Free Radical Biology and Medicine p. 367 - 382 (2021)
Update date:2022-08-15
Topics:
Moine, Espérance
Boukhallat, Manel
Cia, David
Jacquemot, Nathalie
Guillou, Laurent
Durand, Thierry
Vercauteren, Joseph
Brabet, Philippe
Crauste, Céline
Dry age-related macular degeneration and Stargardt disease undergo a known toxic mechanism caused by carbonyl and oxidative stresses (COS). This is responsible for accumulation in the retinal pigment epithelium (RPE) of A2E, a main toxic pyridinium bis-retinoid lipofuscin component. Previous studies have shown that carbonyl stress in retinal cells could be reduced by an alkyl-phloroglucinol-DHA conjugate (lipophenol). Here, we performed a rational design of different families of lipophenols to conserve anti-carbonyl stress activities and improve antioxidant properties. Five synthetic pathways leading to alkyl-(poly)phenol derivatives, with phloroglucinol, resveratrol, catechin and quercetin as the main backbone, linked to poly-unsaturated fatty acid, are presented. These lipophenols were evaluated in ARPE-19 cell line for their anti-COS properties and a structure-activity relationship study is proposed. Protection of ARPE-19 cells against A2E toxicity was assessed for the four best candidates. Finally, interesting anti-COS properties of the most promising quercetin lipophenol were confirmed in primary RPE cells.
View MoreShanghai Standard Biotech Co., Ltd.
Contact:+86-18502101150
Address:Room 103, Building 2nd, NO.720, Cailun Road , Pudong District, Shanghai, China
Contact:+86-29-88710656
Address:South Tai bai Road, High Tech Development Zone, Xi'an China
Contact:+86+21-58956006 15800617331
Address:402 Room, 150# Cailun Road, Zhangjiang high tech park, Shanghai
Shandong Xinke Petrochemical Co., Ltd.
Contact:+86-546-7277016
Address:Gudao Industrial Park, Hekou District, Dongying, Shandong Province, China
Shandong united-rising pharmaceutical cooperation.,ltd.
Contact:008653187965009
Address:171No., Jing5 Road, Shizhong District, Jinan, China
Doi:10.1080/10426500903567547
(2010)Doi:10.1080/10426500214894
(2002)Doi:10.1039/c0ob00357c
(2010)Doi:10.1016/j.ica.2010.08.039
(2010)Doi:10.1016/j.ejmech.2014.04.005
(2014)Doi:10.1016/S0040-4039(00)99290-6
(1989)