Cytotoxic Activities, SAR and Anti-Invasion Effects of Butylphthalide Derivatives on Human Hepatocellular Carcinoma SMMC7721 Cells
Yihan Hu,
Xiaoxu Bi,
Pu Zhao,
Huachuan Zheng,
Xueshi Huang
Affiliations
Yihan Hu
Laboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, China
Xiaoxu Bi
Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, China
Pu Zhao
Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, China
Huachuan Zheng
Cancer Research Center, Key Laboratory of Brain and Spinal Cord Injury of Liaoning Province, and Laboratory Animal Center, the First Affiliated Hospital of Liaoning Medical University, Jinzhou 121001, China
Xueshi Huang
Laboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, China
A series of butylphthalide derivatives (BPDs) 1–8 were isolated from the extract of the dried rhizome of Ligusticum chuanxiong Hort. (Umbelliferae). The cytotoxic activities of BPDs 1–8 were evaluated using a panel of human cancer cell lines. In addition, the SAR analysis and potential anti-invasion activities were investigated. The sp2 carbons at C-7 and C-7a appeared to be essential for the cytotoxic activities of BPDs. BPDs 5 and 6 remarkably inhibited the migration and invasion of cancer cells. The anti-invasion activity of dimer 6 was demonstrated to be significantly higher than monomer 5.
