Rat Paw Edema Method Research Articles

Synthesis, Molecular Docking Studies and Biological Evaluation of N-(α-Benzamido Cinnamoyl) Piperonal Hydrazones

Background: Nowadays, inflammation is recognized as the underlying cause of a number of diseases, but NSAIDs are the first drug of choice, having several side effects. Additionally, excessive cellular oxidative stress is often considered a major contributor to pathophysiological conditions, the development of cancer, and other diseases. Antimicrobial resistance is a global concern, hence, there is a critical need for the development of novel therapeutic agents to fight the emergence and increasing prevalence of resistant pathogens. This creates an initiation to introduce new molecules which act as efficient therapeutic agents with diminished side effects. Objective: As a part of our search for newer agents with enhanced activity profiles, it was planned to synthesize novel 2- (benzamido)-N-((benzo[d][1,3]dioxol-4-yl)methylene)-3-(substituted phenyl) acrylohydrazides and to investigate them for antiinflammatory, antioxidant, cytotoxic, antimicrobial activities. Furthermore, in silico studies were performed for title compounds to predict molecular properties, bioavailability, drug-likeness, and bioactivity scores, molecular docking studies were also performed against biological targets. Methods: The title compounds 1-14 were synthesized by nucleophilic addition of piperonal in ethanol, few drops of acetic acid to the intermediate 2-(benzamido)-3-(aryl)acrylohydrazides. The title compounds were tested for their antiinflammatory activity by in vivo carrageenan-induced rat paw edema method, in vitro COX-2 inhibition assay; in vitro cytotoxic activity evaluation by MTT assay; antioxidant activity by Lipid peroxidation, DPPH assay, Nitric Oxide scavenging assay and Hydrogen peroxide scavenging assay; and antimicrobial activity by cup plate method. Physicochemical properties and bioactive scores of title compounds were evaluated by in silico studies. Molecular docking studies were carried out for the title compounds against COX-2 (PDB: 5F19) and EGFR (PDB:1XKK). Results: Among the series, 4-Hydroxy-3,5-dimethoxy derivative (5) displayed good anti-inflammatory and antioxidant activities; Vanillinyl derivative (4) displayed good cytotoxicity and antimicrobial activity when compared to that of the respective standards. Compounds 5 & 4 also exhibited good docking scores with COX-2 and EGFR, respectively. All title compounds obeyed Lipinski’s rule of five and also exhibited acceptable molecular properties, drug-likeness properties, and moderate to good bioactivity scores in in silico studies. Conclusion: The study suggested that the title compounds showed notable pharmacological properties, could emerge as lead compounds, and be further explored as promising therapeutic agents.

3,4-Dihydropyrimidine-2(1H)-one/thione Derivatives as Anti-inflammatory and Antioxidant Agents: Synthesis, Biological Activity, and Docking Studies

aims: A series of sixteen new 4-(substituted phenyl) - 6-(substituted phenylamino)-3, 4-dihydropyrimidine-2(1H)-ones/thiones derivatives have been synthesized in two step reaction. background: Free radicals are widely known to play a significant part in the inflammatory process. Many non-steroidal anti-inflammatory medicines have been shown to work as radical scavengers or as inhibitors of free radical generation. Inflammation is a part of the vascular tissues' complicated biological reaction to adverse stimuli like bacteria, damaged cells, or irritants. The organism's protective response to damaging stimuli is inflammation, which aims to get rid of them and start the healing process. The inflammatory response has several advantageous effects, such as stopping the spread of dangerous substances to nearby tissues, getting rid of cell waste and infections, and getting the body ready for repair objective: To synthesize new derivatives as anti-inflammatory and antioxidant agents. method: In first step chalcones (I1-I6) was obtained and in the second step, these chalcones were reacted with urea and thiourea in the presence of potassium hydroxide to obtain the corresponding pyrimidinones and thiopyrimidinones. The structures of the synthesized compounds 4-(substituted phenyl)-6-(substituted phenylamino)-3,4-dihydropyrimidine-2(1H)-ones/thione derivatives are investigated by means of TLC (visualized it in Iodine chamber), IR, mass, 1H-NMR spectral and elemental analysis. The title compounds evaluated for anti-inflammatory as well as antioxidant activity. Anti-inflammatory activity in vivo was carried out by carrageenan induced rat-paw edema method and compared with standard drug diclofenac sodium and antioxidant activity was measured by DPPH, FRAP and Hydrogen peroxide (H2O2) method and compared with standard ascorbic acid. result: Electron donating groups showed better antioxidant activity as compared to electron withdrawing ones in both activities. All the compounds exhibited good to moderate activity. Compound DHPM8 shows better antioxidant activity and compound DHPM6 shows better anti-inflammatory activity while compound DHPM11 shows minimum antioxidant as well as anti-inflammatory activity than other compounds. conclusion: To better understanding, we have performed molecular docking simulation. The molecular docking studies revealed that all synthesized compound were showed good receptor binding interaction in which compound 9 had highest docking score of 9.8 due to interaction with CYS36, PRO153, TYR130, GLY45, LEU152, ARG469, LYS468 and GLU465. other: NA

