Acute Paw Edema Research Articles

In-vitro, in-vivo and in-silico anti-inflammatory evaluation of hedychenone and its semisynthetic derivative

Hedychium spicatum is a perennial shrub that is commonly found in the Himalayan region. Thin layer chromatography fingerprint screening of various Hedychium species revealed that only the species Hedychium spicatum possesses hedychenone. Purification and isolation of hedychenone was carried out from methanolic extract of Hedychium spicatum rhizomes powder using column chromatography. After crystallization of enriched fraction, 2.19% of hedychenone crystalline powder was yielded. The physiochemical, pharmacokinetic, and pharmacodynamic evaluation of the active pharmaceutical components was conducted using artificial learning and machine learning (AL/ML) approaches. The results indicate that both medications adhere to Lipinski’s rule of five. The docking study indicated that compound 2 (MBE-10.4 kcal/mol) exhibited a more sub-stantial interaction with the cannabinoid receptor 2 compared to hedychenone (MBE -9.85 kcal/mol). A study was done to assess the physical and chemical stability of hedychenone under biological pH conditions. Furthermore, the administration of both medication concentrations, 100 mg/kg and 200 mg/ kg, effectively inhibits the development of acute paw edema caused by ovalbumin. A preliminary investigation of hedychenone and its synthetic derivative indicated that these compounds have the potential to be utilized as active medicinal ingredients in herbal pharmaceutical preparations.

Pharmacological evaluation of 2-(2-hydroxy phenylimino)-N-(2-chlorophenyl)-5-isopropyl-4-methylthiophene-3-carboxamide compound for anti-inflammatory activity in rats

Background: Thiophene, also known as thiofuran, is a heterocyclic molecule represented by the chemical formula C4H4S. Aims and Objectives: The aim of this study was to evaluate the anti-inflammatory activity of 2-(2-hydroxy phenylimino)-N-(2-chlorophenyl)-5-isopropyl-4-methylthiophene-3-carboxamide compound in Wistar rats by acute carrageenan-induced paw edema and chronic cotton pellet-induced granuloma methods. Materials and Methods: This study consists of two stages: An acute inflammation study using carrageenan-induced paw edema in rats, which involves four groups of rats, and a chronic inflammation study using cotton pellet-induced granuloma, which involves three groups of rats. Mean paw edema volume and percentage of inhibition were measured in acute stage. The mean weight of the pellets in each group was determined during the chronic stage. Results: There was increase in the mean paw volume at 3 h and a slow decrease at 6 h and 24 h in control group to thiophene derivative-20 mg/kg/p.o from 0 h to 24 h. The mean difference from control and at 3 h, 6 h, and 24 h showed that mean difference was slowly decreased and it was statistically significant. The mean dry granuloma weight in control group, i.e., 10% tween 80 treated group was 146.6 ± 4.38. The mean dry granuloma weight in standard group, i.e., indomethacin 3 mg/kg treated group was 87.7 ± 3.41. The mean dry granuloma weight in substituted thiophene 10 mg/kg group was 101.91 ± 3.76. Conclusions: The newly synthesized substituted (fused) thiophene compound demonstrated inhibition of inflammation in both acute inflammation induced by carrageenan-induced paw edema and chronic inflammation induced by cotton pellet-induced granuloma in Wistar rats. The compound’s anti-inflammatory effects were comparable to those of the standard drug indomethacin, with a dosage of 10 mg/kg in the acute model and 3 mg/kg in the chronic inflammation model. This concludes that the test compound has anti-inflammatory activity.

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.

Discovery of novel aporphine alkaloid derivative as potent TLR2 antagonist reversing macrophage polarization and neutrophil infiltration against acute inflammation.

