MS-8209, a new Amphotericin B derivative that inhibits HIV-1 replicationin vitroand restores T-cell activation via the CD3/TcR in HIV-infected CD4+ cells
作者:
Daniel Céfai,
Fabienne Hadida,
Magdalena Jung,
Patrice Debre,
Jean-Gilles Vernin,
Michel Seman,
期刊:
AIDS
(OVID Available online 1991)
卷期:
Volume 5,
issue 12
页码: 1453-1461
ISSN:0269-9370
年代: 1991
出版商: OVID
关键词: HIV-1 infection;antiviral activity;CD3/T-cell antigen receptor;phospholipase C
数据来源: OVID
摘要:
A new Amphotericin B derivative, MS-8209, which retains high antifungal activity with greatly reduced toxicity and improved solubility, has been developed. We investigated the antiviral properties of MS-8209 in Jurkat and CEM T-cell lines and in peripheral blood mononuclear cells infectedin vitrowith HIV-1BRU. Our results demonstrate, by determination of reverse transcriptase activity and p24 antigen level titration in cell culture supernatants, that MS-8209 inhibits HIV-1 replication in all cell types at concentrations without cytotoxicity. MS-8209 also prevents membrane expression of the HIV-1 large envelope glycoprotein gp120 and the decrease in CD4 level at the surface of infected cells. HIV-1-infected Jurkat cells exhibit a severe signalling defect at CD3 stimulation. Treatment with MS-8209 restores normal responsiveness at CD3 as assessed by measurement of inositol triphosphate accumulation and calcium flux. Finally, our results indicate that MS-8209 inhibits HIV-1BRUreplication without preventing virus binding and penetration into target cells.
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