Carrageenin-induced Edema In Rats Research Articles

Extracts of Brocchia cinerea (Delile) Vis Exhibit In Vivo Wound Healing, Anti-Inflammatory and Analgesic Activities, and Other In Vitro Therapeutic Effects.

The plant Brocchia cinerea (Delile) (B. cinerea) has many uses in traditional pharmacology. Aqueous (BCAE) and ethanolic extracts (BCEE) obtained from the aerial parts can be used as an alternative to some synthetic drugs. In vitro, DPPH, FRAP and TAC are three tests used to measure antioxidant efficacy. Antibacterial activities were determined against one Gram positive and two Gram negative strains of bacteria. The analgesic power was evaluated in vivo using the abdominal contortion model in mice, while carrageenan-induced edema in rats was the model chosen for the anti-inflammatory test; wound healing was evaluated in an experimental second degree burn model. The results of the phytochemical analysis showed that BCEE had the greatest content of polyphenols (21.06 mg AGE/g extract), flavonoids (10.43 mg QE/g extract) and tannins (24.05 mg TAE/g extract). HPLC-DAD reveals the high content of gallic acid, quercetin and caffeic acid in extracts. BCEE has a strong antiradical potency against DPPH (IC50 = 0.14 mg/mL) and a medium iron reducing activity (EC50 = 0.24 mg/mL), while BCAE inhibited the growth of the antibiotic resistant bacterium, P. aeruginosa (MIC = 10 mg/mL). BCAE also exhibited significant pharmacological effects and analgesic efficacy (55.81% inhibition 55.64% for the standard used) and the re-epithelialization of wounds, with 96.91% against 98.60% for the standard. These results confirm the validity of the traditional applications of this plant and its potential as a model to develop analogous drugs.

A POWERFUL ELISA TECHNIQUE TO TEST THE POTENTIAL OF EXTRA VIRGIN OLIVE OIL IN REDUCING TNF-Α LEVEL AND EDEMA VOLUME IN MALE Rattus norvegicus EXPOSED TO CARRAGEENAN

Extra virgin Olive oil is extracted from fruit that can be used as anti-inflammatory agent. This research aimed to test the potential of extra virgin olive oil in reducing edema volume and TNF-α plasma in carrageenan-induced rats. This research was purely experimental research with the post test control group design. A total of twenty eight Wistar rats were divided randomly into four treatment groups. Group I was a control negative group, while the group II, III, and IV were orally administered with extra virgin Olive oil at the dose of 0.9 ; 1.8 ; 2.7 mL/day, respectively. Paw edema was measured one hour before the rats was induced to carrageenan and every hour until four hours after it was induced to carrageenan. TNF-α plasma was measured at four hours. Analysis of the data was done by calculating the presentation of edema inhibition in every group, then the data was statistically analyzed by Anova, Repeated Anova, LSD and Kruskal Wallis test with 95% confidence interval. The result showed that extra virgin olive oil has an anti-inflammatory effect. The highest decrease in edema volume percentage was in group III (14.21%). There was a significant difference in the edema volume of all treatment groups at each time of the experiment with TNF-α value (p < 0.05). In conclusion, the administration of extra virgin olive oil can lower the volume of carrageenan-induced edema in rats depend on the dose. Also, the administration of extra virgin olive oil can be dose-dependent in reducing the levels of TNF-α in carrageenan-induced edema in rats.

Marine sponges Sarcotragus foetidus, Xestospongia carbonaria and Spongia obscura constituents ameliorate IL-1 β and IL-6 in lipopolysaccharide-induced RAW 264.7 macrophages and carrageenan-induced oedema in rats.

