Toxicity is the totality of adverse effects, which can be functional and morphological lesions in a living organism, caused by a substance introduced in relatively high single doses or in small, repeated doses. The ai...Toxicity is the totality of adverse effects, which can be functional and morphological lesions in a living organism, caused by a substance introduced in relatively high single doses or in small, repeated doses. The aim of this study was to assess the OECD-recommended acute oral toxicity and anti-inflammatory activity of ethanolic extract of Ficus umbellata leaves. Animals were given a single oral dose of 1000, 3000 and 5000 mg/Kg body weight (BW) of the extract. For the anti-inflammatory activity test, rats were given the ethanolic extract of F. umbellata leaves at doses of 100, 300 and 500 mg/Kg or aspirin® at a concentration of 100 mg/Kg PC orally, one hour before injection of 0.05 ml of 1% formalin under the plantar fascia of the rat’s right hind paw. Paw volume measurements were taken one, two and three hours after formalin injection, using an electronic caliper. After 14 days of observation, no deaths were observed in treated rats. The LD50 of ethanolic extract of Ficus umbellata leaf powder is greater than 5000 mg/Kg body weight. This extract has no significant effects on hematological parameters and on the main markers of nephrotoxicity and hepatotoxicity for a single dose of less than 5000 mg/Kg PC. It reduces formalin-induced edema. Evaluation of the percentage inhibition showed that the extract had greater anti-inflammatory activity at 3 hours after the start of the experiment. However, better inhibition of inflammatory oedema of the paw of rats treated with 500 mg/Kg was observed at 5 hours after the start of the experiment, with a percentage inhibition of 69.23 ± 1.02, compared with the reference group treated with aspirin® 100 mg/Kg, which showed an inhibition of 63.50 ± 0.98. These results show that F. umbellata leaves possess anti-inflammatory activity, which would justify their use in traditional African medicine to prevent or treat inflammation.展开更多
In this editorial we comment on the article titled“Inflammatory bowel diseases patients suffer from significant low levels and barriers to physical activity:The BE-FIT-IBD study”published in a recent issue of the Wo...In this editorial we comment on the article titled“Inflammatory bowel diseases patients suffer from significant low levels and barriers to physical activity:The BE-FIT-IBD study”published in a recent issue of the World Journal of Gastroen-terology 2023;29(41):5668-5682.Inflammatory bowel diseases(IBD)are emerging as a significant global health concern as their incidence continues to rise on a global scale,with detrimental impacts on quality of life.While many advances have been made regarding the management of the disease,physical inactivity in these patients represents an underexplored issue that may hold the key for further and better understanding the ramifications of IBD.Chronic pain,fatigue,and fear of exacerbating symptoms promotes physical inactivity among IBD patients,while the lack of clear guidelines on safe exercise regimens contributes to a norm of physical inactivity.Physical activity(PA)is accepted to have a positive effect on disease outcomes and quality of life,while inactivity exacerbates comorbidities like cardiovascular disease and mental health disorders.The“BE-FIT-IBD”study,focusing on PA levels and barriers in IBD patients of Southern Italy,revealed that a significant proportion(42.9%)were physically inactive.This lack of PA is attributed to barriers such as fear of flare-ups and misconceptions about exercise exacerbating the disease.The study also highlighted the need for better communication between healthcare providers and patients regarding the benefits of PA and safe incorporation into lifestyles.Moreover,physical inactivity may also contribute to disability in IBD patients,having a great impact on employment status.Of note is the fact that IBD also comes with an important psychological burden with relevant evidence suggesting that regular PA can improve mood,reduce anxiety,and enhance mental health.The“BE-FIT-IBD”study advocated for the integration of PA into IBD management,emphasizing the bidirectional link between PA and IBD.Regular exercise can influence the course of IBD,potentially reducing symptom severity and prolonging remission periods.As such,it is mandatory that healthcare providers actively educate patients,dispel misconceptions,and tailor exercise recommendations to improve the quality of life and reduce IBD-related complications.展开更多
