1. Moscow State University of Technologies and Management, Moscow, Russia 2. IBMC - EcoBioPharm LLC, Moscow, Russia 3. Institute of Biomedical Chemistry, Moscow, Russia 4. Kursk State Medical University, Kursk, Russia
Abstract: The effects of natural polyphenols, resveratrol (RES) and dihydroquercetin (DHQ), included in phospholipid nanoparticles, have been compared with free substances of RES and DHQ in in vitro and in vivo experiments. Preincubation of healthy donor plasma low density lipoproteins (LDL) with RES or DHQ included in phospholipid nanoparticles caused a more pronounced decrease in Cu2+ induced lipid oxidation compared with the free substances, and reduced the formation of lipid peroxides products. Bioavailabilities of RES and DHQ in phospholipid formulations after oral administration in rats were increased by 1.5-2 times. In an acute hypoxia model in mice prophylactic two-week administration of RES or DHQ phospholipid formulations resulted in 25% increase in survival and 1.5-fold increase in catalase activity in brain homogenates compared to free substances. Using the model of endothelial dysfunction in rats induced by L-NAME it was shown, that RES markedly attenuated the inhibition effect of L-NAME on NO synthesis. RES in phospholipid nanoparticles had the same action at a dose 10 times lower compared to free RES. Load test with resistance (clamping of the ascending aorta for 30 sec) showed that phospholipid formulation of RES possessed more pronounced protective effect due to the stimulation of endothelial NO-synthase.
Reference: Guseva D.A., Khudoklinova Yu.Yu., Medvedeva N.V., Baranova V.S., Zakharova T.S., Artyushkova E.B., Torkhovskaya T.I., Ipatova O.M., Influence of resveratrol and dihydroquercetin inclusion into phospholipid nanopatricles on their bioavailability and specific activity, Biomeditsinskaya khimiya, 2015, vol:
2. Vang O., Ahmad N., Baile C.A., Baur J.A., Brown K., Criszar A., Das D.K., Delmas D., Gottfried C., Lin H.Y., Ma O.Y., Mukhopadhyay P., Nalini J.M. et al. (2011) PLoS One, 6(6), e18881, 1-11. Scholar google search
8. Potenza M.A., Marasciulo F.L., Tarquinio M., Tiravanti E., Colantuono G., Federici A., Kim J.A., Quon M.J., Montagnani M. (2007) Am. J. Physiol. Endocrinol. Metab., 292(5), E1378-13287. CrossRef Scholar google search
13. Neves A.R., Lucio M., Lima J.L., Reis S. (2012) Curr. Med. Chem., 19(11), 1663-1668. Scholar google search
14. Ipatova O.M., Torkhovskaya T.I., Medvedeva N.V., Prozorovskiy V.N., Ivanova N.D., Shironin A.V., Baranova V.S., Archakov A.I., Bioavailability of oral drug formulations and methods for its improvement, Biomeditsinskaya khimiya, 2010, vol: 56(1), 101-119. CrossRef Scholar google search
15. Shironin A.V., Ipatova O.M., Medvedeva N.V., Prozorovskiy V.N., Tikhonova E.G., Zakharova T.S., Sanzhakov M.A., Torkhovskaya T.I., The increase of bioavailability and antiinflammatory effect of indomethacin included into phospholipid nanoparticles, Biomeditsinskaya khimiya, 2011, vol: 57(6), 671-676. CrossRef Scholar google search