Anti-inflammatory and analgesic activities with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonian Eunicella singularis

Objective: To explore anti-inflammatory activities of organic extract and its semi-purified fractions(ethanol, acetone, methanol/dichloromethane) from the Mediterranean gorgonian Eunicella singularis. Methods: The anti-inflammatory and analgesic activities were evaluated, using the carrageenan-induced rat paw edema model and the acetic acid writhing test in mice. The gastroprotective activity was determined using HCl/Et OH induced gastric ulcers in rats. The purification and structure elucidation of compound(s) from the more effective fraction were determined by chromatographic and spectroscopic methods and in comparison with data reported in the literature. Results: The fraction F-Et OH showed an important antiinflammatory activity associated with significant analgesic and gastroprotective properties. The purification and structure elucidation of compound(s) from this fraction lead to the identification of one diterpenoid and four sterols. Conclusions: These results suggested that components from the active fraction can be used to treat various anti-inflammatory diseases.

Anti-inflammatory and analgesic activities of Melanthera scandens

Objective:To evaluate the anti-inflammatory and analgesic activities of leaf extract of Melanthera scandens(M.scandens).Methods:The crude leaf extract(39-111 mg/kg)of M.scandens was investigated for anti-inflammatory and analgesic activities using various experimental models.The anti-inflammatory activity was investigated using carragenin,egg-albumin induced oedema models,while acetic acid,formalin-induced paw licking and thermal-induced pain models were used to evaluate the antinociceptive property.Results:The extract caused a significant(P<0.05-0.001)dose-dependent reduction of inflammation and pains induced by different agents used.Conclusions:The leaf extract possesses anti-inflammatory and analgesic effects which may be mediated through the phytochemical constituents of the plant.

[1-(4-Nitrobenzyl)-2-butyl-4-chloro-1<i>H</i>-imidazol-5-yl]-4, 5-dihydro-1-phenyl-1<i>H</i>-pyrazole: Synthesis, Anti-Inflammatory and Analgesic Activities

In the present investigation, series of Bis (heterocycle)s bearing pyrazoline in combination of the imidazole derivatives have been synthesized via 1,3-dipolar cycloaddition reactions of N-(nitrobenzyl)-imidazole nitrile imines with different dipolarophiles. All the newly synthesized compounds were characterized and screened for analgesic-anti-inflammatory activities and were compared with the standard drugs. The compounds exhibited excellent anti-inflammatory and analgesic activities. Out of the compounds studied 4b, 4d and 4g compounds shown statistically significant activity comparable to the standard drugs Ibuprofen and Aspirin at the same dose.

Analgesic and anti-inflammatory activity of Cotinus coggygria Scop.extracts in vivo

Objective:To assess the analgesic and anti-inflammatory effects of standardized extract of Cotinus coggygria(C.coggygria)in different animal models.Methods:C.coggygria extracts(25,50,and 100 mg/kg)were administered to rats and mice(n=6)during hot plate,tail-flick,acetic acid-induced writhing,and formalin tests to determine its analgesic efficacy.The anti-inflammatory activity of C.coggygria extracts was evaluated by histamine and carrageenan-induced paw edema,cotton pellet-induced granuloma,and acetic acid-induced peritoneal capillary dye leakage tests.Results:C.coggygria extracts(50 and 100 mg/kg)significantly alleviated thermal and chemical-induced pain in rodents(P<0.05).It also demonstrated notable anti-inflammatory properties by mitigating histamine and carrageenan-induced paw edema,granuloma deposits,and vascular permeability(P<0.05).Moreover,C.coggygria extracts remarkably reduced TNF-α,IL-1β,IL-6,COX-2,and oxidative stress in rat paws(P<0.05).Carrageenan-induced histological aberrations in hind paw tissues were effectively(P<0.05)mitigated by treatment with C.coggygria extracts.Conclusions:C.coggygria Scop.extracts show analgesic and anti-inflammatory effects via inhibition of COX-2 and inflammatory and oxidative mediators.

