Attivita di farmaci inhibitor del virus dell'immunodeficienza umana in macrofagi umani e correlazione con l'efficacia clinica

Translated title of the contribution: Correlation between HIV inhibiting drugs activity in human macrophages and clinical outcome

S. Aquaro, E. Balestra, S. Panti, A. Cenci, F. Serra, M. Francesconi, D. Abdelahad, R. Calio, C. F. Perno

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Purpose: To assess the comparative efficacy of drugs inhibitors of human immunodeficiency virus (HIV) in human macrophages and lymphocytes, and to correlate the results with the clinical outcome. Materials and Methods: Human primary macrophages and lymphocytes were infected with HIV in the presence of the following HIV inhibitors, all currently in clinical use: zidovudine, stavudine, zalcitabine, didanosine, lamivudine, PMEA, PMPA (all inhibitors of HIV reverse transcriptase), saquinavir and U-75875 (inhibitors of HIV protease). Results: All reverse transcriptase inhibitors tested showed a markedly higher antiviral activity in macrophages than in lymphocytes. Also protease inhibitors have a substantial anti-HIV activity in macrophages, yet their efficacy is markedly diminished if the drugs are added to macrophage culture after HIV, that is when the virus has established a chronical infection. Under these experimental conditions, however, only protease inhibitors among all HIV-inhibitors in clinical use are able to decrease virus replication in chronically-infected macrophages. Conclusions: The results have strong clinical implications, due to the important role of macrophages in the pathogenesis of HIV infection. Macrophages are the major source of HIV at extralymphoid tissue levels, particularly in the central nervous system, where the blood-brain barrier strongly limits the penetration of antiviral drugs. For these reasons, only drugs, like stavudine and zidovudine, provided with good anti-HIV activity in macrophages, and reasonable barrier penetration have substantial chances to be effective in the central nervous system, and thus affect virus replication in a sanctuary where HIV hides and replicates out of the control of the immune system.

Original languageItalian
Pages (from-to)37-41
Number of pages5
JournalClinica Terapeutica
Volume149
Issue number1
Publication statusPublished - Jan 1998

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Human Activities
Macrophages
HIV
Pharmaceutical Preparations
Stavudine
Zidovudine
Lymphocytes
Virus Replication
Protease Inhibitors
Antiviral Agents
Central Nervous System
Zalcitabine
Saquinavir
Didanosine
HIV Reverse Transcriptase
Reverse Transcriptase Inhibitors
Lamivudine
Virus Diseases
Blood-Brain Barrier
Immune System

ASJC Scopus subject areas

  • Medicine(all)

Cite this

Attivita di farmaci inhibitor del virus dell'immunodeficienza umana in macrofagi umani e correlazione con l'efficacia clinica. / Aquaro, S.; Balestra, E.; Panti, S.; Cenci, A.; Serra, F.; Francesconi, M.; Abdelahad, D.; Calio, R.; Perno, C. F.

In: Clinica Terapeutica, Vol. 149, No. 1, 01.1998, p. 37-41.

Research output: Contribution to journalArticle

Aquaro, S, Balestra, E, Panti, S, Cenci, A, Serra, F, Francesconi, M, Abdelahad, D, Calio, R & Perno, CF 1998, 'Attivita di farmaci inhibitor del virus dell'immunodeficienza umana in macrofagi umani e correlazione con l'efficacia clinica', Clinica Terapeutica, vol. 149, no. 1, pp. 37-41.
Aquaro S, Balestra E, Panti S, Cenci A, Serra F, Francesconi M et al. Attivita di farmaci inhibitor del virus dell'immunodeficienza umana in macrofagi umani e correlazione con l'efficacia clinica. Clinica Terapeutica. 1998 Jan;149(1):37-41.
Aquaro, S. ; Balestra, E. ; Panti, S. ; Cenci, A. ; Serra, F. ; Francesconi, M. ; Abdelahad, D. ; Calio, R. ; Perno, C. F. / Attivita di farmaci inhibitor del virus dell'immunodeficienza umana in macrofagi umani e correlazione con l'efficacia clinica. In: Clinica Terapeutica. 1998 ; Vol. 149, No. 1. pp. 37-41.
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