Carrageenan-induced Hind Paw Edema Model Research Articles

Phytochemical characterization of Typha domingensis and the assessment of therapeutic potential using in vitro and in vivo biological activities and in silico studies.

Typha domingensis, a medicinal plant with significant traditional importance for curing various human diseases, has potentially bioactive compounds but was less explored previously. Therefore, this study aims to investigate the therapeutic potential of T. domingensis by evaluating the phytochemical profile through high-performance liquid chromatography (HPLC) techniques and its biological activities (in vitro and in vivo) from the methanolic extract derived from the entire plant (TDME). The secondary metabolite profile of TDME regulated by reverse phase ultra-high-performance liquid chromatography-mass spectrometry (RP-UHPLC-MS) revealed some bioactive compounds by -ve and +ve modes of ionization. The HPLC quantification study showed the precise quantity of polyphenols (p-coumaric acid, 207.47; gallic acid, 96.25; and kaempferol, 95.78μg/g extract). The enzyme inhibition assays revealed the IC50 of TDME as 44.75 ± 0.51, 52.71 ± 0.01, and 67.19 ± 0.68µgmL-1, which were significant compared to their respective standards (indomethacin, 18.03 ± 0.12; quercetin, 4.11 ± 0.01; and thiourea, 8.97 ± 0.11) for lipoxygenase, α-glucosidase, and urease, respectively. Safety was assessed by in vitro hemolysis (4.25% ± 0.16% compared to triton × 100, 93.51% ± 0.36%), which was further confirmed (up to 10g/kg) by an in vivo model of rats. TDME demonstrated significant (p < 0.05) potential in analgesic activity by hot plate and tail immersion tests and anti-inflammatory activity by the carrageenan-induced hind paw edema model. Pain latency decreased significantly, and the anti-inflammatory effect increased in a dose-dependent way. Additionally, in silico molecular docking revealed that 1,3,4,5-tetracaffeoylquinic acid and formononetin 7-O-glucoside-6″-O-malonate possibly contribute to enzyme inhibitory activities due to their higher binding affinities compared to standard inhibitors. An in silico absorption, distribution, metabolism, excretion, and toxicological study also predicted the pharmacokinetics and safety of the chosen compounds identified from TDME. To sum up, it was shown that TDME contains bioactive chemicals and has strong biological activities. The current investigations on T. domingensis could be extended to explore its potential applications in nutraceutical industries and encourage the isolation of novel molecules with anti-inflammatory and analgesic effects.

Anti-inflammatory Activity of the Phenolic Compounds from Vanda roxburghii R. Br.

Inflammation is implicated in the pathogenesis of several neurodegenerative diseases including Alzheimer’s disease (AD). Vanda roxburghii R. Br. is used as folk medicine in the treatment of various ailments and diseases including inflammation, rheumatoid arthritis and neurological disorders. We reported earlier that the plant possesses anti-inflammatory activity and the activity is high in the chloroform fraction among other fractions tested. Therefore, the present work was designed to isolate the compounds from the chloroform fraction responsible for anti-inflammatory activity. Four compounds namely syringaldehyde (1), vanillin (2), dihydroconiferyl dihydro-p-coumarate and (3) and gigantol (4) were isolated and purified using chromatographic methods. The isolated compounds were identified by analysis of their NMR spectral data. The compounds were evaluated for anti-inflammatory activity using carrageenan-induced hind paw edema model in mice. All the compounds showed significant activity at a dose of 100 mg/kg. Among the compounds, gigantol displayed the highest activity which was comparable to the activity of the standard drug indomethacin. At the same dose the other three compounds syringaldehyde, vanillin and dihydroconiferyl dihydro-p-coumarate exhibited similar activity. These results suggest that the isolated compounds from the chloroform fraction have potential anti-inflammatory activity that might be useful in the prevention and treatment of AD. Bangladesh Pharmaceutical Journal 26(1): 1-6, 2023 (January)

Synthesis and Biological Evaluation of Some New Chalcone Derivatives as Anti-inflammatory Agents.

