Xylene-induced Ear Edema Test Research Articles

Research on the effects of processing Heishunpian from Aconiti lateralis radix on components and efficacy using the “step knockout” strategy

Heishunpian is obtained through complex processing of Aconiti lateralis radix praeparata. However, the impact of each processing step on chemical compositions and pharmacological activities is still unclear. The mechanism of the processing needs to be further studied. The samples were all prepared using the “step knockout” strategy for UPLC-QTOF-MS analysis, and analgesic and anti-inflammatory efficacy evaluation. Each sample was analyzed by UPLC-QTOF-MS to determine the component differences. The hot plate test and acetic acid writhing test were used to evaluate the analgesic effect. Anti-inflammatory efficacy was evaluated by xylene-induced ear edema test. The correlation between components and efficacies was studied to screen the effective components for further investigating the processing of Heishunpian. Mass spectrum analysis results showed that 49 components were identified, and it appeared that brine immersion and rinsing had a great influence on the components. In the hot plate test, ibuprofen and Heishunpian had the most significant effect, while ibuprofen and the sample without rinsing showed the best efficacy for the acetic acid writhing test. The sample without dyeing had the best effect on ear edema. The correlation analysis indicated that mesaconine, aconine, 3-deoxyaconine, delbruine, and asperglaucide were potentially considered effective analgesic components. It is not recommended to remove brine immersion and rinsing. Boiling and steaming are necessary processes that improve efficacy. Dyeing, which does not have a significant impact on components and efficacy, may be an unnecessary process. This research has been of great significance in identifying anti-inflammatory and analgesic components and optimizing processing for Heishunpian.

Anti-inflammatory and Antinociceptive Activity of Terminalia avicennioides Guill. & Perr. Stem Bark Extract is Distinct from the Antioxidant Effect Mediated by Its Phenolic-rich Fraction

Background: Terminalia avicennioides stem bark has been used in the management of pain and inflammatory disorders in northern Nigeria. This study evaluated the antinociceptive and anti-inflammatory properties of T. avicennioides stem bark extract and its fractions. The correlation of these effects to the presence and concentration of phenolics was also ascertained.
 Study Design: Experimental Design.
 Place and Duration of Study: Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, Idu, Abuja, Nigeria. The study was conducted from October to December 2022.
 Methods: A 70%v/v ethanol extract of T. avicennioides stem bark was prepared. Aqueous and ethyl acetate fractions (AF, EF) and sub-fractions (EF1 – EF4) were also prepared. The antioxidant capacity of the extract and fractions were determined using DPPH radical scavenging test, while xylene-induced topical ear edema and formalin test were used to assess antinociceptive and anti-inflammatory activity. The ethyl acetate sub-fractions were further assessed using the egg albumin–induced inflammation. The extract and fractions were characterized by High-Performance Liquid Chromatography (HPLC), and phenolic content was quantified as gallic acid equivalent (GAE)/mg of extract or fraction.
 Results: The ethyl acetate and aqueous fractions showed higher antioxidant capacity compared to the parent ethanol extract. T. avicennioides ethanol extract significantly inhibited pain (p<0.001) and inflammatory responses (p<0.05) and these effects were more significant compared to those produced by the fractions. Fractions AF and EF exhibited similar activity, although EF produced better inhibition of pain and topical edema. The subfraction EF2 also showed anti-inflammatory activity but this effect was insignificant (p>0.05). The HPLC profiles of the extract and fractions showed peaks corresponding to caffeic acid, chlorogenic acid, and gallic acid. The EF and AF revealed higher peak areas corresponding to gallic acid and rutin respectively. This correlated with a comparatively high gallic acid content and antioxidant effect of the ethyl acetate fraction (GAE: 1.32/mg, IC50 = 0.036 mg/ml), relative to the extract (GAE: 0.88/mg, IC50 = 0.052 mg/ml).
 Conclusion: The constituents responsible for the antinociceptive and anti-inflammatory activity of T. avicennioides extract appear distinct from antioxidative principles in phenolics-rich fractions.

Toxicity and Anti-Inflammatory Effects of Agave sisalana Extract Derived from Agroindustrial Residue.

