Uncaria Rhynchophylla and hirsuteine as TRPV1 agonists inducing channel desensitization

Taewoong Ha; Bokeum Kang; Mi Sun Kim; Jung Woong Chu; Kyungmin Kim; Wooseung Yoon; Soon Ho Kim; Taek Kang; Min Soo Kim; Chungho Kim; Joo Young Cha; Uhtaek Oh; Kyungreem Han; Chun Whan Choi; Gyu Sang Hong

doi:10.1016/j.jep.2024.118869

Uncaria Rhynchophylla and hirsuteine as TRPV1 agonists inducing channel desensitization

Taewoong Ha
, Bokeum Kang
, Mi Sun Kim
, Jung Woong Chu
, Kyungmin Kim
, Wooseung Yoon
, Soon Ho Kim
, Taek Kang
, Min Soo Kim
, Chungho Kim
, Joo Young Cha
, Uhtaek Oh
, Kyungreem Han^*
, Chun Whan Choi^*
, Gyu Sang Hong^*

^*Corresponding author for this work

Department of Life Sciences

Research output: Contribution to journal › Article › peer-review

Abstract

Ethnopharmacological relevance: 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. Materials and methods: Electrophysiological recordings and calcium imaging experiments were conducted to assess TRPV1 activation by UR extract and HST in HEK293T cells and sensory neurons. Results: 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. Conclusion: 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.

Original language	English
Article number	118869
Journal	Journal of Ethnopharmacology
Volume	337
DOIs	https://doi.org/10.1016/j.jep.2024.118869
Publication status	Published - 2025 Jan 30

Bibliographical note

Publisher Copyright:
© 2024 KIST

Keywords

Desensitization
Hirsuteine
Sensory neuron
TRPV1
Uncaria rhynchophylla

ASJC Scopus subject areas

Pharmacology
Drug Discovery

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10.1016/j.jep.2024.118869

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title = "Uncaria Rhynchophylla and hirsuteine as TRPV1 agonists inducing channel desensitization",

abstract = "Ethnopharmacological relevance: 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. Materials and methods: Electrophysiological recordings and calcium imaging experiments were conducted to assess TRPV1 activation by UR extract and HST in HEK293T cells and sensory neurons. Results: 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. Conclusion: 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.",

keywords = "Desensitization, Hirsuteine, Sensory neuron, TRPV1, Uncaria rhynchophylla",

author = "Taewoong Ha and Bokeum Kang and Kim, \{Mi Sun\} and Chu, \{Jung Woong\} and Kyungmin Kim and Wooseung Yoon and Kim, \{Soon Ho\} and Taek Kang and Kim, \{Min Soo\} and Chungho Kim and Cha, \{Joo Young\} and Uhtaek Oh and Kyungreem Han and Choi, \{Chun Whan\} and Hong, \{Gyu Sang\}",

note = "Publisher Copyright: {\textcopyright} 2024 KIST",

year = "2025",

month = jan,

day = "30",

doi = "10.1016/j.jep.2024.118869",

language = "English",

volume = "337",

journal = "Journal of Ethnopharmacology",

issn = "0378-8741",

publisher = "Elsevier Ireland Ltd",

}

TY - JOUR

T1 - Uncaria Rhynchophylla and hirsuteine as TRPV1 agonists inducing channel desensitization

AU - Ha, Taewoong

AU - Kang, Bokeum

AU - Kim, Mi Sun

AU - Chu, Jung Woong

AU - Kim, Kyungmin

AU - Yoon, Wooseung

AU - Kim, Soon Ho

AU - Kang, Taek

AU - Kim, Min Soo

AU - Kim, Chungho

AU - Cha, Joo Young

AU - Oh, Uhtaek

AU - Han, Kyungreem

AU - Choi, Chun Whan

AU - Hong, Gyu Sang

PY - 2025/1/30

Y1 - 2025/1/30

N2 - Ethnopharmacological relevance: 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. Materials and methods: Electrophysiological recordings and calcium imaging experiments were conducted to assess TRPV1 activation by UR extract and HST in HEK293T cells and sensory neurons. Results: 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. Conclusion: 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.

AB - Ethnopharmacological relevance: 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. Materials and methods: Electrophysiological recordings and calcium imaging experiments were conducted to assess TRPV1 activation by UR extract and HST in HEK293T cells and sensory neurons. Results: 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. Conclusion: 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.

KW - Desensitization

KW - Hirsuteine

KW - Sensory neuron

KW - TRPV1

KW - Uncaria rhynchophylla

UR - https://www.scopus.com/pages/publications/85205893293

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DO - 10.1016/j.jep.2024.118869

M3 - Article

C2 - 39353479

AN - SCOPUS:85205893293

SN - 0378-8741

VL - 337

JO - Journal of Ethnopharmacology

JF - Journal of Ethnopharmacology

M1 - 118869

ER -

Uncaria Rhynchophylla and hirsuteine as TRPV1 agonists inducing channel desensitization

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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