STRUCTURE DETERMINATION AND SYNTHESIS OF LYSINE ISOPEPTIDES INFLUENCING ON CELL-PROLIFERATION

The clavicepamines are lysine-rich basic proteins isolated from saprop hytic culture of ergot (Claviceps purpurea), having human pharmacologi cal importance. Based on structure determinations, it was demonstrated that the epsilon-lysine (poly)peptides are the fundamental structural units of clavicepamines. To study the relationship between chemical s tructure and biological effect, solution and solid-phase synthesis of lysine isopeptides were performed Poly-epsilon-lysines were synthesize d with polycondensation via application of p-nitrophenylester temporar ily protecting groups together with simultaneous activation. The biolo gical investigations of poly-epsilon-lysines showed a cell-proliferati on retarding effect, so they inhibit growth of some animal tumors, pra ctically without toxic side effects. (C) 1997 John Wiley & Sons, Inc.