In several countries, the leaf juice of Agave sisalana (also known as sisal) is widely used topically, especially as an antiseptic, and orally for the treatment of different pathologies. However, in Brazil, which is the largest producer of Agave sisalana, its residue, which represents the majority of its weight, has been thrown away. For this reason, the determination of the pharmacological and toxicological potentials of sisal residue and its possible therapeutic use is seen as a way to contribute to the sustainable development and social promotion of the largest producer of sisal in Brazil, the interior of Bahia State, which is among the poorest areas in the country. Given the scarcity of available scientific studies on the pharmacological and toxicological properties of sisal residue juice, this study aimed to promote the acid hydrolysis of this juice to potentiate the anti-inflammatory effect already described in the literature. Furthermore, it aimed to evaluate the toxicological profile of the hydrolyzed extract (EAH) and to determine its acute toxicity, as well as its side effects on the reproductive aspects of rats. The anti-inflammatory effect of EAH was evaluated in vitro using the induction of hemolysis by hypotonic solution and in vivo in rats using the carrageenan-induced paw edema test and the xylene-induced ear edema test. The acute toxicity, resulting from a single-dose administration, was investigated for some manifestation of toxic symptoms related to motor control and consciousness in rats. At a concentration of 100 mg/kg, by repeated doses, the reproductive toxicity effects of EAH in rats were assessed. In vitro anti-inflammatory activity was positive using the human red blood cell membrane stabilization method. In both in vivo tests used to assess the anti-inflammatory activity, EAH (at three doses) significantly inhibited edema when compared to the control group. At a dose of 50 mg/kg, EAH exhibited a greater effect than indomethacin, a nonsteroidal anti-inflammatory drug with known activity. In vivo toxicological studies have shown that EAH does not present toxic effects when administered orally in a single dose, up to 1000 mg/kg. Finally, EAH promoted a gonadotoxic effect and increased the embryonic mortality rate after implantation. It is suggested that the anti-edematogenic effect of the acid hydrolysis extract from sisal juice is due to the high concentration of steroidal sapogenins. Therefore, this extract can be considered a potential new anti-inflammatory or even an important sapogenin source for the development of steroidal glucocorticoids. However, further studies are needed to elucidate the chemical composition of sisal juice. Regarding toxicology studies, EAH did not show cytotoxic and clastogenic potentials, but it presented a powerful reproductive toxic effect in rats.

Evaluation of Wound Healing and Anti-Inflammatory Activities of 80% Methanol Crude Extract and Solvent Fractions of Trichilia dregeana Sond (Meliaceae) Leaves in Mice.

The leaves of Trichilia dregeana Sond are traditionally used to treat wounds. Even though there have been in vitro studies and claims supporting wound healing, there are no scientific data on in vivo wound healing and anti-inflammatory activities of the leaves of T. dregeana. This study aimed to evaluate wound healing and anti-inflammatory activity of 80% methanol crude extract and solvent fractions of T. dregeana in mice. The leaves of T. dregeana were dried, ground, and macerated with 80% methanol three times successively. The crude extract was fractioned by water, ethyl acetate, and hexane separately. The acute dermal and oral toxicity tests were done by applying 2000 mg/kg of 10% (w/w) crude extract ointment (CEO) topically and 2000 mg/kg of crude extract orally, respectively. The wound healing activity of the crude extract was evaluated on excision, incision, and burn wound models while the fractions were evaluated only on excision wound model. The anti-inflammatory activity of the crude extract was evaluated on xylene-induced ear edema and cotton pellet granuloma tests. Both acute dermal and oral toxicity tests were found to be safe after topical application of 2000 mg/kg of 10% (w/w) CEO and oral administration of 2000 mg/kg of crude extract suspension, respectively. Both 5% and 10% (w/w) CEO produced significant (p < 0.001) wound contraction and period of epithelialization from day 4 onwards as compared to simple ointment (SO) on both excision and burn wounds. The tensile strength was increased significantly (p < 0.001) for the CEO-treated mice as compared to both untreated and SO groups. The crude extract also showed anti-inflammatory activity at 100, 200, and 400 mg/kg by inhibiting ear edema, exudate, and granuloma formation as compared to the SO group. The increase in wound contraction, reduction in period of epithelialization, and increase in tensile strength support the traditional claims of T. dregeana for wound healing.

