Helmholtz National Medical Center of Eye Diseases, Moscow, Russia.
Department of Chemistry, Lomonosov Moscow State University, Moscow, Russia.
Chem Biol Drug Des. 2024 Mar;103(3):e14504. doi: 10.1111/cbdd.14504.
We conducted a study on the impact of intraperitoneal injections of melatonin and its three bioisosteres (compounds 1-3) on the development of oxygen-induced retinopathy in newborn rats during a 21-day experiment. It was demonstrated that melatonin and its analogues 1-3 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 1-3 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 1-3 are comparable to melatonin and can be utilized as potential therapeutic agents for the treatment of retinopathy of prematurity.
我们在一项为期 21 天的实验中研究了腹腔内注射褪黑素及其三种生物等排体（化合物 1-3）对新生大鼠氧诱导性视网膜病变发展的影响。结果表明，褪黑素及其类似物 1-3 可有效降低新生大鼠玻璃体中总蛋白浓度，降低 VEGF-A 浓度，并降低氧化应激水平（通过玻璃体中抗氧化活性的正常化来指示）。褪黑素及其类似物 1-3 同样可使 VEGF-A 水平正常化。类似物 1 和 2 甚至在降低蛋白流入玻璃体方面的能力超过了褪黑素。然而，类似物 2 对抗氧化活性没有影响，而类似物 1 和 3 则导致该参数显著增加，类似物 3 甚至略微超过了褪黑素。因此，可以得出结论，类似物 1-3 与褪黑素相当，可作为治疗早产儿视网膜病变的潜在治疗剂。
