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ABSTRACT: The present study examined the potential antinociceptive activity of flavokawin B (6'-hydroxy-2',4'-dimethoxychalcone), a synthetic chalcone using chemical- and thermal-induced nociception models in mice. It was demonstrated that flavokawin B (FKB; 0.3, 1, 3 and 10 mg/kg) administered via both oral (p.o.) and intraperitoneal (i.p.) routes produced significant and dose-dependent inhibition in the abdominal constrictions induced by acetic acid, with the i.p. route producing antinociception of approximately 7-fold more potent than the p.o. route. It was also demonstrated that FKB produced significant inhibition in the two phases of the formalin-induced paw licking test. In addition, the same treatment of flavokawin B (FKB) exhibited significant inhibition of the neurogenic nociceptive induced by intraplantar injections of glutamate and capsaicin. Likewise, this compound also induced a significant increase in the response latency period to thermal stimuli in the hot plate test and its antinociceptive effect was not related to muscle relaxant or sedative action. Moreover, the antinociception effect of the FKB in the formalin-induced paw licking test and the hot plate test was not affected by pretreatment of non-selective opioid receptor antagonist, naloxone. The present results indicate that FKB produced pronounced antinociception effect against both chemical and thermal models of pain in mice that exhibited both peripheral and central analgesic activity.
European journal of pharmacology 11/2010; 647(1-3):103-9. · 2.59 Impact Factor
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ABSTRACT: The anti-inflammatory activity of zerumbone (1), a natural cyclic sesquiterpene isolated from Zingiber zerumbet Smith was investigated using carrageenan-induced paw edema and cotton pellet-induced granuloma tissue formation test in mice. It was demonstrated that intraperitoneal administration of 1 at a dose of 5, 10, 50 and 100 mg/kg produced significant dose-dependent inhibition of paw edema induced by carrageenan. It was also demonstrated that 1 at similar doses significantly suppressed granulomatous tissue formation in cotton pellet-induced granuloma test.
Fitoterapia 10/2010; 81(7):855-8. · 1.85 Impact Factor
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ABSTRACT: Alpinia conchigera Griff. (Zingiberaceae), locally known to the Malays as "lengkuas ranting", is native to Peninsular Malaysia. The Malays traditionally used it to treat infection and rashes, and as a health drink. This study evaluated the analgesic and anti-inflammatory activities of the ethanol extract of A. conchigera rhizomes in mice and rats, respectively. The analgesic activity was elucidated using the acetic acid-induced writhing test, hot plate test, and formalin test, while the anti-inflammatory activity was determined using carrageenan-induced paw edema. The extract (30, 100, and 300 mg/kg) given intraperitoneally (i.p.) exhibited antinociceptive and anti-inflammatory activities in all tests used. The range of percentage of analgesia obtained for all doses of extract in the writhing test was 50-92%, and in the early and late phases of the formalin test was 25-62% and 63-98%, respectively. In addition, naloxone (5 mg/kg) given subcutaneously (s.c.) was found to reverse the extract (300 mg/kg)-induced antinociceptive activity in the writhing, hot plate, and formalin tests. Based on the results obtained, it can be concluded that the ethanol extract of A. conchigera rhizomes possessed a peripheral and central antinociceptive activity that was mediated, in part, via the opioid receptor, as well as anti-inflammatory activity.
Pharmaceutical Biology 08/2010; 48(8):861-8. · 0.88 Impact Factor
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ABSTRACT: In a previous communication we showed that atrovirinone, a 1,4-benzoquinone isolated from the roots of Garcinia atroviridis, was able to inhibit several major proinflammatory mediators of inflammation. In this report we show that atrovirinone inhibits NO and PGE(2) synthesis through inhibition of iNOS and COX-2 expression. We also show that atrovirinone inhibits the secretion of IL-1beta and IL-6 in a dose dependent fashion whereas the secretion of IL-10, the anti-inflammatory cytokine, was enhanced. Subsequently we determined that the inhibition of proinflammatory cytokine synthesis and inducible enzyme expression was due to a dose-dependent inhibition of phosphorylation of p38 and ERK1/2. We also showed that atrovirinone prevented phosphorylation of I-kappaBalpha, which resulted in a reduction of p65NF-kappaB nuclear translocation as demonstrated by expression analysis. We conclude that atrovirinone is a potential anti-inflammatory drug lead that targets both the MAPK and NF-kappaB pathway.
