Abstract: A novel actinonin derivative and a salt thereof are provided, which are useful as enzyme inhibitors and particularly have strong inhibitory activities against enkephalinase and angiotensin-converting enzymes. This actinonin derivative is represented by general formula (I): ##STR1## wherein R.sup.1 is sulfoxymethyl or carboxyl or a substituted carboxyl group selected from carboxamide, hydroxyaminocarbonyl and alkoxycarbonyl groups; and R.sup.2 is hydroxyl, alkoxy, hydroxyamino or sulfoxyamino group.
Abstract: Actinonin or a salt thereof is active as an inhibitor of angiogenesis in a mammal and is useful as a therapeutic agent for inhibiting angiogenesis in a mammal having diabetic retinopathy or inflammatory response accompanied by angiogenesis.