A series of 2 (E) (4 hydroxy 3 methoxybenzylidene) 5 (N substituted ami nomethyl) cyclopentanones was synthesized and evaluated for the anti inflammatory activity. All of the target compounds were confirmed ...A series of 2 (E) (4 hydroxy 3 methoxybenzylidene) 5 (N substituted ami nomethyl) cyclopentanones was synthesized and evaluated for the anti inflammatory activity. All of the target compounds were confirmed by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several compounds exerted appreciable inhibitory effect on xylene induced ear edema in mice and that alteration of the substituents of anilines had significant influence in anti inflammatory potency.展开更多
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 th...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.展开更多
The present study aimed at isolating,purifying,characterizing the structure and estimating the anti-inflammatory activity of a polysaccharide named THSA which was obtained from Thamnolia subuliformis(Ehrh.) W.Culb(T.s...The present study aimed at isolating,purifying,characterizing the structure and estimating the anti-inflammatory activity of a polysaccharide named THSA which was obtained from Thamnolia subuliformis(Ehrh.) W.Culb(T.subuliformis).A newheteroglycan THSA was gained by hot water extraction and further continuously purification through Sephadex G-75 and Superdex 200 column chromatography.The structural characteristics of THSA were primarily investigated by molecular mass estimation,monosaccharide composition analysis and Fourier transforminfrared spectroscopy(FT-IR).The anti-inflammatory effects of THSA was also estimated in lipopolysaccharide(LPS)-stimulated mouse macrophages cell line RAW264.7 through the method of reverse transcription polymerase chain reaction(RT-PCR) and quantitative real-time PCR.The results indicate that THSA is composed of Glc,Gal,Man in the ratio 1:2.1:6.16,with average molecular weight of about 12.4 k Da,and significantly inhibits the mRNA expression of tumor necrosis factor alpha(TNF-α),IL-6 at100 or 1 000 μg/m L and increases the anti-inflammatory cytokine level of IL-10 at 100 μg/m L.It indicates that polysaecharide THSA has strong anti-inflammatory activity.展开更多
Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphyl...Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.展开更多
Objective:To investigate the antioxidant and anti-inflammatory activity of orally administered methanolic leaf extract of Dalbergia paniculala(D.paniculata) in Carrageenan induced inflammation in rats.Methods:In vitro...Objective:To investigate the antioxidant and anti-inflammatory activity of orally administered methanolic leaf extract of Dalbergia paniculala(D.paniculata) in Carrageenan induced inflammation in rats.Methods:In vitro antioxidant activity was evaluated for superoxide radical, Hydroxyl radical and DPPH radical scavenging activity.Three doses 200 mg/kg,400 mg/kg and 800 mg/kg of D.paniculala were tested for anti-inflammatory activity in Carrageenan induced rat paw edema model and paw thickness was measured every one hour up to 6 h. Results:The melhanolic leaf extract of D.paniculala produced dose dependent inhibition of Superoxide radical,Hydroxyl radical and OPPH radicals.In Carrageenan induced inflammation model,all three doses produced significant percentage inhibition of rat paw edema and 800 mg/kg dose produced maximum percent inhibition of rat paw edema(47.83%) at 3h compared to control group.Conclusions:In the present study we found that methanolic leaf extract of D.paniculata showed good in vitro antioxidant activity and in vivo anti-inflammatory activity in rats.展开更多
[Objectives] To compare the anti-inflammatory activities of three extraction processes of the exotic plant Bidens alba(L.) DC in Lingnan(south of the Five Ridges in China).[Methods]The alcohol extracts of B.alba(L.) D...[Objectives] To compare the anti-inflammatory activities of three extraction processes of the exotic plant Bidens alba(L.) DC in Lingnan(south of the Five Ridges in China).[Methods]The alcohol extracts of B.alba(L.) DC were extracted and separated with petroleum ether,chloroform and ethyl acetate respectively.The anti-inflammatory activity experiment of these three extracts was carried out with the RAW264.7 inflammatory model of mouse macrophages in vitro.[Results]When the concentration was 0.05-1.6 mg/L,the petroleum ether extract of B.alba(L.) DC produced strong inhibitory effects on nitric oxide(NO) release of RAW264.7 macrophages induced by LPS;the inhibition of ethyl acetate extract was weak,and the chloroform extract showed no significant inhibition.[Conclusions]Petroleum ether is the best extractant for active anti-inflammatory ingredients of B.alba(L.) DC.展开更多
