Department of Pharmacognosy, School of Pharmacy, China Medical University, Shenyang 110122, China.
Department of Pharmacognosy, School of Pharmacy, China Medical University, Shenyang 110122, China.
Eur J Pharmacol. 2024 Dec 5;984:177021. doi: 10.1016/j.ejphar.2024.177021. Epub 2024 Oct 1.
Diabetes mellitus is a chronic metabolic disease characterized by abnormally elevated blood glucose levels. Type II diabetes accounts for approximately 90% of all cases. Several drugs are available for hyperglycemia treatment. However, the current therapies for managing high blood glucose do not prevent or reverse the disease progression, which may result in complications and adverse effects, including diabetic neuropathy, retinopathy, and nephropathy. Hence, developing safer and more effective methods for lowering blood glucose levels is imperative. Transient receptor potential vanilloid-1 (TRPV1) is a significant member of the transient receptor potential family. It is present in numerous body tissues and organs and performs vital physiological functions.
This review aimed to develop new targeted TRPV1 hypoglycemic drugs by systematically summarizing the mechanism of action of the TRPV1-based signaling pathway in preventing and treating diabetes and its complications.
Literature searches were performed in the PubMed, Web of Science, Google Scholar, Medline, and Scopus databases for 10 years from 2013 to 2023. The search terms included "diabetes," "TRPV1," "diabetic complications," and "capsaicin."
TRPV1 is an essential potential target for treating diabetes mellitus and its complications. It reduces hepatic glucose production and food intake and promotes thermogenesis, metabolism, and insulin secretion. Activation of TRPV1 ameliorates diabetic nephropathy, retinopathy, myocardial infarction, vascular endothelial dysfunction, gastroparesis, and bladder dysfunction. Suppression of TRPV1 improves diabetes-related osteoporosis. However, the therapeutic effects of activating or suppressing TRPV1 may vary when treating diabetic neuropathy and periodontitis.
This review demonstrates that TRPV1 is a potential therapeutic target for diabetes and its complications. Additionally, it provides a theoretical basis for developing new hypoglycemic drugs that target TRPV1.
糖尿病是一种以血糖水平异常升高为特征的慢性代谢性疾病。其中，2 型糖尿病约占所有病例的 90%。目前有多种药物可用于治疗高血糖。然而，现有的高血糖管理疗法并不能预防或逆转疾病进展，这可能导致并发症和不良反应，包括糖尿病神经病变、视网膜病变和肾病。因此，开发更安全、更有效的降血糖方法至关重要。瞬时受体电位香草醛 1（TRPV1）是瞬时受体电位家族的重要成员。它存在于许多身体组织和器官中，发挥着重要的生理功能。
本综述旨在通过系统总结 TRPV1 信号通路在预防和治疗糖尿病及其并发症中的作用机制，开发新的靶向 TRPV1 的降血糖药物。
从 2013 年到 2023 年，在 PubMed、Web of Science、Google Scholar、Medline 和 Scopus 数据库中进行了为期 10 年的文献检索。检索词包括“糖尿病”、“TRPV1”、“糖尿病并发症”和“辣椒素”。
TRPV1 是治疗糖尿病及其并发症的重要潜在靶点。它可降低肝葡萄糖生成和食物摄入，促进产热、代谢和胰岛素分泌。激活 TRPV1 可改善糖尿病肾病、视网膜病变、心肌梗死、血管内皮功能障碍、胃轻瘫和膀胱功能障碍。抑制 TRPV1 可改善与糖尿病相关的骨质疏松症。然而，在治疗糖尿病性神经病变和牙周炎时，激活或抑制 TRPV1 的治疗效果可能有所不同。
本综述表明 TRPV1 是治疗糖尿病及其并发症的潜在治疗靶点。此外，它为开发靶向 TRPV1 的新型降血糖药物提供了理论依据。