Aim-The present research work aims to prepare a series of 1-(4-(2-(1H-indol-1-yl)-2-oxoethoxy)phenyl)-3-phenylprop-2-en-1-one derivatives. Method- The major compound was achieved by the reaction of indole with chloroacetylchloride in benzene afforded 2-chloro-1-(indoline-1-yl) ethanone which reacts o- hydroxy acetophenone in presence of acetonitrile to form 2-(4-acetylphenoxy)-1-(1H-indol-1-yl)ethan-1-one then is goes through aldol condensation to give various final derivatives. Results and conclusion- After synthesis of compounds, the synthesized compounds were characterized by checking their solubility, melting point, thin layer chromatography, IR, 1HNMR spectral data and elemental analysis. All of prepared derivatives were evaluated for their anti-inflammatory activity on wistar albino rats by following carrageenan induced Rat Hind Paw Edema model.

Evaluation of Wound Healing and Anti-Inflammatory Activity of Hydroalcoholic Leaf Extract of Clematis simensis Fresen (Ranunculaceae).

IntroductionClematis simensis is one of the most widely used medicinal plant for the treatment of wound traditionally. However, its claim was not scientifically tested, the current study therefore assessed the anti-inflammatory and wound healing properties of 80% methanol leaf extract of C. simensis.MethodsThe dried and powdered leaf of C. simensis was macerated with 80% methanol. The topical ointment was then made in two concentrations (5% and 10% w/w), and two models, excision and incision, were used to test the extract’s capacity to treat wounds in mice. In addition, anti-inflammatory test was also conducted using carrageenan-induced hind paw edema model in three doses (100, 200, and 400 mg/kg) in rats. The DPPH test was used to determine the extract’s anti-oxidant properties where ascorbic acid was used as standard agent.ResultsWhen wounds were treated with ointments containing 5% and 10% (w/w) extract, the rate of wound contraction, the length of time it took for the epithelium to form, and the strength of the skin to break were all significantly increased (p < 0.05). There was no discernible difference in wound healing activity between the 10% (w/w) and 5% (w/w) extracts. Moreover, they had also similar impact as that of the positive control nitrofurazone in wound healing activity. Compared to the negative control, C. simensis extract considerably (p < 0.01-p < 0.001) reduced inflammation. The extract also demonstrated antioxidant activity with IC50 values of 0.7 mg/mL for the extract and 1.04 mg/mL for ascorbic acid, respectively.ConclusionOverall, it is plausible to draw the conclusion that C. simensis 80% methanol extract possesses wound healing activity, perhaps as a result of its anti-inflammatory and antioxidant effects.

Anti-inflammatory, Antinociceptive, and Antitumorigenesis Activities ofTerminalia Bellerica(Gaertn.) Roxb. in Animal Models

Previous pharmacological research has demonstrated that Terminalia bellerica (Gaertn.) Roxb. (TB) extract possesses several pharmacological activities. However, there is scant evidence documenting the therapeutic activities of TB extract on inflammation, pain, and cancers. Our study examined the in vivo anti-inflammation, antinociception, and antitumorigenesis effects of TB extract and investigated possible mechanisms for those effects. Anti-inflammation activities of TB extract were evaluated using ethyl phenylpropiolate (EPP)- and arachidonic acid (AA)-induced ear edema models, a cotton pellet-induced granulation formation model, and a carrageenan-induced hind paw edema model. An antinociceptive property of TB extract was assessed using a formalin-induced nociception test. An anticarcinogenesis effect was investigated using a 7,12-dimethylbenz( a) anthracene (DMBA) and 12- O-tetradecanoylphorbol-13-acetate (TPA)-induced tumorigenesis model. In the study, TB extract exhibited significant anti-inflammatory effects against EPP-induced ear edema and carrageenan-induced hind paw edema in rats. However, the TB extract showed insignificant inhibitory activity against AA-induced ear edema and cotton pellet-induced granuloma. A dose-dependent decrease in analgesic activity was observed with TB extract evidenced by decreased licking time in formalin-induced pain in mice in both the early and late phases. TB extract also significantly inhibited DMBA/TPA-induced mouse skin tumorigenesis. In conclusion, TB extract possesses anti-inflammatory, analgesic, and anticarcinogenesis properties which act, at least in part, through inhibitory effects of inflammatory mediator production.

