RESUMEN

Hyptis crenata, commonly known as "salva-do-Marajó", "hortelã-do-campo", and "hortelãzinha", is used in folk medicine in Northeast Brazil as tea or infusion to treat inflammatory diseases. Due to the pharmacological efficacy and the low toxicity of the essential oil of Hyptis crenata (EOHc), we decided to investigate the EOHc antiedematogenic effect in experimental models of inflammation. EOHc was administrated orally at doses of 10-300 mg/kg to male Swiss albino mice. Paw edema was induced by subcutaneous injection in the right hind paw of inflammatory stimuli (carrageenan, dextran, histamine, serotonin, and bradykinin) 60 min after administration of EOHc. EOHc significantly inhibited the induced edema. The inhibitory effect of EOHc on dextran-induced edema extended throughout the experimental time. For the 30, 100, and 300 mg/kg doses of EOHc, the inhibition was of 40.28±1.70, 51.18±2.69, and 59.24±2.13%, respectively. The EOHc inhibitory effect on carrageenan-induced edema started at 10 mg/kg at the second hour (h) and was maintained throughout the observation period. At 30, 100, and 300 mg/kg doses the inhibition started earlier, from 30 min. At the edema peak of 180 min, 56, 76, and 82% inhibition was observed for 30, 100, and 300 mg/kg doses, respectively. Additionally, the effect of EOHc on carrageenan-induced paw edema was influenced by the time of administration. The EOHc also inhibited myeloperoxidase activity. In conclusion, the EOHc showed a potent effect, both preventing and reversing the edema, consistent with its anti-inflammatory use in folk medicine.

Asunto(s)

Edema/tratamiento farmacológico , Hyptis/química , Inflamación/tratamiento farmacológico , Aceites Volátiles/uso terapéutico , Animales , Brasil , Carragenina , Edema/inducido químicamente , Inflamación/inducido químicamente , Masculino , Ratones , Extractos Vegetales/uso terapéutico

RESUMEN

Hyptis crenata, commonly known as "salva-do-Marajó", "hortelã-do-campo", and "hortelãzinha", is used in folk medicine in Northeast Brazil as tea or infusion to treat inflammatory diseases. Due to the pharmacological efficacy and the low toxicity of the essential oil of Hyptis crenata (EOHc), we decided to investigate the EOHc antiedematogenic effect in experimental models of inflammation. EOHc was administrated orally at doses of 10-300 mg/kg to male Swiss albino mice. Paw edema was induced by subcutaneous injection in the right hind paw of inflammatory stimuli (carrageenan, dextran, histamine, serotonin, and bradykinin) 60 min after administration of EOHc. EOHc significantly inhibited the induced edema. The inhibitory effect of EOHc on dextran-induced edema extended throughout the experimental time. For the 30, 100, and 300 mg/kg doses of EOHc, the inhibition was of 40.28±1.70, 51.18±2.69, and 59.24±2.13%, respectively. The EOHc inhibitory effect on carrageenan-induced edema started at 10 mg/kg at the second hour (h) and was maintained throughout the observation period. At 30, 100, and 300 mg/kg doses the inhibition started earlier, from 30 min. At the edema peak of 180 min, 56, 76, and 82% inhibition was observed for 30, 100, and 300 mg/kg doses, respectively. Additionally, the effect of EOHc on carrageenan-induced paw edema was influenced by the time of administration. The EOHc also inhibited myeloperoxidase activity. In conclusion, the EOHc showed a potent effect, both preventing and reversing the edema, consistent with its anti-inflammatory use in folk medicine.

Asunto(s)

Animales , Masculino , Conejos , Aceites Volátiles/uso terapéutico , Hyptis/química , Edema/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Brasil , Extractos Vegetales/uso terapéutico , Carragenina , Edema/inducido químicamente , Inflamación/inducido químicamente

