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葡萄糖胺-肝素盐的制备、抗凝和抗氧化性能。

Preparation, Anticoagulant and Antioxidant Properties of Glucosamine-Heparin Salt.

机构信息

Key Laboratory of Coastal Biology and Bioresource Utilization, Yantai Institute of Coastal Zone Research, Chinese Academy of Sciences, Yantai 264003, China.

Center for Ocean Mega-Science, Chinese Academy of Sciences, 7 Nanhai Road, Qingdao 266071, China.

出版信息

Mar Drugs. 2022 Oct 18;20(10):646. doi: 10.3390/md20100646.

Abstract

Excessive inorganic ions in vivo may lead to electrolyte disorders and induce damage to the human body. Therefore, preparation of enhanced bioactivity compounds, composed of activated organic cations and organic anions, is of great interest among researchers. In this work, glucosamine-heparin salt (GHS) was primarily synthesized with positively charged glucosamine hydrochloride (GAH) and negatively charged heparin sodium (Heps) by ion exchange method. Then, the detailed structural information of the GHS was characterized by FTIR, H NMR spectroscopy and ICP-MS. In addition, its anticoagulant potency and antioxidant properties were evaluated, respectively. The results demonstrated that GHS salt achieved enhanced antioxidant activities, including 98.78% of O• radical scavenging activity, 91.23% of •OH radical scavenging rate and 66.49% of DPPH radical scavenging capacity at 1.6 mg/mL, severally. Meanwhile, anticoagulant potency (ATTP) of GHS strengthened from 153.10 ± 17.14 to 180.03 ± 6.02 at 0.75 μmol/L. Thus, introducing cationic glucosamine residues into GHS could improve its anticoagulant activity. The findings suggest that GHS product with a small amount of inorganic ions can greatly abate the prime cost of antioxidants and anticoagulants, and has significant economic benefits and practical significance.

摘要

体内过量的无机离子可能导致电解质紊乱,并对人体造成损害。因此,制备由活化的有机阳离子和有机阴离子组成的增强生物活性化合物引起了研究人员的极大兴趣。在这项工作中,通过离子交换法主要合成了带正电荷的盐酸氨基葡萄糖(GAH)和带负电荷的肝素钠(Heps)的氨基葡萄糖-肝素盐(GHS)。然后,通过傅里叶变换红外光谱(FTIR)、核磁共振波谱(H NMR)和电感耦合等离子体质谱(ICP-MS)对 GHS 的详细结构信息进行了表征。此外,还分别评估了其抗凝性能和抗氧化性能。结果表明,GHS 盐在 1.6mg/mL 时具有增强的抗氧化活性,包括 98.78%的 O•自由基清除活性、91.23%的•OH 自由基清除率和 66.49%的 DPPH 自由基清除能力。同时,GHS 的抗凝活性(ATTP)从 153.10±17.14 增强到 0.75μmol/L 时的 180.03±6.02。因此,将阳离子氨基葡萄糖残基引入 GHS 可以提高其抗凝活性。研究结果表明,具有少量无机离子的 GHS 产品可以大大降低抗氧化剂和抗凝剂的主要成本,具有显著的经济效益和实际意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3aee/9604614/a516a0ae210c/marinedrugs-20-00646-g0A1.jpg

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