机构：[a]Laboratory of Ethnopharmacology, Institute for Nanobiomedical Technology and Membrane Biology, West China Hospital, Sichuan University, Chengdu 610041, China[b]Regenerative Medicine Research Center, West China Hospital, Sichuan University, Chengdu 610041, China[c]Department of Integrated Traditional Chinese and Western Medicine, West China Hospital, Sichuan University, Chengdu 610041, China[d]Institute of Sort Science, Sichuan University, Chengdu 610041, China[e]College of Mathematics, Sichuan University, Chengdu 610041, China
A series of diosgenyl analogs were prepared from diosgenin to evaluate their anticancer activity and antithrombotic property. Analog 4, which had a spiroketal structure with a 6-aminohexanoic acid residue, exhibited the highest potency against all five tumor cell lines. It significantly blocked tumor growth, induced cell apoptosis and autophagy, and regulated cellular calcium concentration, mitochondrial membrane potential, adenosine triphosphate, and cell cycle. In addition, fluorescence-tagged compounds indicated that the analogs could rapidly accumulate in the cytoplasm, but no specific localization in the nucleus of cancer cells was observed. Furthermore, preliminary structure-activity relationship studies demonstrated that spiroketal analogs exhibit better antithrombotic activity than furostanic analogs, which exhibit the opposite effect by promoting thrombosis. Our study indicates that compound 4 may be a promising anticancer drug candidate for cancer patients with thromboembolism.
基金：
China National "12.5" Research Foundation [2011BAJ07B04]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China [20972105]; Sichuan Province Research Foundation [2008SZ0024]
语种：
外文
WOS：
PubmedID：
中科院(CAS)分区：
出版当年[2017]版：
大类|4 区医学
小类|4 区应用化学4 区药物化学4 区药学4 区植物科学
最新[2023]版：
大类|3 区医学
小类|4 区应用化学4 区药物化学4 区药学4 区植物科学
第一作者：
第一作者机构：[a]Laboratory of Ethnopharmacology, Institute for Nanobiomedical Technology and Membrane Biology, West China Hospital, Sichuan University, Chengdu 610041, China
通讯作者：
通讯机构：[a]Laboratory of Ethnopharmacology, Institute for Nanobiomedical Technology and Membrane Biology, West China Hospital, Sichuan University, Chengdu 610041, China[b]Regenerative Medicine Research Center, West China Hospital, Sichuan University, Chengdu 610041, China[c]Department of Integrated Traditional Chinese and Western Medicine, West China Hospital, Sichuan University, Chengdu 610041, China
推荐引用方式(GB/T 7714)：
Bao-Zhan Huang,Guang Xin,Li-Mei Ma,et al.Synthesis, characterization, and biological studies of diosgenyl analogs.[J].Journal of Asian natural products research.2017,19(3):272-298.doi:10.1080/10286020.2016.1202240.
APA：
Bao-Zhan Huang,Guang Xin,Li-Mei Ma,Ze-Liang Wei,Yan Shen...&Wen Huang.(2017).Synthesis, characterization, and biological studies of diosgenyl analogs..Journal of Asian natural products research,19,(3)
MLA：
Bao-Zhan Huang,et al."Synthesis, characterization, and biological studies of diosgenyl analogs.".Journal of Asian natural products research 19..3(2017):272-298
