Michl Carina, Vivarelli Fabio, Weigl Julia, De Nicola Gina Rosalinda, Canistro Donatella, Paolini Moreno, Iori Renato, Rascle Anne
Stat5 Signaling Research Group, Institute of Immunology, University of Regensburg, Regensburg, Germany.
Molecular toxicology unit, Department of Pharmacy and Biotechnology, University of Bologna, Bologna, Italy.
PLoS One. 2016 Jun 15;11(6):e0157430. doi: 10.1371/journal.pone.0157430. eCollection 2016.
Sulforaphane (SFN) and moringin (GMG-ITC) are edible isothiocyanates present as glucosinolate precursors in cruciferous vegetables and in the plant Moringa oleifera respectively, and recognized for their chemopreventive and medicinal properties. In contrast to the well-studied SFN, little is known about the molecular pathways targeted by GMG-ITC. We investigated the ability of GMG-ITC to inhibit essential signaling pathways that are frequently upregulated in cancer and immune disorders, such as JAK/STAT and NF-κB. We report for the first time that, similarly to SFN, GMG-ITC in the nanomolar range suppresses IL-3-induced expression of STAT5 target genes. GMG-ITC, like SFN, does not inhibit STAT5 phosphorylation, suggesting a downstream inhibitory event. Interestingly, treatment with GMG-ITC or SFN had a limited inhibitory effect on IFNα-induced STAT1 and STAT2 activity, indicating that both isothiocyanates differentially target JAK/STAT signaling pathways. Furthermore, we showed that GMG-ITC in the micromolar range is a more potent inhibitor of TNF-induced NF-κB activity than SFN. Finally, using a cellular system mimicking constitutive active STAT5-induced cell transformation, we demonstrated that SFN can reverse the survival and growth advantage mediated by oncogenic STAT5 and triggers cell death, therefore providing experimental evidence of a cancer chemopreventive activity of SFN. This work thus identified STAT5, and to a lesser extent STAT1/STAT2, as novel targets of moringin. It also contributes to a better understanding of the biological activities of the dietary isothiocyanates GMG-ITC and SFN and further supports their apparent beneficial role in the prevention of chronic illnesses such as cancer, inflammatory diseases and immune disorders.
萝卜硫素(SFN)和辣木素(GMG - ITC)是可食用的异硫氰酸盐,分别作为十字花科蔬菜和辣木植物中硫代葡萄糖苷前体存在,并因其化学预防和药用特性而闻名。与研究充分的SFN相比,关于GMG - ITC靶向的分子途径知之甚少。我们研究了GMG - ITC抑制癌症和免疫疾病中经常上调的关键信号通路的能力,如JAK/STAT和NF - κB。我们首次报道,与SFN类似,纳摩尔范围内的GMG - ITC可抑制IL - 3诱导的STAT5靶基因表达。GMG - ITC与SFN一样,不抑制STAT5磷酸化,表明是下游抑制事件。有趣的是,用GMG - ITC或SFN处理对IFNα诱导的STAT1和STAT2活性的抑制作用有限,表明这两种异硫氰酸盐对JAK/STAT信号通路的靶向作用不同。此外,我们表明微摩尔范围内的GMG - ITC比SFN更有效地抑制TNF诱导的NF - κB活性。最后,使用模拟组成型活性STAT5诱导的细胞转化的细胞系统,我们证明SFN可以逆转致癌性STAT5介导的存活和生长优势并触发细胞死亡,因此提供了SFN癌症化学预防活性的实验证据。这项工作因此确定STAT5以及在较小程度上的STAT1/STAT2是辣木素的新靶点。它还有助于更好地理解膳食异硫氰酸盐GMG - ITC和SFN的生物学活性,并进一步支持它们在预防癌症、炎症性疾病和免疫疾病等慢性疾病方面的明显有益作用。