摘要/Abstract
小分子氢过硫化物(RSSH)具有独特的化学性质, 近年来其生物学活性备受瞩目. 近五年间, 生理或病理条件下即可实现RSSH原位释放供体化合物取得了突破性的进展, 这类供体将成为研究RSSH生理功能、作用机制以及治疗潜能的有力工具. 按照激活模式将现有供体分子分为五类, 即酯酶激活型、ROS(活性氧物种)激活型、pH依赖型、光激活型以及硝基还原酶激活型, 并对各类供体进行综述. 现有供体在细胞水平表现出理想的抗氧化应激活性, 部分供体已经应用于心肌缺血再灌注模型的干预中, 并取得了积极效果. 此外, 还介绍了供体的释放机理及其概念验证过程, 并对供体分子的发展前景进行了展望.
关键词: 氢过硫化物, 供体, 氧化应激, 酯酶, 硫烷硫
The unique chemical structure endowed small-molecular hydropersulfides (RSSH) with unclear but fascinating biological activities, which have been attracted much attention. The donors that could release RSSH smoothlyin situ under physiological or pathological conditions will become powerful chemical tools for exploring the physiological functions, mechanism of action, and potential therapeutic benefit of RSSH. Over the past five years, a substantial breakthrough had been achieved in the design and development of RSSH donors, which is summarized in this perspective. According to the activation patterns, the existing donors are divided into five categories, namely esterase-activated donor, ROS (reactive oxygen species)-activated donor, pH-dependent donor, light-activated donor, and nitroreductase-activated donor. All kinds of donors played ideal roles in improving the oxidative stress at the cellular level, part of which also show a positive therapeutic effect in the context of myocardial ischemia-reperfusion injury. Besides, the related release mechanisms and the proof of concept of the donors are briefly introduced. In the next five years, waves of novel donors are emerging. On one hand, diverse donors, with stable and controllable release rate, clear release process, and identified release components, will be designed. On the other hand, the indispensable toolbox of donors will be fully assembled for more in-depth and comprehensive biological activity researches.
Key words: hydropersulfides, donor, oxidative stress, esterase, sulfane sulfur
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