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Table 3 Induction of transactivation of PPARs

From: Epidermal anti-Inflammatory properties of 5,11,14 20:3: Effects on mouse ear edema, PGE2 levels in cultured keratinocytes, and PPAR activation

 

PPARα

PPARγ

PPARδ

FA

100 μM

200 μM

100 μM

200 μM

100 μM

200 μM

18:2n-6

23

43

8

12

11

13

20:3n-6

17

19

3

3

20

4

20:3n-3

19

49

18

30

53

67

5,11,14 20:3

16

35

22

27

28

56

9,11/10,12 18:2

76

98

11

14

15

32

22:6n-3

65

574

50

298

140

428

  1. Luciferase activity in HeLa cells transfected with human PPARα, δ and γ cDNAs measured 24 h after addition of unesterified FA at indicated concentration. Values represent % of transactivation values obtained in presence of the positive control Wy14,643 at 10 μM for PPARα, and of BRL49653 at 1 μM for PPARγ and PPARδ, taken as 100%. Significant activation is considered >50% of Wy14,643 for PPARα; >75% of BRL49653 for PPARγ and >100% of BRL49653 for PPARδ. Under the assay conditions employed, inhibition values could not be determined. Values represent mean of 3 replicates in independent experiments, with 4 replicates in each experiment.