PMID: 7188Jun 1, 1976

Mechanism of action of miconazole: labilization of rat liver lysosomes in vitro by miconazole

Antimicrobial Agents and Chemotherapy
K H SwamyG R Rao

Abstract

Miconazole, a potent antifungal agent, labilizes rat liver lysosomes. Its labilizing effect is followed by measuring the release of lysosomal hydrolases, namely, acid phosphatase, beta-glucuronidase, and arylsulfatase A. The effect of miconazole is concentration dependent in the range of 10(-5) to 1.2 x 10(-4) M. However, at higher concentrations, miconazole inhibits enzyme release but does not inhibit enzyme activities per se. The effect of miconazole depends on the drug/lysosome ratio and is influenced by the pH of the incubation media, being minimal at alkaline pH. Membrane-active drugs such as nystatin, 2-phenethyl-alcohol, hexachlorophene, and digitonin have been compared with miconazole for their lysosome-labilizing action. The effect of miconazole on the lysosomal membrane is confirmed by a decrease in turbidity of the lysosomal suspension.

References

May 1, 1975·Antimicrobial Agents and Chemotherapy·S De Nollin, M Borgers
Feb 1, 1974·Chemico-biological Interactions·T R Corner
Jul 1, 1974·Biochemical Pharmacology·G Flores, D R Buhler
Jan 1, 1972·Chemotherapy·J M Van Cutsem, D C Thienpont
Sep 1, 1969·Journal of Medicinal Chemistry·E F GodefroiP A Janssen
Oct 1, 1970·Archives of Dermatology·J P BrugmansD C Thienpont
Jun 1, 1967·Biochemical Pharmacology·G WeissmannV A Bevans

Citations

Feb 1, 1988·Journal of Medical and Veterinary Mycology : Bi-monthly Publication of the International Society for Human and Animal Mycology·R D Cannon, D Kerridge
Jun 1, 1982·Antimicrobial Agents and Chemotherapy·J UnoT Arai
Jan 1, 1992·Diagnostic Microbiology and Infectious Disease·D W DenningD A Stevens
Sep 1, 1989·Clinical and Experimental Dermatology·J Mesquita-GuimarãesM R Carvalho
May 1, 1994·Journal of the American Academy of Dermatology·A K GuptaN H Shear

Related Concepts

Acid Phosphatase
Hydrogen-Ion Concentration
Imidazoles
Liver
Lysosomes
Brentan
Turbidimetry
August Rats

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