Phenethyl Isothiocyanate, a Dual Activator of Transcription Factors NRF2 and HSF1,Molecular Nutrition & Food Research

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Phenethyl Isothiocyanate, a Dual Activator of Transcription Factors NRF2 and HSF1
Molecular Nutrition & Food Research ( IF 4.5 ) Pub Date : 2018-06-19 , DOI: 10.1002/mnfr.201700908
Sharadha Dayalan Naidu _{1,

2} , Takafumi Suzuki ₃ , Masayuki Yamamoto ₃ , Jed W Fahey _{1,

2,

4,

5} , Albena T Dinkova-Kostova _{1,

2,

4,

6}

Affiliation

Cruciferous vegetables are rich sources of glucosinolates which are the biogenic precursor molecules of isothiocyanates (ITCs). The relationship between the consumption of cruciferous vegetables and chemoprotection has been widely documented in epidemiological studies. Phenethyl isothiocyanate (PEITC) occurs as its glucosinolate precursor gluconasturtiin in the cruciferous vegetable watercress (Nasturtium officinale). PEITC has multiple biological effects, including activation of cytoprotective pathways, such as those mediated by the transcription factor nuclear factor erythroid 2 p45‐related factor 2 (NRF2) and the transcription factor heat shock factor 1 (HSF1), and can cause changes in the epigenome. However, at high concentrations, PEITC leads to accumulation of reactive oxygen species and cytoskeletal changes, resulting in cytotoxicity. Underlying these activities is the sulfhydryl reactivity of PEITC with cysteine residues in its protein targets. This chemical reactivity highlights the critical importance of the dose of PEITC for achieving on‐target selectivity, which should be carefully considered in the design of future clinical trials.

中文翻译：

异硫氰酸苯乙酯，转录因子 NRF2 和 HSF1 的双重激活剂

十字花科蔬菜富含芥子油苷，芥子油苷是异硫氰酸盐 (ITC) 的生物前体分子。流行病学研究中已广泛记录了食用十字花科蔬菜与化学保护之间的关系。异硫氰酸苯乙酯 (PEITC) 在十字花科蔬菜西洋菜 ( Nasturtium officinale ) 中以其芥子油苷前体葡糖苷 (gluconasturtiin) 的形式存在。 PEITC 具有多种生物学效应，包括激活细胞保护途径，例如由转录因子核因子红细胞 2 p45 相关因子 2 (NRF2) 和转录因子热休克因子 1 (HSF1) 介导的效应，并可引起表观基因组。然而，在高浓度下，PEITC 会导致活性氧的积累和细胞骨架的变化，从而产生细胞毒性。这些活性的基础是 PEITC 与其蛋白质靶标中的半胱氨酸残基的巯基反应性。这种化学反应性凸显了 PEITC 剂量对于实现靶向选择性的至关重要性，在未来临床试验的设计中应仔细考虑这一点。

更新日期：2018-06-19

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