Evaluation of PD 404,182 as an anti-HIV and anti-herpes simplex virus microbicide

Antimicrob Agents Chemother. 2014;58(2):687-97. doi: 10.1128/AAC.02000-13. Epub 2013 Nov 11.

Abstract

PD 404,182 (PD) is a synthetic compound that was found to compromise HIV integrity via interaction with a nonenvelope protein viral structural component (A. M. Chamoun et al., Antimicrob. Agents Chemother. 56:672-681, 2012). The present study evaluates the potential of PD as an anti-HIV microbicide and establishes PD's virucidal activity toward another pathogen, herpes simplex virus (HSV). We show that the anti-HIV-1 50% inhibitory concentration (IC50) of PD, when diluted in seminal plasma, is ∼1 μM, similar to the IC50 determined in cell culture growth medium, and that PD retains full anti-HIV-1 activity after incubation in cervical fluid at 37°C for at least 24 h. In addition, PD is nontoxic toward vaginal commensal Lactobacillus species (50% cytotoxic concentration [CC50], >300 μM), freshly activated human peripheral blood mononuclear cells (CC50, ∼200 μM), and primary CD4(+) T cells, macrophages, and dendritic cells (CC50, >300 μM). PD also exhibited high stability in pH-adjusted Dulbecco's phosphate-buffered saline with little to no activity loss after 8 weeks at pH 4 and 42°C, indicating suitability for formulation for transportation and storage in developing countries. Finally, for the first time, we show that PD inactivates herpes simplex virus 1 (HSV-1) and HSV-2 at submicromolar concentrations. Due to the prevalence of HSV infection, the ability of PD to inactivate HSV may provide an additional incentive for use as a microbicide. The ability of PD to inactivate both HIV-1 and HSV, combined with its low toxicity and high stability, warrants additional studies for the evaluation of PD's microbicidal candidacy in animals and humans.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • CD4-Positive T-Lymphocytes / cytology
  • CD4-Positive T-Lymphocytes / drug effects
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Dendritic Cells / cytology
  • Dendritic Cells / drug effects
  • Drug Stability
  • Extracellular Fluid / chemistry
  • Female
  • HEK293 Cells
  • HIV-1 / drug effects*
  • HIV-1 / growth & development
  • Herpesvirus 1, Human / drug effects*
  • Herpesvirus 1, Human / growth & development
  • Humans
  • Imines / pharmacology*
  • Inhibitory Concentration 50
  • Macrophages / cytology
  • Macrophages / drug effects
  • Male
  • Primary Cell Culture
  • Semen / chemistry
  • Temperature
  • Thiazines / pharmacology*
  • Vero Cells

Substances

  • 6H-6-imino-(2,3,4,5-tetrahydropyrimido)(1,2-c)-(1,3)benzothiazine
  • Antiviral Agents
  • Imines
  • Thiazines