Objective:To evaluate the acute toxicity and to investigate the effect of Premna corymbosa ethanolic extract(PCEE) at doses of 200 and 400 mg /kg body weight in acute and chronic models of inflammation in experimental...Objective:To evaluate the acute toxicity and to investigate the effect of Premna corymbosa ethanolic extract(PCEE) at doses of 200 and 400 mg /kg body weight in acute and chronic models of inflammation in experimental animals.Methods:In the acute toxicity study,a single dose of PCEE of 2 000 mg/kg body weight,p.o.was administered and observed for 48 h.In acute models as egg albumin induced paw edema and chronic model as cotton pellet methods was followed. Results:In acute models,egg albumin induced paw edema PCEE significantly(P【0.01) inhibited the edema formation.In chronic model,cotton pellet induced granuloma formation in rats PCEE significantly(P【0.01) reduced the granuloma formation with percentage inhibition of 35.17%and 50.38%respectively.Conclusions:The present study establishes the antiinflammatory activity of Premna corymbosa leaves.展开更多
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 analys...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.展开更多
Flavonoids exhibit a wide range of biological activities including anti-inflammatory activity, while some 1,3-benzoxazine derivatives show anti-inflammatory activity. In order to explore the novel anti-inflammatory ag...Flavonoids exhibit a wide range of biological activities including anti-inflammatory activity, while some 1,3-benzoxazine derivatives show anti-inflammatory activity. In order to explore the novel anti-inflammatory agents, based on the principles of bioisosterism and hybridization, ten novel ehromeno[8,7-e][1,3]oxazin-4-ones were syn- thesized and characterized with IR, ^1H NMR, MS and elemental analyses. The anti-inflammatory activities of the target compounds were evaluated via the croton oil-induced ear oedema test in Swiss mice. According to screened resuits, some target compounds show potent anti-inflammatory activity.展开更多
The extracts of Prunella vulgaris L. (Labiatae), a popular Western and Chinese herbal medicine, was shown to have anti-inflammatory properties, which might be due to partially, their rosmarinic acid content. Inhition ...The extracts of Prunella vulgaris L. (Labiatae), a popular Western and Chinese herbal medicine, was shown to have anti-inflammatory properties, which might be due to partially, their rosmarinic acid content. Inhition of prostaglandine E2 (PGE2) production in lipopolysaccharide (LPS) stimulated RAW264.7 mouse macrophage cells was assessed with an enzyme immunoassay (EIA) following 8-hour treatments with Prunella vulgaris extracts or fractions. Results showed that 95% ethanol extracts from P. vulgaris significantly inhibited PGE2 production. In further studies, fraction 2 from the 95% ethanol extract of P. vulgaris significantly reduced PGE2 production at 66 μg/ml (72% reduction). Cytotoxic-ity did not play a role in the noted reduction of PGE2 seen in either the extracts or fractions from P. vulgaris. High performance liquid chromatography analysis showed that there was 1.4 mM rosmarinic acid in 95% ethanol Prunella extract (201 mg/ml crude extract). Our results suggest that rosmarinic acid may contribute toward the anti-inflammatory activity of Prunella in a dose-response manner. Prunella might have a potential to be used as a functional food for anti-inflammatory activity.展开更多
Geldanamycin (1) had been isolated as a major compound from Streptomyces zerumbet W14;an endophyte of Zingiber zerumbet (L.) Smith. Two new geldanamycin derivatives;17-(tryptamine)-17-demethoxygeldanamycin (2) and 17...Geldanamycin (1) had been isolated as a major compound from Streptomyces zerumbet W14;an endophyte of Zingiber zerumbet (L.) Smith. Two new geldanamycin derivatives;17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5’-methoxytryptamine)-17-demethoxygeldanamycin (3) were synthe- sized and their anti-inflammatory activity was evaluated in LPS-induced macrophage RAW 264.7 cells by investigating their effects on the inhibition of production of NO, PGE2, TNF-α, IL-1β, IL-6 and IL-10. The data obtained were consistent with the modulation of TNF-α, IL-1β, IL-6, IL-10 production by these derivatives at concentration of 1 to 5 μg/ml. A similar effect was also observed when LPS-induced NO release and PGE2 production were tested. The inhibitory effects were shown in concentration-dependent manners. From the obtained results, it was concluded that two new gelda- namycin derivatives possess anti-inflammatory activity on LPS-induced RAW 264.7 cells. They could be useful for the management of inflammatory diseases.展开更多
