Song Baofeng, Zhang Wei, Peng Rong, Huang Jie, Nie Ting, Li Ying, Jiang Qing, Gao Rong
College of Chemistry, Sichuan University, Chengdu, PR China.
Colloids Surf B Biointerfaces. 2009 May 1;70(2):181-6. doi: 10.1016/j.colsurfb.2008.12.018. Epub 2008 Dec 24.
It is important for gene carrier to transport DNA into target cells. Although viral vectors are very efficient gene-transfer vehicles, significant drawbacks limit their applications. Chitosan (CS) has been researched widely as a non-viral vector. However, the low cell specificity and low transfection efficiency of chitosan need to be overcome. In order to conquer the drawback of chitosan, the present paper is concerned with the synthesis of novel galactosylated chitosan (GC) through etherization of chitosan and galactose in THF using BF(3).OEt(2) as promoter. The final product was characterized and confirmed by FT-IR and (1)H NMR. The degree of O-substitution (DS) of chitosan by galactose was measured to be 10.38% using anthrone-sulfuric acid colorimetric method. The mean particle diameter and average zeta potential of the GC/DNA complex were 350 nm and +22.1 mV, respectively. The GC/DNA nanoparticle was tested to transfect HEK293 cells, and the viability of HEK293 cells was not affected by the GC/DNA nanoparticle compared to that of the control.
基因载体将DNA转运到靶细胞中是很重要的。尽管病毒载体是非常有效的基因传递工具，但一些显著的缺点限制了它们的应用。壳聚糖（CS）作为一种非病毒载体已被广泛研究。然而，壳聚糖的低细胞特异性和低转染效率需要克服。为了克服壳聚糖的缺点，本文涉及通过在四氢呋喃中使用三氟化硼乙醚（BF(3).OEt(2)）作为促进剂，使壳聚糖与半乳糖进行醚化反应来合成新型半乳糖基化壳聚糖（GC）。最终产物通过傅里叶变换红外光谱（FT-IR）和核磁共振氢谱（(1)H NMR）进行表征和确认。使用蒽酮 - 硫酸比色法测得壳聚糖被半乳糖取代的取代度（DS）为10.38%。GC/DNA复合物的平均粒径和平均ζ电位分别为350 nm和 +22.1 mV。对GC/DNA纳米颗粒转染人胚肾293（HEK293）细胞进行了测试，与对照组相比，GC/DNA纳米颗粒对HEK293细胞的活力没有影响。
