National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun 130012, China.
Key Laboratory for Molecular Enzymology and Engineering the Ministry of Education, School of Life Sciences, Jilin University, Changchun 130012, China.
Molecules. 2017 Jul 26;22(8):1253. doi: 10.3390/molecules22081253.
In this study, a novel conjugate consisting of glycol chitosan (GCS) and ethylene diamine tetraacetic acid (EDTA) was synthesized and characterized in terms of conjugation and heavy metal ion chelating capacity. Moreover, its potential application as a metalloenzyme inhibitor was evaluated with three thymopoietin oligopeptides in the presence of leucine aminopeptidase. The results from FTIR and NMR spectra revealed that the covalent attachment of EDTA to GCS was achieved by the formation of amide bonds between the carboxylic acid group of EDTA and amino groups of GCS. The conjugated EDTA lost part of its chelating capacity to cobalt ions compared with free EDTA as evidenced by the results of cobalt ion chelation-mediated fluorescence recovery of calcein. However, further investigation confirmed that GCS-EDTA at low concentrations significantly inhibited leucine aminopeptidase-mediated degradation of all thymopoietin oligopeptides.
在这项研究中，合成了一种新型的壳聚糖乙二醇（GCS）和乙二胺四乙酸（EDTA）缀合物，并从缀合和重金属离子螯合能力两方面对其进行了表征。此外，还通过亮氨酸氨基肽酶存在下的三种胸腺肽寡肽，评估了其作为金属酶抑制剂的潜在应用。FTIR 和 NMR 光谱的结果表明，EDTA 与 GCS 的共价连接是通过 EDTA 的羧酸基团与 GCS 的氨基之间形成酰胺键实现的。与游离 EDTA 相比，缀合的 EDTA 对钴离子的部分螯合能力丧失，这一点可以通过钙黄绿素钴离子螯合介导的荧光恢复实验结果得到证明。然而，进一步的研究证实，低浓度的 GCS-EDTA 可显著抑制亮氨酸氨基肽酶介导的所有胸腺肽寡肽的降解。
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