Potent antiviral activity of amprenavir in primary macrophages infected by human immunodeficiency virus

Stefano Aquaro, Tania Guenci, Fabiola Di Santo, Mauro Francesconi, Raffaele Caliò, Carlo Federico Perno

Research output: Contribution to journalArticle

Abstract

Objective of the present study was then to assess the antiviral activity of the protease inhibitor amprenavir in macrophages (M/M), and to compare it with its efficacy in peripheral blood lymphocytes (PBL). M/M were obtained from blood of sero-negative healthy donors and infected with M-tropic HIV-1 strain (HIV-1Ba-L). The stabilized infection was assessed by monitoring the HIV-1 p24 gag antigen production in the supernatants of M/M cultures. In the setting of acute infection (treatment before HIV-1 challenge), amprenavir showed substantial activity both in M/M and PBL at similar concentrations (EC50: 0.011 and 0.031μM, respectively); complete inhibition of HIV-1 replication was achieved in both cell types at concentration of about 2μM. In the setting of chronical infection (i.e. antiviral treatment several days after established infection), an antiviral effect of amprenavir was achieved in M/M, but at concentrations higher than those active in acutely infected M/M (EC50: 0.72μM, EC90: 18.2μM). The antiviral effect in chronically infected M/M was sustained for at least 2 weeks of continuous treatment. These findings suggest that amprenavir (at relatively high concentrations) has a clinically relevant antiviral effect in persistently infected reservoirs of HIV.

Original languageEnglish
Pages (from-to)133-137
Number of pages5
JournalAntiviral Research
Volume61
Issue number2
DOIs
Publication statusPublished - Feb 2004

Keywords

  • CD4-lymphocytes
  • HAART
  • Protease inhibitors
  • Reservoirs
  • Therapy

ASJC Scopus subject areas

  • Virology
  • Pharmacology

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