Toll-like receptor 2 (TLR2) mediated macrophages regulate the protective immune response to infectious microorganisms, but the aberrant activation of macrophages often leads to pathological inflammation, including tissue damage. In this study, we identified antagonists of TLR2 by screening 2100 natural products and subsequently identified Taspine, an aporphine alkaloid, as an excellent candidate. Furthermore, analysis of the 10 steps chemical synthesis route and structural optimization yielded the Taspine derivative SMU-Y6, which has higher activity, better solubility, and improved drug-feasible property. Mechanistic studies and seq-RNA analysis revealed that SMU-Y6 inhibited TLR2 over other TLRs, hindered the formation of TLR2/MyD88 complex, and blocked the downstream NF-κB and MAPK signaling pathway, thus suppressing the release of inflammatory cytokines. SMU-Y6 could stabilize TLR2 and bind to TLR2 protein with a Kd of 0.18μmol/L. Additionally, SMU-Y6 could efficiently reverse the M1 phenotype macrophage polarization, reduce the production of cytokines as well as infiltration of neutrophiles and alleviate the local inflammation in mice with acute paw edema and colitis. Collectively, we reported the first aporphine alkaloid derivative that selectively inhibits TLR2 with high binding affinity and superior drug-feasible property, thus providing an urgently-needed molecular probe and potential drug candidate for inflammatory and autoimmune disease therapy.

Investigation of chalcone cyclized pyrazole derivatives as an anti-inflammatory agent: In-vivo and in-silico molecular docking approach

A novel pyrazole condensed with chalcone and pyrazoline derivatives have been synthesized and evaluated against anti-inflammatory activity using a standard method of acute carrageenan-induced rat paw edema in vivo. NJD1 would be the most potent compound (30.10 ± 0.02%) found to be inhibitory in rats and exhibiting activity similar to celecoxib as a reference standard. Molecular docking studies have been conducted on PDB: 1TD7, the 3D X-ray crystallographic structure of group I protein phospholipase A2 (PLA2), -5.609 kcal/mol is the binding affinity of the standard celecoxib. The synthesized derivatives NJD1 and NJD2 (-6.283, -6.057 kcal/mol) has exhibited greater binding affinity, respectively.

Cинтез, антиэкссудативные и противовоспали-тельные свойства замещенных 2-метил-4-(2-фурил)-N-(2,4-дихлорфенил)-5-циано-1,4-дигидропиридин-3-карбоксамидов

One-pot reaction of cyanothioacetamide, N-(2,4-dichlorophenyl)acetoacetamide and furfural in the presence of excessive N-methylmorpholine in EtOH at 25 °C gives N-methylmorpholinium 5-[(2,4-dichlorophenyl)carbamoyl]-3-cyano-4-(2-furyl)-6-methyl-1,4-dihydropyridin-2-thiolate, yielding 82%. Subsequent S-alkylation of the prepared thiolate with N-substituted α-chloroacetamides occurs in a regiospecific way to form N-(2,4-dichlorophenyl)-5-cyano-4-(2-furyl)-2-methyl-6-[(2-oxo-2-{[substituted aryl]amino}ethyl)sulfanyl]-1,4-dihydropyridin-3-carboxamides 10–17. Compounds 10–17 were identified by means of IR and NMR spectroscopy, as well as by elemental analysis. Synthesized compounds 10–17 were examined for anti-exudative and anti-inflammatory activity. White laboratory rats numbering 112 individuals were divided into control (“acute formalin-induced paw edema”) and intact groups, 4 reference groups (acetylsalicylic acid, indomethacin, nimesulide, and paracetamol) and 8 experimental groups, according to the number of tested 1,4-dihydropyridine derivatives. The efficacy of the anti-inflammatory activity of the samples was evaluated in the model of “acute formalin paw edema” in rats, which was simulated by injecting 0.1 mL of 2% formalin solution into the aponeurosis of the right hind limb. The studied compounds were given intragastrically at a dose of 5 mg/kg 1.5 hours before the induction of the inflammatory process. Oncometric changes were measured quantitatively by limb girth. It was shown that the most pronounced anti-inflammatory activity was possessed by: N-(2,4-dichlorophenyl)-5-cyano-4-(2-furyl)-2-methyl-6-[(2-oxo-2-{[3-(trifluoromethyl)phenyl]-amino}ethyl)sulfanyl]-1,4-dihydropyridin-3-carboxamide 12 (1.09–1.81 times more effective than the reference drugs); 6-[(2-anilino-2-oxoethyl)sulfanyl]- N-(2,4-dichlorophenyl)-5-cyano-4-(2-furyl)-2-methyl-1,4-dihydropyridin-3-carboxamide 16, which reduced the induced paw edema by 42.91% compared to control; N-(2,4-dichlorophenyl)-5-cyano-4-(2-furyl)-2-methyl-6-({2-[(3-methylphenyl)amino]-2-oxoethyl}sulfanyl)-1,4-dihydropyridin-3-carboxamide 14 (1.65–2.85 times higher anti-inflammatory activity compared to the reference drugs in 18-hour experiments). N-(2,4-Dichlorophenyl)-5-cyano-4-(2-furyl)-2-methyl-6-({2-[(3,5-dimethylphenyl)amino]-2-oxoethyl}sulfanyl)-1,4-dihydropyridin-3-carboxamide 11 was found to be the most active, reducing paw edema 2.9 times more effectively than nimesulide

