Center for BioEnergetics, Biodesign Institute, Arizona State University, Tempe, Arizona 85287-2904, USA.
J Nat Prod. 2012 Dec 28;75(12):2209-15. doi: 10.1021/np3007099. Epub 2012 Nov 28.
The synthesis of benzoquinone natural product 2 and three analogues is described. The synthesized compounds were tested for their ability to protect Friedreich's ataxia (FRDA) lymphocytes from induced oxidative stress. One of the analogues (3) conferred cytoprotection in a dose-dependent manner in FRDA lymphocytes at micromolar concentrations. The biological assays suggest that the modification of the 2-hydroxy and N-(3-carboxypropyl) groups in the natural product can improve its antioxidant activity and significantly enhance its ability to protect mitochondrial function under conditions of oxidative stress.
本文描述了苯醌天然产物 2 及其三个类似物的合成。测试了合成化合物保护弗里德里希共济失调症（FRDA）淋巴细胞免受诱导性氧化应激的能力。其中一个类似物（3）以剂量依赖的方式在微摩尔浓度下在 FRDA 淋巴细胞中具有细胞保护作用。生物测定表明，天然产物中 2-羟基和 N-（3-羧丙基）基团的修饰可以提高其抗氧化活性，并显著增强其在氧化应激条件下保护线粒体功能的能力。
