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1.
Rev. chil. nutr ; 50(2)abr. 2023.
Artículo en Español | LILACS-Express | LILACS | ID: biblio-1515172

RESUMEN

En Chile, al 31 de diciembre del 2020 un 12,5% de los extranjeros eran de nacionalidad haitiana. Se desconoce el estado nutricional (EN) en embarazadas y lactantes; así como también la prevalencia de lactancia materna exclusiva (LME) de la población haitiana en Chile. Los objetivos de este trabajo fueron comparar: (i) el EN de embarazadas haitianas y chilenas, (ii) el EN de lactantes y (iii) la duración de la LME en hijos de madres haitianas y chilenas. Para esto se analizó la base de datos de la población haitiana y chilena atendidos entre los años 2016-2019 en el Centro de Salud Familiar (CESFAM) "Los Castaños" ubicado en la comuna de La Florida. En la etapa pre-gestacional, las embarazadas haitianas presentaron mayor prevalencia de bajo peso en comparación a embarazadas chilenas (p= 0,0003), mientras que al término del embarazo presentaron una mayor prevalencia de estado nutricional normal (p= 0,0001) y menor prevalencia de obesidad (p= 0,0001). Respecto al estado nutricional de los lactantes, sólo se observaron diferencias en el primer mes de vida, donde un 82% de los lactantes haitianos tenían un EN normopeso en comparación al 24% en los lactantes chilenos (p= 0,0001). No se observaron diferencias significativas en la prevalencia de LME hasta los 6 meses entre lactantes haitianos y chilenos (35,3% vs 30%, respectivamente). Es importante mencionar que ninguno de los dos grupos de lactantes cumplió con la meta establecida por la Organización Mundial de la Salud (OMS) que propone LME en los primeros seis meses de vida hasta al menos 50%. En conclusión, se evidencian diferencias en el EN de las embarazadas y lactantes de ambos países, mientras que la prevalencia de LME en ambos grupos fue similar.


In Chile, until December 31st, 2020, 12.5% of foreign residents were from Haiti. The nutritional status (NS) in pregnant women and infants is unknown; as well as the prevalence of exclusive breastfeeding (EBF) of the Haitian population residing in Chile. This study aimed to compare: (i) the NS of Haitian and Chilean pregnant women, (ii) the NS of infants, and (iii) the duration of EBF in children of Haitian and Chilean mothers. We analyzed the database of the Haitian and Chilean population attended between the years 2016-2019 at the Primary Care Health Center (CESFAM) "Los Castaños" located in the commune of La Florida. During the pregestational stage, the Haitian pregnant women had a higher prevalence of low weight compared to the Chilean pregnant women (p= 0,0003), whereas, at the end of the pregnancy, they had a higher prevalence of normal nutritional status (p= 0,0001) and a lower prevalence of obesity and a tendency at the end of pregnancy. Whereas at the end of the pregnancy, Chilean women had a higher prevalence of obesity. Regarding the nutritional status of the infants, differences were only observed in the first month of life, where 82% of Haitian infants had a normal weight compared to 24% of Chilean infants (p= 0.0001). No significant differences were observed in the prevalence of EBF up to 6 months between Haitian and Chilean infants (35.3% vs. 30%, respectively). It is important to mention that neither of the two groups of infants met the goal established by the World Health Organization (WHO) that proposes EBF for the first six months of life up to at least 50%. In conclusion, there are differences in the NE of pregnant and lactating women in both countries, while the prevalence of EBF in both groups was similar.

2.
Rev Med Inst Mex Seguro Soc ; 60(3): 328-337, 2022 May 01.
Artículo en Español | MEDLINE | ID: mdl-35763408

RESUMEN

Background: Studies carried out in Mexico show that the COVID-19 pandemic has negatively impacted families in every field. Confinement has generated problems and economic, social and health instability in a large sector of the population, especially in the most vulnerable, to which children and adolescents are part of. Objective: To identify the impact of the confinement and closure of children daycare centers from the Instituto Mexicano del Seguro Social (IMSS) derived from the COVID-19 pandemic. Material and methods: Three questionnaire-type surveys were implemented via email for workers who were users of IMSS children daycare centers from September to November 2020. The surveys had a perception design, one- and two-stage, simple random and with results by segments. Results were obtained for independent proportions. The z-test was applied at 95% confidence. Results: Effects on workers and child users of the service derived from the closure of children daycare centers were observed, and it was greater in entities with closed children daycare centers than with those ones in operation (p < 0.0001). Conclusions: The negative impact derived from the closure of children daycare centers due to the confinement by COVID-19 in workers who use the service and their children was identified. The spheres with the greatest impact were the economic, the working environment, as well as the children's health (and their families).


