Formalin-induced Rat Paw Edema Research Articles

Design, synthesis of new 2,4-thiazolidinediones: In-silico, in-vivo anti-diabetic and anti-inflammatory evaluation

In this study, a series of nine novel heterocyclic compounds were synthesized through a concise three-step reaction process. The synthesis involved Knoevenagel condensation at the 5th position of the 2,4-thiazolidinedione or rhodanine ring-system. Comprehensive physicochemical and spectral analyses, including FTIR, Mass, 1H NMR and 13C NMR, were performed to characterize the synthesized compounds. The synthesized derivatives were subjected to evaluation for their potential in various therapeutic domains. In-vivo anti-diabetic activity was assessed diabetes induced wistar rats, anti-inflammatory effects were gauged using the carrageenan and formalin induced rat paw edema model. Additionally, the in-vitro PPAR-γ modulatory activity, glucose uptake by using Saccharomyces cerevisiae and rat hemidiaphragm and cyclooxygenase inhibitory activity along with scavenge free radicals was tested by FRAP and DPPH method. According to the potential binding patterns of the most potent anti-diabetic compounds, namely 7a and 13a with the active sites of target PPAR-γ (PDB ID: 5U5L), was obtained through molecular docking using Schrodinger’s Glide model. Among the tested compounds, the compound 13a demonstrated significant antidiabetic activity with reduction in blood glucose levels (108.5 ± 2.171 mg/dL), comparable to the effect of pioglitazone (101.66 ± 0.95 mg/dL), similarly anti-inflammatory activity at fourth hour paw volume 93.6% and thickness at 3.99 ± 0.076 mm, respectively closer to that of standard drug diclofenac sodium (91.2% and 4.7 ± 0.057 mm) in carrageenan-induced paw edema in rat. The compound 13a displayed promising COX-2 inhibitory activity (IC50 = 7.82 μM) and DPPH antioxidant activity showcasing its multifaceted therapeutic potential. This study not only presents multi-targeting approach and highlights the significant potential compounds as a lead molecule for further therapeutic development.

Chromone-based small molecules for multistep shutdown of arachidonate pathway: Simultaneous inhibition of COX-2, 15-LOX and mPGES-1 enzymes

As a new approach to the management of inflammatory disorders, a series of chromone-based derivatives containing a (carbamate)hydrazone moiety was designed and synthesized. The compounds were assessed for their ability to inhibit COX-1/2, 15-LOX, and mPGES-1, as a combination that should effectively impede the arachidonate pathway. Results revealed that the benzylcarbazates (2a-c) demonstrated two-digit nanomolar COX-2 inhibitory activities with reasonable selectivity indices. They also showed appreciable 15-LOX inhibition, in comparison to quercetin. Further testing of these compounds for mPGES-1 inhibition displayed promising activities. Intriguingly, compounds 2a-c were capable of suppressing edema in the formalin-induced rat paw edema assay. They exhibited an acceptable gastrointestinal safety profile regarding ulcerogenic liabilities in gross and histopathological examinations. Additionally, upon treatment with the test compounds, the expression of the anti-inflammatory cytokine IL-10 was elevated, whereas that of TNF-α, iNOS, IL-1β, and COX-2 were downregulated in LPS-challenged RAW264.7 macrophages. Docking experiments into the three enzymes showed interesting binding profiles and affinities, further substantiating their biological activities. Their in silico physicochemical and pharmacokinetic parameters were advantageous.

Anti-Inflammatory Activity of Ethanol Leaf Extract of Arthropteris Orientalis in Wistar Albino Rat

The study investigated the anti-inflammatory activity of ethanol leaf extract of Arthropteris orientalis in wistar albino rat. The plant extract was obtained with the procedure as described by Khalifa et al. [1] and both acute and chronic anti-inflammatory properties was assessed. Five groups of five animals each were utilized for acute and chronic inflammation respectively. Anti-inflammatory effect of the extract was evaluated on egg albumin induced paw edema in albino rats and edema induced by formalin in the wistar albino rats’ paw for acute and chronic inflammation respectively. The extract had 26.665% tannin while flavonoid, saponin, phenol, and glycoside had 0.784%, 0.631%, 0.183% and 0.057% respectively. The result revealed that the extract at 500 mg/kg exhibited significant inhibition (p<0.05) of systemic acute paw edema at the 4th hour of the second phase of edema in comparison with the standard drug. The results reveal that intraperitoneal administration of ethanol leaf extract of Arthropteris orientalis on formalin-Induced paw edema in wistar albino rats at (100 and 500mg/kg) and (100mg/kg) exhibited significant inhibition (p<0.05) in mean paw volumes on day 1 and 2 respectively. The extract did not produce any significant hematological change. These results show that Arthropteris orientalis has potential anti-inflammatory properties.