Investigation of Pharmacological Screening Techniques for Diabetes Mellitus

Diabetes is the medical term for a condition in which the body fails to generate or use insulin as intended, leading to high blood sugar levels. Both in-vitro and in-vivo techniques are employed to assess the antidiabetic potential of synthetic or natural compounds that have been extracted from conventional plants. The rat paw oedema method is frequently used to screen anti-inflammatory medications. The use of animals in this procedure has drawbacks related to ethical concerns. We proposed an in vitro system in this context that would not have these drawbacks. Rat in vivo experiments are frequently used to screen anti-hyperlipidemic medications. Pharmacological screening currently entails testing novel chemical entities as plant extracts or any other type of material (synthetic or semisynthetic) in isolated preparations before testing on entire animals. Rats and mice are typically used, but occasionally higher animals like dogs and monkeys are as well. These techniques have been used to assess the majority of medications now used in therapy. Wherever possible, non-animal alternatives are being developed. Pharmacologists' constant struggle is to reconcile in vitro and in vivo results. A thorough grasp of the in vivo performance is one of the main objectives of pharmacological screening. Therefore, it would be praiseworthy to establish in vitro assessments that might be connected to in vivo performance.

Antioxidant and Anti-inflammatory activity of the Terpenoidal fraction of Ethanolic extract of Byttneria herbacea

The goal of this study was to identify the bioactive principle of the plant Byttneria herbacea (Malvaceae) which has a wide range of traditional therapeutic uses.Column chromatography was used to separate the ethanolic extract of aerial parts of the plant with mobile phase Chloroform: Methanol (5:5). The fraction with Rf 0.62 on TLC with mobile phase Toluene:Ethyl acetate (85:15) imparting bluish color under UV 254 nm was giving the test of Terpenoids. The same fraction was assessed for Antioxidant and Anti-inflammatory activity.Antioxidant activity was performed by measuring the decolourizing activity followed by capturing the unpaired electron from the free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) and compared it with the standard anti-oxidant Gallic acid. To test anti-inflammatory activity in an experimental model of acute inflammation, the carrageenan-induced in rat paw edema method was employed.The antioxidant and the anti-inflammatory activities of the Terpenoid fraction were found to be satisfactory.

Synthesis of 1,3-substituted 1H-indazole derivatives and evaluation of anti-inflammatory activity in Sprague Dawley rats

