Effects of an essential oil from the bark of Croton cajucara Benth. on experimental gastric ulcer models in rats and mice.

Croton cajucara Benth. (Euphorbiaceae) is widely used in Amazonian folk medicine for the treatment of a wide range of gastrointestinal symptoms. The essential oil from its bark was investigated for acute toxicity in mice and for its ability to prevent the formation of ulceration of the gastric mucosa in different models of experimentally induced gastric ulcer in mice and rats. When previously administered orally at a dose of 100 mg kg(-1), the essential oil significantly reduced (P < 0.01) the gastric injury induced by hypothermic restraint stress (48%), indomethacin (47%), ethanol (86%) and pylorus ligature models (87%) in rats. In the HCl/ethanol-induced gastric ulcer model in mice, at oral doses of 100 and 200 mg kg(-1), the essential oil from C. cajucara significantly reduced (P < 0.01) the formation of gastric lesions by 52% and 67%, respectively, when compared with the control group. In rats submitted to pylorus ligature, the essential oil given orally increased the volume of gastric juice when compared with the control group (P < 0.01). When the essential oil (100 mg kg(-1)) was administered intraduodenally to mice, significant modifications were found in gastric parameters such as pH and total acid content after oil treatment. We observed significant changes (P < 0.01) in gastric juice parameters such as an increase in volume and a decrease in gastric acidity (pH and total acid content). The acute toxicologic effects of the essential oil from C. cajucara were assessed in mice. The LD50 values were 9.3 g kg(-1) by the oral route and 680 mg kg(-1) by the intraperitoneal route. The good yield of essential oil obtained from dried C. cajucara bark (1%) as well as its anti-ulcerogenic activity and low toxicity suggest that pharmacological studies of this substance as a potential new anti-ulcerogenic drug are warranted.     

Antinociceptive and anti-inflammatory effects of the essential oil from Eremanthus erythropappus leaves

The chemical composition of the essential oil from air-dried leaves of Eremanthus erythropappus was studied. The main compounds were beta-pinene (23.24%), beta-caryophyllene (22.92%), beta-myrcene (10.03%) and germacrene D (9.40%). The essential oil had an LD50 of 2.90 g kg(-1) in mice. Doses of 200 and 400 mg kg(-1) inhibited 10.69% and 27.06% of acetic-acid-induced writhing in mice, respectively. In the formalin-induced nociception test in mice, the essential oil inhibited the first phase of paw licking by 29.13% (400 mg kg(-1)) and the second phase by 32.74% (200 mg kg(-1)) and 37.55% (400 mg kg(-1)). In the hot-plate test in mice, doses of 200 mg kg(-1) and 400 mg kg(-1) significantly increased the reaction time after 30, 60 and 90 min of treatment. Doses of 200 and 400 mg kg(-1) inhibited carrageenan-induced paw oedema in rats by 15.18% and 36.61%, respectively. Doses of 200 and 400 mg kg(-1) administered 4 h before intrapleural injection of carrageenan significantly reduced exudate volume (by 20.20% and 48.70%, respectively) and leucocyte mobilization (by 5.88% and 17.29%, respectively). These results demonstrate that E. erythropappus has analgesic and anti-inflammatory properties, supporting the use of this plant in folk medicine.     

Bulgarian propolis induces analgesic and anti-inflammatory effects in mice and inhibits in vitro contraction of airway smooth muscle