Anti-inflammatory activity of a series of tri-substituted pyrimidine derivatives was predicted using two Quantitative Structure-Activity Relationship models. These relationships were developed from molecular descripto...Anti-inflammatory activity of a series of tri-substituted pyrimidine derivatives was predicted using two Quantitative Structure-Activity Relationship models. These relationships were developed from molecular descriptors calculated using the DFT quantum chemistry method using the B3LYP/6-31G(d,p) level of theory and molecular lipophilicity. Thus, the four descriptors which are the dipole moment μ<sub>D</sub>, the energy of the highest occupied molecular orbital E<sub>HOMO</sub>, the isotropic polarizability α and the ACD/logP lipophilicity were selected for this purpose. The Multiple Linear Regression (MLR) and Artificial Neural Network (ANN) models are respectively accredited with the following statistical indicators: R<sup>2</sup>=91.28%, R<sup>2</sup><sub>aj</sub>=89.11%, RMCE = 0.2831, R<sup>2</sup><sub>ext</sub>=86.50% and R<sup>2</sup>=98.22%, R<sup>2</sup><sub>aj</sub>=97.75%, RMCE = 0.1131, R<sup>2</sup><sub>ext</sub>=98.54%. The results obtained with the artificial neural network are better than those of the multiple linear regression. However, these results show that the two models developed have very good predictive performance of anti-inflammatory activity. These two models can therefore be used to predict anti-inflammatory activity of new similar pyrimidine derivatives.展开更多
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 acti...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.展开更多
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...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.展开更多
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 ant...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.展开更多
Puerarin, a major isoflavonoid derived from the Chinese medical herb radix puerariae (Gegen), has been reported to inhibit neuronal apoptosis and play an anti-inflammatory role in focal cerebral ischemia model rats....Puerarin, a major isoflavonoid derived from the Chinese medical herb radix puerariae (Gegen), has been reported to inhibit neuronal apoptosis and play an anti-inflammatory role in focal cerebral ischemia model rats. Recent findings regarding stroke pathophysiology have recognized that anti-inflammation is an important target for the treatment of ischemic stroke. The cholinergic anti-inflammatory pathway is a highly robust neural-immune mechanism for inflammation control. This study was to investigate whether activating the cholinergic anti-inflammatory pathway can be involved in the mechanism of inhibiting the inflammatory response during puerarin-induced cerebral ischemia/reperfusion in rats. Results showed that puerarin pretreatment (intravenous injection) re- duced the ischemic infarct volume, improved neurological deficit after cerebral ischemia/reperfusion and decreased the levels of interleukin-1β, interleukin-6 and tumor necrosis factor-a in brain tissue. Pretreatment with puerarin (intravenous injection) attenuated the inflammatory response in rats, which was accompanied by janus-activated kinase 2 (JAK2) and signal transducers and activators of transcription 3 (STAT3) activation and nuclear factor kappa B (NF-KB) inhibition. These observa- tions were inhibited by the alpha7 nicotinic acetylcholine receptor (a7nAchR) antagonist a-bungarotoxin (a-BGT). In addition, puerarin pretreatment increased the expression of a7nAchR mRNA in ischemic cerebral tissue. These data demonstrate that puerarin pretreatment strongly protects the brain against cerebral ischemia/reperfusion injury and inhibits the inflammatory re- sponse. Our results also indicated that the anti-inflammatory effect of puerarin may partly be medi- ated through the activation of the cholinergic anti-inflammatory pathway.展开更多
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...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.展开更多
