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1.
Carbohydr Polym ; 254: 117415, 2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33357899

RESUMEN

Grapefruit peel nanofibrillated cellulose (GNFC) was used as fat substitute in ice cream. GNFC was characterized by TEM, SEM, and XRD. The effects of GNFC on textural profiles, rheological properties, melting resistance, sensory properties, microstructure, and gross energy (GE) of ice cream were investigated. The results showed that GNFC was short rod-shaped crystal. Ice cream added with GNFC exhibited elastic-dominated behavior and better textural properties. The sensory evaluation score reached the highest level with desirable three-dimensional network structure at 0.4 % GNFC addition. GE of ice cream significantly decreased with reducing fat with maximal reduction rate of 17.90 %. Furthermore, the results of in vitro simulated digestion showed that GNFC addition and fat reduction significantly inhibited fat digestibility of ice cream due to coalescence of fat droplets on GNFC. This study provides new sustainable perspectives for the application of GNFC prepared from agricultural waste as fat substitute in food products.


Asunto(s)
Celulosa/química , Citrus paradisi/química , Sustitutos de Grasa/química , Helados , Nanofibras/química , Nanopartículas/química , Extractos Vegetales/química , Celulosa/farmacología , Óxidos N-Cíclicos/química , Digestión/efectos de los fármacos , Elasticidad , Sustitutos de Grasa/farmacología , Ácidos Grasos no Esterificados/química , Manipulación de Alimentos/métodos , Congelación , Jugo Gástrico/química , Jugo Gástrico/efectos de los fármacos , Concentración de Iones de Hidrógeno , Leucina/química , Extractos Vegetales/farmacología , Reología/métodos , Gusto
2.
Molecules ; 25(23)2020 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-33260419

RESUMEN

Inulae Flos, the flower of Inula britannica L., is used as a dietary supplement, beverage, and medicine in East Asia. In this study, we evaluated the gastroprotective effects of Inulae Flos extract (IFE) against gastric mucosal lesions induced by hydrochloric acid (HCl)/ethanol in rats and explored its potential mechanisms by measuring antioxidant enzyme activity, mucus secretion, and prostaglandin E2 (PGE2) levels. Pretreatment with IFE at doses of 100 and 300 mg/kg significantly inhibited gastric lesions in HCl/ethanol-treated rats. IFE increased the activities of superoxide dismutase and catalase and the levels of glutathione and PGE2 in gastric tissues. The administration of IFE also significantly increased the gastric wall mucus contents in HCl/ethanol-induced gastric lesions. These findings suggest that IFE has gastroprotective effects against HCl/ethanol-induced gastric lesions and exerts these effects through increased antioxidant levels and gastric mucus secretion. Inulae Flos may be a promising agent for the prevention and treatment of gastritis and gastric ulcers.


Asunto(s)
Flores/química , Inula/química , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Úlcera Gástrica/tratamiento farmacológico , Animales , Antioxidantes/metabolismo , Catalasa/metabolismo , Dinoprostona/metabolismo , Modelos Animales de Enfermedad , Etanol/toxicidad , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/patología , Glutatión Peroxidasa/metabolismo , Ácido Clorhídrico/toxicidad , Masculino , Malondialdehído/metabolismo , Moco/metabolismo , Extractos Vegetales/administración & dosificación , Sustancias Protectoras/administración & dosificación , Ratas Sprague-Dawley , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/patología , Superóxido Dismutasa/metabolismo
3.
J Ethnopharmacol ; 257: 112825, 2020 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-32320728

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Semen Arecae (SA) is one of the most commonly used Traditional Chinese Medicine. Charred Semen Arecae (CSA) is the processed product of SA. Alkaloids are considered as pharmacological mechanisms of SA and CSA on gastrointestinal motility. Recent studies have shown alkaloids decreased quickly after procession. However, the promoting on gastrointestinal motility were not decreased. Is gastrointestinal motility related to alkaloids of CSA? This study explored the effects of SA, CSA, Semen Arecae-Removal (SA-R), and Charred Semen Arecae-Removal (CSA-R) on gastrointestinal motility, Gastric Inhibitory Polypeptide (GIP), Glucagon Like Peptide-1 (GLP-1), gastric juice and bile in rats. MATERIAL AND METHODS: Rats were randomly divided into six groups, including the Control group, SA group, CSA group, SA-R group, CSA-R group, and Positive drug group (Mosapride). Alkaloids of samples were knocked out by using the "target constituent removal" strategy. Gastric residue and intestinal propulsion rate were evaluated in rats. Serum levels of GIP and GLP-1 were measured by Enzyme-Linked Immunosorbent Assay (ELISA). Gastric juice and bile were examined, respectively. RESULTS: CSA-R and SA-R have been investigated by the Preparative Thin-layer Chromatography (PTLC) method. Intestinal propulsion and gastric residue assessments confirmed the effectiveness of CSA and CSA-R. CSA-R was higher than SA-R in the GLP-1, pepsin activity, the secretion of bile, Bilirubin (BIL), and Cholesterol (CHO). The statistical comparison demonstrated that there is no difference between the CSA group and CSA-R group. CONCLUSIONS: After processing, the promoting gastrointestinal motility might be not related to alkaloids. Maillard reaction could be produced to promote the secretion of GLP-1, bile, and CHO for gastrointestinal motility. Our findings provide a pharmacological reference for the clinical application of SA and CSA in the treatment of digestive diseases.


