title: Parameters of inhibition of HIV-1 infection by small anionic microbicides.
abstract: Sulfonated porphyrins and phthalocyanines have been shown to have anti-HIV activity and are under consideration as microbicides. Both categories of compounds are small negatively charged molecules and both were previously shown to inhibit cell fusion induced by the HIV Env protein and to block binding of gp120 to the CD4 receptor. In the present study we show that these compounds inhibit transmission of cell-associated HIV, inactivate a broad range of HIV-1 primary isolates and are active against DS polyanion-resistant virus. The compounds tested are active over a range of pH values, and possess no detectable activity against normal bacterial flora. These results support the conclusion that anionic tetrapyrroles are promising candidates as microbicides for HIV prevention.
authors.affiliation: Department of Microbiology and Immunology, Emory University, 1510 Clifton Road, Room 3001, Atlanta, GA 30322, USA.
authors.forename: Andrei N
authors.initials: AN
authors.lastname: Vzorov
authors.forename: Jadranka
authors.initials: J
authors.lastname: Bozja
authors.forename: Dabney W
authors.initials: DW
authors.lastname: Dixon
authors.forename: Luigi G
authors.initials: LG
authors.lastname: Marzilli
authors.forename: Richard W
authors.initials: RW
authors.lastname: Compans
mesh_terms: D000838:Anions / Q000737:chemistry / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000494:pharmacology*; D002460:Cell Line; D002478:Cells, Cultured; D005260:Female; D015658:HIV Infections; D015497:HIV-1 / Q000145:classification / Q000187:drug effects*; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D054833:Isoindoles; D007778:Lactobacillus / Q000187:drug effects; D008214:Lymphocytes / Q000821:virology; D008826:Microbial Sensitivity Tests / Q000379:methods; D011166:Porphyrins / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014621:Vagina / Q000382:microbiology
chemical_list: D000838:Anions; D019380:Anti-HIV Agents; D007211:Indoles; D054833:Isoindoles; D011166:Porphyrins; C013647:phthalocyanine