具有抗凝血活性的聚氨基酸的合成及性能研究

Synthesis and properties of polyamino acids with anticoagulant activity

通过亲核试剂三乙烯四胺(TETA)引发L-酪氨酸和L-谷氨酸的α-氨基酸N-环内酸酐(NCAs)的活性可控开环聚合(ROP),并进行氯磺酸酯化修饰,制备了一种具有抗凝血活性的磺酸酯化聚(L-酪氨酸-co-L-谷氨酸)(PTG-SO_3),并对PTG-SO_3的结构、酶促降解性能、细胞毒性以及血液相容性等进行了测试.结果表明,合成产物为PTG-SO_3,具有良好的生物降解性(16 d后可降解约65%)、低细胞毒性(培育72 h后,细胞活性约为70%)、良好的抗凝血性能和血液相容性(活化的部分凝血活酶时间延长约37 s).该聚合物有望应用于生物医学领域.

Using the nucleophilic reagent triethylenetetramine (TETA) as initiator, L-tyrosine and L-glutamic acid alpha amino acid N-carboxylic acid anhydride (NCAs) were actively controlled to occur the ring opening polymerization(ROP).Then,esterification modification of chlorosulfonic acid was prepared,a sulfonic acid esterification poly(L-tyrosine-co-L-glutamic acid)(PTG-SO 3) with anticoagulant activity had been prepared.The structure of PTG-SO 3,enzymatic degradation performance,cytotoxicity and blood compatibility were tested.The results showed that the product is PTG-SO 3 which has good biodegradability (about 65% biodegradable 16 d later),low cytotoxicity ( after 72 h of culture,the cell activity is about 70%),favourable anticoagulant energy and blood compatibility( activated partial thrombin time can be extended by about 37 s).The polymer is expected to be used in biomedical applications.