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1.
J Oncol Pharm Pract ; 30(4): 737-751, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38477532

RESUMEN

BACKGROUND: Natural and synthetic cannabinoids are being used worldwide to treat various symptoms in cancer patients. This study aims to map the therapeutic benefits and adverse effects associated with the use of cannabis-based drugs in these outcomes. METHODS: Following Joanna Briggs Institute guidelines a scoping review was conducted. The study protocol was available in the Open Science Framework public repository. An extensive search strategy involving databases like Cochrane Library, Embase, CINAHL, Medline/PubMed, Lilacs, Google Scholar, and Open Gray for gray literature analysis was executed by a skilled librarian. The inclusion criteria were primary studies (observational and randomized) that evaluated the efficacy and safety of cannabinoids in cancer patients. The review encompassed studies of diverse designs, publication years, and types, as long as they addressed cannabinoids' impact in oncology. RESULTS: Twenty-nine (82.86%) out of total of 35 were randomized and 6 (14.14%) were non-randomized. About 57.1% of studies utilized registered products as interventions, with THC being the most natural cannabinoid cited in variable doses and administration routes. Moreover, 62.85% of studies specified the cancer types (breast, lung, sarcomas, hematological and reproductive system), while only one study detailed cancer staging. The evaluated outcomes encompassed nausea and vomiting (77.14%), appetite (11.43%), pain (8.57%), and tumor regression (2.86%) across different proportions of studies. CONCLUSION: Cannabinoids show promise in managing pain, emesis, and anorexia/cachexia linked to cancer progression. New randomized clinical trials with a larger number of participants and observational studies on long-term safety are crucial to affirm their medicinal utility for cancer patients unresponsive to conventional drugs.


Asunto(s)
Cannabinoides , Marihuana Medicinal , Neoplasias , Humanos , Marihuana Medicinal/uso terapéutico , Marihuana Medicinal/efectos adversos , Neoplasias/tratamiento farmacológico , Cannabinoides/uso terapéutico , Cannabinoides/efectos adversos , Vómitos/inducido químicamente , Ensayos Clínicos Controlados Aleatorios como Asunto , Náusea/inducido químicamente
2.
Biochim Biophys Acta Mol Basis Dis ; 1863(1): 139-151, 2017 01.
Artículo en Inglés | MEDLINE | ID: mdl-27677832

RESUMEN

Macrophage infiltration into adipose tissue (AT) is a hallmark of the chronic inflammatory response in obesity and is supported by an intense monocyte migration towards AT. Although it has been detected an increased proportion of circulating CD16+ monocyte subsets in obese subjects, the mechanisms underlying this effect and the contribution of these cells to the inflamed profile of obese AT are still poorly understood. We investigated whether factors secreted by human obese omental AT could polarize monocytes to CD16+ enriched phenotype, and how these changes could modify their migratory capacity towards adipose tissue itself. We show that explants of human obese omental AT, obtained during bariatric surgery, released higher levels of MIP1-α, TNFα, leptin and also VEGF, together with increasing amounts of microparticles (MP), when compared to explants of lean subcutaneous AT. A higher content of circulating MP derived from preadipocytes and leukocytes was also detected in plasma of obese subjects. Conditioned media or MP released from obese omental AT increased CD16 and CCR5 expression on CD14+CD16- monocytes and augmented their migratory capacity towards the conditioned media from obese omental AT, itself. This effect was inhibited when MIP1-α was neutralized. Additionally, we demonstrate that MP derived from obese omental AT carry and transfer TLR8 to monocytes, thus triggering an increase in CD16 expression in those cells. Our data shows a positive feedback loop between blood monocytes and obese omental AT, which releases chemotactic mediators and TLR8-enriched MP, thus inducing an up-regulation of CD16+ monocytes, favoring leukocyte infiltration in the obese omental AT.


