In-vivo Anti-inflammatory Activity Research Articles

Evaluation of In-vivo Anti-inflammatory activity of methyl 2-(5-butyl-6-thioxo-1, 3, 5-thiadiazinan-3yl), butanoate

Inflammation is the body's way of fending off damage. Nonetheless, continuous and increasing inflammation may lead to the development of some chronic illnesses. It is still needed to evaluate new and safe anti-inflammatory therapies because existing medications have major side effects. Objective: To examine a novel compound's anti-inflammatory properties of methyl 2-(5-butyl-6-thioxo-1, 3, 5-thiadiazinan-3yl), butanoate (MBTTB) in albino mice models. Method: To test the anti-inflammatory effects in vivo, carrageenan-induced paw edema in albino mice of both sexes was utilized, and inflammation was measured by using Digital Plethysmometer. After extraction of carrageenan induced paw edematous, tissue level of inflammatory mediators like TNF-α, IL-1β, NF-ĸβ, and cox2 was ascertained by Western Blot analysis. Result: Based on in-vivo anti-inflammatory effects, compound MBTTB was shown to exhibit a maximum percentage inhibition of 16.7% after 1 hour, which is comparable to the standard drugs 12.8%. Following three hours, compound MBTTB showed the highest percentage inhibition of 23.2%, while the standard was 14.5%. Compound MBTTB showed the highest percentage inhibition after five hours (26.2 %), while the standard was 15.4%. The expression of many mediators' proteins, including TNF-α, IL-1β, NF-ĸβ, and COX-2, was ascertained. The computational analysis was carried out to forecast the level of decline of various mediators, including Tumor Necrosis Factor-α, (TNF) Interleukin-1β, NF-ĸβ, and COX-2. Conclusion: When considered as a whole, our current research indicates that MBTTB is a viable option for preventing inflammation in mice that has been caused by carrageenan in edematous paw.

Invitro and Invivo anti-inflammatory activity of Tabebuia pallida leaves

As any change in the body like injury or destruction and inflammation is characterized by the changes in the body evaluation like heat, discomfort, swelling, redness and some physiological changes in the processes. The inflammatory process is a complicated series of relationship among substances and some elements that included in the connective tissue. An inflammatory response is the primary cause for wide range of disorders like allergies, metabolic syndromes, cancer and syndromic disorders etc., Immune related disorder plays as financial burden on individuals, in such conditions some drugs and medicines are used like steroids, nonsteroids and immunosuppressants which are some common medications for controlling the inflammatory response in the body. Most of these medications have side effects on the body like allergies and gastric ulcers. In such conditions they find the natural goods like plants having historically an excellent medication activity for inflammatory illnesses. But there is no specific information on the inflammatory activity reports used in literature. Scientists need to find new process with low cost, straightforward to invitro methodologies and to access the natural anti-inflammatory activity and focus on the anti-inflammatory methodology which can evaluate the natural anti-inflammatory substances. These are cost effective and easy to operate with minor alternatives. The activity is performed on egg albumin to know about its anti-inflammatory properties.

Synthesis, molecular docking and pharmacological evaluations of novel naphthalene-pyrazoline hybrids as new orally active anti-inflammatory agents

The pyrazoline nucleus is widely present in diverse compounds as it serves as a valuable template for the discovery of new class of bioactive compounds. Various substituted 2-pyrazolines exhibit a spectrum of pharmacological activities, including antimicrobial, anti-inflammatory, analgesic, and antitumor properties. In view of this, we have synthesized a novel class of naphthalene-pyrazoline hybrids (PY1-PY20). All the synthesized hybrids were thoroughly characterized by means of standard spectroscopic techniques and tested for their in-vivo anti-inflammatory activity. Most of the compounds exhibited significant anti-inflammatory activity and in particular the compounds bearing electron withdrawing groups had potential in vivo activity. Further, in-silico molecular docking studies were carried out using the ‘Molegro Virtual Docker’ as a docking tool against the target proteins such as COX-1 (PDB ID: 1EQH) and COX-2 (PDB ID: 1PXX). The results revealed that the majority of pyrazolines form hydrogen interactions with key residues (Ser 530, Tyr 385, Tyr 355, Arg 120, Ser 353, Arg 83) in the active binding sites of COX-1 (1EQH) and COX-2 (1PXX). Notably, interactions with residues Tyr 355, Arg 120, Ser 530 for COX-1, and Tyr 355, Arg 120, Gln 192, Leu 352, Ser 353, His 90, Tyr 38, Ser 530, and Tyr 385 for COX-2 are crucial for the reported anti-inflammatory activity of diverse compounds. Ligand-protein inverse molecular docking studies highlight specific hydrogen bond interactions, with PY-8, PY-11, PY-15, and PY-17 showing significant interactions. The study was able to identify potential anti-inflammatory naphthalene-pyrazoline derivatives.

