Inhibition Of Paw Edema Research Articles

Antiarthritic activity of OA-DHZ; a gastroprotective NF-κB/MAPK/COX inhibitor.

Arthritis, a primary autoimmune disorder having a global incidence of 2.03% person/year, is presently being treated by many commercially available drugs that treat symptomatically or improve the disease's clinical state; however, all the therapies pose varying amount of side effects. Therefore, it has become a fundamental need to search for therapeutics that offer better efficacy and safety profile, and the natural or nature-derived products are known for their outstanding performance in this arena. OA-DHZ, known to possess anti-inflammatory and analgesic properties, when explored for its efficacy against arthritis in adjuvant-induced arthritis (AIA) model, was found to inhibit paw edema by 34% and TNF-α, IL-6, and IL-1β by 67%, 39%, and 45% respectively when compared to diseased control. It was also able to reduce the inflamed spleen size by 45% and successfully normalized biochemical and hematological changes that followed arthritis. In vitro studies revealed that the underlying mechanism for inhibiting arthritis progression might be due to NF-κB /MAPK pathway modulation. OA-DHZ also showed selective inhibition of COX-2 in vitro while showing gastroprotective effects when evaluated for ulcerogenic and antiulcer potential in vivo. In contrast to the results obtained from in vivo experimentation, there is a disparity in the pharmacokinetic profile of OA-DHZ, where it showed low oral exposure and high clearance rate. OA-DHZ being antiarthritic acting via NF-κB /MAPK/ COX inhibition while showing gastroprotective effects, can be a suitable candidate to be in the drug pipeline and further exploration.

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 < 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.

Ethosomes-based gel formulation of karanjin for treatment of acne vulgaris: in vitro investigations and preclinical assessment.

The online version contains supplementary material available at 10.1007/s13205-021-02978-3.

In Vivo and In Vitro Evaluation of Preventive Activity of Inflammation and Free Radical Scavenging Potential of Plant Extracts from Oldenlandia corymbosa L.

Aims: The present study evaluates the anti-inflammatory and antioxidant activity of the crude dichloromethane (CDCME), ethyl acetate (CEAE), and methanol (CMeE) extracts from the plant Oldenlandia corymbosa L. Background:Oldenlandia species have been popular among the people of the Indian subcontinent to treat several types of internal and external inflammation for a long time. Plant decoctions have been used to battle inflammation in cases of tonsilitis, pneumonia and cholecystitis, among others. Objective: The present work designed to demonstrate the properties of the previously mentioned plant extracts to prevent inflammation both in vivo and in vitro. This work is the first investigation of such extracts from this species and their relationship with anti-inflammatory activity. Method: The anti-inflammatory properties of the Oldenlandia corymbosa L. extracts were evaluated in vitro with the Red Blood Cell (RBC) membrane stabilization method and the protein denaturation method and in vivo with the carrageenan-induced paw oedema method. Furthermore, the free radical scavenging activity of the extracts was carried out with the 1,1-diphenyl-2- picrylhydrazyl (DPPH) radical oxidation, total antioxidant capacity and iron reduction assay. Result: Both in vivo and in vitro studies showed that CDCME had the most predominant effects with the value of 80.5% for RBC membrane stabilization, 60% for inhibition of protein denaturation at the concentration of 1000 µg/mL and 63.28% (after 3 h, * p < 0.05) for inhibition of paw oedema (300 mg/kg bwt) compared to carrageenan-induced mice. The free radical scavenging activity was studied by DPPH, total antioxidant and reducing activity assay. CDCME showed scavenging activity in all the methods and an IC50 value of 473.86 µg/mL for DPPH method. Conclusions: The findings of the study remarked that CDCME of the plant has strong anti-inflammatory and antioxidant effects that validate the traditional use of the plant to get remedy from pain. Other: The plants Oldenlandia corymbosa L. were provided by the Bangladesh Council of Scientific and Industrial Research Laboratory campus, Rajshahi, Bangladesh. Experiments on animals were conducted by ethical permission of Institute of Biological Sciences, University of Rajshahi, Bangladesh (license no: 225/320-IAMEBBC/IBSc).

