Division of Redox Regulation, DKFZ-ZMBH Alliance, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120 Heidelberg, Germany.
Division of Redox Regulation, DKFZ-ZMBH Alliance, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120 Heidelberg, Germany; Faculty of Biosciences, Heidelberg University, 69120 Heidelberg, Germany.
Pharmacol Ther. 2021 Dec;228:107916. doi: 10.1016/j.pharmthera.2021.107916. Epub 2021 Jun 23.
Initially adopted as a mucolytic about 60 years ago, the cysteine prodrug N-acetylcysteine (NAC) is the standard of care to treat paracetamol intoxication, and is included on the World Health Organization's list of essential medicines. Additionally, NAC increasingly became the epitome of an "antioxidant". Arguably, it is the most widely used "antioxidant" in experimental cell and animal biology, as well as clinical studies. Most investigators use and test NAC with the idea that it prevents or attenuates oxidative stress. Conventionally, it is assumed that NAC acts as (i) a reductant of disulfide bonds, (ii) a scavenger of reactive oxygen species and/or (iii) a precursor for glutathione biosynthesis. While these mechanisms may apply under specific circumstances, they cannot be generalized to explain the effects of NAC in a majority of settings and situations. In most cases the mechanism of action has remained unclear and untested. In this review, we discuss the validity of conventional assumptions and the scope of a newly discovered mechanism of action, namely the conversion of NAC into hydrogen sulfide and sulfane sulfur species. The antioxidative and cytoprotective activities of per- and polysulfides may explain many of the effects that have previously been ascribed to NAC or NAC-derived glutathione.
最初作为黏液溶解剂使用,大约 60 年前,半胱氨酸前体药物 N-乙酰半胱氨酸(NAC)被用作对乙酰氨基酚中毒的标准治疗方法,也被列入世界卫生组织的基本药物清单。此外,NAC 越来越成为“抗氧化剂”的代名词。可以说,它是实验细胞和动物生物学以及临床研究中使用最广泛的“抗氧化剂”。大多数研究人员使用和测试 NAC 的想法是,它可以预防或减轻氧化应激。传统上,人们认为 NAC 可以作为(i)二硫键的还原剂,(ii)活性氧物质的清除剂和/或(iii)谷胱甘肽生物合成的前体。虽然这些机制在特定情况下可能适用,但它们不能被概括为解释 NAC 在大多数情况下的作用。在大多数情况下,其作用机制仍不清楚,也未经检验。在这篇综述中,我们讨论了传统假设的有效性以及一种新发现的作用机制的范围,即 NAC 转化为硫化氢和硫烷硫物种。过硫化物和多硫化物的抗氧化和细胞保护活性可以解释许多以前归因于 NAC 或 NAC 衍生的谷胱甘肽的作用。
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