Synthesis and evaluation as potential antitumor agents of novel ursolic acid derivatives

被引：15

作者：

Liu, Ming-Chuan ^{[1
,2
]}

Yang, Sheng-Jie ^{[1
,2
]}

Jin, Lin-Hong ^{[1
]}

Hu, De-Yu ^{[1
]}

Xue, Wei ^{[1
]}

Yang, Song ^{[1
]}

机构：

[1] Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China

[2] Sinphar Tian Li Pharmaceut Co Ltd, Res Inst, Hangzhou 311100, Zhejiang, Peoples R China

来源：

MEDICINAL CHEMISTRY RESEARCH | 2016年 / 25卷 / 10期

关键词：

Ursolic acid derivatives; Synthesis; Antitumor activity; Apoptosis; NITRIC-OXIDE PRODUCTION; HIGHLY-ACTIVE INHIBITORS; CELL-CYCLE ARREST; ANTI-HIV ACTIVITY; MOUSE MACROPHAGES; OLEANOLIC ACID; IN-VITRO; URSANE TRITERPENOIDS; CYTOTOXIC ACTIVITY; CARCINOMA-CELLS;

D O I：

10.1007/s00044-016-1680-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel ursolic acid derivatives were synthesized, and their structures were confirmed by MS, IR, H-1 NMR and C-13 NMR spectral analysis. In vitro antitumor activities of these compounds against MGC-803 (gastric cancer cell) and Bcap-37 (breast cancer cell) human cancer cell lines were evaluated by MTT assay. The pharmacological screening results revealed that many derivatives exhibited moderate to high activities against the tested cell lines, and that most demonstrated more potent inhibitory activities than that of ursolic acid. Preliminarily mechanism study of representative compound 3h were carried out by acridine orange/ethidium bromide staining, Hoechst 33258 staining, terminal deoxynucleotidyl transferase biotin-dUTP nick end labeling assay, and flow cytometry which indicated that compound 3h can induce cell apoptosis of MGC-803 cells, and the apoptosis ratio reached 34.59 % after 36 h treatment at 10 mu M.

引用

页码：2267 / 2279

页数：13

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