Propolis is a bee product, which has long been used in folk medicine for the management of different diseases. In this study we evaluated the analgesic and anti-inflammatory effects of a standard ethanolic extract of Bulgarian propolis (Et-Blg) in mice and its in vitro effect on airway smooth muscle. Et-Blg inhibited acetic acid-induced abdominal contortions with an ID(50) = 7.4 +/- 0.7 mg. kg(-1). In the formalin test, the extract caused a significant reduction in pain in mice treated with 100 mg. kg(-1) Et-Blg during the neurogenic phase and for the inflammatory phase with all doses of the extract, with an ID(50) = 2.5 +/- 0.4 mg. kg(-1). Et-Blg inhibited also the capsaicin-induced ear edema in mice; however, this extract was ineffective when assessed in the tail-flick and hot-plate thermal assays. The analgesic effect of Et-Blg was associated with the inhibition of inflammatory responses and not to a simple irritation of nervous terminals. In vitro, this extract inhibited the contraction of trachea smooth muscle induced by histamine (IC(50) = 50 +/- 5 microg. mL(-1)), capsaicin (IC(50) = 26.8 +/- 3 microg. mL(-1)), 80 mM KCl (IC(50) = 27.8 +/- 3 microg. mL(-1)), and carbachol (IC(50) = 54 +/- 2 microg. mL(-1)).     

Anti-nociceptive and anti-inflammatory effects of cyanocobalamin (vitamin B12) against acute and chronic pain and inflammation in mice

In this study, the anti-nociceptive and anti-inflammatory effects of cyanocobalamin (Vit B12) against acute and chronic pain and inflammation were evaluated in mice. Vit B12 (0.87, 1 and 1.77 mg/kg) were injected intraperitoneally. The anti-nociceptive effects against acute pain were examined using hot-plate and writhing tests. The chronic pain was examined 14 days after sciatic nerve ligation using the hot-plate test. Morphine (10 mg/kg) was used as a positive control. Anti-inflammatory effects of Vit B12 against acute and chronic inflammation were assessed using xylene-induced edema in ears and granuloma caused by compressed cotton implantation, respectively. In these tests, sodium diclofenac (15 mg/kg) was used as a positive control. Vit B12 showed a dose related effect in acute anti-nociceptive test and increased the anti-nociceptive effect of morphine in chronic treatment. Vit B12 demonstrated an anti-nociceptive effect in chronic studies as single or continues daily treatment and increased significantly the anti-nociceptive effect of morphine. All doses of Vit B12 significantly decreased xylene-induced ear edema. Maximum anti-inflammatory effect (37.5%) was obtained at dose of 1 mg/kg. In chronic inflammation, Vit B12 significantly decreased granuloma formation in mice. In conclusion our work presents some experimental evidence supporting the administration of cyanocobalamin in controlling acute and chronic neuropathic pain. Cyanocobalamin may have anti-inflammatory effect. It may reduce tolerance to anti-nociceptive effect of morphine as well.     

Antinociceptive effects of Teucrium polium L total extract and essential oil in mouse writhing test.

In this study, the effect of Teucrium polium L, a wild-growing flowering plant belonging to the family Labiatae and found abundantly in Iran was studied on writhing test, a visceral pain model in mice. The total extract and essential oil were administered intraperitoneally 30 min before acetic acid 0.6% injection. Total extract in doses (mg x kg(-1)) of 150 (39.13%, P<0.001), 225 (65.44%, P<0.001), 300 (21.41%, P<0.01) induced reduction in writhing response as compared to control with the ED(50) 67.92 mg x kg(-1).The essential oil in doses (mg x kg(-1)) of 9.37 (35.22%, P<0.001), 18.75 (59.63%, P<0.001), 37.5 (86.60%, P<0.001), 75 (90.22%, P<0.001) and 150 (78.58%, P<0.001) induced significant reduction in writhing response when compared to control with the ED(50) of 29.41 mg x kg(-1). In order to ensure the importance of essence in production of visceral antinociception, the extract free from essential oil was prepared and injected into mice at a dose of 225 mg x kg(-1) (the most effective dose of the extract) which in comparison to total extract, the antinociception, reduced from 65.44 to 49.85% (P<0.001). It is concluded that essential oil is responsible for analgesic properties of T. polium. This study confirms the antivisceral pain properties of T. polium comparable to those of hyoscine and indomethacin and suggests a good place for it in antispasmodic therapies in human. The presence of flavonoids and sterols might be responsible for the anti-inflammatory activity of this plant.     

