, Marialbert; Blanca-López, Natalia; Doña, Inmaculada; Torres, María J.; Mayorga, Cristobalina; Guéant-Rodríguez, Rosa M.; Ayuso, Pedro; Fernández, Javier; Laguna, José J.; Agúndez, José A. G.; García-Martín, Elena; Guéant, Jean-Louis; Canto, Gabriela; Blanca, Miguel

    2014-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are the most consumed drugs worldwide because of their efficacy and utility in the treatment of pain and inflammatory diseases. However, they are also responsible for an important number of adverse effects including hypersensitivity reactions. The most important group of these reactions is triggered by non-immunological, pharmacological mechanisms catalogued under the denomination of cross-intolerance (CRI), with acute urticaria/angioedema induced by multiple NSAIDs (MNSAID-UA) the most frequently associated clinical entity. A recent genome-wide association study identified the gene encoding the centrosomal protein of 68 KDa (CEP68) as the major locus associated with aspirin intolerance susceptibility in asthmatics. In this study, we aimed to assess the role of this locus in susceptibility to CRI to NSAIDs by examining 53 common gene variants in a total of 635 patients that were classified as MNSAID-UA (n = 399), airway exacerbations (n = 110) or blended pattern (n = 126), and 425 controls. We found in the MNSAID-UA group a number of variants (17) associated (lowest p-value = 1.13×10−6), including the non-synonymous Gly74Ser variant (rs7572857) previously associated with aspirin intolerance susceptibility in asthmatics. Although not being significant in the context of multiple testing, eight of these variants were also associated with exacerbated respiratory disease or blended reactions. Our results suggest that CEP68 gene variants may play an important role in MNSAID-UA susceptibility and, despite the different regulatory mechanisms involved depending on the specific affected organ, in the development of hypersensitivity reactions to NSAIDs. PMID:24618698

  8. 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.

  9. 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.

  10. 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.

  11. 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.

  12. Effects of Preoperative Non-Steroidal Anti-Inflammatory Drugs on Pain Mitigation and Patients’ Shoulder Performance Following Rotator Cuff Repair

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    Alireza Rouhani

    2014-12-01

    Full Text Available Purpose: Pain is one of the most important factors adversely affecting clinical outcomes of operated patients. The present study aims at evaluating effects of preoperative COX2 non-steroidal anti-inflammatory inhibitors on pain mitigation and performance of patients with shoulder rotator cuff tear. Methods: This case-control study was conducted on 60 patients suffering from rotator cuff injury candidate for arthroscopic repair. The patients were classified in two parallel and matched groups. One group (case group was treated using Celecoxib (200mg/12h started 48 hours before surgery and continued for 10 days after operation. In the control group, the placebo was prescribed in the same way. Postoperative pain, side effects, sleep disturbance, and short-term outcomes were compared between two groups using DASH questionnaire. Results: Postoperative pain in the Celecoxib group significantly decreased in comparison with the control one. The difference was statistically meaningful (P<0.001. Well motion ability was seen in 80% of patients of the Celecoxib group. It was 26.6% in the placebo group since pain inhibited them from exercising more motions. In this regard, there was a statistically meaningful difference between these two groups (P=0.02. Sleep disturbance was meaningfully at higher levels in the placebo group (P=0.001. Following up the patients for three months, it was made clear that performance of the Celecoxib group was better than that of the placebo one. Conclusion: COX2 inhibitors are well efficient in patients’ pain management after arthroscopic rotator cuff repair surgery. It results in less life complications, less sleep disturbances, improvement of patients’ short-term clinical outcome, and more quick recovery.

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

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    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

  14. Poly(2-aminobenzothiazole)-coated graphene oxide/magnetite nanoparticles composite as an efficient sorbent for determination of non-steroidal anti-inflammatory drugs in urine sample.

    Science.gov (United States)

    Asgharinezhad, Ali Akbar; Ebrahimzadeh, Homeira

    2016-02-26

    In this study, for the first time, 2-aminobenzothiazole monomer was polymerized on Fe3O4 NPs, graphene oxide/Fe3O4 (GO/Fe3O4) and graphene/Fe3O4 (G/Fe3O4) nanocomposites. The synthesized magnetic nanosorbents were characterized by various techniques. The extraction ability of these nanosorbents including Fe3O4, GO/Fe3O4, G/Fe3O4, Fe3O4@poly(2-aminobenzothiazole) (Fe3O4@PABT), GO/Fe3O4@PABT and G/Fe3O4@PABT were compared for dispersive-micro-solid phase extraction of three non-steroidal anti-inflammatory drugs. The results revealed that GO/Fe3O4@PABT nanocomposite demonstrates higher extraction efficiency for naproxen, diclofenac and ibuprofen as selected model analytes. Following the sorption and elution steps, the model analytes were quantified by high performance liquid chromatography-photo diode array detection. Afterwards, a central composite design methodology combined with desirability function approach was applied to find out the optimal experimental conditions. Under the optimized conditions, the limits of detection and linear dynamic ranges were achieved in the range of 0.07-0.3 μg L(-1) and 0.25-2000 μg L(-1), respectively. The percent of extraction recovery was 87.4, 85.5 and 90.5% for naproxen, diclofenac and ibuprofen, respectively. The obtained relative standard deviation (n=5) was 7.2, 5.4 and 6.4% for naproxen, diclofenac and ibuprofen, respectively. Ultimately, this method was employed for urinary monitoring of the target analytes and satisfactory results were obtained.

  15. Micropropagation and non-steroidal anti-inflammatory and anti-arthritic agent boswellic acid production in callus cultures of Boswellia serrata Roxb.

    Science.gov (United States)

    Nikam, Tukaram D; Ghorpade, Ravi P; Nitnaware, Kirti M; Ahire, Mahendra L; Lokhande, Vinayak H; Chopra, Arvind

    2013-01-01

    Micropropagation through cotyledonary and leaf node and boswellic acid production in stem callus of a woody medicinal endangered tree species Boswellia serrata Roxb. is reported. The response for shoots, roots and callus formation were varied in cotyledonary and leafy nodal explants from in vitro germinated seeds, if inoculated on Murshige and Skoog's (MS) medium fortified with cytokinins and auxins alone or together. A maximum of 8.0 ± 0.1 shoots/cotyledonary node explant and 6.9 ± 0.1 shoots/leafy node explants were produced in 91 and 88 % cultures respectively on medium with 2.5 μM 6-benzyladenine (BA) and 200 mg l(-1) polyvinylpyrrolidone (PVP). Shoots treated with 2.5 μM IBA showed the highest average root number (4.5) and the highest percentage of rooting (89 %). Well rooted plantlets were acclimatized and 76.5 % of the plantlets showed survival upon transfer to field conditions. Randomly amplified polymorphic DNA (RAPD) analysis of the micropropagated plants compared with mother plant revealed true-to-type nature. The four major boswellic acid components in calluses raised from root, stem, cotyledon and leaf explants were analyzed using HPLC. The total content of four boswellic acid components was higher in stem callus obtained on MS with 15.0 μM IAA, 5.0 μM BA and 200 mg l(-1) PVP. The protocol reported can be used for conservation and exploitation of in vitro production of medicinally important non-steroidal anti-inflammatory metabolites of B. serrata.

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

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    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

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

    Directory of Open Access Journals (Sweden)

    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.

  18. GINGIVAL TISSUE IL-1beta AND PGE2 LEVELS IN PATIENTS WITH CHRONIC PERIODONTITIS AFTER ADDITIONAL THERAPY WITH NON-STEROIDAL ANTI-INFLAMMATORY DRUGS

    Directory of Open Access Journals (Sweden)

    Christina Popova

    2010-10-01

    evaluation of gene expression levels of IL-1beta and PGE2 in gingival tissue of periodontal patients was applied. Results: Statistically significant differences were found between additional Aulin® therapy group and conventional therapy group. Received correlative coefficient with Spearman analysis was respectively t = -0.72 (p< 0,05 for IL-1beta and t = 0.81(p<0,05 for PGE2. The negative values of ddCt in test group reveal lower level of inhibition of gene expression. The comparative analysis of the collected data demonstrates fewer differences between both groups. The deviations in gene expression levels of IL -1beta and PGE2 are higher in the patients treated with adjunctive medication with Aulin®. Conclusion: This study confirms the effectiveness of non-surgical therapy in moderate and severe periodontitis. Additional use of non-steroidal anti-inflammatory agent Aulin® results in higher inhibition of the pro-inflammatory cytokines IL-1beta and PGE2. This data may be the base for modifying the conventional non-surgical therapy by including anti-inflammatory agents in the treatment of chronic periodontitis.

  19. Tenoxicam, a non-steroid anti-inflammatory drug, is unable to increase the response rate in patients with chronic hepatitis C treated by alpha interferon.

    Science.gov (United States)

    Zarski, J P; Maynard-Muet, M; Chousterman, S; Baud, M; Barnoud, R; Abergel, A; Bacq, Y; Combis, J M; Causse, X; Tran, A; Oberti, F; Minello, A; Bresson-Hadni, S; Bailly, F; Raabe, J J; Leroy, V; Hamici, L; Hicham, T; Girardin, M F

    1998-03-01

    The purpose of this study is to compare a combination of interferon (IFN)-alpha2a (Roferon) + Tenoxicam with IFN-alpha2a alone in the treatment of chronic hepatitis C. This prospective, randomized double-blind study included 149 patients, all of whom were diagnosed with active chronic hepatitis C but non-cirrhotic (ALT > or = 1.5 upper limit of normal, anti-hepatitis C virus (HCV) positive by enzyme-linked immunosorbant assay2 and RIBA3). The patients were randomized in two groups, as follows: G1 (n = 76): IFNalpha2a 3 million units times per week during 6 months + placebo; and G2 (n = 73): IFNalpha2a 3 million units three times per week + Tenoxicam (20 mg/day) during 6 months. Alanine aminotransferase (ALT) and HCV RNA were determined before and at months 6 and 12 of treatment. 2'5' oligoadenylate synthetase activity (2'5' AS) was dosed in mononuclear cells before and at 3-month treatment intervals in 28 patients. Liver biopsy was performed before and 6 months after the end of therapy. Parameters were similar before therapy for both groups. Biochemical and virological responses were similar for both groups at month 6 (49.3% vs. 42.9% and 43.3% vs. 38.3%, respectively) and month 12 (28.3% vs. 23.8% and 17.2% vs. 17.5%, respectively). HCV RNA level significantly decreased in both groups at month 6, with no difference whatever the therapy; however, the HCV RNA level returned to initial values at month 12 and was the only significant prognostic factor of a sustained response. No peak of 2'5' AS activity was observed during treatment in patients with dual therapy. A histological improvement was also noted in both groups without difference, regardless of therapy. The percentage of adverse events was identical for both groups. Paracetamol intake, assessed in 80 patients, was 49.1 g per 6 months in the G1 group and 22.5 g per 6 months in the G2 group (not significant). In conclusion, the non-steroid anti-inflammatory drug, Tenoxicam, does not increase IFNalpha efficacy in

  20. Detection of the non-steroidal anti-inflammatory drug niflumic acid in humans: a combined 19F-MRS in vivo and in vitro study.

    Science.gov (United States)

    Bilecen, Deniz; Schulte, Anja-Carina; Kaspar, Armin; Küstermann, Eckerhardt; Seelig, Joachim; Elverfeldt, Dominik; Scheffler, Klaus

    2003-05-01

    This study describes for the first time results of a (19)F-MRS study on humans exposed to the fluorinated non-steroidal anti-inflammatory drug niflumic acid. The accumulation and elimination of this commercially available selective prostaglandin synthase inhibitor is studied after an oral bolus in the human liver, in blood plasma and in urine samples. The in vivo spectra of the liver display two resonances with a similar increase in signal intensity during the investigation period of 240 min. One resonance refers to the parent compound niflumic acid (P), whereas the second resonance corresponds to a metabolite (M1) formed by the biotransformation by liver enzymes. The spectroscopic comparison with model compounds suggests 4'-hydroxyniflumic acid as the metabolite. During the entire experiment the concentration ratios of these resonances (P/M1) ranged between 0.7 and 0.9, indicating a high metabolite concentration most probably due to an efficient first pass metabolism. Both resonances (P, M1) were observed in the in vitro study of the blood plasma samples after plasma protein denaturation. However, in comparison to the liver spectra, the amount of the metabolite M1 is very small with a P/M1-ratio of 36.6 after 90 min and 16.1 after the end of measurement. This finding suggests an efficient biliary excretion of the metabolite M1, which bypasses the blood circulation system. Both resonances are also identified in the native urine samples. The signal intensity of the parent compound dominates the spectra of all urine samples, whereas the signal intensity of M1 increases slowly reaching a similar value to the parent compound P at the end of the measurement. This observation demonstrates an effective renal elimination of niflumic acid and suggests the existence of an enterohepatic circuit with a re-entry mechanism for the biliary excreted metabolite M1. In the urine spectra, an additional metabolite M2 is found. This resonance exhibits a low but constant signal

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

    Directory of Open Access Journals (Sweden)

    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

  2. Prescribing patterns of non-steroidal anti-inflammatory drugs in chronic kidney disease patients in the South African private sector.

    Science.gov (United States)

    Meuwesen, Willem P; du Plessis, Jesslee M; Burger, Johanita R; Lubbe, Martie S; Cockeran, Marike

    2016-08-01

    Background Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used pharmaceutical agents worldwide. NSAIDs are considered nephrotoxic and should therefore be used with caution or be avoided completely in high risk patients, such as chronic kidney disease (CKD) patients. Objective This study aimed to investigate the prescribing of NSAIDs in CKD patients in order to generate awareness and improve the outcome of these patients. Setting The study was conducted using medicine claims data in the private health sector of South Africa. Method A descriptive, quantitative study was performed, using retrospective data obtained from a Pharmaceutical Benefit Management company. Data from 1 January 2009 to 31 December 2013 were analysed. The study population consisted of all patients with an ICD-10 code for a CKD (N18), in association with a paid claim for an NSAID. Main outcome measure The stratification of NSAID prescribing volume among the CKD population in terms of gender, age, NSAID type, dosage and prescriber type. Results The prescribing of NSAIDs in CKD patients varied between 26 and 40 % over the 5 year study period. No association between gender and CKD patients who received NSAIDs versus those who did not was found, with p > 0.05 and Cramer's V < 0.1 for each year of the study. The association between age groups and CKD patients who received NSAIDs versus those who did not was statistically significant, but practically weak (p < 0.05; Cramer's V ≥ 0.1). Most NSAID prescriptions (52-63 %) were for patients aged 35-64 years. Diclofenac (34.25 %) was the single most frequently prescribed NSAID, but the COX-2-inhibitors (celecoxib, meloxicam and etoricoxib) were the preferred NSAID class to be prescribed. The majority (61.6 %) of the NSAIDs were prescribed by general medical practitioners in dosages meeting and even exceeding the recommended daily dosage of patients with normal kidney function. Conclusions Even though NSAIDs are

  3. Quinolones and non-steroidal anti-inflammatory drugs interacting with copper(II), nickel(II), cobalt(II) and zinc(II): structural features, biological evaluation and perspectives.

    Science.gov (United States)

    Psomas, George; Kessissoglou, Dimitris P

    2013-05-14

    The structural features of copper(II), nickel(II), cobalt(II) and zinc(II) complexes with the antimicrobial drugs quinolones and non-steroidal anti-inflammatory drugs (NSAIDs) as ligands are discussed. The binding properties of these complexes to biomolecules (calf-thymus DNA, bovine or human serum albumin) are presented and evaluated. The biological activity (antimicrobial, antioxidant and antiproliferative) of selected complexes is investigated. Further perspectives concerning the synthesis and the biological activity of novel complexes with quinolones or NSAIDs attractive to synthetic chemists, biochemists and/or biologists are presented.

  4. Anti-inflammatory Diets.

    Science.gov (United States)

    Sears, Barry

    2015-01-01

    Chronic disease is driven by inflammation. This article will provide an overview on how the balance of macronutrients and omega-6 and omega-3 fatty acids in the diet can alter the expression of inflammatory genes. In particular, how the balance of the protein to glycemic load of a meal can alter the generation of insulin and glucagon and the how the balance of omega-6 and omega-3 fatty acids can effect eicosanoid formation. Clinical results on the reduction of inflammation following anti-inflammatory diets are discussed as well as the molecular targets of anti-inflammatory nutrition. To overcome silent inflammation requires an anti-inflammatory diet (with omega-3s and polyphenols, in particular those of Maqui). The most important aspect of such an anti-inflammatory diet is the stabilization of insulin and reduced intake of omega-6 fatty acids. The ultimate treatment lies in reestablishing hormonal and genetic balance to generate satiety instead of constant hunger. Anti-inflammatory nutrition, balanced 40:30:30 with caloric restriction, should be considered as a form of gene silencing technology, in particular the silencing of the genes involved in the generation of silent inflammation. To this anti-inflammatory diet foundation supplemental omega-3 fatty acids at the level of 2-3 g of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) per day should be added. Finally, a diet rich in colorful, nonstarchy vegetables would contribute adequate amounts of polyphenols to help not only to inhibit nuclear factor (NF)-κB (primary molecular target of inflammation) but also activate AMP kinase. Understanding the impact of an anti-inflammatory diet on silent inflammation can elevate the diet from simply a source of calories to being on the cutting edge of gene-silencing technology.

  5. Effect of a non-steroidal, anti-inflammatory drug (Indocin) on selected parameters of muscular function following concentric and eccentric work

    OpenAIRE

    Vejarano, Maria Eugenia

    1985-01-01

    Evidence from various studies indicates that eccentric contractions produce more post-exercise changes in muscular function than do concentric contractions. Delayed muscular soreness, the pain and tenderness present 1 or 2 days after exercise, is negatively correlated with muscular performance and occurs particularly after eccentric work. The action of an analgesic, anti-inflammatory drug (Indocin) on muscular soreness indicates it may be effective in accelerating recover...

  6. 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

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

    OpenAIRE

    Di Pierro F; Di Maio E; Di Paola G; Felice R; Murina F

    2013-01-01

    Francesco Di Pierro,1 Eleonora Di Maio,2 Gaetana Di Paola,3 Raffaele Felice,4 Filippo Murina41Velleja Research, Milan, Italy; 2Molinette Hospital, Turin, Italy; 3ASL TO-3/TO-4, Turin, Italy; 4Outpatient Department of Vulvar Disease, V Buzzi Hospital-ICP, Milan, ItalyAim: 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 w...

  8. 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.

  9. In vitro evaluation of the effects of anti-fungals, benzodiazepines and non-steroidal anti-inflammatory drugs on the glucuronidation of 19-norandrosterone: implications on doping control analysis.

    Science.gov (United States)

    Palermo, Amelia; Alessi, Beatrice; Botrè, Francesco; de la Torre, Xavier; Fiacco, Ilaria; Mazzarino, Monica

    2016-09-01

    We have studied whether the phase II metabolism of 19-norandrosterone, the most representative metabolite of 19-nortestosterone (nandrolone), can be altered in the presence of other drugs that are not presently included on the Prohibited List of the World Anti-Doping Agency. In detail, we have evaluated the effect of non-prohibited drugs belonging to the classes of anti-fungals, benzodiazepines, and non-steroidal anti-inflammatory drugs on the glucuronidation of 19-norandrosterone. In vitro assays based on the use of either pooled human liver microsomes or specific recombinant isoforms of uridine diphosphoglucuronosyl-transferase were designed and performed to monitor the formation of 19-norandrosterone glucuronide from 19-norandrosterone. Determination of 19-norandrosterone (free and conjugated fraction) was performed by gas chromatography - mass spectrometry after sample pretreatment consisting of an enzymatic hydrolysis (performed only for the conjugated fraction), liquid/liquid extraction with tert-butylmethyl ether, and derivatization to form the trimethylsilyl derivative. In parallel, a method based on reversed-phase liquid chromatography coupled to tandem mass spectrometry in positive electrospray ionization with acquisition in selected reaction monitoring mode was also developed to identify the non-prohibited drugs considered in this study. Incubation experiments have preliminarily shown that the glucuronidation of 19-norandrosterone is principally carried out by UGT2B7 (39%) and UGT2B17 (31%). Inhibition studies have shown that the yield of the glucuronidation reaction is reduced in the presence of the anti-fungals itraconazole, ketoconazole, and miconazole, of the benzodiazepine triazolam and of the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen, while no alteration was recorded in the presence of all other compounds considered in this study. Copyright © 2015 John Wiley & Sons, Ltd.

  10. Safety of selective cyclooxygenase-2 inhibitors and a basic non-steroidal anti-inflammatory drug (NSAID) in Japanese patients with NSAID-induced urticaria and/or angioedema: Comparison of meloxicam, etodolac and tiaramide.

    Science.gov (United States)

    Inomata, Naoko; Osuna, Hiroyuki; Yamaguchi, Junko; Onoda, Masahito; Takeshita, Yoshihiro; Chiba, Yoshiyuki; Kambara, Takeshi; Ikezawa, Zenro

    2007-03-01

    The identification of a safe and reliable alternative for patients with non-steroidal anti-inflammatory drug (NSAID)-induced urticaria/angioedema is a frequent problem for dermatologists and other practitioners. Cyclooxygenase-2 (COX-2) inhibitors have been reported to be safe for NSAID-intolerant patients from the US and Europe but not all of them have yet been approved for use in Japan. It was our objective to investigate the clinical manifestations of oral NSAID challenges in Japanese patients with histories of urticaria and/or angioedema after the intake of NSAIDs and to find safe alternative drugs, including COX-2 inhibitors and a basic anti-inflammatory drug. Twenty subjects suspected NSAID-induced urticaria/angioedema from histories were included in a double-blind or single-blind, placebo-controlled oral challenge protocol using NSAIDs. Skin prick tests using NSAIDs, which were dissolved in saline, were conducted. The mean age of the patients was 37.3 years; 14 patients were female. The results of other challenge tests showed that the most frequently intolerated drugs was loxoprofen (100%), followed by acetyl salicylic (94.4%), etodolac (53.3%), dicrofenac (50%), acetaminophen (38.5%), meloxicam (33%), and tiaramide (21.4%). Urticaria and angioedema were induced after aspirin intake in 83.3% and 22.2% of patients, respectively, whereas an asthmatic response was seen in 5.6%. Skin prick tests with NSAIDs were 100% negative. This study showed that among the NSAIDs that are available in Japan and that were investigated in this study, tiaramide, which does not inhibit COX, is the relatively safe alternative drug for Japanese patients with NSAID-induced urtiacaria and/or angioedema. Furthermore, meloxicam seems to be better tolerated than etodolac between two selective COX-2 inhibitors.

  11. 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.

  12. 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.

  13. Effects of β-d-mannuronic acid, as a novel non-steroidal anti-inflammatory medication within immunosuppressive properties, on IL17, RORγt, IL4 and GATA3 gene expressions in rheumatoid arthritis patients

    Science.gov (United States)

    Barati, Anis; Jamshidi, Ahmad Reza; Ahmadi, Hossein; Aghazadeh, Zahra; Mirshafiey, Abbas

    2017-01-01

    Rheumatoid arthritis (RA) is the most common form of chronic inflammatory arthritis characterized by pain, swelling and destruction of joints, with a resultant disability. Disease-modifying anti-rheumatic drugs (DMARDs) and biological drugs can interfere with the disease process. In this study, the effect of β-d-mannuronic acid (M2000) as a novel non-steroidal anti-inflammatory drug (NSAID) with immunosuppressive and anti-inflammatory effects together with antioxidant effects was evaluated on IL17, RORγt, IL4 and GATA3 gene expression in 12 RA patients. Previously, M2000 driven from sodium alginate (natural product; patented, DEU: 102016113018.4) has shown a notable efficacy in experimental models of multiple sclerosis, RA and nephrotic syndrome. This study was performed on 12 patients with RA who had an inadequate response to conventional treatments. During this trial, patients were permitted to continue the conventional therapy excluding NSAIDs. M2000 was administered orally at a dose of 500 mg twice daily for 12 weeks. The peripheral blood mononuclear cells (PBMCs) were collected before and after treatment to evaluate the expression levels of IL4, GATA3, IL17 and RORγt. The gene expression results showed that M2000 has a potent efficacy, so that it could not only significantly decrease IL17 and RORγt levels but also increase IL4 and GATA3 levels after 12 weeks of treatment. Moreover, the gene expression results were in accordance with the clinical and preclinical assessments. In conclusion, M2000 as a natural novel agent has therapeutic and immunosuppressive properties on RA patients (identifier: IRCT2014011213739N2).

  14. Inhibition of tolbutamide 4-methylhydroxylation by a series of non-steroidal anti-inflammatory drugs in V79-NH cells expressing human cytochrome P4502C10

    NARCIS (Netherlands)

    Kappers, W.A.; Groene, E.M. de; Kleij, L.A.; Witkamp, R.F.; Zweers-Zeilmaker, W.M.; Feron, V.J.; Horbach, G.J.

    1996-01-01

    1. To study the role of cytochrome P4502C10 in the metabolism of the non-steroidal antiinflammatory drugs (NSAIDs) diclofenac, phenylbutazone, fenoprofen, ibuprofen, flurbiprofen, ketoprofen and naproxen, a cell line was developed stably expressing CYP2C10 cDNA. A retroviral vector construct, contai

  15. 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

  16. [The effect of steroidal and nonsteroidal anti-inflammatory agents on the ultrastructure of chondrocytes in the rat. Electron microscope and morphometric study].

    Science.gov (United States)

    Annefeld, M; Raiss, R; Cleres, C

    1984-01-01

    In order to obtain indications regarding the different influences of antiinflammatory drugs on the articular cartilage, the effects of a steroidal drug (dexamethasone) and of nonsteroidal antiinflammatory substances (indometacin and phenylbutazone) on the ultrastructure of the chondrocyte were examined in comparison with tiaprofenic acid (Surgam). Using an equiefficient dosage of the active principles, referred to the ED50 in the model of adjuvant arthritis in the rat, the synthetic apparatus of the chondrocytes was stimulated by tiaprofenic acid while it was diminished by indometacin and phenylbutazone and particularly by dexamethasone.

  17. The evaluation of topical anti-inflammatory activity on rat ears subjected to thermal injury.

    Science.gov (United States)

    Bronaugh, R L; Roller, R G; Cargill, R

    1978-10-01

    Topical anti-inflammatory activity of steroidal and non-steroidal agents was assessed on inflammation produced by heat. A burn was produced on the ears of rats and the inflammation was quantitated gravimetrically. Steroidal anti-inflammatory agents were ranked in order of decreasing activity: triamcinolone acetonide, dexamethasone, prednisolone and hydrocortisone acetate. The nonsteroidal agents phenylbutazone and indomethacin were also effective in inhibiting the inflammation. Cholesterol, a steroid devoid of anti-inflammatory activity, was inactive in this test. Hydrocortisone acetate, in particular, appears to be less effective in inhibiting this type of inflammation than inflammation produced by croton oil.

  18. In vitro inhibitory effects of non-steroidal anti-inflammatory drugs on 4-methylumbelliferone glucuronidation in recombinant human UDP-glucuronosyltransferase 1A9--potent inhibition by niflumic acid.

