Free University of Berlin, Institute of Pharmacy, Berlin, Germany.
Arch Pharm (Weinheim). 2011 Apr;344(4):217-23. doi: 10.1002/ardp.201000237. Epub 2011 Jan 14.
Schiff base transition metal complexes are an important class of compounds with great potential for therapeutic interventions. However, data on antileukemic and antilymphoma effects of these complexes are limited. The activity of N,N'-bis(salicylidene)-1,2-phenylenediamine (salophene, 1), its iron(II/III) and manganese(II/III) complexes as well as rac-trans-N,N'-bis(salicylidene)-1,2-cyclohexanediamine (saldach, 2) and its respective iron(II/III) complexes was evaluated against U-937 non-Hodgkin's lymphoma and the HL-60, SUP-B15, and K-562 leukemia cell lines. The free ligands induced in all cell lines, if at all, only marginal, concentration-dependent growth inhibitory effects, and did not trigger Cu/Zn superoxide dismutase (Cu/Zn SOD) release or induce apoptosis. [Fe(II) (salophene)] (3) and [Fe(III) (salophene)Cl] (4) blocked cellular growth, caused a strong release of Cu/Zn SOD and induced apoptosis. In contrast, the manganese analogs [Mn(II) (salophene)] (5) and [Mn(III) (salophene)OAc] (6) inhibited cell growth, caused the programmed cell death only at higher concentrations and did not provoke release of Cu/Zn SOD in any of the four cell lines. Weaker cell death-promoting effects were observed when the salophene moiety of 3 and 4 was replaced with saldach (complexes 7 and 8), indicating the influence exerted by the ligand structure. In conclusion, Schiff base transition metal complexes induce strong inhibitory effects on human lymphoma and leukemia cells.
席夫碱过渡金属配合物是一类具有很大治疗干预潜力的重要化合物。然而,这些配合物的抗白血病和抗淋巴瘤作用的数据有限。N,N'-双(水杨醛基)-1,2-苯二胺(水杨醛,1)及其铁(II/III)和锰(II/III)配合物、rac-trans-N,N'-双(水杨醛基)-1,2-环己二胺(水杨达嗪,2)及其相应的铁(II/III)配合物的活性针对 U-937 非霍奇金淋巴瘤和 HL-60、SUP-B15 和 K-562 白血病细胞系进行了评估。游离配体在所有细胞系中,如果有的话,仅诱导轻微的、浓度依赖性的生长抑制作用,并且不会触发 Cu/Zn 超氧化物歧化酶(Cu/Zn SOD)释放或诱导细胞凋亡。[Fe(II)(水杨醛)](3)和[Fe(III)(水杨醛)Cl](4)阻断细胞生长,引起 Cu/Zn SOD 的强烈释放并诱导细胞凋亡。相比之下,锰类似物[Mn(II)(水杨醛)](5)和[Mn(III)(水杨醛)OAc](6)抑制细胞生长,仅在较高浓度下引起程序性细胞死亡,并且在四个细胞系中均不会引发 Cu/Zn SOD 的释放。当 3 和 4 的水杨醛部分被水杨达嗪取代时(配合物 7 和 8),观察到较弱的促进细胞死亡的作用,这表明配体结构的影响。总之,席夫碱过渡金属配合物对人淋巴瘤和白血病细胞具有强烈的抑制作用。