International Journal of Pharmacology (IJP) is published by IMR Press from Volume 21 Issue 4 (2025). Previous articles were published by another publisher under the CC-BY licence, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement.
[5-(3-Indol-1-ylpropoxy)-1H-indol-3-yl] Acetic Acid Enhances Adipocyte Differentiation and Glucose Uptake in 3T3-L1 Cells
1 Department of Biochemistry, Research Institute for Endocrine Sciences and Diabetes Research Center, Chonbuk National University Medical School, Jeonju, Jeonbuk, 561-756, Republic of Korea
2 College of Pharmacy, Sookmyung Women`s University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea
3 Division of Biotechnology, College of Environmental and Bioresource Sciences, Chonbuk National University, Iksan, Jeonbuk, 570-752, Republic of Korea
Abstract
The nuclear receptor peroxisome proliferator-activated receptor γ (PPARγ) plays an important role in adipocyte differentiation and is the target for anti-diabetic drugs known as thiazolidinediones. Here, we synthesized and characterized a new PPARγ agonist, SPA0432. COS-7 cells treated with SPA0432 showed significantly increased PPARγ transcriptional activity compared to that of vehicle-treated cells. However, its efficacy was less than that of rosiglitazone. Using a standard differentiation protocol, SPA0432 effectively enhanced differentiation of 3T3-L1 preadipocytes as evidenced by increased lipid droplet formation and triglyceride accumulation. Real-time RT-PCR analysis indicated that SPA0432 significantly increased the expressions of adipogenesis-related genes, CAAT/enhancer binding protein α, PPARγ, fatty acid synthase, aP2 and lipoprotein lipase and significantly decreased the expression of Pref-1, a preadipocyte marker. Moreover, SPA0432 increased insulin-stimulated glucose uptake in differentiated 3T3-L1 adipocytes. These results suggest that SAP0432 may exert beneficial effects against insulin resistance through its ability to promote adipocyte differentiation and insulin-stimulated glucose uptake.
Keywords
- PPARy
- adipogenesis
- glucose uptake
- insulin
- adipocyte
- rosiglitazone
