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Isolation and inhibitory activity of gabaculine, a new potent inhibitor of γ‐aminobutyrate aminotransferase produced by a Streptomyces
Author(s) -
Kobayashi Kazuo,
Miyazawa Shigeru,
Endo Akira
Publication year - 1977
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(77)80153-1
Subject(s) - fermentation , library science , chemistry , biochemistry , computer science
It is well known that GABA plays an inhibitory role in crustacean ans mammalian central nervous system [ 1,2]. Since GABA does not cross the blood-brain barrier, various inhibitors of GABA aminotransferase which cause an increase in its cerebral level have been introduced into this field of research [3-121. Most of these inhibitors are very toxic and not specific for GABA aminotransferase. During our search for new inhibitors of GABA aminotransferase from microbial origin, a potent inhibitor (designated as gabaculine) was found to be present in the culture of a Streptomyces. The present paper describes isolation and inhibitory activity of gabaculine. The results indicate that this new microbial metabolite is a potent, competitive inhibitor of GABA aminotransferase from both beef brain and Pseudomonas ovalis, having Ki values of 0.37-0.80 PM. The physicochemical properties and identification of chemical structure of gabaculine have been reported elsewhere [13].