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1.
An Acad Bras Cienc ; 94(2): e20210715, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35830084

RESUMEN

Samanea tubulosa Benth. it has been widely used in traditional medicine to treat inflammatory processes. The present study aimed to investigate the antinociceptive effect and mechanism of action of the fractions obtained from the Samanea tubulosa pods in mice. The antinociceptive activity was evaluated in formalin, capsaicin and glutamate tests and the. The possible mechanisms of action involved in the antinociceptive effect of the hexane and ethyl acetate fraction in the opioid system, also the the K + ATP channels and the L-arigine pathways of nitric oxide were evaluated. The chemical characterization analysis revealed in the hexane fraction the presence of triterpenes such as lupenone and lupeol. In the glutamate test, the hexane and ethyl acetate fractions showed antinociceptive activity at the dose of 12.5 and 25 mg kg-1. The antinociception produced by the hexane and ethyl acetate fractions was significantly reversed by naloxone, indicating that the fractions act through the opioid pathway. Antinociceptive response of the ethyl acetate fraction was blocked by glibenclamide, indicating that this fraction acts via the K + ATP channels activation. It is concluded that the fractions under study exert antinociceptive activity possibly related to the opioid route and through K+ ATP channels activation.


Asunto(s)
Dolor Agudo , Fabaceae , Dolor Agudo/tratamiento farmacológico , Adenosina Trifosfato , Analgésicos/farmacología , Analgésicos/uso terapéutico , Analgésicos Opioides , Animales , Fabaceae/metabolismo , Ácido Glutámico , Hexanos , Ratones
2.
J Ethnopharmacol ; 218: 100-108, 2018 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-29471086

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Pilosocereus gounellei Cactaceae), popularly known as "xique xique", is a species native from Caatinga region of Northeast Brazil, which is used by traditional communities in folk medicine for a variety of health problems, especially inflammatory processes and gastritis. AIM OF THE STUDY: The present study investigates the possible gastric antiulceractivity of ethanol extracts obtained from the cladodes and roots of Pilosocereus gounellei (EECPG and EERPG, respectively) and mechanisms of action underlying this effect. MATERIALS AND METHODS: Mice were used for the evaluation of the acute toxicity, and mice and rats to study the gastroprotective activity. The gastroprotective action of EECPG and EERPG was analyzed in the absolute ethanol in mice, ischemia-reperfusion and cold restraint stress in rats. In the investigation of the gastroprotective mechanisms of EECPG and EERPG, the participation of the NO and prostaglandins, the levels of the non-protein sulfhydril groups (NP-SH) and the catalase activity using the ethanol-induced gastric mucosa lesion model and the quantification of the gastric mucus and the antisecretory activity through pylorus ligature model in rats were analyzed. RESULTS: The animals did not present any signs of acute toxicity for the EECPG and EERPG, and it was not possible to calculate the DL50. EECPG and EERPG (200 and 400 mg/kg) exhibited a significant gastroprotective effect in absolute ethanol, ischemia-reperfusion-induced and cold restraint stress gastric lesion models. Gastroprotection of EECPG and EERPG (200 mg/kg) was significantly decreased in pre-treated mice with L-NAME. Our studies revealed that EECPG and EERPG (200 mg/kg) prevented the decrease of the non-protein sulfhydril groups (NPSH) and increased the catalase levels in ethanol-treated animals. However, the gastric secretion parameters (volume, [H+], pH) did not show any alteration. CONCLUSIONS: Our results indicate that the ethanolic extract from the cladodes and roots of Pilosocereus gounellei exhibits a significant gastroprotection, because it inhibits the formation of gastric lesions using different models. The participation of the nitric oxide, prostaglandins, the non-protein sulfhydril groups (NP-SH), catalase seem to be involved in the gastroprotection activity of the EECPG and EERPG. Nevertheless, this activity does not seem to be related to antisecretory mechanisms.


Asunto(s)
Antiulcerosos/uso terapéutico , Cactaceae , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/tratamiento farmacológico , Animales , Antiulcerosos/farmacología , Catalasa/metabolismo , Frío , Modelos Animales de Enfermedad , Etanol/efectos adversos , Etanol/química , Mucosa Gástrica/metabolismo , Masculino , Ratones , Óxido Nítrico/metabolismo , Fitoterapia , Extractos Vegetales/farmacología , Raíces de Plantas , Prostaglandinas/metabolismo , Ratas Wistar , Daño por Reperfusión/complicaciones , Daño por Reperfusión/tratamiento farmacológico , Restricción Física , Solventes/efectos adversos , Solventes/química , Estómago/efectos de los fármacos , Estómago/patología , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología
3.
J Med Food ; 17(6): 694-700, 2014 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-24476221

