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学科主题: 药学
题名:
The therapeutic efficacy of conjugated linoleic acid - Paclitaxel on glioma in the rat
作者: Ke, Xi-Yu1; Zhao, Bo-Jun1; Zhao, Xin1; Wang, Ying1; Huang, Yue1; Chen, Xiao-Mei1; Zhao, Bing-Xiang1; Zhao, Shan-Shan1; Zhang, Xuan1; Zhang, Qiang1,2
关键词: Conjugated linoleic acid (CLA) ; Paclitaxel (PTX) ; Conjugate ; Blood-brain barrier ; Brain glioma-bearing rats ; Anti-tumor efficacy
刊名: BIOMATERIALS
发表日期: 2010-08-01
DOI: 10.1016/j.biomaterials.2010.03.079
卷: 31, 期:22, 页:5855-5864
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Engineering, Biomedical ; Materials Science, Biomaterials
研究领域[WOS]: Engineering ; Materials Science
关键词[WOS]: BREAST-CANCER CELLS ; HUMAN PLASMA ; DRUG-DELIVERY ; FATTY-ACID ; IN-VITRO ; BRAIN ; GROWTH ; TAXOL ; ANGIOGENESIS ; METABOLISM
英文摘要:

Considering the effects of conjugated linoleic acid (CLA) on anti-tumor and anti-angiogenic in brain tumor, synergistic anti-tumor activity with taxane as well as potential activity for transporting chemotherapeutic agents across the blood brain barrier (BBB), the purpose of this study was to synthesize CLA-paclitaxel (CLA-PTX) conjugate which could reach to the brain tissue and target brain tumor. The CLA was covalently linked to PTX. The conjugate was stable in PBS and rat plasma in vitro and had no microtubule assembly activity in solution and slight effect of arresting cell cycle progression at the G(2)-M phase. The in vitro cytotoxicity of conjugate was lower than that of PTX (p<0.05). The conjugate showed higher cellular uptake efficiency on C6 glioma cells. The entire pharmacokinetic index revealed the significant enhancement of the conjugate pharmacokinetics compared with that in PTX (p<0.01). The conjugate, unlike PTX, could distribute in brain tissue and retained higher concentrations throughout 360 h. The anti-tumor efficacy in brain tumor-bearing rats after administering conjugate was significantly higher than that after giving Taxol (p<0.01). In conclusion, this CLA-PTX conjugate showed great potential to become a new prodrug of PTX and the methodology can be applied to other anticancer drugs. (C) 2010 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 30873170 ; 2007CB935800 ; 2009CB930300
项目资助者: National natural science foundation of China ; National Basic Research Program of China
WOS记录号: WOS:000279092900016
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/63749
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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作者单位: 1.Peking Univ, Dept Pharmaceut, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China

Recommended Citation:
Ke, Xi-Yu,Zhao, Bo-Jun,Zhao, Xin,et al. The therapeutic efficacy of conjugated linoleic acid - Paclitaxel on glioma in the rat[J]. BIOMATERIALS,2010,31(22):5855-5864.
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