Preparation, characterization and evaluation of anti-inflammatory and anti-nociceptive effects of brucine-loaded nanoemulgel

Brucine (BRU) is a natural product derived from nux-vomica seeds. It is commonly used as an anti-inflammatory and anti-nociceptive drug to relieve arthritis and traumatic pain. Nevertheless, its use is significantly limited by its low aqueous solubility, as well as the gastrointestinal problems and systemic toxicity that may occur following oral administration. The goal of this study, therefore, was to formulate and evaluate a nanoemulgel formulation of BRU for enhanced topical anti-inflammatory and anti-nociceptive activities. Different formulations were developed (BRU gel, emulgel and nanoemulgel) using 1% w/w NaCMC as a gelling agent. The formulated preparations were assessed for their physical appearance, spreadability, viscosity, particle size, in vitro drug release and ex vivo permeation studies. In addition, the carrageenan-induced rat hind paw edema method was adopted to scrutinize the anti-inflammatory activity, while the hot plate method and acetic acid-induced writhing test were used to assess the anti-nociceptive activity of different formulations in male BALB/c mice. The formulated BRU-loaded preparations showed good physical characteristics. Cumulative drug release from BRU-loaded nanoemulgel was remarkably higher than that of the other formulations. Ex vivo drug permeation of the nanoemulgel formulation across rat skin showed enhanced drug permeation and higher transdermal flux as compared to BRU-loaded gel or emulgel. Most importantly, the carrageenan-induced rat hind paw edema model verified the efficient anti-inflammatory potential of BRU-loaded nanoemulgel. In addition, BRU-loaded nanoemulgel exhibited significant protective effects against thermal stimulation in the hot plate test and remarkably inhibited acetic acid-induced abdominal writhing in mice. Furthermore, a skin irritation test indicated that BRU-loaded nanoemulgel elicited neither edema nor erythema upon application to rat skin. Collectively, our results suggest that myrrh oil-based nanoemulgel might represent a promising delivery vehicle for potentiating the anti-inflammatory and anti-nociceptive actions of brucine.

Anti-inflammatory effects of memantine in carrageenan-induced paw edema model in rats

Background: The anti-inflammatory effect of memantine (MEM) was investigated using carrageenan-induced hind paw edema model in rats. Materials and Methods: Thirty male Wistar rats were randomly assigned to five groups (n = 6). Group 1 received 0.1 mL of 1% carrageenan at the right hind paw. Group 2 received dexamethasone (10 mg/kg) and Groups 3, 4, and 5 received 5, 10, and 20 mg/kg MEM intraperitoneally (ip), 20 min after injection of carrageenan into the right hind paw, respectively. Animals’ paw thickness was measured at 0, 1, 2, 3, 4, and 5 h after carrageenan injection. Then, animals were euthanized and myeloperoxidase (MPO) and malondialdehyde (MDA) levels were measured in the paw tissues. The tissue samples were further examined histopathologically using light microscopy. One-way ANOVA and Tukey post hoc test was used to compare the mean values between the groups. Results: Treating with MEM at all doses significantly decreased hind paw thickness at 2 (P < 0.05 and P < 0.01 at MEM 10 mg/kg and MEM 5 and 20 mg/kg, respectively), 3 (P < 0.001), and 4 (P < 0.001 at 5 mg/kg and P < 0.01 at MEM 10 and 20 mg/kg) hours after carrageenan injection in comparison to the carrageenan group. There was a significant (P < 0.05 and P < 0.001, respectively) reduction in MPO activity and MDA levels in MEM-treated groups when compared with the carrageenan group. Conclusion: This study showed that MEM decreased paw edema, leukocyte infiltration, MPO activity, and MDA levels, and MEM can be considered as an effective anti-inflammatory agent.

The In Vivo Antinociceptive and Antiinflammatory Effects of Verbascum exuberans Hub.-Mor.

Safe and effective drugs are still lacking for many pain therapies. In recent years, growing interest has been devoted thus on herbal drugs as an option to identify new pain killers. Based on this, extensive researches are carried out on Verbascum L. genus due to its therapeutic potency on pain and inflammation therapy. In this study, among Verbascum species, the antinociceptive effect of Verbascum exuberans Hub.-Mor., and its contributions to nitrergic, serotonergic, or opioidergic pathways as well as its antiinflammatory acitivity were investigated. Tail clip, tail flick, and hot plate tests were used to determine the central (spinal and supraspinal) antinociceptive effect, while an acetic acid-induced writhing test was used to measure the peripheral antinociceptive effect of the extract (250 and 500 mg/kg). The extract (250 mg/kg) was then combined with nω-nitro-L-arginine methyl ester, cyproheptadine, and naloxone to evaluate its involvement in nitrergic, serotonergic, or opioidergic pathways, respectively. Carrageenan-induced hind paw edema model was used to determine the antiinflammatory effect of the extract (250 mg/kg). The extract shows central spinal but not central supraspinal antinociceptive effect, and presents peripheral antinociceptive effect. The antinociceptive actions of the extract is largely regulated via targeting the nitrergic pathway, while the opioidergic pathway is partly involved. Further, the extract shows antiinflammatory effect due to the significant inhibitions on the time dependent edema progression and the cytokine (tumor necrosis factor-alfa and interleukin-1beta) productions. V. exuberans could be stated as a new source with a high beneficial potential in alleviating pain and inflammation.

