Squalamine as a broad-spectrum systemic antiviral agent with therapeutic potential

Proc Natl Acad Sci U S A. 2011 Sep 20;108(38):15978-83. doi: 10.1073/pnas.1108558108. Epub 2011 Sep 19.

Abstract

Antiviral compounds that increase the resistance of host tissues represent an attractive class of therapeutic. Here, we show that squalamine, a compound previously isolated from the tissues of the dogfish shark (Squalus acanthias) and the sea lamprey (Petromyzon marinus), exhibits broad-spectrum antiviral activity against human pathogens, which were studied in vitro as well as in vivo. Both RNA- and DNA-enveloped viruses are shown to be susceptible. The proposed mechanism involves the capacity of squalamine, a cationic amphipathic sterol, to neutralize the negative electrostatic surface charge of intracellular membranes in a way that renders the cell less effective in supporting viral replication. Because squalamine can be readily synthesized and has a known safety profile in man, we believe its potential as a broad-spectrum human antiviral agent should be explored.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Cell Line
  • Cell Membrane / chemistry
  • Cell Membrane / drug effects
  • Cells, Cultured
  • Cholestanols / chemistry
  • Cholestanols / pharmacology
  • Cricetinae
  • Female
  • Hepatitis B virus / drug effects
  • Hepatitis B virus / growth & development
  • Hepatitis Delta Virus / drug effects
  • Hepatitis Delta Virus / growth & development
  • Hepatocytes / drug effects
  • Hepatocytes / virology
  • Humans
  • Male
  • Mesocricetus
  • Mice
  • Mice, Inbred BALB C
  • Molecular Structure
  • Muromegalovirus / drug effects
  • Muromegalovirus / growth & development
  • Scattering, Small Angle
  • Virus Diseases / drug therapy*
  • Virus Diseases / virology
  • Virus Replication / drug effects*
  • X-Ray Diffraction
  • rac1 GTP-Binding Protein / chemistry

Substances

  • Anti-Bacterial Agents
  • Antiviral Agents
  • Cholestanols
  • rac1 GTP-Binding Protein
  • squalamine