Introducción: : estudios realizados en México muestran que la pandemia por COVID-19 ha impactado de forma negativa a las familias en todos los ámbitos. El confinamiento ha generado problemas e inestabilidad económica, social y en la salud en un gran sector de la población, especialmente en el más vulnerable, donde se encuentran los niños y adolescentes. Objetivo: identificar el impacto del confinamiento y el cierre de guarderías del Instituto Mexicano del Seguro Social (IMSS) derivado de la pandemia por COVID-19. Material y métodos: se aplicaron vía correo electrónico tres encuestas tipo cuestionario a trabajadores usuarios del servicio de guardería del IMSS de septiembre a noviembre de 2020. Las encuestas tenían diseño de percepción uni y bietápico, aleatorio simple y con resultados por segmentos. Se obtuvieron resultados para proporciones independientes. Se aplicó el z-test con un 95% de confianza. Resultados: se observó afectación en los trabajadores y en los niños usuarios del servicio derivado del cierre de las guarderías del IMSS, la cual fue mayor en las entidades con guarderías cerradas que en aquellas en operación (p < 0.0001). Conclusiones: se identificó el impacto negativo derivado del cierre de guarderías IMSS por el confinamiento por COVID-19 en trabajadores usuarios del servicio y sus hijos. Los ámbitos con más afectación fueron el económico, el laboral, así como la salud de los niños (y sus familias).


Asunto(s)
COVID-19 , Adolescente , COVID-19/epidemiología , Niño , Guarderías Infantiles , Humanos , México/epidemiología , Pandemias , Encuestas y Cuestionarios
3.
J Nat Prod ; 73(4): 639-43, 2010 Apr 23.
Artículo en Inglés | MEDLINE | ID: mdl-20359186

RESUMEN

Carnosic acid (1) has been shown to possess gastroprotective activity in vitro and in vivo. However, little is known of the gastroprotective effect or cytotoxicity of carnosic acid gamma-lactone (3). To determine structure-activity relationships, a series of 17 esters of 3 were prepared including aliphatic, aromatic, and heterocyclic derivatives. Also, two units of 3 were coupled with succinic and phthalic acid as linkers. The compounds were assessed for their gastroprotective effect in the HCl/EtOH-induced gastric lesions model in mice and for cytotoxicity in human lung fibroblasts, human adenocarcinoma AGS cells, and Hep G2 hepatocellular carcinoma cells. At a single oral dose of 40 mg/kg, the gastroprotective effect increased moderately with the length of the alkyl chain. The best effects were observed for the butyrate (9) and chloroacetate (6) derivatives. Activity of fatty acid esters increased with chain length but decreased with unsaturation. The best gastroprotective effect, with lowest cytotoxicity, was found for the palmitate (11) and oleate (12) derivatives.


Asunto(s)
Abietanos/síntesis química , Abietanos/farmacología , Antiulcerosos/química , Antiulcerosos/farmacología , Mucosa Gástrica/efectos de los fármacos , Lactonas/química , Lactonas/farmacología , Ácido Oléico/farmacología , Palmitatos/farmacología , Extractos Vegetales/síntesis química , Extractos Vegetales/farmacología , Abietanos/química , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Ácido Oléico/síntesis química , Ácido Oléico/química , Palmitatos/síntesis química , Palmitatos/química , Extractos Vegetales/química , Estereoisomerismo , Relación Estructura-Actividad
4.
J Pharm Pharmacol ; 60(2): 245-51, 2008 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-18237473