Atrial Natriuretic Peptide (ANP) Suppress λ-Carrageenan-Induced Acute Paw Edema by Modulating Pro-inflammatory Genes in Swiss Albino Mice

Atrial Natriuretic Peptide (ANP) Suppress λ-Carrageenan-Induced Acute Paw Edema by Modulating Pro-inflammatory Genes in Swiss Albino Mice

Oral administration of botryosphaeran [(1 → 3)(1 → 6)-β-d-glucan] reduces inflammation through modulation of leukocytes and has limited effect on inflammatory nociception.

Several biological activities of the fungal exopolysaccharide (1 → 3)(1 → 6)-β-d-glucan (botryosphaeran) have been described in the literature, but its effects on inflammation have not been evaluated. This study aimed to investigate the action of botryosphaeran on experimental mice models of carrageenan-induced acute pleurisy and acute paw edema, and complete Freund's adjuvant-induced persistent paw edema. All botryosphaeran doses tested (1.0, 2.5, 5.0, and 10.0 mg/kg birth weight [b.w.], orally administered) reduced leukocyte recruitment, nitric oxide (NO) levels, and protein extravasation in the pleural cavity. Botryosphaeran (5 mg/kg b.w.) did not diminish edema and mechanical hyperalgesia in the paw within 4 h; however, cold allodynia was alleviated within the first 2 h. In the persistent paw inflammation model, the effects of daily oral administration of botryosphaeran (5 mg/kg b.w.) were evaluated over 3 and 7 days. The fungal β-glucan significantly reduced the levels of the cytokines, tumor necrosis factor(TNF)-α, interleukin (IL)-6), and IL-10, in the paw homogenates in both protocols, while paw edema and the levels of advanced oxidation protein products (AOPP) only diminished on Day 7. No effect in mechanical hyperalgesia was observed. Oral treatment for 3 or 7 days also decreased the plasma levels of NO, AOPP, TNF-α, and IL-10. On Day 7, the number of leukocytes in the blood was also reduced by this treatment. Importantly, botryosphaeran did not induce inflammation in mice when administered alone over 7 days. This study demonstrated the anti-inflammatory and antinociceptive potential of botryosphaeran in these experimental models, making this fungal β-glucan a new possibility for complementary treating acute and chronic inflammation.

