Abstract
Background: MBT1805 is a novel pan-Peroxisome Proliferator-Activated Receptor (PPAR) agonist. Materials and Methods: In vitro, transfection and luciferase assays tested EC50 values of MBT1805. In vivo, hypoglycemic and hypolipidemic effects of MBT1805 were observed in db/db mice compared with Rosiglitazone. Results: In vitro, MBT1805 activates human PPARα, PPARγ and PPARδ with EC50 values of 8.46μM, 11.94μM, 11.15μM, respectively. Results showed that the bodyweight of db/db mice treated with MBT1805 was not changed. By contrast, Rosiglitazone-treated mice showed significant weight gain (p<0.05). MTB1805 decreased blood glucose level without causing noticeable hepatocytes damage. Conclusion: The novel balanced pan-PPAR agonist, MBT1805 has moderate hypoglycemic and hypolipidemic effects, and does not cause weight gain, hepatocyte damage and hepatic lipid deposition. These experimental results indicate that MBT1805 is safe in the treatment of type 2 diabetes.
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