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Title: Synthesis and Characterization of a New Bivalent Ligand Combining Caffeine and Docosahexaenoic Acid
Author: Fernández Dueñas, Víctor
Azuaje, Jhonny
Morató Arús, Xavier
Cordobilla, Begoña
Domingo, Pere (Domingo Pedrol)
Sotelo, Eddy
Ciruela Alférez, Francisco
Keywords: Malalties neurodegeneratives
Neurodegenerative diseases
Issue Date: 27-Feb-2017
Publisher: MDPI
Abstract: Caffeine is a promising drug for the management of neurodegenerative diseases such as Parkinson's disease (PD), demonstrating neuroprotective properties that have been attributed to its interaction with the basal ganglia adenosine A2A receptor (A2AR). However, the doses needed to exert these neuroprotective effects may be too high. Thus, it is important to design novel approaches that selectively deliver this natural compound to the desired target. Docosahexaenoic acid (DHA) is the major omega-3 fatty acid in the brain and can act as a specific carrier of caffeine. Furthermore, DHA displays properties that may lead to its use as a neuroprotective agent. In the present study, we constructed a novel bivalent ligand covalently linking caffeine and DHA and assessed its pharmacological activity and safety profile in a simple cellular model. Interestingly, the new bivalent ligand presented higher potency as an A2AR inverse agonist than caffeine alone. We also determined the range of concentrations inducing toxicity both in a heterologous system and in primary striatal cultures. The novel strategy presented here of attaching DHA to caffeine may enable increased effects of the drug at desired sites, which could be of interest for the treatment of PD.
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It is part of: Molecules, 2017, vol. 22, num. 366
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ISSN: 1420-3049
Appears in Collections:Articles publicats en revistes (Bioquímica i Biomedicina Molecular)
Articles publicats en revistes (Institut de Neurociències (UBNeuro))
Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL))
Articles publicats en revistes (Patologia i Terapèutica Experimental)

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