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1.
Biochem Pharmacol ; 103: 53-63, 2016 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-26774455

RESUMEN

Pyruvate is a key intermediate of the carbohydrate metabolism with endogenous scavenger properties. However, it cannot be used in clinics due to its instability. Ethyl pyruvate (EP) has shown better stability as well as an antioxidant and anti-inflammatory activity. Calcium pyruvate monohydrate (CPM) is another stable pyruvate derivative that could also provide the benefits from calcium, fundamental for bone health. Considering everything, we propose CPM as a therapeutic strategy to treat diseases with an immune component in which there is also a significant dysregulation of the skeletal homeostasis. This could be applicable to inflammatory bowel disease, which is characterized by over-production of pro-inflammatory mediators, including cytokines and reactive oxygen and nitrogen metabolites that induces intestinal mucosal damage and chronic inflammation, and extra-intestinal symptoms like osteopenia and osteoporosis. The effects of CPM and EP (20, 40 and 100mg/kg) were evaluated on the trinitrobenzenesulfonic acid (TNBS) model of colitis in rats, after a 7-day oral treatment, with main focus on colonic histology and inflammatory mediators. Both pyruvates showed intestinal anti-inflammatory effects in the TNBS-induced colitis. They were evident both histologically, with a recovery of the mucosal cytoarchitecture and a reduction of the neutrophil infiltration, and through the profile of inflammatory mediators (IL-1, IL-6, IL-17, IL-23, iNOS). However, CPM appeared to be more effective than ethyl pyruvate. In conclusion, CPM exerts intestinal anti-inflammatory effect on the TNBS-induced colitis in rats, although further experiments are needed to explore its beneficial effects on bone health and osteoporosis.


Asunto(s)
Antiinflamatorios no Esteroideos/uso terapéutico , Colitis/tratamiento farmacológico , Piruvatos/uso terapéutico , Ácido Trinitrobencenosulfónico , Animales , Antiinflamatorios no Esteroideos/farmacología , Colitis/inducido químicamente , Colitis/metabolismo , Colitis/patología , Colon/efectos de los fármacos , Colon/inmunología , Colon/metabolismo , Colon/patología , Femenino , Expresión Génica , Mediadores de Inflamación/metabolismo , Mucosa Intestinal/efectos de los fármacos , Mucosa Intestinal/inmunología , Mucosa Intestinal/metabolismo , Mucosa Intestinal/patología , FN-kappa B/metabolismo , Infiltración Neutrófila , Fosforilación , Piruvatos/farmacología , Ácido Pirúvico/farmacología , Ácido Pirúvico/uso terapéutico , Ratas Wistar
2.
Eur J Med Res ; 11(8): 343-50, 2006 Aug 30.
Artículo en Inglés | MEDLINE | ID: mdl-17052970

RESUMEN

OBJECTIVE: The aim of this study was to evaluate the efficacy and safety of composite extracts in reducing weight, as the main outcome measure. Secondary measures of the study were body composition change. DESIGN: Randomised, double blind, placebo-controlled clinical trial. SETTING: Tertiary university clinic. SUBJECTS: hundred and five subjects, 5 of them withdrawn consent, 2 drop-outs not related to study preparation. INTERVENTION: two tablet per meal concept supposed to generate a "psychological" therapy-like approach during 12 weeks supported by measured physical activity. The tablets 1 (one hour before meals, comprises extracts of Asparagus, Green tea, Black tea, Guarana, Mate and Kidney beans) and 2 (taken half an hour after meals, comprises extracts of Kidney bean pods, Garcinia cambogia, and Chromium yeast) are taken twice daily with two main meals. RESULTS: A significant change of the Body Composition Improvement Index (BCI) was observed in the active extract group compared to placebo (p = 0.012). Weight, BMI, waist-to-hip ratio was not statistically different between groups. Body fat loss was greater in active group (p = 0.011) compared to placebo. A weight loss parameter corrected for exercise was introduced and found to be higher in active group (p = 0.046) than in placebo, meaning that the formula was more efficacious, due to a concurrently performed exercise program--a recommended strategy for life style modification. CONCLUSIONS: A significant change of the Body Composition Improvement Index and the decrease in body fat was statistically significant in active extract subjects compared to placebo. A change in some outcome measures like: weight, BMI failed to produce significant difference between groups.