Inflammatory bowel disease(IBD),including Crohn’s disease and ulcerative colitis,showed a wide spectrum of intestinal and extra-intestinal manifestations,which rendered the patients physically inactive and impaired t...Inflammatory bowel disease(IBD),including Crohn’s disease and ulcerative colitis,showed a wide spectrum of intestinal and extra-intestinal manifestations,which rendered the patients physically inactive and impaired their quality of life.It has been found that physical activity is a non-pharmacological intervention that improves the quality of life for those patients.Irisin is one member of the myokines secreted by muscle contraction during exercise and could be used as an antiinflammatory biomarker in assessing the physical activity of IBD patients.In addition,experimental studies showed that exogenous irisin significantly decreased the inflammatory markers and the histological changes of the intestinal mucosa observed in experimental colitis.Furthermore,irisin produces changes in the diversity of the microbiota.Therefore,endogenous or exogenous irisin,via its anti-inflammatory effects,will improve the health of IBD patients and will limit the barriers to physical activity in patients with IBD.展开更多
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
There is considerable controversy on the role of physical activity in irritable bowel disease(IBD)since published reports are conflicting.It is well known that there is known relapse with specific treatment in IBD.Thi...There is considerable controversy on the role of physical activity in irritable bowel disease(IBD)since published reports are conflicting.It is well known that there is known relapse with specific treatment in IBD.This,in addition to onset of extraintestinal symptoms creates a need to think of alternate approaches.In this context,the current article describes the need of a multi-institutional study with standard protocol of physical activity for documenting its effect on both the primary disease and the extra alimentary manifestations.This paper also points out the possibility of using adjuvant complementary medicine such as yoga,whose effects have been documented in other diseases like irritable bowel syndrome.A third approach could be to focus on the intestinal dysbiosis in IBD and concentrate on research on restoring the microbial flora to normal,to see whether the extraintestinal symptoms are alleviated.展开更多
BACKGROUND Patients with ankylosing spondylitis(AS)frequently suffer from comorbid sleep disorders,exacerbating the burden of the disease and affecting their quality of life.AIM To investigate the clinical significanc...BACKGROUND Patients with ankylosing spondylitis(AS)frequently suffer from comorbid sleep disorders,exacerbating the burden of the disease and affecting their quality of life.AIM To investigate the clinical significance of serum inflammatory factors,health index and disease activity scores in patients with AS complicated by sleep disorders.METHODS A total of 106 AS patients with comorbid sleep disorders were included in the study.The patients were grouped into the desirable and undesirable prognosis groups in accordance with their clinical outcomes.The serum levels of inflammatory factors,including C-reactive protein,erythrocyte sedimentation rate,interleukin(IL)-6,tumour necrosis factor-αand IL-1β,were measured.Disease activity scores,such as the Bath AS functional index,Bath AS disease activity index,Bath AS metrology index and AS disease activity score,were assessed.The health index was obtained through the Short Form-36 questionnaire.RESULTS The study found significant associations amongst serum inflammatory factors,health index and disease activity scores in AS patients with comorbid sleep disorders.Positive correlations were found between serum inflammatory factors and disease activity scores,indicating the influence of heightened systemic inflammation on disease severity and functional impairment.Conversely,negative correlations were found between disease activity scores and health index parameters,highlighting the effect of disease activity on various aspects of healthrelated quality of life.Logistic regression analysis further confirmed the predictive value of these factors on patient outcomes,underscoring their potential utility in risk assessment and prognostication.CONCLUSION The findings demonstrate the intricate interplay amongst disease activity,systemic inflammation and patientreported health outcomes in AS patients complicated by sleep disorders.The results emphasise the need for comprehensive care strategies that address the diverse needs and challenges faced by these patients and underscore the potential relevance of serum inflammatory factors,health index and disease activity scores as prognostic markers in this patient population.展开更多