RESUMEN

The present work reports the anti-inflammatory and antinociceptive activities of the ethanol extract obtained from the stem bark of Sterculia striata A. St.-Hil. & Naudin (Ss-EtOH) in the experimental models of edema induced by carrageenan, dextran, or histamin and nociception induced by chemical stimuli, such as acetic acid, formalin, capsaicin, or glutamate. The Ss-EtOH (50 mg/kg) promoted a marked inhibition on the hind paw edema induced by carrageenan or dextran (30% and 73%, respectively). Besides, Ss-EtOH (25 mg/kg) exhibited a slight activity (30%) on the hind paw edema induced by histamin. The Ss-EtOH (12.5 and 25 mg/kg) showed the antinociceptive activity on chemical stimuli induced by acetic acid (65.59% and 38.37%, respectively), formalin, in the initial (35.08% and 31.5%, respectively) and late phases (44.09% and 83.57%, respectively), capsaicin (43.77% and 51.31%, respectively), or glutamate (36.6% and 52.12%, respectively). Regarding the possible mechanism involved in the antinociceptive effect, Ss-EtOH (12.5 mg/kg) showed a decrease in the antinociceptive effect (65.8%) in the acetic acid model after pretreatment with naloxone. Thus, opioid mechanisms might be underlying this response.


Asunto(s)
Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Inflamación/tratamiento farmacológico , Dolor/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/uso terapéutico , Sterculia , Ácido Acético , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Capsaicina , Carragenina , Dextranos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Formaldehído , Ácido Glutámico , Histamina , Inflamación/inducido químicamente , Masculino , Ratones , Naloxona/farmacología , Corteza de la Planta , Extractos Vegetales/farmacología , Tallos de la Planta , Ratas Wistar
4.
Z Naturforsch C J Biosci ; 68(3-4): 97-107, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-23819304

RESUMEN

This study investigates the gastroprotective effect of a crude ethanolic extract of Neoglaziovia variegata (Arruda) Mez (Bromeliaceae), designated Nv-EtOH, in experimental models of gastric ulcer. In the ethanol-induced gastric ulcer model, Nv-EtOH showed gastroprotection at doses of 200 and 400 mg/kg body weight (BW) (57.0% and 79.7%, respectively). Nv-EtOH also significantly reduced the formation of gastric lesions induced by ethanol/HCl (31.6% and 63.5%), ibuprofen (70.0% and 74.3%), or ischemia/reperfusion in rats (65.0% and 87.0%) at 200 and 400 mg/kg BW when compared with the vehicle group. In the antioxidant activity assessment, Nv-EtOH (400 mg/kg BW) increased the catalase activity and sulfhydryl groups (SH) levels, respectively. Moreover, gastroprotection against ethanol damage was decreased after ibuprofen pretreatment. Nv-EtOH (400 mg/kg BW) promoted a significant increase in the content of gastric wall mucus. The Nv-EtOH effect was significantly reduced in mice pretreated with N(G)-nitro-L-arginine (L-NOARG) or glibenclamide, inhibitors of nitric oxide synthase and K(ATP) channel activation, respectively, suggesting the involvement of these mechanisms in the Nv-EtOH-induced gastroprotective effect. Nv-EtOH decreased the total acidity, but did not modify other gastric juice parameters. Nv-EtOH was also effective in promoting the healing process in chronic gastric ulcer induced by acetic acid in rats.


Asunto(s)
Antiulcerosos/farmacología , Bromeliaceae/química , Etanol/química , Extractos Vegetales/farmacología , Animales , Catalasa/metabolismo , Mucosa Gástrica/metabolismo , Masculino , Ratones , Extractos Vegetales/química , Prostaglandinas/metabolismo , Ratas , Ratas Wistar , Estómago/efectos de los fármacos , Estómago/enzimología
5.
J Med Food ; 15(11): 984-91, 2012 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-22892022

RESUMEN

This study reports a pharmacological evaluation of anti-inflammatory and anti-ulcer activities of carvacrol, a phenolic monoterpene constituent of essential oils produced by oregano and other several aromatic plants and spices, in experimental models of edema induced by different phlogistic agents and gastric lesions induced by acetic acid. In models of paw edema induced by dextran or histamine, carvacrol was effective at 50 mg/kg (46% and 35%, respectively); in these models, cyproheptadine reduced edema formation (61% and 43%, respectively). In edema induced by substance P, carvacrol (100 mg/kg) and ruthenium red (3 mg/kg) also decreased the edema formation (46% and 40%, respectively). Carvacrol significantly reduced the ear edema induced by 12-O-tetradecanoylphorbol acetate and arachidonic acid at 0.1 mg per ear (43% and 33%, respectively), similar to indomethacin at 0.5 mg per ear or 2.0 mg per ear (55% and 57%, respectively). Carvacrol (at doses of 25, 50, and 100 mg/kg) showed a healing capacity on gastric lesions induced by acid acetic (60%, 91%, and 81%, respectively) after 14 days of treatment. These results suggest that carvacrol acts on different pharmacological targets, probably interfering in release and/or synthesis of inflammatory mediators, such as the prostanoids, and thus favoring the healing process for gastric ulcers.


