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

Bulletin of the Korean chemical society

Eun-Rhan Woo¹  Jin-Kyoung Kim¹  Qinglong Jin¹  Juneyoung Lee¹  Dong Gun Lee¹  Soyoung Shin¹  Do-Young Yoon¹  Eunjung Lee¹  Sojung Lee¹  Yangmee Kim¹  Jee-Young Lee¹ 

关键词: Biapigenin;    PPARγ agonist;    Biflavonoid;    Anticancer agents;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 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.

【 授权许可】

Unknown