Giannopoulou Panagiota C, Missiri Dionissia A, Kournoutou Georgia G, Sazakli Eleni, Papadopoulos Georgios E, Papaioannou Dionissios, Dinos George P, Athanassopoulos Constantinos M, Kalpaxis Dimitrios L
Department of Biochemistry, School of Medicine, University of Patras, GR-26504 Patras, Greece.
Laboratory of Synthetic Organic Chemistry, Department of Chemistry, University of Patras, GR-26504 Patras, Greece.
Antibiotics (Basel). 2019 Jan 29;8(1):9. doi: 10.3390/antibiotics8010009.
Over the last years, we have been focused on chloramphenicol conjugates that combine in their structure chloramphenicol base with natural polyamines, spermine, spermidine and putrescine, and their modifications. Conjugate , with spermidine (SPD) as a natural polyamine linked to chloramphenicol base, showed the best antibacterial and anticancer properties. Using as a prototype, we here explored the influence of the antibacterial and anticancer activity of additional benzyl groups on N1 amino moiety together with modifications of the alkyl length of the aminobutyl fragment of SPD. Our data demonstrate that the novel modifications did not further improve the antibacterial activity of the prototype. However, one of the novel conjugates () showed anticancer activity without affecting bacterial growth, thus emerging as a promising anticancer agent, with no adverse effects on bacterial microflora when taken orally.
在过去几年里,我们一直专注于氯霉素共轭物,其结构将氯霉素碱与天然多胺、精胺、亚精胺和腐胺及其修饰相结合。以亚精胺(SPD)作为与氯霉素碱相连的天然多胺的共轭物表现出最佳的抗菌和抗癌特性。以[共轭物名称未给出]为原型,我们在此探索了N1氨基部分上额外苄基对抗菌和抗癌活性的影响以及SPD氨基丁基片段烷基长度的修饰。我们的数据表明,这些新修饰并未进一步提高原型的抗菌活性。然而,其中一种新型共轭物([共轭物名称未给出])显示出抗癌活性且不影响细菌生长,因此成为一种有前景的抗癌剂,口服时对细菌微生物群没有不良影响。