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.

Fruits of Vitex doniana sweet: toxicity profile, anti-inflammatory and antioxidant activities, and quantification of one of its bioactive constituents oleanolic acid

BackgroundVitex doniana Sweet fruit, an under-utilised crop specie of Ghana, has not been validated for its ethnomedical use in managing inflammatory conditions. Therefore, the study sought to investigate its anti-inflammatory and antioxidant activities as well as isolate and quantify one of its active constituents. Materials and methodsIn-vivo anti-inflammatory activity of the methanol fruit extract was evaluated using the carrageenan-induced oedema model in chicks. The in-vitro antioxidant property was also investigated using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. The acute and subacute toxicity studies of the fruit extract were evaluated in rodent models. ResultsNo signs of autonomic and central nervous system stimulation/depression were recorded. The LD50 by oral route, was estimated to be beyond 3000 mg/kg. Subacute studies revealed an increase in red blood cell and lymphocyte counts. Liver enzymes, serum proteins and bilirubin levels did not significantly increase. The crude extracts at doses of 10, 30 and 100 mg/kg inhibited paw oedema considerably. The ethyl acetate fraction showed the highest antioxidant activity (IC50 = 99.35 ± 0.77 μg/mL). Oleanolic acid, isolated from the ethyl acetate extract, showed significant anti-inflammatory and antioxidant activities. A sensitive high-performance liquid chromatography method for the detection and estimation of oleanolic acid, as a biomarker compound for V. doniana fruit, was developed and validated for quality assurance purposes. ConclusionThe extract of V. doniana fruits possesses considerable anti-inflammatory and antioxidant properties and was non-toxic under laboratory conditions.

Polar extracts from Gymnosporia senegalensis (syn. Maytenus senegalensis) root bark, its effects on nociception, edema, and malarial infection

BackgroundGymnosporia senegalensis (syn. Maytenus senegalensis) is a commonly used medicinal plant for the treatment of infectious and inflammatory diseases. MethodsThe crude methanol extract (CMGS) and the polar fraction (PFGS) from G. senegalensis root bark were tested for antimalarial, antiedematogenic (paw edema induced by egg albumin), and antinociceptive (hot plate) activities. The PFGS was characterized using gas chromatography coupled with mass spectroscopy (GC–MS). Hematological and biochemical parameters were analyzed after 3 weeks of administration and 2 weeks after the extract intake was discontinued. ResultsThe PFGS at 200 and 300 mg/kg exhibited higher suppression of malaria infection (43.70 ± 1.16 and 47.69 ± 1.03% all p < 0.01) and prolonged the survival days of the mice better than the CMGS at 800 mg/kg (29.72±0.23% p < 0.05) but lower than the chloroquine (73.13 ± 2.34% p < 0.001). The CMGS caused 51.92 ± 2.34 and 54.66 ± 1.35% inhibition of paw edema at 400 and 800 mg/kg while the PFGS caused 57.12 ± 3.35 and 58.22 ± 2.90% inhibition of paw edema at 200 and 300 mg/kg, respectively. In addition, CMGS demonstrated a dose-dependent antinociceptive effect (p < 0.01) against thermal-induced pain in rats. GC–MS analysis revealed the presence of four polar compounds: 5,6,7,7a-tetrahydro-2(4H)-benzofuranone (isomintlactone); ((20a)-3‑hydroxy-2-oxo-24-nor-friedela-1(10),3,5,7-tetraen (pristimerin); 2H,6H-pyrano[3,2-b] xanthen-6-one (jacareubin) and 5,7,3′-trihydroxy-6,4′-dimethoxyisoflavone (iristectrorigenin) as the major components of PFGS, having percentage occurrence of 25.89, 21.95, 20.97 and 9.23, respectively. The serum activities and concentrations of AST, ALT, ALP, total proteins, sodium, and potassium increases after 3 weeks of administration and were reversed 2 weeks after the extracts intake was discontinued. Conclusionour studies provide preclinical evidence of the antimalarial, antiedematogenic, and antinociceptive activities of CMGS and PFGS suggesting its potentials for the treatment of malaria and inflammation diseases.

