Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro
文献类型：期刊论文
| 作者 | Liu, Shuangxi2; Zhang, Kaili1,3; Zhu, Qiwen2; Shen, Qianqian1; Zhang, Qiumeng2; Yu, Jiahui2; Chen, Yi1 ; Lu, Wei2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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| 出版日期 | 2019-04-01 |
| 卷号 | 27期号:7页码:1405-1413 |
| ISSN号 | 0968-0896 |
| 关键词 | PTX SAHA Co-prodrug Nanomicelles |
| DOI | 10.1016/j.bmc.2019.02.046 |
| 通讯作者 | Chen, Yi(ychen@simm.ac.cn) ; Lu, Wei(wlu@chem.ecnu.edu.cn) |
| 英文摘要 | Paclitaxel (PTX) is the first-line treatment drug for breast cancer. However, drug resistance after a course of treatment and low selectivity restricted its clinical utility sometimes. In this study, we successfully bound PTX and vorinostat (SAHA) to form co-prodrugs based on the synergistic anticancer effects. The PTX-SAHA co-prodrugs were conjugated by glycine (1a) and succinic acid (1b) respectively and the former has shown better activity in cytotoxicity, cell cycle arrest and western-blot experiments. Therefore, 1a was further prepared to nanomicelles with mPEG(2000-)PLA(1750) as the carrier by using thin film method. PTX-SAHA co-prodrug nanomicelles were spherical with a particle size of 20-100 nm. In vitro drug release test showed 1a nanomicelles had sustained release effect, which could reduce the resistance of PTX. In vitro cytotoxicity was evaluated by SRB assay in HCT-116 cells, MCF-7 cells and drug-resistant MCF-7/ADR cells. The results showed 1a nanomicelles had comparable or even better cytotoxicity than PTX especially in the MCF-7/ADR cells. All the results suggested that PTX-SAHA co-prodrug nanomicelles were promising treatment for PTX resistance cancer. |
| WOS关键词 | HISTONE DEACETYLASE INHIBITORS ; HYDROXAMIC ACID SAHA ; DELIVERY |
| 资助项目 | Shanghai Science and Technology Council[16DZ2280100] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000461168400022 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290252]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Chen, Yi; Lu, Wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China 2.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Shuangxi,Zhang, Kaili,Zhu, Qiwen,et al. Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2019,27(7):1405-1413. |
| APA | Liu, Shuangxi.,Zhang, Kaili.,Zhu, Qiwen.,Shen, Qianqian.,Zhang, Qiumeng.,...&Lu, Wei.(2019).Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.BIOORGANIC & MEDICINAL CHEMISTRY,27(7),1405-1413. |
| MLA | Liu, Shuangxi,et al."Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro".BIOORGANIC & MEDICINAL CHEMISTRY 27.7(2019):1405-1413. |
入库方式： OAI收割
来源：上海药物研究所
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