Membrane perturbations induced by new analogs of neocryptolepine.

摘要: Indoloquinoline alkaloids represent an important class of antimalarial, antibacterial and antiviral compounds. Indolo[2,3-b]quinolines are a family DNA intercalators inhibitors topoisomerase II, synthetic analogs neocryptolepine, alkaloid traditionally used in African folk medicine. These cytotoxic substances promising anticancer agents. Active representatives indolo[2,3-b]quinolines affect model natural membranes. The distinct structure hydrophobicity the compounds leads to marked differences disturbing effects on membrane organization function. Our results also indicated strong relationship between presence chain Poct molecule as well capacity for incorporation into carboxyfluorescein-trapped liposomes 0.02-0.06 mM range. Moreover, correlation binding neutral dimyristoylphosphatidylcholine (DMPC) or negative charged dimyristoylphosphatidylcholine:dimyristoylphosphatidylglycerol (DMPC:DMPG, 9:1 w/w) liposomes, erythrocyte ghosts pKa, was found. All cause hemolysis isotonic conditions with concentration causing 50% (HC50) 0.12-0.88 mM concentration-dependent inhibitory effect tested agents ghosts' acetylcholinesterase activity studied.