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Melatonin and its bioisosteres as potential therapeutic agents for the treatment of retinopathy of prematurity
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2024-03-14 , DOI: 10.1111/cbdd.14504
N. A. Osipova 1 , A. Y. Panova 1 , A. M. Efremov 2 , N. A. Lozinskaya 2 , O. V. Beznos 1 , L. A. Katargina 1
Affiliation  

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.

中文翻译:

褪黑素及其生物等排体作为治疗早产儿视网膜病的潜在治疗剂

我们进行了一项为期 21 天的实验,研究腹腔注射褪黑激素及其三种生物等排体(化合物 1-3)对新生大鼠氧诱导视网膜病变的影响。结果表明,褪黑素及其类似物1-3可有效降低幼鼠玻璃体中的总蛋白浓度,降低VEGF-A的浓度,并降低氧化应激水平(玻璃体中抗氧化活性的正常化表明)身体)。褪黑素及其类似物 1-3 同样可以使 VEGF-A 水平正常化。类似物 1 和 2 减少蛋白质流入玻璃体的能力甚至超过了褪黑激素。然而,类似物2对抗氧化活性没有影响,而类似物1和3则导致该参数显着增加,其中类似物3甚至略微超过褪黑激素。因此,可以得出结论,类似物1-3与褪黑激素相当,可以用作治疗早产儿视网膜病的潜在治疗剂。
更新日期:2024-03-14
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