3 ',4 '-Dimethoxythioflavone induces endothelium-dependent vasorelaxation through activation of epidermal growth factor receptor
- Authors
- Jang, Eun Jin; Seok, Young Mi; Lee, Jae In; Cho, Hyun Min; Sohn, Uy Dong; Kim, In Kyeom
- Issue Date
- Apr-2013
- Publisher
- SPRINGER
- Keywords
- 3 ',4 '-Dimethoxythioflavone; Endothelium-dependent vasorelaxation; EGF receptor; Src/ERK pathway
- Citation
- NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, v.386, no.4, pp 339 - 350
- Pages
- 12
- Journal Title
- NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
- Volume
- 386
- Number
- 4
- Start Page
- 339
- End Page
- 350
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/14724
- DOI
- 10.1007/s00210-012-0818-z
- ISSN
- 0028-1298
1432-1912
- Abstract
- It is of interest to investigate whether synthetic thioflavonoids have vasorelaxant actions as natural flavonoids. We tested the hypothesis that 3',4'-dimethoxythioflavone induces endothelium-dependent vasorelaxation through activation of epidermal growth factor (EGF) receptor. Rat aortic rings were mounted in organ baths and subjected to relaxation upon contraction. 3',4'-Dimethoxythioflavone induced endothelium-dependent vasorelaxation, which was attenuated by pretreatment with either l-N (omega)-nitroarginine methyl ester, an inhibitor of nitric oxide synthase, or 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, an inhibitor of soluble guanylate cyclase. 3',4'-Dimethoxythioflavone-induced vasorelaxation was not affected by pretreatment with a general estrogen receptor antagonist ICI 182,780, a selective estrogen receptor-alpha antagonist methyl-piperidino-pyrazole dihydrochloride, or a G protein-coupled receptor 30 antagonist G15. However, pretreatment with EGF receptor blockers AG1478 or DAPH, but not with a phosphatidylinositol-3 kinase inhibitor LY294002 or an Akt1/2 kinase inhibitor Akt inhibitor VIII, attenuated 3',4'-dimethoxythioflavone-induced vasorelaxation. In addition, pretreatment with a Src inhibitor PP2 or an ERK inhibitor U0126 also attenuated vascular relaxation induced by the cumulative addition of 3',4'-dimethoxythioflavone. However, neither a mitochondrial electron transport inhibitor rotenone, an NADPH oxidase inhibitor apocynin, nor a superoxide dismutase mimetic MnTMPyP affected the vascular relaxation induced by the cumulative addition of 3',4'-dimethoxythioflavone. In conclusion, 3',4'-dimethoxythioflavone induces endothelium-dependent vasorelaxation through activation of EGF receptor and Src/ERK pathway in rat aorta.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - College of Pharmacy > School of Pharmacy > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.