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1.
Clin. transl. oncol. (Print) ; 17(1): 74-84, ene. 2015. tab, ilus
Artigo em Inglês | IBECS | ID: ibc-131907

RESUMO

Background. Choline kinase alpha (ChoKα) is a critical enzyme in the synthesis of phosphatidylcholine, a major structural component of eukaryotic cell membranes. ChoKα is overexpressed in a large variety of tumor cells and has been proposed as a target for personalized medicine, both in cancer therapy and rheumatoid arthritis. Materials and methods. Triterpene quinone methides (TPQ) bioactive compounds isolated from plants of the Celastraceae family and a set of their semisynthetic derivatives were tested against the recombinant human ChoKα. Those found active as potent enzymatic inhibitors were tested in vitro for antiproliferative activity against HT29 colorectal adenocarcinoma cells, and one of the active compounds was tested for in vivo antitumoral activity in mice xenographs of HT29 cells. Results. Among 59 natural and semisynthetic TPQs tested in an ex vivo system, 14 were highly active as inhibitors of the enzyme ChoKα with IC50 <10 μM. Nine of these were potent antiproliferative agents (IC50 <10 μM) against tumor cells. At least one compound was identified as a new antitumoral drug based on its in vivo activity against xenographs of human HT-29 colon adenocarcinoma cells. Conclusions. The identification of a new family of natural and semisynthetic compounds with potent inhibitory activity against ChoKα and both in vitro antiproliferative and in vivo antitumoral activity supports further research on these inhibitors as potential anticancer agents. Their likely role as antiproliferative drugs deserves further studies in models of rheumatoid arthritis (AU)


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Assuntos
Colina Quinase/análise , Colina Quinase/metabolismo , Produtos Biológicos/metabolismo , Produtos Biológicos/farmacocinética , Produtos Biológicos/uso terapêutico , Produtos Biológicos/análise , Produtos Biológicos/imunologia , Fosfatidilcolina-Esterol O-Aciltransferase , Fosfatidilcolina-Esterol O-Aciltransferase/metabolismo
2.
Clín. investig. arterioscler. (Ed. impr.) ; 22(supl.1): 12-16, abr. 2010. ilus
Artigo em Espanhol | IBECS | ID: ibc-145467

RESUMO

La capacidad de las lipoproteínas de alta densidad (HDL) para transportar el colesterol desde los tejidos periféricos hasta el hígado para su excreción se considera crucial para prevenir la acumulación de macrófagos “espumosos” en la íntima arterial. La adquisición del colesterol celular se inicia con la cesión de éste a la apolipoproteína (apo) A-I mediante ABCA1, generándose así pre-β HDL. La esterificación del colesterol por la lecitinacolesterol aciltransferasa promueve la formación de HDL maduras (α HDL). En humanos, prácticamente todos los ésteres de colesterol de las HDL llegan al hígado tras su transferencia a las lipoproteínas de muy baja (VLDL) y baja (LDL) densidad por la proteína transferidora de ésteres de colesterol y posterior captación mediante el receptor de LDL. Sin embargo, las HDL pueden entregar directamente colesterol libre al hígado mediante el receptor CLA-1/SR-BI, paso facilitado por la acción previa de la lipasa hepática. Estas últimas interacciones causan la liberación de HDL pequeñas y apo A-I, que adquirirán nuevamente colesterol en los tejidos periféricos (AU)


The ability of high-density lipoproteins (HDL) to transport cholesterol from peripheral tissues to the liver for excretion is considered crucial to prevent the accumulation of foamy macrophages in the arterial intima. The acquisition of cellular cholesterol is initiated by ABCA1-mediated cholesterol efflux to apolipoprotein (apo) A-I, thus generating pre-β-HDL. Cholesterol esterification by lecithin-cholesterol acyltransferase promotes the formation of mature HDL (α-HDL). In humans, practically all HDL cholesterol esters reach the liver after being transferred to very low (VLDL)- and low (LDL)-density lipoproteins by the cholesteryl ester transfer protein and subsequent uptake by the LDL receptor. However, HDL can deliver free cholesterol directly to the liver through the CLA- 1/SR-B1 receptor, a step that is aided by the prior action of hepatic lipase. These latter interactions lead to the release of small HDL particles and apo A-I, which then can newly acquire cholesterol in the peripheral tissues (AU)


