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Discovery and synthesis of rocaglaol derivatives inducing apoptosis in HCT116 cells via suppression of MAPK signaling pathway
Yang,Hao-Jie; Li,Ya-Nan; Yan,Chen; Yang,Jue; Zeng,Yan-Rong; Yi,Ping; Li,Yan-Mei; Hao,Xiao-Jiang; Yuan,Chun-Mao
2021
发表期刊FITOTERAPIA
ISSN0367-326X
卷号151页码:104876
摘要Six rocaglaol derivatives were isolated from Dysoxylum gotadhora, and those compounds showed good cytotoxic activity with IC50 values ranging from 10 to 350 ng/mL against five different cancer cells. Obviously, further total synthesis of rocaglaol derivatives for medical chemistry study is of great significance. Then, twenty six rocaglaol derivatives including 25 new compounds were designed, synthesized, and evaluated for their cytotoxic activities against three human cancer cell lines: human colon cancer cells (HCT116), colorectal cancer stem cells (P6C), and human red leukocyte leukemia cells (HEL), using MTT assay. Most of derivatives showed good cytotoxic activities, with the lowest IC50 being 3.2 nM for HEL cells, which was 169 times stronger than that of the positive control (doxorubicin). Further mechanism study indicated that 11k could significantly suppress MAPK pathway in HCT116 cells, which may responsible for induction of apoptosis and cell cycle arrest.
关键词Dysoxylum gotadhora Rocaglaol derivatives HCT116 Cytotoxic activity MAPK pathway FLAVAGLINES
DOI10.1016/j.fitote.2021.104876
WOS记录号WOS:000663435300023
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文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/73493
专题中国科学院昆明植物研究所
作者单位1.Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China
2.Chinese Acad Sci, Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550014, Peoples R China
3.An Shun City Peoples Hosp, Anshun 561000, Peoples R China
4.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
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Yang,Hao-Jie,Li,Ya-Nan,Yan,Chen,et al. Discovery and synthesis of rocaglaol derivatives inducing apoptosis in HCT116 cells via suppression of MAPK signaling pathway[J]. FITOTERAPIA,2021,151:104876.
APA Yang,Hao-Jie.,Li,Ya-Nan.,Yan,Chen.,Yang,Jue.,Zeng,Yan-Rong.,...&Yuan,Chun-Mao.(2021).Discovery and synthesis of rocaglaol derivatives inducing apoptosis in HCT116 cells via suppression of MAPK signaling pathway.FITOTERAPIA,151,104876.
MLA Yang,Hao-Jie,et al."Discovery and synthesis of rocaglaol derivatives inducing apoptosis in HCT116 cells via suppression of MAPK signaling pathway".FITOTERAPIA 151(2021):104876.
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