Anti-inflammatory activity of Codium elongatum on Carrageenan-induced paw edema in Wistar male rats

Inflammation is the physiological defence system of the body to initiate the healing mechanism for tissue and eliminate injurious stimuli. In the present study, the anti-inflammatory activity of Codium elongatum was evaluated. Water extract (250 mg/kg, b.w.) and isolated polysaccharide (500 mg/kg, b.w.) are investigated in the carrageenan-induced rat paw edema model using phenylbutazone as a standard drug. Both water extract and isolated polysaccharide showed significant anti-inflammatory activity by blocking the cyclooxygenase 2 pathway. This is the first report to demonstrate the in-vivo anti-inflammatory activity of Codium elongatum.

Development of Orally Active Anti-Inflammatory Agents: In Vivo and In Silico Analysis of Naphthalene-Chalcone Derivatives Based on 2-Acetyl-6-Methoxy Naphthalene

Chalcone compounds are reported to have diverse biological activities such as antiviral, antimicrobial, antimalarial, antitumor, antifungal, anticancer, and so forth. Herewith, we wish to report the in-vivo anti-inflammatory activities of previously synthesized naphthalene-chalcone hybrids from 2-Acetyl-6-Methoxy Naphthalene derivatives (C1-C25). All synthesized chalcones (C1-C25) were thoroughly characterized with standard spectroscopic techniques and tested for their in-vivo anti-inflammatory activities. The currently employed in-silico docking methodology uses the ‘Molegro Virtual Docker’ as a docking tool and target proteins as COX-1 (PDB ID: 1EQH) and COX-2 (PDB ID: 1PXX). Molecular docking analysis of chalcones (C1-C25) suggested that compound C-24 exhibited best docking score of -117.495 kcal/mol than the standard flurbiprofen -115.259 kcal/mol on COX-1 target. To understand more about pharmacokinetics aspects, we predicted theoretical ADME properties using ‘QikProp, 2022’ and found that all compounds were exhibited acceptable pharmacokinetic properties.

Design, synthesis, biological evaluation, and in silico studies of quinoxaline derivatives as potent p38α MAPK inhibitors.

A new series of quinoxaline derivatives possessing the hydrazone moiety were designed, synthesized, and screened for in-vitro anti-inflammatory activity by the bovine serum albumin (BSA) denaturation technique, and for antioxidant activity, by the (2,2'-diphenyl-1-picrylhydrazyl(DPPH) radical scavenging assay. The synthesized compounds were also tested for p38α mitogen-activated protein (MAP) kinase inhibition. The in-vivo anti-inflammatory activity was assessed by the carrageenan-induced rat paw edema inhibition method. All the compounds (4a-n) exhibited moderate to high in-vitro anti-inflammatory activity. Compound 4a displayed the highest inhibitory activity in the BSA assay (83.42%) in comparison to the standard drug diclofenac sodium (82.90%), while 4d exhibited comparable activity (81.87%). The DPPH assay revealed that compounds 4a and 4d have free radical scavenging potential (74.70% and 74.34%, respectively) comparable to the standard butylated hydroxyanisole (74.09%). Furthermore, the p38α MAP kinase inhibition assay demonstrated that compound 4a is highly selective against p38α MAP kinase (IC50 = 0.042) in comparison to the standard SB203580 (IC50 = 0.044). The five most active compounds (4a-4d and 4f) with good in-vitro profiles were selected for in-vivo anti-inflammatory studies. Compounds 4a and 4d were found to display the highest activity (83.61% and 82.92% inhibition, respectively) in comparison to the standard drug diclofenac sodium (82.65% inhibition). These compounds (4a and 4d) also exhibited better ulcerogenic and lipid peroxidation profiles than diclofenac sodium. The molecular docking and molecular dynamics simulation studies were also performed and found to be in agreement with the p38α MAP kinase inhibitory activity.

