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

摘要

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