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用于动脉粥样硬化治疗的细胞因子-药物复合物的虚拟筛选与分子动力学

Virtual Screening and Molecular Dynamics of Cytokine-Drug Complexes for Atherosclerosis Therapy.

作者信息

Rodríguez-Fernández María Angélica, Tristán-Flores Fabiola Estefanía, Casique-Aguirre Diana, Negrete-Rodríguez María de la Luz Xochilt, Cervantes-Montelongo Juan Antonio, Conde-Barajas Eloy, Acosta-García Gerardo, Silva-Martínez Guillermo Antonio

机构信息

Posgrado de Ingeniería Bioquímica, Tecnológico Nacional de México/IT de Celaya, Celaya 38010, Guanajuato, Mexico.

Departamento de Ciencias Básicas, Tecnológico Nacional de México/IT de Celaya, Celaya 38010, Guanajuato, Mexico.

出版信息

Int J Mol Sci. 2025 Mar 24;26(7):2931. doi: 10.3390/ijms26072931.

Abstract

Cardiovascular disease remains the leading global cause of mortality, largely driven by atherosclerosis, a chronic inflammatory condition characterized by lipid accumulation and immune-cell infiltration in arterial walls. Macrophages play a central role by forming foam cells and secreting pro-atherogenic cytokines, such as TNF-α, IFN-γ, and IL-1β, which destabilize atherosclerotic plaques, expanding the lipid core and increasing the risk of thrombosis and ischemia. Despite the significant health burden of subclinical atherosclerosis, few targeted therapies exist. Current treatments, including monoclonal antibodies, are limited by high costs and immunosuppressive side effects, underscoring the urgent need for alternative therapeutic strategies. In this study, we employed in silico drug repositioning to identify multitarget inhibitors against TNF-α, IFN-γ, and IL-1β, leveraging a virtual screening of 2750 FDA-approved drugs followed by molecular dynamics simulations to assess the stability of selected cytokine-ligand complexes. This computational approach provides structural insights into potential inhibitors. Additionally, we highlight nutraceutical options, such as fatty acids (oleic, linoleic and eicosapentaenoic acid), which exhibited strong and stable interactions with key cytokine targets. Our study suggests that these bioactive compounds could serve as effective new therapeutic approaches for atherosclerosis.

摘要

心血管疾病仍然是全球主要的死亡原因,主要由动脉粥样硬化驱动,动脉粥样硬化是一种慢性炎症性疾病,其特征是脂质在动脉壁中积累以及免疫细胞浸润。巨噬细胞通过形成泡沫细胞和分泌促动脉粥样硬化细胞因子(如TNF-α、IFN-γ和IL-1β)发挥核心作用,这些细胞因子会破坏动脉粥样硬化斑块的稳定性,扩大脂质核心并增加血栓形成和局部缺血的风险。尽管亚临床动脉粥样硬化带来了巨大的健康负担,但针对性的治疗方法却很少。目前的治疗方法,包括单克隆抗体,受到高成本和免疫抑制副作用的限制,这凸显了对替代治疗策略的迫切需求。在本研究中,我们利用计算机辅助药物重新定位来识别针对TNF-α、IFN-γ和IL-1β的多靶点抑制剂,利用对2750种FDA批准药物的虚拟筛选,随后进行分子动力学模拟以评估所选细胞因子-配体复合物的稳定性。这种计算方法为潜在抑制剂提供了结构见解。此外,我们强调了营养补充剂选项,如脂肪酸(油酸、亚油酸和二十碳五烯酸),它们与关键细胞因子靶点表现出强烈而稳定的相互作用。我们的研究表明,这些生物活性化合物可以作为动脉粥样硬化有效的新治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e6a/11988346/d5e1833606ad/ijms-26-02931-g001.jpg

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