Anti-inflammatory properties of methanolic extract of "sikari laharo" (Periploca calophylla)

Inflammation, orchestrated in a series of cardinal signs is a pathophysiological condition that occurs during various clinical presentations. Periploca calophylla is a herbal plant which is used traditionally as an anti-inflammatory agent for a myriad of malaises in Nepalese countryside. The scientific research on the anti-inflammatory property of this plant is scanty, and if available elsewhere, its properties are not proven scientifically, except sporadic empirical evidence reported by the traditional faith healers. The main objective of this research was to establish a proof of concept on the anti-inflammatory property of P. calophylla based on the results obtained from a scientific experiment. Accordingly, Adult albino mice animal model was used for in vivo assessment of its property. Three different doses of 80% methanolic extract of the vine of P. calophylla (1.5 mg/ kg, 2 mg/kg, and 2.5 mg/kg) were administered intra-peritoneally to the animals of the test groups. Indomethacin (25 mg/ kg) and distilled water (3 mL/kg) were used as positive and negative controls, via the same route of administration. The anti-inflammatory property was evaluated by the Carrageenan-induced hind paw oedema model test, fresh egg albumin induced paw oedema test, formalin-induced paw oedema test, and haematology. Extract of P. calophylla (1.5 mg/kg) significantly (p&lt;0.01) inhibited inflammatory responses in all the evaluated tests in the animal model. The data obtained from this study indicated that the phyto-extract of P. calophylla possessed a significant amount of anti-inflammatory property. This justifies the empirical and traditional use of this plant as an anti-inflammatory agent. Isolation of the particular compound related to this property needs further experimentation and scientific investigation.

Anti-Nociceptive and Anti-Inflammatory Activity of Hygrophila schulli Leaves.

PurposeThe management of pain and inflammation with non-steroidal anti-inflammatory drugs and opioid analgesics are currently encountering severe adverse reactions. To overcome these problems, herbal remedies may offer new alternative medicines. Hygrophila schulli is a medicinal plant traditionally used for the treatment of pain and inflammation-related disorders; yet, these claims are not scientifically validated. Hence, this study was aimed to validate the traditional use of Hygrophila schulli leaves as anti-inflammatory and analgesic remedy.MethodsIn vitro anti-hyaluronidase assay and in vivo carrageenan-induced hind paw oedema model were used to evaluate the anti-inflammatory property of ethanolic leaf extract of Hygrophila schulli. Tail immersion and acetic acid-induced writhing tests were performed to determine the central and peripheral analgesic activity of the leaf extract, respectively.ResultsThe ethanolic leaf extract exhibited significant anti-hyaluronidase activity (P<0.001) and significant inhibition of carrageenan-induced paw oedema (P<0.05) compared to untreated controls. Similarly, the extract significantly prolonged the reaction time of mice (P<0.05) for the hot-water stimuli. Furthermore, an oral dose of the extract showed significant inhibition (P<0.01) of acetic acid-induced abdominal contractions of mice. Besides, the ethanolic leaf extract did not cause any obvious sign of acute toxicity at a single oral dose of 2 g/kg.ConclusionThe findings of this study may partially support the acclaimed traditional use of Hygrophila schulli leaves for the treatment of pain and inflammatory conditions.

In Vivo Evaluation of Wound Healing and Anti-Inflammatory Activity of 80% Methanol Crude Flower Extract of Hagenia abyssinica (Bruce) J.F. Gmel in Mice.