ACAZY is a plant formula used in traditional medicine in Burkina Faso to treat respiratory infections. After phytochemical analysis, this study evaluated extracts’ anti-inflammatory, antioxidant and antibacterial pro...ACAZY is a plant formula used in traditional medicine in Burkina Faso to treat respiratory infections. After phytochemical analysis, this study evaluated extracts’ anti-inflammatory, antioxidant and antibacterial properties from the ACAZY recipe. Three extractions, an aqueous macerate (AM), an aqueous decoction (AD) and an hydroethanolic macerate (HEM) of the ACAZY recipe powder were carried out. Phytochemical screening of the extracts was carried out using high-performance thin-layer chromatography (HPTLC) and the determination of phenolic compounds. The anti-inflammatory potential was assessed in vitro using pro-inflammatory enzyme inhibition tests. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and Ferric-reducing antioxidant power (FRAP) antioxidant properties were also determined. The antibacterial activity was evaluated on Staphylococcus aureus and Streptococcus pneumoniae strains. Phytochemical analysis revealed the presence of flavonoids, saponins, tannins, anthracenosids, sterols and triterpenes in the extracts. The extracts inhibited pro-inflammatory enzymes by more than 40% at only 100 µg/mL. The extracts also showed potent antibacterial activity with a minimum inhibitory concentration 1 mg/mL on Staphylococcus aureus and 2 mg/mL on Streptococcus pneumoniae. The extracts in the ACAZY formula have shown anti-inflammatory and antioxidant properties in vitro. The AD also showed an antibacterial activity. This justifies its use in traditional medicine to treat acute respiratory infections.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
To evaluate the anti-inflammatory intestinal effect of the ethanolic extract (EtOHE) and hexane phase (HexP) obtained from the leaves of Combretum duarteanum (Cd).METHODSInflammatory bowel disease was induced using tr...To evaluate the anti-inflammatory intestinal effect of the ethanolic extract (EtOHE) and hexane phase (HexP) obtained from the leaves of Combretum duarteanum (Cd).METHODSInflammatory bowel disease was induced using trinitrobenzenesulfonic acid in acute and relapsed ulcerative colitis in rat models. Damage scores, and biochemical, histological and immunohistochemical parameters were evaluated.RESULTSBoth Cd-EtOHE and Cd-HexP caused significant reductions in macroscopic lesion scores and ulcerative lesion areas. The vegetable samples inhibited myeloperoxidase increase, as well as pro-inflammatory cytokines TNF-α and IL-1β. Anti-inflammatory cytokine IL-10 also increased in animals treated with the tested plant samples. The anti-inflammatory intestinal effect is related to decreased expression of cyclooxygenase-2, proliferating cell nuclear antigen, and an increase in superoxide dismutase.CONCLUSIONThe data indicate anti-inflammatory intestinal activity. The effects may also involve participation of the antioxidant system and principal cytokines relating to inflammatory bowel disease.展开更多
Objective:To study detail pharmacognosy and anti-inflammatory activity of Callistemon lanceolatus(C.lanceolatus) leaf.Methods:Leaf sample was studied by organoleptic, macroscopical,microscopical,phytochemical and othe...Objective:To study detail pharmacognosy and anti-inflammatory activity of Callistemon lanceolatus(C.lanceolatus) leaf.Methods:Leaf sample was studied by organoleptic, macroscopical,microscopical,phytochemical and other WHO recommended methods for standardizations.The methanolic leaf extract of the plant was also screened for antiinflammatory activity on carrageenan-induced paw edema in rat at doses of 200 and 400 mg/kg, orally.The detail pharmacognostic study of the C.lanceolatus leaf was carried out to lay down the standards which could be useful in future experimental studies.Results:C.lanceolatus methanolic leaf extract showed significant(P<0.0S) anti-inflammatory activity at doses of 200 mg/kg and 400 mg/kg.This significant anti-inflammatory of C.lanceolatus methanolic leaf extract at the dose of 400 mg/kg was comparable with diclofenac sodium.Conchuioiis:The pharmacognostic profile of the C.lanceolatus leaf is helpful in standardization for quality,purity and sample identification.The methanolic extract at a dose of 400 mg/kg shows a significant activity in comparison with the standard drug diclofenac sodium(50 mg/kg).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
A series of imidazo[1,2-a]pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests sugges...A series of imidazo[1,2-a]pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests suggested that these compounds have antiinflammatory activities with COX-2 selectivity to some extent.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