Phytomedicine: international journal of phytotherapy and phytopharmacology 04/2010; 17(10):732-9. · 2.17 Impact Factor
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ABSTRACT: Piper sarmentosum (Piperaceae) is a medicinal plant traditionally used by the Malays to treat headaches, toothaches, coughs, asthma and fever.
In order to establish the pharmacological properties of the leaf of this plant, studies were performed on anti-nociceptive and anti-inflammatory activities.
The aqueous extract of Piper sarmentosum (AEPS) was prepared in the doses of 30, 100 and 300 mg/kg. Anti-nociceptive activity of AEPS was evaluated by abdominal constriction and hot-plate tests. AEPS was also pre-challenged with 5mg/kg naloxone to determine the involvement of opioid receptors. Anti-inflammatory activity was evaluated using carrageenan-induced paw edema assay.
Subcutaneous administration of AEPS exhibited anti-nociceptive activity (P<0.05) in a dose-dependent manner in the abdominal constriction and hot-plate tests. Pre-treatment with naloxone completely (P<0.05) diminished the extract anti-nociceptive activity in both tests. The AEPS, at all doses used, exerted significant (P<0.05) anti-inflammatory activity in a dose-dependent manner.
The AEPS exhibits opioid-mediated anti-nociceptive activity at the peripheral and central levels, as well as anti-inflammatory activity, which confirmed the traditional uses of the plant in the treatment of pain- and inflammatory-related ailments.
Journal of ethnopharmacology 03/2010; 128(1):42-8. · 2.32 Impact Factor
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ABSTRACT: Objective: The present study was carried out to determine the antiinflammatory and antinociceptive activities of a methanol extract of Zingiber zerumbet rhizomes (MEZZ) using various experimental model systems.
The MEZZ was prepared by macerating oven-dried (50 degrees C) powdered rhizomes (1.2 kg) of Z. zerumbet in 80% methanol in a ratio of 1:20 (w/v) for 48 h. The supernatant was collected, filtered and evaporated to dryness under reduced pressure (50 degrees C) yielding approximately 21.0 g of the crude dried extract. The crude dried extract was stored at -20 degrees C prior to use and was dissolved in normal saline (0.9% NaCl) immediately before administration at concentrations required to produce doses of 25, 50 and 100 mg/kg.
All dosages of MEZZ showed significant (p < 0.05) antiedema activity when assessed using the carrageenan-induced paw edema test and the cotton-pellet-induced granuloma test. The MEZZ exhibited significant (p < 0.05) antinociceptive activity when assessed by the writhing, hot plate and formalin tests. Pretreatment with naloxone (5 mg/kg) significantly decreased the latency of discomfort produced by the 100 mg/kg dose of MEZZ in the hot plate test.
MEZZ produced antiinflammatory and antinociceptive activities which may involve the inhibition of bradykinin-, prostaglandin-, histamine- and opioid-mediated processes.
Medical Principles and Practice 01/2010; 19(4):287-94. · 0.89 Impact Factor
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ABSTRACT: To study the effects of Tamarindus indica L. aqueous fruit extract on the antinociceptive activities in rodent models.
The analgesic effect was evaluated using acetic acid-induced writhing, hot plate and formalin tests.
The extract (60-600 mg/kg) significantly (p < 0.05) inhibited the writhing test in a dose-dependent manner with the percentage of analgesia recorded between 51.8 and 74.1%. In addition, the extract also significantly (p < 0.05) increased the latency time in the hot plate test in a dose-dependent manner. Further study showed that the extract elicited inhibitory activity in both the early and late phases of the formalin test. Moreover, pretreatment with 5 mg/kg naloxone, a nonselective opioid receptor antagonist, significantly (p < 0.05) modified the antinociceptive effect of the extract in all tests.
The aqueous extract of T. indica possesses potential antinociceptive activity at both the peripheral and central levels, which are mediated via activation of the opioidergic mechanism.
Medical Principles and Practice 01/2010; 19(4):255-9. · 0.89 Impact Factor
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ABSTRACT: The ethanolic extract of Alpinia conchigera Griff. leaves (EACL) was evaluated for its antinociceptive and anti-inflammatory activities in several in vivo experimental models. Antinociceptive activity was determined using the acetic acid-induced abdominal writhing test, the hot plate test and the formalin test. Anti-inflammatory activity was determined using the carrageenan-induced paw edema test. The extract (30, 100 and 300 mg/kg i.p.) was found to possess significant, dose-dependent inhibitory activity in all test models. In addition, the antinociceptive effect of the extract in the acetic acid-induced writhing and hot plate tests was reversed by naloxone, suggesting that this activity is mediated through activation of the opioid system. These findings suggest that EACL presents notable analgesic and anti-inflammatory activities, which support its folkloric use for painful and inflammatory conditions.
