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Review
. 2001 Jan;14(1):150-64.
doi: 10.1128/CMR.14.1.150-164.2001.

Drug targets and mechanisms of resistance in the anaerobic protozoa

Affiliations
Review

Drug targets and mechanisms of resistance in the anaerobic protozoa

P Upcroft et al. Clin Microbiol Rev. 2001 Jan.

Abstract

The anaerobic protozoa Giardia duodenalis, Trichomonas vaginalis, and Entamoeba histolytica infect up to a billion people each year. G. duodenalis and E. histolytica are primarily pathogens of the intestinal tract, although E. histolytica can form abscesses and invade other organs, where it can be fatal if left untreated. T. vaginalis infection is a sexually transmitted infection causing vaginitis and acute inflammatory disease of the genital mucosa. T. vaginalis has also been reported in the urinary tract, fallopian tubes, and pelvis and can cause pneumonia, bronchitis, and oral lesions. Respiratory infections can be acquired perinatally. T. vaginalis infections have been associated with preterm delivery, low birth weight, and increased mortality as well as predisposing to human immunodeficiency virus infection, AIDS, and cervical cancer. All three organisms lack mitochondria and are susceptible to the nitroimidazole metronidazole because of similar low-redox-potential anaerobic metabolic pathways. Resistance to metronidazole and other drugs has been observed clinically and in the laboratory. Laboratory studies have identified the enzyme that activates metronidazole, pyruvate:ferredoxin oxidoreductase, to its nitroso form and distinct mechanisms of decreasing drug susceptibility that are induced in each organism. Although the nitroimidazoles have been the drug family of choice for treating the anaerobic protozoa, G. duodenalis is less susceptible to other antiparasitic drugs, such as furazolidone, albendazole, and quinacrine. Resistance has been demonstrated for each agent, and the mechanism of resistance has been investigated. Metronidazole resistance in T. vaginalis is well documented, and the principal mechanisms have been defined. Bypass metabolism, such as alternative oxidoreductases, have been discovered in both organisms. Aerobic versus anaerobic resistance in T. vaginalis is discussed. Mechanisms of metronidazole resistance in E. histolytica have recently been investigated using laboratory-induced resistant isolates. Instead of downregulation of the pyruvate:ferredoxin oxidoreductase and ferredoxin pathway as seen in G. duodenalis and T. vaginalis, E. histolytica induces oxidative stress mechanisms, including superoxide dismutase and peroxiredoxin. The review examines the value of investigating both clinical and laboratory-induced syngeneic drug-resistant isolates and dissection of the complementary data obtained. Comparison of resistance mechanisms in anaerobic bacteria and the parasitic protozoa is discussed as well as the value of studies of the epidemiology of resistance.

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Figures

FIG. 1
FIG. 1
Structures of the drugs commonly used against the anaerobic protozoa. Structures are redrawn from the Merck Index except for nitazoxanide, which was redrawn for direct comparison with the nitroimidazoles, nitrofurans, and benzimidazoles (166).
FIG. 2
FIG. 2
Proposed fundamental metabolism of the anaerobic protozoa, with PFOR replacing the pyruvate dehydrogenase of aerobic organisms. Electrons derived from oxidative decarboxylation of pyruvate (catalyzed by PFOR) are transferred to ferredoxin (oxidized [ox]), which subsequently donates electrons to NAD(P)+ (catalyzed by putative ferredoxin:NAD oxidoreductase), regenerating intracellular pools of NAD(P)H and oxidized ferredoxin. In the process of ferredoxin reduction, acetyl-CoA is generated from pyruvate and reduced CoA (CoASH). Alternatively, ferredoxin has a sufficiently low redox potential to reduce (activate) metronidazole (R-NO2) to its toxic nitroradical RNO2· via reduced (red) ferredoxin (194, 196). NADH oxidase then serves as the terminal oxidase in the transfer of electrons to O2, producing H2O. NADH oxidase also has the potential to reduce furazolidone to its toxic nitro radical. Adapted from Giardia data in references to . The PFOR reaction occurs in the hydrogenosome in T. vaginalis. There are likely to be other coupled reactions, including alternative oxidoreductases, ferredoxins, and flavodoxins (22, 25, 117, 194, 216).

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