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

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

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

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

Systematic review and network meta-analysis of different nonsteroidal anti-inflammatory drugs for juvenile idiopathic arthritis

BACKGROUND Various non-steroidal anti-inflammatory drugs(NSAIDs)have been used for juvenile idiopathic arthritis(JIA).However,the optimal method for JIA has not yet been developed.AIM To perform a systematic review and network meta-analysis to determine the optimal instructions.METHODS We searched for randomized controlled trials(RCTs)from PubMed,EMBASE,Google Scholar,CNKI,and Wanfang without restriction for publication date or language at August,2023.Any RCTs that comparing the effectiveness of NSAIDs with each other or placebo for JIA were included in this network meta-analysis.The surface under the cumulative ranking curve(SUCRA)analysis was used to rank the treatments.P value less than 0.05 was identified as statistically significant.RESULTS We included 8 RCTs(1127 patients)comparing 8 different instructions including meloxicam(0.125 qd and 0.250 qd),Celecoxib(3 mg/kg bid and 6 mg/kg bid),piroxicam,Naproxen(5.0 mg/kg/d,7.5 mg/kg/d and 12.5 mg/kg/d),inuprofen(30-40 mg/kg/d),Aspirin(60-80 mg/kg/d,75 mg/kg/d,and 55 mg/kg/d),Tolmetin(15 mg/kg/d),Rofecoxib,and placebo.There were no significant differences between any two NSAIDs regarding ACR Pedi 30 response.The SUCRA shows that celecoxib(6 mg/kg bid)ranked first(SUCRA,88.9%),rofecoxib ranked second(SUCRA,68.1%),Celecoxib(3 mg/kg bid)ranked third(SUCRA,51.0%).There were no significant differences between any two NSAIDs regarding adverse events.The SUCRA shows that placebo ranked first(SUCRA,88.2%),piroxicam ranked second(SUCRA,60.5%),rofecoxib(0.6 mg/kg qd)ranked third(SUCRA,56.1%),meloxicam(0.125 mg/kg qd)ranked fourth(SUCRA,56.1%),and rofecoxib(0.3 mg/kg qd)ranked fifth(SUCRA,56.1%).CONCLUSION In summary,celecoxib(6 mg/kg bid)was found to be the most effective NSAID for treating JIA.Rofecoxib,piroxicam,and meloxicam may be safer options,but further research is needed to confirm these findings in larger trials with higher quality studies.

Non-steroidal anti-inflammatory drugs in postoperative hand fracture management:Do they positively or negatively impact recovery?

This editorial explores the impact of non-steroidal anti-inflammatory drugs(NSAIDs)on postoperative recovery in hand fracture patients,amidst shifting pain management strategies away from opioids due to their adverse effects.With hand fractures being significantly common and postoperative pain management crucial for recovery,the potential of NSAIDs offers a non-addictive pain control alternative.However,the controversy over NSAIDs'effects on bone healing—stemming from their Cyclooxygenase-2 inhibition and associated risks of fracture non-union or delayed union—necessitates further investigation.Despite a comprehensive literature search,the study finds a lack of specific research on NSAIDs in postoperative hand fracture management,highlighting an urgent need for future studies to balance their benefits against possible risks.

Roles of Community Pharmacists in Screening and Disseminating of Information about Non-Steroidal Anti-Inflammatory Drugs Risks: Implications for Drug Safety Assessment

