A glyoxalase I inhibitor of a new structural type produced by Streptomyces.
Many streptomyces strains produced an inhibitor of crude glyoxalase prepared from rat liver which did not inhibit glyoxalase I prepared from yeast. Another inhibitor, C11H14O6, which inhibited glyoxalases prepared from both rat liver and yeast was obtained from a cultured broth of Streptomyces griseosproeus and crystallized. Preincubation of this inhibitor with reuduced glutathione increased its inhibitory activity, which suggested its reaction with reduced glutathione. It showed a strong inhibition of growth of HeLa cells and inhibition of Ehrlich ascites carcinoma by daily injection. It also showed weak inhibition of the solid type of Ehrlich carcinoma and prolonged the survival period of mice inoculated with L-1210 cells.
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000302:isolation & purification* / Q000494:pharmacology / Q000627:therapeutic use; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D055598:Chemical Phenomena; D002621:Chemistry; D005978:Glutathione / Q000494:pharmacology; D006367:HeLa Cells / Q000187:drug effects; D007791:Lactoylglutathione Lyase / Q000037:antagonists & inhibitors*; D007928:Lethal Dose 50; D007939:Leukemia L1210 / Q000188:drug therapy; D008099:Liver / Q000201:enzymology; D008190:Lyases / Q000037:antagonists & inhibitors*; D051381:Rats; D012441:Saccharomyces cerevisiae / Q000201:enzymology; D013302:Streptomyces / Q000378:metabolism*
D000903:Antibiotics, Antineoplastic; D008190:Lyases; D007791:Lactoylglutathione Lyase; D005978:Glutathione