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丁苯酞衍生物对人肝癌SMMC7721细胞的细胞毒活性、构效关系及抗侵袭作用

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

作者信息

Hu Yihan, Bi Xiaoxu, Zhao Pu, Zheng Huachuan, Huang Xueshi

机构信息

Laboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, China.

Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, China.

出版信息

Molecules. 2015 Nov 12;20(11):20312-9. doi: 10.3390/molecules201119699.

Abstract

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.

摘要

从川芎(伞形科)干燥根茎提取物中分离得到一系列丁苯酞衍生物(BPDs)1 - 8。使用一组人类癌细胞系评估了BPDs 1 - 8的细胞毒性活性。此外,还研究了构效关系分析和潜在的抗侵袭活性。C - 7和C - 7a处的sp²碳似乎对BPDs的细胞毒性活性至关重要。BPDs 5和6显著抑制癌细胞的迁移和侵袭。二聚体6的抗侵袭活性被证明明显高于单体5。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0262/6332190/3341ca10ec62/molecules-20-19699-g001.jpg

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