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 journalArticlepeer-review


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
Issue number2
Publication statusPublished - Nov 2011


  • HIV
  • Integrase inhibitors
  • Lymphocytes
  • Macrophages
  • PBMC

ASJC Scopus subject areas

  • Virology
  • Pharmacology


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