水溶性的半胱氨酸-β-环糊精铂配合物的合成及生物活性研究

Synthesis and bioactivity of the water-soluble L-cysteine-β-cyclodextrin platinum complexes

利用半胱氨酸修饰的β-环糊精与K2PtCl4反应得到了水溶性的铂配合物(Pt(L-Cys-β-CD)Cl_2).通过质谱、元素分析和核磁等手段对合成的铂配合物进行表征.利用MTT法对该铂配合物的抗肿瘤活性进行研究.主要选择K562,HepG2和7701三种细胞对这种铂配合物的细胞毒性进行研究,结果表明该铂配合物具有较高的细胞抑制率.其在K562细胞中的IC50值为(89.5±2.6)μmol/L.更有意义的是,这种铂配合物对正常细胞7701的细胞毒性要明显低于另外两种癌细胞.因此,该类铂配合物有望作为潜在的抗肿瘤药物.

We synthesized a water-soluble L-cysteine-β-cyclodextrin platinum complex（Pt（LCys-β-CD）Cl_2）,and the platinum complex was obtained by the reaction of the ligand L-cysteine-modifiedβ-cyclodextrin with K_2PtCl_4.The Pt（L-Cys-β-CD）Cl_2complex has been characterized using ESI-MS,elemental analysis and 1~H NMR.The antitumor activity of Pt（L-Cys-β-CD）Cl_2complex has been studied by MTT assay.The in vitro cytotoxicity of the platinum complex was evaluated in K562,HepG2 and 7701cells and higher cell inhibition ratio was observed.Interestingly,the Pt（L-Cys-β-CD）Cl_2 complex was less toxic on the normal 7701 cells than other two types of cancer cells.So the type of Pt complexes could be used as potential antitumor drug.