Exploring the therapeutic potential of Prinsepia utilis Royle seed oil: A comprehensive study on chemical composition, physicochemical properties, anti-inflammatory, and analgesic activities

Ethnopharmacological relevancePrinsepiautilis (PU) Royle, native to the Himalayan region, is a deciduous thorny shrub with numerous traditional uses of its roots, leaves and seeds for treatment of conditions such as rheumatic pain, joint pain, arthritis, and inflammation. Aim of the studyKeeping in mind the growing demand of products of natural origin as alternate medicine, the present study was undertaken to scientifically validate for the first time the traditional claims of healing pain and inflammation by evaluating the fatty oil isolated from the seeds using established in vitro and in vivo models. Materials and methodsPU Seeds were Soxhlet extracted using n-hexane and fatty oil was isolated. Chemical composition of the oil was established with the aid of Gas Chromatography-Flame Ionization Detection (GC-FID) and Gas Chromatography-Mass Spectrometry (GC-MS). The oil was then subjected to in vitro anti-inflammatory activity by following the established protocols of trypsin inhibitory and bovine serum albumin denaturation assays. The acute toxicity of the oil was also studied using OECD guidelines 423. The anti-inflammatory property of the oil was further evaluated using carrageenan-induced and formalin-induced edema in the rat paw. Moreover, hot plate latency and tail immersion assay were employed to evaluate analgesic activity of the oil. To establish the quality of the oil, various physicochemical properties were also studied. ResultsGC-FID and GC-MS analysis of the oil revealed the presence of linoleic acid (59.06 ± 0.00%), oleic acid (28.11 ± 0.01%), palmitic acid (9.51 ± 0.01%) and stearic acid (3.32 ± 0.01%). In vitro trypsin inhibitory and bovine serum albumin denaturation assay revealed dose-dependent notable activity of the oil with IC50 value of 63.57 μg/mL and 518.14 μg/mL, respectively. The physico-chemical characterization demonstrated that the oil possesses a low acidity and a high oxidative stability index. The oil was found to be non-toxic and displayed effective anti-inflammatory activities with significant inhibition till 4 h in carrageenan-induced and formalin-induced rat paw edema at maximum tested dose of 200 mg/kg b.w. The oil also exhibited significant results in hot plate latency and tail immersion assay with positive effects showing up to 4 h after dose administration. ConclusionThese findings, besides supporting the traditional claims, suggest that P. utilis seed oil has potential therapeutic applications as a natural anti-inflammatory and analgesic agent. Further studies are warranted to explore its mechanisms of action and potential use in pharmaceutical and nutraceutical industries.

Effect of solvents on anti-inflammatory and analgesic activities of leaves extract of Mussa paradisiaca Linn

The present study was undertaken to evaluate anti-inflammatory and analgesic activities of two different solvated leaves extracts of Mussa paradisiaca Linn (MP) on experimental animals. Anti-inflammatory activity was carried out using formalin induced rat paw edema and cotton pellet induced granuloma models. Analgesic activity was evaluated using acetic acid induced writhing and tail immersion models. Acute toxicity studies were carried out for the extracts and the test drug doses for screening were selected depending upon LD50 values. Aqueous and ethanolic leaves extracts of MP Linn in the dose of 200 & 400 mg/kg b.w, by oral route were used after confirmation of acute toxicity. Aspirin at a dose of 100 mg/kg, b.w was used as standard analgesic drug. Both doses of the extract inhibited the rat paw edema significantly (P<0.001) and significant (P<0.001) decrease in granuloma formation. It also suppressed the pain threshold of rat in tail immersion model (P<0.001), as well as inhibited the acetic acid induced writhing (P<0.001) when compared to the control group. It is concluded that the administration of aqueous and ethanolic leaves extracts of MP produced significant anti-inflammatory and analgesic effects in experimental animals by dose dependent manner but the ethanol leaves extract showed more significant activity than former solvent.

