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Castanospermine: a potent inhibitor of sucrase from the human enterocyte‐like cell line Caco‐2
Author(s) -
Trugnan Germain,
Rousset Monique,
Zweibaum Alain
Publication year - 1986
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(86)80123-5
Subject(s) - enterocyte , caco 2 , sucrase , chemistry , biochemistry , cell , enzyme , small intestine
The addition of castanospermine (5–50 μM) 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 (ED 50 at 4 nM after 1 h preincubation period) and of the fully non‐competitive type. The calculated K i (2.6 nM) suggests that castanospermine is the most potent inhibitor of sucrase so far reported.