Asunto(s)
Tejido Adiposo/inmunología , Micropartículas Derivadas de Células/inmunología , Monocitos/inmunología , Obesidad/inmunología , Receptores CCR5/inmunología , Receptores de IgG/inmunología , Receptor Toll-Like 8/inmunología , Tejido Adiposo/patología , Adulto , Micropartículas Derivadas de Células/patología , Femenino , Proteínas Ligadas a GPI/análisis , Proteínas Ligadas a GPI/inmunología , Humanos , Inflamación/inmunología , Inflamación/patología , Masculino , Persona de Mediana Edad , Monocitos/patología , Obesidad/patología , Receptores CCR5/análisis , Receptores de IgG/análisis , Receptor Toll-Like 8/análisis
3.
J Ethnopharmacol ; 119(1): 179-84, 2008 Sep 02.
Artículo en Inglés | MEDLINE | ID: mdl-18647645

RESUMEN

The aim of this study was to investigate the effect of chronic treatment with C. multijuga oil on Ehrlich tumor evolution. C. multijuga was fractionated in a KOH impregnated silica gel column chromatography to give three distinct fractions, i.e., hexanic, chloroformic, and methanolic, mainly composed by hydrocarbon sesquiterpenes, oxygenated sesquiterpenes and acidic diterpenes, respectively. Results demonstrated that the C. multijuga oil, the hexanic, and chloroformic fractions did not develop toxic effects. The oil, hexanic and chloroformic fractions (doses varying between 100 and 200mg/kg) showed antineoplasic properties against Ehrlich ascitic tumor (EAT) and solid tumor during 10 consecutive days of treatment inhibiting ascitic tumor cell number, reverting medulla and blood cell counts to values similar to control group, and inhibiting the increase on several inflammatory mediators (total protein, PGE(2), nitric oxide, and TNF) on ascitic fluid. The treatment also inhibited the increase in paw volume on tumor-inoculated mice. In conclusion, C. multijuga as well as its fractions demonstrated antineoplasic effect even after oral administration confirming its use by traditional medicine.


Asunto(s)
Carcinoma de Ehrlich/tratamiento farmacológico , Fabaceae/química , Extractos Vegetales/farmacología , Aceites de Plantas/farmacología , Administración Oral , Animales , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Líquido Ascítico/efectos de los fármacos , Líquido Ascítico/metabolismo , Recuento de Células Sanguíneas , Carcinoma de Ehrlich/metabolismo , Relación Dosis-Respuesta a Droga , Mediadores de Inflamación/metabolismo , Masculino , Ratones , Extractos Vegetales/administración & dosificación , Aceites de Plantas/administración & dosificación , Ratas , Ratas Wistar
4.
Eur J Pharmacol ; 556(1-3): 200-6, 2007 Feb 05.
Artículo en Inglés | MEDLINE | ID: mdl-17141756

RESUMEN

Isatin is a versatile compound with a diversity of effects. We designed to investigate the inhibitory effect of isatin derivatives on lipopolysaccharide/interferon-gamma-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins, production of prostaglandin E(2) (PGE(2)), nitric oxide (NO), tumor necrosis factor (TNF-alpha), and their capacity to scavenge NO. Isatins inhibit TNF-alpha production and iNOS and COX-2 protein expression resulting on reduced levels of NO and PGE(2). Our results indicate isatin and it derivatives as inhibitors of iNOS and COX-2 enzymes, which might be used as anti-inflammatory and antitumoral agents.


Asunto(s)
Ciclooxigenasa 2/metabolismo , Isatina/farmacología , Macrófagos/efectos de los fármacos , Óxido Nítrico Sintasa de Tipo II/metabolismo , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Inhibidores de la Ciclooxigenasa/farmacología , Lipopolisacáridos/farmacología , Macrófagos/enzimología , Ratones , Óxido Nítrico/biosíntesis , Óxido Nítrico Sintasa de Tipo II/antagonistas & inhibidores
5.
J Ethnopharmacol ; 109(3): 486-92, 2007 Feb 12.
Artículo en Inglés | MEDLINE | ID: mdl-17029841

