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The therapeutic efficacy of conjugated linoleic acid - Paclitaxel on glioma in the rat
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
2010-08-01
DOI10.1016/j.biomaterials.2010.03.079
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
WOS记录号WOS:000279092900016
项目编号30873170 ; 2007CB935800 ; 2009CB930300
资助机构National natural science foundation of China ; National Basic Research Program of China
引用统计
被引频次:36[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/63749
专题北京大学药学院_药剂学系
北京大学医学部管理机构_研究生院
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
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GB/T 7714
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.
APA Ke, Xi-Yu.,Zhao, Bo-Jun.,Zhao, Xin.,Wang, Ying.,Huang, Yue.,...&Zhang, Qiang.(2010).The therapeutic efficacy of conjugated linoleic acid - Paclitaxel on glioma in the rat.BIOMATERIALS,31(22),5855-5864.
MLA Ke, Xi-Yu,et al."The therapeutic efficacy of conjugated linoleic acid - Paclitaxel on glioma in the rat".BIOMATERIALS 31.22(2010):5855-5864.
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