title: Polyazamacrocycles as potential antitumor agents for human prostate cancer cells.
abstract: Polyazamacrocycles are currently being studied and used in a variety of applications beyond their traditional place in supramolecular and co-ordination 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 in proliferation rate and cell viability of LNCaP and PNTA1, after treatment with these compounds. The decrease in 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 L2 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.
authors.affiliation: CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal. carlacruz@fcsaude.ubi.pt
authors.forename: Carla
authors.initials: C
authors.lastname: Cruz
authors.forename: Elisa
authors.initials: E
authors.lastname: Cairrão
authors.forename: Olga
authors.initials: O
authors.lastname: Lourenço
authors.forename: Paulo
authors.initials: P
authors.lastname: Almeida
authors.forename: Ignacio
authors.initials: I
authors.lastname: Verde
authors.forename: João A
authors.initials: JA
authors.lastname: Queiroz
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D001372:Aza Compounds / Q000737:chemistry*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D047028:Macrocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D008856:Microscopy, Fluorescence; D011471:Prostatic Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D001372:Aza Compounds; D047028:Macrocyclic Compounds