RESUMEN

Essential oils (EO) are volatile liquids responsible for the aroma of plants. Pterodon polygalaeflorus seeds have received widespread use in folk medicine for the treatment of inflammatory diseases. For this reason and because Pterodon polygalaeflorus seeds have great EO content, which is frequently pharmacologically active, the present study aimed to evaluate the antinociceptive effect of EO from Pterodon polygalaeflorus (EOPPgfl) and its acute toxic effects. The EEOPPgfl sample, which was extracted by steam distillation of the seeds, had a yield of 2.4% of the seeds weight and had, as major constituents, beta-elemene (48.19%), trans-caryophyllene (19.51%), and epi-bicyclosesquiphellandrene (12.24%). The EOPPgfl sample showed mild acute toxicity and its calculated median lethal dose (LD50) was 3.38 g/kg. EOPPgfl (20-60 mg/kg) showed antinociceptive activity as evidenced by several tests and inhibited writhing induced by acetic acid. The maximum effect was obtained with the 30 mg/kg dose and at 60 min after its administration. EOPPgfl also decreased formalin-induced nociception, as verified by the inhibition of the first and second phase of the formalin test. At 30 mg/kg, EOPPgfl also decreased thermally stimulated nociception. Nociception may be related to inflammatory and antiedematogenic activity and at doses ranging 10-100 mg/kg, EOPPgfl blocked dextran- and carrageenan-induced edema. The results demonstrated that EOPPgfl presented, at doses approximately 100 times smaller than LD50, an antinociceptive effect that probably was due to anti-inflammatory activities.

Asunto(s)

Analgésicos/farmacología , Fabaceae/química , Nocicepción/efectos de los fármacos , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Aceites de Plantas/farmacología , Animales , Antiinflamatorios/farmacología , Ratones , Dimensión del Dolor , Distribución Aleatoria , Reproducibilidad de los Resultados , Semillas/química , Factores de Tiempo , Resultado del Tratamiento

RESUMEN

Essential oils (EO) are volatile liquids responsible for the aroma of plants. Pterodon polygalaeflorus seeds have received widespread use in folk medicine for the treatment of inflammatory diseases. For this reason and because Pterodon polygalaeflorus seeds have great EO content, which is frequently pharmacologically active, the present study aimed to evaluate the antinociceptive effect of EO from Pterodon polygalaeflorus (EOPPgfl) and its acute toxic effects. The EEOPPgfl sample, which was extracted by steam distillation of the seeds, had a yield of 2.4% of the seeds weight and had, as major constituents, beta-elemene (48.19%), trans-caryophyllene (19.51%), and epi-bicyclosesquiphellandrene (12.24%). The EOPPgfl sample showed mild acute toxicity and its calculated median lethal dose (LD50) was 3.38 g/kg. EOPPgfl (20-60 mg/kg) showed antinociceptive activity as evidenced by several tests and inhibited writhing induced by acetic acid. The maximum effect was obtained with the 30 mg/kg dose and at 60 min after its administration. EOPPgfl also decreased formalin-induced nociception, as verified by the inhibition of the first and second phase of the formalin test. At 30 mg/kg, EOPPgfl also decreased thermally stimulated nociception. Nociception may be related to inflammatory and antiedematogenic activity and at doses ranging 10-100 mg/kg, EOPPgfl blocked dextran- and carrageenan-induced edema. The results demonstrated that EOPPgfl presented, at doses approximately 100 times smaller than LD50, an antinociceptive effect that probably was due to anti-inflammatory activities.

Asunto(s)

Animales , Conejos , Aceites de Plantas/farmacología , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Nocicepción/efectos de los fármacos , Analgésicos/farmacología , Fabaceae/química , Semillas/química , Factores de Tiempo , Dimensión del Dolor , Distribución Aleatoria , Reproducibilidad de los Resultados , Resultado del Tratamiento , Antiinflamatorios/farmacología

RESUMEN

Estragole is a volatile terpenoid, which occurs naturally as a constituent of the essential oils of many plants. It has several pharmacological and biological activities. The objective of the present study was to investigate the mechanism of action of estragole on neuronal excitability. Intact and dissociated dorsal root ganglion neurons of rats were used to record action potential and Na+ currents with intracellular and patch-clamp techniques, respectively. Estragole blocked the generation of action potentials in cells with or without inflexions on their descendant (repolarization) phase (Ninf and N0 neurons, respectively) in a concentration-dependent manner. The resting potentials and input resistances of Ninf and N0 cells were not altered by estragole (2, 4, and 6 mM). Estragole also inhibited total Na+ current and tetrodotoxin-resistant Na+ current in a concentration-dependent manner (IC50 of 3.2 and 3.6 mM, respectively). Kinetic analysis of Na+ current in the presence of 4 mM estragole showed a statistically significant reduction of fast and slow inactivation time constants, indicating an acceleration of the inactivation process. These data demonstrate that estragole blocks neuronal excitability by direct inhibition of Na+ channel conductance activation. This action of estragole is likely to be relevant to the understanding of the mechanisms of several pharmacological effects of this substance.

