Chronic Anti-inflammatory Effects Research Articles

Anti-inflammatory effect of the mixture of Ageratum conyzoides L. extract and eggshell membrane hydrolysates and in silico active compound predictions

Context: Ageratum conyzoides L. and eggshell membrane have the potential to be used as medicine. The independent use of A. conyzoides extract or eggshell membrane hydrolysates independently as a natural medicine has been widely known, but the mixture of the two as an anti-inflammatory has not been studied. Aims: To evaluate both the in vivo and in vitro anti-inflammatory effects of A. conyzoides extract and eggshell membrane hydrolysates, independently and in combination. In silico testing was conducted to identify chemicals that have a key role in inflammation signaling pathways. Methods: The chronic anti-inflammatory effects of A. conyzoides extract and eggshell membrane hydrolysates were evaluated on cotton pellet-induced rats using diclofenac-Na as a control. In vitro anti-inflammatory effects were studied via protein denaturation, membrane stability, and antiprotease activity. Furthermore, molecular docking was performed on the p38-MAPK signaling pathway using compounds found in A. conyzoides extract and eggshell membrane hydrolysates. Results: A. conyzoides extract and eggshell membrane hydrolysates given separately or in combination can inhibit the formation of exudates and granulomas. Molecular docking simulations showed that the metabolites in the extract and hydrolysate interact with p38-MAPK. Nobiletin in the extract is the potential metabolite that interacts with the p38-MAPK receptor with a free energy of binding and inhibition constant of -8.92 kcal/mol and 260.80 nM. Amino acids in the hydrolysates showed weaker interactions compared to the compound in the extract. Conclusions: A. conyzoides extract and eggshell membrane hydrolysates work additively to inhibit the severity of chronic inflammation.

Improved Anti-nociceptive, Anti-pyretic and Anti-inflammatory Effects of Orally Administered Liposome-encapsulated Piroxicam

Piroxicam, a nonsteroidal anti-inflammatory drug, has been shown with low oral bioavailability and delayed onset of its therapeutic effects. In this work, a promising nano/liposomal drug delivery system was exploited to improve the in vivo therapeutic efficacies of piroxicam. The current liposome-encapsulated piroxicam formulation effectively boosted and prolonged peripherally mediated anti-nociceptive activities in tests for abdominal writhing induced by acetic acid (inhibition of pain 70.19% was in mice treated with 30 mg/kg liposome-encapsulated piroxicam), paw licking induced by formalin (81.36% inhibition when compared to free unencapsulated piroxicam), and hyperalgesia induced by carrageenan (55.8% inhibition when compared to free unencapsulated piroxicam). Even lower dose of liposomes-encapsulated piroxicam was also significantly inhibit Brewer’s yeast-induced hyperthermia. Carrageenan-induced paw-edema test and cotton pellet-induced granuloma test revealed that liposomes-encapsulated piroxicam had significantly more potent acute and chronic anti-inflammatory effects than piroxicam, even if lower drug dosages were used to treat animals. A better modulation in the generation of inflammatory mediators (nitric oxide, tumour necrosis factor-α, interleukin-1β, and interleukin-10) at 18.02% (TNFa), 23.97% (IL-1β) and 10.27% (IL-10) inhibition when compared to 30mg/kg free piroxicam group respectively. was ascribed to the higher in vivo therapeutic actions. Present nano-encapsulated piroxicam also significantly enhanced the inhibition of cyclooxgenase-2 (total percentage inhibition was increased by 18.25% and 19.22% at drug dosage of 3 and 30 mg/kg, respectively), but not cyclooxgenase-1 enzyme. In conclusion, present study showed that liposomal drug formulation was able to improve the in vivo therapeutic effects of orally administered piroxicam.

