Albertini R, Gasparri Fava G, Pinelli S, Tarasconi P, Starcich B
Istituto di Patologia Speciale Medica, Università degli Studi di Parma.
Boll Soc Ital Biol Sper. 1991 Jul;67(7):673-80.
Thiosemicarbazones are a wide group of organic derivatives whose biological activities are a function of the parent aldehyde or ketone and of the coordination metal type. Some thiosemicarbazones possess a broad spectrum of potentially useful chemotherapeutic properties (antitumor, antibacterial, antiviral, antimalarial). The present study reports the biological effects of pyridoxal thiosemicarbazone, H2L, and relative complexes with copper, [(Cu(HL)(OH2))2]++ and with cobalt, [Co(III)(L)(HL)] on the differentiation of Friend erythroleukemia cells (FLC). They are murine proerythroblasts chronically infected by a producing Friend leukemia virus complex; their exposure to dimethylsulfoxide (Me2SO) or other chemical agents induces these cells to terminal erythroid differentiation, therefore these cells represent a good model of differentiation in vitro. Here we describe induction differentiation experiment of pyridoxal thiosemicarbazone and relative complexes of copper and cobalt on FLC performed with concentrations of 50 ug/ml (ligand), 2 ug/ml (complexes). These have little effects on cell proliferation at doses used in these experiments. Higher doses have evident cytotoxic effects. The treatment with the copper complex induces a moderate differentiation of FLC and enhances effects on erythroid differentiation of Me2SO-induced FLC. On the contrary H2L and [Co(III)(L)(HL)] haven't inducing effects or enhancing effects on Me2SO-induced FLC hemopoietic differentiation. In conclusion, the present study shows that copper complexes of pyridoxal thiosemicarbazone exert action of inducing agent and are able to enhance Me2SO-induced FLC hemopoietic differentiation.
硫代氨基脲是一大类有机衍生物,其生物活性取决于母体醛或酮以及配位金属类型。一些硫代氨基脲具有广泛的潜在有用的化疗特性(抗肿瘤、抗菌、抗病毒、抗疟疾)。本研究报告了吡哆醛硫代氨基脲(H2L)以及与铜形成的配合物[(Cu(HL)(OH2))2]++和与钴形成的配合物[Co(III)(L)(HL)]对Friend红白血病细胞(FLC)分化的生物学效应。它们是长期感染产生Friend白血病病毒复合物的小鼠早幼红细胞;将它们暴露于二甲基亚砜(Me2SO)或其他化学试剂会诱导这些细胞向终末红细胞分化,因此这些细胞代表了体外分化的良好模型。在此我们描述了用50μg/ml(配体)、2μg/ml(配合物)浓度的吡哆醛硫代氨基脲及其铜和钴的相关配合物对FLC进行的诱导分化实验。在这些实验中使用的剂量下,它们对细胞增殖影响很小。更高剂量有明显的细胞毒性作用。用铜配合物处理可诱导FLC适度分化,并增强对Me2SO诱导的FLC红细胞分化的影响。相反,H2L和[Co(III)(L)(HL)]对Me2SO诱导的FLC造血分化没有诱导作用或增强作用。总之,本研究表明吡哆醛硫代氨基脲的铜配合物发挥诱导剂作用,并且能够增强Me2SO诱导的FLC造血分化。