RESUMEN
Boerhaavia diffusa is an Ayurvedic remedy used traditionally for the treatment of a number of diseases, including those affecting the gastrointestinal tract. In the current investigation, a methanol extract obtained from roots of B. diffusa exhibited a significant spasmolytic activity in the guinea pig ileum, probably through a direct effect on the smooth muscle. A detailed phytochemical analysis of this methanol extract led to the isolation of one new (12) and six known (6-11) rotenoid derivatives. The structure of the new compound was determined through interpretation of its MS and NMR data. All the isolated rotenoids were evaluated for their effect on intestinal motility in vitro, and the results obtained showed unambiguously that they are active spasmolytic constituents. Preliminary structure-activity relationships for this class of compounds are suggested.
Asunto(s)
Medicina Ayurvédica , Nyctaginaceae/química , Parasimpatolíticos/aislamiento & purificación , Plantas Medicinales/química , Rotenona/análogos & derivados , Rotenona/aislamiento & purificación , Parasimpatolíticos/química , Parasimpatolíticos/farmacología , Raíces de Plantas/química , Rotenona/química , Rotenona/farmacología , Relación Estructura-ActividadRESUMEN
Clinical studies suggest that the Ayurvedic plant Boswellia serrata may be effective in reducing diarrhoea in patients with inflammatory bowel disease. In the present study, we evaluated the effect of a Boswellia serrata gum resin extract (BSE) on intestinal motility and diarrhoea in rodents. BSE depressed electrically-, acetylcholine-, and barium chloride-induced contractions in the isolated guinea-pig ileum, being more potent in inhibiting the contractions induced by acetylcholine and barium chloride. The inhibitory effect of BSE on acetylcholine-induced contractions was reduced by the L-type Ca(2+) channel blockers verapamil and nifedipine, but not by the sarcoplasmic reticulum Ca(2+)-ATPase inhibitor cyclopiazonic acid, by the phosphodiesterase type IV inhibitor rolipram or by the lipoxygenase inhibitor zileuton. 3-acetyl-11-keto-beta-boswellic acid, one of the main active ingredients of B. serrata, inhibited acetylcholine-induced contractions. BSE inhibited upper gastrointestinal transit in croton oil-treated mice as well as castor oil-induced diarrhoea. However, BSE did not affect intestinal motility in control mice, both in the small and in the large intestine. It is concluded that BSE directly inhibits intestinal motility with a mechanism involving L-type Ca(2+) channels. BSE prevents diarrhoea and normalizes intestinal motility in pathophysiological states without slowing the rate of transit in control animals. These results could explain, at least in part, the clinical efficacy of this Ayurvedic remedy in reducing diarrhoea in patients with inflammatory bowel disease.
Asunto(s)
Boswellia , Diarrea/prevención & control , Motilidad Gastrointestinal/efectos de los fármacos , Enfermedades Inflamatorias del Intestino/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/farmacología , 3',5'-AMP Cíclico Fosfodiesterasas/antagonistas & inhibidores , Animales , Calcio/metabolismo , Canales de Calcio Tipo L/fisiología , Fosfodiesterasas de Nucleótidos Cíclicos Tipo 4 , Relación Dosis-Respuesta a Droga , Estimulación Eléctrica , Tránsito Gastrointestinal/efectos de los fármacos , Cobayas , Masculino , Ratones , Ratones Endogámicos ICRRESUMEN
Flavonoids are a large heterogeneous group of benzo-gamma-pyrone derivatives, which are abundantly present in our diet. In this study we investigated the effect of ten flavonoids (quercetin, kaempferol, morin, galangin, rutin, apigenin, flavone, naringenin, hesperitin and silybin) on the contractile response elicited by electrical field stimulation in the rat isolated vas deferens. All flavonoids tested inhibited vas deferens contractions. The relative order of potency of the tested flavonoids was naringenin > hesperitin > morin > kaempferol > apigenin > silybin > flavone > rutin > quercetin > galangin. Analysis of the chemical structures showed that the saturation of C-2-C-3 double bond and the presence of hydroxyl groups on the flavonoidic scaffold play an important role in the activity of flavonoids.
Asunto(s)
Flavonoides/farmacología , Conducto Deferente/efectos de los fármacos , Animales , Estimulación Eléctrica , Flavonoides/química , Técnicas In Vitro , Masculino , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Músculo Liso/fisiología , Ratas , Ratas Wistar , Relación Estructura-Actividad , Conducto Deferente/fisiologíaRESUMEN
The paper describes the private book collection owned by Adalberto Pazzini and kept in the Library of the Sezione di Storia della Medicina. Gathered from the 1930s to the 1970s, the collection allows a reconstruction of the 'state of the art' of medical history in this period in Italy. Books were sent and dedicated to Pazzini by colleagues, mostly active in Italy and in the Spanish-speaking countries; many of them deal with the history of medicine, but some also with medicine itself.
Asunto(s)
Archivos , Historia de la Medicina , Libros/historia , Historiografía , Historia del Siglo XX , Italia , Ciudad de RomaRESUMEN
A bioassay-guided separation of a methanolic extract obtained from the roots of Boerhaavia diffusa L. (Nyctaginaceae) allowed us to isolate five compounds belonging to the class of rotenoids: the known boeravinone D ( 1), boeravinone E ( 2), compound 5 and two novel compounds that we have named boeravinone G ( 3) and boeravinone H ( 4). The structures of the new molecules have been determined on the basis of their HR-EI-MS, (1)H- and (13)C-NMR and 2D-NMR (HMQC, HMBC) data. All the isolated rotenoids have been evaluated for their effect on intestinal motility in vitro. Three of them (boeravinone G, boeravinone E and compound 5) exhibited spasmolytic activity. Preliminary structure-activity relationships have been established highlighting the effect of substitutions on rings B and D.
Asunto(s)
Motilidad Gastrointestinal/efectos de los fármacos , Nyctaginaceae , Parasimpatolíticos/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Animales , Relación Dosis-Respuesta a Droga , Cobayas , Masculino , Parasimpatolíticos/administración & dosificación , Parasimpatolíticos/uso terapéutico , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , Raíces de PlantasRESUMEN
Caffeic acid phenethyl ester (CAPE), one of the major components of propolis (honeybee resin), has demonstrated a wide spectrum of activities including suppression of eicosanoids by inhibition of cyclooxygenase-1 and cyclooxygenase-2 enzyme activities. The aim of this study was to investigate the effect of CAPE on basal and secretagogues-stimulated gastric acid secretion in vitro. In the isolated, lumen-perfused, stomach preparation of mouse, CAPE (10-100 microM) did not affect the basal gastric acid secretion nor the secretion stimulated by histamine, pentagastrin, isobutyl methylxanthine and high levels of K+. By contrast, CAPE increased the gastric acid secretion induced by the muscarinic receptor agonist, 5-methylfurmethide (5-MEF). CAPE also inhibited the acetylcholinesterase activity in an in vitro colorimetric assay. Eserine (10 microM), a well known acetylcholinesterase inhibitor, also increased 5-MEF-stimulated acid secretion. Our results show that CAPE increases gastric acid secretion stimulated by an acetylcholine agonist receptor likely through inhibition of acetylcholinesterase activity.