Complete Freund’s adjuvant-induced arthritis in rats: Anti-inflammatory and antioxidant properties of Allanblackia gabonensis (guttiferae) aqueous extract

Objectives: Allanblackia gabonensis (Guttiferae) stem bark extract is generally used in Cameroonian traditional medicine for its beneficial activities as antibiotics, anti-inflammatory, and antinociceptive. However, the claimed chronic anti-inflammatory and antioxidant effects have not yet been largely elucidated scientifically. The present study was designed to evaluate the anti-inflammatory and antioxidant effects of A. gabonensis stem bark aqueous extract on Freund’s complete adjuvant (CFA)-induced arthritis in rats. Materials and Methods: Arthritis was induced by intradermal injection of CFA (0.1 mL) into the right hind paw of each rat. Pain relieving effects were measured in the treated animals using an analgesiometer and antioxidant activity determined by measuring oxidative stress parameters. In addition, the hematological index, serum nitric oxide (NO), and transaminase activities were evaluated in the experimental animals. Results: A. gabonensis significantly protected animals against pain from day 15 to 18 and decreased (P < 0.01) the paw edema from day 12 to the end of the experimentation (day 22). The number of white blood cells increased while the NO levels in serum and organs decreased in CFA animals as compared to the control group. An increase in serum transaminases was observed in the CFA group. A. gabonensis at the dose of 200 mg/kg significantly increased (36.36%) glutathione levels in the spleen in comparison with the CFA group. There was also a significant increase (P < 0.01) of liver and cardiac catalase in animals receiving extract at 100 and 200 mg/kg. Conclusion: Our findings revealed the anti-arthritic and antioxidant potential of A. gabonensis and, thus, validate its traditional claim.

Study on the anti-arthritic effects of Tinospora sinensis Merr.

The Tinospora sinensis Merr. was ultrasonically extracted using 80% ethanol at a temperature of 50°C. The resulting solution was distilled to remove the solvent under reduced pressure, yielding the extract. The extract was then dissolved in distilled water, and this solution was administered to the experimental mice. The results showed that even at the maximum allowable dose, no mice experienced mortality. The anti-inflammatory effects of Tinospora sinensis Merr. extract were tested in experiments. The results demonstrated that at a dose equivalent to 1.6 g of plant material per kilogram of body weight per day, the extract exhibited acute anti-inflammatory activity in a model of carrageenan-induced foot edema in mice, comparable to a dose of 80 mg/kg body weight per day of aspirin. Additionally, at a dose equivalent to 2.8 g of plant material per kilogram of body weight per day, the extract showed chronic anti-inflammatory effects in a model of amian-induced granuloma in white mice. These findings suggest a novel direction in using plant-derived medicines, specifically the Tinospora sinensis Merr.

The analgesic and anti-inflammatory effects of soursop leaf ethanol extract of Gnetum montanum Markgr. in vivo

This study was conducted to investigate evaluate the anti-inflammatory and analgesic effects of Gnetum montanum Markgr. extract. Methods: the anti-inflammatory effect was studied in two models of carragenin-in- duced paw edema and FCA-induced edema; the analgesic effect was studied on the model of colic pain and the Tail-immersion method. Results: In addition, the study also showed that at all 3 levels of tested doses, 150mg/kg, 250mg/kg and 500mg/kg Gnetum montanum Markgr extract exhibited acute and chronic anti-inflammatory effects, central analgesic and anti-inflammatory effects peripheral in experimental animals.

Rubiadin exerts an acute and chronic anti-inflammatory effect in rodents

Rubiadin is identified as a bioactive anthraquinone that exists in some quinone rich plants. The current research was carried out to evaluate the potential anti-inflammatory impact of Rubiadin in acute and chronic inflammation test models in rodents. The anti-inflammatory activity of Rubiadin was examined in cotton pellet-induced granuloma and carrageenan-induced edema as chronic and acute inflammation models in rats. TNF-α level and histopathological changes were assessed using sampled foot tissue of rat in the acute model. Also, the IL-1β level was assessed in the chronic model. One-way ANOVA (post hoc Tukey's) analysis was used for comparing the groups. Rubiadin (0.5 mg/kg, i.p.) induced a significant reduction in TNF α level and the paw edema compared to the control group in carrageenan test. Also, it was observed that the anti-inflammatory activity of Rubiadin (0.5 mg/kg, i.p.) is comparable to mefenamic acid (30 mg/kg, i.p.) as the standard drug. Rubiadin was effective in granuloma induced by cotton pellet concerning the granuloma and transudate formation amount. Rubiadin's anti-inflammatory effects were associated with a significant IL-1β decrease in this model. The results suggest that Rubiadin as a natural compound can possess significant peripheral anti-inflammatory impacts.

