DL-α-ヒドラチノカルボン酸類によるアミノ酸代謝系酵素類の活性阻害

概要

論文の詳細を見る
Sixteen kinds of DL-α-hydrazinocarboxylic acids were synthesized and their effect on the activity of enzymes related to amino acid metabolism was examined. These derivatives strongly inhibited the activity of diamine oxidase (substrate : histamine) and of amino acid decarboxylase (L-glutamic acid and 5-hydroxy-L-tryptophan). The inhibiting potency was dependent on the chain length of alkyl group in these derivatives. The maximum inhibition against the diamine oxidase activity was obtained with α-hydrazinocaprylic acid ; the I_<50> value was about 1.0×10^<-5>M. Inhibition of the diamine oxidase activity was non-competitive for substrate and prevented by preincubation with an α-keto acid, probably due to the formation of a non-inhibitory complex between the α-hydrazino group and keto group of the acid added. All of these α-hydrazinocarboxylic acids did not affect the activities of monoamine oxidase (butylamine, β-phenethylamine and tyramine), aminotransferase (aspartate : α-ketoglutarate) and D-amino acid oxidase (D-alanine). From comparison with known inhibitors of related structure, it is assumed that the inhibition with α-hydrazinocarboxylic acids is due mainly to the reactivity of hydrazino group and is affected by carboxyl group in their structure.
公益社団法人日本薬学会の論文
1971-10-25