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

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.

Keywords: Aflatoxins; Antifungal activity; Genotoxicity; Metal complexes; Toxicity.

MeSH terms

  • Antifungal Agents / adverse effects
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • DNA Damage / drug effects
  • Drug Evaluation
  • Drug Evaluation, Preclinical
  • Fungi / drug effects*
  • Fungi / metabolism
  • Humans
  • Microbial Sensitivity Tests
  • Mutagens / adverse effects
  • Mutagens / chemistry
  • Mutagens / pharmacology
  • Mycotoxins / metabolism*
  • Thiosemicarbazones / adverse effects
  • Thiosemicarbazones / chemistry*
  • Thiosemicarbazones / pharmacology*

Substances

  • Antifungal Agents
  • Mutagens
  • Mycotoxins
  • Thiosemicarbazones