瞬时受体电位香草醛亚家族1(TRPV1)的生物学功能
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湖北中医药大学基础医学院,武汉 430072

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国家自然科学基金(82174020) 资助项目。


Biological Functions of TRPV1
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School of Basic Medicine, Hubei University of Chinese Medicine, Wuhan 430072, China

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This work was supported by a grant from The National Natural Science Foundation of China (82174020).

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    摘要:

    瞬时受体电位香草醛亚家族1(TRPV1)又称辣椒素受体(VR1),是一类可被辣椒素、热(>43℃)、酸(pH<6.0)所激活的配体门控性非选择性阳离子通道,对Ca2+有高度通透性。早期研究发现TRPV1主要分布在神经系统并介导瘙痒及痛觉反应,近些年研究表明其在非神经细胞如肥大细胞、膀胱上皮细胞、单核细胞、皮肤角化上皮细胞、胰岛细胞等中也广泛分布,在代谢性疾病、消化、呼吸和心血管系统疾病、皮肤病及肿瘤等疾病的发生发展中均发挥了重要作用。本文介绍了TRPV1的分布、结构特征及其功能研究的最新进展,并重点综述了TRPV1介导的瘙痒和疼痛信号通路及以TRPV1为靶点的中草药研究进展,以期为以TRPV1为潜在治疗靶点相关疾病的中西医防治提供理论指导。

    Abstract:

    Transient receptor potential vanilloid subfamily member 1 (TRPV1), also known as capsaicin receptor (VR1), is a kind of ligand gated non-selective cation channel which can be activated by capsaicin, heat (>43℃) and H+ (pH<6.0). TRPV1 is highly permeable to Ca2+. Previous studies found that TRPV1 mainly distributes in nervous system and mediates pruritus and pain response. Recent studies have shown that TRPV1 also widely distributes in non-nervous cells such as mast cells, bladder epithelial cells, monocytes, skin keratinized epithelial cells, islet cells and so on. TRPV1 has a wide range of functions and can mediate beneficial or harmful biological effects on the body. In the nervous system, TRPV1 related signal pathway mainly mediates itching and pain response. Relevant studies in pancreatic cells have shown that the upregulation of TRPV1 can alleviate the process of diabetes, but studies in pulmonary epithelial cells, pulmonary vascular endothelial cells, bronchial smooth muscle cells, etc. have shown that the upregulation of TRPV1 can accelerate the development of respiratory diseases. In addition, TRPV1 has dual effects of promotion or inhibition on the disease progression in cardiovascular system, digestive system and skin system. In cancer research, it was also found that the upregulation of TRPV1 played an important antineoplastic effect, which could inhibit the proliferation, invasion and migration of tumor cells in human tongue squamous cell carcinoma, prostate cancer, breast cancer and so on, arrest the cell cycle and induce cell apoptosis. At present, many studies have been carried out on the mechanism of TRPV1, among which the mechanism of TRPV1 mediating itching and pain is relatively in depth. TRPV1 has become a promising therapeutic target due to its extensive functions. New drugs targeted to TRPV1 have been developed to ameliorate diabetes, cardiovascular diseases, and some kinds of cancers. This paper introduces the latest progress in the distribution, structural characteristics and functions of TRPV1, and focuses on the research progress of pruritus and pain related signaling pathways mediated by TRPV1. We also introduced the Chinese herbal medicine with TRPV1 as the target, looking forward to providing theoretical guidance for taking TRPV1 as a potential therapeutic target by combination of traditional Chinese medicine and modern medicine.

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刘夏阳,李壮,周欣悦,郭晓红.瞬时受体电位香草醛亚家族1(TRPV1)的生物学功能[J].生物化学与生物物理进展,2023,50(3):437-447

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  • 收稿日期:2022-03-31
  • 最后修改日期:2023-02-11
  • 接受日期:2022-08-01
  • 在线发布日期: 2023-03-22
  • 出版日期: 2023-03-20