海葵肽的抗焦虑作用，TRPV1 和 ASIC 通道的调节剂。

Anxiolytic Effect of Peptides from Sea Anemone Heteractis crispa, Modulators of TRPV1 and ASIC Channels.

机构信息

Elyakov Pacific Institute of Bioorganic Chemistry, Far East Branch, Russian Academy of Sciences, Vladivostok, Russia.

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Pushchino Branch, Russian Academy of Sciences, Pushchino, Moscow oblast, Russia.

出版信息

Dokl Biochem Biophys. 2022 Aug;505(1):145-150. doi: 10.1134/S1607672922040093. Epub 2022 Aug 29.

DOI:10.1134/S1607672922040093

PMID:36038679

Abstract

A number of studies confirmed the involvement of transient receptor potential vanilloid (TRPV) and acid-sensing (ASIC) ion channels in the physiological processes associated with the development of anxiety disorders. This makes their ligands new potential anxiolytic agents. We examined the efficacy of two peptides from the sea anemone Heteractis crispa, Hcr 1b-2 and HCRG21, affecting ASIC1a and TRPV1 channels, respectively, in the open field and elevated plus maze tests. According to the obtained data, HCRG21 significantly decreases both the level of anxiety and stimulates the activity of animals at doses of 0.01-1 mg/kg, whereas Hcr 1b-2 has a weak anxiolytic effect only at a dose of 0.1 mg/kg. The pharmacodynamic study showed that the HCRG21 has an anxiolytic effect for 2 h, and its effectiveness is higher than that of the reference drug.

摘要

多项研究证实，瞬时受体电位香草酸（TRPV）和酸感应（ASIC）离子通道参与了与焦虑症发展相关的生理过程。这使得它们的配体成为新的潜在抗焦虑药物。我们研究了来自海葵 Heteractis crispa 的两种肽 Hcr 1b-2 和 HCRG21 的功效，它们分别作用于 ASIC1a 和 TRPV1 通道，在旷场和高架十字迷宫测试中。根据获得的数据，HCRG21 在 0.01-1mg/kg 的剂量下显著降低焦虑水平并刺激动物的活动，而 Hcr 1b-2 仅在 0.1mg/kg 的剂量下具有较弱的抗焦虑作用。药效学研究表明，HCRG21 具有 2 小时的抗焦虑作用，其效果高于参考药物。