Triterpenes involved in the anti-inflammatory effect of ethanolic extract of Pterodon emarginatus Vogel stem bark

Bioassay-guided fractionation of the ethanolic extract of Pterodon emarginatus Vogel stem bark (EtEx) resulted in the isolation and characterization of lupeol and betulin. Their structures were elucidated by spectroscopic methods including IR, ¹H-NMR, ¹³C-NMR and comparison with literature values. This study showed the anti-inflammatory activity of EtEx, the hexane (HexL) and dichloromethane (DichL) layers, and lupeol and betulin. The extract, HexL, DichL, lupeol and betulin were able to inhibit acetic acid-induced writhing. In the formalin test, EtEx decreased licking time only in the second phase characterizing anti-inflammatory activity. In the oil-induced ear oedema test, EtEx, lupeol and betulin decrease edema formation. In conclusion, EtEx has antinociceptive effects arising from anti-inflammatory activity; this activity could be due to the presence of lupeol and betulin.     

Analgesic and anti-inflammatory effect of aqueous extract of the stem bark of <Emphasis Type="Italic">Allanblackia gabonensis</Emphasis> (Guttiferae)

Allanblackia gabonensis (Guttiferae) is a plant used in the African traditional medicine as remedies against pain, rheumatism, inflammations. In the present work, the analgesic effect of aqueous extract has been evaluated using acetic acid, formalin, hot-plate test, tail immersion and paw-pressure test. The anti-inflammatory effect of this extract was also investigated on carrageenan, histamine or serotonin induced by paw oedema. Aqueous extract of stem bark of A. gabonensis administrated p.o. showed significant activity against paw oedema induced by carrageenan, with a maximum percentage of inhibition reaching the 74.01% at the preventive test at a dose of 200 mg/kg. A. gabonensis exhibited a significant reduction of paw oedema induced by both histamine and serotonin with a maximal inhibition of 56.94% (200 mg/kg) and 40.83% (100 mg/kg), respectively. It showed significant protective effects against chemical stimuli (acetic acid and formalin) in the mouse. Administered orally at the doses of 100–400 mg/kg, exhibited protective effect of at least 69.78% on the pain induced by acetic acid and also reduced first (67.18% at 200 mg/kg) and second (83.87% at 400 mg/kg) phase of pain-induced par formalin. It also produced a significant increase of the threshold of sensitivity to pressure and hot plate-induced pain in the rats. These results suggest a peripheral and central analgesic activities as well as an anti-inflammatory effect of the stem bark of A. gabonensis.     

Antinociceptive and anti-inflammatory effects of the ethyl acetate stem bark extract of Bridelia scleroneura (Euphorbiaceae)

Bridelia scleroneura is a member of the Euphorbiaceae family. In folk medicine in Cameroon, the stem bark of this plant is used for relieving abdominal pain, contortion, arthritis and inflammation. In this study, the antinociceptive and anti-inflammatory activities of the ethyl acetate stem bark extract have been evaluated. The putative analgesic effect of the plant extract was examined in abdominal constriction, hot plate, formalin and on pain using tail immersion mouse models and in carrageenan-induced paw edema in rats. The extract (150–600 mg/kg) exhibited a dose-dependent analgesic effect (46.27–78.97%) in acetic acid-induced abdominal constriction in mice. B. scleroneura extract increased the pain latency of nociceptive response to thermal stimuli at the higher dose of 600 mg/kg. B. scleroneuna induced significant dose-dependent reduction of the nociception in both early and late phases of the formalin test. The extract at the dose of 300 mg/kg, increased significantly, by 63.70% and 52.01% the tail-immersion latency time, 1 and 2 h post-dosing. In the carrageenan test, B. scleroneura (150–600 mg/kg, p.o) had dose-dependent and significant effects at different time intervals. This behaviour was similar to indometacin (10 mg/kg) used as a standard drug. These results show that the ethyl acetate stem bark extract of B. scleroneura possesses peripheral and central analgesic properties as well as anti-inflammatory activity against acute inflammation processes, in support of the folk medicinal use of the plant.     

