Department of Pharmacy, People's Hospital of Peking University, Beijing, China; School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Department of Pharmacy, People's Hospital of Peking University, Beijing, China; School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.
Mol Immunol. 2024 Nov;175:55-62. doi: 10.1016/j.molimm.2024.09.008. Epub 2024 Sep 20.
The founding family member, Interleukin (IL)-17A, is commonly known as IL-17 and has garnered increasingly attention for proinflammatory functions in autoimmune disorders. Although the effects of IL-17A on hepatic important drug-metabolizing enzymes and transporters (DMETs) expression still remain unclear, it is critical to ascertain owing to the well-established alterations of the drug disposition capacity of the liver occurring during immune imbalance. The present study was designed to explore the effects and mechanisms of IL-17A on DMETs mRNA and protein expression in HepaRG cells by real-time quantitative reverse transcription polymerase chain reaction and Western blot, respectively. It is discovered that IL-17A can inhibit most DMETs mRNA expression (drug-metabolizing enzymes of CYP1A2, CYP3A4, CYP2C9, CYP2C19, GSTA1 and UGT1A1 and transporters of NTCP, OCT1, OATP1B1, BCRP and MDR1) as well as the protein expression of CYP3A4 and CYP2C19, via the janus kinase 2 (JAK2)-signal transducer and activator of transcription 3 (STAT3) signaling pathway. Thus, abnormal regulation of DMETs in IL-17A-mediated immune disorders such as psoriasis may cause alterations in pharmacokinetic processes and may occasionally result in unexpected drug-drug interactions (DDIs) in clinical practice.
该创始家族成员白细胞介素(IL)-17A 通常被称为 IL-17,因其在自身免疫性疾病中的促炎功能而受到越来越多的关注。尽管 IL-17A 对肝脏重要药物代谢酶和转运体(DMETs)表达的影响尚不清楚,但鉴于免疫失衡期间肝脏药物处置能力的改变已得到充分证实,确定这一点至关重要。本研究旨在通过实时定量逆转录聚合酶链反应和 Western blot 分别探讨 IL-17A 对 HepaRG 细胞中 DMETs mRNA 和蛋白表达的影响及其机制。研究发现,IL-17A 可通过 Janus 激酶 2(JAK2)-信号转导和转录激活因子 3(STAT3)信号通路抑制大多数 DMETs mRNA 表达(CYP1A2、CYP3A4、CYP2C9、CYP2C19、GSTA1 和 UGT1A1 等药物代谢酶和 NTCP、OCT1、OATP1B1、BCRP 和 MDR1 等转运体)以及 CYP3A4 和 CYP2C19 的蛋白表达。因此,IL-17A 介导的免疫紊乱中 DMETs 的异常调节可能导致药代动力学过程的改变,并在临床实践中偶尔导致意想不到的药物相互作用(DDI)。