Indazole is a very significant group of heterocyclics. Aim of the research was thus planned to synthesize novel derivatives of indazole and evaluate their anti-inflammatory activity. Novel compounds of indazole were first synthesized from reaction of 2-chlorobenzonitrile with phenylhydrazine in presence of catalyst potassium t-butoxide (t-BuOK) and the solvent diglyme. Synthesized derivatives of indazole were analyzed by 1H-NMR and MS spectroscopic techniques. All the synthesized derivatives of indazole were evaluated for their anti-inflammatory activity in Sprague Dawley rats by carrageenan-induced rat paw edema method. All the synthesized derivatives of indazole had shown very good activity in both docking and anti-inflammatory activity in rats in comparison to the standard etoricoxib. Compound 1a in a dose of 30 ​mg/kg body weight had shown most significant inhibition of edema as compared to toxic group and the inhibition was comparable to that of the standard drug, etoricoxib in a dose of 10 ​mg/kg body weight. A convenient means for the synthesis of derivatives of indazole was developed which may find applications in heterocyclic synthesis of derivatives of indazole. Compound 1a i.e., 3-(4-carboxyphenyl)amino-1-phenyl-1H-indazole had shown best anti-inflammatory activity amongst all the synthesized compounds.

DOCKING STUDIES OF INDOLE ASSIMILATED PYRAZOLINE MOLECULAR HYBRIDS: DESIGN, SYNTHESIS AS ANTIINFLAMMATORY AGENTS AND ANTICANCER AGENTS

A series of novel compounds (4a-4l) have been synthesized by Claisen-Schmidt condensation, Schiff’s base and Cyclization mechanism. All the molecule structures were affirmation by IR, 1H NMR and Mass spectral data. The synthesized hybrids were screened for in vivo anti-inflammatory and invitro anticancer activities. Ant inflammatory activity was performed using carrageenan induced rat paw edema method using Diclofenac as standard drug. The anticancer activity has been assessing by using MTT assay against MCF7 and SKOV3 cell lines and Doxorubicin was used as reference standard. Among the compounds compound 4l exhibited the highest % inhibition of 98.4 when compared with the standard Diclofenac 94.2%.Compound 4f exhibited the lowest IC50 at concentration of 20.01µg against MCF7 cell lines and 32.87µg against SKOV3 cell lines. The molecular docking studies was performed using the Ligprep tool of Schrodinger suite. This study revealed that novel thiazolidne-4-one-pyrazole hybrids(4a-4j) had good interaction with the active site of EGFR receptor. Among the docked compounds, dock score of the compounds ranged from from -3.186 to -5.212. The highest score was exhibited by 4f with -5.212 with Glide binding energy of -34.697 Kcal/mol.

Antiinflammatory Activity of Polyherbal Gel Formulation

The present study has been undertaken with the aim to formulate and evaluate the new polyherbal gel formulation containing 0.3 % hydroalcoholic extract from Trigonellafoenum-graecum and Glycyrrhiza glabra for its topical anti inflammatory activity against carrageenan induced rat paw edema method .The studies were conducted on Wistar rats of either sex (150-180g).The polyherbal gel formulation was designed by using Carbopol 934, SodiumCMC, Trigonellafoenum-graecum, Glycyrrhizaglabra extract, Ethanol, propylene glycol 400, methyl paraben, propyl paraben, and required amount of distilled water. The skin ph (6.8-7) was maintained by drop wise addition of tri- ethanolamine. The prepared polyherbal gels were evaluated for physical appearance, pH, spreadability, skin irritation to observe side effect. It was inferred from the results that polyherbal gel formulations were good in appearance and homogeneity. The overall result of this research the prepared poly herbal gel formulation shows significant anti-inflammatory activity.

Antimicrobial, Antioxidant, Anti-Inflammatory and Acute Toxicity Screening of Leaf Extracts of Morinda lucida (Rubiaceae)