Anti-inflammatory and analgesic activities of the latex containing triterpenes from Himatanthus sucuuba

Some triterpenes and iridoids were previously isolated from the stem bark of Himatanthus sucuuba. The latex from Himatanthus sucuuba is used in popular amazonian medicine as an anti-inflammatory remedy. Fractions of the latex were pharmacologically evaluated with a view to verify this popular use in the carrageenan-induced rat paw edema and in the acetic acid-induced mouse constriction tests. The hexane fraction inhibited the edema formation by 35.9% at a dose of 200 mg/kg (p.o.) but no activity was observed at 100 mg/kg (p.o.). The triterpenes present in the hexane fraction were identified as lupeol acetate, alpha-amyrin and lupeol cinnamates. The fraction containing only cinnamates inhibited the edema and the abdominal constrictions by 50-40% and 57.9%, respectively, at 100 mg/kg (p.o.). Among all the fractions studied, the fraction containing only cinnamates showed the greatest anti-inflammatory activity which suggests that these compounds were responsible for the previously described activity of the crude extract.     

In vivo analgesic and anti-inflammatory activities of Rosmarinus officinalis aqueous extracts,rosmarinic acid and its acetyl ester derivative

Abstract

Context: Despite several pharmacological applications of Rosmarinus officinalis L. (Lamiaceae), studies on its analgesic and anti-inflammatory properties have been scarce.

Objective: The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of the aqueous extracts obtained from leaves (AEL) and stems (AES) of Rosmarinus officinalis, as well as its isolated compound – rosmarinic acid (RA). We also prepared and assessed the acetyl ester derivative of RA.

Materials and methods: The analgesic activity was evaluated using abdominal constriction and formalin tests. For the evaluation of the anti-inflammatory effects, carrageenin-induced paw edema in rats were used. The extracts were used at doses of 100, 200 and 400?mg?kg^?1 compounds were tested at 10, 20 and 40?mg?kg^?1.

Results: Orally administered AEL, AES and RA were not significantly active at any of the doses tested during the abdominal constriction test; the acetyl ester derivative of RA displayed significant analgesic activity. In the carrageenin-induced paw edema assay, the acetyl derivative of RA at all the tested doses produced significant anti-inflammatory effects and reduced the number of paw licks in the second phase of the formalin test.

Discussion and conclusion: The results suggest that the analgesic effects of the acetyl derivative of RA operate via a peripheral-mediated mechanism. The acetyl ester derivative of RA is potentially applicable as a new lead compound for the management of pain and inflammation.     

镰形棘豆总提取物的镇痛抗炎作用

目的研究藏药镰形棘豆总提取物的镇痛抗炎活性。方法使用小鼠扭体法和热板法观察镰形棘豆总提取物的镇痛效应,确定镇痛类型;采用小鼠耳廓肿胀法和大鼠棉球肉芽肿胀法观察镰形棘豆总提取物的抗炎效应。结果镰形棘豆总提取物经灌胃给药可明显减少由醋酸引起的小鼠扭体次数(P<0.05),但是不能明显提高小鼠热刺激的痛反应时间;可明显减轻二甲苯致小鼠耳廓肿胀程度和模型大鼠肉芽组织的增生。结论镰形棘豆具有良好的外周镇痛活性和抗炎活性。     

Antinociceptive effect of Lafoensia pacari A. St.-Hil. independent of anti-inflammatory activity of ellagic acid

This study was performed to determine the antinociceptive and anti-inflammatory activities of ethanolic extract of Lafoensia pacari A. St.-Hil. (PEtExt) stem bark and its fractions using various animal models such as acetic acid-induced abdominal writhing, formalin-induced pain and croton oil-induced ear edema tests. The PEtExt inhibited the acetic acid-induced abdominal writhing, reduced the pain reaction time on both phases of the formalin test and decreased the edema in a dose-dependent manner. Pre-treatment with naloxone did not reverse the antinociceptive effect. Only the ethyl acetate fraction showed antinociceptive and anti-inflammatory effects. Our results also showed that this extract contains compounds with analgesic action independent of anti-inflammatory activity.     

