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Trans-ε-viniferin as an inhibitor of TMEM16A preventing intestinal smooth muscle contraction
Xin-Yi Liu1, Yan Zhao1, Ling-Ling Jin2
1School of Life Sciences, Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Liaoning Normal University, Dalian 116081, China.
Abstract:
TMEM16A regulator is an important tool to study the physiological functions and pathogenesis related to TMEM16A. In the present study, trans-ε-viniferin (TV) was identified as a TMEM16A inhibitor with inhibitory activity against TMEM16A mediated Cl- currents, which was reversible, without affecting intracytoplasmic Ca2+ concentration and TMEM16A protein expression. TV inhibited intestinal peristalsis and prolonged gastrointestinal transport time. TV could inhibit autonomic and Eact-stimulated intestinal contractility, and was equally effective in ACh- and HA-induced high contractile states. The results indicate that TV significantly inhibits the intestinal smooth muscle contraction, which may be applied in the treatment of TMEM16A-related intestinal dynamic abnormalities.
Insights
Trans-epsilon-viniferin (TV) inhibits TMEM16A calcium-activated chloride channels, reducing intestinal smooth muscle contraction. This TMEM16A regulator may treat intestinal dynamic abnormalities.
Area of Science:
- Physiology
- Pharmacology
- Gastroenterology
Background:
- TMEM16A (Anoctamin 1) is a calcium-activated chloride channel protein crucial for various physiological functions.
- Dysregulation of TMEM16A is implicated in the pathogenesis of several diseases, including gastrointestinal disorders.
- Identifying specific TMEM16A regulators is essential for understanding its role and developing therapeutic strategies.
Purpose of the Study:
- To identify and characterize novel regulators of TMEM16A.
- To investigate the effects of trans-epsilon-viniferin (TV) on TMEM16A activity and function.
- To evaluate the potential therapeutic applications of TV in TMEM16A-related intestinal abnormalities.
Main Methods:
- Electrophysiological recordings to measure TMEM16A-mediated Cl- currents.
- Assessment of intracellular calcium (Ca2+) concentrations.
- Western blot analysis to determine TMEM16A protein expression levels.
- In vivo studies on intestinal peristalsis and gastrointestinal transit time.
- In vitro studies on intestinal smooth muscle contractility stimulated by various agents (e.g., acetylcholine, histamine).
Main Results:
- Trans-epsilon-viniferin (TV) was identified as a reversible TMEM16A inhibitor.
- TV inhibited TMEM16A-mediated Cl- currents without altering intracellular Ca2+ levels or TMEM16A protein expression.
- TV significantly inhibited intestinal peristalsis and prolonged gastrointestinal transit time in vivo.
- TV effectively suppressed intestinal smooth muscle contractility induced by autonomic stimulation, acetylcholine (ACh), and histamine (HA).
Conclusions:
- Trans-epsilon-viniferin (TV) acts as a functional inhibitor of TMEM16A.
- TV demonstrates significant inhibitory effects on intestinal smooth muscle contraction.
- TV holds potential as a therapeutic agent for treating TMEM16A-associated intestinal dynamic disorders.
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