Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).target：α- and β-glucosidases.IC 50: 1.2 uM [2] in vitro :Castanospermine, [(1 S,6S,7R,8R,8aR)-1 ,6,7,8-tetrahydroxyoctahydroindolizine]is a potent and specific inhibitor of mammalian and plant α-and β-D-glucosidases in vitro [1] in vivo: Experiments in vivo with castanospermine, an inhibitor of the glucosidases that convert protein N-linked high mannose carbohydrates to complex oligosaccharides, resulted in significant inhibition of tumor growth in nude mice.[3]
References:
[1]. Bryan G, Anthony C et al. The structural basis of the inhibition of human glycosidases bycastanospermine analogues. Biochem. J. (1990) 269, 227-231.
[2]. Eisaku Tsujii et al. Nectrisine Is a Potent Inhibitor of a-Glucosidases, DemonstratingActivities Similarly at Enzyme and Cellular Levels. Biochemical and Biophysical Research Communications 220, 459-466 (1996)
[3]. Pili R et al. The alpha-glucosidase I inhibitor castanospermine alters endothelial cell glycosylation, preventsangiogenesis, and inhibits tumor growth. Cancer Res. 1995 Jul 1;55(13):2920-6.