Delivery of acetylthevetin B, an antitumor cardiac glycoside, using polymeric micelles for enhanced therapeutic efficacy against lung cancer cells
文献类型：期刊论文
| 作者 | Zhu, Jing-jing1,2; Zhang, Xin-xin2 ; Miao, Yun-qiu2; He, Shu-fang2; Tian, Dan-mei1; Yao, Xin-sheng1; Tang, Jin-shan1,3; Gan, Yong2
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2017-02 |
| 卷号 | 38期号:2页码:290-300 |
| 关键词 | cardiac glycoside acetylthevetin B antitumor lung cancer polymeric micelle drug delivery A549 xenograft tumor model |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2016.113 |
| 文献子类 | Article |
| 英文摘要 | Acetylthevetin B (ATB), a cardiac glycoside from the seed of Thevetia peruviana (Pers) K Schum (yellow oleander), exhibits not only antitumor activity but also potential cardiac toxicity. In the present study, we attempted to enhance its antitumor action and decrease its adverse effects via chitosan-Pluronic P123 (CP) micelle encapsulation. Two ATB-loaded CP micelles (ATB-CP1, ATB-CP2) were prepared using an emulsion/solvent evaporation technique. They were spherical in shape with a particle size of 40-50 nm, showed a neutral zeta potential, and had acceptable encapsulation efficiency (>90%). Compared to the free ATB (IC50=2.94 mu mol/L), ATB-loaded CP micelles exerted much stronger cytotoxicity against human lung cancer A549 cells with lower IC50 values (0.76 and 1.44 mu mol/L for ATB-CP1 and ATB-CP2, respectively). After administration of a single dose in mice, the accumulation of ATB-loaded CP1 micelles in the tumor and lungs, respectively, was 15.31-fold and 9.49-fold as high as that of free ATB. A549 xenograft tumor mice treated with ATB-loaded CP1 micelles for 21 d showed the smallest tumor volume (one-fourth of that in the control group) and the highest inhibition rate (85.6%) among all the treatment groups. After 21-d treatment, no significant pathological changes were observed in hearts and other main tissues. In summary, ATB may serve as a promising antitumor chemotherapeutic agent for lung cancer, and its antitumor efficacy was significantly improved by CP micelles, with lower adverse effects. |
| WOS关键词 | OVERCOMING MULTIDRUG-RESISTANCE ; IN-VIVO EVALUATION ; CHITOSAN NANOPARTICLES ; BLOCK-COPOLYMERS ; DRUG-DELIVERY ; POLYETHYLENE-GLYCOL ; TARGETED DELIVERY ; PROTEIN CORONA ; TUMOR ; CARCINOMA |
| 资助项目 | National Natural Science Foundation of China[81571796] ; National Natural Science Foundation of China[81673320] ; Youth Innovation Promotion Association[2015229] ; SA-SIBS Scholarship Program[00000000] ; State Key Laboratory of Drug Research[SIMM1403KF-15] ; State Key Laboratory of Drug Research[SIMM1601KF-09] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5906838 |
| WOS记录号 | WOS:000393013400013 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275660]  |
| 专题 | 药物制剂研究中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Zhang, Xin-xin; Tang, Jin-shan; Gan, Yong |
| 作者单位 | 1.Ji Nan Univ, Coll Pharm, Inst Tradit Chinese Med & Nat Prod, Guangzhou 510632, Guangdong, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Jing-jing,Zhang, Xin-xin,Miao, Yun-qiu,et al. Delivery of acetylthevetin B, an antitumor cardiac glycoside, using polymeric micelles for enhanced therapeutic efficacy against lung cancer cells[J]. ACTA PHARMACOLOGICA SINICA,2017,38(2):290-300. |
| APA | Zhu, Jing-jing.,Zhang, Xin-xin.,Miao, Yun-qiu.,He, Shu-fang.,Tian, Dan-mei.,...&Gan, Yong.(2017).Delivery of acetylthevetin B, an antitumor cardiac glycoside, using polymeric micelles for enhanced therapeutic efficacy against lung cancer cells.ACTA PHARMACOLOGICA SINICA,38(2),290-300. |
| MLA | Zhu, Jing-jing,et al."Delivery of acetylthevetin B, an antitumor cardiac glycoside, using polymeric micelles for enhanced therapeutic efficacy against lung cancer cells".ACTA PHARMACOLOGICA SINICA 38.2(2017):290-300. |
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。