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OBJECTIVE: The present study was aimed at investigating the antinociceptive and anti-inflammatory activities of the solvent fractions of the roots of Echinops kebericho Mesfin in rodent models of pain and inflammation. METHODS: Successive maceration was used as a method of extraction using solvents of increasing polarity: methanol and water. Ethyl acetate, chloroform and distilled water were used as solvents of the fraction process. Swiss albino mice models were used in acetic acid induced writhing, hot plate, carrageenan induced paw edema and cotton pellet granuloma to assess the analgesic and anti-inflammatory activities. The test groups received different doses (100 mg/kg, 200 mg/kg and 400 mg/kg) of the three fractions (chloroform, ethyl acetate and aqueous). The positive control groups received ASA (150 mg/kg) for the writing test, morphine (10 mg/kg) for the hot plate method, diclofenac Na for carrageenan-induced paw edema, and dexamethasone (10 mg/kg) for granuloma, while the negative control group received distilled water. RESULTS: EA fraction at all test doses employed (100 mg/kg, 200 mg/kg, and 400 mg/kg) showed statistically significant (p<0.05, p<0.01, p<0.001 respectively) analgesic and anti-inflammatory activities in a dose-dependent manner. The AQ fraction on the other hand produced statistically significant (p<0.05, p<0.012) analgesic and anti-inflammatory activities at the doses of 200 mg/kg and 400 mg/kg, while the CH fraction exhibited statistically significant (p<0.05) analgesic and anti-inflammatory activity at the dose of 400 mg/kg. CONCLUSIONS: In general, the data obtained from the present study elucidated that the solvent fractions of the study plant possessed significant analgesic and anti-inflammatory activities and were recommended for further investigations.

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The present study was designed to investigate the anti-inflammatory potential of Amycolatopsis thermoflava producing 1-O-methyl chrysophanol (OMC), a member of the hydroxyanthraquinone family. The anti-inflammatory potential was evaluated initially through in silico analysis against tumor necrosis factor- α and cyclooxygenase-2. The same activity was further confirmed based on the in vitro protein denaturation method as well as in vivo by a carrageenan-induced paw edema model in rats. The OMC compound was isolated, purified, and characterized from the fermentation broth of Amycoloptosis thermoflava. In vitro data revealed that the OMC possesses significant protein denaturation properties with an IC50 of 63.50±2.19 µg/ml higher than the standard drug, with an IC50 value of 71.42±0.715 µg/ml. The percentage of inhibition in paw swelling was observed to be 40.03±5.5 in OMC-treated group, which is comparable to the standard group (52.8±4.7). The histopathological evaluation and immunohistochemistry revealed the anti-inflammatory potential of OMC.

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Background: The roots of Impatiens rothii has been used as a traditional remedy for painful conditions, rheumatism, isthmus and crural aches. However, the analgesic and anti-inflammatory properties of this plant have yet to be scientifically confirmed. The purpose of this study was to explore possible analgesic and anti-inflammatory activities 80% methanolic root extract of Impatiens rothii. Methods: To obtain the crude extract, the roots of Impatiens rothii that had been dried and ground up were macerated in 80% methanol. The analgesic activity was determined using acetic acid-induced writhing and hot plate tests in mice, whereas the anti-inflammatory activity was analyzed using carrageenan-induced paw edema model in rats. The extract was orally administered at a dose of 100, 200 and 400 mg/kg. Results: All tested doses of Impatiens rothii extract showed significant analgesic activity (p<0.05) at observations of 30 to 120 minutes compared to the negative control in the hot plate test. In acetic acid-induced writhing test all tested doses of the 80% methanol extract of Impatiens rothii significantly (p < 0.001) reduced the number of writhing. In comparison to the control group, all tested doses displayed a significant decrease in paw edema, which appeared 2-5 hours after induction (p<0.05). Conclusion: From the results of this study, it can be stated that 80% methanolic extract of Impatiens rothii possessed substantial analgesic and anti-inflammatory activities, hence providing scientific basis for the use of this plant in the treatment of pain and inflammatory diseases.

