Abstract
Resveratrol is a natural (poly)phenol primarily found in plants protecting them against pathogens, as well as harmful effects of physical and chemical agents. In higher eukaryotic cells and organisms, this compound displays a remarkable range of biological activities, such as anti-oxidant, anti-inflammatory, anti-cancer, anti-aging, cardio- and neuro-protective properties. Here, biological activities of synthetic selenium-containing derivatives of resveratrol—benzo[b]selenophenes—have been studied in lower eukaryotes Saccharomyces cerevisiae. Their toxicity, as well as DNA damaging and reactive oxygen species (ROS) inducing potencies, manifested through their ability to act as redox active anti-microbial agents, have been examined. We show that some benzo[b]selenophenes can kill yeast cells and that the killing effects are not mediated by DNA damage types that can be detected as DNA double-strand breaks. These benzo[b]selenophenes could potentially be used as anti-fungal agents, although their concentrations relevant to application in humans need to be further evaluated. In addition, most of the studied benzo[b]selenophenes display redox-modulating/anti-oxidant activity (comparable or even higher than that of resveratrol or Trolox) causing a decrease in the intracellular ROS levels in yeast cells. Therefore, after careful re-evaluation in other biological systems these observations might be transferred to humans, where resveratrol-inspired benzo[b]selenophenes could be used as supra-anti-oxidant supplements.
Highlights
Free radicals and other reactive oxygen species (ROS) are historically considered as harmful molecules playing a role, besides aging, in more than 100 human pathologies including cancer, stroke, Alzheimer’s and Parkinson’s diseases, cardiovascular and neurodegenerative diseases, and arthritis and diabetes [1,2]
Toxicity of Benzo[b]selenophenes Measured by Spot Test
Biological activity of the selected group of benzo[b]selenophenes, synthesis of which was inspired by the structure of resveratrol, was examined in terms of the toxic effects and the ability to induce
Summary
Free radicals and other reactive oxygen species (ROS) are historically considered as harmful molecules playing a role, besides aging, in more than 100 human pathologies including cancer, stroke, Alzheimer’s and Parkinson’s diseases, cardiovascular and neurodegenerative diseases, and arthritis and diabetes [1,2]. These molecules contain one or more unpaired electron and are highly reactive to compensate this deficiency. One of the endogenous ROS—superoxide (O2 − )—is produced in mitochondria within the oxidative phosphorylation chain and dismutates spontaneously or with the help of superoxide. H2O2 itself is not very reactive, but in the presence of dismutase to like hydrogen is notreactive very reactive, butradical in the presence
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