来自海绵Aaptos lobata的两性亲和聚胺α-突触核蛋白聚集抑制剂。
Amphiphilic Polyamine α-Synuclein Aggregation Inhibitors from the Sponge Aaptos lobata.
发表日期:2023 Feb 16
作者:
Tanja M Voser, Joshua B Hayton, Dale W Prebble, Ju Jin, Gary Grant, Merrick G Ekins, Anthony R Carroll
来源:
JOURNAL OF NATURAL PRODUCTS
摘要:
对海绵Aaptos lobata的生物测定引导探索导致分离和确认两个新的疏水性多胺,aaptolobamine A(1)和B(2)。通过NMR和MS数据分析确定了它们的结构。 MS分析还表明A. lobata含有复杂的aaptolobamine同系物混合物。 aaptolobamine A(1)和B(2)均表现出广泛的生物活性,包括对癌细胞系的细胞毒性,对耐甲氧西林的金黄色葡萄球菌的中等抗菌活性,以及对铜绿假单胞菌菌株的微弱活性。 aaptolobamine同系物混合物表明含有与帕金森病相关的β淀粉样蛋白α-突触核蛋白结合并抑制其聚集的化合物。
Bioassay-guided investigation of the sponge Aaptos lobata resulted in the isolation and identification of two new amphiphilic polyamines, aaptolobamines A (1) and B (2). Their structures were determined through analysis of NMR and MS data. MS analysis also indicated that A. lobata contained a complex mixture of aaptolobamine homologues. Both aaptolobamines A (1) and B (2) show broad bioactivity, including cytotoxicity against cancer cell lines, moderate antimicrobial activity against a methicillin-resistant strain of Staphylococcus aureus, and weak activity against a Pseudomonas aeruginosa strain. The mixtures of aaptolobamine homologues were shown to contain compounds that bind to the Parkinson's disease associated amyloid protein α-synuclein and inhibit its aggregation.