RESUMEN

The gastroprotective mechanism of the natural diterpene ferruginol was assessed in mice and rats. The involvement of gastric prostaglandins (PGE(2)), reduced glutathione, nitric oxide or capsaicin receptors was evaluated in mice either treated or untreated with indometacin, N-ethylmaleimide (NEM), N-nitro-L-arginine methyl ester (L-NAME) or ruthenium red, respectively, and then orally treated with ferruginol or vehicle. Gastric lesions were induced by oral administration of ethanol. The effects of ferruginol on the parameters of gastric secretion were assessed in pylorus-ligated rats. Gastric PGE(2) content was determined in rats treated with ferruginol and/or indometacin. The reduction of gastric glutathione (GSH) content was determined in rats treated with ethanol after oral administration of ferruginol, lansoprazole or vehicle. Finally, the acute oral toxicity was assessed in mice. Indometacin reversed the gastroprotective effect of ferruginol (25 mg kg(-1)) but not NEM, ruthenium red or L-NAME. The diterpene (25 mg kg(-1)) increased the gastric juice volume and its pH value, and reduced the titrable acidity but was devoid of effect on the gastric mucus content. Ferruginol (25, 50 mg kg(-1)) increased gastric PGE(2) content in a dose-dependent manner and prevented the reduction in GSH observed due to ethanol-induced gastric lesions in rats. Single oral doses up to 3 g kg(-1) ferruginol did not elicit mortality or acute toxic effects in mice. Our results showed that ferruginol acted as a gastroprotective agent stimulating the gastric PGE(2) synthesis, reducing the gastric acid output and improving the antioxidant capacity of the gastric mucosa by maintaining the GSH levels.


Asunto(s)
Abietanos/farmacología , Antiulcerosos/farmacología , Dinoprostona/metabolismo , Jugo Gástrico/efectos de los fármacos , 2-Piridinilmetilsulfinilbencimidazoles/farmacología , Abietanos/administración & dosificación , Administración Oral , Animales , Antiulcerosos/administración & dosificación , Relación Dosis-Respuesta a Droga , Etanol , Jugo Gástrico/metabolismo , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Glutatión/efectos de los fármacos , Glutatión/metabolismo , Lansoprazol , Masculino , Ratones , Ratas , Ratas Wistar , Compuestos de Sulfhidrilo , Pruebas de Toxicidad Aguda
5.
J Pharm Pharmacol ; 59(2): 289-300, 2007 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-17270082

RESUMEN

The gastroprotective abietane diterpene ferruginol has been shown to present high cytotoxicity. In order to obtain active compounds with less cytotoxicity, 18 semisynthetic ferruginol derivatives and totarol were assessed for their gastroprotective effects in the HCl/ethanol-induced gastric lesion model in mice, as well as for cytotoxicity in human gastric epithelial cells (AGS) and human lung fibroblasts (MRC-5). At 20 mg kg(-1), the greatest gastroprotective effects were provided by abieta-8,11,13-triene (1), abieta-8,11,13-trien-12-yl-2-chloropropanoate (8), abieta-8,11,13-trien-12-yl propenoate (9), 12-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyloxy)-abieta-8,11,13-triene (17) and 12-(beta-D-galactopyranosyloxy)-abieta-8,11,13-triene (18), all of which were as active as the reference drug lansoprazole at 20 mg kg(-1), reducing gastric lesions by 69, 76, 67, 72 and 61%, respectively. No relation was observed between lipophilicity and the gastroprotective effect. Compounds that showed the greatest cytotoxicity towards AGS cells were ferruginol (2), the corresponding formate (5), acetate (6), propionate (7), 8, 9, 12-(beta-D-glucopyranosyloxy)-abieta-8,11,13-triene (16), 18 and totarol (20) (IC50 18-44 microM). Ferruginol and compounds 5-9, 16, 18 and 20 were the most toxic compounds against fibroblasts (IC50 19-56 microM), with a correlation to AGS cells. The derivative 19 was much more active against AGS cells than towards fibroblasts. The best activity/cytotoxicity ratio was found for compound 17, with a lesion index comparable with lansoprazole at 20 mg kg(-1) and cytotoxicity >1000 microM towards MRC-5 and AGS cells, respectively. In conclusion, some derivatives showed a better gastroprotective effect/cytotoxicity ratio than the parent compound ferruginol. A total of 13 new compounds are reported here for the first time.