Anti-inflammatory activity of Atavijambira (Atalantia monophylla DC.) root and stem

Abstract Background: Atalantia monophylla DC. family Rutaceae, a promising drug, has multifaceted ethnomedicinal claims to treat rheumatism, arthritis, paralysis, cough, skin diseases, etc., In traditional practice, root and stem are administered to treat rheumatism and arthritis, respectively. Aim: The aim of this study was to evaluate the anti-inflammatory activity of the root and stem of A. monophylla against carrageenan-induced acute paw edema in wistar albino rats. Materials and methods: Shade dried root and stem were grinded separately into a fine powder (120#) by the mechanical grinder. Test drugs were prepared in Phanta (hot infusion) form and used as fresh (A. monophylla root Phanta [AMRP] and A. monophylla stem Phanta [AMSP]). Difference between the groups was statistically determined by one-way ANOVA, followed by Dunnett’s multiple “t” test for unpaired data. Results: AMSP showed a significant decrease in paw inflammation at all-time interval (P < 0.05), whereas AMRP produced nonsignificant decrease in paw inflammation at 1 h (43.53%) and 5 h (25.74%) while significant (P < 0.05) anti-inflammatory activity at 3 h (36.35%) in comparison with the normal control group. Conclusion: The present study concluded that A. monophylla stem is having significant anti-inflammatory activity in comparison to its root when administered in Phanta form against carrageenan-induced acute inflammation in rats.

Study of novel 1,4-dihydropyridine derivatives as prospective anti-inflammatory remedies: a randomised controlled trial

Background. Over the past decades, scientific community is motivated on finding new anti-inflammatory agents with a safe and high-effective profile to manage pathology.Objectives. A study of the anti-inflammatory action of novel compounds, 1,4-dihydropyridine derivatives, in a classical formalin-induced paw oedema test in white rats.Methods. Originally synthesised 1,4-dihydropyridine derivatives were preliminarily subjected to virtual screening using the SwissTargetPrediction toolkit. White laboratory rats (130 animals) were divided into a control (formalin oedema) and intact group, 4 comparison (meloxicam, sodium metamizole, sodium diclofenac and indomethacin) and 7 experiment groups by the number of 1,4-dihydropyridine derivatives studied. The samples anti-inflammatory efficacy was evaluated in acute formalin-induced paw oedema model simulated by right hind limb subplantar injection of 0.1 mL 2% formalin. The studied substances were administered intragastrically at 5 mg/kg 1.5 h prior to oedema induction. Oncometry was assessed quantitatively by limb circumference. Animals were managed in compliance with GOST 33044–2014 “Principles of Good Laboratory Practice” at all experiment steps. Experimental data were analysed statistically to describe quantitative variability with variance σ2, mean limb girth a and standard deviation σ. Data homogeneity and reliability were estimated by variation coefficient V and the Wilcoxon T(W) criterion.Results. As the most anti-inflammatory effective, partially hydrogenated mar-040 pyridines (ethyl 4-({[5-cyano-6-{[2-(diphenylamino)-2-oxoethyl]thio}-4-(2-furyl)-2-methyl-1,4-dihydropyridin-3-yl]carbonyl}amino) benzoate) were shown 33-fold superior to indomethacin, 26-fold — to sodium diclofenac, 25-fold — to meloxicam and 30-fold — to sodium metamizole; mar-037 pyridines (ethyl 4-[({[3-cyano-5-({[4-(ethoxycarbonyl)phenyl]amino}carbonyl)-4-(2-furyl)-6-methyl-1,4-dihydropyridin-2-yl]thio}acetyl)amino] benzoate) — 17–23-fold superior vs. reference drugs. We also show that mаr-014 (ethyl 4-({[5-cyano-6-({2-[(3,5-dichlorophenyl) amino]-2-oxoethyl}thio)-4-(2-furyl)-2-methyl-1,4-dihydropyridin-3-yl]carbonyl}amino)benzoate) and mar033 (ethyl 2-[({[3-cyano-5-({[4-(ethoxycarbonyl)phenyl]amino}carbonyl)-4-(2-furyl)-6-methyl-1,4-dihydropyridin-2-yl]thio}acetyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylate) compounds are 2.7-fold more effective vs. reference drugs.Conclusion. The synthesised 1,4-dihydropyridine compounds reveal high efficacy in experimental assays. Selected novel 1,4-dihydropyridine derivatives exhibit a marked anti-inflammatory activity and offer value in future preclinical trials.

