Curcumin derivative, inhibitor of DNMT1, a-amylase, and WIF- (C08-0488-876)

Bisdemethoxycurcumin, like its parent compound curcumin, exhibits anticancer, antioxidative, anti-diabetic, anti-inflammatory, and antibacterial activities. Bisdemethoxycurcumin inhibits Wnt signaling by inhibiting WIF-1 promoter demethylation and inhibits DNA methyltransferase 1 (DNMT1), inducing apoptosis in non-small cell lung cancer (NSCLC) cells. Bisdemethoxycurcumin also induces apoptosis in other in vitro cancer models through increases in reactive oxygen species (ROS) and increases in the expression of p53, p21, p16, and retinoblastoma (Rb) protein. This compound activates SIRT1 and AMPK signaling. Bisdemethoxycurcumin inhibits PDGF signaling in smooth muscle cells, preventing cell migration and proliferation. Bisdemethoxycurcumin may also display potential benefit in the treatment of type 2 diabetes, as it acts as a noncompetitive inhibitor of pancreatic a-amylase. Like other curcuminoids, this compound also displays phototoxic antibacterial activity, although it is active primarily against gram-positive bacteria only.