Design, Synthesis, Anti-inflammatory Evaluation and in silico Molecular Docking of Novel Furan-based Derivatives as Potential TNF-α Production Inhibitors

Introduction: Inflammation is the first response and an alarming signal for the onset of chronic disease. Most of the anti-inflammatory drugs available in the market are reported to have undesirable gastrointestinal toxicities. Therefore, it is of urgent significance to develop anti-inflammatory drugs with low toxicity and good efficacy. METHOD: We created a targeted scaffold based on a literature review by combining the different structural characteristics of furan and benzyl amides into a single pharmacophore. A series of eighteen furan-based derivatives (1-18) were designed, synthesized for in-vitro and in-vivo anti-inflammatory activity. The characterization of synthesized compounds was elucidated by techniques like 1H-NMR, 13C-NMR, FT-IR and MS. Result: The synthetic compounds were examined through molecular docking studies on TNF-α for probable binding mode and interactions with hydrophilic and hydrophobic pocket of TNF-α in comparison to standard drug (Indomethacin). Conclusion: When compared to the standard treatment, compounds 18, 15 and 9 displayed a remarkable inhibitory effect on the production of TNF-α and in-vivo inflammatory activity with no damage to stomach and reduction of LPO. The compounds 18, 15 and 9 might be a good consideration for potential anti-inflammatory agents.

EVALUATION OF THE ACUTE TOXICITY, ANTI-INFLAMMATORY AND ANALGESIC ACTIVITIES OF FOUR PLANTS USED IN THE BENINESE PHARMACOPOEIA (ANNONA SENEGALENSIS, SARCOCEPHALUS LATIFOLIUS, COMBRETUM GLUTINOSUM AND DETARIUM MICROCARPUM)

Inflammation and pain are a common feature of almost all non-communicable diseases. Annona senegalensis, Sarcocephaluslatifolius, Combretum glutinosum and Detariummicrocarpum have been traditionally used to treat different types of diseases. This study aimed to evaluate in-vivo anti-inflammatory and analgesic activities of these plants extracts, as well as their acute toxicity. The hydroethanolic extracts of the leaves were used for in-vivo tests on Wistar rats. The anti-inflammatory activity was evaluated by the 2% formalin-induced edema test, while the analgesic activity was evaluated by the acetic acid test. The acute toxicity of the crude hydroethanol extract was evaluated by oral administration of the extract to Wistar rats. A single dose of 2000 mg/kg body weight was administered and the effects on biochemical parameters were evaluated. The two plants tested showed a significant analgesic activity with a percentage of inhibition of cramps of 85.37 % for D. microcarpum and 87.37 % for A.senegalensis compared to aspirin which is 45.07%. The percentage of edema inhibition at 100 mg/kg reached 37.47 % for Detariummicrocarpum and 68.0 % for Annona senegalensis against 34.10 % for diclofenac. The toxicity test performed on rats by the oral route at a dose of 2000 mg/kg body weight showed no adverse effects and no deaths during the 14 days of observation.

ANTI-INFLAMMATORY STUDY (IN-VITRO AND IN-VIVO) AND HPTLC DENSITOMERIC DETERMINATION OF QUERCETIN FROM METHANOLIC LEAF EXTRACT OF HOTTUYNIA CORDATA THUNB. FROM MIZORAM, INDIA

