[Show abstract][Hide abstract] ABSTRACT: tMaqui, Aristotelia chilensis (Mol.) Stuntz, Elaeocarpaceae, is a berry with one of the highest antioxidantactivities known, and which is exploited from the wild as raw material for nutraceutical products. Thepresent work studies factors that might affect fruit quality in further industrial processing and proposesHPTLC fingerprint methods for routine quality control of metabolites and radical scavengers. Polyphenoland anthocyanin concentrations in fruit were determined in cultivated maqui. Polyphenol concentrationdid not vary significantly during the ripening process, but differed from one growing season to another(2.1 and 2.8 g GAE/100 g dry weight). Anthocyanin concentration increased during maturation from 0.07to 1.13 g Cy-3-glu/100 g dry weight, whereas antioxidant ORAC value remained stable (194–241 �molTE/g DW). Anthocyanins were concentrated only in the fleshy parts of ripe fruits (4.2 g Cy-3-glu/100 gDW), while other polyphenols were found in the seeds (2.1 g GAE/100 g DW). Polyphenol and anthocyanincontents did not decrease during desiccation, cooling or freezing processes. Desiccation approximatelydoubled sugar contents, from 24.5◦Brix in fresh to 50◦Brix in dry fruit. Frozen fruit retained their solublesolids content and anthocyanins, while polyphenols increased.
[Show abstract][Hide abstract] ABSTRACT: Cardiovascular Diseases (CVD) represent about 30% of all causes of death worldwide. The development of CVD is related in many cases with the previous existence of metabolic syndrome (MS). It is known that apple consumption has a cardiovascular protecting effect, containing phenolic compounds with antioxidant effect, which are concentrated in the fruit peel. The objective of this study was to test the effect of apple peel consumption in a murine model of MS and apoE−/− mice. Apple supplemented diets reduced the biochemical parameters (glycaemia, total cholesterol, HDL-cholesterol, LDL-cholesterol, ureic nitrogen, triglycerides, insulin, and asymmetric dimethylarginine (ADMA)) of MS model in CF1 mice significantly. The model apoE−/− mouse was used to evaluate the capacity of the apple peel to revert the progression of the atherogenesis. FD with HAP reverts cholesterol significantly and slows down the progression of the plate diminishing the cholesterol accumulation area. With these results, it can be concluded that the consumption of apple peel reduces several MS parameters and the atherogenic progression in mice.
Evidence-based Complementary and Alternative Medicine 05/2015; 2015:1-10. DOI:10.1155/2015/918384 · 1.88 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Postharvest sunscald on apples is a physiological disorder that develops on the skin during cold storage. The symptoms develop only on sun-exposed sections of the fruit with or without sun-injury and they appear as superficial dark-brown patches. In order to determine the role of different antioxidant systems in sunscald development, fruit with different sun exposures and sun-injury levels on the tree were harvested and stored at 0 °C for up to 4 months. Ascorbic acid (AsA), glutathione (GSH), AsA–GSH recycling enzymes activities and transcripts levels, and flavonoids and carotenoid concentrations were monitored monthly. Unexposed fruit (shaded) did not develop sunscald. On sun-exposed sections of the fruit, sunscald incidence increased and appeared closer to harvest, as sunburn severity increased. Total ascorbic acid (AsA) was the highest on fruit with no sunburn symptoms (shaded and sun-exposed), but over 90% of it was in its oxidized form. There were no clear differences for any of the AsA–GSH recycling enzyme activities or transcription levels between sun exposures levels during cold storage.
All quercetin glycosides were higher in fruit with sun-injury compared to those sun-exposed or shaded throughout the storage period. In severe sunburned or shaded fruit, quercetin glycosides represented 73% and 10% of total phenolic content, respectively. Quercetin glycosides contents at harvest were highly correlated with sunscald appearance in storage.