Methods and Findings in Experimental and Clinical Pharmacology 06/2009; 31(4):241-7. · 0.93 Impact Factor
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ABSTRACT: We have investigated the antinociceptive activity of zerumbone (1), a natural cyclic sesquiterpene isolated from Zingiber zerumbet Smith, in acetic acid-induced abdominal writhing test and hot plate test in mice. 1 given by intraperitoneal route produced significant dose-dependent antinociceptive effect in all the test models used. In addition, the antinociceptive effect of 1 in the hot plate test was reversed by the non-selective opioid receptor antagonist naloxone, suggesting that the opioid system is involved in its analgesic mechanism of action.
Fitoterapia 03/2009; 80(4):230-2. · 1.85 Impact Factor
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ABSTRACT: Moringa oleifera L. (Moringaceae) is known to possess high nutritional value and is used in a folklore medicine to treat various ailments related to pain and inflammation. The aim of the present study was to evaluate the antinociceptive and anti-inflammatory effects of the aqueous extract of the leaves of M. oleifera in laboratory animals, using the writhing, hot-plate and formalin tests as the antinociceptive assays, and carrageenan-induced paw edema test as the anti-inflammatory assay. The extract (10, 30 and 100 mg/kg) exhibited significant (P < 0.05) antinociceptive activity, which occurred in a dose-dependent manner, in all tests used. The extract also exhibited significant (P < 0.05) anti-inflammatory activity in a dose-dependent manner. Furthermore, the extract antinociceptive activity was suggested to be modulated via opioid receptors at the central, but not peripheral, antinociceptive level, based on the ability of 5 mg/kg naloxone to reverse the extract activity in the hot-plate, but not the writhing test. In conclusion, M. oleifera leaves possess peripherally non-opioid mediated and centrally opioid mediated antinociceptive and anti-inflammatory activities. This study also confirms the traditional uses of M. oleifera in the treatment of ailments, particularly those related to pain and inflammation.
01/2009; 46(12):838-845.
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ABSTRACT: To determine the anti-inflammatory and antinociceptive activities of Mitragyna speciosa Korth methanol extract in rodents. Materials and
Anti-inflammatory activity was evaluated using carrageenan-induced paw edema and cotton pellet-induced granuloma tests in rats. Antinociceptive activity was measured using the writhing test and the hot plate test in mice, and the formalin test in rats. All drugs and extracts were diluted in dH(2)O and administered through the intraperitoneal route. Results were analyzed using one-way ANOVA followed by Dunnett's test for multiple comparisons among groups.
Results showed that intraperitoneal administration of the extract at doses of 100 and 200 mg/kg produced significant dose-dependent activity in all of the nociceptive models evaluated (p < 0.05). With the formalin test, the antinociceptive activity in mice was inhibited only at the highest dose of the extract (200 mg/kg). The study also showed that intraperitoneal administration of the methanol extract of M. speciosa (100 and 200 mg/kg) significantly and dose-dependently suppressed the development of carrageenan-induced rat paw edema (p < 0.05). In the chronic test, however, significant reduction in granulomatous tissue formation in rats was observed only at the highest dose of the methanol extract of M. speciosa (200 mg/kg, p < 0.05).
The present study suggests the presence of potent antinociceptive and anti-inflammatory principles in the extract, supporting its folkloric use for the treatment of these conditions.
Medical Principles and Practice 01/2009; 18(5):378-84. · 0.89 Impact Factor
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ABSTRACT: The present study was carried out to explore the antinociceptive as well as the anti-inflammatory effects of an ethanol extract of Stachytarpheta jamaicensis (L.) Vahl (EESJ) using 3 models of nociception and 2 models of inflammation in experimental animals.
EESJ was prepared by overnight soaking of the oven-dried (50 degrees C; 72 h) ground leaves (500 g) in 80% ethanol (1:5; w/v). The filtrate was evaporated to dryness (50 degrees C), resuspended in distilled water at concentrations to provide the desired doses of 50, 100 and 150 mg/kg. For antinociceptive effects, 3 models were used: acetic acid-induced abdominal writhing, hot-plate- and formalin-induced paw-licking tests; for anti-inflammatory effects, 2 models were used--carrageenan-induced paw edema and cotton-pellet-induced granuloma tests. Appropriate doses were administered intraperitoneally (i.p.) to mice/rats prior to each test. The mechanisms of antinociceptive action of the extract were also investigated by pretreatment with naloxone (5 mg/kg, i.p.).
