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 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.

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.

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.

Analysis of Lavandulyl Flavonoids from Sophora flavescens with Antiinflammatory Activity Based on Molecular Network Technology

[Objectives]This study was conducted to screen lavandulyl flavonoids with anti-inflammatory activity from Sophora flavescens.[Methods]35 compounds were screened from traditional Chinese medicine S.flavescens using the nitric oxide(NO)anti-inflammatory activity model.[Results]Five components,8(xanthohumol),13(kurarinol),27(4-methoxysalicylic acid),28(b-resorcic acid)and 30(b-resorcic acid),exhibited significant anti-inflammatory activity,with IC 50 values of 5.99,4.76,6.96,3.41 and 5.22μM,respectively.Especially,8(xanthohumol)and 13(kurarinol)were typical lavandulyl flavonoids in S.flavescens,which were worth further exploration.Furthermore,UPLC-Q-Exactive and GNPS molecular networking technique were used for rapid analysis of lavandulyl flavonoids from S.flavescens.A total of 15 components were identified.[Conclusions]This work lays a theoretical foundation for further separation and analysis of lavandulyl flavonoids with anti-inflammatory activity from S.flavescens.

Screening of Anti-inflammatory Active Ingredients from Gancao Qinlian Extract and Study of Its Efficacy

[Objectives]To establish the chromatographic fingerprint of Gancao Qinlian Extracts(GQE)and reveal the possible material basis of the anti-inflammatory effect of GQE by the correlation analysis between the fingerprint chromatographic peaks of different components of GQE and its anti-inflammatory activity.[Methods]Ultra-performance liquid chromatography(UPLC)was used to detect the different ingredients of GQE to establish its chromatographic fingerprint and analyze the differences among the three medicine components;LPS stimulated RAW264.7 cells to construct an inflammatory cell model.The NO secretion of cells was detected by the Griess method.ELISA was used to detect the changes in TNF-αand IL-10 contents.RT-qPCR tested the mRNA expression levels of TNF-αand IL-10.Grey relational analysis was carried out by combining fingerprint chromatographic peak data and anti-inflammatory activity data.[Results]The GQE fingerprint was established,34 fingerprint characteristic peaks were calibrated,and 33 related chromatographic peaks were screened out.The corresponding chromatographic peaks in the three components were obtained,and the content of the components was calculated;the anti-inflammatory results showed that the content of NO,TNF-α,and the expression of TNF-αmRNA in the high and medium-dose groups of GQE were significantly lower than those in the blank group(P<0.01).The NO content and TNF-αmRNA expression in the high-dose group of GQE I was considerably lower than those in the blank group(P<0.01).The secretion of NO,TNF-α,and the expression of TNF-αmRNA in the high,medium,and low dose groups of GQE II were significantly lower than those in the blank group(P<0.01);the results of grey relational analysis showed that the correlation degree of the three components was GQE II>GQE>GQE I,and the characteristic fingerprint peaks 12,15,22,23,28,31,33 may be closely related to the anti-inflammatory effect.[Conclusions]The best component of the anti-inflammatory effect in GQE is water-soluble component,and its main components are flavonoids and alkaloids.These components can alleviate cellular inflammatory damage by inhibiting the excessive secretion of NO and reducing the expression of TNF-αmRNA.

Study on the Anti-Inflammatory and Analgesic Mechanisms of Breast Lump Resolution Detergent in a Rat Model of Breast Hyperplasia