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Background: Ethnobotanical studies in various districts of Ethiopia reported that Ehretia cymosa (E. cymosa) is used for the management of headache, abdominal pain, arthritis and rheumatism. However, there is no scientific investigation done so far to confirm these traditional claims. Thus, the aim of this study was to assess the analgesic and anti-inflammatory effects of the 80% methanol extract and fractions of E. cymosa leaves. Methods: The dried and pulverized leaves of E. cymosa were soaked with 80% methanol to obtain a crude extract. Fractionation was done using chloroform, ethyl acetate and water by a soxhlet apparatus. The analgesic effects of the crude extract and solvent fractions were assessed using acetic acid-induced writhing and hot plate tests whereas anti-inflammatory activities were investigated using carrageenan-induced paw edema and cotton-pellet-induced granuloma models. Results: In all the tested doses, the 80% methanol extract and solvent fractions revealed substantial (p < 0.001) analgesic activities in acetic acid induced writhing test. In the hot plate method, all the tested doses of E. cymosa crude extract and the solvent fractions produced significant analgesic activities (p < 0.05). In the carrageenan-induced acute inflammation model, all tested doses of the crude extract and solvent fractions resulted in a significant decline in paw edema. The 80% methanol extract and solvent fractions of E. cymosa at all the tested doses significantly reduced inflammatory exudates and granuloma mass formations (p < 0.001). Conclusion: From the results of this investigation, it can be stated that 80% methanol extract, aqueous, ethyl acetate and chloroform fractions of E. cymosa exhibited considerable analgesic and anti-inflammatory activities, supporting the plant's traditional use as a remedy for a variety of painful and inflammatory conditions.

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OBJECTIVE: This study aims to investigate the anti-inflammatory mechanism of monoamine oxidase inhibitor (MAOI) in carrageenan (CARR) induced inflammation models to reprofile their use. We also aimed to explore the role of monoamine oxidase (MAO)-mediated H2O2-NF-κB-COX-2 pathway in acute inflammation. METHODS: In vitro anti-inflammatory activity and hydrogen peroxide (H2O2) scavenging activity were performed according to the established procedure. Inflammation was induced using CARR in BALB/c mice at the foot paw and peritoneal cavity. Hourly measurement of paw swelling was performed. The level of nitric oxide (NO), myeloperoxidase (MPO), cyclooxygenase-2 (COX-2), prostaglandin E2 (PGE2) and nuclear factor κB (NF-κB) was determined using enzyme-linked immunosorbent assay (ELISA). Peritoneal fluid was collected to investigate total count, differential count of leukocytes, and capillary permeability. RESULTS: In vitro anti-inflammatory evaluations revealed the potential role of MAOI to inhibit heat-induced protein denaturation and human red cell membrane destabilization. H2O2 inhibition activity of MAOI also proved their powerful role as an H2O2 scavenger. Treatment with MAOI in CARR-induced mice significantly reduced paw edema, leukocyte extravasation, and total and differential leukocyte count. The result of ELISA showed MAOI effectively reduce the level of COX-2, PGE2 and NF-κB in inflamed tissue. CONCLUSIONS: In short, this study demonstrates that inhibition of H2O2 by MAOI alleviates CARR-induced paw edema possibly by inhibiting the H2O2-mediated NF-κB-COX-2 pathway. The present investigation identifies MAOI might reprofile for the treatment of acute inflammation also, the MAO enzyme may use as a novel therapeutic target to design and develop new class of anti-inflammatory agents.

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Dexamethasone (Dex) is a popular and highly potent anti-inflammatory drug, frequently used to treat a wide range of inflammatory disorders. However, the existing oral and parenteral delivery modes have several limitations, including systemic adverse effects and reduced patient compliance. This study aimed to develop a biodegradable microneedle (MN)-based transdermal delivery system capable of sustained, safe and effective delivery of Dex. A Quality by Design (QbD) approach was applied to design the Dex-loaded MN arrays. The formulation variables were optimized using a central composite design (CCD) model, generated with the statistical software package Design- Expert®. The optimized MNs were sharp, with heights ranging between 800 and 900 µm, appropriate for transdermal delivery. The MN arrays did not exhibit any cytotoxic effects on the fibroblast and keratinocyte cells. Moreover, the ex vivo studies confirmed the enhanced efficacy of MN-mediated skin permeation of Dex compared to passive permeation of drug solution. Finally, the in vivo anti-inflammatory efficacy was investigated using the carrageenan-induced rat paw edema model. The efficacy of the MN arrays to inhibit paw edema formation was found to be comparable to that of intravenous Dex injection and significantly greater than topical solution. Cytokine analysis also revealed that application of MN arrays downregulated the expressions of pro-inflammatory cytokines and upregulated the expressions of anti-inflammatory cytokines. Overall, the findings suggest that MN array could be a safe, easy, effective and minimally invasive alternative to the existing means of Dex delivery and could potentially be used for the treatment of inflammatory disorders.

