In vivo analgesic and anti-inflammatory activities of a standardized Rhinacanthus nasutus leaf extract in comparison with its major active constituent rhinacanthin-C

Rhinacanthus nasutus (R. nasutus) leaf extract was prepared and standardized to obtain rhinacanthins rich extract that contained total rhinacanthin-C (Rn-C) of not less than 70% w/w. Rn-C was also isolated from the standardized R. nasutus leaf extract (SRLE). SRLE was investigated on pain and inflammatory models in parallel with its main naphthoquinone constituent, Rn-C in order to compare their efficacy in experimental animals. The analgesic activities of SRLE and Rn-C were evaluated by the acetic acid-induced writhing test, a hot-plate test and formalin test at doses of 20, 40, and 80 mg/kg. The anti-inflammatory activities were investigated by carrageenan induced paw edema and the cotton pellet induced granuloma in rats at doses of 80, 160, and 320 mg/kg. SRLE and Rn-C inhibited the acetic acid induced writhing in a dose dependent manner; inhibited the early phase of the formalin test at 80 mg/kg and the late phase at 40 and 80 mg/kg. However, none of the tested doses were effective in protecting against the hot plate test. In the animal models of inflammation, SRLE and Rn-C dose dependently inhibited edema formation in the carrageenan induced paw edema and suppressed granuloma formation in the cotton pellet induced granuloma in rats. The effects of SRLE in these tests were similar to those of the Rn-C. This study confirms the analgesic and anti-inflammatory activities of SRLE and Rn-C in animal models as well as demonstrating that they have a similar efficacy

Antinociceptive activity of the alkaloid extract from Kopsia macrophylla leaves in mice

The effects of the alkaloid extract from the leaves of Kopsia macrophylla Hk. f. K. (K. macrophylla) on nociceptive response using writhing, hot plate and formalin test and the antipyretic activity in yeast-induced fever in mice, were examined. General behavior was also examined using pentobarbital-induced sleep in mice. The LD50 value of intraperitoneally injected K. macrophylla extract in mice was 318.46 mg/kg. Oral administration of K. macrophylla extract at the dose of 400 mg/kg significantly decreased the number of contortions and stretchings induced by acetic acid and licking activity of the late phase in the formalin test but not in the heat-induced pain in mice. The K. macrophylla extract (100-400 mg/kg, p.o.) had no effect on fever induced by yeast in mice. The alkaloid extract of K. macrophylla prolonged the duration of pentobarbitalinduced sleep in mice. These results suggest that the alkaloid extract of K. macrophylla possesses analgesic action via peripheral pathway but no antipyretic activity

In vivo anti-inflammatory, analgesic and antipyretic activities of novel thiazolidine-2,4-dione analogs derived from some classical NSAIDs

In an attempt to develop selective inhibitors for the cyclooxygenase-2 enzymes as candidates for drugs to treat inflammation and pain, two thiazolidine-2,4-dione analogs were designed and synthesized, (E)-5-(4-isobutylbenzylidene)thiazolidine-2,4-dione (AW 01) and (E)-5-(2-hydroxybenzylidene)thiazolidine-2,4-dione (AW 05). They were synthesized byrefluxing 4-isobutylbenzaldehyde or 2-hydroxybenzaldehyde, respectively in dried toluene, with thiazolidine-2,4-dione, glacialacetic acid and piperidine. The anti-inflammatory activities of AW 01 and AW 05 were investigated in a rat model of acarrageenan-induced paw edema and a croton oil-induced mouse ear edema. The analgesic and antipyretic activities of AW01 and AW 05 were evaluated using the mouse model of acetic acid-induced writhing and in a rat model using yeast-inducedfever, respectively. Oral administration of AW 01 and AW 05 at a dose of 20 mg/kg significantly inhibited the carrageenaninduced rat paw edema. Administration of AW 01 and AW 05 at the higher dose of 40 and 80 mg/kg, also exhibited a significant reduction of paw edema that was similar to the lower dose of 20 mg/kg. When AW 01 or AW 05 was applied topicallyat doses of 0.5, 1.0 and 2.0 mg/ear, it had no significant effect on the mouse ear edema induced by croton oil. An analgesicactivity of AW 01 and AW 05 was observed at a lower dose (10 mg/kg, p.o.) in the acetic acid-induced writhing model. Afteradministration of AW 01 at a dose of 20, 40 and 80 mg/kg, it significantly reduced writhing, compared with the control group.A similar result was also observed after administration of AW 05 at the same dosage range as for AW 01. For the antipyreticactivity, AW 01 and AW 05 at the dose of 10 mg/kg, p.o. reduced rat rectal temperature at all time intervals (1-5 h) in the sameway as did the standard drugs. When using AW 01 and AW 05 at the higher dose of 20, 40 and 80 mg/kg, both compoundssignificantly reduced pyrexia that was similar to the lower administered dose. Both AW 01 and AW 05 demonstrated a similarmagnitude of anti-inflammatory, analgesic and antipyretic effects. The oral LD50 values of AW 01 and AW 05 were 1631 mg/kg and greater than 2000 mg/kg, respectively in mice. These results indicate that AW 01 and AW 05, thiazolidine-2,4-dioneanalogs, possess systemic anti-inflammatory, analgesic as well as antipyretic potentials but have no topical anti-inflammatoryactivity in experimental animal models

