Abstract
BackgroundTerpenoid derivatives originating from many plants species, are interesting compounds with numerous biological effects, such as anti-HIV-1 activity. The zinc tetra-ascorbo-camphorate complex (or "C14"), a new monoterpenoid derivative was evaluated in vitro for its anti-HIV-1 activity on both R5- and X4-HIV-1 infection of primary target cells (macrophages, dendritic cells and T cells) and on HIV-1 transfer from dendritic cells to T cells.ResultsThe toxicity study was carried out in vitro and also with the New Zealand White rabbit vaginal irritation model. C14 was found to be no cytotoxic at high concentrations (CC50 > 10 μM) and showed to be a potential HIV-1 inhibitor of infection of all the primary cells tested (EC50 = 1 μM). No significant changes could be observed in cervicovaginal tissue of rabbit exposed during 10 consecutive days to formulations containing up to 20 μM of C14.ConclusionOverall, these preclinical studies suggest that zinc tetra-ascorbo-camphorate derivative is suitable for further testing as a candidate microbicide to prevent male-to-female heterosexual acquisition of HIV-1.
Highlights
Terpenoid derivatives originating from many plants species, are interesting compounds with numerous biological effects, such as anti-HIV-1 activity
monocyte-derived macrophages (MDM), monocyte-derived dendritic cells (MDDC) and T cells were exposed to serial concentrations of each C14 derivate ranging from 1 to 12 μM for 24 hours
The C14 compound used in the study showed potent HIV1 inhibitor with IC50 of 1 μM in the different primary cells, and was able to inhibit the transfer of HIV-1 from MDDC to autologous CD4+ T lymphocytes
Summary
Terpenoid derivatives originating from many plants species, are interesting compounds with numerous biological effects, such as anti-HIV-1 activity. Interventions aimed to provide significant changes in sexual behaviour and increased frequency of barrier methods (male and female condoms) use have not proven their efficacy to decrease the HIV-1 epidemic in developing countries [2]. Microbicides may theoretically target the incoming virus at several steps of molecular events driving viral entry and/or viral replication. Unlike condoms, they will not create a physical barrier to intimate contact, nor will they neces-. AIDS Research and Therapy 2008, 5:10 http://www.aidsrestherapy.com/content/5/1/10 sarily be contraceptive. The fact that their use will be controlled by women obviously constitutes a very significant advantage
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