Analgesic and anti-inflammatory activities of the ethanol extract of the leaves of Helianthus Annus in Wistar rats

Objective:To investigate the anti-inflammatory and analgesic effects of the ethanol extract of leaves of Helianthus annus L.(H.annus) in acclimatized Wistar rats.Methods:It was undertaken using the albumin induced paw edema model of inflammation as well as both the hotplate and tail immersion analgesic test methods.Doses of the extract tested in experimental rats were 0.5 g/kg,2 g/kg and 4 g/kg while negative and positive control rats received distilled water and indomethacin respectively.Results:It was shown that treatment with the tested doses of the extract effectively inhibited paw edema induced by egg albumin.This effect was comparable if not better than the observations made in rats treated with 10 mg/kg of indomethacin orally.Treatment with the extract was also observed to have significantly increased the mean tolerance time of rats to thermal noxious stimuli compared to control animals that had distilled water and appeared to be more effective than 10 mg/kg of indomethacin treatment.Conclusions: These observations confirmed the presence of a strong anti-inflammatory and anti-noiciceptive activity in the ethanol extract of the leaves of H.annus and therefore validated the folkloric use of the leaves of this plant in treatment of pro-inflammatory,post traumatic situations.

Analgesic and anti-inflammatory activities of Passiflora foetida L.

Objective:To investigate the analgesic and anti-inflammatory activities of ethanol extract of Passiflora foetida(P.foetida) leaves.Methods:Ethanol extract of P.foetida leaf was evaluated for analgesic action by acetic acid-induced writhing and hot plate method in albino mice.The anti-inflammatory property of ethanolic leaf extract was tested by carrageenan induced acute paw edema and histamine induced acute paw edema in rats.Results:The dose 200 mg/kg of P. foetida leaf extract exhibited highest significant analgesic activity[(13.50±0.43) min]at a reaction time of 20 min in hot plate method in mice.The ethanol extract of leaf dose 100 mg/kg produced a highly significant anti inflammatory effect[(1.302±0.079) mL]in rats.Conclusions:It is very clear that P.foetida also has analgesic and anti-inflammatory activities for the pharmaceuticals.

Analgesic,anti-inflammatory and anti-diarrheal activities of ethanolic leaf extract of Typhonium trilobatum L.Schott

Objective:To explore the efficacy of ethanolic leaf extract of Typhonium trilobatum L.Schott in treating diarrhea,pain and inflammation using experimental models.Methods:In the present study,acetic acid-induced writhing,xylene-induced ear edema and castor oil-imluced diarrlieal model were used to evaluate the analgesic,anti-inflammatory and anti-diarrheal activities,respectively.Acute toxicity test was carried out to fix the safe doses of the plant extract.Results:The plant extract demonstrated a significant inhibition of writhing(P<0.01)compared with the control group in acetic acid-induced writhing test in mice.The extract also significantly inhibited the xylene induced ear edema formation(P<0.05).In anti-diarrheal test,the extract significantly decreased the frequency of defecation and increased the mean latent period(P<0.0l)in castor oil-induced diarrheal model mice at the doses of 250 and 500 mg/kg body weight.Conclusions:These results suggest that the extract possesses significant analgesic,anti-inflammatory and anti-diarrheal activities that support to the ethnopharmacologicl uses of this plant.

Evaluation of Analgesic and Anti-Inflammatory Activities on Ethanolic Extract of <i>Terminalia chebula</i>Fruits in Experimental Animal Models

