探讨曲美他嗪与人血清白蛋白相互作用的潜在毒性。

IF 2.4 3区 化学 Q3 CHEMISTRY, ANALYTICAL Methods and Applications in Fluorescence Pub Date : 2023-07-19 DOI:10.1088/2050-6120/ace513
Aya Barseem, Fathalla Belal, Mokhtar Mabrouk, Sherin Hammad, Hytham Ahmed
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引用次数: 0

摘要

人血清白蛋白(HSA)转运会影响小分子药物的药效学和药代动力学,因此我们采用不同的方法研究了HSA与广泛使用的抗缺血性药物曲美他嗪(TMZ)的相互作用。同步荧光光谱显示,相互作用影响酪氨酸残基周围微环境的确认。位点竞争实验表明,TMZ对HSA的子结构域iia(位点II)具有亲和力。焓变(ΔH)和熵变(ΔS)分别为37.75 kj mol-1和0.197 kj mol-1,表明分子间相互作用主要是疏水力。FTIR研究表明,HSA与TMZ的相互作用导致多肽羰基-氢键重排。TMZ使HSA酯酶活性降低。对接分析证实了现场竞争实验和热力学结果。本研究表明TMZ与HSA相互作用,并影响HSA的结构和功能。本研究有助于了解TMZ的药动学,为其安全使用提供基础资料。
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Probing the potential toxicity of trimetazidine by characterizing its interaction with human serum albumin.

The small molecular drugs pharmacodynamics and pharmacokinetics could be affected by human serum albumin (HSA) transport, so we studied the interaction between HSA and the widely used anti-ischemic agent, trimetazidine (TMZ), using different approaches. As shown by synchronous fluorescence spectroscopy, the interaction affects the microenvironment confirmation around tyrosine residues. The site-competitive experiments showed that TMZ had an affinity toward subdomain III A (site II) of HSA. The enthalpy and entropy changes (ΔH and ΔS), which were 37.75 and 0.197 K J mol-1, respectively, showed that the predominant intermolecular interactions are hydrophobic forces. According to FTIR research, the interaction between HSA and TMZ caused polypeptide carbonyl-hydrogen bonds to rearrange. The HSA esterase enzyme activity was decreased with TMZ. Docking analysis confirmed the site-competitive experiments and thermodynamic results. This study demonstrated that TMZ interacted with HSA, and the structure and function of HSA were influenced by TMZ. This study could aid in understanding the pharmacokinetics of TMZ and provide basic data for safe use.

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来源期刊
Methods and Applications in Fluorescence
Methods and Applications in Fluorescence CHEMISTRY, ANALYTICALCHEMISTRY, PHYSICAL&n-CHEMISTRY, PHYSICAL
CiteScore
6.20
自引率
3.10%
发文量
60
期刊介绍: Methods and Applications in Fluorescence focuses on new developments in fluorescence spectroscopy, imaging, microscopy, fluorescent probes, labels and (nano)materials. It will feature both methods and advanced (bio)applications and accepts original research articles, reviews and technical notes.
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