Asunto(s)
Alcaloides/farmacología , Areca , Medicamentos Herbarios Chinos/farmacología , Motilidad Gastrointestinal/efectos de los fármacos , Animales , Bilis/efectos de los fármacos , Polipéptido Inhibidor Gástrico/análisis , Polipéptido Inhibidor Gástrico/sangre , Polipéptido Inhibidor Gástrico/metabolismo , Jugo Gástrico/efectos de los fármacos , Péptido 1 Similar al Glucagón/sangre , Péptido 1 Similar al Glucagón/metabolismo , Ratas , Ratas Sprague-Dawley
4.
Int J Biol Macromol ; 123: 300-307, 2019 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-30445072

RESUMEN

Gel microparticles were prepared from pectins of campion (SVCgel) and duckweed (LMCgel) callus cultures, as well as from commercial apple pectin (APgel) by emulsion dehydration techniques with successive ionotropic gelation. The morphology and swelling behavior of the microparticles were determined after successive incubation in simulated gastric (SGF), intestinal (SIF), and colonic (SCF) fluids. Both SVCgel and LMCgel microparticles were found to swell in SGF and SIF gradually, and at oral administration decreased food intake by laboratory mice during the first 5 h of free-feeding. The SVCgel microparticles demonstrated the higher stability in SCF within 24 h than LMCgel ones. Only the SVCgel microparticles were shown to decrease food intake by 24% during the 21 h of free-feeding and decreased body weight of mice by 4% during 24 h after oral administration. The APgel microparticles lost their shape in SIF, then fully disintegrated after 0.5 h of incubation in SCF, and failed to affect food intake or mice body weight. The data obtained indicated that sustainability and swelling of the gel microparticles from the SVC pectin in the colonic fluid may provide the stronger satiating effect compared to that of the LMCgel microparticles.


Asunto(s)
Líquidos Corporales/efectos de los fármacos , Callo Óseo/química , Ingestión de Alimentos/efectos de los fármacos , Pectinas/administración & dosificación , Administración Oral , Animales , Colon/efectos de los fármacos , Portadores de Fármacos , Edema/tratamiento farmacológico , Emulsiones/administración & dosificación , Emulsiones/química , Jugo Gástrico/efectos de los fármacos , Humanos , Intestinos/efectos de los fármacos , Malus/química , Ratones , Tamaño de la Partícula , Pectinas/química , Células Vegetales/química
5.
J Nat Med ; 73(2): 339-352, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30523551

RESUMEN

The aim of this study was to elucidate the gastroprotective activity and possible mechanism of involvement of araloside A (ARA) against ethanol- and aspirin-induced gastric ulcer in mice. The experimental mice were randomly divided into control, model, omeprazole (20 mg/kg, orally) and ARA (10, 20 and 40 mg/kg, orally). Gastric ulcer in mice was induced by intragastric administration of 80% ethanol (10 mL/kg) containing 15 mg/mL aspirin 4 h after drug administration on day 7. The results indicated that ARA could significantly raise gastric juice volume and acidity; ameliorate gastric mucosal blood flow, gastric binding mucus volume, ulcer index and ulcer inhibition rate; suppress H+/K+-ATPase activity, which was confirmed by computer-aided docking simulations; inhibit the release of mitochondrial cytochrome c into the cytoplasm; inhibit caspase-9 and caspase-3 activities and down-regulate mRNA expression levels; down-regulate the mRNA and protein expressions of apoptosis protease-activating factor-1 and protein expression of cleaved poly(ADP ribose) polymerase-1; and up-regulate Bcl-2 mRNA and protein expressions and down-regulate Bax mRNA and protein expressions, thus elevating the Bcl-2/Bax ratio in a dose-dependent manner. Histopathological observations further provided supportive evidence for the aforementioned results. The results demonstrated that ARA exerted beneficial gastroprotective effects on alcohol- and aspirin-induced gastric ulcer in mice, which was related to suppressing H+/K+-ATPase activity as well as pro-apoptotic protein expression, and promoting anti-apoptotic protein expression, thus alleviating gastric mucosal injury and cell death.


Asunto(s)
Antiulcerosos/uso terapéutico , Mucosa Gástrica/efectos de los fármacos , ATPasa Intercambiadora de Hidrógeno-Potásio/efectos de los fármacos , Ácido Oleanólico/análogos & derivados , Saponinas/uso terapéutico , Úlcera Gástrica/prevención & control , Animales , Antiulcerosos/aislamiento & purificación , Antiulcerosos/farmacología , Factor Apoptótico 1 Activador de Proteasas/metabolismo , Aralia/química , Aspirina/efectos adversos , Caspasa 3/metabolismo , Caspasa 9/metabolismo , Citocromos c/metabolismo , Evaluación Preclínica de Medicamentos , Etanol/efectos adversos , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/irrigación sanguínea , Mucosa Gástrica/metabolismo , ATPasa Intercambiadora de Hidrógeno-Potásio/metabolismo , Masculino , Ratones , Mitocondrias/metabolismo , Simulación del Acoplamiento Molecular , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Ácido Oleanólico/uso terapéutico , Fitoterapia , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Poli(ADP-Ribosa) Polimerasa-1/metabolismo , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Distribución Aleatoria , Flujo Sanguíneo Regional/efectos de los fármacos , Saponinas/aislamiento & purificación , Saponinas/farmacología , Úlcera Gástrica/inducido químicamente
6.
Drug Des Devel Ther ; 10: 1973-86, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27366052