Objective: This study aimed to investigate the anti-inflammatory activity of the methanolic leaf extract of Houttuynia cordata Thunb. from Mizoram, India, using in-vitro and in-vivo models. In addition, the study also aimed to determine the quercetin content of the methanolic leaf extract using high-performance thin-layer chromatography (HPTLC) densitometry. Methods: The methanolic leaf extract of H. cordata was prepared using successive Soxhlet extraction, and its anti-inflammatory activity was evaluated using in-vitro models such as inhibition of protein denaturation and inhibition of proteinase activity. The in-vivo anti-inflammatory activity of the extract was evaluated using carrageenan-induced paw edema in rats. The quercetin content of the extract was determined using HPTLC densitometry. Results: The methanolic leaf extract of H. cordata showed significant anti-inflammatory activity in both in-vitro and in-vivo models. The extract exhibited a dose-dependent inhibition of protein denaturation and proteinase activity and also significantly reduced paw edema in the rat model. The IC50 values of egg albumin and bovine serum albumin denaturation studies were 317.365 μg/mL and 198.918 μg/mL, respectively. The results showed that the methanolic leaf extract of the plant was 200 mg/kg b.w. and 400 mg/kg b.w., which considerably reduced carrageenan-induced paw edema, and their effects were comparable to those of the standard diclofenac sodium. The HPTLC densitometry analysis revealed the presence of quercetin in the extract, with a quercetin content of 21.8 ng/μL. Conclusion: The methanolic leaf extract of H. cordata Thunb. from Mizoram, India demonstrated significant anti-inflammatory activity in both in-vitro and in-vivo models. The presence of quercetin in the extract may contribute to its anti-inflammatory properties. These findings provide scientific evidence for the traditional use of H. cordata as an anti-inflammatory agent.

Anti-inflammatory, anti-proliferative and anti-psoriatic potential of apigenin in RAW 264.7 cells, HaCaT cells and psoriasis like dermatitis in BALB/c mice

AimsPsoriasis is an immune-mediated skin disease characterized by keratinocytes hyperproliferation, abnormal differentiation and inflammation. Therefore, this study aimed to investigate in-vitro and in-vivo anti-inflammatory and anti-proliferative activity to evaluate anti-psoriatic potential of apigenin. Main methodsFor in-vivo study, 5 % imiquimod cream was used to induce psoriasis-like skin inflammation in BALB/c mice to mimic human psoriatic conditions. PASI score, CosCam score, histopathology, immunohistochemistry, qRT-PCR, and ELISA were done to evaluate the anti-psoriatic potential of topically applied apigenin. For in-vitro studies, LPS-induced inflammation in RAW 264.7 was done, and qRT-PCR, ELISA, and immunofluorescence were conducted to evaluate the anti-inflammatory activity of apigenin. Migration and cell doubling assay in HaCaT cells were performed to assess the anti-proliferative effect of apigenin. Acute dermal toxicity profile of apigenin has also been done as per OECD guidelines. Key findingsResults showed that apigenin significantly reduce the PASI and CosCam scores, ameliorate the deteriorating histopathology, and effectively downregulated the expression of CCR6, IL-17A, and NF-κB. Apigenin effectively downregulated the expression and secretion of pro-inflammatory cytokines through IL-23/IL-17/IL-22 axis. Apigenin suppressed nuclear translocation of NF-κB in LPS-induced RAW 264.7 cells. Cell migration and cell doubling assay in HaCaT cells showing the anti-proliferative potential of apigenin and it was found safe in acute dermal toxicity study. SignificanceApigenin was found effective against psoriasis in both in-vitro and in-vivo models suggesting apigenin as a potential candidate for the development of anti-psoriatic agent.

Impact of Eucalyptus maculata Hook resin exudate constituents on reducing COX-2 gene expression: In-vivo anti-inflammatory, molecular docking and dynamics studies

Ethnopharmacological relevanceEucalyptus maculata Hook from the Myrtaceae family is a native Australian plant that is frequently cultivated in Egypt. Many Eucalyptus species, including E. maculata, were widely used by the Dharawal, the indigenous Australian people, for their anti-inflammatory properties. Aim of the study: The purpose of this study was to determine the anti-inflammatory activity of the ethanol extract of E. maculata resin exudate, its methylene chloride and n-butanol fractions, as well as the isolated compounds. Materials and methods: the ethanol extract was partitioned by methylene chloride, and n-butanol saturated with water. The fractions were chromatographed to isolate pure compounds. In-vivo anti-inflammatory activity of the ethanol extract, the fractions at a dose of 200 mg/kg, and the isolated compounds (20 mg/kg) was estimated using carrageenan-induced rat paws edema method against indomethacin (20 mg/kg). The activity was supported by histopathological and biochemical parameters. Results: Three isolated compounds were identified as aromadendrin (C1), 7-O-methyl aromadendrin (C2), and naringenin (C3). Our findings demonstrated that the tested fractions significantly reduced the paw edema starting from the 3rd to the 5th hour as compared to the positive control, compounds C2 and C3 showed the greatest significant reduction in paw edema. The ethanol extract, fractions, C2, and C3 demonstrated an anti-inflammatory potential through reducing the levels of TNF-α, IL-6, and PGE2, as well as COX-2 protein expression compared to the negative control. These results were supported by molecular docking, which revealed that the isolated compounds had high affinity to target COX-1 and COX-2 active sites with docking scores ranging from −7.3 to −9.6 kcal mol−1 when compared to ibubrofen (−7.8 and −7.4 kcal mol−1, respectively). Molecular dynamics simulations were also performed and confirmed the docking results. Conclusion: The results supported the traditional anti-inflammatory potency of E. maculata Hook, and the biochemical mechanisms underlying this activity were highlighted, opening up new paths for the development of potent herbal anti-inflammatory medicine. Finally, our findings revealed that E. maculata resin constituents could be considered as promising anti-inflammatory drug candidates.