    Science.gov (United States)

    Mano, Yuji; Usui, Takashi; Kamimura, Hidetaka

    2006-01-01

    The inhibitory potencies of non-steroidal anti-inflammatory drugs (NSAIDs) on UDP-glucuronosyltransferase (UGT) 1A9 activity were investigated in recombinant human UGT1A9 using 4-methylumbelliferone (4-MU) as a substrate for glucuronidation. 4-MU glucuronidation (4-MUG) showed Michaelis-Menten kinetics with a Km value of 6.7 microM. The inhibitory effects of the following seven NSAIDs were investigated: acetaminophen, diclofenac, diflunisal, indomethacin, ketoprofen, naproxen and niflumic acid. Niflumic acid had the most potent inhibitory effect on 4-MUG with an IC50 value of 0.0341 microM. The IC50 values of diflunisal, diclofenac and indomethacin were 1.31, 24.2, and 34.1 microM, respectively, while acetaminophen, ketoprofen and naproxen showed less potent inhibition. Niflumic acid, diflunisal, diclofenac and indomethacin inhibited 4-MUG competitively with Ki values of 0.0275, 0.710, 53.3 and 69.9 microM, respectively, being similar to each IC50 value. In conclusion, of the seven NSAIDs investigated, niflumic acid was the most potent inhibitor of recombinant UGT1A9 via 4-MUG in a competitive manner.

  19. 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.

  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...... on these strategies exist at the moment. A third potential approach involves novel agents whose mechanism of action is closely related to COPD mechanisms and pathophysiology. Such novel treatments are of great interest since they may treat both COPD and co-morbidities. Several novel agents are currently under...

  1. 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

    OpenAIRE

    Mittal, N.; S. Singh Kanwar; S. Nath Sanyal

    2008-01-01

    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/...

  2. 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

  3. Use of Non-Steroidal Anti-Inflammatory Drugs in Orthopedic Patients%2013年医院骨科患者非甾体抗炎药物用药分析

    Institute of Scientific and Technical Information of China (English)

    王沐; 王建

    2014-01-01

    Objective To analyze the use situation of non-steroidal anti-inflammatory drugs(NSAIDs)in the orthopedic department of the hospital during one year to provide reference for clinical rational drug use. Methods The 68 754 pieces of prescription containing NSAIDs prescribed by the orthopedic department during 2013 were performed the statistical analysis. The frequency of drug use(DDDs), average daily cost(DDC),patients distribution and disease distribution of different non-steroidal anti-inflammatory drugs were ana-lyzed. Results The DDDs of Celecoxib Capsule was highest and reached 190 782,and its DDC was also highest(14. 64);the patients using NSAIDs were mainly distributed in the age group of 56-65 years old,accounting for 24. 57% of all patients;NSAIDs were mainly used in orthopedic fractures,osteoarthritis,rheumatoid arthritis,shoulder arthritis,ankylosing spondylitis,bone tumors,etc. Conclusion The market share of the new type cyclooxygenase-2(COX-2) inhibitors is continuously expanding;in the application process of NSAIDs, the appropriate drugs should be selected according to the patient's condition and the economic status. During the medication process,the monitoring of adverse drug reactions should be paid more attention to and the occurrence of drug abuse should be prevented.%目的:统计并分析医院骨科1年来非甾体抗炎药物(NSAIDs)的使用情况,为临床合理用药提供参考依据。方法对医院2013年度骨科开具的68754张NSAIDs处方进行统计和分析,比较不同NSAIDs的用药频度(DDDs)、日均费用(DDC)、患者分布、疾病分布等。结果塞来昔布胶囊的DDDs最高,达190782,DDC最高,达14.64;使用NSAIDs的患者主要分布在56~65岁,约占24.57%;NSAIDs主要应用于骨科骨折、骨关节炎、类风湿关节炎、肩关节炎、强直性脊柱炎、骨肿瘤等疾病。结论新型环氧化物酶(COX)-2抑制剂的市场份额在不断扩大,在NSAIDs应用过程中

  4. 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

  5. Evaluation of preventive and therapeutic activity of novel non-steroidal anti-inflammatory drug, CG100649, in colon cancer: Increased expression of TNF-related apoptosis-inducing ligand receptors enhance the apoptotic response to combination treatment with TRAIL.

    Science.gov (United States)

    Woo, Jong Kyu; Kang, Ju-Hee; Jang, Yeong-Su; Ro, Seonggu; Cho, Joong Myung; Kim, Hwan-Mook; Lee, Sang-Jin; Oh, Seung Hyun

    2015-04-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been suggested as the potential new class of preventive or therapeutic antitumor agents. The aim of the present study was to evaluate the antitumor activity of the novel NSAID, CG100649. CG100649 is a novel NSAID dual inhibitor for COX-2 and carbonic anhydrase (CA)-I/-II. In the present study, we investigated the alternative mechanism by which CG100649 mediated suppression of the colon cancer growth and development. The anchorage‑dependent and -independent clonogenic assay showed that CG100649 inhibited the clonogenicity of human colon cancer cells. The flow cytometric analysis showed that CG100649 induced the G2/M cell cycle arrest in colon cancer cells. Animal studies showed that CG100649 inhibited the tumor growth in colon cancer xenograft in nude mice. Furthermore, quantitative PCR and FACS analysis demonstrated that CG100649 upregulated the expression of TNF-related apoptosis-inducing ligand (TRAIL) receptors (DR4 and DR5) but decreased the expression of decoy receptors (DcR1 and DcR2) in colon cancer cells. The results showed that CG100649 treatment sensitized TRAIL‑mediated growth suppression and apoptotic cell death. The combination treatment resulted in significant repression of the intestinal polyp formation in APCmin/+ mice. Our data clearly demonstrated that CG100649 contains preventive and therapeutic activity for colon cancer. The present study may be useful for identification of the potential benefit of the NSAID CG100649, for the achievement of a better treatment response in colon cancer.

  6. 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.

  7. 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.

  8. Determination of widely used non-steroidal anti-inflammatory drugs in water samples by in situ derivatization, continuous hollow fiber liquid-phase microextraction and gas chromatography-flame ionization detector.

    Science.gov (United States)

    Es'haghi, Z

    2009-05-08

    The aim of this study was to develop an analytical procedure which allows the quantification of pharmaceuticals in water at the ng L(-1) level. Hence, it is reported research on the application of a rapid, inexpensive and simple continuous hollow fiber liquid-phase micro extraction (CHF-LPME) for the pre-concentration and determination of non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen (IBP), naproxen (NAP), and ketoprofen (KEP), in wastewater. In this method, a 2.50 cm end sealed piece of a polypropylene hollow fiber was immersed into the organic solvent, octanol, for 30 s. After solvent impregnation with the pores of the fiber, the excess amounts of solvent were removed from inside the fiber, and 4.0 microL of octanol, as the acceptor phase, was injected into the fiber carefully. The fiber was settled using a microsyringe into a 10.0 mL glass test tube, and 20.00 mL of the aqueous solution (the donor phase), was circulated by a pump around it. After analyte extraction for an optimized period of time (20 min), 2 microL of the organic solvent was withdrawn into the microsyringe and injected into the GC-FID for further analysis. Finally, based on the optimized analytical conditions, the method was linear in the range of 2.5-500 ng L(-1). The limits of detection were 1-2 ng L(-1). Repeatability of this method on an intra-day scale was 3.4-10.2% (RSD%). NSAIDs have been detected in several municipal wastewater samples, and the concentration range was 9.0-19.0 ng L(-1).

  9. 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

  10. 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

  11. 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

  12. 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.

  13. Online eluent-switching technique coupled anion-exchange liquid chromatography–ion trap tandem mass spectrometry for analysis of non-steroidal anti-inflammatory drugs in pig serum.

    Science.gov (United States)

    Chang, Kai Chun; Lin, Jyh Shiun; Cheng, Cheanyeh

    2015-11-27

    A novel method for online extraction, pH-gradient separation, and analysis of nine non-steroidal anti-inflammatory drugs (NSAIDs) was developed by coupling online eluent-switching technique to single anion-exchange chromatographic column/ion trap mass spectrometer (MS) and used for monitoring NSAIDs residues in pig serum. A neutral eluent and a pH-gradient eluent were used for extraction and separation of NSAIDs, respectively. Each of nine NSAIDs has an MS precursor ion of either [M−H]− or [M−Na]−. The extracted ion chromatogram for a specific product ion of each NSAID was used for its quantitative analysis. The dynamic linear ranges of calibration curves were all 0–200 ng mL−1 (R2 > 0.9950). The analysis accuracies estimated by spiking standard concentrations at 20, 100, and 200 ng mL−1 were 80.5–99.9%. The corresponding intra-day and inter-day precisions (RSD%) were 2.5–14.5% and 2.9–15.2%, respectively. The limit of detection/limit of quantitation of NSAIDs were 1.3/4.3, 0.5/1.6, 0.2/0.5, 2.5/8.2, 1.5/4.9, 0.6/2.1, 0.6/2.0, 0.5/1.7, and 0.6/2.1 ng mL−1 for carprofen, diclofenac, flunixin, ibuprofen, ketoprofen, meclofenamic acid sodium, mefenamic acid, niflumic acid, and tolfenamic acid, respectively. After 1 h injection of a dose containing 2 mg kg−1 weight pig of flunixin and tolfenamic acid to the pigs, a residue amount of 3480 ± 36 ng mL−1 and 431 ± 13 ng mL−1, respectively, was reached for the incurred pig serum specimens and both residues were reduced to about 20 ng mL−1 at the time of 24 h.

  14. 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。

  15. 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

  16. The effect of a non-steroidal anti-inflammatory drug on two important predictors for accidental falls: postural balance and manual reaction time. A randomized, controlled pilot study.

    Science.gov (United States)

    Hegeman, Judith; Nienhuis, Bart; van den Bemt, Bart; Weerdesteyn, Vivian; van Limbeek, Jacques; Duysens, Jacques

    2011-04-01

    Accidental falls in older individuals are a major health and research topic. Increased reaction time and impaired postural balance have been determined as reliable predictors for those at risk of falling and are important functions of the central nervous system (CNS). An essential risk factor for falls is medication exposure. Amongst the medications related to accidental falls are the non-steroidal anti-inflammatory drugs (NSAIDs). About 1-10% of all users experience CNS side effects. These side effects, such as dizziness, headaches, drowsiness, mood alteration, and confusion, seem to be more common during treatment with indomethacin. Hence, it is possible that maintenance of (static) postural balance and swift reactions to stimuli are affected by exposure to NSAIDs, indomethacin in particular, consequently putting older individuals at a greater risk for accidental falls. The present study investigated the effect of a high indomethacin dose in healthy middle-aged individuals on two important predictors of falls: postural balance and reaction time. Twenty-two healthy middle-aged individuals (59.5 ± 4.7 years) participated in this double-blind, placebo-controlled, randomized crossover trial. Three measurements were conducted with a week interval each. A measurement consisted of postural balance as a single task and while concurrently performing a secondary cognitive task and reaction time tasks. For the first measurement indomethacin 75 mg (slow-release) or a visually identical placebo was randomly assigned. In total, five capsules were taken orally in the 2.5 days preceding assessment. The second measurement was without intervention, for the final one the first placebo group got indomethacin and vice versa. Repeated measures GLM revealed no significant differences between indomethacin, placebo, and baseline in any of the balance tasks. No differences in postural balance were found between the single and dual task conditions, or on the performance of the dual task

  17. Antiinflamatorios no esteroides como terapia adjunta al raspado y alisado radicular en periodontitis Non-steroidal anti-inflammatory as an adjunct to scaling and root planning in periodontitis

    Directory of Open Access Journals (Sweden)

    C.M. Ardila Medina

    2012-04-01

    Full Text Available La destrucción periodontal resulta de la interacción entre la placa bacteriana y la respuesta inflamatoria inducida por mediadores que incluyen enzimas del huésped, citoquinas, y metabolitos del ácido araquidónico (AA tales como las prostaglandinas (PGs. Las PGs participan en la regulación de diversas funciones celulares bajo condiciones fisiológicas y patológicas. La ciclooxigenasa (COX proporciona la conversión de AA a PGs en tres formas funcionalmente distintas: COX-1, COX-2 y COX-3. COX-2, se induce después de estimular una variedad de citoquinas inflamatorias, factores de crecimiento y lipopolisacáridos. Expresiones elevadas de COX-2 en periodontitis incrementan los niveles de PGs E2, considerados como los mayores mediadores de la destrucción tisular periodontal. Los antiinflamatorios no esteroides (AINES inhiben la elaboración de productos COX y pueden atenuar el avance de la pérdida ósea, convirtiéndose en una alternativa terapéutica para el manejo de la periodontitis.Periodontal tissue destruction occurs as a result of the interaction between dental plaque bacteria and the immunoinflamatory response induced by mediators like host enzymes, cytokines, and arachidonic acid metabolites such as prostaglandins (PGs. PGs play a role in the regulation of diverse cellular functions under physiological and pathological conditions. The ciclooxigenase (COX enzyme providing the conversion of AA to PGs exists in two functionally distinct COX isoforms: COX-1 and COX-2. COX-2. The COX-2, is induced after stimulation by a variety of inflammatory cytokines, growth factors, and lipopolysaccarides. Higher expressions of COX-2 in periodontitis results in increases of the levels of prostaglandin E2 which are major mediators of periodontal tissue destruction. Non-steroidal anti-inflammatory drugs inhibit the production of COX products and can attenuate the progression of periodontal bone loss, become a therapeutic alternative for the

  18. 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

  19. 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

  20. 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

  1. 非甾体类抗炎药物对急性高原病的预防效果%Observation of the effect of non-steroid anti-inflammatory drug to prevent acute mountain sickness

    Institute of Scientific and Technical Information of China (English)

    张俊才; 王引虎; 冯英凯; 刘友生; 崔建华; 李丽; 高江峰; 王琰

    2011-01-01

    目的 验证非甾体类抗炎药物盐酸苄达明对急性高原病的预防效果.方法 将急进5 200 m高原的118例健康青年官兵随机分为安慰剂组(n=20)、复方红景天组(n=33)、复方党参组(n=33)、盐酸苄达明组(n=33),自海拔1 400 m,历时5 d进入5 200 m高原.从出发前5 d开始分别服用盐酸苄达明片、复方红景天胶囊、复方党参胶囊和安慰剂胶囊,定期测试其血氧饱和度(SaO2)和心率(HR),并以军用卫生标准GJB1098-91随访记录受试者急性高原反应症状,然后分度评分;进入高原后第7天进行高原习服基础生理指标测定,进行药效评价.结果 盐酸苄达明对全程试验期内受试者高原缺氧所致头痛和呕吐的预防效果显著优于安慰剂,且对头痛症状的预防效果优于复方红景天与复方党参.盐酸苄达明组受试者急性高原反应GJB评分,进入海拔5 200 m高原第3、5天SaO2、心率,高原习服基础生理指标等均显著优于安慰剂组.结论 非甾体类抗炎药物盐酸苄达明防治急性高原病效果显著.%Objective To test and verify the effects of benzyamine hydrochloride, a non steroid anti inflammatory drug, to prevent acute mountain sickness. Methods Totally 118 cases of healthy young soldiers were randomly divided into four groups respectively treated by placebo(n=20) ,compound rhodiola(n=33) ,compound codonopsis capsules(n=33) ,benzyamine hydrochloride(n=33) starting 5 days before departure and quickly approached into the altitude 5 200 m from 1 400 m in 5 days. Blood oxygen saturation(SaO2 ) and heart rate(HR) were regularly tested and acute mountain sickness symptoms of subjects were follow up recorded and scored according to the military standard GJB1098 91;Basic high altitude acclimatization physiological parameters were determined and evaluated from seventh day after reaching the plateau. Results The effect of benzyamine hydrochloride to prevent head ache and vomiting due to high altitude was

  2. Use of Fixed Dose Combination (FDC Drugs in India: Central Regulatory Approval and Sales of FDCs Containing Non-Steroidal Anti-Inflammatory Drugs (NSAIDs, Metformin, or Psychotropic Drugs.

    Directory of Open Access Journals (Sweden)

    Patricia McGettigan

    2015-05-01

    Full Text Available In 2012, an Indian parliamentary committee reported that manufacturing licenses for large numbers of fixed dose combination (FDC drugs had been issued by state authorities without prior approval of the Central Drugs Standard Control Organization (CDSCO in violation of rules, and considered that some ambiguity until 1 May 2002 about states' powers might have contributed. To our knowledge, no systematic enquiry has been undertaken to determine if evidence existed to support these findings. We investigated CDSCO approvals for and availability of oral FDC drugs in four therapeutic areas: analgesia (non-steroidal anti-inflammatory drugs [NSAIDs], diabetes (metformin, depression/anxiety (anti-depressants/benzodiazepines, and psychosis (anti-psychotics.This was an ecologic study with a time-trend analysis of FDC sales volumes (2007-2012 and a cross-sectional examination of 2011-2012 data to establish the numbers of formulations on the market with and without a record of CDSCO approval ("approved" and "unapproved", their branded products, and sales volumes. Data from the CDSCO on approved FDC formulations were compared with sales data from PharmaTrac, a database of national drug sales. We determined the proportions of FDC sales volumes (2011-2012 arising from centrally approved and unapproved formulations and from formulations including drugs banned/restricted internationally. We also determined the proportions of centrally approved and unapproved formulations marketed before and after 1 May 2002, when amendments were made to the drug rules. FDC approvals in India, the United Kingdom (UK, and United States of America (US were compared. For NSAID FDCs, 124 formulations were marketed, of which 34 (27% were centrally approved and 90 (73% were unapproved; metformin: 25 formulations, 20 (80% approved, five (20% unapproved; anti-depressants/benzodiazepines: 16 formulations, three (19% approved, 13 (81% unapproved; anti-psychotics: ten formulations, three (30

  3. 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。

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

    OpenAIRE

    Befus A Dean; Davison Joseph S; Mathison Ronald D; Gingerich Daniel A

    2010-01-01

    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 hom...

  5. Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues

    Directory of Open Access Journals (Sweden)

    Eliezer J. Barreiro

    2012-11-01

    Full Text Available In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1, a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637 and 14g (LASSBio-1639 were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2 at concentrations of 10 mM.

  6. Design, synthesis, antinociceptive and anti-inflammatory activities of novel piroxicam analogues.

    Science.gov (United States)

    de Miranda, Amanda Silva; Bispo Júnior, Walfrido; da Silva, Yolanda Karla Cupertino; Alexandre-Moreira, Magna Suzana; Castro, Rosane de Paula; Sabino, José Ricardo; Lião, Luciano Morais; Lima, Lídia Moreira; Barreiro, Eliezer J

    2012-11-28

    In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 mM.

  7. Anti-inflammatory glucocorticoid drugs: reflections after 60 years.

    Science.gov (United States)

    Whitehouse, Michael W

    2011-02-01

    This review considers the problem of the serious concomitant side effects of powerful anti-inflammatory drugs modelled upon the principal human glucocorticoid hormone, cortisol. The very nature of the original bio-assays to validate their cortisol-like hormonal and anti-inflammatory activities ensured that pleiotropic toxins were selected for clinical studies. Other complicating factors have been (1) considerable reliance on bio-assays conducted in laboratory animals that primarily secrete corticosterone, not cortisol, as their principal anti-inflammatory adrenal hormone; (2) some differences in the binding of xenobiotic cortisol analogues (vis á vis cortisol) to transport proteins, detoxifying enzymes and even some intra-cellular receptors; (3) the "rogue" properties of these hormonal xenobiotics, acting independently of--but still able to suppress--hormonal mechanisms regulating endogenous cortisol; and (4) problems of intrinsic/acquired "steroid resistance", diminishing their clinical efficacy, but not necessarily all their toxicities. The rather gloomy conclusion is that devising new drugs to reproduce the effect of multi-potent hormones may be a recipe for disaster, in contexts other than simply remedying an endocrine deficiency. Promising new developments include "designed" combination therapies that allow some reduction in total steroid doses (and hopefully their side effects); sharpening strategies to limit the actual duration of steroid administration; and resurgent interest in searching for more selective analogues (both steroidal and non-steroid) with less harmful side effects. Some oversights and neglected areas of research are also considered. Overall, it now seems timely to engage in some drastic rethinking about (retaining?) these "licensed toxins" as fundamental therapies for chronic inflammation.

  8. Non-steroidal Anti-inflammatory Drugs induced Urticaria and Angioedema%非甾体类抗炎药所致荨麻疹和血管性水肿

    Institute of Scientific and Technical Information of China (English)

    徐迎阳; 支玉香

    2014-01-01

    非甾体抗炎药(nonsteroidal anti-inflammatory drugs,NSAIDs)较易引起药物不良反应,其中大部分是由于个体对NSIADs高敏感所致,最常见表现为荨麻疹和(或)血管性水肿.本文将针对NSAIDs所致的荨麻疹和血管性水肿分类、表现、诊断及处理原则进行阐述.

  9. Anti-inflammatory effects of electronic signal treatment.

    Science.gov (United States)

    Odell, Robert H; Sorgnard, Richard E

    2008-01-01

    Inflammation often plays a key role in the perpetuation of pain. Chronic inflammatory conditions (e.g. osteoarthritis, immune system dysfunction, micro-circulatory disease, painful neuritis, and even heart disease) have increased as baby boomers age. Medicine's current anti-inflammatory choices are NSAIDs and steroids; the value in promoting cure and side effect risks of these medications are unclear and controversial, especially considering individual patient variations. Electricity has continuously been a powerful tool in medicine for thousands of years. All medical professionals are, to some degree, aware of electrotherapy; those who directly use electricity for treatment know of its anti-inflammatory effects. Electronic signal treatment (EST), as an extension of presently available technology, may reasonably have even more anti-inflammatory effects. EST is a digitally produced alternating current sinusoidal electronic signal with associated harmonics to produce theoretically reasonable and/or scientifically documented physiological effects when applied to the human body. These signals are produced by advanced electronics not possible even 10 to 15 years ago. The potential long-lasting anti-inflammatory effects of some electrical currents are based on basic physical and biochemical facts listed in the text below, namely that of stimulating and signaling effective and long-lasting anti-inflammatory effects in nerve and muscle cells. The safety of electrotherapeutic treatments in general and EST in particular has been established through extensive clinical use. The principles of physics have been largely de-emphasized in modern medicine in favor of chemistry. These electrical treatments, a familiar application of physics, thus represent powerful and appropriate elements of physicians' pain care armamentaria in the clinic and possibly for prescription for use at home to improve overall patient care and maintenance of quality of life via low-risk and potentially

  10. Effect of non-steroidal anti-inflammatory drugs on small intestinal barrier function in rats%非甾体消炎药对大鼠小肠黏膜机械屏障功能的影响

    Institute of Scientific and Technical Information of China (English)

    张烁; 吕宾; 姒健敏; 陈方明; 孟立娜; 吴伟峰; 俞蕾敏

    2009-01-01

    Objective To approach the effect on mechanical barricade of the mucous membrane of small intestine caused by non-steroidal anti-inflammatory drugs(NSAIDs).Methods Thirty-two male SD rats were randomly divided into control group and model group.The rats of the model group were given 7.5 mg/kg diclofenac by gavage,bid;the rats of the control group were given the same dose of saline.Then thev were further randomly divided into two subgroups(n=8)at the first day and the fifth day after making the models to observe the scores of anatomical lesion on stomach and small intestine and the scores of tissue damage of mucous membrane and to quantitatively analyze the height of villi,as well as the thickness and the section area of mucous membrane with Carl Zeiss Imaging Systems.Observation of the change of ultrastructural organization of mucous membrane was carried out with transmission electron microscope.Results The mucous membrane of stomach of the model groups was slightly edematous.There was no difference between the scores of the model groups and control groups.It was seen that the mucous membrane of small intestine of the first day model group presented with erythema,anabrosis and ulcer.The ulcer was distributed along mesentery.The mucous membrane of small intestine of the fifth day model group showed bleeding,perforation and sinus tract formation,and the scores of anatomical lesion was higher than that of the control group(P<0.05).The scroes of the lesions of the first and fifth day model groups were 3.5 and 5.0.The difference had statistical significance when compared with those of the control groups(the scores were O)(P<0.05).Cell degeneration and cellular necrosis of epithelial mueosa of small intestine wag also seen in the first day model group.The top of villi was ablated.The height of the pile on jejunum was (126.9±32.0)μm and that on ileum wag(118.6±22.9)μm They were lower than those of the control group(P<0.05).However there was no difference of the

  11. 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.

  12. Simultaneous analysis of non-steroidal anti-inflammatory drugs using electrochemically controlled solid-phase microextraction based on nanostructure molecularly imprinted polypyrrole film coupled to ion mobility spectrometry.

    Science.gov (United States)

    Ameli, Akram; Kalhor, Hamideh; Alizadeh, Naader

    2013-06-01

    A simple, rapid, and highly sensitive method for simultaneous analysis of anti-inflammatory drugs (naproxen, ibuprofen, and mefenamic acid) in diluted human serum was developed using the electrochemically controlled solid-phase microextraction coupled to ion mobility spectrometry. A conducting molecularly imprinted polymer film based on polypyrrole was synthesized for the selective uptake and release of drugs. The film was prepared by incorporation of a template molecule (naproxen) during the electropolymerization of pyrrole onto a platinum electrode using cyclic voltammetry method. The measured ion mobility spectrometry intensity was related to the concentration of analytes taken up into the films. The calibration graphs (naproxen, ibuprofen, and mefenamic acid) were linear in the range of 0.1-30 ng/mL and detection limits were 0.07-0.37 ng/mL and relative standard deviation was lower than 6%. On the basis of the results obtained in this work, the conducting molecularly imprinted polymer films as absorbent have been applied in the electrochemically controlled solid-phase microextraction and ion mobility spectrometry system for the selective clean-up and quantification of trace amounts of anti-inflammatory drugs in human serum samples. Scanning electron microscopy has confirmed the nano-structure morphology of the polypyrrole film.

  13. 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

  14. Anti-inflammatory phytochemicals for chemoprevention of colon cancer.

    Science.gov (United States)

    Madka, Venkateshwar; Rao, Chinthalapally V

    2013-06-01

    Every year more than a million new cancer cases and 600,000 deaths are reported world-wide. Colorectal cancer is the fourth most commonly occurring and second leading cause of cancer deaths in the United States. Significant progress has been made in understanding colorectal cancer through epidemiological, laboratory and clinical studies. Development of metastatic adenocarcinomas is a multistage process occurring over several years during which multiple genetic alterations and pathophysiological changes are associated. Colorectal cancer can be prevented if the transformation of normal colonic crypt cells to malignant can be halted or reversed. Some of the key molecules that are altered significantly and play important roles in colorectal tumor progression are associated with inflammation. Since chronic inflammation is now recognized as a potential risk factor for tumor development, targeting inflammatory pathways has proven effective in preventing formation of colonic tumors and their malignant progression in both preclinical and clinical studies. Synthetic non-steroidal anti-inflammatory drugs (NSAIDS) have been identified as potential colorectal cancer chemopreventive agents; however, most of these synthetic agents are associated with unwanted and sometimes fatal side effects. There is mounting evidence in support of the efficacy of naturally-occurring phytochemicals possessing anti-inflammatory activity. In this review we discuss key inflammatory pathways associated with colorectal cancer and promising naturally-occurring phytochemicals as anti-inflammatory agents for the prevention and treatment of colorectal cancer.