The present study was undertaken to evaluate the analgesic and anti-inflammatory activities of ethanolic extract of Terminalia chebula (commonly known as Haritaki) fruits in experimental animal models. The study was carried out using Swiss Albino mice (20-25 g) and Long Evans rats (100-150 g) of either sex. The analgesic activity of Terminalia chebula was assessed by using hot plate method. For the determination of analgesic effect, doses of ethanolic extract of Terminalia chebula used in the present study were 250 mg/kg and 500 mg/kg body weight (BW). Anti-inflammatory effect was analyzed by carrageenan induced paw edema method with the administration dose of 300 mg/kg BW of animals. The analysis of experimental data was performed by statistical process of ANOVA to determine the variability of sample, while Dunnet’s test was performed for evaluation of comparative analgesic and anti-inflammatory activity of Terminalia chebula with control and standard. The animals were divided into four treatment groups of six animals each and the “Mean ± SEM” is the statistical identifiable value of the data and P values <0.05 was considered statistically significant. Hot plate test showed a significant increase in the mean reaction time to heat stimuli in hot plate method at both 250 mg/kg and 500 mg/kg BW doses throughout the observation period in 30 minutes and 60 minutes after treatment, which was comparable to the standard ketorolac and control group. In carrageenan induced paw edema method, considerable results were found after determining the percentage change in paw volume in extract. In both cases of analgesic and anti-inflammatory study, % inhibition of pain and inflammation were evaluated. Comparing with control, largest inhibition was found in inhibiting inflammation 5 hours after treatment, while the largest inhibition of pain was obtained in 30 minutes and 60 minutes after treatment of doses. The present study suggests that ethanolic extract of Terminalia chebula fruits has significant analgesic and anti-inflammatory activities.

Synthesis and analgesic activities studies on bispiperazinium (BPZ) salts

Selecting compound 97-9-G4 as lead compound, a series of bispiperazinittm salts 5a-h were designed, synthesized and evaluated for their analgesic activities. The results show that phenylethyl group of 97-9-G4 is a crucial pharmacophore; the intro- duction of electron-withdrawing group on benzene ring is favorable to the activity.

Effect of simulated gastrointestinal digestion on antioxidant,and anti-inflammatory activities of bioactive peptides generated in sausages fermented with Staphylococcus simulans QB7

Dry-fermented sausages are a good source of bioactive peptides,whose stability against gastrointestinal(GI)digestion determines their bioaccessibility.This study focused on evaluating the effect of peptide extracts from sausages fermented with Staphylococcus simulans QB7 during in vitro simulated GI digestion,including peptide profiles and antioxidant and anti-inflammatory activities.Peptides present in sausages were degraded during digestion,with molecular weight reduced from>12 kDa to<1.5 kDa.Besides,the content of amino acids increased from 381.15 to 527.07 mg/g,especially tyrosine being found only after GI digestion.The anti-inflammatory activities were increased after GI digestion,however,the changes in antioxidant activities were the opposite.A total number of 255,252 and 386 peptide sequences were identified in undigested,peptic-digested and GI-digested samples,respectively.PeptideRanker,BIOPEP-UWM and admetSAR were used to further predict the functional properties and intestinal absorption of the identified peptide sequences from GI digestion.Finally,18 peptides were discovered to possess either antioxidant or anti-inflammatory capacities.

Structural characterization and anti-inflammatory activities of novel polysaccharides obtained from Pleurotus eryngii

Natural polysaccharides named PEP-0.1-1,PEP-0-1 and PEP-0-2 from edible mushroom species Pleurotus eryngii were obtained in the present study.Results showed that molecular weights of these polysaccharides were 3235,2041 and 23933 Da,respectively.Further,structural characterization revealed that PEP-0.1-1 had a→4-α-D-Glcp-1→backbone and contained→4)-α-D-Glcp and→4)-β-D-Glcp reducing end groups.PEP-0-1 backbone contained→4-α-D-Glcp-1→and→6-α-3-O-Me-D-Galp-1→,and the side chains containedα-D-Glcp,β-D-Manp-1→andα-D-Glcp-3→.However,PEP-0-2 backbone consisted of→4-α-DGlcp-1→and→6-α-3-O-Me-D-Galp-(1→6)-α-D-Galp-1→while the side chains containedα-D-Glcp andβ-D-Manp-1→.Biological activity analysis was then carried out and found that all these polysaccharides could significantly suppress the relative mRNA expression of toll-like receptor 4,nitric oxide(NO),tumor necrosis factor-α,interleukin(IL)-1βand IL-6 in lipopolysaccharide(LPS)-induced inflammation of RAW264.7 cells,as well as the over secretion of the above cell cytokines.Moreover,Western blotting analysis revealed that all these purified fractions displayed significant inhibition effects on the expression of c-Jun N-terminal kinases protein induced by LPS in mitogen activated protein kinase pathway,along with the relieving on the inhibition effect of LPS on IκB-αprotein expression.In summary,the information generated by the present study could provide a theoretical basis for the exploration of novel healthy food materials from edible mushroom with antiinflammation activities.

