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寡核苷酸聚赖氨酸修饰物的脂质体制备及其对HepG2细胞的细胞毒活性研究
引用本文:程立华,费学萍,潘卫三,张景海,王思玲.寡核苷酸聚赖氨酸修饰物的脂质体制备及其对HepG2细胞的细胞毒活性研究[J].沈阳药科大学学报,2006,23(5):261-264.
作者姓名:程立华  费学萍  潘卫三  张景海  王思玲
作者单位:1. 沈阳药科大学,药学院,辽宁,沈阳,110016
2. 中国医科大学,附属第四医院,辽宁,沈阳,110032
3. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016
摘    要:目的研究反义寡核苷酸的聚赖氨酸修饰物对脂质体包封率的影响及对HepG2细胞活性的初步测定。方法利用反义药物的聚赖氨酸修饰物,采用薄膜分散法制备反义寡核苷酸及其聚赖氨酸修饰物的脂质体;紫外分光光度法测定包封率的差异并考察对HepG2细胞细胞毒活性的影响。结果高密度正电荷的聚赖氨酸与带负电荷的反义寡核苷酸偶联后,脂质体的载药量大大增加,并且细胞的摄入量增加,对HepG2细胞生长具有抑制作用。结论聚赖氨酸修饰物增加了反义寡核苷酸的脂质体包封率,有效诱导人肝癌细胞的凋亡作用。

关 键 词:反义寡核苷酸  聚赖氨酸  靶向脂质体  细胞毒作用
文章编号:1006-2858(2006)05-0261-04
收稿时间:2005-10-08
修稿时间:2005年10月8日

Delivery of poly(L-lysine)conjugated oligodeoxynucleotides to HepG2 cells using N-stearyllactobionamide modified liposomes and its inhibition on the proliferation of HepG2 cells
CHENG Li-hua,FEI Xue-ping,PAN Wei-san,ZHANG Jing-hai,WANG Si-ling.Delivery of poly(L-lysine)conjugated oligodeoxynucleotides to HepG2 cells using N-stearyllactobionamide modified liposomes and its inhibition on the proliferation of HepG2 cells[J].Journal of Shenyang Pharmaceutical University,2006,23(5):261-264.
Authors:CHENG Li-hua  FEI Xue-ping  PAN Wei-san  ZHANG Jing-hai  WANG Si-ling
Institution:1. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China ; 2. Nursing Department, the Fourth Hospital, China Medical University, Shenyang 110032, China ; 3. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Abstract:Objective To research the effect of poly(L-lysine)conjugated ODN on entrapment rate of N-SLBA liposomes and its inhibition on the proliferation of HepG2 cells.Methods ODNs covalent linkage to poly(L-lysine),preparation of N-SLBA liposomal ODN and N-SLBA liposomal poly(L-lysine)conjugated ODN,encapsulated ODN,poly(L-lysine)conjugated ODN were determined by direct measurement using LC-10 UV instrument,poly(L-lysine)conjugated ODN encapsulated in N-SLBA liposomes inhibited the proliferation of HepG2 cells.Results Amino groups in poly(L-lysine) neutralized negative charges in ODNs and reduced repulsion with liposomal membrane.Effective HepG2 cell transfection could be achieved with the improved entrapment ratio and inhibition on HepG2 cell growth.Conclusions poly(L-lysine)modification of ODN encapsulated in target liposomes improves the encapsulation efficiency and increase the apoptosis of HepG2 cells.
Keywords:oligodeoxynucleotide(ODN)  poly(L-lysine)  target liposomes  cytotoxicity activity
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