Fractions of chemically oversulphated galactosaminoglycan sulphates inhibit three enveloped viruses: human immunodeficiency virus type 1, herpes simplex virus type 1 and human cytomegalovirus

Antivir Chem Chemother. 1999 Jan;10(1):33-8. doi: 10.1177/095632029901000104.

Abstract

A series of chemically oversulphated galactosaminoglycans (SO3H:COOH ratio > or = 2) were tested in vitro as antiviral agents against human immunodeficiency virus type 1 (HIV-1), the aetiological agent of AIDS, and against herpes simplex virus type 1 and human cytomegalovirus, two agents responsible for opportunistic infections in HIV-infected people. The oversulphated derivatives displayed an increase in activity ranging from one to four orders of magnitude against the three viruses, as compared to the natural parent compounds (SO3H:COOH, ratio approx. 1). The antiviral activity of these polyanions appears to be favoured by a high degree of sulphation and a high molecular mass. An oversulphated dermatan, with a SO3H:COOH ratio of 2.86 and molecular mass of 23.2 kDa, was the most potent anti-HIV-1 compound (EC50 0.04 microgram/ml). A second oversulphated dermatan, with a SO3H:COOH ratio of 2.40 and molecular mass of 25 kDa, displayed the highest activity against HSV-1 (EC50 0.01 microgram/ml). An oversulphated chondroitin, with a SO3H:COOH ratio of 2.80 and molecular mass of 17.3 kDa, was the strongest anti-HCMV agent (EC50 0.4 microgram/ml). In view of the absence of the side-effects typical of heparin-like compounds, a combination of these derivatives could have therapeutic potential.

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / metabolism
  • Anti-HIV Agents / pharmacology
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / metabolism
  • Antiviral Agents / pharmacology*
  • Carbohydrate Sequence
  • Cytomegalovirus / drug effects
  • HIV-1 / drug effects
  • Herpesvirus 1, Human / drug effects
  • Humans
  • Nucleocapsid / antagonists & inhibitors*
  • Polysaccharides / chemistry
  • Polysaccharides / metabolism
  • Polysaccharides / pharmacology*
  • Sulfates / chemistry
  • Sulfates / metabolism
  • Sulfates / pharmacology*
  • T-Lymphocytes / virology
  • Viruses / drug effects*

Substances

  • Anti-HIV Agents
  • Antiviral Agents
  • Polysaccharides
  • Sulfates
  • galactosaminoglycan