Résumé
The biosynthetic pigment from Chromobacterium violaceum BB-78, 1,3-dihydro-2H-indol-2-one and its derivatives exhibit biological activities such as antimicrobial action, low hemolytic effects on red blood cells and in vitro trypanocide activity. A relatively high cytotoxicity on V-79 hamster fibroblast cells of the biosynthetic pigment was found, although with the methylol derivative the toxicity was almost eliminated. The methylol derivative exhibited similar toxicity as Nifurtimox, a known, commercial trypanocide compound
Sujets)
Animaux , Cricetinae , Antibactériens/toxicité , Chromobacterium/métabolisme , Hémolyse , Indoles/toxicité , Pigments biologiques/toxicité , Antibactériens/isolement et purification , Bactéries/effets des médicaments et des substances chimiques , Lignée cellulaire , Survie cellulaire/effets des médicaments et des substances chimiques , Chromobacterium/croissance et développement , Fibroblastes/effets des médicaments et des substances chimiques , Indoles/isolement et purification , Tests de sensibilité microbienne , Nifurtimox/toxicité , Pigments biologiques/isolement et purification , Trypanosoma cruzi/effets des médicaments et des substances chimiques , Trypanosoma cruzi/croissance et développementRésumé
It has been found that the pigment-I from Chromobacterium violaceum, 3 [1,2 dihydro 5 (5 hydroxy 1H indol 3 yl) 2 oxo 3H pyrrol-3 ylidiene] 1,3 dihydro 2H indol 2 one, has trypanocide activity. The formylated derivatives, pigment-III, immobilized 100% of the Trypanosoma cruzi at a level of 46 micronM after 48h of interaction with a total growth inhibition in the same period. Pigment I exhibited low toxicity and a DNA synthesis inhibition similar to that of Nifurtimox, a known trypanocide compound