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Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application
Yang, Zihao1; Ge, Guangbo3; Liu, Fengyu2; Chen, Su-Shing4; Sun, Shiguo1
关键词Artesunate (Art) Fluorophore Covalent Modification
刊名DYES AND PIGMENTS
2017-11-01
DOI10.1016/j.dyepig.2017.07.031
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
关键词[WOS]RAT-LIVER MICROSOMES ; BIOLOGICAL-FLUIDS ; THIOL PROBE ; CELL-DEATH ; ANTIMALARIAL ; METABOLISM ; DIHYDROARTEMISININ ; ESTERASE ; MALARIA
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.
语种英语
WOS记录号WOS:000410010100052
引用统计
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/149925
专题中国科学院大连化学物理研究所
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
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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.
APA Yang, Zihao,Ge, Guangbo,Liu, Fengyu,Chen, Su-Shing,&Sun, Shiguo.(2017).Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application.DYES AND PIGMENTS,146,414-419.
MLA Yang, Zihao,et al."Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application".DYES AND PIGMENTS 146(2017):414-419.
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