Retinoprotective Effect of 2-Ethyl-3-hydroxy-6-methylpyridine Nicotinate

Abstract

An important task of pharmacology is to find effective agents to improve retinal microcirculation and resistance to ischemia. The purpose of the study is to pharmacologically evaluate the retinoprotective effect of 2-ethyl-3-hydroxy-6-methylpyridine nicotinate in a rat model of retinal ischemia–reperfusion. A retinal ischemia–reperfusion model was used, in which an increase in intraocular pressure (IOP) to 110 mmHg was carried out within 30 min. The retinoprotective effect of 2-ethyl-3-hydroxy-6-methylpyridine nicotinate at a dose of 3.8 mg/kg, in comparison with nicotinic acid at a dose of 2 mg/kg and emoxipine at a dose of 2 mg/kg, was estimated by the changes in the eye fundus during ophthalmoscopy, the retinal microcirculation level with laser Doppler flowmetry (LDF), and electroretinography (ERG) after 72 h of reperfusion. The use of 2-ethyl-3-hydroxy-6-methylpyridine nicotinate prevented the development of ischemic injuries in the fundus and led to an increase in the retinal microcirculation level to 747 (median) (lower and upper quartiles: 693;760) perfusion units (p = 0.0002) in comparison with the group that underwent no treatment. In the group with the studied substance, the b-wave amplitude increased significantly (p = 0.0022), and the b/a coefficient increased reliably (p = 0.0002) in comparison with the group with no treatment. Thus, 2-ethyl-3-hydroxy-6-methylpyridine nicotinate has established itself as a potential retinoprotector.

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Studies to elucidate the effect and antiapoptotic mechanism of 2-ethyl-3-hydroxy-6- methylpyridine-n-acetyltaurinate in a rat model of retinal ischemia–reperfusion

“…It is widely accepted that I/R injury is caused by the increased generation of reactive oxygen species (ROS) during the process of I/R, including superoxide (O 2 ), hydrogen peroxide (H2O2) and hydroxyl radicals (OH -). The overproduction of ROS can induce apoptosis in the retina [3,4,5]. As a result, inflammation and cell apoptosis are considered to be major causes of the pathological changes following I/R injury.…”

Study to elucidate the pharmacological activity of retinalamin in a rat model of ischemic retinopathy

“…The retinopathy model was created by transiently increasing the IOP to 110 mmHg (Peresypkina et al 2020) by applying mechanical pressure on the anterior chamber of the eye for 30 minutes. Next, a 72-hour reperfusion followed and after that the drugs were administered.…”

“…For between-group comparisons, the Student's t-test for independent groups was used if the distribution of variables was normal; otherwise, the U-test (Mann-Whitney test) was performed. P-values ≤ 0.05 were considered statistically significant (Peresypkina et al 2020).…”