Studies on Novel 7‐Acyl‐5‐chloro‐2‐oxo‐3H‐benzoxazole Derivatives as Potential Analgesic and Anti‐Inflammatory Agents
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Abstract In this study, a series of (7‐acyl‐5‐chloro‐2‐oxo‐3 H ‐benzoxazol‐3‐yl)alkanoic acid derivatives were synthesized and evaluated for their analgesic and anti‐inflammatory activities by using the p‐benzoquinone‐induced writhing test and the carrageenan hind paw edema model, respectively. Acetic acid‐induced peritoneal capillary permeability test and serotonin‐induced hind paw edema test were also employed for the most active compounds. The test results indicated that (7‐acyl‐2‐oxo‐3 H ‐benzoxazol‐3‐yl)alkanoic acids (Compounds 6 a—c , 8 a—c , 10 a—c ) were equally or more potent analgesic and anti‐inflammatory agents than aspirin and indomethacin respectively. The compounds 8a and 8c , but not 8b have the longest carbon chain on alkanoic acid moiety did not induce gastric lesion in mice.Keywords:
Carrageenan
Moiety
Vascular permeability
【Objectives : The present study was examined to evaluate the anti-inflammatory effects of the Humulus japonicus MeOH extracts (HJE) in the carrageenan-induced paw edema model in rats. Methods : The effects of HJE on anti-inflammation were measured in the carrageenan-induced paw edema model in rats and infiltrated Inflammatory Cells. Results : 1. HJE (1.0 g/kg) and dexamethasone effectively inhibited paw edema measured 1~4 h after carrageenan injection. HJE (0.3 g/kg) effectively inhibited paw edema measured 1, 3, 4 hr. 2. In histopathological study in rats, 1.0 g/kg HJE and dexamethasone effectively inhibited the increases of hind paw skin thicknesses and inflammatory cell infiltrations induced by carrageenan treatment. But quite similar histopathological changes were detected in 0.3 g/kg HJE treated group as compared with carrageenan control.】
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Carrageenan
Extravasation
Interstitial fluid
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Paw edema formation after the subplantar injection of carrageenan was enhanced in rats treated with 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). The enhanced carrageenan response could be detected as early as 4.5 hr after TCDD; however, the magnitude of enhancement was greatest when rats were challenged with carrageenan 5 days after TCDD. In the latter case, the ED50 of TCDD in enhancing the carrageenan response was 6 micrograms/kg. TCDD also enhanced dextran-induced paw edema, which follows a time course different from that of carrageenan-induced edema and is produced by a different mechanism. The enhancement of carrageenan and dextran paw edemas was due to an increase in the edema-producing potency of the irritants and not to a change in their maximum effect. The ability of other 3-methylcholanthene-type inducers to enhance carrageenan-induced paw edema and the inability of phenobarbital-type inducers to cause the response suggest that the TCDD binding protein might be involved in edema enhancement. TCDD also enhanced carrageenan-induced pleural edema; however, the number and type of leukocytes recovered in the pleural exudate was not affected. TCDD did not alter granuloma formation produced by the subcutaneous implantation of cotton pellets, indicating that enhancement by TCDD was peculiar to edema formation and not to inflammation in general. It is suggested that TCDD may enhance carrageenan and dextran edemas by increasing the availability of mediators involved in each type of edema formation and/or by increasing the responsiveness of the vasculature to mediators.
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ABSTRACT The aim of this study was to investigate the anti-inflammatory effect of alcoholic extract of Tarantula cubensis alcoholic extract (TCAE) in experimentally induced inflammation in rats. Fifty-four adult Sprague-Dawley male rats were randomly divided into nine groups. Paw edema was induced by 0.2mL subplantar (s.p.) injection of 1% carrageenan (CAR) into the right hind paw. Rats were treated with the nonsteroidal anti-inflammatory drug (NSAID) indomethacin (INDO) (10mg/kg, p.o.) or TCAE at different doses (1, 10 or 100µg/kg) injected s.c. for systemic or s.p. for local anti-inflammatory effect. Saline was used as control. Changes in paw thickness, volume, and weight were calculated as percentages. Formalin-fixed paws were used for histopathological examination. We detected that TCAE applied s.c. at 10µg/kg and 100µg/kg doses resulted in thinner paw thickness, lower paw volume, and lower paw weights four hours after the induction of inflammation when compared with the INDO group (p<0.05). The paw edema inhibitory effect of TCAE applied at a dose of 10µg/kg, s.c. was 68% when compared with the INDO which had an inhibitory effect of 56%. These results were verified with similar histopathological findings. The anti-inflammatory feature of 10µg/kg of TCAE given systematically was similar to the effects of INDO. Our results suggest that TCAE has anti-inflammatory effects by reducing edema and decreasing inflammatory reaction. These results may be attributed to the inhibition of the production of proinflammatory mediators. Thus, TCAE may be considered as a potential anti-inflammatory agent for treating acute inflammatory conditions.
