Trypanocidal activity and acute toxicity assessment of triterpene acids

Ferreira, Daniele da Silva; Esperandim, Viviane Rodrigues; Toldo, Míriam Paula Alonso; Saraiva, Juliana; Cunha, Wilson Roberto; Albuquerque, Sérgio de

doi:10.1007/s00436-010-1740-2

Cited by 31 publications

(13 citation statements)

References 23 publications

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“…UA is generally considered to be safe and have minimal adverse effect. Neither mortality nor any signs of toxicity with orally administrating a single dose as high as 2,000 mg/Kg was observed in acute toxicity study in mice [29]. In our study, no toxic effect on experimental animals was observed in our administrating dose of UA (about 200 mg/Kg body weight day in H-UA group).…”

Section: Discussioncontrasting

confidence: 65%

Therapeutic Role of Ursolic Acid on Ameliorating Hepatic Steatosis and Improving Metabolic Disorders in High-Fat Diet-Induced Non-Alcoholic Fatty Liver Disease Rats

et al. 2014

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BackgroundNon-alcoholic fatty liver disease (NAFLD) is one of the most prevalent liver diseases around the world, and is closely associated with obesity, diabetes, and insulin resistance. Ursolic acid (UA), an ubiquitous triterpenoid with multifold biological roles, is distributed in various plants. This study was conducted to investigate the therapeutic effect and potential mechanisms of UA against hepatic steatosis in a high-fat diet (HFD)-induced obese non-alcoholic fatty liver disease (NAFLD) rat model.Methodology/Principal FindingsObese NAFLD model was established in Sprague-Dawley rats by 8-week HFD feeding. Therapeutic role of UA was evaluated using 0.125%, 0.25%, 0.5% UA-supplemented diet for another 6 weeks. The results from both morphologic and histological detections indicated that UA significantly reversed HFD-induced hepatic steatosis and liver injury. Besides, hepatic peroxisome proliferator-activated receptor (PPAR)-α was markedly up-regulated at both mRNA and protein levels by UA. Knocking down PPAR-α significantly inhibited the anti-steatosis role of UA in vitro. HFD-induced adverse changes in the key genes, which participated in hepatic lipid metabolism, were also alleviated by UA treatment. Furthermore, UA significantly ameliorated HFD-induced metabolic disorders, including insulin resistance, inflammation and oxidative stress.Conclusions/SignificanceThese results demonstrated that UA effectively ameliorated HFD-induced hepatic steatosis through a PPAR-α involved pathway, via improving key enzymes in the controlling of lipids metabolism. The metabolic disorders were accordingly improved with the decrease of hepatic steatosis. Thereby, UA could be a promising candidate for the treatment of NAFLD.

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Section: Discussioncontrasting

confidence: 65%

Therapeutic Role of Ursolic Acid on Ameliorating Hepatic Steatosis and Improving Metabolic Disorders in High-Fat Diet-Induced Non-Alcoholic Fatty Liver Disease Rats

et al. 2014

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“…La saponina denominada ácido 3-O-β-D-glucopiranosil oleanólico aislada de las semillas de Randia dumetornm Lam. [75], y de otras plantas [76][77][78], ha mostrado una importante actividad antiinflamatoria en las fases exudativa y de proliferación de la inflamación con dosis entre 25 y 100 mg/kg. Puesto que este mismo tipo de saponina ha sido previamente identificado en las semillas de quinua (véase tabla 1), se podría esperar la manifestación de esta misma actividad por la fracción de saponinas de quinua.…”

Section: Actividad Antiinflamatoriaunclassified

Saponinas de quinua (Chenopodium quinoa Willd.): un subproducto con alto potencial biológico

Ahumada

Ortega

Chito

et al. 2016

Rev. Colomb. Cienc. Quim. Farm.