  15. ANTI-INFLAMMATORY ACTIVITY OF DODONAEA VISCOSE

    OpenAIRE

    Mahadevan, N.; Venkatesh, Sama; Suresh, B

    1998-01-01

    Dodonaea viscose, Linn is a widely grown plant of Nilgiris district of Tamil and is commonly used by the tribals of Nilgiris as a traditional medicine for done fracture and joint sprains. Since it is generally believed tat fractures are accompanied by either some degree of injury or inflammations, it was felt desirable to carry our anti inflammatory activity of Dodonaea viscose. Anti-inflammatory activity of the plant was carried out by carrageenin induced paw edema method in Wister albino rats.

  16. Anti-inflammatory activity of dodonaea viscose.

    Science.gov (United States)

    Mahadevan, N; Venkatesh, S; Suresh, B

    1998-10-01

    Dodonaea viscose, Linn is a widely grown plant of Nilgiris district of Tamil and is commonly used by the tribals of Nilgiris as a traditional medicine for done fracture and joint sprains. Since it is generally believed tat fractures are accompanied by either some degree of injury or inflammations, it was felt desirable to carry our anti inflammatory activity of Dodonaea viscose. Anti-inflammatory activity of the plant was carried out by carrageenin induced paw edema method in Wister albino rats.

  17. Desensitization to acetyl-salicylic acid as a treatment for non-steroid anti-inflammatory drugs (NSAIDs-exacerbated respiratory disease = Desensibilización al ácido acetil-salicílico como tratamiento para la enfermedad respiratoria exacerbada por antiinflamatorios no esteroides

    Directory of Open Access Journals (Sweden)

    Cardona Villa, Ricardo

    2014-07-01

    Full Text Available Desensitization to acetyl-salicylic acid as a treatment for non-steroid anti-inflammatory drugs (NSAIDs-exacerbated respiratory disease The coexistence of hypersensitivity to acetylsalicylic acid (ASA and other NSAIDs with disease of the upper or the lower airways (rhinosinusitis/sinonasal polyposis, or asthma is defined as NSAIDs-exacerbated respiratory disease. Treatment options include the avoidance of all analgesics that inhibit COX-1 or ASA desensitization, continuing its daily consumption. The latter treatment has shown to improve quality of life, reduce the formation of sinonasal polyps, the episodes of sinus infection, the frequency of hospitalizations and surgeries for resection of polyps and the need for systemic steroid treatment. Multiple desensitization schedules have been used, trying to reduce the risk associated with the procedure and the adverse effects of chronic use of ASA. In this paper we present a review of the different methods of desensitization and two illustrative clinical cases to help understand the factors that influence the choice of treatment for these patients.

  18. Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution.

    Science.gov (United States)

    Jabeen, Talat; Singh, Nagendra; Singh, Rajendra K; Sharma, Sujata; Somvanshi, Rishi K; Dey, Sharmistha; Singh, Tej P

    2005-12-01

    Phospholipase A(2) (PLA(2); EC 3.1.3.4) catalyzes the first step of the production of proinflammatory compounds collectively known as eicosanoids. The binding of phospholipid substrates to PLA(2) occurs through a well formed hydrophobic channel. Surface plasmon resonance studies have shown that niflumic acid binds to Naja naja sagittifera PLA(2) with an affinity that corresponds to a dissociation constant (K(d)) of 4.3 x 10(-5) M. Binding studies of PLA(2) with niflumic acid were also carried out using a standard PLA(2) kit that gave an approximate binding constant, K(i), of 1.26 +/- 0.05 x 10(-6) M. Therefore, in order to establish the viability of PLA(2) as a potential target molecule for drug design against inflammation, arthritis and rheumatism, the three-dimensional structure of the complex of PLA(2) with the known anti-inflammatory agent niflumic acid [2-[3-(trifluoromethyl)anilino]nicotinic acid] has been determined at 2.5 Angstroms resolution. The structure of the complex has been refined to an R factor of 0.187. The structure determination reveals the presence of one niflumic acid molecule at the substrate-binding site of PLA(2). It shows that niflumic acid interacts with the important active-site residues His48 and Asp49 through two water molecules. It is observed that the niflumic acid molecule is completely buried in the substrate-binding hydrophobic channel. The conformations of the binding site in PLA(2) as well as that of niflumic acid are not altered upon binding. However, the orientation of the side chain of Trp19, which is located at the entry of the substrate-binding site, has changed from that found in the native PLA(2), indicating its familiar role.

  19. 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

  20. Mechanisms of action underlying the anti-inflammatory and immunomodulatory effects of propolis: a brief review

    Directory of Open Access Journals (Sweden)

    Marcio A. R. Araujo

    2012-02-01

    Full Text Available Many biological properties have been attributed to various types of propolis, including anti-inflammatory, antimicrobial, antioxidant, antitumor, wound healing, and immunomodulatory activities. This article reviewed studies published that investigated the anti-inflammatory activity of propolis of different origins and/or its isolated components, focusing on the mechanisms of action underlying this activity and also addressing some aspects of immunomodulatory effects. The search was performed of the following databases: PubMed, Science Direct, HighWire Press, Scielo, Google Academics, Research Gate and ISI Web of Knowledgement. The anti-inflammatory activity was associated with propolis or compounds such as polyphenols (flavonoids, phenolic acids and their esters, terpenoids, steroids and amino acids. CAPE is the most studied compounds. The main mechanisms underlying the anti-inflammatory activity of propolis included the inhibition of cyclooxygenase and consequent inhibition of prostaglandin biosynthesis, free radical scavenging, inhibition of nitric oxide synthesis, reduction in the concentration of inflammatory cytokines and immunosuppressive activity. Propolis was found to exert an anti-inflammatory activity in vivo and in vitro models of acute and chronic inflammation and others studies, indicating its promising potential as anti-inflammatory agent of natural origin and as a source of chemical compounds for the development of new drugs.

  1. Exploration of possible mechanisms for anti-inflammatory activity of Ipomoea aquatica Forsk. (Convolvulaceae

    Directory of Open Access Journals (Sweden)

    Mital N. Manvar

    2015-11-01

    Full Text Available Currently used steroidal and non steroidal anti-inflammatory drugs have severe side effects. These side effects are very difficult to manage than the disease itself. Hence, there is to search new safe resources to cure such diseases that the use of plant based drugs. This study deals with anti-inflammatory evaluation of the hydroalcoholic extract of Ipomoea aquatica leaves as well as their possible mechanism of action. A carrageenan‐induced rat paw oedema model was used for anti-inflammatory study. The mechanism/s by which Ipomoea aquatica is mediated the ant-inflammatory activity was determined by its effects in antihistamine activity, prostaglandin synthesis inhibition activity, membrane stabilizing activity and protein denaturation inhibition activity. Dose dependent anti-inflammatory activity was found with HAEIA in rat paw oedema model using carrageenan. HAEIA effective to suppressed the wheal area formed by histamine. HAEIA revealed dose dependent prostaglandin synthesis inhibition activity. HAEIA was effectively inhibited the heat induced hemolysis of HRBCs as well as heat induced albumin denaturation. Therefore, it was concluded that the HAEIA has anti-inflammatory activity possibly mediated through inhibition of release of mediator histamine and prostaglandin and has also HRBCs membrane stabilization and protein denaturation inhibition properties.

  2. 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

    OpenAIRE

    Chopra, S; R. Kishore Saini; S. Nath Sanyal

    2007-01-01

    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...

  3. 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

  4. Anti-Inflammatory Activity of Natural Products

    Directory of Open Access Journals (Sweden)

    Abdullatif Azab

    2016-10-01

    Full Text Available This article presents highlights of the published literature regarding the anti-inflammatory activities of natural products. Many review articles were published in this regard, however, most of them have presented this important issue from a regional, limited perspective. This paper summarizes the vast range of review and research articles that have reported on the anti-inflammatory effects of extracts and/or pure compounds derived from natural products. Moreover, this review pinpoints some interesting traditionally used medicinal plants that were not investigated yet.

  5. Antinociceptive and anti-inflammatory activities of a pomegranate (Punica granatum L.) extract rich in ellagitannins.

    Science.gov (United States)

    González-Trujano, María Eva; Pellicer, Francisco; Mena, Pedro; Moreno, Diego A; García-Viguera, Cristina

    2015-01-01

    Pomegranate (Punica granatum L.) has been used for centuries for the treatment of inflammatory diseases. However, there is a lack of comprehensive information focused on the properties of a certain pomegranate (poly)phenolic profile to cure pain and gastric injury induced by anti-inflammatory drugs. This study investigated the systemic effects of different doses of a HPLC-characterized pomegranate extract on the formalin-induced nociceptive behavior in mice. The effect of the extract against gastric injury caused by non-steroidal anti-inflammatory drugs and ethanol was also assessed. Pomegranate reduced nociception in both phases of the formalin test, suggesting central and peripheral activities to inhibit nociception. Indomethacin-induced gastric injury was not produced in the presence of pomegranate, which also protected against ethanol-induced gastric lesions. The present results reinforce the benefits of pomegranate (poly)phenolics in the treatment of pain as well as their anti-inflammatory properties.

  6. Anti-inflammatory drug therapy in asthma

    NARCIS (Netherlands)

    Rottier, Bart L.; Duiverman, Eric J.

    2009-01-01

    Asthma is a disease with chronic inflammation of the airways and and-inflammatory treatment is a logical treatment. Inhaled corticosteroids [ICS] remain the cornerstone of anti-inflammatory therapy in recent international guidelines. Asthma cannot be cured by any medication: if the drug is discontin

  7. ANTI INFLAMMATORY ACTIVITY OF MORINGA OLIEFERA. LAM

    OpenAIRE

    1999-01-01

    The aqueous and ethanolic (90%) extract of the leaves of M.Oliera Lam (Fam: Moringaceae) were studied for their anti inflammatory action in ale albino rats. Two extracts exhibited maximum action within two hours of challenge. The aqueous extract sowed significant (P

  8. Anti-inflammatory effect of (+)-pinitol.

    Science.gov (United States)

    Singh, R K; Pandey, B L; Tripathi, M; Pandey, V B

    2001-02-01

    In the carrageenin-induced paw oedema in rats, (+)-pinitol (2.5-10 mg/kg, i.p.), isolated from Abies pindrow leaves, showed a significant anti-inflammatory effect, the highest dose being comparable to phenylbutazone (100 mg/kg, i.p.).

  9. Anti-inflammatory activity of D-002: an active product isolated from beeswax.

    Science.gov (United States)

    Carbajal, D; Molina, V; Valdés, S; Arruzazabala, M L; Más, R; Magraner, J

    1998-10-01

    D-002 is a natural mixture of high molecular weight alcohols isolated and purified from beeswax, which contains triacontanol among its main components. This study was undertaken to investigate the anti-inflammatory effects of D-002 administered by the oral route in two animal models commonly used in the pharmacological screening of anti-inflammatory drugs. D-002 administered orally to rats (100 and 200 mg/kg) produced a mild but significant reduction of exudate volume in carrageenan-induced pleuritic inflammation that was accompanied by a marked and significant decrease of leukotriene B4 (LTB4) levels in the exudate. D-002 (25, 50 and 200 mg/kg) also significantly diminished the granuloma weight in the cotton pellet granuloma in rats. In both cases, D-002 was less effective than indomethacin, which was used as an established anti-inflammatory reference drug. On the other hand, D-002 administered from 25-1000 mg/kg did not induce erosions or gastromucosal lesions in rats, which differs from results usually obtained with non steroidal anti-inflammatory drugs. These results indicate that D-002 is a mild anti-inflammatory agent without any ulcerogenic effect associated. The results suggest that these effects are probably not mediated through an inhibition of cyclooxygenase, but a reduction in LTB4 levels induced by D-002 could explain these results.

  10. Pharmacological interactions of anti-inflammatory-analgesics in odontology.

    Science.gov (United States)

    Gómez-Moreno, Gerardo; Guardia, Javier; Cutando, Antonio; Calvo-Guirado, José Luis

    2009-02-01

    In this second article we describe the more interesting pharmacological interactions in dental practice based on the prescription of analgesic narcotics, paracetamol and non-selective non-steroid anti-inflammatory drugs (NSAI) (which inhibit cyclooxigenase 1 -COX 1- and cyclooxigenase 2 -COX 2-) and selective NSAIs (COX 2 inhibitors). The importance of preventing the appearance of these pharmacological interactions is because these are medicaments prescribed daily in odontology for moderate pain treatment and inflammation in the oral cavity. Paracetamol can interact with warfarin and therefore care should be taken with chronic alcoholic patients. All NSAIs reduce renal blood flow and consequently are capable of reducing the efficacy of medicaments used for treating arterial hypertension, which act via a renal mechanism. Especial attention should be taken considering the risk of interaction between the antagonists of AT1 receptors of angiostensin II (ARAII) and the NSAIs.

  11. Nonsteroidal Anti-Inflammatory Drugs and the Kidney

    Directory of Open Access Journals (Sweden)

    Walter H. Hörl

    2010-07-01

    Full Text Available Non-steroidal anti-inflammatory drugs (NSAIDs inhibit the isoenzymes COX-1 and COX-2 of cyclooxygenase (COX. Renal side effects (e.g., kidney function, fluid and urinary electrolyte excretion vary with the extent of COX-2-COX-1 selectivity and the administered dose of these compounds. While young healthy subjects will rarely experience adverse renal effects with the use of NSAIDs, elderly patients and those with co-morbibity (e.g., congestive heart failure, liver cirrhosis or chronic kidney disease and drug combinations (e.g., renin-angiotensin blockers, diuretics plus NSAIDs may develop acute renal failure. This review summarizes our present knowledge how traditional NSAIDs and selective COX-2 inhibitors may affect the kidney under various experimental and clinical conditions, and how these drugs may influence renal inflammation, water transport, sodium and potassium balance and how renal dysfunction or hypertension may result.

  12. 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.

  13. 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.

  14. Ketogenic diet exhibits anti-inflammatory properties.

    Science.gov (United States)

    Dupuis, Nina; Curatolo, Niccolo; Benoist, Jean-François; Auvin, Stéphane

    2015-07-01

    The ketogenic diet (KD) is an established treatment for refractory epilepsy, including some inflammation-induced epileptic encephalopathies. In a lipopolysaccharide (LPS)-induced fever model in rats, we found that animals given the KD for 14 days showed less fever and lower proinflammatory cytokine levels than control animals. However, KD rats exhibited a decrease in circulating levels of arachidonic acid and long-chain n-3 polyunsaturated fatty acids (PUFAs), suggesting that the anti-inflammatory effect of KD was probably not due to an increase in anti-inflammatory n-3 PUFA derivatives. These properties might be of interest in some conditions such as fever-induced refractory epileptic encephalopathy in school-aged children.

  15. Anti inflammatory activity of moringa oliefera. Lam.

    Science.gov (United States)

    Rao, K N; Gopalakrishnan, V; Loganathan, V; Nathan, S S

    1999-01-01

    The aqueous and ethanolic (90%) extract of the leaves of M.Oliera Lam (Fam: Moringaceae) were studied for their anti inflammatory action in ale albino rats. Two extracts exhibited maximum action within two hours of challenge. The aqueous extract sowed significant (P<0.01) odema suppression similar to that of Ibuprofen at the first hour of carrageenan injection. The results confirms the folkers claim of the plant.

  16. 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

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    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

  17. Anti-Inflammatory Effect of Allium ursinum

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    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.

  18. 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。

  19. 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.

  20. 2008~2010年北京地区门诊口服非甾体抗炎药动态分析%Dynamic Analysis of Oral Non-steroid Anti-inflammatory Drugs Use in Outpatients of Twenty-two Hospitals in Beijing During the Year of 2008-2010

    Institute of Scientific and Technical Information of China (English)

    郭婕; 金岩; 杜小莉

    2012-01-01

    目的:了解北京地区门诊非甾体抗炎药(NSAIDs)的使用情况及发展趋势,比较NSAIDs药物使用状况,为临床合理应用提供参考.方法:采用《医院处方分析》课题组提供的数据,以限定日剂量、用药频度、限定日费用为统计指标,对2008~2010年北京地区门诊口服NSAIDs的应用情况进行统计和分析.结果:2008~ 2010年北京地区NSAIDs销售金额和用药频度呈现下降;用药频度最高为洛索洛芬、萘丁美酮、美洛昔康.结论:北京地区NSAIDs使用基本合理,疗效肯定、不良反应小的NSAIDs具有广阔的市场前景.%Objective: To investigate the current use and change trend of non-steroid anti-inflammatory drugs (NSAIDs) in outpatients of Beijing area to compare the usage of NASIDs and provide the references for the clinical applications. Method: The data on the usage of oral NSAIDs in Beijing area during the year of 2008 to 2010 were provided by the Hospital Prescriptions Analysis Project Group. Statistical analysis was performed with the DDD and daily drug expenses as the indices. Result; The consumption sum and DDDs of NSAIDs used in Beijing area decreased year by year. Loxoprofen, nabumetone and meloxicam were the three most frequently used drugs. Conclusion; The usage of NSAIDS in Beijing area is reasonable. NSAIDs with promising efficacy and few adverse reactions show good market prospect.

  1. 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.

  2. Synthesis and biological evaluation of phenyl-1H-1,2,3-triazole derivatives as anti-inflammatory agents.

    Science.gov (United States)

    Kim, Tae Woo; Yong, Yeonjoong; Shin, Soon Young; Jung, Hyeryoung; Park, Kwan Ha; Lee, Young Han; Lim, Yoongho; Jung, Kang-Yeoun

    2015-04-01

    Rapid and efficient synthesis of a phenyl-1H-1,2,3-triazole library enabled cost-effective biological testing of a range of novel non-steroidal anti-inflammatory drugs with potential for improved drug efficacy and toxicity profiles. Anti-inflammatory activities of the phenyl-1H-1,2,3-triazole analogs synthesized in this report were assessed using the xylene-induced ear edema model in mice. At least four analogs, 2a, 2b, 2c, and 4a, showed more potent effects than the reference anti-inflammatory drug diclofenac at the same dose of 25 mg/kg. To explore relationships between the structural properties of phenyl-1H-1,2,3-triazole analogs and their anti-inflammatory activities in xylene-induced ear edema, comparative molecular field analysis was performed, and pharmacophores showing good anti-inflammatory activities were identified based on an analysis of contour maps obtained from comparative molecular field analysis. The anti-inflammatory effect on the molecular level was tested by the expression of tumor necrosis factor-alpha induced COX-2 using Western blots. Because the addition of the analog 2c caused the expression change of TNF-α induced COX-2, the molecular binding mode between 2c and COX-2 was elucidated using in silico docking.

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

    DEFF Research Database (Denmark)

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

    2015-01-01

    . RESULTS: In total 149 patients were included. Of those, 39 patients (26.2%) had a positive OPT. Twenty-nine patients were classified as cross-reactive responders and 9 patients as single NSAID responders after positive OPTs with the culprit NSAID, but not to acetylsalicylic acid. All single NSAID...

  4. 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

  5. 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

  6. Anti-Inflammatory Chemical Profiling of the Australian Rainforest Tree Alphitonia petriei (Rhamnaceae

    Directory of Open Access Journals (Sweden)

    Ritesh Raju

    2016-11-01

    Full Text Available Chronic inflammation is an important pathological condition in many human diseases, and due to the side effects of the currently used non-steroidal anti-inflammatory drugs, discovery of novel anti-inflammatory drugs is of general interest. Anti-inflammatory activity guided compound isolation from the plant Alphitonia petriei led to the isolation of the known plant sterols emmolic acid (1, alphitolic acid (2, trans- and cis-coumaroyl esters of alphitolic acid (3 and 4 and betulinic acid (5. A detailed spectroscopic analysis led to the structure elucidation of the alphitolic acid derivatives (1–5, and the semi-synthetic emmolic acid acetate (6. When tested in LPS (Lipopolysaccharides + IFN-γ (Interferon gamma activated RAW 264.7 macrophages, all compounds except (1 exhibited potent anti-inflammatory activity (IC50 values as low as 1.7 μM in terms of downregulation of NO and TNF-α production, but also demonstrated some considerable cytotoxicity.

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

    Directory of Open Access Journals (Sweden)

    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.

  8. NONSPECIFIC ANTI-INFLAMMATORY AGENTS. SOME NOTES ON THEIR PRACTICAL APPLICATION, ESPECIALLY IN RHEUMATIC DISORDERS.

    Science.gov (United States)

    BOLAND, E W

    1964-03-01

    A number of acute and chronic inflammatory disorders are amenable to varying degrees of therapeutic control with the administration of nonspecific anti-inflammatory drugs. An evaluation of these suppressive agents in the field of rheumatic diseases and practical suggestions regarding their administration are presented. Eight synthetically modified corticosteroid compounds are available commercially. Each of them exhibits qualitative differences in one or several physiologic actions, each has certain advantages and disadvantages in therapy, and each shares the major deterrent features of corticosteroids. Prednisone, prednisolone, methylprednisolone, fluprednisolone and paramethasone have similar therapeutic indices, and there is little choice between them for the usual rheumatoid patient requiring steroid therapy. Conversely, the therapeutic indices of dexamethasone, betamethasone and triamcinolone are lower than that of prednisolone; they are less desirable for routine use and should be reserved for specially selected cases. Salicylates are preferred to adrenocortical steroids in the treatment of the ordinary patient with acute rheumatic fever. Steroid therapy should be reserved for resistant cases and for those with significant carditis. Salicylates are mainstays for pain relief in rheumatoid arthritis, but with the analgesic doses usually employed their anti-inflammatory action is slight.Phenylbutazone is a highly useful anti-inflammatory agent, especially in management of acute gouty arthritis and ankylosing (rheumatoid) spondylitis; its metabolite, oxyphenylbutazone, does not exhibit clear-cut advantages. Colchicine specifically suppresses acute gouty arthritis. Its analogues, desacetylcolchicine and desacetylthiocolchicine, produce fewer unpleasant gastrointestinal symptoms, but may promote agranulocytosis and alopecia.A number of indole preparations with anti-inflammatory activity have been tested clinically. One of them, indomethacin, has received extensive

  9. A Review on Anti-Inflammatory Activity of Monoterpenes

    Directory of Open Access Journals (Sweden)

    Damião Pergentino de Sousa

    2013-01-01

    Full Text Available Faced with the need to find new anti-inflammatory agents, great effort has been expended on the development of drugs for the treatment of inflammation. This disorder reduces the quality of life and overall average productivity, causing huge financial losses. In this review the anti-inflammatory activity of 32 bioactive monoterpenes found in essential oils is discussed. The data demonstrate the pharmacological potential of this group of natural chemicals to act as anti-inflammatory drugs.

  10. Antimicrobial and anti-inflammatory activity of folklore: Mallotus peltatus leaf extract.

    Science.gov (United States)

    Chattopadhyay, Debprasad; Arunachalam, G; Mandal, Asit B; Sur, Tapas K; Mandal, Subash C; Bhattacharya, S K

    2002-10-01

    Since ages Mallotus peltatus (Geist) Muell. Arg. var acuminatus (Euphorbiaceae) leaf and stem bark is used in folk medicine to cure intestinal ailments and skin infections. In several intestinal ailments, localized inflammation is of common occurrence and hence we have evaluated the antimicrobial as well as anti-inflammatory activity of M. peltatus leaf extract. The crude methanol extract of M. peltatus leaves was found to be active against Staphylococcus aureus, Staphylococcus saprophyticus, Streptococcus faecalis, Bacillus subtilis, Escherichia coli and Proteus mirabilis and the dermatophytic fungi Microsporum gypseum. The minimum inhibitory concentration (MIC) ranges from 128 to 2000 microg ml(-1) for bacteria and 128 mg ml(-1) for fungi, while the minimum bactericidal concentration (MBC) was 2-4-fold higher than MIC. The methanol-water fraction of the extract showed similar activity against Staphylococcus, Streptococcus, Bacillus and Proteus isolates. The anti-inflammatory activity of the extract against carrageenan (acute model) and dextran-induced (subacute model) rat paw oedema and cotton pellet-induced granuloma (chronic model) in rats were studied using indomethacin (10 mg kg(-1)), a nonsteroid anti-inflammatory drug, as standard. The methanol extract at 200 and 400 mg kg(-1), and the n-butanol fractions A and B at 25 mg kg(-1), exhibited significant anti-inflammatory activity in Albino rats, compared with indomethacin. Phytochemical study revealed the presence of tannins, saponins, terpenoids, steroids and reducing sugars in the crude extract while the n-butanol fractions showed the presence of ursolic acid, beta-sitosterol and some fatty acids as major compounds. Further study with fractions showed that the antibacterial and anti-inflammatory activity is due to either fraction A (ursolic acid) alone or the combination of fractions A and B (beta-sitosterol and fatty acids) of the extract.

  11. Review of Anti-Inflammatory Herbal Medicines

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    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.

  12. Increased temperature and entropy production in cancer: the role of anti-inflammatory drugs.

    Science.gov (United States)

    Pitt, Michael A

    2015-02-01

    Some cancers have been shown to have a higher temperature than surrounding normal tissue. This higher temperature is due to heat generated internally in the cancer. The higher temperature of cancer (compared to surrounding tissue) enables a thermodynamic analysis to be carried out. Here I show that there is increased entropy production in cancer compared with surrounding tissue. This is termed excess entropy production. The excess entropy production is expressed in terms of heat flow from the cancer to surrounding tissue and enzymic reactions in the cancer and surrounding tissue. The excess entropy production in cancer drives it away from the stationary state that is characterised by minimum entropy production. Treatments that reduce inflammation (and therefore temperature) should drive a cancer towards the stationary state. Anti-inflammatory agents, such as aspirin, other non-steroidal anti-inflammatory drugs, corticosteroids and also thyroxine analogues have been shown (using various criteria) to reduce the progress of cancer.

  13. 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

    detection thresholds (MPDT) and the intensity of burn-induced erythema (erythema index, EI) were assessed in the area of the thermal injury, and areas of hyperalgesia to pin prick were determined outside the injury before and 3, 6 and 24 h after the burn injury. Burn injury led to a decrease in HPDT, HPT......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 0.2)....

  14. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  16. Synthesis and evaluation of the anti-inflammatory effects of niflumic acid lipophilic prodrugs in brain edema.

    Science.gov (United States)

    el Kihel, L; Bourass, J; Richomme, P; Petit, J Y; Letourneux, Y

    1996-11-01

    Five new lipophilic prodrugs of the non-steroidal anti-inflammatory drug, niflumic acid (Nifluril, CAS 4394-00-7), were synthetized and evaluated on the experimental brain edema (injection of phospholipase A2). The effect of these drugs in comparison with dexamethasone which elicits a marked effect on clinical and experimental brain edema was evaluated. Niflumic acid was vectorised by cholesterol, hexadecanol and by three 1,3-diacylglycerols. The anti-inflammatory activity of these compounds on experimental brain edema was evaluated by determination of the prostaglandin E2 (PGE2) brain tissue concentration. Niflumic acid reduced the prostaglandin E2 production more significantly than dexamethasone. Niflumic acid prodrug forms (1,3-dihexadecanoyl-2-[2-[3-(trifluoromethyl)anilino]nicotinoyl] glycerol and 1,3-dihexadecanoyl-2-[2-[3-(trifluoromethyl)anilino]nicotinoyloxybuta noyl] glycerol also showed a marked anti-inflammatory activity at low concentrations.