RESUMEN

Estragole is a volatile terpenoid, which occurs naturally as a constituent of the essential oils of many plants. It has several pharmacological and biological activities. The objective of the present study was to investigate the mechanism of action of estragole on neuronal excitability. Intact and dissociated dorsal root ganglion neurons of rats were used to record action potential and Na+ currents with intracellular and patch-clamp techniques, respectively. Estragole blocked the generation of action potentials in cells with or without inflexions on their descendant (repolarization) phase (Ninf and N0 neurons, respectively) in a concentration-dependent manner. The resting potentials and input resistances of Ninf and N0 cells were not altered by estragole (2, 4, and 6 mM). Estragole also inhibited total Na+ current and tetrodotoxin-resistant Na+ current in a concentration-dependent manner (IC50 of 3.2 and 3.6 mM, respectively). Kinetic analysis of Na+ current in the presence of 4 mM estragole showed a statistically significant reduction of fast and slow inactivation time constants, indicating an acceleration of the inactivation process. These data demonstrate that estragole blocks neuronal excitability by direct inhibition of Na+ channel conductance activation. This action of estragole is likely to be relevant to the understanding of the mechanisms of several pharmacological effects of this substance.

RESUMEN

Vascular disease has importance in chronic diabetes mellitus but long-term impact of maternal diabetes (MD) on vascular function in the offspring is poorly investigated. This study aimed to examine the alterations produced by MD in K (+) channels activity on endothelium-dependent aortic relaxation induced by acetylcholine (ACh) in adult offspring rats. Diabetes mellitus was induced in female Wistar rats by streptozotocin (STZ; 42 mg/kg, i. p.) injected on the 7 (th) day of pregnancy. Body weights of offspring rats from diabetic mothers (O-DR) were significantly lesser than those of offspring rats from control mothers (O-CR). At 120 days of age, triglyceride but not glucose and cholesterol level was significantly higher in O-DR than in O-CR. In aortic preparations from O-DR, norepinephrine (NE)-induced contractions were significantly higher than those observed in O-CR. In aortic preparations from O-DR precontracted with NE (1 muM), vasorelaxant response to either ACh (0.1, 1 and 10 muM) or sodium nitroprusside (0.1, 1 and 10 nM) was significantly reduced when compared to O-CR. In both groups, vasorelaxant responses to ACh were reduced in the presence of tetraethylamonium chloride and 4-aminopyridine. However, pretreatment with glybenclamide reduced vasorelaxant effects of lowest concentration (0.1 muM) of ACh only in preparations from O-CR. Our results suggest a reduced K (+)(ATP) activity in the cholinergic relaxation of aortic rings of adult offspring born to STZ-diabetic mothers.

Asunto(s)

Diabetes Mellitus Experimental/fisiopatología , 4-Aminopiridina/farmacología , Acetilcolina/farmacología , Envejecimiento/fisiología , Animales , Aorta/efectos de los fármacos , Aorta/fisiología , Aorta/fisiopatología , Glucemia/metabolismo , Peso Corporal , Femenino , Norepinefrina/farmacología , Embarazo , Ratas , Ratas Wistar , Tetraetilamonio/farmacología , Triglicéridos/sangre , Vasodilatación/efectos de los fármacos , Vasodilatación/fisiología

RESUMEN

Plants of the genus Croton have been used extensively in the northeast of Brazil for treating various clinical conditions. Previous studies have demonstrated that the essential oil of some specimens of Croton sp. have a relaxing effect on tracheal smooth muscle. Our study aimed to characterize the effects of Croton sonderianus essential oil samples, collected at 1:00 pm (EO-13) and 9:00 pm (EO-21), on rat tracheal smooth muscle. The two samples were submitted to gas chromatography (GC) and mass spectrometry (MS) analysis to identify their components. Rat tracheal smooth muscle strips were used to assess the biological activity. The major constituents of EO-21 were: spathulenol (18.32%), beta-caryophyllene (14.58%) and caryophyllene oxide (8.54%) and the major constituents of EO-13 were bicyclogermacrene (16.29%), beta-phellandrene (15.42%) and beta-caryophyllene (13.82%). These samples showed an antispasmodic effect on tracheal smooth muscle strips pre-contracted with high K+ concentration (80 mM) or with acetylcholine. EO-21 increased baseline tonus while EO-13 provoked a decrease. These results demonstrated that EO-13 and EO-21 have different chemical composition and showed myorelaxant activity. In conclusion, EO-13 and EO-21 may have potential therapeutic use in the treatment of bronchospasm.