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Las saponinas son un tipo de metabolito secundario ampliamente estudiado por susreconocidas propiedades biológicas. Gran parte de las investigaciones en fitoquímicaestán dirigidas a encontrar nuevas fuentes naturales de saponinas con aplicaciónmedicinal. La quinua (Chenopodium quinoa Willd.) es una planta que ha alcanzadoun valioso reconocimiento por ser una fuente de alimentos altamente nutritivos, asícomo una especie rica en saponinas triterpénicas contenidas, principalmente, en lacáscara de las semillas. A la fecha, se han identificado alrededor de 30 saponinas derivadasde la hederagenina y de los ácidos oleanólico, fitolacagénico y serjanico en laplanta. El consumo del grano de quinua implica la remoción de la cáscara a fin dereducir su sabor amargo, la ingesta de niveles residuales de saponinas y la obtenciónde un subproducto rico en las mismas. Esta revisión, inicialmente, ofrece una contextualizacióngeneral de las saponinas; posteriormente, recopila las característicasestructurales de las saponinas identificadas en la quinua, describe el efecto del procesamientodel grano en su contenido de saponinas y, finalmente, expone los efectosbiológicos explorados con extractos de saponinas de quinua, los cuales pueden serconsiderados como punto de partida en investigaciones futuras dirigidas al fortalecimientode su uso en el campo farmacéutico y/o nutracéutico.

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“…In addition, other triterpenoid molecules structurally related to MA display very different cytotoxic and antiparasitic activities. Thus, cucurbitane-type triterpenoids have been recently shown to display anti-malarial activity [27], while ursane-type urosolic acid was reported to inhibit growth of Trypanosoma cruzi [28] showing in contrast low anti-plasmodial activity [29]. However, hybrid molecules consisting on ursolic acid bound to pharmacophores showed enhanced inhibitory activity on Plasmodium, presumably by facilitating the access of the bound pharmacophore to haem [30].…”

Section: Introductionmentioning

confidence: 99%

Parasitostatic effect of maslinic acid. I. Growth arrest of Plasmodium falciparum intraerythrocytic stages

Moneriz

Marín-García

Garcı́a-Granados

et al. 2011

Malar J

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BackgroundNatural products have played an important role as leads for the development of new drugs against malaria. Recent studies have shown that maslinic acid (MA), a natural triterpene obtained from olive pomace, which displays multiple biological and antimicrobial activities, also exerts inhibitory effects on the development of some Apicomplexan, including Eimeria, Toxoplasma and Neospora. To ascertain if MA displays anti-malarial activity, the main objective of this study was to asses the effect of MA on Plasmodium falciparum-infected erythrocytes in vitro.MethodsSynchronized P. falciparum-infected erythrocyte cultures were incubated under different conditions with MA, and compared to chloroquine and atovaquone treated cultures. The effects on parasite growth were determined by monitoring the parasitaemia and the accumulation of the different infective stages visualized in thin blood smears.ResultsMA inhibits the growth of P. falciparum Dd2 and 3D7 strains in infected erythrocytes in, dose-dependent manner, leading to the accumulation of immature forms at IC50 concentrations, while higher doses produced non-viable parasite cells. MA-treated infected-erythrocyte cultures were compared to those treated with chloroquine or atovaquone, showing significant differences in the pattern of accumulation of parasitic stages. Transient MA treatment at different parasite stages showed that the compound targeted intra-erythrocytic processes from early-ring to schizont stage. These results indicate that MA has a parasitostatic effect, which does not inactivate permanently P. falciparum, as the removal of the compound allowed the infection to continueConclusionsMA displays anti-malarial activity at multiple intraerythrocytic stages of the parasite and, depending on the dose and incubation time, behaves as a plasmodial parasitostatic compound. This novel parasitostatic effect appears to be unrelated to previous mechanisms proposed for current anti-malarial drugs, and may be relevant to uncover new prospective plasmodial targets and opens novel possibilities of therapies associated to host immune response.

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Trypanocidal activity and acute toxicity assessment of triterpene acids

Cited by 31 publications

References 23 publications

Therapeutic Role of Ursolic Acid on Ameliorating Hepatic Steatosis and Improving Metabolic Disorders in High-Fat Diet-Induced Non-Alcoholic Fatty Liver Disease Rats

Therapeutic Role of Ursolic Acid on Ameliorating Hepatic Steatosis and Improving Metabolic Disorders in High-Fat Diet-Induced Non-Alcoholic Fatty Liver Disease Rats

Saponinas de quinua (Chenopodium quinoa Willd.): un subproducto con alto potencial biológico

Parasitostatic effect of maslinic acid. I. Growth arrest of Plasmodium falciparum intraerythrocytic stages

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