Asunto(s)
Antiinflamatorios/farmacología , Antiulcerosos/farmacología , Inflamación/tratamiento farmacológico , Monoterpenos/farmacología , Aceites Volátiles/farmacología , Origanum/química , Úlcera Gástrica/tratamiento farmacológico , Animales , Ácido Araquidónico/efectos adversos , Cimenos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Femenino , Indometacina/efectos adversos , Masculino , Ratones , Ratas , Ratas Wistar , Rojo de Rutenio/farmacología , Úlcera Gástrica/inducido químicamente , Sustancia P/efectos adversos , Acetato de Tetradecanoilforbol/efectos adversos , Acetato de Tetradecanoilforbol/análogos & derivados
6.
Biol Res ; 43(4): 459-65, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-21526273

RESUMEN

This study evaluated the antiulcer activity of an ethanolic extract of Encholirium spectabile (ES-EtOH) by using different standard experimental models of induced acute gastric ulceration. ES-EtOH (100 mg/kg p.o) protected the gastric mucosa against ulceration that was induced by absolute ethanol (53%), ethanol/HCl (75%), ibuprofen (52 %) and ischemia/reperfusion (43 %). It also restored catalase activity and non-protein sulfhydryl group concentration in the gastric wall of mice that had been treated with ethanol. The pre-treatment of mice with N-nitro-L-arginine (70 mg/kg i.p.) abolished the protective activity of ES-EtOH, which indicates that prostaglandins, antioxidant compounds and nitric oxide synthase activity are involved in the gastroprotective activity of the extract.


Asunto(s)
Antiulcerosos/uso terapéutico , Bromeliaceae/química , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/prevención & control , Animales , Antiinflamatorios no Esteroideos/efectos adversos , Bromeliaceae/clasificación , Modelos Animales de Enfermedad , Etanol/efectos adversos , Mucosa Gástrica/efectos de los fármacos , Indometacina/efectos adversos , Masculino , Ratones , Hojas de la Planta/química , Ratas , Ratas Wistar , Úlcera Gástrica/inducido químicamente
7.
Biol Res ; 43(4): 451-7, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-21526272

RESUMEN

Parkia platycephala Benth. (Leguminosae--Mimosoideae), popularly known as "visgueira", fava bean tree or "fava-de-bolota", is widely found in the Northern and Northeastern regions of Brazil. Its pods are used as cattle food supplement in the drought period. Compounds with a gastroprotective activity were obtained from the genus Parkia. Therefore, this study aimed at investigating the gastroprotective effect of the ethanolic extract of Parkia platycephala Benth. leaves (Pp-EtOH), as well as evaluating its possible mechanisms of action in experimental ulcer induction models. Lesions were induced by absolute ethanol, ethanol-HCl, ischemia-reperfusion and indomethacin in rodents. Pp-EtOH showed a protective effect in the lesion models (66, 48 and 52%, respectively), but it was not able to protect gastric mucosa against indomethacin-induced lesions. Results show a possible participation of the NO-synthase pathway in the gastroprotection and an antioxidant activity, by the increase of the catalase activity. The participation of prostaglandins and potassium channels sensitive to ATP in the gastroprotective effect of Pp-EtOH seems less likely to occur. More comprehensive studies, therefore, should be carried out to elucidate the antiulcerative effects of this promising natural product against this gastrointestinal disorder.


Asunto(s)
Antiulcerosos/uso terapéutico , Fabaceae/química , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/prevención & control , Enfermedad Aguda , Animales , Antiinflamatorios no Esteroideos/efectos adversos , Antiulcerosos/efectos adversos , Modelos Animales de Enfermedad , Etanol/efectos adversos , Fabaceae/clasificación , Mucosa Gástrica/efectos de los fármacos , Indometacina/efectos adversos , Masculino , Ratones , Extractos Vegetales/efectos adversos , Hojas de la Planta/química , Ratas , Ratas Wistar , Úlcera Gástrica/inducido químicamente
8.
Biol. Res ; 43(4): 451-457, 2010. ilus
Artículo en Inglés | LILACS | ID: lil-582860