Asunto(s)

Croton/química , Músculo Liso/efectos de los fármacos , Aceites Volátiles/farmacología , Tráquea/efectos de los fármacos , Animales , Cromatografía de Gases y Espectrometría de Masas , Masculino , Contracción Muscular/efectos de los fármacos , Músculo Liso/fisiología , Ratas , Ratas Wistar , Tráquea/fisiología

RESUMEN

Various essential oils are rich in carvacrol, a monoterpenic phenol isomeric with thymol. This study was undertaken to assess the vasorelaxant effects of thymol and carvacrol in rat isolated aorta and the putative mechanisms underlying these effects. Thymol and carvacrol produced a concentration-dependent relaxation on the aortic ring preparations pre-contracted using KCl (IC(50) value of 64.40 +/- 4.41 and 78.80 +/- 11.91 microm, respectively) or using phenylephrine (PHE, 0.1 microm) (IC(50) value of 106.40 +/- 11.37 and 145.40 +/- 6.07 microm, respectively) and inhibited the concentration-response curves of aortic rings to PHE or KCl. In Ca(2+)-free medium with ethylene glycol-bis(2-aminoethylether)-N,N,N',N'-tetraacetic acid (2 mm), thymol and carvacrol both at 1000 microm completely abolished the phasic component of PHE-induced endothelium-containing ring contractions. At 400 microm, thymol and carvacrol significantly reduced the CaCl(2)-induced contractions in Ca(2+)-free medium. Furthermore, both thymol and carvacrol (300 and 1000 microm) significantly reduced the contraction evoked by phorbol dibutyrate (1 microm), an activator of protein kinase C. Magnitude of this inhibitory effect was enhanced in the presence of the Ca2+ pump inhibitor, thapsigargin (1 microm). At 1000 microm, neither thymol nor carvacrol altered the resting potential of vascular smooth muscle cells. In conclusion, thymol and carvacrol induced an endothelium-independent relaxation in rat isolated aorta, an effect that seems mediated through some mechanisms probably involving a transduction pathway between Ca(2+) release from sarcoplasmic reticulum and/or regulation of the Ca2+ sensitivity of the contractile system. Moreover, it's conceivable that thymol and carvacrol, at low concentrations, block the Ca(2+) influx through the membrane.

Asunto(s)

Aorta Torácica/efectos de los fármacos , Monoterpenos/farmacología , Músculo Liso Vascular/efectos de los fármacos , Timol/farmacología , Vasodilatación/efectos de los fármacos , Vasodilatadores/farmacología , Animales , Aorta Torácica/fisiología , Cimenos , Esquema de Medicación , Endotelio Vascular/efectos de los fármacos , Endotelio Vascular/fisiología , Masculino , Monoterpenos/química , Músculo Liso Vascular/fisiología , Técnicas de Cultivo de Órganos , Fenoles/química , Fenoles/farmacología , Ratas , Ratas Wistar , Estereoisomerismo , Timol/química , Vasodilatación/fisiología , Vasodilatadores/química

RESUMEN

Mentha x villosa Huds (Labiatae) is an aromatic herb widely used in folk medicine. Since the essential oil of the herb has many pharmacological activities, including antispasmodic effects, we determined whether the oil and its major constituent, piperitenone oxide (PO), have antinociceptive activity. The essential oil of M. x villosa (EOMV) and PO administered orally at 200 mg/kg (vehicle: 0.1% Tween 80 in water) significantly reduced the writhings induced by acetic acid from control values of 59.5 +/- 3.1 s (N = 10) to 31.9 +/- 2.8 s (N = 10) and 23.8 +/- 3.4 s (N = 10), respectively. When administered at 100 and 200 mg/kg, EOMV reduced the paw licking time for the second phase of the formalin test from the control value of 20.6 +/- 2.1 s (N = 13) to 5.3 +/- 2.2 s (N = 12) and 2.7 +/- 1.2 s (N = 18), respectively. At 100 and 200 mg/kg, PO reduced this second phase to 8.3 +/- 2.7 s (N = 12) and 3.0 +/- 1.2 s (N = 10), respectively. This effect of EOMV and PO was not reversed by naloxone. EOMV and PO had no significant effect on the first phase of the formalin test. As evaluated by the hot-plate and tail immersion test, EOMV and PO, at doses up to 200 mg/kg, showed no analgesic activity. These results show that EOMV and PO have antinociceptive activity and suggest that this effect is probably an indirect anti-inflammatory effect, which does not involve the central nervous system.