Further evidence to support acute and chronic anti-inflammatory effects of Nasturtium officinale.

Background and purpose:Previously, we reported the anti-inflammatory properties of Nasturtium officinale (watercress) in several models of acute inflammation. This study was designed to explore the effects of topical and systemic administrations of N. officinale in the two chronic inflammatory models and to evaluate the role of TNF-α and IL-1β in these effects.Experimental approach:Folin-Ciocalteu and aluminum chloride methods were used to estimate the extract’s total phenol and flavonoid content, respectively. Carrageenan-induced paw edema was carried out and TNF-α and IL-1β concentrations in the carrageenan-treated paw tissue were determined. Formalin injection into rat hind paws (7 days) and the application of 12-O-tetradecanoyl phorbol-13-acetate (TPA) on mouse ears (9 days) were used to simulate chronic inflammation. Furthermore, a histological assessment of the inflamed tissues was carried out.Findings/Results:The extract’s flavonoid and phenolic contents were 90.26 ± 4.81 mg rutin equivalents/g and 68 ± 8.16 gallic acid equivalents/g gallic acid, respectively. N. officinale pretreatment in all doses administered considerably decreased carrageenan-induced edema. The extract also reduced IL-1β levels in carrageenan- treated paws while did not affect TNF-α levels. Oral and topical administrations of N. officinale considerably reserved the paw and ear edema. The extract also ameliorated the tissue injuries due to formalin and TPA challenges.Conclusion and implications:The data confirmed the topical and systemic anti-inflammatory effects of watercress against two chronic models of inflammation. They suggested that these properties are not related to TNF-α but could be attributed to inhibition of IL-1β and inhibition of leukocyte infiltration.

Analgesic, anti-inflammatory and acute oral toxicity profile of leaf and bark extracts of Albizia procera

BackgroundPain and inflammation are associatory events in cancer, diabetes, cardiovascular diseases, arthritis and other chronic diseases. Corticosteroids, non-steroidal anti-inflammatory drugs exert potential side effects on long term use. This study was aimed to investigate the acute oral toxicity, anti-inflammatory and analgesic activities of leaf and bark extracts of Albizia procera in experimental animal models.MethodsEthyl acetate, ethanol, and hydroalcoholic extracts of Albizia procera (leaf and bark) were subjected for acute oral toxicity, anti-inflammatory and analgesic screening. Carrageenan and cotton pellet granuloma models were used to assess acute and chronic anti-inflammatory effects, respectively. Intraplanar formalin test was used to assess the analgesic activity.ResultsAll the extracts of Albizia procera were found to be well-tolerated up to 2000 mg/kg in female rats. Ethanolic leaf (ETLE) and bark (ETBE) of Albizia procera showed anti-inflammatory actions. But, only ETBE produced significant protection in chronic inflammation and analgesic activity.ConclusionIn summary, Albizia procera possess significant anti-inflammatory and analgesic properties. This study adds evidence on the traditional use of Albizia procera plant for treating painful inflammatory disorders.

Acute and Chronic Anti-inflammatory effect of Bryophyllum pinnatum Leaf Extract on Wistar Rats

Bryophyllum pinnatum (Lam.) Oken (Crassulaceae) is used traditionally to treat many ailments. This study investigated the anti-inflammatory effect of hydro-ethanol leaf extract of Bryophyllum pinnatum on Wistar rats using acute and chronic models and also evaluates the bioactive compounds of the leaf extract. The phytochemical constituents of the plant extract were quantitatively determined by Gas Chromatography-Flame Ionization Detector (GC-FID) and acute anti-inflammatory activity was carried out with the aid of plethysmometer while chronic anti-inflammatory activity was investigated using cotton pellet. Results showed that the leaf extract of B. pinnatum was rich in kaempferol (7.006 ±0.02 μg/g), sapogenin (3.372 ±0.02 μg/g), rutin (1.837 ±0.01 μg/g) and lunamarine (1.359 ±0.01 μg/g). The findings showed that the plant had considerable anti-inflammatory effects in a dose dependent manner, returning edema in carragenean-induced and cotton pellet induced granuloma in Wistar rats to normal within 120 minutes and 7 days respectively. The findings of this work have shown that the leaf of B. pinnatum was rich in bioactive compounds which could be synthesized to produce new plant based product to fight inflammatory disorders with fewer side effects.