We herein disclose a series of novel pyrrole derivatives as well as fused pyrrolopyridines 6a,b and 7a,b, pyrrolopyrazoles 8a, b, pyrrolo[2,3-d]pyrimidine derivatives 10a-d, 12a,b, 14a,b, 18a,b, 20a,b, 21a,b, 22a,b, 2...We herein disclose a series of novel pyrrole derivatives as well as fused pyrrolopyridines 6a,b and 7a,b, pyrrolopyrazoles 8a, b, pyrrolo[2,3-d]pyrimidine derivatives 10a-d, 12a,b, 14a,b, 18a,b, 20a,b, 21a,b, 22a,b, 23a,b, 24a,b, 31a,b, 36a,b, 40a,b, pyrrolo[1,2,6]thiadiazine derivatives 19a,b, pyrrolotriazolopyrimidines 25a,b, 26a,b, 27a,b and 28a,b, pyrrolo[2,3-d][1,2,3]triazine derivatives 32a,b and pyrrolo[2,3-d][1,3]oxazine derivatives 39a,b as novel compounds. All compounds were evaluated for their anti-inflammatory, analgesic (compared to the reference drug Indomethacin) and antimicrobial activities (compared to the reference drug Ampicillin and Fluconazole). Compounds 4d, 5b-d, 6a,b, 9c,d, 10d, 12ab, 13b, 19a,b, 21b, 23b, 31a,b, 38b and 40a were found to be the most active anti-inflammatory drugs exhibiting potency ranging from 1 - 1.01 compared to the reference drug indomethacin. In addition to docking study of these highly active twenty compounds against the active site of cyclooxygenase-2 enzyme (COX-2), among the tested compounds, compounds 5d, 9d, 11b, 12a, 13b and 32a showed multiple activities;anti-inflammatory, analgesic and anti-bacterial activities.展开更多
Objective:To investigate antinociceptive and anti-inflammatory activities of crude extract from Ipomoea involucrata leaves(Convolvulaceae) in mice and rats.Methods:The antinociceptive activity was tested using acetic ...Objective:To investigate antinociceptive and anti-inflammatory activities of crude extract from Ipomoea involucrata leaves(Convolvulaceae) in mice and rats.Methods:The antinociceptive activity was tested using acetic acid-induced abdominal writhing test in mice.The antiinflammatory activity was evaluated using egg albumin -induced oedema of rat paw.Results: Phytochemical screening showed the presence of alkaloids,flavonoids,saponins,terpenoids and tannin.At the doses of 25-100 mg/kg,Ipomoea involucrata exhibited dose-dependent and significant increase in pain threshold in acetic acid -induced writhing test of mice (P【0.05,student t-test) The administration of Ipomoea involucrata leaf extract(25-100 mg/ kg) showed dose-dependent decreases in paw volume of egg albumin induced oedema in rats and a significant higher anti-inflammatory activity compared to the standard control(Aspirin). Conclusions:These results support the claims on the traditional use of the of Ipomoea involucrata leaves in the treatment of toothache,rheumatic pains and other inflammatory conditions.Studies on the isolation and structural elucidation of the active principle are still needed being carried out.展开更多
Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyc...Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization.Then the reaction of substituted coumarins(a-e)with potassium O-ethyl/methyl carbonodithioate(1)by using absolute ethanol as solvent,afforded coumarin-carbonodithioate(1a-1j)derivatives under microwave irradiation and the conventional method.The spectroscopic analysis was used for the characterization of coumarin derivatives.The title(1a-1j)compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard.Drug-likeness.In-silico toxicity was predicted with LD_(50)value and bioactivity score was also calculated for all the compounds.Results:All coumarin(1a-1j)compounds exhibited promisingin-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs.All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule.It was observed that the synthesized compounds followed rule of five,indicating more'drug-like'nature.Conclusions:All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities.From the physicochemical properties of coumarin derivatives,it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five.It is concluded that the coumarin-carbonodithioate hybrids act with more'drug-like'nature.展开更多
文摘A series of 2 (E) (4 hydroxy 3 methoxybenzylidene) 5 (N substituted ami nomethyl) cyclopentanones was synthesized and evaluated for the anti inflammatory activity. All of the target compounds were confirmed by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several compounds exerted appreciable inhibitory effect on xylene induced ear edema in mice and that alteration of the substituents of anilines had significant influence in anti inflammatory potency.
