Search results for "Apoptosis"
showing 10 items of 1809 documents
Antiproliferative activity of green, black tea and olive leaves polyphenols subjected to biosorption and in vitro gastrointestinal digestion in Caco-…
2020
Olive (Olea europaea L.) leaves and tea (Camellia sinensis) are rich sources of bioactive compounds, especially polyphenols. Our previous studies have evidenced the potential use of Saccharomyces cerevisiae as a natural delivery system for these antioxidants and a means to improve their bioaccessibility in the human gut. In the present work, the antiproliferative effect of green tea (GT), black tea (BT) and olive leaves (OL) infusions and suspensions of S. cerevisiae were evaluated, for the first time, in human colon cancer cells (Caco-2) after biosorption and in vitro gastrointestinal digestion. The bioaccessible fractions (BF) were not overtly cytotoxic, not affecting cell viability. ROS …
2-cinnamamido, 2-(3-phenylpropiolamido) and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity and mechanism of action
2013
Several new 2-cinnamamido, 2-(3-phenylpropiolamido) and 2-(3-phenylpropanamido)benzamides were synthesized by stirring in pyridine the opportune acid chlorides with the appropriate anthranilamide derivatives. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).
Characterizing BCL-2 family protein domains in membranes:insertion, interaction and apoptotic modulation roles
2015
El objetivo de mi tesis doctoral es el estudio de los dominios transmembrana (TMD) de las proteínas de la familia Bcl-2. La principal función de esta familia de proteínas es la regulación del proceso apoptótico (1,2). Para Ello, se establece un balance de interacciones proteína-proteína entre los miembros pro- y antiapoptóticos de esta familia proteica (3,4). Nuestra hipótesis de trabajo postula que los fragmentos transmembrana de dichas proteínas pueden estar implicados no sólo en su localización subcelular sino también en el establecimiento de la red de interacciones entre proteínas Bcl-2 así como en el desarrollo de su función apoptótica.. Para corroborar esta hipótesis, hemos analizado …
Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality.
2015
Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptos…
Retinoic-Acid-Induced Downregulation of the 67 KDa Laminin Receptor Correlates with Reduced Biological Aggressiveness of Human Neuroblastoma Cells
2012
Neuroblastoma is a common tumor of the childhood arising from embryonal sympathetic neural cell precursors. Despite of the improved therapeutic strategies, the survival rate of high-risk neuroblastoma patients is poor. Although complete clinical remissions can be achieved, relapse is relatively frequent, indicating a role for the persistence of the minimal residual disease (for review, Maris, 2010). Treatments with derivatives of retinoic acid (RA), the biologically active form of vitamin A, produce significant improvements on the therapy of high-risk neuroblastoma patients, when used together with intensive multimodal therapies (Reynolds et al., 2003, for review). Despite some controversy …
New tricyclic systems as photosensitizers towards triple negative breast cancer cells.
2022
AbstractNineteen pyrrolo[1,2-h][1,7]naphthyridinones and pyrido[2,3-c]pyrrolo[1,2-a]azepinones were synthesized as new tricyclic systems in which the pyridine ring is annelated to the 6,7-dihydroindolizin-8(5H)-one and 5,6,7,8-tetrahydro-9H-pyrrole[1,2-a]azepine-9-one moieties to obtain potential photosensitizing agents. They were tested for their photoantiproliferative activity on a triple-negative breast cancer cell line, MDA-MB-231, in the dark and under UVA light (2.0 J/cm2). We demonstrated that their toxicity, only when exposed to light, was primarily due to the generation of reactive oxygen species while their photodegradation products were not responsible for their activity. The mos…
New Tripentone Analogs with Antiproliferative Activity
2017
Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with fair overall yields (34–57%). All tripentone derivatives were tested in the range of 0.1–100 μM for cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivative, with GI50 values of 4.25 µM and 20.73 µM for HCT-116 a…
Funciones protectoras de los astrocitos en la inflamación y el estrés oxidativo cerebral
2018
La enfermedad de Alzheimer (EA) es una enfermedad neurodegenerativa que se presenta con mayor prevalencia en la población anciana. Afecta a alrededor de 37 millones de personas en todo el mundo. Desde el punto de vista inmunohistoquímico, la EA se caracteriza por la presencia de placas neuríticas (con el péptido tóxico Aβ1-42, entre otros) y ovillos neurofibrilares en diversas áreas del cerebro, responsables de la pérdida neuronal, el deterioro de las conexiones sinápticas y la gliosis reactiva causando la inflamación característica de esta enfermedad. Resultados previos indican que los astrocitos son células de protección para las neuronas y que podrían proteger de la inflamación y del est…
Estudio del papel de la proteína activadora de la apoptosis apaf-1 en modelos celulares de la enfermedad de huntington
2012
La apoptosis es un proceso biológico regulado a través de interacciones proteína-proteína que conforman diversos complejos. Estos complejos representan puntos interesantes de intervenciones químicas en diversas enfermedades neurodegenerativas como la enfermedad de Huntington (HD). Esta enfermedad se presenta debido a la expansión de poliglutaminas en el extremo N-terminal de la proteína huntingtina (Htt). En la actualidad, una de las características más estudiadas de esta patología es la formación de agregados de proteínas en el espacio citosólico y nuclear que incluyen a fragmentos N-terminal de la proteína huntingtina mutante (mHtt). El papel de los agregados en la patología es aún discut…
Abstract C75: Overcoming KRAS/LKB1 mutant NSCLC resistance to BET bromodomain inhibitors with gemcitabine or Mcl-1 inhibition
2015
Abstract The purpose of our study was to define a method and mechanism for overcoming the resistance of clinically relevant KRAS-mutant/LKB1-deficient NSCLC cells to the BET-bromodomain inhibitor JQ1. LKB1 (Serine/threonine kinase 11) is mutated with loss of function in conjunction with mutated KRAS in 7-10% of NSCLC. Importantly, KRAS-mutant/LKB1-deficiency is associated with tumor aggressiveness and poor survival in human patients as well as in genetically engineered mouse models. Indeed, although the BET bromodomain inhibitor JQ1 dramatically reduces tumor volume in KRAS mutant mice, it has little effect in KRAS-mutant/LKB1-deficient mice. BET bromodomain proteins are chromatin readers t…