Objective:To evaluate the anti-oxidani and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions.Methods:In vitro DPPH radical scavenging activity and lipoxygenase(LOX)...Objective:To evaluate the anti-oxidani and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions.Methods:In vitro DPPH radical scavenging activity and lipoxygenase(LOX) inhibition assays were used to evaluate the anti-oxidant and anti-inflammatory activities respectively.Methanolic extract(MEMI),successive water extract (SWMI) and ethyl acetate fraction(EMEMI),n-butanol fraction(BMEMI) and water soluble fraction (WMEMI) of methanolic extract were evaluated along with respective reference standards. Results:In in ritro DPPH radical scavenging activity,the MEMI,EMEMI and BMEMI have offered significant antioxidant activity with IC<sub>50</sub> values of 13.37.3.55 and 14.19μig/mL respectively.Gallic acid,a reference standard showed significant antioxidant activity with IC? value of 1.88 and found to be more potent compared to all the extracts and fractions.In m vitro LOX inhibition assay,the MEMI,EMEMI and BMEMI have showed significant inhibition of LOX enzyme activity with IC<sub>50</sub> values of 96.71.63.21 and 107.44μg/mL respectively.While,reference drug Indometlhacin also offered significant inhibtion against LOX enzyme activity with IC<sub>50</sub> of 57.75.Furthermore,MEMI was found to more potent than SWMI and among the fractions EMEMI was found to possess more potent antioxidant and anti-inflammatory activity.Conclusions:These findings suggest that the MEMI and F.MEMT possess potent anti-oxidani and anti-inflammatory activities in in vitro conditions.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 investigate the anti-inflammatory activity of different fractions and glutinol(isolated compound),using nitric oxide synthase and cyclooxygenase(COX) inhibition as an indication of anti-inflammatory acti...Objective: To investigate the anti-inflammatory activity of different fractions and glutinol(isolated compound),using nitric oxide synthase and cyclooxygenase(COX) inhibition as an indication of anti-inflammatory activity,Methods: Anti-inflammatory activity was evaluated using an in vitro assay determining the inhibition of the activity of pro-inflammatory enzyme model,Cyclooxygenases and inducible nitric oxide synthase are crucial enzymes involved in the pathogenesis of many chronic inflammatory conditions,Results: Sub-fraction F3.3 that was derived from n-hexane fraction of PA leaves significantly inhibited(P = 0.01) the catalytic activity of COX-2(IC50 = 0.67 μg/m L) better than isolated compound,glutinol(IC50 = 1.22 μg/m L),compound 2(CP2)(IC50 = 1.71 μg/m L) and sub-fraction F3.3.0(IC50 = 1.30 μg/m L),A similar trend was observed in investigation of the inhibition of nitric oxide synthesis in RAW 264.7 cells by F3.3,glutinol,CP2 and F3.3.0,Inducible COX-2 and inducible nitric oxide synthase are among potent signalling enzymes that exacerbate inflammation,Conclusions: Bioactive sub-fractions(F3.3 and F3.3.0) derived from the n-hexane fraction of PA had good anti-inflammatory activity,and the isolated compound,and glutinol may be useful as a template for the development of new anti-inflammatory drugs.展开更多
Objective:To screen the anti-inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti-inflammatory mechanism of some compounds based on NF-κB signaling pathway.Methods:LPS was used ...Objective:To screen the anti-inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti-inflammatory mechanism of some compounds based on NF-κB signaling pathway.Methods:LPS was used to induce RAW264.7 to establish a model of cellular inflammatory reaction.CCK-8 method was used to detect the effect of monomer compounds on the activity of RAW264.7 cells.The release of nitric oxide(NO)in the superneant was measured by Griess method,and NO inhibition rate was calculated.The anti-inflammatory activity gradient of some monomeric compounds was also measured.The effects of monomer compound 21 on the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS induced by LPS were detected by ELISA.Results:The concentration of monomer compound of Berchemia lineata(L.)DC.was 50μmol/L,and it was administered for 24 h.The results showed that anthraquinone compound No.19 had obvious drug toxicity,while other compounds had weak or no obvious drug toxicity.The concentration was 50μmol/L,and the drug was administered for 12 h.The results showed that all the monomer compounds could inhibit the release of NO to varying degrees,and the highest NO inhibition rate was over 90%,which showed obvious anti-inflammatory activity.NO inhibition rate of No.01 new skeleton compound can reach 70.81%.The results of anti-inflammatory activity gradient showed that the monomer compound of Berchemia lineata(L.)DC.could inhibit the release of NO in a dose-dependent manner.The results of ELISA showed that phenolic compound 21 could inhibit the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS in RAW264.7 cells.Conclusion:The monomer compound of Berchemia lineata(L.)DC.has a certain anti-inflammatory activity,among which flavonoids and bibenzyl components isolated from this plant for the first time may be the material basis for its anti-inflammatory activity.The simple phenolic monomer compound 21 may play an anti-inflammatory role by regulating NF-κB signaling pathway.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