Asunto(s)

Analgésicos/uso terapéutico , Mentha/química , Monoterpenos/uso terapéutico , Aceites Volátiles/uso terapéutico , Dolor/tratamiento farmacológico , Aceites de Plantas/uso terapéutico , Analgésicos/aislamiento & purificación , Animales , Masculino , Ratones , Monoterpenos/aislamiento & purificación , Dimensión del Dolor/efectos de los fármacos , Hojas de la Planta/química , Factores de Tiempo

RESUMEN

Mentha x villosa Huds (Labiatae) is an aromatic herb widely used in folk medicine. Since the essential oil of the herb has many pharmacological activities, including antispasmodic effects, we determined whether the oil and its major constituent, piperitenone oxide (PO), have antinociceptive activity. The essential oil of M. x villosa (EOMV) and PO administered orally at 200 mg/kg (vehicle: 0.1% Tween 80 in water) significantly reduced the writhings induced by acetic acid from control values of 59.5 ± 3.1 s (N = 10) to 31.9 ± 2.8 s (N = 10) and 23.8 ± 3.4 s (N = 10), respectively. When administered at 100 and 200 mg/kg, EOMV reduced the paw licking time for the second phase of the formalin test from the control value of 20.6 ± 2.1 s (N = 13) to 5.3 ± 2.2 s (N = 12) and 2.7 ± 1.2 s (N = 18), respectively. At 100 and 200 mg/kg, PO reduced this second phase to 8.3 ± 2.7 s (N = 12) and 3.0 ± 1.2 s (N = 10), respectively. This effect of EOMV and PO was not reversed by naloxone. EOMV and PO had no significant effect on the first phase of the formalin test. As evaluated by the hot-plate and tail immersion test, EOMV and PO, at doses up to 200 mg/kg, showed no analgesic activity. These results show that EOMV and PO have antinociceptive activity and suggest that this effect is probably an indirect anti-inflammatory effect, which does not involve the central nervous system.

Asunto(s)

Animales , Masculino , Ratones , Analgésicos/uso terapéutico , Mentha/química , Monoterpenos/uso terapéutico , Aceites Volátiles/uso terapéutico , Dolor/tratamiento farmacológico , Aceites de Plantas/uso terapéutico , Analgésicos/aislamiento & purificación , Monoterpenos/aislamiento & purificación , Dimensión del Dolor/efectos de los fármacos , Hojas de la Planta/química , Factores de Tiempo

RESUMEN

Alpinia zerumbet (Pers.) Burtt. et Smith is an aromatic plant that is distributed widely in the tropical and sub-tropical regions of the world. In Brazil, where A. zerumbet is called "colonia", it is used widely in folk medicine for the treatment of various diseases, including hypertension. In the present study, the antinociceptive effects of the orally administered essential oil of A. zerumbet (EOAz) were evaluated in male Swiss mice (20-25 g each). In the acetic acid-induced writhing test, EOAz (30, 100 and 300 mg/kg body wt.; n = 10, n = 13 and n = 15, respectively) was effective at all doses. In the hot-plate test, EOAz significantly increased the latency at doses of 100 and 300 mg/kg body wt., but not at 30 mg/kg body wt., at all observation times up to the 180th min (n = 10 for each dose). In the formalin test, EOAz significantly reduced paw licking time in the second phase of the test at 100 mg/kg body wt. (n = 10), but decreased it in both phases at 300 mg/kg body wt. (n = 10). At 30 mg/kg body wt., the effect of EOAz did not differ from control values in either phase of the formalin test (n = 10). Pretreatment with naloxone (5 mg/kgbodywt., i.p.) caused a significant reversal of the analgesic effect of 300 mg/kg body wt. EOAz (n = 8) that was complete for the first phase, but only partial for the second phase of the formalin test. The data show that orally administered OEAz promotes a dose-dependent antinociceptive effect, with a mechanism of action which probably involves the participation of opiate receptors.

