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Synthesis of Multiarm Peptide Dendrimers for Dual Targeted Thrombolysis
ACS Macro Letters ( IF 5.1 ) Pub Date : 2020-02-03 , DOI: 10.1021/acsmacrolett.0c00054 Shao-Fei Zhang 1, 2 , Shaoyu Lü 1 , Jiandong Yang 2 , Mengjie Huang 1 , Yongming Liu 3 , Mingzhu Liu 1
ACS Macro Letters ( IF 5.1 ) Pub Date : 2020-02-03 , DOI: 10.1021/acsmacrolett.0c00054 Shao-Fei Zhang 1, 2 , Shaoyu Lü 1 , Jiandong Yang 2 , Mengjie Huang 1 , Yongming Liu 3 , Mingzhu Liu 1
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Current thrombolytic agents generally possess low specificity and pose a high risk of intracranial hemorrhage. Here, various generations of multiarm polylactic acid–polyglutamic acid peptide dendrimers were synthesized, and then nattokinase-combining magnetic Fe3O4 nanoparticles and RGD-modified dendrimers (Fe3O4-(4-PLA(G3)4)-RGD) were fabricated for targeted thrombi dissolution. Their in vitro and in vivo thrombolytic properties were determined. In vitro determination indicated that Fe3O4-(4-PLA(G3)4)-RGD/nattokinase provided 3-fold higher blood clot dissolution than that obtained with free nattokinase. An in vivo thrombolytic examination revealed that most of the thrombi were dissolved under an external magnetic field. In addition, there were many nanoparticles in vascular endothelial cells, demonstrating the RGD and magnetic dual targeting capacity of Fe3O4-(4-PLA(G3)4)-RGD/nattokinase. These results demonstrated that Fe3O4-(4-PLA(G3)4)-RGD nanoparticles not only will deliver targeted thrombolytic agents to enhance the efficacy of site-specific thrombolytic treatment but also have potential in the diagnosis of thrombotic disease in its early stages.
中文翻译：
用于双靶向溶栓的多臂肽树枝状大分子的合成
目前的溶栓剂通常具有低特异性并且造成颅内出血的高风险。在这里，合成了多代多臂聚乳酸-聚谷氨酸肽树枝状大分子，然后将纳豆激酶结合磁性 Fe 3 O 4纳米粒子和 RGD 修饰的树枝状大分子 (Fe 3 O 4 -(4-PLA(G 3 ) 4 )-RGD ) 被制造用于靶向血栓溶解。测定了它们的体外和体内溶栓特性。体外测定表明Fe 3 O 4 -(4-PLA(G 3 ) 4)-RGD/纳豆激酶提供的血凝块溶解比游离纳豆激酶高 3 倍。体内溶栓检查显示大部分血栓在外部磁场下溶解。此外，血管内皮细胞中有许多纳米颗粒，证明了Fe 3 O 4 -(4-PLA(G 3 ) 4 )-RGD/纳豆激酶的RGD和磁性双重靶向能力。这些结果表明，Fe 3 O 4 -(4-PLA(G 3 ) 4)-RGD 纳米颗粒不仅可以递送靶向溶栓剂以提高部位特异性溶栓治疗的功效，而且在血栓性疾病的早期诊断中也具有潜力。
更新日期：2020-02-03
中文翻译：
用于双靶向溶栓的多臂肽树枝状大分子的合成
目前的溶栓剂通常具有低特异性并且造成颅内出血的高风险。在这里，合成了多代多臂聚乳酸-聚谷氨酸肽树枝状大分子，然后将纳豆激酶结合磁性 Fe 3 O 4纳米粒子和 RGD 修饰的树枝状大分子 (Fe 3 O 4 -(4-PLA(G 3 ) 4 )-RGD ) 被制造用于靶向血栓溶解。测定了它们的体外和体内溶栓特性。体外测定表明Fe 3 O 4 -(4-PLA(G 3 ) 4)-RGD/纳豆激酶提供的血凝块溶解比游离纳豆激酶高 3 倍。体内溶栓检查显示大部分血栓在外部磁场下溶解。此外，血管内皮细胞中有许多纳米颗粒，证明了Fe 3 O 4 -(4-PLA(G 3 ) 4 )-RGD/纳豆激酶的RGD和磁性双重靶向能力。这些结果表明，Fe 3 O 4 -(4-PLA(G 3 ) 4)-RGD 纳米颗粒不仅可以递送靶向溶栓剂以提高部位特异性溶栓治疗的功效，而且在血栓性疾病的早期诊断中也具有潜力。
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