Anti-inflammatory, analgesic, and acute toxicity evaluation of Litchi chinensis seed extract in albino rat

Litchi chinensis is a edible fruits of soapberry family commonly known as lychee; is traditionally used for the treatment of inflammation, headache, and body pain. The present study investigated the toxicity, anti-inflammatory, and analgesic activity of the ethanolic crude extract of Litchi chinensis to support its traditional use in its folk medicine and to screen the phytochemical constituents. 70% ethanolic extract of seeds of Litchi chinensis (LCSE) was prepared and preliminary phytochemical screening was performed. Acute toxicity of LCSE was carried out based on OECD guidelines 423. In vivo anti-inflammatory and analgesic effect of the extract was evaluated using carrageenan-induced paw edema and hot plate methods in Wistar albino rat's model. Results revealed that LCSE contains phenols, tannins, flavonoids, saponins, steroids, and alkaloids. LD50 values were found to be higher than 5000 mg/kg body weight; no any sign of toxicity, behavior changes, moribund, and mortality were observed in LCSE treated animals. Oral administration of LCSE at the dose of 150, 300, and 600 mg/kg produced a significant (p&lt;0.05) dose-dependent inhibition in carrageenan-induced rat paw edema and hot plate. These results suggest that LCSE is non-toxic, and shows potent anti-inflammatory and analgesic activities over Wistar albino rats. These finding demonstrate that lychee seed extract acts as a good therapeutic candidate for the safe anti-inflammatory agents.

Anti-rheumatoid activity of a hexane-insoluble fraction from Plantago major in female Wistar rats induced by Complete Freund's Adjuvant

Background and aimPlantago major has long been used for medical purposes in Indonesia. However, reports on the anti-arthritic activities of P. major are limited. Experimental procedureThe anti-arthritic properties of an n-hexane-insoluble fraction of dichloromethane extracts of P. major (IPM) were evaluated using Complete Freund's Adjuvant (CFA)-induced arthritis induced in female Wistar rat by CFA. Diclofenac was used as a positive control. The volume of paw oedema, white blood cell count, lymphocytes, neutrophils, expression of TNF-α and Interleukin-6 and the histopathological features of the joint tissues were assessed to characterise IPM activity. ResultsThe IPM extract at doses of 280 and 420 mg/kg BW and diclofenac inhibited paw oedema by 15.70 %, 15.94 % and 19.71 % respectively. IPM also reduced the incidence of arthritis and arthritic index. Unlike untreated rats, animals treated with IPM showed a significant decrease in the number of neutrophils and decreased expression of TNF-α and Interleukin-6. Histopathological examination showed a reduction in the number of inflammatory cells and hyperplasia of the synovium after IPM treatment. ConclusionThis study showed that P. major displays anti-rheumatoid arthritis activity.

Antibacterial activity and phytochemical characterisation of Saussurea gossypiphora D. Don.

The study demonstrates that S. gossypiphora contain number of secondary metabolites such as steroids, tannins, flavonoids, phenolics, carbohydrates, saponins, and amino acids. Methanolic extract (MESG) of the plant contained highest quantity of phenolics, flavonoids and has greater antioxidant, anti-inflammatory and antibacterial activity in comparison to other extracts. Moreover, acute toxicity studies revealed that none of the extracts produced any toxic symptoms and mortality when administered orally to mice at a dose of 2000mg/kg b. w. Furthermore, in MESG, the SG-4 fraction exhibited the highest antibacterial activity than other isolated fractions against all tested bacterial strains in a dose-dependent manner. SG-4 fraction showed significant anti-inflammatory effect (60.91%) as evident by maximum inhibition of Carrageenan-induced paw oedema in rat model. The HPTLC analysis confirmed the presence of apigenin and luteolin in the SG-4 fraction of methanolic extract. A noticeable number of mineral elements were also found to be present in S. gossypiphora. Conclusively, our study reveals that Saussurea gossypiphora contains plethora of bioactive compounds that contributes to its antioxidant, anti-inflammatory and antibacterial activity. Apigenin and luteolin possibly being one of them. Besides, the presence of ample minerals hints is utilisation as nutritionally valuable herb.