RESUMEN

Copaiba oil resins are extensively commercialized in Brazil as capsules or crude oil and used as anti-inflammatory and anti-septic. Comparative pharmacological studies between different species of Copaiba oils are scarce. In the present work we compared the antinociceptive activity of two Amazonian Copaiba oils (Copaifera multijuga Hayne and Copaifera reticulata Ducke, Fabaceae) administered by oral route using peripheral (acetic acid-induced abdominal writhing and formalin), spinal (tail flick) and supra-spinal (hot plate) models. Results demonstrated that the Copaiba oils did not develop toxic effects. Doses ranging from 30 to 150 mg/kg were enough to significantly develop peripheral antinociceptive effect. All Copaiba oils demonstrate central activity but with less effect on supra-spinal regions of the brain. Administration of the opioid receptor antagonist, naloxone completely inhibited the antinociceptive effect induced by both Copaiba oils. Our results indicate that Copaiba oils demonstrate peripheral and central antinociceptive effect. This new comprobate effect may be useful in the treatment of algesic disorders.


Asunto(s)
Analgésicos no Narcóticos/farmacología , Fabaceae/química , Dolor/tratamiento farmacológico , Aceites de Plantas/farmacología , Acetatos , Analgésicos no Narcóticos/toxicidad , Animales , Brasil , Calor , Dosificación Letal Mediana , Masculino , Medicina Tradicional , Ratones , Dolor/inducido químicamente , Dimensión del Dolor , Aceites de Plantas/toxicidad
6.
Eur J Pharmacol ; 550(1-3): 47-53, 2006 Nov 21.
Artículo en Inglés | MEDLINE | ID: mdl-17030031

RESUMEN

The objective of this study was to investigate spinal and supraspinal antinociceptive effects of a new synthetic compound, (+/-)-cis-(6-ethyl-tetrahydropyran-2-yl)-formic acid (tetrahydropyran derivative). Its activity was compared with those from morphine. In peripheral models of inflammation and hyperalgesia, tetrahydropyran derivative significantly reduced nociceptive effect induced by acetic acid or formalin in mice. Tetrahydropyran derivative developed antinociceptive effect on the tail-flick and hot-plate tests with a long-acting curve maintaining the effect for 4 h longer than morphine. The opioid receptor antagonist naloxone totally reverted tetrahydropyran derivative effects on both models. Morphine as well as tetrahydropyran derivative induced tolerance and sedation in mice. However, tetrahydropyran derivative-induced tolerance had its onset retarded and the sedative activity was lower when compared to that induced by morphine. These results indicate that this new substance develops an antinociceptive activity and may be used in the future as a substitute for traditional opioids.


Asunto(s)
Analgésicos/farmacología , Formiatos/farmacología , Piranos/farmacología , Ácido Acético , Analgésicos/síntesis química , Analgésicos/toxicidad , Animales , Relación Dosis-Respuesta a Droga , Tolerancia a Medicamentos , Formaldehído , Formiatos/síntesis química , Formiatos/toxicidad , Calor , Masculino , Ratones , Actividad Motora , Naloxona/farmacología , Antagonistas de Narcóticos/farmacología , Dimensión del Dolor/efectos de los fármacos , Piranos/síntesis química , Piranos/toxicidad , Tiempo de Reacción/efectos de los fármacos , Receptores Opioides/efectos de los fármacos , Columna Vertebral/efectos de los fármacos
7.
J Ethnopharmacol ; 107(2): 291-6, 2006 Sep 19.
Artículo en Inglés | MEDLINE | ID: mdl-16635558

RESUMEN

The palm Euterpe oleracea is a plant of great economic value in Brazil. Although the heart of palm extracted from its trunk is considered a delicacy the world over, its fruits are popular only among Brazilians. In some poor regions of Brazil, there are reports on the popular use of its juice in the treatment of several disorders, mainly those of oxidative onset as cardiovascular ones. Because of its wide utilization; because there are very few scientific studies of this species, and to discover if its use in folk medicine for problems related with oxidation is in fact justifiable, we decided, in this study, to evaluate the effects of Euterpe oleracea flowers, fruits and spikes fractions on: nitric oxide (NO) production, NO scavenger capacity, and on the expression of inducible nitric oxide synthase enzyme, as well. Results showed that the fractions obtained from fruits were the most potent in inhibiting NO production, followed by those from flowers and spikes. Only in high doses, did some fractions reduce cell viability. Reduction on NO production was not due to NO scavenger activity. These results were accompanied by inhibition of iNOS expression. The more pronounced effect was observed in the fractions in which the concentration of cyanidin-3-O-glucoside and cyanidin-3-O-rhamnoside were higher. To sum up, our results indicate that fractions from Euterpe oleracea inhibits NO production by reducing the levels of inducible nitric oxide synthase expression.