Analgesic, anti-inflammatory and hypouricemic effects of GT1 film-coated tablets on experimental animals

Aim: To evaluate pain relief, anti-inflammatory and hypouricemic effects of GT1 tablets on experimental animals.
 Method: GT1 at the doses of 22.32 g/kg/day and 66.96 g/kg/day were evaluated for its analgesic effect in three models (hot plate, pain threshold, and acetic acid-induced writhing), its chronic anti-inflammatory effect in the granulomatous reaction model, and its hypouricemic effect in potassium oxonate-induced hyperuricemic mice. Acute anti-inflammatory effects of GT1 at the doses of 11.16 g/kg/day and 33.48 g/kg/day were evaluated in rats with two models: carrageenin-induced paw edema and peritonitis.
 Results: GT1 prolonged the temperature reaction time on the hot plate (22.73 s and 20.37 s at both doses of 22.32 g/kg and 66.96 g/kg, respectively, compared to 16.96 s in control group), reduced the number of acid acetic-induced writhing effects, decreased the weight of granulomas, and decreased the level of acid uric in blood and urine (p < 0.05). GT1 caused a significant reduction in paw edema after subplantar injection of carrageenan in rats (p < 0.05). Moreover, there was a substantial decline of GT1 at the dose of 11.16 g/kg/day in terms of the volume and the quantity of protein in the inflammation fluid of the peritonitis model (p < 0.05).
 Conclusion: GT1 at both doses of 11.16 g/kg/day and 33.48 g/kg/day posed acute anti-inflammatory effects on rats. GT1 at both doses of 22.32 g/kg/day and 66.96 g/kg/day exerted analgesic, chronic anti-inflammatory and hypouricemic effects on mice.

Anti-inflammatory and antinociceptive activities of Salvia keerlii

Background: Inflammation is a response to an attack on the body and is treated with several drugs that cause severe side effects. An alternative treatment source is plants, such as Salvia keerlii (SAKE) Benth. Objective: The objective is to study the determination of the anti-inflammatory and antinociceptive properties and chemical composition of the chloroform extract of SAKE. Materials and Methods: The plant was defatted with hexane, and then, chloroform and methanol extracts were obtained by heating, and the solvent was evaporated. The chemical composition of the extract was analyzed using gas chromatography–mass spectrometer. Total phenolic was determined using Folin–Ciocalteu reagent, and total flavonoid was determined by AlCl3assay. The acute and chronic anti-inflammatory effects of SAKE were evaluated on ear edema induced with 12-O-tetradecanoylphorbol-13-acetate, and the antinociceptive activity was determined. The effects of SAKE on protein denaturation and membrane stabilization were determined. The levels of nitric oxide, tumor necrosis factor-alpha (TNF-α), interleukin (IL)-1β, IL-6, and IL-10 were measured in J774A.1 macrophages stimulated with lipopolysaccharide. Results: SAKE at 2 mg/ear inhibited ear edema by 84.96% in the acute assay, whereas 100 and 200 mg/kg (p. o.) SAKE decreased inflammation in the chronic assay. In macrophages, SAKE decreased the levels of TNF-α (1.7-fold), IL-1β (1.7-fold), and IL-6 (1.9-fold) but increased the levels of IL-10 (1.9-fold). SAKE inhibited protein denaturation (IC50 =8.68 μg/mL). The inhibition of writhing obtained with SAKE at doses of 10, 50, 100, and 200 mg/kg was 28.73%, 46.48%, 56.1%, and 63.05%, respectively. Conclusions: SAKE has in vitro and in vivo anti-inflammatory and antinociceptive effects.

