A powerful inhibitor of hexosaminidases.

Inhibitions of b-N-acetylglucosaminidases, enzymes which catalyse the hydrolysis of b-N-acetylglucosamine residues of lipid or protein-linked oligosaccharides, are potentially useful targets for cancer chemotherapy. b-N-acetylglucosaminidases may be associated with the invasiveness of certain tumors and high activity levels of these enzymes have been found in serum and urine of patients with various malignancies.

6-Acetamido-6-deoxycastanospermine was tested against a panel of glycosidases and was found to be a very potent inhibitor of b-N-acetylglucosaminidases from human placenta (IC50 = 0.5 m M), bovine kidney (IC50 = 1.5 m M), jack bean (IC50 = 1.6 m M), porcine placenta (IC50 = 0.4 m M) and bovine epididymis (IC50 = 0.7 m M).

Tett. Lett. 32, 6, 719-720.