作者:Jan Balzarini、Christophe Pannecouque、Erik De Clercq、Andrey Y. Pavlov、Svetlana S. Printsevskaya、Olga V. Miroshnikova、Marina I. Reznikova、Maria N. Preobrazhenskaya
DOI:10.1021/jm0300882
日期:2003.6.1
natural antibacterial glycopeptide antibiotics such as vancomycin, eremomycin, ristocetin A, teicoplanin A(2)-2, DA-40926, their aglycons, and also the products of their partial degradation with a destroyed or modified peptide core show marked anti-retroviral activity in cell culture. In particular, aglycon antibiotic derivatives containing various substituents of a preferably hydrophobic nature displayed
多种天然抗菌糖肽抗生素的半合成衍生物,例如万古霉素,埃雷霉素,瑞斯托菌素A,替考拉宁A(2)-2,DA-40926,它们的糖苷配基,以及具有被破坏或修饰的肽核的部分降解产物在细胞培养中具有明显的抗逆转录病毒活性。尤其是,含有优选具有疏水性的各种取代基的糖苷配基抗生素衍生物在较低的微摩尔浓度下(50%抑制浓度)显示出对人类免疫缺陷病毒1型(HIV-1),HIV-2和莫洛尼鼠肉瘤病毒的活性(1-浓度范围为5 microM),而在250 microM或更高的浓度下不会对人淋巴细胞产生细胞抑制作用。抗生素糖苷配基衍生物的抗HIV作用方式可归因于病毒进入过程的抑制。