Synthesis, in vivo and in silico analgesic and anti-inflammatory studies of α-D-ribofuranose derivatives

Five α-D-ribofuranose analogues (2, 3, 4, 5 and 6) were synthesized in good yields from 3-O-benzyl-4-C-(hydroxymethyl)-1, 2-O-isopropylidene-α-D-ribofuranose (1). The synthesized compounds were then subjected to analgesic, anti-inflammatory, antimicrobial and antioxidant assays. Compound 3 demonstrated 79.74% (P < 0.001) writhing inhibition and highest reaction time of 2.55 ± 0.13 min (P < 0.001) after 30 min of oral administration in peripheral and central analgesic assay, respectively, at 50 mg/kg dose. Compound 2 and 6 exhibited significant anti-inflammatory activity at 100 mg/kg dose with paw edema inhibition of 91.15% (P < 0.001) and 95.13% (P < 0.001), respectively, in 4th hour. The synthesized analogues did not show notable antioxidant and antibacterial properties. Molecular docking study revealed higher binding affinity of −8.1 kcal/mol and −8.9 kcal/mol of compound 3 towards cyclooxygenase-1 and phospholipase A2, respectively, compared to −7.7 and −7.6 kcal/mol respectively for corresponding native ligands. Compound 2 demonstrated binding affinity of −9.1 kcal/mol towards interleukin-1 receptor-associated kinase-4 compared to −8.7 kcal/mol of the native ligand. The molecular properties related to drug likeness of compounds were found to be within acceptable range. Synthesized D-ribofuranose analogues demonstrated promising analgesic and anti-inflammatory activities and further development may lead to new potent analgesic and anti-inflammatory agents.

Anti-Inflammatory and Antinociceptive Properties of Kielmeyerone A, a Chromenone Isolated from the Roots of Kielmeyera reticulata

Four new chromenones, kielmeyerones A-D (1-4), were obtained from the roots of Kielmeyera reticulata. Their structures were elucidated based on spectroscopic data (NMR and HRESIMS) interpretation. The pharmacological activity of kielmeyerone A (1), the major compound, was evaluated using in vitro and in vivo inflammation and pain models. During in vitro screening, 1, at noncytotoxic concentrations (0.097-1.56 μM), inhibited NO production by J774 macrophages stimulated with LPS and IFN-γ. In the complete Freund's adjuvant-induced inflammation model in mice, 1 (12.5-50 mg/kg) inhibited paw edema, demonstrating an anti-inflammatory effect. Additionally, 1 (12.5-50 mg/kg) induced a dose-dependent antinociceptive effect in the late phase of the formalin test, a profile similar to those of nonsteroidal anti-inflammatory drugs. Mice treated with 1 (100 mg/kg) did not show motor performance alterations using a rota-rod test. Thus, the present study has characterized new chromenones from Kielmeyera reticulata and has provided evidence of the anti-inflammatory and antinociceptive properties of one of these, kielmeyerone A (1).

EVALUATION OF ANTI-INFLAMMATORY (IN VIVO) ACTIVITY OF ARIFLEX LINIMENT IN COMPARISON WITH DICLOFENAC GEL IN CARRAGEENAN INDUCED RAT PAW EDEMA MODEL

Objective: The present study was conducted to evaluate anti-inflammatory activity of Ariflex liniment (conceptualized and developed by Ari Healthcare Pvt. Ltd) in comparison with Diclofenac gel in carrageenan induced rat paw edema model.&#x0D; Methods: Wistar rats of either sex weighing 150-180 g were taken and divided into 3 groups with 6 animals in each group i.e. Group 1 (Controlled Group), Group 2 (Diclofenac gel) and Group 3 (Ariflex liniment). The study drugs were topically applied 30 min prior to carrageenan injection. After 30 min 1% w/v of 0.05 ml carrageenan was injected subcutaneously in the paw. The paw was marked with ink at the level of lateral malleolus and immersed in mercury up to the lateral malleolus mark. The paw volume was measured plethysmographically, immediately after injection i.e. on 0 min, and then on 30 min,1h, 2h,3h, 4h and 5hr after injection.&#x0D; Results: Diclofenac gel sodium treated group showed significant inhibition (p&lt;0.01) of paw edema at 30 min, 1, 2, 3, 4 and 5th hrs as compared to control group. Ariflex Liniment showed significant inhibition (p&lt;0.05) of paw edema at 30 min, 1, 2, 3, and 4th hrs as compared to the control group. Group treated with Ariflex Liniment did not show any significant decrease in paw edema volume at 5th hrs when compared to the control group.&#x0D; Conclusion: Ariflex Liniment possesses anti-inflammatory activity.

