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首页> 外文期刊>Polymers for advanced technologies >Methoxy poly (ethylene glycol) thiosulfonate: new activated polymer derivatives for thiol-specific modification
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Methoxy poly (ethylene glycol) thiosulfonate: new activated polymer derivatives for thiol-specific modification

机译：甲氧基聚（乙二醇）硫代磺酸盐：用于硫醇特异性修饰的新型活化聚合物衍生物

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摘要

Thiol-reactive methoxy poly (ethylene glycol) (mPEG) derivatives, mPEG methanethiosulfonate (mPEG-MTS) and mPEG phenylthiosulfonate (mPEG-PTS), were synthesized by one-step S-alkylation of mPEG-halide with the corresponding sodium thiosulfonate. These functionalized polymers were fully characterized by ~1H NMR, ~(13)C NMR, GPC as well as MALDI-TOF. To demonstrate the potential application of mPEG-MTS and mPEG-PTS, papain and recombinant human granulocyte colony-stimulating factor (rhG-CSF) were used as prototype protein for thiol-selective PEGylation. The PEGylated products were verified by one or more of the following methods: SDS-PAGE, HPLC, HPSEC as well as MALDI-TOF. Compared with native rhG-CSF, the PEGylated rhG-CSF was further characterized by in vitro cell proliferative assay and preserved 59% biological activity. Furthermore, mPEG 20k-MTS was used to modify BSA nanoparticles coated with thiol groups. FT-IR and ζ-potential assay demonstrated that mPEG thiosulfonate can be effectively immobilized at the nanoparticles' surface via disulfide linkage to form hydrophilic and neutral corona. Therefore, we have demonstrated thiol-selective PEG derivatives, endowed with unusual versatility, for practical use and potential exploitation.
机译：巯基反应性甲氧基聚乙二醇（mPEG）衍生物，mPEG甲硫代磺酸盐（mPEG-MTS）和mPEG苯硫代磺酸盐（mPEG-PTS）是通过mPEG-卤化物与相应的硫代磺酸钠的一步S-烷基化反应合成的。这些官能化的聚合物通过〜1H NMR，〜（13）C NMR，GPC以及MALDI-TOF进行了充分表征。为了证明mPEG-MTS和mPEG-PTS的潜在应用，木瓜蛋白酶和重组人粒细胞集落刺激因子（rhG-CSF）被用作巯基选择性PEG化的原型蛋白。通过以下一种或多种方法验证PEG化产品：SDS-PAGE，HPLC，HPSEC以及MALDI-TOF。与天然rhG-CSF相比，聚乙二醇化的rhG-CSF通过体外细胞增殖试验进一步表征，并保留了59％的生物学活性。此外，mPEG 20k-MTS用于修饰涂有巯基的BSA纳米颗粒。 FT-IR和ζ电位分析表明，mPEG硫代磺酸盐可以通过二硫键有效地固定在纳米颗粒的表面，形成亲水性和中性的电晕。因此，我们已经证明了硫醇选择性PEG衍生物具有非凡的多功能性，可用于实际用途和潜在的开发用途。

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