Introduction: Morinda lucida is a medicinal plant popular for its traditional uses in the treatment of several illnesses such as malaria, inflammation, diabetes, jaundice, hypertension and dysentery. In this study, the leaf extract of the plant which is the most commonly used in ethnomedicine was subjected to biological screenings for anti-microbial, anti-inflammatory and anti-oxidant activities, and oral acute toxicity test to confirm its claimed potency in traditional healthcare. Methods: The powdered dried leaf of Morinda lucida was successively extracted with petroleum ether, ethyl acetate and methanol to obtain the corresponding extracts. The extracts obtained were screened for phytochemicals, antimicrobial, antioxidant and anti-inflammatory activities as well as determined its acute toxicity concentration and total phenolic content. The inhibitory activity (sensitivity test) of the extracts was carried out using agar well diffusion method, while the minimum inhibitory concentration determination was done using tube dilution method with the mueller hinton broth used as a diluent. For sensitivity tests the diameters of the zones were measured using a transparent ruler calibrated in millimeter and the results were recorded. The free radical scavenging activity of the extracts of the leaves of Morinda lucida, based on the scavenging activity of the stable 2,2-Diphenyl-1-Picryl Hydrazyl (DPPH) free radical, was determined using the measurement of the absorbance at 517 nm of the reduction of violet to yellow color in the presence of antioxidants. The oral acute toxicity study was carried out in vivo using albino mice in two phases. Each phase had groups of animals and each group received 1200, 1600, 2900 or 5000 mg/kg of the extracts of dried leaves of M. lucida except the control which received normal saline. All the animals were subjected to four hours of fasting prior to treatment and their respective body weights taken. The mice were then carefully monitored for clinical signs of toxicity such as weakness or drowsiness, aggressiveness, loss of weight, diarrhea, discharge from eyes and ears, noisy breathing and the number of deaths in each treated group and the control. The observation was carefully recorded and result documented. For anti-inflammatory activity, Carrageenan induced rat paw oedema method was used and the animals were wistar rats (17-31 g) of either sex. The animals received the crude extract in three different doses (250, 500 and 1000 mg/kg) body weight with piroxicam (10 mg/kg) as the reference drug. Measurement of right hind paw in circumference was taken using digital caliper. Results: Phytochemical analysis showed the presence of alkaloids, phenols, terpenoids, flavonoids, reducing sugars, steroids, saponins, carbohydrates, lignans, xanthones and peptides but no anthraquinines. The phytochemicals were substantially in the methanol and ethylacetate extracts. The extracts exhibited characteristic strong Concentration-Dependent Activity (CDA) against the test organisms with zones of inhibition ranging from 10-23 mm at various concentrations. The petroleum ether extract was completely inactive against E. coli and K. pneumonia bacteria while ethyl acetate extract also showed no activity against K. pneumonia. However, the methanol extract demonstrated high activity against S. aureus, B. subtilis, E. coli, S. typhi, K. pneumonia and P. aeroginosa. All the extracts had no activity against the fungi C. albicans and A. niger. The extracts exhibited free radical scavenging activity of 66.2%, 55.3% and 45.0% at the concentration of 1.0 mg/ml, respectively for methanol, ethyl acetate and petroleum ether, compared to that of the standard, ascorbic acid, which recorded 81.7% at the same concentration. Using DPPH free radical and spectrophotometry, the extracts displayed reducing antioxidant power of 0.594, 0.408 and 0.396 nm, respectively for methanol, ethyl acetate and petroleum ether compared to the standard, ascorbic acid with 0.826 nm at 1.0 mg/ml. The extracts gave total phenolic content of 62.2, 106.0 and 170.7 mg/g for petroleum spirit, ethyl acetate and methanol, respectively. The results of the acute toxicity profile showed that all the animals of different body weights survived at all the concentrations ranging from the lowest concentration of 10 mg/kg to the highest concentration of 5000 mg/kg per oral test dose. Physical and behavioral observations of the experimental mice revealed no visible sign of acute toxicity. The extracts showed significant inhibitory effect on oedema formation at the doses of 250, 500 and 1000 mg/kg body weight when compared to the standard drug, piroxicam, at the dose of 10 mg/kg body weight. The oedema inhibition was found to be concentration dependent only with petroleum ether extract unlike the ethyl acetate and methanol extracts. Conclusion: The results of this study demonstrated that the various extracts of Morinda lucida have great potentials as antimicrobial, antioxidant, anti-inflammatory agents and have low toxicity. The leaf extracts can therefore safely be used to manage human pathogenic infections. These biological activities and the phyto-constituents validate its acclaimed ethnomedicinal uses.

