title: Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes.
abstract: A small group of hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment have been investigated for their ability to inhibit the expression of the VEGF, hTERT and c-Myc genes. The VEGF gene is involved in the generation of the vascular endothelial growth factor (VEGF) and thus in the angiogenic process whereas the two latter ones are related to the activation of telomerase. All three genes therefore may be of paramount importance in the cancer generation process. It has been found that colchicine and some of its derivatives display a measurable ability to inhibit the expression of the VEGF and the two other telomerase-related genes. In the case of some of the hybrids, the available data point to the colchicine fragment being responsible for the observed biological activities. It is the first time that the last biological feature has been reported for colchicine or derivatives thereof.
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Concepción
authors.initials: C
authors.lastname: Vilanova
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Santiago
authors.initials: S
authors.lastname: Díaz-Oltra
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Juan
authors.initials: J
authors.lastname: Murga
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain. Electronic address: efalomir@qio.uji.es.
authors.forename: Eva
authors.initials: E
authors.lastname: Falomir
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Miguel
authors.initials: M
authors.lastname: Carda
authors.affiliation: Depart. de Q. Orgánica, Univ. de Valencia, E-46100 Burjassot, Valencia, Spain. Electronic address: alberto.marco@uv.es.
authors.forename: J Alberto
authors.initials: JA
authors.lastname: Marco
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D003078:Colchicine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D015870:Gene Expression / Q000187:drug effects; D016259:Genes, myc / Q000187:drug effects*; D019073:HT29 Cells; D006801:Humans; D011753:Pyrones / Q000138:chemical synthesis* / Q000494:pharmacology*; D019098:Telomerase / Q000096:biosynthesis* / Q000235:genetics / Q000378:metabolism; D042461:Vascular Endothelial Growth Factor A / Q000096:biosynthesis* / Q000235:genetics
chemical_list: D020533:Angiogenesis Inhibitors; D011753:Pyrones; D042461:Vascular Endothelial Growth Factor A; C088446:pironetin; C509186:TERT protein, human; D019098:Telomerase; D003078:Colchicine
keywords: Antiangiogenesis; Colchicine; Hybrid molecules; Pironetin; Telomerase