Asunto(s)
Arecaceae/química , Inhibidores Enzimáticos/farmacología , Macrófagos/efectos de los fármacos , Óxido Nítrico Sintasa de Tipo II/antagonistas & inhibidores , Óxido Nítrico Sintasa de Tipo II/biosíntesis , Óxido Nítrico/antagonistas & inhibidores , Extractos Vegetales/farmacología , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Inhibidores Enzimáticos/aislamiento & purificación , Macrófagos/enzimología , Macrófagos/metabolismo , Ratones , Componentes Aéreos de las Plantas/química , Extractos Vegetales/aislamiento & purificación
8.
J Ethnopharmacol ; 100(3): 254-9, 2005 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-15905056

RESUMEN

The anti-inflammatory activity of Lantana trifolia (Verbenaceae) was determined by carrageenan, serotonin and histamine-induced rat paw edema and the analgesic activity of this plant was studied by acetic acid-induced writhings and tail flick tests in mice. Lantana trifolia extracts (at 30 mg/kg) inhibited carrageenan and histamine-induced rat paw edema. Although the extracts did not produce any effect on acetic acid-induced writhings, they all develop a significant increase on tail flick antinociceptive index (doses varying between 1 and 30 mg/kg), indicating a spinal antinociceptive effect. These results provide support for the use of Lantana trifolia in relieving inflammatory pain.


Asunto(s)
Analgésicos no Narcóticos/farmacología , Antiinflamatorios no Esteroideos/farmacología , Lantana/química , Ácido Acético , Animales , Edema/inducido químicamente , Edema/prevención & control , Calor , Lantana/toxicidad , Masculino , Ratones , Dimensión del Dolor/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/toxicidad , Hojas de la Planta/química , Ratas , Tiempo de Reacción/efectos de los fármacos
9.
J Ethnopharmacol ; 92(2-3): 269-73, 2004 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-15138011

RESUMEN

In the current study, the analgesic and free radical scavenging properties of an aqueous extract from the husk fiber of Cocos nucifera L. (Palmae) were demonstrated by the use of in vivo and in vitro models. The orally administered Cocos nucifera aqueous extract (200 or 400 mg/kg) inhibited the acetic acid-induced writhing response in mice. Tail flick and hot plate assays demonstrated that treatment of animals with this plant extract at 200 mg/kg induced attenuation in the response to a heat stimulus. A LD(50) of 2.30 g/kg was obtained in acute toxicity tests. Topic treatment of rabbits with the Cocos nucifera extract indicated that it does not induce any significant dermic or ocular irritation. In vitro experiments using the 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) photometric assay demonstrated that this plant extract also possesses free radical scavenging properties.


Asunto(s)
Analgésicos , Cocos/química , Depuradores de Radicales Libres , Dolor/tratamiento farmacológico , Administración Oral , Administración Tópica , Analgésicos/aislamiento & purificación , Analgésicos/farmacología , Analgésicos/uso terapéutico , Animales , Modelos Animales de Enfermedad , Ojo/efectos de los fármacos , Femenino , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Depuradores de Radicales Libres/uso terapéutico , Instilación de Medicamentos , Dosificación Letal Mediana , Masculino , Ratones , Epidermis de la Planta/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Conejos , Piel/efectos de los fármacos , Pruebas de Toxicidad Aguda
10.
J Ethnopharmacol ; 135(2): 530-7, 2011 May 17.
Artículo en Inglés | MEDLINE | ID: mdl-21463669