Objective: This study aimed to investigate the anti-inflammatory and analgesic mechanisms of a breast lump resolution detergent in a rat model of breast hyperplasia. Methods: A rat model of breast hyperplasia was established using injections of estradiol benzoate combined with progesterone. The effects of the breast lump resolution detergent on nipple height and diameter in the rat model were observed, along with its impact on serum levels of estradiol (E2), prolactin (PRL), and progesterone (P). Additionally, the study examined the morphological changes in breast tissue. The impact of the breast nodule detergent on blood rheology parameters was also observed. Furthermore, the anti-inflammatory effect of the breast nodule detergent was assessed using the cotton ball granuloma experiment, and the analgesic effect was observed using the writhing test. Results: The breast lump resolution detergent reduced nipple height and diameter in the rat model, decreased serum levels of E2, PRL, and P, and alleviated pathological changes in breast tissue. It also lowered hemorheological parameters including whole blood high, medium, and low shear viscosity, plasma viscosity, red blood cell hematocrit, red blood cell aggregation index, red blood cell deformability index, red blood cell electrophoresis time, and erythrocyte sedimentation rate in the acute “blood stasis” rat model. The detergent reduced the weight of cotton ball granulomas in mice and decreased the number of writhing episodes caused by acetic acid. Conclusion: The breast lump resolution detergent demonstrates favorable therapeutic effects in treating breast hyperplasia, promoting blood circulation and removing blood stasis, exerting anti-inflammatory properties, and providing analgesic effects. The downregulation of serum E2 and PRL levels and the upregulation of P levels may be critical mechanisms underlying its efficacy.

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.

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.

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.

[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.

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.

Anti-inflammatory Activity of Berbamine

Berbamine, a kind of alkaloid, was studied for anti-inflammatory activity. Thedrug was tested on carrageenan-induced rat paw oedema and kaolin-induced arthritis in rats.Berbamine has shown significant anti-inflammatory and anti-arthritic activities.

Estimation of total phenolic content,in-vitro antioxidant and anti-inflammatory activity of flowers of Moringa oleifera

Objective:To evaluate and compare the antioxidant potential and anti-inflammatory activity of ethanolic extract of flowers of Moringa oleifera(M.oleifera)grown in Oman.Methods:Flowers of M.oleiferawere collected in the month of December 2012 and identified by a botanist.Alcoholic extract of the dry pulverized flowers ofM.oleiferawere obtained by cold maceration method.The ethanolic flower extract was subjected to preliminary phytochemical screening as the reported methods.Folin-Ciocalteu reagent was used to estimate total phenolic content.DPPH was used to determinein-vitroantioxidant activity and anti-inflammatory activity of flowers was investigated by protein denaturation method.Results:Phytochemical analysis of extract showed presence of major classes of phytochemicals such as tannins,alkaloids,flavonoids,cardiac glycosidesetc.M.oleiferaflowers were found to contain 19.31 mg/g of gallic acid equivalent of total phenolics in dry extract but exhibited moderate antioxidant activity.The anti-inflammatory activity of plant extract was significant and comparable with the standard drug diclofenac sodium.Conclusions:The results of our study suggest that flowers ofM.oleiferapossess potent anti-inflammatory activity and are also a good source of natural antioxidants.Further study is needed to identify the chemical compounds responsible for their anti-inflammatory activity.

Chicken collagen hydrolysates differentially mediate anti-inflammatory activity and type I collagen synthesis on human dermal fibroblasts

Collagen is a major extracellular matrix protein.Given the potential anti-inflammatory and antioxidant profiles of these bioactive compounds,there has been increasing interest in using collagen derived peptides and peptide-rich collagen hydrolysates for skin health,due to their immunomodulatory,antioxidant and proliferative effects on dermal fibroblasts.However,all hydrolysates are not equally effective in exerting the beneficial effects;hence,further research is needed to determine the factors that improve the therapeutic applicability of such preparations.We used different enzymatic conditions to generate a number of different collagen hydrolysates with distinct peptide profiles.We found that the use of two rather than one enzyme for hydrolysis generates a greater abundance of low molecular weight peptides with consequent improvement in bioactive properties.Testing these hydrolysates on human dermal fibroblasts showed distinct actions on inflammatory changes,oxidative stress,type I collagen synthesis and cellular proliferation.Our findings suggest that different enzymatic conditions affect the peptide profile of hydrolysates and differentially regulate their biological activities and potential protective responses on dermal fibroblasts.