Dey Jyotirmayee, Mahapatra Soumya Ranjan, Raj T Kiran, Misra Namrata, Suar Mrutyunjay
School of Biotechnology, Kalinga Institute of Industrial Technology (KIIT) Deemed to be University, Bhubaneswar, 751024, India.
Department of Biotechnology & Bioinformatics, School of Life Sciences, JSS Academy of Higher Education & Research, Mysore, India.
Mol Divers. 2024 Oct;28(5):3111-3128. doi: 10.1007/s11030-023-10738-z. Epub 2023 Oct 6.
Klebsiella pneumoniae, which is among the top three pathogens on WHO's priority list, is one of the gram-negative bacteria that doctors and researchers around the world have fought for decades. Capsular polysaccharide (CPS) protein is extensively recognized as an important K. pneumoniae virulence factor. Thus, CPS has become the most characterized target for the discovery of novel drug candidates. The ineffectiveness of currently existing antibiotics urges the search for potent antimicrobial compounds. Flavonoids are a group of plant metabolites that have antibacterial potential and can enhance the present medications to elicit improved results against diverse diseases without adverse reactions. Henceforth, the present study aims to illustrate the inhibitory potential of flavonoids with varying pharmacological properties, targeting the CPS protein of K. pneumoniae by in silico approaches. The flavonoid compounds (n = 169) were retrieved from the PubChem database and screened using the structure-based virtual screening approach. Compounds with the highest binding score were estimated through their pharmacokinetic effects by ADMET descriptors. Finally, four potential inhibitors with PubChem CID: (4301534, 5213, 5481948, and 637080) were selected after molecular docking and drug-likeness analysis. All four lead compounds were employed for the MDS analysis of a 100 ns time period. Various studies were undertaken to assess the stability of the protein-ligand complexes. The binding free energy was computed using MM-PBSA, and the outcomes indicated that the molecules are having stable interactions with the binding site of the target protein. The results revealed that all four compounds can be employed as potential therapeutics against K. pneumoniae.
肺炎克雷伯菌是世界卫生组织重点病原体名单上的前三位病原体之一,是全球医生和研究人员几十年来一直在对抗的革兰氏阴性菌之一。荚膜多糖(CPS)蛋白被广泛认为是肺炎克雷伯菌的一种重要毒力因子。因此,CPS已成为发现新型候选药物最具特征的靶点。现有抗生素的无效性促使人们寻找有效的抗菌化合物。黄酮类化合物是一类具有抗菌潜力的植物代谢产物,可以增强现有药物对多种疾病的疗效且无不良反应。因此,本研究旨在通过计算机模拟方法,阐明具有不同药理特性的黄酮类化合物对肺炎克雷伯菌CPS蛋白的抑制潜力。从PubChem数据库中检索黄酮类化合物(n = 169),并使用基于结构的虚拟筛选方法进行筛选。通过ADMET描述符评估具有最高结合分数的化合物的药代动力学效应。最后,经过分子对接和类药性分析,选择了四种潜在抑制剂,其PubChem CID分别为:(4301534、5213、5481948和637080)。所有四种先导化合物都用于100纳秒时间段的分子动力学模拟分析。进行了各种研究以评估蛋白质-配体复合物的稳定性。使用MM-PBSA计算结合自由能,结果表明这些分子与靶蛋白的结合位点具有稳定的相互作用。结果显示,所有四种化合物都可用作抗肺炎克雷伯菌的潜在治疗药物。