Design, synthesis and biological evaluation of the novel ligustrazine derivatives
10.16438/j.0513-4870.2017-0323
- VernacularTitle:新型川芎嗪类衍生物的设计、合成及其生物活性的研究
- Author:
Yang ZHANG
1
;
Yu YANG
1
;
Jia-ming LI
1
;
Xiao-dong MA
1
;
Yan-chun ZHANG
1
;
Yu-jun WANG
1
;
Pan-hu ZHU
1
Author Information
1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230038, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
ligustrazine derivative;
migration;
invasion;
cell cycle
- From:
Acta Pharmaceutica Sinica
2017;52(11):1722-1730
- CountryChina
- Language:Chinese
-
Abstract:
Using ligustrazine as the leading compound, we designed and synthesized ten novel ligustrazine derivatives, whose structures were determined by 1H NMR, 13C NMR and MS. Inhibitory effects of the new compounds on the proliferation of A549, A549/DDP and HBE cells were detected by MTT assay. The inhibi-tory activity of the synthesized compounds on migration and invasion of A549 cells were evaluated through scratch assay and transwell assay. Mechanism of the inhibition on migration and invasion was investigated by Western blotting. In addition, the cell cycle was analyzed with flow cytometry. The results showed that, both compounds Z8 and Z10 have an anti-proliferative activity, and the potencies of inhibition of tumor-cell migration and invasion were attributed to the down-regulation of MMP-2 and MMP-9. The compounds Z8 and Z10 could also enhance G2/M arrest in A549 cell as revealed by cell cycle analysis.
