Selected article for: "aqueous stability and cell proliferation"
Author: Xing, Liang; Sun, Feng; Wang, Zhendong; Li, Yan; Yang, Zhifang; Wang, Fengshan; Zhai, Guangxi; Tan, Haining
Title: Characterization and bioactivity of self-assembled anti-angiogenic chondroitin sulfate-ES2-AF nanoparticle conjugate
  • Document date: 2019_4_10
    • ID: x8f598x2_44
    Snippet: The active peptide that inhibits endothelial cell proliferation in the ES2-AF peptide is ES2, which is derived from the ES sequence (amino acid position 60-70) and is about three times more active than the ES sequence. 28 The ES2 can directly block tyrosine phosphorylation of VEGF receptor on the endothelial cell surface, thereby blocking the transmission of VEGF-mediated signaling pathway. 44 In addition, studies have speculated that nucleolin m.....
    Document: The active peptide that inhibits endothelial cell proliferation in the ES2-AF peptide is ES2, which is derived from the ES sequence (amino acid position 60-70) and is about three times more active than the ES sequence. 28 The ES2 can directly block tyrosine phosphorylation of VEGF receptor on the endothelial cell surface, thereby blocking the transmission of VEGF-mediated signaling pathway. 44 In addition, studies have speculated that nucleolin may be a potential receptor for ES2 in the nucleus of endothelial cells. When ES2-AF enters the endothelial cells, the ES2 fragment can inhibit the phosphorylation process of the nucleolus, directly affecting the biosynthesis and maturation of ribosomes and indirectly influencing the process of chromatin replication and nucleogenesis. Then, the mitotic process of the endothelial cells is arrested, inhibiting the endothelial cell proliferation. 45 The MTT assay was used to evaluate the inhibitory effects of ES2-AF and its glycosylation modification products on the proliferation of EA.hy926 cells. It was found that the inhibitory activities of both the drugs were dose-dependent. The activity of polypeptide drugs is often related to their structure. Compared with small molecule drugs, polypeptide drugs tend to have poor stability in aqueous solution due to their spatial structure. The peptide ES2-AF was modified with CS, and the stability of the modified product CS-ES2-AF was improved in aqueous solution. The CS can increase the solubility of ES2-AF in aqueous solution as the CS group forces water molecules around the polypeptide ES2-AF to improve the stability of ES2-AF. Moreover, the higher the concentration of ES2-AF, the more the stability of ES2-AF. Previous research also supports this conclusion. 46 In addition, MTT results are also related to cell status and degree of differentiation, so cells with better status should be selected for experiments.

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