Asunto(s)
Abietanos/química , Antiulcerosos/química , Abietanos/uso terapéutico , Abietanos/toxicidad , Animales , Antiulcerosos/uso terapéutico , Antiulcerosos/toxicidad , Células Cultivadas , Células Epiteliales/efectos de los fármacos , Mucosa Gástrica/efectos de los fármacos , Humanos , Ratones , Sustancias Protectoras/química , Sustancias Protectoras/uso terapéutico , Sustancias Protectoras/toxicidad , Gastropatías/tratamiento farmacológico , Pruebas de Toxicidad
6.
Life Sci ; 79(14): 1349-56, 2006 Aug 29.
Artículo en Inglés | MEDLINE | ID: mdl-16712876

RESUMEN

The triterpene oleanolic acid 1 and its semisynthetic derivatives 2-7 were assessed for gastroprotective and ulcer-healing effect using human epithelial gastric cells (AGS) and human lung fibroblasts (MRC-5). The ability of the compounds to protect the AGS cells against the damage induced by sodium taurocholate (NaT), to stimulate the cellular reduced glutathione (GSH) and prostaglandin E(2) content, to enhance AGS and MRC-5 cell proliferation and to scavenge superoxide anion in vitro was studied. The cytotoxicity of the compounds was assessed towards MRC-5 and AGS cells. In addition, the gastroprotective activity of the compounds was assessed in vivo using the HCl/EtOH-induced ulcer model in mice. All the assayed compounds displayed a significant reduction of AGS cells damage after incubation with NaT. None of the studied compounds was active as a superoxide anion scavenger nor stimulated the GSH content in AGS cell cultures. Compounds 1, 2, 4 and 6 were able to increase the prostaglandin content in AGS cell cultures. Concerning the proliferation assays, a significant stimulating effect was observed for compounds 3 and 7 on AGS cells and for 1 and 7 on MRC-5 fibroblasts. Regarding cytotoxicity, derivatives 2, 4, 6 and 7 were less toxic than the parent compound oleanolic acid. Our results strongly support the predictive capacity of the in vitro assessment of gastroprotective activity allowing the reduction of experimental animals.


Asunto(s)
Antiulcerosos/uso terapéutico , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacología , Úlcera Gástrica/prevención & control , 2-Piridinilmetilsulfinilbencimidazoles , Animales , Antiulcerosos/síntesis química , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Depresores del Sistema Nervioso Central , Fenómenos Químicos , Química Física , Dinoprostona/metabolismo , Células Epiteliales , Etanol , Fibroblastos , Depuradores de Radicales Libres/farmacología , Mucosa Gástrica/citología , Mucosa Gástrica/efectos de los fármacos , Glutatión/metabolismo , Humanos , Ácido Clorhídrico , Lansoprazol , Masculino , Ratones , Ácido Oleanólico/síntesis química , Omeprazol/análogos & derivados , Omeprazol/farmacología , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/patología , Superóxidos/metabolismo , Ácido Taurocólico/antagonistas & inhibidores , Ácido Taurocólico/toxicidad
7.
Life Sci ; 78(21): 2503-9, 2006 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-16309708

RESUMEN

The gastroprotective activity of the diterpene ferruginol isolated from Prumnopitys andina wood and bark was determined on HCl/EtOH-induced gastric lesions in mice. The effect of the compound on the healing of subacute gastric lesions in rats was also studied. The mode of action of the diterpene was assessed using human gastric epithelial cells (AGS) and MRC-5 fibroblasts. The effect of ferruginol on the prostaglandin E2 content, protection against sodium taurocholate induced-damage and reduced glutathione content was evaluated on AGS cells as well as on the growth of AGS and fibroblast cultures. The free radical scavenging effect of ferruginol was assessed by the 1,1-diphenyl-2-picryl-hydrazil radical and superoxide anion assays. The effect of ferruginol on human erythrocyte membrane lipoperoxidation was determined. The cytotoxicity of the compound was assessed by means of the neutral red uptake. At 25 mg/kg, ferruginol inhibited the appearance of gastric lesions by 60% showing similar effects than lansoprazole at 20 mg/kg. Additionally, the compound displayed a significant ulcer healing activity in rats at 25 and 50 mg/kg with curative ratios of 36.0% and 92.5%, respectively, while the reference compound ranitidine at 50 mg/kg showed a curative ratio of 79.6%. At 6 and 12 microM, ferruginol increased significantly the prostaglandin E2 content. A strong inhibition of lipoperoxidation was found (IC50: 1.4 microM), but no effect was observed on the sodium taurocholate induced-damage or reduced glutathione content. Ferruginol stimulated cell proliferation at 1-2 microM in AGS cells and at 4-8 microM in fibroblasts, with cytotoxicities (IC50) of 24 and 26 microM, respectively. Our results support that ferruginol acts as gastroprotective increasing the PGs content, protecting the cells against lipid peroxidation and improving the gastric ulcer healing by a stimulating effect on the cell proliferation. These findings encourage further pharmacological studies of ferruginol as a potential new anti-ulcerogenic drug.


