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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Copper(II) complexes with naringenin and hesperetin: cytotoxic activity against A 549 human lung adenocarcinoma cells and investigation on the mode of action

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Tamayo, Lenka V. [1] ; Gouvea, Ligiane R. [1] ; Sousa, Anna C. [1] ; Albuquerque, Ronniel M. [1] ; Teixeira, Sarah Fernandes [2] ; de Azevedo, Ricardo Alexandre [2] ; Louro, Sonia R. W. [3] ; Ferreira, Adilson Kleber [2, 4] ; Beraldo, Heloisa [1]
Total Authors: 9
[1] Univ Fed Minas Gerais, Dept Quim, BR-31270901 Belo Horizonte, MG - Brazil
[2] Univ Sao Paulo, Inst Ciencias Biomed, Dept Imunol, BR-05508900 Sao Paulo, SP - Brazil
[3] Pontificia Univ Catolica Rio De Janeiro, Dept Fis, BR-22653900 Rio De Janeiro, RJ - Brazil
[4] Univ Groningen, Univ Med Ctr Groningen, Dept Med Oncol, Hanzepl 1, NL-9713 Groningen - Netherlands
Total Affiliations: 4
Document type: Journal article
Source: BIOMETALS; v. 29, n. 1, p. 39-52, FEB 2016.
Web of Science Citations: 13

Copper(II) complexes {[}Cu(H (2) O) (2) (L1)(phen)](ClO (4) ) (1) and {[}Cu(H (2) O)(L2)(phen)](ClO (4) ) (2) (HL1 = naringenin; HL2 = hesperetin) were obtained, in which an anionic flavonoid ligand is attached to the metal center along with 1,10-phenanthroline (phen) as co-ligand. Complexes (1) and (2) were assayed for their cytotoxic activity against A549 lung carcinoma and against normal lung fibroblasts (LL-24) and human umbilical vein endothelial cells (HUVEC). We found IC50 = 16.42 A mu M (1) and IC50 = 5.82 A mu M (2) against A549 tumor cells. Complexes (1) and (2) exhibited slight specificity, being more cytotoxic against malignant than against non-malignant cells. 1 and 2 induced apoptosis on A549 cells in a mitochondria-independent pathway, and showed antioxidant activity. The antioxidant effect of the complexes could possibly improve their apoptotic action, most likely by a PI3K-independent reduction of autophagy. Complexes (1) and (2) interact in vitro with calf thymus DNA by an intercalative binding mode. EPR data indicated that 1 and 2 interact with human serum albumin (HSA) forming mixed ligand species. (AU)

FAPESP's process: 13/07273-2 - Rational design and development of new prototypes derived of antitumor phospholipids as potential inhibitors of the enzyme CtP: phosphoethanolamine citidililtransferase and antitumor agents in non-small cell lung cancer
Grantee:Jose Alexandre Marzagão Barbuto
Support type: Regular Research Grants
FAPESP's process: 09/54599-5 - Dendritic cells: integrative elements of the immune system - an applied approach
Grantee:Jose Alexandre Marzagão Barbuto
Support type: Research Projects - Thematic Grants