Bio-Evaluation, In-Vitro and In-Vivo Anti-Inflammatory Activity, Therapeutic Efficacy, and Genotoxicity of the Potentials of the Green Seaweed Valoniopsis Pachynema using Zebra Fish Larvae (Danio Rerio) as an Animal Model

Advancement in the medical sectors to treat regular diseases are increasing day-by-day. Yet, there is a considerable growth in the demand for the natural/herbal products as well due to their low level of side effects, cost efficiency and their multiple inhibition properties. Based on this, the present research works with an objective to examine the bioactive components, in vitro anti-inflammatory and in vivo antiinflammatory behaviour of the green marine macro algae Valoniopsis pachynema using zebra fish (Danio rerio) larvae as a skin inflammation model. In this study, the secondary metabolites are extracted using methanol solvent from the marine green seaweed, V. pachynema using the Gas Chromatography-Mass Spectrometry (GC-MS) analysis and these are further evaluated for their anti-inflammatory effects. Further screening process is accomplished for the in vitro anti-inflammatory activity by the albumin-denaturation inhibition. Results from concentration-dependent analysis is documented. The efficacy, therapeutic efficacy, and genotoxicity of the compound Valp at various concentrations are determined by recapitulating the pathophysiology of Skin inflammation in Zebrafish larvae. In evaluating the efficiency of the study, Valp at 1 pg, 10 pg, 100 pg are observed and progressed for the evaluation of therapeutic efficacy and genotoxicity. In the assessment of genotoxicity, the gene expression of mgmt gene is observed to be in control level at Valp 100 pg treated group confirming no genotoxicity. According to the results obtained, the green seaweed V. pachynema can be potentially explored as an effectual anti-inflammatory agent for its bio-functionalities

Synthesis of Novel Benzoxazole Derivatives: Exploration of Their Possible Pharmacological Profiles with Computational Studies

