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 anti-inflammatory 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 mu g/ml). On the other hand, also at lower nontoxic concentrations (5, 25 and 50 mu g/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.

Synthesis, characterization and evaluation of gemfibrozil-stilbene hybrid as antioxidant agent

Amoroso, Rosa;Leporini, Lidia;Cacciatore, Ivana;Marinelli, Lisa;Ammazzalorso, Alessandra;Bruno, Isabella;De Filippis, Barbara;Fantacuzzi, Marialuigia;Maccallini, Cristina;Menghini, Luigi;Di Stefano, Antonio;Giampietro, Letizia
2018

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 anti-inflammatory 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 mu g/ml). On the other hand, also at lower nontoxic concentrations (5, 25 and 50 mu g/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.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11564/700861
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