Evaluation of anti-inflammatory activity of chloroform extract of Bryonia laciniosa in experimental animal models

The anti-inflammatory effect of the leaves of Bryonia laciniosa was evaluated using carrageenan, dextran, histamine, serotonin induced rat paw oedema and cotton pellet induced granuloma (chronic) models in rats. In mice, carrageenan peritonitis test was performed for the extract by oral administration. The chloroform extract of Bryonia laciniosa (CEBL) exhibited significant anti-inflammatory effect at the dose 50, 100 and 200 mg/kg. Maximum inhibition (52.4%) was noted at the dose of 200 mg/kg after 3 h of drug treatment in carrageenan induced paw oedema, whereas the indomethacin (standard drug) produced 62.1% of inhibition. The extract exhibited significant anti-inflammatory activity in dextran induced paw oedema in a dose dependent manner. The extract also exhibited significant inhibition on the hind paw oedema in rats caused by histamine and serotonin respectively. In the chronic model (cotton pellet induced granuloma) the CEBL (200 mg/kg) and standard drug showed decreased formation of granuloma tissue by 50.1 and 57.3% (p<0.001) respectively. The extract also inhibited peritoneal leukocyte migration in mice. Thus, the present study revealed that the chloroform extract of Bryonia laciniosa exhibited significant anti-inflammatory activity in the tested models.     

Free radical scavengers,anti-inflammatory and analgesic activity of Acaena magellanica

Extracts of the whole plant Acaena magellanica (Rosaceae) were assessed for anti-inflammatory, antipyretic and analgesic activity in animal models. At 600 mg kg(-1), the global ethanolic extract (GEE), dichloromethane (DCM) and defatted methanol (MeOH) fractions showed a mild anti-inflammatory effect in the carrageenan-induced guinea-pig paw oedema. The GEE, DCM and defatted MeOH fractions significantly reduced inflammation by 43.2, 40.5 and 42.1%, respectively. The GEE did not showed any significant antipyretic activity in doses up to 600 mg kg(-1). A 20% w/v infusion administered orally at 16 mL kg(-1) presented analgesic effect in the acetic acid-induced abdominal constriction test in mice. The GEE and MeOH extract of A. magellanica showed free radical scavenging activity in the diphenylpicrylhydrazyl decolouration assay. Assay-guided isolation led to quercetin, Q-3-O-beta-glucoside, Q-3-O-beta-D-galactoside, ellagic acid and catechin as the free radical scavengers. The saponins tormentic acid 28-O-beta-D-galactopyranoside and 28-O-beta-D-glucopyranoside were isolated from the polar extract. The structures were determined by spectroscopic methods.     

Evaluation of analgesic and anti-inflammatory activities of Nectandra megapotamica (Lauraceae) in mice and rats

The bioactivity-guided phytochemical investigation of the crude hydralcoholic extract of Nectandra megapotamica was carried out using the abdominal constriction test in mice, which led to the isolation of three active compounds: alpha-asarone (1), galgravin (2) and veraguensin (3). The crude extract (EBCA, 300 mg kg(-1)) and isolated compounds 1,2, and 3, at different doses, were evaluated using the acetic acid-induced abdominal constriction test in mice, carrageenan-induced paw oedema in rats, and hot plate tests in rats. The EBCA showed a significant effect in the abdominal constriction and hot plate tests, but did not show activity in the rat paw oedema assay. All isolated compounds displayed activity in the abdominal constriction test, but only compound 1 was active in the hot plate test. Compounds 2 and 3 displayed activity in the anti-inflammatory assay. It was suggested that the analgesic effects obtained for EBCA could be due mainly to the presence of its major compound, alpha-asarone (1).     

Evaluation of the anti-inflammatory and analgesic properties of the extract of Russelia equisetiformis (Schlecht &; Cham) Scrophulariacae

A methanolic extract of Russelia equisetiformis whole plant was studied for anti-inflammatory and analgesic activities in rats and mice using carrageenan-induced rat paw oedema, aceticacid-induced writhing and tail-flick test. The extract, at 10, 20 and 40 mg/kg, significantly (P <0.05) inhibited carrageenan-induced oedema in rats. Abdominal constriction induced by acetic acid was also inhibited by the extract, within the same dose range. The extract at the same dose also prolonged the latency period in the tail-flick response test, which was reverted by naloxone. The results suggested that the extract possesses potential anti-inflammatory and analgesic properties.     