  17. 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.

  18. 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

  19. 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.

  20. Anti-inflammatory activity of Taraxacum officinale.

    Science.gov (United States)

    Jeon, Hye-Jin; Kang, Hyun-Jung; Jung, Hyun-Joo; Kang, Young-Sook; Lim, Chang-Jin; Kim, Young-Myeong; Park, Eun-Hee

    2008-01-04

    Taraxacum officinale has been widely used as a folkloric medicine for the treatment of diverse diseases. The dried plant was extracted with 70% ethanol to generate its ethanol extract (TEE). For some experiments, ethyl acetate (EA), n-butanol (BuOH) and aqueous (Aq) fractions were prepared in succession from TEE. TEE showed a scavenging activity in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, a diminishing effect on intracellular reactive oxygen species (ROS) level, and an anti-angiogenic activity in the chicken chorioallantoic (CAM) assay. In the carrageenan-induced air pouch model, TEE inhibited production of exudate, and significantly diminished nitric oxide (NO) and leukocyte levels in the exudate. It also possessed an inhibitory effect on acetic acid-induced vascular permeability and caused a dose-dependent inhibition on acetic acid-induced abdominal writhing in mice. Suppressive effects of TEE on the production of NO and expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-stimulated macrophages were also assessed. Among the fractions, the n-butanol fraction (BuOH) was identified to be most effective in the CAM assay. Collectively, Taraxacum officinale contains anti-angiogenic, anti-inflammatory and anti-nociceptive activities through its inhibition of NO production and COX-2 expression and/or its antioxidative activity.

  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. 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

    Directory of Open Access Journals (Sweden)

    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

  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. 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

  6. 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

  7. 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.

  8. Anti-inflammatory activity of different agave plants and the compound cantalasaponin-1.

    Science.gov (United States)

    Monterrosas-Brisson, Nayeli; Ocampo, Martha L Arenas; Jiménez-Ferrer, Enrique; Jiménez-Aparicio, Antonio R; Zamilpa, Alejandro; Gonzalez-Cortazar, Manases; Tortoriello, Jaime; Herrera-Ruiz, Maribel

    2013-07-10

    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.

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

    Directory of Open Access Journals (Sweden)

    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.

  10. Anti-inflammatory and ulcerogenic effects of indomethacin and tenoxicam in combination with cimetidine.

    Science.gov (United States)

    Maciel, Hermelinda P F; Cardoso, Luiz G V; Ferreira, Luciano R; Perazzo, Fábio F; Carvalho, José Carlos T

    2004-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been widely used for the modulation of the inflammatory response. However, a number of facts involving the occurrence of gastrointestinal lesions have limited the chronic use of NSAIDs. In order to diminish the occurrence of gastrointestinal damage caused by NSAIDs, the combination of NSAIDs with the H2 receptor blocker, cimetidine, has been evaluated. The anti-inflammatory and ulcerogenic effects of indomethacin and tenoxicam in association with or without cimetidine were determined at pre-clinical levels. It was observed that the group of animals treated with indomethacin and cimetidine, or tenoxicam and cimetidine (10 mg/kg, p.o.) demonstrated a significant reduction (P < 0.05, ANOVA followed by Tukey-Kramer multiple comparison test) of type-III gastric ulcers. Furthermore, indomethacin or tenoxicam (10 mg/kg, p.o.) in association with cimetidine increased the anti-inflammatory activity. The group, which received indomethacin and cimetidine presented the best performance in decreasing the inflammatory process (P < 0.05, ANOVA followed by Tukey-Kramer multiple comparison test).

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

    Science.gov (United States)

    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.

  12. Comparative anti-inflammatory effects of anti-arthritic herbal medicines and ibuprofen.

    Science.gov (United States)

    Kang, Joshua J; Samad, Mohammed A; Kim, Kye S; Bae, Soochan

    2014-09-01

    Non-steroidal anti-inflammatory drugs (NSAIDS), such as ibuprofen, are widely used over-the-counter drugs to treat arthritis, but they are often associated with side effects. Herbal medicines have been used to treat various diseases such as arthritis, but the scientific profiles are not well understood. In this study, we examined, in comparison with ibuprofen, the inhibitory effects on various inflammatory markers of the most commonly used herbal medicines to treat arthritis, boswellia (Boswellia sapindales), licorice (Glycyrrhiza glabra), guggul (Commiphora wightii), and neem (Azadirachta indica). To elicit inflammatory response, we exposed mouse myoblast C2C12 cells to lipopolysaccharide (LPS). Tumor necrosis factor-alpha (TNF-α) and monocyte chemotactic protein-1 (MCP-1), which are cytokines activated during an inflammatory response, were determined. The optimal non-toxic concentration was determined by exposing different concentrations of drugs (from 0.01 to 10 mg/mL). Cell death measurement revealed that the drug concentrations lower than 0.05 mg/mL were non-toxic concentrations for each drug, and these doses were used for the main experiments. We found that neem and licorice showed robust anti-inflammatory responses compared with ibuprofen. However, boswellia and guggul did not demonstrate significant anti-inflammatory responses. We concluded that neem and licorice are more effective than ibuprofen in suppressing LPS-induced inflammation in C2C12 cells.

  13. Evaluation of Anti-Inflammatory Drug-Conjugated Silicon Quantum Dots: Their Cytotoxicity and Biological Effect

    OpenAIRE

    Kenji Yamamoto; Akiyoshi Hoshino; Yasuhiro Futamura; Noriyoshi Manabe; Kouki Fujioka; Sanshiro Hanada

    2013-01-01

    Silicon quantum dots (Si-QDs) have great potential for biomedical applications, including their use as biological fluorescent markers and carriers for drug delivery systems. Biologically inert Si-QDs are less toxic than conventional cadmium-based QDs, and can modify the surface of the Si-QD with covalent bond. We synthesized water-soluble alminoprofen-conjugated Si-QDs (Ap-Si). Alminoprofen is a non-steroid anti-inflammatory drug (NSAID) used as an analgesic for rheumatism. Our results showed...

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

    Directory of Open Access Journals (Sweden)

    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.

  15. Anti-Inflammatory Activity of Ipomoea reniformis Methanolic Extract

    OpenAIRE

    Sanja S. D.; Sheth N.R.; Joshi D. M.; Golwala D.K.; Patel Dhaval; Raval M. K.

    2009-01-01

    In the present study, methanolic extract of Ipomoea reniformis herb (MEIR) in acute, subacute and chronic models of inflammation was assessed in rats. Administration of MEIR (200, 400 mg/kg, p.o.) exhibited significant anti-inflammatory activity. In acute inflammation as produced by Carrageenan 59.55 % and 64.04 % protection was observed. While in subacute anti-inflammatory models using formaldehyde-induced hind paw edema (after 1.5 h) 38.36 % and 47.95 % and in chronic anti-inflammatory mode...

  16. Cannabinoids as novel anti-inflammatory drugs.

    Science.gov (United States)

    Nagarkatti, Prakash; Pandey, Rupal; Rieder, Sadiye Amcaoglu; Hegde, Venkatesh L; Nagarkatti, Mitzi

    2009-10-01

    Cannabinoids are a group of compounds that mediate their effects through cannabinoid receptors. The discovery of Δ9-tetrahydrocannabinol (THC) as the major psychoactive principle in marijuana, as well as the identification of cannabinoid receptors and their endogenous ligands, has led to a significant growth in research aimed at understanding the physiological functions of cannabinoids. Cannabinoid receptors include CB1, which is predominantly expressed in the brain, and CB2, which is primarily found on the cells of the immune system. The fact that both CB1 and CB2 receptors have been found on immune cells suggests that cannabinoids play an important role in the regulation of the immune system. Recent studies demonstrated that administration of THC into mice triggered marked apoptosis in T cells and dendritic cells, resulting in immunosuppression. In addition, several studies showed that cannabinoids downregulate cytokine and chemokine production and, in some models, upregulate T-regulatory cells (Tregs) as a mechanism to suppress inflammatory responses. The endocannabinoid system is also involved in immunoregulation. For example, administration of endocannabinoids or use of inhibitors of enzymes that break down the endocannabinoids, led to immunosuppression and recovery from immune-mediated injury to organs such as the liver. Manipulation of endocannabinoids and/or use of exogenous cannabinoids in vivo can constitute a potent treatment modality against inflammatory disorders. This review will focus on the potential use of cannabinoids as a new class of anti-inflammatory agents against a number of inflammatory and autoimmune diseases that are primarily triggered by activated T cells or other cellular immune components.

  17. Utilization of spray drying technique for improvement of dissolution and anti-inflammatory effect of Meloxicam.

    Science.gov (United States)

    Shazly, Gamal; Badran, Mohamed; Zoheir, Khairy; Alomrani, Abdullah

    2015-01-01

    Meloxicam (MLX) is a poorly water-soluble non steroidal anti-inflammatory drug (NSAID). The main objective of the present work was to enhance the dissolution of MLX and thus its bioavailability by the aid of additives. The novelty of this work rises from the utilization of spray drying technology to produce micro particulates solid dispersion systems containing MLX in the presence of small amount of additives. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and Scan Electron Microscope (SEM) were used for studying the physico-chemical and morphological properties of MLX samples. The dissolution of MLX samples was investigated in two different pH media. The morphology of MLX solid dispersion micro-particles was spherical in shape according to SEM. FT-IR profiles indicated that a complex was formed between MLX and the additives. DSC patterns of the MLX micro-particles suggested a reduction in the crystallinity of MLX and probability of presence of an interaction between MLX and the additives. The rate of dissolution of the spray-dried MLX enhanced as compared with the unprocessed MLX in both acidic and neutral media. It was found that 100% of the added MLX released within 5 min in phosphate buffer dissolution medium (pH 7.4) compared to that of the unprocessed MLX (15% in 60 min). Such increase rate in the dissolution of the spray dried MLX could be attributed to the increase in wettability of MLX particles and the hydrophilic nature of the additives. The anti-inflammatory effect of the spray dried MLX was explored using formalin induced rat paw edema model. The spray-dried samples showed an increase in the anti-inflammatory activity of MLX as compared to the unprocessed MLX. This work reveals that the spray drying technique is suitable for preparation of micro-particles with improved dissolution and anti-inflammatory effect of MLX.

  18. 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.

  19. 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.

  20. 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

  1. 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.

  2. Anti-inflammatory Strategies to Prevent Diabetic Cardiovascular Disease.

    Science.gov (United States)

    Jialal, I; Devaraj, S

    2015-08-01

    Diabetes is a proinflammatory state and inflammation is crucial in the genesis of vascular complications. While there are many anti-inflammatory strategies, most of which have been shown to reduce inflammation in diabetes, there is sparse data on reduction in cardiovascular events (CVEs). To date, the only anti-inflammatory strategies that have been shown to reduce CVE in diabetes include statins, angiotensin receptor blockers, metformin, and pioglitazone. We also discuss the role of novel emerging therapies.

  3. 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.

  4. Effect of non-steroidal anti-inflammatory drug etoricoxib on the hematological parameters and enzymes of colon and kidney Efecto del fármaco antiinflamatorio no esteroideo etoricoxib sobre los parámetros hematológicos y las enzimas del colon y el riñón

    OpenAIRE

    N. Behal; S. Singh Kanwar; Sharma, P.; S. N. Sanyal

    2009-01-01

    The present study was designed to investigate the effects of a selective COX-2 inhibitor, etoricoxib in rats on the hematological and toxicity parameters in colon and kidney at two different doses of the drug, one within the therapeutic anti-inflammatory range as based on the reported ED50 value (Eto-1) while the other at ten times higher (Eto-2), relative to the toxicity studies which have not been reported so far. The results showed that the control and the drug treated animals achieved sim...

  5. 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.

  6. 牛乳制品对非甾体消炎药所致小肠黏膜机械屏障损伤的影响%The effects of milk and milk products on non-steroidal anti-inflammatory drug induced intestinal damage in rats

    Institute of Scientific and Technical Information of China (English)

    张烁; 吕宾; 晁冠群; 陈方明; 陈敏艳; 陈汉卿

    2011-01-01

    目的 探讨牛乳制品对非甾体消炎药所致小肠黏膜损伤的形态学结构及黏膜中表皮生长因子(EGF)表达的影响.方法 雄性SD大鼠80只,随机分为5组(每组16只),空白对照组和模型组予自由饮水,其余3组从第1天起分别予10%牛乳、10%牛初乳、酸牛乳管饲,第5天时除空白对照组外其余各组予双氯芬酸15 mg/kg管饲1次.于造模后24h和48 h分别评价小肠大体损伤评分、病理损伤评分,检测绒毛高度、肠黏膜超微结构变化.免疫组化法观察小肠黏膜EGF的表达.结果 24h和48 h时点牛初乳组大体和病理损伤评分均低于模型组.牛初乳组24h和48 h小肠绒毛高度分别为(145.7±16.5)μm和(139.2±19.0)μm,明显高于模型组[(119.2±19.2)μm和(105.4±18.4)μm],P<0.05.牛初乳组透射电镜下见小肠黏膜微绒毛较整齐,扫描电镜下见小肠绒毛表面光滑,顶端微绒毛密集;而模型组、牛乳组、酸牛乳组的超微结构改变相似,透射电镜下可见微绒毛水肿,排列紊乱,部分脱落,扫描电镜下见小肠黏膜表面粗糙不平,局部破溃,微绒毛减少甚至缺失.牛初乳组48 h时点小肠黏膜EGF阳性面积为(6170.5±1483.9)μm2,显著高于模型组[(3517.1±985.8)μm2],P<0.05.牛乳组、酸牛乳组的大体损伤评分、病理损伤评分、小肠绒毛高度、EGF阳性面积与模型组相似,差异无统计学意义.结论 牛初乳可有效防治双氯芬酸所致小肠黏膜损伤,维护小肠黏膜机械屏障的完整,推测其机制可能与牛初乳中的成分可维持小肠黏膜内EGF含量有关.%ObjectiveTo investigate the effect of milk and milk products on morphological structure and epidermal growth factor (EGF) of non-steroidal anti-inflammatory drugs (NSAIDs) induced small intestinal damage in animals.Methods Eighty male SD rats were randomly divided into 5 groups:control group,diclofenac group,diclofenac with 10% low fat milk group,diclofenac with 10% colostrum group

  7. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  9. Anti-inflammatory role of obestatin in autoimmune myocarditis.

    Science.gov (United States)

    Pamukcu, Ozge; Baykan, Ali; Bayram, Latife Cakir; Narin, Figen; Cetin, Nazmi; Narin, Nazmi; Argun, Mustafa; Ozyurt, Abdullah; Uzum, Kazim

    2016-01-01

    Obestatin is a popular endogeneous peptide, known to have an autoimmune regulatory effect on energy metabolism and the gastrointestinal system. Studies regarding the anti-inflammatory effects of obestatin are scarce. The aim of this study was to show the anti-inflammatory effect of obestatin in an experimental model of autoimmune myocarditis in rats. Experimental autoimmune myocarditis was induced in Lewis rats by immunization with subcutaneous administration of porcine cardiac myosin, twice at 7-day intervals. Intraperitoneal pretreatment with obestatin (50 μg/kg) was started before the induction of myocarditis and continued for 3 weeks. The severity of myocarditis was evidenced by clinical, echocardiographic and histological findings. In addition, by-products of neutrophil activation, lipid peroxidation, inflammatory and anti-inflammatory cytokines were measured in serum. Obestatin significantly ameliorated the clinical and histopathological severity of autoimmune myocarditis. Therapeutic effects of obestatin in myocarditis were associated with reduced lipid peroxidation, suppression of polymorphonuclear leukocyte infiltration and enhancement of glutathione synthesis, inhibition of serum inflammatory and activation of anti-inflammatory cytokines. Histopathologically, the left ventricle was significantly dilated, and its wall thickened, along with widespread lymphocytic and histocytic infiltration. The myocardium was severely infiltrated with relatively large mononuclear cells. These histopathological changes were observed in lesser degrees in obestatin-treated rats. This study demonstrated a novel anti-inflammatory effect of obestatin in an experimental model of autoimmune myocarditis. Consequently, obestatin administration may represent a promising therapeutic approach for myocarditis and dilated cardiomyopathy in the future.

  10. FORMULATION AND EVALUATION OF POLYHERBAL GEL FOR ANTI - INFLAMMATORY ACTIVITY

    Directory of Open Access Journals (Sweden)

    Gouri Dixit*, Ganesh Misal, Vijay Gulkari and Kanchan Upadhye

    2013-03-01

    Full Text Available ABSTRACT: In the present study, three medicinal plants Cynodon dactylon (L. Pers, Cassia tora Linn. and Cassia alata Linn having significant anti-inflammatory potential were selected to be formulated as polyherbal gels. The gels were prepared using the dried methanolic extract of Cassia tora Linn, Cassia alata Linn and Cynodon dactylon (L. Pers. Polyherbal gel formulations were evaluated for its pH, appearance and homogeneity, viscosity, spreadability and skin irritation studies. Assessment of Anti-inflammatory activity was done by carrageenan induced rat paw edema and formalin- induced rat paw edema. Individual and polyherbal gel of Cassia alata Linn,Cassia tora Linn. and Cynodon dactylon (L. Pers were found to possess anti-inflammatory effect in acute and chronic models. Polyherbal gel also showed synergistic effect as compared to individual gels which can be useful for the treatment of local inflammation.

  11. Anti-inflammatory Activity of Crinum defixum Ker-Gawl

    Directory of Open Access Journals (Sweden)

    Shilpa K

    2012-04-01

    Full Text Available Crinum defixum Ker-Gawl is a bulbous herb which has a wide geographical distribution in India. It is commonly called Bon-naharu (meaning wild garlic in Assam. Traditionally the bulb has been reported to have nauseant, emetic, emollient, diaphoretic properties and it is also used in various inflammatory conditions. The anti-inflammatory activity of the bulbs of the plants has been investigated in the present study in order to establish its traditional claims. The ethyl acetate, chloroform and ethanol extracts of bulbs of Crinum defixum were screened for anti-inflammatory activity by using carrageenan induced rat paw edema method. The study revealed that the ethyl acetate extract of the plant had significant anti-inflammatory activity than the chloroform and ethanol extracts. The study supports the ethanomedicinal use of this plant for inflammatory conditions.

  12. 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...... the overall antidepressant effect of adjunctive anti-inflammatory agents in the treatment of bipolar depression. METHODS: Completed and ongoing clinical trials of anti-inflammatory agents for BD published prior to 15 May 15 2015 were identified through searching the PubMed, Embase, Psych...... 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...

  13. 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.

  14. Hypoglycemic agents and potential anti-inflammatory activity

    Directory of Open Access Journals (Sweden)

    Kothari V

    2016-04-01

    Full Text Available Vishal Kothari,1 John A Galdo,2 Suresh T Mathews3 1Department of Nutrition and Dietetics, Boshell Diabetes and Metabolic Diseases Research Program, Auburn University, Auburn, 2Department of Pharmacy Practice, 3Department of Nutrition and Dietetics, Samford University, Birmingham, AL, USA Abstract: Current literature shows an association of diabetes and secondary complications with chronic inflammation. Evidence of these immunological changes include altered levels of cytokines and chemokines, changes in the numbers and activation states of various leukocyte populations, apoptosis, and fibrosis during diabetes. Therefore, treatment of diabetes and its complications may include pharmacological strategies to reduce inflammation. Apart from anti-inflammatory drugs, various hypoglycemic agents have also been found to reduce inflammation that could contribute to improved outcomes. Extensive studies have been carried out with thiazolidinediones (peroxisome proliferator-activated receptor- agonist, dipeptidyl peptidase-4 inhibitors, and metformin (AMP-activated protein kinase activator with each of these classes of compounds showing moderate-to-strong anti-inflammatory action. Sulfonylureas and alpha glucosidase inhibitors appeared to exert modest effects, while the injectable agents, insulin and glucagon-like peptide-1 receptor agonists, may improve secondary complications due to their anti-inflammatory potential. Currently, there is a lack of clinical data on anti-inflammatory effects of sodium–glucose cotransporter type 2 inhibitors. Nevertheless, for all these glucose-lowering agents, it is essential to distinguish between anti-inflammatory effects resulting from better glucose control and effects related to intrinsic anti-inflammatory actions of the pharmacological class of compounds. Keywords: diabetes, inflammation, insulin, metformin, thiazolidinedione, gliptin

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

    Science.gov (United States)

    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.

  16. Investigation Of Anti-Inflammatory Activity Of Bergamot Oil

    OpenAIRE

    2007-01-01

    Aim: Essential oil of Bergamot (BO) was investigated for anti-inflammatory activity using carrageenan-induced rat paw oedema test. Methods: For the anti-inflammatory activity measurement six different groups were established and BO was administered in three different doses: 0.025, 0.05 and 0.10 mL/kg. Indomethacin was used as a reference agent. Results: It was found that reduction in the inflammation was 95.70% with indomethacin, 27.56% with 0.025 mL/kg BO, 30.77% with 0.05 mL/kg BO and 63.39...

  17. Synthesis and anti-inflammatory activity of three nitro chalcones.

    Science.gov (United States)

    Gómez-Rivera, Abraham; Aguilar-Mariscal, Hidemí; Romero-Ceronio, Nancy; Roa-de la Fuente, Luis F; Lobato-García, Carlos E

    2013-10-15

    The aim of this study was to synthesize three nitro substituted chalcones and to evaluate their anti-inflammatory activity in the model of carrageenan induced edema in rats. The nitro chalcone were prepared by aldol condensation using of mechanical agitation and environmentally friendly solvents with 72-73% yields in approximately 2h. The three structures were evaluated on biological activity at dose of 200mg/kg and they showed anti-inflammatory protective effect by both oral and intraperitoneal administration, this effect was time dependent.

  18. EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF FICUS RETUSA (MORACEAE)

    OpenAIRE

    N. Jaya Raju; N. Sreekanth

    2011-01-01

    The study was designed to evaluate the anti-inflammatory effect of leaves of Ficus retusa (Moraceae) in Sanskrit, it is known as ‘Kantalaka’, ‘Kshudra’ and in Telugu it is well known as ‘Yerrajuvvi’. It is also called as “Indian Laurel Fig" of ethyl acetate and methanolic extracts in carrageenan induced albino wistar rats of either sex (175-250g). The anti-inflammatory effects of ethyl acetate extract of Ficus retusa 200, 400 mg/kg p.o were found to be significant (P

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

    Directory of Open Access Journals (Sweden)

    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

  20. 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.

  1. MECHANISMS OF ANTI-INFLAMMATORY ACTIVITY OF THE LEAF EXTRACT AND FRACTIONS OF MILLETTIA ABOENSIS

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    Ajaghaku Daniel Lotanna

    2013-09-01

    Full Text Available The acute and chronic anti-inflammatory effect of the crude extracts and fractions of Millettia aboensis leaves, a popular Nigerian traditional anti-inflammation remedy and possible mechanism of effect was investigated. Phytochemical analysis of the crude and fraction revealed the presence of anti-inflammatory phyto-compounds – terpenoids, steroids, flavonoids, tannins, saponins and glycosides. No death was recorded from acute toxicity study. The crude and methanol fraction at 300 and 200 mg/kg showed significant (p < 0.05 inhibition of egg albumin induced paw edema. Effect of the extract and fraction on topical oedema induced by xylene on mouse ear revealed that methanol fraction at 5 mg/ear had the highest activity with percentage inhibition of 61.90 % compared to the 54.76 % inhibition produced by Indomethacin. Methanol fraction at 300 mg/kg produced a significant (p < 0.05 inhibition of formaldehyde induced arthritis with percentage inhibition of 40.93 %. Result of the ulcergenic effect in rat demonstrated that both the crude and methanol fraction possess ulcergenic effect though lower than that produced by Indomethacin. Methanol fraction at 400 mg/kg also produced significant (p < 0.05 inhibition of leucocytes migration compared with the control. Both extract and methanol fraction produced stabilization effect on the heat-induced and hypotonicity induced red blood cell haemolysis. These results suggest that the ethanol leaf extract of M. aboensis possess acute and chronic anti-inflammatory activity that is most active in the methanol fraction. The activity may be as a result of combined inhibition of prostaglandin synthesis, leukocyte migration and membrane stabilization effect.

  2. On radiation damage to normal tissues and its treatment. Pt. 2; Anti-inflammatory drugs

    Energy Technology Data Exchange (ETDEWEB)

    Michalowski, A.S. (MRC Cyclotron Unit, Hammersmith Hospital, London (United Kingdom))

    1994-01-01

    In addition to transiently inhibiting cell cycle progression and sterilizing those cells capable of proliferation, irradiation disturbs the homeostasis effected by endogenous mediators of intercellular communication (humoral component of tissue response to radiation). Changes in the mediator levels may modulate radiation effects either by a assisting a return to normality (e.g., through a rise in H-type cell lineage-specific growth factors) or by aggravating the damage. The latter mode is illustrated with reports on changes in eicosanoid levels after irradiation and on results of empirical treatment of radiation injuries with anti-inflammatory drugs. Prodromal, acute and chronic effects of radiation are accompanied by excessive production of eicosanoids (prostaglandins, prostacyclin, thromboxanes and leukotrienes). These endogenous mediators of inflammatory reactions may be responsible for the vasodilatation, vasoconstriction, increased microvascular permeability, thrombosis and chemotaxis observed after radiation exposure. Glucocorticoids inhibit eicosanoid synthesis primarily by interfering with phospholipase A[sub 2] whilst non-steroidal anti-inflammatory drugs prevent prostaglandin/thromboxane synthesis by inhibiting cycloxygenase. When administered after irradiation on empirical grounds, drugs belonging to both groups tend to attenuate a range of prodomal, acute and chronic effects of radiation in man and animals. Taken together, these two sets of observations are highly suggestive of a contribution of humoral factors to the adverse responses of normal tissues and organs to radiation. A full account of radiation damage should therefore consist of complementary descriptions of cellular and humoral events. Further studies on anti-inflammatory drug treatment of radiation damage to normal organs are justified and desirable. (orig.).

  3. Investigating the anti-inflammatory effects of curcumin on Endotoxin-induced uveitis in rabbits' eyes

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    Nader Kavian

    2016-09-01

    Full Text Available Corticosteriods are used in the treatment of inflammatory diseases of the eye such as uveitis, but these drugs have many side effects such as cataract and primary open angle glaucoma (POAG and aggravation of keratitis caused by herpes simplex, fungal keratitis, etc. Therefore, the efforts to find new medicines that control ocular inflammation while lacking any steroid side effects continue. Curcumin is a yellow substance found in turmeric and in traditional medicine it is used as an antiseptic, analgesic, anti-inflammatory and antioxidant. In this study, the anti-inflammatory effect of this substance was investigated. For this purpose, six adult rabbits of the same breed were used. To create the inflammation, 100mg of polysaccharide of Escherichia coli bacteria endotoxin was injected into the vitreous of the rabbits' both eyes. Then …0.1cc.. curcumin pure extract was injected into the vitreous of their right eye. After three days, the eyes were removed and placed in a formalin for 2 weeks to fixate them, and then using microscopic studies, the degrees of inflammation of both eyes, with and without the injection of the drug, were compared. The results show no inflammation or inflammatory cells in the eyes injected with curcumin. From the present study, it is concluded that curcumin can be considered in treatment of ocular inflammations as a complementary substance or drug.

