Spergualin: a new antitumour antibiotic.
Spergualin was isolated from the culture filtrate of Bacillus laterosporus as an antitumour substance. It had a unique structure and was shown to have chemotherapeutic effects on mouse transplantable leukaemias such as L-1210, P-388, P-815, C-1489, EL-4 and RL male 1. It was especially effective to L-1210 leukaemia and the leukaemia-bearing mice were even curable by the optimal dose of this drug. When the spergualin-treated cured mice were inoculated again by L-1210 cells, those leukaemic cells did not grow in the animals suggesting that specific immunity to L-1210 had been induced. In this induction of immunity cytotoxic T lymphocytes were suggested to be involved. Cytostatic effect of spergualin in cell culture was dependent on the content of amine oxidase in serum. In the study of structure-activity relationship, the 15-hydroxy group was found to be not necessary, while the spermidine moiety was essential for antitumour activity. 15-Deoxy derivative of spergualin was found to be more potent in antitumour activity.
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D055598:Chemical Phenomena; D002621:Chemistry; D006146:Guanidines / Q000494:pharmacology; D007939:Leukemia L1210 / Q000188:drug therapy* / Q000276:immunology; D051379:Mice; D000587:Oxidoreductases Acting on CH-NH Group Donors / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013602:T-Lymphocytes, Cytotoxic / Q000187:drug effects
D000903:Antibiotics, Antineoplastic; D006146:Guanidines; C033797:spergualin; D000587:Oxidoreductases Acting on CH-NH Group Donors