Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes

Fernanda Scopelliti, Michela Pollicita, Francesca Ceccherini-Silberstein, Fabiola Di Santo, Matteo Surdo, Stefano Aquaro, Carlo Federico Perno

Research output: Contribution to journal › Article

22 Citations (Scopus)

Abstract

The activity of raltegravir and 4 other integrase inhibitors (MK-2048, L870,810, IN2, and IN5) was investigated in primary human macrophages, PBMC and C8166-lymphocytic T cells, in order to determine their relative potency and efficacy in different cellular systems of HIV infection. Raltegravir showed better protective efficacy in all cell types; MK-2048, L870,810 and IN5 showed a potent anti-HIV-1 activity in macrophages, while in lymphocytes only MK-2048 and L870,810 showed an inhibitory effect comparable to raltegravir. IN2 was a poorly effective anti-HIV-1 compound in all cellular systems. All effective integrase inhibitors exhibited a potent antiviral activity against both X4 and R5 HIV-1 strains. In general, raltegravir, MK-2048, L870,810 and IN5 showed anti HIV activity similar or slightly higher in macrophages compared to PBMC and C8166 T cells: for MK-2048, the EC 50 was 0.4, 0.9, 11.5nM in macrophages, in PBMCs and T cells, respectively; for L870,810, the EC 50 was 1.5, 14.3, and 10.6nM, respectively; for IN5 the EC 50 was 0.5, 13.7, and 5.7nM, respectively.

Original languageEnglish
Pages (from-to)255-261
Number of pages7
JournalAntiviral Research
Volume92
Issue number2
DOIs
Publication statusPublished - Nov 2011

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Integrase Inhibitors
Antiviral Agents
Macrophages
Lymphocytes
HIV-1
T-Lymphocytes
HIV Infections
HIV
Raltegravir Potassium

Keywords

  • HIV
  • Integrase inhibitors
  • Lymphocytes
  • Macrophages
  • PBMC

ASJC Scopus subject areas

  • Virology
  • Pharmacology

Cite this

Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes. / Scopelliti, Fernanda; Pollicita, Michela; Ceccherini-Silberstein, Francesca; Di Santo, Fabiola; Surdo, Matteo; Aquaro, Stefano; Perno, Carlo Federico.

In: Antiviral Research, Vol. 92, No. 2, 11.2011, p. 255-261.

Research output: Contribution to journal › Article

Scopelliti, F, Pollicita, M, Ceccherini-Silberstein, F, Di Santo, F, Surdo, M, Aquaro, S & Perno, CF 2011, 'Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes', Antiviral Research, vol. 92, no. 2, pp. 255-261. https://doi.org/10.1016/j.antiviral.2011.08.008
Scopelliti F, Pollicita M, Ceccherini-Silberstein F, Di Santo F, Surdo M, Aquaro S et al. Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes. Antiviral Research. 2011 Nov;92(2):255-261. https://doi.org/10.1016/j.antiviral.2011.08.008
Scopelliti, Fernanda ; Pollicita, Michela ; Ceccherini-Silberstein, Francesca ; Di Santo, Fabiola ; Surdo, Matteo ; Aquaro, Stefano ; Perno, Carlo Federico. / Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes. In: Antiviral Research. 2011 ; Vol. 92, No. 2. pp. 255-261.
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