Division of Clinical Pharmacology, Toxicology and Therapeutic Innovation, Division of Gastroenterology, Children's Mercy Hospital, Kansas City, Missouri 64108, USA; Department of Pediatrics, University of Kansas Medical Center, Kansas City, Kansas 66160, USA.
Department of Internal Medicine, University of Kansas Medical Center, Kansas City, Kansas 66160, USA.
Toxicol Appl Pharmacol. 2020 Sep 15;403:115136. doi: 10.1016/j.taap.2020.115136. Epub 2020 Jul 15.
The Aryl hydrocarbon receptor (AhR) is primarily known as one of the xenosensors and regulators of drug-metabolizing genes. Bile acids (BAs) are synthesized in the liver, and undergo several enterohepatic recirculations in which the liver removes BAs from the portal blood, minimizing the BAs that spill over into the systemic circulation. Previous studies revealed a lifelong patent ductus venosus (PDV) in AhR-null mice. Increased concentration of total BAs (Σ-BAs) in AhR-null mice is known; however, the impact of PDV on BA homeostasis in liver and bile remains unclear. This work investigated the consequences of PDV on BA homeostasis by comparing AhR-null and wild-type (WT) mice of both genders. In serum, Σ-BAs were markedly higher (64-85-fold) in AhR-null mice than in WT mice, especially due to the increase of tri-OH primary BAs (86-142-fold). Despite the extremely high concentration of serum BAs, the concentration of BAs in livers of AhR-null mice remained similar to WT mice. AhR-null livers were protected against increased BA influx by downregulation of uptake transporters and BA synthetic enzymes in the alternative pathway. Although livers of AhR-null mice are 20-25% smaller than WT mice, biliary excretion of BAs was maintained in the AhR-null mice, and even tended to increase. Surprisingly, intestinal Fgf15 expression was not increased, even though there was a marked increase in serum BA concentrations. Although PDV resulted in extremely high BA concentrations in serum of AhR-null mice, they maintained a concentration of BAs in liver and biliary excretion of BAs similar to control mice.
芳香烃受体(AhR)主要作为一种外源性传感器和药物代谢基因的调节剂而为人所知。胆汁酸(BAs)在肝脏中合成,并经历多次肠肝再循环,其中肝脏从门静脉血液中去除 BAs,使进入全身循环的 BAs 最小化。先前的研究揭示了 AhR 基因敲除(KO)小鼠存在终身的动脉导管未闭(PDA)。已知 AhR 基因敲除小鼠的总胆汁酸(Σ-BAs)浓度增加;然而,PDA 对肝脏和胆汁中 BA 动态平衡的影响尚不清楚。这项工作通过比较雌雄两性的 AhR 基因敲除和野生型(WT)小鼠,研究了 PDA 对 BA 动态平衡的影响。在血清中,Σ-BAs 在 AhR 基因敲除小鼠中比 WT 小鼠高得多(64-85 倍),尤其是由于三羟初级胆汁酸(86-142 倍)的增加。尽管血清中 BA 的浓度极高,但 AhR 基因敲除小鼠肝脏中 BA 的浓度仍与 WT 小鼠相似。AhR 基因敲除小鼠的肝脏通过下调替代途径中的摄取转运体和 BA 合成酶来防止 BA 内流增加。尽管 AhR 基因敲除小鼠的肝脏比 WT 小鼠小 20-25%,但 AhR 基因敲除小鼠的胆汁中 BA 的排泄仍得以维持,甚至有增加的趋势。令人惊讶的是,尽管血清 BA 浓度有明显增加,但肠道 Fgf15 表达并未增加。尽管 AhR 基因敲除小鼠的血清中 BA 浓度极高,但它们维持了与对照小鼠相似的肝脏 BA 浓度和胆汁排泄。