Department of Phototrophic Microorganisms-ALGATECH, Institute of Microbiology, Academy of Science of the Czech Republic, Opatovický mlýn, 379 81 Třeboň (Czech Republic).
Chembiochem. 2013 Nov 25;14(17):2329-37. doi: 10.1002/cbic.201300246. Epub 2013 Oct 2.
Aeruginosin-865 (Aer-865), isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety, and is the first aeruginosin to be found in the genus Nostoc. Mass spectrometry, chemical and spectroscopic analysis as well as one- and two-dimensional NMR and chiral HPLC analysis of Marfey derivatives were applied to determine the peptidic sequence: D-Hpla, D-Leu, 5-OH-Choi, Agma, with hexanoic and mannopyranosyl uronic acid moieties linked to Choi. We used an AlphaLISA assay to measure the levels of proinflammatory mediators IL-8 and ICAM-1 in hTNF-α-stimulated HLMVECs. Aer-865 showed significant reduction of both: with EC50 values of (3.5±1.5) μg mL(-1) ((4.0±1.7) μM) and (50.0±13.4) μg mL(-1) ((57.8±15.5) μM), respectively. Confocal laser scanning microscopy revealed that the anti-inflammatory effect of Aer-865 was directly associated with inhibition of NF-κB translocation to the nucleus. Moreover, Aer-865 did not show any cytotoxic effect.
从陆生蓝细菌 Nostoc sp. Lukešová 30/93 中分离得到的 Aeruginosin-865 (Aer-865) 是第一个既含有脂肪酸又含有碳水化合物部分的 Aeruginosin 型肽，也是第一个在 Nostoc 属中发现的 Aeruginosin。质谱、化学和光谱分析以及一维和二维 NMR 和手性 HPLC 分析的马费衍生物用于确定肽序列：D-Hpla、D-Leu、5-OH-Choi、Agma，带有己酸和甘露吡喃糖醛酸部分与 Choi 相连。我们使用 AlphaLISA 测定法测量了 hTNF-α 刺激的 HLMVECs 中促炎介质 IL-8 和 ICAM-1 的水平。Aer-865 对两者均显示出显著的降低作用：EC50 值分别为（3.5±1.5）μg mL-1（（4.0±1.7）μM）和（50.0±13.4）μg mL-1（（57.8±15.5）μM）。共聚焦激光扫描显微镜显示，Aer-865 的抗炎作用与抑制 NF-κB 向细胞核易位直接相关。此外，Aer-865 没有表现出任何细胞毒性作用。