RESUMEN

Parkia platycephala Benth. (Leguminosae - Mimosoideae), popularly known as "visgueira", fava bean tree or "fava-de-bolota", is widely found in the Northern and Northeastern regions of Brazil. Its pods are used as cattle food supplement in the drought period. Compounds with a gastroprotective activity were obtained from the genus Parkia. Therefore, this study aimed at investigating the gastroprotective effect of the ethanolic extract of Parkia platycephala Benth. leaves (Pp-EtOH), as well as evaluating its possible mechanisms of action in experimental ulcer induction models. Lesions were induced by absolute ethanol, ethanol-HCl, ischemia-reperfusion and indomethacin in rodents. Pp-EtOH showed a protective effect in the lesion models (66, 48 and 52 percent, respectively), but it was not able to protect gastric mucosa against indomethacin-induced lesions. Results show a possible participation of the NO-synthase pathway in the gastroprotection and an antioxidant activity, by the increase of the catalase activity. The participation of prostaglandins and potassium channels sensitive to ATP in the gastroprotective effect of Pp-EtOH seems less likely to occur. More comprehensive studies, therefore, should be carried out to elucidate the antiulcerative effects of this promising natural product against this gastrointestinal disorder.


Asunto(s)
Animales , Masculino , Ratones , Ratas , Antiulcerosos/uso terapéutico , Fabaceae/química , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/prevención & control , Enfermedad Aguda , Antiinflamatorios no Esteroideos/efectos adversos , Antiulcerosos/efectos adversos , Modelos Animales de Enfermedad , Etanol/efectos adversos , Fabaceae/clasificación , Mucosa Gástrica/efectos de los fármacos , Indometacina/efectos adversos , Extractos Vegetales/efectos adversos , Hojas de la Planta/química , Ratas Wistar , Úlcera Gástrica/inducido químicamente
9.
Biol. Res ; 43(4): 459-465, 2010. ilus
Artículo en Inglés | LILACS | ID: lil-582861

RESUMEN

This study evaluated the antiulcer activity of an ethanolic extract of Encholirium spectabile (ES-EtOH) by using different standard experimental models of induced acute gastric ulceration. ES-EtOH (100 mg/kg p.o) protected the gastric mucosa against ulceration that was induced by absolute ethanol (53 percent), ethanol/HCl (75 percent), ibuprofen (52 percent) and ischemia/reperfusion (43 percent). It also restored catalase activity and non-protein sulfhydryl group concentration in the gastric wall of mice that had been treated with ethanol. The pre-treatment of mice with N-nitro-L-arginine (70 mg/kg i.p.) abolished the protective activity of ES-EtOH, which indicates that prostaglandins, antioxidant compounds and nitric oxide synthase activity are involved in the gastroprotective activity of the extract.


Asunto(s)
Animales , Masculino , Ratones , Ratas , Antiulcerosos/uso terapéutico , Bromeliaceae/química , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/prevención & control , Antiinflamatorios no Esteroideos/efectos adversos , Bromeliaceae/clasificación , Modelos Animales de Enfermedad , Etanol/efectos adversos , Mucosa Gástrica/efectos de los fármacos , Indometacina/efectos adversos , Hojas de la Planta/química , Ratas Wistar , Úlcera Gástrica/inducido químicamente
10.
J Ethnopharmacol ; 124(3): 457-62, 2009 Jul 30.
Artículo en Inglés | MEDLINE | ID: mdl-19481144