ศึกษาฤทธิ์ต้านการอักเสบ ระงับปวด และลดไข้ และความเป็นพิษเฉียบพลันของสารสังเคราะห์ไทเอโซลอะนาล็อกในสัตว์ทดลอง:รายงานการวิจัยฉบับสมบูรณ์

Prince of Songkla Universit

ศึกษาฤทธิ์ต้านการอักเสบ ระงับปวด และลดไข้ และความเป็นพิษเฉียบพลันของสารสังเคราะห์ไทเอโซลอะนาล็อกในสัตว์ทดลอง: รายงานวิจัยฉบับสมบูรณ์

Prince of Songkla Universit

Antipyretic activity of the extracts of Hibiscus sabdariffa calyces L. in experimental animals

The effects of the extracts from Hibiscus sabdariffa calyces L. (H. sabdariffa) on nociceptive response using writhing, hot plate and formalin test in mice and the antipyretic activity in yeast-induced fever in rats, were examined. Anti-inflammatory activity was also investigated on carrageenin-induced paw edema in rats. No acute toxicity was observed in mice after oral administration of the ethanol and aqueous extract of H. sabdariffa calyces at the dose of 15 g/kg. Oral administration of the ethanol extract at the dose of 800 mg/kg significantly decreased the number of contortions and stretchings induced by acetic acid in mice. The aqueous extracts had no effect on this test. Neither the ethanol nor aqueous extract had an effect in the formalin and hot plate tests in mice. The ethanol and the vacuum dried extract of H. sabdariffa calyces (200-800 mg/kg, p.o.) decreased the yeast-induced fever in rats. The H. sabdariffa extract had no effect on carrageenininduced paw edema in rats. These results suggest that the ethanol and aqueous extract (vacuum dry) of H. sabdariffa calyces possess antipyretic action through mechanisms that are different from that of aspirin

พิษเฉียบพลันและพิษกึ่งเรื้อรังของสไปรูไลน่าในสัตว์ทดลอง : รายงานการวิจัยเรื่อง

Prince of Songkla Universit

การพัฒนาตำรับยา tramadol ทางทวารหนัก และประเมินฤทธิ์แก้ปวดในหนูถีบจักรและหนูขาว : รายงานวิจัยฉบับสมบูรณ์

Prince of Songkla Universit

Antinociceptive and antipyretic activities of extracts and fractions from Dracaena loureiri in experimental animals

Dried coarsely powdered material from the stem woods of Dracaena loureiri Gagnep (D loureiri) has extracted with hexane and methanol to give hexane and methanol extracts, respectively. The methanol extract was roughly separated into four fractions. They were methanol, methanol + water, chloroform and ethyl acetate fractions. The effects of the methanol extract, hexane extract, methanol fraction, methanol + water fraction, ethyl acetate fraction and chloroform fraction on nociceptive response using writhing, hot plate and formalin tests in mice and the antipyretic activity in yeast-induced fever in rats, were examined. General behavior was also examined using pentobarbital-induced sleep in mice. The LD5 0 value of intraperitoneally injected the methanol extract, hexane extract, methanol fraction, ethyl acetate fraction and chloroform fraction in mice was 1.67 g/kg, >7 g/kg, 739.73 mg/kg, 489.77 mg/kg and 1.67 g/kg, respectively. Oral administration of the methanol extract and methanol fraction of D. loureiri (100-400 mg/kg) dose de- pendently decreased the number of writhings and stretchings induced by acetic acid and licking activity of the late phase in the formalin test. All extracts or fractions of D. loureiri had no effects on heat-induced pain in mice. Only the methanol fraction of D. loureiri suppressed yeast-induced fever in rats. Neither extracts nor fractions affected paw edema induced by carrageenin in rats. The methanol extract of D. loureiri (100- 400 mg/kg, p.o.) prolonged the duration of pentobarbital-induced sleep in mice. These results suggest that the methanol extract and the methanol fraction of D. loureiri possess analgesic effect. Only the methanol fraction of the extract exhibited antipyretic effect