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Anti-inflammatory, analgesic and antipyretic effects of methanol extract from Bauhinia racemosa stem bark in animal models.

In this study, the anti-inflammatory, analgesic, and antipyretic effects of 50, 100 and 200 mg/kg body weight of methanol extract obtained from Bauhinia racemosa stem bark, the so-called MEBR, were investigated. The effects of MEBR on the acute and chronic phases of inflammation were studied in carrageenan, dextran and mediators (histamine and serotonin)-induced paw oedema and cotton pellet-induced granuloma, respectively. Analgesic effect of MEBR was evaluated in acetic acid-induced writhing and hotplate tests. Antipyretic activity of MEBR was evaluated by yeast-induced hyperpyrexia in rats. The anti-oedema effect of MEBR was compared with 10 mg/kg of indomethacin orally. In acute phase of inflammation, a maximum inhibition of 44.9, 43.2, 44.8 and 45.9% (P<0.001) was noted at the dose of 200 mg/kg b.w. after 3h of treatment with MEBR in carrageenan, dextran, histamine and serotonin-induced paw oedema, respectively. Administration of MEBR (200 mg/kg b.w.) and indomethacin (10 mg/kg b.w.) significantly (P<0.05) decreased the formation of granuloma tissue induced by cotton pellet method at a rate of 50.4 and 56.2%, respectively. The extract also inhibited peritoneal leukocyte migration in mice. The MEBR also produced significant (P<0.01) analgesic activity in both models. Further, the MEBR potentiated the morphine- and aspirin-induced analgesic in mice. Treatment with MEBR showed a significant (P<0.01) dose-dependent reduction in pyrexia in rats. The results suggest that MEBR possess potent anti-inflammatory, analgesic and antipyretic activity.

Analgesia↗

Anti-inflammatory, analgesic and antipyretic activities of loxoprofen sodium given intramuscularly in animals.

The evaluation of the anti-inflammatory, analgesic and antipyretic activities of loxoprofen sodium given in intramuscular route was investigated as compared to oral application in rats and mice. The intramuscular ED50 values of loxoprofen sodium in carrageenan edema and vascular permeability tests are 1.15 and 7.8 mg/kg, respectively, which represent more potent than in case of oral application. Its therapeutic effects in adjuvant arthritis were shown at 6 mg/kg i.m. and 3mg/kg p.o. Analgesic effect was shown to be more potent as given intramuscularly. Similar potency of antipyretic effects was shown in both administration routes. Considerably weak gastric damages were observed in intramuscular application.

Analgesics, Non-Narcotic↗

4-(1,2-Benzisothiazol-3-yl)alkanoic and phenylalkanoic acids: synthesis and anti-inflammatory, analgesic and antipyretic activities.

Continuing their studies on benzisothiazolyl derivatives, Authors refer to the preparation and pharmacological properties of 4-(1,2-benzisothiazol-3-yl) alkanoic and phenylalkanoic acids. All substances were tested for anti-inflammatory, analgesic and antipyretic properties. As reference compounds, 1,2-benzisothiazolin-3-one and 4-(3-oxo-1,2-benzisothiazolin-3-yl) phenylacetic acid, as prototypes of benzisothiazolinonic derivation. Ibuprofen, as a prototype of substituted arylalkanoic acids, and Phenylbutazone were used. Analysis of the data leaded to the following conclusions. Introduction of the aryl moiety, passing from benzisothiazolylalkanoic to benzisothiazolyl-phenylalkanoic structures, produced a remarkable increase of activity. 2-[4-(1,2-benzisothiazol-3-yl)phenyl] propionic and 2-[4-(1,2-benzisothiazol-3-yl)phenyl]butyiric acids showed anti-inflammatory, analgesic and antipyretic properties comparable to those of Ibuprofen. Substantial differences in variations in activities were observed comparing the properties of benzisothiazolylphenylalcanoic acids with those of the benzisothiazolinonic series, object of preceding studies.

Animals↗

Design and synthesis of 3,4-methylenedioxy-6-nitrophenoxyacetylhydrazone derivatives obtained from natural safrole: new lead-agents with analgesic and antipyretic properties.