Based on the interaction with PDB protein 1PXX of the cox-2 enzyme, a novel series of substituted thiazolidinones (TZD 5a-s) and azetidinones (AZT 6a-s) was designed and synthesized. Molecules were synthesized from 2-mercapto benzoxazole (1) using both conventional and microwave irradiation methods, and their in-vitro antioxidant activity was evaluated using the DPPH free radical scavenging activity, as well as their in-vivo anti-inflammatory activity using the carrageenin-induced rat paw edema method. The reaction time, yield, and purity of microwave and conventionally produced molecules are compared in this work. The molecule ethyl 2-(benzoxazol-2-ylthio)acetate (2) is obtained by reacting 2-mercapto benzoxazole (1) with ethyl 2-chloroacetate in the presence of potassium carbonate and dry acetone. The molecule 2-(benzoxazol-2-ylthio)acetohydrazide (3) was synthesized by reacting ethyl 2-(benzoxazol-2-ylthio)acetate (2) with hydrazine hydrate in the presence of absolute alcohol. Compound 2-(benzoxazol-2-ylthio)acetohydrazide (3) on reacting with different aromatic and heterocyclic aldehyde derivative forms 2-(benzoxazol-2-ylthio)-N'-substituted acetohydrazide Schiff bases (4a-s). 2-(benzoxazol-2-ylthio)-N-(4-oxo-2-substituted thiazolidin-3-yl)acetamide (5a-s) i.e. thiazolidinones benzoxazole derivatives obtained on reacting Schiff bases (4a-s) with thioglycolic acid in a dioxane medium and anhydrous zinc chloride. The Schiff bases (4a-s) were converted into 2-(Benzo[d]oxazol-2-ylthio)-N-(3-chloro-2-oxo-4-substituted azetidin-1-yl)acetamide (6a-s) after treatment with chloroacetyl chloride in the presence of triethanol amine and dioxane. This study focuses on screening of novel synthesized benzoxazole derivatives for in vitro antioxidant, in vivo anti-inflammatory activity, and the evaluation of ulcerogenic activity. The in vivo activity is correlated with the in silico activity, the 3 D QSAR studies were performed for all the compounds by using computer program i.e. SYBYL-X 2.1.1 software. The best CoMFA and CoMSIA models were obtained for the training set compounds with 0.753 and 0.646 leave-one-out coefficients (q2), 0.714 and 0.619 cross validated correlation coefficients (r2cv), and 0.975 and 0.983 conventional coefficients (r2), respectively. Both models were validated with a test set of eight compounds, giving the CoMFA and CoMSIA models a satisfactory prediction (r2pred) of 0.788 and 0.663, respectively. The findings of the study would provide valuable information for the design of new compounds and would also help in predicting the activity of designed compounds. To identify the lead molecule docking studies are performed on COX-2 enzyme of protein 1PXX, the molecules 5c, 5q, 5j, 6q, and 6 g derivatives obtained good - c-docker interaction energy respectively, and in vivo acute ulcerogenic activity.

Evaluation of Anti-inflammatory, Antioxidant and Xanthine Oxidase Inhibitory Potential of N-(2-hydroxy phenyl) Acetamide

Nonsteroidal anti-inflammatory drugs has long been used to treat various pathological conditions like arthritis, gout, diabetes, cancer, and cardiovascular diseases. Although exploring the effective anti-inflammatory agents possessing antioxidant along with pain relieving properties is still challenging. Acetamide-containing compounds are known to possess analgesic and anti-inflammatory activity. The purpose of this study is to evaluate the anti-inflammatory, anti-oxidant, xanthine oxidase, and analgesic activity of an acetamide derivative, N-(2-Hydroxyphenyl) Acetamide. In-vitro anti-inflammatory and antioxidant activities were assessed by protein denaturation inhibition and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, respectively. Xanthine oxidase potential was also evaluated. In-vivo anti-inflammatory activity was determined by the Formalin-induced paw edema method and analgesic potential was evaluated by an acetic acid-induced writhing test. Results of in-vitro anti-inflammatory activity showed significant (p< 0.001) inhibition of protein denaturation by N-(2-Hydroxyphenyl) Acetamide at both100 and 300 µg/ml. It also exhibited high radical scavenging activity (88.16%) by DPPH at 300 µg/ml. In-vivo Formalin-induced paw edema method revealed significant (p < 0.05) inhibition of paw edema when compared with control and formalin groups. Likewise, NA-2 also significantly (p < 0.001) reduced the number of writhes in the Acetic acid-induced writhing test. Moreover, in both aforementioned in-vivo tests, NA-2 showed comparable results with Indomethacin (10 mg/kg). This study demonstrates that N-(2-Hydroxyphenyl) Acetamide possesses substantial anti-inflammatory, antioxidant, and analgesic activity.

Evaluation of Anti-Inflammatory and Antipyretic Activities of The Aqueous Stem Bark Extract of Lophira Lanceolata Van Tiegh. Ex Keay