Marine sponges are prolific producers of an array of diverse chemical structures containing compounds with multiple biological activities. In this study, whole methanol extracts and fractionated compounds from three marine sponges namely Xestospongia carbonaria, Sarcotragus foetidus and Spongia obscura were thoroughly investigated for their antibacterial, antifungal, antioxidant and anti-inflammatory activities. Methanol extracts and fractionated compounds were characterised using high performance liquid chromatography-mass spectrometry and gas chromatography-mass spectrometry. Extracts were checked for cytotoxicity in RAW macrophages by MTT assay, before using them for the treatment study. Enzyme linked immunosorbent assay kits were used to check the effects on inflammatory mediator's levels (PGE2, COX-2, IL-6, IL-1β, TNF-α) in vitro. The results demonstrated good anti-inflammatory activity of all the three marine sponges; X. carbonaria, S. foetidus and S. obscura suppressed the levels of anti-inflammatory cytokines in vitro. Reverse transcriptase-polymerase chain reaction confirmed the inhibition of IL-1β and IL-6 genes expression by the isolates of X. carbonaria and S. foetidus, while reducing cytokine levels in lipopolysaccharide-induced inflammation in vitro as well as in carrageenan-induced inflammation in rats. Two semi pure compounds isolated from X. carbonaria and S. foetidus also confirmed suppression of IL-1β and IL-6 genes expression in RAW macrophages.

Anti-inflammatory effect of date seeds (Phoenix dactylifera L) on carrageenan-induced edema in rats

Purpose: To investigate the influence of sodium hypochlorite (NaOCl) on human dental stem cell proliferation and differentiation.Method: Dental pulp stem cells (DPSCs), periodontal ligament stem cell (PDLSCs), and gingival mesenchymal stem cells (GMSCs) were treated with NaOCl. Cell viability was evaluated with cellular counting kit-8 (CCK8), and cellular adenosine triphosphate (ATP) levels were analyzed by bromodeoxyuridine (BrdU) incorporation and subsequent flow cytometry. Quantitative polymerase chain reaction (qPCR) and western blotting were performed to detect the expressions of differentiation markers.Results: The viability and ATP levels of all three stem cells types were impaired by NaOCl in a concentration- and time-dependent manners. However, the decrease ATP in GMSCs was less than the other two stem cell population (p < 0.05). NaOCl treatment significantly suppressed the proliferation of dental stem cells (p < 0.05). With regard to differentiation marker expression levels, the decrease in Stro-1 was greater in treatment groups when compared to control on Day 7, while increase in levels of dentin sialophosphoprotein (DSPP), bone sialoprotein (BSP), and osteocalcin (OC) was smaller (p < 0.05). The expressional changes of Stro-1, DSPP, BSP, and OC were more prominent in DPSMs and PDLSCs than in GMSCs.Conclusion: NaOCl dose-dependently impairs the viability, proliferation and differentiation of dental stem cells. Thus, its toxicity to dental stem cells needs to be considered in clinical application.Keywords: Dental stem cells, Sodium hypochlorite, Viability, Proliferation, Differentiation

Appraisal of Antioxidant and Anti-Inflammatory Activities of Various Extracts from the Fruiting Bodies of Pleurotus florida

Pleurotus florida has been widely used for nutritional and medicinal purposes. The present study was conducted to evaluate the antioxidant and anti-inflammatory effects of the fruiting bodies of P. florida extracted with acetone, methanol, and hot water. The antioxidant activities of the acetone and methanol extracts of P. florida showed stronger inhibition of β-carotene-linoleic acid compared to that of the hot water extract. The acetone extract (8 mg/mL) showed a high reducing power of 1.86. The acetone and methanol extracts showed more effective DPPH radical scavenging activities than the hot water extract. The chelating effect of the extracts at lower concentrations was significantly effective compared to that of the positive control. Thirteen phenolic compounds were detected from acetonitrile and hydrochloric acid solvent extracts. Nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in lipolysaccahride (LPS) stimulated RAW 264.7 cells, a murine macrophage cell line, were inhibited significantly by the mushroom extracts in a concentration dependent manner. The anti-inflammatory activity on carrageenan-induced edema in the rat hind-paw reduced significantly by the mushroom extracts. Therefore, we have demonstrated that P. florida fruiting bodies possess antioxidant and anti-inflammatory activites related to their inhibitory activities on NO production, iNOS protein expression, and carrageenan-induced paw edema in rats. The results suggest that the fruiting bodies of P. florida are a good source of natural antioxidant and anti-inflammatory agents.

