Synthesis, conformation and cytotoxicity of new, branched polymeric polypeptides containing hydrophobic amino acid or arginine moiety
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- 作者：Mónika Sebestyén ; Rita Szabó ; László Kőhidai ; Éva Pállinger…
- 关键词：polylysine based polypeptides ; hydrophobic side chain ; solution conformation ; in vitro cytotoxicity
- 刊名：Structural Chemistry
- 出版年：2017
- 出版时间：April 2017
- 年：2017
- 卷：28
- 期：2
- 页码：527-535
- 全文大小：
- 刊物类别：Chemistry and Materials Science
- 刊物主题：Computer Applications in Chemistry; Physical Chemistry; Theoretical and Computational Chemistry;
- 出版者：Springer US
- ISSN：1572-9001
- 卷排序：28
文摘
In this paper we report on the synthesis and solution conformation of a new set of structurally related polycationic branched chain polypeptides (poly[Lys(Xi-dl-Alam)]) with hydrophobic (Ile, Nle, Val) or cationic (Arg) amino acids at the N-terminal end of the side chains as well as their cytotoxic effect on murine bone marrow derived macrophages. Solution conformation of the polypeptides was studied with circular dichroism spectroscopy under different conditions (pH, ionic strength). The results of these comparative studies indicate that a) polypeptides could adopt an ordered (mainly helical) conformation at physiological pH and salt concentration (pH 7.4, 0.2 M NaCl); b) the nature of side chain terminal amino acid (X) could determine under which conditions the ordered structure was formed. Thus, the solution conformation of branched polypeptides could be modulated by the selection of amino acid X under physiological conditions. All polypeptides with hydrophobic amino acid at the terminal position were essentially non-toxic on macrophages, whereas the polypeptide with terminal Arg proved to be markedly cytotoxic.