Phytochemical Screening and Pharmacological Evaluation of the Methanolic Extract of Cissus Elongata Roxb. Leaves

This study evaluates the pharmacological activity of the methanolic extract of Cissus elongata Roxb. leaves. Dried leaves of C. elongata were extracted with methanol. The crude extract was then tested to identify the presence of different phytoconstituents. To evaluate the pharmacological effects of this plant- analgesic, anti-diarrheal, anti-inflammatory and antipyretic, tests were conducted using animal models. Analgesic activity was evaluated by an acetic acid-induced writhing test, formalin-induced paw-licking test paw-licking immersion test. Castor oil-induced anti-diarrheal test was performed to evaluate anti-diarrheal activity. Xylene-induced ear edema and brewer’s yeast-induced pyrexia test were performed to investigate anti-inflammatory and antipyretic activity respectively. Phytochemical screening revealed the presence of carbohydrates, tannins, fat, and fixed oil. In writhing test, the extract showed 45.68±3.99 % and 52.28±1.67 % inhibition of writhing at a dose of 200 mg/kg and 400 mg/kg respectively whereas it was 73.09±1.01 % for the standard drug compared to the control group. In the formalin-induced paw-licking test, the percentage inhibition of licking by both doses of the extract was more in the delayed phase than in the acute phase. In the tail immersion test, 200 mg/kg dose didn’t show a significant effect but 40 0mg/kg showed significant (*P&lt;0.05 vs. control) analgesic activity at 30 min, 60 min and 120 min time periods. In an anti-diarrheal study, 400 mg/kg dose showed (68.42±0.87 % inhibition of diarrhea) almost similar anti-diarrheal effect as the standard drug loperamide HCl (71.05±0.58 %). In xylene induced ear edema test, both doses of the extract showed little anti-inflammatory effect compared to the standard drug but both doses showed significant (*P&lt;0.05 vs. control) reduction in body temperature in the antipyretic study.

Antinociceptive and Anti-Inflammatory Like Effects of Berberis baluchistanica.

Numerous therapeutic agents are in clinical practice for the treatment of inflammatory and painful conditions, but their applications have been challenged by various side /toxic effects. Therefore, new effective and safe therapies are most warrant, for which medicinal plant could be a significant alternative. Berberis baluchistanica has traditionally been used as analgesic and anti-inflammatory without any scientific background. The current study was designed to evaluate the analgesic and anti-inflammatory like effects of extract B. baluchistanica in animal models. For the study of antinociceptive effect, an extractof B. baluchistanica (100, 200 and 300 mg/kg i.p.), was tested in acetic acid-induced writhing and formalin tests. While for the anti-inflammatory action, carrageenan-induced paw edema, cotton pellet induced granuloma and xylene induced ear edema tests were used. The results showed the significant dose-dependent antinociceptive effect of extract of B. baluchistanica in acetic acid-induced writhing and formalin-induced flinching behavior tests. However, the effect was strongly antagonized by the injection of naloxone, suggesting the expression via opioidergic receptors. Similarly, strong anti-inflammatory action was illustrated in carrageenan- induced paw edema, cotton pellet induced granuloma and xylene induced ear edema tests and thus provided evidence for the versatile phytochemical nature of its phytochemical. In short, it is concluded that the extract of B. baluchistanica exhibited significant antinociceptive and anti-inflammatory effects in animal models. Further detailed studies on the efficacy and safety as well as on the phytochemical investigation are required to ascertain its clinical uses.

Quantitative screening of phytochemicals and pharmacological attributions of the leaves and stem barks of Macropanax dispermus (Araliaceae) in treating the inflammation and arthritis

