Thiazolidinediones, synthetic ligands for the peroxisome proliferator-activated receptor-g (PPAR-g) are antidiabetic drugs which improve insulin resistance and ameliorate consequences of metabolic syndrome. Therefore in the present study we investigated the metabolic response to novel PPARg agonists. These compounds were chosen from the library of 8000 molecules designed by Organic Synthesis Laboratory, Adamed Ltd. according to competition binding test with the recombinant PPARg Ligand Binding Domain and adipogenic potential performed on mouse embryonic fibroblast 3T3 L1 line.

We measured the effects of orally administrated novel PPARg agonists (10 mg/kg body weight for two weeks): AD10 369, AD10 371, AD10 797, AD10 798 and AD10 1025 on glucose, triglyceride, total cholesterol, LDL and HDL plasma levels in db/db mice - an animal type 2 diabetes model. Additionally we estimated the effect of novel PPARg agonists on de novo glucose and lactate synthesis in primary cultured renal tubule cells isolated from rabbits and growing in hormonally defined medium. The metabolic action of novel PPARg agonists were compared with the effect of rosiglitazone - a compound licensed for use in selected diabetes patients.

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1. New phenylpropanoic acid derivative with antidiabetic potential acting as a partial PPAR gamma agonist – preclinical studies.
2. New phenylpropanoic acid derivative with antidiabetic potential acting as a partial PPAR gamma agonist – preclinical studies.
3. MODULATION OF TRANSCRIPTIONAL ACTIVITY IN ADIPOSE TISSUE OF db/db MICE AFTER ORAL ADMINISTRATION OF NOVEL POTENTIAL ANTIDIABETIC DRUGS (AD10369, AD10371, AD10797, AD10798 AND AD101025).