Kojima Chie, Irie Kotaro
Nanoscience and Nanotechnology Research Center, Research Organization for the 21st Century, Osaka Prefecture University, Japan.
Biopolymers. 2013 Nov;100(6):714-21. doi: 10.1002/bip.22276.
Dendrimers are synthetic macromolecules with a unique structure that are potential unimolecular drug carriers and potential scaffolds for peptides. Elastin is one of the main components of the extracellular matrix, as well as a temperature-sensitive biomacromolecule. Val-Pro-Gly-Val-Gly repeats, an elastin-like peptide, have been used for designing artificial elastin molecules. In this study, we have synthesized a novel type of temperature-dependent drug carrier by conjugating Ac-Val-Pro-Gly-Val-Gly to a dendrimer, named elastin-mimetic dendrimer. The elastin-mimetic dendrimer formed β-turn structure by heating. The elastin-mimetic dendrimer exhibited the inverse phase transition, depending on pH and NaCl concentration in addition to temperature. The elastin-mimetic dendrimer could encapsulate a model drug, rose bengal, even though the complex stability was similar to the dendrimer without elastin-like peptide. Therefore, the elastin-mimetic dendrimer is a potential drug carrier with temperature- and pH-dependent properties.
树枝状大分子是具有独特结构的合成大分子，是潜在的单分子药物载体和肽的潜在支架。弹性蛋白是细胞外基质的主要成分之一，也是一种温度敏感的生物大分子。弹性蛋白样肽Val-Pro-Gly-Val-Gly重复序列已被用于设计人工弹性蛋白分子。在本研究中，我们通过将Ac-Val-Pro-Gly-Val-Gly与树枝状大分子共轭，合成了一种新型的温度依赖性药物载体，称为弹性蛋白模拟树枝状大分子。弹性蛋白模拟树枝状大分子通过加热形成β-转角结构。除了温度外，弹性蛋白模拟树枝状大分子还表现出取决于pH值和NaCl浓度的反相转变。弹性蛋白模拟树枝状大分子可以包封模型药物孟加拉玫瑰红，尽管其复合物稳定性与不含弹性蛋白样肽的树枝状大分子相似。因此，弹性蛋白模拟树枝状大分子是一种具有温度和pH依赖性特性的潜在药物载体。
