Anti-HIV Effects of Chloroquine: Inhibition of Viral Particle Glycosylation and Synergism with Protease Inhibitors

Andrea Savarino, Mothanje B. Lucia, Elena Rastrelli, Sergio Rutella, Caterina Golotta, Emanuella Morra, Enrica Tamburrini, Carlo Federico Perno, Johan R. Boelaert, Kirk Sperber, Roberto Cauda

Research output: Contribution to journalArticlepeer-review


Objective: We tested the effects of chloroquine (CQ) on glycosylation of HIV particles and in combination with protease inhibitors (PIs) on HIV replication and on P-glycoprotein (P-gp)/multidrug resistance protein-1 (MRP1). Design: CD4+ cell lines were infected with laboratory strains and peripheral blood mononuclear cells were infected with primary isolates for evaluation of the anti-HIV effects. Peripheral blood lymphocytes were evaluated for of P-gp and MRP1 functions. Methods: HIV replication was assessed by enzyme-linked immunosorbent assay. HIV glycosylation was measured by metabolic labeling of viral particles with [3H] glucosamine. Synergism was tested using isobolograms. P-gp and MRP1 functions were assayed using rhodamine 123 (Rh123) and carboxyfluorescein (CF) efflux assays, respectively. Results: CQ alone inhibited HIV replication and glycosylation in a dose-dependent manner. In combination with indinavir (IDV), ritonavir, or saquinavir (SQV), CQ had a synergistic effect at concentrations found in plasma of subjects receiving malaria prophylaxis. CQ decreased the 50% effective concentration of IDV in primary isolates from Africa and restored the response to IDV or SQV in 3 PI-resistant isolates. CQ increased the block of Rh123 and CF efflux activity exerted by PIs. Conclusion: The inhibitory effects of CQ on HIV glycosylation are associated with synergistic effects in combination with PIs. The CQ/PI combination exerts combined inhibitory effects on P-gp and MRP1 function.

Original languageEnglish
Pages (from-to)223-232
Number of pages10
JournalJournal of Acquired Immune Deficiency Syndromes
Issue number3
Publication statusPublished - Mar 1 2004


  • Antimalarial
  • Developing countries
  • Multidrug resistance protein-1
  • P-glycoprotein
  • Protease inhibitors
  • Synergism

ASJC Scopus subject areas

  • Virology
  • Immunology


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