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

FEBS Letters

Trugnan, Germain¹  Zweibaum, Alain¹  Rousset, Monique¹ 

[1] Unité de Recherches sur le Métabolisme et la Différenciation de Cellules en Culture, INSERM U 178, Bâtiment INSERM, 16 avenue Paul-Vaillant Couturier, 94807 Villejuif Cédex, France

关键词: Castanospermine Sucrase Protein glycosylation Enzyme inhibition Cell differentiation (Human colon cancer cells);   

DOI  :  10.1016/0014-5793(86)80123-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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.

【 授权许可】

Unknown