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The anti-inflammatory effects of the aqueous extract of licorice (Glycyrrhizae Radix, GR), glycyrrhizin (GL). and 18β-glycyrrhetinic acid (GA) on carrageenan-induced edema of the rat hind-paw were compared. Tested drugs were administered orally 1 hr prior to the subplantar injection of 0.1 m1 mixture of 1 % lambda carrageenan into the right hind-paw of the rat. The edema formation during 1-6 hr was completely blocked by 5 mg/kg indomethacin (as a positive control) and was partially attenuated by 200 mg/kg GA. Both GL and GR, at the doses containing equivalent quantities of 100, 200, and 500 mg/kg of GL, had little effects on edema formation. In contrast to 200 mg/kg GA, 500 mg/kg GA facilitated and increased the carrageenan-induced edema formation. This result indicates that GA has very narrow margin of anti-inflammatory activity on carrageenan induced edema.
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1. Injection of carrageenan into the mouse paw produced a biphasic edema. During the first phase, which developed up to 24 h, edema was of low intensity and unrelated to the dose of carrageenan given. During the second phase, after 24 h, edema was more pronounced, presented a clear dose-response relationship and peaked at 72 h after injection. 2. Histological analysis of the subplantar area 4 h after carrageenan injection revealed a diffuse cellular infiltrate with predominance of polymorphonuclear neutrophils. Between 48 and 72 h, an intense accumulation of macrophages, eosinophils and lymphocytes was observed, together with a great increase in the number of circulating leukocytes and platelets. 3. Pretreatment with the anti-inflammatory drugs indomethacin and dexamethasone reduced both phases of edema in a dose-dependent fashion. 4. The present study shows that carrageenan-induced mouse paw edema constitutes a new and interesting model for the study of the mediators of inflammation and for the screening of new anti-inflammatory drugs.
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Abstract The antiinflammatory effect of an ointment containing propolis extract (3%–7%) was examined using carrageenan‐induced hind paw edema in rats. Treatment with the ointment inhibited the edema moderately, and the inhibition was significant at 5% and 7%. Additionally, the effect of the ointment on chemotaxis of human polymorphonuclear leukocytes (PMNs) was investigated using the agarose plate method. Migration of PMNs toward zymosan‐treated serum was inhibited in the presence of 5% propolis ointment. These results demonstrate that topical application of propolis extract is effective in inhibiting carrageenan‐induced rat hind paw edema, and its inhibitory effect on the chemotaxis of PMNs may also contribute to the antiinflammatory effect. Copyright © 2007 John Wiley & Sons, Ltd.
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The aim of present study was to investigate the effect of W-7, a calmodulin antagonist, on carrageenan-induced rat's paw edema. W-7(50 microMol/kg) was given intraperitoneally synchronous with the intraplantar injection of 0.1 ml of 0.5% carrageenan solution. After four hours, paw edema was assessed by calculating the paw volume changes which measured by hydroplethysmometer. In adrenalectomized rats, both adrenal glands were removed. Treatment of animals with W-7 reduced carrageenan-induced paw edema by 50%. In adrenalectomized rats, W-7 was also effective in reduction of paw edema (52%). There was no significant difference between the effect of W-7 in adrenalectomized and control animals. Our findings suggest that W-7 as a calmodulin inhibitor reduce carrageenan-induced paw edema and the inhibitory effect of W-7 on edema formation appears not to be dependent on adrenal function.
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For the simple assay of anti-inflammatory agents and the analysis of their mode of action, the early inflammatory reactions of the carrageenin abscess model in rats were studied by determining abscess (exudate) weight, vascular permeability measured by extravascular dye leakage, protein, prostaglandins (PGs), and DNA (an index of leucocyte infiltration). Subcutaneous injection of 0.5 ml of 2% carrageenin in the dorsal sacral region of rats induced an edema with an initial weak phase (3 hr) followed by a second pronounced phase, reaching a maximum (2.3 g) at 15 hr and declining steadily thereafter. During the first 15 hr, there was a good correlation between the edema formation and changes in the increased vascular permeability, and also the PGE contents in the exudate paralleled the permeability, but thereafter, these components did not follow the same time course. The marked increase in DNA content in the exudate started after a lag time of a few hr in correspondence with the second accelerated edema formation. The edema formation was effectively inhibited by indomethacin and dexamethasone given simultaneously with the irritant injection; maximum inhibition with indomethacin (2 mg/kg, p.o.) was 36% at 15 hr and 48% with dexamethasone (0.1 mg/kg, p.o.) at 9 hr. Indomethacin very significantly affected exudate PGE levels and vascular permeability, rather than suppressing the edema formation. When the treatment was initiated at 9 hr after injury, it was not effective in reducing the weight of the 24-hr abscess, whereas it had significant effect on the PGE concentration. Dexamethasone did not exert significant effect on the PGE levels despite its potent and steady anti-edematous activities.(ABSTRACT TRUNCATED AT 250 WORDS)
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