Sunscald symptoms appearance was associated with lower quercetin glycosides concentration on fruit skin. The results indicate that the AsA–GSH cycle does not play a direct role in ‘sunscald’ development on Granny Smith apples. Instead, quercetin glycosides appear to be directly related with sunscald expression postharvest, i.e. the higher their concentration in the tissue, the faster the accumulation of their brown oxidative products.
[Show abstract][Hide abstract] ABSTRACT: Sun-injury (=sunscald, sunburn) in fruit crops is caused by photodynamic reactions on heated fruit sections exposed to direct sunlight. There is evidence supporting the oxidative nature of this disorder. Nevertheless, there are other physiological events, typically observed in water-stressed plants, such as water relations and osmoregulation that greatly influence external and internal quality of sun-injured fruit and have poorly addressed in the literature. Apple tissues (skin and flesh) with different levels of sun exposure and sun-injury (mild, moderate (Mod), severe (Sev)) were sampled at different growing stages during 2011 and 2012, in Royal Gala and Fuji. Water, solutes, and turgor potentials, relative water content (RWC), carbohydrates concentration (sucrose, sorbitol, glucose, fructose), internal ethylene concentration (IEC), and textural curves were determined. Skin water potential decreased with fruit development and it was significantly more negative in sun-injured tissue compared to unexposed ones. Solutes potential also decreased in skin and flesh with increasing sun damage, but the opposite was found in turgor potential. Fruit RWC at harvest decreased with increasing sunburn severity. Sun exposure induced sorbitol and glucose accumulation in fruit peel and flesh. Tissue with Mod and Sev sunscald showed higher IEC early in the season. Fruit shape and firmness were also altered by sun exposure. The results might indicate that sun-exposed tissue via more negative water potentials activates an abiotic stress-response cascade, perhaps mediated by sugars and ethylene, to cope with the environmental stress caused by high irradiance and heat, whose consequences are peculiar fruit quality traits.
Scientia Horticulturae 09/2013; 161:143-152. DOI:10.1016/j.scienta.2013.06.035 · 1.37 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Buddleja globosa Hope (matico) is a Chilean plant used by native medicine mainly in the treatment of wound healing and as an anti‐inflammatory agent. We have developed a standardized hydroalcoholic extract from matico leaves, in terms of total polyphenolic content. This extract may be useful in accelerating the wound healing process. To this end, we studied the in vivo effects of this extract in a rat model, in terms of general homeostasis. Data showed that oral treatment of adult male Sprague‐Dawley rats with this extract, for up to 12 days, did not alter their hemogram and clinical chemistry parameters. In addition, we showed that topical treatment with the same extract was able to accelerate wound healing in these animals, most likely through shortening the inflammatory stage of the healing process. Altogether, our data demonstrate that local effects of this particular
standardized matico extract are likely to retain their wound healing properties while not altering the general homeostasis of the animals. We discuss these results in terms of the possible pharmacological applications of this extract.
[Show abstract][Hide abstract] ABSTRACT: El alto contenido de principios activos con poder antioxidante que poseen las hojas de Ugni molinae, arbusto componente del sotobosque nativo, motivaron la búsqueda de material promisorio para su cultivo. El objetivo del trabajo fue determinar la capacidad de enraizamiento de estacas de dos procedencias del límite norte de distribución de la especie y el efecto de la exposición y edad de la hoja sobre su concentración de taninos y flavonoides. El ensayo de enraizamiento se realizó en cama caliente con estacas provenientes de 10 plantas madres de cada procedencia. Al cabo de tres meses se logró enraizamiento en más del 70 % de las estacas superando la procedencia Cordillera de Los Andes a la procedencia Cordillera de la Costa. La aplicación de hormona de enraizamiento a la base de las estacas (1,5 mg g-1 AIB), mejoró significativamente el porcentaje de enraizamiento y la calidad de las raíces formadas. Para la cuantificación de principios activos se cosecharon hojas de cinco plantas de sol y cinco plantas de sombra de cada procedencia. Las hojas de sol presentaron mayor concentración de flavonoides que las hojas de sombra en ambas procedencias. Las hojas de sol de la Cordillera de Los Andes contenían más taninos que las hojas de sombra de la misma procedencia. La edad de la hoja no influyó en su concentración de principios activos.
