The antidiabetic activity of the new composition “Thigliben” on the experimental dexamethasone diabetes mellitus model in rats

N. Tsubanova, O. H. Berdnyk, Н. А. Цубанова, О. Г. Бердник
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Abstract

Being a metabolic disease with long-term hyperglycemia, diabetes mellitus significantly increases the risk of microvascular and macrovascular diseases and organ pathologies, respectively. The creation of the new composition “Thigliben”, which allows not only qualitatively controlling diabetic hyperglycemia, but also providing a preventive and/or therapeutic effect on the development of diabetic polyneuropathy was pathogenetically reasonable. Aim. To study the antidiabetic activity of “Thigliben” on the experimental dexamethasone diabetes mellitus in rats. Materials and methods. The pharmacological study of the antidiabetic activity of the new composition “Thigliben” in the dose of 4 mg/kg was performed. The experimental studies were conducted on a standard model of the experimental dexamethasone type 2 diabetes mellitus in rats. Glibenclamide in the dose of 0.6 mg/kg (corresponds to an average human daily dose of 10 mg) was selected as the reference drug. Results. It was found that by its effects on the carbohydrate and lipid metabolism the new composition “Thigliben” was similar to the reference drug glibenclamide administered in a higher dose. By the antioxidant activity this composition exceeded the effect of the reference drug, provided that normalization of the TBA-RS level in the liver homogenate was significant. The new composition “Thigliben” normalized all the parameters of the cerebral energy metabolism studied relative to the control pathology group and its efficiency was significantly higher than that of the reference drug glibenclamide. The new composition “Thigliben” increased the content of ATP by 109 % compared to the control pathology group, in contrast to 68 % on the background of glibenclamide; restored the activity of citrate synthase by 65 %, succinate dehydrogenase by 134 %, and pyruvate dehydrogenase by 61 % relative to the control pathology group. For glibenclamide the change in these indicators was 28 %, 50 %, and 22 %, respectively. The results obtained suggest that the metabolic effect of “Thigliben” composition is significantly more effective than that of the reference drug glibenclamide. Conclusions. The new composition “Thigliben” is a promising antidiabetic drug with a pronounced hypolipidemic, antioxidant effect and the ability to restore energy deficiency; it is its significant advantage over the standard treatment regimens, including the average therapeutic doses of glibenclamide.
新组合物“替格利本”对实验性地塞米松糖尿病模型大鼠的降糖活性
糖尿病是一种长期高血糖的代谢性疾病,可显著增加微血管疾病、大血管疾病和器官病变的风险。新组合物“Thigliben”的创造,不仅可以定性地控制糖尿病高血糖,而且还可以对糖尿病多发性神经病变的发展提供预防和/或治疗作用,在病理学上是合理的。的目标。目的:研究蒂格利本对实验性地塞米松型糖尿病大鼠的抗糖尿病作用。材料和方法。对新组合物Thigliben在4 mg/kg剂量下的抗糖尿病活性进行了药理学研究。实验研究采用地塞米松2型糖尿病大鼠标准模型。选择剂量为0.6 mg/kg(相当于人平均日剂量10 mg)的格列本脲作为对照药物。结果。通过对碳水化合物和脂质代谢的影响发现,新组合物“Thigliben”与对照药物格列本脲类似,但剂量更高。在肝脏匀浆中TBA-RS水平显著正常化的条件下,该成分的抗氧化活性超过了参比药的作用。新组合物“Thigliben”相对于对照病理组的脑能代谢指标均归一化,其效率显著高于对照药物格列本脲。与对照病理组相比,新组合物“Thigliben”使ATP含量增加了109%,而格列本脲背景组的ATP含量为68%;与对照组相比,恢复了65%的柠檬酸合成酶、134%的琥珀酸脱氢酶和61%的丙酮酸脱氢酶的活性。对于格列本脲,这些指标的变化分别为28%,50%和22%。结果表明,“Thigliben”组合物的代谢作用明显优于对照药物格列本脲。结论。新组合物“Thigliben”是一种很有前途的降糖药物,具有显著的降血脂、抗氧化作用和恢复能量不足的能力;与标准治疗方案(包括格列苯脲的平均治疗剂量)相比,这是它的显著优势。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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