RESUMO
Flaxseed orbitides (linusorbs) are a family of N to C linked bioactive cyclic octa-, nona-, and decapeptides present in flaxseed oil. They are highly hydrophobic and thermally stable. Our previous studies showed that [1-9-NαC]-linusorb B3 (LOB3) and [1-9-NαC]-linusorb B2 (LOB2) exhibited cytotoxic effects towards human breast cancer HER2-subtype Sk-Br-3 cells at a concentration of ~400 µM. However, this high concentration significantly limits their potential clinical applications. In the current study, we developed a novel polyethylene glycol-based formulation for linusorbs and showed that both LOB3 and LOB2, especially LOB3, exhibited strong cytotoxicity towards human breast cancer triple-negative-subtype MDA-MB-231 cells at low nanomolar concentrations.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Linho/química , Peptídeos Cíclicos/farmacologia , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/isolamento & purificação , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Feminino , Humanos , Peptídeos Cíclicos/administração & dosagem , Peptídeos Cíclicos/isolamento & purificação , Polietilenoglicóis/química , Sementes , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Neoplasias de Mama Triplo Negativas/patologiaRESUMO
[This corrects the article DOI: 10.1039/C6RA05154E.].