Evaluation of the anti-inflammatory property of the extract of <Emphasis Type="Italic">Combretum micranthum</Emphasis> G. Don (Combretaceae)

A methanol extract of Combretum micranthum leaves was studied for anti-inflammatory activity in rats and mice using the carrageenan-induced rat paw oedema and the acetic acid-induced vascular permeability in mice. The effect of the extract on cellular-type inflammation was also investigated in the cotton pellet granuloma in rats. The extract (50, 100 mg/kg) significantly (P < 0.05) inhibited oedema production induced by carrageenan in rats. Increased vascular permeability caused by acetic acid injection was also inhibited by the extract, within the same dose range. C. micranthum extract (100 mg/kg) inhibited granuloma formation in rats to a similar degree as indomethacin (5 mg/kg). These results provide evidence for the anti-inflammatory property of C. micranthum leaves.     

Antinociceptive effect in mice of a hydroalcoholic extract of Neurolaena lobata (L.) R. Br. and its organic fractions

An infusion of the aerial parts of Neurolaena lobata (L.) R. Br. (Compositae-Asteraceae) is used in Caribbean folk medicine to treat several kinds of pain. In this investigation we studied the acute oral toxicity of the hydroalcoholic extract of the plant and the antinociceptive effect of the extract and of its hexane- and chloroform-partitioned fractions, given orally, in nociception and inflammatory models in mice. No signs of toxicity were observed for oral doses up to 5000 mg kg(-1) in mice. Morphine hydrochloride (100 mg kg(-1)), dipyrone sodium (200 mg kg(-1)), the hydroalcoholic extract (1000 mg kg(-1)), and its chloroform- and hexane-partitioned fractions (100 mg kg(-1)) significantly inhibited acetic acid-induced abdominal constriction in mice (100, 95, 47, 62 and 60% inhibition, respectively when compared with the negative control). In the hot-plate test in mice, morphine hydrochloride, the chloroform- and hexane-partitioned fractions, but not the hydroalcoholic extract, resulted in a significant latency increase in all observation times. In the acetic acid-induced abdominal constriction in mice, pretreatment of the animals with naloxone significantly reversed the analgesic effect of morphine, but not that of the hydroalcoholic extract or of its hexane- and chloroform-partitioned fractions. Finally, administration of the hexane- and chloroform-partitioned fractions (100 mg kg(-1)) had a significant anti-oedematogenic effect on carrageenan-induced oedema in mice. These data show that the hydroalcoholic extract of N. lobata and, in particular, its partitioned fractions have significant analgesic properties when assessed through these pain models. Their antinociceptive effect might be the result of interference with the inflammatory process.     

The lipid-lowering effect of trans-dehydrocrotonin, a clerodane diterpene from Croton cajucara Benth. in mice fed on high-fat diet

The clerodane diterpene trans-dehydrocrotonin extracted and isolated from the stem bark of Croton cajucara Benth. was investigated for its lipid-lowering effect in mice fed on a high-fat diet. Mice fed on a high-fat diet for a two-week period demonstrated significantly increased blood levels of total cholesterol and triglycerides, compared with normal controls. Oral treatment with trans-dehydrocrotonin at a dose of 25 or 50 mg kg(-1) daily markedly suppressed the high-fat-diet associated rise in total cholesterol and triglyceride levels. The hypocholesterolaemic effect of trans-dehydrocrotonin was more prominent at the dose of 50 mg kg(-1) with significant decreases in high-density lipoprotein, very-low-density lipoprotein and low-density lipoprotein cholesterol levels. The lower atherogenic index of the trans-dehydrocrotonin-treated groups suggests the hypolipidaemic potential of this plant-based drug. These results indicate that orally administered trans-dehydrocrotonin is effective in suppressing high-fat-diet-induced hyperlipidaemia in mice and suggest its likely beneficial use as anti-atherogenic agent.     

Evaluation of the anti-inflammatory, anti-nociceptive and gastric effects of Ginkgo biloba in the rat.

