Derivatives of amphotericin inhibit infection with human immunodeficiency virus in vitro by different modes of action.

Abstract

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 microgram/ml; N-(N'-(3-dimethylaminopropyl)N"-ethyl guanyl) amphotericin B (DAPEG) did so at 5-11 micrograms/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 micrograms/ml.

• Authors: J E Hansen, N M Witzke, C Nielsen, L R Mathiesen, L S Teglbjaerg, C M Nielsen, J O Nielsen
• Journal: Antiviral research (Antiviral Res) Vol. 14 Issue 3 Pg. 149-59 (Sep 1990) ISSN: 0166-3542 [Print] Netherlands
• PMID: 2080870 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• HIV Antigens
• methylamphotericin B
• N-(N'-(2-(4'-methylmorpholinio)ethyl)-N''-cyclohexylguanyl)amphotericin B methyl ester
• Amphotericin B
• amphotericin B, N-(N'-(3-dimethylaminopropyl)-N''-ethylguanyl)-

Topics

• Amphotericin B (analogs & derivatives, pharmacology, toxicity)
• Cell Fusion (drug effects)
• Cell Line
• Cell Survival (drug effects)
• Giant Cells (drug effects)
• HIV Antigens (analysis)
• HIV-1 (drug effects, physiology)
• Humans