Inhibition of HIV-1 in Monocyte/Macrophage Cultures by 2′,3′-Dideoxycytidine-5′-Triphosphate, Free and in Liposomes

Janos Szebeni, Sharon M. Wahl, Gurupadappa V. Betageri, Larry M. Wahl, Suzanne Gartner, Mikulas Popovic, Robert J. Parker, Christopher D.v. Black, John N. Weinstein

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41 Citations (Scopus)

Abstract

The antiviral effects of 2′,3′-dideoxycytidine (ddC), 2′,3′-dideoxycytidine-5′-triphosphate (ddCTP) and liposome-encapsulated ddCTP [L(ddCTP)] were compared in cultured human monocyte-macrophages (M/M) infected with HIV-1. These treatments inhibited virus replication at nanomolar drug levels with activities in the order ddC > ddCTP = L(ddCTP). Studies on drug stability and uptake suggest that a large part of the free ddCTP is dephosphorylated before entering the cells, whereas L(ddCTP) remains stable over days and is taken up, probably by endocytosis. The response to L(ddCTP) suggests that the capability of liposomes for targeting drugs to macrophages in vivo could potentially be exploited to improve the therapeutic index of dideoxynucleoside drugs.

Original languageEnglish
Pages (from-to)691-702
Number of pages12
JournalAIDS Research and Human Retroviruses
Volume6
Issue number5
DOIs
Publication statusPublished - May 1990

ASJC Scopus subject areas

  • Immunology
  • Virology
  • Infectious Diseases

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    Szebeni, J., Wahl, S. M., Betageri, G. V., Wahl, L. M., Gartner, S., Popovic, M., Parker, R. J., Black, C. D. V., & Weinstein, J. N. (1990). Inhibition of HIV-1 in Monocyte/Macrophage Cultures by 2′,3′-Dideoxycytidine-5′-Triphosphate, Free and in Liposomes. AIDS Research and Human Retroviruses, 6(5), 691-702. https://doi.org/10.1089/aid.1990.6.691