一种新的丙酸双药效团衍生物的抗炎活性研究

V. S. Slyusarenko, M. Korokin, S. Kovalenko, Aleksandr N. Stadnichenko, L. Korokina
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引用次数: 1

摘要

本实验动物研究的目的是在模拟急性和慢性炎症反应时,新的双药效团衍生物德布洛芬和纳布西坦的抗炎活性。所研究的以德西布洛芬和纳布西坦为基础的双药效团化合物,其化学式为(2S) - n-((1-苄基-5-羟基吡咯烷-3-基)甲基)-2-(4-异丁基苯基)丙酰胺。德昔布以80 mg/kg的剂量灌胃给药;德西布洛芬和纳布西坦以40 mg/kg的剂量灌胃。脚掌水肿的最小增加记录是在用地外筋治疗的动物组。为初始值的33.61±7.41,低于对照组和单药治疗组,差异有统计学意义(p <0.05)。与对照组相比,使用德昔布可减少肉芽肿干重增加43.09% (p <0.05)。在本研究中,在研究急性和慢性炎症模型的抗炎作用的严重程度时,我们发现不同治疗方向的分子片段具有积极的药效学相互作用,结合在一种创新的双药效团化合物中,实验室名称为dexibuneb。在将卡拉胶引入足底腱膜后,对足跖水肿的抑制作用以及植入大鼠腋窝的肉芽肿肿块的增加,在使用地西布洛芬和纳布西坦单药治疗的动物组中具有统计学意义。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Anti-Inflammatory Activity of a New Dipharmacophore Derivative of Propionic Acid
This experimental laboratory animals research aimed at the anti-inflammatory activity of a new dipharmacophore derivative dexibuprofen and nebracetam when modeling an acute and chronic inflammatory reaction. The studied dipharmacophore compound based on dexibuprofen and nebracetam is indicated by the dexibuneb laboratory code and has the chemical formula (2S) -N - ((1-benzyl-5-hydroxypyrrolidin-3-yl) methyl) -2- (4-isobutylphenyl) propanamide. Dexibuneb was administered intragastrically at a dose of 80 mg/kg; dexibuprofen and nebracetam were administered intragastrically at a dose of 40 mg/kg. The minimum increase in paw edema was recorded in the group of animals treated with dexibuneb. It amounted to 33.61 ± 7.41 of the initial value, which is statistically significantly (p <0.05) less than the values both in the control group and in the groups treated with dexibuprofen nebracetam monotherapy. The use of dexibuneb reduced the increase in dry weight of the granuloma by 43.09% (p <0.05) relative to the increase in the control group. In this study, when studying the severity of the anti-inflammatory effect on acute and chronic inflammation models, we found a positive pharmacodynamic interaction of molecular fragments of various therapeutic orientations, combined in an innovative dipharmacophore compound with the laboratory name dexibuneb. Inhibition of paw edema after introducing carrageenan into the plantar aponeurosis and the increase in the mass of granulomas implanted in rat armpits was statistically significantly more pronounced in the groups of animals treated with dexibuneb than with dexibuprofen and nebracetam monotherapy.
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