The extract exhibited significant (p < 0.05) antinociceptive activity in all nociceptive models tested with dose-dependent activity observed using the abdominal writhing and formalin tests. Pretreatment with naloxone partially, but significantly (p < 0.05) reversed the antinociceptive activity of the extract when assessed using the abdominal-writhing- and formalin-induced paw-licking tests, and completely inhibited its activity when the hot-plate test was used. The extract also showed significant (p < 0.05) anti-inflammatory activity in both the acute (carrageenan-induced paw edema test) and the chronic (cotton-pellet granuloma test) tests.
This study showed the potential of EESJ to exert antinociceptive and anti-inflammatory activities, the former being modulated via peripheral and central mechanisms and involving, in part, activation of the opioid receptor system.
Medical Principles and Practice 01/2009; 18(4):272-9. · 0.89 Impact Factor
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ABSTRACT: The aqueous extract of Ficus deltoidea leaves was evaluated for possible antinociceptive activity in three models of nociception, namely, acetic acid-induced abdominal writhing, formalin and hot plate test. The results of the present study showed that intraperitoneal administration of the F. deltoidea leaves aqueous extract at the dose of 1, 50 and 100 mg/kg, 30 min prior to pain induction produced significant dose-dependent antinociceptive effect in all the models used, which indicating the presence of both central and peripherally mediated activities. Furthermore, the antinociceptive effect of the extract in the formalin and hot plate test was reversed by the non-selective opioid receptor antagonist naloxone suggesting that the endogenous opioid system is involved in its analgesic mechanism of action. Thus, the present results demonstrated that F. deltoidea leaves aqueous extract contains pharmacologically active constituents which possess antinociceptive activity justifying its popular therapeutic use in treating conditions associated with the painful conditions.
Fitoterapia 08/2008; 79(7-8):557-61. · 1.85 Impact Factor
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ABSTRACT: Cardamonin, a chalcone isolated from the fruits of a local plant Alpinia rafflesiana, has demonstrated anti-inflammatory activity in cellular models of inflammation. In this report, we evaluated the ability of cardamonin to suppress both NO and PGE2 synthesis, iNOS and COX-2 expression and enzymatic activity, and key molecules in the NF-kappaB pathway in order to determine its molecular target. Cardamonin suppressed the production of NO and PGE2 in interferon-gamma (IFN-gamma)- and lipopolysaccharide (LPS)-induced RAW 264.7 cells. This inhibition was demonstrated to be caused by a dose-dependent down-regulation of both inducible enzymes, iNOS and COX-2, without direct effect upon iNOS or COX-2 enzyme activity. Subsequently we determined that the inhibition of inducible enzyme expression was due to a dose-dependent inhibition of phosphorylation and degradation of I-kappaBalpha, which resulted in a reduction of p65NF-kappaB nuclear translocation. We conclude that cardamonin is a potential anti-inflammatory drug lead that targets the NF-kappaB pathway.
Molecular Immunology 03/2007; 44(5):673-9. · 2.90 Impact Factor
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ABSTRACT: The leaves of Melicope ptelefolia (Rutaceae) afforded a new acetophenone named 2,4,6-trihydroxy-3-geranylacetophenone. The structure of the compound was established by mass and NMR spectroscopy.
Natural Product Research 06/2006; 20(5):415-9. · 1.01 Impact Factor
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ABSTRACT: Itraconazole and fluconazole are potent wide spectrum antifungal drugs. Both of these drugs induce hepatotoxicity clinically. The mechanism underlying the hepatotoxicity is unknown. The purpose of this study was to investigate the role of phenobarbital (PB), an inducer of cytochrome P450 (CYP), and SKF 525A, an inhibitor of CYP, in the mechanism of hepatotoxicity induced by these two drugs in vivo. Rats were pretreated with PB (75 mg/kg for 4 days) prior to itraconazole or fluconazole dosing (20 and 200 mg/kg for 4 days). In the inhibition study, for 4 consecutive days, rats were pretreated with SKF 525A (50 mg/kg) or saline followed by itraconazole or fluconazole (20 and 200 mg/kg) Dose-dependent increases in plasma alanine aminotransferase (ALT), gamma-glutamyl transferase (gamma-GT), and alkaline phosphatase (ALP) activities and in liver weight were detected in rats receiving itraconazole treatment. Interestingly, pretreatment with PB prior to itraconazole reduced the ALT and gamma-GT activities and the liver weight of rats. No changes were observed in rats treated with fluconazole. Pretreatment with SKF 525A induced more severe hepatotoxicity for both itraconazole and fluconazole. CYP 3A activity was inhibited dose-dependently by itraconazole treatment. Itraconazole had no effects on the activity of CYP 1A and 2E. Fluconazole potently inhibited all three isoenzymes of CYP. PB plays a role in hepatoprotection to itraconazole-induced but not fluconazole-induced hepatotoxicity. SKF 525A enhanced the hepatotoxicity of both antifungal drugs in vivo. Therefore, it can be concluded that inhibition of CYP may play a key role in the mechanism of hepatotoxicity induced by itraconazole and fluconazole.