Anti-inflammatory activity of Jefea gnaphalioides (a. gray), Astereaceae

BackgroundInflammation is a symptom associated with many diseases. This symptom is treated with steroidal and non-steroidal anti-inflammatory drugs, which can cause severe side effects when used as long-term treatments. Natural products are an alternative source of new compounds with anti-inflammatory activity. Jefea gnaphalioides (Astereaceae) (A. Gray) is a plant species used to treat inflammatory problems, in Mexico. This study determined the anti-inflammatory activity and the composition of the methanol extract of Jefea gnaphalioides (MEJG).MethodsThe extract was obtained by heating the plant in methanol at boiling point for 4 h, and then the solvent was evaporated under vacuum (MEJG). The derivatization of the extract was performed using Bis-(trimethylsilyl) trifluoroacetamide, and the composition was determined by GC-MS.Total Phenols and flavonoids were determined by Folin-Ciocalteu AlCl3 reaction respectively.The antioxidant activity of MEJG was determined by DPPH method.The acute and chronic anti-inflammatory effects were evaluated on a mouse ear edema induced with 12-O-Tetradecanoylphorbol-13-acetate (TPA).Acute oral toxicity was tested in mice at doses of MEJG of 5000, 2500 and 1250 mg/kg.The levels of NO, TNF-α, IL-1β and IL-6 were determinate in J774A.1 macrophages stimulated by Lipopolysaccharide. The production of inflammatory interleukins was measured using commercial kits, and nitric oxide was measured by the Griess reaction.ResultsThe anti-inflammatory activity of MEJG in acute TPA-induced ear edema was 80.7 ± 2.8%. This result was similar to the value obtained with indomethacin (IND) at the same dose (74.3 ± 2.8%). In chronic TPA-induced edema at doses of 200 mg/kg, the inhibition was 45.7%, which was similar to that obtained with IND (47.4%). MEJG have not toxic effects even at a dose of 5000 mg/kg. MEJG at 25, 50, 100 and 200 μg/mL decreased NO, TNF-α, IL-1β and IL-6 production in macrophages stimulated with LPS.The major compounds in MEJG were α-D-Glucopyranose (6.71%), Palmitic acid (5.59%), D-(+)-Trehalose (11.91%), Quininic acid (4.29%) and Aucubin (1.17%). Total phenolic content was 57.01 mg GAE/g and total flavonoid content was 35.26 mg QE/g MEJG had antioxidant activity.ConclusionsMEJG has anti-inflammatory activity.

Anti-inflammatory activity and chemical composition of Pycnocycla bashagardiana fruit's essential oil in animal models.

Objective(s):Pycnocycla bashagardiana is an endemic species found only in Iran. Due to the presence of myristicin as the major component of the fruit’s oil we were prompted to assess the antinociceptive and anti-inflammatory properties of P. bashagardiana fruit’s essential oil (PBFEO).Materials and Methods:The analgesic activities of PBFEO (100, 200, and 400 mg/kg, IP) were studied by hot-plate and formalin tests in mice. Control and standard groups received vehicle and morphine (5 mg/kg, IP), respectively. The acute anti-inflammatory effect of PBFEO (200 and 400 mg/kg, IP) were assessed by carrageenan-induced paw edema method in 30 min, 1, 2, 3, and 4 hr after carrageenan injection and the chronic anti-inflammatory effect of PBFEO (50 and 100 mg/kg, IP) were assessed by the cotton pellet-induced granuloma method in rats.Results:In hot-plate and formalin tests, the studied doses of PBFEO were not effective. However, in carrageenan test, all studied doses of PBFEO significantly reduced the paw edema in comparison to the control animals (P<0.05). Anti-inflammatory activity of PBFEO (200 and 400 mg/kg, P<0.05) was found to be more than mefenamic acid (30 mg/kg). In cotton pellet-induced granuloma, PBFEO was also effective regarding the transudate and granuloma formation amount. PBFEO was analyzed by gas chromatography-mass spectrometry and 12 constituents, representing 96.0% of the oil, were identified. The major component of the oil was characterized as myristicin which might be responsible for the anti-inflammatory activity.Conclusion:The results suggest that PBFEO possesses biologically active constituents that have significant peripheral anti-inflammatory effects.

Anti-inflammatory activity of Elaeagnus angustifolia fruit extract on rat paw edema.

