He Yan-Jun, Xiao Di, Gong Qi-Zhe, Zhu Jia-Xin, Jiang Xue-Yang, Dai Wei-Qiang, Wen Xiao-Dong, Feng Feng, Qu Wei
Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, China.
State Key Laboratory Natural Medicines, China Pharmaceutical University, Nanjing, China.
Nat Prod Res. 2025 Feb 3:1-8. doi: 10.1080/14786419.2025.2459804.
-Sauchinone is a bioactive lignan isolated from (Lour.) Baill could suppress the migration and invasion of hepatocellular carcinoma (HCC) cells. The study involves the structural modification of -sauchinone to augment its inhibitory effect on HCC progression and to investigate the mechanisms involved. In this study, a series of -sauchinone based amide derivatives were synthesised and the anticancer activities were evaluated against two hepatoma cell lines. Among them, compound exhibited excellent resistance to migration and invasion by reversing the epithelial-mesenchymal transition (EMT) and inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3) and the expression of matrix metalloproteinases (MMPs). Molecular docking results indicate that compound may exert its inhibitory effect on the progression of liver cancer by acting on the DNA-binding domain of STAT3. These results suggested that compound could be a potential anticancer agent, especially for metastatic cancer therapy.