RESUMEN
Byrsonima crassifolia (Malpighiaceae) has been used in traditional medicine for the treatment of some mental-related diseases; however, its specific neuropharmacological activities remain to be defined. The present study evaluates the anxiolytic, anticonvulsant, antidepressant, sedative effects produced by the extracts of Byrsonima crassifolia, and their influence on motor activity in ICR mice. Additionally, we determine the acute toxicity profiles of the Byrsonima crassifolia extracts and the presence of neuroactive constituents. Our results show that the methanolic extract of Byrsonima crassifolia produces a significant (P<0.05) antidepressant effect in the forced swimming test in mice at 500 mg/kg dose. However, it does not possess anxiolytic, sedative, or anticonvulsant properties, and does not cause a reduction of mice locomotion (P>0.05). Although the main compound of the methanolic extract was identified as quercetin 3-O-xyloside (12 mg/kg), our findings suggest that flavonoids, such as rutin (4.4 mg/kg), quercetin (1.4 mg/kg) and hesperidin (0.7 mg/kg), may be involved in the antidepressant effects. To the best of our knowledge, the present study constitutes the first report on the presence of the flavonoids with neuropharmacological activity rutin and hesperidin in Byrsonima crassifolia. In conclusion, the present results showed that the methanolic extract standardized on flavonoids content of Byrsonima crassifolia possesses potential antidepressant-like effects in the FST in mice, and could be considered as relatively safe toxicologically with no deaths of mice when orally administered at 2000 mg/kg.
Asunto(s)
Antidepresivos/farmacología , Flavonoides/farmacología , Malpighiaceae/química , Extractos Vegetales/farmacología , Administración Oral , Animales , Ansiolíticos/farmacología , Antidepresivos/química , Cromatografía Líquida de Alta Presión , Evaluación de Medicamentos , Sistema Nervioso Entérico/efectos de los fármacos , Prueba de Esfuerzo , Femenino , Flavonoides/química , Flavonoides/toxicidad , Cobayas , Pérdida de Tono Postural/efectos de los fármacos , Malpighiaceae/toxicidad , Metanol/química , Ratones , Ratones Endogámicos ICR , Actividad Motora , Pentobarbital/farmacología , Pentilenotetrazol/efectos adversos , Extractos Vegetales/administración & dosificación , Extractos Vegetales/normas , Extractos Vegetales/toxicidad , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Natación , Pruebas de Toxicidad AgudaRESUMEN
The aim of the present work is to evaluate the putative antidepressant-like effects of a hydro-ethanolic extract (CEAp) and their fractions from the aerial parts of Aloysia polystachya (Griseb.) Moldenke (Verbenaceae) on the performance of male mice in the forced swimming test (FST). A single dose (100.0mg/kgp.o.) of CEAp, in male mice provoked a significant reduction of the immobility time (p<0.01). Such effect was also observed with short-term treatment (7 days) with single doses of 1.0 (p<0.01), 10.0 (p<0.05) and 100.0 (p<0.05)mg/kg/day of CEAp. Additionally, in a different set of experiments, repeated administration in a 24-h period (24, 18 and 1h before swimming test) with doses of 1.0 (p<0.05) and 10.0 (p<0.05)mg/kg p.o., of CEAp and 10.0mg/kgp.o., (p<0.05) of ethyl acetate fraction, provoked significant reduction of the immobility time of male mice in the FST. Moreover, it was noted important differences in the onset of the antidepressant-like effect in the FST, depending on the modality of treatment with CEAp (acute, short-term or repeated). Both, efficacy and potency were higher when repeated administration of CEAp was used, and surprisingly the dose of 10mg/kg (24, 18 and 1h before swimming test) was more effective than imipramine. In the same way, the short term administration (7 days) improved significantly efficacy and potency of the CEAp in comparison to a single dose treatment. The ethyl acetate fraction submitted to TLC demonstrated that main and minor components are phenolics and terpenes, respectively. In addition, this fraction gives a negative Shinoda's test for flavonoids. These results indicate an antidepressant-like profile of action for the hydro-ethanolic extract and the component(s) of the ethyl acetate fraction obtained from A. polystachya, which deserve further investigation.
