GA 2017

Peroxisome proliferator-activated receptorγ (PPARγ), one of the transcription factors that regulate lipid metabolism and energy use in tumor cells, is a viable target for cancer therapy. In our search for potential PPARγ activator, extracts from five Formosan plants were tested. Among them, Momordica charantia showed the highest ability to activate PPARγ, which led us to identify its potential constituents. Among the seven compounds isolated from M. Charantia, a triterpenoid (Compound 1), was identified as a PPARγ activator with an IC₅₀ of 10 μM in MCF-7 breast cancer cells. Flow cytometric analysis indicated that compound 1 induced G1 cell cycle arrest which might be attributable to the modulation of phosphorylation and expression of numerous key signaling effectors, including cyclin D1, CDK6, and p53. Taken together, these findings suggest that compound 1 may have therapeutic applications in cancer treatment through PPARγ activation.