Ginkgo biloba extract (GbE) was assessed in models of acute inflammation induced by carrageenan, formalin or capsaicin in the rat, in models of nociceptive pain, such as hot-plate (55 degrees C) latency, tail-electric stimulation assay and capsaicin-induced paw licking and in the model of acute gastric damage induced by indomethacin. The agent showed marked anti-inflammatory activity in the carrageenan model of paw oedema. When given subcutaneously (s.c.) (25 and 50 mg kg(-1)) 30 min before challenge, GbE inhibited paw oedema with a maximal effect of 43.7 and 56.9%, respectively, at 2h post-carrageenan. Significant inhibition of oedema was also observed when GbE (50 mg kg(-1), s.c.) was given 30 min after carrageenan challenge. The agent was also active p.o. in acute inflammation caused by carrageenan. The administration of GbE with indomethacin, rofecoxib, celecoxib, dexamethasone or melatonin resulted in an additive effect. GbE (50 mg kg(-1), s.c.) caused significant inhibition of formalin-induced paw oedema, but did not reduce the capsaicin-induced paw oedema. In tests of nociception, GbE (25, 50 or 100 mg kg(-1)) decreased in dose-dependent manner the capsaicin-induced hind paw licking time and was similarly effective in the hot-plate assay of nociception. In contrast, when assessed in the tail-electric stimulation test, GbE was only effective in the highest dose (100 mg kg(-1)). In pylorus-ligated rats, GbE (25 or 50 mg kg(-1)) increased gastric acid secretion, but reduced gastric mucosal damage caused by IND. Results suggest that GbE may be of clinical value as an anti-inflammatory and analgesic drug alone or in conjunction with NSAIDs.     

7-Chloro-4-phenylsulfonyl quinoline,a new antinociceptive and anti-inflammatory molecule: Structural improvement of a quinoline derivate with pharmacological activity

The present study was designed to examine the antinociceptive and anti-inflammatory effects of 7-chloro-4-phenylsulfonyl quinoline (PSOQ). Mice were orally (p.o) pretreated with PSOQ (0.01–10 mg/kg), meloxicam (10 mg/kg), 30 min prior to the acetic acid, hot-plate and open field tests. PSOQ reduced abdominal writhing induced by acetic acid, while meloxicam presented no effect. The latency time in the hot-plate test and locomotor/exploratory activities in the open field test were not altered by treatments. In order to evaluate the gastric tolerability after oral administration of PSOQ or meloxicam (10 mg/kg), mice were fasted for 18 h prior to drug exposure. Four hours later, the development of lesions was assessed. PSOQ and meloxicam did not induce ulcer at the dose and time evaluated. Indeed, anti-inflammatory and anti-edematogenic properties of PSOQ were investigated. For this, animals were pretreated with PSOQ (0.01–50 mg/kg; p.o.), meloxicam (50 mg/kg; p.o.), 30 min prior to croton oil application. PSOQ and meloxicam (50 mg/kg) diminished the edema formation and myeloperoxidase activity induced by croton oil in the ear tissue. Taken together these data demonstrated that PSOQ exerts acute anti-inflammatory and antinociceptive actions, suggesting that it may represent an alternative in the development of future new therapeutic strategies.     

In vivo anti-inflammatory and analgesic activities of strictosamide from Nauclea officinalis

Context: Strictosamide is the main representative constituent of Nauclea officinalis Pierre ex Pitard (Rubiaceae), which has been used for a long time in China to treat diseases related to infection and inflammation, but its pharmacological activities are not well studied.

Objective: This work evaluates the anti-inflammatory and analgesic activities of strictosamide by in vivo experiments.

Materials and methods: The anti-inflammatory activity was assessed in mice by models of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema, acetic acid-elevated vascular permeability, and carboxymethylcellulose sodium (CMC–Na)-induced leukocyte migration. The analgesic activity was estimated in mice using acetic acid-induced writhing and hot-plate tests. Compound was injected to mice twice a day for 3?d at doses of 10, 20, and 40?mg/kg.

