题名

Effect of 158 herbal remedies on human TRPV1 and the two-pore domain potassium channels KCNK2, 3 and 9

DOI

10.1016/j.jtcme.2020.04.005

作者

Robin Herbrechter；Leopoldo R. Beltrán；Paul M. Ziemba；Sascha Titt；Konstantin Lashuk；André Gottemeyer；Janina Levermann；Katrin M. Hoffmann；Madeline Beltrán；Hanns Hatt；Klemens F. Störtkuhl；Markus Werner；Günter Gisselmann

关键词

KCNK channel ； TRPV1 ； Kampo medicine ； Traditional Chinese medicine (TCM) ； Angelica pubescens (radix) ； Alchemilla xanthochlora (herba)

期刊名称

Journal of Traditional and Complementary Medicine

卷期/出版年月

10卷5期（2020 / 09 / 01）

页次

446 - 453

内容语文

英文
中文摘要

Background and aim: Herbal medicines are used to treat a broad number of maladies. However, the pharmacological profile of most remedies is poorly understood. We investigated the effect of herbal remedies from kampo, traditional Chinese medicine (TCM) and other phytotherapies on human twopore domain potassium channels (KCNK channels; TREK-1, TASK-1 and TASK-3) as well as the human TRPV1 channel. KCNK channels are responsible for the background potassium current of excitable cells, thus essential for the maintenance of the resting membrane potential. Hence, modulators of KCNK channels are of medical significance, e.g. for the treatment of sleep disorders and pain. The transient receptor potential channel TRPV1 is a pain detector for noxious heat. Agonists of this receptor are still used for the treatment of pain in ectopic applications. Experimental procedure: We evaluated the effect of 158 herbal remedies on these channels in a heterologous expression system (Xenopus laevis oocytes) using the two-electrode voltage-clamp technique with the aim of increasing the comprehension of their pharmacological profile. Results and conclusion: Some remedies with modulating effects were identified such as Angelica pubescens (radix), which inhibit TASK-1 and TASK-3 channels. Furthermore, the modulatory effects of the most effective remedies on the two TASK family members TASK-1 and TASK-3 correlate positively, reflecting their close relation. For the TRPV1 channel Terminalia chebula and Alchemilla xanthochlora were identified as potentiators. This study identifies a variety of herbal remedies as modulators of human K2P and TRPV1 channels and gives new insights into the pharmacological profile of these herbal remedies.
主题分类 醫藥衛生 > 中醫藥學
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