Introduction The omega 3 polyunsaturated fatty acid (PUFAs) formulation containing eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) with a 6:1 ratio is a potent inducer of endothelium-dependent nitric oxide (NO)-mediated vasorelaxation that also improves ageing-related and angiotensin II-induced endothelial dysfunction in rats. Purpose Since PUFAs are unstable, the possibility that nanoencapsulation of EPA:DHA 6:1 followed by coating potentiates the bioactivity was evaluated. Methods EPA:DHA 6:1 was emulsified in water phase and coated with proteins and gum derivatives or used in native form. Changes in isometric tension of porcine coronary artery rings were determined using organ chambers. The role of NO was assessed using Nw-nitro-L-arginine (L-NA, NO synthase inhibitor), prostanoids using indomethacin (Indo, COX inhibitor) and endothelium-derived hyperpolarization (EDH) using TRAM-34 and UCL-1684 (Ca2 + -dependent potassium channel inhibitors). Results Coated EPA:DHA 6:1 nanoparticles (NP) caused in a concentration-dependent manner endothelium-dependent relaxations that were more sustained than those of the native form. At 0.3%, coated and native forms induced 56.6 ± 2.8% and 51.1 ± 1.5%relaxations at 10 min, and 93.8 ± 2.1% and 35.1 ± 1.7% at 60 min, respectively. The response to the coated EPA:DHA 6:1 NP was inhibited by L-NA and not affected by Indo, TRAM-34 plus UCL-1684, and by the previous incubation of rings with another oil (corn oil 0.3%). In contrast, L-NA, Indo, and TRAM-34 plus UCL-1684 inhibited the relaxation to EPA:DHA 6:1. Conclusion Nanoencapsulation of EPA:DHA 6:1 followed by coating perpetuated their ability to cause endothelium-dependent relaxation of coronary artery rings that is exclusively mediated by NO. In contrast, the relaxing activity of the native form involved NO, EDH and vasorelaxant prostanoids. Therefore, coated EPA:DHA 6:1 NP appear to be an attractive approach to enhance the vasoprotective effect of omega 3 PUFAs.
Nanoencapsulation of EPA:DHA 6:1 potentiates the endothelium-dependent relaxation of coronary artery rings compared to native form: role of NO, endothelium-dependent hyperpolarization and prostanoids
Belcastro, E.;
2020-01-01
Abstract
Introduction The omega 3 polyunsaturated fatty acid (PUFAs) formulation containing eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) with a 6:1 ratio is a potent inducer of endothelium-dependent nitric oxide (NO)-mediated vasorelaxation that also improves ageing-related and angiotensin II-induced endothelial dysfunction in rats. Purpose Since PUFAs are unstable, the possibility that nanoencapsulation of EPA:DHA 6:1 followed by coating potentiates the bioactivity was evaluated. Methods EPA:DHA 6:1 was emulsified in water phase and coated with proteins and gum derivatives or used in native form. Changes in isometric tension of porcine coronary artery rings were determined using organ chambers. The role of NO was assessed using Nw-nitro-L-arginine (L-NA, NO synthase inhibitor), prostanoids using indomethacin (Indo, COX inhibitor) and endothelium-derived hyperpolarization (EDH) using TRAM-34 and UCL-1684 (Ca2 + -dependent potassium channel inhibitors). Results Coated EPA:DHA 6:1 nanoparticles (NP) caused in a concentration-dependent manner endothelium-dependent relaxations that were more sustained than those of the native form. At 0.3%, coated and native forms induced 56.6 ± 2.8% and 51.1 ± 1.5%relaxations at 10 min, and 93.8 ± 2.1% and 35.1 ± 1.7% at 60 min, respectively. The response to the coated EPA:DHA 6:1 NP was inhibited by L-NA and not affected by Indo, TRAM-34 plus UCL-1684, and by the previous incubation of rings with another oil (corn oil 0.3%). In contrast, L-NA, Indo, and TRAM-34 plus UCL-1684 inhibited the relaxation to EPA:DHA 6:1. Conclusion Nanoencapsulation of EPA:DHA 6:1 followed by coating perpetuated their ability to cause endothelium-dependent relaxation of coronary artery rings that is exclusively mediated by NO. In contrast, the relaxing activity of the native form involved NO, EDH and vasorelaxant prostanoids. Therefore, coated EPA:DHA 6:1 NP appear to be an attractive approach to enhance the vasoprotective effect of omega 3 PUFAs.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