Results: At 20 and 40?mg/kg, strictosamide obviously decreased the TPA-induced mice ear edema (24.7 and 28.1% inhibition, respectively), and significantly inhibited acetic acid-stimulated peritoneal vascular permeability in mice (23.3 and 33.4% inhibition, respectively). It also significantly decreased the leukocytes in the mice peritoneal cavity induced by CMC–Na at all the tested doses (46.0, 49.1, and 58.7% inhibition, respectively). To acetic acid-induced writhing test in mice, strictosamide markedly prolonged the pain latency at 20 and 40?mg/kg and decreased the writhing counts at 40?mg/kg (49.7% inhibition). However, it did not obviously improve the pain threshold of mice in hot-plate test.

Discussion and conclusion: Strictosamide may have important effects on inflammation and inflammatory pain. The results provide scientific support for the role of strictosamide in the use of N. officinalis to treat inflammatory diseases.     

赖氨匹林的解热、镇痛和抗炎作用

目的：应用大鼠及小鼠研究赖氨匹林的抗炎、镇痛及解热作用。方法：用大鼠足跖肿胀研究抗炎作用，用小鼠醋酸扭体法及热板法测定镇痛作用，用鲜酵母法测定解热作用。结果：赖氨匹林对大鼠足跖肿胀有明显抑制作用，最大抑制率为８０％（Ｐ＜０．０１）。小鼠醋酸扭体法测得镇痛ＥＤ５０＝７２±２３ｍｇ／ｋｇ，对鲜酵母致大鼠体温升高有明显抑制作用。小鼠半数致胃溃疡剂量ＵＤ５０＝０．１８±０．０６ｍｍｏｌ／ｋｇ，是阿司匹林的２．４倍。结论：赖氨匹林具有和阿司匹林相当的解热、镇痛和抗炎作用，而对胃肠道的毒副作用比阿司匹林小。     

Analgesic and anti-inflammatory activities of total extract and individual fractions of Chinese medicinal ants Polyrhachis lamellidens

The ethanol extract of Chinese medicinal ants Polyrhachis lamelliden was evaluated for its analgesic and anti-inflammatory activities in mice. It was shown that the extract significantly inhibited acetic acid-induced writhing response and increased hot-plate pain threshold of mice at doses of 1.5 and 3.0 g crude drug/kg. Meanwhile, the extract significantly inhibited the increase in vascular permeability induced by acetic acid and in ear edema induced by xylene in mice. However, it had no obvious effect on leukocyte migration induced by carboxymethylcellulose sodium (CMC-Na). The ethanol extract suspended in water was partitioned with diethyl ether, ethyl acetate and n-butanol successively to yield four fractions including water fraction. Among these fractions, diethyl ether and ethyl acetate fractions were found to increase hot-plate pain threshold and to inhibit acetic acid-induced writhing response in mice. Water fractions markedly inhibited acetic acid-induced writhing response and reduced the dye leakage to the peritoneal cavity induced by acetic acid and ear edema induced by xylene. These results suggest that P. lamellidens presents remarkable analgesic and anti-inflammatory activity, which supported the traditional use of the medicinal ants in the treatment of various diseases associated with inflammation. The diethyl ether fraction has greater contribution to the overall analgesic activity, whereas the water fraction showed the greatest anti-inflammatory and peripheral analgesic activities.     

Antidiarrheal and anti-inflammatory effects of berberine

Berberine sulfate (Ber) 40 and 80 mg/kg ig reduced the purging effects of castor oil or Cassia angustifolia leaf in mice, but did not affect the gastrointestinal transport function of Chinese ink in normal mice. Ber 60 mg/kg ig significantly inhibited the increased vascular permeability induced by ip 0.7% acetic acid in mice. Ber 20 and 50 mg/kg sc markedly inhibited the increased vascular permeability induced by histamine 100 micrograms/0.1 ml ic in rats. Ber 4 and 8 mg/kg sc produced obvious inhibition in the xylene-induced swelling of mouse ear. The anti-inflammatory effects were enhanced in a dose-dependent manner. It is suggested that the antidiarrheal effect of Ber is relative to its restriction against exudative inflammation to a certain extent.     

