Journal
EUROPEAN JOURNAL OF PHARMACOLOGY
Volume 906, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ejphar.2021.174220
Keywords
5-HT3A receptor; Schisandrin C; IBS; TEVC; EPSP; 3D modeling
Categories
Funding
- 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]
- National Research Foundation of Korea (NRF) - Korea government (MSIT) [2019R1F1A1059156, 2019R1F1A1060984]
- National Research Foundation of Korea [2019R1F1A1059156, 2019R1F1A1060984] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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.
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