Background: The increasing use of non-steroidal anti-inflammatory drugs (NSAIDs) both on prescription and over the counter raises a major global health concern because of the risks associated with their use if no proper guidance is given by the health care provider. This study assessed the roles of community pharmacists in screening and disseminating information about the risks associated with NSAID use in Zambia. Methodology: This was a national cross-sectional study in which a structured self-administered questionnaire was administered to 245 registered community pharmacists in Zambia. Stata/BE, version 15.1 (Stata Corporation, College Station, Texas, USA) and multivariate logistic regression model was used to determine factors associated with information dissemination about ADRs of NS-NSAIDs. Results: 231 of the 245 distributed questionnaires were returned giving a response rate of 94.3%. All (100%) participating community pharmacists claimed to have practiced dispensing NSAIDs. However, only 26 (11.0%) and 71 (30.8%) regularly screened for risk factor of selective COX-2 NSAIDS (SC2-NSAIDS) and non-selective NSAIDS (NS-NSAIDs) respectively. Information dissemination on adverse drug reactions (ADRs) of SC2-NSAIDS was regularly provided by only 22 (9.5%) of pharmacists while that of NS-NSAIDs was regularly provided by 49 (21.2%). In the multivariate logistic regression model, being the owner of a pharmacy (AOR: 5.4, CI: 1.84 - 16.4) was significantly associated with information dissemination about ADRs of NS-NSAIDs while an hour increase in the working hours per day (AOR: 0.9, CI: 0.64 - 0.95) was associated with less likelihood of information dissemination. Conclusion: Pharmacists working in community pharmacies in Zambia did not regularly screen and disseminate information about the risks associated with NSAID use. Therefore, pharmacists should be able to screen and monitor patients at risk and be aware of the majority of risk factors while dispensing NSAIDs to minimize the associated complications.

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

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

Analgesic and anti-inflammatory activities of Passiflora foetida L.

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

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

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

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

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

A drug-loaded flexible substrate improves the performance of conformal cortical electrodes

Cortical electrodes are a powerful tool for the stimulation and/or recording of electrical activity in the nervous system.However,the inevitable wound caused by surgical implantation of electrodes presents bacterial infection and inflammatory reaction risks associated with foreign body exposure.Moreover,inflammation of the wound area can dramatically worsen in response to bacterial infection.These consequences can not only lead to the failure of cortical electrode implantation but also threaten the lives of patients.Herein,we prepared a hydrogel made of bacterial cellulose(BC),a flexible substrate for cortical electrodes,and further loaded antibiotic tetracycline(TC)and the anti-inflammatory drug dexamethasone(DEX)onto it.The encapsulated drugs can be released from the BC hydrogel and effectively inhibit the growth of Gram-negative and Gram-positive bacteria.Next,therapeutic cortical electrodes were developed by integrating the drug-loaded BC hydrogel and nine-channel serpentine arrays;these were used to record electrocorticography(ECoG)signals in a rat model.Due to the controlled release of TC and DEX from the BC hydrogel substrate,therapeutic cortical electrodes can alleviate or prevent symptoms associated with the bacterial infection and inflammation of brain tissue.This approach facilitates the development of drug delivery electrodes for resolving complications caused by implantable electrodes.

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

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

Anti-inflammatory and analgesic activities of Melanthera scandens

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

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

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

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

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

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

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

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

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

Opinion on double strategy to fight against COVID-19:Vaccination and home treatment with non-steroidal anti-inflammatory drugs

The goals of global vaccination are to control,eliminate,or eradicate infectious diseases in a sustainable way that strengthens public health systems.Although the use of vaccines is essential for the control of epidemics,the vaccines against coronavirus disease 2019(COVID-19)proved to be inadequate to end the pandemic and thus are considered incomplete.These vaccines failed to prevent infection,so their primary purpose has been shifted to prevent severe disease and reduce hospitalizations and deaths.Therefore,we believe that all the strategies available to reduce transmission,hospitalizations and deaths due to COVID-19 will be put in place.It is reported that uncontrolled inflammation and thrombosis are the principal mechanisms for aggravation and death in patients with COVID-19.Unlike corticosteroids that should not be administered at the beginning of the symptoms for their immunosuppressive action,which could worsen the evolution of the disease,the usefulness of non-steroidal anti-inflammatory drugs in the early at-home treatment of the disease is becoming evident.

