尼美舒利和一种新的4-噻唑烷酮衍生物对实验性炎症过程中血液学参数的影响

T. Rumynska
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摘要

这项工作的目的是鉴定一种新合成的4-噻唑烷酮类药物的抗炎作用。因此,我们对Les6490和非甾体抗炎药尼美舒利两种药物的疗效进行了比较研究。该药属于非甾体类抗炎药(NSAIDs),具有明显的抗炎、镇痛和解热作用。尼美舒利属于环加氧酶及其同工酶(COX-2)的高选择性抑制剂,用于治疗肌肉骨骼系统的各种病理。新合成的化合物Les6490属于4-噻唑烷酮衍生物族。噻唑烷酮环是许多现有潜在的抗菌和抗炎药物的一部分,并且可以与具有相同结构的药效团吡唑片段联合使用,并有助于提高治疗效果。研究了大鼠在相关炎症过程的实验复制过程中血液学变化的特点,使用弗洛伊德辅助模型进行了研究。通过对这两种药物的血液学指标进行抗炎活性研究,新合成的4-噻唑烷酮衍生物和非甾体抗炎药尼美舒利的抗炎活性得以揭示,其抗炎活性可与药物Les6490的微弱优势相媲美。同时,在不影响红细胞数量水平的情况下,在炎症过程条件下,尼美舒利和Les6490引起红细胞总数明显增加。未发现对红细胞数量有影响。白细胞分子式的分析表明,4-噻唑烷酮类的Les6490的活性在某种程度上比尼美舒利的活性更明显。在af诱导的炎症过程中,白细胞配方的变化最明显的是中性粒细胞:研究物质Les6490的作用比尼美舒利的作用更明显。新化合物Les6490的引入部分引起了单核细胞的正常化,在af相关炎症过程条件下,未观察到明显变化。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The effect of the nimesulide and a new 4-thiazolidinone derivative on hematological parameters in the conditions of an experimental inflammatory process
The aim of the work was to identify the anti-inflammatory effect of a newly synthesized drug from the group of 4-thiazolidinones. Thus, a comparative study of the effect of two agents was conducted: the drug Les6490 and the non-steroidal anti-inflammatory drug nimesulide. This drug belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs), which have pronounced anti-inflammatory, analgesic and antipyretic effects. Nimesulide belongs to highly selective inhibitors of cyclooxygenase and its isoenzymes (COX-2) and is used for treatment in various pathologies of the musculoskeletal system. The newly synthesized compound Les6490 belongs to the group of 4-thiazolidinone derivatives. The thiazolidinone ring is part of many existing potential antibacterial and anti-inflammatory agents, and can be combined with pyrazole fragments, which are pharmacophores of the same structure, and can contribute to increased therapeutic efficacy. The study of the peculiarities of hematological changes in rats during the experimental reproduction of the associated inflammatory process using the Freund’s adjuvant model has been conducted. As a result of the study of anti-inflammatory activity based on hematological indicators of the drugs — a new synthesized derivative of 4-thiazolidinones and a nonsteroidal anti-inflammatory drug nimesulide — their anti-inflammatory activity was revealed, which can be considered comparable to the slight advantage of the drug Les6490. At the same time, without affecting the quantitative level of erythrocytes with isolated administration, under the conditions of the inflammatory process, nimesulide and Les6490 caused a significant increase in the total number of erythrocytes. No effect on the amount of erythrocytes was found. The analysis of leukocyte formula suggests the evidence that the activity of Les6490 from the group of 4-thiazolidinones is to some extent more pronounced than the activity of nimesulide. The most pronounced changes in the leukocyte formula during AF-induced inflammation were observed on the part of neutrophils: the effect of the studied substance Les6490 was more pronounced compared to the effect of nimesulide. The introduction of the new compound Les6490 partially caused the normalization of monocytes, and under the conditions of the AF-associated inflammatory process, no significant changes were observed.
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