Background Hagenia abyssinica (Bruce) J.F. Gmel (Rosaceae) is distributed in the highlands of Ethiopia. The flowers of Hagenia abyssinica (Bruce) J.F. Gmel are used traditionally to treat wound. However, there was no scientific report on wound healing activity of Hagenia abyssinica (Bruce) J.F. Gmel. Thus, this study was initiated to investigate the wound healing and anti-inflammatory activities of 80% methanol crude extract of flowers of Hagenia abyssinica in mice. Objective The objective of this study was to evaluate the wound healing and anti-inflammatory activity of 80% methanol crude flower extract of Hagenia abyssinica in mice. Methods Air-dried flowers of Hagenia abyssinica were grounded and macerated three times successively by 80% methanol. The dried extract was fractionated with chloroform, ethyl acetate, and water. Phytochemical screening tests were performed according to established procedures. The crude extract and solvent fractions were formulated as ointments. Wound healing activity of the crude extract was evaluated using excision and incision wound models, and the wound healing activities of solvent fractions were evaluated by using the excision wound model. The anti-inflammatory activity of the 80% methanol extract of Hagenia abyssinica was evaluated using carrageenan-induced hind paw edema model in mice. Result The 2000 mg/kg test dose of the 10% (w/w) crude extract ointment was safe in rats. Both the 5% (w/w) and 10% (w/w) crude extract ointment-treated groups showed significant wound contraction starting from the day 4th. Both 5% (w/w) and 10% (w/w) crude extract ointments showed significant (P < 0.001) increment of tensile strength compared to the negative control. The 10% (w/w) aqueous and ethyl acetate fraction ointment revealed high (P < 0.001) percentage of wound contraction. The 100 mg/kg, 200 mg/kg, and 400 mg/kg oral administration of the crude extract had significant inhibition of the paw edema in mice of carrageenan-induced inflammation. Conclusion The results of this study evidenced that both 5% w/w and 10% w/w 80% methanol extract ointment of the flowers of Hagenia abyssinica have wound healing and anti-inflammatory effects.

Anti-nociceptive, anti-inflammatory and possible mechanism of anti-nociceptive action of methanol leaf extract of Nymphaea lotus Linn (Nymphaeceae)

The leaf of Nymphaea lotus has been used traditionally for the management of pain and inflammatory diseases. The methanol leaf extract of Nymphaea lotus (NLE) was evaluated for possible anti-nociceptive and anti-inflammatory activities in rats and mice (at the doses of 250, 500 and 1,000 mg/kg) to investigate the existence of scientific basis for the folkloric use of the plant. The standard drugs used were piroxicam (10 mg/kg) and morphine (10 mg/kg). The possible pharmacological mechanism involved in the anti-nociceptive activity was also investigated. The acute toxicity was determined in mice and rats using method of Lorke. The anti-nociceptive activity was evaluated using acetic acid-induced writhing and hot plate tests in mice, while the anti-inflammatory activity was evaluated using carrageenan-induced hind paw edema model in rats. The oral median lethal dose of NLE was found to be greater than 5,000 mg/kg in rats and mice. NLE demonstrated significant and dose-dependent protection against acetic acid induced writhes and increased the reaction time of mice in hot plate test. Pretreatment of the animals with naloxone (2 mg/kg) significantly (p < 0.05) attenuated the anti-nociception elicited by both NLE and morphine. NLE at the doses of 250 and 1,000 mg/kg significantly (p < 0.05) decreased rat paw edema at the 2nd hour in the carrageenan-induced paw edema test. The result of the study revealed that Nymphaea lotus possesses anti-nociceptive activities which may be mediated via the opioidergic system as well as mild anti-inflammatory activities thus providing scientific basis for the use of the plant in the management of pain and inflammatory diseases.

Multiple activities contribute to the wound healing effect of 80% methanol leaf extract of &lt;i&gt;Discopodium penninervum&lt;/i&gt; Hochst (Solanaceae) in mice