Synthesis and anti-inflammatory activity of 2-amino-4,5-diphenyl-1-(substituted)-1H-pyrrole-3- carbonitrile derivatives

Pyrrole is privileged and active heterocycle with diverse pharmacological activities that specifically serve as a promising scaffold for antiinflammatory, antimalarial, antimicrobial, antiviral, antitubercular, and enzyme-inhibiting drugs. In an attempt to explore this scaffold, a series of 2- amino-4,5-diphenyl-1-(substituted)-1H-pyrrole-3-carbonitrilewere synthesized and screened for anti-inflammatory activity. The structures of synthesized novel compounds were characterized by 1H Nuclear Magnetic Resonance, Mass and Fourier Transfer Infrared spectroscopic data. All the compounds are screened for anti-inflammatory activity using the rat paw edema method. Among all, compound 1e exhibited more potent activity than the standard drug etoricoxib with the highest inhibition in paw edema at 3 h and 5 h.

Anti-inflammatory activity of methanol and ethyl acetate fractions of Sesbania grandiflora roots in rats

The anti-inflammatory potential of methanol and ethyl acetate fractions of Sesbania grandiflora Linn., roots were evaluated by carrageenan induced rat paw oedema method and cotton pellet induced granuloma in rats. Female Wistar rats were treated orally with methanol (MFSGR) and ethyl acetate (EAFSGR) fractions of Sesbania grandiflora roots (100 and 200 mg/kg) and Diclofenac sodium (15 mg/kg). One-hour post treatment, Carrageenan (0.1 ml of 1 % w/v, s.c.) was administered in the sub plantar region of the left hind limb of rat. Thereafter, paw volume was measured at 0, 30 min, 1, 2, 3 and 4 h. Percentage inhibition (PI) of oedema was calculated. In cotton pellet-induced granuloma model, male Wistar rats were treated with Diclofenac sodium (10 mg/kg, p.o.) and MFSGR and EAFSGR (100 and 200 mg/kg, p.o.) respectively. Thirty-minutes after respective treatment, an autoclaved cotton pellet of 20±1 mg was aseptically implanted subcutaneously. Fraction and standard diclofenac were administered once daily for the next 7 days. On 8th day, excised cotton granuloma was dried and weighed, body weight and organ index were calculated. MFSGR and EAFSGR (100 and 200 mg/kg) exhibited a significant inhibition in paw volume against carrageenan-induced paw oedema. In cotton pellet induced granuloma model, MFSGR and EAFSGR exhibited significant inhibition of cotton dry and wet weight. The present study suggests that the methanol and ethyl acetate fractions of Sesbania grandiflora roots exhibit anti-inflammatory activity. The observed effect could be attributed to the presence of vital phytoconstituents.

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 ACTIVITIES OF ALCOHOLIC EXTRACT OF CUSCUTA REFLEXA ROXB. STEM ON EXPERIMENTAL ANIMALS

Aim of the study: To evaluate the anti-Inammatory activity of alcoholic extract of Cuscuta reexa stem on experimental animals Stems of Cuscuta reexa were collected, air dried and powdered.Materials and Methods: Methanolic extract was obtained by percolating the dried powder with 99.8% methanol. Alcoholic extracts of Cuscuta reexa stem (100mg/kg) was used as test drug. Anti-inammatory activity was on acute inammation was evaluated by carrageenan induced rat paw oedema method and chronic inammation was studied by Freund's complete adjuvant-induced arthritis method. For each of the studies albino rats of either sex weighing 100-200gms were divided into 3 groups with 5 animals in each group. Group A received normal saline 10 ml/kg. Test groups B, received alcoholic extracts of Cuscuta reexa stem (100mg/kg), Standard group C received Aspirin (100mg/kg). Acute oral toxicity test of the extract was performed as per OECD 425 (OECD Guidelines, 2001). The results were analysed by ANOVA followed by Dunnett'sResults: multiple comparison test. Alcoholic extracts of Cuscuta reexa stem (100mg/kg) showed signicant (p<0.01) anti-inammatory activity when compared to the control in carrageenan induced acute inammation. AECR was also effective in chronic arthritis model. TheConclusion: present study indicates that alcoholic extracts of Cuscuta reexa stem (100mg/kg) showed signicant (p<0.01) anti-inammatory activity against acute inammation as well as chronic inammation.