RESUMEN

AIM OF THE STUDY: Hancornia speciosa Gomes (Apocynaceae) is a tree that is widely distributed throughout Brazil. Its latex is collected and used extensively to treat acne, warts, diseases related to bursitis, and inflammation. In this work, we describe the anti-inflammatory effects of the latex. MATERIALS AND METHODS: The latex from Hancornia speciosa (0.06-1.3mg/kg, p.o.) and the reference drug acetylsalicylic acid (ASA, 200mg/kg, p.o.) were evaluated in analgesia (formalin-induced licking, acetic acid-induced contortions, and hot plate) and inflammation models (formalin-induced licking, paw oedema, and subcutaneous air pouch, with measurement of cell migration, exudate volume, protein extravasations, nitric oxide, prostaglandin E2, TNF-α, and IL-6, and expression of the enzymes inducible nitric oxide synthase and cyclooxygenase 2). RESULTS: The latex from Hancornia speciosa significantly inhibited the number of writhings and the time that the animal spent licking the formalin-injected paw (second phase). Doses of 0.1-1.3mg/kg latex reduced carrageenan-induced rat paw oedema. However, only the highest doses (0.6 and/or 1.3mg/kg) reduced the oedema induced by bradykinin, histamine, and serotonin. The latex also inhibited inflammation induced by subcutaneous carrageenan injection, cell migration, exudate volume, protein extravasations, increased levels of inflammatory mediators (nitric oxide, prostaglandin E2, TNF-α, and IL-6) produced in the pouch, and increased expression of the enzymes nitric oxide synthase and cyclooxygenase 2. CONCLUSIONS: Our results indicate that the latex obtained from Hancornia speciosa demonstrates significant anti-inflammatory activity through the inhibition of nitric oxide, PGE2, and cytokine production, thus confirming the popular use of this plant as an anti-inflammatory agent.


Asunto(s)
Antiinflamatorios/farmacología , Apocynaceae/química , Látex/farmacología , Animales , Masculino , Ratones , Ratones Endogámicos BALB C , Ratas , Ratas Sprague-Dawley
11.
J Ethnopharmacol ; 134(3): 725-32, 2011 Apr 12.
Artículo en Inglés | MEDLINE | ID: mdl-21277967

RESUMEN

AIM OF THE STUDY: Hyptis pectinata Poit (Lamiaceae) is grown in the northeastern regions of Brazil and is popularly known as "sambacaitá" or "canudinho". It is extensively used in folk medicine to treat inflammatory conditions, bacterial infections, pain, and cancer. MATERIALS AND METHODS: Hyptis pectinata essential oil (EO, 10, 30, and 100mg/kg, p.o.) and the reference drugs morphine (5mg/kg, p.o.) and acetylsalicylic acid (ASA, 200mg/kg, p.o.) were evaluated using models for analgesia (acetic acid-induced contortions and hot plate) or inflammation (formalin-induced licking response and the subcutaneous air-pouch model). To elucidate the EO's mechanism of action, animals were pre-treated with the opioid receptor antagonist naloxone (1mg/kg, i.p.), the cholinergic antagonist atropine (1mg/kg, i.p.), or l-nitro arginine methyl ester (l-NAME, 3mg/kg, i.p.) 30 min prior to the oral administration of the EO. RESULTS: The EO significantly inhibited the number of writhings and the time the animals spent licking their formalin-injected paws (second phase). The EO, at doses of 30 and 100mg/kg, increased baseline measurements and area under the curve measurements in the hot plate model, respectively. The administration of naloxone reversed the antinociceptive effect of the EO in the hot plate model. l-NAME significantly reversed the effects of the EO in the contortions and hot plate models. Atropine completely reversed the antinociceptive activity of the EO in all models. Additionally, the EO inhibited the inflammatory process induced by subcutaneous carrageenan injection by reducing cell migration, exudate volume, protein concentration, and inflammatory mediators (nitric oxide, prostaglandin E2, IL-6, and TNF-α) produced in the pouch. CONCLUSIONS: Our results indicate that the Hyptis pectinata essential oil exhibits antinociceptive effects, likely mediated by opioid and cholinergic receptors, and anti-inflammatory activity through the inhibition of nitric oxide and PGE2 production.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Hyptis/química , Aceites Volátiles/farmacología , Animales , Dinoprostona/metabolismo , Relación Dosis-Respuesta a Droga , Interleucina-6/metabolismo , Masculino , Ratones , Ratones Endogámicos BALB C , Óxido Nítrico/biosíntesis , Factor de Necrosis Tumoral alfa/metabolismo
12.
J Ethnopharmacol ; 135(2): 406-13, 2011 May 17.
Artículo en Inglés | MEDLINE | ID: mdl-21420477

