Transient receptor potential (TRP) channels are non-selective cation channels that are implicated in analgesia, bowel motility, wound healing, thermoregulation, vasodilation and voiding dysfunction. Many natural products have been reported to affect the activity of TRP channels. We hypothesize that numerous traditional herbal medicines (THMs) might exert their pharmacological activity through modulating the activity of TRP channels. The present study aimed to evaluate the effects of flavonoid aglycones and their glycosides, which are the main components of many THMs, on the TRP channel subtypes. A Ca²⁺ influx assay was performed using recombinant human TRPA1, TRPV1, TRPV4 and TRPM8 cell lines. Our findings showed that flavonoid aglycones and glycycoumarin activated TRPA1. In particular, isoflavone and chalcone compounds displayed potent TRPA1 agonistic activity. Furthermore, flavone aglycones showed concomitant potent TRPM8 inhibiting activity. Indeed, flavone, isoflavone aglycones, non-prenylated chalcones and glycycoumarin were found to be TRPM8 inhibitors. Hence, flavonoid aglycones metabolized by lactase-phlorizin hydrolase and β-glucosidase in the small intestine or gut microbiota of the large intestine could generate TRPA1 agonists and TRPM8 antagonists.

瞬态受体电位（TRP）通道是非选择性阳离子通道，与镇痛，肠蠕动，伤口愈合，体温调节，血管舒张和排尿功能障碍有关。据报道许多天然产物会影响TRP通道的活性。我们假设许多传统草药（THMs）可能通过调节TRP通道的活性发挥其药理活性。本研究旨在评估类黄酮苷元及其糖苷（它们是许多THM的主要成分）对TRP通道亚型的影响。钙²⁺使用重组人TRPA1，TRPV1，TRPV4和TRPM8细胞系进行流入检测。我们的研究结果表明类黄酮苷元和糖香豆素激活了TRPA1。特别是，异黄酮和查尔酮化合物显示出有效的TRPA1激动活性。此外，黄酮苷元显示出有效的TRPM8抑制活性。的确，黄酮，异黄酮苷元，非炔丙基查耳酮和香豆素被发现是TRPM8抑制剂。因此，在大肠的小肠或肠道菌群中，由乳糖酶-lo嗪水解酶和β-葡萄糖苷酶代谢的类黄酮苷元可以产生TRPA1激动剂和TRPM8拮抗剂。