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Curcumin possesses a wide spectrum of liver cancer inhibition effects, yet it has chemical instability and poor metabolic properties as a drug candidate. To alleviate these problems, a series of new mono-carbonyl curcumin derivatives <b>G1–G7</b> were designed, synthesized, and evaluated by in vitro and in vivo studies. Compound <b>G2</b> was found to be the most potent derivative (IC₅₀ = 15.39 μM) compared to curcumin (IC₅₀ = 40.56 μM) by anti-proliferation assay. Subsequently, molecular docking, wound healing, transwell, JC-1 staining, and Western blotting experiments were performed, and it was found that compound <b>G2</b> could suppress cell migration and induce cell apoptosis by inhibiting the phosphorylation of AKT and affecting the expression of apoptosis-related proteins. Moreover, the HepG2 cell xenograft model and H&E staining results confirmed that compound <b>G2</b> was more effective than curcumin in inhibiting tumor growth. Hence, <b>G2</b> is a promising leading compound with the potential to be developed as a chemotherapy agent for hepatocellular carcinoma.