A phytosphingosine derivative mYG-II-6 inhibits histamine-mediated TRPV1 activation and MRGPRX2-dependent mast cell degranulation
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Adhikari, Nisha | - |
dc.contributor.author | Lee, Wook-Joo | - |
dc.contributor.author | Park, Soojun | - |
dc.contributor.author | Kim, Sanghee | - |
dc.contributor.author | Shim, Won-Sik | - |
dc.date.accessioned | 2024-06-06T09:00:18Z | - |
dc.date.available | 2024-06-06T09:00:18Z | - |
dc.date.issued | 2024-05 | - |
dc.identifier.issn | 1567-5769 | - |
dc.identifier.issn | 1878-1705 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/91454 | - |
dc.description.abstract | Background: Phytosphingosine and its derivative are known for their skin-protective properties. While mYG-II-6, a phytosphingosine derivative, has shown anti-inflammatory and antipsoriatic effects, its potential antipruritic qualities have yet to be explored. This study aimed to investigate mYG-II-6 ' s antipruritic properties. Methods: The calcium imaging technique was employed to investigate the activity of ion channels and receptors. Mast cell degranulation was confirmed through the beta-hexosaminidase assay. Additionally, in silico molecular docking and an in vivo mouse scratching behavior test were utilized. Results: Using HEK293T cells transfected with H1R and TRPV1, we examined the impact of mYG-II-6 on histamine-induced intracellular calcium rise, a key signal in itch-mediating sensory neurons. Pretreatment with mYG-II-6 significantly reduced histamine-induced calcium levels and inhibited TRPV1 activity, suggesting its role in blocking the calcium influx channel. Additionally, mYG-II-6 suppressed histamine-induced calcium increase in primary cultures of mouse dorsal root ganglia, indicating its potential antipruritic effect mediated by histamine. Interestingly, mYG-II-6 exhibited inhibitory effects on human MRGPRX2, a G protein-coupled receptor involved in IgE-independent mast cell degranulation. However, it did not inhibit mouse MrgprB2, the ortholog of human MRGPRX2. Molecular docking analysis revealed that mYG-II-6 selectively interacts with the binding pocket of MRGPRX2. Importantly, mYG-II-6 suppressed histamine-induced scratching behaviors in mice. Conclusions: Our findings show that mYG-II-6 can alleviate histamine-induced itch sensation through dual mechanisms. This underscores its potential as a versatile treatment for various pruritic conditions. | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | Elsevier | - |
dc.title | A phytosphingosine derivative mYG-II-6 inhibits histamine-mediated TRPV1 activation and MRGPRX2-dependent mast cell degranulation | - |
dc.type | Article | - |
dc.identifier.wosid | 001234601000001 | - |
dc.identifier.doi | 10.1016/j.intimp.2024.112113 | - |
dc.identifier.bibliographicCitation | International Immunopharmacology, v.133 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.scopusid | 2-s2.0-85190838962 | - |
dc.citation.title | International Immunopharmacology | - |
dc.citation.volume | 133 | - |
dc.type.docType | Article | - |
dc.publisher.location | 네델란드 | - |
dc.subject.keywordAuthor | Itch | - |
dc.subject.keywordAuthor | TRPV1 | - |
dc.subject.keywordAuthor | MRGPRX2 | - |
dc.subject.keywordAuthor | Histamine | - |
dc.subject.keywordAuthor | Mast cell degranulation | - |
dc.subject.keywordPlus | ACID PHENETHYL ESTER | - |
dc.subject.keywordPlus | PSEUDO-ALLERGIC REACTIONS | - |
dc.subject.keywordPlus | NF-KAPPA-B | - |
dc.subject.keywordPlus | IN-VITRO | - |
dc.subject.keywordPlus | MRGPRX2 | - |
dc.relation.journalResearchArea | Immunology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Immunology | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
1342, Seongnam-daero, Sujeong-gu, Seongnam-si, Gyeonggi-do, Republic of Korea(13120)031-750-5114
COPYRIGHT 2020 Gachon University All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.