Drug and Chemical Toxicology 02/2006; 29(3):237-53. · 1.08 Impact Factor
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ABSTRACT: The current study was designed to evaluate whether compounds
isolated from local medicinal plants in Malaysia
suppressed nitric oxide (NO) production in inflammation.
The murine monocytic macrophage (RAW
264.7) cell line was used as a target cell and activated
by interferon-c (IFN-c) and lipopolysaccharide (LPS).
Our current study has identified four phytochemicals,
namely atrovirinone, cardamonin, flavokawin B, and
zerumbone, that inhibit pathological NO generation.
These compounds are candidates for further bioassay
studies to determine their suitability as drug leads.
Pharmaceutical Biology 01/2006; 44(1):50-59. · 0.88 Impact Factor
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ABSTRACT: The antinociceptive effect of the ethanolic extract of Melastoma malabathricum (MME) was investigated using acetic acid-induced abdominal writhing test and hot-plate test in mice. It was demonstrated that the extract (30-300 mg/kg, i.p.) strongly and dose-dependently inhibited the acetic acid-induced writhing with an ED(50) of 100 (78-160) mg/kg i.p. It also significantly increased the response latency period to thermal stimuli. Furthermore, the nonselective opioid receptor antagonist, naloxone blocked the antinociceptive effect of the extract in both tests, suggesting that M. malabathricum may act both at peripheral and central levels.
Fitoterapia 01/2005; 75(7-8):667-72. · 1.85 Impact Factor
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ABSTRACT: An experiment was conducted with the objective to enhance mucosal immunity against ovalbumin (OVA) by co-administration of OVA with an aqueous extract from the fruit of Solanum torvum (STE). Five groups of female ICR mice aged approximately 8 weeks at the commencement of the experiment were caged in groups of eight and received various treatments. The treatments included OVA alone, OVA with cholera toxin (CT), and OVA with various doses of STE. Mice were primed intraperitoneally with 500 microg of OVA alone or co-administered with 0.1 microg CT, or with 1 microg STE. All mice were boosted orally via gastric intubation 14 days after priming with 10 mg OVA alone, or co-administered with 10 microg CT or with 10 mg, 1 mg or 0.1 mg STE. One week later all mice were killed and organs obtained for analysis of the immune response. Intestinal, faecal and pulmonary OVA-specific sIgA concentration was significantly increased (p<0.05) in mice that received booster combinations of OVA/CT and OVA with all extract doses (p<0.05). Specific serum IgG titres did not differ significantly between groups. It is concluded that STE can significantly enhance secretory immunity in the intestine to OVA with mucosal homing to the lungs. The adjuvant effect of STE is comparable to that of CT.
Life Sciences 07/2004; 75(4):397-406. · 2.53 Impact Factor
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ABSTRACT: Methanol extracts of seven Malaysian medicinal plants were screened for antioxidant and nitric oxide inhibitory activities. Antioxidant activity was measured by using FTC, TBA and DPPH free radical scavenging methods and Griess assay was used for the measurement of nitric oxide inhibition in lipopolysaccharide (LPS) and interferon-gamma (IFN-gamma)-treated RAW 264.7 cells. All the extracts showed strong antioxidant activity comparable to or higher than that of alpha-tocopherol, BHT and quercetin in FTC and TBA methods. The extracts from Leea indica and Spermacoce articularis showed strong DPPH free radical scavenging activity comparable with quercetin, BHT and Vit C. Spermacoce exilis showed only moderate activity but other species were weak as compared to the standards. In the Griess assay Lasianthus oblongus, Chasalia chartacea, Hedyotis verticillata, Spermacoce articularis and Leea indica showed strong inhibitory activity on nitric oxide production in LPS and IFN-gamma-induced RAW 264.7 cells. Extracts from Psychotria rostrata and Spermacoce exilis also inhibited NO production but this was due to their cytotoxic effects upon cells during culture.
Journal of Ethnopharmacology 07/2004; 92(2-3):263-7. · 3.01 Impact Factor
