Department of General Biophysics, Faculty of Biology and Environmental Protection, University of Łódź, Pomorska 141/143, 90-236 Łódź, Poland.
Cell Mol Biol Lett. 2013 Sep;18(3):459-78. doi: 10.2478/s11658-013-0100-5. Epub 2013 Jul 26.
Dendrimers containing viologen (derivatives of 4,4'-bipyridyl) units in their structure have been demonstrated to exhibit antiviral activity against human immunodeficiency virus (HIV-1). It has also recently been revealed that novel dendrimers with both viologen units and phosphorus groups in their structure show different antimicrobial, cytotoxic and hemotoxic properties, and have the ability to influence the activity of cholinesterases and to inhibit α-synuclein fibrillation. Since the influence of viologen-phosphorus structures on basic cellular processes had not been investigated, we examined the impact of such macromolecules on the murine neuroblastoma cell line (N2a). We selected three water-soluble viologen-phosphorus (VPD) dendrimers, which differ in their core structure, number of viologen units and number and type of surface groups, and analyzed several aspects of the cellular response. These included cell viability, generation of reactive oxygen species (ROS), alterations in mitochondrial activity, morphological modifications, and the induction of apoptosis and necrosis. The MTT assay results suggest that all of the tested dendrimers are only slightly cytotoxic. Although some changes in ROS formation and mitochondrial function were detected, the three compounds did not induce apoptosis or necrosis. In light of these results, we can assume that the tested VPD are relatively safe for mouse neuroblastoma cells. Although more research on their safety is needed, VPD seem to be promising nanoparticles for further biomedical investigation.
树状聚合物中含有二茂铁（4,4'-联吡啶的衍生物）单元，已被证明具有抗人类免疫缺陷病毒（HIV-1）的抗病毒活性。最近还发现，具有二茂铁单元和磷基团的新型树状聚合物具有不同的抗菌、细胞毒性和血液毒性特性，并且能够影响胆碱酯酶的活性并抑制α-突触核蛋白的纤维化。由于尚未研究二茂铁-磷结构对基本细胞过程的影响，我们研究了此类大分子对小鼠神经母细胞瘤细胞系（N2a）的影响。我们选择了三种水溶性二茂铁-磷（VPD）树状聚合物，它们在核心结构、二茂铁单元数量以及表面基团的数量和类型上有所不同，并分析了细胞反应的几个方面。这些方面包括细胞活力、活性氧（ROS）的产生、线粒体活性的改变、形态学改变以及细胞凋亡和坏死的诱导。MTT 测定结果表明，所有测试的树状聚合物的细胞毒性都非常低。尽管检测到 ROS 形成和线粒体功能的一些变化，但这三种化合物并未诱导细胞凋亡或坏死。根据这些结果，我们可以假设测试的 VPD 对小鼠神经母细胞瘤细胞相对安全。尽管需要对其安全性进行更多研究，但 VPD 似乎是用于进一步生物医学研究的有前途的纳米颗粒。
