Uncaria Rhynchophylla and hirsuteine as TRPV1 agonists inducing channel desensitization

Uncaria rhynchophylla (UR) is recognized for its therapeutic applications in treating hypertension and inflammation. However, the specific molecular mechanisms how UR and its bioactive constituents modulate inflammatory pathways remain unknown. This study investigates the effects of UR extract and i...

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Published in:Journal of ethnopharmacology 2025-01, Vol.337 (Pt 2), p.118869, Article 118869
Main Authors: Ha, Taewoong, Kang, Bokeum, Kim, Mi-Sun, Chu, Jung Woong, Kim, Kyungmin, Yoon, Wooseung, Kim, Soon Ho, Kang, Taek, Kim, Min Soo, Kim, Chungho, Cha, Joo Young, Oh, Uhtaek, Han, Kyungreem, Choi, Chun Whan, Hong, Gyu-Sang
Format: Article
Language:English
Subjects:
Animals
Calcium - metabolism
Capsaicin - pharmacology
Desensitization
HEK293 Cells
Hirsuteine
Humans
Plant Extracts - pharmacology
Sensory neuron
Sensory Receptor Cells - drug effects
Sensory Receptor Cells - metabolism
TRPV Cation Channels - agonists
TRPV Cation Channels - metabolism
TRPV1
Uncaria - chemistry
Uncaria rhynchophylla
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Summary:Uncaria rhynchophylla (UR) is recognized for its therapeutic applications in treating hypertension and inflammation. However, the specific molecular mechanisms how UR and its bioactive constituents modulate inflammatory pathways remain unknown. This study investigates the effects of UR extract and its constituent, hirsuteine (HST), on TRPV1 channel modulation which is related to hypertension and inflammation. Electrophysiological recordings and calcium imaging experiments were conducted to assess TRPV1 activation by UR extract and HST in HEK293T cells and sensory neurons. UR extract and HST activated TRPV1 in HEK293T cells, with repeated applications causing channel desensitization. HST application on TRPV1-positive sensory neurons significantly reduced electrical activity compared to capsaicin. This study demonstrated UR extract and HST are a novel TRPV1 agonists inducing channel desensitization and a potent agent for treatment of TRPV1 dependent pain relief. [Display omitted] •Identification of the selective activation and subsequent desensitization of TRPV1 by UR extract and hirsuteine.•Detailed characterization of the interaction between hirsuteine and TRPV1.•Hirsuteine modulates neuronal excitability in TRPV1-positive sensory neurons.
ISSN:0378-8741
1872-7573
1872-7573
DOI:10.1016/j.jep.2024.118869