  4. Antinociceptive, Anti-Inflammatory, and Antipyretic Activity of Mangrove Plants: A Mini Review

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    J. A. Shilpi

    2012-01-01

    Full Text Available Mangrove plants are specialised plants that grow in the tidal coasts of tropic and subtropic regions of the world. Their unique ecology and traditional medicinal uses of mangrove plants have attracted the attention of researchers over the years, and as a result, reports on biological activity of mangrove plants have increased significantly in recent years. This review has been set out to compile and appraise the results on antinociceptive, anti-inflammatory, and antipyretic activity of mangrove plants. While the Web of Knowledge, Google Scholar, and PubMed were the starting points to gather information, other pieces of relevant published literature were also adequately explored for this purpose. A total of 29 reports on 17 plant species have been found to report such activities. While 19 reports were on the biological activity of the crude extracts, 10 reports identified the active compound(s of various chemical classes of natural products including terpenes, steroids, and flavonoids. This review finds that antinociceptive, anti-inflammatory, and antipyretic activity appears to be widespread in mangrove plants.

  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. Anti-inflammatory and anti-arthritic effects of yucca schidigera: A review

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    Piacente S

    2006-03-01

    Full Text Available Abstract Yucca schidigera is a medicinal plant native to Mexico. According to folk medicine, yucca extracts have anti-arthritic and anti-inflammatory effects. The plant contains several physiologically active phytochemicals. It is a rich source of steroidal saponins, and is used commercially as a saponin source. Saponins have diverse biological effects, including anti-protozoal activity. It has been postulated that saponins may have anti-arthritic properties by suppressing intestinal protozoa which may have a role in joint inflammation. Yucca is also a rich source of polyphenolics, including resveratrol and a number of other stilbenes (yuccaols A, B, C, D and E. These phenolics have anti-inflammatory activity. They are inhibitors of the nuclear transcription factor NFkappaB. NFkB stimulates synthesis of inducible nitric oxide synthase (iNOS, which causes formation of the inflammatory agent nitric oxide. Yucca phenolics are also anti-oxidants and free-radical scavengers, which may aid in suppressing reactive oxygen species that stimulate inflammatory responses. Based on these findings, further studies on the anti-arthritic effects of Yucca schidigera are warranted.

  7. A novel compound isolated from Sclerochloa dura has anti-inflammatory effects

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    Bukhari Syed Majid

    2016-01-01

    Full Text Available The activation of PLA2 by means of pro-inflammatory cytokines results in the subsequent release of arachidonic acid (AA and generates eicosanoids, which further propagate inflammation. By 6the cyclooxygenases (COX1/2 responsible for the enzymatic conversion of AA to eicosanoids, the non-steroidal anti-inflammatory drugs are effective in relieving the pain and discomfort of inflammation. By using AA release assay as a guide for biological and anti-inflammatory activity, novel compound 1-O-(3-O-linolenoyl-6-deoxy-6-sulfo-α-D-glucopyranosyl-glycerol (1 together with five known compounds isovitexin, byzantionoside B, tricin 4’-O-(erythro-β-guaiacylglyceryl ether 7-O-β-glucopyranoside, 1-O-feruloyl glycerol and tricin 7-glucoside were isolated from the methanol extract of the aerial parts of Sclerochloa dura using LC techniques (Sephadex LH-20 column chromatography, preparative HPLC and semi-preparative HPLC. All isolated compounds were identified using spectroscopic NMR spectroscopy and MS spectrometry. Novel compound (1 was found to be an effective inhibitor of AA release with an IC50 value of 0.09 ± 0.03 mg mL-1.

  8. 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.

  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. Proinflammatory and anti-inflammatory cytokines in meningococcal disease.

    OpenAIRE

    Riordan, F A; Marzouk, O; Thomson, A. P.; Sills, J A; Hart, C. A.

    1996-01-01

    Interleukin-10 (IL-10), an anti-inflammatory cytokine, was measured in 131 children with meningococcal disease. IL-10 concentrations were significantly higher in children who died and correlated positively with proinflammatory cytokines. Children who die from meningococcal disease have high IL-10 concentrations, which do not suppress proinflammatory cytokines.

  11. 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.

  12. 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.

  13. 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.

  14. Anti-inflammatory activity of mycelial extracts from medicinal mushrooms.

    Science.gov (United States)

    Geng, Yan; Zhu, Shuiling; Lu, Zhenming; Xu, Hongyu; Shi, Jin-Song; Xu, Zheng-Hong

    2014-01-01

    Medicinal mushrooms have been essential components of traditional Chinese herbal medicines for thousands of years, and they protect against diverse health-related conditions. The components responsible for their anti-inflammatory activity have yet to be fully studied. This study investigates the anti-inflammatory activity of n-hexane, chloroform, ethyl acetate, and methanol extracts of mycelia in submerged culture from 5 commercially available medicinal mushrooms, namely Cephalosporium sinensis, Cordyceps mortierella, Hericium erinaceus, Ganoderma lucidum, and Armillaria mellea. MTT colorimetric assay was applied to measure the cytotoxic effects of different extracts. Their anti-inflammatory activities were evaluated via inhibition against production of lipopolysaccharide (LPS)-induced nitric oxide (NO) in murine macrophage-like cell line RAW264.7 cells. Of the 20 extracts, n-hexane, chloroform, ethyl acetate, and methanol extracts from C. sinensis, C. mortierella, and G. lucidum; chloroform extracts from H. erinaceus and A. mellea; and ethyl acetate extracts from A. mellea at nontoxic concentrations (mushrooms exhibited anti-inflammatory activity that might be attributable to the inhibition of NO generation and can therefore be considered a useful therapeutic and preventive approach to various inflammation-related diseases.

  15. Marine Diterpenoids as Potential Anti-Inflammatory Agents

    Science.gov (United States)

    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

  16. Anti-Inflammatory Activity of Ipomoea reniformis Methanolic Extract

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    Sanja S. D.

    2009-10-01

    Full Text Available In the present study, methanolic extract of Ipomoea reniformis herb (MEIR in acute, subacute and chronic models of inflammation was assessed in rats. Administration of MEIR (200, 400 mg/kg, p.o. exhibited significant anti-inflammatory activity. In acute inflammation as produced by Carrageenan 59.55 % and 64.04 % protection was observed. While in subacute anti-inflammatory models using formaldehyde-induced hind paw edema (after 1.5 h 38.36 % and 47.95 % and in chronic anti-inflammatory model using cotton pellet granuloma 15.02 % and 19.19 % protection from inflammation was observed. MEIR did not show any sign of toxicity and mortality up to a dose level of 1000 mg/kg, p.o. in rats. The results obtained suggest that the methanolic extract of Ipomoea reniformis herb (MEIR is endowed with effective anti-inflammatory activity mediated via either by inhibition of cyclooxygenase cascade and by blocking the release of vasoactive substances (histamine, serotonin and kinins. These findings seem to justify the use of the plant in traditional Indian medicine in the treatment of inflammation, including arthritic conditions.

  17. Boswellia carterii liquisolid systems with promoted anti-inflammatory activity.

    Science.gov (United States)

    Mostafa, Dina Mahmoud; Ammar, Nagwa Mohammed; Abd El-Alim, Sameh Hosam; Kassem, Ahmed Alaa; Hussein, Rehab Ali; Awad, Gamal; El-Awdan, Sally Abdul-Wanees

    2015-01-01

    Boswellia carterii (BC) Birdwood oleogum resin is an ancient remedy of inflammation processes known since Ancient Egyptian time. Of boswellic acids, 3-acetyl-11-keto-β-boswellic acid (AKBA) is the most potent anti-inflammatory active principle. Liquisolid systems of the biologically active fraction of BC oleogum resin were prepared for improving dissolution properties using low dose oral delivery to achieve enhanced anti-inflammatory activity, in comparison with the standard oral anti-inflammatory; Indomethacin. AKBA was assayed, employing an accurate and sensitive HPLC method. Detection was carried out at 210 nm using UV/Vis detector. A solubility study for the bioactive fraction was conducted. Microcrystalline cellulose and Aeroperl®300 Pharma were used as carrier and coating materials. Angle of slide, liquid load factor and Carr's flow index were estimated. Six systems were prepared using polyethylene glycol 400, solvent and two drug loading concentrations; 20 and 40 %. For each concentration, three carrier: coat ratios were dispensed; 20:1, 10:1, and 5:1. Dissolution study was performed and two systems were selected for characterization and in vivo evaluation by investigating upper GIT ulcerogenic effect and anti-inflammatory efficacy in rats. Results indicate absence of ulcers and significantly higher and prolonged anti-inflammatory efficacy for formulations F1 and F2, with carrier: coat ratio, 5:1 and drug loads of 20 and 40 %, respectively, compared with standard oral indomethacin. We conclude higher efficacy of BC bioactive fraction liquisolids compared with Indomethacin with greater safety on GIT, longer duration of action and hence better patient compliance.

  18. 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

  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...... injury occurs in diverse situations and the nature of muscle injuries varies significantly, complicating extrapolations between experimental models and "real life." Classical muscle strain injuries occur at the interphase between the muscle fibers and connective tissue, most often in the myotendinuous...... junction, whereas contusion or overload injury can damage both myofibers and intramuscular connective tissue. The role of NSAIDs in muscle repair is complicated by differences in injury models used, variables evaluated, and time point(s) selected for evaluations. While the temporal pattern of the influence...

  20. Anti-inflammatory and cytotoxic activities of Bursera copallifera

    Science.gov (United States)

    Columba-Palomares, M. F. María C.; Villareal, Dra. María L.; Acevedo Quiroz, M. C. Macdiel E.; Marquina Bahena, M. C. Silvia; Álvarez Berber, Dra. Laura P.; Rodríguez-López, Dra. Verónica

    2015-01-01

    Background: The plant species Bursera copallifera (DC) bullock is used in traditional medicine to treat inflammation. The leaves of this plant can be prepared as an infusion to treat migraines, bronchitis, and dental pain Objective: The purpose of this study was to determine the anti-inflammatory and cytotoxic activities of organic extracts from the stems, stem bark, and leaves of B. copallifera, which was selected based on the knowledge of its traditional use. Materials and Methods: We evaluated the ability of extracts to inhibit mouse ear inflammation in response to topical application of 12-O tetradecanoylphorbol-13-acetate. The extracts with anti-inflammatory activity were evaluated for their inhibition of pro-inflammatory enzymes. In addition, the in vitro cytotoxic activities of the organic extracts were evaluated using the sulforhodamine B assay. Results: The hydroalcoholic extract of the stems (HAS) exhibited an anti-inflammatory activity of 54.3% (0.5 mg/ear), whereas the anti-inflammatory activity of the dichloromethane-methanol extract from the leaves (DMeL) was 55.4% at a dose of 0.1 mg/ear. Methanol extract from the leaves (MeL) showed the highest anti-inflammatory activity (IC50 = 4.4 μg/mL), hydroalcoholic extract of leaves, and DMeL also reduce the enzyme activity, (IC50 = 6.5 μg/mL, IC50 = 5.7 μg/mL), respectively, from stems HAS exhibit activity at the evaluated concentrations (IC50 =6.4 μg/mL). The hydroalcoholic extract of the stems exhibited the highest cytotoxic activity against a breast adenocarcinoma cell line (MCF7, IC50 = 0.90 μg/mL), whereas DMeL exhibited an IC50 value of 19.9 μg/mL. Conclusion: In conclusion, extracts from leaves and stems inhibited cyclooxygenase-1, which is the target enzyme for nonsteroidal anti inflammatory drugs, and some of these extracts demonstrated substantial antiproliferative effects against the MCF7 cell line. These results validate the traditional use of B. copallifera. PMID:26664022

  1. New Isorhamnetin Derivatives from Salsola imbricata Forssk. Leaves with Distinct Anti-inflammatory Activity

    OpenAIRE

    Osman, Samir M.; El Kashak, Walaa A.; Michael Wink; 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 ...

  2. Synthesis and pharmacological evaluation of polyfunctional benzimidazole-NSAID chimeric molecules combining anti-inflammatory, immunomodulatory and antioxidant activities.

    Science.gov (United States)

    Bansal, Yogita; Silakari, Om

    2014-11-01

    Polyfunctional compounds comprise a novel class of therapeutic agents for treatment of multifactorial diseases. The present study reports a series of benzimidazole-non-steroidal anti-inflammatory drugs (NSAIDs) conjugates (1-10) as novel polyfunctional compounds synthesized in the presence of orthophosphoric acid. The compounds were evaluated for anti-inflammatory (carageenan-induced paw edema model), immunomodulatory (direct haemagglutination test and carbon clearance index models), antioxidant (in vitro and in vivo) and for ulcerogenic effects. Each of the compound has retained the anti-inflammatory activity of the corresponding parent NSAID while exhibiting significantly reduced gastric ulcers. Additionally, the compounds are found to possess potent immunostimulatory and antioxidant activities. The compound 8 was maximally potent (antibody titre value 358.4 ± 140.21, carbon clearance index 0.053 ± 0.002 and antioxidant EC50 value 0.03 ± 0.006). These compounds, exhibiting such multiple pharmacological activities, can be taken as lead for the development of potent drugs for the treatment of chronic multifactorial diseases involving inflammation, immune system modulation and oxidative stress such as cancers. The Lipinski's parameters suggested the compounds to be bear drug like properties.

  3. 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

  4. ANTI-INFLAMMATORY ACTIVITY OF LEPIDAGATHIS CRISTATA FLOWER EXTRACTS

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    Aravinda Reddy Purma

    2013-12-01

    Full Text Available The Lepidigathis cristata Wlld belong to the family of Acanthecae. In the present study the Anti-inflammatory activity of flower extracts were performed. The methanol, ethyl acetate, chloroform extracts were prepared by soxhlet extraction method and were used for Anti-inflammatory activity in two dose level that is 200 and 400 mg/kg body weight in two screening methods, one is carrageenans induced paw edema method (n = 5, another is Formalin induced paw edema method (n = 5. The flower chloroform extracts showed maximum activity in both models with 50 and 43.4 % of protection at 120 and 180 minutes intervals at the dose of 400 mg/kg body weight respectively.

  5. Anti-Inflammatory and Gastroprotective Evaluation of Prodrugs of Piroxicam

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    Vivekkumar K. Redasani

    2014-01-01

    Full Text Available Therapeutically potential prodrugs of piroxicam were synthesized by effective masking of enolic hydroxyl group through generation of ester congeners. The reaction facilitated using N,N′-dicyclohexylcarbodiimide coupled with acetic acid, benzoic acid, p-toluic acid, m-toluic acid, and cinnamic acid. Synthesized prodrugs were characterized for confirmation of the said structures. The modification of piroxicam showed better anti-inflammatory activity as evoked by all prodrugs. Interestingly, compound 3e, cinnamic acid ester prodrug, depicted 75 percent inhibition of rat paw edema as compared to 56 percent for parent piroxicam at 6 h of study. The present work proves the applicability not only with increased anti-inflammatory activity, but also with marked attenuation in ulcerogenicity. Novel prodrug 3e, cinnamic acid derivative, was found to be the least ulcerogenic having ulcer index of 0.67 as compared to parent drug piroxicam with 2.67.

  6. CHEMICAL COMPOSITION AND ANTI-INFLAMMATORY ACTIVITY OF Roldana platanifolia

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    Amira Arciniegas

    2015-11-01

    Full Text Available The chemical study of Roldana platanifolia led to the isolation of β-caryophyllene, five eremophilanolides, chlorogenic acid, and a mixture of β-sitosterol-stigmasterol, β-sitosteryl glucopyranoside, and sucrose. The anti-inflammatory activities of the extracts and isolated products were tested using the 12-O-tetradecanoylphorbol-13-acetate (TPA model of induced acute inflammation. The acetone and methanol extracts showed dose dependent activities (ID50 0.21 and 0.32 mg/ear, respectively, while none of the isolated compounds exhibited relevant edema inhibition. The active extracts were also evaluated with the myeloperoxidase assay technique (MPO to determine their ability to prevent neutrophil infiltration. Results showed that the anti-inflammatory activity was related to the compound’s ability to inhibit pro-inflammatory mediators such as neutrophils.

  7. 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.

  8. 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.

  9. Effect of non-steroidal anti-inflammatory drug etoricoxib on the hematological parameters and enzymes of colon and kidney Efecto del fármaco antiinflamatorio no esteroideo etoricoxib sobre los parámetros hematológicos y las enzimas del colon y el riñón

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    N. Behal

    2009-06-01

    Full Text Available The present study was designed to investigate the effects of a selective COX-2 inhibitor, etoricoxib in rats on the hematological and toxicity parameters in colon and kidney at two different doses of the drug, one within the therapeutic anti-inflammatory range as based on the reported ED50 value (Eto-1 while the other at ten times higher (Eto-2, relative to the toxicity studies which have not been reported so far. The results showed that the control and the drug treated animals achieved similar linear growth rate and also showed no major alterations in the histological parameters in the liver and kidney tissue. The animals treated with lower dose of etoricoxib showed an overall decrease in total leukocytes counts as well as in the number of neutrophils, lymphocytes, monocytes and eosinophills while the higher dose of the drug produced a highly significant increase in all the cell counts. However, the drug treatment at both the dose level produced significant fall in the activities of alkaline phosphatase, sucrase, lactase and maltase in the kidney but increased the activity of alkaline phosphatase in colon. The treatment of etoricoxib did not produce any change in the nitric oxide and citrulline levels in kidney while an increase was noted in the colonic tissue. It was concluded that etoricoxib is a relatively safe drug at its anti-inflammatory ED50 dose in rats when the hematological parameters and the structural and functional characteristics of kidney and colonic tissues were studied.El presente estudio se diseñó para investigar los efectos de un inhibidor selectivo de la COX-2, etoricoxib, sobre los parámetros hematológicos y de toxicidad en colon y riñón de rata, con dos dosis distintas del fármaco, una dentro del rango terapéutico sobre la base del valor ED50 notificado (Eto-1 mientras que la otra fue diez veces superior (Eto-2, relativa a los estudios de toxicidad que aún no han sido publicados. Los resultados mostraron que los

  10. Anti-inflammatory activity of arctigenin from Forsythiae Fructus.

    Science.gov (United States)

    Kang, Hyo Sook; Lee, Ji Yun; Kim, Chang Jong

    2008-03-05

    Oleaceae Forsythiae Fructus has been used for anti-inflammatory, diuretics, antidote, and antibacterials in traditional herbal medicine. Our previous screening of medicinal plants showed that methanol (MeOH) extract of Forsythiae Fructus had significant anti-inflammatory activity, but the active ingredients remain unclear. For isolation of active ingredient of MeOH extract of Forsythiae Fructus, it was partitioned with n-hexane and ethylacetate (EtOAc), and arctigenin was isolated from EtOAc fraction by column chromatography with anti-inflammatory activity-guided separation. Its activity was evaluated in the animal models of inflammation including myeloperoxidase (MPO) and eosinophil peroxidase (EPO) activities in the edematous tissues homogenate, and silica-induced reactive oxygen species (ROS) production in the RAW 264.7 cell line. It was shown that arctigenin (100 mg/kg) had significantly decreased not only carrageenan-induced paw edema 3 and 4h after injection of carrageenan, arachidonic acid (AA)-induced ear edema at a painting dose of 0.1-1.0mg/ear, and acetic acid-induced writhing response and acetic acid-induced capillary permeability accentuation at an oral dose of 25-100, and 100 mg/kg, respectively, but also MPO and EPO activities at a painting dose of 0.1-1.0mg/ear in the AA-induced edematous tissues homogenate as indicators of neutrophils and eosinophils recruitment into the inflamed tissue. Further, arctigenin (0.1-10 microM) also significantly inhibited the intracellular ROS production by silica. These results indicate that arctigenin is a bioactive agent of Forsythiae Fructus having significant anti-inflammatory action by inhibition of the exudation, and leukocytes recruitment into the inflamed tissues. The pharmacologic mechanism of action of arctigenin may be due to the inhibition of release/production of inflammatory mediators such as AA metabolites and free radicals.

  11. Anti-inflammatory activity of Lychnophora passerina, Asteraceae (Brazilian Arnica).

    OpenAIRE

    Oliveira, Patricia Capelari de; Paula, Carmem Aparecida de; Rezende, Simone Aparecida; Campos, Fernanda Torres; Guimarães, Andrea Grabe; Lombardi, Júlio Antônio; Guimarães, Dênia Antunes Saúde

    2011-01-01

    Ethnopharmacological relevance: Lychnophora passerina (Asteraceae), popularly known as arnica, is used to treat inflammation, pain, rheumatism, contusions, bruises and insect bites in Brazilian traditional medicine. Materials and methods: The anti-inflammatory activity of crude ethanolic extract of aerial parts of L. passerina and its ethyl acetate and methanolic fractions had their abilities to modulate the production of NO, TNF-α and IL-10 inflammatory mediators in LPS/IFN-γ-stimulated J774...

  12. Mangiferin: A xanthonoid with multipotent anti-inflammatory potential.

    Science.gov (United States)

    Saha, Sukanya; Sadhukhan, Pritam; Sil, Parames C

    2016-09-10

    Over the last era, small molecules sourced from different plants have gained attention for their varied and long-term medicinal benefits. Their advantageous therapeutic effects in diverse pathological complications lead researchers to give an ever-increasing emphasis on them and discover their novel therapeutic potentials. Among these, the heat stable, xanthonoid group of organic molecules has gained special importance with distinctive regards to the bioactive molecule mangiferin due to its solubility in water. Mangiferin, a yellow polyphenol having C-glycosyl xanthone structure, is widely present in different edible sources like mango, and possesses numerous biological activities. Extensive research with this molecule shows its antioxidant, anti-inflammatory, antidiabetic, anticancer, antimicrobial, analgesic, and immunomodulatory properties. Thus, it provides protection against a wide range of physiological disorders. The C-glucosyl linkage and polyhydroxy groups in mangiferin's structure contribute essentially to its free radical-scavenging activity. Moreover, its ability in regulating various transcription factors like NF-κB, Nrf-2, etc. and modulating the expression of different proinflammatory signaling intermediates like tumor necrosis factor-α, COX-2, etc. contribute to its anti-inflammatory, anticancer, and antidiabetic potentials. In this comprehensive article, information has been provided about the sources, chemical structure, metabolism, and different biological activities of mangiferin with special emphasis on the underlying cellular signal transduction pathways. Insights into an in-depth assessment of mangiferin's anti-inflammatory therapeutic potential have also been discussed in detail. On an overall perspective, this review aims to stage mangiferin's diversified therapeutic applications and its emerging possibility as a promising drug in future based on its anti-inflammatory property. © 2016 BioFactors, 42(5):459-474, 2016.

  13. 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.

  14. 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

    2015-08-05

    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.

  15. 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.

  16. 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.

  17. 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.

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

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

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    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.

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

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

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    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.

  2. [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.

  3. ANTI-INFLAMMATORY AND ANTIOXIDANT EFFECT OF ARECA CATECHU

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    Reena Rosy Nelson Anthikat* and A. Michael

    2012-01-01

    Full Text Available Context: The present investigation provides proof for the effectiveness of Arecanut extract as an anti-inflammatory agent. Arecanut extract is a natural plant product mimic of peroxidase.Objective: To explore the Anti-inflammatory activity of aqueous extract of Areca catechu L in carrageenan, dextran and formalin induced inflammation models in Swiss albino mice, by injection into the interdigital area, through the subplantar region of the paw. To explore the antioxidant effects of Arecanut extract on the in-vitro system.Method: Treatment with aqueous extract at 250 mg/kg.bwt and 500 mg/kg.body weight and untreated group was started orally 1 hour prior to the subplantar injection of carrageenan. The paw volume was measured using vernier calipers, before and one hour after carrageenan injection. Similarly in the case of dextran, initial readings were taken on the first day, prior to Formalin administration. Day one readings were taken one hour post formalin administration. This was taken during seven consecutive days challenge period. The drug aqueous arecanut extract at 200mg/kg.bwt, 500 mg/kg.bwt produced reduction in inflammation of the paw produced due to carrageenan, formalin and dextran. In-vitro antioxidant studies showed that aqueous arecanut extract could inhibit superoxide radical production, could inhibit hydroxyl radicals, and could prevent lipid peroxidation. Arecanut extract could scavenge DPPH radicals and also ABTS. In FRAP assay, the reduction of ferric to ferrous is also seen in a concentration dependant manner.Results: The present investigation provides proof for the effectiveness of treatment as an anti-inflammatory and antioxidant agent. Compared with the control group, the arecanut treated group showed free radical scavenging ability. Compared with the control group, the treatment of mice with Arecanut extract showed reduction in paw oedema in a dose dependent manner at 200 mg/kg.bwt and 500 mg/kg.bwt.Discussion and

  4. 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...

  5. Terpenoids with anti-inflammatory activity from Abies chensiensis.

    Science.gov (United States)

    Zhao, Qian-Qian; Wang, Shu-Fang; Li, Ya; Song, Qiu-Yan; Gao, Kun

    2016-06-01

    The phytochemical investigation of Abies chensiensis led to the isolation and identification of nine new compounds including eight triterpenoids (1-8) and a new abietane-type diterpene (9), along with three known compounds (10-12). The absolute configuration of 9 was assigned by X-ray diffraction analysis. Compounds 1-11 were evaluated for the anti-inflammatory activity. Among the tested compounds, 1, 2, 5 and 6 exhibited potent inhibitory activity with IC50 values of 15.97, 18.73, 20.18 and 10.97μM, respectively.

  6. Morroniside cinnamic acid conjugate as an anti-inflammatory agent.

    Science.gov (United States)

    Takeda, Yoshinori; Tanigawa, Naomi; Sunghwa, Fortunatus; Ninomiya, Masayuki; Hagiwara, Makoto; Matsushita, Kenji; Koketsu, Mamoru

    2010-08-15

    A morroniside cinnamic acid conjugate was prepared and evaluated on E-selectin mediated cell-cell adhesion as an important role in inflammatory processes. 7-O-Cinnamoylmorroniside exhibited excellent anti-inflammatory activity (IC(50)=49.3 microM) by inhibiting the expression of E-selectin; further, it was more active than another cinnamic-acid-conjugated iridoid glycoside (harpagoside; IC(50)=88.2 microM), 7-O-methylmorroniside, and morroniside itself. As a result, 7-O-cinnamoylmorroniside was observed to be a potent inhibitor of TNF-alpha-induced E-selectin expression.

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

    OpenAIRE

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

    2015-01-01

    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 Δ9-tetrahydrocannabinol (Δ9-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 therape...

  8. 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....

  9. 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.

