Synthesis and antitumor evaluation of amino acid conjugates of monocarbonyl curcumin in hepatocellular carcinoma cell.

ABSTRACT: Curcumin possesses a variety of pharmacological properties, particularly anticancer activity. However, its clinical utility is limited by its poor water solubility and low bioavailability. To alleviate the problems, our previous research demonstrated that mono-carbonyl curcumin easters can be employed for the development of novel anticancer agents. In this study, further structural optimization was performed and a series of novel amino acid conjugates of mono-carbonyl curcumin H1-H6 were designed, synthesized, and evaluated by in vitro and in vivo studies. Compound H1 was found as the most potent derivative (IC₅₀ = 8.66 µM) compared to curcumin (IC₅₀ = 36.19 µM) by anti-proliferation assay. Subsequently, wound healing, transwell, JC-1 staining, the HepG2 cell xenograf

SUBMITTER: Cao W 

PROVIDER: S-EPMC11894097 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature