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Keywords:

  • Dermatophytes;
  • squalenoid derivatives;
  • fungitoxicity;
  • sterol biosynthesis

Summary. We report a preliminary study of the in vitro anti-dermatophyte activity of six squalenoid derivatives that inhibit 2,3-oxidosqualene cyclase and squaiene epoxidase: 2-aza-2.3-dihydrosqua-lene, 22,23–epoxy-2–aza-2,3–dihydrosqualene. azasqualene alcohol, 19–aza-18.19.22,23-tetra-hydrosqualene, 2,3–epoxy-19–aza-18,19,22.23–tetrahydrosqualene and hexafluorosqualene epoxide. The tests were done by inoculating 10μl of Trichophyton mentagrophytes (Robin) Blanchard or Microsporum canis Bodin homogenate into 1 ml of Sabouraud glucose liquid medium containing serial dilutions from 100 to 0.25 μg ml-1 of the substance. For each compound the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) were determined. The most effective compounds were 22,23–epoxy-2–aza-2,3–dihydrosqualene and azasqualene alcohol, with MICs respectively of 3 and 6.25 μg ml-1 for each of the two species of dermatophyte. The first of these compounds was the only one to show fungicidal activity over the range of concentrations tested.

Zusammenfassung. Wir berichten über eine vorläufige Studie zur Anti-Dermatophyten-Aktivität von sechs Squalenoidderivaten in vitro. die die 2.3–Oxidosqualen-Cyclase und die Squa-len-Epoxidase hemmen: 2–Aza-2.3–Dihydrosqualen, 22.23 Epoxy-2–Aza-2.3-Dihydresqualen. Azasqualen Alkohol. 19–Aza-18, 19.22,23–Tetra-hydrosqualen und Hexafluorosqualen-Epoxid. Fü jede Verbindung wurde die minimale Hemmkon-zentration (MIC) und die minimale fungizide Konzentration (MFC) für Trichophyton mentagrophytes und Microsporum canis bestimmt. Die wirksamsten Verbindungen waren 22,23–Epoxy-2–Aza-2.3–Dihydrosqualen und Azasqualen-Alkohol. mit MICs von 3 bzw. 6.25 μg ml-1 für jede der beiden Dermatophytenarten. Die erste dieser Verbindungen war die einzige, die fungizide Aktivität innerhalb der getesteten Konzentrationen zeigte.