Departamento de Química, Universidad Técnica Federico Santa María, Avenida España 1680, 2390123 Valparaíso, Chile.
Centro de Investigaciones Biomédicas (CIB), Escuela de Medicina, Universidad de Valparaiso, Avenida Hontaneda 2664, 2340000 Valparaíso, Chile.
Bioinorg Chem Appl. 2015;2015:920143. doi: 10.1155/2015/920143. Epub 2015 Feb 28.
A new oxaliplatin analog [Pt(dach)(L5)] (1) was synthesized and characterized as a continuation of a study of the previously reported [Pt(dach)(L6)] (2), where dach = (1R,2R)-diaminocyclohexane, L5 = 3-carboxyboldine, and L6 = 3-carboxypredicentrine. Compounds 1 and 2 exhibited a substantially enhanced antioxidant activity compared to oxaliplatin (130 and 30 times for 1 and 13 and 4 times for 2 using the DPPH and FRAP assays, resp.). In addition, 1 and 2 exhibited cytotoxic activity in the same range as oxaliplatin toward the two human tumor cell lines (MCF-7 and HT-29) studied and two to four times lower activity in the human colon nontumor cell line (CCD-841). Preadministration of L5 or L6 to the colon tumor (HT-29) and the colon nontumor (CCD-841) cell lines prior to oxaliplatin addition increased the viability of the nontumor cell line to a greater extent than that of the tumor cell line.
一种新的奥沙利铂类似物[Pt(dach)(L5)]（1）被合成并进行了表征，这是对先前报道的[Pt(dach)(L6)]（2）的研究的延续，其中dach = (1R,2R)-二氨基环己烷，L5 = 3-羧基波多尼定，L6 = 3-羧基普瑞地辛。与奥沙利铂相比，化合物 1 和 2 表现出显著增强的抗氧化活性（使用 DPPH 和 FRAP 测定法，分别为 130 和 30 倍和 13 和 4 倍）。此外，1 和 2 在对所研究的两种人肿瘤细胞系（MCF-7 和 HT-29）和两种至四种人结肠非肿瘤细胞系（CCD-841）的细胞毒性活性与奥沙利铂相当。在奥沙利铂加入之前，将 L5 或 L6 预给药于结肠肿瘤（HT-29）和结肠非肿瘤（CCD-841）细胞系，可使非肿瘤细胞系的活力增加程度大于肿瘤细胞系。
