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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Letter Article

Synthesis, Characterization and Evaluation of Gemfibrozil-Stilbene Hybrid as Antioxidant Agent

Author(s): Rosa Amoroso, Lidia Leporini, Ivana Cacciatore, Lisa Marinelli, Alessandra Ammazzalorso, Isabella Bruno, Barbara De Filippis, Marialuigia Fantacuzzi, Cristina Maccallini, Luigi Menghini, Antonio Di Stefano and Letizia Giampietro*

Volume 15 , Issue 11 , 2018

Page: [1230 - 1238] Pages: 9

DOI: 10.2174/1570180815666180321163246

Price: $65

Abstract

Background: Oxidative stress and inflammation are important processes involved in cardiovascular disease. Antioxidant agents, like drugs or natural products from plants or plant-based food, represent a promising approach to treat these pathologies.

Methods: In light of this, a gemfibrozil-stilbene hybrid (GEM-STIL) was synthesized as a strategy to combine the well-known antioxidant activity of stilbenes with the reported antioxidant and antiinflammatory actions of fibrates such as gemfibrozil. The physicochemical properties, including aqueous solubility, partition coefficient, chemical stability and enzymatic hydrolysis of GEM-STIL have been studied and indicated that it is stable and has a good lipophilicity. The biological activity was also evaluated for its effect on C2C12 cell line viability and antioxidant activities.

Results: The results indicated that GEM-STIL was well tolerated and induced a reduction of cell viability only at higher concentration (100 µg/ml). On the other hand, also at lower nontoxic concentrations (5, 25 and 50 µg/ml) exhibited a significant reduction of ROS production as well as a protective effect against the induced oxidative stimulus.

Conclusion: These findings suggest that GEM-STIL is a potential new antioxidant agent useful in oxidative stress-related pathologies.

Keywords: Gemfibrozil, 4-hydroxystilbene, antioxidant, ROS, plasma stability, hybrid.

Graphical Abstract

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