A Potent (R)-alpha-bis-lipoyl Derivative Containing 8-Hydroxyquinoline Scaffold: Synthesis and Biological Evaluation of Its Neuroprotective Capabilities in SH-SY5Y Human Neuroblastoma Cells

Ivana Cacciatore; Erika Fornasari; Leonardo Baldassarre; Catia Cornacchia; Stefania Fulle; Ester Sara Di Filippo; Tiziana Pietrangelo; Francesco Pinnen

doi:10.3390/ph6010054

A Potent (R)-alpha-bis-lipoyl Derivative Containing 8-Hydroxyquinoline Scaffold: Synthesis and Biological Evaluation of Its Neuroprotective Capabilities in SH-SY5Y Human Neuroblastoma Cells

Pharmaceuticals (Basel). 2013 Jan 7;6(1):54-69. doi: 10.3390/ph6010054.

Authors

Ivana Cacciatore¹, Erika Fornasari, Leonardo Baldassarre, Catia Cornacchia, Stefania Fulle, Ester Sara Di Filippo, Tiziana Pietrangelo, Francesco Pinnen

Affiliation

¹ Dipartimento di Farmacia, Università degli Studi "G. D'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy. cacciatore@unich.it.

Abstract

A novel bis-lipoyl derivative containing 8-hydroxyquinoline scaffold (LA-HQ-LA, 5) was synthesized as a new multifunctional drug candidate with antioxidant, chelant, and neuroprotective properties for the treatment of neurodegenerative diseases. We have investigated the potential effectiveness of LA-HQ-LA against the cytotoxicity induced by 6-OHDA and H2O2 on human neuroblastoma SH-SY5Y cell line. Our outcomes showed that LA-HQ-LA resulted in significant neuroprotective and antioxidant effects against H2O2- and 6-OHDA-induced neurotoxicity in human neuroblastoma SH-SY5Y cells, as assessed by MTT assay. In particular, it showed potent neuroprotective effects against 6-OHDA in RA/PMA differentiated cells at all the tested concentrations.