Evaluation of anti-inflammatory response of berberine-loaded gum nanocomplexes in carrageenan-induced acute paw edema in rats.

Berberine is a natural plant alkaloid and has been reported to possess anti-inflammatory activity. However, berberine's poor bioavailability and low solubility have limited its clinical applicability. Nanoencapsulation of berberine using a suitable carrier can be a promising strategy to improve its efficacy. Therefore, this study aimed to produce berberine-loaded gum nanocomplexes to evaluate their therapeutic effects in a carrageenan-induced rat model. Berberine-loaded gum nanocomplexes were prepared by the ionic complexation between the negative charges of the gums (tragacanth and acacia gum) using a cross-linker for loading cationic berberine and their anti-inflammatory activity was evaluated against carrageenan-induced paw edema in rats. ELISA and qRT-PCR were employed to measure the concentration and mRNA expression level of inflammatory mediators in plasma and paw tissue, respectively. Berberine nanocomplexes were characterized for particle size (219.5nm), zeta potential by the dynamic light scattering (DLS), and for entrapment efficiency (93.2%) Infrared spectroscopy affirmed the loading of berberine in gum nanocomplexes. Transmission electron microscopy of formulation showed the spherical shape of nanocomplexes and small particle size (100-150nm). Pretreatment of rats with berberine nanocomplexes significantly reduced the paw edema in inflamed rat paws, decreased the production of nitrite and TNF-α in plasma and repressed the mRNA expression levels of TNF-α and IL-1β in paw tissue in comparison to berberine per se treated rats. The obtained berberine-loaded gum nanocomplexes produced a better anti-inflammatory effect as compared to berberine alone and hence can be used as an efficient candidate in the treatment of inflammation. The schematic representation of the preparation of the preparation of berberine-loaded tragacanth/acacia gum nanocomplexes and the evaluation in vivo for anti-inflammatory effects.

Anti-Inflammatory Activities of the Ethanol Extract of Prasiola japonica, an Edible Freshwater Green Algae, and Its Various Solvent Fractions in LPS-Induced Macrophages and Carrageenan-Induced Paw Edema via the AP-1 Pathway

Prasiola japonica possesses several biological activities. However, reports on the anti-inflammatory activities and molecular mechanisms of its different solvent fractions remain limited. In this study, we investigated the potential anti-inflammatory activities of P. japonica ethanol extract (Pj-EE) and four solvent fractions of Pj-EE made with hexane (Pj-EE-HF), chloroform (Pj-EE-CF), butanol (Pj-EE-BF), or water (Pj-EE-WF) in both in vitro (LPS-induced macrophage-like RAW264.7 cells) and in vivo (carrageenan-induced acute paw edema mouse models) experiments. The most active solvent fraction was selected for further analysis. Various in vitro and in vivo assessments, including nitric oxide (NO), cytokines, luciferase assays, real-time polymerase chain reactions, and immunoblotting analyses were performed to evaluate the underlying mechanisms. In addition, the phytochemical constituents were characterized by Liquid chromatography-tandem mass spectrometry. In in vitro studies, the highest inhibition of NO production was observed in Pj-EE-CF. Further examination revealed that Pj-EE-CF decreased the expression of inflammation-related cytokines in LPS-induced RAW264.7 cells and suppressed subsequent AP-1-luciferase activity by inhibition of phosphorylation events in the AP-1 signaling pathway. Pj-EE-CF treatment also demonstrated the strongest reduction in thickness and volume of carrageenan-induced paw edema, while Pj-EE-BF showed the lowest activity. Furthermore, Pj-EE-CF also reduced gene expression and cytokines production in tissue lysates of carrageenan-induced paw edema. These findings support and validate the evidence that Pj-EE, and especially Pj-EE-CF, could be a good natural source for an anti-inflammatory agent that targets the AP1 pathway.

