江汉大学学报（自然科学版）2026，Vol.54Issue(2)：26-37,12.DOI:10.16389/j.cnki.cn42-1737/n.2026.02.003
光谱法研究具有细胞毒性活性的铂-苯并噁唑杂化剂及其三齿螯合铂单元与人血清白蛋白的相互作用
Spectroscopic Analyses on the Interaction of a Cytotoxic Pt-Benzoxazole Hybrid Agent and Its Tridentate Chelating Platinum Unit with Human Serum Albumin
摘要
Abstract
Interactions between platinum complexes and human serum albumin(HSA)play crucial roles in the bioavailability and toxicology of platinum-based anticancer drugs.Platinum-intercalator hybrid pharmacophores are a novel class of DNA-targeted cytotoxic agents that show potent activity across a broad range of solid tumor cell lines.In this study,the interactions of a cytotoxic Pt-benzoxazole hybrid agent,[PtLCl]Cl(1,where L=N-(4-(benzo[d]oxazol-2-yl)phenyl)-2-(bis(2-ethylthioethyl)amino)acetamide)and its tridentate chelating platinum unit,[PtL′Cl]Cl(2,where L′=bis(2-ethylthioethyl)amine),with HSA were investigated by multiple spectroscopic methods.The results revealed that both complexes exhibited moderate HSA binding affinity(1>2),triggering conformation and microenvironmental changes of the protein and suppressing its intrinsic fluorescence via static quenching pathways.The thermodynamic parameters(ΔG°,ΔH°,ΔS°)calculated from fluorescence data at different temperatures suggested that the binding reaction between the complexes and HSA was a spontaneous process dominated by hydrophobic interactions.The binding site number indicated 1∶1 stoichiometry for both complexes at a single primary binding site on HSA.Furthermore,site marker competition assays demonstrated that complexes 1 and 2 could bind to the drug binding sites I(bromophenol blue-binding domain)and site II(ibuprofen-binding domain)on HSA,respectively.关键词
铂-插层杂化试剂/人血清白蛋白/荧光淬灭/抗癌金属药物Key words
platinum-intercalator hybrid agent/human serum albumin/fluorescence quenching/anticancer metallodrugs分类
生物科学引用本文复制引用
马晓萌,曲焓萁,张子宁,雷鸿声,陈战芬..光谱法研究具有细胞毒性活性的铂-苯并噁唑杂化剂及其三齿螯合铂单元与人血清白蛋白的相互作用[J].江汉大学学报（自然科学版）,2026,54(2):26-37,12.基金项目
Excellent Discipline Cultivation Project of Jianghan University(2023XKZ006) （2023XKZ006）
Four New Disciplines Special Project of Jianghan University(2022SXZX02) （2022SXZX02）
Jianghan University Re-search Projects(2023zd037,2024zd043,2024yb105) （2023zd037,2024zd043,2024yb105）
