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Design, Synthesis, and Biological Evaluation of Novel Biotinylated Podophyllotoxin Derivatives as Potential Antitumor Agents

文献类型：期刊论文

作者Zi, Cheng-Ting1,2,3,4,5; Gao, Yin-Sheng6; Yang, Liu1,2; Feng, Shu-Yun6; Huang, Yue6; Sun, Li6; Jin, Yi5; Xu, Feng-Qing1,2; Dong, Fa-Wu1,2; Li, Yan1,2
刊名FRONTIERS IN CHEMISTRY
出版日期2019-06-18
卷号7页码:14
关键词podophyllotoxin derivatives biotin anticancer activity synthesis apoptosis
ISSN号2296-2646
DOI10.3389/fchem.2019.00434
通讯作者Jiang, Zi-Hua(zjiang@lakeheadu.ca) ; Yuan, Sheng-Tao(cpuYuanst@163.com) ; Hu, Jiang-Miao(hujiangmiao@mail.kib.ac.cn)
英文摘要Podophyllotoxin has long been used as an active substance for cytotoxic activity. Fourteen novel biotinylated podophyllotoxin derivatives were designed, synthesized, and evaluated for cytotoxic activity for this study. The synthesized compounds were evaluated for cytotoxic activity in the following human cancer cell lines, SW480, MCF-7, A-549, SMMC-7721, and HL-60 by MTT assay. Most of them exhibited potent cytotoxic effects and compound 15 showed the highest cytotoxic activity among the five cancer cell lines tested, having its IC50 values in the range of 0.13 to 0.84 mu M. Apoptosis analysis revealed that compound 15 caused obvious induction of cell apoptosis. Compound 15 significantly down-regulated the expression level of the marker proteins (caspase-3 and PARP) in H1299 and H1975 cells, activated the transcription of IRE1 alpha, increased the expression of GRP78 and XBP-1s, and finally induced apoptosis of H1299 cells. In vivo studies showed that 15 at a dose of 20 mg/kg suppressed tumor growth of S180 cell xenografts in icr mice significantly. Further molecular docking studies suggested that compound 15 could bind well with the ATPase domain of Topoisomerase-II. These data suggest that compound 15 is a promising agent for cancer therapy deserving further research.
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000471844200001
源URL[http://ir.kib.ac.cn/handle/151853/67249]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
通讯作者Jiang, Zi-Hua; Yuan, Sheng-Tao; Hu, Jiang-Miao
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming, Yunnan, Peoples R China
2.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Nat Med Chem, Kunming, Yunnan, Peoples R China
3.China Pharmaceut Univ, Jiangsu Key Lab Drug Screening, Nanjing, Jiangsu, Peoples R China
4.China Pharmaceut Univ, Jiangsu Ctr Pharmacodynam Res & Evaluat, Nanjing, Jiangsu, Peoples R China
5.Yunnan Agr Univ, Coll Sci, Key Lab Pu Er Tea Sci, Minist Educ, Kunming, Yunnan, Peoples R China
6.Yunnan Univ, Key Lab Med Chem Nat Resource, Minist Educ, Sch Chem Sci & Technol, Kunming, Yunnan, Peoples R China
7.Lakehead Univ, Dept Chem, Thunder Bay, ON, Canada
推荐引用方式
GB/T 7714		 Zi, Cheng-Ting,Gao, Yin-Sheng,Yang, Liu,et al. Design, Synthesis, and Biological Evaluation of Novel Biotinylated Podophyllotoxin Derivatives as Potential Antitumor Agents[J]. FRONTIERS IN CHEMISTRY,2019,7:14.
APA Zi, Cheng-Ting.,Gao, Yin-Sheng.,Yang, Liu.,Feng, Shu-Yun.,Huang, Yue.,...&Hu, Jiang-Miao.(2019).Design, Synthesis, and Biological Evaluation of Novel Biotinylated Podophyllotoxin Derivatives as Potential Antitumor Agents.FRONTIERS IN CHEMISTRY,7,14.
MLA Zi, Cheng-Ting,et al."Design, Synthesis, and Biological Evaluation of Novel Biotinylated Podophyllotoxin Derivatives as Potential Antitumor Agents".FRONTIERS IN CHEMISTRY 7(2019):14.

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来源：昆明植物研究所

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