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The species Lippia gracilis Schauer, known in Brazil as "Alecrim-da-chapada", is popularly used in folk medicine to treat cough, bronchitis, nasal congestion, and headache. MATERIALS AND METHODS: Lippia gracilis essential oil (EO; 10, 30, and 100mg/kg, p.o.) and the reference drugs morphine (5mg/kg, p.o.) and acetylsalicylic acid (ASA; 200mg/kg, p.o.) were evaluated using models for analgesia (acetic acid-induced contortion, formalin-induced licking, and hot plate) or inflammation (formalin-induced licking response and subcutaneous air pouch model). To elucidate the antinociceptive mechanism of action, animals were pre-treated with naloxone (opioid receptor antagonist; 1mg/kg, i.p.), atropine (cholinergic antagonist; 1mg/kg, i.p.) or l-nitro arginine methyl ester (L-NAME; 3mg/kg, i.p.) 30 min prior to oral administration of EO. RESULTS: EO significantly inhibited the number of writhings in acetic acid-induced contortions and the time that the animal spent licking the formalin-injected paw (second phase). All doses of EO increased the baseline and the area under the curve in the hot plate model. The administration of naloxone did not reverse the antinociceptive effect of EO in the acetic acid-induced contortion and formalin-induced licking models. L-NAME and atropine significantly reversed the effect of EO in the models of contortion, formalin, and hot plate. EO also inhibited the inflammatory process induced by subcutaneous carrageenan injection, reducing cell migration, exudate volume, extravased protein, and inflammatory mediators (nitric oxide, prostaglandin E2, TNF-α, and IFN-γ) produced in the pouch. CONCLUSIONS: Our results indicate that the essential oil from Lippia gracilis produces an antinociceptive effect that could be potentially mediated by cholinergic receptors and the nitric oxide pathway. Our data also suggest that the anti-inflammatory activity caused by EO exposure occurs through inhibition of nitric oxide and PGE2 production.


Asunto(s)
Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Lippia/química , Aceites Volátiles/uso terapéutico , Animales , Femenino , Cromatografía de Gases y Espectrometría de Masas , Masculino , Ratones , Ratones Endogámicos BALB C
13.
J Ethnopharmacol ; 127(2): 407-13, 2010 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-19861155

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Couroupitaguianensis Aubl. (Lecythidaceae) is popularly known in Brazil as "abricó-de-macaco". Infusions or teas obtained from its leaves, flowers, and barks are used in South America for the treatment of several disorders such as pain and inflammatory processes. AIM OF THE STUDY: Evaluate antinociceptive effects of crude ethanol extract (CEE) and its fractions in three analgesic models (acetic acid-induced contortions, tail flick, and hot plate) and study the possible mechanism of their action. MATERIALS AND METHODS: CEE, hexane, dichloromethane, ethyl acetate, and butanol fractions (10, 30, and 100mg/kg, p.o.) and the reference drug morphine (5mg/kg, s.c.) were evaluated. To elucidate the mechanism of action from the fractions, animals were pre-treated (30 min) with atropine (muscarinic receptor antagonist, 1mg/kg, s.c.), mecamylamine (nicotinic receptor antagonist, 2mg/kg, s.c.), naloxone (opioid receptor antagonist, 1mg/kg, s.c.) or L-nitro arginine methyl ester (L-NAME, nitric oxide synthase inhibitor, 3mg/kg, s.c.). RESULTS: CEE and fractions significantly inhibited the number of contortions induced by acetic acid. All fractions showed antinociceptive activity in the tail flick model, being the hexane and ethyl acetate the most potent and long acting fractions. In the hot plate method the highest effect observed was at the dose of 100mg/kg from all fractions. Administration of naloxone inhibited the antinociceptive effect of fractions. Pre-treatment of mice with atropine reduced the antinociceptive activity of CEE and its fractions, the exception being the dichloromethane fraction. Mecamylamine did not inhibited the effect of dichloromethane fraction. L-NAME reduced the anti-hyperalgesic effect of all fractions, but the most prominent effect was observed in the antinociceptive activity caused by CEE and butanol fraction. CONCLUSIONS: Results obtained demonstrated that Couroupita guianensis CEE and its fractions have antinociceptive activity that is mediated, at least in part, by opioid and cholinergic systems and nitric oxide pathway.


