Abstract
Isopeptides (ε-peptides) of lysine, with a given Mw and low polydispersity (10–400 units), were synthesized to study the relationship between their chemical structure and biological effect. The designed compounds were of high purity, low polydispersity and high stereochemical purity. The effect of the compounds was tested on a human erythroleukemia cell line (K-562) and on four transplantable mouse tumors (L1210 lymphoid leukemia, P38 macrophage derived tumor, Ehrlich ascites carcinoma, Lewis lung tumor /LLT/). In case of the L1210 and P388 tumors and the Ehrlich carcinoma, survival of the animals was used as an indicator of the effect. In case of the Lewis lung tumor, the number and size of metastases in the lung and/or liver of treated and untreated mice were used as indicators. The polymers of polymerisation degree 80–120 (Mw 10.2–15.4 KD) showed the strongest antiproliferative effect both on K562 cells and the tumors growing in vivo. This effect was manifest with a significantly higher survival rate as compared to the control (L1210, P38, Ehrlich ascites), furthermore, by a decrease in the number and size of liver and lung metastases (LLT).
Highlights
Isopeptides (ε-peptides) of lysine, with a given Mw and low polydispersity (10–400 units), were synthesized to study the relationship between their chemical structure and biological effect
We found that the "backing off" activation method is highly applicable for preparing isopeptides and salts consisting of diamino carboxylic acids
Tumor cell number: 5 × 106 liver and lung metastases (LLT) cells inoculated into the spleen
Summary
Address: 11st Institute of Pathology and Experimental Cancer Research, Joint Research Organisation, Hungarian Academy of Sciences and Semmelweis University, H-1085. Üllõi út 26, Hungary, 2Department of Organic Chemistry, Lóránt Eötvös University, H-1518. 112, P.O. Box 32, Hungary and 3Research Institute of Plant Protection, Hungarian Academy of Sciences, H-1022.
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