In this work, we reported the synthesis and evaluation of the analgesic, anti-inflammatory, and antipyretic properties of new 2-(6-nitro-benzo[1,3]dioxol-5-yloxy)-acetylhydrazone derivatives (3), designed exploring molecular hybridization and isosteric replacement approaches between nimesulide (1) and carbanalogue NAH series (2) developed at LASSBio. Target compounds were synthesized in very good yields exploiting abundant Brazilian natural product safrole (4) as starting material. The evaluation of the antinociceptive properties of this series led us to discover a new potent prototype of analgesic and antipyretic agent, that is, NAH derivative 3c, named LASSBio-891, which showed to be more potent than dipyrone used as standard.

Analgesics↗

Nonsteroidal antiinflammatory agents-part 2 antiinflammatory, analgesic and antipyretic activity of some substituted 3-pyrazolin-5-ones and 1,2,4,5,6,7-3H-hexahydroindazol-3-ones.

As a part of a research project on the synthesis of a number of substituted 1-(pyrimidin-2-yl)-3-pyrazolin-5-ones and 2-(pyrimidin-2-yl)hexahydroindazol-3-ones and as a result of the interesting antiinflammatory, analgesic and antipyretic activities recorded for some of these compounds, some new 3-pyrazolin-5-ones and hexahydroindazol-3-ones linked to substituted imidazolyl, pyrimidyl and tetrahydroquinazolinyl moieties were prepared and evaluated for such activity (). A structure-activity relationship (SAR) comparative study indicated that some compounds from 3-pyrazolin-5-one (2, 6-8, 10) and indazolone (18, 20, 24, 27, 29) series exhibited pronounced antiinflammatory, analgesic and antipyretic activities relative to indomethacin. Most of these compounds were found to be nearly equipotent in the antiinflammatory screen (ED(50)=16.8-19.9 mg/kg) whereas the lead compound, 2-indazolyl-4-pyrimidineacetic acid 24 (), was found to be the most potent among this series (ED(50)=9.9 mg/kg). Additionally, the most active compounds were shown to have a large safety margin (ALD(50)=3.0 g/kg, po) and devoid of ulcerogenic potentialities when administered orally at a dose of 300 mg/kg.

Administration, Oral↗

The anti-inflammatory, analgesic and antipyretic activity of Nigella sativa.

The aqueous extract of Nigella sativa (N. sativa) was investigated for anti-inflammatory, analgesic and antipyretic activities in animal models. The extract has an anti-inflammatory effect demonstrated by its inhibitory effects on Carrageenan induced paw edema. It also produced significant increase in the hot plate reaction time in mice indicating analgesic effect. However, N. sativa crude suspension had no effect on yeast induced pyrexia. This study therefore, supports its use in folk medicine both as analgesic and anti-inflammatory agent and calls for further investigations to elucidate its mechanism of action.

Analgesia↗

Influence of some anti-inflammatory, antipyretic and analgesic agents on urinary enzyme level in rats.

The influence of single oral dose of anti-inflammatory, antipyretic and analgesic agents on urinary enzymes was investigated in rats as a indicator of nephrotoxic effect. Urinary LDH activity was significantly elevated by aspirin, ketophenylbutazone, aminopyrine, phenacetin and acetaminophen. These drugs increased also H/M ratio of LDH isoenzymes. Although other test drugs have no effect on LDH in urine phenylbutazone and indomethacin elevated GPT and A1-P, oxyphenbutazone did gamma-GT and anthranilic acid derivatives did Al-P and gamma-GT. Other drugs such as sodium salicylate, ibufenac, ibuprofen, bucolome, aminopropylone, sulfinpyrazone, benzydamine and mepirizole did not significantly influence any enzyme activities measured in urine.

Aniline Compounds↗

[Synthesis and anti-inflammatory, antipyretic and analgesics properties of 5-(1,2-benzisothiazolyl)tetrazoles].

Tetrazole analogs of a series of known 1,2-benzisothiazolalkanoic acids were synthesized and tested for anti-inflammatory, antipyretic and analgesic activities in comparison with their corresponding carboxylic acids. The benzisothiazoliltetrazoles showed high antipyretic activity and each tetrazole, except one, was appreciably more potent than the corresponding acid. The examined tetrazoles are generally inactive as anti-inflammatory agents and weakly active in the mouse writhing test, with effect comparable with those of the corresponding carboxylic acids.

Animals↗