Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application
文献类型：期刊论文
| 作者 | Sun, Shiguo1; Chen, Su-Shing3; Liu, Fengyu4; Ge, Guangbo2; Yang, Zihao1 |
| 刊名 | DYES AND PIGMENTS
 |
| 出版日期 | 2017-11-01 |
| 卷号 | 146页码:414-419 |
| 关键词 | Artesunate (ART) Fluorophore Covalent modification |
| 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. |
| 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 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000410010100052 |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/150025]  |
| 专题 | 大连化学物理研究所_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.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China 3.Univ Florida, Dept Comp Informat Sci & Engn, Syst Biol Lab, Gainesville, FL USA 4.Dalian Univ Technol, Sch Chem, State Key Lab Fine Chem, 2 Linggong Rd, Dalian 116023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Shiguo,Chen, Su-Shing,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 | Sun, Shiguo,Chen, Su-Shing,Liu, Fengyu,Ge, Guangbo,&Yang, Zihao.(2017).Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application.DYES AND PIGMENTS,146,414-419. |
| MLA | Sun, Shiguo,et al."Study of a series of fluorophore-labeled artesunate derivatives Design, analysis and application".DYES AND PIGMENTS 146(2017):414-419. |
入库方式： OAI收割
来源：大连化学物理研究所
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