Anti-inflammatory Potential of Silk Sericin

Silk sericin was found to suppress the production of pro-inflammatory cytokines, which are related to the inflammatory reaction. The objectives of this study were to investigate the anti-inflammatory effect of sericin in vivo using the carrageenan-induced rat edema model and changes in the histology of tissues. The effects of sericin on the expression of COX-2 and iNOS were also evaluated. Sericin solutions at 0.004-0.080 mg/mL were applied topically to the top of the hind paw and carrageenan (1.0 mg) was injected subcutaneously to the plantar surface of the right hind paw. Our results indicated that sericin significantly reduced the inflammation in rats' paw compared with the negative control (water and acetone) and its effect at 0.080 mg/mL was only slightly lower than that of 1.0% w/v indomethacin. Similar numbers of polymorphonuclear and macrophage cells were found in rats' tissue treated with indomethacin and sericin solution, while the numbers were significantly higher in their absence. The gene expression results by RT-PCR showed that the COX-2 and iNOS genes were down-regulated in samples treated with sericin in a dose dependent manner. These data indicated that the anti-inflammatory properties of sericin may be partly attributable to the suppression of the COX-2 enzyme and nitric oxide production.

Synthesis and Biological Evaluation of a Novel Series of Pyrazolylcoumarins as Anti-Inflammatory and Antioxidant Agents

A new series of pyrazolylcoumarins (4a-k) was synthesized by reaction of appropriate dibromochalcones (3a-k) with phenyl hydrazine in ethanol. Structures of all new synthesized compounds were characterized on the basis of elemental analysis and spectral data (UV, IR and 1H NMR). The title compounds were screened for in vivo anti-inflammatory activities at a dose of 200 mg/kg b.w. Among the 11 prepared compounds, Compounds 4c, d, h and i exhibited significant anti-inflammatory activity in model of acute inflammation such as carrageenan-induced rat edema paw while compound 4d showed considerable activity in model of chronic inflammation such as adjuvant-induced arthritis along with minimum ulcerogenic index and were compared with diclofenac (13.5 mg/kg b.w.) as a standard drug. Additionally, the synthesized compounds were evaluated for their in vitro antioxidant activity. Compound 4k was found to be the most active antioxidant in the series compared with standard vitamin C.

Non-Selective Inhibition of Cyclooxygenase Enzymes by Aminoacetylenic Isoindoline 1,3-Diones

The reported pharmacological activities of acetylenic and phthalimide groups promoted our interest to synthesize a novel series of N-[4-(t-amino-yl)-but-2-yn-1-yl] isoindoline-1,3-diones as anti-inflammatory compounds. The aim of this research is to investigate the selectivity of two compounds, ZM4 and ZM5, on inhibiting cyclooxygenase (COX) in vitro and in silico as well as reducing carrageenan-induced edema in rats. Oral administration of 5-20 mg/kg ZM4 and ZM5 reduced significantly carrageenan-induced edema in dose-and time dependent manner. Furthermore, the IC50 values induced by ZM4 and ZM5 were in the range of 3.0-3.6 μM for COX1 and COX 2 but were higher than those induced by Diclofenac and Celecoxib, respectively. Docking of ZM4 and ZM5 in both COX enzymes, on the other hand, exhibited the conventional binding modes that are usually adopted by different non-steroidal anti-inflammatory drugs (NSAIDs). Furthermore, ZM4 and ZM5 bind to COX enzymes as strongly as Flurbiprofen and Celecoxib. In conclusion, aminoacetylenic isoindoline 1, 3-dione compounds have shown anti-inflammatory activity by inhibiting COX-1 and COX-2 enzymes. Interestingly, the best hits showed inhibition at low micromolar levels although they are not selective at this stage. Further research will be conducted to improve both selectivity and potency.

Quantitative analysis and simulation of anti-inflammatory effects from the active components of Paino Powder () in rats.

