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.

Quasi-Static, Poiseuille Flow of Analgesics from an Elastomeric Pump: Theoretical Determination of Infusion Times and Toxicity Conditions

Background: Elastomeric pumps (elastic balls into which analgesics or antibiotics can be inserted) push medicines through a catheter to a nerve or blood vessel. Since elastomeric pumps are small and need no power source, they fit easily into a pocket during infusion, allowing patient mobility. Elastomeric pumps are widely used and widely studied experimentally, but they have well-known problems, such as maintaining reliable flow rates and avoiding toxicity or other peak-and-trough effects. Objectives: Our research objective is to develop a realistic theoretical model of an elastomeric pump, analyze its flow rates, determine its toxicity conditions, and otherwise improve its operation. We believe this is the first such theoretical model of an elastomeric pump consisting of an elastic, medicine-filled ball attached to a horizontal catheter. Method: Our method is to model the system as a quasi-Poiseuille flow driven by the pressure drop generated by the elastic sphere. We construct an engineering model of the pressure exerted by an elastic sphere and match it to a solution of the one-dimensional radial Navier-Stokes equation that describes flow through a horizontal, cylindrical tube. Results: Our results are that the model accurately reproduces flow rates obtained in clinical studies. We also discover that the flow rate has an unavoidable maximum, which we call the “toxicity bump”, when the radius of the sphere approaches its terminal, unstretched value—an effect that has been observed experimentally. Conclusions: We conclude that by choosing the properties of an elastomeric pump, the toxicity bump can be restricted to less than 10% of the earlier, relatively constant flow rate. Our model also produces a relation between the length of time that the analgesic fluid infuses and the physical properties of the fluid, of the elastomeric sphere and the tube, and of the blood vessel into which the analgesic infuses. From these, we conclude that elastomeric pumps can be designed, using our simple model, to control infusion times while avoiding toxicity effects.

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.

Biomaterials-based anti-inflammatory treatment strategies for Alzheimer's disease

The current therapeutic drugs for Alzheimer's disease only improve symptoms,they do not delay disease progression.Therefo re,there is an urgent need for new effective drugs.The underlying pathogenic factors of Alzheimer's disease are not clear,but neuroinflammation can link various hypotheses of Alzheimer's disease;hence,targeting neuroinflammation may be a new hope for Alzheimer's disease treatment.Inhibiting inflammation can restore neuronal function,promote neuro regeneration,reduce the pathological burden of Alzheimer's disease,and improve or even reverse symptoms of Alzheimer's disease.This review focuses on the relationship between inflammation and various pathological hypotheses of Alzheimer's disease;reports the mechanisms and characteristics of small-molecule drugs(e.g.,nonsteroidal anti-inflammatory drugs,neurosteroids,and plant extracts);macromolecule drugs(e.g.,peptides,proteins,and gene therapeutics);and nanocarriers(e.g.,lipid-based nanoparticles,polymeric nanoparticles,nanoemulsions,and inorganic nanoparticles)in the treatment of Alzheimer's disease.The review also makes recommendations for the prospective development of anti-inflammatory strategies based on nanocarriers for the treatment of Alzheimer's disease.

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.

Isolation and bioactivity screening of soy isoflavones from soybean glycolipids identifies daidzin as a promising anti-inflammatory agent

Background:Soybean has long been utilized in the realm of traditional Chinese medicine.One of its extracts,soybean glycolipids,serves as a vital by-product of soybean oil refining,but its chemical composition and pharmacological potential have yet to be fully elucidated.Methods:In this study,the chemical components were isolated,and the inhibitory effects of these isolates were explored in different zebrafish inflammatory models by survival rate,Histological examination assay and quantitative Real-time PCR assay.The cytotoxicity of daidzin in RAW264.7 cells was evaluated by cell viability assay,and the effect of daidzin on the release of inflammatory cytokines in RAW264.7 cells was detected by enzyme linked immunosorbent assay(ELISA).Western blotting,immunofluorescence assay and alpha7 nicotinic acetylcholine receptors siRNA transfection assay were used to further explore the anti-inflammatory mechanism of daidzin.Results:Four compounds(verticilloside,soya-cerebroside I,soya-cerebroside II and daidzin)were firstly isolated from the soybean glycolipids,among which verticilloside and daidzin inhibited the lipopolysaccharide,CuSO4-and tail cut-stimulated zebrafish inflammation.Noticeably,daidzin exhibited anti-inflammatory activities by increasing the survival rate,alleviating the inflammatory cells infiltration,and down-regulating the expression of pro-inflammatory cytokines and nuclear factor kappa-B,NF-kappa-B inhibitor alpha,and signal transducer and activator of transcription3 in zebrafish.Moreover,daidzin decreased the secretion of IL-6 and TNF-α,inhibited the nuclear translocations of nuclear factor kappa-B p65 and p-signal transducer and activator of transcription3 as well as the NF-kappa-B inhibitor alpha phosphorylation at Ser32 in RAW 264.7 cells.More importantly,it elevated the expression level of alpha7 nicotinic acetylcholine receptors in both zebrafish and RAW 264.7 cells,and the inhibitory effect of daidzin was attenuated after the addition of alpha7 nicotinic acetylcholine receptors siRNA.Conclusion:Our study revealed that daidzin inhibited inflammation by activating the cholinergic anti-inflammatory pathway and further inhibiting the nuclear factor kappa-B and signal transducer and activator of transcription3 signaling.At the same time,it also promotes the recycling of crude soybean glycolipids and supports the potential use of daidzin as a functional food or natural dietary anti-inflammatory agent.

Anti-inflammatory Mechanism of Yao Medicine Laggerae Alatae Herba

[Objectives]To study the anti-inflammatory effect of Laggerae Alatae Herba extract and its mechanism.[Methods]Inflammation models of xylene-induced ear edema in mice,acetic acid-induced increased permeability of abdominal capillaries in mice,and carrageenan-induced paw edema in mice were established;xylene-induced ear swelling model in bilateral adrenalectomized mice was established.The levels of MDA,NO and SOD in inflammatory tissues of paw were measured.[Results]Compared with the model group,the high and medium dose groups of Laggerae Alatae Herba extract had significant inhibitory effect on xylene-induced ear edema in mice,except for the low dose group(P>0.05);Laggerae Alatae Herba extract inhibited the increase of celiac capillary permeability induced by acetic acid and paw edema induced by carrageenan in mice.Compared with the model group,in the mice model with bilateral adrenal glands removed,the high and medium dose groups of Laggerae Alatae Herba extract could significantly inhibit the xylene induced ear swelling of the mice.The high and medium dose groups of Laggerae Alatae Herba extract could significantly decrease the levels of MDA and NO,and significantly increase the level of SOD in the paw tissue.[Conclusions]The Laggerae Alatae Herba extracts have anti-inflammatory activity,and the anti-inflammatory effect of the extracts does not depend on the hypothalamic-pituitary-adrenal axis(HPAA)system.In addition,the anti-inflammatory mechanism of Laggerae Alatae Herba extract is related to the decrease of MDA and NO and the increase of SOD.

Analgesic Effect of Combined Spinal-Epidural Anesthesia and its Effect on TNF-α and CRP Levels in Elderly Patients with Hip Fracture During Surgical Treatment

Objective:To observe the analgesic effect of combined spinal and epidural anesthesia on older patients undergoing hip fracture surgery.Method:One hundred and twenty elderly hip fracture surgery patients treated in our hospital from January 2021 to December 2022 were selected and randomly divided into two groups,with 60 cases in the experimental group and 60 in the control group.The experimental group was given combined spinal-epidural anesthesia intervention measures,while the control group was given epidural anesthesia intervention measures.The analgesic effect,tumor necrosis factor-alpha(TNF-α),C-reactive protein(CRP)levels,and other observation indicators were analyzed after anesthesia intervention.Result:After the intervention,the analgesic effect and the evaluation results of the subjects in the experimental group were better than those in the control group(P<0.05);the obtained values of TNF-αand CRP levels in the experimental group were higher than those of the control group(P<0.05).Conclusion:The combined spinal-epidural anesthesia intervention demonstrated positive outcomes.The analgesic effect of patients during surgery and their inflammatory factor levels improved,which makes this intervention worthy of clinical application and promotion.

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.

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.

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.

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.

Screening of Anti-inflammatory and Analgesic Parts of Ardisia gigantifolia stapf.and Its Toxicological Safety Study

[Objectives] To screen out the anti-inflammatory and analgesic parts of Ardisia gigantifolia stapf.and to explore the toxicological safety of each part.[Methods]The carrageenan-induced toe swelling experiment of mice,acetic acid-induced peritoneal capillary permeability experiment,pain writhing test,and mouse maximum tolerated dose experiment were carried out.Taking mouse toe swelling,capillary permeability,pain writhing reaction times,and animal death number as indicators,anti-inflammatory and analgesic effects were screened and toxicological safety was evaluated for petroleum ether,ethyl acetate,n-butanol and water parts of A.gigantifolia.[Results] The petroleum ether part of A.gigantifolia can significantly reduce the degree of carrageenan-induced toe swelling of(P < 0.05),significantly inhibit the glacial acetic acid induced capillary permeability of mice(P < 0.05) and the times of pain writhing of mice(P < 0.01),no death was observed in each group after 150-fold of clinical equivalent dose administration,and no abnormality was observed in body weight and tissues of mice.[Conclusions]The petroleum ether part of A.gigantifolia is active part of anti-inflammatory and analgesic effect,and each part is low in toxicological safety.

Diabetic retinopathy:Role of inflammation and potential therapies for anti-inflammation

Diabetic retinopathy is a leading cause of blindness among working-age adults.Despite many years of research,treatment options for diabetic retinopathy remain limited and with adverse effects.Discovery of new molecular entities with adequate clinical activity for diabetic retinopathy remains one of the key research priorities in ophthalmology.This review is focused on the therapeutic effects of cannabidiol(CBD),a nonpsychoactive native cannabinoid,as an emerging and novel therapeutic modality in ophthalmology based on systematic studies in animal models of inflammatory retinal diseases including diabetic retinopathy-a retinal disease associated with vascular-neuroinflammation.Special emphasis is placed on novel mechanisms which may shed light on the pharmacological activity asso c iated with CBD preclinically.These include a selfdefence system against inflammation and neurodegeneration mediated by inhibition of equilibrat ive nucleoside transporter and activation of adenosine receptor by treatment with CBD.

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.