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Ann Pharm Fr ; 77(6): 488-495, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31563266

RESUMO

Nanodiamonds (NDs) are emerging delivery systems with biomedical applications and interesting perspectives in oncology. Their use has been proposed to assist the internalization of anticancer drugs and to decrease administered drug doses. The pro-apoptotic peptide ERα17p, which is issued from the hinge/N-terminus parts of the AF2 region of the human estrogen receptor α (ERα), is active at a concentration of 10µM on breast cancer cells and particularly on those cancer cells that are ERα-positive. We have synthesized ND@ERα17p conjugates by physisorption of the cationic peptide ERα17p on the surface of anionic NDs. Resulting ND@ERα17p suspensions were characterized by far-UV electronic circular dichroism (ECD), dynamic light scattering (DLS) and zetametry. We then tested the anti-proliferative action of ND@ERα17p on ERα-positive MCF-7 breast carcinoma cells. ND@ERα17p allowed a decrease of the active concentration to 0.1nM (ND@ERα17p), revealing unambiguously that NDs could be used to improve the anti-proliferative action of this peptide. This preliminary study proposes a novel approach for enhancing the apoptotic action displayed by ERα17p, in the context of breast cancer.


Assuntos
Adenocarcinoma/patologia , Neoplasias da Mama/patologia , Nanoconjugados , Nanodiamantes , Fragmentos de Peptídeos/farmacologia , Sequência de Aminoácidos , Apoptose/efeitos dos fármacos , Divisão Celular/efeitos dos fármacos , Dicroísmo Circular , Portadores de Fármacos , Desenho de Fármacos , Difusão Dinâmica da Luz , Receptor alfa de Estrogênio/química , Feminino , Humanos , Células MCF-7 , Microscopia Eletrônica , Fragmentos de Peptídeos/química , Eletricidade Estática
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