Asunto(s)
Antidepresivos/análisis , Pérdida de Tono Postural/efectos de los fármacos , Fitoterapia , Extractos Vegetales/administración & dosificación , Verbenaceae/química , Animales , Depresión/tratamiento farmacológico , Masculino , Ratones , Estrés Psicológico/tratamiento farmacológico , Natación/psicologíaRESUMEN
The aim of the present work is to demonstrate the putative sedative and anxiolytic-like effects of a hydro-ethanolic extract obtained from the aerial parts of Aloysia polystachya (Verbenaceae) in male mice using several behavioural assays. Groups of male mice orally treated with doses of 1.0, 10.0 and 100.0 mg/kg of the extract did not show any significant alteration of their locomotor activity, body temperature or motor coordination. The same treatment increased the duration of the sleeping time induced by 30.0 mg/kg i.p. of sodium pentobarbital. However, the sleeping time induced by ethyl ether was not modified by the oral administration of the extract, not confirming the putative sedative effect of the plant. The ethanolic extract also significantly increased the percentage of both entries (1.0 and 100.0 mg/kg) and the time spent (10.0 and 100.0 mg/kg) into the open arms of the elevated plus maze (EPM). Nevertheless, the binding of (3)H-flunitrazepam ((3)H-FNZ) to the benzodiazepine binding site (BDZ-bs), in washed crude synaptosomal membranes from rat cerebral cortex, was not affected by the semi-purified components from Aloysia polystachya. These results indicate an anxiolytic-like profile of action for the extract of Aloysia polystachya without sedative side effect, being this activity probably mediated by other mechanism than BDZ-bs modulation at the GABA(A) receptors.
Asunto(s)
Ansiolíticos/farmacología , Extractos Vegetales/farmacología , Verbenaceae , Animales , Conducta Animal/efectos de los fármacos , Temperatura Corporal/efectos de los fármacos , Flunitrazepam/metabolismo , Masculino , Aprendizaje por Laberinto/efectos de los fármacos , Ratones , Actividad Motora/efectos de los fármacos , Sueño/efectos de los fármacosRESUMEN
Behavioral effects of a hydroalcoholic (60% ethanol) extract from the leaves of Salvia elegans Vahl (Lamiaceae) were studied in male Sprague-Dawley rats. The extract was administered intraperitoneally and its effects on spontaneous motor activity (total motility, locomotion, rearing and grooming behavior) were monitored. Putative anxiolytic and antidepressant properties of Salvia elegans were studied in the elevated plus-maze test (EPM) and in the forced swimming test (FST), respectively. Deleterious effects of Salvia elegans on learning and memory were also studied by using active and passive avoidance paradigms. The results revealed that all doses (3.12, 12.5, 25 and 50 mg/kg) of the extract caused a significant decrease in total motility, locomotion, rearing and grooming behavior. Only the dose of 12.5 mg/kg increased the exploration of the EPM open arms in a similar way to that of diazepam (1 mg/kg). In the FST, all doses of the extract induced a reduction of immobility, in a similar way to that of fluoxetine (10 mg/kg) and imipramine (12.5 mg/kg), along with a significant increase in the time spent in swimming behavior. Acquisition of active avoidance responses was disrupted by pre-treatment with the extract, but retention of a passive avoidance response was not significantly modified. These results suggest that some of the components of the hydroalcoholic extract of Salvia elegans have psychotropic properties, which deserve further investigation.
Asunto(s)
Ansiolíticos/farmacología , Antidepresivos/farmacología , Actividad Motora/efectos de los fármacos , Extractos Vegetales/uso terapéutico , Salvia/química , Animales , Ansiedad/psicología , Masculino , Aprendizaje por Laberinto/efectos de los fármacos , Fitoterapia , Ratas , Ratas Sprague-Dawley , Natación/psicologíaRESUMEN
An infusion prepared with aerial parts from Galphimia glauca has been widely used in Mexican traditional medicine as a remedy for nervous excitement. The sedative activity of a methanolic extract from this plant has been demonstrated by neuropharmacological tests. This effect was attributed to the nor-secotriterpene named galphimine B (GB). In the present work, the anxiolytic and antidepressant-like effects of G. glauca methanolic extract (standardized on GB content, 8.3mg/g) were assayed by using the elevated plus-maze, light-dark test and the forced swimming paradigm, on ICR albino mice. This extract, administered orally, three times (24, 18 and 1h before the test), and in different doses (125, 250, 500, 1,000 and 2,000 mg/kg) was able to increase significantly (p<0.05) the number of entries, as well as the time spent in the open arms of the elevated plus-maze, indicating an anxiolytic-like effect. A similar effect was observed in the light-dark paradigm test, the time spent in the light box was increased in treated mice. Nevertheless, this treatment was unable to change any parameter in the forced swimming test. Altogether, these results suggest an anxiolytic-like effect to the methanolic standardized extract of G. glauca on ICR inbred mice.
