Fig. 2.
t9,t11-CLA mediated induction of the LXR target genes SREBP-1c, ABCA1 and ABCG1 requires LXRα. Displayed is the relative mRNA expression of THP-1 RG108 pretreated with no siRNA, control siRNA or siRNA against human LXRα, measured with qRT-PCR. THP-1 cells were stimulated with 100 μM t9,t11-, 100 μM c9,t11-CLA or 1 μM T0901317 for 24 h.
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Effective concentration range of t9,t11-CLA
To determine the effective concentration range of t9,t11-CLA isomer human primary macrophages were treated with doses from 5 μM to 50 μM and ABC-transporter expression was determined. To evaluate the t9,t11-CLA mediated activation potency expression levels were compared to well described and established doses of 22(R)-HC, GW3965 and T0901317. t9,t11-CLA induced transcription of the ABC-transporters concentration dependently ( Fig. 3). Most importantly, 10 μM t9,t11-CLA induced ABCA1 expression and ABCG1 expression significantly. Concerning activation potency a dose of 25 μM t9,t11-CLA was comparable to 5 μM 22(R)-HC and 50 μM t9,t11-CLA was comparable to 5 μM GW3965.