Research On Synthesis Of Peptide Dendrimer

Dendrimers are a kind of new type synthetic nano-sized macromolecules in recent years. It has characteristics of monodisperse, highly branched three-dimensional with accurately controlled structures, and a large number of controllable peripheral functional groups. Dendrimers can be designed to reach specific molecular size, shape and structure. They generally have lumen and high density of functional terminal groups. Peptide dendrimers are radially branched macromolecules that contain a peptidyl branching core or peripheral peptide chains. Peptide dendrimers have properties similar to proteins and some special characteristics, such as more better biocompatibility, water solubility and resistance to proteolytic digestion compared to linear peptides. There are large number of controllable peripheral functional groups on the polymer surface, so they can be grafted many functional groups. Pept-ide dendrimers are monodispersity with high molecular weights and ability to be easily functionalized. They are used in a wide variety of applications, whi-ch including be used as protein mimetics, catalysts, solubilizing agents, biom-edical diagnostic reagents, drug and gene delivery vehicles.Most of the pharmacologically active anti-cancer drugs are limited in the clinical application due to their low solubility, unfavorable biodistribution characteristics, and serious side effects. Peptide dendrimers show the potential value in resolving the above problems. With the unique structure and properties, Peptide dendrimers have the advantages of both of the dendrimer and peptide. As drug delivery, peptide dendrimers show excellent biocompat-ibility and biodegradability, to improve the solubility of drugs, enhance the biological activity and protect drug from deactivation at the same time presse-rve its activity during circulation. On the other hand, they also make the drugs have the properties of targeting and sustained-release, and reduce the antige-nic activity of the drug leading to a less pronounced immunological body response. In short, the introduction of peptide dendrimer reduces the overall adverse drug reactions and improve efficacy.According to the idea of macromolecular-drug conjugate, the objective of our work is to synthesis sector peptide dendrimers, and then study them as drug delivery. A series of novel peptide dendrimers are designed and synthesi-zed based on natural amino acids Glu and Lys:(a) The sector peptide dendrim-ers; (b) The surface modification of peptide dendrimers; (c) peptide dendrime-rs with glutaric acid or 1,3,5-Benzenetricarboxylic trichloride as a core.We synthesized a series of peptide dendrimers by divergent approach and convergent approach in solution phase, and all target compounds are novel. The structures of all target compounds were indentified by IR,1H-NMR, MS.