  10. Anti-inflammatory and antinociceptive activity of Urera aurantiaca.

    Science.gov (United States)

    Riedel, R; Marrassini, C; Anesini, C; Gorzalczany, S

    2015-01-01

    Urera aurantiaca Wedd. (Urticaceae) is a medicinal plant commonly used in traditional medicine to relieve pain in inflammatory processes. In the present study, the in vivo anti-inflammatory and antinociceptive effects of U. aurantiaca methanolic extract and its possible mechanisms of action were investigated. The extract showed anti-inflammatory activity in the ear edema in mice test (34.3% inhibition), myeloperoxidase (MPO) activity was markedly reduced in animals administered with the extract: within 49.6% and 68.5%. In the histological analysis, intense dermal edema and intense cellular infiltration of inflammatory cells were markedly reduced in the ear tissue of the animals treated with the extract. In the carrageenan-induced hind paw edema in rats assay the extract provoked a significant inhibition of the inflammation (45.5%, 5 h after the treatment) and the MPO activity was markedly reduced (maximum inhibition 71.7%), The extract also exhibited significant and dose-dependent inhibitory effect on the increased vascular permeability induced by acetic acid. The extract presented antioxidant activity in both 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis 3-ethylbenzothiazoline 6-sulfonic acid tests and its total phenol content was 35.4 ± 0.06 mg GAE/g of extract. Also, the extract produced significant inhibition on nociception induced by acetic acid (ED50 : 8.7 mg/kg, i.p.) administered intraperitoneally and orally. Naloxone significantly prevented this activity.

  11. 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.

  12. 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.

  13. 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.

  14. 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.

  15. Anti-Inflammatory Oleanolic Triterpenes from Chinese Acorns

    Directory of Open Access Journals (Sweden)

    Jie Huang

    2016-05-01

    Full Text Available Acorns play an important role in human history and are a source of food and recipes for many cultures around the world. In this study, eleven oleanolic triterpenes, one of which was novel, were isolated from Chinese acorns (Quercus serrata var. brevipetiolata. The chemical structure of the novel triterpene, which was identified as 2α,3β,19α-trihydroxy-24-oxo-olean-12-en-28-oic acid (1, was established based on the interpretation of chemical and spectroscopic analyses, including IR, HR-ESI-MS, and NMR experiments (1H, 13C NMR, DEPT, 1H-1H COSY, HSQC, HMBC, and NOESY. All isolated compounds were tested for their inhibitory effects on LPS-induced nitric oxide (NO production in RAW 264.7 macrophages. Compared with the positive control drug indomethacin (IC50 = 47.4 μM, compounds 1, 3, 6 and 8 exhibited remarkable anti-inflammatory activities with IC50 values of 5.4, 7.8, 4.0 and 8.9 μM, respectively. Besides, compounds 2, 4, 7 and 9 also showed moderate anti-inflammatory activities with IC50 values of 10.1, 13.0, 20.1 and 17.2 μM, respectively. Furthermore, Compound 1 could inhibit TNF-α-induced IL-6 and IL-8 production in MH7A cells.

  16. Antioxidant activity of anti-inflammatory plant extracts.

    Science.gov (United States)

    Schinella, G R; Tournier, H A; Prieto, J M; Mordujovich de Buschiazzo, P; Ríos, J L

    2002-01-18

    The antioxidant properties of twenty medical herbs used in the traditional Mediterranean and Chinese medicine were studied. Extracts from Forsythia suspensa, Helichrysum italicum, Scrophularia auriculata, Inula viscosa, Coptis chinensis, Poria cocos and Scutellaria baicalensis had previously shown anti-inflammatory activity in different experimental models. Using free radical-generating systems H. italicum. I. viscosa and F. suspensa protected against enzymatic and non-enzymatic lipid peroxidation in model membranes and also showed scavenging property on the superoxide radical. All extracts were assayed at a concentration of 100 microg/ml. Most of the extracts were weak scavengers of the hydroxyl radical and C. chinensis and P. cocos exhibited the highest scavenging activity. Although S. baicalensis inhibited the lipid peroxidation in rat liver microsomes and red blood cells, the extract showed inhibitory actions on aminopyrine N-demethylase and xanthine oxidase activities as well as an pro-oxidant effect observed in the Fe3+-EDTA-H2O2 system. The results of the present work suggest that the anti-inflammatory activities of the same extracts could be explained, at least in part, by their antioxidant properties.

  17. Anticancer and anti-inflammatory activities of some dietary cucurbits.

    Science.gov (United States)

    Sharma, Dhara; Rawat, Indu; Goel, H C

    2015-04-01

    In this study, we investigated few dietary cucurbits for anticancer activity by monitoring cytotoxic (MTT and LDH assays), apoptotic (caspase-3 and annexin-V assays), and also their anti-inflammatory effects by IL-8 cytokine assay. Aqua-alcoholic (50:50) whole extracts of cucurbits [Lagenaria siceraria (Ls), Luffa cylindrica (Lc) and Cucurbita pepo (Cp)] were evaluated in colon cancer cells (HT-29 and HCT-15) and were compared with isolated biomolecule, cucurbitacin-B (Cbit-B). MTT and LDH assays revealed that the cucurbit extracts and Cbit-B, in a concentration dependent manner, decreased the viability of HT-29 and HCT-15 cells substantially. The viability of lymphocytes was, however, only marginally decreased, yielding a potential advantage over the tumor cells. Caspase-3 assay revealed maximum apoptosis with Ls while annexin V assay demonstrated maximum efficacy of Lc in this context. These cucurbits have also shown decreased secretion of IL-8, thereby revealing their anti-inflammatory capability. The results have demonstrated the therapeutic potential of dietary cucurbits in inhibiting cancer and inflammatory cytokine.

  18. 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.

  19. 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

  20. Degradable magnesium-based implant materials with anti-inflammatory activity.

    Science.gov (United States)

    Peng, Qiuming; Li, Kun; Han, Zengsheng; Wang, Erde; Xu, Zhigang; Liu, Riping; Tian, Yongjun

    2013-07-01

    The objective of this study was to prepare a new biodegradable Mg-based biomaterial, which provides good mechanical integrity in combination with anti-inflammatory function during the degradation process. The silver element was used, because it improved the mechanical properties as an effective grain refiner and it is also treated as a potential anti-inflammatory core. The new degradable Mg-Zn-Ag biomaterial was prepared by zone solidification technology and extrusion. The mechanical properties were mostly enhanced by fine grain strengthening. In addition, the alloys exhibited good cytocompatibility. The anti-inflammatory function of degradation products was identified by both interleukin-1α and nitric oxide modes. The anti-inflammatory impact was significantly associated with the concentration of silver ion. It was demonstrated that Mg-Zn-Ag system was a potential metallic stent with anti-inflammatory function, which can reduce the long-term dependence of anti-inflammatory drug after coronary stent implantation.

  1. Topical anti-inflammatory activity of pinda thailam, a herbal gel formulation.

    Science.gov (United States)

    Periyanayagam, K; Venkatarathnakumar, T; Nagaveni, A; Subitha, V G; Sundari, P; Vaijorohini, M; Umamaheswari, V

    2004-07-01

    The present study aims to evaluate the topical anti-inflammatory activity of "Pinda thailam", a herbal gel formulation containing aqueous extract of roots of Rubia cordifolia (Rubiaceae) and Hemidesmus indicus (Asclepiadaceae) which are known for their anti-inflammatory activity using the technique of carrageenin induced paw oedema in albino rats. The herbal gel formulation showed significant anti-inflammatory activity comparable to the reference standard Diclofenac sodium gel.

  2. Physalins with anti-inflammatory activity are present in Physalis alkekengi var. franchetii and can function as Michael reaction acceptors.

    Science.gov (United States)

    Ji, Long; Yuan, Yonglei; Luo, Liping; Chen, Zhe; Ma, Xiaoqiong; Ma, Zhongjun; Cheng, Lin

    2012-04-01

    Michael reaction acceptors (MRAs) are a class of active molecules that are directly or indirectly involved in various cellular processes, including the regulation of many signaling pathways. In this study, the inducible nitric oxide synthase (iNOS) assay was used to demonstrate that the dichloromethane extract of Physalis alkekengi var. franchetii (DCEP) possesses anti-inflammatory activity that might be attributed to the modification of key cysteine residues in IKKβ by the MRAs in DCEP. To isolate these MRAs, glutathione (GSH) was employed, and a simple ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) screening method was developed to investigate the GSH conjugates with potential MRAs. Five physalins, including one new compound isophysalin A (2), together with four known steroidal compounds, physalin A (1), physalin O (3), physalin L (4) and physalin G (5), were isolated to evaluate the GSH conjugating abilities, and it was indicated that compounds 1, 2 and 3, which had a common α,β-unsaturated ketone moiety, exhibited conjugating abilities with GSH and also showed significant nitric oxide (NO) production inhibiting activities. The anti-inflammatory activities of compounds 1, 2 and 3 might be attributed to their targeting multiple cysteine residues on IKKβ; therefore, the alkylation of IKKβ by compound 1 was further studied by micrOTOF-MS. The result showed that six cysteine residues (C(59), C(179), C(299), C(370), C(412), and C(618)) were alkylated, which indicated that IKKβ is a potential target for the anti-inflammatory activity of physalin A.

  3. Green synthesis and anti-inflammatory studies of a series of 1,1-bis(heteroaryl)alkane derivatives.

    Science.gov (United States)

    Jaratjaroonphong, Jaray; Tuengpanya, Surisa; Saeeng, Rungnapha; Udompong, Sarinporn; Srisook, Klaokwan

    2014-08-18

    Molecular iodine has been used as an efficient catalyst for a double Friedel-Crafts reaction of various heteroarenes, i.e. 2-methylfuran, 2-ethylfuran, 2-methylthiophene, pyrrole, N-methylpyrrole and indole, using aldehydes as alkylating agents under "open-flask" conditions with toluene or water as the reaction media. In the presence of 10 mol% iodine in toluene at room temperature, both aliphatic and aromatic aldehydes reacted smoothly to give the corresponding bis(heteroaryl)alkanes in good to excellent yields. Interestingly, with water as the solvent, the bis(heteroaryl)alkane adducts were obtained in moderate to good yields. The use of mild reaction conditions, low catalyst loadings, and eco-friendly reagents in a single step synthesis are the advantages of the present procedure. In an effort to discover novel non-steroidal anti-inflammatory agents, the synthesized bis(heteroaryl)alkanes were evaluated for the anti-inflammatory activity in the lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage model. These compounds (50 μM) significantly inhibited NO production and did not exhibit significant cytotoxic effects on macrophage cells. Among them, bis[(5-methyl)2-furyl](4-nitrophenyl) methane exhibited the most potent inhibition of NO with IC50 value of 42.4 ± 1.9, which is similar to that of the positive control, aminoguanidine (43.3 ± 2.5 μM). Thus, the bis[(5-methyl)2-furyl](4-nitrophenyl) methane could be considered a lead compound for the development of novel anti-inflammatory agents.

  4. Biogenic guaianolide-type sesquiterpene lactones with antioxidative and anti-inflammatory properties from natural mangrove hybrid Rhizophora annamalayana.

    Science.gov (United States)

    Raola, Vamshi Krishna; Chakraborty, Kajal

    2017-02-24

    Previously undescribed guaianolide-type sesquiterpene lactones were isolated from the chloroform fraction of the natural hybrid mangrove Rhizophora annamalayana, and were characterised as (Z)-3α,4,5,6-tetrahydro-5α-isobutyl-2β-(methoxymethyl)-7-methyl-3H-cyclohepta[b]carbolactone (1) and (7Z)-isopentyl 3α,4,5,6,7,8-hexahydro-2β-((E)-11-methylbut-10-enyl)-1-oxo-2H-cyclohepta[b]furan-6-carboxylate (2). Compound 2 displayed greater antioxidative activities {1, 1-diphenyl-2-picrylhydrazyl (DPPH) and 2, 2'-azino-bis-3 ethylbenzothiozoline-6-sulphonic acid diammonium salt (ABTS), IC50 0.65 and 0.62 mg/mL, respectively)} compared to 1 (IC50 0.83 and 1.14 mg/mL, respectively) (p < 0.05). Compound 2 recorded no significant difference in DPPH(.) scavenging activities (IC50 0.65 mg/mL) compared to α-tocopherol (IC50 0.63 mg/mL). Pro-inflammatory 5-lipoxygenase inhibitory activity of 2 was found to be comparable (IC50 0.98 mg/mL) to that displayed by synthetic anti-inflammatory drug ibuprofen (IC50 0.93 mg/mL). Compound 2 showed significantly greater selectivity index (anti-cyclooxygenase-1/anti-cyclooxygenase-2 = 2.15) than non-steroidal anti-inflammatory ibuprofen (<0.5) (p < 0.05), and therefore, might be used as selective cyclooxygenase-2 inhibitor. The hitherto undescribed guaianolide lactones might be used as potential anti-inflammatory and antioxidative pharmacophore leads.

  5. 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.

  6. 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.

  7. Anti-inflammatory and antioxidant effects of Croton celtidifolius bark.

    Science.gov (United States)

    Nardi, G M; Felippi, R; DalBó, S; Siqueira-Junior, J M; Arruda, D C; Delle Monache, F; Timbola, A K; Pizzolatti, M G; Ckless, K; Ribeiro-do-valle, R M

    2003-03-01

    Croton celtidifolius Baill commonly known as "sangue-de-adave" is a tree found in the Atlantic Forest of south of Brazil, mainly in Santa Catarina. The bark and leaf infusions of this medicinal plant have been popularly used for the treatment of inflammatory diseases. In this study we evaluated the anti-inflammatory and antioxidant properties of crude extract (CE), aqueous fraction (AqF), ethyl acetate fraction (EAF), butanolic fraction (BuF) and catechin, gallocatechin and sub-fractions, 19SF, 35SF and 63SF that contained a mixture of proanthocyanidins and were derived from the EAF fraction. The CE, AqF, EAF, BuF, catechin and sub-fractions 35SF and 63SF reduced paw edema induced by carrageenan. The CE, fractions, sub-fractions and isolated compounds showed antioxidant properties in vitro, all were able to scavenge superoxide anions at a concentration of 100 microg ml(-1). The EAF, catechin and gallocatechin were most effective in the deoxyribose assay, IC50 0.69 (0.44-1.06), 0.20 (0.11-0.39), 0.55 (0.28-1.08) microg x ml(-1) respectively. The CE and other fractions and sub-fractions inhibited deoxyribose degradation up to 1 microg x ml(-1). In the hydrophobic system only AqF did not show lipid peroxidation inhibition. The CE, other fractions, sub-fractions and isolated compounds inhibited lipidid peroxidation only at a concentration of 100 microg x ml(-1). In summary, this study demonstrates that Croton celtidifolius bark has significant anti-inflammatory and antioxidant activity.

  8. 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.

  9. Evaluation of Anti-Inflammatory Drug-Conjugated Silicon Quantum Dots: Their Cytotoxicity and Biological Effect

    Directory of Open Access Journals (Sweden)

    Kenji Yamamoto

    2013-01-01

    Full Text Available Silicon quantum dots (Si-QDs have great potential for biomedical applications, including their use as biological fluorescent markers and carriers for drug delivery systems. Biologically inert Si-QDs are less toxic than conventional cadmium-based QDs, and can modify the surface of the Si-QD with covalent bond. We synthesized water-soluble alminoprofen-conjugated Si-QDs (Ap-Si. Alminoprofen is a non-steroid anti-inflammatory drug (NSAID used as an analgesic for rheumatism. Our results showed that the “silicon drug” is less toxic than the control Si-QD and the original drug. These phenomena indicate that the condensed surface integration of ligand/receptor-type drugs might reduce the adverse interaction between the cells and drug molecules. In addition, the medicinal effect of the Si-QDs (i.e., the inhibition of COX-2 enzyme was maintained compared to that of the original drug. The same drug effect is related to the integration ratio of original drugs, which might control the binding interaction between COX-2 and the silicon drug. We conclude that drug conjugation with biocompatible Si-QDs is a potential method for functional pharmaceutical drug development.

  10. 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.

  11. 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.

  12. Purification and properties of a 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol and its inhibition by anti-inflammatory drugs.

    Science.gov (United States)

    Penning, T M; Mukharji, I; Barrows, S; Talalay, P

    1984-01-01

    An NAD(P)-dependent 3 alpha-hydroxysteroid dehydrogenase (EC 1.1.1.50) was purified to homogeneity from rat liver cytosol, where it is responsible for most if not all of the capacity for the oxidation of androsterone, 1-acenaphthenol and benzenedihydrodiol (trans-1,2-dihydroxycyclohexa-3,5-diene). The dehydrogenase has many properties (substrate specificity, pI, Mr, amino acid composition) in common with the dihydrodiol dehydrogenase (EC 1.3.1.20) purified from the same source [Vogel, Bentley, Platt & Oesch (1980) J. Biol. Chem. 255, 9621-9625]. Since 3 alpha-hydroxysteroids are by far the most efficient substrates, the enzyme is more appropriately designated a 3 alpha-hydroxysteroid dehydrogenase. It also promotes the NAD(P)H-dependent reductions of quinones (e.g. 9,10-phenanthrenequinone, 1,4-benzoquinone), aromatic aldehydes (4-nitrobenzaldehyde) and aromatic ketones (4-nitroacetophenone). The dehydrogenase is not inhibited by dicoumarol, disulfiram, hexobarbital or pyrazole. The mechanism of the powerful inhibition of this enzyme by both non-steroidal and steroidal anti-inflammatory drugs [Penning & Talalay (1983) Proc. Natl. Acad. Sci. U.S.A. 80, 4504-4508] was examined with several substrates. Most non-steroidal anti-inflammatory drugs are competitive inhibitors (e.g. Ki for indomethacin, 0.20 microM for 9,10-phenanthrenequinone reduction at pH 6.0, and 0.835 microM for androsterone oxidation at pH 7.0), except for salicylates, which act non-competitively (e.g. Ki for aspirin, 650 microM for androsterone oxidation). The inhibitory potency of these agents falls sharply as the pH is increased from 6 to 9. Most anti-inflammatory steroids are likewise competitive inhibitors, except for the most potent (betamethasone and dexamethasone), which act non-competitively. The enzyme is inhibited competitively by arachidonic acid and various prostaglandins. PMID:6435601

  13. Fatores associados ao uso de antiinflamatórios não esteróides em população de funcionários de uma universidade no Rio de Janeiro: Estudo Pró-Saúde Factors associated with the use of non-steroidal anti-inflammatory drugs in a population of a university in Rio de Janeiro: "Pró-Saúde" Study

    Directory of Open Access Journals (Sweden)

    Tatiana Chama Borges Luz

    2006-12-01

    Full Text Available Os Antiinflamatórios Não-Esteróides (AINE estão entre os medicamentos mais utilizados no mundo. Estima-se que mais de 30 milhões de pessoas tomem AINE diariamente, apesar de sua toxicidade e de seus efeitos adversos, principalmente gastrointestinais. O presente trabalho utilizou dados seccionais da Fase 1 (1999 de um estudo de coorte (Estudo Pró-Saúde coletados entre 4.030 funcionários técnico-administrativos de uma universidade no Rio de Janeiro, nos quais foram aplicados questionários autopreenchíveis. Nesse estudo, os AINE apareceram entre os principais produtos consumidos nas duas semanas que antecederam à pesquisa, com prevalência de 7%. Verificou-se que as mulheres têm maior chance de serem usuárias (OR = 2,11; IC 95%: 1,59 - 2,79. Os dados foram submetidos a análise multivariada, tendo sido propostos modelos logísticos por sexo. A carga horária trabalhada na semana foi um importante preditor do uso de AINE (OR = 1,03; IC 95%: 1,01 - 1,04, para homens, e OR = 1,02; IC 95%: 1,00 - 1,03, para mulheres. Dor incapacitante e artrose também se mostraram relevantes, com OR = 2,89 (IC 95%: 1,77 - 4,71 e OR = 2,29 (IC 95%: 1,10 - 4,75, respectivamente, para os homens, e OR = 2,65 (IC 95%: 1,89 - 3,70 e OR = 2,00 (IC 95%: 1,37 - 2,93, respectivamente, para as mulheres. Outros preditores importantes foram a hérnia de disco (OR = 2,27; IC 95%: 0,93 - 5,54 para os homens, e LER (OR = 1,64; IC 95%: 1,15 - 2,35, cálculos vesical (OR = 1,85; IC 95%: 1,00 - 3,45 e renal (OR = 1,81; IC 95%: 1,12 - 2,91 para as mulheres. Mulheres e indivíduos com maior carga horária de trabalho semanal constituem grupos mais vulneráveis, em termos de uso irracional, e, portanto, mais sujeitos a programas de intervenção. Os resultados apontam para a importância das condições de trabalho no processo de desencadeamento de doenças.Non-steroidal Anti-inflammatory Drugs (NSAIDs are some of the most widely used drugs worldwide. It is estimated that

  14. 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.

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

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    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.

  16. 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

  17. Chemical composition and anti-inflammatory activity of the leaves of Byrsonima verbascifolia

    NARCIS (Netherlands)

    Saldanha, Aline Aparecida; Carmo, Do Lucas Fernandes; Nascimento, Do Sara Batista; Matos, de Natália Alves; Carvalho Veloso, de Clarice; Castro, Ana Hortência Fonsêca; Vos, de Ric C.H.; Klein, André; Siqueira, de João Máximo; Carollo, Carlos Alexandre; Nascimento, Do Thalita Vieira; Toffoli-Kadri, Mônica Cristina; Soares, Adriana Cristina

    2016-01-01

    An ethnopharmacological survey indicates that the genus Byrsonima has some medicinal species that are commonly found in the Brazilian Cerrado and has been used as an anti-inflammatory and for gastroduodenal disorders. The aim of this study was to evaluate the anti-inflammatory and antioxidant act

  18. 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

  19. 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....

  20. 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.

  1. 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.

  2. 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...

  3. 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

  4. Invited review: The anti-inflammatory properties of dairy lipids.

    Science.gov (United States)

    Lordan, R; Zabetakis, I

    2017-03-22

    Dairy product consumption is often associated with negative effects because of its naturally high levels of saturated fatty acids. However, recent research has shown that dairy lipids possess putative bioactivity against chronic inflammation. Inflammation triggers the onset of several chronic diseases, including cardiovascular disease, type 2 diabetes mellitus, obesity, and cancer. This review discusses the anti-inflammatory properties of dairy lipids found in milk, yogurt, and cheese, and it examines them in relation to their implications for human health: their protective effects and their role in pathology. We also consider the effect of lipid profile alteration in dairy products-by using ruminant dietary strategies to enrich the milk, or by lipid fortification in the products. We critically review the in vivo, in vitro, ex vivo, and epidemiological studies associated with these dairy lipids and their role in various inflammatory conditions. Finally, we discuss some suggestions for future research in the study of bioactive lipids and dairy products, with reference to the novel field of metabolomics and epidemiological studies.

  5. 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.

  6. Anti-inflammatory polysaccharides of Azadirachta indica seed tegument

    Directory of Open Access Journals (Sweden)

    Lívia de Paulo Pereira

    2012-06-01

    Full Text Available Azadirachta indica A. Juss., Meliaceae, or Indian neem is a plant used to treat inûammatory disorders. Total polysaccharide (TPL and FI (fractioned by ion exchange chromatography from the seed tegument of A. indica were evaluated in models of acute inflammation (paw edema/peritonitis using Wistar rats. Paw edema (measured by hydroplethysmometry was induced s.c. by Λ-carrageenan (300 µg, histamine (100 µg, serotonin (20 µg, compound 48/80 (10 µg, prostaglandin (PGE2 30 µg or L-arginine (15 µg. Peritonitis (analyzed for leukocyte counts/protein dosage was induced i.p. by carrageenan (500 mg or N-formyl-methionyl-leucyl-phenylalanine (fMLP 50 ng. Animals were treated i.v. with TPL (1 mg/kg or FI (0.01, 0.1, 1 mg/kg 30 min before stimuli. FI toxicity (at 0.1 mg/kg, i.v. for seven days was analyzed by the variation of body/organ mass and hematological/biochemical parameters. TPL extraction yielded 1.3%; FI, presenting high carbohydrate and low protein content, at 0.1 mg/kg inhibited paw edema induced by carrageenan (77%, serotonin (54%, PGE2 (69% and nitric oxide (73%, and the peritonitis elicited by carrageenan (48% or fMLP (67%, being well tolerated by animals. FI exhibited potent anti-inflammatory activity, revealing to be important active component in traditionally prepared remedies to treat inflammatory states.

  7. Modification of palm oil for anti-inflammatory nutraceutical properties.

    Science.gov (United States)

    Zainal, Zaida; Longman, Andrea J; Hurst, Samantha; Duggan, Katrina; Hughes, Clare E; Caterson, Bruce; Harwood, John L

    2009-07-01

    Palm oil is one of the most important edible oils in the world. Its composition (rich in palmitate and oleate) make it suitable for general food uses but its utility could be increased if its fatty acid quality could be varied. In this study, we have modified a palm olein fraction by transesterification with the n-3 polyunsaturated fatty acids, alpha-linolenate or eicosapentaenoic acid (EPA). Evaluation of the potential nutritional efficacy of the oils was made using chondrocyte culture systems which can be used to mimic many of the degenerative and inflammatory pathways involved in arthritis. On stimulation of such cultures with interleukin-1alpha, they showed increased expression of cyclooxygenase-2, the inflammatory cytokines tumour necrosis factor-alpha (TNF-alpha), IL-1alpha and IL-1beta and the proteinase ADAMTS-4. This increased expression was not affected by challenge of the cultures with palm olein alone but showed concentration-dependent reduction by the modified oil in a manner similar to EPA. These results show clearly that it is possible to modify palm oil conveniently to produce a nutraceutical with effective anti-inflammatory properties.

  8. Chondroprotective and anti-inflammatory effects of sesamin.

    Science.gov (United States)

    Phitak, Thanyaluck; Pothacharoen, Peraphan; Settakorn, Jongkolnee; Poompimol, Wilart; Caterson, Bruce; Kongtawelert, Prachya

    2012-08-01

    Osteoarthritis (OA) is a major disability of elderly people. Sesamin is the main compound in Sesamun indicum Linn., and it has an anti-inflammatory effect by specifically inhibiting Δ5-desaturase in polyunsaturated fatty acid biosynthesis. The chondroprotective effects of sesamin were thus studied in a porcine cartilage explant induced with interleukin-1beta (IL-1β) and in a papain-induced osteoarthritis rat model. With the porcine cartilage explant, IL-1β induced release of sulfated-glycosaminoglycan (s-GAG) and hydroxyproline release, and this induction was significantly inhibited by sesamin. This ability to inhibit these processes might be due to its ability to decrease expression of MMP-1, -3 and -13, which can degrade both PGs and type II collagen, both at the mRNA and protein levels. Interestingly, activation of MMP-3 might also be inhibited by sesamin. Moreover, in human articular chondrocytes (HACs), some pathways of IL-1β signal transduction were inhibited by sesamin: p38 and JNK. In the papain-induced OA rat model, sesamin treatment reversed the following pathological changes in OA cartilage: reduced disorganization of chondrocytes in cartilage, increased cartilage thickness, and decreased type II collagen and PGs loss. Sesamin alone might increase formation of type II collagen and PGs in the cartilage tissue of control rats. These results demonstrate that sesamin efficiently suppressed the pathological processes in an OA model. Thus, sesamin could be a potential therapeutic strategy for treatment of OA.

  9. 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.

