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Synthesis and Bioactivity Profile of 5-S-Lipoylhydroxytyrosol-Based Multidefense Antioxidants with a Sizeable (Poly)sulfide Chain

机译:合成和生物活性

摘要

Novel polyfunctionalized antioxidants, 5-S-lipoylhydroxytyrosol (1) and its disulfide 2, trisulfide 3, and tetrasulfide 4, were prepd. from tyrosol and dihydrolipoic acid in the presence, when appropriate, of sulfur. Compd. 1 exhibited significant activity in the ferric reducing/antioxidant power (FRAP) assay (1.60 Trolox equiv), whereas polysulfides 2-4 were more efficient in the DPPH redn. assay (88-93% redn. vs 68% by Trolox). At 10 μM concn., all compds. 1-4 proved to be efficient hydroxyl radical scavengers (56-69% inhibition) in a Fenton reaction assay. When administered to human HepG2 cells, 1-4 proved to be nontoxic and exhibited marked protective effects against reactive oxygen species (ROS) generation (60-84% inhibition at 1 μM concn.) and cell damage induced by 400 μM tert-butylhydroperoxide. All compds. 1-4 exhibited overall greater antioxidant activity than hydroxytyrosol.
机译:制备了新型的多官能抗氧化剂5-S-脂酰羟基酪醇(1)及其二硫化物2,三硫化物3和四硫化物4。在适当的情况下,在硫存在下,从酪醇和二氢硫辛酸中提取。编译图1的样品在铁还原/抗氧化能力(FRAP)分析中显示出显着的活性(1.60 Trolox当量),而多硫化物2-4在DPPH氧化还原中更有效。分析(88-93%的还原,而Trolox的68%)。所有浓度均为10μM。在Fenton反应测定中,1-4被证明是有效的羟基自由基清除剂(抑制56-69%)。当对人类HepG2细胞给药时,1-4被证明是无毒的,并且对活性氧(ROS)生成(在1μM浓度下抑制60-84%)和400μM叔丁基过氧化氢诱导的细胞损伤表现出显着的保护作用。所有compds。 1-4表现出比羟基酪醇总体上更大的抗氧化活性。

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