Asunto(s)
Analgésicos/uso terapéutico , Lecythidaceae , Dolor/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Analgésicos/aislamiento & purificación , Analgésicos/farmacología , Animales , Relación Dosis-Respuesta a Droga , Masculino , Ratones , Dolor/patología , Dimensión del Dolor/efectos de los fármacos , Dimensión del Dolor/métodos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología
14.
J Ethnopharmacol ; 128(1): 177-83, 2010 Mar 02.
Artículo en Inglés | MEDLINE | ID: mdl-20064592

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Copaifera multijuga Hayne (Leguminosae) is a tree that produces an oleoresin, which is extensively commercialized in Brazil as capsules or crude oil for the treatment of several disorders. Ethnopharmacological studies show a diversity of indications such as anti-inflammatory and epidermal wound cicatrization. AIM OF THE STUDY: In the present work three fractions obtained from Copaifera multijuga oleoresin (hexane (HF), chloroform (CF), and methanol (MF) from a KOH impregnated silica gel column chromatography, representing the three main classes of compounds in the Copaifera genus (hydrocarbon sesquiterpenes, oxygenated sesquiterpenes and acidic diterpenes), were evaluated using antinociceptive and anti-inflammatory models. MATERIALS AND METHODS: HF, CF, and MF (doses ranging between 1 and 150 mg/kg, depending on the model used), Copaifera multijuga oleoresin (CMO, 100mg/kg, p.o.) and the reference drug morphine (5mg/kg, p.o.) were evaluated using models for analgesia (acetic acid-induced contortions and tail flick) or inflammation (rat paw oedema and increase in vascular permeability). To elucidate the mechanism of action from the fractions, animals were pre-treated with naloxone (opioid receptor antagonist, 5mg/kg, i.p.). RESULTS: Fractions significantly inhibited (in a concentration-dependant way) the number of contortions induced by acetic acid and the second phase of formalin-induced licking response. Similar results were observed in the tail flick model. The central antinociceptive effect for HF and CF at the doses of 50 and 100mg/kg was higher than the one observed for morphine (1mg/kg). Administration of naloxone inhibited the antinociceptive effect of fractions indicating that HF, CF, and MF may be acting on opioid receptors. All three fractions also inhibited rat paw oedema and the increase in vascular permeability induced by several phlogistic agents (carrageenan, histamine, and serotonin). CONCLUSIONS: Our results indicate that fractions obtained from Copaifera multijuga Hayne demonstrate an antinociceptive effect probably mediated by opioid receptors, and anti-inflammatory activity through inhibition of histaminergic and serotoninergic pathways.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Fabaceae/química , Extractos Vegetales/farmacología , Animales , Permeabilidad Capilar/efectos de los fármacos , Cromatografía en Gel , Relación Dosis-Respuesta a Droga , Ratones , Ratas
15.
J Ethnopharmacol ; 122(3): 541-6, 2009 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-19429325

