Emodin, an 11 beta-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts anti-diabetic effect in ob/ob mice
文献类型：期刊论文
| 作者 | Wang, Yue-jing; Huang, Su-ling ; Feng, Ying; Ning, Meng-meng; Leng, Ying
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2012-09 |
| 卷号 | 33期号:9页码:1195-1203 |
| 关键词 | emodin 11 beta-hydroxysteroid dehydrogenase type 1 adipocyte glucocorticoid type 2 diabetes ob/ob mice |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2012.87 |
| 文献子类 | Article |
| 英文摘要 | Aim: Emodin (1,3,8-trihydroxy-6-methylanthraquinone) is a potent and selective inhibitor of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) with the ability to ameliorate metabolic disorders in diet-induced obese mice. In the present study, we investigated the effects of emodin on adipocyte function and the underlying mechanisms in vitro, and its anti-diabetic effects in ob/ob mice. Methods: 3T3-L1 adipocytes were used for in vitro studies. 11 beta-HSD1A activity was evaluated with a scintillation proximity assay. The adipogenesis, glucose uptake, lipolysis and adiponectin secretion were investigated in 3T3-L1 adipocytes treated with emodin in the presence of active (corticosterone) or inactive glucocorticoid (11-dehydrocorticosterone). For in vivo studies, ob/ob mice were administered emodin (25 and 50 mg.kg(-1).d(-1), ip) for 26 d. On the last day of administration, the serum was collected and the mesenteric and perirenal fat were dissected for analyses. Results: Emodin inhibited the 11 beta-HSD1 activity in 3T3-L1 adipocytes in concentration-and time-dependent manners (the IC50 values were 7.237 and 4.204 mu mol/L, respectively, after 1 and 24 h treatment. In 3T3-L1 adipocytes, emodin (30 mu mol/L) suppressed 11-dehydrocorticosterone-induced adipogenesis without affecting corticosterone-induced adipogenesis; emodin (3 mu mol/L) reduced 11-dehydrocorticosterone-stimulated lipolysis, but had no effect on corticosterone-induced lipolysis. Moreover, emodin (3 mu mol/L) partly reversed the impaired insulin-stimulated glucose uptake and adiponectin secretion induced by 11-dehydrocorticosterone but not those induced by corticosterone. In ob/ob mice, long-term emodin administration decreased 11 beta-HSD1 activity in mesenteric adipose tissues, lowered non-fasting and fasting blood glucose levels, and improved glucose tolerance. Conclusion: Emodin improves the inactive glucocorticoid-induced adipose tissue dysfunction by selective inhibition on 11 beta-HSD1 in adipocyte in vitro and improves glycemic control in ob/ob mice. |
| WOS关键词 | INDUCED OBESE MICE ; ADIPOSE-TISSUE ; PEROXISOME-PROLIFERATOR ; GLUCOCORTICOID ACTION ; INSULIN SENSITIVITY ; METABOLIC SYNDROME ; VISCERAL OBESITY ; RESISTANCE ; MINIREVIEW |
| 资助项目 | National Basic Research Program of China (973 Program)[2009CB522300] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program", China[2009ZX09103-061] ; National Natural Science Foundation of China[30873106] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4635871 |
| WOS记录号 | WOS:000308391000012 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277968]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Leng, Ying |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Yue-jing,Huang, Su-ling,Feng, Ying,et al. Emodin, an 11 beta-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts anti-diabetic effect in ob/ob mice[J]. ACTA PHARMACOLOGICA SINICA,2012,33(9):1195-1203. |
| APA | Wang, Yue-jing,Huang, Su-ling,Feng, Ying,Ning, Meng-meng,&Leng, Ying.(2012).Emodin, an 11 beta-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts anti-diabetic effect in ob/ob mice.ACTA PHARMACOLOGICA SINICA,33(9),1195-1203. |
| MLA | Wang, Yue-jing,et al."Emodin, an 11 beta-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts anti-diabetic effect in ob/ob mice".ACTA PHARMACOLOGICA SINICA 33.9(2012):1195-1203. |
入库方式： OAI收割
来源：上海药物研究所
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