Asunto(s)
Ansiolíticos/farmacología , Antidepresivos/farmacología , Galphimia/química , Extractos Vegetales/farmacología , Animales , Ansiolíticos/química , Antidepresivos/química , Relación Dosis-Respuesta a Droga , Masculino , Medicina Tradicional , México , Ratones , Ratones Endogámicos ICR , Componentes Aéreos de las Plantas , Extractos Vegetales/químicaRESUMEN
In order to evaluate the effects produced by the hydroalcoholic extract of leaves from Casimiroa edulis on the central nervous system, different behavioral tests and animal models of depression and anxiety were performed. The extract was administered intraperitoneally in male and female rats and tested on spontaneous motor activity, locomotor activity, exploration of an elevated plus-maze (EPM) and in the forced swimming test (FST). In addition, the extract was administered orally in male and female mice and evaluated in the following tests: general observation, pentobarbital-induced hypnosis, EPM, rota-rod, hole-board, and marble-burying. The results revealed that, in rats, the extract caused considerable reduction of locomotor and exploratory activities and increased the exploration of the EPM open arms in a similar way that diazepam. In the FST, the extract was as effective as fluoxetine in inducing shortening of immobility, along with a significant increase on climbing duration. On the other hand, in mice, the extract prolonged pentobarbital-induced hypnosis, increased exploration of the EPM open arms and partially protected from the pentylenetetrazol-induced convulsions. No significant effect was evident on motor coordination, hole-board and marble-burying tests. These results suggest that the hydroalcoholic extract of Casimiroa edulis may contain sedative principles with potential anxiolytic and antidepressant properties, which need further investigation.
Asunto(s)
Ansiolíticos/farmacología , Conducta Animal/efectos de los fármacos , Casimiroa , Sistema Nervioso Central/efectos de los fármacos , Actividad Motora/efectos de los fármacos , Extractos Vegetales/farmacología , Administración Oral , Animales , Ansiolíticos/aislamiento & purificación , Etnofarmacología , Femenino , Locomoción/efectos de los fármacos , Masculino , Ratones , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta , Ratas , Ratas Sprague-Dawley , NataciónRESUMEN
Scorpions, especially in urban areas of tropical and subtropical regions, present a common risk of poisoning. In Mexico, scorpion envenomation is considered a public health problem. Despite the frequency of scorpion sting cases, there are to date no uniform criteria for their treatment. In Mexican traditional medicine, different plant species have been widely used as a remedy for treating scorpion poisoning. The aim of this work was to evaluate the effect of Bouvardia ternifolia, Aristolochia elegans and Vitex mollis extracts on Centruroides limpidus limpidus venom lethality in mice, and to determine their antagonist activity on guinea pig ileum. The hexane and methanol extract from B. ternifolia modified the LD50 of C. limpidus limpidus venom from 0.750 +/- 0.08 to 1.64 +/- 0.19 and 1.16 +/- 0.14 mg/kg, respectively. The extracts of A. elegans produced lower antitoxic activity, while extracts of V. mollis did not show any protection. On in vitro test, addition of B. ternifolia and A. elegans extracts strongly inhibited, in a concentration-dependent manner, the ileum contractions induced by venom. In general, the results demonstrated the effectiveness of these two plant species in modifying the lethality of C. limpidus limpidus venom in mice.
Asunto(s)
Antivenenos/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Plantas Medicinales , Picaduras de Escorpión/tratamiento farmacológico , Venenos de Escorpión/antagonistas & inhibidores , Escorpiones , Animales , Antivenenos/administración & dosificación , Antivenenos/uso terapéutico , Aristolochia , Relación Dosis-Respuesta a Droga , Femenino , Cobayas , Masculino , Medicina Tradicional , México , Ratones , Ratones Endogámicos BALB C , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Raíces de Plantas , Rubiaceae , Venenos de Escorpión/toxicidad , VitexRESUMEN
In order to compare the antihypertensive effectiveness and tolerability of a standardized extract from Hibiscus sabdariffa with captopril, a controlled and randomized clinical trial was done. Patients from 30 to 80 years old with diagnosed hypertension and without antihypertensive treatment for at least 1 month before were included. The experimental procedure consisted of the administration of an infusion prepared with 10 g of dry calyx from H. sabdariffa on 0.51 water (9.6 mg anthocyanins content), daily before breakfast, or captopril 25 mg twice a day, for 4 weeks. The outcome variables were tolerability, therapeutic effectiveness (diastolic reduction > or = 10 mm Hg) and, in the experimental group, urinary electrolytes modification. Ninety subjects were included, 15 withdrew from the study due to non-medical reasons; so, the analysis included 39 and 36 patients from the experimental and control group, respectively. The results showed that H. sabdariffa was able to decrease the systolic blood pressure (BP) from 139.05 to 123.73mm Hg (ANOVA p < 0.03) and the diastolic BP from 90.81 to 79.52mm Hg (ANOVA p < 0.06). At the end of the study, there were no significant differences between the BP detected in both treatment groups (ANOVA p > 0.25). The rates of therapeutic effectiveness were 0.7895 and 0.8438 with H. sabdariffa and captopril, respectively (chi2, p > 0.560), whilst the tolerability was 100% for both treatments. A natriuretic effect was observed with the experimental treatment. The obtained data confirm that the H. sabdariffa extract, standardized on 9.6mg of total anthocyanins, and captopril 50 mg/day, did not show significant differences relative to hypotensive effect, antihypertensive effectiveness, and tolerability.
