Melatonin and its bioisosteres as potential therapeutic agents for the treatment of retinopathy of prematurity

Author:

Osipova N. A.1,Panova A. Y.1,Efremov A. M.2,Lozinskaya N. A.2,Beznos O. V.1,Katargina L. A.1

Affiliation:

1. Helmholtz National Medical Center of Eye Diseases Moscow Russia

2. Department of Chemistry Lomonosov Moscow State University Moscow Russia

Abstract

AbstractWe conducted a study on the impact of intraperitoneal injections of melatonin and its three bioisosteres (compounds 13) on the development of oxygen‐induced retinopathy in newborn rats during a 21‐day experiment. It was demonstrated that melatonin and its analogues 13 effectively reduce the total protein concentration in the vitreous body of rat pups, decrease concentration of VEGF‐A, and lower the level of oxidative stress (as indicated by normalization of antioxidant activity in the vitreous body). Melatonin and its analogues 13 equally normalize the level of VEGF‐A. Analogues 1 and 2 even exceed melatonin in their ability to reduce protein influx into the vitreous body. However, analogue 2 had no effect on antioxidant activity, while analogues 1 and 3 caused a significant increase in this parameter, with analogue 3 even slightly exceeding melatonin. Thus, it can be concluded that analogues 13 are comparable to melatonin and can be utilized as potential therapeutic agents for the treatment of retinopathy of prematurity.

Funder

Russian Science Foundation

Publisher

Wiley

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