Varghese Oommen P, Kisiel Marta, Martínez-Sanz Elena, Ossipov Dmitri A, Hilborn Jöns
Department of Material Chemistry, Uppsala University, Box 538, S-75121, Uppsala, Sweden.
Macromol Rapid Commun. 2010 Jul 1;31(13):1175-80. doi: 10.1002/marc.200900906. Epub 2010 May 17.
In this report, a new guanidinylating reagent is presented, which was developed without any protection/deprotection strategy and was successfully employed for linking to hyaluronan in aqueous solution. The dually functionalised HA biopolymer bearing guanidinium and hydrazide groups was synthesised to form hydrogel in less than a minute when mixed with aldehyde-modified HA. This hydrogel exhibited higher storage modulus with enhanced stability in PBS when compared to the non-guanidine-containing gel. The gel shift assay showed that this biopolymer formed a stable complex with DNA as well as efficient gene transfection to cells that express HA-receptor CD44. The toxicity studies of this polymer with fibroblast cells revealed that the cells were almost 80% viable after 4 d of incubation at high HA concentration (2.5 × 10(-3) M).
在本报告中，介绍了一种新型胍基化试剂，其开发过程中未采用任何保护/脱保护策略，并成功用于在水溶液中与透明质酸连接。合成了带有胍基和酰肼基团的双功能化透明质酸生物聚合物，当与醛基修饰的透明质酸混合时，在不到一分钟的时间内形成水凝胶。与不含胍的凝胶相比，这种水凝胶在PBS中表现出更高的储能模量和增强的稳定性。凝胶迁移试验表明，这种生物聚合物与DNA形成了稳定的复合物，并对表达透明质酸受体CD44的细胞进行了有效的基因转染。对这种聚合物与成纤维细胞的毒性研究表明，在高透明质酸浓度（2.5×10⁻³ M）下孵育4天后，细胞存活率几乎达到80%。
