The triterpene echinocystic acid and its 3-O-glucoside derivative are revealed as potent and selective glucocorticoid receptor agonists
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- 作者：Demetra Georgatzaa ; 1 ; Vyron A. Gorgogietasa ; 1 ; Paraskevi Kylindria ; Maria Ch. Charalambousa ; Kalliope K. Papadopouloua ; Joseph M. Hayesb ; Anna-Maria G. Psarraa ; ampsarra@bio.uth.gr" class="auth_mail" title="E-mail the corresponding author ; ampsarra@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：GCs ; glucocorticoids ; GR ; glucocorticoid receptor ; SEGRA ; selective glucocorticoid receptor agonist ; EA ; echinocystic acid ; EA-3G ; echinocystic acid 3-O-glucoside ; PEPCK ; phosphoenolpyruvate carboxykinase ; NF-κB ; nuclear factor kappa beta ; TNF α ; tumour necrosis factor alpha ; CMX ; mito tracker red CMXRos ; DEX ; dexamethasone ; DAC ; deacylcortivazol ; GREs ; glucocorticoid responsive elements ; LBD ; ligand binding domain ; HPA ; hypothalamic&ndash ; pituitary&ndash ; adrenal ; RLU ; relative luciferase units
- 刊名：International Journal of Biochemistry and Cell Biology
- 出版年：2016
- 出版时间：October 2016
- 年：2016
- 卷：79
- 期：Complete
- 页码：277-287
- 全文大小：2731 K
文摘
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Prediction of glucocorticoid receptor-echinocytic acids binding via molecular docking.
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Echinocystic acids induce glucocorticoid receptor nuclear translocation.
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Echinocystic acids induce NFκΒ transrepression via glucocorticoid receptor activation.
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Echinocystic acids act as potent dissociated glucocorticoid receptor ligands.
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Echinocystic acids augment DEX-induced mitochondrial dependent apoptosis.