A new homodimer of aciclovir as a prodrug with increased solubility and antiviral activity
Résumé
Aciclovir (ACV) is the drug of choice against herpes simplex virus type 1 (HSV-1) infection. However, its limited solubility in water and limited oral bioavailability represent the main limitations of this drug. Utilising a plaque reduction assay, this study assessed the antiherpetic activity of a new homodimer of ACV (ACVpACV) with a higher water solubility. ACVpACV markedly inhibited HSV-1 replication in Vero cells [50% effective concentration (EC) of 2.8μM vs. 6.6μM for ACV] and was non-toxic in the cells at concentrations ≤15μM. ACVpACV encapsulated in erythrocytes provides effective protection against HSV-1 replication in human macrophages and also partially against the HSV-1 thymidine kinase-deficient strain. Thus, ACVpACV acts as an effective antiviral prodrug against HSV-1.
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PEER_stage2_10.1016%2Fj.ijantimicag.2009.02.025.pdf (219.02 Ko)
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