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题名: Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application
作者: Yang, Zihao1;  Ge, Guangbo3;  Liu, Fengyu2;  Chen, Su-Shing4;  Sun, Shiguo1
关键词: Artesunate (ART) ;  Fluorophore ;  Covalent modification
刊名: DYES AND PIGMENTS
发表日期: 2017-11-01
DOI: 10.1016/j.dyepig.2017.07.031
卷: 146, 页:414-419
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Physical Sciences ;  Technology
类目[WOS]: Chemistry, Applied ;  Engineering, Chemical ;  Materials Science, Textiles
研究领域[WOS]: Chemistry ;  Engineering ;  Materials Science
英文摘要: Artesunate (ART) Is an antimalarial and potential anticancer drug which exerts diverse physiological and pathological functions. Unfortunately, the detailed mechanisms of operation of ART derivatives still remain elusive. To solve this, modification of ART with fluorophores can be a good choice. However, whether the modification has any influence on the drug itself is still a problem that remains to be solved. Herein, three different fluorophores (anthracene (E), pyrene (B) and naphthalimide (N)) were designed and synthesized to covalently link with ART to get three fluorophore-labeled ART derivatives (AE, AB and AN). The result demonstrated that the spectral characteristics of these derivatives was not affected by different fluorophores. While, AN cannot be hydrolyzed by the most common drug metabolism enzymes like human liver microsomes (HLM), rat liver microsomes (RLM) and mouse liver microsomes (MLM). In comparison, AE and AB can be hydrolyzed much easier than AN, leading to the release of ART. Co localization studies suggest that AN exhibited superior lysosome-targeting ability than AE and AB, due to the preferential accumulation of ART in lysosome and the remarkable enzyme hydrolysis stability of AN. Furthermore, not much cytotoxicity was observed for the corresponding fluorophore-labeled ART derivatives compared with that of ART alone. (C) 2017 Elsevier Ltd. All rights reserved.
关键词[WOS]: RAT-LIVER MICROSOMES ;  BIOLOGICAL-FLUIDS ;  THIOL PROBE ;  CELL-DEATH ;  ANTIMALARIAL ;  METABOLISM ;  DIHYDROARTEMISININ ;  ESTERASE ;  MALARIA
语种: 英语
WOS记录号: WOS:000410010100052
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/150025
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Northwest A&F Univ, Coll Chem & Pharm, Shaanxi Key Lab Nat Prod & Chem Biol, Xinong Rd 22, Yangling 712100, Shaanxi, Peoples R China
2.Dalian Univ Technol, Sch Chem, State Key Lab Fine Chem, 2 Linggong Rd, Dalian 116023, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
4.Univ Florida, Dept Comp Informat Sci & Engn, Syst Biol Lab, Gainesville, FL USA

Recommended Citation:
Yang, Zihao,Ge, Guangbo,Liu, Fengyu,et al. Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application[J]. DYES AND PIGMENTS,2017,146:414-419.
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