Asunto(s)

Analgésicos/farmacología , Dolor/prevención & control , Fitoterapia , Aceites de Plantas/farmacología , Zingiberales , Ácido Acético , Administración Oral , Analgésicos/administración & dosificación , Analgésicos/uso terapéutico , Analgésicos Opioides/administración & dosificación , Analgésicos Opioides/farmacología , Analgésicos Opioides/uso terapéutico , Animales , Relación Dosis-Respuesta a Droga , Formaldehído , Calor , Masculino , Ratones , Dolor/inducido químicamente , Dimensión del Dolor/efectos de los fármacos , Hojas de la Planta , Aceites de Plantas/administración & dosificación , Aceites de Plantas/uso terapéutico

RESUMEN

Alpinia zerumbet, known popularly as "colônia" in Northeastern Brazil, is a medicinal plant that has been used widely in folk medicine as teas and infusions for the treatment of intestinal and cardiovascular diseases, including arterial hypertension. Our previous studies have demonstrated that the essential oil of A. zerumbet (OEAZ) is very active on excitable tissues, such as smooth muscle, and in this study we verified its effects on the compound action potential (CAP) of rat sciatic nerve. EOAZ induced a dose-dependent blockade of the CAP. Control peak-to-peak amplitude and conduction velocity of CAPs were 7.6 +/- 0.43 mV and 80.6 +/- 3.19 m/s, respectively. At 60 microg/ml, EOAZ induced no demonstrable effect. Conduction velocity was significantly reduced at 180 min of preparation exposure to 100 microg/ml of EOAZ. At 300, 600 and 2000 microg/ml doses of EOAZ, the peak-to-peak amplitudes of CAPs following 180 min exposure of the nerve to the drug were reduced significantly, to 75.3 +/- 7.36%, 50.45 +/- 2.17% and 0% respectively, of control value. Conduction velocity was reduced significantly by 300, 600 and 2000 microg/ml of EOAZ, at 180 min, to 83.61 +/- 3.28%, 64.06 +/- 8.21% and 22.7 +/- 5.79%, respectively, of control value. All these effects developed slowly and were reversible upon a 180-min wash.

Asunto(s)

Alpinia , Fitoterapia , Aceites de Plantas/farmacología , Nervio Ciático/efectos de los fármacos , Potenciales de Acción/efectos de los fármacos , Animales , Relación Dosis-Respuesta a Droga , Masculino , Hojas de la Planta , Aceites de Plantas/administración & dosificación , Aceites de Plantas/uso terapéutico , Ratas , Ratas Wistar

RESUMEN

Estragole, a relatively nontoxic terpenoid ether, is an important constituent of many essential oils with widespread applications in folk medicine and aromatherapy and known to have potent local anesthetic activity. We investigated the effects of estragole on the compound action potential (CAP) of the rat sciatic nerve. The experiments were carried out on sciatic nerves dissected from Wistar rats. Nerves, mounted in a moist chamber, were stimulated at a frequency of 0.2 Hz, with electric pulses of 50-100-æs duration at 10-20 V, and evoked CAP were monitored on an oscilloscope and recorded on a computer. CAP control parameters were: peak-to-peak amplitude (PPA), 9.9 ± 0.55 mV (N = 15), conduction velocity, 92.2 ± 4.36 m/s (N = 15), chronaxy, 45.6 ± 3.74 æs (N = 5), and rheobase, 3.9 ± 0.78 V (N = 5). Estragole induced a dose-dependent blockade of the CAP. At 0.6 mM, estragole had no demonstrable effect. At 2.0 and 6.0 mM estragole, PPA was significantly reduced at the end of 180-min exposure of the nerve to the drug to 85.6 ± 3.96 and 13.04 ± 1.80 percent of control, respectively. At 4.0 mM, estragole significantly altered PPA, conduction velocity, chronaxy, and rheobase (P <= 0.05, ANOVA; N = 5) to 49.3 ± 6.21 and 77.7 ± 3.84, 125.9 ± 10.43 and 116.7 ± 4.59 percent, of control, respectively. All of these effects developed slowly and were reversible upon a 300-min wash-out. The data show that estragole dose-dependently blocks nerve excitability.