  10. Topical nonsteroidal anti-inflammatory drugs for osteoarthritis.

    Science.gov (United States)

    Barthel, H Richard; Axford-Gatley, Robert A

    2010-11-01

    Nonsteroidal anti-inflammatory drugs (NSAIDs) are mainstays of the treatment of osteoarthritis (OA) but have dose- and age-related risks of gastrointestinal, cardiovascular, and renal adverse events (AEs). As a result, US and international guidelines recommend caution when prescribing oral NSAIDs, particularly in older patients and those with significant comorbidities. For OA of the hands and knees, topical NSAIDs provide efficacy similar to oral NSAIDs, with far less systemic distribution. Treatment-related cardiovascular, renal, and other serious AEs with topical NSAIDs have not been reported. At present, only 2 topical NSAIDs are approved in the United States for the treatment of OA: diclofenac sodium 1% gel for hand or knee OA and diclofenac sodium 1.5% in 45.5% dimethylsulfoxide solution for knee OA. Clinical trial data for these products have demonstrated efficacy superior to placebo or similar to oral diclofenac with AE profiles similar to placebo, except for application site reactions. In large double-blind trials, gastrointestinal AEs were infrequent and did not include ulcers, perforations, or bleeding. The purpose of this brief review is to examine the data from controlled double-blind trials evaluating the use of topical NSAIDs in patients with OA. Articles included were identified via a search of PubMed covering the period from January 1, 2005 through March 31, 2010. Reference lists from OA treatment guidelines and meta-analyses were reviewed for additional citations of importance.

  11. 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

  12. 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.

  13. 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.

  14. 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.

  15. 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

  16. 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

  17. 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.

  18. Evaluation of anti-inflammatory, analgesic and antipyretic activities of Thymus serphyllum Linn. in mice.

    Science.gov (United States)

    Alamger; Mazhar, Uzma; Mushtaq, Muhammad Naveed; Khan, Hafeez Ullah; Maheen, Safirah; Malik, Muhammad Nasir Hayat; Ahmad, Taseer; Latif, Fouzia; Tabassum, Nazia; Khan, Abdul Qayyum; Ahsan, Haseeb; Khan, Wasim; Javed, Ibrahim; Ali, Haider

    2015-01-01

    The present study was conducted to evaluate the analgesic, anti-inflammatory and antipyretic activities of Thymus serphyllum Linn. in mice. Anti-inflammatory activity was evaluated by carrageenan and egg albumin induced paw edema in mice, while analgesic activity was assessed using formalin induced paw licking and acetic acid induced abdominal writhing in mice. For determination of antipyretic activity, pyrexia was induced by subcutaneous injection of 20% yeast. All the extracts produced significant anti-inflammatory effect however, ether extract produced maximum effect 34% inhibition (p Thymus serphyllum in traditional medicine for inflammation accompanied by pain and fever.

  19. 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.

  20. 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

  1. 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

  2. Characterics of exposure to non-steroid anti-inflammatory drugs in European databases.

    NARCIS (Netherlands)

    Vries, F. de; Kieler, H.; Dijk, L. van; Svensson, T.; Staa, T. van

    2010-01-01

    Background: A systematic review reported that users of naproxen, ibuprofen and piroxicam did not have an increased risk of myorcardial infarction (MI), whilst users of diclofenac and indomethacin showed significantly increased risk of MI (RRs 1.4 and 1.3). While there may be biological plausible exp

  3. 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

  4. Commentary on neostigmine interactions with non steroidal anti-inflammatory drugs by Miranda et al.

    Science.gov (United States)

    Tallarida, Ronald J

    2002-04-01

    The article by Miranda et al. presents data showing significant synergism between NEO and certain NSAIDs administered i.p. in the mouse. Their conclusions follow from isobolar analysis accompanied by statistical confidence limits that show significant differences between the additive (expected) and experimental potencies. This commentary discusses the features of the graphical method of analysis and points out other experimental designs and the methods used to analyse them.

  5. Commentary on Neostigmine Interactions with Non steroidal Anti-inflammatory Drugs by Miranda et al.

    OpenAIRE

    Tallarida, Ronald J.

    2002-01-01

    The article by Miranda et al. presents data showing significant synergism between NEO and certain NSAIDs administered i.p. in the mouse. Their conclusions follow from isobolar analysis accompanied by statistical confidence limits that show significant differences between the additive (expected) and experimental potencies. This commentary discusses the features of the graphical method of analysis and points out other experimental designs and the methods used to analyse them.

  6. Commentary on Neostigmine Interactions with Non steroidal Anti-inflammatory Drugs by Miranda et al.

    Science.gov (United States)

    Tallarida, Ronald J

    2002-01-01

    The article by Miranda et al. presents data showing significant synergism between NEO and certain NSAIDs administered i.p. in the mouse. Their conclusions follow from isobolar analysis accompanied by statistical confidence limits that show significant differences between the additive (expected) and experimental potencies. This commentary discusses the features of the graphical method of analysis and points out other experimental designs and the methods used to analyse them. PMID:11934797

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

    DEFF Research Database (Denmark)

    Klein, Mads; Gögenur, Ismail; Rosenberg, Jacob

    2012-01-01

    to achieve this, the following studies were performed. Study I was a retrospective, case-control study in 75 patients undergoing laparoscopic colorectal resection for colorectal cancer. 33 of these patients received the NSAID diclofenac in the postoperative period; the remaining 42 did not receive any NSAID....... 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...... for the subsequent studies. Study II was an experimental, randomized, case-control study in 32 Wistar rats. The rats had a colonic anastomosis performed and were randomized to diclofenac or placebo treatment. After three days, the rats were sacrificed and the anastomoses were harvested. First, the anastomotic...

  8. 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

    for the use of the two NSAIDs diclofenac and ibuprofen were recorded. The data from six colorectal departments in eastern Denmark were compared. RESULTS: Of the 2,754 patients analyzed overall, 40.6% received NSAIDs as part of their analgesic treatment. The percentage of the patients receiving NSAIDs......, receiving a pre-defined dosage as a minimum and receiving NSAIDs as p.r.n. medication, and the type of NSAID were significantly different both between department and within departments. The median dose of ibuprofen and diclofenac were 1200 mg (400-2,400 mg) and 100 mg (50-200 mg), respectively. CONCLUSIONS...

  9. Non-steroidal anti-inflammatory drug use and risk of endometrial cancer

    DEFF Research Database (Denmark)

    Verdoodt, Freija; Friis, Søren; Dehlendorff, Christian

    2016-01-01

    or non-aspirin (NA-) NSAIDs, we performed a systematic review and meta-analysis of observational studies. METHODS: We conducted a bibliographic database search in PubMed, Embase and Cochrane Library. Relative risk estimates were extracted from eligible case-control and cohort studies and pooled using...

  10. [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.

  11. Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.

    Science.gov (United States)

    Zughaier, Susu; Karna, Prasanthi; Stephens, David; Aneja, Ritu

    2010-02-11

    Noscapine, a plant-derived, non-toxic, over-the-counter antitussive alkaloid has tubulin-binding properties. Based upon the structural resemblance of noscapine to colchicine, a tubulin-binding anti-inflammatory drug, noscapine and its semi-synthetic brominated analogs were examined for in vitro anti-inflammatory activity. Brominated noscapine analogs were found to inhibit cytokine and chemokine release from macrophage cell lines but did not affect cell viability. Brominated noscapine analogs demonstrated anti-inflammatory properties in both TLR- and non-TLR induced in vitro innate immune pathway inflammation models, mimicking septic and sterile infection respectively. In addition, electron microscopy and immunoblotting data indicated that these analogs induced robust autophagy in human macrophages. This study is the first report to identify brominated noscapines as innate immune pathway anti-inflammatory molecules.

  12. Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.

    Directory of Open Access Journals (Sweden)

    Susu Zughaier

    Full Text Available Noscapine, a plant-derived, non-toxic, over-the-counter antitussive alkaloid has tubulin-binding properties. Based upon the structural resemblance of noscapine to colchicine, a tubulin-binding anti-inflammatory drug, noscapine and its semi-synthetic brominated analogs were examined for in vitro anti-inflammatory activity. Brominated noscapine analogs were found to inhibit cytokine and chemokine release from macrophage cell lines but did not affect cell viability. Brominated noscapine analogs demonstrated anti-inflammatory properties in both TLR- and non-TLR induced in vitro innate immune pathway inflammation models, mimicking septic and sterile infection respectively. In addition, electron microscopy and immunoblotting data indicated that these analogs induced robust autophagy in human macrophages. This study is the first report to identify brominated noscapines as innate immune pathway anti-inflammatory molecules.

  13. Isobolographic analysis of the antinociceptive interactions of clonidine with nonsteroidal anti-inflammatory drugs.

    Science.gov (United States)

    Miranda, H F; Pinardi, G

    2004-09-01

    The present study was undertaken to characterize the interactions between nonsteroidal anti-inflammatory drugs and the alpha(2)-adrenoceptor agonist clonidine in an acute nociceptive test. The writhing test was selected as a model of acute visceral pain. Isobolograms were constructed to assess the interactions of clonidine and each nonsteroidal anti-inflammatory drugs, when coadministered intraperitoneally and intrathecally (i.t.). The simultaneous intraperitoneal administration of fixed ratios of ED(50) fractions of all nonsteroidal anti-inflammatory drugs (naproxen, piroxicam, paracetamol, dipyrone or metamizol and nimesulide) combined with clonidine resulted in synergistic interactions. The same combinations administered intrathecally were additive. The synergistic interactions between systemic nonsteroidal anti-inflammatory drugs and clonidine may involve supraspinal mechanisms.

  14. 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.

  15. 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.

  16. 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...

  17. Effect of Anti-inflammatory Treatment on Depression, Depressive Symptoms, and Adverse Effects

    DEFF Research Database (Denmark)

    Köhler, Karl Ole; Benros, Michael E; Nordentoft, Merete

    2014-01-01

    adverse effects of anti-inflammatory interventions. DATA SOURCES: Trials published prior to December, 31, 2013, were identified searching Cochrane Central Register of Controlled Trials, PubMed, EMBASE, PsychINFO, Clinicaltrials.gov, and relevant review articles. STUDY SELECTION: Randomized placebo......-controlled trials assessing the efficacy and adverse effects of pharmacologic anti-inflammatory treatment in adults with depressive symptoms, including those who fulfilled the criteria for depression. DATA EXTRACTION AND SYNTHESIS: Data were extracted by 2 independent reviewers. Pooled standard mean difference (SMD......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...

  18. 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.

  19. The antioxidant properties of salicylate derivatives: A possible new mechanism of anti-inflammatory activity.

    Science.gov (United States)

    Borges, Rosivaldo S; Castle, Steven L

    2015-11-01

    The synthesis and antioxidant evaluation by DPPH scavenging of a series of salicylic acid derivatives is described. Gentisic acid and its ester, amide, and amino analogs possess more radical scavenging capacity than salicylic acid and other salicylate derivatives. This property can possibly provide an additional pathway for anti-inflammatory activity through either single electron or hydrogen atom transfer, leading to a new strategy for the design of anti-inflammatory agents.

  20. Preliminary evaluation of the analgesic and anti-inflammatory effects of Tacca integrifolia in rodents

    Directory of Open Access Journals (Sweden)

    Thatree Autsavakitipong

    2015-01-01

    Full Text Available Summary. This is a preliminary investigation of the ethyl acetate extract of the leaf of Tacca integrifolia (TIE for the analgesic activity using writhing response in mice, tail flick test in rats and for anti-inflammatory activity using ethyl phenyl propiolate (EPP-induced ear edema, carrageenan- and arachidonic acid-induced hind paw edema, as well as cotton pellet-induced granuloma formation in rats. The results showed that TIE (200 mg/kg, PO significantly inhibited pain caused by acetic acid injection (65.9% but did not exhibit effect in tail flick test in rats. These findings suggest that analgesic mechanism of TIE may act via peripherally pathway. The study of anti-inflammatory effect showed that TIE significantly inhibited ear edema induced by EPP. TIE (200 mg/kg, PO inhibited paw edema induced by carrageenan (55.5% and arachidonic acid (48.6% but had no effect on cotton-induced granuloma formation in rats. In conclusion, the ethyl acetate extract of leaf of T. integrifolia possessed anti-inflammatory activity in acute inflammation and analgesic activity.Industrial relevant. Plants of the genus Tacca have been reported to possess many activities such as analgesic, anti-inflammatory and, antipyretic activities. Many species have been used to treat high blood pressure, burn, gastric ulcer, and hepatitis. The scientific studies supporting the traditional uses of Tacca integrifolia for some of the alleged activities are still lacking. The screening test for analgesic and anti-inflammatory effect of the ethyl acetate extract of the leaf of Tacca integrifolia provides scientific data to confirm the potentials of T. integrifolia as an analgesic and anti-inflammatory medicinal plant. In addition, the outcomes may be useful to develop a new analgesic and anti-inflammatory drug in the future. Key words. Tacca integrifolia; Taccaceae; ethyl acetate extract; analgesic activity; anti-inflammatory activity

  1. Immune-stimulatory and anti-inflammatory activities of Curcuma longa extract and its polysaccharide fraction

    OpenAIRE

    Chandrasekaran, Chinampudur V.; Kannan Sundarajan; Edwin, Jothie R.; Giligar M Gururaja; Deepak Mundkinajeddu; Amit Agarwal

    2013-01-01

    Background: While curcuminoids have been reported to possess diverse biological activities, the anti-inflammatory activity of polar extracts (devoid of curcuminoids) of Curcuma longa (C. longa) has seldom been studied. In this study, we have investigated immune-stimulatory and anti-inflammatory activities of an aqueous based extract of C. longa (NR-INF-02) and its fractions in presence and absence of mitogens. Materials and Methods: Effects of NR-INF-02 (Turmacin TM , Natural Remedies Pvt. Lt...

  2. Anti Bacterial and Anti Inflammatory efficacy of Zingiber officinale and Decalepis hamiltonii ? In Vitro Study

    OpenAIRE

    Arun kumar M; Tejaswi B; Susila V Anand

    2014-01-01

    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: Ethano...

  3. Anti-inflammatory effect of the sclerotium of Lignosus rhinocerotis (Cooke) Ryvarden, the Tiger Milk mushroom

    OpenAIRE

    Lee, Sook Shien; Tan, Nget Hong; Fung, Shin Yee; Sim, Si Mui; Tan, Chon Seng; Ng, Szu Ting

    2014-01-01

    Background The sclerotium of Lignosus rhinocerotis (Cooke) Ryvarden (Tiger Milk mushroom) is used as a traditional medicine to relieve cough, asthma and chronic hepatitis. The traditional uses of the sclerotium are presumably related to its anti-inflammatory effect. The present study was carried out to evaluate the anti-inflammatory activity of the sclerotial powder of L. rhinocerotis (Cooke) Ryvarden (Tiger Milk mushroom) cultivar TM02. Methods The anti-acute inflammatory activity of the scl...

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

    OpenAIRE

    Jaime Tortoriello; Maribel Herrera-Ruiz; Manases Gonzalez-Cortazar; Alejandro Zamilpa; Antonio R. Jiménez-Aparicio; Enrique Jiménez-Ferrer; Martha L. Arenas Ocampo; Nayeli Monterrosas-Brisson

    2013-01-01

    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 ede...

  5. DIURETIC AND ANTI-INFLAMMATORY ACTIVITY OF AQUEOUS EXTRACT OF AERVA SANGUINOLENTA (L.) BLUME

    OpenAIRE

    Srinivas Reddy K; Rajeev Reddy E; Ganapaty S

    2011-01-01

    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 sho...

  6. Antibacterial and Anti-Inflammatory Activities of Physalis Alkekengi var. franchetii and Its Main Constituents

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    Zunpeng Shu

    2016-01-01

    Full Text Available This study was designed to determine whether the 50% EtOH fraction from AB-8 macroporous resin fractionation of a 70% EtOH extract of P. Alkekengi (50-EFP has antibacterial and/or anti-inflammatory activity both in vivo and in vitro and to investigate the mechanism of 50-EFP anti-inflammatory activity. Additionally, this study sought to define the chemical composition of 50-EFP. Results indicated that 50-EFP showed significant antibacterial activity in vitro and efficacy in vivo. Moreover, 50-EFP significantly reduced nitric oxide (NO, prostaglandin E2 (PGE2, tumor necrosis factor alpha (TNF-α, interleukin 1 (IL-1, and interleukin 6 (IL-6 production in lipopolysaccharide- (LPS- stimulated THP-1 cells. Nitric oxide synthase (iNOS and cyclooxygenase-2 (COX-2 (examined at the protein level in THP-1 cells were suppressed by 50-EFP, which inhibited nuclear translocation of p65. Consistent with this anti-inflammatory activity in vitro, 50-EFP reduced inflammation in both animal models. Finally, seventeen compounds (8 physalins and 9 flavones were isolated as major components of 50-EFP. Our data demonstrate that 50-EFP has antibacterial and anti-inflammatory activities both in vitro and in vivo. The anti-inflammatory effect appears to occur, at least in part, through the inhibition of nuclear translocation of p65. Moreover, physalins and flavones are probably the active components in 50-EFP that exert antibacterial and anti-inflammatory activities.

  7. 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

  8. 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.

  9. Antimicrobial, Antiparasitic, Anti-Inflammatory, and Cytotoxic Activities of Lopezia racemosa

    Science.gov (United States)

    Cruz Paredes, Carla; Bolívar Balbás, Paulina; Juárez, Zaida Nelly; Sánchez Arreola, Eugenio; Hernández, Luis Ricardo

    2013-01-01

    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. PMID:23843731

  10. Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs.

    Science.gov (United States)

    Theoduloz, Cristina; Delporte, Carla; Valenzuela-Barra, Gabriela; Silva, Ximena; Cádiz, Solange; Bustamante, Fernanda; Pertino, Mariano Walter; Schmeda-Hirschmann, Guillermo

    2015-06-18

    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.

  11. Effect of new hybrids based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug on the growth of a human astrocytoma cell line (U373).

    Science.gov (United States)

    Garrido, Mariana; González-Arenas, Aliesha; Camacho-Arroyo, Ignacio; Cabeza, Marisa; Alcaraz, Belén; Bratoeff, Eugene

    2015-03-26

    In spite of the fact that anaplastic astrocytoma is an uncommon disease, very often the pathology of this disease is associated with lethal effects due to the late diagnosis and unspecific treatments. This paper reports the synthesis and the biological effect on the growth of U373 cell line (human anaplastic astrocytoma) of new hybrid compounds based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug (6a-e). Moreover, we also determined the cell growth effect of five non-steroidal anti-inflammatory drugs (naproxen, ibuprofen, ketoprofen, indomethacin and sulindac) as well as the free steroidal alcohol 5. The results from this study indicated that sulindac as well as compound 5 decreased the number of U373 cells at different concentrations. However, when an anti-inflammatory drug was bound to the steroidal structure (5), the resulting compounds (6a-e) showed an enhanced biological effect with exception of hybrid 6c. Furthermore, derivative 6e (sulindac hybrid) did not allow cell growth during six days of experiment at a concentration of 10 μM. The overall data indicated that these molecules showed an anti-proliferative activity on anaplastic astrocytoma cell line.

  12. Influence of He-Ne laser therapy on the dynamics of wound healing in mice treated with anti-inflammatory drugs

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    W.L.S. Gonçalves

    2007-06-01

    Full Text Available We determined the effects of helium-neon (He-Ne laser irradiation on wound healing dynamics in mice treated with steroidal and non-steroidal anti-inflammatory agents. Male albino mice, 28-32 g, were randomized into 6 groups of 6 animals each: control (C, He-Ne laser (L, dexamethasone (D, D + L, celecoxib (X, and X + L. D and X were injected im at doses of 5 and 22 mg/kg, respectively, 24 h before the experiment. A 1-cm long surgical wound was made with a scalpel on the abdomens of the mice. Animals from groups L, D + L and X + L were exposed to 4 J (cm²-1 day-1 of He-Ne laser for 12 s and were sacrificed on days 1, 2, or 3 after the procedure, when skin samples were taken for histological examination. A significant increase of collagen synthesis was observed in group L compared with C (168 ± 20 vs 63 ± 8 mm². The basal cellularity values on day 1 were: C = 763 ± 47, L = 1116 ± 85, D = 376 ± 24, D + L = 698 ± 31, X = 453 ± 29, X + L = 639 ± 32 U/mm². These data show that application of L increases while D and X decrease the inflammatory cellularity compared with C. They also show that L restores the diminished cellularity induced by the anti-inflammatory drugs. We suggest that He-Ne laser promotes collagen formation and restores the baseline cellularity after pharmacological inhibition, indicating new perspectives for laser therapy aiming to increase the healing process when anti-inflammatory drugs are used.

  13. Pharmacoutilization of anti-inflammatory and gastroprotective drugs in patients with osteoarthritis: comparison between COXIBs and conventional NSAIDs by using administrative records

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    Luca Degli Esposti

    2006-12-01

    Full Text Available The aim of the study was to analyze anti-inflammatory and gastroprotective drug utilization in patients with osteoarthritis comparing conventional non-steroidal anti-inflammatory drugs (NSAIDs versus cyclo-oxygenase 2 (COX 2 inhibitors. A retrospective observational cohort study was conducted and health-assisted subjects from the Local Health Units of Turin and Caserta were enrolled. Data linkage techniques were used to cross demographical, pharmaceutical and nosological databases. All subjects aged ≥18 years who were hospitalized for osteoarthritis from July 1st 2002 to June 30th 2004 were enrolled in the study. Concurrent prescriptions of non-steroidal anti-inflammatory and gastroprotective drugs were considered. Other demographic and clinical characteristics were recorded. A total of 1,002 subjects with a diagnosis of osteoarthritis treated with NSAIDs were enrolled. Of these subjects, 438 patients were treated with non selective NSAIDs (80.8%, 104 with COXIBs (19.2% and 460 with multiple therapy. There were no significant differences between the demographic and clinical characteristics of the three groups. Gastroprotective drugs were prescribed in 37.0% and 35.6% of subjects treated with NSAIDs and COXIBs, respectively. Gastroprotective drug prescriptions increased from the index date to the follow-up period (from 20.4% to 41.1% of subjects treated with NSAIDs. In high-risk subjects with gastrointestinal events, gastroprotective drug utilization was undersized and increased from the index date to the follow up period (from 19.4% to 40.8% of high-risk subjects. Evidence from this study indicated that non selective NSAIDs and COXIBs are used indiscriminately with respect to patient characteristics and gastroprotection.

  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. 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.

  16. Anti-inflammatory and antinociceptive activities of methanolic extract from red seaweed Dichotomaria obtusata

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    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

  17. 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.

  18. Anti-inflammatory activity of the methanolic extracts of leaves and stems from Tabebuia hypoleuca (C. Wright Urb.

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    Ada I. Regalado

    2015-10-01

    Full Text Available Context: There are reports in the literature of species belonging to the genus Tabebuia with pharmacological potential as anti-inflammatory: Tabebuia avellanedae, Tabebuia chrysanta, Tabebuia rosea, Tabebuia ochracea, among others; however, about of the species Tabebuia hypoleuca no studies demonstrating this activity so far. Aims: To determine the anti-inflammatory activity in the acute phase of the methanolic extracts of T. hypoleuca. Methods: Leaves and stems of T. hypoleuca were collected. The anti-inflammatory activity was assessed using the carrageenin-induced paw edema models and the croton oil induced auricular edema in mice. The qualitative identification of secondary metabolites present in the methanolic extracts was performed by a preliminary phytochemical screening. Results: The anti-inflammatory activity assessments showed that methanol extract of the leaves do not have anti-inflammatory activity at doses tested, while the methanol extract of the stems at the dose of 500 mg/kg showed a significant anti-inflammatory activity in the model of carrageenan-induced paw edema. In the model of croton oil induced auricular edema the methanol extract of the stems administered orally and intraperitoneally showed a significant anti-inflammatory activity at all doses tested. The anti-inflammatory activity found could be due to the presence of metabolites such as tannins, phenols and alkaloids. Conclusions: These studies demonstrate the anti-inflammatory activity of the methanol extract of the stems of Tabebuia hypoleuca, and constitute the first report about this species as anti-inflammatory.

  19. 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.

  20. 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.

  1. Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.

    Science.gov (United States)

    El-Nezhawy, Ahmed O H; Biuomy, Ayman R; Hassan, Fatma S; Ismaiel, Ayman K; Omar, Hany A

    2013-04-01

    A new series of novel benzimidazole derivatives containing substituted pyrid-2-yl moiety and polyhydroxy sugar conjugated to the N-benzimidazole moiety has been synthesized and evaluated as orally bioavailable anti-inflammatory agents with anti-ulcerogenic activity. The anti-inflammatory and anti-ulcerogenic activities of these compounds were compared to diclofenac and omeprazole, respectively. In carrageenan-induced paw oedema assay, 2-methyl-N-((3,4-dimethoxypyridin-2-yl)methyl)-1H-benzimidazol-5-amine (12d) and 1-(1,2,3,5-tetrahydroxy-α-D-mannofuranose)-5-(((3,4-dimethoxypyridin-2yl)methyl)amino)-2-methyl-1H-benzimidazole (15d) displayed dose-dependent anti-inflammatory activities by decreasing the inflammation by 62% and 72%, respectively which is comparable to that of diclofenac (73%). In contrast to diclofenac, the anti-inflammatory activity of these compounds was not only free from any side effects on the gastric mucosa but also showed significant anti-ulcerogenic activity in rat pyloric ligation and ethanol-induced gastric ulcer models similar to that of omeprazole. Together, these findings suggest that 12d and 15d are potent anti-inflammatory agents with concurrent anti-ulcerogenic activity and support its clinical promise as a component of therapeutic strategies for inflammation, for which the gastric side effects are always a major limitation.

  2. 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.

  3. 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.

  4. Anti-inflammatory activity of Urera baccifera (Urticaceae) in Sprague-Dawley rats.

    Science.gov (United States)

    Badilla, B; Mora, G; Lapa, A J; Emim, J A

    1999-09-01

    On a preliminary test, anti-inflammatory and analgesic dose-related activities on rats were observed for the aqueous fraction of Urera baccifera; this extract was bioassay-guided fractionated and the final aqueous fraction was used according the ethnobotanical use. Carrageenan-induced edema (n = 6), was used as an assay in the fractionating process. The anti-inflammatory and antinociceptive properties of the final aqueous fraction were studied using in vivo models. For the anti-inflammatory activity rat paw edema (n = 6), pleurisy induced by carrageenan (n = 6) and ear edema induced by topical croton oil (n = 6) models were used, and tail-flick test (n = 6), abdominal constrictions induced by acetic acid (n = 6), and formalin test (n = 6), were used for the antinociceptive activity. The tests performed showed an inhibition effect on leukocyte migration, and a reduction on pleural exudate, as well as dose-dependant peripheral analgesic activity, at a range of 25-100 mg/kg i.p. The final aqueous fraction contains most of the anti-inflammatory activity of the plant U. baccifera. A possible mechanism of action is discussed and based on the results we conclude that this plant has a potential for both anti-inflammatory and analgesic activity at the clinical level.

  5. 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.

  6. 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.

  7. 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.

