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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![]() | |
2021 | |
发表期刊 | FITOTERAPIA
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ISSN | 0367-326X |
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 |
DOI | 10.1016/j.fitote.2021.104876 |
WOS记录号 | WOS:000663435300023 |
引用统计 | |
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 |
推荐引用方式 GB/T 7714 | 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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