Anti –Inflammatory Effect of Methanolic and Aqueous Extracts of Urtica pilulifera L. Seed in Rats

Wide range of acute and chronic inflammatory ailments, side effects of their available therapies and incomplete treatment of such patients push the researches to find new and more effective drugs. To reach this aim, in the current study, we evaluate Urtica pilulifera L. (family Urticaceae) as an introduced traditional herb for treatment of inflammation in Persian Medicine (PM). In an animal study, Anti-inflammatory effects of U. pilulifera were assessed in formalin-induced hind paw edema in rats. Sodium salicylate (300 mg/kg, i.p., SS) injection was used as a positive control drug and compared with methanolic extract of U. pilulifera (20 mg/kg; i.p.) (MUP), three different doses of aqueous extract of U. pilulifera (20, 40 and 80 mg/kg; i.p.) (AUP) and a group of distilled water (6 mL/kg; i.p.). As acute anti-inflammatory effect, AUP in doses 40 and 80 mg/kg decreased edema significantly (p<0.05). In chronic anti-inflammatory response, results indicated that all AUP doses had anti-inflammatory effects (p <0.05) with no significant difference with SS group. In conclusion, AUP had anti-inflammatory effects on both acute and chronic edema; while MUP was only effective in chronic inflammation.

UHPLC-MS and GC-MS phytochemical profiling, amelioration of pain and inflammation with chloroform extract of Funaria hygrometrica Hedw. via modulation of inflammatory biomarkers.

People of Pakistan have undisturbed customs for the employment of medicinal plants for healthcare requisites. Chloroform extract of F. hygrometrica (CE FH) was examined for its ability to reduce inflammation and to produce analgesia. Carrageenan and formalin-induced paw edema model for inflammatory activity, hot-plate and tail-flick methods to assess analgesic activity were executed. Phytochemical analysis was done by UHPLC-MS and GC-mass spectrometer. The results demonstrated that in carrageenan-induced paw edema, maximum reduction in inflammation was observed at 5th hour at the dose 100mg/kg; while at doses 250 and 500mg/kg, maximum response was observed at 5th and 6th hours. Analgesic activity results indicated that maximum analgesia was observed up to 120min at 100mg/kg, while up to 90min in case of 250 and 500mg/kg doses. The formalin-induced rat paw edema showed significant (p < 0.05) anti-inflammatory activity after 5days treatment. After, testing period of 10days, the biochemical parameters such as CBC, CRP, serum enzymes like CAT, SOD, GSH and inflammatory mediators like TNF-α, IL-6, IL-4 and IL-10 were estimated. The administration of formalin resulted in an increase in the level of leucocytes, total WBC, CRP, serum enzymes and in the diameters of paw thickness, while pre-treatment with CE FH at dose levels of 100, 250 and 500mg/kg exhibited a diminution in the levels of SOD, GSH, CAT, total RBC and HB. Acute inflammatory mediators such as TNFα, IL -6 and IL-4 were reduced, and IL-10 was upregulated in the treated group as compared to the control. Many phytoconstituents, i.e., chitobiose, chlorovulone III, γ-tocotrienol, emmotin, cassine, hexacosanedioic acid, neophytadiene, fumaric acid, neophytadiene, hexadecanoic acid, phytol and stigmasterol were detected during UHPLC-MS and GC-MS analysis seems to be responsible for the said activity in correlation with the already reported data about these compounds. The results concluded that CE FH possess noteworthy anti-inflammatory and central analgesic action at different doses (100, 250 and 500mg/kg).

Bioflavonoid exerts analgesic and anti-inflammatory effects via transient receptor potential 1 channel in a rat model.

