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作为非小细胞肺癌治疗的细胞外信号调节激酶2抑制剂的盐肤木植物化学物质的计算机模拟研究。

In silico investigation of Toxicodendron succedaneum phytochemicals as extracellular signal-regulated kinase 2 inhibitors for non-small cell lung cancer therapy.

作者信息

Ahmed Sheikh Sunzid, Rahman M Oliur, Hasan Md Siddiq, Uddin S M Nasir, Begum Momtaz

机构信息

Department of Botany, Faculty of Biological Sciences, University of Dhaka, Dhaka, 1000, Bangladesh.

出版信息

Med Oncol. 2025 Jun 15;42(7):260. doi: 10.1007/s12032-025-02800-7.

Abstract

Non-small cell lung cancer (NSCLC) accounts for 85-90% of global lung cancer cases and causes over 1.7 million deaths annually worldwide. Despite therapeutic advancements, existing treatments remain expensive and are often associated with significant side effects, underscoring the need for alternative drug candidates. Natural compounds offer promising prospects as safer and more affordable therapeutic options for NSCLC. Toxicodendron succedaneum, a medicinally important plant species from the family Anacardiaceae, contains a diverse phytoconstituents with potential anticancer activity. Investigating these bioactive compounds may uncover therapeutic potential to facilitate NSCLC drug discovery. In this study, a comprehensive structure-based drug design approach was employed to identify drug candidates targeting the extracellular signal-regulated kinase 2 (ERK2) receptor. Using molecular docking, molecular dynamics (MD) simulation, ADMET analysis, MM/GBSA calculations, and DFT assessments, two lead compounds: rhusflavone ( - 10.9 kcal/mol) and hinokiflavone ( - 9.9 kcal/mol), were identified, both revealing favorable drug-likeness and toxicity profiles. MD simulation spanning 500 ns timescale confirmed the structural stability of the identified leads, further corroborated by principal component analysis (PCA) and Gibbs free energy landscape (FEL) evaluations. Rhusflavone emerged as the most promising candidate, with a free binding energy of - 57.15 ± 5.28 kcal/mol. DFT analysis revealed enhanced molecular reactivity of the lead compounds upon transitioning from the free to the bound states. These results could contribute to the development of novel lung anticancer drugs, warranting further in vitro and in vivo validation.

摘要

非小细胞肺癌(NSCLC)占全球肺癌病例的85 - 90%,每年在全球导致超过170万人死亡。尽管治疗取得了进展,但现有治疗方法仍然昂贵,且常常伴有严重的副作用,这凸显了对替代候选药物的需求。天然化合物作为NSCLC更安全、更实惠的治疗选择具有广阔前景。漆树科的重要药用植物盐肤木含有多种具有潜在抗癌活性的植物成分。研究这些生物活性化合物可能会发现促进NSCLC药物研发的治疗潜力。在本研究中,采用了一种基于结构的综合药物设计方法来识别靶向细胞外信号调节激酶2(ERK2)受体的候选药物。通过分子对接、分子动力学(MD)模拟、ADMET分析、MM/GBSA计算和DFT评估,确定了两种先导化合物:漆黄素(-10.9 kcal/mol)和扁柏黄酮(-9.9 kcal/mol),两者均显示出良好的类药性和毒性特征。跨越500 ns时间尺度的MD模拟证实了所确定先导化合物的结构稳定性,主成分分析(PCA)和吉布斯自由能景观(FEL)评估进一步证实了这一点。漆黄素成为最有前景的候选药物,其自由结合能为-57.15±5.28 kcal/mol。DFT分析表明,先导化合物从游离态转变为结合态后分子反应性增强。这些结果可能有助于新型肺癌抗癌药物的开发,值得进一步进行体外和体内验证。

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