Anticancer,Anti-inflammatory,Analgesic,and Anxiolytic Effects of Koumine and Their Molecular Mechanisms

Koumine is an indole alkaloid monomer extracted from the Chinese herb Gelsemium elegans,which has a variety of pharmacological effects.This paper provides a comprehensive summary of the pharmacological effects and molecular mechanisms of koumine,with a particular emphasis on its mechanisms of action in the context of anticancer,anti-inflammatory,analgesic,and anxiolytic properties.The aim is to provide a theoretical foundation for further research and the application of koumine in clinical practice.

Synthesis and anti-inflammatory-analgesic activity of 2',4'-difluoro-3-(carbamoyl)biphenyl-4-yl benzoates

Eighteen 2′,4′-difluoro-3-（carbamoyl）biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analysis. The anti-inflammatory activity and analgesic activity for 18 compounds were evaluated. The preliminary assay results showed that compounds 4a and 4p exhibited potent anti-inflammatory-analgesic activity.

Analgesic and Anti-Inflammatory Activity of Total Crude Leaf Extract of <i>Phytolacca dodecandra</i>in Wistar Albino Rats

Background: Pain is a common problem encountered in daily life among humans and animal and it is commonly managed conventionally using modern medicines and traditionally by use of medicinal plants. Phytolacca dodecandra is a common herb in Uganda, used traditionally to alleviate pain and inflammatory conditions. However, its activity in alleviating pain and inflammatory diseases has not been fully scientifically evaluated. Aim of Study: To evaluate the analgesic and anti-inflammatory activity of total crude leaf extracts of P. dodecandra in Wistar albino rats. Materials and Methods: It was a laboratory-based experimental study. Acetic acid-induced writhing test was used to determine the analgesic activity and the histamine-induced paw edema formation for anti-inflammatory activity of the extract. Twenty eight animals were divided into 7 groups each with 4 rats and two (2) sets of data were obtained from each animal per group as per guidance of the refinement rule of 3Rs. For analgesic activity, Group I was dosed with 1.0ml of normal saline (negative control), group II, III, IV, V, VI were dosed with 1000.0, 600.0, 150.0, 40.0 and 5.0 mg/kg bwt of extract respectively. Group VII was dosed 10.0 mg/kg bwt diclofenac sodium (Na) drug (positive control). For anti-inflammatory activity, Group I was dosed with 1.0ml of normal saline (negative control), Group II, III, IV, V, VI were dosed with 1000.0, 600.0, 300.0, 40.0 and 5.0 mg/kg bwt of extract respectively. Group VII was dosed 10.0 mg/kg bwt diclofenac Na. The percentage mean paw volume inhibition and percentage writhing protection were determined. Results: The mean percentage paw volume inhibitions were 29.1%, 74.2% and 32.3% at doses of 5.0, 40.0 mg/kg bwt and 10.0 mg/kg bwt diclofenac Na respectively. The mean percentage writhing protection was 8.9%, 10.4%, 78.5% and 98.7% at doses of 150.0, 600.0, 1000.0 mg/kg of extract and 10.0 mg/kg bwt diclofenac Na respectively. Conclusions: Total crude leaf extracts of P. dodecandra has analgesic and anti-inflammatory activity that may be attributed to the presence of polyphenolic, saponins and many others phytochemicals that are present in the plant.

