title: Anti-HIV-1 activity of sulfated amphotericin B in vitro.
abstract: To reduce the toxicity of amphotericin B methyl ester (AME), which shows some anti-HIV-1 activity, sulfated amphotericin B (SAB) was prepared from amphotericin B (AB), and its anti-HIV-1 activity was examined in vitro. SAB at concentration of 7.8 micrograms/ml completely suppressed the HIV-1-induced cytopathic effect in MT-4 cells, at 3.9 micrograms/ml inhibited the expression of HIV-1 antigen in peripheral blood mononuclear cells infected with freshly isolated HIV-1 and at 22 micrograms/ml completely suppressed formation of giant cells in cocultures of MOLT-4 with MOLT-4/HIV-1 cells. Reverse transcriptase activity was inhibited by SAB, but only at higher concentrations (0.2-1 mg/ml). Furthermore, the toxicity of SAB was lower than that of AME or AB, and SAB did not affect the proliferation of MT-4 cells at concentrations up to 0.5 mg/ml. The anti-coagulant effect of SAB was 10-fold less than that of dextran sulfate (MW = 8000). The anti-HIV-1 effect of SAB is attributed to inhibition of binding of virions to target cells.
authors.affiliation: Osaka Prefectural Institute of Public Health, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Otake
authors.forename: K
authors.initials: K
authors.lastname: Miyano
authors.forename: H
authors.initials: H
authors.lastname: Mori
authors.forename: M
authors.initials: M
authors.lastname: Morimoto
authors.forename: N
authors.initials: N
authors.lastname: Ueba
authors.forename: N
authors.initials: N
authors.lastname: Kunita
authors.forename: H
authors.initials: H
authors.lastname: Nakashima
authors.forename: T
authors.initials: T
authors.lastname: Kurimura
mesh_terms: D000666:Amphotericin B / Q000031:analogs & derivatives / Q000494:pharmacology*; D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D003588:Cytopathogenic Effect, Viral; D016264:Dextran Sulfate / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D051379:Mice; D013601:T-Lymphocytes; D014407:Tumor Cells, Cultured; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; C017501:methylamphotericin B; D000666:Amphotericin B; D016264:Dextran Sulfate