Navarro-Ranninger C, Ochoa P A, Pérez J M, Rodríguez J H, Masaguer J R, Alonso C
Departamento de Química, Universidad Autónoma de Madrid, Spain.
J Inorg Biochem. 1992 Nov 15;48(3):163-71. doi: 10.1016/0162-0134(92)84027-k.
Four platinum(II) aminobenzamidine complexes have been prepared and characterized by IR and 1H and 13C NMR spectroscopy, and tested for their ability to interact with the nicked and closed circular forms of the pUC8 plasmid DNA. The results show that the complexes of formula [Pt(LH)2Cl2]2X have a cis- geometry with an amino-Pt bonding, where L is either p- or m-aminobenzamidine and where 2X is 2Cl- or PtCl4(2-). It was observed that these complexes significantly alter the electrophoretic mobility of nicked and closed circular forms of DNA and that the alteration in electrophoretic mobility due to Pt(II)-p-aminobenzamidine binding is higher than that due to Pt(II)-m-aminobenzamidine. No difference in mobility was observed whether the DNA interacted with complexes having as counteranion Cl- or PtCl4(2-). The synthesized compounds were, in addition, assayed for antitumor activity in vitro against colon (CX-1), lung (LX-1), and mammary (MX-1) human tumor cells. The results show that these complexes inhibited the multiplication of the tumor cells and that they show higher specificity for lung cells.
已制备了四种铂（II）氨基苯甲脒配合物，并通过红外光谱、1H 和 13C 核磁共振光谱对其进行了表征，并测试了它们与 pUC8 质粒 DNA 的切口和闭环形式相互作用的能力。结果表明，式为[Pt(LH)2Cl2]2X 的配合物具有顺式几何结构，存在氨基-铂键，其中 L 为对氨基苯甲脒或间氨基苯甲脒，2X 为 2Cl-或 PtCl4(2-)。观察到这些配合物显著改变了 DNA 的切口和闭环形式的电泳迁移率，并且由于 Pt(II)-对氨基苯甲脒结合导致的电泳迁移率变化高于由于 Pt(II)-间氨基苯甲脒导致的变化。无论 DNA 与具有 Cl-或 PtCl4(2-)作为抗衡阴离子的配合物相互作用，均未观察到迁移率的差异。此外，还对合成的化合物进行了体外抗结肠（CX-1）、肺（LX-1）和乳腺（MX-1）人肿瘤细胞的抗肿瘤活性测定。结果表明，这些配合物抑制了肿瘤细胞的增殖，并且它们对肺细胞表现出更高的特异性。
