2,2-diphenyl-1-picrylhydrazyl hydrate, a stable free radical, is an α-glycosidase inhibitor

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Title
2,2-diphenyl-1-picrylhydrazyl hydrate, a stable free radical, is an α-glycosidase inhibitor
Author(s)
Dong Sun Lee; Nam Soon Kim; Sang Han Lee
Bibliographic Citation
Biological & Pharmaceutical Bulletin, vol. 24, no. 6, pp. 727-728
Publication Year
2001
Abstract
Glycosidases play a pivotal role in processing of various glycoproteins and glycolipids. It is well known that glycosidases are also involved in a variety of degenerative metabolic disorders such as cancer and AIDS. In order to develop potent α-glucosidase inhibitors, we first screened 2,2-diphenyl-1-picrylhydrazyl hydrate as a candidate. 2,2-Diphenyl-1-picrylhydrazyl hydrate was found to inhibit α- and β-glucosidases as well as α- and β-mannosidases. It was also shown to be a non-competitive inhibitor of yeast α-glucosidase with a Ki value of 1.1×10-6 M. Taken together, we anticipate that 2,2-diphenyl-1-picrylhydrazyl hydrate may be a potent inhibitor for some incurable metabolic disorders including AIDS.
Keyword
2,2-diphenyl-1-picrylhydrazyl hydrateα-glucosidase inhibitorenzyme kineticsnon-competitive inhibition
ISSN
0918-6158
Publisher
Pharmaceutical Soc Japan
DOI
http://dx.doi.org/10.1248/bpb.24.727
Type
Article
Appears in Collections:
Division of Biomedical Research > Rare Disease Research Center > 1. Journal Articles
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