中国药科大学学报2017，Vol.48Issue(1)：31-41,11.DOI:10.11665/j.issn.1000-5048.20170105
新型熊果酸衍生物与查耳酮缀合物的合成及其抗肿瘤活性初步评价
Synthesis and preliminary anti-tumor activity of novel ursolic acid derivative-chalcone conjugates
裴婷 1王玉英2
作者信息
- 1. 华中科技大学同济医学院附属武汉中心医院药学部，武汉430014
- 2. 孝感市孝南区妇幼保健计划生育服务中心，孝感432000
- 折叠
摘要
Abstract
Ten novel conjugates with ursolic acid core and different chalcone ligands were synthesized via esteri-fication using the natural ursolic acid as starting material. The structures of these conjugates were confirmed by 1 H NMR, 13 C NMR and HRMS. The preliminary biological results showed that these compounds displayed signifi-cant antiproliferative effect on CNE2, KB, MCF-7, A549 and HepG2 cells. These compounds were more effective than ursolic acid and tamoxifen against MCF-7 cells. Especifically, compound 11e ( IC50 =4. 7 μmol/L) showed the greatest potency against MCF-7, which was about 3-times more potent than tamosifen ( IC50 =15. 2 μmol/L) . Additionally, all conjugates were nontoxic to health MCF-10A and VERO cells, and had higher security than tamoxifen.关键词
熊果酸衍生物/查耳酮缀合物/合成/抗肿瘤活性Key words
ursolic acid derivative-chalcone conjugates/synthesis/anti-tumor activity分类
医药卫生引用本文复制引用
裴婷,王玉英..新型熊果酸衍生物与查耳酮缀合物的合成及其抗肿瘤活性初步评价[J].中国药科大学学报,2017,48(1):31-41,11.