RESUMEN

AIM OF THE STUDY: Cocos nucifera cultivated in Brazil is known as "coco-da-Bahia" or "coqueiro-da-India". The tea from the husk fiber is widely used to several inflammatory disorders. Crude extract and fractions obtained from Cocos nucifera "common variety" were evaluated to test the anti-inflammatory and antinociceptive activities. MATERIALS AND METHODS: Crude extract (CE, 50, 100, and 150 mg/kg), fraction 1 (F1, molecular weight lesser than 1 kDa, 1, 10, and 50mg/kg), fraction 2 (F2, molecular weight higher than 1 kDa, 1, 10, and 50mg/kg), and the references drugs morphine (5mg/kg), acetilsalicilic acid (200mg/kg), prometazine (30 mg/kg), and metisergide (5mg/kg) were evaluated on models of analgesia and inflammation. RESULTS: CE, F1, and F2 significantly develop peripheral and central antinociceptive activity but with less effect on supra-spinal regions of the brain. Administration of the opioid antagonist, naloxone (5mg/kg) inhibited the antinociceptive effect indicating that Cocos nucifera crude extract and fractions may be acting in opioid receptors. CE and F1 also inhibited rat paw edema induced by histamine, and serotonin. CONCLUSIONS: results demonstrated that Cocos nucifera and its fractions have antinociceptive and anti-inflammatory activities which confirm the popular use of this plant in several inflammatory disorders.


Asunto(s)
Analgésicos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Cocos , Edema/tratamiento farmacológico , Dolor/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/uso terapéutico , Ácido Acético , Analgésicos/farmacología , Animales , Edema/inducido químicamente , Frutas , Masculino , Ratones , Naloxona/farmacología , Antagonistas de Narcóticos/farmacología , Dolor/inducido químicamente , Extractos Vegetales/farmacología
16.
Rev. bras. farmacogn ; 21(5): 874-883, Sept.-Oct. 2011. ilus, graf
Artículo en Inglés | LILACS | ID: lil-600971

RESUMEN

Vitex cymosa Bertero ex Spreng., Lamiaceae, is found in Central and Amazon regions of Brazil, where it is popularly used as antirheumatic. Extracts from the leaves of V. cymosa were tested in analgesia models such as abdominal contortions induced by acetic acid and formalin to test peripheral analgesia; as well as the tail flick and hot plate models, to test spinal and supraspinal analgesia. A significant reduction was observed in the number of contortions with all extracts and in all doses. In the formalin model, a reduction in the second phase (inflammatory) was observed with all extracts, whereas only the n-butanol extract was able to act in the first, neurogenic, phase. In the tail flick model, all extracts increased latency time. Naloxone treatment reverted analgesic effect of all extracts with the exception of the dichloromethane one. All extracts developed peripheral and central analgesic activity. In the hot plate model no antinociceptive effect was observed for all tested extracts. All these results taken together suggest that V. cymosa leaf extracts were able to promote peripheral and central antinociceptive activity mediated by the opioid system.Twenty three substances were isolated and identified in the extracts and include flavonoids (C-glucosyl flavones, flavones and flavonols), triterpene acids from ursane and oleanane types, iridoids (free and glucosides), as well as simple phenols.

17.
Bioorg Med Chem Lett ; 14(6): 1573-5, 2004 Mar 22.
Artículo en Inglés | MEDLINE | ID: mdl-15006406

RESUMEN

We described in this paper the first synthesis to the (+/-) cis (6-ethyl-tetrahydropyran-2-yl) formic acid (1) using the very efficient Prins cyclization reaction as strategy to construction of its tetrahydropyran skeleton. This new compound presented a significant antinociceptive property by the tail-flick model.


Asunto(s)
Analgésicos/química , Analgésicos/farmacología , Formiatos/química , Formiatos/farmacología , Dimensión del Dolor/efectos de los fármacos , Animales , Ratones , Dimensión del Dolor/métodos
18.
Rev. bras. farmacogn ; 12(supl.1): 52-53, 2002. ilus
Artículo en Portugués | LILACS | ID: lil-528748

RESUMEN

Extratos de flores (ETFA) e espigas (ETEA) de Açaí (Euterpe oleraceae Mart.) foram avaliados quanto a sua atividade antinociceptiva. ETFA mostrou significativa atividade periférica, reduzindo em até 50 por cento o número total de contorções abdominais. Já ETEA mostrou reduzido efeito no modelo de contorções abdominais, mas seu efeito espinhal pode ser observado com as doses maiores. Nenhum dos extratos foi capaz de alterar os índices de analgesia na placa quente.

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