Rasoolzadeh Reza, Baptista Leonardo, Vajedi Fahimeh Sadat, Nikoofard Vahid
Department of Inorganic Chemistry, Institute of Chemistry, Fluminense Federal University, Niterói, Rio de Janeiro 24020-140, Brazil.
Department of Chemistry and Environmental, Faculty of Technology, Rio de Janeiro State University, Resende, Rio de Janeiro 27537-000, Brazil.
ACS Omega. 2024 Aug 6;9(33):35821-35836. doi: 10.1021/acsomega.4c04515. eCollection 2024 Aug 20.
In this work, the main purpose is to analyze and understand the mechanism and thermodynamic interactions of carboxylic acid-functionalized multiwalled carbon nanotubes (cf-MWCNTs) and 4-aminoantipyrine (AAP) with human hepcidine25 (Hep25) using multispectroscopic and molecular docking modeling methods, binding free energy calculations, and molecular dynamics (MD) simulations under physiological conditions. AAP belongs to a class of persistent environmental contaminants, and its residue is a potential hazard to human health, exhibiting a high binding affinity with blood peptides. Hepcidin is a 25-residue peptide hormone with four disulfide bonds that regulates the iron balance in vertebrates and contributes to host immunity as a cysteine-rich antimicrobial peptide. Due to their diverse properties and pollutant absorption capabilities, CNTs demonstrate important biological effects in biological applications, particularly in the noncovalent interactions with blood peptides. A comprehensive molecular dynamics simulation integrated with molecular docking methodologies was employed to explore the binding free energy between AAP and Hep25, identify binding sites, elucidate thermodynamic characteristics, and evaluate the binding forces governing their interaction. The investigation delved into elucidating the precise binding site of AAP within the Hep25 protein and thoroughly analyzed the impact of AAP on the microenvironment and conformational dynamics of Hep25. The circular dichroism (CD) experimental results highlight a reduction in β-sheet composition following the introduction of AAP and cf-MWCNT. In addition, outcomes from fluorescence spectroscopy demonstrate that both cf-MWCNT and AAP significantly attenuated Hep-25 fluorescence via a static quenching mechanism. According to the MD simulations, the presence of AAP induces changes in the secondary structure of Hep25 and enhances its hydrophobicity. Additionally, our findings demonstrated that alongside the alteration in protein structure and functionality induced by contaminants, cf-MWCNTs possess the capability to mitigate the contaminant-induced effects on Hep25 activity while preserving the overarching structural integrity of Hep25. Based on the distance and RDF data, we found that during the simulation the presence of the cf-MWCNT causes the AAP to move away from the Hep25, and as a result fewer and weaker interactions of the AAP with the Hep25 will be observed. Likewise, free energy calculations indicate that the binding of Hep25 to AAP and cf-MWCNT involves electrostatic, π-cationic, and π-π stacking interactions. The research findings offer invaluable insights into the intricate influence of pollutants and carbon nanotubes on protein functionality within the circulatory system and their toxicity in vivo for prospective investigations.
在本研究中,主要目的是利用多光谱和分子对接建模方法、结合自由能计算以及生理条件下的分子动力学(MD)模拟,分析和理解羧酸功能化多壁碳纳米管(cf-MWCNTs)和4-氨基安替比林(AAP)与人类铁调素25(Hep25)之间的作用机制和热力学相互作用。AAP属于一类持久性环境污染物,其残留对人类健康具有潜在危害,与血液肽表现出高结合亲和力。铁调素是一种含有四个二硫键的25个残基的肽激素,可调节脊椎动物的铁平衡,并作为富含半胱氨酸的抗菌肽促进宿主免疫。由于其多样的性质和污染物吸收能力,碳纳米管在生物应用中表现出重要的生物学效应,特别是在与血液肽的非共价相互作用方面。采用结合分子对接方法的综合分子动力学模拟来探索AAP与Hep25之间的结合自由能,确定结合位点,阐明热力学特征,并评估控制它们相互作用的结合力。该研究深入阐明了AAP在Hep25蛋白内的精确结合位点,并全面分析了AAP对Hep25微环境和构象动力学的影响。圆二色性(CD)实验结果表明,引入AAP和cf-MWCNT后β-折叠组成减少。此外,荧光光谱结果表明,cf-MWCNT和AAP均通过静态猝灭机制显著减弱Hep-25荧光。根据MD模拟,AAP的存在会导致Hep25二级结构发生变化并增强其疏水性。此外,我们的研究结果表明,除了污染物引起的蛋白质结构和功能改变外,cf-MWCNTs能够减轻污染物对Hep25活性的影响,同时保持Hep25的整体结构完整性。基于距离和径向分布函数(RDF)数据,我们发现在模拟过程中cf-MWCNT的存在会使AAP远离Hep25,因此将观察到AAP与Hep25之间更少且更弱的相互作用。同样,自由能计算表明,Hep25与AAP和cf-MWCNT的结合涉及静电、π-阳离子和π-π堆积相互作用。研究结果为污染物和碳纳米管对循环系统中蛋白质功能的复杂影响及其体内毒性提供了宝贵的见解,以供未来研究参考。