Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 서은경 | * |
dc.date.accessioned | 2016-08-28T12:08:54Z | - |
dc.date.available | 2016-08-28T12:08:54Z | - |
dc.date.issued | 2010 | * |
dc.identifier.issn | 0378-8741 | * |
dc.identifier.other | OAK-7062 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/221176 | - |
dc.description.abstract | Aim of the study: Poncirus fructus (PF) - also known as the dried, immature fruit of Poncirus trifoliata (L.) Raf. (Rutaceae) - is a natural substance that has long been used for various gastrointestinal disorders in eastern Asia. An aqueous extract of PF (PF-W) has particularly potent gastroprokinetic effects, but its molecular mechanism was not well understood. Identification of the underlying prokinetic mechanism of PF-W was pursued in the present study. Materials and methods: Changes in in vitro cAMP levels and in vivo intestinal transit rate (ITR) caused by PF-W were measured after pretreatment with GR125487, an antagonist for serotonin receptor subtype 4 (5-HT4R). An [ 3H] astemizole binding assay and electrophysiology experiments were performed to determine if PF-W has any interaction with the human ether-à-go-go related gene (hERG) potassium channel. Results: PF-W induced an increase in intracellular cAMP in 5-HT4R-expressing HEK293T cells, indicating that PF-W does activate 5-HT4R. Moreover, pretreatment with GR125487 successfully blocked the increase, suggesting that the response was 5-HT4R-specific. More importantly, pretreatment of GR125487 in rats inhibited the elevation of ITR by PF-W, indicating that the prokinetic effect of PF-W was indeed exerted via 5-HT4R. On the other hand, both [ 3H]-astemizole binding assay and electrophysiological experiments revealed that PF-W did not interfere at all with the hERG channel. Conclusion: It was found that PF-W exerts its prokinetic activity through a 5-HT4R-mediated pathway, with no interaction with hERG channels. Therefore, PF-W is a good candidate that might be developed as a prokinetic agent with fewer expected cardiac side effects. © 2010 Elsevier Ireland Ltd. | * |
dc.language | English | * |
dc.title | An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction | * |
dc.type | Article | * |
dc.relation.issue | 1 | * |
dc.relation.volume | 132 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 328 | * |
dc.relation.lastpage | 333 | * |
dc.relation.journaltitle | Journal of Ethnopharmacology | * |
dc.identifier.doi | 10.1016/j.jep.2010.08.042 | * |
dc.identifier.wosid | WOS:000284442100042 | * |
dc.identifier.scopusid | 2-s2.0-77957798837 | * |
dc.author.google | Shim W.-S. | * |
dc.author.google | Back H. | * |
dc.author.google | Jung S.-W. | * |
dc.author.google | Kim J.-W. | * |
dc.author.google | Jang Y. | * |
dc.author.google | Lee B. | * |
dc.author.google | Seo E.-K. | * |
dc.author.google | Oh U. | * |
dc.author.google | Shim C.-K. | * |
dc.contributor.scopusid | 서은경(7005953758) | * |
dc.date.modifydate | 20240118144717 | * |