Pain is an uncomfortable sensation in the body. Kaempferol is a flavonoid with antinociceptive effects. Transient receptor potential (TRP) channels have been characterized in the sensory system. This study evaluated the central antinociceptive effect of Kaempferol and possible mechanisms of action of transient receptor potential cation channel subfamily V member 1 (TRPV1). Capsaicin as a TRPV agonist (5 μg/μL, intracerebroventricular [ICV]) and capsazepine as its antagonist (10 μg/μL, icv) were used to test the analgesic effect of kaempferol (1.5 mg, ICV). Morphine (10 μg, ICV) was used as a positive control. The other groups were treated with a combination of kaempferol and capsaicin, kaempferol and capsazepine, and capsaicin and capsazepine. The cannula was implanted in the cerebroventricular area. The tail-flick, acetic acid, and formalin tests were used to assess analgesic activity. For evaluation of antiinflammatory effect, the formalin-induced rat paw edema was used. Kaempferol significantly decreased pain in the acute pain models, including the tail-flick and the first phase of the formalin test. In the late phase of the formalin test, as a valid model of nociception, capsazepine inhibited the antinociceptive effect of kaempferol. Kaempferol has an analgesic effect in the acute pain model and can affect inflammatory pain. Also, the TRPV1 channel plays a role in the antinociceptive activity of kaempferol.

Синтез и определение активности нового производного гидроксиоксопиримидина — потенциального объекта для изготовления противовоспалительного геля

Introduction. Compounds with a hydroxypyrimidine fragment in their structure exhibit pronounced and diverse biological activity. The low solubility of many hydroxypyrimidine derivatives in water is a significant drawback in the development of new medicines. From 5-butyl-6-hydroxy-2,3-diphenylpyrimidin-4(3H)-one, its water-soluble form being a sodium salt was obtained. This compound, as it was revealed during the computer screening of its possible biological acti¬vity in silico, can potentially be used as a pharmaceutical substance for the production (manufacture) of drugs. Since the line of hydroxypyrimidine drugs in the topical dosage forms is extremely limited, and the resulting compound has hydrophilic properties, it is important to enclose the substance in a gel dosage form. Aim. Synthesis of a water-soluble form of new hydroxypyrimidine derivative, determination of its acute toxicity and anti-inflammatory activity, as well as critical stages of development and further production of a topical hydrophilic dosage form based on the obtained compound. Materials and Methods. The target compound was obtained from the interaction of 5-butyl-6-hydroxy-2,3-diphenylpyrimidin-4(3H)-one and an equimolar amount of an aqueous solution of sodium hydroxide. Acute toxicity was determined on white mice (5 groups of 10 animals, which were injected with a solution of the study compound at a dose of 1100, 1200, 1300, 1400, and 1500 mg/kg respectively), observing the development of the main symptoms and recording the time of death of the animals within 72 h from the moment of the drug administration. For the experimental assessment of anti-inflammatory activity, two models were used: formalin-induced mice paw edema and cotton pellet implantation-induced granuloma in rats (for each model there were 3 groups with 10 animals per group: the 1st group received the reference drug diclofenac, the 2nd – the compound under study, the 3rd (control) – sodium chloride solution). Results. The yield of the obtained sodium 5-butyl-1,2-diphenyl-6-oxo-1,6-dihydropyrimidine-4-olate was 85 ± 1%. It has been proven in vivo that the test compound belongs to the 5th class of toxicity (practically non-toxic) and has a pronounced anti-inflammatory activity. An Ishikawa diagram was drawn up to determine the critical stages of the development and manufacture of a semisolid dosage form, a gel with a target substance. Conclusion. A new compound with anti-inflammatory action has been synthesized, sodium 5-butyl-1,2-diphenyl-6-oxo-1,6-dihydropyrimidin-4-olate, which has low toxicity and pronounced anti-inflammatory activity. The critical stages in the development and manufacture of a gel with synthesized compound are: preparation of the base and drug substance, introduction of the drug substance into the base, homogenization and packaging.

Total phenolic and flavonoid contents, cytotoxic, immunomodulatory and anti-inflammatory potential of whole plant of Astragalus creticus (Fabaceae)