RESUMEN

Clausena excavata is a natural herb with both antioxidant and anti-inflammatory properties. It has been used for decades in folkloric practice for the amelioration of various ailments. In this study, the gastroprotective activity of methanolic extract of C. excavata leaves (MECE) was determined in the Sprague Dawley rat ethanol-induced gastric ulcer model. Rats were pretreated with a single dose of vehicle (5% Tween 20), 20 mg/mL omeprazole, 400 and 200 mg/mL of MECE dissolved in 5% Tween 20. Ulcer was induced with 5 mL/kg of ethanol and stomach tissue was obtained after 1 hour. Histological examination was done on hematoxylin and eosin, periodic acid-Schiff, and immunochemically stained gastric mucosal tissues. Prostaglandin E2, superoxide dismutase, catalase, glutathione peroxidase, and lipid peroxidation levels of the gastric tissue homogenates were also determined. Significantly (P<0.05) smaller ulcer areas, less intense edema, and fewer leukocytes' infiltration were observed in MECE- and omeprazole-treated than in untreated gastric mucosa with ulcer. The gastric pH, mucus production, superoxide dismutase, catalase, and glutathione peroxidase contents increased, while the lipid peroxidation content decreased as a result of MECE treatment. Bcl-2-associated X protein was underexpressed, while heat shock protein 70 and transforming growth factor-beta protein were overexpressed in the ulcerated gastric mucosa tissues treated with omeprazole and MECE. Similarly, there was a reduction in the levels of tumor necrotic factor-alpha and interleukin-6, while the level of interleukin-10 was increased. This study showed that the gastroprotective effect of MECE is achieved through inhibition of gastric juice secretion and ulcer lesion development, stimulation of mucus secretion, elevation of gastric pH, reduction of reactive oxygen species production, inhibition of apoptosis in the gastric mucosa, and modulation of inflammatory cytokines.


Asunto(s)
Antiulcerosos/farmacología , Clausena/química , Etanol , Extractos Vegetales/farmacología , Hojas de la Planta/química , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/prevención & control , Animales , Antiulcerosos/química , Antiulcerosos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Citocinas/metabolismo , Modelos Animales de Enfermedad , Jugo Gástrico/efectos de los fármacos , Jugo Gástrico/metabolismo , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patología , Masculino , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Ratas , Ratas Sprague-Dawley , Úlcera Gástrica/patología
7.
Bull Exp Biol Med ; 159(5): 638-41, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26468023

RESUMEN

Gastroprotective effect of Cichorium intybus L. root extract is demonstrated on H. Shay's model of experimental ulcer in rats. The effect is attributed to the antisecretory activity of the plant and stimulation of defense barrier function of the gastric mucosa. The regulatory effect of the phytocomplex on seasonal characteristics of the gastric secretory and defense functions in dogs with Basov's fistula is detected.


Asunto(s)
Antiulcerosos/farmacología , Cichorium intybus/química , Mucosa Gástrica/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Úlcera Gástrica/tratamiento farmacológico , Animales , Antiulcerosos/aislamiento & purificación , Carbacol/farmacología , Perros , Famotidina/farmacología , Femenino , Fístula Gástrica , Jugo Gástrico/química , Jugo Gástrico/efectos de los fármacos , Jugo Gástrico/metabolismo , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patología , Masculino , Extractos Vegetales/aislamiento & purificación , Raíces de Plantas/química , Ratas , Ratas Sprague-Dawley , Estaciones del Año , Estómago/efectos de los fármacos , Estómago/patología , Úlcera Gástrica/patología
8.
J Ethnopharmacol ; 166: 176-84, 2015 May 26.
Artículo en Inglés | MEDLINE | ID: mdl-25792014

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Helicteres sacarolha A. St.- Hil. et al. popularly known in Brazil as 'semente-de-macaco', is widely employed in the popular medicine in many of parts of Brazil in the alleviation of symptoms of ailments such as peptic ulcer and inflammation. Up to the present, there is no study addressing the gastroprotective activity of the hydroethanolic extract of H. sacarolha and its possible mechanism of actions. MATERIALS AND METHODS: The hydroethanolic (70%) extract of H. sacarolha (HEHs) was obtained by maceration. The gastroprotective activity was assessed using gastric ulcer models induced by acidified ethanol, piroxicam, and water restraint stress in mice and rats at doses of 20, 50 and 250mg/kg p.o. Mechanistic studies involved the antisecretory assay evaluated with pylorus ligation in rats and pre-treatments with appropriate antagonists/inhibitors such as yohimbine, glibenclamide, indomethacin and l-NAME, effect on catalase and myeloperoxidase activities and gastric mucus determination using acidified ethanol- induced ulcer in mice. RESULTS: HEHs at all doses tested demonstrated potent gastroprotective activities in the acute ulcer models. The gastroprotective activity of HEHs was attenuated by pre-treatments with yohimbine, glibenclamide, indomethacin and l-NAME. HEHs effectively reduced basal gastric juice production without any effect on the free and total acidity. The gastroprotective action of HEHs involved increasing the antioxidant enzyme catalase and mucus secretion and inhibition of neutrophyl infiltration as reflected by the reduction in the myeloperoxidase activity. CONCLUSION: The results of this study gave a scientific support for the popular use of the leaves of H. sacarolha in the treatment of gastric ulcers and that it has a multi-targeted action.


