Biapigenin, Candidate of an Agonist of Human Peroxisome Proliferator-Activated Receptor γ with Anticancer Activity

Abstract

School of Life Sciences and Biotechnology, College of Natural Sciences, Kyungpook National University, Daegu 702-701, KoreaReceived June 27, 2011, Accepted June 30, 2011Peroxisome proliferator-activated receptors (PPARs) are a subfamily of nuclear receptors (NRs). Humanperoxisome proliferator-activated receptor gamma (hPPARγ) has been implicated in the pathology ofnumerous diseases, including obesity, diabetes, and cancer. ELISA-based hPPARγ activation assay showedthat biapigenin increased the binding between hPPARγ and steroid receptor coactivator-1 (SRC-1) byapproximately 3-fold. In order to confirm that biapigenin binds to hPPAR γ, fluorescence quenching experimentwas performed. The results showed that biapigenin has higher binding affinity to hPPARγ at nanomolarconcentrations compared to indomethacin. Biapigenin showed anticancer activity against HeLa cells.Biapigenin was noncytotoxic against HaCa T cell. All these data implied that biapigenin may be a potentagonist of hPPARγ with anticancer activity. We will further investigate its anticancer effects against humancervical cancer.Key Words : Biapigenin, PPARγ agonist, Biflavonoid, Anticancer agentsIntroductionPeroxisome proliferator-activated receptors (PPARs) are asubfamily of nuclear receptors (NRs). Nuclear receptors(NRs) are ligand activated transcription factors found incells that are responsible for perceiving hormones and othermolecules.