Introduction: Inflammation is a major cause of arthritis. Since the conventional medicines used for the treatment of this disease have many side effects, herbal remedies can be proved to be effective in this case. So, the present study was aimed at investigating the quantitative detection of phytochemicals, screening of in vivo anti-inflammatory and the possible anti-arthritic activities of the crude methanol extracts of a traditional medicinal plant Macropanax dispermus leaves (MDML) and stem barks (MDMS). Methods: Quantitative screening of phytochemical constituents was analyzed by standard procedures. The in vivo anti-inflammatory activity was conducted on Swiss albino mice by using carrageenan and formalin-induced paw edema tests, and xylene-induced ear edema test. The possible anti-arthritic activity was done by evaluating the in vitro inhibition of bovine serum albumin (BSA) denaturation. Results: The current research showed that MDML contained a considerable amount of flavonoids and alkaloids, and MDMS contained a considerable amount of phenols. MDMS (200, 400 mg/kg) was observed to be an effective and significant (P &lt; 0.001) peripheral anti-inflammatory agent in carrageenan and formalin-induced paw edema tests, whereas MDML (400 mg/kg) was observed to have an effective and significant (P &lt; 0.001) neurogenic anti-inflammatory effect in xylene-induced ear edema test as compared to the negative control group. MDMS was observed to be an effective anti-arthritic agent as compared to that of the negative control group. All those effects were dose and concentration-dependent.Conclusion: The present research proved that MDML and MDMS were effective medications for the treatment of inflammation and arthritis.

Scrophularia Tenuipes Coss and Durieu: Phytochemical Composition and Biological Activities.

Scrophularia tenuipes is an Algerian-Tunisian endemic species, which has not been studied yet. Ethyl acetate (EA) and n-butanol (Bu) fractions obtained from Scrophularia tenuipes were investigated for their health benefit properties, in particular with respect to in vivo/in vitro anti-inflammatory and antioxidant activities, as well as their potential to inhibit key enzymes with impact in diabetes (α-glucosidase and α-amylase). The fractions had a distinct phytochemical composition, of which EA was richer in total phenolic compounds (225 mg GAE/g) and mostly composed of the phenylethanoid acetyl martynoside. Compared to EA, Bu had higher amounts of total flavonoids, and according to the result obtained from UHPLC-DAD-ESI-MSn analysis, harpagoside (iridoid) was its major phytochemical. EA fraction was quite promising with regard to the in vivo (at 200 mg/kg, po) anti-inflammatory effect (62% and 52% for carrageenan-induced rat paw edema and xylene-induced ear edema tests, respectively), while Bu fraction exhibited a stronger antioxidant capacity in all tests (IC50 = 68 µg/mL, IC50 = 18 µg/mL, IC50 = 18 µg/mL and A0.50 = 43 µg/mL for DPPH●, ABTS•+, O2•− scavenging assays and cupric-reducing antioxidant capacity method, respectively). Both fractions also showed a strong effect against α-amylase enzyme (IC50 = 8 µg/mL and 10 µg/mL for EA and Bu fraction, respectively).

Anti-inflammatory effect and chemical constituents of Microcos paniculata total flavone glycosides fraction

Microcos paniculata is an edible and medicinal plant in Lingnan, China. The present study investigated the anti-inflammatory effect and chemical constituents of its’ total flavone glycosides (MpTFG) fraction. MpTFG (10, 15, 20 μg/mL) was applied to 1 μg/mL LPS-induced RAW 264.7 macrophages in vitro; and MpTFG (10, 20, 40 mg/kg body weight) was employed to xylene-induced ear edema test. As a result, 20 μg/mL MpTFG decreased the levels of pro-inflammatory cytokines IL-6, IL-1β and TNF-α in LPS-stimulated RAW 264.7 cells supernatant significantly, and 40 mg/kg MpTFG could effectively ameliorate xylene-induced mice ear swelling. The results showed that MpTFG had potential anti-inflammatory effect. Meanwhile, ten compounds were purified by making use of macro-porous resin, sephadex LH-20 gel column chromatography and semi-preparation HPLC successively. They were characterized to be vicenin-2 (i), isoschaftoside (ii), schaftoside (iii), vitexin (iv), vicenin-1 (v), isovitexin (vi), isoviolanthin (vii), nicotiflorin (viii), astragalin (ix), narcissoside (x) by 1H-NMR, 13C-NMR and HRMS spectral analysis.

