Abstract
This study aimed to investigate the mechanism of intervening type II diabetes by flavonoid compound from Agrimonia pilosa Ledeb in vitro. We found flavonoid compound exhibited moderate peroxisome proliferator-activated receptor gamma agonist activity which was lower than that of rosiglitazone by luciferase reporter assay. 3T3-L1 cell differentiation was induced typically in the presence of various concentrations of flavonoid compound or pioglitazone for assaying insulin sensitization. We found that flavonoid compound effectively promoted 3T3-L1 preadipocyte differentiation and lipid deposition, but its intensity was lower than that of pioglitazone. Quantitative polymerase chain reaction assays showed that flavonoid compound promoted the expression of peroxisome proliferator-activated receptor gamma, CCAAT enhancer binding protein-α, and sterol regulatory element-binding protein 1 in a dose-dependent manner. As a result, the expressions of Glut4 and adiponectin were significantly enhanced. Additionally, the expressions of AP2 and lipoprotein lipase induced by flavonoid compound were lower than those by pioglitazone. These findings indicate that flavonoid compound from Agrimonia pilosa Ledeb exhibits the good property of partial peroxisome proliferator-activated receptor gamma agonism, and shares similar insulin-sensitizing effects with pioglitazone, but has lower adipogenic capacity. It is implied that flavonoid compound has a promising prospect of fighting insulin resistance as a partial agonist of peroxisome proliferator-activated receptor gamma.
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Abbreviations
- APL:
-
Agrimonia pilosa Ledeb
- FC:
-
Flavonoid compound
- HEK 293T cells:
-
Human embryonic kidney (HEK) 293T cells
- Q-PCR:
-
Quantitative polymerase chain reaction
- PPARγ:
-
Peroxisome proliferator-activated receptor gamma
- C/EBP-α:
-
CCAAT enhancer binding protein-α
- SREBP-1:
-
Sterol regulatory element-binding protein 1
- Glut4:
-
Glucose transporter
- LPL:
-
Lipoprotein lipase
- AP2:
-
Fat acid binding protein
- IR:
-
Insulin resistance
- TZDs:
-
Thiazolidinediones
- SPPARγMs:
-
Selective PPARγ modulators
- T2DM:
-
Type 2 diabetes
- TCM:
-
Traditional Chinese medicine
- FFA:
-
Free fatty acid
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Acknowledgements
Thank Prof. Xiaoqiu Xiao (Chongqing Medical University) for the gift of 293T cells and Changhua Wang (Chongqing Academy of Chinese Materia Medica) for the verification of plant material. This work was supported by the Fundamental Research Funds for the Central Universities (106112015CDJXY230001), the Basic and Frontier Research Project of Chongqing (cstc2014jcyjA10097), and Three Gorges Natural Medicine Engineering Research Center of Chongqing University of Education (167011).
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Zhu, L., Tan, J., Lou, D. et al. The effects of flavonoid compound from Agrimonia pilosa Ledeb on promotting 3T3-L1 preadipocytes differentiation by activating PPARγ partially. Med Chem Res 26, 2920–2928 (2017). https://doi.org/10.1007/s00044-017-1991-x
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DOI: https://doi.org/10.1007/s00044-017-1991-x