文摘Toxicity is the totality of adverse effects, which can be functional and morphological lesions in a living organism, caused by a substance introduced in relatively high single doses or in small, repeated doses. The aim of this study was to assess the OECD-recommended acute oral toxicity and anti-inflammatory activity of ethanolic extract of Ficus umbellata leaves. Animals were given a single oral dose of 1000, 3000 and 5000 mg/Kg body weight (BW) of the extract. For the anti-inflammatory activity test, rats were given the ethanolic extract of F. umbellata leaves at doses of 100, 300 and 500 mg/Kg or aspirin® at a concentration of 100 mg/Kg PC orally, one hour before injection of 0.05 ml of 1% formalin under the plantar fascia of the rat’s right hind paw. Paw volume measurements were taken one, two and three hours after formalin injection, using an electronic caliper. After 14 days of observation, no deaths were observed in treated rats. The LD50 of ethanolic extract of Ficus umbellata leaf powder is greater than 5000 mg/Kg body weight. This extract has no significant effects on hematological parameters and on the main markers of nephrotoxicity and hepatotoxicity for a single dose of less than 5000 mg/Kg PC. It reduces formalin-induced edema. Evaluation of the percentage inhibition showed that the extract had greater anti-inflammatory activity at 3 hours after the start of the experiment. However, better inhibition of inflammatory oedema of the paw of rats treated with 500 mg/Kg was observed at 5 hours after the start of the experiment, with a percentage inhibition of 69.23 ± 1.02, compared with the reference group treated with aspirin® 100 mg/Kg, which showed an inhibition of 63.50 ± 0.98. These results show that F. umbellata leaves possess anti-inflammatory activity, which would justify their use in traditional African medicine to prevent or treat inflammation.
文摘In this editorial we comment on the article titled“Inflammatory bowel diseases patients suffer from significant low levels and barriers to physical activity:The BE-FIT-IBD study”published in a recent issue of the World Journal of Gastroen-terology 2023;29(41):5668-5682.Inflammatory bowel diseases(IBD)are emerging as a significant global health concern as their incidence continues to rise on a global scale,with detrimental impacts on quality of life.While many advances have been made regarding the management of the disease,physical inactivity in these patients represents an underexplored issue that may hold the key for further and better understanding the ramifications of IBD.Chronic pain,fatigue,and fear of exacerbating symptoms promotes physical inactivity among IBD patients,while the lack of clear guidelines on safe exercise regimens contributes to a norm of physical inactivity.Physical activity(PA)is accepted to have a positive effect on disease outcomes and quality of life,while inactivity exacerbates comorbidities like cardiovascular disease and mental health disorders.The“BE-FIT-IBD”study,focusing on PA levels and barriers in IBD patients of Southern Italy,revealed that a significant proportion(42.9%)were physically inactive.This lack of PA is attributed to barriers such as fear of flare-ups and misconceptions about exercise exacerbating the disease.The study also highlighted the need for better communication between healthcare providers and patients regarding the benefits of PA and safe incorporation into lifestyles.Moreover,physical inactivity may also contribute to disability in IBD patients,having a great impact on employment status.Of note is the fact that IBD also comes with an important psychological burden with relevant evidence suggesting that regular PA can improve mood,reduce anxiety,and enhance mental health.The“BE-FIT-IBD”study advocated for the integration of PA into IBD management,emphasizing the bidirectional link between PA and IBD.Regular exercise can influence the course of IBD,potentially reducing symptom severity and prolonging remission periods.As such,it is mandatory that healthcare providers actively educate patients,dispel misconceptions,and tailor exercise recommendations to improve the quality of life and reduce IBD-related complications.