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Curcuma longa L. (CL) is a yellow rhizome that is used in African traditional medicine to treat palpitation, hypertension or other related blood circulation disorders. AIM OF THE STUDY: To justify the use of CL in ethnomedicine, we investigated the vasorelaxant effect of methanolic extract of CL (CLME) and its underlying mechanisms in isolated rat mesenteric artery. MATERIALS AND METHODS: The effect of CLME on the mean arterial pressure (MAP) and heart rate (HR) (pulse interval) were determined in vivo in non-anaesthetized rats. Superior mesenteric rings were isolated, suspended in organ baths containing Tyrode solution at 37 degrees C and gassed with 95% O(2)+5% CO(2), under a resting tension of 0.75 g. The vasorelaxant effects of CLME were studied by means of isometric tension recording experiments. RESULTS: In normotensive rats, CLME (10, 20 and 30 mg/kg, i.v.) induced dose-dependent hypotension (2.0+/-0.5%; 27.1+/-5.0% and 26.7+/-4.6%, respectively), and pronounced bradycardia (5.8+/-1.2%, 19.3+/-3.2% and 22.9+/-4.6%, respectively). CLME (1-1000 microg/mL) induced concentration-dependent relaxation of tonic contractions evoked by phenylephrine (Phe) (10 microM) and KCl (80 mM) in rings with intact-endothelium (E(max)=82.3+/-3.2% and 97.7+/-0.7%) or denuded-endothelium (E(max)=91.4+/-1.0% and 97.8+/-1.1%). Also, in a depolarized, Ca(2+) free medium, CLME inhibited CaCl(2) (1 microM-30 mM)-induced contractions and caused a concentration-dependent rightward shift of the response curves, indicating that CLME inhibited the contractile mechanisms involving extracellular Ca(2+) influx. In addition, in Ca(2+) free media containing EGTA (1 mM), CLME inhibited the transient contraction of denuded rings constricted with Phe, but not those evoked by caffeine (20 mM). In contrast, neither glibenclamide, BaCl(2), tetraethylammonium nor 4-aminopyridine affected CLME-induced relaxation. CONCLUSIONS: These results demonstrate the hypotensive and bradycardic effects of CLME, as well as its potent vasodilation of rat mesenteric arteries. These effects, may in part, be due to the inhibition of extracellular Ca(2+) influx and/or inhibition of intracellular Ca(2+) mobilization from Phe-sensitive stores.


Asunto(s)
Antihipertensivos/farmacología , Curcuma/química , Vasodilatadores/farmacología , Animales , Presión Sanguínea/efectos de los fármacos , Cafeína/farmacología , Calcio/metabolismo , Bloqueadores de los Canales de Calcio/farmacología , Relación Dosis-Respuesta a Droga , Endotelio Vascular/fisiología , Etnofarmacología , Técnicas In Vitro , Masculino , Arterias Mesentéricas/efectos de los fármacos , Metanol , Nifedipino/farmacología , Fenilefrina/farmacología , Inhibidores de Fosfodiesterasa/farmacología , Ratas , Ratas Wistar , Solventes , Vasoconstrictores/farmacología
11.
Planta Med ; 72(1): 34-9, 2006 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-16450293

RESUMEN

In the search for novel natural compounds effective against visceral nociception, the triterpenoid mixture alpha- and beta-amyrin, isolated from Protium heptaphyllum resin, was assessed in two established mouse models of visceral nociception. Mice were pretreated orally with alpha- and beta-amyrin (3, 10, 30, and 100 mg/kg) or vehicle, and the pain-related behavioral responses to intraperitoneal cyclophosphamide or to intracolonic mustard oil were analyzed. The triterpenoid mixture showed a dose-related significant antinociception against the cyclophosphamide-induced bladder pain, and at 100 mg/kg, the nociceptive behavioral expression was almost completely suppressed. Intracolonic mustard oil-induced nociceptive behaviors were maximally inhibited by 10 mg/kg alpha- and beta-amyrin mixture in a naloxone-reversible manner. While pretreatment with ruthenium red (3 mg/kg, s. c.), a non-specific transient receptor potential cation channel V1 (TRPV1) antagonist, also caused significant inhibition, the alpha (2)-adrenoceptor antagonist, yohimbine (2 mg/kg, s. c.), showed no significant effect. The triterpene mixture (10 mg/kg, p. o.) neither altered significantly the pentobarbital sleeping time, nor impaired the ambulation or motor coordination in open-field and rotarod tests, respectively, indicating the absence of sedative or motor abnormalities that could account for its antinociception. These results indicate that the antinociceptive potential of alpha- and beta-amyrin possibly involves the opioid and vanilloid (TRPV1) receptor mechanisms and further suggests that it could be useful to treat visceral pain of intestinal and pelvic origins.


Asunto(s)
Analgésicos/farmacología , Burseraceae/química , Nociceptores/efectos de los fármacos , Ácido Oleanólico/análogos & derivados , Vísceras , Antagonistas Adrenérgicos alfa , Animales , Masculino , Ratones , Estructura Molecular , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Dimensión del Dolor , Extractos Vegetales/química , Extractos Vegetales/farmacología , Resinas de Plantas/química , Resinas de Plantas/farmacología , Rojo de Rutenio/farmacología , Canales Catiónicos TRPV/antagonistas & inhibidores , Triterpenos/química , Triterpenos/farmacología , Yohimbina/farmacología
12.
Vascul Pharmacol ; 43(1): 11-8, 2005 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-15975531

