Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging
文献类型：期刊论文
| 作者 | Chen, Hao2,3; Wang, Jing1,2; Feng, Xin1,4; Zhu, Mark1; Hoffmann, Simon1; Hsu, Alex1; Qian, Kun1; Huang, Daijuan1; Zhao, Feng1; Liu, Wei2 |
| 刊名 | CHEMICAL SCIENCE
 |
| 出版日期 | 2019-09-14 |
| 卷号 | 10期号:34页码:7946-7951 |
| ISSN号 | 2041-6520 |
| DOI | 10.1039/c9sc01410a |
| 通讯作者 | Zhang, Huimao(huimaozhanglinda@163.com) ; Cheng, Zhen(zcheng@stanford.edu) |
| 英文摘要 | Fluorescent mitochondria-accumulating delocalized lipophilic cations (DLCs) for cancer therapy have drawn significant attention in the field of cancer theranostics. One of the most promising fluorescent DLCs, F16, can selectively trigger the apoptosis and necrosis of cancer cells, making it an attractive targeted theranostic drug candidate. However, it suffers from low clinical translation potential, largely due to its inefficient anti-cancer activity (IC50 in the mu M range) and poorly understood structure-activity relationship (SAR). In this report, eleven indole-ring substituted F16 derivatives (F16s) were synthesized. Among these derivatives, 5BMF was identified as a highly effective theranostic agent, with in vitro studies showing a low IC50 of similar to 50 nM (to H2228 cells) and high cancer to normal cell selectivity index of 225. In vivo studies revealed that tumors treated with 5BMF were significantly suppressed (almost no growth over the treatment period) compared to the PBS treated control group, and also no obvious toxicity to mice was found. In addition, the tumor imaging capability of 5BMF was demonstrated by in vivo fluorescence imaging. Finally, we report for the first time a proposed SAR for F16 DLCs. Our work lays down a solid foundation for translating 5BMF into a novel and highly promising DLC for cancer theranostics. |
| WOS关键词 | DELOCALIZED LIPOPHILIC CATIONS ; RHODACYANINE DYE ; ANTICARCINOMA ACTIVITY ; LUNG-CANCER ; DERIVATIVES ; COMPOUND ; MKT-077 ; CELLS ; F-16 |
| 资助项目 | Office of Science (BER), U.S. Department of Energy[DE-SC0008397] ; National Natural Science Foundation of China[81871406] ; 6th youth development foundation from the First Hospital of Jilin University[JDYY52015032] ; Jilin Provincial Health Special Project from the finance department of Jilin Province[2018SCZWSZX-018] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000482978700009 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/288785]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Huimao; Cheng, Zhen |
| 作者单位 | 1.Stanford Univ, Canary Ctr Stanford Canc Early Detect, Dept Radiol, MIPS,BioX Program, Stanford, CA 94305 USA 2.Jilin Univ, Hosp 1, Dept Radiol, Changchun 130021, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Mol Imaging Res, Shanghai 201203, Peoples R China 4.Jilin Univ, Coll Vet Med, Changchun 130021, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Hao,Wang, Jing,Feng, Xin,et al. Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging[J]. CHEMICAL SCIENCE,2019,10(34):7946-7951. |
| APA | Chen, Hao.,Wang, Jing.,Feng, Xin.,Zhu, Mark.,Hoffmann, Simon.,...&Cheng, Zhen.(2019).Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging.CHEMICAL SCIENCE,10(34),7946-7951. |
| MLA | Chen, Hao,et al."Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging".CHEMICAL SCIENCE 10.34(2019):7946-7951. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。