Anti-inflammatory and antinociceptive properties of blueberry extract (Vaccinium corymbosum)

Blueberries are among the edible fruits that are recognized best for their potential health benefits. The crude extract from Vaccinium corymbosum was assessed in anti-inflammatory and antinociceptive models. The crude hydroalcoholic extract was administered orally at doses of 100, 200 or 300 mg kg (-1) for all the assays. In the carrageenan test, the crude extract reduced rat paw oedema by 9.8, 28.5 and 65.9%, respectively. For the histamine assay, the reductions of oedema were 70.1, 71.7 and 81.9%, respectively. In the myeloperoxidase (MPO) assay, 300 mg kg (-1) crude extract produced a significant inhibition of the MPO activity, at 6 h and 24 h after injection of carrageenan, by 42.8 and 46.2%, respectively. With the granulomatous tissue assay dexamethasone displayed significant activity, whereas the blueberry extract was inactive. For the abdominal constriction test, inhibitions of 49.0, 54.5, 53.5%, respectively, were observed for the crude extract, and 61.4% for indometacin. In the formalin test, the crude extract (200 and 300 mg kg (-1)) and indometacin inhibited only the second phase by 36.2, 35.3 and 45.8%, respectively. Considering that the crude extract of blueberry displayed antinociceptive and anti-inflammatory activity, its consumption may be helpful for the treatment of inflammatory disorders.     

Inhibitory role of Syzygium cumini on autacoid-induced inflammation in rats

The ethanolic extract of Syzygium cumini bark has been reported to possess anti-inflammatory activity in our previous studies. The present study is an attempt to elucidate the anti-inflammatory activity of S. Cumini bark against inflammation induced by individual autacoid insult. Histamine (1 mg/ml), 5-HT (1 mg/ml), bradykinin (0.02 mg/ml) and PGE2 (0.001 mg/ml) were used as inflammogens. One of these agents (0.1 ml) was injected s.c. into the right hind paw of each rat. The ethanolic extract of S. cumini bark was tested at the doses of 100, 300 and 1000 mg/kg, p.o. The results indicated the anti-inflammatory activity of S. cumini bark in histamine, 5-HT and PGE2-induced rat paw oedema. However, there was no such significant inhibition of oedema volume observed in bradykinin-induced rat paw oedema at any dose level. Thus, it is concluded that S. cumini exhibits inhibitory role on inflammatory response to histamine, 5-HT and PGE2.     

Preventive Effects of Unsei-in and Oren-gedoku-to,Chinese Traditional Medicines,Against Rat Paw Oedema and Abdominal Constriction in Mice

Oren-gedoku-to and Unsei-in are complex mixtures of ingredients derived from plants. These two drugs are clinically most frequently used in the treatment of Behçet's disease, we have investigated the anti-inflammatory and analgesic actions of Oren-gedoku-to and Unsei-in using a battery of tests; rat paw oedema induced by five different agents; abdominal constriction; mouse ear swelling; and dye leakage tests, designed to clarify the therapeutic potential of these medicines. The findings in this study that these medicines are able to inhibit the rat paw oedema, suppress the abdominal constriction and inhibit the increased dye permeability confirm the analgesic and anti-inflammatory effects of these compounds. From these results there seems a clear rationale for exploring the effectiveness of these Chinese medicines in the treatment øf chronic and acute inflammatory diseases.     

