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Plos One : Curcumin as a Potent and Selective Inhibitor of 11B- Hydroxysteroid Dehydrogenase 1 ; Improving Lipid Profiles in High-fat-diet-treated Rats, Volume 7

By Verma, Chandra

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Book Id: WPLBN0003935750
Format Type: PDF eBook :
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Reproduction Date: 2015

Title: Plos One : Curcumin as a Potent and Selective Inhibitor of 11B- Hydroxysteroid Dehydrogenase 1 ; Improving Lipid Profiles in High-fat-diet-treated Rats, Volume 7  
Author: Verma, Chandra
Volume: Volume 7
Language: English
Subject: Journals, Science, Medical Science
Collections: Periodicals: Journal and Magazine Collection
Historic
Publication Date:
Publisher: Plos

Description
Description : Background : 11b-hydroxysteroid dehydrogenase 1 (11b-HSD1) activates glucocorticoid locally in liver and fat tissues to aggravate metabolic syndrome. 11b-HSD1 selective inhibitor can be used to treat metabolic syndrome. Curcumin and its derivatives as selective inhibitors of 11b-HSD1 have not been reported. Methodology : Curcumin and its 12 derivatives were tested for their potencies of inhibitory effects on human and rat 11b- HSD1 with selectivity against 11b-HSD2. 200 mg/kg curcumin was gavaged to adult male Sprague-Dawley rats with highfat- diet-induced metabolic syndrome for 2 months. Results and Conclusions : Curcumin exhibited inhibitory potency against human and rat 11b-HSD1 in intact cells with IC50 values of 2.29 and 5.79 mM, respectively, with selectivity against 11b-HSD2 (IC50, 14.56 and 11.92 mM). Curcumin was a competitive inhibitor of human and rat 11b-HSD1. Curcumin reduced serum glucose, cholesterol, triglyceride, low density lipoprotein levels in high-fat-diet-induced obese rats. Four curcumin derivatives had much higher potencies for Inhibition of 11b-HSD1. One of them is (1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one (compound 6), which had IC50 values of 93 and 184 nM for human and rat 11b-HSD1, respectively. Compound 6 did not inhibit human and rat kidney 11b-HSD2 at 100 mM. In conclusion, curcumin is effective for the treatment of metabolic syndrome and four novel curcumin derivatives had high potencies for inhibition of human 11b-HSD1 with selectivity against 11b-HSD2.

 

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