Department of Biochemistry, Punjab Institute of Medical Sciences, Jalandhar, India.
Eur J Pharmacol. 2013 Nov 15;720(1-3):55-62. doi: 10.1016/j.ejphar.2013.10.053. Epub 2013 Nov 5.
Capsaicin is the active ingredient of chili peppers and gives them the characteristic pungent flavor. Understanding the actions of capsaicin led to the discovery of its receptor, transient receptor potential vanilloid subfamily member 1 (TRPV1). This receptor is found on key sensory afferents, and so the use of capsaicin to selectively activate pain afferents has been studied in animal and human models for various indications. Capsaicin is unique among naturally occurring irritant compounds because the initial neuronal excitation evoked by it is followed by a long-lasting refractory period, during which the previously excited neurons are no longer responsive to a broad range of stimuli. This process known as defunctionalisation has been exploited for therapeutic use of capsaicin in various painful conditions. We reviewed different studies on mechanisms of action of capsaicin and its utility in different clinical conditions. A beneficial role of capsaicin has been reported in obesity, cardiovascular and gastrointestinal conditions, various cancers, neurogenic bladder, and dermatologic conditions. Various theories have been put forth to explain these effects. Interestingly many of these pharmacological actions are TRPV1 independent. This review is aimed at providing an overview of these mechanisms and to also present literature which contradicts the proposed beneficial effects of capsaicin. Most of the literature comes from animal studies and since many of these mechanisms are poorly understood, more investigation is required in human subjects.
辣椒素是辣椒的活性成分,赋予它们特有的辛辣味。对辣椒素作用机制的理解导致了其受体——瞬时受体电位香草酸亚型 1(TRPV1)的发现。该受体存在于关键的感觉传入神经上,因此在动物和人类模型中研究了使用辣椒素选择性激活疼痛传入神经的各种适应症。辣椒素在天然刺激性化合物中是独一无二的,因为它最初引起的神经元兴奋之后是一个长时间的不应期,在此期间,先前兴奋的神经元对广泛的刺激不再有反应。这种被称为去功能化的过程已被用于各种疼痛状况下辣椒素的治疗用途。我们回顾了关于辣椒素作用机制及其在不同临床情况下的应用的不同研究。已经报道了辣椒素有在肥胖症、心血管和胃肠道疾病、各种癌症、神经性膀胱和皮肤病等方面的有益作用。已经提出了各种理论来解释这些作用。有趣的是,许多这些药理学作用是 TRPV1 非依赖性的。这篇综述旨在提供对这些机制的概述,并介绍与辣椒素提出的有益作用相矛盾的文献。大部分文献来自动物研究,由于许多这些机制尚未得到充分理解,需要在人体受试者中进行更多的研究。