Anti-inflammatory and analgesic effects of 6α,7β–dihydroxy-vouacapan-17β-oic acid isolated from <Emphasis Type="Italic">Pterodon emarginatus</Emphasis> Vog. fruits

6α,7β-dihydroxy-vouacapan-17β-oic (tricyclic furanoid diterpene; DHVO) acid was isolated from the hexane extract of Pterodon emarginatus fruits and evaluated for anti-inflammatory and analgesic effects using an assay that induces paw oedema with carrageenan, dextran and prostaglandin E₂ (PGE₂) in rats and the writhing and formalin tests in mice. Oral administration of 50 mg/kg DHVO significantly inhibited carrageenan-induced oedema formation by 24% (p < 0.05). This treatment did not inhibit dextran-induced oedema but was effective when the inflammatory effect was triggered by PGE₂, inhibiting oedema formation by 39% (p < 0.05). In the writhing test, doses of 50, 200 and 400 mg/kg resulted in a dose-dependent effect with a correlation coefficient (r) of 0.983 (F = 29.04, ANOVA). Doses of 50 and 100 mg/kg inhibited both the neurogenic and inflammatory phases (p < 0.05) in the formalin test but were not effective for increasing the lag time in the hot plate test. Together, these results suggest that DHVO has both anti-inflammatory and peripheral analgesic effects.     

Anti-inflammatory and gastromucosal protective effects of Calotropis procera (Asclepiadaceae) stem bark

This study was aimed at evaluating the anti-inflammatory and gastromucosal protective effect of chloroform extract (CH) and hydroalcoholic extract (HE) of the stem bark of Calotropis procera obtained successively by cold maceration. The anti-inflammatory effect of the CH and HE extracts of the stem bark of Calotropis procera against carrageenan-induced paw oedema and also its gastromucosal protective effect has been studied by using two acute models: aspirin (100 mg/kg, p.o.) and ethanol (96%) in albino rats. CH and HE extracts showed significant anti-inflammatory activity at 200 and 400 mg/kg, while CH extract at 400 mg/kg was also found to have a significant gastromucosal protective effect. As part of investigations to obtain compounds with anti-inflammatory and gastromucosal protective effects in this work, a bioassay was carried out with fractions obtained from the CH extract with n-hexane (NF1), 1-butanol (BF1), ethyl acetate (EF1) and chloroform (CF1). The HE extract of the stem bark was fractionated with n-hexane (NF2), 1-butanol (BF2), ethyl acetate (EF2), chloroform (CF2) and water (WF2). The fractions were evaluated for their anti-inflammatory and gastromucosal protective effects. Fractions NF1, CF1, BF2 and EF2 (20 mg/kg) showed significant anti-inflammatory activity, while NF1 and BF2 (20 mg/kg) also showed gastromucosal protective effects. The results obtained for gastromucosal protective effects were also well supported by histopathological examination of the open excised rat stomach.     

Anti-inflammatory, analgesic and antipyretic effects of friedelin isolated from Azima tetracantha Lam. in mouse and rat models

Objectives Friedelin was isolated from Azima tetracantha Lam. leaves collected from Kallakurichi, Villuppuram district, Tamil Nadu, India. The anti‐inflammatory, analgesic and antipyretic activities of friedelin have been investigated in Wistar rats and mice. Methods Friedelin was isolated from the hexane extract of leaves of A. tetracantha using column chromatography. The effects of friedelin on inflammation were studied by using carrageenan‐induced hind paw oedema, croton oil‐induced ear oedema, acetic acid‐induced vascular permeability, cotton pellet‐induced granuloma and adjuvant‐induced arthritis. The analgesic effect of friedelin was evaluated using the acetic acid‐induced abdominal constriction response, formalin‐induced paw licking response and the hot‐plate test. The antipyretic effect of friedelin was evaluated using the yeast‐induced hyperthermia test in rats. Key findings In the acute phase of inflammation, maximum inhibitions of 52.5 and 68.7% (P < 0.05) were noted with 40 mg/kg friedelin in carrageenan‐induced paw oedema and croton oil‐induced ear oedema, respectively. Administration of friedelin (40 mg/kg) significantly (P < 0.05) decreased the formation of granuloma tissue induced by cotton pellet at a rate of 36.3%. In the adjuvant‐induced arthritis test friedelin inhibited 54.5% of paw thickness. Friedelin inhibited acetic acid‐induced vascular permeability in mice. Friedelin also produced significant (P < 0.05) analgesic activity in the acetic acid‐induced abdominal constriction response and formalin‐induced paw licking response. In the hot‐plate test, friedelin did not show any significant results when compared with control. Treatment with friedelin showed a significant (P < 0.05) dose‐dependent reduction in pyrexia in rats. Conclusions The results suggested that friedelin possessed potent anti‐inflammatory, analgesic and antipyretic activities.     

