Castanospermine: a potent inhibitor of sucrase from the human enterocyte‐like cell line Caco‐2

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Abstract
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 (ED50 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.