Formulation and Evaluation of Herbal Gel of Alhagi Camelorum with its Anti-inflammatory Activity

This paper emphasizes the anti-inflammatory effects of Alhagi Camelorum. Most of the diseases are caused by a continuous swelling, including cancer. There is hence a need to neutralize inflammation. A. Camelorum, a medicinal plant, has been historically utilized as a remedy in Ayurveda and other systems of folk medicine. Thus, several techniques were utilized by Wister rats to examine A. Camelorum anti-inflammatory properties. The plant material was crushed into a coarse powder in a grinder after drying and stored at a room temperature for further investigation. The powdered plant material of A. Camelorum was subjected to successive solvent extraction (hexane, petroleum ether, chloroform, and methanol) in soxlet extraction method. Different extracts were analyzed using a traditional procedure to evaluate the various physicochemical properties. The HPTLC report is included to the file. It was discovered that the methanol and chloroform drug extract contained flavonoids (good anti-inflammatory properties) when quercetine was used as a marker. Topical gel of methanol and chloroform drug extract of A. Camelorum were prepared with Carbopol 934, hydroxypropyl methylcellulose (HPMC) and carboxymethyl cellulose. These gel formers have been created, tested, and gel chosen, which showed good propagation and consistency, to get the right consistency of the gel formulation. Gel containing methanol drug extract FM2 and FM10 formulation showed highest in-vitro release which were selected and subjected to carrageenan induced rat paw edema method. Our study reveals the anti-inflammatory effects of methanol extract of A. Camelorum were found to be significant.

Study of anti-inflammatory activity of aqueous and methanolic extracts of dry powder of zingiber officinale (SUNTH) in Wistar rats

To evaluate the anti-inflammatory activity of aqueous and methanolic extracts of dry powder of plant Zingiber Officinale (SUNTH). 1. To evaluate anti-inflammatory activity of all extracts in two doses and the standard drug in wistar rats by using Carrageenan induced paw edema method. 2. To compare anti-inflammatory activity of both extracts with that of standard drug. The study was conducted after animal ethics committee approval. Animals were divided into six groups. Control group received 0.2ml NS IP while test groups received aspirin (150mg/kg), Aqueous extract of dry powder of plant Zingiber Officinale (SUNTH) (100 and 200mg/kg), Methanolic extract of dry powder of Z. officinale (SUNTH) (100 and 200 mg/kg). Acute model of inflammation consisting of carrageenan induced rat paw edema method was used to investigate anti-inflammatory activity of Ginger. The present study clearly showed significant anti-inflammatory activity of aqueous and methanolic extracts of dry powder of plant Zingiber Officinale (p < 0.05) in acute model of inflammation when compared to control and its activity was comparable to aspirin at all time interval. Aqueous and methanolic extracts of dry powder of plant Zingiber officinale (SUNTH) have significant anti‑inflammatory property.

Anti-inflammatory Activity and Isolation of Luteolin from Plagiochasma appendiculatum Methanol Extract