Discopodium Penninervum Hochst is among the Ethiopian medicinal plants traditionally used for wound healing activity. However, to date, there is no scientific report on its wound healing activity. Thus, the main aim of this study was to investigate the wound healing activity of 80% methanol leaf extract of D. penninervum in mice. Wound healing activity was investigated using excision and incision wound models. Mice were randomly assigned and treated with simple ointment (negative control), nitrofurazone (positive control), 5%, and 10% of D. Penninervum extract. Parameters such as wound contraction, period of epithelialization and tensile strength were evaluated. In addition, anti-inflammatory test using carrageenan-induced hind paw oedema model, in vitro antibacterial activity using agar well diffusion technique against several common bacterial strains that cause wound infection and antioxidant activity studies were performed at different doses of the extract. Both 5% and 10% (w/w) ointments exhibited significant (p &lt; 0.001) increase in wound contraction and shorter epithelization period in excision wound model. Animals treated with 5% and 10% (w/w) ointments showed about 97% and 98% wound closure, respectively, on day fifteen, while the closure of negative control was 88%. In addition, both preparations of the crude extract showed significant increase (p &lt; 0.001) in wound tensile strength as compared to negative controls. Mice treated with 100 mg/kg, 200 mg/kg and 400 mg/kg extract showed significant (p &lt; 0.001) reduction in paw oedema starting from the 2nd h as compared to negative controls with maximum inhibition of 56.27%, 57.36% and 58.18%, respectively. The crude extract also showed antibacterial activity against both Gram- positive and Gram-negative bacteria, with the former being more sensitive than the latter. The lowest MIC values were observed for S. aureus, (2.6 µg/µl) and the highest (350 µg/µl) for all the studied Gram-negative organisms. The MICindex of the extract was found to be 2. The extract was effective in scavenging DPPH radicals and its IC50 value was 2.77 mg/ml. In addition, quantification of total flavonoid content revealed the presence of 43.03 mg quercetin equivalent flavonoids in the extract. In conclusion, the extract of D. penninervum is endowed with significant wound healing activity that could be attributed to antibacterial, anti-inflammatory and antioxidant activities of the plant.Keywords: Discopodium penninervum, wound healing, excision and incision models, antibacterial activity, anti-oxidant activity

A PHARMACOLOGICAL STUDY ON THE ANTI-INFLAMMATORY EFFECTS OF CALENDULA OFFICINALIS EXTRACT ON EXPERIMENTAL ANIMALS

Introduction: Calendula officinalis is one of those plants which have medicinal importance due to its flowers has pharmacological activity the important pharmacological parameters have been less investigated properly and can be scientifically proved by reverse pharmacology. It was found of interest to evaluate these properties of extract of flowers of Calendula officinalis scientifically in experimental models.&#x0D; Methods: Study was conducted in Albino Wistar rats.Fresh Calendula officinalis flowers were collected, extraction and drug formulation was made. Anti-inflammatory activity of hydroalcoholic extract of Calendula officinalis (HECO) flowers was studied in the Carrageenan induced paw edema model &amp; Cotton pellet induced granuloma models The differences between experimental groups were compared by ANOVA followed by Students “t” unpaired test.&#x0D; Results: The Calendula officinalis extract of flowers at 200 and 400 mg/kg showed significant and highly significant inhibition (p&lt; 0.05 and p&lt;0.001, respectively) of paw edema after giving the carrageenan in the rat paw in comparison of control. In cotton pellets induced granuloma pouch method also, the Hydrochloric extract of Calendula officinalis (HECO) flowers showed very significant reduction of weight of granuloma (p&lt;0.01) with 22.80% protection as compared with control.&#x0D; Conclusion: We conclude that the Anti-inflammatory activity was noted with Hydrochloric extract of Calendula officinalis in a dose-dependent manner in acute (carrageenan-induced hind paw edema model) as well as sub-acute (cotton pellet induced granuloma model) inflammatory experimental models. They decrease the chemical mediators of inflammation&#x0D; Key Words: Calendula Officinalis, anti inflammation, Paw Edema Model, granuloma pouch method , HECO

Anti-inflammatory and antinociceptive features of Bryonia alba L.: As a possible alternative in treating rheumatism

AbstractBryonia species have traditionally been used as a diuretic and laxative, to reduce edema and relieve joint pain. B. alba roots are used especially to treat rheumatic pain and applied to painful joints in Turkish folk medicine. B. alba roots were extracted with n-hexane, ethyl acetate (EtOAc), and methanol, successively. The carrageenan-induced hind paw edema model and the Whittle method were used to evaluate the anti-inflammatory activity of the extracts in mice. The p-benzoquinone-induced abdominal constriction test and tail flick test were used to evaluate the antinociceptive activity of the extracts in mice. DPPH-radical-scavenging activity, ABTS radical–scavenging activity, total antioxidant activity, and hydroxyl radical– scavenging activity were assessed. Furthermore, the total phenolic and total flavonoid contents were calculated for all the extracts. The EtOAc extract prepared from B. alba roots had the most promising anti-inflammatory, antinociceptive, and antioxidant activities. Moreover, it had high phenolic and flavonoid contents. Therefore, B. alba roots could be alternative treatment method for rheumatic disorders.

