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Two New Cytotoxic Maytansinoids Targeting Tubulin from Trewia nudiflora
Lei, Chun1; Li, Ya-Nan1; Li, Jia-Nan2,4,5; Zhou, Yu-Bo2,4,5; Cui, Ming-Jun3; Fu, Kai-Cong3; Li, Jia2,4,5; Hou, Ai-Jun1
刊名PLANTA MEDICA
2021-10-29
页码7
关键词Trewia nudiflora Euphorbiaceae maytansinoids cytotoxicity tubulin polymerization
ISSN号0032-0943
DOI10.1055/a-1530-1128
通讯作者Li, Jia(jli@simm.ac.cn) ; Hou, Ai-Jun(ajhou@shmu.edu.cn)
英文摘要Two new maytansinoids, N -methyltreflorine ( 1 ) and methyltrewiasine ( 2 ), were isolated from the dried fruits of Trewia nudiflora , together with three known congeners ( 3 - 5 ). Their structures were elucidated by spectroscopic methods, and the absolute configuration of 1 and 2 was determined by X-ray crystallographic analysis. Compounds 1 - 5 exhibited strong cytotoxicity against human tumor cell lines, including HeLa, MV-4-11, and MCF-7, with IC (50) values ranging from 0.12 to 11nM. Compounds 1 and 4 also showed inhibitory activity against the MCF-7/ADR cell line with IC (50) values of 13 and 28nM, respectively. Compounds 1 and 2 significantly inhibited tubulin polymerization in vitro with IC (50) values of 3.6 and 3.2 mu M, respectively.
资助项目Shanghai Commission of Science and Technology[19495800800] ; National Natural Science Foundation of China[21672040] ; National Natural Science Foundation of China[82073717]
WOS关键词TUMOR INHIBITORS
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
语种英语
出版者GEORG THIEME VERLAG KG
WOS记录号WOS:000712591300001
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/298683]  
专题中国科学院上海药物研究所
通讯作者Li, Jia; Hou, Ai-Jun
作者单位1.Fudan Univ, Sch Pharm, Zhang Heng Rd 826, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, State Key Lab Drug Res, Guo Shoujing Rd 189, Shanghai 201203, Peoples R China
3.Puer Inst Tradit Ethnomed, Kunming, Yunnan, Peoples R China
4.Univ Chinese Acad Sci, Beijing, Peoples R China
5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing, Peoples R China
推荐引用方式
GB/T 7714
Lei, Chun,Li, Ya-Nan,Li, Jia-Nan,et al. Two New Cytotoxic Maytansinoids Targeting Tubulin from Trewia nudiflora[J]. PLANTA MEDICA,2021:7.
APA Lei, Chun.,Li, Ya-Nan.,Li, Jia-Nan.,Zhou, Yu-Bo.,Cui, Ming-Jun.,...&Hou, Ai-Jun.(2021).Two New Cytotoxic Maytansinoids Targeting Tubulin from Trewia nudiflora.PLANTA MEDICA,7.
MLA Lei, Chun,et al."Two New Cytotoxic Maytansinoids Targeting Tubulin from Trewia nudiflora".PLANTA MEDICA (2021):7.
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