Cytotoxic Activities, SAR and Anti-Invasion Effects of Butylphthalide Derivatives on Human Hepatocellular Carcinoma SMMC7721 Cells

Molecules

Yihan Hu²  Xiaoxu Bi¹  Pu Zhao¹  Huachuan Zheng³  Xueshi Huang² 

[1] Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, China;Laboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, China;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;

关键词: Ligusticum chuanxiong;    butylphthalides;    cytotoxic activity;    SAR;    anti-invasion;   

DOI  :  10.3390/molecules201119699

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.