Jiang Dejun, Kwon Hyuk-Ku, Kwon Oh Wook, Choi Youngjin
Department of Environmental Engineering, Hoseo University, Asan 31499, Republic of Korea.
Pet-Loss Center, Hoseo University, Asan 31499, Republic of Korea.
Molecules. 2025 Feb 15;30(4):907. doi: 10.3390/molecules30040907.
In this study, we investigated the inhibitory potential of 60 flavonoids from six distinct subgroups on the programmed cell death ligand 1 (PD-L1) dimer through molecular docking and dynamics simulations. Using AutoDock Vina for docking, the binding poses and affinities were evaluated, revealing an average binding affinity of -8.5 kcal/mol for the flavonoids. Among them, ginkgetin exhibited the highest binding free energy of -46.73 kcal/mol, indicating a strong interaction with PD-L1, while diosmin followed closely, with -44.96 kcal/mol. Molecular dynamics simulations were used to further elucidate the dynamic interactions and stability of the flavonoid-PD-L1 complexes, with the analyses showing minimal root mean square deviation (RMSD) and favorable root mean square fluctuation (RMSF) profiles for several compounds, particularly formononetin, idaein, and neohesperidin. Additionally, contact number and hydrogen bond analyses were performed, which highlighted ginkgetin and diosmin as key flavonoids with significant binding interactions, evidenced by their stable conformations and robust molecular interactions throughout the simulations. Ultimately, a cell-based assay confirmed their ability to inhibit the proliferation of cancer cells. These results, validated through cell-based assays, indicate that the strategy of identifying natural compounds with anticancer activity using computational modeling is highly effective.
在本研究中,我们通过分子对接和动力学模拟研究了来自六个不同亚组的60种黄酮类化合物对程序性细胞死亡配体1(PD-L1)二聚体的抑制潜力。使用AutoDock Vina进行对接,评估了结合姿势和亲和力,结果显示黄酮类化合物的平均结合亲和力为-8.5千卡/摩尔。其中,银杏双黄酮表现出最高的结合自由能,为-46.73千卡/摩尔,表明与PD-L1有强烈相互作用,而地奥司明紧随其后,为-44.96千卡/摩尔。分子动力学模拟用于进一步阐明黄酮类化合物-PD-L1复合物的动态相互作用和稳定性,分析表明几种化合物,特别是芒柄花素、山奈酚-3-葡萄糖苷和新橙皮苷的均方根偏差(RMSD)最小,均方根波动(RMSF)曲线良好。此外,还进行了接触数和氢键分析,结果突出显示银杏双黄酮和地奥司明是具有显著结合相互作用的关键黄酮类化合物,在整个模拟过程中,它们稳定的构象和强大的分子相互作用证明了这一点。最终,基于细胞的试验证实了它们抑制癌细胞增殖的能力。通过基于细胞的试验验证的这些结果表明,使用计算模型识别具有抗癌活性的天然化合物的策略非常有效。