Center for Pharmacogenetics and Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, Pennsylvania, USA.
Center for Pharmacogenetics and Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, Pennsylvania, USA; Department of Pharmacology & Chemical Biology, University of Pittsburgh, Pittsburgh, Pennsylvania, USA.
J Biol Chem. 2023 Mar;299(3):103026. doi: 10.1016/j.jbc.2023.103026. Epub 2023 Feb 15.
Autoimmune hepatitis (AIH) is a typical T cell-mediated chronic liver disease with a higher incidence in females. However, the molecular mechanism for the female predisposition is poorly understood. Estrogen sulfotransferase (Est) is a conjugating enzyme best known for its function in sulfonating and deactivating estrogens. The goal of this study is to investigate whether and how Est plays a role in the higher incidence of AIH in females. Concanavalin A (ConA) was used to induce T cell-mediated hepatitis in female mice. We first showed that Est was highly induced in the liver of ConA-treated mice. Systemic or hepatocyte-specific ablation of Est, or pharmacological inhibition of Est, protected female mice from ConA-induced hepatitis regardless of ovariectomy, suggesting the effect of Est inhibition was estrogen independent. In contrast, we found that hepatocyte-specific transgenic reconstitution of Est in the whole-body Est knockout (EstKO) mice abolished the protective phenotype. Upon the ConA challenge, EstKO mice exhibited a more robust inflammatory response with elevated production of proinflammatory cytokines and changed liver infiltration of immune cells. Mechanistically, we determined that ablation of Est led to the hepatic induction of lipocalin 2 (Lcn2), whereas ablation of Lcn2 abolished the protective phenotype of EstKO females. Our findings demonstrate that hepatocyte Est is required for the sensitivity of female mice to ConA-induced and T cell-mediated hepatitis in an estrogen-independent manner. Est ablation may have protected female mice from ConA-induced hepatitis by upregulating Lcn2. Pharmacological inhibition of Est might be a potential strategy for the treatment of AIH.
自身免疫性肝炎(AIH)是一种典型的 T 细胞介导的慢性肝病,女性发病率较高。然而,女性易感性的分子机制尚不清楚。雌激素硫酸转移酶(Est)是一种结合酶,以其磺化和失活雌激素的功能而闻名。本研究旨在探讨 Est 是否以及如何在女性 AIH 发病率较高中发挥作用。刀豆蛋白 A(ConA)用于诱导雌性小鼠的 T 细胞介导的肝炎。我们首先表明,Est 在 ConA 处理的小鼠肝脏中高度诱导。系统或肝细胞特异性敲除 Est 或 Est 的药理学抑制,无论卵巢切除术如何,均可保护雌性小鼠免受 ConA 诱导的肝炎,表明 Est 抑制的作用不受雌激素影响。相比之下,我们发现肝细胞特异性转基因重建整个身体 Est 敲除(EstKO)小鼠中的 Est 消除了保护表型。在 ConA 挑战后,EstKO 小鼠表现出更强的炎症反应,促炎细胞因子的产生增加,免疫细胞在肝脏中的浸润发生改变。从机制上讲,我们确定了 Est 的消融导致了肝细胞中脂联素 2(Lcn2)的诱导,而 Lcn2 的消融消除了 EstKO 雌性动物的保护表型。我们的研究结果表明,Est 在肝细胞中对于雌性小鼠对 ConA 诱导和 T 细胞介导的肝炎的敏感性是必需的,而与雌激素无关。Est 消融可能通过上调 Lcn2 来保护雌性小鼠免受 ConA 诱导的肝炎。Est 的药理学抑制可能是治疗 AIH 的一种潜在策略。