Purpose: To determine total phenolic and flavonoid contents, as well as the cytotoxic, immunemodulatoryand anti-inflammatory potentials of the whole plant of Astragalus creticus (Fabaceae).Methods: Folin-Ciocalteu (FCR) method was used for determination of total phenolic and flavonoid contents of the methanol and dichloromethane extracts of Astragalus creticus. The cytotoxic potential of the extracts on 3T3 and HeLa cell lines were evaluated using MTT assay. Brine shrimp larvae mortality was determined by lethality bioassay, while inhibitory effects were determined on mouse fibroblast (3T3)and cervical cancer (HeLa) cell lines. In vitro immunomodulatory and in vivo anti-inflammatory effectswere assessed using reactive oxygen species (ROS) chemiluminescence and formalin-induced rat paw edema assays, respectively.Results: Dichloromethane extract had higher contents of phenolics (TPC = 324.75 ± 2.47 mg GAE/g) and flavonoids (TFC = 95.51 ± 0.82 QE/g) than the methanol extract (TPC = 79.82 ± 1.53 mg GAE/g, TFC = 56.11 ± 0.93 QE/g). The dichloromethane extract exhibited high cytotoxic andimmunomodulatory potentials, with 76.66 % mortality in brine shrimp lethality bioassay and 83.9 % inhibition (IC50 = 18.0 ± 1.1 μg/mL) in chemiluminescence assay. The extract also resulted in 22 and 13 % inhibition of viability of HeLa and 3T3 cells, respectively, while the methanol extract produced 13 % inhibition of both cell lines. The methanol extract produced very significant anti-inflammatory activity,with a maximum of 49 % inhibition of paw edema at a dose of 160 mg/kg (p &lt; 0.01).Conclusion: These results suggest that the dichloromethane and methanol extracts of Astragalus creticus (Fabaceae) exert cytotoxic, immunomodulatory and anti-inflammatory effects. These findings provide scientific validation for the traditional medicinal use of the Astragalus genus.

Effect of ethanolic extract of Stachys pilifera Benth on subacute experimental models of inflammation and some underlying mechanisms.

Background and purpose:This study was designed to evaluate the anti-inflammatory activities of S. pilifera (HESP) in two sub-acute models of inflammation and clarified some possible mechanisms.Experimental approach:Colorimetric methods were used to determine total phenol and flavonoid contents. Carrageenan or formalin-induced rat paw edema (seven days) and multiple application TPA-induced ear edema in mice (9 days) were used. The concentration of IL-1 and TNF-α were measured in the inflamed paw, as well as MDA levels in the serum and liver. Histopathological studies and in vitro anti-inflammatory effects of the extract were also studied using heat-or hypotonicity-induced hemolysis in RBC humans.Findings/Results:Total phenol and flavonoid contents of HESP were 101.35 ± 2.96 mg GAE/g extract and 660.79 ± 10.06 mg RE g extract, respectively. Oral (100 and 200 mg/kg) and topical application (5 mg/ear) of HESP significantly inhibited formalin-induced paw edema and multiple TPA-induced ear edema. The extract also significantly decreased the serum and liver levels of MDA in the carrageenan and formalin tests. The elevated levels of TNF-α and IL-1β in the carrageenan-injected paw were not affected by HESP. The extract (50-800 μg/mL) inhibited heat-or hypotonicity-induced hemolysis. Histopathological examination of the inflamed tissues revealed that HESP inhibited congestion and leukocyte infiltration.Conclusion and implications:The findings confirmed the potent anti-inflammatory effects of S. pilifera in two sub-acute inflammation models and suggested that these properties were not related to IL-1 and TNF-α, but could be attributed to inhibition of lipid peroxidation, membrane stabilization, and inhibition of leukocyte penetration.

The Anti-Inflammatory Effect of a γ-Lactone Isolated from Ostrich Oil of Struthio camelus (Ratite) and Its Formulated Nano-Emulsion in Formalin-Induced Paw Edema.

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory in eczema and contact dermatitis. The anti-inflammatory effect of a γ-lactone (5-hexyl-3H-furan-2-one) isolated from ostrich oil and its formulated nano-emulsion in formalin-induced paw edema was investigated in this study. Ostrich oil was saponified using a standard procedure; the aqueous residue was fractionated, purified, and characterized as γ-lactone (5-hexyl-3H-furan-2-one) through the interpretation of IR, NMR, and MS analyses. The γ-lactone was formulated as nano-emulsion using methylcellulose (MC) for oral solubilized form. The γ-lactone methylcellulose nanoparticles (γ-lactone-MC-NPs) were characterized for their size, shape, and encapsulation efficiency with a uniform size of 300 nm and 59.9% drug content. The γ-lactone was applied topically, while the formulated nanoparticles (NPs) were administered orally to rats. A non-steroidal anti-inflammatory drug (diclofenac gel) was used as a reference drug for topical use and ibuprofen suspension for oral administration. Edema was measured using the plethysmograph method. Both γ-lactone and γ-lactone-MC-NPs showed reduction of formalin-induced paw edema in rats and proved to be better than the reference drugs; diclofenac gel and ibuprofen emulsion. Histological examination of the skin tissue revealed increased skin thickness with subepidermal edema and mixed inflammatory cellular infiltration, which were significantly reduced by the γ-lactone compared to the positive control (p-value = 0.00013). Diuretic and toxicity studies of oral γ-lactone-MC-NPs were performed. No diuretic activity was observed. However, lethargy, drowsiness, and refusal to feeding observed may limit its oral administration.

