Section 2
Chapter 1,360

Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate

Ryder, N.S.; Frank, I.; Dupont, M.C.

Antimicrobial Agents and Chemotherapy 29(5): 858-860


ISSN/ISBN: 0066-4804
PMID: 3524433
DOI: 10.1128/aac.29.5.858
Accession: 001359343

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The thiocarbamate antimycotics tolnaftate and tolciclate blocked sterol biosynthesis in fungal cells and cell extracts, with accumulation of squalene. This point of action was confirmed by the direct inhibition of microsomal squalene epoxidase from Candida albicans. There was no inhibition of other steps in ergosterol biosynthesis. In whole Candida cells, ergosterol biosynthesis inhibition was not complete at drug concentrations up to 100 mg/litter, whereas full inhibition occurred in a cell-free test system. Rat liver cell-free cholesterol biosynthesis was much less sensitive to the drugs. The biochemical action of tolnaftate and tolciclate is thus similar to that of the allylamine antimycotics naftifine and terbinafine.

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