Anthelmintic activity of cytochrome P450 inhibitors miconazole and clotrimazole: in-vitro effect on the liver fluke Opisthorchis felineus

International Journal of Antimicrobial Agents
Viatcheslav A MordvinovMaria Y Pakharukova

Abstract

Discovery of drugs for the treatment of opisthorchiasis and schistosomiasis is a high priority. The basic metabolic cytochrome P450 (CYP) system in parasitic flatworms contains a single gene. CYP of the liver fluke Opisthorchis felineus, the causative agent of opisthorchiasis, is important for survival of the worm, so it may be a promising target for therapeutics against liver fluke infection. The aims of this study were: (i) to analyse in-vitro anthelmintic activity of various CYP inhibitors using standard motility and mortality assays against juvenile and adult O. felineus worms; and (ii) to characterize their anthelminthic effects. Azole inhibitors (ketoconazole, miconazole, triadimenol, clotrimazole and 4-phenyl imidazole) and other inhibitors of haem-containing enzymes (disulfiram, metyrapone, benzyl isothiocyanate, and ticlopidine) were tested. This study revealed that inhibitors of haem mono-oxygenase enzymes possess anthelmintic activity. The most effective anthelmintic agents against the newly excysted metacercariae (NEM) were the antifungal agents miconazole [concentration to reduce the response by 50% (IC50) 0.79 µM] and clotrimazole (IC50 1.25 µM), both approved by the US Food and Drug Administration. The activity o...Continue Reading

Citations

Jan 13, 2019·Parasites & Vectors·Maria Y PakharukovaViatcheslav A Mordvinov
Apr 25, 2018·European Journal of Drug Metabolism and Pharmacokinetics·Takaya UnoMitsutaka Takada
Dec 7, 2018·Molecular Diversity·Xuelian LiuZhaohai Qin
Mar 5, 2021·Vavilovskiĭ Zhurnal Genetiki I Selekt︠s︡ii·V A MordvinovM Y Pakharukova
Apr 4, 2021·Pathogens·Viatcheslav A MordvinovMaria Y Pakharukova
Aug 6, 2021·Journal of Basic Microbiology·Saraswathi NagarajShoba Narayan

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