The bark of Lophira lanceolata (Ochnaceae) has been used traditionally for the treatment of many disease conditions such as dysentery, headaches, diarrhoea, cough, abdominal pains, fungal infections, nociception and cardiovascular diseases. However, no specific work on its anti-inflammatory or antipyretic effect has been reported which forms the basis of this study. This study evaluates the in-vivo anti-inflammatory and antipyretic activities of the aqueous extract of the stem bark of Lophira lanceolata using laboratory animal model. The methods adopted for this study were formalin induced inflammation and yeast induced hyperpyrexia in rats. All the results were expressed as mean ± S.E. The data were statistically analysed by one way analysis of variance (ANOVA) followed by Dunnett's multiple comparison and p-values 0.05 were considered as significant. The result of this study showed a significant anti-inflammatory effect different from the control (distilled water) at p 0.05 characterized by oedema formation, change in temperature, redness, and itching in the paw of the rats which is comparable with the standard indomethacin. The inhibition of oedema was statistically dose dependent as the group 4 rats which received 400 mg/kg body weight demonstrated more effect than the group 1 rats which received 100 mg/kg body weight of the aqueous extract of the stem bark of Lophira lanceolata. The aqueous at the dose of 400 mg/kg body weight showed the highest antipyretic effect. Hence the antipyretic activity was also dose- dependent. The study demonstrated that the aqueous Lophira lanceolata stem bark extract possesses anti-inflammatory and antipyretic activities.

In vivo Acute Anti-Inflammatory Activity of Essential Oils: A Review.

In recent years, there has been a significant increase in the search for new therapeutic strategies for the treatment of inflammatory diseases. In this sense, natural products emerge as a potential source for the discovery of new drugs, with the research of the pharmacological properties of these products being very important. In addition to its function in plants (insect attraction and repellency), essential oils present pharmacological effects, such as antibacterial, antifungal, antimutagenic, antiviral, antiprotozoal, antioxidant, antidiabetic and anti-inflammatory properties. In this review, we describe the mostly used in vivo acute inflammatory experimental models and the studies showing the in vivo anti-inflammatory activity of essential oils. Essential oil from species from the Apiaceae, Asteraceae, Burseraceae, Boraginaceae, Cupressaceae, Euphorbiaceae, Fabaceae, Lamiaceae, Lauraceae, Myrtaceae, Piperaceae, Poaceae, Rutaceae, Verbenaceae and Zingiberaceae families were described as being anti-inflammatory in vivo. Five models of acute inflammation are commonly used to investigate the anti-inflammatory activity in vivo: ear and paw edema, pleurisy, peritonitis and the subcutaneous air pouch model. In addition to in vivo analysis, ex vivo and in vitro experiments are carried out to study the anti-inflammatory action of essential oils. The most commonly used model was paw edema, especially due to this model being easy to perform. In order to suggest or elucidate the mechanisms involved in the anti-inflammatory effect, many studies measured some inflammatory mediators, such as cytokines, COX-2 expression and the levels of PGE2, and NO, or evaluated the effect of essential oils or their major compounds on inflammation response directly induced by inflammatory mediators.

Synthesis, characterization, In-Silico studies, and anti-inflammatory activity of Novel Imidazole-5(4H)-Ones

Several new imidazole-5(4H)-one analog was synthesized using multi-step synthesis. All the synthesized compounds were characterized using FT-IR, 1H-NMR, Mass spectroscopy, and microanalysis to confirm their chemical structure. Molecular properties of the title compounds were predicted using Molinspiration online tool and binding studies of the title analogs against COX-1 & COX-2 were predicted by the molecular docking method. All novel imidazole-5(4H)-one analog were tested for their in-vivo anti-inflammatory activity using carrageenan-induced paw edema test in Wistar rats. Varying degree (weak to excellent) of anti-inflammatory activity was displayed by title compounds. In addition, in vitro anticancer potency of test compounds was estimated by the MTT assay method and found that most of the tested analogs were found to be inactive at 10 µM concentration against the tested cell lines. Among twelve tested title compounds, 2-methyl-1-(4-methyl piperazine-1-yl)-4-(naphthalen-1-ylmethylene)-1H-imidazol-5(4H)-one AL01, and 4-benzylidene-2-methyl-1-(4-methylpiperazin-1-yl)-1H-imidazol-5(4H)-one AL02 displayed more potent anti-inflammatory activity which is slightly higher than reference diclofenac.

Pharmacological investigation of antioxidant and anti-inflammatory activities of aqueous extract from Mitracarpus frigidus (Rubiaceae).