Pharmacological and Biochemical evaluation of anti-arthritic activity of Justicia gendarussa extract in FCA induced arthritis in Wistar rats

The present study is carried out to evaluate anti-inflammatory and anti-arthritic potential of Justicia gendarussa. Leaves and stem extracted with ethanol and chloroform. These extract is tested against in-vitro (HRBC membrane stabilization method and Inhibition of protein denaturation method) and in-vivo (Carrageenan induced paw edema model) anti-inflammatory models. To assess the anti-arthritic activity, FCA induced arthritis model is used. Assessment of arthritis is done by paw volume, joint diameter, body weight, biochemical parameters, hematological parameters (Hb, RBC, WBC, ESR). The effect of in-vitro anti-inflammatory model depends on concentration. Both test extract and standard Diclofenac sodium has been shown concentration dependent effect. The maximum anti-inflammatory effect of the test extract achieved at 2000μg/ml. The test (JGLE, JGLC, JGSE) has been shown inhibition of paw edema induced by carrageenan at 50mg/kg body weight. The extract JGLE, JGLC, JGSE at 50mg/kg body weight and 100mg/kg body weight orally showed the significant (P&lt; 0.05) and dose dependent inhibitory effect against FCA induced arthritis model. Diclofenac sodium 20mg/kg body weight orally is used as a standard. JGLE exhibit more significant and most promising anti-arthritic and anti-inflammatory effect than other extracts these effects support the traditional role of J. gendarussa in arthritis and other inflammatory condition.

Delonix Regia Bark Alleviated Inflammation by Stimulating Defense Responses in Rats

ABSTRACT The methanol extract of Delonix regia bark (DMeOH) was investigated for its anti-inflammatory property in kappa-carrageenan (Carr)-induced hind paw edema of rats. DMeOH was orally administered and evaluated as a measure of edema, tissue destruction, and neutrophil migration to the inflammation site. The pro-inflammatory mediators, p-p65 subunit of NFκB, interleukin (IL)-1β, cycloxygenase (COX)-2 and inducible nitric oxide synthase (iNOS) were analyzed. Catalase (CAT) and superoxide dismutase (SOD) enzyme activity assays and malondialdehye (MDA) were quantified. The LC-MS fingerprint of the extract identified 10 polyphenols, of which five were structurally characterized based on their [M-H]− peak, UV-vis absorption compared to published data. Anti-inflammatory studies revealed that pre-treatment with DMeOH (0.5 g kg−1) prior to Carr-injection inhibited paw edema abating tissue destruction with decreased neutrophil infiltration. Carr-injection resulted in increased NO(•-) production, iNOS transcript and p-p65 subunit of NF-κB protein. DMeOH feed inhibited NO(•-) production and iNOS transcript levels. A decreased expression of NF-κB p-p65 subunit, COX-2 and IL-1β at 0.5 g kg−1 b.w oral feed suggest that DMeOH exerted its anti-inflammatory property by inhibiting NFκB activation. An increase in the antioxidant enzyme activities of CAT (78%) and SOD (49%) with reduced MDA levels was recorded.

