Abstract
We previously demonstrated susceptibility of Leishmania sp. to glibenclamide, a K+-ATP transport blocker which interacts with members of the superfamily of adenosine 5′ triphosphate-binding cassette transporters. In order to characterize the molecular differences between a sensitive Leishmania strain, NR(Gs), and an experimentally selected glibenclamide-resistant strain, NR(Gr), specific biochemical and functional parameters have been evaluated both in the wild type and in the resistant strain. Most noteworthy, NR(Gr) exhibit an increased expression of P-glycoprotein and a decreased activity of functional key enzymes such as acid phosphatase, a prominent virulent factor of the parasite, and pyruvate kinase, a key control enzyme for both carbohydrate and protein metabolism. The specific biochemical, metabolic and functional changes observed in the resistant strain correlated with a reduced infectivity of stationary phase NR(Gr) in J774 macrophages and suggested a mechanism to overcome the effect of glibenclamide.
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Received: 21 January 2000 / Accepted: 1 March 2000
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García, N., Figarella, K., Mendoza-León, A. et al. Changes in the infectivity, pyruvate kinase activity, acid phosphatase activity and P-glycoprotein expression in glibenclamide-resistant Leishmania mexicana . Parasitol Res 86, 899–904 (2000). https://doi.org/10.1007/s004360000257
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DOI: https://doi.org/10.1007/s004360000257
- AbbreviationsABC transporters Adenosine 5′ triphosphate-binding cassette transporters
- CFTR Cystic fibrosis transmembrane conductance regulator
- FDP Fructose-2,6-diphosphate
- GLIB: Glibenclamide
- LDH Lactate dehydrogenase
- NR(Gs) Glibenclamide-sensitive Leishmania strain NR
- NR(Gr) Glibenclamide-resistant Leishmania strain NR
- PEP Phosphoenolpyruvate
- Pgp P-Glycoprotein
- SUR Sulfonylurea receptor