Dip.to di Chimica, University of Torino, Via Giuria 7, I-10125 Torino, Italy.
J Inorg Biochem. 2013 Nov;128:26-37. doi: 10.1016/j.jinorgbio.2013.07.015. Epub 2013 Jul 18.
Vanadium compounds are known to display a number of therapeutic effects, namely insulin-mimetic and cardiovascular effects. Evidence of the antiproliferative and proapoptotic activity of a number of vanadyl complexes, together with their low toxicity, establishes these metal compounds as promising antitumoral therapeutic agents. In the present work, we describe the synthesis and full characterization of six new vanadyl complexes with acetylacetonate derivatives bearing asymmetric substitutions on the β-dicarbonyl moiety: the complexes were characterized in the solid state as well as in solution. Our results show that all complexes are in square pyramidal geometry; cis isomers in the equatorial plane are favored in the presence of strongly coordinating solvents. EPR evidence suggests that all complexes are in the bis-chelate form, although in two cases the mono-chelated complex seems to be present as well. Preliminary tests carried out on non-tumor and tumor cell lines show that these complexes are effective in suppressing cell viability and elicit a distinct response of tumor and non-tumor cells.
钒化合物具有多种治疗作用,包括胰岛素模拟和心血管作用。许多氧钒配合物具有抗增殖和促凋亡活性,且毒性低,这使这些金属化合物成为很有前途的抗肿瘤治疗剂。在本工作中,我们描述了六种新的氧钒配合物的合成和全谱表征,这些配合物带有β-二羰基部分的不对称取代基的乙酰丙酮衍生物:这些配合物在固态和溶液中都进行了表征。我们的结果表明,所有配合物均为四方锥几何构型;在强配位溶剂存在下,有利于形成平面的顺式异构体。EPR 证据表明,所有配合物均为双螯合形式,但在两种情况下,似乎也存在单螯合配合物。在非肿瘤和肿瘤细胞系上进行的初步测试表明,这些配合物能有效抑制细胞活力,并对肿瘤和非肿瘤细胞产生明显的反应。