Department of Medicinal Chemistry and Technology, Universita degli Studi di Palermo, Palermo, Italy.
Biofouling. 2010;26(4):433-8. doi: 10.1080/08927011003718673.
With the goal of discovering new anti-infective agents active against microbial biofilms, this investigation focused on some natural pyrrolomycins, a family of halogenated pyrrole antibiotics. In this study the anti-staphylococcal biofilm activity of pyrrolomycins C, D, F1, F2a, F2b, F3 and of the synthesized related compounds I, II, III were investigated. The susceptibility of six staphylococcal biofilms was determined by methyltiazotetrazolium staining. Most of the compounds were active at concentrations of 1.5 microg ml(-1) with significant inhibition percentages. A few of the compounds were active at the lowest screening concentration of 0.045 microg ml(-1). The population log reduction of activity against the two best biofilm forming Staphylococcus aureus strains as determined by viable plate counts is also reported. In order to adequately assess the utility of these compounds, their toxicity against human cells was evaluated. It is concluded that pyrrolomycins and synthetic derivatives are promising compounds for developing novel effective chemical countermeasures against staphylococcal biofilms.
为了发现对抗微生物生物膜有活性的新型抗感染药物,本研究集中研究了一些天然吡咯霉素,这是一类卤化吡咯抗生素。本研究测定了吡咯霉素 C、D、F1、F2a、F2b、F3 以及合成的相关化合物 I、II、III 的抗葡萄球菌生物膜活性。采用甲臜比色法测定了 6 种葡萄球菌生物膜的敏感性。大多数化合物在 1.5 µg/ml 的浓度下具有显著的抑制百分比,有少数几种化合物在最低筛选浓度 0.045 µg/ml 下具有活性。通过活菌平板计数法测定了对两种最佳成膜的金黄色葡萄球菌菌株的活性的群体对数减少,也报告了这一结果。为了充分评估这些化合物的实用性,评估了它们对人细胞的毒性。结论是,吡咯霉素和合成衍生物是开发针对葡萄球菌生物膜的新型有效化学对抗措施的有前途的化合物。