Anti-Inflammatory and Antinociceptive Activities of the Ethanolic Extract of Propolis in Male Mice and Rats

Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are usually used to alleviate pain and Inflammation. The widespread use of NSAIDs has caused the risk and side effects of these drugs commonly increase. Objectives: This study aimed to examine the anti-inflammatory and antinociceptive activities of ethanolic extract of propolis (EEP) in male mice and rats. Methods: In this experimental study, EEP was prepared and administered in doses of 100, 200, and 400 mg/kg of body weight. The anti-inflammatory potential was assessed by inflammatory models of xylene-induced ear edema and cotton pellet granuloma tests, whereas the antinociceptive potential was assessed by formalin and acetic acid-induced writhing methods. Results: The EEP at doses of 100 (P < 0.05), 200 (P < 0.001) and 400 mg/kg (P < 0.001) significantly diminished the foundation of edema caused by xylene. A significant decrease was seen in granuloma weight in EEP at doses of 200 (P < 0.001) and 400 mg/kg (P < 0.001). The extract caused a significant decrease in licking time at first phase in EEP at 100 (P < 0.01), 200 (P < 0.001), and 400 mg/kg (P < 0.001). A significant decrease was observed (P < 0.001) in licking time at the second phase in EEP at doses of 100, 200, and 400 mg/kg. In the writhing model, a significant decrease was observed in the number of writhes in EEP at doses of 100 (P < 0.05), 200 (P < 0.001), and 400 mg/kg (P < 0.001). Conclusions: The findings of this research showed that the ethanolic extract of propolis has considerable anti-inflammatory and antinociceptive activities.

Anti-inflammatory, antinociceptive and antidiarrhoeal activities of methanol and ethyl acetate extract of Hemigraphis alternata leaves in mice

BackgroundThe study was designed to investigate the qualitative phytochemical constituents and evaluate the anti-inflammatory, anti-nociceptive and anti-diarrhoeal activities of methanol (MHAL) and ethyl acetate (EAHAL) extract of Hemigraphis alternata leaves in Swiss albino mice.MethodsQualitative phytochemical constituents of MHAL and EAHAL were determined by different tests such as Molisch’s test, Fehling test, Mayer’s test, Frothing test, FeCl3 test, Alkali test, Salkowski’s test, Keller-killiani test and CuSO4 test. In addition, Xylene induced-ear edema test and Cotton pellet-induced granuloma formation test had been performed to evaluate the anti-inflammatory activity. Moreover, Formalin-induced paw licking test, Acetic acid-induced writhing tests and Castor oil induced antidiarrheal test had been performed to evaluate the anti-nociceptive and anti-diarrhoeal activities respectively.ResultsThese crude extracts were figured the presence of carbohydrates, flavonoids, tannins, glycosides, triterpenoids, fat and fixed oils. No mortality, behavioral changes or sign of any toxicity were observed up to the dose as high as 4000 mg/kg in mice. During anti-inflammatory test, MHAL 400 mg/kg and EAHAL 200 mg/kg & 400 mg/kg were significantly reduced ear weight differences and granuloma formation in mice. Highest percentage inhibition was offered by EAHAL 400 mg/kg dose (35.15 ± 11.78% and 34.76 ± 11.30%) in both anti-inflammatory tests respectively. In anti-nociceptive experiments, all extracts were significantly reduced paw licking and abdominal writhing of mice. Highest percentage inhibition was offered by EAHAL 400 mg/kg dose (88.21 ± 2.23% and 54.00 ± 2.38%) in both anti-nociceptive tests respectively. In addition, both extracts were showed significant inhibition of percentage of diarrhea in anti-diarrhoeal models except EAHAL 200 mg/kg dose and the apex percentage inhibition is offered by MHAL 400 mg/kg dose (67.73 ± 5.77%).ConclusionThese results confirm that the leaves extract of Hemigraphis alternata are nontoxic and may provide a source of plant compounds with anti-inflammatory, anti-nociceptive and anti-diarrhoeal activities.

Antioxidant Activity, Anti-Inflammatory and Analgesic Effects of Caralluma europaea (Eddaghmouss) in Mice