Leaves of Stereospermum suaveolens DC Exhibit Anti-inflammatory and Anti-arthritic Potential Action in Experimental Animals

Aim: The experimental investigation of current research work was to identify traditional rich claim of Stereospermum suaveolens DC leaves for anti-inflammatory and anti-arthritic potential action in animals.&#x0D; Study design: Ethyl acetate fraction of Stereospermum suaveolens DC (Bignoniaceae) methanolic extract of leaves evaluated at 125mg/kg, 250mg/kg and 500mg/kg (p.o.) doses for anti-inflammatory and anti-arthritic activity.&#x0D; Methodology: Ethyl acetate fraction of Stereospermum suaveolens DC (Bignoniaceae) methanolic extract of leaves was evaluated for phytochemical investigation for total flavonoid content using UV spectroscopy and TLC study. Carrageenan induced rat paw edema (Acute method) and Freund’s complete adjuvant (FCA) induced chronic arthritis in wistar rats were used as an animal models to claim Stereospermum suaveolens DC leaves for anti-inflammatory and anti-arthritic potential. The rat paw volume and percentage inhibition of the paw edema were evaluated for anti-inflammatory activity. The assessments of arthritis in rats were measured by haematological values and radiological examinations.&#x0D; Result: Ethyl acetate fraction of Stereospermum suaveolens DC (Bignoniaceae) methanolic extract of leaves showed presence of total flavonoids and saponins. The significant inhibition in paw volume and edema (p &lt; .01) obtained at 250mg/kg and 500mg/kg oral dose. These obtained results were established confirmation outcome for presence of rich flavonoid contents in Stereospermum suaveolens DC leaves and provides valuable source of bioactive phytocomponents. &#x0D; Conclusion: Ethyl acetate fraction of Stereospermum suaveolens DC (Bignoniaceae) methanolic extract of leaves showed significant inhibition of inflammatory reaction as compared to standard drug indomethacin Sterospermum Suaveolens DC leaves were showed potential therapeutic role in treatment of inflammation and arthritis cases.

Anti-oedematous and antinociceptive activities assessment of stem bark aqueous extract of Ficus exasperata Vahl. (Moraceae) in rat and mice.

Background: Ficus exasperata Vahl. (Moraceae) is widely used in African traditional medicine for the treatment of various diseases. The present study is undertaken to assess the anti-oedematous and antinociceptive activities of the stem bark aqueous extract of Ficus exasperata in mice and rats. Methods: The anti-oedematous activity was investigated following carrageenan or histamine-induced rat paw oedema models. Antinociceptive activity was evaluated using acetic acid induced writhing test (1 %, 10 ml/kg), capsaicin-induced neurogenic pain (32 µg/mL, 30 µL) and formalin-induced test (1%, 20 µL). Extract was administrated orally at 37.5, 75 and 150 mg/kg. Results: Pre-treatment of rats with Ficus exasperata stem bark aqueous extract exhibited significant inhibition of paw oedema during all the phases of both carrageenan and histamine induced edema in rat. The maximum inhibition percentages were 94.75 % (3 h) and 30.64 % after one hour at the dose of 37.5 mg/kg, respectively, in carrageenan or histamine models. Antinociceptive activity showed that aqueous extract reduced significantly (p &lt; 0.001) the pain induced by acetic acid with an inhibition percentage of 70.8% (150 mg/kg). In the formalin-induced test, the extract also reduced significantly (p &lt; 0.001) licking time during neurogenic phase and inflammatory phase with inhibition percentages of 44.75% and 52.78% respectively at the dose of 75 and 150 mg/kg. In addition, aqueous extract of F. exasperata reduced significantly (p &lt; 0.001) neurogenic pain induced by capsaïcin by 71.28 % at the highest dose (150 mg/kg). Conclusion: This finding suggests that the stem bark aqueous extract of Ficus exasperata possess potent anti-oedematous and antinociceptive activities.

Anti-Inflammatory Activity of Artemisia vulgaris Leaves, Originating from Three Different Altitudes of Nepal.