Anti-anaphylactic and anti-inflammatory activities of a bioactive alkaloid from the root bark of Plumeria acutifolia Poir

Objective:To investigate the anti-anaphylactic,anti-inflammatory and membrane stabilizing properties of plumerianine(compound 1)isolated from the root bark of Plumeria acuifolia Poir.Methods:The anti-anaphylactic activity of compound 1(10,25 and 50 mg/kg)was studied by using models such as passive cutaneous anaphylaxis,passive paw anaphylaxis and its antiinflammatory activity against carrageenin induced paw edema and cotton pellet granuloma in albino rats was also investigated using ketotifen and indomethacin as reference drugs.Results:A dose-dependent beneficial effect was observed on leakage of evans blue dye in skin challenged with antigen and on paw anaphylaxis induced by antiserum.The compound 1 also exhibited significant(P<0.01)inhibition of rat paw edema and granuloma tissue formation,including significant protection of RBC against the haemolytic effect of hypotonic solution,an indication of membrane-stabilizing activity.Conclusions:Anti-anaphylactic activity of compound 1 may be possibly due to inhibition of the release of various inflammatory mediators.Anti-inflammatory activity of compound may be related to the inhibition of the early phase and late phase of inflammatory events.

Antipyretic,anti-inflammatory and analgesic properties of nilavembu kudineer choornam:a classical preparation used in the treatment of chikungunya fever

Objective:To investigate the efficacy of ethanolic extract of nilavembu kudineer choornam (EENKC) in inflammation,pain and fever using animal models to support its actions.Methods: Acute toxicity study of EENKC was performed in mice to fix the effective dose.The antipyretic, anti-inflammatory and analgesic activity of EENKC was evaluated in brewer’s yeast induced pyrexia in rats,carrageenan-induced inflammation in rats and acetic-acid induced writhing in mice model.Results:Acute toxicity revealed that EENKC didn’t show death and toxic signs up to 2 000 mg/kg.In brewer’s yeast induced pyrexia and carrageenan-induced inflammation EENKC at the doses of 200 and 400 mg/kg inhibited fever and inflammation significantly(P【0.01 and【0.05) compared to control animals.In mice,the number of writhing induced by acetic-acid was significantly(P【0.01) reduced after treatment with both the dose of EENKC than control animals. EENKC 200 mg/kg inhibits inflammation higher level in carrageenan-induced paw edema,but there is no significant difference when compared to indomethacin 10 mg/kg.Conclusions:The present findings revealed that EENKC possesses antipyretic,anti-inflammatory and analgesic activity which supports nilavembu kudineer choornam efficacy in chikungunya fever.

Phytochemical constituents,analgesic and anti-inflammatory effects of methanol extract of Triumfetta rhomboidea leaves in animal models

Objective:To investigate the analgesic and anti-inflammatory effects of the methanolic extract of the leaves of Triumfetta rhomboidea on mice and rats respectively.And to screen the phytochemical constituent of the extract. Methods:The analgesic effect was determined by acetic acid-induced writhing test in mice.While the anti-inflammatory activity was determined by egg albumin-induced oedema of the rat paw.Phytochemical screening was done by standard procedures.Results:Triumfetta rhomboidea leaf extract(50 -400 mg/kg) caused a statistically significant inhibition on the egg albumin-induced eodema or inflammation in Wister albino rats with P【0.001(ANOVA).This effect was higher than the observed effect with Piroxicam(0.5 mg/kg) which was used as a standard.The effect was also dose-dependent.Furthermore,Triumfetta rhomboidea extract caused a statistically significant reduction in the number of acetic acid-induced writhing in mice,with P【0.001(ANOVA).These effects were also does-dependent and greater than the analgesic effects by paracetamol which was used as a reference drug.Phytochemical screening revealed the presence of flavonoids,steroids, triterpenoids alkaloids,tannins and saponins in Truimfetta rhomboidea leaf extract.Conclusion:Triumfetta rhomboidea can be recommended for acute inflammatory disorders and diseases associated with pains.This also supports its traditional use as an anti-snake bite and anti-cancer or anti-tumor agent.Further study is on the way to find out the mechanism of its action and also to isolate,identify and characterize the active principle responsible for these effects in this plant.