OBJECTIVE: To explore different combinations of the active ingredients of Paino Powder ()), including paeoniflorln, naringin, neohesperidln and platyeodin-D, which are responsible for the inhibition of carrageenin-induced edema in rats, and to evaluate the performance of the orthogonal simulation method in quantitative analysis and the simulation of the combinations. METHODS: A 1-level (used) and 2-level (unused) orthogonal design was applied to assign 7 combinations of active components. Aspirin and saline were set as the two controls. The carrageen In-Induced edema in the right hind paws of rats was established as the acute inflammation model The efficacy indices were expressed by the area under the curve (AUC) and the peak value of the swelling change (%) over time in rats. RESULTS: Compared with the saline group, the rats in active component combinations showed a significant reduction of AUG and peak value in the swelling (P<0.05). The maximum anti-inflammatory effect was from the whole four-ingredient combination. Among the four ingredients, naringin showed a dominant contribution to the combination, while paeoniflorin > platycodin-D > naringin contributed in succession. These results are consistent with the results of computer simulation. CONCLUSIONS: A single component from Paino Powder does not exhibit any anti-inflammatory effect, but some combinations show such effect. The strongest inhibition to edema comes from the full 4-ingredient combination. The orthogonal simulation method is feasible in the research on decomposed formulas of Chinese medicine.

Anti-inflammatory activity of the non-peptidyl low molecular weight radical scavenger IAC in carrageenan-induced oedema in rats

In this research we investigated the anti-inflammatory activity of a non-peptidyl low molecular weight radical scavenger (IAC) in an acute and chronic animal model of inflammation. For this purpose the effect of IAC (10, 25, 50 mg/kg) was tested in rats on the associated behavioral responses to subsequent inflammatory and noxious challenges, such as hind paw oedema induced by intra-plantar injection of carrageenan and granuloma induced by subcutaneous implant of a cotton pellet, using indometacin (2.5 mg/kg) as reference drug. Moreover, the serum level of several cytokines was tested in the animal treated (or not) with IAC (50 mg/kg) both in the absence and presence of carrageenan-induced inflammation. IAC showed a significant anti-inflammatory activity in both in acute and chronic models of inflammation. In addition IAC down regulated significantly the serum levels of interleukin (IL) 2 and IL6 whereas it increased the serum concentration of IL1α and glutathione. Although it remains to be elucidated whether or not the antioxidant property of IAC is directly responsible for the modulation of the tested cytokines, these results suggest IAC to be a possible candidate for a novel anti-inflammatory compound.

Synthesis and pharmacological evaluation of aminoacetylenic isoindoline-1,3-dione derivatives as anti-inflammatory agents

Aminoacetylenic isoindoline-1,3-dione derivatives were synthesized from the reaction of potassium phthalimide with propargyl bromide to generate 2-(prop-2-yn-1-yl)isoindoline-1,3-dione (ZM1). Treatment of 2-(prop-2-yn-1-yl)isoindoline-1,3-dione with appropriate cyclic amines through Mannich reaction yielded five desired aminoacetylenic isoindoline-1,3-diones called, ZM2–ZM6. The IR, NMR and elemental analysis were consistent with the assigned structures. These synthetic compounds, except ZM6, produced significant (p<0.05–0.01) dose-related inhibition of carrageenan-induced edema in rats following 3 and 5h post-oral administration of 5, 10, and 20mg/kg doses. The percent inhibition of edema varied between the compounds at 10mg/kg dose being ZM3>ZM5>ZM4>ZM2. These percent inhibitions for ZM3 and ZM5 were not significantly different than those of induced by Ibuprofen, Diclofenac and Celecoxib. At 20mg/kg dose, ZM4 produced a statistically significant reduction of inflammation (p<0.01) 1h following administration and persisted for 5h. Furthermore, all the compounds showed inhibition of COX-1 and COX-2 with maximum inhibition at 5μM. However, the inhibition values were less than Diclofenac and Celecoxib. The best response was by ZM4 for COX-2 inhibition ranging from 28%, 91%, and 44%, for 2, 5, and 10μM, respectively. Other ZM compounds such as ZM2, ZM3, and ZM5 exhibited inhibitory responses for COX-2 more than COX-1 at 5μM. These results indicate that these ZM compounds have the potential to become anti-inflammatory drugs following further pharmacological and toxicological evaluations.