Synthesis and Biological Evaluation of Novel 2-(4-acetyl-3-methyl- 5-(arylamino) thiophen-2-yl)-3-arylquinazolin-4(3H)-one Derivatives as Potential Anti-inflammatory and Antioxidant Agents.

A new series of 2-(4-acetyl-3-methyl-5-(arylamino) thiophen-2- yl)-3-arylquinazolin-4(3H)-one derivatives (11a-11j) were synthesized from acetyl acetone, phenyl isothiocyanate and 2-chloromethyl quinazolinone. Due to side effects of Non Steroidal Anti-Inflammatory Drugs (NSAID), an attempt was made to identify the novel tetrasubstituted thiophene lead compound as potential anti-inflammatory and antioxidant agent. Then newly synthesized compounds were characterized by IR spectroscopy, 1H NMR and mass spectrometry. The synthesized compounds were screened for their in vivo anti-inflammatory activity in carrageenan-induced rat hind paw edema model at dose 20mg/kg body weight using diclofenac sodium as a standard drug. The compounds were also evaluated for their in vitro DPPH free radical-scavenging activity and nitric oxide radical scavenging activity at the concentrations of 10, 20, 40, 60, 80 and 100 µg/mL using ascorbic acid as standard drug. The results from carrageenan-induced rat hind paw edema showed that compounds 11e, 11f and 11b show a significant anti-inflammatory activity of 46.61%, 48.94% and 47.04 % protection respectively to inflamed paw but less than diclofenac sodium. Compounds 11h and 11e show good DPPH free radical scavenging and nitric oxide radical scavenging activity, respectively. From results, it was observed that highly substituted thiophene scaffold exhibits anti-inflammatory and antioxidant activity.

Eco-friendly synthesis, characterization, in vitro and in vivo anti-inflammatory activity of silver nanoparticle-mediated &lt;em&gt;Selaginella myosurus&lt;/em&gt; aqueous extract

IntroductionThere is emerging interest in medicinal plants in the biomedical field, due to their multitude of chemicals which show anti-inflammatory, antimicrobial, antiviral, or antitumoral potential. Research on medicinal plants has shown that nanotechnology could offer new solutions in the quality control, delivery aspects, or in sustaining herbal biological activities. This work reports on the preparation and characterization of silver nanoparticle-mediated Selaginella myosurus plant extract.MethodsUltraviolet-visible spectroscopy, Fourier transform infrared spectroscopy, powder X-ray diffraction, energy dispersive X-ray spectroscopy, high-resolution scanning electron microscopy, high-resolution transmission electron microscopy, and selected area electron diffraction have been used to characterize the prepared silver nanoparticles. The synthetic stability was studied by varying concentrations and pH of reactants. Egg albumin denaturation and carrageenan-induced rat paw edema model were used to ascertain the anti-inflammation.ResultsUltraviolet-visible spectroscopy gave plasmon resonance ranging between 420 and 480 nm while Fourier transform infrared spectroscopy proved nano interface functionalized with organics. The powder X-ray diffraction pattern is in agreement with silver and silver chloride nanoparticles of crystallite size 33.7 nm and 44.2 nm for silver and silver chloride, respectively. Energy dispersive X-ray spectroscopy enables elemental characterization of the particles consisting of silver and silver chloride among main elements. Spherical silver grain of 58.81 nm average size has been depicted with high-resolution scanning electron microscopy and high-resolution transmission electron microscopy. Inhibitions of 99% and 60% were obtained in vitro and in vivo, respectively.ConclusionThe albumin denaturation and carrageenan-induced rat hind paw edema model to assess the anti-inflammatory potential of generated nanoparticles suggests that the silver nanoparticles may act as reducing/inhibiting agents on the release of acute inflammatory mediators. Hence, this work clearly demonstrated that silver nanoparticles mediated-Selaginella myosurus could be considered as a potential source for anti-inflammatory drugs.

Synthesis of New Isoxazole-, Pyridazine-, Pyrimidopyrazines and Their Anti-Inflammatory and Analgesic Activity.