A Preliminary Study on Anti-inflammatory and Analgesic Effects of Millettia speciosa and Tinpspora sinensis and Their Compatibility

[Objectives]To study the anti-inflammatory and analgesic effects of Millettia speciosa and Tinpspora sinensis and their compatibility.[Methods](i)In the glacial acetic acid writhing experiment,60 SPF-grade Kunming mice were adopted,and the mice were randomly divided into 6 groups at male-female ratio of 1∶1,namely,the blank control group,M.speciosa group,T.sinensis group,M.speciosa compatible with T.sinensis group at the ratio of 1∶2(expressed as 1∶2 compatibility group),M.speciosa compatible with T.sinensis group at the ratio of 1∶1(expressed as 1∶1 compatibility group),and M.speciosa compatible with T.sinensis group at the ratio of 2∶1(expressed as 2∶1 compatibility group),12 mice for each group.Mice of the experimental groups were administered at a dose of 20 mL/kg,and the corresponding concentration of the Chinese medicine extract was given at 1 g/mL.The control group was administered with an equal volume of 0.9%physiological saline,and was intragastrically administered once every 24 h for 14 d.After intragastric administration for one hour on day 14,intraperitoneal injection of 0.5%glacial acetic acid solution was performed to induce pain.(ii)In the hot plate experiment,60 Kunming female SPF mice were adopted,grouped,intragastrically administered with the same glacial acetic acid writhing experiment for 14 d.After intragastric administration for one hour on day 14,the mice were placed on a hot plate apparatus at(55±0.5)℃.to measure the time of licking their hind feet.(iii)In the anti-inflammatory experiment,60 Kunming SPF mice were adopted,grouped,intragastrically administered with the same glacial acetic acid writhing experiment for 14 d.After intragastric administration for one hour on day 14,xylylene was administered to the left ears of mice at a dose of 50μL/piece to induce inflammation.[Results](i)In the glacial acetic acid writhing experiment,compared with the blank control group,the experimental group showed analgesic effects.Specifically,M.speciosa group,T.sinensis group,1∶2 compatibility group,1∶1 compatibility group,2∶1 compatibility group showed significant effect(P<0.05),the writhing inhibition rate was 17.65%,20.59%,29.41%,26.47%,and 44.12%,respectively,and 2∶1 compatibility group showed the most significant analgesic effects.(ii)In the hot plate experiment,compared with the control group,all experimental groups showed analgesic effect.Specifically,M.speciosa group,T.sinensis group,1∶2 compatibility group,1∶1 compatibility group,2∶1 compatibility group showed significant effect(P<0.05),the pain threshold improvement rates were 16.13%,14.55%,14.96%,29.95%,and 58.68%,respectively,and 2∶1 compatibility group showed the most significant analgesic effect.(iii)In the anti-inflammatory experiment,the swelling degree of the 1∶2 compatibility group was significantly different from that of the blank control group,M.speciosa group,T.sinensis group(P<0.05).and 1∶2 compatibility group showed the most significant anti-inflammatory effect.[Conclusions]M.speciosa,T.sinensis,and their compatibility had anti-inflammatory and analgesic effects.The 2∶1 compatibility group had the best analgesic effects,and 1∶2 compatibility group had the best anti-inflammatory effects.

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

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

A preliminary study on the anti-inflammatory and analgesic effects of two extracts of pine pollen on anoxia and fatigue resistance

Background:To study the anti-inflammatory,analgesic,fatigue resistant and antihypoxia effects of ethanol extract and water extract of pine pollen.Methods:Two different extracts of pine pollen were prepared into there different concentrations,that is 1.5 mg·mL^-1,4.5 mg·mL^-1 and 7.5 mg·mL^-1 respectively.The extract were studied by xylene-induced ear swelling,acetic acid distortion test and hot plate test.The antihypoxia and antifatigue effects were explored by weight-bearing swimming experiment,routine pressure hypoxia tolerance experiment and liver weight coefficient comparison.Results:Through the study of the four pharmacological effects of ethanol extract and water extract,we found that the anti-inflammatory,analgesic,antithyposia and antifatigue effects of ethanol extract were better than that of water extract.Moreover,the experimental effects significantly improved with the increase of the concentration,and the effect of alcohol increased dose group was accurate(P<0.05).Conclusion:Pine pollen has excellent effects of anti-inflammatory,analgesic,antihypoxia and anti-fatigue.Besides,with the increase of drug concentration,effects tend to be more obvious with positive correlation.