RESUMEN

Previous studies have established the gastroprotective, hypoglycemic, and hypolipidemic effects of trans-dehydrocrotonin (t-DCTN), a major diterpene isolated from the Amazon medicinal plant Croton cajucara. This study aims to examine the potential effects of t-DCTN on hemodynamic parameters that include resting arterial blood pressure and heart rate in vivo, and on left atrial force, spontaneous beating atria, and aortic rings of rats in vitro. Intravenous bolus injections of t-DCTN (5, 10, or 15 mg/kg) to urethane anesthetized normotensive rats reduced the mean arterial pressure and heart rate in a dose-dependent manner. The hypotensive effect of t-DCTN (10 mg/kg) appears not mediated through effects on the muscarinic cholinergic receptor, beta-adrenoceptor, or ganglionic blockade, for it was not affected by atropine, propranolol, or hexamethonium but was abolished by N(w)-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor. The diterpene t-DCTN showed no significant influence on inotropism. In isolated rat aortic rings with intact or denuded endothelium, t-DCTN relaxed the tonic contraction induced by phenylephrine (1 microM). Its vasorelaxant effect seen at smaller concentrations in endothelium intact preparations was, however, abolished in endothelium denuded or in l-NAME treated tissues. These data indicate the hypotensive and bradycardia effects of t-DCTN, possibly related in part to the release of nitric oxide and in part to direct effects on vascular smooth muscle, and cardiac pacemaker activity.


Asunto(s)
Croton/química , Diterpenos de Tipo Clerodano/farmacología , Hemodinámica/efectos de los fármacos , Vasodilatadores/farmacología , Animales , Aorta Torácica/efectos de los fármacos , Atropina/farmacología , Presión Sanguínea/efectos de los fármacos , Inhibidores Enzimáticos/farmacología , Atrios Cardíacos/efectos de los fármacos , Frecuencia Cardíaca/efectos de los fármacos , Compuestos de Hexametonio/farmacología , Técnicas In Vitro , Masculino , NG-Nitroarginina Metil Éster/farmacología , Óxido Nítrico Sintasa/antagonistas & inhibidores , Óxido Nítrico Sintasa de Tipo III , Fenilefrina/farmacología , Ratas , Ratas Wistar , Vasoconstrictores/farmacología
13.
Life Sci ; 77(23): 2942-52, 2005 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-15964027

RESUMEN

The triterpene mixture, alpha- and beta-amyrin, isolated from Protium heptaphyllum resin was evaluated on capsaicin-evoked nociception in mice. Orally administered alpha- and beta-amyrin (3 to 100 mg/kg) significantly suppressed the nociceptive behaviors--evoked by either subplantar (1.6 microg) or intracolonic (149 microg) application of capsaicin. The antinociception produced by alpha- and beta-amyrin against subplantar capsaicin-induced paw-licking behavior was neither potentiated nor attenuated by ruthenium red (1.5 mg/kg, s.c.), a non-specific antagonist of vanilloid receptor (TRPV1), but was greatly abolished in animals pretreated with naloxone (2 mg/kg, s.c.), suggesting an opioid mechanism. However, participation of alpha2-adrenoceptor involvement was unlikely since yohimbine (2 mg/kg, i.p.) pretreatment failed to block the antinociceptive effect of alpha- and beta-amyrin in the experimental model of visceral nociception evoked by intracolonic capsaicin. The triterpene mixture (3 to 30 mg/kg, p.o.) neither altered significantly the pentobarbital sleeping time, nor impaired the ambulation or motor coordination in open-field and rota-rod tests, respectively, indicating the absence of sedative or motor abnormality that could account for its antinociception. Nevertheless, alpha- and beta-amyrin could significantly block the capsaicin (10 mg/kg, s.c.)-induced hyperthermic response but not the initial hypothermia. These results suggest that the triterpene mixture, alpha- and beta-amyrin has an analgesia inducing effect, possibly involving vanilloid receptor (TRPV1) and an opioid mechanism.


Asunto(s)
Analgésicos/uso terapéutico , Burseraceae/química , Ácido Oleanólico/análogos & derivados , Dolor/tratamiento farmacológico , Administración Oral , Analgésicos/farmacología , Animales , Conducta Animal/efectos de los fármacos , Capsaicina/administración & dosificación , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Combinación de Medicamentos , Hipotermia/inducido químicamente , Ratones , Actividad Motora/efectos de los fármacos , Ácido Oleanólico/farmacología , Ácido Oleanólico/uso terapéutico , Dolor/inducido químicamente , Equilibrio Postural/efectos de los fármacos , Resinas de Plantas/farmacología , Resinas de Plantas/uso terapéutico , Sueño/efectos de los fármacos
14.
J Ethnopharmacol ; 98(1-2): 103-8, 2005 Apr 08.
Artículo en Inglés | MEDLINE | ID: mdl-15763370