Formulation and preclinical evaluation of Anti-inflammatory activity of Triticum aestivum

A wide scope of medical advantages has been credited to wheatgrass, the young grass of the wheat plant Tritium aestivum. Wheat grass is a decent wellspring of mineral supplements. It contains critical measures of iron, phosphorous, magnesium, manganese, copper and zinc. Wheatgrass is a rich supplement of tocopherols with high vitamin E content. Wheatgrass is beneficial in restoring more infections due to its significant function that, it can arrest the development of antagonistic microbes which are responsible for spreading certain diseases. constituents of wheatgrass may be obtained from fresh juice, frozen juice, powder, tablets with compositions differing as per their production methods which otherwise depends on growing conditions of wheatgrass. Anti-inflammatory activity of wheatgrass tablets was assessed by using formalin induced rat paw edema model. The results obtained were compared with aceclofenac, standard drug.&#x0D; Keywords: Triticum aestivum, Flaxseed gel, Anti-inflammatory, Aceclofenac, Formalin.

Directed Search of Anti-inflammatory Agents Among (3HQuinazoline- 4-ylidene)hydrazides of N-protected Amino acids and their Heterocyclization Products.

Background: (Quinazoline-4-ylidene)hydrazides are valued intermediates in modern organic chemistry, as they are commonly used for the synthesis of substituted [1,2,4]triazolo [1,5-c]quinazolines.Objective: Unknown N-acyl-2-([1,2,4]triazolo [1,5-c]quinazoline-2-yl)-alkyl-(alkaryl-, aryl-)amines were synthesized and evaluated for anti-inflammatory potential.Methods: The peculiarities of the synthesized compounds structures were studied by IR-, NMR spectroscopy and chromatography-mass spectrometry and were discussed in detail. Probable molecular mechanisms of activity (inhibition of COX-1 and COX-2) were predicted due to molecular docking. Anti-inflammatory activity of synthesized compounds was determined by their ability to reduce the formalin-induced paw edema in rats. Diclofenac sodium was used as reference drug.Results: In this study, the synthesis of N-acetyl-(benzoyl)-2-([1,2,4]triazolo [1,5-c]quinazo-linе-2-yl)alkyl-(aralkyl-, aryl-)amines, using (3H-quinazoline-4-ylidene)hydrazides of N-protected amino acids or 4-hydrazinoquinazoline and N-prorotected amino acids as starting compounds was developed. It was established that the reaction of (3H-quinazoline-4-ylidene)hydrazides of Boc-amino acids occurred with the formation of N-acetyl-substituted triazoloquinazolines. High anti-inflammatory activity was detected for unknown (3H-quinazoline-4-ylidene)hydrazides Boc-amino acids (1.13-1.15) and N-acetyl-(benzoyl)-2-([1,2,4]triazolo [1,5-c]quinazoline-2-yl-)aralkyl-(aryl-)amines (3.2, 3.3, 3.11, 3.12), using the experimental formalin test.Conclusion: The conducted SAR-analysis allowed to detect critical fragments. Namely, the Boc-aminoaralkyl-(aryl-)acid residue in (3H-quinazoline-4-ylidene)hydrazides (1.13-1.15), benzyl and phenyl linker groups in N-acetyl-(benzoyl)-2-([1,2,4]triazolo [1,5-c]quinazoline-2-yl-)aralkyl-(aryl-) amines (3.2, 3.3, 3.11, 3.12) are believed to be substantial for anti-inflammatory activity.

