Department of Science, University of Kragujevac, Institute of Information Technologies, Jovana Cvijica bb, 34000 Kragujevac, Serbia.
Faculty of Science, University of Kragujevac, Radoja Domanovića 12, 34000 Kragujevac, Serbia.
Oxid Med Cell Longev. 2021 Apr 28;2021:8849568. doi: 10.1155/2021/8849568. eCollection 2021.
Two newly synthesized 4-hydroxycoumarin bidentate ligands (L1 and L2) and their palladium(II) complexes (C1 and C2) were screened for their biological activities, and . Structures of new compounds were established based on elemental analysis, H NMR, C NMR, and IR spectroscopic techniques. The obtained compounds were tested for their antioxidative and cytotoxic activities and results pointed to selective antiradical activity of palladium(II) complexes towards OH and OOH radicals and anti-ABTS (2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) cation radical) activity comparable to that of ascorbate. Results indicated the effect of C1 and C2 on the enzymatic activity of the antioxidative defense system. cytotoxicity assay performed on different carcinoma cell lines (HCT166, A375, and MIA PaCa-2), and one healthy fibroblast cell line (MRC-5) showed a cytotoxic effect of both C1 and C2, expressed as a decrease in carcinoma cells' viability, mostly by induction of apoptosis. toxicity tests performed on zebrafish embryos indicated different effects of C1 and C2, ranging from adverse developmental effect to no toxicity, depending on tested concentration. According to docking studies, both complexes (C1 and C2) showed better inhibitory activity in comparison to other palladium(II) complexes.
两种新合成的 4-羟基香豆素双齿配体(L1 和 L2)及其钯(II)配合物(C1 和 C2)被筛选用于生物活性测试,结果表明。新化合物的结构是基于元素分析、H NMR、C NMR 和 IR 光谱技术建立的。所得化合物进行了抗氧化和细胞毒性测试,结果表明钯(II)配合物对 OH 和 OOH 自由基具有选择性的抗自由基活性,对 ABTS(2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)cation radical)的活性可与抗坏血酸相媲美。结果表明,C1 和 C2 对抗氧化防御系统的酶活性有影响。在不同的癌细胞系(HCT166、A375 和 MIA PaCa-2)和一种健康成纤维细胞系(MRC-5)上进行的细胞毒性测定表明,C1 和 C2 都具有细胞毒性作用,表现为癌细胞活力下降,主要通过诱导细胞凋亡。在斑马鱼胚胎上进行的毒性测试表明,C1 和 C2 的作用不同,取决于测试浓度,从不利的发育影响到无毒性。根据对接研究,与其他钯(II)配合物相比,两种配合物(C1 和 C2)都显示出更好的抑制活性。