This study aimed to evaluate and compare the in vivo chronic anti-inflammatory efficacy, from the ethyl acetate and ethanolic extracts of Artemisia vulgaris leaves, grown at three different altitudes in Nepal, by formalin-induced paw edema in Swiss albino mice. Edema was induced on the mice paw by administering 0.2% of formalin injection. Indomethacin was used as a standard drug at the concentration of 5 mg/kg of body weight. Ethyl acetate and ethanolic leaves extract, at the concentration of 200 mg/kg and 400 mg/kg, were used as test drugs. Standard drug and all the extracts were administered 30 min before formalin injection. The paw thickness was measured at 0, 1, 2, 3, 24, 48, and 72 hours after formalin injection, using a Vernier caliper. It was observed that both ethyl acetate and ethanolic extract from all the altitudes exhibited significant inhibition of paw edema (p < 0.05) induced by formalin. Maximum activity was shown by 400 mg/kg of the plant leaf extract taken from the temperate zone, with 54.05% of paw edema inhibition, and it is almost similar to the inhibition of standard drug (56.75%). Moreover, the ethanolic extract was found to be more effective than ethyl acetate extract in all the plant samples. The results suggested that the anti-inflammatory effect of A. vulgaris leaves increases with an increase in altitudes and this plant can be used as a useful source of medicine to treat chronic inflammation.

Pharmacological Screening of Substituted Benzimidazole Derivatives

In the present study some substituted benzimidazole derivatives were screened for several biological activities. The synthesized compounds were subjected to evaluation of central analgesic, anti-inflammatory, cytotoxicity, antimicrobial and antioxidant activities by radiant heat induced tail flicking, carrageenan induced rat paw edema inhibition, brine shrimp lethality bioassay, disc diffusion and DPPH free radical scavenging methods, respectively. Compounds 2a, 2c and 2d elongated the tail flicking time by 58.07-, 51.59- and 76.65%, respectively (p &lt; 0.001) at 50 mg/kg body weight dose compared to the standard morphine (87.17%). Compounds 2b, 2c and 2d showed prominent anti-inflammatory activity at 100 mg/kg body weight dose (% of paw edema inhibition 81.75%, 79.09% and 86.69%, respectively) compared to the standard aceclofenac (87.83%). Among the synthesized benzimidazole derivatives, compounds 1a, 1b, 1c, 2a and 2d exhibited potent cytotoxicity with the IC50 values of 5.47-, 11.92-, 4.55-, 7.63- and 7.94 μg/ml, respectively. In addition, compounds 1c and 2d displayed mild to moderate zone of inhibition (8-12 mm). On the other hand, 1a and 1b showed very mild antioxidant activity with IC50 values of 12.25 × 103 μg/ml and 87.33 ×103 μg/ml. Among all the derivatives, 2c, 2d and 1c can be potential candidates for designing new analgesic, anti-inflammatory and anti-cancer agents in future.&#x0D; Dhaka Univ. J. Pharm. Sci. 20(1): 95-102, 2021 (June)

Pyrazoles and Pyrazolines as Anti-Inflammatory Agents.

The five-membered heterocyclic group of pyrazoles/pyrazolines plays important role in drug discovery. Pyrazoles and pyrazolines present a wide range of biological activities. The synthesis of the pyrazolines and pyrazole derivatives was accomplished via the condensation of the appropriate substituted aldehydes and acetophenones, suitable chalcones and hydrazine hydrate in absolute ethanol in the presence of drops of glacial acetic acid. The compounds are obtained in good yields 68–99% and their structure was confirmed using IR, 1H-NMR, 13C-NMR and elemental analysis. The novel derivatives were studied in vitro for their antioxidant, anti-lipid peroxidation (AAPH) activities and inhibitory activity of lipoxygenase. Both classes strongly inhibit lipid peroxidation. Compound 2g was the most potent lipoxygenase inhibitor (IC50 = 80 µM). The inhibition of the carrageenin-induced paw edema (CPE) and nociception was also determined, with compounds 2d and 2e being the most potent. Compound 2e inhibited nociception higher than 2d. Pyrazoline 2d was found to be active in a preliminary test, for the investigation of anti-adjuvant-induced disease (AID) activity. Pyrazoline derivatives were found to be more potent than pyrazoles. Docking studies of the most potent LOX inhibitor 2g highlight hydrophobic interactions with VAL126, PHE143, VAL520 and LYS526 and a halogen bond between the chlorine atom and ARG182.