Comparison of effects of green tea catechins on apicomplexan hexose transporters and mammalian orthologues

Autor: Elvira T. Derbyshire, Sanjeev Krishna, Ksenija Slavic, Henry M. Staines, Richard J. Naftalin
Rok vydání: 2009
Předmět:
Oocyte
Catechin
Xenopus laevis
chemistry.chemical_compound
0302 clinical medicine
PfHT
Plasmodium falciparum hexose transporter
Enzyme Inhibitors
PfHT
Mammals
chemistry.chemical_classification
Glucose Transporter Type 1
0303 health sciences
biology
Glucose Transporter Type 5
BboHT1
Babesia bovis hexose transporter 1
3. Good health
Biochemistry
Babesia bovis
3OMG
3-O-methyl-d-glucose
medicine.symptom
GLUT1/5
mammalian facilitative glucose transporter 1/5
Monosaccharide Transport Proteins
Short Communication
Plasmodium falciparum
Transport
03 medical and health sciences
medicine
Animals
Hexose
EC
(−)-epicatechin
GLUT1/5
EGCG
(−)-epigallocatechin-gallate
Molecular Biology
030304 developmental biology
Tea
Glucose transporter
Transporter
Molecular biology
Catechin binding
BboHT1
Glucose
chemistry
Mechanism of action
Oocytes
biology.protein
EGC
(−)-epigallocatechin
Parasitology
GLUT1
ECG
(−)-epicatechin-gallate
030217 neurology & neurosurgery
Zdroj: Molecular and Biochemical Parasitology
ISSN: 0166-6851
DOI: 10.1016/j.molbiopara.2009.06.008
Popis: Here we have investigated the inhibitory properties of green tea catechins on the Plasmodium falciparum hexose transporter (PfHT), the Babesia bovis hexose transporter 1 (BboHT1) and the mammalian facilitative glucose transporters, GLUT1 and GLUT5, expressed in Xenopus laevis oocytes. (-)-Epicatechin-gallate (ECG) and (-)-epigallocatechin-gallate (EGCG) inhibited D-glucose transport by GLUT1 and PfHT, and D-fructose transport by GLUT5, with apparent K(i) values between 45 and 117 microM. BboHT1 was more potently inhibited by the ungallated catechins (-)-epicatechin (EC) and (-)-epigallocatechin (EGC), with apparent K(i) values of 108 and 168 microM, respectively. Site-directed mutagenesis experiments provided little further support for previously reported models of catechin binding to hexose transporters. Furthermore, P. falciparum growth inhibition by catechins was not affected by the external D-glucose concentration. Our results provide new data on the inhibitory action of catechins against sugar transporters but were unable to elucidate the antimalarial mechanism of action of these agents.
Databáze: OpenAIRE
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