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Background: The leaves of V. auriculifera has been used traditionally for the treatment of inflammatory disorders, and pain in various parts of Ethiopia. However, to our knowledge, the analgesic and anti-inflammatory activity of the crude extract and solvent fractions has never been experimentally studied. Objective: To assess the analgesic and anti-inflammatory activities of V. auriculifera leaf extract and solvent fractions in rodent models. Material and methods: Air-dried leaves of V. auriculifera were grounded and macerated using 80% methanol. The air-dried, grounded leaves were also successively extracted with ethyl acetate, and methanol. The residue was then macerated in water for 72 hr. The extract's peripheral analgesic activity, as well as the solvent fractions, were determined using an acetic acid-induced writhing test. The hot plate model was used to assess the central analgesic effect. Carrageenan-induced hind paw edema and cotton pellet-induced granuloma models were used to assess the anti-inflammatory effect in rats. Results: The 80% methanol leaf extract and solvent fractions have demonstrated significant (p < 0.05) peripheral and central analgesic activity. Both 80% methanol leaf extract and solvent fractions of V. auriculifera were found to have anti-inflammatory activity in a carrageenan-induced rat paw edema model. In the cotton pellet-induced granuloma model, all concentrations of 80% methanol leaf extract (ME), methanol fraction (MEF), and aqueous fractions (AQF) of V. auriculifera inhibited exudate and granuloma formation. Although all tested doses significantly inhibited granuloma mass formation, only the medium and highest ethyl acetate fraction (EAF) doses significantly inhibited the generation of inflammatory exudate. Conclusion: This study's findings indicate that the solvent fractions and 80% methanol extract of V. auriculifera have analgesic and anti-inflammatory properties. This study's findings not only confirm the plants' traditional claim but also provide clues for further investigation of the active principles of this plant for the development of effective and safe analgesic and anti-inflammatory drugs.

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ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal properties of hyssop have been used in traditional medicine since ancient times, inter alia, in diseases/conditions with an inherent inflammatory process. AIM OF THE STUDY: Accordingly, the aim of this study was to investigate the anti-inflammatory properties of hyssop herb preparations (essential oil and methanol extracts) in vivo, in vitro and in silico. MATERIALS AND METHODS: For in vitro testing of essential oils and extracts of hyssop herb, the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme assays were used. In vivo anti-inflammatory potential of the extracts (at doses of 50, 100 and 200 mg/kg) was assessed using the carrageenan-induced rat paw edema test. Molecular docking and dynamics were used for in silico testing of the inhibitory activity of chlorogenic (CA) and rosmarinic (RA) acids, as the dominant compounds in the tested methanol extracts against COX-1 and COX-2 enzymes. RESULTS: Significant inhibitory activity was shown in the COX-2 test regarding extracts (essential oils did not exhibit any significant activity). Namely, all analyzed extracts, at a concentration of 20 µg/mL, showed a percentage of inhibition of COX-2 enzyme (54.04-63.04%), which did not indicate a statistically significant difference from the positive control of celecoxib (61.60%) at a concentration of 8.8 µM. In vivo testing showed that all methanol extracts of hyssop herb, at the highest test dose of 200 mg/kg in the third and fourth hours, after carrageenan administration, exhibited a statistically significant (p < 0.05) inhibitory effect on the increase in rat paw edema in relation to control. This activity is comparable or higher in relation to the reference substance, indomethacin, at a concentration of 8 mg/kg. The preliminary in silico results suggest that investigated compounds (RA and CA) showed better inhibitory activity against COX-1 and COX-2 than standard non-steroidal anti-inflammatory drug (NSAID), ibuprofen, as evident from the free binding energy (ΔGbind in kJ mol-1). The binding energies of the docked compounds to COX-1 and -2 were found to be in the range between -47.4 and -49.2 kJ mol-1. Ibuprofen, as the one NSAID, for the same receptors targets, showed remarkably higher binding energy (ΔGbind = -31.3 kJ mol-1 to COX-1, and ΔGbind = -30.9 kJ mol-1 to COX-2). CONCLUSION: The results obtained not only support the traditional use of hyssop herb in inflammatory conditions in folk medicine, but also open the door to and the need for further in vivo testing of extracts in order to examine the molecular mechanism of anti-inflammatory activity in living systems and possibly develop a new anti-inflammatory drug or supplement.