This study aimed to evaluate the potential of aqueous extract from Mitracarpus frigidus aerial parts (MFAq) in the treatment of inflammation and oxidative stress, as well as to characterize its chemical constituents. Total phenolic and flavonoid contents were determined, and phytoconstituents were detected by ultra-fast liquid chromatography/quadrupole-time-of-flight tandem mass spectrometry (UFLC-QTOF-MS). The antioxidant activity was evaluated by DPPH, TAC and β-carotene/linoleic acid assays. In-vitro anti-inflammatory activity, cell viability and cell cycle were performed in J774A.1 cell line. In-vivo anti-inflammatory activity was investigated by two ear oedema assays (croton oil and phenol). Chlorogenic acid, clarinoside, quercetin-hexosylpentoside, rutin, kaempferol-3-O-rutinoside, kaempferol-rhamnosylhexoside, quercetin-pentosylrhamnosylhexoside, harounoside, 2-azaanthraquinone and sucrose were identified by UFLC-QTOF-MS. MFAq showed antioxidant activity, which was positively correlated to the content of phenolic compounds. MFAq significantly inhibited the production of nitric oxide, did not decrease viability in MTT assay (all concentrations) and showed no changes in membrane permeability and cell cycle of J774A.1 cell line. Furthermore, MFAq showed a reduction in ear oedema in all tested doses. MFAq was effective in some antioxidant and inflammatory parameters, in the experimental conditions that were used in the study. This is the first report of chemical composition and bioactivities from this extract.

Design, synthesis, in silico studies, in vivo and in vitro assessment of pyridones and thiazolidinones as anti-inflammatory, antipyretic and ulcerogenic hits

Pyridine derivatives have occupied a unique position in medicinal chemistry. Aseries of 2(1H)-pyridone molecules, bearing a 4-hydroxyphenyl moiety 4, 5, 6a-c,7a-c, 8a-f and 9a,b were synthesized via a one-pot reaction of 2-cyano-N-(4-hydroxyphenyl)acetamide with diketones such as acetylacetone, isatin, ethyl acetoacetate, arylidine malononitriles, or arylidene esters. Additionally, the thiazole moiety has been incorporated instead of the pyridine skeleton through the isothiocyanates in N, N-dimethylformamide to furnish the non-isolable intermediate salt. Upon reaction of the intermediate with ethyl chloroacetate the corresponding 2-cyano-N-(4-hydroxyphenyl)-2-(4-oxo-3-phenylthiazolidine-2-ylidene)-acetamide (11) was afforded as a final product, which further reacted with aromatic aldehydes to produce 12a,b. All novel hybrids were assessed for their in-vitro and in-vivo anti-inflammatory, ulcerogenic, and antipyretic activities demonstrating moderate to high activity against IL-6 ranging from 24.403% to 89.307% when ompaired to Paracetamol and Phenylbutazone as reference drugs. Furthermore, in-silico prediction methodology were considered for predicting the physicochemical drug-likeliness and ADME characteristics of all synthesised compounds as well as the standard reference drugs: paracetamol and phenylbutazone. The docking tests were performed on the most promising IL-6 derivatives 4, 8a, 8b, 8c, 8f, 12b, Paracetamol, and Phenylbutazone, and their docking scores were compared to the scores of the aforementioned standard drugs.

Antioxidant-Anti-Inflammatory Evaluation of a Polyherbal Formula.

Most disease—both acute and chronic—results from inflammation, and reactive oxygen species (ROS) are considered some of the strongest stimuli of inflammation. Many studies reported the traditional use of herbal species for treating inflammation, especially when ROS are involved. The present study aims to demonstrate the antioxidant–anti-inflammatory effects of a patented preparation based on Populus nigra and Rosmarinus officinalis extracts and to highlight its applicative potential; the formula was characterized by HPTLC and HPLC and in-vitro studies were conducted on TNF-α-stimulated HUVECs. The antioxidant activity of the formula was determined by DPPH assay and the phosphomolybdenum method; to assess in-vivo anti-inflammatory activity, a rat paw edema model was used; the formula contains high amounts of polyphenols. It exhibited scavenging activity of 50–85% at 1–10 mg/mL, it inhibited nitrite production and ICAM-1 expression in TNF-α-stimulated endothelial cell cultures dose-dependently, at a maximum of 58.7% at the maximum dose administered and exerted an obvious anti-inflammatory effect in vivo, settling early and decreasing at 180 min; a new herbal bioactive product was presented with promising therapeutic potential that can be an adjunct to conventional therapies for diseases based on oxidative stress and inflammation.