Csekő Kata, Beckers Bram, Keszthelyi Daniel, Helyes Zsuzsanna
Department of Pharmacology and Pharmacotherapy, Medical School and Molecular Pharmacology Research Group, Szentágothai Research Centre, University of Pécs, H-7624 Pécs, Hungary.
Division of Gastroenterology-Hepatology, Department of Internal Medicine, Maastricht University Medical Center (MUMC+), 6202 AZ Maastricht, The Netherlands.
Pharmaceuticals (Basel). 2019 Mar 30;12(2):48. doi: 10.3390/ph12020048.
Inflammatory bowel diseases (IBD) have long been recognized to be accompanied by pain resulting in high morbidity. Transient receptor potential vanilloid 1 (TRPV1) and ankyrin 1 (TRPA1) ion channels located predominantly on the capsaicin-sensitive sensory neurons play a complex role in hyperalgesia and neurogenic inflammation. This review provides an overview of their expression and role in intestinal inflammation, in particular colitis, that appears to be virtually inconsistent based on the thorough investigations of the last twenty years. However, preclinical results with pharmacological interventions, as well as scarcely available human studies, more convincingly point out the potential therapeutic value of TRPV1 and TRPA1 antagonists in colitis and visceral hypersensitivity providing future therapeutical perspectives through a complex, unique mechanism of action for drug development in IBD.
炎症性肠病(IBD)长期以来被认为伴有疼痛,导致发病率很高。主要位于对辣椒素敏感的感觉神经元上的瞬时受体电位香草酸亚型1(TRPV1)和锚蛋白1(TRPA1)离子通道在痛觉过敏和神经源性炎症中起复杂作用。这篇综述概述了它们在肠道炎症,特别是结肠炎中的表达和作用,基于过去二十年的深入研究,其表现似乎几乎不一致。然而,药理学干预的临床前结果以及为数不多的人体研究更有说服力地指出,TRPV1和TRPA1拮抗剂在结肠炎和内脏超敏反应中具有潜在的治疗价值,通过一种复杂、独特的作用机制为IBD药物开发提供了未来的治疗前景。