Anti-inflammatory and antinociceptive properties of dantrolene sodium in rats and mice

Our study aimed at examining the possible anti-inflammatory and antinociceptive effects of dantrolene sodium in rats and mice. The anti-inflammatory effect of dantrolene sodium (2.5, 5 and 10 mg kg (-1)) was investigated and compared with diclofenac sodium (5 mg kg (-1)) using the formalin-, histamine-, and carrageenan-induced paw oedema and cotton pellet granuloma tests. Analgesic effects of dantrolene sodium were evaluated and compared with metamizol (200 mg kg (-1)) in acetic acid-induced writhing and formalin-induced paw licking tests. It was found that dantrolene sodium significantly diminished the nociceptive response in mice, showing at the same time considerable anti-inflammatory properties in rats.     

Evaluation of the Antinociceptive and Anti-inflammatory Activities of Satureja thymbra. L. Essential Oil

Abstract

The aim of this study was to investigate the antinociceptive and anti-inflammatory activities of the essential oil of Satureja thymbra. L. (Lamiaceae). Antinociceptive activity of the essential oil was measured by the formalin test in mice and by the light tail-flick and hot-plate methods in rats. The paw-edema test was performed in rats to evaluate the anti-inflammatory effect of the essential oil. Motor coordination was assessed with a rotarod apparatus. Although the essential oil produced an antinociceptive effect during both the early (50 and 100 mg kg^?1) and late phases (25, 50, and 100 mg kg^?1) of the formalin test, it did not exert any significant antinociceptive and anti-inflammatory effects in tail-flick and paw-edema tests, respectively. In addition, a significant antinociceptive effect was detected in the hot-plate test (100 and 200 mg kg^?1). No significant change was detected in sensory motor performance. In conclusion, S. thymbra. L. essential oil does not exert any anti-inflammatory effect while it may have central analgesic activity in mice and rats.     

Assessment of antinociceptive,anti-inflammatory and antioxidant properties of Cymbopogon winterianus leaf essential oil

The present study investigated the antinociceptive, anti-inflammatory and antioxidant effects of the leaf essential oil (LEO) of Cymbopogon winterianus Jowitt (Poaceae). In the acetic acid-induced writhing and formalin tests, the LEO (50, 100, and 200?mg/kg, p.o.) significantly reduced (p?<?0.05) the number of writhings and paw licking times in the first (0-5?min) and second (15-30?min) phases, respectively. In contrast, the LEO did not alter the latency time for mice licking the rear paws in hot-plate test. The LEO inhibited the carrageenan-induced neutrophil migration to the peritoneal cavity in a dose-dependent manner (35.5%, 42.8%, and 66.1% at doses of 50, 100, and 200?mg/kg, respectively, p?<?0.001). Moreover, LEO exhibited higher scavenging activity toward 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals with an IC₅₀ (12.66?±?0.56 μg/mL). Our present results demonstrated that the LEO has antinociceptive, anti-inflammatory, and antioxidant properties.     

Antinociceptive effect of the essential oil of tarragon (Artemisia dracunculus)

Context: Tarragon [Artemisia dracunculus L. (Asteraceae)] is used as a commercial flavoring and in perfumery. In traditional folk medicine, tarragon has been used for treatment of pain and gastrointestinal disturbances.

Objective: This study investigated the antinociceptive effect of the essential oil of A. dracunculus (EOAD) in various experimental models.

Materials and methods: The median lethal dose (LD₅₀) of EOAD was estimated using the method of Lorke. The antinociceptive effect was assessed using chemical (formalin and acetic acid) and thermal (hot-plate) nociceptive tests in rats and mice. In all experiments, EOAD was administered intraperitoneally at the doses of 10, 30, 100 and 300?mg/kg.