Asunto(s)
Antiulcerosos/química , Antiulcerosos/farmacología , Malvaceae/química , Extractos Vegetales/farmacología , Úlcera Gástrica/tratamiento farmacológico , Animales , Antioxidantes/farmacología , Catalasa/metabolismo , Etanol/química , Jugo Gástrico/efectos de los fármacos , Jugo Gástrico/metabolismo , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Gliburida/farmacología , Indometacina/farmacología , Ratones , NG-Nitroarginina Metil Éster/farmacología , Fitoterapia/métodos , Extractos Vegetales/química , Hojas de la Planta/química , Ratas , Ratas Wistar , Úlcera Gástrica/metabolismo , Yohimbina/farmacología
9.
PLoS One ; 10(3): e0121060, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25798602

RESUMEN

BACKGROUND: Zingiber zerumbet Smith is a perennial herb, broadly distributed in many tropical areas. In Malaysia, it's locally known among the Malay people as "lempoyang" and its rhizomes, particularly, is widely used in traditional medicine for the treatment of peptic ulcer disease beyond other gastric disorders. AIM OF THE STUDY: The aim of the current study is to evaluate the gastroprotective effect of zerumbone, the main bioactive compound of Zingiber zerumbet rhizome, against ethanol-induced gastric ulcer model in rats. MATERIALS AND METHODS: Rats were pre-treated with zerumbone and subsequently exposed to acute gastric ulcer induced by absolute ethanol administration. Following treatment, gastric juice acidity, ulcer index, mucus content, histological analysis (HE and PAS), immunohistochemical localization for HSP-70, prostaglandin E2 synthesis (PGE2), non-protein sulfhydryl gastric content (NP-SH), reduced glutathione level (GSH), and malondialdehyde level (MDA) were evaluated in ethanol-induced ulcer in vivo. Ferric reducing antioxidant power assay (FRAP) and anti-H. pylori activity were investigated in vitro. RESULTS: The results showed that the intragastric administration of zerumbone protected the gastric mucosa from the aggressive effect of ethanol-induced gastric ulcer, coincided with reduced submucosal edema and leukocyte infiltration. This observed gastroprotective effect of zerumbone was accompanied with a significant (p <0.05) effect of the compound to restore the lowered NP-SH and GSH levels, and to reduce the elevated MDA level into the gastric homogenate. Moreover, the compound induced HSP-70 up-regulation into the gastric tissue. Furthermore, zerumbone significantly (p <0.05) enhanced mucus production, showed intense PAS stain and maintained PG content near to the normal level. The compound exhibited antisecretory activity and an interesting minimum inhibitory concentration (MIC) against H. pylori strain. CONCLUSION: The results of the present study revealed that zerumbone promotes ulcer protection, which might be attributed to the maintenance of mucus integrity, antioxidant activity, and HSP-70 induction. Zerumbone also exhibited antibacterial action against H. pylori.


Asunto(s)
Antioxidantes/administración & dosificación , Helicobacter pylori/efectos de los fármacos , Sesquiterpenos/administración & dosificación , Úlcera Gástrica/prevención & control , Zingiberaceae/química , Animales , Antibacterianos/administración & dosificación , Antibacterianos/farmacología , Antioxidantes/farmacología , Etanol , Jugo Gástrico/efectos de los fármacos , Glutatión/metabolismo , Masculino , Malondialdehído/metabolismo , Extractos Vegetales/química , Extractos Vegetales/farmacología , Ratas , Sesquiterpenos/farmacología , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo
10.
J Coll Physicians Surg Pak ; 24(1): 39-42, 2014 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-24411541

RESUMEN

OBJECTIVE: To determine the efficacy of extract of Ammi visnaga on volume and acidity of stimulated gastric secretion in rabbits and also its safety on liver and kidney function. STUDY DESIGN: Quasi experimental study. PLACE AND DURATION OF STUDY: Pharmacology Department, Saidu Medical College, Swat, in the years 2008-9. METHODOLOGY: Thirty rabbits weighing 1 - 1.5 kg were divided into groups A, B and C each having 10 animals. After fasting for 48 hours, pylorus of animals of group A and B was ligated. Group A was administered Carbachol and group B was given extracts of Ammi visnaga followed by Carbachol after 15 minutes intraperitoneally. After 4 hours, stomach contents were measured for volume and then centrifuged and estimated for acidity. The extract was also administered to group C animals for 45 days to observe its effects on liver and kidney function. RESULTS: In group B, reduction in volume, free and total acidity of gastric juice was highly significant when the mean values were compared with group A. In group C, mean values of liver and kidney function test compared with pre-treated values, were found statistically non-significant. CONCLUSION: Ammi visnaga extract can be used effectively and safely in the treatment of hyper acidity conditions and peptic ulcer after evaluation of its effects in human being.


