title: In vitro susceptibility of fungi to acyclic inhibitors of 2,3-oxidosqualene cyclases.
abstract: In the present study we determine the antifungal properties of two acyclic inhibitors of 2,3-oxidosqualene cyclases: 22,23-epoxy-2-aza-2,3-dihydrosqualene (EAS) and azasqualene alcohol (ASA). Fungistatic and fungicidal activity towards dermatophytes and other fungi involved in cutaneous and systemic infections was tested (48 isolates from 10 species). The tests were carried out by inoculating 10 microliters of mycelial homogenate in 1 ml of Sabouraud glucose liquid medium containing serial dilutions of 100 to 0.25 micrograms ml-1 of the substance. For each isolate, the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) of both compounds were determined. EAS was more active (MIC range 1.5-25 micrograms ml-1) than ASA (MIC range 3-50 micrograms ml-1). At the highest concentration tested, EAS also showed fungicidal action towards some isolates of Trichophyton mentagrophytes, T. terrestre, Epidermophyton floccosum, Microsporum canis and Scopulariopsis brumptii. The most sensitive species was T. mentagrophytes, the most resistant T. rubrum.
authors.affiliation: Dipartimento di Biologia Vegetale, Università di Torino, Turin, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Airaudi
authors.forename: M
authors.initials: M
authors.lastname: Ceruti
authors.forename: C
authors.initials: C
authors.lastname: Bianco
authors.forename: V
authors.initials: V
authors.lastname: Filipello Marchisio
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D004821:Epidermophyton / Q000187:drug effects; D005658:Fungi / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D019751:Intramolecular Transferases; D007535:Isomerases / Q000037:antagonists & inhibitors*; D008826:Microbial Sensitivity Tests; D008864:Microsporum / Q000187:drug effects; D003904:Mitosporic Fungi / Q000187:drug effects; D013185:Squalene / Q000031:analogs & derivatives* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014249:Trichophyton / Q000187:drug effects
chemical_list: D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D013185:Squalene; D007535:Isomerases; D019751:Intramolecular Transferases; C021924:lanosterol synthase