Kaur Gurmeet, Bansal Manisha, Rehman Hafiz Muzzammel, Kaur Mandeep, Kaur Amandeep
Synthetic and Medicinal Chemistry Laboratory, Department of Chemistry, Punjabi University, Patiala, 147002, India.
Department of Chemistry, Punjabi University, Patiala, 147002, India.
Mol Divers. 2024 Feb;28(1):97-110. doi: 10.1007/s11030-023-10616-8. Epub 2023 Feb 28.
Pro-inflammation, which is developed due to the increased production of cytokines, mainly interleukin-6 (IL-6), during the working of immune system pathways, becomes a major concern these days for many researchers. So, it is desired to design, screen, and synthesize new molecules with multi-parametric features showing their efficacy for Toll-like receptors (TLRs) and inhibiting the disease-causing receptor sites like viral infections, cancers, etc. along with controlling inflammation, fever, and other side effects during such pathways. Further, looking at the literature, curcumin a multi-targeted agent is showing its efficiency toward various receptor sites involved in many diseases as mentioned above. This fascinated us to build up new molecules which behave like curcumin with minimum side effects. In silico studies, involving ADMET studies, toxicological data, and docking analyses, of newly synthesized compounds (3-5) along with tautomers of curcumin i.e., (1-2), and some reported compounds like 9 and 10 have been studied in detail. Great emphasis has been made on analyzing binding energies, protein-ligand structural interactions, stabilization of newly synthesized molecules against various selected receptor sites using such computational tools. Compound 3 is the most efficient multifunctional agent, which has shown its potential toward most of the receptor sites in docking analysis. It has also responded well in Molecular dynamics (MD) simulation toward 5ZLN, 4RJ3, 4YO9, 4YOJ, and 1I1R sites. Finally, studies were extended to understand in vitro anti-inflammatory activity for particularly compound 3 in comparison to diclofenac and curcumin, which signifies the efficiency of compound 3.
在免疫系统途径运作过程中,由于细胞因子(主要是白细胞介素-6,即IL-6)产生增加而引发的促炎反应,如今已成为许多研究人员的主要关注点。因此,人们期望设计、筛选和合成具有多参数特征的新分子,这些分子对Toll样受体(TLRs)具有功效,并能抑制诸如病毒感染、癌症等致病受体位点,同时在这些途径中控制炎症、发热及其他副作用。此外,从文献来看,姜黄素这种多靶点药物对上述许多疾病所涉及的各种受体位点都显示出了疗效。这促使我们构建新分子,使其表现得像姜黄素且副作用最小。对新合成的化合物(3 - 5)以及姜黄素的互变异构体(即(1 - 2)),还有一些报道的化合物如9和10,进行了包括ADMET研究、毒理学数据和对接分析在内的计算机模拟研究。利用此类计算工具,重点分析了结合能、蛋白质-配体结构相互作用以及新合成分子针对各种选定受体位点的稳定性。化合物3是最有效的多功能药物,在对接分析中已显示出对大多数受体位点的潜力。在分子动力学(MD)模拟中,它对5ZLN、4RJ3、4YO9、4YOJ和1I1R位点也有良好反应。最后,研究扩展到了解化合物3与双氯芬酸和姜黄素相比的体外抗炎活性,这表明了化合物3的有效性。