Asunto(s)
Ammi , Ácido Gástrico/metabolismo , Jugo Gástrico/efectos de los fármacos , Jugo Gástrico/metabolismo , Extractos Vegetales/farmacología , Animales , Bloqueadores de los Canales de Calcio/farmacología , Bloqueadores de los Canales de Calcio/uso terapéutico , Carbacol/farmacología , Agonistas Colinérgicos/farmacología , Ayuno , Pruebas de Función Renal , Pruebas de Función Hepática , Modelos Animales , Úlcera Péptica/tratamiento farmacológico , Úlcera Péptica/prevención & control , Conejos
11.
Rev. peru. med. exp. salud publica ; 30(4): 608-615, oct.-dic. 2013. tab
Artículo en Español | LILACS, LIPECS | ID: lil-698120

RESUMEN

Objetivos. Determinar el efecto gastroprotector y antisecretor del extracto etanólico de las hojas de matico (Piper aduncum) en modelos animales. Materiales y métodos. Para la evaluación del efecto gastroprotector se utilizó 220 ratones de la cepa Balb C57, los cuales fueron aleatorizados en 22 grupos de diez animales, a los cuales se les indujo la formación de úlceras gástricas con indometacina, la gastroprotección se determinó a través de tres aspectos: inflamación, número de bandas hemorrágicas y número de úlceras. Para evaluar el efecto antisecretor se utilizó 64 ratas albinas machos Holtzman, los cuales fueron aleatorizados en ocho grupos de ocho animales, un control y siete grupos de tratamiento con un nivel de dosis de los extractos y dos niveles de dosis en los fitofármacos; la antisecreción se realizó con el ensayo de ligazón pilórica. Resultados. Para la gastroprotección, los extractos de diclorometano, cloroformo, hexano y metanol, lograron una disminución de la inflamación de más del 66% (p<0,05); el extracto etanólico presenta una actividad de 100% para disminuir el número de bandas hemorrágicas (p<0,05); el extracto clorofórmico presenta una actividad antiulcerosa de 75% (p<0,05). Respecto a la antisecreción, el fitofármaco en cápsulas conteniendo el extracto etanólico logró un 72% de reducción del volumen de la secreción gástrica (p<0,01) y un incremento del pH en 104,3% (p<0,01). Conclusiones. En condiciones experimentales los extractos etanólico, sus fracciones y su fitofármaco son gastroprotectores en ratones y antisecretores en ratas.


Objectives. To determine the gastroprotective and antisecretory effect of ethanol extract from matico leaves (Piper aduncum) in animal models. Materials and methods. To evaluate the gastroprotective effect, 220 mice of the Balb C57 strain were used. They were randomized in 22 groups of ten animals each, in which the formation of gastric ulcers was induced with indomethacin. Gastroprotection was determined by evaluating three aspects: inflammation, number of hemorrhagic shocks and number of ulcers. To evaluate the antisecretory effect, 64 white male Holtzman rats were used, which were randomized in eight groups of eight animals, one control and seven groups of treatment with one extract dose level and two phytochemical dose levels. Antisecretion was obtained through the pylorus ligation. Results. Regarding gastroprotection, dichloromethane, chloroform, hexane and methanol extracts decreased inflammation to over 66% (p<0,05). The ethanolic extract shows 100% activity in reducing the number of hemorrhagic bands (p<0,05). The chloroform extract shows antiulcer activity at 75% (p<0,05). In terms of antisecretion, the phytochemical in capsules containing the ethanolic extract achieved 72% reduction of the gastric secretion volume (p<0,01) and 104,3% (p<0,01) PH increase. Conclusions. In experimental conditions, ethanolic extracts, their fractions and phytochemicals have a gastroprotective effect in mice and antisecretory effect in rats.


Asunto(s)
Animales , Ratones , Ratas , Jugo Gástrico/efectos de los fármacos , Jugo Gástrico , Fitoterapia , Piper , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Gastropatías/prevención & control , Etanol , Ratones Endogámicos BALB C
12.
Biol Pharm Bull ; 36(10): 1535-9, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-24088252

RESUMEN

In this study, we evaluated the gastric protective activities of mokdanpi in vitro. Further, we used experimental ulcer models to identify the active ingredients of mokdanpi. As a preliminary evaluation of mokdanpi ethanolic extract and its ingredients, we assessed its radical scavenging activities. In addition, its antimicrobial activity against Helicobacter pylori (H. pylori) was investigated. The antiulcerogenic activity of the active ingredients was evaluated in pylorus-ligated rats, an HCl/ethanol-induced and an absolute ethanol-induced ulcer model. We confirmed the scavenging effect of the ethanolic extract of mokdanpi and its ingredients against 2,2-diphenyl-1-picrylhydrazyl, nitric oxide and superoxide radicals, and we demonstrated that mokdanpi could inhibit the colonization of H. pylori. In an HCl-ethanol-induced ulcer model, gallic acid and catechin (100 mg/kg) inhibited 40.6% and 41.7% of gastric lesions, respectively. Catechin (100 mg/kg) significantly reduced (p<0.05) the gastric secretion induced by pylorus ligature in rats in comparison to the control group. Gallic acid (100 mg/kg) significantly increased (p<0.05) the mucus contents in an ethanol-induced ulcer model. The antioxidant ingredients (catechin and gallic acid) present in mokdanpi play a major role in antiulcerogenic activity, and demonstrate novel activity against H. pylori.