The Elaeagnus angustifolia fruit has been traditionally used in Iranian herbal medicine to treat diarrhea and rheumatoid arthritis. In the present study, the effects of E. angustifolia fruit extract on the acute and chronic phases of formalin-induced rat paw edema were examined. The acute and chronic anti-inflammatory effects of E. angustifolia fruit extract were investigated through the subcutaneous injection of 100 μL of formalin (2.5%) into a rat's hind paw. Thirty minutes before the procedure, the experimental groups were treated intraperitoneally with hydroalcoholic fruit extracts of E. angustifolia (concentrations of 100, 300, 700, and 1000 mg/kg); sodium salicylate (SS, 400 mg/kg) and distilled water were used as positive and negative control groups, respectively. Treatment with SS and the fruit extracts were performed daily for 8 days, and the degree of edema was measured by using mercury plethysmometer and digital caliper. In the acute anti-inflammatory study, the extract showed a significant anti-inflammatory effect in a dose-dependent manner. The results of 1000 mg/kg of the extract was significantly different compared with the negative control group (p<0.05) and was comparable to sodium salicylate (p<0.05). Results from the chronic study suggested that E. angustifolia extract significantly reduced paw edema and inflammation in a dose-dependent manner. The results also showed that the measurement by digital caliper and mercury plethysmometer were both reliable and might be applied interchangeably (p<0.01). Phytochemical tests indicated that the hydroalcoholic fruit extract of E. angustifolia was positive for cardiac glycosides, flavonoids, terpenoids, and saponins. Based on our findings, the E. angustifolia fruit extract probably has acute and chronic anti-inflammatory activities to support its applications in folk medicine.

Pulmonary anti-inflammatory effects and spasmolytic properties of Costa Rican noni juice (Morinda citrifolia L.)

Ethnopharmacological relevanceMorinda citrifolia L. (Noni) is a medicinal plant used in Polynesia for many properties such as anti-inflammatory, anti-diabetic and antineoplastic effects. Recent studies showed that noni juice have anti-oxidant and acute anti-inflammatory activities likely due to polyphenols, iridoids and vitamin C content. The present study was undertaken to evaluate chronic anti-inflammatory and spasmolytic effects of noni juice. Materials and methodsTherefore, we evaluated the effect of oral or intraperitoneal administrations of noni juice in vivo on the lung inflammation in ovalbumin (OVA) sensitized Brown Norway rat (with prednisolone 10mg/kg intraperitoneously as reference compound) and the ex vivo effect of noni juice on BaCl2 (calcium signal) or methacholine (cholinergic signal) induced spasms in jejunum segments. ResultsWe found that noni juice (intraperitoneously 2.17mL/kg and orally 4.55mL/kg) reduced the inflammation in OVA-sensitized Brown Norway rat with regard to the decreased number of inflammatory cells in lung (macrophages minus 20–26%, lymphocytes minus 58–34%, eosinophils minus 53–30%, neutrophils minus 70–28% respectively). Noni juice demonstrated a dose-dependent NO scavenging effect up to 8.1nmol of nitrites for 50µL of noni juice. In addition noni juice inhibited (up to 90%) calcium and cholinergic induced spasms on the jejunum segments model with a rightward shift of the concentration response curve. ConclusionWe describe for the first time that noni juice demonstrate (1) a chronic anti-inflammatory activity on sensitized lungs along with (2) a spasmolytic effect integrating a calcium channel blocker activity component.

ANTI-IFLAMMATORY EFFECTS OF GRANULES OF TIEN LIET THANH GIAI ON EXPERIMENTAL ANIMAL MODELS

Acute and chronic anti-inflammatory effects of granules of Tien liet thanh giai were evaluated. For acute anti-inflammatory effect, granules of Tien liet thanh giai didn’t change the test indicators. In the chronic inflammation model, granules of Tien liet thanh giai remarkably provoked chronic anti-inflammatory effect through significantly decreasing granuloma weight as compared with the control group. key words: granules of Tien liet thanh giai, acute anti-inflammatory effect, chronic anti-inflammatory effect.

A Novel Anti-Inflammatory Effect for High Density Lipoprotein.

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.