Anti-inflammatory Activity of Sulphated Polysaccharide Isolated from Ulva fasciata

Abstract: There are various components to an inflammatory reaction that can contribute to the associated symptoms and tissue injury and these include Oedema formation, leukocyte infiltration and granuloma formation. Anti-inflammatory activity of the polysaccharide isolated from Ulva fasciata was analysed by carrageenan induced acute paw Oedema and formalin induced chronic paw Oedema. The isolated polysaccharide showed anti-inflammatory activity. Keywords: Ulva fasciata, Sulphated Polysaccharide, Paw Oedema, Anti-inflammatory Activity

Central and peripheral effects of environmental enrichment in a mouse model of arthritis

This study analyzed whether environmental enrichment (EE) modulates the nociceptive and inflammatory responses in the mouse model of arthritis induced by Complete Freund’s Adjuvant (CFA). Ninety male mice (C57BL/6-JUnib, 4-weeks-old; 20–25 g) were distributed into EE and standard (SE) groups. For EE, mice were kept in bigger cages using an alternation of materials to chew (wood and paper), for nesting (cotton), to use as hiding places (plastic tunnels), and for voluntary exercise (wheel running). Arthritis was induced by an injection of CFA (50 μL) into the right hind paw or saline solution in the control group. Separate groups received the anti-inflammatory drug dexamethasone (0.5 mg/kg; every 48 h). Inflammatory and pain measurements were performed from 1 to 35 days after CFA administration. EE per se reduced the acute paw edema formation and arthritis scores. The serum levels of tumor necrosis factor (TNF) were undetectable in any experimental groups. EE diminished the immunopositivity for the microglia marker IBA1 in the pre-frontal cortex, with slight changes for hippocampal GFAP-positive activated astrocytes. Finally, EE induced a marked increment of brain-derived nerve factor (BDNF) expression in the hippocampus, an effect that was fully prevented by dexamethasone. These data bring novel evidence on the peripheral and central effects of EE in a mouse arthritis model.

An Investigation of Algerian Dates (Phoenix dactylifera L.); Antioxidant, Anti-inflammatory Properties and Phenolic Compositons H

Date fruit (Phoenix dactylifera L.) is not only known for its nutritional properties but also its therapeutic virtues. The objective was to investigate the phenolic compounds and evaluate the antioxidant and anti-inflammatory activities of pulp, seed, and whole fruit of Algerian dates. The total phenolic and flavonoid contents of ethanolic pulp (EP), seed (ES), and whole fruit (EF) extracts were measured using colorimetric methods. Phenolic acids and flavonoid profiles were determined by RP-HPLC-UV. The examination of the antioxidant potential was established by Free radical scavenging DPPH and FRAP assays. Anti-inflammatory activity of aqueous pulp (AP), seed (AS), and whole fruit (AF) of dates at 100, 200, and 300 mg/kg BW of each extract were carried out according to the experimental model of carrageenan-induced acute paw edema in mice, using diclofenac (50 mg/kg) as a reference product. Measurement of the percentage of inhibition of paw edema in mice as well as the histological study of the paw tissue, allowed us to assess the anti-inflammatory effect of the extracts investigated. Ethanolic pulp, seed, and whole fruit of date extracts contained total phenolic and flavonoids compounds at different concentrations as well as a diverse phenolic profile. The strongest antioxidant capacity was determined in ethanolic date seed extract. Concerning anti-inflammatory activity, the administration of aqueous pulp (100 and 200 mg/kg), seed (100mg/kg), and fruit (100, 200, and 300 mg/kg) of date extract induced a higher anti-inflammatory response from the fourth hour after carrageenan injection compared to the standard group treated with diclofenac. It is concluded that pulp, seed, and whole fruit of Algerian date possess antioxidant activity with phenolic and flavonoid contents and anti-inflammatory activity and dates with pulp and seed parts could be used as a natural bioactive substance for supporting anti-inflammatory therapies.

