葡聚糖-两性霉素B的制备及其抑菌活性研究

Preparation and Antibacterial Activities of Dextran-Amphotericin B Conjugates

摘要:

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。

Abstract:

Three oxidation degree of dextran derivatives（D-CHO） were synthesized with oxidation of sodium periodate. Dextran-amphotericin B（D-CHO-AmB） conjugate was prepared by Schiff's 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.