Automated evaluation of pharmaceutically active ionic liquids鈥?(eco)toxicity through the inhibition of human carboxylesterase and Vibrio fischeri

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• 作者：Susana P.F. Costa ; Vanessa D. Justina ; Katharina Bica ; Maria Vasiloiu ; Paula C.A.G. Pinto ; M. L煤cia M.F.S. Saraiva
• 关键词：ILs ; ionic liquids ; IL-APIs ; pharmaceutical active ionic liquids ; APIs ; active pharmaceutical ingredients ; SIA ; sequential injection analysis ; HCE ; human carboxylesterase ; MUA ; 4-methylumbeliferyl acetate ; BACl ; benzalkonium chloride ; BASal ; benzalkonium salicylate ; BETf2N ; benzethonium bistriflimide ; BECl ; benzethonium chloride ; BED ; benzethonium docusate ; BESal ; benzethonium salicylate ; CetPyCl ; cetylpyridinium chloride ; CetPySal ; cetylpyridinium salicylate ; emimCl ; 1-ethyl-3-methyl-imidazoliu
• 刊名：Journal of Hazardous Materials
• 出版年：30 January, 2014
• 年：2014
• 卷：265
• 期：Complete
• 页码：133-141
• 全文大小：900 K

文摘

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.