Asunto(s)
Antiulcerosos , Diterpenos/farmacología , Úlcera Gástrica/tratamiento farmacológico , Úlcera Gástrica/prevención & control , Abietanos , Ácido Acético , Animales , Compuestos de Bifenilo , Línea Celular , Supervivencia Celular/efectos de los fármacos , Dinoprostona/metabolismo , Células Epiteliales/efectos de los fármacos , Membrana Eritrocítica/efectos de los fármacos , Etanol , Fibroblastos/efectos de los fármacos , Depuradores de Radicales Libres/farmacología , Mucosa Gástrica/patología , Glutatión/metabolismo , Ácido Clorhídrico , Peroxidación de Lípido/efectos de los fármacos , Masculino , Ratones , Oxidación-Reducción , Picratos/metabolismo , Ranitidina/farmacología , Ratas , Ratas Sprague-Dawley , Solventes , Úlcera Gástrica/inducido químicamente , Superóxidos/metabolismo , Ácido Taurocólico/farmacología
8.
Phytother Res ; 19(12): 1038-42, 2005 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-16372369

RESUMEN

An infusion or decoction of the aerial parts of Fabiana imbricata (Solanaceae) is used in traditional medicine in Chile and Argentina as a digestive and diuretic agent. The main sesquiterpene of the plant was identified as 11-hydroxy-4-amorphen-15-oic acid. At doses of 25, 50 and 100 mg/kg, the compound showed a dose-dependent gastroprotective effect in HCl/EtOH-induced gastric lesions in mice reducing the lesions by 68% at 100 mg/kg. Seven derivatives of the terpene were prepared and their gastroprotective effect was assessed in HCl/EtOH-induced gastric lesions in mice. The cytotoxicity of the products was evaluated in fibroblasts and AGS cells. At 100 mg/kg, 11-hydroxy-4-amorphen-15-p-toluidinamide presented the best gastroprotective effect reducing the gastric lesions by 80%, showing a similar effect to lansoprazole at 20 mg/kg. The compound, however, presented higher cytotoxicity than other derivatives with the IC50 ranging between 110 and 145 microm in AGS cells and fibroblasts, respectively. Most compounds proved to be non-toxic showing cytotoxicity values higher than 1000 microm. The spectroscopic data of six 11-hydroxy-4-amorphen-15-oic acid derivatives are presented here for the first time.


Asunto(s)
Antiulcerosos/uso terapéutico , Sesquiterpenos/uso terapéutico , Solanaceae/química , Úlcera Gástrica/tratamiento farmacológico , Animales , Antiulcerosos/química , Antiulcerosos/toxicidad , Células Cultivadas , Humanos , Espectroscopía de Resonancia Magnética , Ratones , Estructura Molecular , Fitoterapia , Componentes Aéreos de las Plantas , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Extractos Vegetales/toxicidad , Sesquiterpenos/química , Sesquiterpenos/farmacología , Sesquiterpenos/toxicidad
9.
Z Naturforsch C J Biosci ; 60(7-8): 511-22, 2005.
Artículo en Inglés | MEDLINE | ID: mdl-16163822

