4.7 Article

Identification and molecular study on the interaction of Schisandrin C with human 5-HT3A receptor

期刊

EUROPEAN JOURNAL OF PHARMACOLOGY
卷 906, 期 -, 页码 -

出版社

ELSEVIER
DOI: 10.1016/j.ejphar.2021.174220

关键词

5-HT3A receptor; Schisandrin C; IBS; TEVC; EPSP; 3D modeling

资金

  1. Korea Institute of Planning and Evaluation for Technology in Food, Agriculture and Forestry(IPET) through Useful Agricultural Life Resources Industry Technology Development Program [120049-2]
  2. National Research Foundation of Korea (NRF) - Korea government (MSIT) [2019R1F1A1059156, 2019R1F1A1060984]
  3. National Research Foundation of Korea [2019R1F1A1059156, 2019R1F1A1060984] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

向作者/读者索取更多资源

The component Schisandrin C from Schisandra interacts with the 5-HT3A receptor to potentially treat IBS by suppressing excessive neuronal serotonin signaling.
Schisandrin C (Sch C) is one of the main components of Schisandra chinensis (Schisandra). Since the olden times, Schisandra has been used as a traditional herbal medicine in Asia. Recent studies have shown that Schisandra is effective against irritable bowel syndrome (IBS) in an animal model and affects IBS through the 5-HT3A pathway in the IBS rat model. However, there lacks fundamental research on the interaction of specific components of Schisandra with the 5-HT3A receptor for the treatment of IBS. We hypothesized that a component of Schisandra binds to the 5-HT3A receptor and identified Sch C via a screening work using two electrode-voltage clamps (TEVC). Thus, we aimed to elucidate the neuropharmacological actions between Sch C and the 5-HT3A receptor at molecular and cellular levels. Co-treatment of Sch C with 5-HT inhibited I5-HT in a reversible, concentrate-dependent, like-competition, and voltage-independent manner, and IC50 values of Sch C. Besides, the main binding positions of Sch C were identified through 3D modeling and point mutation were V225A and V288Y on 5-HT3A receptor. Thus, we suggest the potential of Sch C in treating IBS in a manner that suppresses excessive neuronal serotonin signaling in the synapse of sensory neurons and enterochromaffin (EC) cells. In conclusion, the results demonstrate the mechanism of interaction between Sch C and 5-HT3A receptor and reveal Sch C as a novel antagonist.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.7
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据