基金Supported by the Department of Pharmacy,Oman Medical College,Muscat,Oman(Grant No.OMC-PHAR/425-08/12)
文摘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.
基金Fundamental Research Funds for the Central Universities,China(No.16D110523)
文摘The present study aimed at isolating,purifying,characterizing the structure and estimating the anti-inflammatory activity of a polysaccharide named THSA which was obtained from Thamnolia subuliformis(Ehrh.) W.Culb(T.subuliformis).A newheteroglycan THSA was gained by hot water extraction and further continuously purification through Sephadex G-75 and Superdex 200 column chromatography.The structural characteristics of THSA were primarily investigated by molecular mass estimation,monosaccharide composition analysis and Fourier transforminfrared spectroscopy(FT-IR).The anti-inflammatory effects of THSA was also estimated in lipopolysaccharide(LPS)-stimulated mouse macrophages cell line RAW264.7 through the method of reverse transcription polymerase chain reaction(RT-PCR) and quantitative real-time PCR.The results indicate that THSA is composed of Glc,Gal,Man in the ratio 1:2.1:6.16,with average molecular weight of about 12.4 k Da,and significantly inhibits the mRNA expression of tumor necrosis factor alpha(TNF-α),IL-6 at100 or 1 000 μg/m L and increases the anti-inflammatory cytokine level of IL-10 at 100 μg/m L.It indicates that polysaecharide THSA has strong anti-inflammatory activity.
文摘Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.
文摘Objective:To investigate the antioxidant and anti-inflammatory activity of orally administered methanolic leaf extract of Dalbergia paniculala(D.paniculata) in Carrageenan induced inflammation in rats.Methods:In vitro antioxidant activity was evaluated for superoxide radical, Hydroxyl radical and DPPH radical scavenging activity.Three doses 200 mg/kg,400 mg/kg and 800 mg/kg of D.paniculala were tested for anti-inflammatory activity in Carrageenan induced rat paw edema model and paw thickness was measured every one hour up to 6 h. Results:The melhanolic leaf extract of D.paniculala produced dose dependent inhibition of Superoxide radical,Hydroxyl radical and OPPH radicals.In Carrageenan induced inflammation model,all three doses produced significant percentage inhibition of rat paw edema and 800 mg/kg dose produced maximum percent inhibition of rat paw edema(47.83%) at 3h compared to control group.Conclusions:In the present study we found that methanolic leaf extract of D.paniculata showed good in vitro antioxidant activity and in vivo anti-inflammatory activity in rats.