[Show abstract][Hide abstract] ABSTRACT: Boldo (Peumus boldus Mol.) is a medicinal plant native to the central zone of Chile and part of the sclerophyll forest. More than 2000tons of dried leaves exported annually are wild collected. To develop a cultivation system that supports sustainable production of boldo leaves, we have studied growth and harvest of boldo under different light and soil water conditions. The leaf yield per plant as well as the alkaloid and essential oil content were the same for plants grown under shade and for plants exposed to full sun. The only difference between the shaded and the full sun plants was a higher percentage of stem in the harvested product of shade grown plants. This result would permit the intercropping of boldo in forest plantations without affecting the leaf yield and medicinal quality. The excellent adaptation to dry conditions was confirmed, as the different treatments of soil water led to similar leaf yields and plant heights. Plants submitted to water stress produced fewer but longer shoots and contained less essential oil. None of the treatments except water stress affected the medicinal quality requirements of alkaloid or essential oil concentration in the leaves. Wild collected leaves are inexpensive because of low production costs. To be able to compete with wild supplied leaves in the international market, we have evaluated high density plantings as a way to lower costs of a cultivated product by mechanizing harvest. High planting densities led to loweryielding individuals, but leaf yield per area increased. Plant height and the percentage of leaves in the harvested product was the same for densities of 8- and 16 plants m−2. The leaves produced by cultivated boldo generally fulfill the requirements described in the European Pharmacopoeia. We conclude that boldo can be successfully cultivated under the described cultivation conditions.
[Show abstract][Hide abstract] ABSTRACT: Buddleja globosa is a medicinal shrub native to Chile. Its leaves have been traditionally used for wound and ulcer healing. Different medicinal properties, such as outstanding antioxidant, anti-inflammatory, wound healing and analgesic activities have been shown. Today, all raw materials for pharmaceutical process are coming from wild collection or recently established crops but not from selected plants. Studies of the genetic or environmental variability of the species would permit the optimization of yield and quality factors through the selection of genetic material or suitable production sites and management techniques.To assess which traits are determined genetically some yield related plant and leaf characteristics were studied in three wild populations and the cultivated accessions from the same provenances. The cultivated accessions also included three clones coming from individuals found in rural home gardens. For the cultivation studies individuals were arranged in a randomised block design, and those for the irrigation studies in split plots watered at 20% and 65% field capacity.Plant characteristics such as height and width of the plant, the ratio of both, stem diameter and leaf density differed significantly among natural populations. In leaf characteristics only the presence of stipules showed significant differences. The cultivated progenies or clones may give an idea if these differences among populations are due to environmental or to genetic effects. Compared with other provenances, plants from the coastal provenance Los Ruiles are tallest in both natural populations and cultivated clones and also showed superior leaf yields in spite of their lower leaf density.The hairy leaves may cause allergic reactions at the moment of harvest. This characteristic is not influenced by different irrigation treatments and shows no significant differences between cultivated and wild plants.Because of the significant higher leaf yields per plant in home garden clones we assume that formerly individuals with a higher leaf production were selected for cultivation.