Plagiochasma appendiculatum, a flavonoid rich liverwort, is reported to be used in the treatment of cuts, burns, outside wounds, bacteriostatic, pulmonary tuberculosis, neurasthenia, fractures, convulsions, scalds, uropathy, and inflammation by tribal communities. In the present study, flavonoid luteolin, reported to possess anti-inflammatory potential, is isolated from P. appendiculatum methanol extract and extract is evaluated for anti-inflammatory effect. Anti-inflammatory potential was studied by protein denaturation assay and carrageenan-induced rat paw edema method. Plant flavonoid is isolated from methanol extract by column chromatography, using petroleum ether and ethyl acetate in various proportion, as mobile phase. Further identified by spectroscopic analysis. In vitro studies, at a concentration of 800 μg/ml, P. appendiculatum methanolic extract (PAME) exhibited 74% inhibition while indomethacin showed 79% inhibition at the same concentration. The extract exhibits a decrease in inflammation in rat hind paw when tested with carrageenan-induced paw edema. PAME at a dose of 150 mg/kg displayed the most potent anti-inflammatory activity compared to the other groups during the course of the observation period. The methanol extract yielded a yellow color crystalline compound which is characterized as 2-(3,4-Dihydroxyphenyl)-5,7-dihydroxy-4-chromenone, commonly known as luteolin. Isolation of luteolin from P. appendiculatum is first time reported, which supports the ethnobotanical claims and provides scientific explanation for anti-inflammatory use of mentioned liverwort.

Study of anti-inflammatory activity of aqueous and methanolic extracts of fresh rhizome of Zingiber Officinale in Wistar rats

To evaluate the anti-inflammatory activity of aqueous and methanolic extracts of fresh rhizome of plant Zingiber officinale: 1. To evaluate anti-inflammatory activity of all extracts in two doses and the standard drug in wistar rats by using Carrageenan induced paw edema method. 2. To compare anti-inflammatory activity of both extracts with that of standard drug. The study was conducted after animal ethics committee approval. Animals were divided into six groups. Control group received 0.2ml NS IP while test groups received aspirin (150mg/kg) , Aqueous extract of fresh rhizome of Z. officinale (100 and 200mg/kg) , Methanolic extract of fresh rhizome of Z. officinale (100 and 200 mg/kg). Acute model of inflammation consisting of carrageenan induced rat paw edema method was used to investigate anti-inflammatory activity of Ginger. The present study clearly showed significant anti-inflammatory activity of aqueous and methanolic extracts of fresh rhizome (p < 0.05) in acute model of inflammation when compared to control and its activity was comparable to aspirin at all time interval. Aqueous and methanolic extracts of gingiber officinale have significant anti‑inflammatory property.

Zinc(II) complex: Spectroscopic, physicochemical calculations, anti-inflammatory and in silico molecular docking studies

As a continuation of the work in the present article, we described the spectroscopic and physicochemical properties of the synthesized Zn(II)-2-amino-3-pyridinecarboxaldehyde complex was investigated experimentally and theoretically. The zinc(II) complex was optimized with B3LYP and B3PW91 functional with 6–311++G(d,p) basis set. Fourier transform infrared spectrum of zinc(II) complex was recorded in the spectral range 4000–400 cm−1 and Raman counterparts were measured in the spectral region 4000–50 cm−1. The experimental FTIR and Raman results are compared to theoretical geometrical parameters. The rms error between experimental and theoretical vibrational frequencies of the titled compound was found to be 8.9 cm−1. The HOMO-LUMO energy gap demonstrates the compound is highly chemically reactive. The Natural Bond Orbital (NBO) and Quantum Theory of Atoms in Molecules (QTAIM) analyses were employed to obtain a precise picture of the conjugative and hyper conjugative interactions within the structure of the investigated molecule. Additionally, zinc(II) complex was also screened for their anti-inflammatory activity, using the carrageenan-induced rat paw edema method. The investigated complex exhibited significant anti-inflammatory potencies compared to standards. Furthermore, the compound was also assessed for their molecular docking studies against protein receptor cyclooxygenase COX-2 (PDBID: 5IKT) and showed their binding energy value of −7.98 kcal/mol, towards the anti-inflammatory activity.

ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF ETHANOLIC EXTRACT OF LEAVES OF PUNICA GRANATUM L. ON EXPERIMENTAL ANIMAL MODELS

Objective: The aim of the study is to evaluate the analgesic and anti-inflammatory activities of the ethanolic extract of Punica granatum L. (EEPG) on experimental animal models. Methods: Tail-flick method was used to test the central analgesic activity, using Pethidine as standard drug. The tail flick latencies or the basal reaction time of the animals were assessed using an analgesiometer. Glacial acetic acid induced writhing response was used to test the peripheral analgesic activity, using Aspirin as standard drug. Number of writhing responses was counted for 20 min in each group and the percentage protection was calculated. And Carrageenan induced rat paw edema method was used to test anti-inflammatory activity of EEPG against acute inflammation, using Aspirin as standard drug. The inhibition of rat paw edema was calculated in percentage. Results: In central analgesic activity, the extract and pethidine showed significant increase in the reaction time. In peripheral analgesic activity, the extract and aspirin significantly reduced the number of writhes induced by acetic acid. And in anti-inflammatory activity, the extract produced significant reduction of the carrageenan induced paw edema. Conclusion: The EEPG has demonstrated significant analgesic and anti-inflammatory activity.

Drug Design, Synthesis and Biological Evaluation of Heterocyclic Molecules as Anti-Inflammatory Agents.

Non-steroidal anti-inflammatory drugs (NSAIDs) are generally utilized for numerous inflammatory ailments. The long-term utilization of NSAIDs prompts adverse reactions such as gastrointestinal ulceration, renal dysfunction and hepatotoxicity; however, selective COX-2 inhibitors prevent these adverse events. Various scientific approaches have been employed to identify safer COX-2 inhibitors, as in any case, a large portion of particular COX-2 inhibitors have been retracted from the market because of severe cardiovascular events. This study aimed to develop and synthesize a novel series of indomethacin analogues with potential anti-inflammatory properties and fewer side effects, wherein carboxylic acid moiety was substituted using DCC/DMAP coupling. This study incorporates the docking of various indomethacin analogues to detect the binding interactions with COX-2 protein (PDB ID: 3NT1). MD simulation was performed to measure the stability and flexibility of ligand–protein interactions at the atomic level, for which the top-scoring ligand–protein complex was selected. These compounds were evaluated in vitro for COX enzymes inhibition. Likewise, selected compounds were screened in vivo for anti-inflammatory potential using the carrageenan-induced rat paw oedema method and their ulcerogenic potential. The acute toxicity of compounds was also predicted using in silico tools. Most of the compounds exhibited the potent inhibition of both COX enzymes; however, 3e and 3c showed the most potent COX-2 inhibition having IC50 0.34 µM and 1.39 µM, respectively. These compounds also demonstrated potent anti-inflammatory potential without ulcerogenic liability. The biological evaluation revealed that the compound substituted with 4-nitrophenyl was most active.

Exploration of Antioxidant, Anti-inflammatory and Anticancer Potential of Substituted 4-Thiazolidinone Derivatives: Synthesis, Biological Evaluation and Docking Studies

Heterocyclic scaffolds are playing the important role in drug discovery and development. Currently many heterocyclic scaffolds like thiazole, thiazolidinone or thiazolidinedione have proved to be vital or provide life support against cancer and inflammation. The present work reports the ten 4-thiazolidinone derivatives synthesized via conventional route using three subsequent steps. The structural identification of the compounds was determined through spectrophotometric analysis. Further, the synthesized compounds were subjected to antioxidant, anti-inflammatory, and anticancer activities. All the synthesized derivatives possessed good to moderate antioxidant effects with maximum scavenging exhibited by FP7 and FP10. The in vivo anti-inflammatory activity was performed by the carrageenan-induced rat paw edema method and the compounds FP4 and FP7 possessed maximum inhibition. The synthesized analogs were subjected to in vitro antitumor activity over MOLT-4, EAC cell lines and it was found that compounds FP4, FP7, and FP10 emerged out as the most potent analogs against the tested cell lines. Molecular docking studies were carried out using Auto Dock 4.2.6 software. Structure-activity relationship gave a clear picture of title compounds such as electron-donating (OH, OCH3) groups at arylidene ring at position-5 increase antioxidant activity and is decreased by the presence of an electron-withdrawing group at the same position. Chloro substituted phenyl imino group at second position enhanced the anti-inflammatory activity while substituting electron-donating groups on arylidene moiety attached with fifth position of 4-thiazolidinone improved the anticancer activity.