基金Supported by Special Research Fund for Medical and Health of Huadu District of Guangzhou City(17-HDWS-037)Special Fund for Scientific and Technological Development of Guangdong Province(2017A020225023)President Fund of Guangdong Academy of Agricultural Sciences(201627)
文摘[Objectives] To compare the anti-inflammatory activities of three extraction processes of the exotic plant Bidens alba(L.) DC in Lingnan(south of the Five Ridges in China).[Methods]The alcohol extracts of B.alba(L.) DC were extracted and separated with petroleum ether,chloroform and ethyl acetate respectively.The anti-inflammatory activity experiment of these three extracts was carried out with the RAW264.7 inflammatory model of mouse macrophages in vitro.[Results]When the concentration was 0.05-1.6 mg/L,the petroleum ether extract of B.alba(L.) DC produced strong inhibitory effects on nitric oxide(NO) release of RAW264.7 macrophages induced by LPS;the inhibition of ethyl acetate extract was weak,and the chloroform extract showed no significant inhibition.[Conclusions]Petroleum ether is the best extractant for active anti-inflammatory ingredients of B.alba(L.) DC.
文摘Objective:To evaluate the acute toxicity and to investigate the effect of Premna corymbosa ethanolic extract(PCEE) at doses of 200 and 400 mg /kg body weight in acute and chronic models of inflammation in experimental animals.Methods:In the acute toxicity study,a single dose of PCEE of 2 000 mg/kg body weight,p.o.was administered and observed for 48 h.In acute models as egg albumin induced paw edema and chronic model as cotton pellet methods was followed. Results:In acute models,egg albumin induced paw edema PCEE significantly(P【0.01) inhibited the edema formation.In chronic model,cotton pellet induced granuloma formation in rats PCEE significantly(P【0.01) reduced the granuloma formation with percentage inhibition of 35.17%and 50.38%respectively.Conclusions:The present study establishes the antiinflammatory activity of Premna corymbosa leaves.
基金the Opening Foundation of The Biochemical Engineering Key Discipline (No.20050105) Zhejiang,China,for financial supportthe National Center for Drug Screening,Shanghai,China,for evaluation of anti-inflammatory and analgesic activity.
文摘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.
基金Supported by the National Natural Science Foundation of China(No.40724053)
文摘Flavonoids exhibit a wide range of biological activities including anti-inflammatory activity, while some 1,3-benzoxazine derivatives show anti-inflammatory activity. In order to explore the novel anti-inflammatory agents, based on the principles of bioisosterism and hybridization, ten novel ehromeno[8,7-e][1,3]oxazin-4-ones were syn- thesized and characterized with IR, ^1H NMR, MS and elemental analyses. The anti-inflammatory activities of the target compounds were evaluated via the croton oil-induced ear oedema test in Swiss mice. According to screened resuits, some target compounds show potent anti-inflammatory activity.
文摘The extracts of Prunella vulgaris L. (Labiatae), a popular Western and Chinese herbal medicine, was shown to have anti-inflammatory properties, which might be due to partially, their rosmarinic acid content. Inhition of prostaglandine E2 (PGE2) production in lipopolysaccharide (LPS) stimulated RAW264.7 mouse macrophage cells was assessed with an enzyme immunoassay (EIA) following 8-hour treatments with Prunella vulgaris extracts or fractions. Results showed that 95% ethanol extracts from P. vulgaris significantly inhibited PGE2 production. In further studies, fraction 2 from the 95% ethanol extract of P. vulgaris significantly reduced PGE2 production at 66 μg/ml (72% reduction). Cytotoxic-ity did not play a role in the noted reduction of PGE2 seen in either the extracts or fractions from P. vulgaris. High performance liquid chromatography analysis showed that there was 1.4 mM rosmarinic acid in 95% ethanol Prunella extract (201 mg/ml crude extract). Our results suggest that rosmarinic acid may contribute toward the anti-inflammatory activity of Prunella in a dose-response manner. Prunella might have a potential to be used as a functional food for anti-inflammatory activity.