[Show abstract][Hide abstract] ABSTRACT: Sun-damage (sunburn) in apples is one of the main causes in Chile for rejection of apples for export cultivated in areas with high temperatures and high levels of sunlight. The objective of this study was to determine the effect of increasing levels of sunburn on the peel (exocarp) and flesh (mesocarp) of different apple cultivars (cvs) in terms of pigment, phenolics content and antioxidant activity. During 2006/07 to 2008/09 seasons two assays were carried out: (1) concentration of total phenolics and total antioxidant activity in the peels of cvs Fuji, Braeburn and Granny Smith, with and without sunburn; and (2) pigments (chlorophylls, carotenoids and anthocyanins), total phenolics, total antioxidant activity and quercetins (Q) in different areas of the peel and flesh of cv Fuji apples. The antioxidant activity in apple peel on the exposed side at severe (SL2) (1.7±2.4 mg*g FW-1) and moderate levels of damage (SL1) (11.2±0.9 mg*g FW-1) was significantly higher than that found in peel of undamaged or healthy fruit (SL0) exposed to direct sunlight (7.0±0.9 mg*g FW-1). The same relationship for sun-damaged and un-damaged tissue was observed in the concentration of phenolics. The concentration of Q glycosylates in the peel of Fuji apples with SL2 and SL1 damage at both the center of the exposed side and its surroundings was significantly higher than that of the unexposed side. Q galactoside presented the highest concentration in both healthy and damaged fruit. Q glucoside showed the highest increase in sun-damaged fruit, while Q arabinoside decreased in relative terms. A decrease in chlorophylls and anthocyanins, and an increase in carotenoids were also observed in sun-damaged fruit. The fact that sun-damaged apples presented a higher concentration of phenolic compounds and antioxidant activity, given the favorable effects of these on human health, represents an alternative commercial opportunity.
Journal of Food Agriculture and Environment 07/2010; 8(3-4):920-925. · 0.44 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Cardiovascular diseases account for the majority of deaths worldwide. Many of their risk factors have been identified but, for their continued study, research centering on new murine models is of interest. In this study, a high fat diet (HFD) and a normal diet (ND) (25 and 4.4% fat, respectively) were tested over a 40-day period to induce the same metabolic alterations in CF-1 mice in two separate experiments. The parameters measured for these effects corresponded to the weight of ingested food and water, to the weight of the mice and their selected organs (adipose tissue, gastrocnemius, liver and heart), to their biochemical profile (glycemia, blood uric nitrogen, uric acid, triglycerides, cholesterol, proteins and albumin) and to the percentage of fat in their livers. The biochemical profile of the CF-1 mice fed a diet high in fat but balanced in proteins (16.9%) showed statistically significant increases in glycemia, cholesterol and triglyceride levels. A statistically significant increase in the weight of adipose tissue was also observed. No statistically significant differences were observed in the muscular mass of either of the groups of mice, but a high percentage of fat was found in the liver. The results lead to the conclusion that CF-1 mice fed a HFD develop metabolic alterations that correspond to an equivalent metabolic syndrome. This is important in the evaluation of the effects of various interventions, such as food, exercise and molecules, on metabolic alterations in mice induced by the intake of a HFD.
Molecular Medicine Reports 05/2008; 1(3):401-5. DOI:10.3892/mmr.1.3.401 · 1.55 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Drimys winteri (Winteraceae) is a tree with medicinal properties native to Chile. Its bark contains polygodial and drimenol in unknown quantities, with antimicrobial and antinociceptive activity. The purpose of the present study was to quantify polygodial and drimenol concentrations in leaves of five populations of D. winteri and one of Drimys andina from different regions of Chile, by GC analysis of the hexane extract. The concentration of these compounds was also determined in the bark of one of the D. winteri populations. In dried leaves mean concentrations of 0.99% for polygodial and 0.011% for drimenol could be observed, both differing significantly among the studied populations. It is concluded that polygodial and drimenol are present in the leaves and the bark of D. winteri and in D. andina leaves, this being the first report of the presence of these compounds in the latter species.
[Show abstract][Hide abstract] ABSTRACT: 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.