Asunto(s)

Animales , Ratas , Potenciales de Acción , Aceites Volátiles , Nervio Ciático , Relación Dosis-Respuesta a Droga , Electromiografía , Conducción Nerviosa , Ratas Wistar

RESUMEN

Estragole, a relatively nontoxic terpenoid ether, is an important constituent of many essential oils with widespread applications in folk medicine and aromatherapy and known to have potent local anesthetic activity. We investigated the effects of estragole on the compound action potential (CAP) of the rat sciatic nerve. The experiments were carried out on sciatic nerves dissected from Wistar rats. Nerves, mounted in a moist chamber, were stimulated at a frequency of 0.2 Hz, with electric pulses of 50-100-micros duration at 10-20 V, and evoked CAP were monitored on an oscilloscope and recorded on a computer. CAP control parameters were: peak-to-peak amplitude (PPA), 9.9 +/- 0.55 mV (N = 15), conduction velocity, 92.2 +/- 4.36 m/s (N = 15), chronaxy, 45.6 +/- 3.74 micros (N = 5), and rheobase, 3.9 +/- 0.78 V (N = 5). Estragole induced a dose-dependent blockade of the CAP. At 0.6 mM, estragole had no demonstrable effect. At 2.0 and 6.0 mM estragole, PPA was significantly reduced at the end of 180-min exposure of the nerve to the drug to 85.6 +/- 3.96 and 13.04 +/- 1.80% of control, respectively. At 4.0 mM, estragole significantly altered PPA, conduction velocity, chronaxy, and rheobase (P < or = 0.05, ANOVA; N = 5) to 49.3 +/- 6.21 and 77.7 +/- 3.84, 125.9 +/- 10.43 and 116.7 +/- 4.59%, of control, respectively. All of these effects developed slowly and were reversible upon a 300-min wash-out. The data show that estragole dose-dependently blocks nerve excitability.

Asunto(s)

Potenciales de Acción/efectos de los fármacos , Anisoles/farmacología , Aceites Volátiles/farmacología , Nervio Ciático/efectos de los fármacos , Derivados de Alilbenceno , Animales , Relación Dosis-Respuesta a Droga , Electromiografía , Conducción Nerviosa/efectos de los fármacos , Ratas , Ratas Wistar

RESUMEN

Croton nepetaefolius Baill., is an aromatic plant native to the northeast of Brazil where it is extensively used in folk medicine as a sedative, orexigen and antispasmodic agent. In the present study the antinociceptive effects of the essential oil of C. nepetaefolius (EOCn), administered orally, were evaluated in male Swiss mice (20-25 g). In the acetic acid-induced writhing test, EOCn (100 and 300 mg/kg; N = 14 and N = 12, respectively) was effective at the highest dose. In the hot-plate test, EOCn at 30 and 300 mg/kg, but not at 3 mg/kg, significantly increased the latency at all observation times up to the 180th min (N = 12 for each dose). In the formalin test, EOCn significantly reduced paw licking in the second phase of the test at 100 mg/kg (N = 12), but decreased it in both phases at 300 mg/kg (N = 12). At 30 mg/kg, the effect of EOCn did not differ from control values in either phase of the formalin test (N = 6). Pretreatment with naloxone (5 mg/kg, ip) significantly reversed the analgesic effect of morphine (5 mg/kg, sc) on both phases, but not that of EOCn at 300 mg/kg (N = 6) on both phases of the formalin test. The data show that orally administered EOCn promotes a dose-dependent antinociceptive effect whose mechanisms remain to be elucidated.

Asunto(s)

Analgésicos/uso terapéutico , Euphorbiaceae , Aceites Volátiles/uso terapéutico , Dimensión del Dolor/efectos de los fármacos , Plantas Medicinales , Administración Oral , Animales , Evaluación Preclínica de Medicamentos , Masculino , Ratones

RESUMEN

Croton nepetaefolius Baill., is an aromatic plant native to the northeast of Brazil where it is extensively used in folk medicine as a sedative, orexigen and antispasmodic agent. In the present study the antinociceptive effects of the essential oil of C. nepetaefolius (EOCn), administered orally, were evaluated in male Swiss mice (20-25 g). In the acetic acid-induced writhing test, EOCn (100 and 300 mg/kg; N = 14 and N = 12, respectively) was effective at the highest dose. In the hot-plate test, EOCn at 30 and 300 mg/kg, but not at 3 mg/kg, significantly increased the latency at all observation times up to the 180th min (N = 12 for each dose). In the formalin test, EOCn significantly reduced paw licking in the second phase of the test at 100 mg/kg (N = 12), but decreased it in both phases at 300 mg/kg (N = 12). At 30 mg/kg, the effect of EOCn did not differ from control values in either phase of the formalin test (N = 6). Pretreatment with naloxone (5 mg/kg, ip) significantly reversed the analgesic effect of morphine (5 mg/kg, sc) on both phases, but not that of EOCn at 300 mg/kg (N = 6) on both phases of the formalin test. The data show that orally administered EOCn promotes a dose-dependent antinociceptive effect whose mechanisms remain to be elucidated

