葡聚糖-两性霉素B的制备及其抑菌活性研究

摘要

Three oxidation degree ofdextran derivatives (D-CHO) were synthesized with oxidation of sodium periodate.Dextran-amphotericin B (D-CHO-AmB) conjugate was prepared by Schiffs base reaction between aldehyde groups of D-CHO and amino groups of AmB.MALS/GPC results indicated that the molecular weight of dextran was reduced with the increase of oxidation degree.The drug loadings of D-CHO-AmB were 18.9％ to 36.7％,which increased with the oxidation degree.Compared with AmB injection,the hemolytic effect of D-CHO-AmB was decreased significantly and the critical concentration of hemolysis was almost tenfold.The inhibition zone test proved that D-CHO-AmB conjugates had an excellent antifungal effect.%通过高碘酸钠氧化,合成了3种氧化度的葡聚糖衍生物(D-CHO),并利用D-CHO醛基和两性霉素B(AmB)氨基的席夫碱反应,制备了水溶性葡聚糖-AmB(D-CHO-AmB)共轭物.多角度激光光散射凝胶色谱仪结果表明,随着葡聚糖的相对分子质量随着氧化度的增大而降低.不同D-CHO-AmB的载药量在18.9％-36.7％之间,且氧化度越高,载药量越大.D-CHO-AmB的溶血作用比AmB注射剂显著性降低,且具有较好的抑菌效果.