Ghrelin receptor is activated by naringin and naringenin, constituents of a prokinetic agent Poncirus fructus
- Authors
- Jang, Yongwoo; Kim, Su-Won; Oh, Jungeun; Hong, Gyu-Sang; Seo, Eun-Kyoung; Oh, Uhtaek; Shim, Won-Sik
- Issue Date
- 9-Jul-2013
- Publisher
- ELSEVIER IRELAND LTD
- Keywords
- Poncirus fructus; Naringin; Naringenin; Prokinetic; Ghrelin receptor; Motilin receptor
- Citation
- JOURNAL OF ETHNOPHARMACOLOGY, v.148, no.2, pp.459 - 465
- Journal Title
- JOURNAL OF ETHNOPHARMACOLOGY
- Volume
- 148
- Number
- 2
- Start Page
- 459
- End Page
- 465
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/14415
- DOI
- 10.1016/j.jep.2013.04.039
- ISSN
- 0378-8741
- Abstract
- Ethnopharmacological relevance: Poncirus fructus (PF), also known as a dried immature fruit of Poncirus trifoliata (L) Raf. (Rutaceae), has long been traditionally used for the various gastrointestinal disorders in Eastern Asia. Aim of study: The aqueous extract of PF (PF-W) has the strong prokinetic effect, yet the underlying mechanism is still elusive. The present study investigated whether PF-W has any effect on motilin receptor or ghrelin receptor, since these receptors enhance intestinal motility when activated. Materials and methods: The effect of PF-W and its components on motilin or ghrelin receptor was determined by calcium imaging and whole-cell patch clamp methods. Results: PF-W activates the ghrelin receptor, but not the motilin receptor, resulting in a transient increase of intracellular calcium levels. Furthermore, among various constituents of PF, only naringin and naringenin evoked the intracellular calcium augmentation via the ghrelin receptor. Moreover, cortistatin-8 - a ghrelin receptor inhibitor - specifically blocked naringin- and naringenin-induced calcium increases. In addition, naringin and naringenin induced inward currents in ghrelin receptor-expressing cells under whole-cell patch clamp configuration. Conclusion: PF-W activates the ghrelin receptor, and naringin and naringenin are key constituents responsible for the activation of ghrelin receptor. Therefore, the present study suggests that the ghrelin receptor is a molecular entity responsible for the strong prokinetic activity of PF-W. (C) 2013 Elsevier Ireland Ltd. All rights reserved.
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