Inhibition on hepatitis B virus e-gene expression of 10?3 DNAzyme delivered by novel chitosan oligosaccharide¨Cstearic acid micelles

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• 作者：Jing  ; Miao^a ; Xing-guo  ; Zhang^a ;   ; ^{xgzhang666@yahoo.com.cn} ; Yun  ; Hong^a ; Yue-feng  ; Rao^a ; Qian  ; Li^a ; Xian-ji  ; Xie^a ; Jian-er  ; Wo^a ;   ; ^b ; Min-wei  ; Li^a ;   ; ^b
• 关键词：10&ndash ; 23 DNAzyme ; Anti-hepatitis B virus ; Chitosan oligosaccharide&ndash ; stearic acid ; Micelles
• 刊名：Carbohydrate Polymers
• 出版年：2012
• 出版时间：15 January 2012
• 年：2012
• 卷：87
• 期：2
• 页码：1342-1347
• 全文大小：624 K

文摘

10?3 DNAzyme (DrzBC) could block the expression of HBV e-gene with application limit of dependence on exogenous delivery. Stearic acid grafted chitosan oligosaccharide (CSSA) could self-aggregate to form micelles in aqueous medium and bind with DrzBC by electrostatic interaction. Compared with Lipofectamine?2000, the CSSA micelles showed much lower cytotoxicity (412.5 ¦Ìg/mL) and advantaged target in subcellular organelles-cytoplasm. Both including DrzBC of 1 ¦Ìmol/L, Lipofectamine?2000/DrzBC complex showed maximum inhibition rate (IR) on HBeAg expression of 46.53 ¡À 2.00 % at 48 h, and then decreased rapidly, while CSSA/DrzBC complex showed maximum IR of 82.51 ¡À 1.28 % at 72 h, and hold on IR above 70 % until 96 h. Moreover, within a concentration range of 0.1?.0 ¦Ìmol/L, and equally incubating for 48 h, the IR of Lipofectamine?2000/DrzBC complex was from 23.20 ¡À 1.61 % to 66.27 ¡À 1.96 % , while the IR of CSSA/DrzBC complex increased from 40.23 ¡À 3.28 % to 80.95 ¡À 1.69 % . CSSA/DrzBC complex is a promising effective system for inhibiting HBeAg expression.