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Rheumatoid arthritis (RA) is a chronic inflammatory illness affecting the joints. The characteristic of RA is gradual joint deterioration. Current RA treatment alleviates signs such as inflammation and pain and substantially slows the progression of the disease. In this study, we aimed to boost the transdermal delivery of berberine (a natural product) by encapsulating it in chitosan, surface-modified bilosomes nanogel for better management of the inflammation of RA. The chitosan-coated bilosomes loaded with berberine (BER-CTS-BLS) were formulated according to the thin-film hydration approach and optimized for various causal variables, considering the effect of lipid, sodium deoxycholate, and chitosan concentrations on the size of the particles, entrapment, and the surface charge. The optimized BER-CTS-BLS has 202.3 nm mean diameter, 83.8% entrapment, and 30.8 mV surface charge. The optimized BER-CTS-BLS exhibited a delayed-release profile in vitro and increased skin permeability ex vivo. Additionally, histological examination revealed that the formulated BLS had no irritating effects on the skin. Furthermore, the optimized BER-CTS-BLS ability to reduce inflammation was evaluated in rats with carrageenan-induced paw edema. Our results demonstrate that the group treated with topical BER-CTS-BLS gel exhibited a dramatic reduction in rat paw edema swelling percentage to reach 24.4% after 12 h, which was substantially lower than other groups. Collectively, chitosan-coated bilosomes containing berberine have emerged as a promising therapeutic approach to control RA inflammation.

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Rice cake is a traditional food in Korea, and is made by rice alone, or with other grain powder. To improve the health benefits of fermented rice cake, the rice powder was supplemented with strawberry powder. Anti-inflammatory activities of the mixture of strawberry and rice powder were evaluated. Treatment with the mixture significantly decreased the production of nitric oxide (NO). The mixture of strawberry and rice powder in the ratio 10: 90 effectively and dose-dependently reduced the immune-associated genes iNOS, IL-1ß, IL-6, COX-2, and TNF-α. Furthermore, carrageenan-injected mice were used to study the anti-inflammatory effect of the mixture. Pre-oral administration of the mixture of strawberry and rice powder at doses of 50 and 100 mg/kg BW significantly reduced paw edema induced by carrageenan. These results suggest that for fermented rice cake production and processing, the strawberry and rice powder mixture may be a potential source of anti-inflammatory activity.

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INTRODUCTION: The various fractions of leaves of Achyranthes aspera L. (A. aspera) have not yet been explored scientifically for in-vivo wound healing and anti-inflammatory activities. The objective of this study was, therefore, to evaluate in-vivo wound healing and anti-inflammatory activities of solvent fractions of 80% methanol leaf extract of A. aspera in rats. METHODS: The 80% methanol leaf extract of A. aspera was fractionated with chloroform, n-butanol and water. Wound healing and anti-inflammatory activities were evaluated using excision and incision wound models, rat paw edema and cotton pellet-induced granuloma models, respectively. For wound healing activity, fractions were evaluated at 5 and 10% ointments. The positive control groups were treated with nitrofurazone 0.2% ointment. Simple ointment treated for excision wound model and untreated for incision wound model rats were assigned as negative controls. For anti-inflammatory activity, fractions were evaluated at 100, 200 and 400mg/kg. Positive control groups were treated with indomethacin 10mg/kg for both rat paw edema and cotton pellet-induced granuloma models. The 2% Tween 80 treated rats were assigned as negative controls for both anti-inflammatory activity models. All groups comprised of 6 rats and treatment administrations were made topically and orally for evaluation of wound healing and anti-inflammatory activities. RESULTS: The 10% w/w chloroform fraction ointment revealed a high percentage of wound contraction and reduced period of epithelialization (p <0.01). Chloroform fraction was also found to be the most active fraction, which demonstrated the maximum percentage inhibition of edema (52.50%; p <0.01) and transudative and proliferative component of chronic inflammation (37.52 and 52.81%; p <0.01), which was comparable to indomethacin. CONCLUSION: Data obtained from this study collectively indicated that a chloroform fraction of 80% methanol leaf extract of A. aspera possessed significant wound healing and anti-inflammatory activities.