文摘Geldanamycin (1) had been isolated as a major compound from Streptomyces zerumbet W14;an endophyte of Zingiber zerumbet (L.) Smith. Two new geldanamycin derivatives;17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5’-methoxytryptamine)-17-demethoxygeldanamycin (3) were synthe- sized and their anti-inflammatory activity was evaluated in LPS-induced macrophage RAW 264.7 cells by investigating their effects on the inhibition of production of NO, PGE2, TNF-α, IL-1β, IL-6 and IL-10. The data obtained were consistent with the modulation of TNF-α, IL-1β, IL-6, IL-10 production by these derivatives at concentration of 1 to 5 μg/ml. A similar effect was also observed when LPS-induced NO release and PGE2 production were tested. The inhibitory effects were shown in concentration-dependent manners. From the obtained results, it was concluded that two new gelda- namycin derivatives possess anti-inflammatory activity on LPS-induced RAW 264.7 cells. They could be useful for the management of inflammatory diseases.
文摘Anti-inflammatory activity of a series of tri-substituted pyrimidine derivatives was predicted using two Quantitative Structure-Activity Relationship models. These relationships were developed from molecular descriptors calculated using the DFT quantum chemistry method using the B3LYP/6-31G(d,p) level of theory and molecular lipophilicity. Thus, the four descriptors which are the dipole moment μ<sub>D</sub>, the energy of the highest occupied molecular orbital E<sub>HOMO</sub>, the isotropic polarizability α and the ACD/logP lipophilicity were selected for this purpose. The Multiple Linear Regression (MLR) and Artificial Neural Network (ANN) models are respectively accredited with the following statistical indicators: R<sup>2</sup>=91.28%, R<sup>2</sup><sub>aj</sub>=89.11%, RMCE = 0.2831, R<sup>2</sup><sub>ext</sub>=86.50% and R<sup>2</sup>=98.22%, R<sup>2</sup><sub>aj</sub>=97.75%, RMCE = 0.1131, R<sup>2</sup><sub>ext</sub>=98.54%. The results obtained with the artificial neural network are better than those of the multiple linear regression. However, these results show that the two models developed have very good predictive performance of anti-inflammatory activity. These two models can therefore be used to predict anti-inflammatory activity of new similar pyrimidine derivatives.
文摘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.
文摘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.
文摘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.
基金supported by the Young Scientists Foundation of Hubei Provincial Health Department,No.QJX2012-16
文摘Puerarin, a major isoflavonoid derived from the Chinese medical herb radix puerariae (Gegen), has been reported to inhibit neuronal apoptosis and play an anti-inflammatory role in focal cerebral ischemia model rats. Recent findings regarding stroke pathophysiology have recognized that anti-inflammation is an important target for the treatment of ischemic stroke. The cholinergic anti-inflammatory pathway is a highly robust neural-immune mechanism for inflammation control. This study was to investigate whether activating the cholinergic anti-inflammatory pathway can be involved in the mechanism of inhibiting the inflammatory response during puerarin-induced cerebral ischemia/reperfusion in rats. Results showed that puerarin pretreatment (intravenous injection) re- duced the ischemic infarct volume, improved neurological deficit after cerebral ischemia/reperfusion and decreased the levels of interleukin-1β, interleukin-6 and tumor necrosis factor-a in brain tissue. Pretreatment with puerarin (intravenous injection) attenuated the inflammatory response in rats, which was accompanied by janus-activated kinase 2 (JAK2) and signal transducers and activators of transcription 3 (STAT3) activation and nuclear factor kappa B (NF-KB) inhibition. These observa- tions were inhibited by the alpha7 nicotinic acetylcholine receptor (a7nAchR) antagonist a-bungarotoxin (a-BGT). In addition, puerarin pretreatment increased the expression of a7nAchR mRNA in ischemic cerebral tissue. These data demonstrate that puerarin pretreatment strongly protects the brain against cerebral ischemia/reperfusion injury and inhibits the inflammatory re- sponse. Our results also indicated that the anti-inflammatory effect of puerarin may partly be medi- ated through the activation of the cholinergic anti-inflammatory pathway.