Journal of Pharmacy and Pharmacology 02/2007; 59(2):289-300. DOI:10.1211/jpp.59.2.0015 · 2.26 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: The gastroprotective effect of the sesquiterpene cyperenoic acid and seven semi-synthetic derivatives was assessed in the HCl/ethanol-induced gastric ulcer model in mice. At doses of 25, 50 and 100 mg kg(-1), cyperenoic acid showed a dose-dependent gastroprotective effect reducing the lesions by 45 and 75% at 50 and 100 mg kg(-1), respectively. Seven derivatives of the sesquiterpene were prepared and their gastroprotective activity compared at 50 mg kg(-1). The cytotoxicity of the compounds was evaluated in fibroblasts and AGS cells. At 50 mg kg(-1), patchoulan-15-oic acid (compound 8) presented the best gastroprotective effect, reducing the gastric lesions by 86%, with a similar effect to lansoprazole at 20 mg kg(-1). The gastroprotective effect of cyperenol, cyperenoic acid methyl ester and the ethylamide and butylamide from cyperenoic acid were in the same range, reducing the gastric lesions by 72-77%. Cyperenol and cyperenoic acid methyl ester, however, were more cytotoxic with IC50 (concentration that produces a 50% inhibitory effect) values of 44 and 75, 48 and 75 microM against AGS cells and fibroblasts, respectively. The best gastroprotective effect with lower cytotoxicity was found for the compound 8, cyperenoic acid and the p-anisidyl derivative 7.
Journal of Pharmacy and Pharmacology 12/2006; 58(11):1507-13. DOI:10.1211/jpp.58.11.0012 · 2.26 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: 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.
Life Sciences 09/2006; 79(14):1349-56. DOI:10.1016/j.lfs.2006.03.044 · 2.70 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: 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.
Phytotherapy Research 12/2005; 19(12):1038-42. DOI:10.1002/ptr.1784 · 2.66 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: The labdane diterpene solidagenone 1 and its semisynthetic and biotransformation derivatives 2-10 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), prostaglandin E(2) content, 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 fibroblasts and AGS cells. A significant reduction of cell damage after NaT incubation was observed when the AGS cells were pretreated with compounds 2 and 6. Treatment with compounds 4-6, 8 and 9 significantly stimulated the GSH content in AGS cell cultures. None of the studied compounds was active as a superoxide anion scavenger. In AGS cells treated with compounds 1-10, only compound 5 was able to increase prostaglandin content. Concerning the proliferation assays, a significant stimulating effect was observed for compounds 2, 8, 9 on AGS cells and for 5, 7-9 on MRC-5 fibroblasts. Regarding cytotoxicity, solidagenone showed higher toxicity while compounds 4 and 7 were the less toxic. Our results showed that most of the studied compounds act in vitro as gastroprotectors increasing the cellular GSH content. Additionally, some derivatives exhibited in vitro ulcer-healing effect stimulating the cell proliferation.
Life Sciences 10/2005; 77(17):2193-205. DOI:10.1016/j.lfs.2005.04.007 · 2.70 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: "Bailahuén" is the common name of a medicinal shrub native to Chile where this resinous herb is widely used for its liver stimulating properties. Although the official species is Haplopappus baylahuen Remy (Asteraceae), other species of the same genus are also used in different regions as "bailahuén". A thin layer chromatography (TLC) method for rapid identification of different species and detection of adulterations is described for four of the species: Haplopappus baylahuen, Haplopappus taeda Reiche, Haplopappus multifolius Phil., and Haplopappus remyanus Wedd. To confirm efficiency in all species antioxidant properties were screened in resins, infusions, and methanolic extracts by tests of lipid peroxidation in erythrocytes and free radical scavenging activity by DPPH. In both studies Haplopappus baylahuen showed the lowest antioxidant capacity. In DPPH analyses, infusion and resins of Haplopappus baylahuen also showed the lowest and Haplopappus remyanus the major inhibiting activity of free radicals, while Haplopappus multifolius proved to have the highest result when the methanolic extracts were used. The chemical characterization of the studied species showed important levels of flavonoids and coumarins, with flavonoids predominating in Haplopappus taeda, coumarins in Haplopappus multifolius and both of them in Haplopappus baylahuen and Haplopappus remyanus.
Journal of Ethnopharmacology 03/2005; 97(1):97-100. DOI:10.1016/j.jep.2004.10.027 · 3.00 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: 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.
Journal of Pharmacy and Pharmacology 03/2005; 57(2):265-71. DOI:10.1211/0022357055461 · 2.26 Impact Factor