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BACKGROUND: NSAIDs are the most widely prescribed medications worldwide for their anti-inflammatory, antipyretic, and analgesic effects. However, their chronic use can lead to several adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastrosparing NSAIDs also suffer from serious adverse effects which limit their efficacy. OBJECTIVE: Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine, etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant) potential. METHODS: The designing process utilized three dimensional similarity studies and utilized an isoxazole core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity. The compounds were assayed for their anti-inflammatory activity in established in vivo models. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. RESULTS: Compounds 5, 6, 9 and 10 showed antiinflammatory activity comparable to the standard drugs and were also found to be non-ulcerogenic at the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0- 50.0 µmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good oral absorption. CONCLUSION: A new series of isoxazole based compounds is being reported with good antiinflammatory activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.

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Curcumin diglutaric acid (CurDG), an ester prodrug of curcumin, has the potential to be developed as an anti-inflammatory agent due to its improved solubility and stability. In this study, the anti-inflammatory effects of CurDG were evaluated. The effects of CurDG on inflammatory mediators were evaluated in LPS-stimulated RAW 264.7 macrophage cells. CurDG reduced the increased levels of NO, IL-6, and TNF- α, as well as iNOS and COX-2 expression in cells to a greater extent than those of curcumin, along with the potent inhibition of MAPK (ERK1/2, JNK, and p38) activity. The anti-inflammatory effects were assessed in vivo by employing a carrageenan-induced mouse paw edema model. Oral administration of CurDG demonstrated significant anti-inflammatory effects in a dose-dependent manner in mice. The effects were significantly higher compared to those of curcumin at the corresponding doses (p < 0.05). Moreover, 25 mg/kg curcumin did not exert a significant anti-inflammatory effect for the overall time course as indicated by the area under the curve data, while the equimolar dose of CurDG produced significant anti-inflammatory effects comparable with 50, 100, and 200 mg/kg curcumin (p < 0.05). Similarly, CurDG significantly reduced the proinflammatory cytokine expression in paw edema tissues compared to curcumin (p < 0.05). These results provide the first experimental evidence for CurDG as a promising anti-inflammatory agent.

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Phytochemical investigation of the ethanolic extract of Glandularia x hybrida roots resulted in the isolation and identification of five previously undescribed saponins, 3-O-ß-ᴅ-xylopyranosyl-hederagenin-28-O-ß-ᴅ-glucopyranosyl (1→2)-O-ß-ᴅ-glucopyranosyl ester, 3-O-ß-ᴅ-xylopyranosyl-hederagenin-28-O-ß-ᴅ-glucopyranosyl (1→2)-[ß-ᴅ-glucopyranosyl (1→6)]-ß-ᴅ-glucopyranosyl ester, hederagenin-28-O-ß-ᴅ-glucopyranosyl (1→2)-[ß-ᴅ-glucopyranosyl (1→6)]-ß-ᴅ-glucopyranosyl ester, 23-O-acetyl-3-O-ß-ᴅ-xylopyranosyl-pomolic acid-28-O-ß-ᴅ-glucopyranosyl ester, and 23-O-acetyl-pomolic acid-3-O-ß-ᴅ-xylopyranoside, along with eleven structurally diverse compounds. The structural characterizations of the isolated compounds were determined using physical data, comprehensive 1D and 2D NMR spectral analysis, and HRESIMS. All isolated saponins are hederagenin or pomolic acid glycosides conjugated with differentiable sugar units bound to C-3 and/or C-28 of the aglycone through ether and/or ester glycosidic linkages, respectively. Structural diversity of these isolated secondary metabolites would have a great impact on the future chemosystematic studies of this plant. Four saponins, obtained in good yield were evaluated for their anti-inflammatory activities in a rat model using the carrageenan-induced paw edema protocol. Two of these exhibited significant anti-inflammatory activities demonstrated through inhibition of the paw edema by 64 and 60%.