Results: In the acute toxicity test, the value of estimated LD₅₀ for EOAD was 1250?mg/kg. EOAD (100 and 300?mg/kg) significantly reduced (p?p?Conclusions: This study reported the peripheral and central antinociceptive activity of the EOAD and rationalized the traditional use of the plant in the treatment of different painful conditions.     

Inhibitors of fatty acid amide hydrolase reduce carrageenan-induced hind paw inflammation in pentobarbital-treated mice: comparison with indomethacin and possible involvement of cannabinoid receptors

The in vivo effect of inhibitors of fatty acid amide hydrolase (FAAH) upon oedema volume and FAAH activity was evaluated in the carrageenan induced hind paw inflammation model in the mouse. Oedema was measured at two time points, 2 and 4 h, after intraplantar injection of carrageenan to anaesthetised mice. Intraperitoneal (i.p.) injections of the FAAH inhibitor URB597 (0.1, 0.3, 1 and 3 mg kg(-1)) 30 min prior to carrageenan administration, dose-dependently reduced oedema formation. At the 4 h time point, the ED(50) for URB597 was approximately 0.3 mg kg(-1). Indomethacin (5 mg kg(-1) i.p.) completely prevented the oedema response to carrageenan. The antioedema effects of indomethacin and URB597 were blocked by 3 mg kg(-1) i.p. of the CB(2) receptor antagonist SR144528. The effect of URB597 was not affected by pretreatment with the peroxisome proliferator-activated receptor gamma antagonist bisphenol A diglycidyl ether (30 mg kg(-1) i.p.) or the TRPV1 antagonist capsazepine (10 mg kg(-1) i.p.), when oedema was assessed 4 h after carrageenan administration. The CB(1) receptor antagonists AM251 (3 mg kg(-1) i.p.) and rimonabant (0.5 mg kg(-1) i.p.) gave inconsistent effects upon the antioedema effect of URB597. FAAH measurements were conducted ex vivo in the paws, spinal cords and brains of the mice. The activities of FAAH in the paws and spinal cords of the inflamed vehicle-treated mice were significantly lower than the corresponding activities in the noninflamed mice. PMSF treatment almost completely inhibited the FAAH activity in all three tissues, as did the highest dose of URB597 (3 mg kg(-1)) in spinal cord samples, whereas no obvious changes were seen ex vivo for the other treatments. In conclusion, the results show that in mice, treatment with indomethacin and URB597 produce SR144528-sensitive anti-inflammatory effects in the carrageenan model of acute inflammation.     

Methanol extract from mycelium of endophytic fungus Rhizoctonia sp. induces antinociceptive and anti-inflammatory activities in mice

The present study aimed to elucidate the antinociceptive and anti-inflammatory properties of the methanol extract from the mycelium of the endophytic fungus Rhizoctonia sp. (MEMRh) in mice. The antinociceptive activity was assessed using the abdominal constriction, hot plate, and formalin tests. The anti-inflammatory activity was assessed using a murine model of paw edema. Intraperitoneal administration of MEMRh (0.1, 1, 10 and 100?mg/kg, i.p.) produced an inhibition of acetic acid-induced writhing in mice for at least 8?h. In addition, all doses tested of the methanol extract were able to prevent thermal nociception in the hot-plate test. Furthermore, treatment with MEMRh (10?mg/kg, i.p.) inhibited both the early and late phases of formalin-induced nociception. This antinociceptive effect exhibited by MEMRh in the formalin test was reversed by the systemic administration of naloxone. MEMRh produced inhibition in a carrageenan-induced edema model at a dose of 10?mg/kg. The same extract also displayed significant activity against a histamine- or PGE(2)-induced edema model. The experimental data demonstrated that MEMRh showed remarkable anti-inflammatory and antinociceptive activities. Further studies are warranted to define and isolate the active anti-inflammatory and antinociceptive components from this endophytic fungus, which may yield effective agents for the treatment of inflammatory disorders.