Asunto(s)
Antiinfecciosos/uso terapéutico , Antiulcerosos/uso terapéutico , Antioxidantes/uso terapéutico , Helicobacter pylori/efectos de los fármacos , Paeonia/química , Fitoterapia , Úlcera Gástrica/tratamiento farmacológico , Animales , Antiinfecciosos/farmacología , Antiulcerosos/farmacología , Antioxidantes/farmacología , Compuestos de Bifenilo/metabolismo , Catequina/farmacología , Catequina/uso terapéutico , Etanol , Ácido Gálico/farmacología , Ácido Gálico/uso terapéutico , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/microbiología , Helicobacter pylori/crecimiento & desarrollo , Ligadura , Moco/metabolismo , Óxido Nítrico/metabolismo , Picratos/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Raíces de Plantas , Ratas , Ratas Sprague-Dawley , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología , Superóxidos/metabolismo
13.
Eur J Pharm Biopharm ; 84(3): 633-41, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-23434923

RESUMEN

Human biorelevant media have been shown to be a useful tool in pharmaceutical development and to provide input for in silico prediction of pharmacokinetic profiles after oral dosing. Dogs, in particular Beagles, are often used as animal models for preclinical studies. Key differences in the composition of human and canine gastric and intestinal fluids are described in the literature and underscore the need to develop a discrete set of biorelevant media, adapted to the conditions of the proximal canine gastrointestinal (GI) tract, to improve forecast and interpretation of preclinical results using in vitro dissolution studies. Canine biorelevant media can also be used in the development of oral dosage forms for companion animals, which is a rapidly growing market. The compositions of Fasted State Simulated Gastric Fluid canine (FaSSGFc) and Fasted State Simulated Intestinal Fluid canine (FaSSIFc) are adapted to the physiological composition of the corresponding gastrointestinal fluids in terms of pH, buffer capacity, osmolality, surface tension, as well as the bile salt, phospholipid, and free fatty acid content (in terms of concentration and reported subtypes). It was demonstrated that canine Fasted State Simulated Intestinal Fluid (FaSSIFc) is superior in predicting the solubility of model compounds in Canine Intestinal Fluid (CIF) compared to the human biorelevant media (FaSSIF and FaSSIF-V2). Two different versions of FaSSGFc, composed at pH 1.5 and pH 6.5, offer the possibility to design in vitro studies which correspond to the in vivo study design, depending on whether pentagastrin is used to decrease the gastric pH in the dogs or not. Canine biorelevant media can therefore be recommended to achieve more accurate forecasting and interpretation of pharmacokinetic studies of oral drug products in dogs.


Asunto(s)
Ayuno , Tracto Gastrointestinal/efectos de los fármacos , Administración Oral , Animales , Tampones (Química) , Calibración , Cromatografía Líquida de Alta Presión , Perros , Evaluación Preclínica de Medicamentos , Interacciones Alimento-Droga , Jugo Gástrico/efectos de los fármacos , Contenido Digestivo/química , Humanos , Concentración de Iones de Hidrógeno , Absorción Intestinal/fisiología , Concentración Osmolar , Fosfolípidos/química , Solubilidad , Tensión Superficial
14.
Rev Peru Med Exp Salud Publica ; 30(4): 608-15, 2013.
Artículo en Español | MEDLINE | ID: mdl-24448937

RESUMEN

OBJECTIVES: To determine the gastroprotective and antisecretory effect of ethanol extract from matico leaves (Piper aduncum) in animal models. MATERIALS AND METHODS: To evaluate the gastroprotective effect, 220 mice of the Balb C57 strain were used. They were randomized in 22 groups of ten animals each, in which the formation of gastric ulcers was induced with indomethacin. Gastroprotection was determined by evaluating three aspects: inflammation, number of hemorrhagic shocks and number of ulcers. To evaluate the antisecretory effect, 64 white male Holtzman rats were used, which were randomized in eight groups of eight animals, one control and seven groups of treatment with one extract dose level and two phytochemical dose levels. Antisecretion was obtained through the pylorus ligation. RESULTS: Regarding gastroprotection, dichloromethane, chloroform, hexane and methanol extracts decreased inflammation to over 66% (p<0,05). The ethanolic extract shows 100% activity in reducing the number of hemorrhagic bands (p<0,05). The chloroform extract shows antiulcer activity at 75% (p<0,05). In terms of antisecretion, the phytochemical in capsules containing the ethanolic extract achieved 72% reduction of the gastric secretion volume (p<0,01) and 104,3% (p<0,01) PH increase. CONCLUSIONS: In experimental conditions, ethanolic extracts, their fractions and phytochemicals have a gastroprotective effect in mice and antisecretory effect in rats.


Asunto(s)
Jugo Gástrico/efectos de los fármacos , Jugo Gástrico/metabolismo , Fitoterapia , Piper , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Gastropatías/prevención & control , Animales , Etanol , Ratones , Ratones Endogámicos BALB C , Ratas
15.
Zhong Yao Cai ; 35(7): 1123-5, 2012 Jul.
Artículo en Chino | MEDLINE | ID: mdl-23252281

RESUMEN

OBJECTIVE: To investigate the therapeutical effect of Canghuopingwei Granules on chronic gastritis in rats. METHODS: Rat models of chronic gastritis and bile reflux gastritis were used. After rat models were established, the rats were divided into 6 groups and were treated with different drugs. The tissue samples were obtained after one week. The volume of gastric juice, acidity of gastric juice and pepsase activity were determined, and changes of the gastric mucosa were studied by microscopy. RESULTS: The acidity of gastric juice was reversed with Canghuopingwei granules treatment. Gastric pathologic examination suggested that Canghuopingwei granules could markedly attenuate the pathological changes of gastric mucosa in rats. CONCLUSION: Canghuopingwei granules has remarkably therapeutical effect on chronic gastritis and bile reflux gastritis in rats.