文摘Inflammatory bowel disease(IBD),including Crohn’s disease and ulcerative colitis,showed a wide spectrum of intestinal and extra-intestinal manifestations,which rendered the patients physically inactive and impaired their quality of life.It has been found that physical activity is a non-pharmacological intervention that improves the quality of life for those patients.Irisin is one member of the myokines secreted by muscle contraction during exercise and could be used as an antiinflammatory biomarker in assessing the physical activity of IBD patients.In addition,experimental studies showed that exogenous irisin significantly decreased the inflammatory markers and the histological changes of the intestinal mucosa observed in experimental colitis.Furthermore,irisin produces changes in the diversity of the microbiota.Therefore,endogenous or exogenous irisin,via its anti-inflammatory effects,will improve the health of IBD patients and will limit the barriers to physical activity in patients with IBD.
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.
文摘There is considerable controversy on the role of physical activity in irritable bowel disease(IBD)since published reports are conflicting.It is well known that there is known relapse with specific treatment in IBD.This,in addition to onset of extraintestinal symptoms creates a need to think of alternate approaches.In this context,the current article describes the need of a multi-institutional study with standard protocol of physical activity for documenting its effect on both the primary disease and the extra alimentary manifestations.This paper also points out the possibility of using adjuvant complementary medicine such as yoga,whose effects have been documented in other diseases like irritable bowel syndrome.A third approach could be to focus on the intestinal dysbiosis in IBD and concentrate on research on restoring the microbial flora to normal,to see whether the extraintestinal symptoms are alleviated.
基金Supported by the Immuno Inflammatory Diseases Research Support Project,No.J202301E036.
文摘BACKGROUND Patients with ankylosing spondylitis(AS)frequently suffer from comorbid sleep disorders,exacerbating the burden of the disease and affecting their quality of life.AIM To investigate the clinical significance of serum inflammatory factors,health index and disease activity scores in patients with AS complicated by sleep disorders.METHODS A total of 106 AS patients with comorbid sleep disorders were included in the study.The patients were grouped into the desirable and undesirable prognosis groups in accordance with their clinical outcomes.The serum levels of inflammatory factors,including C-reactive protein,erythrocyte sedimentation rate,interleukin(IL)-6,tumour necrosis factor-αand IL-1β,were measured.Disease activity scores,such as the Bath AS functional index,Bath AS disease activity index,Bath AS metrology index and AS disease activity score,were assessed.The health index was obtained through the Short Form-36 questionnaire.RESULTS The study found significant associations amongst serum inflammatory factors,health index and disease activity scores in AS patients with comorbid sleep disorders.Positive correlations were found between serum inflammatory factors and disease activity scores,indicating the influence of heightened systemic inflammation on disease severity and functional impairment.Conversely,negative correlations were found between disease activity scores and health index parameters,highlighting the effect of disease activity on various aspects of healthrelated quality of life.Logistic regression analysis further confirmed the predictive value of these factors on patient outcomes,underscoring their potential utility in risk assessment and prognostication.CONCLUSION The findings demonstrate the intricate interplay amongst disease activity,systemic inflammation and patientreported health outcomes in AS patients complicated by sleep disorders.The results emphasise the need for comprehensive care strategies that address the diverse needs and challenges faced by these patients and underscore the potential relevance of serum inflammatory factors,health index and disease activity scores as prognostic markers in this patient population.
文摘ACAZY is a plant formula used in traditional medicine in Burkina Faso to treat respiratory infections. After phytochemical analysis, this study evaluated extracts’ anti-inflammatory, antioxidant and antibacterial properties from the ACAZY recipe. Three extractions, an aqueous macerate (AM), an aqueous decoction (AD) and an hydroethanolic macerate (HEM) of the ACAZY recipe powder were carried out. Phytochemical screening of the extracts was carried out using high-performance thin-layer chromatography (HPTLC) and the determination of phenolic compounds. The anti-inflammatory potential was assessed in vitro using pro-inflammatory enzyme inhibition tests. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and Ferric-reducing antioxidant power (FRAP) antioxidant properties were also determined. The antibacterial activity was evaluated on Staphylococcus aureus and Streptococcus pneumoniae strains. Phytochemical analysis revealed the presence of flavonoids, saponins, tannins, anthracenosids, sterols and triterpenes in the extracts. The extracts inhibited pro-inflammatory enzymes by more than 40% at only 100 µg/mL. The extracts also showed potent antibacterial activity with a minimum inhibitory concentration 1 mg/mL on Staphylococcus aureus and 2 mg/mL on Streptococcus pneumoniae. The extracts in the ACAZY formula have shown anti-inflammatory and antioxidant properties in vitro. The AD also showed an antibacterial activity. This justifies its use in traditional medicine to treat acute respiratory infections.