RESUMEN

In the search of hepatoprotective agents from natural sources, alpha- and beta-amyrin, a triterpene mixture isolated from the trunk wood resin of folk medicinal plant, Protium heptaphyllum was tested against acetaminophen-induced liver injury in mice. Liver injury was analysed by quantifying the serum enzyme activities and by histopathological observations. In mice, acetaminophen (500 mg/kg, p.o.) caused fulminant liver damage characterized by centrilobular necrosis with inflammatory cell infiltration, an increase in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, a decrease in hepatic glutathione (GSH) and 50% mortality. Pretreatment with alpha- and beta-amyrin (50 and 100 mg/kg, i.p. at 48, 24, and 2 h before acetaminophen) attenuated the acetaminophen-induced acute increase in serum ALT and AST activities, replenished the depleted hepatic GSH, and considerably reduced the histopathological alterations in a manner similar to N-acetylcysteine, a sulfhydryls donor. Also, the acetaminophen-associated mortality was completely suppressed by terpenoid pretreatment. Further, alpha- and beta-amyrin could potentiate the pentobarbital (50 mg/kg, i.p.) sleeping time, suggesting the possible suppression of liver cytochrome-P450. These findings indicate the hepatoprotective potential of alpha- and beta-amyrin against toxic liver injury and suggest that the diminution in oxidative stress and toxic metabolite formation as likely mechanisms involved in its hepatoprotection. In conclusion, this study supports the traditional use of Protium heptaphyllum resin as a medicinal agent and suggests the feasibility of developing herbal drugs for treatment of liver disorders.


Asunto(s)
Burseraceae/química , Fallo Hepático Agudo/tratamiento farmacológico , Fitoterapia , Plantas Medicinales/química , Sustancias Protectoras/farmacología , Triterpenos/uso terapéutico , Acetaminofén , Administración Oral , Alanina Transaminasa/efectos de los fármacos , Alanina Transaminasa/metabolismo , Animales , Aspartato Aminotransferasas/efectos de los fármacos , Aspartato Aminotransferasas/metabolismo , Modelos Animales de Enfermedad , Esquema de Medicación , Sinergismo Farmacológico , Glutatión/antagonistas & inhibidores , Glutatión/efectos de los fármacos , Glutatión/metabolismo , Inyecciones Intraperitoneales , Fallo Hepático Agudo/inducido químicamente , Fallo Hepático Agudo/mortalidad , Masculino , Ratones , Necrosis/inducido químicamente , Necrosis/patología , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/química , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/uso terapéutico , Pentobarbital/farmacología , Corteza de la Planta/química , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/uso terapéutico , Resinas de Plantas/química , Resinas de Plantas/farmacología , Sueño/efectos de los fármacos
15.
Planta Med ; 70(8): 780-2, 2004 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-15368675

RESUMEN

This investigation evaluated the role of capsaicin-sensitive afferent neurons in the gastroprotective effect of alpha- and beta-amyrin, a triterpenoid mixture isolated from Protium heptaphyllum resin. Gastric mucosai damage was induced in mice by intragastric ethanol and assessed by planimetry. Mice pretreated orally with the amyrin mixture (50 and 100 mg/kg) or capsaicin (2.5 and 5 mg/kg), the pungent principle from red hot peppers, showed a significantly lower intensity of ethanol-associated gastric mucosal damage, in relation to vehicle-treated controls. At higher doses both these agents produced either a diminished protection or no significant effect. The maximal gastroprotection that was observed at the dose of 100 mg/kg amyrin mixture was almost abolished in mice with their sensory afferents chemically ablated by a neurotoxic dose of capsaicin, suggesting that the gastro-protective mechanism of alpha- and beta-amyrin mixture involves at least in part the activation of capsaicin-sensitive primary afferent neurons.


Asunto(s)
Burseraceae , Gastritis/tratamiento farmacológico , Fármacos Gastrointestinales/farmacología , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacología , Fitoterapia , Administración Oral , Animales , Capsaicina , Relación Dosis-Respuesta a Droga , Quimioterapia Combinada , Etanol , Gastritis/inducido químicamente , Fármacos Gastrointestinales/administración & dosificación , Fármacos Gastrointestinales/química , Fármacos Gastrointestinales/uso terapéutico , Masculino , Ratones , Neuronas Aferentes/efectos de los fármacos , Ácido Oleanólico/administración & dosificación , Ácido Oleanólico/química , Ácido Oleanólico/uso terapéutico , Madera
16.
Pharmacol Biochem Behav ; 78(4): 719-25, 2004 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-15301927