基金Supported by University Hospital Nedir Mohamed of TiziOuzou(Grant No.cnp-um/8819-136/2014)Laboratory Analytical Biochemistry & Biotechnology Research(LABAB),Faculty of Biological Sciences and Agricultural Sciences,Mouloud Mammeri University of Tizi-Ouzou,Algeria(Grant No.bn-001375-14-993)
文摘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.
文摘We herein disclose a series of novel pyrrole derivatives as well as fused pyrrolopyridines 6a,b and 7a,b, pyrrolopyrazoles 8a, b, pyrrolo[2,3-d]pyrimidine derivatives 10a-d, 12a,b, 14a,b, 18a,b, 20a,b, 21a,b, 22a,b, 23a,b, 24a,b, 31a,b, 36a,b, 40a,b, pyrrolo[1,2,6]thiadiazine derivatives 19a,b, pyrrolotriazolopyrimidines 25a,b, 26a,b, 27a,b and 28a,b, pyrrolo[2,3-d][1,2,3]triazine derivatives 32a,b and pyrrolo[2,3-d][1,3]oxazine derivatives 39a,b as novel compounds. All compounds were evaluated for their anti-inflammatory, analgesic (compared to the reference drug Indomethacin) and antimicrobial activities (compared to the reference drug Ampicillin and Fluconazole). Compounds 4d, 5b-d, 6a,b, 9c,d, 10d, 12ab, 13b, 19a,b, 21b, 23b, 31a,b, 38b and 40a were found to be the most active anti-inflammatory drugs exhibiting potency ranging from 1 - 1.01 compared to the reference drug indomethacin. In addition to docking study of these highly active twenty compounds against the active site of cyclooxygenase-2 enzyme (COX-2), among the tested compounds, compounds 5d, 9d, 11b, 12a, 13b and 32a showed multiple activities;anti-inflammatory, analgesic and anti-bacterial activities.
文摘Objective:To investigate antinociceptive and anti-inflammatory activities of crude extract from Ipomoea involucrata leaves(Convolvulaceae) in mice and rats.Methods:The antinociceptive activity was tested using acetic acid-induced abdominal writhing test in mice.The antiinflammatory activity was evaluated using egg albumin -induced oedema of rat paw.Results: Phytochemical screening showed the presence of alkaloids,flavonoids,saponins,terpenoids and tannin.At the doses of 25-100 mg/kg,Ipomoea involucrata exhibited dose-dependent and significant increase in pain threshold in acetic acid -induced writhing test of mice (P【0.05,student t-test) The administration of Ipomoea involucrata leaf extract(25-100 mg/ kg) showed dose-dependent decreases in paw volume of egg albumin induced oedema in rats and a significant higher anti-inflammatory activity compared to the standard control(Aspirin). Conclusions:These results support the claims on the traditional use of the of Ipomoea involucrata leaves in the treatment of toothache,rheumatic pains and other inflammatory conditions.Studies on the isolation and structural elucidation of the active principle are still needed being carried out.
文摘Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization.Then the reaction of substituted coumarins(a-e)with potassium O-ethyl/methyl carbonodithioate(1)by using absolute ethanol as solvent,afforded coumarin-carbonodithioate(1a-1j)derivatives under microwave irradiation and the conventional method.The spectroscopic analysis was used for the characterization of coumarin derivatives.The title(1a-1j)compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard.Drug-likeness.In-silico toxicity was predicted with LD_(50)value and bioactivity score was also calculated for all the compounds.Results:All coumarin(1a-1j)compounds exhibited promisingin-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs.All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule.It was observed that the synthesized compounds followed rule of five,indicating more'drug-like'nature.Conclusions:All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities.From the physicochemical properties of coumarin derivatives,it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five.It is concluded that the coumarin-carbonodithioate hybrids act with more'drug-like'nature.