Asunto(s)
Antihipertensivos/uso terapéutico , Hibiscus , Hipertensión/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/uso terapéutico , Adulto , Anciano , Anciano de 80 o más Años , Antihipertensivos/administración & dosificación , Presión Sanguínea/efectos de los fármacos , Captopril/administración & dosificación , Captopril/uso terapéutico , Esquema de Medicación , Femenino , Humanos , Hipertensión/patología , Masculino , Persona de Mediana Edad , Extractos Vegetales/administración & dosificación , Índice de Severidad de la Enfermedad , Resultado del TratamientoRESUMEN
Galphimia glauca is used for the treatment of asthma and allergies in Latin American traditional medicine. The ethylacetate fraction from its aerial parts was assayed for bronchoconstriction induced by antigen and several agonists in guinea pig tracheae. The organic fraction significantly inhibited the contractile response to ovalbumin in tracheae from sensitized guinea pigs, and significantly and selectively inhibited the bronchoconstriction induced by leukotriene D(4) (LTD(4)). The relative potency of the ethylacetate fraction of G. glauca to produce a concentration-dependent rightward shift of LTD(4) concentration-response curve was similar to that reported for SK&F 104353, a well-known competitive LTD(4)-antagonist.
Asunto(s)
Antiasmáticos/farmacología , Leucotrieno D4/antagonistas & inhibidores , Contracción Muscular/efectos de los fármacos , Extractos Vegetales/farmacología , Tráquea/efectos de los fármacos , Animales , Antiasmáticos/aislamiento & purificación , Broncoconstricción/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Cobayas , Leucotrieno D4/efectos adversos , Masculino , Ovalbúmina/antagonistas & inhibidores , Extractos Vegetales/aislamiento & purificaciónRESUMEN
Eighteen crude extracts, including six hexanic, six chloroformic and six methanolic from six different plant species used in Mexican traditional medicine for the treatment of respiratory infections, were evaluated for potential antimicrobial activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, and Candida albicans. The minimal inhibitory concentration was determined for each extract using a two-fold dilution assay. The results showed that 16 crude extracts (89%) exhibited antimicrobial activity against at least one of the microorganisms tested at concentrations of 5 mg/ml or below. The extracts from Gnaphalium oxyphyllum, Gnaphalium americanum, and Crescentia alata possessed strong antimicrobial activity against the pathogens tested.
Asunto(s)
Antibacterianos/uso terapéutico , Bacterias Grampositivas/efectos de los fármacos , Medicina Tradicional , Pruebas de Sensibilidad Microbiana/métodos , Extractos Vegetales/uso terapéutico , Antibacterianos/aislamiento & purificación , Etnofarmacología , México , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales , Enfermedades Respiratorias/tratamiento farmacológicoRESUMEN
Baccharis serraefolia is a widely used plant to treat diarrhoea in Mexican traditional medicine. Although the methanolic extract of this plant has shown an important dose-dependent spasmolytic activity, its underlying mechanism has not been studied. In the present work, the methanolic extract of B. serraefolia significantly delayed the onset of tonic seizures induced by strychnine and pentylenetetrazol; besides, it diminished the death rate and number of animals that exhibited convulsions. It produced potentiation of the hypnotic effect of pentobarbital. Oral administration produced an inhibition of gastrointestinal transit in mice as effective as that produced by loperamide. As to the effect on smooth muscles, the active extract produced an inhibition of contraction induced electrically, which could not be reversed by naloxone. The calcium concentration-contraction curve showed a rightward displacement when the extract was added to isolated guinea pig ileum depolarized with high K+ and cumulative concentrations of Ca2+. The results suggest that the methanolic extract does not interact with classical opiate receptors and its effects, at least that produced on smooth muscle, may be due to a probable interference with calcium influx and/or calcium release from an intra-cellular store.
