Polyazamacrocycles are currently being studied and used in a variety of applications beyond their traditional place in supramolecular and coordination chemistry.
This study suggests additional applications of these compounds with particular emphasis on their use as antiproliferative agents that could be potentially used to treat cancer. Four polyazamacrocycles were tested in human prostate cancer LNCaP and prostate epithelial PNTA1 cells to analyze changes in cell proliferation and cell death capabilities. Their intracellular localization was also evaluated by confocal microscopy. The results show a decrease of proliferation rate and cell viability of LNCaP and PNTA1, after treatment with these compounds. The decrease of the number of viable cells is similar for the majority of the compounds studied and at higher concentration, the proliferation efficiency decreased significantly in the cell lines studied. Also, our results suggest that L and L(2) induce early apoptosis in PNTA1 cells and late apoptosis/necrosis in LNCaP cells. The compounds did not induce a significant increase in necrosis of both cell types. Although the compounds did not localize in a unique organelle, all of them have as main target the Golgi apparatus and other localization profiles differed depending on the cell line.
Written by:
Cruz C, Cairrão E, Lourenço O, Almeida P, Verde I, Queiroz JA Are you the author?
CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Av. Infante D. Henrique, 6200-506, Covilhã, Portugal
Reference: Chem Biol Drug Des. 2012 Dec 14(Epub ahead of print)
doi: 10.1111/cbdd.12098
PubMed Abstract
PMID: 23241370
