Effects of phenylated compounds of methylglyoxal bis(guanylhydrazone) on diamine oxidase activity from rat small intestine.
Two phenylated compounds of methylglyoxal bis(guanylhydrazone), potentially inhibitors of diamine oxidase activity, have been synthesized: phenylglyoxal bis(guanylhydrazone) and diphenylglyoxal bis(guanylhydrazone). Their inhibitory capacity was tested: while PGBG was able to reduce the enzyme activity by 50% at 1.3 microM, DPGBG was only able to reduce diamine oxidase activity by less than 2% at a concentration 1000-fold higher. The inhibition of PGBG was non-competitive and the Ki calculated by a Dixon plot was estimated as 1.7 microM.
Balaña-Fouce
R
R
Pulido
T G
TG
Escudero
D O
DO
Sanz-Sanchez
F
F
D006631:Amine Oxidase (Copper-Containing) / Q000037:antagonists & inhibitors*; D000818:Animals; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000201:enzymology*; D007700:Kinetics; D008935:Mitoguazone / Q000031:analogs & derivatives* / Q000494:pharmacology; D011506:Proteins / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
D011506:Proteins; C048255:propylglyoxal bis(guanylhydrazone); C049009:diphenylglyoxal bis(guanylhydrazone); D006631:Amine Oxidase (Copper-Containing); D008935:Mitoguazone