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一系列检测作为一种综合方法,用于评估硫代氨基脲衍生物筛选中的真菌和霉菌毒素抑制特性以及细胞毒性/遗传毒性副作用,以便进行优先级排序。

A battery of assays as an integrated approach to evaluate fungal and mycotoxin inhibition properties and cytotoxic/genotoxic side-effects for the prioritization in the screening of thiosemicarbazone derivatives.

作者信息

Zani Claudia, Bisceglie Franco, Restivo Francesco Maria, Feretti Donatella, Pioli Marianna, Degola Francesca, Montalbano Serena, Galati Serena, Pelosi Giorgio, Viola Gaia V C, Carcelli Mauro, Rogolino Dominga, Ceretti Elisabetta, Buschini Annamaria

机构信息

Department of Medical and Surgical Specialities, Radiological Sciences and Public Health, University of Brescia, Italy.

Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Italy; Parma Unit, CIRCMSB (Consorzio Interuniversitario di Ricerca in Chimica dei Metalli nei Sistemi Biologici), Italy.

出版信息

Food Chem Toxicol. 2017 Jul;105:498-505. doi: 10.1016/j.fct.2017.05.008. Epub 2017 May 5.

Abstract

Aflatoxins represent a serious problem for a food economy based on cereal cultivations used to fodder animal and for human nutrition. The aims of our work are two-fold: first, to perform an evaluation of the activity of newly synthesized thiosemicarbazone compounds as antifungal and anti-mycotoxin agents and, second, to conduct studies on the toxic and genotoxic hazard potentials with a battery of tests with different endpoints. In this paper we report an initial study on two molecules: S-4-isopropenylcyclohexen-1-carbaldehydethiosemicarbazone and its metal complex, bis(S-4-isopropenylcyclohexen-1-carbaldehydethiosemicarbazonato)nickel (II). The outcome of the assays on fungi growth and aflatoxin production inhibition show that both molecules possess good antifungal activities, without inducing mutagenic effects on bacteria. From the assays to ascertain that the compounds have no adverse effects on human cells, we have found that they are cytotoxic and, in the case of the nickel compound, they also present genotoxic effects.

摘要

黄曲霉毒素对于以用于喂养动物和人类营养的谷类种植为基础的食品经济而言是一个严重问题。我们工作的目标有两个:第一,评估新合成的硫代半卡巴腙化合物作为抗真菌和抗霉菌毒素剂的活性;第二,通过一系列具有不同终点的测试,对毒性和遗传毒性危害潜力进行研究。在本文中,我们报告了对两种分子的初步研究:S-4-异丙烯基环己烯-1-甲醛硫代半卡巴腙及其金属配合物双(S-4-异丙烯基环己烯-1-甲醛硫代半卡巴腙基)镍(II)。关于真菌生长和黄曲霉毒素产生抑制的测定结果表明,这两种分子都具有良好的抗真菌活性,且不会对细菌产生诱变作用。从确定这些化合物对人类细胞无不良影响的测定中,我们发现它们具有细胞毒性,并且对于镍化合物而言,它们还具有遗传毒性作用。

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