Activators of peroxisome proliferator-activated receptors
a technology of activated receptors and peroxisomes, applied in the field of activated peroxisome proliferatoractivated receptors, can solve problems such as clinical problems, and achieve the effect of reducing adverse effects
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example 1
Expression of PPARα and PPARγ mRNA in Human Cell Line
[0025] Caco-2 cells (derived from colon cancer) as a human cell line were cultured at 37° C. in RPMI-1640 medium containing 10% fetal calf serum in the presence of 5% CO2. The medium was then replaced with serum-free RPMI-1640 medium and the cells were cultured for 48 hours. In order to examine the effect of NIK-333, a solution of NIK-333 in ethanol was added at a final concentration of 10 μM. At 0, 0.5, 1, 2 and 5 hours after the addition, RNA was extracted to observe mRNA for PPARα, PPARγ 1 and PPARγ 2 by the RT-PCR method.
[0026] As a result, expression of PPARα mRNA was observed from 0.5 hour after the addition of NIK-333 (FIG. 1). Further, expression of PPARγ 1 mRNA was also observed from 0.5 hour after the addition of NIK-333 (FIG. 2), whilst expression of PPARγ 2 mRNA was not observed.
example 2
Ligand Activity for PPARα
[0027] COS-7 cells, a cell line derived from monkey kidney, were cultured at 37° C. in DMEM medium containing 10% fetal calf serum in the presence of 5% CO2. Then, expression vectors of RXRα (retinoic acid X receptor α) and PPARα, and a reporter vector incorporated with PPRE (peroxisome proliferator-responsive element) as a PPAR-responsive element were cotransfected into the cells, and the cells were cultured for 24 hours. In order to examine the effect of NIK-333, a solution of NIK-333 or Wy-14643 (selective agonist of PPARα) in ethanol was added at a final concentration of 10 μM. After cultivation for 24 hours, the activity of firefly luciferase was measured. The measured values were represented as values standardized by using the renilla luciferase activity.
[0028] As shown in FIG. 3, NIK-333 and Wy-14643 failed to increase the luciferase activity when the PPARα expression vector was not introduced (−), whereas they increased the luciferase activity only ...
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