Role of CMHX003,a novel peroxisome proliferator-activated receptor γ selective partial agonist in enhancing insulin sensitivity in 3T3-L1 cells
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Role of CMHX003,a novel peroxisome proliferator-activated receptor γ selective partial agonist in enhancing insulin sensitivity in 3T3-L1 cells
Journal of Chongqing Medical UniversityVol. 38, Issue 5, Pages: 573-577(2014)
作者机构:
1. 重庆医科大学附属第一医院脂糖代谢实验室,重庆,400016
2. 重庆医科大学药学院药物化学教研室,重庆,400016
3. 重庆医科大学公共卫生与管理学院营养与卫生学教研室,重庆,400016
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Published:2014,
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Ming Yue, Hu Xiangnan, LI Jibin, et al. Role of CMHX003,a novel peroxisome proliferator-activated receptor γ selective partial agonist in enhancing insulin sensitivity in 3T3-L1 cells. [J]. Journal of Chongqing Medical University 38(5):573-577(2014)
DOI:
Ming Yue, Hu Xiangnan, LI Jibin, et al. Role of CMHX003,a novel peroxisome proliferator-activated receptor γ selective partial agonist in enhancing insulin sensitivity in 3T3-L1 cells. [J]. Journal of Chongqing Medical University 38(5):573-577(2014)DOI:
Role of CMHX003,a novel peroxisome proliferator-activated receptor γ selective partial agonist in enhancing insulin sensitivity in 3T3-L1 cells
Objective:To investigate the effect of CMHX003,a novel peroxisome proliferator-activated receptor γ(PPARγ) selective partial agonist,on the enhancement of insulin sensitivity in 3T3-L1 preadipocytes. Methods:PPARγ agonist activity was determined by using luci-ferase reporter gene assay. 3T3-L1 preadipocytes were differentiated into adipocytes according to standard protocols. Oil red O staining was performed at the end of differentiation and the adiponectin and aP2 mRNA levels were detected by real-time PCR. The secreted adiponectin levels in the culture medium were measured with mouse adiponectin ELISA kit. Results:The result of luciferase reporter assay suggested that PPARγ agonist activity of CMHX003 was higher than that of rosiglitazone(2.46±0.08,3.31±0.15,F=132.19,P=0.008). CMHX003 had weaker role in promoting 3T3-L1 preadipocyte differentiation and triglyceride accu-mulation than rosiglitazone but similar role in increasing expression and secretion of adiponectin(59.41±3.01,107.91±16.49, χ2=9.031,P=0.112)(74.61±16.94,140.07±30.67, χ2=9.051,P=0.135) as rosiglitazone. Meanwhile,CMHX003 was less likely to increase aP2 expression(3.07±1.86,75.95±26.04, χ2=8.868,P=0.049). Conclusions:CMHX003 may potentially be developed into an effective and safe agent in the treatment of type 2 diabetes mel-litus and metabolic disorders.
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