Hypericin, a Naphthodianthrone Derivative, Prevents Methylglyoxal-Induced Human Endothelial Cell Dysfunction
Biomolecules & Therapeutics
;
: 158-164, 2017.
Article
in English
| WPRIM
| ID: wpr-32629
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pyruvaldehyde
/
Protein Kinase C
/
Cell Death
/
Reactive Oxygen Species
/
Apoptosis
/
Hypericum
/
Mitogen-Activated Protein Kinases
/
Endothelial Cells
/
Atherosclerosis
/
Human Umbilical Vein Endothelial Cells
Limits:
Humans
Language:
English
Journal:
Biomolecules & Therapeutics
Year:
2017
Type:
Article
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