Antinociceptive and anti-inflammatory activities of sulphated polysaccharides from the red seaweed Gracilaria cornea

Seaweeds have attracted special interest as good sources of sulphated polysaccharides (SP) for use in pharmaceutical industries and biotechnology. In this study, we evaluated the effects of SP from the red seaweed Gracilaria cornea (Gc-TSP) in nociceptive and inflammatory models. In mice, Gc-TSP (3, 9 or 27 mg/kg) significantly reduced nociceptive responses, as measured by the number of writhes, at all tested doses. In a formalin test, Gc-TSP significantly reduced licking time in both phases of the test at a dose of 27 mg/kg. In a hot-plate test, the antinociceptive effect was observed only in animals treated with 27 mg/kg of Gc-TSP, suggesting that the analgesic effect occurs through a central action mechanism at the highest dose. Gc-TSP (3, 9 or 27 mg/kg) caused only a slight reduction in neutrophil migration in the rat peritoneal cavity. However, lower doses of Gc-TSP (3 and 9 mg/kg) significantly inhibited paw oedema induced by carrageenan, especially at 3 hr after treatment. Reduction in oedema was confirmed by myeloperoxidase activity in the affected paw tissue. In addition, treatment (s.c.) of animals with different doses of Gc-TSP inhibited paw oedema induced by dextran within the first hour in all doses tested. After 14 consecutive days of intraperitoneal administration of Gc-TSP (9 mg/kg), we measured the wet weight of the liver, kidney, heart, spleen and thymus and performed biochemical, haematological and histopathological evaluations. No systemic damage was found. These results indicate that Gc-TSP possesses analgesic and anti-inflammatory effects and is a potentially important tool worthy of further study.     

Anti-inflammatory properties of extracts, fractions and lignans isolated from Phyllanthus amarus

This study assessed the anti-inflammatory effect of the extracts and purified lignans obtained from Phyllanthus amarus. Given orally, the hexane extract (HE), the lignan-rich fraction (LRF), or the lignans phyltetralin, nirtetralin, niranthin, but not hypophyllanthin or phyllanthin, inhibited carrageenan (Cg)-induced paw oedema and neutrophil influx. The HE, the LRF or nirtetralin also inhibited the increase of IL1-beta tissue levels induced by Cg. Furthermore, bradykinin (BK)-, platelet activating factor (PAF)- and endothelin-1 (ET-1)-induced paw oedema were significantly inhibited by the HE or LRF while histamine- and substance P-induced paw oedema were unaffected. Finally, nirtetralin or phyltetralin caused inhibition of paw oedema induced by PAF or ET-1. These results show that the HE, the LRF and the lignans niranthin, phyltetralin and nirtetralin exhibited marked anti-inflammatory properties and suggest that these lignans seem to be the main active principles responsible for the anti-inflammatory properties reported for the HE of P. amarus.     

Anti-inflammatory and analgesic activities of the aqueous extract of Acacia karroo stem bark in experimental animals

The aqueous extract of the stem bark of Acacia karroo Hayne was investigated for its anti-inflammatory and analgesic activities in animal models. The extract at 100 and 200 mg/kg reduced significantly the formation of oedema induced by carrageenan and histamine. In the acetic acid-induced writhing model, the extract showed a good analgesic effect characterized by a significant reduction in the number of writhes with two doses (100 and 200 mg/kg) used when compared to the untreated control group. In the tail immersion test, the extract at the doses used (100 and 200 mg/kg) increased reaction time to pain after 30 min. of oral administration of the extract. Indomethacin at 10 mg/kg served as reference drug in all these tests. The results gave a scientific basis to the traditional uses of Acacia karroo mainly for wound poultices, eye treatments and cold remedies.