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白藜芦醇启发的苯并[b]硒吩类化合物在酵母中作为抗氧化剂。

Resveratrol-Inspired Benzo[b]selenophenes Act as Anti-Oxidants in Yeast.

机构信息

Department of Genetics, Cancer Research Institute, Biomedical Research Center, Slovak Academy of Sciences, Dúbravská Cesta 9, 845 05 Bratislava, Slovakia.

Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.

出版信息

Molecules. 2018 Feb 24;23(2):507. doi: 10.3390/molecules23020507.

DOI:10.3390/molecules23020507
PMID:29495287
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6017489/
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[]selenophenes-have been studied in lower eukaryotes . 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[]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[]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[]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[]selenophenes could be used as supra-anti-oxidant supplements.

摘要

白藜芦醇是一种天然(多)酚,主要存在于植物中,用于保护它们免受病原体以及物理和化学因素的有害影响。在高等真核细胞和生物中,该化合物表现出广泛的生物学活性,如抗氧化、抗炎、抗癌、抗老化、心脏和神经保护特性。在这里,研究了白藜芦醇-苯并[]硒吩的合成含硒衍生物在较低等真核生物中的生物活性。通过它们作为氧化还原活性抗微生物剂的能力,研究了它们的毒性以及损伤 DNA 和诱导活性氧 (ROS) 的能力。我们表明,一些苯并[]硒吩可以杀死酵母细胞,并且杀伤作用不是通过可以检测到 DNA 双链断裂的 DNA 损伤类型介导的。这些苯并[]硒吩可能可被用作抗真菌剂,尽管需要进一步评估其在人类中应用的相关浓度。此外,大多数研究的苯并[]硒吩表现出氧化还原调节/抗氧化活性(与白藜芦醇或 Trolox 相当或更高),导致酵母细胞内 ROS 水平降低。因此,在其他生物系统中进行仔细重新评估后,这些观察结果可能会转移到人类身上,在那里,受白藜芦醇启发的苯并[]硒吩可以用作超抗氧化补充剂。

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