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In vitro and in vivo effects of 3-bromopyruvate against Echinococcus metacestodes
Qi Xin1, Miaomiao Yuan1,2, Huanping Li1
1Institute of Pathogenic Biology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
Abstract:
While searching for novel anti-echinococcosis drugs, we have been focusing on glycolysis which is relied on by Echinococcus for energy production and intermediates for other metabolic processes. The aim of this study was to investigate the potential therapeutic implication of glycolytic inhibitors on Echinococcus. Our results demonstrate that at an initial concentration of 40 μM, all inhibitors of glycolysis used in the current experiment [3-bromopyruvate (3-BrPA), ornidazole, clorsulon (CLS), sodium oxamate and 2,6-dihydroxynaphthalene (NA-P2)] show considerable in vitro effects against Echinococcus granulosus protoscoleces and Echinococcus multilocularis metacestodes. Among them, 3-BrPA exhibited the highest activity which was similar to that of nitazoxanide (NTZ) and more efficacious than albendazole (ABZ). The activity of 3-BrPA was dose dependent and resulted in severe ultrastructural destructions, as visualized by electron microscopy. An additional in vivo study in mice infected with E. multilocularis metacestodes indicates a reduction in parasite weight after the twice-weekly treatment of 25 mg/kg 3-BrPA for 6 weeks, compared to that of the untreated control. In particular, in contrast to ABZ, the administration of 25 mg/kg 3-BrPA did not cause toxicity to the liver and kidney in mice. Similarly, at the effective dose against Echinococcus larvae, 3-BrPA showed no significant toxicity to human hepatocytes. Taken together, the results suggest that interfering with the glycolysis of the parasite may be a novel chemotherapeutical option and 3-BrPA, which exhibited a remarkable activity against Echinococcus, may be a promising potential drug against cystic echinococcosis (CE) and alveolar echinococcosis (AE).
Insights
Targeting Echinococcus glycolysis with inhibitors shows promise. 3-bromopyruvate (3-BrPA) demonstrated significant efficacy against Echinococcus parasites in vitro and in vivo, with no observed liver or kidney toxicity in mice.
Area of Science:
- Parasitology
- Drug Discovery
- Biochemistry
Background:
- Echinococcosis is a parasitic disease requiring novel treatments.
- Glycolysis is essential for Echinococcus energy production and metabolic pathways.
Purpose of the Study:
- To investigate the therapeutic potential of glycolytic inhibitors against Echinococcus.
- To evaluate 3-bromopyruvate (3-BrPA) as a lead candidate drug.
Main Methods:
- In vitro screening of glycolysis inhibitors (3-BrPA, ornidazole, clorsulon, sodium oxamate, 2,6-dihydroxynaphthalene) against Echinococcus protoscoleces and metacestodes.
- In vivo efficacy and toxicity studies of 3-BrPA in mice infected with Echinococcus multilocularis.
- Assessment of 3-BrPA toxicity in human hepatocytes.
Main Results:
- All tested glycolytic inhibitors showed in vitro activity.
- 3-BrPA exhibited the highest efficacy, comparable to nitazoxanide and superior to albendazole.
- 3-BrPA treatment reduced parasite weight in vivo without causing liver or kidney toxicity in mice.
- 3-BrPA demonstrated no significant toxicity to human hepatocytes at effective doses.
Conclusions:
- Interfering with parasite glycolysis is a viable strategy for anti-echinococcosis drug development.
- 3-bromopyruvate is a promising candidate drug for treating cystic and alveolar echinococcosis due to its efficacy and safety profile.