Asunto(s)
Reflujo Biliar/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Gastritis/tratamiento farmacológico , Fitoterapia , Administración Oral , Animales , Atractylodes/química , Reflujo Biliar/patología , Enfermedad Crónica , Modelos Animales de Enfermedad , Combinación de Medicamentos , Medicamentos Herbarios Chinos/farmacología , Femenino , Ácido Gástrico/metabolismo , Determinación de la Acidez Gástrica , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/patología , Gastritis/patología , Concentración de Iones de Hidrógeno , Masculino , Plantas Medicinales/química , Ratas
16.
BMC Complement Altern Med ; 12: 168, 2012 Oct 02.
Artículo en Inglés | MEDLINE | ID: mdl-23031805

RESUMEN

BACKGROUND: The leaves and root of Flabellaria paniculata (Malpighiaceae) are frequently used in the treatment of wounds and ulcers in Nigerian folk medicine. The purpose of this study was to compare the effect of ethanolic extracts from the leaves (FPL) and root (FPR) of F. paniculata on gastric ulcers in rats. METHODS: The effect of FPL and FPR (100, 200 and 400 mg/kg) was evaluated in ethanol and indomethacin gastric ulcer models. Control groups for FPL and FPR were orally treated with 3% Tween 20 and distilled water respectively. FPL was further investigated in pylorus ligation model. Misoprostol and cimetidine were used as reference. RESULTS: FPL significantly (P < 0.05) reduced gastric lesions by 82.22% and 67.32% in ethanol and indomethacin induced ulcer models at 100 mg/kg respectively while FPR (100, 200 and 400 mg/kg) did not exert significant effect in the two models. In pylorus ligation model, FPL exerted a significant preventive antiulcer effect as indicated by reduction in gastric volume at 200 and 400 mg/kg doses. Only 400 mg/kg of the extract exerted a significant reduction in ulcer index when compared with the control group. The oral route LD50 of FPL was estimated to be 4570 mg/kg while that of FPR was 2754 mg/kg. The LD50 in intraperitoneal injection was estimated to be 1202.26 and 1380.38 mg/kg for FPL and FPR respectively. The phytochemical investigation showed that both extracts possess triterpenoids and saponin, while the presence of flavonoid was detected only in FPL. CONCLUSIONS: The results of this study indicated that FPL and not FPR is effective against experimentally induced gastric ulcers. The presence of varied phytochemical constituents probably influenced the pharmacological differences between the two extracts.


Asunto(s)
Antiulcerosos/uso terapéutico , Mucosa Gástrica/efectos de los fármacos , Malpighiaceae/química , Fitoterapia , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/tratamiento farmacológico , Animales , Antiulcerosos/análisis , Antiulcerosos/farmacología , Cimetidina/farmacología , Modelos Animales de Enfermedad , Femenino , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/patología , Dosificación Letal Mediana , Masculino , Medicinas Tradicionales Africanas , Misoprostol/farmacología , Nigeria , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta , Raíces de Plantas , Ratas , Ratas Endogámicas , Saponinas/análisis , Saponinas/farmacología , Saponinas/uso terapéutico , Triterpenos/análisis , Triterpenos/farmacología , Triterpenos/uso terapéutico
17.
J Complement Integr Med ; 9: Article 9, 2012 Jun 18.
Artículo en Inglés | MEDLINE | ID: mdl-22713279

RESUMEN

The antiulcer activity of 70% methanolic extract of fruits of Terminalia belerica Roxb. (Combretaceae) was evaluated using ethanol induced, aspirin induced, cold stress restraint and pylorus ligated ulcer in rats. The methanolic extract (100, 250, 500, 1000 mg/kg, p.o.) significantly suppressed the peptic ulcer induced by ethanol. Methanolic extract at a dose of 500 mg/kg showed, promising antiulcer activity hence, this dose was selected for further evaluation of antiulcer studies. The methanolic extract (500 mg/kg) showed significant (p<0.05) reduction in gastric volume, free acidity, total acidity, ulcer index, protein and pepsin content and increase in mucus content in pylorus ligated rats as compared to control. Treatment with Terminalia belerica methanolic extract further provided significant antiulcer protection against aspirin induced ulcers but not in cold stress restraint model. These results suggested that the 70% methanolic extract of Terminalia belerica increased resistance to necrotizing agents, providing a direct protective effect on the gastric mucosa and exhibited antiulcer effect.