  8. Anti-inflammatory and Antihistaminic Study of a Unani Eye Drop Formulation

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    Latif Abdul

    2010-03-01

    Full Text Available The Unani eye drop is an ophthalmic formulation prepared for its beneficial effects in the inflammatory and allergic conditions of the eyes. In the present study, the Unani eye drop formulation was prepared and investigated for its anti-inflammatory and antihistaminic activity, using in vivo and in vitro experimental models respectively. The Unani eye drop formulation exhibited significant anti-inflammatory activity in turpentine liniment-induced ocular inflammation in rabbits. The preparation also showed antihistaminic activity in isolated guinea-pig ileum. The anti-inflammatory and antihistaminic activity of eye drop may be due to presence of active ingredients in the formulation. Although there are many drugs in Unani repository which are mentioned in classical books or used in Unani clinical practice effectively in treatment of eye diseases by various Unani physicians. Inspite of the availability of vast literature, there is a dearth of commercial Unani ocular preparations. So, keeping this in mind, the eye drop formulation was prepared and its anti-inflammatory and antihistaminic activity was carried out in animal models. Thus, in view of the importance of alternative anti-inflammatory and anti- allergic drugs, it becomes imperative to bring these indigenous drugs to the front foot and evaluate their activities.

  9. 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.

  10. Anti-inflammatory effects of eugenol nanoemulsion as a topical delivery system.

    Science.gov (United States)

    Esmaeili, Fariba; Rajabnejhad, Saeid; Partoazar, Ali Reza; Mehr, Shahram Ejtemaei; Faridi-Majidi, Reza; Sahebgharani, Mousa; Syedmoradi, Leila; Rajabnejhad, Mohammad Reza; Amani, Amir

    2016-11-01

    Eugenol is the main constituent of clove oil with anti-inflammatory properties. In this work, for the first time, O/W nanoemulsion of eugenol was designed for the evaluation of anti-inflammatory effects as a topical delivery system. Topical formulations containing 1%, 2% and 4% of eugenol as well as a nanoemulsion system containing 4% eugenol and 0.5% piroxicam were prepared. Further to physicochemical examinations, such as determination of particle size, polydispersity index, zeta potential and physical stability, anti-inflammatory activity was examined in carrageenan-induced paw edema in rats. The optimum formulation was found to contain 2% eugenol (oil phase), 14% Tween 20 (surfactant) and 14% isopropyl alcohol (co-surfactant) in water. Nanoemulsion with polydispersity index of 0.3 and median droplet diameter of 24.4 nm (d50) was obtained. Animal studies revealed that the nanoemulsions exhibited significantly improved anti-inflammatory activity after 1.5 h, compared with marketed piroxicam gel. Additionally, it was shown that increasing the concentration of eugenol did not show higher inhibition of inflammation. Also, the nanoemulsion having piroxicam showed less anti-inflammatory properties compared with the nanoemulsion without piroxicam.

  11. 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

  12. 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.

  13. 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.

  14. Structure–activity relationship of terpenes with anti-inflammatory profile – a systematic review.

    Science.gov (United States)

    Souza, Marilia Trindade de Santana; Almeida, Jackson Roberto Guedes da Silva; Araujo, Adriano Antunes de Souza; Duarte, Marcelo Cavalcante; Gelain, Daniel Pens; Moreira, José Cláudio Fonseca; dos Santos, Marcio Roberto Viana; Quintans-Júnior, Lucindo José

    2014-09-01

    Inflammation is a complex biological response that in spite of having available treatments, their side effects limit their usefulness. Because of this, natural products have been the subject of incessant studies, among which the class of terpenes stands out. They have been the source of study for the development of anti-inflammatory drugs, once their chemical diversity is well suited to provide skeleton for future anti-inflammatory drugs. This systematic review reports the studies present in the literature that evaluate the anti-inflammatory activity of terpenes suffering any change in their structures, assessing whether these changes also brought changes in their effects. The search terms anti-inflammatory agents, terpenes, and structure–activity relationship were used to retrieve English language articles in SCOPUS, PUBMED and EMBASE published between January 2002 and August 2013. Twenty-seven papers were found concerning the structural modification of terpenes with the evaluation of antiinflammatory activity. The data reviewed here suggest that modified terpenes are an interesting tool for the development of new anti-inflammatory drugs.

  15. Anti-inflammatory activity of Sri Lankan black tea (Camellia sinensis L. in rats

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    W D Ratnasooriya

    2009-01-01

    Full Text Available This study examined the anti-inflammatory potential of Sri Lankan black tea (Camellia sinensis L. Family: Theaceae using both acute (carrageenan-induced paw oedema and chronic (formaldehyde-induced paw oedema and cotton pellet granuloma test rat inflammatory models. Three dose of black tea brew (BTB [84 mg/ml, equivalent to 1.5 cups; 168 mg/ml, equivalent to 3 cups; and 501 mg/ml, equivalent to 9 cups] were made using high grown unblend Dust grade No: 1 black tea samples and was orally administed to rats (n = 6-9/ dose/ test. The results showed that Sri Lankan BTB possesses marked and significant (P < 0.05 oral anti-inflammatory activity against both acute and chronic inflammation. This anti-inflammatory activity was dose-dependent in the carrageenan-induced paw oedema test and cotton pellet granuloma test. Further, in the carrageenan paw oedema model, the anti-inflammatory activity of BTB was almost identical to green tea brew of both Chinese and Japanese types. Further, the BTB had significant antihistamine activity (in terms of wheal test phagocytic cell migration inhibitory activity (in terms carrageenan-induced leucocyte peritoneal infiltration test, nitric oxide production inhibitory activity, antioxidant activity (DPPH method and prostaglandin synthesis inhibition activity (in terms of rat enteropooling test. It is concluded that Sri Lankan black tea has marked anti-inflammatory potential against both acute and chronic inflammation which is mediated via multiple mechanisms.

  16. 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...

  17. 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

  18. 3-Aminothiophene-2-Acylhydrazones: Non-Toxic, Analgesic and Anti-Inflammatory Lead-Candidates

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    Yolanda Karla Cupertino da Silva

    2014-06-01

    Full Text Available Different chemotypes are described as anti-inflammatory. Among them the N-acylhydrazones (NAH are highlighted by their privileged structure nature, being present in several anti-inflammatory drug-candidates. In this paper a series of functionalized 3-aminothiophene-2-acylhydrazone derivatives 5a–i were designed, synthesized and bioassayed. These new derivatives showed great anti-inflammatory and analgesic potency and efficacy. Compounds 5a and 5d stand out in this respect, and were also active in CFA-induced arthritis in rats. After daily treatment for seven days with 5a and 5d (50 µmol/Kg, by oral administration, these compounds were not renal or hepatotoxic nor immunosuppressive. Compounds 5a and 5d also displayed good drug-scores and low risk toxicity calculated in silico using the program OSIRIS Property Explorer.

  19. EVALUATION OF ANTI INFLAMMATORY ACTIVITY OF GARCINIA INDICA FRUIT RIND EXTRACTS IN WISTAR RATS

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    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.

  20. Anti-inflammatory activity of the apolar extract from the seaweed Galaxaura marginata (Rhodophyta, Nemaliales

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    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.

  1. 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.

  2. Analgesic and Anti-inflammatory action of Opuntia elatior Mill fruits

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    Sanjay P Chauhan

    2015-01-01

    Full Text Available Background: Opuntia elatio Mill is a xerophytic plant with potentially active nutrients. It is traditionally appreciated for its pharmacological properties; however, the scientific information on this plant is insufficient. Objective: The present study evaluates the antinociceptive and anti-inflammatory action of prickly pear. Materials and Methods: Writhing and tail-immersion tests were carried out to evaluate analgesic action, while the carrageenan-induced paw edema and neutrophil adhesion tests were conducted in Albino wistar rats to assess anti-inflammatory action. Results: ED 50 values of the fruit juice in writhing, tail immersion, and paw edema test were 0.919, 2.77, and 9.282 ml/kg, respectively. The fruits of Opuntia produced analgesic and anti-inflammatory action in a dose-dependent manner. Conclusion: The results establish the folklore use of prickly pear may be due to the presence of betacyanin and/or other phenolic compounds.

  3. 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.

  4. Analgesic and anti-inflammatory activities of leaf extract of Kydia calycina Roxb.

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    Baburao Bhukya

    2009-06-01

    Full Text Available The methanol extract of leaves of Kydia calycina Roxb. was screened for the analgesic (using hot plate test and acetic acid-induced writhing test in mice and anti-inflammatory (using rat paw edema test activity at the doses of 200 and 400 mg/kg body weight. A significant (p < 0.0005 analgesic effect was observed with 200 mg/kg and 400 mg/kg in both tests. The maximum anti-inflammatory response was produced at 3 hour with extract doses of 200 and 400 mg/kg. These results suggest that the methanol extract of K. calycina has exhibited significant analgesic and anti-inflammatory effects, which were comparable with standard drugs.

  5. Anti-Inflammatory Effects of GLP-1-Based Therapies beyond Glucose Control

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    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.

  6. Antinociceptive and anti-inflammatory effects of Elaeagnus angustifolia fruit extract.

    Science.gov (United States)

    Ahmadiani, A; Hosseiny, J; Semnanian, S; Javan, M; Saeedi, F; Kamalinejad, M; Saremi, S

    2000-09-01

    In this study, probable antinociceptive and anti-inflammatory effects of Elaeagnus angustifolia fruit components, were evaluated. For evaluation of antinociceptive effects, the chronic (formalin test) and acute (tail-flick) pain models of rats were used. For the anti-inflammatory effects, the paw inflammation model was used through subcutaneous injection of 5% formalin to the paw of male rats. Water extracts of the fruit and its components in the single dose were assessed through comparison with the antinociceptive and anti-inflammatory effects of sodium salicylate (SS) as a positive control. Administration of 300 mg/kg of SS (i.p.) had no effect on tail flick latency, while 1000 mg/kg of total (i.p. and p.o.) and endocarp (i.p.) extract, increased this latency (Pangustifolia fruit contains flavonoids, terpenoids and cardiac glycosides.

  7. Mushrooms: A Potential Natural Source of Anti-Inflammatory Compounds for Medical Applications

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    Elsayed A. Elsayed

    2014-01-01

    Full Text Available For centuries, macrofungi have been used as food and medicine in different parts of the world. This is mainly attributed to their nutritional value as a potential source of carbohydrates, proteins, amino acids, and minerals. In addition, they also include many bioactive metabolites which make mushrooms and truffles common components in folk medicine, especially in Africa, the Middle East, China, and Japan. The reported medicinal effects of mushrooms include anti-inflammatory effects, with anti-inflammatory compounds of mushrooms comprising a highly diversified group in terms of their chemical structure. They include polysaccharides, terpenoids, phenolic compounds, and many other low molecular weight molecules. The aims of this review are to report the different types of bioactive metabolites and their relevant producers, as well as the different mechanisms of action of mushroom compounds as potent anti-inflammatory agents.

  8. Inflammation in Depression and the Potential for Anti-Inflammatory Treatment

    DEFF Research Database (Denmark)

    Kohler, Ole; Krogh, Jesper; Mors, Ole

    2016-01-01

    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......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...... 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...

  9. 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.

  10. Optimization on Extraction Engineering of the Anti - inflammatory Bioactive Materials from Ainsliaea Fragrans Champ

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    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.

  11. 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.

  12. DIURETIC AND ANTI-INFLAMMATORY ACTIVITY OF AQUEOUS EXTRACT OF AERVA SANGUINOLENTA (L. BLUME

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    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.

  13. 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.

  14. Benzophenone-N-ethyl piperidine ether analogues--synthesis and efficacy as anti-inflammatory agent.

    Science.gov (United States)

    Khanum, Shaukath A; Girish, V; Suparshwa, S S; Khanum, Noor Fatima

    2009-04-01

    A sequence of substituted benzophenone-N-ethyl piperidine ether analogues has been synthesized and evaluated as orally active anti-inflammatory agents with reduced side effects. The anti-inflammatory and ulcerogenic activities of the compounds were compared with naproxen, indomethacin, and phenylbutazone. These analogues showed an interesting anti-inflammatory activity in carrageenan-induced foot pad edema assay. In the air-pouch test, some of the analogues reduced the total number of leukocytes of the exudate, which indicates inhibition of prostaglandin production. Side effects of the compounds were examined on gastric mucosa, in the liver and stomach. None of the compounds illustrated significant side effects compared with standard drugs like indomethacin and naproxen.

  15. 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.

  16. 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.

  17. Identification of an anti-inflammatory potential of Eriodictyon angustifolium compounds in human gingival fibroblasts.

    Science.gov (United States)

    Walker, Jessica; Reichelt, Katharina V; Obst, Katja; Widder, Sabine; Hans, Joachim; Krammer, Gerhard E; Ley, Jakob P; Somoza, Veronika

    2016-07-13

    Polyphenol-rich plant extracts have been shown to possess anti-inflammatory activity against oral pathogen-induced cytokine release in model systems of inflammation. Here, it was hypothesized that a flavanone-rich extract of E. angustifolium exhibits an anti-inflammatory potential against endotoxin-induced inflammatory response in human gingival fibroblasts (HGF-1). HGF-1 cells were stimulated with lipopolysaccharide from Porphyromonas gingivalis (pg-LPS) to release pro-inflammatory cytokines. Concentrations of interleukins IL-6 and IL-8 and macrophage chemoattractant protein-1 in the incubation media upon stimulation were determined by means of magnetic bead analysis. A crude ethanol/water extract of E. angustifolium (EE) was fractionated via gel permeation chromatography into a flavanone-rich fraction (FF) and an erionic acid-rich fraction (EF). Individual flavanones and erionic acids as well as EE, EF and FF were tested in the pg-LPS-stimulated HGF-1 cells for their anti-inflammatory potential. The E. angustifolium extract possessed anti-inflammatory potential in this model system, attenuating the pg-LPS-induced release of IL-6 by up to 52.0 ± 15.5%. Of the individual flavanones, eriodictyol and naringenin had the most pronounced effect. However, a mixture of the flavanones did not possess the same effect as the entire flavanoid fraction, indicating that other compounds may contribute to the anti-inflammatory potential of E. angustifolium. For the first time, an anti-inflammatory potential of E. angustifolium and containing erionic acids has been determined.

  18. 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.

  19. Development of anti-inflammatory drugs - the research and development process.

    Science.gov (United States)

    Knowles, Richard Graham

    2014-01-01

    The research and development process for novel drugs to treat inflammatory diseases is described, and several current issues and debates relevant to this are raised: the decline in productivity, attrition, challenges and trends in developing anti-inflammatory drugs, the poor clinical predictivity of experimental models of inflammatory diseases, heterogeneity within inflammatory diseases, 'improving on the Beatles' in treating inflammation, and the relationships between big pharma and biotechs. The pharmaceutical research and development community is responding to these challenges in multiple ways which it is hoped will lead to the discovery and development of a new generation of anti-inflammatory medicines.

  20. 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.

  1. 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.

  2. Evaluation of In Vitro Anti-inflammatory Activity of Azomethines of Aryl Oxazoles

    Directory of Open Access Journals (Sweden)

    V. Niraimathi

    2011-01-01

    Full Text Available Ability to inhibit erythrocyte hemolysis is often used as a characteristic of the membrane stabilising action of chemical compounds. Azomethines of aryl oxazoles were evaluated for anti-inflammatory by in vitro hemolytic membrane stabilising study. The effect of inflammation condition was studied on erythrocyte exposed to hypotonic solution. In this in vitro method the membrane stabilising action leads to anti-inflammatory activity and was compared with that produced by diclofenac sodium as the reference standard. Results of the evaluation indicate that the synthesised compounds found to exhibit membrane stabilising activity.

  3. ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY OF ETHANOLIC EXTRACT OF BETA VULGARIS LINN. ROOTS

    OpenAIRE

    Chakole, Rita; Zade, Shubhangi; Charde, Manoj

    2011-01-01

    The present study deals with evaluation of antioxidant and anti-inflammatory activity of ethanolic extract of Beta Vulgaris roots. The ethanolic extract was subjected to screen forantioxidant activity using DPPH radical scavenging method. The anti-inflammatory activity was carried out by using carageenan induced rat paw edema method. The tested extract ofdifferent dilutions in range 200 µg/ml to 1000 µg/ml shows activity in range of 4.34% to 18.55%. The extract shows prominent anti-inflamma...

  4. Synthesis and pharmacological evaluation of pyrazolopyrimidopyrimidine derivatives: anti-inflammatory agents with gastroprotective effect in rats

    OpenAIRE

    2013-01-01

    We report the synthesis of new anti-inflammatory 1,7-dihydropyrazolo[3′,4′:4,5]pyrimido[1,6-a]pyrimidine 5 from aminocyanopyrazole. All compounds were characterized by physical, chemical and spectral studies. Preliminary pharmacological evaluation of the resulting products showed that compounds 5a, b, f (50–100 mg/kg, i.p) are active anti-inflammatory agents in carrageenan-induced rat paw oedema assay, and their effects are comparable to that of acetylsalicylic–lysine (300 mg/kg, i.p.), used ...

  5. Anti-Inflammatory Components of the Starfish Astropecten polyacanthus

    Directory of Open Access Journals (Sweden)

    Young Ho Kim

    2013-08-01

    Full Text Available Inflammation is important in biomedical research, because it plays a key role in inflammatory diseases including rheumatoid arthritis and other forms of arthritis, diabetes, heart disease, irritable bowel syndrome, Alzheimer’s disease, Parkinson’s disease, allergies, asthma, and even cancer. In the present study, we describe the inhibitory effect of crude extracts and steroids isolated from the starfish Astropecten polyacanthus on pro-inflammatory cytokine (Interleukin-12 (IL-12 p40, interleukin-6 (IL-6, and tumor necrosis factor α (TNF-α production in lipopolysaccharide (LPS-stimulated bone marrow-derived dendritic cells (BMDCs. Among those tested, compounds 5 and 7 showed potent inhibitory effects on the production of all three pro-inflammatory cytokines with IC50 values ranging from 1.82 ± 0.11 to 7.00 ± 0.16 μM. Potent inhibitory activities were also observed for compound 1 on the production of IL-12 p40 and IL-6 with values of 3.96 ± 0.12 and 4.07 ± 0.13 μM, respectively, and for compounds 3 and 4 on the production of IL-12 p40 with values of 6.55 ± 0.18 and 5.06 ± 0.16 μM, respectively. Moreover, compounds 2 (IC50 = 34.86 ± 0.31 μM and 6 (IC50 = 79.05 ± 2.05 μM exhibited moderate inhibitory effects on the production of IL-12 p40, whereas compounds 3 (IC50 = 22.80 ± 0.21 μM and 4 (IC50 = 16.73 ± 0.25 μM moderately inhibited the production of TNF-α and IL-6, respectively.

  6. Nonsteroidal anti-inflammatory drugs modulate cellular glycosaminoglycan synthesis by affecting EGFR and PI3K signaling pathways

    Science.gov (United States)

    Mozolewski, Paweł; Moskot, Marta; Jakóbkiewicz-Banecka, Joanna; Węgrzyn, Grzegorz; Bocheńska, Katarzyna; Banecki, Bogdan; Gabig-Cimińska, Magdalena

    2017-01-01

    In this report, selected non-steroidal anti-inflammatory drugs (NSAIDs), indomethacin and nimesulide, and analgesics acetaminophen, alone, as well as in combination with isoflavone genistein as potential glycosaminoglycan (GAG) metabolism modulators were considered for the treatment of mucopolysaccharidoses (MPSs) with neurological symptoms due to the effective blood-brain barrier (BBB) penetration properties of these compounds. We found that indomethacin and nimesulide, but not acetaminophen, inhibited GAG synthesis in fibroblasts significantly, while the most pronounced impairment of glycosaminoglycan production was observed after exposure to the mixture of nimesulide and genistein. Phosphorylation of the EGF receptor (EGFR) was inhibited even more effective in the presence of indomethacin and nimesulide than in the presence of genistein. When examined the activity of phosphatidylinositol-3-kinase (PI3K) production, we observed its most significant decrease in the case of fibroblast exposition to nimesulide, and afterwards to indomethacin and genistein mix, rather than indomethacin used alone. Some effects on expression of individual GAG metabolism-related and lysosomal function genes, and significant activity modulation of a number of genes involved in intracellular signal transduction pathways and metabolism of DNA and proteins were detected. This study documents that NSAIDs, and their mixtures with genistein modulate cellular glycosaminoglycan synthesis by affecting EGFR and PI3K signaling pathways. PMID:28240227

  7. Mechanistic and conformational studies on the interaction of anti-inflammatory drugs, isoxicam and tenoxicam with bovine serum albumin

    Energy Technology Data Exchange (ETDEWEB)

    Punith, Reeta; Katrahalli, Umesha; Kalanur, Shankara S. [Department of Chemistry, Karnatak University, Dharwad 580 003 (India); Jaldappagari, Seetharamappa, E-mail: jseetharam@yahoo.co [Department of Chemistry, Karnatak University, Dharwad 580 003 (India)

    2010-11-15

    The mechanism of interaction of the non-steroidal anti-inflammatory drugs, isoxicam (IXM) and tenoxicam (TXM) with bovine serum albumin (BSA) has been studied using spectroscopic techniques, viz., spectrofluorescence, circular dichroism (CD), UV-visible absorption and FT-IR under simulative physiological conditions. Stern-Volmer analysis of fluorescence quenching data shows the presence of the static quenching mechanism. Thermodynamic parameters (negative {Delta}H{sup 0} and positive {Delta}S{sup 0} values obtained in the present study) revealed that the hydrophobic interactions played a major role in the interaction of these drugs with BSA. The distance, r between the donor (BSA) and acceptor (IXM/TXM) was calculated based on the Forster's theory of non-radiation energy transfer and the values were observed to be 3.85 nm and 2.60 nm in IXM-BSA and TXM-BSA system, respectively. CD and FT-IR studies indicated that the binding of IXM/TXM to BSA induced conformational changes in BSA. The effect of common ions on the binding of IXM/TXM to BSA has been investigated.

  8. Use of low-dose aspirin and non-aspirin nonsteroidal anti-inflammatory drugs and risk of glioma

    DEFF Research Database (Denmark)

    Gaist, D; 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...

  9. Anti-inflammatory effects of physalin E from Physalis angulata on lipopolysaccharide-stimulated RAW 264.7 cells through inhibition of NF-κB pathway.

    Science.gov (United States)

    Yang, Yan-Jun; Yi, Lang; Wang, Qing; Xie, Bing-Bing; Dong, Yan; Sha, Cong-Wei

    2017-04-01

    Physalin E is a naturally occurring seco-steroid isolated from the stems and aerial parts of Physalis angulata L. (Solanaceae). This study was aimed to explore the anti-inflammatory effects of physalin E on RAW 264.7 mouse macrophages stimulated by lipopolysaccharide (LPS) and the potential underlying mechanisms. The results showed that physalin E significantly inhibited LPS-induced tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) expression and secretion in a dose-dependent manner. Unlike dexamethasone, these effects could not be blocked by miferstone (RU486). Meanwhile, physalin E reduced the degradation of I-kappa B protein in the cytoplasm and downregulated the nuclear factor-κB (NF-κB) p65 protein in the nuclear, which resulted in the inhibition of the NF-κB nuclear translocation. In conclusion, physalin E exerts its anti-inflammatory activities in LPS-induced macrophages. Physalin E can inhibit the production of inflammatory cytokines by targeting the NF-κB signaling pathway.

  10. Acetylsalicylic Acid reduces the severity of dextran sodium sulfate-induced colitis and increases the formation of anti-inflammatory lipid mediators.

    Science.gov (United States)

    Köhnke, Thomas; Gomolka, Beate; Bilal, Süleyman; Zhou, Xiangzhi; Sun, Yanping; Rothe, Michael; Baumgart, Daniel C; Weylandt, Karsten H

    2013-01-01

    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.

  11. Analgesic, Anti-Inflammatory and Anticancer Activities of Extra Virgin Olive Oil

    Directory of Open Access Journals (Sweden)

    Myriam Fezai

    2013-01-01

    Full Text Available Background. In folk medicine, extra virgin olive oil (EVOO is used as a remedy for a variety of diseases. This study investigates the in vivo antinociceptive, anti-inflammatory, and anti-cancer effects of EVOO on mice and rats. Materials and Methods. In this experimental study, using the acetic acid-induced writhing and formalin tests in mice, the analgesic effect of EVOO was evaluated. Acetylsalicylic acid and morphine were used as standard drugs, respectively. The anti-inflammatory activity was investigated by means of the carrageenan-induced paw edema model in rats using acetylsalicylic acid and dexamethasone as standard drugs. Last, the xenograft model in athymic mice was used to evaluate the anticancer effect in vivo. Results. EVOO significantly decreased acetic acid-induced abdominal writhes and reduces acute and inflammatory pain in the two phases of the formalin test. It has also a better effect than Dexamethasone in the anti-inflammatory test. Finally, the intraperitoneal administration of EVOO affects the growth of HCT 116 tumours xenografted in athymic mice. Conclusion. EVOO has a significant analgesic, anti-inflammatory, and anticancer properties. However, further detailed studies are required to determine the active component responsible for these effects and mechanism pathway.

  12. Fatigue in patients with multiple sclerosis is it related to pro- and anti-inflammatory cytokines?

    NARCIS (Netherlands)

    Malekzadeh, Arjan; Van de Geer-Peeters, Wietske; De Groot, Vincent; Teunissen, Charlotte Elisabeth; Beckerman, Heleen; Heine, M

    2015-01-01

    OBJECTIVE: To investigate the pathophysiological role of pro- and anti-inflammatory cytokines in primary multiple sclerosis-related fatigue. METHODS: Fatigued and non-fatigued patients with multiple sclerosis (MS) were recruited and their cytokine profiles compared. Patients with secondary fatigue w

  13. 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...

  14. Design and In Vivo Anti-Inflammatory Effect of Ketoprofen Delayed Delivery Systems.

    Science.gov (United States)

    Cerciello, Andrea; Auriemma, Giulia; Morello, Silvana; Pinto, Aldo; Del Gaudio, Pasquale; Russo, Paola; Aquino, Rita P

    2015-10-01

    For the treatment of inflammatory-based diseases affected by circadian rhythms, the development of once-daily dosage forms is required to target early morning symptoms. In this study, Zn-alginate beads containing ketoprofen (K) were developed by a tandem technique prilling/ionotropic gelation. The effect of main critical variables on particles micromeritics, inner structure as well as on drug loading and in vitro drug release was studied. The in vivo anti-inflammatory efficacy was evaluated using a modified protocol of carrageenan-induced edema in rat paw administering beads to rats by oral gavage at 0, 3, or 5 h before edema induction. Good drug loading and desired particle size and morphology were obtained for the optimized formulation F20. In vitro dissolution studies showed that F20 had a gastroresistant behavior and delayed release of the drug in simulated intestinal fluid. The in vitro delayed release pattern was clearly reflected in the prolonged anti-inflammatory effect in vivo of F20, compared to pure ketoprofen; F20, administered 3 h before edema induction, showed a significant anti-inflammatory activity, reducing maximum paw volume in response to carrageenan injection, whereas no response was observed for ketoprofen. The designed beads appear a promising platform suitable for a delayed release of anti-inflammatory drugs. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:3451-3458, 2015.

  15. 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. Afte