Fe3+@polyDOPA-b-polysarcosine, a T1-Weighted MRI Contrast Agent via Controlled NTA Polymerization,ACS Macro Letters

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Fe3+@polyDOPA-b-polysarcosine, a T1-Weighted MRI Contrast Agent via Controlled NTA Polymerization
ACS Macro Letters ( IF 5.1 ) Pub Date : 2018-05-29 00:00:00 , DOI: 10.1021/acsmacrolett.8b00287
Yuedong Miao ₁ , Fengnan Xie _{2,

3} , Jiayu Cen ₁ , Fei Zhou ₂ , Xinfeng Tao ₁ , Jingfeng Luo ₂ , Guocan Han ₂ , Xianglei Kong ₂ , Xiaoming Yang ₂ , Jihong Sun _{2,

4} , Jun Ling ₁

Affiliation

α-Amino acid N-thiocarboxyanhydrides (NTAs) are promising cyclic monomers to synthesize polypeptides and polypeptoids via controlled ring-opening polymerizations. Superior to N-carboxyanhydrides requiring protection on hydroxyl groups, NTAs are able to tolerate such nucleophiles. In this work, we report the synthesis of NTA monomers containing unprotected phenolic hydroxyl groups of 3,4-dihydroxy-l-phenylalanine (DOPA) and l-tyrosine (Tyr). Their controlled ROPs and sequential copolymerizations with polysarcosine (PSar) yield PDOPA, PTyr, and PDOPA-b-polysarcosine (PDOPA-b-PSar) products quantitatively with designable degrees of polymerization. Micellar nanoparticles of Fe³⁺@PDOPA-b-PSar have been prepared thanks to the strong chelation of iron(III) cation by catechol ligands that act as T1-weighted magnetic resonance imaging (MRI) contrast agents. For instance, Fe³⁺@PDOPA₁₀-b-PSar₅₀ exhibits higher longitudinal relaxivity (r₁ = 5.6 mM^–1 s^–1) than commercial Gd³⁺-based compounds. Effective MRI contrast enhancement in vivo of nude mice with a moderate duration (150 min) and 3D magnetic resonance angiography in rabbit illustrated by using volume rendering and maximal intensity projection techniques ignite the clinical application of Fe³⁺-based polypept(o)ides in diagnostic radiology as Gd-free MRI contrast agents.

中文翻译：

Fe3+@polyDOPA-b-polysarcosine，一种通过受控 NTA 聚合的 T1 加权 MRI 造影剂

α-氨基酸N-硫代羧酸酐 (NTA) 是有前途的环状单体，可通过受控的开环聚合反应合成多肽和类多肽。优于需要对羟基进行保护的N-羧酸酐，NTA 能够耐受此类亲核试剂。在这项工作中，我们报告了 NTA 单体的合成，该单体含有 3,4-二羟基-l-苯丙氨酸 (DOPA) 和l-酪氨酸 (Tyr)的未保护酚羟基。它们受控的 ROP 和与聚肌氨酸 (PSar) 的顺序共聚可定量地产生具有可设计聚合度的PDOPA、PTyr 和 PDOPA- b-聚肌氨酸 (PDOPA- b -PSar) 产物。Fe的胶束纳米粒子³⁺ @PDOPA- b -PSar 的制备得益于作为 T1 加权磁共振成像 (MRI) 造影剂的儿茶酚配体对铁 (III) 阳离子的强螯合。例如，Fe ³⁺ @PDOPA ₁₀ - b -PSar ₅₀表现出比商业 Gd ³⁺基化合物更高的纵向弛豫率 ( r ₁ = 5.6 mM ^–1 s ^{–1 )。}体绘制和最大强度投影技术显示的中度（150分钟）裸鼠体内有效MRI对比增强和兔3D磁共振血管造影点燃了Fe ^{3+的临床应用}在放射诊断学中作为不含钆的 MRI 造影剂的基于多肽的 (o)ides。

更新日期：2018-05-29

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