160657-48-7Relevant academic research and scientific papers
Novel polyphenols that inhibit colon cancer cell growth affecting cancer cell metabolisms
Gómez de Cedrón, Marta,Vargas, Teodoro,Madrona, Andrés,Jiménez, Aranza,Pérez-Pérez, María-Jesús,Quintela, José-Carlos,Reglero, Guillermo,San-Félix, Ana,Ramírez de Molina, Ana
, p. 377 - 389 (2018)
New series of polyphenols with a hydrophilic galloyl-based head and a hydrophobic N-acyl tail, linked through a serinol moiety, have been synthesized and tested against colon cancer cell growth. Our structure activity relationship studies revealed that galloyl moieties are essential for growth inhibition. Moreover, the length of the N-acyl chain is crucial for the activity. Introduction of a (Z) double bond in the acyl chain increased the anticancer properties. Our findings demonstrate that 16, the most potent compound within this series, has inhibitory effects on colon cancer cell growth and metabolism (glycolysis and mitochondrial respiration) at the same time that it activates 59AMP-activated kinase (AMPK) and induces apoptotic cell death. Based on these results, we propose that 16 might reprogram colon cancer cell metabolism through AMPK activation. This might lead to alterations on cancer cell bioenergy compromising cancer cell viability. Importantly, these antiproliferative and proapoptotic effects are selective for cancer cells. Accordingly, these results indicate that 16, with an unsaturated C18 chain, might be a useful prototype for the development of novel colon cancer cell growth inhibitors affecting cell metabolism.
Synthesis and antiangiogenic activity of new silybin galloyl esters
Ga?ák, Radek,Valentová, Kate?ina,Fuksová, Kate?ina,Marhol, Petr,Kuzma, Marek,Medina, Miguel ángel,Oborná, Ivana,Ulrichová, Jitka,K?en, Vladimír
experimental part, p. 7397 - 7407 (2011/12/14)
The synthesis of various silybin monogalloyl esters was developed, and their antiangiogenic activities were evaluated in a variety of in vitro tests with human umbilical vein endothelial cells (HUVECs). A structure-activity relationship (SAR) study found