Preparation of chitosan/alginate/calcium complex microparticles loaded with lactoferrin and their efficacy on carrageenan-induced edema in rats

Background: Although lactoferrin (LF) possesses useful functions such as antitumor, antiviral, and anti-inflammatory acitivities, it is subject to gastric digestion, resulting in the reduction of efficacy. Therefore, it is important to develop a system delivering LF efficiently to intestinal mucosa or gut-associated lymphoid tissue. Method: Chitosan/alginate/calcium complex microparticles containing LF at a high loading were prepared using alginate, LF, and calcium chloride at the ratio of 6:3:8 (w/w). The release test was performed using Japanese Pharmacopoeia, Fifteenth Edition (JP15) first fluid (pH 1.2) for initial 2 hours, followed by JP15 second fluid (pH 6.8) for another 5 hours. Furthermore, the in vivo efficacy was evaluated from anti-inflammatory effect using rats with carrageenan-induced edema, in which dosing was performed intragastrically at 50 mg LF eq./kg 5, 3, and 1 days before carrageenan injection. Results: Microparticles have 20 – 30 % (w/w) LF content and 1 – 3 mm size. Nearly 60 % of LF was released at pH 1.2 at the first 1 hour, and then slowly released up to 80 % at 7 hours. Suppressive effect against the edema was greater in the order of microparticles LF solution control (saline). Initial burst of LF from microparticles was not associated with their promoted efficacy. Conclusion: Chitosan/alginate/calcium complex microparticles are suggested to be useful for promotion of efficacy of LF at oral administration

Potassium humate inhibits carrageenan-induced paw oedema and a graft-versus-host reaction in rats

It has been shown in a previous study that brown coal-derived potassium humate is safe and effective in suppressing contact hypersensitivity in rats. In this study the efficacy of potassium humate on other types of inflammation was determined. Preparative TLC followed by mass spectroscopy was used in an attempt to fingerprint the product. The effects of potassium humate, at an oral dose of 60 mg/kg bodyweight, on a delayed type hypersensitivity reaction, a carrageenan-induced inflammation model and an allogeneic graft-versus-host reaction (GVHR) in rats were investigated. Paw oedema was used as a measure of inflammation. It was found that potassium humate had no effect on the delayed type hypersensitivity reaction but significantly inhibited the increase in paw volume of the carrageenan-induced oedema in rats which compared favourably with indomethacin treatment. Furthermore, potassium humate inhibited the GVHR induced in normal and cyclophosphamide-treated immune-incompetent rats. The identification of a naturally occurring compound that is safe and effective in reducing different types of inflammation merits further evaluation in clinical trials.

A new therapeutic approach in Parkinson’s disease: Some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents

The increasing life expectancy in our population makes Parkinson’s disease (PD) a growing public health problem. There is a great need to find a way to prevent and delay the disease. It was shown that selective phosphodiesterase 1 (PDE1) inhibitors and anti-inflammatory agents might be effective in treating PD. Therefore, a novel 1,2,9,11-tetrasubstituted-7 H-thieno[2′,3′:4,5]pyrimido[6,1- b]-quinazolin-7-one ( 1–15) and 1,3,10,12-tetrasubstituted-8 H-pyrido[2′,3′:4,5]pyrimido[6,1- b]quinazolin-8-one ( 16– 36) derivatives were synthesized by reported method and investigated for their ability to inhibit PDE1. Most of the synthesized compounds have shown good activity against PDE1 and were less effective than 3-isobutyl-1-methylxanthine. All the compounds were also tested for their in vitro anti-inflammatory activity by carrageenan-induced oedema in rats. In addition, ulcerogenic activity was determined. The combined anti-inflammatory data from in vitro animal model showed that compounds, 9,11-dibromo-1-(2-furyl)-3-(4-tolyl)-8 H-pyrido[2′,3′:4,5]pyrimido[6,1- b]quinazolin-8-one 23, 9,11-dibromo-1-(4-methoxy-phenyl)-3-phenyl-8 H-pyrido[2′,3′:4,5]pyrimido[6,1- b]quinazolin-8-one 24, 9,11-dibromo-1-(4-chloro-phenyl)-3-(4-tolyl)-8 H-pyrido[2′,3′:4,5]pyrimido[6,1- b]quinazolin-8-one 29 and 9-bromo-1-(4-chloro-phenyl)-3-(4-tolyl)-8 H-pyrido[2′,3′:4,5]pyrimido[6,1- b]quinazolin-8-one 36 exhibited even more potent anti-inflammatory activity and low gastric ulceration incidence compare to reference standard Indomethacin. Since compound 23, 24, 29 and 36 exhibits both anti-inflammatory activity and PDE1 inhibition, it needs further detailed studies.

