title: Cytotoxic and apoptotic effects of chalcone derivatives of 2-acetyl thiophene on human colon adenocarcinoma cells.
abstract: Recent studies report that chalcones exhibit cytotoxicity to human cancer cell lines. Typically, the form of cell death induced by these compounds is apoptosis. In the context of the discovery of new anticancer agents and in light of the antitumour potential of several chalcone derivatives, in the present study, we synthesized and tested the cytotoxicity of six chalcone derivatives on human colon adenocarcinoma cells. Six derivatives of 3-phenyl-1-(thiophen-2-yl) prop-2-en-1-one were prepared and characterized on the basis of their (1) H and (13) C NMR spectra. HT-29 cells were treated with synthesized chalcones on two concentrations by three different incubation times. Cells were evaluated by cell morphology, Tetrazolium dye (MTT) colorimetric assay, live/dead, flow cytometry (annexin V) and gene expression analyses to determine the cytotoxic way. Chalcones 3-(4-bromophenyl)-1-(thiophen-2-yl)prop-2-en-1-one (C06) and 3-(2-nitrophenyl)-1-(thiophen-2-yl)prop-2-en-1-one (C09) demonstrated higher cytotoxicity than other chalcones as shown by cell morphology, live/dead and MTT assays. In addition, C06 induced apoptosis on flow cytometry annexin V assay. These data were confirmed by a decreased expression of anti-apoptotic genes and increased pro-apoptotic genes. Our findings indicate in summary that the cytotoxic activity of chalcone C06 on colorectal carcinoma cells occurs by apoptosis.
authors.affiliation: Programa de Pós-Graduação em Química, UFPel, Campus Universitário de Capão do Leão, Pelotas, RS, Brazil.
authors.forename: Alana
authors.initials: A
authors.lastname: de Vasconcelos
authors.forename: Vinicius Farias
authors.initials: VF
authors.lastname: Campos
authors.forename: Fernanda
authors.initials: F
authors.lastname: Nedel
authors.forename: Fabiana Kömmling
authors.initials: FK
authors.lastname: Seixas
authors.forename: Odir A
authors.initials: OA
authors.lastname: Dellagostin
authors.forename: Kevin R
authors.initials: KR
authors.lastname: Smith
authors.forename: Cláudio Martin Pereira
authors.initials: CM
authors.lastname: de Pereira
authors.forename: Francieli Moro
authors.initials: FM
authors.lastname: Stefanello
authors.forename: Tiago
authors.initials: T
authors.lastname: Collares
authors.forename: Alethéa Gatto
authors.initials: AG
authors.lastname: Barschak
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy / Q000235:genetics / Q000378:metabolism / Q000503:physiopathology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects*; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000235:genetics / Q000378:metabolism / Q000503:physiopathology*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D019073:HT29 Cells; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D002599:Chalcone