煤焦油诱导特应性皮炎中 AHR 依赖性皮肤屏障修复。
Coal tar induces AHR-dependent skin barrier repair in atopic dermatitis.
机构信息
Department of Dermatology, Radboud University Nijmegen Medical Centre, Nijmegen Centre for Molecular Life Sciences, P.O. Box 9101, Nijmegen 6500 HB, The Netherlands.
出版信息
J Clin Invest. 2013 Feb;123(2):917-27. doi: 10.1172/JCI65642. Epub 2013 Jan 25.
Topical application of coal tar is one of the oldest therapies for atopic dermatitis (AD), a T helper 2 (Th2) lymphocyte-mediated skin disease associated with loss-of-function mutations in the skin barrier gene, filaggrin (FLG). Despite its longstanding clinical use and efficacy, the molecular mechanism of coal tar therapy is unknown. Using organotypic skin models with primary keratinocytes from AD patients and controls, we found that coal tar activated the aryl hydrocarbon receptor (AHR), resulting in induction of epidermal differentiation. AHR knockdown by siRNA completely abrogated this effect. Coal tar restored filaggrin expression in FLG-haploinsufficient keratinocytes to wild-type levels, and counteracted Th2 cytokine-mediated downregulation of skin barrier proteins. In AD patients, coal tar completely restored expression of major skin barrier proteins, including filaggrin. Using organotypic skin models stimulated with Th2 cytokines IL-4 and IL-13, we found coal tar to diminish spongiosis, apoptosis, and CCL26 expression, all AD hallmarks. Coal tar interfered with Th2 cytokine signaling via dephosphorylation of STAT6, most likely due to AHR-regulated activation of the NRF2 antioxidative stress pathway. The therapeutic effect of AHR activation herein described opens a new avenue to reconsider AHR as a pharmacological target and could lead to the development of mechanism-based drugs for AD.
煤焦油的局部应用是特应性皮炎(AD)的最古老治疗方法之一,AD 是一种由辅助性 T 细胞 2(Th2)淋巴细胞介导的皮肤疾病,与皮肤屏障基因丝聚合蛋白(FLG)的功能丧失性突变有关。尽管煤焦油治疗已有很长的临床应用和疗效,但它的分子机制尚不清楚。我们使用来自 AD 患者和对照的原代角质形成细胞的器官型皮肤模型发现,煤焦油激活了芳香烃受体(AHR),导致表皮分化的诱导。通过 siRNA 敲低 AHR 完全消除了这种效应。煤焦油将 FLG 杂合不足的角质形成细胞中的丝聚合蛋白表达恢复到野生型水平,并抵消了 Th2 细胞因子介导的皮肤屏障蛋白下调。在 AD 患者中,煤焦油完全恢复了主要皮肤屏障蛋白的表达,包括丝聚合蛋白。使用经 Th2 细胞因子 IL-4 和 IL-13 刺激的器官型皮肤模型,我们发现煤焦油可减少海绵形成、凋亡和 CCL26 的表达,这些都是 AD 的特征。煤焦油通过去磷酸化 STAT6 干扰 Th2 细胞因子信号,这很可能是由于 AHR 调节的 NRF2 抗氧化应激途径的激活所致。本文描述的 AHR 激活的治疗效果为重新考虑 AHR 作为一种药理学靶点开辟了新途径,并可能导致针对 AD 的基于机制的药物的开发。