Anti-inflammatory, antioxidant, anti-tumor and physiological studies on Levisticum officinale-Koch plant

Levisticum officinale-Koch (lovage) plant is a member of family Abiaceae" Umbellifera" used as expectorant and stomach stimulant. Essential oil of control plants was extracted by hydrodistillation. Anti-oxidant and anti-tumor activities of essential oil were studied. The essential oil showed antioxidant activity using DPPH method [1] (IC50, 65µg/ml). The essential oil has anti-tumor activity against HepG2 and MCF7 by 98% and 95% at 100µg/ml, respectively and less activity against HT29at the same concentration while the essential oil showed weak activity at 50µg/ml (65% inhibition) and no activities at lower concentrations. Petroleum ether and chloroform extracts of plant have anti-inflammatory activity after 4hrs in carrageenan-induced oedema in rats [2]at dose of 200mg/kg b.wt. Lovage plant seeds were cultivated in loam soil in two successive seasons (October 2007& 2008) at different distances (20, 40 and 60cm in between plants) and fertilized using compost (25, 37.5, 50m3/Hectar). The best cultivation distance was 40cm; it produced 3150g fresh herb/m2 while the best compost level was 50m3/Hectar (750g fresh herb/m2/harvest) as compared to control plant (330g fresh herb/m2/harvest)

Antinociceptive and anti-inflammatory activities of Tabernaemontana catharinensis

In this work we describe the analgesic, anti-inflammatory and toxic activities as well as the phytochemical profile of the ethanol extract from Tabernaemontana catharinensis A. DC. (Apocynaceae) stem bark. Analgesic evaluation was carried out against chemical and thermal stimuli. Anti-inflammatory activity was investigated on carrageenan-induced edema in rats and toxicological studies (LD50) were conducted in mice. Phytochemical analyses were performed by standardized methodology. In an analgesic assay, acetic acid-induced writhings were significantly inhibited by extract doses of 37.5 mg/kg (40.97%), 75 mg/kg (77.70%) and 150 mg/kg (88.98%). A central analgesia was also observed using T. catharinensis extract at all doses tested, particularly noticed at 60 and 90 min following administration. The extract significantly reduced edema development by 30.35% (37.5 mg/kg), 34.46% (75 mg/kg), and 56.42% (150 mg/kg) when assessed 180 min following carrageenan intraplantar injection, demonstrating an effective anti-inflammatory action. The LD50 value was 2200 mg/kg. Phytochemical analyses of ethanol extract from Tabernaemontana catharinensis stem bark showed the presence of alkaloids and terpenoids, which may be responsible for the observed pharmacological activities described in this work.

Fluoroquinolones reduce carrageenan-induced edema in rats and the involvement of the glucocorticoid receptor system

We studied the effect of fluoroquinolones (FQs) on carrageenan-induced edema in the rat footpad. Ciprofloxacin, gatifloxacin, sparfloxacin, norfloxacin, and enoxacin (s.c., 100 mg/kg), which have piperazinyl and/or cyclopropyl groups, inhibited carrageenan-induced edema, whereas levofloxacin, tosufloxacin, and pazufloxacin did not. The reduction of edema by ciprofloxacin, sparfloxacin, and enoxacin was abolished by pretreatment with mifepristone, an antagonist of the glucocorticoid receptor. These results suggest that FQs with piperazinyl and/or cyclopropyl groups can modify biological responses through enhancing the glucocorticoid-glucocorticoid receptor system.

