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

摘要

Peroxisome proliferator-activated receptors (PPARs) are a subfamily of nuclear receptors (NRs). Human peroxisome proliferator-activated receptor gamma (hPPAR_γ) has been implicated in the pathology of numerous diseases, including obesity, diabetes, and cancer. ELISA-based hPPARy activation assay showed that biapigenin increased the binding between hPPAR_γ and steroid receptor coactivator-1 (SRC-1) by approximately 3-fold. In order to confirm that biapigenin binds to hPPAR_γ, fluorescence quenching experiment was performed. The results showed that biapigenin has higher binding affinity to hPPAR_γ at nanomolar concentrations 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 potent agonist of hPPAR_γ with anticancer activity. We will further investigate its anticancer effects against human cervical cancer.