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BACKGROUND: "Opuntia ficus-indica" (prickly pear) is the cactus member of the Cactaceae family as an important nutrient and food source. OBJECTIVE: The purpose of this study was to characterize the phytochemical composition of hydroalcoholic extract of prickly pear seeds that cause therapeutic effects. METHODS: Phytochemical screening based on simple tests and determination of secondary metabolites were performed by High-Performance Liquid with Diode-Array Detection (HPLC-DAD) analysis. For the pharmacological studies, the anti-inflammatory activity in rats was evaluated by carrageenaninduced inflammation, the description of the sedative activity was carried to the following behavioural tests, and the analgesic effect of the extract was assessed by the resistance induced by acetic acid, and the tail immersion test in mice. RESULTS: The test drug at 500 mg/kg dose showed a significant increase in mean latency in the TAIL FLICK test, and a decrease in the average number of twisting movements in the KOSTER test, thus, a significant anti-inflammatory activity in the pattern of paw edema induced by carrageenan, and an important sedative effect on the central nervous system. CONCLUSION: These data suggest that the seeds of the cactus "Opuntia ficus-indica" could be a potential source of natural compound and reveal that the hydroethanolic extract of this species is a promising source, as well as a therapeutic agent for the research of new natural active ingredients.

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Triterpenes possess anti-inflammatory and anti-nociceptive effects. In this study anti-inflammatory activities of Asparacosin A were evaluated' using in-vitro cyclooxygenases 1 and 2 (COX-1/2) inhibition assays. Moreover, anti-nociceptive activities were assessed in-vivo by carrageenan-induced paw edema test, xylene-induced ear edema tests, and acetic acid-induced writhing and formalin tests. Additionally molecular docking was conducted to elucidate the binding mechanism of the compound and to correlate the in-vitro findings with the in-silico data. Oral administration of Asparacosin A at the doses of 10, 20, and 40 mg/kg induced significant anti-inflammatory effects (*p < 0.05, **p < 0.01, and ***p < 0.001) in a dose-dependent manner in both models. Asparacosin A also inhibited the human recombinant COX-2 enzyme and caused a dose-dependent decrease in the levels of TNF-α, IL-1ß, and PGE2 in the carrageenan-induced paws. Moreover, Asparacosin A displayed significant anti-nociceptive effects (*p < 0.05, **p < 0.01, ***p < 0.001) at the doses of 10, 20, and 40 mg/kg in acetic-acid induced writhing test. However, in formalin test, Asparacosin A (10-40 mg/kg, p.o) produced anti-nociceptive effects only in the late phase, similar to the effect observed with the reference drug celecoxib (50 mg/kg, p.o). Molecular docking was carried out on both COX-1 and COX-2 structures which revealed that Asparacosin A targets allosteric binding site similar to the binding mode of the selective COX inhibitor. In conclusion, Asparacosin A exhibits anti-inflammatory and peripheral anti-nociceptive activities which are likely mediated via inhibition of COX-2 enzyme and inflammatory cytokines. Furthermore, Asparacosin A can serve as a model to obtain new and more selective potent anti-inflammatory and anti-nociceptive drugs.

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BACKGROUND: Different processing conditions alter the ginseng bioactive compounds, promoting or reducing its anti-inflammatory effects. We compared black ginseng (BG) - that have been steamed 5 times - with red ginseng (RG). HYPOTHESIS/ PURPOSE: To compare the anti-inflammatory activities and the anti-nociceptive properties of RG and BG. METHODS: Nitric Oxide (NO) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide (MTT) assay, quantitative Reverse Transcriptase-Polymerase Chain Reaction (qRT-PCR), western blot, xylene-induced ear edema, carrageenan-induced paw edema RESULTS: The ginsenoside contents were confirmed using high-performance liquid chromatography (HPLC) and has been altered through increased processing. The highest concentration of these extracts inhibited NO production to near-basal levels in lipopolysaccharide (LPS)-stimulated RAW 264.7 without exhibiting cytotoxicity. Pro-inflammatory cytokine expression at the mRNA level was investigated using qRT-PCR. Comparatively, BG exhibited better inhibition of pro-inflammatory mediators, iNOS and COX-2 and pro-inflammatory cytokines, IL-1ß, IL-6 and TNF-α. Protein expression was determined using western blot analysis and BG exhibited stronger inhibition. Xylene-induced ear edema model in mice and carrageenan-induced paw edema in rats were carried out and tested with the effects of ginseng as well as dexamethasone and indomethacin - commonly used drugs. BG is a more potent anti-inflammatory agent, possesses anti-nociceptive properties, and has a strong potency comparable to the NSAIDs. CONCLUSION: BG has more potent anti-inflammatory and anti-nociceptive effects due to the change in ginsenoside component with increased processing.