RESUMEN

In the search for natural compounds useful against pruritus, alpha,beta-amyrins, the pentacyclic triterpenes isolated from the resin of popular medicinal plant Protium heptaphyllum were examined on scratching behavior induced by dextran T40 and compound 48/80 in mice. The animals were pretreated orally with alpha,beta-amyrins (50, 100 and 200 mg/kg) or cyproheptadine (10 mg/kg), an antagonist of histamine and serotonin receptors and 2 h later, they were given subcutaneous injections of dextran T40 (75 mg/kg) or compound 48/80 (3 mg/kg) into the rostral back, and scratching was quantified for 20 min. The scratching behavior induced by dextran T40 and compound 48/80 was significantly inhibited in mice pretreated with alpha,beta-amyrins (100 and 200 mg/kg) or cyproheptadine (10 mg/kg), In addition, the compound 48/80-elicited degranulation of rat peritoneal mast cells (ex vivo) was also markedly reduced in animals pretreated with alpha,beta-amyrins (100 mg/kg) or ketotifen (1 mg/kg), a known mast cell stabilizer. In the open-field test, alpha,beta-amyrins (100 and 200 mg/kg)-pretreated mice showed no impairment of spontaneous locomotion, suggesting that these triterpenoids possess no sedative activity that could account for suppression of scratching behavior. These results clearly indicate the antipruritic effect of alpha,beta-amyrins and suggest that this effect may be related to a stabilizing action on mast cell membrane.


Asunto(s)
Conducta Animal/efectos de los fármacos , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacología , Prurito/tratamiento farmacológico , Prurito/psicología , Analgésicos Opioides/farmacología , Animales , Degranulación de la Célula/efectos de los fármacos , Ciproheptadina/farmacología , Dextranos , Endorfinas/fisiología , Femenino , Antagonistas de los Receptores Histamínicos H1/farmacología , Cetotifen/farmacología , Mastocitos/efectos de los fármacos , Mastocitos/ultraestructura , Ratones , Morfina/farmacología , Actividad Motora/efectos de los fármacos , Naloxona/farmacología , Antagonistas de Narcóticos/farmacología , Cavidad Peritoneal/citología , Prurito/inducido químicamente , Receptores Opioides mu/efectos de los fármacos , p-Metoxi-N-metilfenetilamina
17.
Pharmacol Res ; 49(2): 105-11, 2004 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-14643690

RESUMEN

The natural resin collected from the trunk wood of Protium heptaphyllum is used in folk medicine to treat inflammatory conditions and to hasten wound repair. In the search of new potential anti-inflammatory agents with gastroprotective property, the present study evaluated its effects in experimental models of gastric ulcer and inflammation. In mice, the resin (200 and 400 mg/kg) significantly attenuated the gastric damage induced by ethanol or acidified ethanol (HCl/ethanol), in a manner similar to N-acetyl-L-cysteine (NAC), a replenisher of sulfhydryls. Unlike NAC the resin failed to restore the ethanol-induced depletion of non-protein sulfhydryl content, indicating a different mechanism of gastroprotection. However, in 4-h pylorus-ligated rats, the resin significantly reduced the total acidity without much change in gastric secretory volume. In rats, at similar doses the resin did not modify the hind-paw edema induced by carrageenan, but effectively reduced the formation of cotton pellet-induced granuloma, suggesting its inhibitory effect on collagen formation but not on acute edema. Furthermore, the vascular permeability increase induced by acetic acid was significantly reduced in mice that received 400 mg/kg resin. The resin demonstrated no overt toxicity in mice up to an oral dose of 5 g/kg. Phytochemical analysis revealed the presence of alpha- and beta-amyrins as principal triterpenoid constituents of resin, which were previously described to have anti-ulcer property. These findings indicate the potential gastroprotective and anti-inflammatory property of P. heptaphyllum resin and further support its popular use in gastrointestinal disorders.


Asunto(s)
Antiinflamatorios/uso terapéutico , Antiulcerosos/uso terapéutico , Burseraceae , Resinas de Plantas/uso terapéutico , Úlcera Gástrica/prevención & control , Ácido Acético , Animales , Antiinflamatorios/toxicidad , Antiulcerosos/toxicidad , Brasil , Permeabilidad Capilar/efectos de los fármacos , Carragenina , Modelos Animales de Enfermedad , Edema/inducido químicamente , Etanol , Pie , Ácido Gástrico/metabolismo , Granuloma de Cuerpo Extraño/etiología , Granuloma de Cuerpo Extraño/prevención & control , Ácido Clorhídrico , Masculino , Ratones , Plantas Medicinales , Ratas , Ratas Wistar , Resinas de Plantas/química , Resinas de Plantas/toxicidad , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Compuestos de Sulfhidrilo/metabolismo , Pruebas de Toxicidad Aguda
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