Alkış Mehmet Eşref, Turan Nevin, Alan Yusuf, Irtegun Kandemir Sevgi, Buldurun Kenan
Department of Occupational Health and Safety, Faculty of Health Sciences, Muş Alparslan University, 49250, Muş, Turkey.
Department of Chemistry, Faculty of Arts and Sciences, Muş Alparslan University, 49250, Muş, Turkey.
Med Oncol. 2021 Sep 22;38(11):129. doi: 10.1007/s12032-021-01579-7.
Zn(II) complex of Schiff base derived from the condensation of 4-aminopyrimidine-2(1H)-one with salicylaldehyde was prepared and characterized by various physico-chemical and spectral methods for structure determination. The cytotoxic activity of the Zn(II) complex was investigated in comparison with 5-fluorouracil (5-FU) against two different human brain tumor cell lines (T98G and U118), while primer human dermal fibroblast cells (HDF) was used as control for biocompatibility. Then, the effectiveness of electroporation (EP) on cytotoxic activities of these compounds has been examined. The cytotoxicities of the 5-FU and new Zn(II) complex, alone or in combination with electroporation, were determined by MTT assay. The Zn(II) complex showed good cytotoxicity against T98G and U118 brain tumor cell lines with IC = 282.47 and 297.91 μM respectively, while it was safe on HDF healthy cells with IC = 826.72 μM. The 5-FU exhibited less cytotoxicity compared to the Zn(II) complex against T98G (IC = 382.35 μM) and U118 (IC = 396.56 μM) tumor cell lines. The combined application of Zn (II) + EP decreased the IC value by 5.96-fold in T98G cells and 4.76-fold in U118 cells. EP showed a similar effect in its combined application with 5-FU, resulting in a decrease of the IC value of 4.22-fold in the T98G cells and 3.84-fold in the U118 cells. In a conclusion, the Zn(II) complex exhibited an anticancer potential against both brain tumor cell lines (T98G and U118) and EP greatly increased the cytotoxicity of Zn(II) complex and 5-FU on these chemotherapy-resistant cells.
制备了由4-氨基嘧啶-2(1H)-酮与水杨醛缩合得到的席夫碱锌(II)配合物,并通过各种物理化学和光谱方法对其进行表征以确定结构。将锌(II)配合物的细胞毒性与5-氟尿嘧啶(5-FU)进行比较,研究其对两种不同的人脑肿瘤细胞系(T98G和U118)的作用,同时以原代人皮肤成纤维细胞(HDF)作为生物相容性对照。然后,研究了电穿孔(EP)对这些化合物细胞毒性的影响。通过MTT法测定5-FU和新型锌(II)配合物单独或与电穿孔联合使用时的细胞毒性。锌(II)配合物对T98G和U118脑肿瘤细胞系显示出良好的细胞毒性,IC值分别为282.47和297.91 μM,而对HDF健康细胞安全,IC值为826.72 μM。与锌(II)配合物相比,5-FU对T98G(IC = 382.35 μM)和U118(IC = 396.56 μM)肿瘤细胞系的细胞毒性较小。锌(II)+EP联合应用使T98G细胞的IC值降低了5.96倍,U118细胞降低了4.76倍。EP与5-FU联合应用也显示出类似效果,使T98G细胞的IC值降低了4.22倍,U118细胞降低了3.84倍。总之,锌(II)配合物对两种脑肿瘤细胞系(T98G和U118)均具有抗癌潜力,电穿孔大大提高了锌(II)配合物和5-FU对这些化疗耐药细胞的细胞毒性。