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Atractylodin Produces Antinociceptive Effect through a Long-Lasting TRPA1 Channel Activation
Hirosato Kanda1,2,3, Yanjing Yang1,4, Shaoqi Duan1
1Department of Pharmacy, School of Pharmacy, Hyogo University of Health Sciences, Kobe 650-8530, Japan.
International Journal of Molecular Sciences
|April 3, 2021
Summary
Atractylodin (ATR) activates the TRPA1 channel, a key player in pain signaling. This activation leads to desensitization of pain-sensing neurons, explaining ATR's anti-pain effects.
Area of Science:
- Pharmacology
- Neuroscience
- Natural Products Chemistry
Background:
- Atractylodes lancea (AL) is traditionally used for pain relief.
- The specific molecular mechanism of Atractylodin (ATR), a key component of AL, in pain management is not well understood.
Purpose of the Study:
- To investigate the molecular mechanism of ATR's anti-pain effects.
- To determine if ATR interacts with the TRPA1 channel and its role in nociception.
Main Methods:
- Assessed ATR's effect on human TRPA1 (hTRPA1) channel activity in HEK293 cells.
- Measured calcium responses in TRPA1 knockout mice neurons.
- Evaluated ATR's effect on nociceptive behavior in vivo using AITC as a control.
Main Results:
- ATR directly activates TRPA1 channel activity, causing prolonged calcium responses.
- ATR-induced nociceptive behavior was abolished in TRPA1 knockout mice.
- Systemic ATR administration dose-dependently inhibited AITC-induced pain responses.
Conclusions:
- ATR is a novel agonist of TRPA1 channels, inducing long-lasting activation.
- ATR exerts anti-nociceptive effects by desensitizing TRPA1-expressing nociceptors.
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