Assuntos
Feminino , Humanos , Masculino , Colesterol/sangue , Fosfatidilcolina-Esterol O-Aciltransferase/administração & dosagem , Deficiência de Proteína S/patologia , Aterosclerose/metabolismo , Fígado/anormalidades , Lipase/deficiência , Bile/enzimologia , Lipólise/genética , Colesterol/metabolismo , Fosfatidilcolina-Esterol O-Aciltransferase/metabolismo , Deficiência de Proteína S/complicações , Aterosclerose/complicações , Fígado/citologia , Lipase/farmacologia , Bile/citologia , Lipólise/fisiologia
3.
Fisioterapia (Madr., Ed. impr.) ; 30(6): 268-272, nov.-dic. 2008. tab, graf
Artigo em Espanhol | IBECS | ID: ibc-61215

RESUMO

Este estudio presenta los efectos conseguidos por la electroporación en la lipólisis abdominal utilizando la vehiculación de la fosfatidilcolina (fosfolípido que facilita la absorción de las grasas). Se llevó a cabo en 10 mujeres voluntarias, nulíparas, sedentarias, con una edad media de 25,10 años e índice de masa corporal entre 18,5 y 25 kg/m2. Recibieron 15 sesiones de tratamiento fisioterápico, constando esta de una aplicación tópica de fosfatidilcolina al 10% liposomada en el abdomen con electroporación. La técnica consistió en colocar el transductor del equipo en la pared abdominal emitiendo ondas electromagnéticas con un voltaje de 500 mV y una frecuencia de 50 Hz durante 30 minutos. Este tratamiento alcanzó una reducción del tejido adiposo subcutáneo de la pared abdominal, comprobada por medida perimétrica del abdomen, medida del pliegue cutáneo infraumbilical y por ultrasonografía. En la perimetría, la reducción media fue de 4,75 cm, en la plicometría de 2,43 mm y la ultrasonografía demostró una disminución del grosor del tejido adiposo que pasó de una media de 2,21 cm a 1,65 cm. Sin embargo, no se halló ninguna reducción ponderal significativa, aunque la disminución presentada en los tres métodos de evaluación sugiere que la utilización de la fosfatidilcolina con la electroporación puede desencadenar efectos lipolíticos(AU)


The present study presents the effects achieved with electroporation in abdominallipolysis using vehiculization of phosphatidylcholine (phospholipide that facilitates fatabsorption). The study was conducted in 10 voluntary women, nulliparous, sedentary women, with a mean age of 25.10 years and body mass index between 18.5 and 25 kg/m2.They were administered 15 sessions of physiotherapy, this being made up of a topicalapplication of 10% liposomal phosphatidylcholine in the abdomen with electroporation.The technique consisted in placing the equipment transductor on the abdominal wall,emitting electromagnetic waves with a 500mV voltage and 50 Hz frequency for 30 minutes.This treatment achieved a reduction of the subcutaneous adipose tissue of the abdominalwall, verified by perimetric measurement of the abdomen, measurement of infraumbilicalskin fold and by ultrasound. In the perimetry, the mean reduction was 4.75 cm, in theplicometry 2.43mm and the ultrasonograph showed a decrease of adipose tissue thicknessthat went from a mean of 2.21 cm to 1.65 cm. However, no significant weight reduction wasfound, although the decrease found in the three evaluation methods suggests that the useof phosphatidylcholine with electroporation may precipitate lipolitic effects(AU)


Assuntos
Humanos , Feminino , Adulto , Eletroporação/estatística & dados numéricos , Eletroporação/tendências , Eletroporação , Lipólise/fisiologia , Lipólise/efeitos da radiação , Fosfatidilcolina-Esterol O-Aciltransferase/uso terapêutico , Índice de Massa Corporal , Testes de Campo Visual/métodos , Modalidades de Fisioterapia/tendências , Modalidades de Fisioterapia , Eletroporação/classificação , Eletroporação/métodos , Parede Abdominal/fisiologia , Parede Abdominal , Testes de Campo Visual/instrumentação , Testes de Campo Visual/tendências , Estudos Transversais
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