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.

Scopelliti, F., Pollicita, M., CECCHERINI SILBERSTEIN, F., Santo, F., Surdo, M., Aquaro, S., et al. (2011). Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes. ANTIVIRAL RESEARCH, 92(2), 255-261 [10.1016/j.antiviral.2011.08.008].

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

POLLICITA, MICHELA;CECCHERINI SILBERSTEIN, FRANCESCA;AQUARO, STEFANO;PERNO, CARLO FEDERICO
2011-01-01

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.
2011
In corso di stampa
Rilevanza internazionale
Articolo
Sì, ma tipo non specificato
Settore MED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICA
English
Con Impact Factor ISI
HIV; integrase inhibitors; macrophages; PBMC; lymphocytes
Scopelliti, F., Pollicita, M., CECCHERINI SILBERSTEIN, F., Santo, F., Surdo, M., Aquaro, S., et al. (2011). Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes. ANTIVIRAL RESEARCH, 92(2), 255-261 [10.1016/j.antiviral.2011.08.008].
Scopelliti, F; Pollicita, M; CECCHERINI SILBERSTEIN, F; Santo, F; Surdo, M; Aquaro, S; Perno, Cf
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/18065
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