DERIVATIVES OF AMPHOTERICIN INHIBIT INFECTION WITH HUMAN-IMMUNODEFICIENCY-VIRUS INVITRO BY DIFFERENT MODES OF ACTION

被引:16
作者
HANSEN, JES
WITZKE, NM
NIELSEN, C
MATHIESEN, LR
TEGLBJAERG, LS
NIELSEN, CM
NIELSEN, JO
机构
[1] HVIDOVRE UNIV HOSP,DEPT INFECT DIS,DK-2650 HVIDOVRE,DENMARK
[2] STATENS SERUM INST,DEPT VIROL,DK-2300 COPENHAGEN,DENMARK
关键词
Amphotericin B; HIV; Syncytium formation;
D O I
10.1016/0166-3542(90)90031-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Three water-soluble derivatives of amphotericin B were tested for inhibition of HIV infection in vitro. The compounds amphotericin B methyl ester (AME) and N-(N′-(2-(4′-methylmorpholinio)ethyl)N″-cyclohexyl guanyl) amphotericin B methyl ester (MCG) inhibited HIV infection by 50% at 1 μg/ml; N-(N′-(3-dimethylaminopropyl)N″-ethyl guanyl) amphotericin B (DAPEG) did so at 5-11 μg/ml. While the virus-inhibitory effect of AME was due to an interaction with target lymphocytes, the effect of MCG was due to a direct anti-viral action. AME increased the potential of infected cells to fuse with uninfected cells, but MCG had no significant effect on cell fusion. All compounds had a lower cellular toxicity than amphotericin B and were not toxic at concentrations below 20 μg/ml. © 1990.
引用
收藏
页码:149 / 160
页数:12
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