REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto, Portugal.
Vienna University of Technology, Institute of Applied and Synthetic Chemistry, A-1060 Vienna, Austria.
J Hazard Mater. 2014 Jan 30;265:133-41. doi: 10.1016/j.jhazmat.2013.11.052. Epub 2013 Dec 1.
The toxicity of 16 pharmaceutical active ionic liquids (IL-APIs) was evaluated by automated approaches based on sequential injection analysis (SIA). The implemented bioassays were centered on the inhibition of human carboxylesterase 2 and Vibrio fischeri, in the presence of the tested compounds. The inhibitory effects were quantified by calculating the inhibitor concentration required to cause 50% of inhibition (EC50). The EC50 values demonstrated that the cetylpyridinium group was one of the most toxic cations and that the imidazolium group was the less toxic. The obtained results provide important information about the safety of the studied IL-APIs and their possible use as pharmaceutical drugs. The developed automated SIA methodologies are robust screening bioassays, and can be used as a generic tools to identify the (eco)toxicity of the structural elements of ILs, contributing to a sustainable development of drugs.
采用基于顺序注射分析（SIA）的自动化方法评估了 16 种药物活性离子液体（IL-APIs）的毒性。所实施的生物测定集中在抑制人羧酸酯酶 2 和发光菌上，同时存在测试化合物。通过计算引起 50%抑制的抑制剂浓度（EC50）来定量抑制作用。EC50 值表明，十六烷基吡啶基团是毒性最大的阳离子之一，而咪唑基团的毒性最小。所获得的结果提供了有关研究 IL-APIs 安全性及其作为药物使用的可能性的重要信息。开发的自动化 SIA 方法是稳健的筛选生物测定法，可以用作识别 IL 结构元素的毒性的通用工具，有助于药物的可持续发展。
