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首页> 外文学位 >Determination of Synergistic Antioxidant Activity of alpha- and delta-Tocopherylcarbamate Co-drugs on Lipid Peroxidation in Skin.
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Determination of Synergistic Antioxidant Activity of alpha- and delta-Tocopherylcarbamate Co-drugs on Lipid Peroxidation in Skin.

机译：确定α-和δ-生育酚氨基甲酸酯副药对皮肤脂质过氧化的协同抗氧化活性。

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摘要

Topical antioxidant (AO) co-drugs, derived from tocopherol (&agr;- and delta-TOC) and lipoylamine (LAM) that are designed to protect the skin against oxidative damage were synthesized. The activity of the carbamate co-drugs were tested for potency against lipid peroxidation (LP) in skin using the thiobarbituric acid reactive substances (TBARS) assay. The ability of the co-drugs and their parent compounds to inhibit LP in porcine skin homogenates after treatment with ferrous sulfate (FeSO4) as the inducer of oxidation was evaluated by measuring the production of malondialdehyde (MDA). Experiments were carried out to confirm that TOC and LAM, the parent compounds of the co-drugs act synergistically to inhibit LP. Penetration and hydrolysis of the carbamate co-drugs in the epidermal (ED) layer of skin was evaluated on intact porcine skin, using Franz diffusion cells and high pressure liquid chromatography (HPLC). Hydrolysis of the co-drugs was evaluated since it is required for optimal AO activity. Following this, the skin was exposed to UVR in order to induce oxidation. AO activity against UVR-induced LP in the ED layer of the intact skin, after treatment with the co-drugs was assessed using the TBARS assay. Potent, synergistic AO activity was observed for &agr;-TOC and LAM and delta-TOC and LAM. Carbamate co-drugs showed potent AO activity, which was a virtue of partial hydrolysis of to the parent compounds, TOC and LAM and the synergism that existed between these parent compounds. HPLC data suggested that these co-drugs penetrated the ED layer and the extent of hydrolysis was found comparable to the observed AO activity. delta-Tocopherol carbamate (delta-TOCCAM) showed more potent AO activity than &agr;- tocopherol carbamate (&agr;- TOCCAM). The enhanced activity of delta-TOCCAM is attributed to greater of hydrolysis relative to the &agr;-analog. Altogether, these data suggest that carbamate co-drugs are potent inhibitors of LP and may offer protection against UVR-induced oxidative damage in the skin.
机译：合成了衍生自生育酚（α-和δ-TOC）和脂酰胺（LAM）的局部抗氧化剂（AO）副药，它们旨在保护皮肤免受氧化损伤。使用硫代巴比妥酸反应性物质（TBARS）分析测试了氨基甲酸酯副药的活性，以评估其抗皮肤脂质过氧化（LP）的能力。通过测量丙二醛（MDA）的产生，评估了共同药物及其母体化合物在用硫酸亚铁（FeSO4）作为氧化诱导剂处理后抑制猪皮肤匀浆中LP的能力。进行实验以确认TOC和LAM（共同药物的母体化合物）具有协同作用以抑制LP。使用Franz扩散池和高压液相色谱（HPLC）在完整的猪皮肤上评估了皮肤表皮（ED）层中氨基甲酸酯类辅药的渗透和水解。评估辅助药物的水解，因为这是最佳AO活性所必需的。此后，将皮肤暴露于UVR以诱导氧化。使用TBARS分析评估了在共用药物治疗后，完整皮肤ED层中针对UVR诱导的LP的AO活性。对于α-TOC和LAM以及δ-TOC和LAM观察到有效的协同AO活性。氨基甲酸酯类药物显示出强大的AO活性，这是母体化合物TOC和LAM部分水解以及这些母体化合物之间存在协同作用的结果。 HPLC数据表明，这些副药穿透了ED层，发现水解程度与观察到的AO活性相当。 δ-生育酚氨基甲酸酯（delta-TOCCAM）显示出比α-生育酚氨基甲酸酯（α-TOCCAM）更强的AO活性。相对于α-类似物，δ-TOCCAM活性增强归因于更大的水解。总而言之，这些数据表明氨基甲酸酯共同药物是LP的有效抑制剂，可以提供抗UVR诱导的皮肤氧化损伤的保护作用。

著录项

  • 作者

    Purohit, Drusha.;

  • 作者单位

    Albany College of Pharmacy and Health Sciences.;

  • 授予单位 Albany College of Pharmacy and Health Sciences.;
  • 学科 Health Sciences Pharmacy.
  • 学位 M.S.
  • 年度 2014
  • 页码 74 p.
  • 总页数 74
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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