Asunto(s)

Animales , Masculino , Ratones , Analgésicos , Euphorbiaceae , Dimensión del Dolor , Aceites de Plantas , Plantas Medicinales , Administración Oral

RESUMEN

Croton zehntneri is an aromatic plant native to Northeastern Brazil, where it is often used in folk medicine. In the present study the antinociceptive effects of the essential oil of Croton zehntneri (EOCz) were evaluated in mice. EOCz administered orally at doses of 100 and 300 mg/kg reduced paw licking time in the second phase of the formalin test from the control value of 41.61 + or - 8.62 to 12.01 + or - 7.97 and 6.57 + or - 3.42 s, respectively. During the first phase of the formalin test only 300 mg/kg induced a significant alteration (from 58.2 + or - 7.02, control, to 28.7 + or - 4.73 s). The number of contortions in response to intraperitoneal injections of acetic acid did not differ significantly between controls (80.6 + or - 9.01) and experimental (300 mg/kg body weight) animals (89.1 + or - 9.53 percent of the control numbers; P > or = 0.05, Student t-test). In the hot-plate test, EOCz at doses > or = 100 mg/kg significantly increased the latency time with respect to controls (11.2 + or - 0.80). At 100 and 300 mg/kg this increase persisted for 180 and 240 min, respectively. The data show that EOCz is effective as an antinociceptive agent

Asunto(s)

Animales , Masculino , Ratones , Analgésicos/administración & dosificación , Aceite de Crotón/administración & dosificación , Dolor , Administración Oral , Análisis de Varianza , Dimensión del Dolor , Tiempo de Reacción

RESUMEN

Croton zehntneri is an aromatic plant native to Northeastern Brazil, where it is often used in folk medicine. In the present study the antinociceptive effects of the essential oil of Croton zehntneri (EOCz) were evaluated in mice. EOCz administered orally at doses of 100 and 300 mg/kg reduced paw licking time in the second phase of the formalin test from the control value of 41.61 +/- 8.62 to 12.01 +/- 7.97 and 6.57 +/- 3.42 s, respectively. During the first phase of the formalin test only 300 mg/kg induced a significant alteration (from 58.2 +/- 7.02, control, to 28.7 +/- 4.73 s). The number of contortions in response to intraperitoneal injections of acetic acid did not differ significantly between controls (80.6 +/- 9.01) and experimental (300 mg/kg body weight) animals (89.1 +/- 9.53% of the control numbers; P > or =0.05, Student t-test). In the hot-plate test, EOCz at doses > or =100 mg/kg significantly increased the latency time with respect to controls (11.2 +/- 0.80). At 100 and 300 mg/kg this increase persisted for 180 and 240 min, respectively. The data show that EOCz is effective as an antinociceptive agent.

Asunto(s)

Analgésicos/administración & dosificación , Aceite de Crotón/administración & dosificación , Dolor/tratamiento farmacológico , Administración Oral , Análisis de Varianza , Animales , Evaluación Preclínica de Medicamentos , Masculino , Ratones , Dimensión del Dolor , Tiempo de Reacción

RESUMEN

The effects of the essential oil of Alpinia speciosa Schum (EOAS) on rat ileum were studied. EOAS (0.1-600 microg/mL) reversibly relaxed ileal basal tonus. Submaximal contractions induced by 60 mM KCl or acetylcholine were concentration dependently inhibited by EOAS with similar IC(50) values ( approximately 44 and 48 microg/mL, respectively). These results show that EOAS possesses both relaxant and antispasmodic actions in the ileum.

Asunto(s)

Íleon/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Parasimpatolíticos/farmacología , Aceites de Plantas/farmacología , Zingiberales , Animales , Masculino , Contracción Muscular/efectos de los fármacos , Aceites Volátiles/farmacología , Ratas