Thiazolopyridines Improve Adipocyte Function by Inhibiting 11 Beta-HSD1 Oxoreductase Activity

Figure 5

Tetrahydrothiazolopyridine derivatives TR-01–4 reduced adipogenesis in the 3T3-L1 adipocytes in a dose-dependent manner. Adipocyte differentiation in the presence of 1 μM cortisone (Csn) was half less efficient than standard 0.25 μM dexamethasone (Dex) induction as evident from induction of the (a) 11β-HSD1 activity, (b) 11β-HSD1 expression, or (c) lipid accumulation. Dosing of cortisone-treated adipocytes with 0–10 μM of TR-01–4 further decreased (d) lipid accumulation as quantified with Oil red O staining and (e) 11β-HSD1 mRNA levels as measured by qPCR. (f) Oil red O staining of adipocytes differentiated with different concentrations of TR-04 for 8 days. Data are the mean ± SEM (), , , and versus vehicle control by Dunnett’s test subsequent to one-way ANOVA.

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