Boron tracedrug : design, synthesis, and pharmacological activity of phenolic BODIPY-containing antioxidants as traceable next-generation drug model

Boron tracedrug : design, synthesis, and pharmacological activity of phenolic BODIPY-containing antioxidants as traceable next-generation drug model
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硼示踪药物:含 BODIPY 的酚类抗氧化剂作为可追溯的下一代药物模型的设计、合成和药理活性

DOI:
10.1007/978-1-4614-1566-4_44
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发表时间:
2012
期刊:
影响因子:
--
通讯作者:
Hori H
Hori H
中科院分区:
医学4区
文献类型:
--
作者:
Nakata E;Koizumi M;Yamashita Y;Uto Y;Hori H

文献摘要

相似文献

我们设计并合成了含酚BODIPY的抗氧化剂作为可追踪的下一代药物模型,命名为硼示踪剂UTX-42、UTX-43和UTX-44。这些药物基本上由酚类抗氧化剂部分和稳定的含硼BODIPY部分组成。通过ABTS自由基阳离子光谱分析和对大鼠肝线粒体脂质过氧化的抑制活性评价了它们的抗氧化活性。它们与ABTS自由基阳离子的反应性显示出高于trolox,这是众所周知的抗氧化剂之一。这些微量药物,特别是UTX-44,也显示出比trolox对RLM脂质过氧化更高的抑制活性。这些结果表明,UTX-44在这些药物中具有最有效的含硼抗氧化剂。
We designed and synthesized phenolic BODIPY-containing antioxidants as traceable next-generation drug model named boron tracedrugs, UTX-42, UTX-43, and UTX-44. These drugs are basically composed of phenolic antioxidant moiety and stable boron-containing BODIPY moiety. Their antioxidant activities were evaluated by spectroscopic analysis with ABTS radical cations and inhibitory activity on lipid peroxidation of rat liver mitochondria. The reactivity of them with ABTS radical cations showed to be higher than trolox, which is one of the well-known antioxidants. These trace drugs, especially UTX-44, also showed much higher inhibitory activity than trolox against RLM lipid peroxidation. These results demonstrated that UTX-44 had the most potent boron-containing antioxidant among these drugs.