Activity of P536, a UDP-glucose analog, against Trypanosoma cruzi
P536, a UDP-glucose analog which was previously described as an antiviral agent, has a potent and selective activity against the intracellular and extracellular stages of Trypanosoma cruzi in vitro. It had a 50% inhibitory concentration of less than 5 micrograms/ml for T. cruzi extracellular cultured forms (epimastigote) and of 25 micrograms/ml for T. cruzi intracellular forms (amastigote) growing inside J774G8 macrophage-like cells. In contrast, the 50% inhibitory concentration was 100 micrograms/ml or greater for cultured mammalian cells and 180 micrograms/ml for the proliferation of mouse spleen lymphocytes. Furthermore, the addition of P536 (50 micrograms/ml) to T. cruzi-infected J774G8 cells cured the infected macrophages, making them able to grow and function normally. Studies on the mechanism of action of this drug indicated that it inhibited incorporation of (TVS)methionine, (TH)thymidine, (TH)mannose, ( UC)-N-acetylglucosamine, and (TH)uridine into macromolecules by T. cruzi epimastigotes, the last being the most sensitive.
- Research Organization:
- Universidad Autonoma, Madrid (Spain)
- OSTI ID:
- 6785421
- Journal Information:
- Antimicrob. Agents Chemother.; (United States), Vol. 32:9
- Country of Publication:
- United States
- Language:
- English
Similar Records
Trypanosoma cruzi cells undergo an alteration in protein N-glycosylation upon differentiation
A dominant negative form of inositol 1,4,5-trisphosphate receptor induces metacyclogenesis and increases mitochondrial density in Trypanosoma cruzi
Related Subjects
ANTI-INFECTIVE AGENTS
BIOLOGICAL EFFECTS
TRYPANOSOMA
VIABILITY
CARBON 14 COMPOUNDS
CULTURE MEDIA
GLUCOSAMINE
LYMPHOCYTES
MACROPHAGES
MANNOSE
METHIONINE
MICE
SPLEEN
SULFONES
SULFUR 35
THYMIDINE
TRACER TECHNIQUES
TRITIUM COMPOUNDS
URIDINE
ALDEHYDES
AMINES
AMINO ACIDS
ANIMAL CELLS
ANIMALS
AZINES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BODY
BODY FLUIDS
CARBOHYDRATES
CARBOXYLIC ACIDS
CONNECTIVE TISSUE CELLS
DAYS LIVING RADIOISOTOPES
DRUGS
EVEN-ODD NUCLEI
HETEROCYCLIC COMPOUNDS
HEXOSAMINES
HEXOSES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
LEUKOCYTES
LIGHT NUCLEI
LIPOTROPIC FACTORS
MAMMALS
MASTIGOPHORA
MATERIALS
MONOSACCHARIDES
NUCLEI
NUCLEOSIDES
NUCLEOTIDES
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
ORGANS
PARASITES
PHAGOCYTES
PYRIMIDINES
RADIOISOTOPES
RIBOSIDES
RODENTS
SACCHARIDES
SOMATIC CELLS
SULFUR ISOTOPES
URACILS
VERTEBRATES
550901* - Pathology- Tracer Techniques