An Erlotinib gold(I) conjugate for combating triple-negative breast cancer.
J Inorg Biochem
; 203: 110910, 2020 02.
Article
em En
| MEDLINE
| ID: mdl-31683128
ABSTRACT
An Erlotinib triphenylphosphane gold(I) conjugate has been prepared from AuCl(PPh3) and its crystal structure has been established by X-ray diffraction, showing a metallo-helicate formation. IC50 values of the new gold conjugate were calculated towards a panel of human tumor cell lines representative of breast (MCF-7, MDA-MB-231) and colon (HT-29) cancer cells. Overall, the gold conjugate exhibited higher cytotoxic activity than that of Erlotinib against the cancer cells studied. Particularly, the antiproliferative effect of the conjugate demonstrated to be 68-fold higher than Erlotinib in highly metastatic and triple negative MDA-MB-231 cell line. The gold conjugate caused DNA damage, reactive oxygen species (ROS) increase and induced apoptosis. Flow cytometry analysis showed that the conjugate induces significant arrest in S and G2/M phases primarily, whereas Erlotinib, as an inhibitor of epidermal growth factor receptor (EGFR), blocks G1/S transition and increases G1 cell population.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Organoáuricos
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Neoplasias de Mama Triplo Negativas
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Cloridrato de Erlotinib
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article