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.
文摘To evaluate the anti-inflammatory intestinal effect of the ethanolic extract (EtOHE) and hexane phase (HexP) obtained from the leaves of Combretum duarteanum (Cd).METHODSInflammatory bowel disease was induced using trinitrobenzenesulfonic acid in acute and relapsed ulcerative colitis in rat models. Damage scores, and biochemical, histological and immunohistochemical parameters were evaluated.RESULTSBoth Cd-EtOHE and Cd-HexP caused significant reductions in macroscopic lesion scores and ulcerative lesion areas. The vegetable samples inhibited myeloperoxidase increase, as well as pro-inflammatory cytokines TNF-α and IL-1β. Anti-inflammatory cytokine IL-10 also increased in animals treated with the tested plant samples. The anti-inflammatory intestinal effect is related to decreased expression of cyclooxygenase-2, proliferating cell nuclear antigen, and an increase in superoxide dismutase.CONCLUSIONThe data indicate anti-inflammatory intestinal activity. The effects may also involve participation of the antioxidant system and principal cytokines relating to inflammatory bowel disease.
基金Supported by a grant from AICTE.New Delhi(No.1-51/RID/CA/4/2009-10)
文摘Objective:To study detail pharmacognosy and anti-inflammatory activity of Callistemon lanceolatus(C.lanceolatus) leaf.Methods:Leaf sample was studied by organoleptic, macroscopical,microscopical,phytochemical and other WHO recommended methods for standardizations.The methanolic leaf extract of the plant was also screened for antiinflammatory activity on carrageenan-induced paw edema in rat at doses of 200 and 400 mg/kg, orally.The detail pharmacognostic study of the C.lanceolatus leaf was carried out to lay down the standards which could be useful in future experimental studies.Results:C.lanceolatus methanolic leaf extract showed significant(P<0.0S) anti-inflammatory activity at doses of 200 mg/kg and 400 mg/kg.This significant anti-inflammatory of C.lanceolatus methanolic leaf extract at the dose of 400 mg/kg was comparable with diclofenac sodium.Conchuioiis:The pharmacognostic profile of the C.lanceolatus leaf is helpful in standardization for quality,purity and sample identification.The methanolic extract at a dose of 400 mg/kg shows a significant activity in comparison with the standard drug diclofenac sodium(50 mg/kg).
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.
基金This research was supported by the National Natural Science Foundation of China (No.30472083).
文摘A series of imidazo[1,2-a]pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests suggested that these compounds have antiinflammatory activities with COX-2 selectivity to some extent.
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.
文摘Objective:To evaluate the anti-oxidani and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions.Methods:In vitro DPPH radical scavenging activity and lipoxygenase(LOX) inhibition assays were used to evaluate the anti-oxidant and anti-inflammatory activities respectively.Methanolic extract(MEMI),successive water extract (SWMI) and ethyl acetate fraction(EMEMI),n-butanol fraction(BMEMI) and water soluble fraction (WMEMI) of methanolic extract were evaluated along with respective reference standards. Results:In in ritro DPPH radical scavenging activity,the MEMI,EMEMI and BMEMI have offered significant antioxidant activity with IC<sub>50</sub> values of 13.37.3.55 and 14.19μig/mL respectively.Gallic acid,a reference standard showed significant antioxidant activity with IC? value of 1.88 and found to be more potent compared to all the extracts and fractions.In m vitro LOX inhibition assay,the MEMI,EMEMI and BMEMI have showed significant inhibition of LOX enzyme activity with IC<sub>50</sub> values of 96.71.63.21 and 107.44μg/mL respectively.While,reference drug Indometlhacin also offered significant inhibtion against LOX enzyme activity with IC<sub>50</sub> of 57.75.Furthermore,MEMI was found to more potent than SWMI and among the fractions EMEMI was found to possess more potent antioxidant and anti-inflammatory activity.Conclusions:These findings suggest that the MEMI and F.MEMT possess potent anti-oxidani and anti-inflammatory activities in in vitro conditions.
