Three new C-27-carboxylated-lupane-triterpenoid derivatives from Potentilla discolor Bunge and their in vitro antitumor activities
文献类型： 外文期刊
作者： Zhang, Jing 1 ; Liu, Chao 2 ; Huang, Ri-Zhen 1 ; Chen, Hui-Feng 1 ; Liao, Zhi-Xin 1 ; Sun, Jin-Yue 2 ; Xia, Xue-Kui 3 ; W 1 ;
作者机构： 1.Southeast Univ, Sch Chem & Chem Engn, Dept Pharmaceut Engn, Nanjing, Jiangsu, Peoples R China
2.Shandong Acad Agr Sci, Inst Agrofood Sci & Technol, Key Lab Agroprod Proc Technol Shandong Prov, Jinan, Peoples R China
3.Shandong Acad Sci, Biotechnol Ctr, Jinan, Peoples R China
4.Inst Shandong River Wetlands, Laiwu, Peoples R China
期刊名称：PLOS ONE （ 影响因子：3.24； 五年影响因子：3.788 ）
ISSN： 1932-6203
年卷期： 2017 年 12 卷 4 期
页码：
收录情况： SCI
摘要： Three new lupane-triterpenoids (1-3) along with six known compounds (4-9) were isolated from the ethanolic extract of whole plant of Potentilla discolor Bunge. The structures of Compounds 1-3 were established by extensive 1D and 2D NMR together with other spectrum analysis, indicating that their C-27 positions were highly oxygenated, which were rarely found in nature. Their in vitro anti-proliferative activities against HepG-2, MCF-7 and T-84 cell lines were evaluated by Cell Counting Kit-8 (CCK-8) assay, and the results showed different activities for three cell lines with IC50 values ranging from 17.84 to 40.64 mu M. In addition, the results from Hoechst 33258 and AO/EB staining as well as annexinV-FITC assays exhibited Compound 1 caused a markedly increased HepG-2 cellular apoptosis in a dose-dependent manner. The further mechanisms of Compound 1-induced cellular apoptosis were confirmed that 1 induced the production of ROS and the alteration of pro-and anti-apoptotic proteins, which led to the dysfunction of mitochondria and activation of caspase-9 and caspase-3 and finally caused cellular apoptosis. These results would be useful in search for new potential antitumor agents and for developing semisynthetic lupane-triterpenoid derivatives with high antitumor activity.
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