tetrahydrocurcumin-di-phenylalanine

Tetrahydrocurcumin-di-phenylalanine (THC-di-Phe) is a small-molecule research compound consisting of tetrahydrocurcumin (a major metabolite of curcumin) conjugated with two phenylalanine amino acids via carbamate ester linkages. It was synthesized and evaluated as a LAT1 (Large Amino Acid Transporter 1)-targeting anticancer agent. In preclinical studies using C6 glioma cells, THC-di-Phe demonstrated significantly higher cytotoxicity (IC50 ~35.8 μM) than tetrahydrocurcumin alone, inducing cell death via necrosis and apoptosis, and inhibiting cell proliferation and migration. It also inhibited the P70SK/S6 signaling pathway downstream of LAT1 and displayed a binding mode to the LAT1 active site similar to known LAT1 inhibitors. The compound is being investigated for the treatment of glioma (brain cancer).

Other names

THC-di-phenylalaninetetrahydrocurcumin-di-phenylalanine conjugate