Anti-inflammatory and anti-nociceptive effects of Zeyheria montana (Bignoniaceae) ethanol extract

In this work, the analgesic and anti-inflammatory activities of Zeyheria montana Mart. ethanol leaf extract were investigated at doses of 75, 150 and 300 mg/kg body weight. In the analgesic assay, against a chemical stimulus in mice, acetic acid-induced writhes were significantly inhibited by the extract at doses of 75 mg/kg (67.27%), 150 mg/kg (49.38%) and 300 mg/kg (82.87%). Also, a vigorous decrease in hyperalgesia was observed when measured after 2 h and 6 h of lipopolysaccharide stimulation of rats for all doses of extract tested. Z. montana extract, at doses of 75 and 300 mg/kg, caused very slight central analgesia in rats submitted to thermal stimulus, particularly noticeable at 30 min following treatment. The anti-inflammatory activity of Z. montana extract on carrageenan-induced oedema in rats was evaluated. The oedema development, measured at 180 min following carrageenan intraplantar injection, was significantly reduced by all tested doses: 75 mg/kg (33.30%), 150 mg/kg (45.80%) and 300 mg/kg (75.00%). The LD50 value was greater than 2000 mg/kg. These results demonstrated that the ethanol extract from Z. montana leaf possesses anti-nociceptive and anti-inflammatory activities, which could be of relevance for the pharmacological control of pain and inflammatory processes.

Synthesis and pharmacological evaluation of a novel series of 5-(substituted)aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines as novel anti-inflammatory and analgesic agents

A novel series of 5-(substituted)aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines ( 3a– l) were synthesized by reacting various substituted 3-aryl-1-(3-coumarinyl)propan-1-ones ( 2a– l) with phenylhydrazine in the presence of hot pyridine. Structures of all new synthesized compounds were characterized on the basis of elemental analysis and spectral data (IR, 1H NMR and 13C NMR). The title compounds were screened for in vivo anti-inflammatory and analgesic activities at a dose of 200 mg/kg b.w. Among the 12 prepared compounds, Compounds 3d, e, i and j exhibited significant anti-inflammatory activity in model of acute inflammation such as carrageenan-induced rat edema paw while compounds 3d and e showed considerable activity in model of chronic inflammation such as adjuvant-induced arthritis and were compared with diclofenac (13.5 mg/kg b.w.) as a standard drug. These compounds were also found to have significant analgesic activity in the acetic acid induced writhing model and antipyretic activity in yeast-induced pyrexia model along with minimum ulcerogenic index.

Comparative anti-inflammatory and antinociceptive effects of terpenoids and an aqueous extract obtained from Croton cajucara Benth

The 19-nor-clerodane trans-crotonin (CTN) and the triterpene acetyl aleuritolic acid (AAA), isolated from the stem bark of Croton cajucara Benth (Euphorbiaceae), a traditional medicinal plant from Amazon region of Brazil, as well as the aqueous extract (AE) from its stem bark, were submitted to pharmacological screening for anti-inflammatory and antinociceptive activities in animal models. The oral administration of AAA (50 mg/kg), CTN (50 mg/kg) or AE (300 mg/kg) inhibited the acetic acid-induced writhing in mice. The AE, CTN and AAA had shown significant inhibition of carrageenin-induced edema in rats, in all time intervals measured after the injection of the stimulus, with the greatest inhibition at the first hour for AAA (47.7%) and the second hour for CTN (54.4%). They have also exhibited significant inhibition in the dextran-induced edema 90 minutes after the stimulus: 31.9% for CTN and 28.5% for AAA. In the histamine-induced edema, the inhibition showed by CTN and AAA were 43.2% and 40.5%, respectively, 90 minutes after the injection of stimulus. This study extends and supports the popular medicine and folkloric uses of Croton cajucara in the Amazon region of Brazil.