Asunto(s)
Composición Corporal/efectos de los fármacos , Suplementos Dietéticos , Sobrepeso/efectos de los fármacos , Extractos Vegetales/uso terapéutico , Pérdida de Peso/efectos de los fármacos , Adulto , Apolipoproteínas A/sangre , Glucemia/análisis , Peso Corporal , Colesterol/sangre , Método Doble Ciego , Ayuno , Femenino , Humanos , Insulina/sangre , Lipoproteínas HDL/sangre , Lipoproteínas LDL/sangre , Masculino , Persona de Mediana Edad , Extractos Vegetales/efectos adversos , Extractos Vegetales/química , Factores de Tiempo , Resultado del Tratamiento , Triglicéridos/sangre
3.
Eur J Med Res ; 9(9): 423-31, 2004 Sep 29.
Artículo en Inglés | MEDLINE | ID: mdl-15546807

RESUMEN

Within a randomized double blind, placebo controlled trial the electrical activity of the human brain has been monitored using charge mode technology (Laplacian estimates) after exposure to a lozenge containing 4 different herbal preparations (lavender oil, extracts from hops, lemon balm and oat) or a matching placebo without any active ingredients. Sixteen healthy volunteers (8 males and 8 females) were tested within a crossover design. After baseline recording each subject sucked a lozenge and 2 hours later a second one. Recording was performed immediately after finishing the lozenge and in hourly intervals thereafter. Comparison to reference periods of 10 min eyes open and 5 min eyes closed, respectively, revealed increases in alpha 1, alpha 2 and beta 1 electrical power at the electrode positions Cz, P3, T3 and T5 which were even more pronounced after a second application two hours later. Since alpha 1 changes repeatedly have been attributed to attentional states, increases of this electrical activity must be seen as indicator of a relaxational psychophysiological state. Changes in the alpha2 frequencies have been related to working memory indicating that an increase can be seen as a correlate for attenuating this circuit. Increases of beta1 activity have been seen in the presence of anxiolytic drugs including major and minor tranquilizers. The changes as observed after the application of this herbal composition are therefore in line with the idea of having induced a state of relaxation and regeneration. This interpretation suggests that one could expect from the ingestion of this lozenge to better cope with psychological and emotional stress. The data are further proof that recording computer aided quantitative EEG is a very fruitful and promising approach in psychophysiology.


Asunto(s)
Avena , Electroencefalografía , Humulus , Lavandula , Melissa , Aceites Volátiles/administración & dosificación , Aceites de Plantas/administración & dosificación , Adulto , Encéfalo/fisiología , Estudios Cruzados , Método Doble Ciego , Femenino , Humanos , Masculino , Persona de Mediana Edad , Extractos Vegetales/administración & dosificación , Estudios Prospectivos , Conducta en la Lactancia/fisiología , Comprimidos , Factores de Tiempo
4.
Lipids ; 38(2): 165-70, 2003 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-12733749

RESUMEN

The current study was carried out to examine the effects of policosanols and phytosterols, alone and in combination, on lipid profiles, cholesterol biosynthesis, and tissue histopathological changes in hamsters. Fifty male Golden Syrian hamsters, weighing 100 to 120 g, were fed a regular rodent chow for 2 wk before being randomly assigned into 5 groups of 10 animals each fed semisynthetic diets for 4 wk. Group 1 was given a control diet that contained 0.25% cholesterol and 5% fat with a PUFA to saturated FA ratio of 0.4. Groups 2 to 5 were fed the control diet and given Octa-6 [a policosanol mixture from sugar cane wax, 25 mg/kg body weight (BW)], Ricewax (a policosanol mixture from rice wax with 50% being converted to the corresponding acids, 50 mg/kg BW), phytosterols (Cholestatin; 1,000 mg/kg BW), and Ricewax (50 mg/kg BW) plus phytosterols (1,000 mg/kg BW), respectively. The results showed that there was no difference between Octa-6 and Ricewax treatments in any of the lipid parameters measured, and both had similar levels of triglyceride (TG), total cholesterol (T-C), and HDL cholesterol (HDL-C) as the control. Octa-6 but not Ricewax increased (P = 0.03) non-HDL-C as compared with the control. Phytosterols reduced T-C (P < 0.0003) and HDL-C (P < 0.004) without a significant effect on TG and non-HDL-C as compared to the control. Ricewax plus phytosterols had effects similar to those with phytosterols alone. Free cholesterol synthetic rates were not different among the treatments. Policosanols or phytosterols did not show any toxic effects in liver, heart, brain, or kidney. Results suggest that, although phytosterols reduce T-C and HDL-C levels, policosanols have no significant favorable effect in changing lipid levels in hamsters.


Asunto(s)
Anticolesterolemiantes/farmacología , Colesterol/biosíntesis , Alcoholes Grasos/farmacología , Lípidos/sangre , Fitosteroles/farmacología , Animales , Peso Corporal , Colesterol/sangre , Cricetinae , Dieta , Sinergismo Farmacológico , Hígado/efectos de los fármacos , Hígado/patología , Masculino , Mesocricetus , Triglicéridos/sangre
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