Asunto(s)
Antiulcerosos/farmacología , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Úlcera Gástrica/tratamiento farmacológico , Terminalia , Animales , Antiulcerosos/uso terapéutico , Aspirina , Biomarcadores/metabolismo , Frío , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Esquema de Medicación , Etanol , Femenino , Frutas , Jugo Gástrico/química , Mucosa Gástrica/metabolismo , Ligadura , Masculino , Medicina Ayurvédica , Metanol , Ratones , Extractos Vegetales/uso terapéutico , Plantas Medicinales , Píloro/cirugía , Ratas , Ratas Wistar , Úlcera Gástrica/etiología , Úlcera Gástrica/metabolismo
18.
J Acupunct Meridian Stud ; 5(2): 80-6, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22483186

RESUMEN

The ethanol extract of the roots of Aerva persica (Burm f) Merrill (Amaranthaceae) was investigated to determine its antiulcer and in vivo antioxidant activities in albino Wistar rats. Ulcers were induced by ethanol and pylorus ligation. The extract was administered at the dose of 200mg/kg orally, p.o. for 15 consecutive days. The ulcer index of the ethanol extract was found to be significantly reduced compared with control animals. The effect was also assessed by determining the free acidity, pepsin activity, total carbohydrate (TC), and protein content (PK) in control, standard, and test group animals. The in vivo antioxidant activity was evaluated by determining the reduced glutathione level (GSH) and malondialdehyde (MDA) level in the tissue homogenates. The results reveal the significant reduction in the level of malondialdehyde and the increase in the level of reduced glutathione in the rats that received the ethanolic extract. Furthermore, histopathological studies have shown that pretreatment with the ethanolic extract of the roots of A persica reduces (100%) ethanol- and pylorus ligation-induced hemorrhagic necrosis in rats.


Asunto(s)
Amaranthaceae , Antiulcerosos/uso terapéutico , Antioxidantes/uso terapéutico , Fitoterapia , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/tratamiento farmacológico , Ácidos/análisis , Animales , Antiulcerosos/administración & dosificación , Antiulcerosos/farmacología , Antioxidantes/administración & dosificación , Antioxidantes/farmacología , Carbohidratos/análisis , Etanol , Femenino , Jugo Gástrico/química , Jugo Gástrico/efectos de los fármacos , Glutatión/sangre , Hemorragia/prevención & control , Humanos , Ligadura , Masculino , Malondialdehído/sangre , Necrosis/prevención & control , Pepsina A/metabolismo , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacología , Raíces de Plantas , Proteínas/análisis , Ratas , Ratas Wistar , Índice de Severidad de la Enfermedad , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología
19.
Asian Pac J Trop Med ; 5(3): 197-201, 2012 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-22305784

RESUMEN

OBJECTIVE: The study was aimed at evaluating the antiulcer activity of ethanolic extract of Achyranthes aspera (EEAA) leaf. METHODS: The anti-ulcer assays were performed on pylorus ligation and chronic ethanol induced ulcer model. The effects of the EEAA on gastric content volume, pH, free acidity, total acidity and ulcer index were evaluated. RESULTS: The percentage of ulcer protection (59.55% and 35.58%) was significantly (P < 0.001) higher in the groups treated with the high dose of EEAA (600 mg/kg), it also reduced the volume of gastric juice and total acidity whereas, gastric pH was increased significantly. CONCLUSIONS: The results of this study show significant gastroprotective activity of EEAA may be due to presence of phyto-constituents like flavanoids, saponins and tannins.


Asunto(s)
Achyranthes/química , Antiulcerosos/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Hojas de la Planta/química , Úlcera Gástrica/tratamiento farmacológico , Animales , Enfermedad Crónica , Etanol , Jugo Gástrico/efectos de los fármacos , Concentración de Iones de Hidrógeno , Ligadura , Ratas , Solventes , Úlcera Gástrica/inducido químicamente
20.
J Med Food ; 15(4): 378-83, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22191571

RESUMEN

Arctium lappa L. has been used in folk medicine as a diuretic, depurative, and digestive stimulant and in dermatological conditions. The mechanisms involved in the anti-ulcerogenic activity of the sesquiterpene onopordopicrin (ONP)-enriched fraction (termed the ONP fraction), obtained from A. lappa leaves, were studied. The gastroprotective mechanism of the ONP fraction was evaluated in experimental in vivo models in rodents, mimicking this disease in humans. ONP fraction (50 mg/kg, p.o.) significantly inhibited the mucosal injury induced by ethanol/HCl solution (75%), indomethacin/bethanecol (68.9%), and stress (58.3%). When the ONP fraction was investigated in pylorus ligature, it did not induce alteration in the gastric volume but did modify the pH and total acid concentration of gastric juice. ONP fraction significantly increased serum somatostatin levels (82.1±4.1 vs. control group 12.7±4 pmol/L) and decreased serum gastrin levels (62.6±6.04 vs. control group 361.5±8.2 µU/mL). Mucus production was not significantly altered by the ONP fraction. Gastroprotection by the ONP fraction was completely inhibited by N-ethylmaleimide treatment and did not modify the effect in the animals pretreated with l-N(G)-nitroarginine methyl ester. These results suggest an antisecretory mechanism involved with the antiulcerogenic effect of the ONP fraction. However, only endogenous sulfhydryls play an important role in gastroprotection of the ONP fraction.


Asunto(s)
Arctium/química , Gastrinas/metabolismo , Lactonas/farmacología , Óxido Nítrico/metabolismo , Sesquiterpenos/farmacología , Somatostatina/metabolismo , Compuestos de Sulfhidrilo/metabolismo , Animales , Antiulcerosos/farmacología , Betanecol/metabolismo , Etanol/efectos adversos , Etilmaleimida , Cromatografía de Gases y Espectrometría de Masas , Jugo Gástrico/efectos de los fármacos , Mucosa Gástrica/efectos de los fármacos , Indometacina/efectos adversos , Indometacina/metabolismo , Masculino , Medicina Tradicional , Extractos Vegetales/farmacología , Hojas de la Planta/química , Ratas , Ratas Wistar
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