The aim of the current study is to evaluate the anti-inflammatory, antioxidant and analgesic properties of ethanolic (100 and 200 mg/kg, p.o.) and ethyl acetate extracts (100 and 200 mg/kg, p.o.) of Caralluma europaea. Formalin-induced paw licking test, Acetic Acid induced Writhing Test and Hot-PlateTest were used to assess the analgesic activity. Xylene-induced ear edema test was used to evaluate anti-inflammatory activity of those extracts. In this work, the High-Performance Liquid Chromatography technique (HPLC), allowed us to identify and quantify the main phenolic compounds present in ethanolic and ethyl acetate extracts. In vitro anti-oxidant propriety was evaluated using two methods, the 2,2-Diphenyl-1Picrylhydrazyl (DPPH) radical scavenging method and reducing power methods. The main phenols identified were Catechin (24%) and quercetin (18%) in ethanolic extract, while in the ethyl acetate extract, they were quercetin (36%), P-coumaric (30%) and 2-hydroxycinnamic (25%). Analysis of our results had shown that Caralluma europaea extracts had exhibited a very potent analgesic activity. Percentage of Pain Inhibition (PPI) in the writhing test, 63.60±4.24% for the Ethanolic Extract (EE) (200 mg/kg, p.o.) and 65.39±3.27% for the Ethyl Acetate Extract (EAE). The PPI of early and late phase in the formalin test were respectively, 41% and 73% for EAE (200 mg/kg; p.o), 28% and 75% for EE. In the hotplate test, latency to the thermal stimuli was increased in a dose dependent manner after the administration of EE and EAE. However, the analgesic potential of EAE seems to be higher than EE. Both EE and EAE presented a significant in vitro redox potential and high anti-inflammatory activity. Our results have shown that Caralluma europaea is rich in phenolic compounds and possesses an important antinociceptive, anti-inflammatory and anti-oxidant activity.

Anti-nociceptive and Anti-inflammatory Activities of Asparacosin A Involve Selective Cyclooxygenase 2 and Inflammatory Cytokines Inhibition: An in-vitro, in-vivo, and in-silico Approach.

Triterpenes possess anti-inflammatory and anti-nociceptive effects. In this study anti-inflammatory activities of Asparacosin A were evaluated' using in-vitro cyclooxygenases 1 and 2 (COX-1/2) inhibition assays. Moreover, anti-nociceptive activities were assessed in-vivo by carrageenan-induced paw edema test, xylene-induced ear edema tests, and acetic acid-induced writhing and formalin tests. Additionally molecular docking was conducted to elucidate the binding mechanism of the compound and to correlate the in-vitro findings with the in-silico data. Oral administration of Asparacosin A at the doses of 10, 20, and 40 mg/kg induced significant anti-inflammatory effects (*p < 0.05, **p < 0.01, and ***p < 0.001) in a dose-dependent manner in both models. Asparacosin A also inhibited the human recombinant COX-2 enzyme and caused a dose-dependent decrease in the levels of TNF-α, IL-1β, and PGE2 in the carrageenan-induced paws. Moreover, Asparacosin A displayed significant anti-nociceptive effects (*p < 0.05, **p < 0.01, ***p < 0.001) at the doses of 10, 20, and 40 mg/kg in acetic-acid induced writhing test. However, in formalin test, Asparacosin A (10–40 mg/kg, p.o) produced anti-nociceptive effects only in the late phase, similar to the effect observed with the reference drug celecoxib (50 mg/kg, p.o). Molecular docking was carried out on both COX-1 and COX-2 structures which revealed that Asparacosin A targets allosteric binding site similar to the binding mode of the selective COX inhibitor. In conclusion, Asparacosin A exhibits anti-inflammatory and peripheral anti-nociceptive activities which are likely mediated via inhibition of COX-2 enzyme and inflammatory cytokines. Furthermore, Asparacosin A can serve as a model to obtain new and more selective potent anti-inflammatory and anti-nociceptive drugs.

Methanol extract of smokeless tobacco alters inflammation and nociception process in animal models

