Castanospermine: a potent inhibitor of sucrase from the human enterocyte-like cell line Caco-2.
The addition of castanospermine (5-50 microM) to a culture medium of Caco-2 cells results in a specific suppression of sucrase activity without modification of the biosynthesis of the enzyme. This effect is due to a direct inhibiting effect of castanospermine on Caco-2 sucrase activity. This inhibition is time-dependent (half-maximum efficiency at 10 min for 100 nM), enhanced by preincubation (suggesting a strong interaction with the enzyme), dose-dependent (ED50 at 4 nM after 1 h preincubation period) and of the fully non-competitive type. The calculated Ki (2.6 nM) suggests that castanospermine is the most potent inhibitor of sucrase so far reported.
Trugnan
G
G
Rousset
M
M
Zweibaum
A
A
D000470:Alkaloids / Q000494:pharmacology*; D000626:Aminopeptidases / Q000378:metabolism; D018826:CD13 Antigens; D002460:Cell Line; D018819:Dipeptidyl Peptidase 4; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / Q000378:metabolism; D006801:Humans; D007212:Indolizines; D007422:Intestines / Q000201:enzymology; D007700:Kinetics; D008871:Microvilli / Q000201:enzymology; D013393:Sucrase / Q000037:antagonists & inhibitors*; D054836:Indolizidines
D000470:Alkaloids; D000626:Aminopeptidases; D018826:CD13 Antigens; D018819:Dipeptidyl Peptidase 4; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases; D007212:Indolizines; D013393:Sucrase; C037806:castanospermine; D054836:Indolizidines