RESUMEN

The resin of the tree Araucaria araucana (Araucariaceae) is used by the Mapuche Amerindians in southern Chile and Argentina to treat ulcers and has been shown to display a gastroprotective effect in animal models. A study was undertaken to isolate, identify and assess the gastroprotective effect of the resin constituents and its semisynthetic derivatives as well as to evaluate the cytotoxicity of the products in cell cultures. Eleven diterpenes (ten labdane and a pimarane) were isolated from a resin sample collected in Chile. The labdane derivatives 15-acetoxylabd-8(17)-en-19-ol as well as 15,19-diacetoxylabd-8(17)-en are reported for the first time as natural products. Six diterpenes previously described from other plant sources are reported for the first time for the A. araucana resin. The structure of all compounds was elucidated by spectroscopic means. Some 24 diterpenes isolated/prepared in amounts over 10 mg were evaluated for gastroprotective effects in the ethanol/HCl-induced ulcer model in mice at 100 mg/kg. The highest gastroprotective activities were provided by 15-hydroxyimbricatolal, 15-acetoxyimbricatolal, 15-acetoxylabd-8(17)-en-19-oic acid methyl ester and 15-acetoxy-19-labdanoic acid, all of them being as active as the reference drug lansoprazole at 20 mg/kg. The cytotoxicity of 30 diterpenes as well as lansoprazole was assessed towards human lung fibroblasts (MRC-5) and 26 compounds were evaluated on the human gastric epithelial cell line AGS by means of the neutral red uptake assay. A concentration-dependent cell viability inhibition was found with IC50 values ranging from 27 up to > 1000 microM. The relationship between the cytotoxicity data and lipophilicity of the products is also discussed.


Asunto(s)
Antiulcerosos , Diterpenos/farmacología , Fitoterapia , Tracheophyta , Antiulcerosos/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Diterpenos/aislamiento & purificación , Diterpenos/toxicidad , Resinas de Plantas , Árboles
10.
Pharmacol Res ; 52(5): 429-37, 2005 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-16125407

RESUMEN

Dehydroabietic acid derivatives have been reported to display antisecretory and antipepsin effect in animal models. Some 19 dehydroabietic acid diterpenes were prepared and assessed for gastroprotective activity in the HCl/EtOH-induced gastric lesions in mice as well as for cytotoxicity in human lung fibroblasts (MRC-5) and human epithelial gastric (AGS) cells. At a single oral dose of 100 mg kg(-1), highest gastroprotective effect was provided by dehydroabietanol, its corresponding aldehyde, dehydroabietic acid (DHA) and its methyl ester, N-(m-nitrophenyl)-, N-(o-chlorophenyl)- and N-(p-iodophenyl)abieta-8,11,13-trien-18-amide (compounds 12-14), N-2-aminothiazolyl- and N-benzylabieta-8,11,13-trien-18-amide (compounds 18-19) being as active as lansoprazole at 20 mg kg(-1) and reducing the lesion index by at least 75%. In the compound series including the alcohol, ester, aldehyde, acid and methyl ester at C-18 (compounds 1-9), highest activity was related with the presence of an alcohol, aldehyde, acid or methyl ester at C-18, the activity being strongly reduced after esterification. The cytotoxicity of the compounds 1-9 towards AGS cells and fibroblasts was higher than the values for the amides 10-19. In the compounds 10-19, the best gastroprotective effect was observed for the aromatic amides 12-14 (75-85% inhibition of gastric lesions) bearing a nitro or halogen function in the N-benzoyl moiety. Lowest cytotoxicity was found for the amides, with IC(50) values >1000 microM for fibroblasts and from 200 up to >1000 microM for AGS cells, respectively. The N-2-aminothiazolyl- and N-benzylamide derivatives were also very active as gastroprotectors with higher cytotoxicity against AGS cells.


Asunto(s)
Abietanos/farmacología , Supervivencia Celular/efectos de los fármacos , Diterpenos/farmacología , Mucosa Gástrica/efectos de los fármacos , Animales , Línea Celular , Relación Dosis-Respuesta a Droga , Fibroblastos/efectos de los fármacos , Humanos , Masculino , Ratones , Relación Estructura-Actividad
11.
J Ethnopharmacol ; 101(1-3): 271-6, 2005 Oct 03.
Artículo en Inglés | MEDLINE | ID: mdl-15985351