Evaluation of Wound healing and Antiinflammatory Activities of New Poly-herbal Formulations

Present investigation evaluated the impact of poly-herbal formulations comprising extracts of Zingiberofficinale, Curcuma longa, Aloe barbadensis, Citrus aurantium, Emblica officinalis and castor oil on wound healing activity using excision wound model and antiinflammatory activity using formalininduced pawedema method. Ointments containing 2, 4 and 6 % w/w of extracts were made and used in wound healing action and all the formulations significantly (p<0.01) reduced the wound area. Ointment of 6 % w/w has shown better results than 2 and 4 % w/w. These results were compared to that of the standard framycetin. Poly-herbal formulation-1, poly-herbal formulation-2 and poly-herbal formulation-3 were prepared and used at doses of 100, 300 and 500 mg/kg to determine antiinflammatory activity. All poly-herbal formulations significantly (p<0.01) inhibited formalin-induced rat paw edema. Poly-herbal formulation-3 displayed greater inhibition than poly-herbal formulations 1 and 2. These results were comparable to that of the standard diclofenac. Present work and previous studies on poly-herbal formulations corroborates that these are safer and effective in treating inflammation and wounds.

In Vitro and In Vivo Evaluation of the Anticancer and Anti-inflammatory Activities of 2-Himachelen-7-ol isolated from Cedrus Libani

Cedrus libani is a majestic evergreen tree native to the Mediterranean mountains of Lebanon, Syria and Turkey. In this study, the tree heart wood was extracted using hexane to produce C. libani oil extract (CLOE) as a dark oil. GCMS analysis of CLOE identified up to 30 compounds whereby 2-himachalen-7-ol (7-HC) was the most abundant (40%). 7-HC was isolated using column chromatography and the identity of the white crystalline solid was confirmed via NMR spectroscopy and X-Ray Crystallography. 7-HC demonstrated potent cytotoxic activity against several human cancer cell lines including brain (SF-268, IC50 8.1 μg/mL) and colon (HT-29, IC50 10.1 μg/mL; Caco-2, IC50 9.9 μg/mL) with ovarian (Sk-OV-3, IC50 > 50 μg/mL) cells being the most resistant. However, while HT-29 displayed resistance to Cisplatin, 7-HC was 8–10 folds more potent. Co-treatment with 7-HC and Cisplatin showed a significant synergistic anti-proliferative effect against SF-268, HT-29 and Caco-2 cells. 7-HC also exhibited significant anti-inflammatory effect in formalin-induced paw edema in rats. Western blot analysis revealed that 7-HC displayed dose dependent inhibition of LPS-induced COX-2 protein expression in isolated rat monocytes. The present study demonstrates that 7-HC possesses promising anticancer and anti-inflammatory activities, and may serve as a lead molecule in cancer therapy.

Analgesic and Anti-inflammatory Activities of the Stem Bark of Yellow Flamboyant (&lt;i&gt;Peltophorum pterocarpum&lt;/i&gt;)

Peltophorum pterocarpum (family; Fabaceae) is an evergreen perennial crop grown in tropical gardens. Different parts of this tree are being used for the management of many diseases. This study investigated the acute toxicity, analgesic and anti-inflammatory potentials of n-hexane extract of P. pterocarpum stem bark. Acute oral toxicity of n-hexane extract of P. pterocarpum stem bark was investigated using standard method. Analgesic activity was investigated by using acetic acid-induced writhing model, using indomethacin as a reference drug. Antiinflammatory activity of n-hexane extract of P. pterocarpum stem bark was investigated by using formalin-induced paw licking model, using aspirin as standard drug. In the acute toxicity study, mortality was observed at 500 and 2500 mg/kg body weight. In the acetic acid induced writhing test, the n-hexane extract of P. pterocarpum (100 and 200 mg/kg body weight) showed a significant reduction in the number of writhing with 55.5 % and 60 % of inhibition respectively. In formalin-induced rat paw oedema test for acute inflammation, the n-hexane extract of P. pterocarpum in 50, 100 and 200 mg/kg body weight showed 26.00 %, 27.89 % and 32.27 % inhibition of oedema respectively after 4hours, which is comparable to that of standard drug-aspirin (33.59 %). These results validated that the extract of P. pterocarpum possesses significant analgesic and anti-inflammatory properties.Keywords: Peltophorum pterocarpum, acute toxicity, analgesic activity, anti-inflammatory activity

In vivo Antiinflammatory Potential of Leaf Extracts of Acacia auriculiformis Benth.

The prime objective of the present study was to evaluate the probable in vivo antiinflammatory potential of various extracts of the leaves of Acacia auriculiformis Benth. using carrageenan and formalin-induced inflammation in the rats. Thereafter gas chromatography-mass spectrometry analysis of the bioactive extract was performed to identify the compounds responsible for the antiinflammatory activity. The in vitro antioxidant potential was determined through 2,2-diphenyl-1-picrylhydrazyl scavenging assay, hydrogen peroxide scavenging assay and reducing power assay. Overall butanol and methanol leaf extracts showed significant antioxidant free radical scavenging activity. The methanol and petroleum ether leaf extracts at a dose of 400 mg/kg showed the highest percent inhibition of 84.88 and 82.12, respectively in the carrageenan-induced rat paw edema model, whereas, in formalin-induced rat paw edema model the chloroform and methanol leaf extracts showed the highest percent inhibition of 65.68 and 63.34 at a dose of 400 mg/kg, respectively. In both the antiinflammatory models, indomethacin (standard, 40 mg/kg) was used for comparison with test extracts. The gas chromatography-mass spectrometry analysis of bioactive butanol and methanol extracts showed the presence of compounds like sterols (stigmasterol, β-sitosterol and γ-sitosterol) and phenolic compounds (phenol, 2,4-bis(1,1-dimethylethyl),2,4-ditert-butylphenol), which could be responsible for the pharmacological activities observed. These in vitro and in vivo studies indicated that the antiinflammatory and antioxidant potential of the methanol leaf extract of Acacia auriculiformis Benth. could due to the presence of high phenolic and sterol content.

Anti-inflammatory properties of Dirinaria consimilis extracts in albino rats

BackgroundEarlier, the lichens are used in traditional medicines by different cultures across the world. As the Dirinaria genus has been shown to be biologically active against inflammation in folklore, we assessed the in vitro and in vivo anti-inflammatory profile of Dirinaria consimilis.Material and methodsInitially, the hydroalcoholic extract of lichen, D. consimilis (Dc-HE) was prepared and re-extracted with n-hexane, chloroform, ethyl acetate, acetone and methanol. The resultant extracts were evaluated for their in vitro (protein denaturation method), acute toxicity and in vivo (formalin-induced rat paw oedema assay) anti-inflammatory studies.ResultsAmong all the tested extracts, the acetone and chloroform extract of D. consimilis depicted prominent anti-inflammatory activity in both the bioassays. The acetone extract inhibited protein denaturation with IC50 value of about 468 µg/mL while the standard (Indomethacin) with 120 µg/mL. Moreover, the Dc-HE was screened for acute toxicity studies in male albino rats up to 2000 mg/Kg b.w dosage. The in vivo anti-inflammatory analysis of acetone extract (200 mg/mL) showed potent reduction of rat paw oedema nearer to that of the standard, whereas chloroform extract depicted moderate depletion and the other extracts revealed mild inhibitory profile against inflammation.ConclusionThis study reveals that the lichen, D. consimilis might be a good source of anti-inflammatory agents.

Phytochemical Screening, Acute Toxicity , Analgesic And Anti-Inflammatory Effects Of Apricot Seeds Ethanolic Extracts

The aim of present study was to investigate the phytochemical screening, acute toxicity and some pharmacological activities of ethanolic extract 70 % and 99.9% of apricot seeds. The phytochemical screening was done for determination of total phenolic compounds by Folin–Ciocalteu method, total flavonoids by aluminum chloride colorimetric method and total carotenoids by colorimetric method. The acute toxicity was done for determination of LD50 in mice by oral administration of upgraded doses of the extracts. The anti-inflammatory activity was done in vivo by formalin-induced paw edema in rats. The analgesic activity was carried out in mice by writhing test and hot plate method. Phytochemical screening revealed that the amount of total phenolic compounds was 179.4 and 191.2 µg gallic acid equivalent / g dry extract and the amount of total flavonoids was 226.18 and 509.34 µg rutin equivalent / g dry extract and the amount of total carotenoids was 0.145 and 0.156 mg/g dry extract for 70 % and 99.9% ethanolic extract, respectively. The acute toxicity revealed that both extracts had no toxic symptoms in rats and no mortalities appear by upgraded doses of 1 g to 10 g / kg b.wt. The 70% and 99.9% ethanolic extracts exhibited significant analgesic and anti-inflammatory activites in a dose of 100 mg/kg b.wt. of both extracts. These results suggest that apricot seed extracts contain significant level of safe non-toxic phytochemical substances that have significant analgesic and anti-inflammatory activities.