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

doi:10.3390/ph6010054

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Pharmaceuticals 2013, 6(1), 54-69; doi:10.3390/ph6010054

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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^1,* , Erika Fornasari¹, Leonardo Baldassarre¹, Catia Cornacchia¹, Stefania Fulle^2,3, Ester Sara Di Filippo^2,3, Tiziana Pietrangelo^2,3 and Francesco Pinnen¹

¹ Dipartimento di Farmacia, Università degli Studi "G. D'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy ² Dipartimento di Neuroscienze e Imaging; IIM - Istituto Interuniversitario di Miologia Università degli Studi “G. D’Annunzio”, Via dei Vestini 31, 66100 Chieti, Italy ³ Ce.S.I. Centro Studi Invecchiamento, Fondazione d'Annunzio, Via Colle dell'Ara, 66100 Chieti, Italy

* Author to whom correspondence should be addressed.

Received: 6 December 2012; in revised form: 18 December 2012 / Accepted: 31 December 2012 / Published: 7 January 2013

(This article belongs to the Special Issue CNS-Drugs and Therapy)

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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.

Keywords: (R)-alpha-lipoic acid; 8-hydroxyquinoline; neuroprotective agent; antioxidants; neurodegenerative diseases

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MDPI and ACS Style

Cacciatore, I.; Fornasari, E.; Baldassarre, L.; Cornacchia, C.; Fulle, S.; Di Filippo, E.S.; Pietrangelo, T.; Pinnen, F. 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 2013, 6, 54-69.

AMA Style

Cacciatore I, Fornasari E, Baldassarre L, Cornacchia C, Fulle S, Di Filippo ES, Pietrangelo T, Pinnen F. 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. 2013; 6(1):54-69.

Chicago/Turabian Style

Cacciatore, Ivana; Fornasari, Erika; Baldassarre, Leonardo; Cornacchia, Catia; Fulle, Stefania; Di Filippo, Ester S.; Pietrangelo, Tiziana; Pinnen, Francesco. 2013. "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 6, no. 1: 54-69.

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