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.
基金financially supported by the National Research Foundation of South Africa(NO.Eloff IPPR 953991)
文摘Objective: To investigate the anti-inflammatory activity of different fractions and glutinol(isolated compound),using nitric oxide synthase and cyclooxygenase(COX) inhibition as an indication of anti-inflammatory activity,Methods: Anti-inflammatory activity was evaluated using an in vitro assay determining the inhibition of the activity of pro-inflammatory enzyme model,Cyclooxygenases and inducible nitric oxide synthase are crucial enzymes involved in the pathogenesis of many chronic inflammatory conditions,Results: Sub-fraction F3.3 that was derived from n-hexane fraction of PA leaves significantly inhibited(P = 0.01) the catalytic activity of COX-2(IC50 = 0.67 μg/m L) better than isolated compound,glutinol(IC50 = 1.22 μg/m L),compound 2(CP2)(IC50 = 1.71 μg/m L) and sub-fraction F3.3.0(IC50 = 1.30 μg/m L),A similar trend was observed in investigation of the inhibition of nitric oxide synthesis in RAW 264.7 cells by F3.3,glutinol,CP2 and F3.3.0,Inducible COX-2 and inducible nitric oxide synthase are among potent signalling enzymes that exacerbate inflammation,Conclusions: Bioactive sub-fractions(F3.3 and F3.3.0) derived from the n-hexane fraction of PA had good anti-inflammatory activity,and the isolated compound,and glutinol may be useful as a template for the development of new anti-inflammatory drugs.
基金This study was supported by National Key Research and Development Program(No.2022YFC3502201)National Natural Science Foundation of China(No.81960762)+3 种基金Guangxi Key Discipline of Traditional Chinese Medicine(No.GZXK-Z-20-62)Guangxi Science and Technology Base and Talent Special Project(No.Guike AD19245183,AD22035052)Guangxi Demonstration Base of External Treatment of Traditional Chinese Medicine(No.14,2019)National Famous TCM Inheritance Studio,National Famous Old TCM Expert Inheritance Studio Construction Project,National Famous TCM Huang Hanru Academic Thinking and Clinical Experience Inheritance and Promotion Center(No.2022V004)。
文摘Objective:To screen the anti-inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti-inflammatory mechanism of some compounds based on NF-κB signaling pathway.Methods:LPS was used to induce RAW264.7 to establish a model of cellular inflammatory reaction.CCK-8 method was used to detect the effect of monomer compounds on the activity of RAW264.7 cells.The release of nitric oxide(NO)in the superneant was measured by Griess method,and NO inhibition rate was calculated.The anti-inflammatory activity gradient of some monomeric compounds was also measured.The effects of monomer compound 21 on the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS induced by LPS were detected by ELISA.Results:The concentration of monomer compound of Berchemia lineata(L.)DC.was 50μmol/L,and it was administered for 24 h.The results showed that anthraquinone compound No.19 had obvious drug toxicity,while other compounds had weak or no obvious drug toxicity.The concentration was 50μmol/L,and the drug was administered for 12 h.The results showed that all the monomer compounds could inhibit the release of NO to varying degrees,and the highest NO inhibition rate was over 90%,which showed obvious anti-inflammatory activity.NO inhibition rate of No.01 new skeleton compound can reach 70.81%.The results of anti-inflammatory activity gradient showed that the monomer compound of Berchemia lineata(L.)DC.could inhibit the release of NO in a dose-dependent manner.The results of ELISA showed that phenolic compound 21 could inhibit the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS in RAW264.7 cells.Conclusion:The monomer compound of Berchemia lineata(L.)DC.has a certain anti-inflammatory activity,among which flavonoids and bibenzyl components isolated from this plant for the first time may be the material basis for its anti-inflammatory activity.The simple phenolic monomer compound 21 may play an anti-inflammatory role by regulating NF-κB signaling pathway.
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.