目的合成四氢苯并噻吩-3-羧酰胺亚甲胺衍生物对健康大鼠及实验性高脂血症条件下脂质代谢指标的影响

Skulte I.V., Luzhnova S.A., K. I.P., Zhilina O.M., Kharitonova O.V., Sigareva S.S.
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引用次数: 0

摘要

根据世卫组织的数据,无论是在俄罗斯还是在其他国家,心血管疾病在人口中所占比例方面都处于领先地位。这些病变发生的先决条件是动脉粥样硬化。现在认识到,药物治疗在抑制动脉粥样硬化及其并发症的发展方面处于领先地位。在这方面,寻找新的降脂药物治疗这种疾病的紧迫性正在增加。近年来的研究表明,利用苯并噻吩骨架具有多种生物学和药理活性,可以在其基础上获得有效的抗菌、抗癌、抗炎、抗氧化、抗结核、抗糖尿病、抗惊厥等药物,有望用于合成新的有效药物。本研究的目的是研究亚甲胺衍生物2-氨基-4,5,6,7-四氢-1-苯并噻吩-3-羧酰胺(实验室代码BF-10)对健康大鼠和实验性高脂血症病理状态下脂质代谢指标的降脂作用。选择阿托伐他汀作为对照药物。在Dixion Torus 120分析仪上使用标准Olvex诊断试剂盒,采用统一的生化方法测定血清和肝脏匀浆中脂质代谢生化参数(胆固醇、甘油三酯、总脂、LDL、VLDL和HDL含量)。通过对所获得的BF-10物质对脂质代谢影响的数据分析,可以得出与高效参比药物阿托伐他汀的作用相当的结论,这使我们可以扩大对亚甲胺衍生物生物活性谱的信息,并认为实验室代码为BF-10的化合物有进一步开发的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
INFLUENCE OF PURPOSEFULLY SYNTHESIZED AZOMETHINE DERIVATIVE OF TETRAHYDROBENZOTHIOPHENE-3-CARBOXAMIDE ON SOME INDICATORS OF LIPID METABOLISM IN HEALTHY RATS AND UNDER CONDITIONS OF EXPERIMENTAL HYPERLIPIDEMIA
According to WHO data, cardiovascular diseases occupy a leading position in terms of the number per share of the population, both in Russia and in other countries. A prerequisite for the development of these pathologies is atherosclerosis. It is now recognized that drug therapy is leading in curbing the development of atherosclerosis and subsequent complications. In this regard, the urgency of the search for new lipid-lowering drugs aimed at the treatment of this disease is increasing. Recent studies have shown the promise of using the benzothiophene backbone for the synthesis of new effective drugs, since this core has various biological and pharmacological activities, which makes it possible to obtain effective antimicrobial, anticancer, anti-inflammatory, antioxidant, anti-tuberculosis, antidiabetic, anticonvulsant and other drugs on its basis.The purpose of this study was to study the lipid-lowering effect of the azomethine derivative 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, a substance under the laboratory code BF-10, on some indicators of lipid metabolism in healthy rats and under pathological conditions with experimental hyperlipidemia. Atorvastatin was chosen as the reference drug. Determination of biochemical parameters of lipid metabolism in the blood serum and in the liver homogenate (the content of cholesterol, triglycerides, total lipids, LDL, VLDL and HDL) was determined by unified biochemical methods using standard Olvex Diagnosticum kits on a Dixion Torus 120 analyzer. Based on the analysis of the obtained data on the effect of the BF-10 substance on lipid metabolism, it can be concluded that they are comparable with the action of the highly effective reference drug atorvastatin, which allows us to expand information on the spectrum of biological activity of azomethine derivatives and consider the compound under the laboratory code BF-10 promising for further development.
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