RESUMEN

The resin from the tree Araucaria araucana (Araucariaceae) has been used since pre-columbian times by the Mapuche amerindians to treat ulcers. The gastroprotective effect of the resin was assessed in the ethanol-HCl-induced gastric ulcer in mice showing a dose-dependent gastroprotective activity at 100, 200 and 300 mg/kg per os. The main three diterpene constituents of the resin, namely imbricatolic acid, 15-hydroxyimbricatolal and 15-acetoxyimbricatolic acid were isolated and evaluated for gastroprotective effect at doses of 50, 100 and 200 mg/kg. A dose-related gastroprotective effect with highly significant activity (P<0.01) was observed at doses up to 200 mg/kg. At 100 mg/kg, the highest gastroprotective activity was provided by 15-hydroxyimbricatolal and 15-acetoxyimbricatolic acid, all of them being as active as the reference drug lansoprazole at 20 mg/kg. The cytotoxicity of the main diterpenes as well as lansoprazole was studied towards human lung fibroblasts (MRC-5) and determined by the MTT reduction assay. A concentration-dependent cell viability inhibition was found with IC50 values ranging from 125 up to 290 microM. Our results support the traditional use of the Araucaria araucana resin by the Mapuche culture.


Asunto(s)
Antiulcerosos/farmacología , Cycadopsida/química , Diterpenos/farmacología , Mucosa Gástrica/efectos de los fármacos , Resinas de Plantas/farmacología , 2-Piridinilmetilsulfinilbencimidazoles , Animales , Células Cultivadas , Diterpenos/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Humanos , Lansoprazol , Ratones , Omeprazol/análogos & derivados , Omeprazol/farmacología , Resinas de Plantas/análisis
12.
J Pharm Pharmacol ; 57(2): 265-71, 2005 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-15720793

RESUMEN

The gastroprotective activity of the new semi-synthetic solidagenone derivative 15,16-epoxy8(9),13(16),14-labdatrien-7 beta-methoxy-6 beta-ol (ELMO) has been assessed on the model of HCl/EtOH-induced gastric lesions in mice. Human gastric epithelial cells (AGS) and fibroblasts (MRC-5) were used to determine its mode of action. The effect of ELMO on the prostaglandin E2 content, cellular reduced glutathione (GSH) and protection against damage induced by sodium taurocholate was assessed against AGS cells. The effect of ELMO on the growth of AGS and fibroblast cultures was evaluated. The superoxide anion scavenging capacity of the compound was studied also. The cytotoxicity of ELMO, expressed as cell viability, was assessed using two independent endpoints: neutral red uptake (NRU) and the reduction of 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) for MRC-5 fibroblasts and NRU for AGS cells. A single oral dose of ELMO (10 and 20 mg kg(-1)) inhibited the appearance of gastric lesions in mice displaying similar values to lansoprazole at 20 mg kg(-1). At 40 microM ELMO increased the prostaglandin E2 content but not GSH in AGS cells. The compound showed no effect on sodium taurocholate-induced damage and was devoid of superoxide anion scavenging activity. Concentrations of 0.5, 1, 2 and 4 microM stimulated fibroblast but not AGS cell proliferation. The compound showed weak cytotoxicity with values (IC50) of 411 (NRU) and 418 microM (MTT) for fibroblasts and 261 microM (NRU) for AGS cells. The results support further pharmacological study of this compound as a potential new anti-ulcerogenic drug.


Asunto(s)
Antiulcerosos/farmacología , Furanos/farmacología , Naftalenos/farmacología , 2-Piridinilmetilsulfinilbencimidazoles , Administración Oral , Animales , Antiulcerosos/química , Línea Celular , Proliferación Celular/efectos de los fármacos , Chile , Dinoprostona/química , Dinoprostona/metabolismo , Modelos Animales de Enfermedad , Diterpenos/administración & dosificación , Diterpenos/síntesis química , Diterpenos/uso terapéutico , Evaluación Preclínica de Medicamentos/métodos , Epitelio/patología , Etanol/administración & dosificación , Etanol/efectos adversos , Fibroblastos/efectos de los fármacos , Fibroblastos/fisiología , Furanos/síntesis química , Furanos/uso terapéutico , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/patología , Humanos , Ácido Clorhídrico/administración & dosificación , Ácido Clorhídrico/efectos adversos , Concentración 50 Inhibidora , Lansoprazol , Pulmón/patología , Ratones , Naftalenos/administración & dosificación , Naftalenos/síntesis química , Naftalenos/uso terapéutico , Rojo Neutro/química , Omeprazol/análogos & derivados , Omeprazol/uso terapéutico , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/tratamiento farmacológico , Sales de Tetrazolio/química
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