综合研究网络药理学、计算模型和药代动力学评估,评估类黄酮对类风湿性关节炎的疗效。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Sukanya Vijayan, Thirumal Margesan
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引用次数: 0

摘要

类风湿性关节炎是一种以炎症和关节损伤为特征的慢性自身免疫性疾病,给全世界的患者带来沉重负担。黄酮类化合物是一类天然化合物,在各种植物性食物中含量丰富,具有良好的抗炎和免疫调节作用,有望成为治疗类风湿性关节炎的药物。在本研究中,我们利用网络药理学、计算建模、硅学方法和药代动力学评估对已鉴定的 LCMS 化合物进行了全面调查,以评估类黄酮在 RA 治疗中的疗效。这项研究通过LCMS鉴定出了5种具有共同靶点的类黄酮结构,并结合网络药理学方法对类黄酮在RA治疗中的药理学特征进行了全面评估,从而为进一步的实验验证和临床开发选择有前景的候选化合物提供了指导。前10个靶点是AKT1、PI3KR1、CDK2、表皮生长因子受体(EGFR)、CDK6、NOS2、FLT3、ALOX5、CCNB1和通过PPI网络的PTPRS。调查强调了几种途径,包括 AGE-RAGE 信号途径、对表皮生长因子受体酪氨酸激酶抑制剂的抗性、PI3K-AKT 信号网络和 Rap 1 信号途径。硅学研究估计其结合亲和力为-7.0至-10.0 kcal/mol。在计算方法中,沙福苷和荆芥苷没有显示出毒性,适合进一步研究。总之,我们的研究强调了黄酮类化合物作为RA治疗药物的潜力,并突出了在药物发现和开发过程中结合网络药理学、计算建模、硅学方法和药代动力学评估的综合方法的实用性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comprehensive investigation of network pharmacology, computational modeling, and pharmacokinetic assessment to evaluate the efficacy of flavonoids in rheumatoid arthritis.

Rheumatoid arthritis is a chronic autoimmune disease characterized by inflammation and joint damage, imposing a significant burden on affected individuals worldwide. Flavonoids, a class of natural compounds abundant in various plant-based foods, have shown promising anti-inflammatory and immunomodulatory effects, suggesting their potential as therapeutic agents for RA. In this study, we conducted a comprehensive investigation of identified LCMS compounds utilizing network pharmacology, computational modeling, in silico approaches, and pharmacokinetic assessment to evaluate the efficacy of flavonoids in RA treatment. The study identified 5 flavonoid structures with common targets via LCMS and Integration of network pharmacology approaches enabled a comprehensive evaluation of the pharmacological profile of flavonoids in the context of RA treatment, guiding the selection of promising candidates for further experimental validation and clinical development. The top 10 targets were AKT1, PI3KR1, CDK2, EGFR, CDK6, NOS2, FLT3, ALOX5, CCNB1, and PTPRS via PPI network. The investigation emphasized several pathways, including the AGE-RAGE signaling pathway, resistance to EGFR tyrosine kinase inhibitors, the PI3K-AKT signaling network, and the Rap 1 signaling pathway. In silico studies estimated binding affinities that ranged from - 7.0 to - 10.0 kcal/mol. Schaftoside and Vitexin showed no toxicity in computational approach and found suitable for further investigations. Overall, our study underscores the potential of flavonoids as therapeutic agents for RA and highlights the utility of integrative approaches combining network pharmacology, computational modeling, in silico methods, and pharmacokinetic assessment in drug discovery and development processes.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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