Novel polyfunctional small amphiphilic peptide dendrimers characterized by incorporation of a new core compounds – tris-amino acids or tetrakis-amino alcohols that originated from a series of basic amino acids – were efficiently synthesized. These new core elements yielded molecules with multiple branching and (+5)/(+6) charge at the 1-st dendrimer generation. Dendrimers exhibited significant antimicrobial potency against Gram(+) and Gram(-) strains involving also multiresistant reference strains (S. aureus ATCC 43300 and E. coli ATCC BAA-198). In addition, high activity against fungi from the Candida genus was detected. More charged and more hydrophobic peptide dendrimers expressed hemolytic properties.
A series of new peptide dendrimers with amphiphilic surface, designed around a dendronized ornithine (Orn) core were synthesized and characterized by ESI-MS, 1 H-, 13 C-NMR, and CD spectrometry. An improved antimicrobial potency against S. aureus and E. coli was detected as a result of an increased charge, higher branching and variable lipophilicity of the residues located at the C-terminus. Minimal inhibitory concentration (MIC) values indicated that the selected dendrimers were not sensitive to the physiological concentration of Na
Antimicrobial drug resistance is a major human health threat. Among the many attempts to tackle this problem, the synthesis of antimicrobial compounds that mimic natural antimicrobial peptides appears as a promising approach. Peptide-based dendrimers can be designed to have higher potency than natural antimicrobial peptides and at the same time they can evade the bacterial defense system. Novel dendrimers with similar chemical structure but varying potency in terms of minimum inhibitory concentration were designed. The dependency between dendrimer structure and antibacterial activity as well as their capacity to attack model cell membranes was studied. The data suggests that supramolecular structure in terms of charge distribution and amphiphilicity, rather than net charge, is the main driver for disruption of cellular membranes and this correlates well with dendrimer hemolytic activity.
Synteza, metody identyfikacji i wybrane medyczne zastosowania dendrymerów Streszczenie-Na podstawie przegl¹du literatury przedstawiono aktualny stan wiedzy na temat otrzymywania dendrymerów, metod ich charakteryzowania i perspektyw zastosowania w medycynie tej nowej klasy zwi¹zków polimerycznych. S³owa kluczowe: dendrymery, synteza rozbie¿na, synteza zbie¿na, nooeniki substancji leczniczych, kuracja przeciwnowotworowa, oerodek kontrastuj¹cy w diagnostyce NMR. SYNTHESES, METHODS OF IDENTIFICATION AND SELECTED MEDICAL APPLICATIONS OF DENDRIMERS Summary-The present state of knowledge about the preparation, methods of characterization and the prospect of medical applications of dendrimers-a new class of polymeric compounds-is presented on the basis of literature review.
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