Synthesis and evaluation of the anti-nociceptive and anti-inflammatory activity of 4-aminoquinoline derivatives

In this paper, we describe the synthesis and pharmacological evaluation of a series of 4-aminoquinolines. The compounds were characterised and tested in models of pain and inflammation, using the writhing test with acetic acid, formalin test, peritonitis test by zymosan and arthritis test with Freund’s adjuvant complete assay. The results revealed that all of the 4-aminoquinolines that were prepared promoted anti-nociceptive activity as well as acute and chronic anti-inflammatory effects, with marked activity in the derivates labelled with BAQ and 7-CF3-MAQ. After 7days of treatment, 7-CF3-MAQ did not induce significant hepatotoxicity, gastrotoxicity or nephrotoxicity.

Analgesic and anti-inflammatory activities of Citrus aurantium L. blossoms essential oil (neroli): involvement of the nitric oxide/cyclic-guanosine monophosphate pathway.

The analgesic and anti-inflammatory properties of Citrus aurantium L. blossoms essential oil (neroli) were investigated in mice and rats. The analgesic activity of neroli was assessed by acetic acid-induced writhing and Eddy's hot plate methods, while acute and chronic anti-inflammatory effects were investigated by inflammatory paw edema in rat and the cotton pellet-induced granuloma tissue model, respectively. Mechanistic studies were conducted using L-nitro arginine methyl ester (L-NAME), an inhibitor of NO synthase. Neroli significantly decreased the number of acetic acid-induced writhes in mice compared to animals that received vehicle only. Also, it exhibited a central analgesic effect, as evidenced by a significant increase in reaction time in the hot plate method. The oil also significantly reduced carrageenan-induced paw edema in rats. The inhibitory activity of neroli (especially at 40mg/kg) was found to be very close to the standard drug, diclofenac sodium (50mg/kg). In cotton pellet-induced granuloma, neroli was effective regarding the transudate and granuloma formation amount. Neroli was analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) and twenty-three constituents, representing 91.0% of the oil, were identified. The major components of neroli were characterized as linalool (28.5%), linalyl acetate (19.6%), nerolidol (9.1%), E,E-farnesol (9.1%), α-terpineol (4.9%), and limonene (4.6%), which might be responsible for these observed activities. The results suggest that neroli possesses biologically active constituent(s) that have significant activity against acute and especially chronic inflammation, and have central and peripheral antinociceptive effects which support the ethnomedicinal claims of the use of the plant in the management of pain and inflammation.

Evaluation of anti-inflammatory activity of methanolic extract of leaves of Bougainvillea spectabilis in experimental animal models.

Background:Bougainvillea spectabilis (BS) (family Nyctaginaceae) is said to possess hypoglycemic and anti-inflammatory activities in experimental animals. We had set forward to examine the potential anti-inflammatory activities of BS in experimental models of inflammation.Materials and Methods:Fresh dried leaves from the flowering plant of BS were collected from the local area during the flowering season and air dried (215.00 g). Methanol was extracted, and the solvent was removed on a rotary evaporator under reduced pressure. The extract was freeze-dried (lyophilized) and the yield was 8 g. This was used as an emulsion prepared in propylene glycol and orally administered (20 and 50 mg/kg). Acute anti-inflammatory activity of BS was evaluated using carrageenan and dextran whereas chronic anti-inflammatory (immunoregulatory) activity was evaluated by Freund's adjuvant-induced arthritis model.Results:BS (20 mg/kg and 50 mg/kg) had shown significant anti-inflammatory effects 20.6% and 67.6%, respectively, on carrageenan-induced acute inflammatory models. In dextran-induced edema, the effect was 30% and 66%, respectively. The standard drug indomethacin (87.3% and 91.5%, respectively) showed better inhibitory response in both models. In arthritic model 50 mg/kg of BS showed significant chronic anti-inflammatory effect (38.46%) in comparison to the standard drug dexamethasone (84.6%).Conclusion:Our data indicate that the methanol extract of BS (50 mg/kg) leaves has significant anti-inflammatory and immunoregulatory activity. Further studies involving isolation of active principles will help to pinpoint the mechanisms contributing to the observed activities of BS.