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BACKGROUND AND OBJECTIVE: N-aryl derivatives of phthalimide and 4-nitro phthalimide have demonstrated cyclooxygenase inhibitory activity. Also, they possess excellent analgesic and antiinflammatory activity. In this work, a new series of N-arylmethylideneamino derivatives of phthalimide and 4-nitro phthalimide were designed and synthesized. METHODS: The designed compounds were synthesized by condensation of the appropriate aldehyde and N-aminophthalimide in ethanol at room temperature at PH around 3. Their analgesic and antiinflammatory activity were evaluated by acetic acid-induced pain test and carrageenan-induced paw edema test in mice and rats, respectively. RESULTS AND CONCLUSION: The details of the synthesis and chemical characterization of the analogs are described. In vivo screening showed compounds 3a, 3b, 3f and 3h were the most potent analgesic compounds. In addition, compounds 3a, 3c, 3d, 3e and 3j indicated comparable anti-inflammatory activity to indomethacin as a reference drug.

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BACKGROUND: Persisting inflammatory stimuli cause chronic inflammation recognized as the major factor contributing to the development of a number of diseases. One group of drugs used in the treatment of chronic inflammation is the group of non-steroidal anti-inflammatory drugs and, more specifically, the selective COX-2 inhibitors (coxibs). However, most of the coxibs were withdrawn from the market in view of their safety profile. In the present study, 2-[3-Acetyl-5-(4-chlorophenyl)- 2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e), an Npyrrolylcarboxylic acid derivative structurally related to celecoxib, is evaluated for anti-inflammatory activity after single and multiple (14 days) administration using an animal inflammation model. AIM: To evaluate the anti-inflammatory properties of 2-[3-Acetyl-5-(4-chlorophenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e) after single and multiple (14 days) administration using an animal inflammation model. MATERIALS AND METHODS: Forty Wistar rats were allocated into 5 groups (n=8) treated with saline (controls), diclofenac (25 mg/kg b.w.), compound 3e (10, 20 and 40 mg/kg b.w.) intraperitoneally. The volume of the right hind paw of the animals of all groups is measured prior to treatment and two, three and four hours after administration of carrageenan using a plethysmometer (Ugo Basile, Italy). The percentage of paw edema is calculated using the Trinus formula. RESULTS: In a single administration, compound 3e in doses of 10 and 20 mg/kg b.w. did not inhibit paw edema, while a dose of 40 mg/kg b.w. significantly inhibited carrageenan-induced paw edema at 2 hours in comparison with the control group. After continuous administration, compound 3e in doses of 10, 20 and 40 mg/kg b.w. significantly reduced paw edema at 2, 3, and 4 hours compared to animals treated with saline. CONCLUSIONS: Compound 3e shows anti-inflammatory properties similar to those of diclofenac after continuous administration.

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BACKGROUND: Recently, pyrazole derivatives have shown significant antiinflammatory activity. Non-steroidal anti-inflammatory drugs have some side effects, mainly gastric irritation and gastric ulceration during the treatment of inflammation. So the current study deals with the synthesis and pharmacological evaluation of a series of novel pyrazole derivatives as anti-inflammatory agents. METHODS: A series of novel ethyl 5-(substituted)-1H-pyrazole-3-carboxylate (2a-j) were synthesized and evaluated for anti-inflammatory activity using carrageenan-induced inflammation in rat paw edema model. In the first step, diethyl oxalate react with acetophenone derivatives in presense of sodium ethoxide to form substituted ethyl-2,4-dioxo-4- phenyl butanoate derivatives as intermediate (1a-j). Further the suspension was prepared from dioxo-esters with hydrazine hydrate in glacial acetic acid yielded novel ethyl 5- (substituted)-1H-pyrazole-3-carboxylate (2a-j) derivatives. The structure of the final analogues (2a-j) has been confirmed on the basis of elemental analysis, IR, 1 H NMR and mass spectra. RESULTS: All the values of elemental analysis, FTIR, 1H NMR, and mass spectra were found to be prominent. The anti-inflammatory activity test revealed that Ethyl 5-(3,4- dimethoxyphenyl)-1H-pyrazole-3-carboxylate (2f) and ethyl 5-(2,3-dimethoxyphenyl)-1Hpyrazole- 3-carboxylate (2e) exhibited significant anti-inflammatory activity as compared to control group. CONCLUSION: The results of the current study indicate that the substitution at pyrazole scaffold could improve anti-inflammatory activity.

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