ANTIVIRAL PORTRAIT SERIES .4. POLYSULFATES AS INHIBITORS OF HIV AND OTHER ENVELOPED VIRUSES

Polysulfates are highly potent and selective inhibitors of the in vitr o replication of HIV and other enveloped viruses. They not only inhibi t the cytopathic effect of HIV, but also prevent HIV-induced syncytium (giant cell) formation. They also act synergistically with other anti -HIV drugs. The anti-HIV activity of polysulfates is a result of their shielding of the positively charged sites in the V3 loop of the viral envelope glycoprotein gp120. When polysulfates were administered intr avenously to rabbits, their half-life was approximately 2 h. Although they are very poorly absorbed following oral administration, they can be made orally bioavailable with the appropriate chemical modification s. Also, polysulfates may lose (much of) their anticoagulant activity upon chemical modification without giving up their anti-HIV activity. Their efficacy in the therapy and/or prophylaxis of retroviral infecti ons remains to be demonstrated both in animal models and in humans.