Exploring cinnamic acid scaffold: development of promising neuroprotective lipophilic antioxidants

• Tipo: Artigo em Revista Científica Internacional
• Data: 2015

Autores

Daniel Chavarria (Autor) Outra; Tiago Silva (Autor) Outra; Daniel Martins (Autor) Outra; Joana Bravo (Autor) Outra; Teresa Summavielle (Autor) Outra; Jorge Garrido (Autor) Outra; Fernanda Borges (Autor) FCUP

Revista

Título: MedChemComm

Vol. 6

ISSN: 2040-2503

Editora: Royal Society of Chemistry

Indexação

ISI Web of Knowledge - 22 Citações

Scopus - 23 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina básica

CORDIS: Ciências Físicas > Química

Outras Informações

ID Authenticus: P-00G-BT2

Abstract (EN): New lipophilic hydroxycinnamic acid based derivatives were designed and synthesized and their antioxidant and neuroprotective activities evaluated. The chemical modification introduced in the cinnamic acid scaffold leads to compounds with amplified lipophilicity and in general with increased antioxidant activity when compared to natural models (caffeic and ferulic acids). The compounds did not display cytotoxicity and present a significant neuroprotective effect against 6-OH-DA induced damage to SH-SY5Y cells. Compound 6 stands out as an efficient radical scavenger and iron(II) chelator that ensures drug-like properties. Moreover, neuroprotection against oxidative damage was observed even at low concentration (1 mu M). Therefore, compound 6 developed by a biology-oriented approach displays a combination of important features for a further optimization process that will generate a new effective antioxidant with therapeutic application for oxidative-stress-related events, namely neurodegenerative diseases.

Idioma: Inglês

Tipo (Avaliação Docente): Científica