AN INVESTIGATION OF THE ANALGESIC AND ANTI-INFLAMMATORY EFFECTS OF AERIAL PARTS OF FLACOURTIA JANGOMAS

Objective: The present study was aimed to evaluate the analgesic and anti-inflammatory effects of leaf and stem part aqueous extract of Flacourtia jangomas.
 Methods: Aqueous extract of leaves (ALE) and aqueous extract stem (ASE) part of Flacourtia jangomas were sequentially prepared by maceration process and subjected to a preliminary phytochemical screening. The anti-inflammatory activity was assessed by the carrageenan-induced acute rat paw oedema model and Analgesic activity was evaluated by acetic acid-induced writhing model and hot plate method in mice. The data were analysed by one-way ANOVA followed by post hoc Dunnet’s test by using SPSS V.15 (student trail version).
 Results: The preliminary phytochemical analysis of extracts of leaves and stems indicated the presence of carbohydrate, alkaloids flavonoids, phenols, tannins, saponins. The extracts showed significant anti-inflammatory and analgesic activities with a dose-dependent manner. The ethanolic extract from the leave extract of Flacourtia jangomas at the dose 200 mg/kg has 55.6% significant anti-inflammatory activity compared to the standard drugs (44.4%). Even at the low dose leave extract has more potent than aqueous stem extract. Where in analgesic effect by Hot plate method basal reaction time results showed that aqueous extract of stem part at the dose of 200 mg /kg has a significant effect at 120 mts 10.0 sec when compared with std pentazocine 13.0 sec. In peripheral analgesic method Acetic acid-induced writhing model results have not shown much more significant when compared with standard drug (42.1%). The potential to cause anti-inflammation by stem extract was comparatively less than that of leave extract. Thus it could be concluded that Flacourtia jangomas leave extract possess significant anti-inflammatory activity
 Conclusion: Our findings suggest that Flacourtia jangomas extract is safe and has potential anti-inflammatory and analgesic activities, which promote this use as a food supplement against pain and inflammation related to inflammatory diseases.

Anti-Inflammatory Activity of Oxycarotenoid Extracts Isolated from Coriander Leaves (Coriandrum Sativum) and Curry Leaves (Murraya koenigii) on Carrageenan Induced Acute Inflammation in Rats

Introduction: Green leafy vegetables are important sources of polyphenols and carotenoids which possess both antioxidant and anti-inflammatory activities. Aim: To study the anti-inflammatory activity of oxycarotenoid extracts isolated from coriander leaves (Coriandrumsativum) and curry leaves (Murraya koenigii) in carrageenan induced acute paw oedema in rats. Materials and Methods: Oxycarotenoid extracts were isolated from the coriander leaves (Coriandrum sativum) and curry leaves (Murraya koenigii) and they were assessed for anti-inflammatory activities by in-vivo methods. The in-vivo anti-inflammatory activity was evaluated in carrageenan induced acute paw oedema model. Indomethacin at a dose of 20 mg/Kg body weight was used as standard anti-inflammatory drug. Results: The results revealed that oxycarotenoids extracted from coriander leaves administered at a dose of 40 mg/kg body weight showed an inhibition of 53.33% whereas the oxycarotenoids extracted from curry leaves showed an inhibition of 60% at the sixth hour after carrageenan injection. The results are comparable with those of indomethacin (20 mg/Kg body weight) administered group which showed an inhibition of 55.53% Conclusion: These findings suggest that oxycarotenoid extracts isolated from leafy vegetables (coriander leaves and curry leaves) have significant anti-inflammatory activities.

Development and Optimization of Epigallocatechin-3-Gallate (EGCG) Nano Phytosome Using Design of Experiment (DoE) and Their In Vivo Anti-Inflammatory Studies.

