Hypericin, a Naphthodianthrone Derivative, Prevents Methylglyoxal-Induced Human Endothelial Cell Dysfunction
- Authors
- Do, Moon Ho; Kim, Sun Yeou
- Issue Date
- 1-Mar-2017
- Publisher
- KOREAN SOC APPLIED PHARMACOLOGY
- Keywords
- Advanced glycation end products; Methylglyoxal; HUVECs; Hypericin; Apoptosis
- Citation
- BIOMOLECULES & THERAPEUTICS, v.25, no.2, pp.158 - 164
- Journal Title
- BIOMOLECULES & THERAPEUTICS
- Volume
- 25
- Number
- 2
- Start Page
- 158
- End Page
- 164
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/6324
- DOI
- 10.4062/biomolther.2016.034
- ISSN
- 1976-9148
- Abstract
- Methylglyoxal (MGO) is a highly reactive metabolite of glucose which is known to cause damage and induce apoptosis in endothelial cells. Endothelial cell damage is implicated in the progression of diabetes-associated complications and atherosclerosis. Hypericin, a naphthodianthrone isolated from Hypericum perforatum L. (St. John's Wort), is a potent and selective inhibitor of protein kinase C and is reported to reduce neuropathic pain. In this work, we investigated the protective effect of hypericin on MGO-induced apoptosis in human umbilical vein endothelial cells (HUVECs). Hypericin showed significant anti-apoptotic activity in MGO-treated HUVECs. Pretreatment with hypericin significantly inhibited MGO-induced changes in cell morphology, cell death, and production of intracellular reactive oxygen species. Hypericin prevented MGO-induced apoptosis in HUVECs by increasing Bcl-2 expression and decreasing Bax expression. MGO was found to activate mitogen-activated protein kinases (MAPKs). Pretreatment with hypericin strongly inhibited the activation of MAPKs, including P38, JNK, and ERK1/2. Interestingly, hypericin also inhibited the formation of AGEs. These findings suggest that hypericin may be an effective regulator of MGO-induced apoptosis. In conclusion, hypericin downregulated the formation of AGEs and ameliorated MGO-induced dysfunction in human endothelial cells.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - 약학대학 > 약학과 > 1. Journal Articles
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/6324)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.