Antiviral effect of the heparan sulfate mimetic, PI-88, against dengue and encephalitic flaviviruses

Date

2006

Authors

Lee, Eva
Pavy, Megan
Young, Nicolie
Freeman, Craig
Lobigs, Mario

Journal Title

Journal ISSN

Volume Title

Publisher

Elsevier

Abstract

Many viruses, including flaviviruses, display affinity for cell surface heparan sulfate (HS) proteoglycans with biological relevance in virus attachment/entry. This raises the possibility of the application of HS mimetics in antiviral therapy. We have evaluated the antiviral effect of the sulfated polysaccharides, suramin, pentosan polysulfate (PPS) and PI-88, which are currently approved or in trial for clinical use, against dengue virus (DEN) and the encephalitic flaviviruses, Japanese encephalitis virus, West Nile virus, and Murray Valley encephalitis virus. A flow cytometry-based method for the measurement of inhibition of virus infectivity was developed, which showed the in vitro antiviral activity of the three compounds, albeit with differences in efficiency which were virus-dependent. The 50% effective concentration (EC 50) values for DEN inhibition were in the order: PPS < suramin < PI-88, and for Japanese encephalitis virus, PPS < PI-88 ≤ suramin. Heparin inhibited the DEN infectivity 30-fold more efficiently than the best of the test compounds, which was not the case for encephalitic flaviviruses. The in vitro anti-flaviviral effectiveness of the HS mimetics did not reliably predict their in vivo therapeutic activity. In mouse models for DEN and flaviviral encephalitis, only PI-88 demonstrated a significant beneficial effect in disease outcome.

Description

Keywords

Keywords: antivirus agent; heparan sulfate; pentosan polysulfate; pi 88; suramin; unclassified drug; animal experiment; antiviral activity; article; concentration response; controlled study; Dengue virus; drug efficacy; Flavivirus; flow cytometry; in vitro study; J Flavivirus; Heparan sulfate mimetic; Japanese encephalitis virus; West Nile virus

Citation

Source

Antiviral Research

Type

Journal article

Book Title

Entity type

Access Statement

License Rights

Restricted until

2037-12-31