Inflammation is responsible for the development of many diseases that make up a significant cause of death. The purpose of the study was to develop a novel nanophytosomal preparation of epigallocatechin-3-gallate (EGCG) and egg phospholipid complex that has a lower particle size with higher drug loading capability, physical stability and anti-inflammatory activities. The impact of different factors and material characteristics on the average particle size was studied along with the drug loading of phytosome using design of experiment (DoE). The in vivo anti-inflammatory study was evaluated using a rat model to investigate the performance of EGCG nanophytosome. UHPLC results showed that 500 µg of EGCG were present in 1 mL of green tea extract. SEM data exhibited that phytosome (phospholipid-drug complex) was in the nanosize range, which was further evident from TEM data. Malvern Zetasizer data showed that the average particle size of the EGCG nanophytosome was in the range of 100–250 nm. High drug loading (up to 90%) was achieved with optimum addition rate, stirring temperature and phospholipid concentration. Stability study data suggest that no significant changes were observed in average particle size and drug loading of nanophytome. The in vivo anti-inflammatory study indicated a significant anti-inflammatory activity of green tea extract, pure EGCG and its phytosomal preparations (p ≤ 0.001) against acute paw edema.

Virucidal Action Against Avian Influenza H5N1 Virus and Immunomodulatory Effects of Nanoformulations Consisting of Mesoporous Silica Nanoparticles Loaded with Natural Prodrugs.

BackgroundCombating infectious diseases caused by influenza virus is a major challenge due to its resistance to available drugs and vaccines, side effects, and cost of treatment. Nanomedicines are being developed to allow targeted delivery of drugs to attack specific cells or viruses.Materials and MethodsIn this study, mesoporous silica nanoparticles (MSNs) functionalized with amino groups and loaded with natural prodrugs of shikimic acid (SH), quercetin (QR) or both were explored as a novel antiviral nanoformulations targeting the highly pathogenic avian influenza H5N1 virus. Also, the immunomodulatory effects were investigated in vitro tests and anti-inflammatory activity was determined in vivo using the acute carrageenan-induced paw edema rat model.ResultsProdrugs alone or the MSNs displayed weaker antiviral effects as evidenced by virus titers and plaque formation compared to nanoformulations. The MSNs-NH2-SH and MSNs-NH2-SH-QR2 nanoformulations displayed a strong virucidal by inactivating the H5N1 virus. They induced also strong immunomodulatory effects: they inhibited cytokines (TNF-α, IL-1β) and nitric oxide production by approximately 50% for MSNs-NH2-SH-QR2 (containing both SH and QR). Remarkable anti-inflammatory effects were observed during in vivo tests in an acute carrageenan-induced rat model.ConclusionOur preliminary findings show the potential of nanotechnology for the application of natural prodrug substances to produce a novel safe, effective, and affordable antiviral drug.

Anti-Inflammatory and Physicochemical Characterization of the Croton rhamnifolioides Essential Oil Inclusion Complex in β-Cyclodextrin

Croton rhamnifolioides is used in popular medicine for the treatment of inflammatory diseases. The objective of this study was to characterize and evaluate the anti-inflammatory effect of C. rhamnifolioides essential oil complexed in β-cyclodextrin (COEFC). The physicochemical characterization of the complexes was performed using different physical methods. The anti-inflammatory activity was evaluated in vivo by ear edema, paw edema, cotton pellet-induced granuloma, and vascular permeability by Evans blue extravasation. The mechanism of action was validated by molecular docking of the major constituent into the cyclooxygenase-2 (COX-2 enzyme). All doses of the COEFC reduced acute paw edema induced by carrageenan and dextran, as well as vascular permeability. Our results suggest the lowest effective dose of all samples inhibited the response induced by histamine or arachidonic acid as well as the granuloma formation. The complexation process showed that the pharmacological effects were maintained, however, showing similar results using much lower doses. The results demonstrated an involvement of the inhibition of pathways dependent on eicosanoids and histamine. Complexation of β-cyclodextrin/Essential oil (β-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs.