Edmond H. Fischer Signal Transduction Laboratory, School of Life Sciences, Jilin University, Changchun, 130012, Qianjin road 2699, China.
Key Laboratory for Molecular Enzymology and Engineering of Ministry of Education, School of Life Sciences, Jilin University, Changchun, 130012, Qianjin road 2699, China.
Comput Biol Med. 2024 Apr;172:108252. doi: 10.1016/j.compbiomed.2024.108252. Epub 2024 Mar 11.
Gout, a painful condition marked by elevated uric acid levels often linked to the diet's high purine and alcohol content, finds a potential treatment target in xanthine oxidase (XO), a crucial enzyme for uric acid production. This study explores the therapeutic properties of alkaloids extracted from sunflower (Helianthus annuus L.) receptacles against gout. By leveraging computational chemistry and introducing a novel R-based clustering algorithm, "TriDimensional Hierarchical Fingerprint Clustering with Tanimoto Representative Selection (3DHFC-TRS)," we assessed 231 alkaloid molecules from sunflower receptacles. Our clustering analysis pinpointed six alkaloids with significant gout-targeting potential, particularly emphasizing the fifth cluster's XO inhibition capabilities. Through molecular docking and the BatchDTA prediction model, we identified three top compounds-2-naphthylalanine, medroxalol, and fenspiride-with the highest XO affinity. Further molecular dynamics simulations assessed their enzyme active site interactions and binding free energies, employing MM-PBSA calculations. This investigation not only highlights the discovery of promising compounds within sunflower receptacle alkaloids via LC-MS but also introduces medroxalol as a novel gout treatment candidate, showcasing the synergy of computational techniques and LC-MS in drug discovery.
痛风是一种疼痛的病症,其特征是尿酸水平升高,通常与饮食中的高嘌呤和酒精含量有关。黄嘌呤氧化酶 (XO) 是尿酸生成的关键酶,它成为了治疗痛风的潜在靶点。本研究探讨了从向日葵(Helianthus annuus L.)花托中提取的生物碱对痛风的治疗特性。通过利用计算化学和引入一种新颖的基于 R 的聚类算法“三维层次指纹聚类与 Tanimoto 代表选择 (3DHFC-TRS)”,我们评估了来自向日葵花托的 231 种生物碱分子。我们的聚类分析确定了六种具有显著痛风靶向潜力的生物碱,特别是强调了第五个簇的 XO 抑制能力。通过分子对接和 BatchDTA 预测模型,我们确定了三种具有最高 XO 亲和力的顶级化合物-2-萘丙氨酸、美多心安和奋乃静。进一步的分子动力学模拟评估了它们在酶活性位点的相互作用和结合自由能,使用 MM-PBSA 计算。这项研究不仅通过 LC-MS 突出了在向日葵花托生物碱中发现有前途的化合物,还将美多心安作为一种新的痛风治疗候选药物,展示了计算技术和 LC-MS 在药物发现中的协同作用。