Isoxazoles, pyridazines, and pyrimidopyrazines have recently attracted attention due to their potent pharmacological activities. They exhibited anticancer, neuroprotective, analgesic and anti-inflammatory effects. The study aimed to synthesize novel isoxazoles, pyridazines, and pyrimidopyrazines through efficient high yield protocol for evaluating their analgesics and anti-inflammatory activities. A series of novel isoxazole-, pyridazine-, pyrimidopyrazine derivatives was prepared from 5,8-alkyl-1,3-dimethyl-5,6-dihydropyrimido[5,6-e]pyrazine-2,4,7-trione (1a,b) as the starting material. The prepared derivatives were synthesized in moderate to good yields (60-75%) in a stepwise efficient protocol under mild condition. These new compounds have been proven by several spectroscopic techniques as IR, 1D and 2D NMR techniques and mass analysis. The in vivo anti-inflammatory was assessed for the synthesized compounds using carrageenan-induced rat hind paw edema model. Also, the in vivo analgesic activity for these products was examined utilizing hot-plate and acetic acid-induced writhing response assays. The isoxazole derivatives (3a-f) showed the most forceful anti-inflammatory and analgesic activities. Pyrimidopyrazines (4a-f) demonstrated weaker but comparable antiinflammatory and analgesic activities to the positive controls.

INTERACTIONS OF CELECOXIB WITH DIFFERENT ANTIDIABETIC DRUGS IN DIABETIC RATS

The selective cyclooxygenase-2 inhibitor, celecoxib, can be prescribed to type 2 diabetic patients receiving oral hypoglycemic agents. This study was conducted to assess whether celecoxib affect the hypoglycemic activity of oral hypoglycemic agents in streptozotocin-induced diabetic rats by measuring blood glucose level followed by determination of glucose uptake of isolated rat epididymal fat pads. Also, the effect of anti-diabetic agents on the anti-inflammatory activity of celecoxib was also assessed using carrageenan-induced hind paw edema model in diabetic rats.This study revealed that the effect of celecoxib on the hypoglycemic activity of glibenclamide was additive and can be explained by stimulation of tissue glucose uptake by celecoxib. On the other hand, the effect of celecoxib on the hypoglycemic activity of glimepiride was not simple additive but synergistic. This synergistic effect can be explained not only by stimulation of tissue glucose uptake by celecoxib but also via a pharmacokinetic interaction by increasing the serum glimepiride concentration.

Phytochemical and biological studies on Alnus glutinosa subsp. glutinosa, A. orientalis var. orientalis and A. orientalis var. pubescens leaves

Ethnopharmacological relevanceAlnus species have been used for the treatment of rheumatism, hemorrhoids and for wound healing in folk medicine. Materials and methodsAqueous and methanol extracts of A. glutinosa (L.) Gaertner subsp. glutinosa, A. orientalis Decne. var. orientalis and A. orientalis var. pubescens Dippel leaves were evaluated for their wound healing, anti-inflammatory and antioxidant activities. In vivo wound models of linear incision and circular excision were performed. “Inhibition of acetic acid-induced capillary permeability”, “carrageenan-induced hind paw edema” and T”PA-induced ear edema” assays were applied to determine the anti-inflammatory effects. For the antioxidant activity assessment, DPPH and ABTS radicals scavenging effect, reducing power and denaturation of nonspecific hydroxyl radical-targeted 2-deoxyribose were used. In vitro inhibitory effects on enzymes hyaluronidase, collagenase and elastase were evaluated. The methanol extract of the leaves of A. glutinosa subsp. glutinosa (MB), the most potent extract, was fractionated by bioassay-guided fractionation technique. The structure of the isolated compound was determined as shikimic acid by using NMR and IR analyses. ResultsMB increased the wound tension by 42.79% value and provided a contraction by 51.58%. Wound tension, contraction capacity and tissue hydroxyproline levels were increased with the application of the fraction EtOAc: MeOH (Fr. D), subfraction D27–38 and shikimic acid. In the “inhibition of acetic acid-induced capillary permeability” assay, MB, Fr. D, subfraction D27–38 and shikimic acid inhibited the permeability with significant inhibition values of 30.22%, 32.46%, 38.24% and 27.19%, respectively. In carrageenan-induced hind paw edema model, MB displayed 29.1% inhibition. Likewise, Fr. D, subfraction D27–38, and shikimic acid were found to exhibit remarkable anti-inflammatory and antioxidant effects. Shikimic acid exhibited significant inhibitory effect (38.24%) on the hyaluronidase enzyme. ConclusionsThis is the first and unique study that investigates wound healing, anti-inflammatory and antioxidant effects of some Alnus taxons growing in Turkey. According to the results, shikimic acid was found to be the major compound responsible from the activity.