Purpose: To investigate the inflammatory and nociceptive alterations due to the use of Nicotiana tabacum or smokeless tobacco (MEST) owing to the fact that it is used by some people to relieve dental pain.Methods: Hepatic biochemical indicators and thiobarbituric acid reactive substances assay were used to assess MEST toxicity and pharmacological doses selection. The effects on inflammation of different pharmacological doses (100, 200 and 500 mg/kg i.p.) of MEST were evaluated using xylene-induced ear edema and cotton pellet granuloma tests. Indomethacin (10 mg/kg, i.p.) was used as positive standard drug, whereas the vehicle 0.5 % CMC treated group was considered as negative control. Acetic acid-induced abdominal contraction test and formalin-induced hind paw licking model were utilized to assess the role of MEST in nociception. Indomethacin (10 mg/kg i.p.) and diclofenac sodium (10 mg/kg i.p.) were used as positives standard drugs. The vehicle used was 0.5% CMC which served as the negative control.Results: MEST (50 %, 200 mg/kg) and indomethacin (47.5 %) both elicited a significant (p < 0.001) anti-edematogenic effect on xylene-induced ear edema. MEST also showed a significant (p < 0.001) inhibitory effect on granuloma formation at all administered doses as compared to the untreated groups which was comparable to standard drug indomethacin. The number of acetic acid induced writhings was observed to be significantly increased (p < 0.001) by MEST at all doses, unlike diclofenac that led to significant reduction (p < 0.001) in the number of writhings, when compared to the untreated group. MEST also showed a significant (p < 0.05) dose-dependent reduction of the hind paw licking caused by formalin when compared to the vehicle control.Conclusion: These results signify that administration of MEST induces inflammatory and nociceptive alterations. However, the extract is not recommended for dental pain due to its other toxic effects that have previously been reported.Keywords: Nicotiana tabacum, Smokeless tobacco, Inflammation, Nociception

Protective effect of chloroform extract of Stereospermum chelonoides bark against amyloid beta42 induced cell death in SH-SY5Y cells and against inflammation in Swiss albino mice.

Background This study was designed to evaluate the free radical scavenging property of chloroform extract of the bark of Stereospermum chelonoides (SCBC) and to investigate its potential in Alzheimer's disease and inflammation, two oxidative stress related disorders. Methods Preliminary phytochemical analysis and in vitro antioxidant potential of SCBC were evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, ferric reducing antioxidant power (FRAP) assay, cupric reducing antioxidant capacity (CUPRAC) and total antioxidant capacity determination assay. Total phenol and total flavonoid contents were also determined. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) based cytotoxicity and cyto-protective assays were performed on human neuroblastoma SH-SY5Y cells. Thioflavin-T assay and caspase activation measurement assay were carried out to elucidate the mechanism of cytoprotection of SCBC observed here. In vivo anti-inflammatory potential was measured using croton oil and xylene induced ear edema tests. Results Phytochemical screening of SCBC revealed the presence of various phytoconstituents. Dose-dependent in vitro antioxidant activity was observed. The extract was enriched in flavonoids and polyphenolic compounds too. SCBC was found to inhibit amyloid-β peptide 1-42 (Aβ42) induced cell death in a dose-dependent manner. Encouraged by the cyto-protective effect, its effects on Aβ42 fibrillogenesis and caspase-3 activated apoptosis were observed. SCBC significantly slowed down the Aβ42 fibrillogenesis and caspase-3 activation in a concentration-dependent manner indicating its probable mechanism of rendering cyto-protection. SCBC has been able to reduce inflammation significantly in croton oil induced ear edema in both doses. Conclusions Thus, this study could form the basis for further study for the potential use of SCBC in oxidative stress associated cell death and inflammation.

Analgesic and Anti-Inflammatory Activities of Diethyl Ether and n-Hexane Extract of Polyalthia suberosa Leaves.

In folk medicine, Polyalthia suberosa is used as abortifacient, laxative, febrifuge analgesic, filler of tooth cavities, and anti-HIV drug and for rheumatism and various skin infections. The present study was directed to evaluate the analgesic and anti-inflammatory activities of diethyl ether and n-hexane extracts of Polyalthia suberosa leaves (PSDE and PSNH). A variety of tests including formalin-induced paw licking test, acetic acid induced writhing test, and tail immersion test were used to assess the analgesic activity. In addition, xylene-induced ear edema test was used to evaluate anti-inflammatory activity of PSDE and PSNH. PSDE and PSNH at 200 and 400 mg/kg doses expressed analgesic as well as anti-inflammatory activities in mice. In formalin-induced paw licking test, acetic acid induced writhing test, and xylene-induced ear edema test, the extracts exhibited significant inhibition (⁎P < 0.05 versus control) of pain and inflammation. Alternatively, in tail immersion test, PSDE 400 mg/kg showed significant (⁎P < 0.05 versus control) latency at 30 min but another tested sample had no significant latency. From this study, it could be shown that Polyalthia suberosa leaves may contain analgesic and anti-inflammatory agents which support its use in traditional medicine.