Asunto(s)
Antidiarreicos/farmacología , Calcio/antagonistas & inhibidores , Músculo Liso/efectos de los fármacos , Extractos Vegetales/uso terapéutico , Convulsiones/prevención & control , Administración Oral , Análisis de Varianza , Animales , Convulsivantes/administración & dosificación , Convulsivantes/toxicidad , Relación Dosis-Respuesta a Droga , Sinergismo Farmacológico , Estimulación Eléctrica , Tránsito Gastrointestinal/efectos de los fármacos , Cobayas , Hipnóticos y Sedantes/administración & dosificación , Hipnóticos y Sedantes/farmacología , Íleon/efectos de los fármacos , Íleon/metabolismo , Loperamida/farmacología , Masculino , Medicina Tradicional , Metanol/química , México , Ratones , Ratones Endogámicos BALB C , Contracción Muscular/efectos de los fármacos , Relajación Muscular/efectos de los fármacos , Pentobarbital/administración & dosificación , Pentobarbital/farmacología , Pentilenotetrazol/administración & dosificación , Pentilenotetrazol/toxicidad , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacología , Plantas Medicinales , Convulsiones/tratamiento farmacológico , Convulsiones/mortalidad , Estricnina/administración & dosificación , Estricnina/toxicidadRESUMEN
The traditional herbal remedy from Psidium guajava leaves has been medically proposed in Mexico as effective treatment of acute diarrhea. A methanolic leaf extract was subjected to a bioassay-guided isolation of spasmolytic constituents. Six fractions were separated on a polyvinylpolypyrrolidine (PVPP) column using a water methanol-gradient. The fraction containing flavonols inhibited peristalsis of guinea pig ileum in vitro. A trace of quercetin aglycone together with five glycosides was isolated from this active fraction and identified as quercetin 3-O-alpha-L-arabinoside (guajavarin); quercetin 3-O-beta-D-glucoside (isoquercetin); quercetin 3-O-beta-D-galactoside (hyperin); quercetin 3-O-beta-L-rhamnoside (quercitrin) and quercetin 3-O-gentobioside. Biological activity of each pure compound was studied in the same bioassay. Obtained results suggest that the spasmolytic activity of the Psidium guajava leaf remedy is mainly due to the aglycone quercetin, present in the leaf and in the extract mainly in the form of five flavonols, and whose effect is produced when these products are hydrolyzed by gastrointestinal fluid.
Asunto(s)
Antidiarreicos , Glicósidos , Íleon/efectos de los fármacos , Parasimpatolíticos/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Quercetina/análogos & derivados , Quercetina/farmacología , Animales , Evaluación Preclínica de Medicamentos , Ácido Gástrico/metabolismo , Cobayas , Hidrólisis , Masculino , Metanol , México , Relajación Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Parasimpatolíticos/aislamiento & purificación , Parasimpatolíticos/metabolismo , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Quercetina/aislamiento & purificación , Quercetina/metabolismoRESUMEN
Galphimia glauca Cav. (Malpighiaceae) is used in Mexican traditional medicine as a sedative in the treatment of mental disorders. Sedative properties of a methanolic extract of the aerial parts of this plant have been established in animal trials and an active compound, named galphimine B, has already been isolated. This compound was submitted to neuropharmacological testing, where it was shown that galphimine B had no significant effect as an anticonvulsant, while it exhibited a strong depressant activity on the nervous system.
Asunto(s)
Anticonvulsivantes/farmacología , Hipnóticos y Sedantes/farmacología , Plantas Medicinales/química , Triterpenos/farmacología , Animales , Anticonvulsivantes/aislamiento & purificación , Femenino , Cobayas , Hipnóticos y Sedantes/aislamiento & purificación , Masculino , Ratones , Estructura Molecular , Triterpenos/aislamiento & purificaciónRESUMEN
An ethnobotanical study of plants used in Mexican traditional medicine was made. The source was the national inquiry done by the IMSS-COPLAMAR health program (1983-1985) in which the plants used to treat mental disorders were selected and analyzed, in order to select the most frequent botanical species used in traditional medicine as sedatives, anticonvulsants and hypnotics.