中文摘要：由于黄曲霉毒素是人畜健康的严重威胁，它们污染食品的问题就构成了目前社会紧急情况。另一方面，还包括了杀虫剂的使用，因为它会长期残留在食品及环境中。本研究提出基于缩氨基硫脲支架的系列螯合配体的合成，评价其抗菌和抑毒的作用。研究结果突出了评价作为作物保护剂研发的抗性物质的安全性的重要性，同时胺苯硫脲支架是发展产黄曲霉毒素菌株抑制剂的良好起点。
外文摘要： The issue of food contamination by aflatoxins presently constitutes a social emergency, since they represent a severe risk for human and animal health. On the other hand, the use of pesticides has to be contained, since this generates long term residues in food and in the environment. Here we present the synthesis of a series of chelating ligands based on the thiosemicarbazone scaffold, to be evaluated for their antifungal and antiaflatoxigenic effects. Starting from molecules of natural origin of known antifungal properties, we introduced the thio-group and then the corresponding copper complexes were synthesised. Some molecules highlighted aflatoxin inhibition in the range 67-92% at 100 mu M. The most active compounds were evaluated for their cytotoxic effects on human cells. While all the copper complexes showed high cytotoxicity in the micromolar range, one of the ligand has no effect on cell proliferation. This hit was chosen for further analysis of mutagenicity and genotoxicity on bacteria, plants and human cells. Analysis of the data underlined the importance of the safety profile evaluation for hit compounds to be developed as crop-protective agents and at the same time that the thiosemicarbazone scaffold represents a good starting point for the development of aflatoxigenic inhibitors.
作者：Rogolino, D；Gatti, A；Carcelli, M；Pelosi, G；Bisceglie, F；Restivo, FM；Degola, F；Buschini, A；Montalbano, S；Feretti, D；Zani, C
作者单位：Univ Parma
期刊名称：SCIENTIFIC REPORTS
期刊影响因子：5.228
出版年份：2017
出版刊次：-
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