Modulation of TRPV1 channel function by natural products in the treatment of pain
Modulation of TRPV1 channel function by natural products in the treatment of pain
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DOI：
10.1016/j.cbi.2020.109178
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发表时间：
2020-10-01
影响因子：
5.1
通讯作者：
Abbas, Manal Ahmad
中科院分区：
文献类型：
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作者：
Abbas, Manal Ahmad
辣椒素受体TRPV1是一种由炎症介质调节的热激活阳离子通道，与急性和慢性疼痛有关。TRPV1通道是开发新型镇痛药研究最多和有针对性的机制之一。多年来，天然产物对现代医学中使用的重要治疗药物的发展做出了巨大贡献。使用Medline、谷歌Scholar和PubMed进行文献综述。搜索文献得到清单136与TRPV1通道相互作用的天然化合物。这些化合物属于不同化学类群的植物化学物质，包括香草类、黄酮类、生物碱、萜类、萜烯酚类、脂肪酸、大麻素、含硫化合物等。其他天然TRPV1调节剂来源于动物、真菌或细菌。一些天然产物是TRPV1的小激动剂或拮抗剂。其他是蛋白质毒液。大多数体外研究利用电生理或钙成像技术，利用大鼠背根和三叉神经节原代培养研究钙通过通道的流动。其他研究使用HEK239、CHO细胞或爪蟾卵母细胞中表达的hTRPV1或rTRPV1。体内研究主要集中在小鼠和大鼠的不同疼痛模型上。综上所述，天然产物对TRPV1的调节作用是高度多样化的。天然产物研究中的许多空白存在于区分模态特异性和多模态拮抗剂方面。在未来的研究中，必须考虑到物种在TRPV1功能上的差异。进入临床试验需要更多的努力，以发现有效的TRPV1拮抗剂没有热疗，主要的副作用。
The capsaicin (vanilloid) receptor, TRPV1, is a heat-activated cation channel modulated by inflammatory mediators and contributes to acute and chronic pain. TRPV1 channel is one of the most researched and targeted mechanisms for the development of novel analgesics. Over the years, natural products have contributed enormously to the development of important therapeutic drugs used currently in modern medicine. A literature review was conducted using Medline, Google Scholar, and PubMed. Searching the literature resulted in listing 136 natural compounds that interacted with TRPV1 channel. These compounds were phytochemicals that belong to different chemical groups including vanilloids, flavonoids, alkaloids, terpenoids, terpenyl phenols, fatty acids, cannabinoids, sulfur_containing compounds, etc. Other natural TRPV1 modulators were of animal, fungal or bacterial origin. Some natural products were small agonists or antagonists of TRPV1. Others were protein venoms. Most in vitro studies utilized electrophysiological or calcium imaging techniques to study calcium flow through the channel using primary cultures of rat dorsal root and trigeminal ganglia. Other studies used hTRPV1 or rTRPV1 expressed in HEK239, CHO cells or Xenopus oocytes. In vivo studies concentrated on different pain models conducted mainly in mice and rats. In conclusion, natural products are highly diverse in their modulatory action on TRPV1. Many gaps in natural product research are present in distinguishing modality-specific from polymodal antagonists. Species' differences in TRPV1 functionality must be taken into account in any future study. Proceeding into clinical trials needs more efforts to discover potent TRPV1 antagonists devoid of hyperthermia, the main side effect.