Atractylodes lancea rhizome water extract reduces triptolide-induced toxicity and enhances anti-inflammatory effects

The present study was designed to explore the influence of water extracts of Atractylodes lancea rhizomes on the toxicity and anti-inflammatory effects of triptolide (TP). A water extract was prepared from A. lancea rhizomes and co-administered with TP in C57BL/6 mice. The toxicity was assayed by determining serum biochemical parameters and visceral indexes and by liver histopathological analysis. The hepatic CYP3A expression levels were detected using Western blotting and RT-PCR methods. The data showed that the water extract of A. lancea rhizomes reduced triptolide-induced toxicity, probably by inducing the hepatic expression of CYP3A. The anti-inflammatory effects of TP were evaluated in mice using a xylene-induced ear edema test. By comparing ear edema inhibition rates, we found that the water extract could also increase the anti-inflammatory effects of TP. In conclusion, our results suggested that the water extract of A. lancea rhizomes, used in combination with TP, has a potential in reducing TP-induced toxicity and enhancing its anti-inflammatory effects.

Pharmacological effects of a synthetic quinoline, a hybrid of tomoxiprole and naproxen, against acute pain and inflammation in mice: a behavioral and docking study.

Objective(s):In the present study, we investigated the potential anti-nociceptive activity and acute anti-inflammatory effect of a synthetic quinoline compound (2-(4-Methoxyphenyl)benzo[h]quinoline-4-carboxylic acid, QC), possessing structural elements of both naproxen and tomoxiprole drugs.Materials and Methods:The anti-nociceptive activity of QC was evaluated using chemical- and thermal-induced nociception models and its acute anti-inflammatory effect was evaluated by xylene-induced ear edema test in mice.Results:QC displayed a dose dependent effect in both acute anti-nociceptive tests (writhing and hot plate). This compound at dose of 6.562 mg/kg showed a high anti-nociceptive effect near equal to diclofenac 5 mg/kg. It also showed high anti-inflammatory effects (less than 6.562 mg/kg) comparable to those of reference drugs diclofenac (5 mg/kg) and celecoxib (100 mg/kg). Docking study showed that this quinoline derivative could inhibit COX-2 enzyme strongly.Conclusion:QC showed high anti-nociceptive and anti-inflammatory effects comparable to reference drugs and can exert its anti-nociceptive and anti-inflammatory activities through COX-2 inhibition.

Enhanced transdermal delivery of sinomenine hydrochloride by ethosomes for anti-inflammatory treatment

Sinomenine hydrochloride (SH) is a valuable anti-inflammatory drug. However, the application of SH is limited by its short half-life and side effects. The aim of this study was to develop a novel SH-loaded ethosome (SE), and make it safe and effective in anti-inflammatory treatment. In this study, the SE was prepared by the injection method and optimized by the single factor test and uniform design. The in vitro skin permeation and deposition of SE was measured and the skin irritation was evaluated by Draize patch test. Finally, the in vivo anti-inflammatory ability of SE was studied by the xylene-induced ear edema test. As a result, the optimized SE was 157.08 nm and negatively charged. The skin penetration and deposition of SH from SE was 663.8 μg/cm2 and 18.5 μg/cm2, respectively. The skin irritation study suggested that the SE showed desirable skin tolerability. Moreover, the SE showed a significant inhibition effect on the ear edema (30.01%). In conclusion, the SE was demonstrated to be a promising vehicle for transdermal delivery of SH and have potential application in the treatment of local inflammation.

Synthesis of 4-Phenylthieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine-5(4H)-one Derivatives and Evaluation of Their Anti-inflammatory Activity

A series of 4-phenylthieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine-5(4H)-ones (5a–p) with triazole or other heterocyclic substituents (6–11) was synthesized and the compounds were evaluated for their anti-inflammatory activity using the xylene-induced ear-edema test. Pharmacological analyses showed that the compound 4-(4-chlorophenyl)thieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine- 5(4H)-one (5m) exhibited the greatest anti-inflammatory activity (50.48% inhibition, 30 min after intraperitoneal administration) and was more potent than the reference drug, indomethacin. The peak activity of 5m was observed 4 h after oral administration, and it showed a higher anti-inflammatory activity than indomethacin did at a dose of 100 mg/kg. Keywords: Synthesis, heterocyclic compounds, anti-inflammatory, triazole, indomethacin, ear-edema test.