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02605 SULFATED POLYMERS TARGET HSV GLYCOPROTEIN B, PREVENT VIRAL BINDING, ENTRY, AND CELL-TO-CELL SPREAD AND MAY IMPACT MUCOSAL IMMUNITY Cheshenko, Natalia1 The observation that herpes simplex virus (HSV) and human immunodeficiency virus (HIV) bind heparan sulfate provided the rationale for development of sulfated or sulfonated polymers (SP) as topical agents. Although several have advanced to clinical trials, the mechanism of anti-viral activity and effects on soluble mediators of inflammation have not been evaluated. These studies address these gaps. Results indicate that PRO 2000, polystyrene sulfonate, cellulose sulfate, polymethylenehydroquinone sulfonate, and a mandelic acid condensation polymer designated SAMMA, which has no surfactant properties and does not contain sulfur, inhibit HSV infection 10,000 fold and are active against clinical isolates including an acyclovir resistant variant. The compounds form stable complexes with glycoprotein B and inhibit viral binding, entry, and cell-to-cell spread. The effects may be long lasting due to the high affinity and stability of the SP-viral complex, evidenced by surface plasmon resonance studies. The microbicides retain anti-viral activity in the presence of cervical secretions and over a broad pH range. There is little reduction in cell viability following repeated exposure of human endocervical cells to SP, although a reduction in secretory leukocyte protease inhibitor (SLPI) levels was observed. Prior to the initiation of large-scale clinical trials, rigorous evaluation of topical microbicides should include a thorough investigation of the changes in inflammatory cells, cytokines, and effects on host defenses following repeated application. Assistant Professor, Natalia Cheshenko, PhD |
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