Anti-inflammatory and analgesic properties of Moroccan medicinal plants:Phytochemistry,in vitro and in vivo investigations,mechanism insights,clinical evidences and perspectives

Moroccan medicinal plants exhibit several pharmacological properties such as antimicrobial,anticancer,antidiabetic,analgesic,and anti-inflammatory effects,which are related to the presence of numerous bioactive compounds,including phenolic acids,flavonoids,and terpenoids.In the present review,we systematically evaluate previously published reports on the anti-inflammatory and analgesic effects of Moroccan medicinal plants.The in vitro investigations revealed that Moroccan medicinal plants inhibit several enzymes related to inflammatory processes,whereas in vivo studies noted significant anti-inflammatory and analgesic effects as demonstrated using different experimental models.Various bioactive compounds exhibiting in vitro and in vivo anti-inflammatory and analgesic effects,with diverse mechanisms of action,have been identified.Some plants and their bioactive compounds reveal specific secondary metabolites that possess important anti-inflammatory effects in clinical investigations.Our review proposes the potential applications of Moroccan medicinal plants as sources of anti-inflammatory and analgesic agents.

Design and Synthesis of Some Enaminonitrile Derivatives of Antipyrine as Potential Novel Anti-Inflammatory and Analgesic Agents

The starting (1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)carbon-hydrazonoyl dicyanide (2) was used as a key intermediate for the syntheses of novel acyclic enaminonitriles 3-10. The newly synthesized compounds were characterized by elemental analyses and spectral data (IR, 1H NMR, 13C NMR and mass spectra). The anti-inflammatory activity data indicated that many of tested compounds protected rats from carrageenan-induced inflammation, and tested compounds 3, 4, 9 and 10 were the most potent among tested compounds. The analgesic activity was determined by the hot plate test (central analgesic activity) and acetic acid induced writhing assay. The results revealed that compounds 3, 4, 9, and 10 exhibited significant activity. However, compound 10 proved to have better or equivalent activities in comparison to the reference drug.

Antioxidant and anti-inflammatory activities of Arbutus unedo aqueous extract

Objective: To evaluate the antioxidant and anti-inflammatory activities of aqueous extract of Arbutus unedo(A. unedo) leaves.Methods: In this context, the in vitro antioxidant activity was demonstrated by 2,2-diphenyl-1-picrylhydrazyl, hydroxyl radical and H_2O_2 radical scavenging, ferrous ion chelating, ferric reducing power, total antioxidant capacity and by the protection against peroxidation of b-carotene-linoleic acid in emulsion. The anti-inflammatory activity was evaluated first by studying the membrane of human red blood cells against different hypotonic concentrations of Na Cl and against heat, inhibiting the denaturation of albumin.Results: Total phenolic and flavonoid content were found respectively [(207.84 ± 15.03)mg gallic acid equivalent/g, and(13.070 ± 0.096) mg quercetin equivalent/g]. The extract displayed significant scavenging activity of some radicals such as 2,2-diphenyl-1-picrylhydrazyl [IC_(50)at(7.956 ± 0.278) mg/m L],OH [IC_(50)=(1 015.74 ± 46.35 mg/m L)], H_2O_2[IC_(50)=(114.77 ± 16.86) mg/m L] and showed a good antioxidant activity through ferrous ion chelating activity [IC_(50)=(1 014.30 ± 36.21) mg/m L], ferric reducing power [IC_(50)=(156.55 ± 17.40) mg/m L], total antioxidant capacity [IC_(50)=(461.67± 4.16) mg/m L] and b-carotene-linoleic acid protection against peroxidation [I% =(87.04 ± 1.21)% at 1 000 mg/m L].Conclusions: A. unedo showed in vitro anti-inflammatory activity by inhibiting the heat induced albumin denaturation and red blood cells membrane stabilization. Our results show that aqueous leaf extract of A. unedo has good antioxidant activity and interesting anti-inflammatory properties. A. unedo aqueous extract can be used to prevent oxidative and inflammatory processes.