Pharmaceutical Sciences Division, University of Wisconsin-Madison, 777 Highland Avenue, Madison, WI 53705, USA.
Mar Drugs. 2013 Dec 16;11(12):5089-99. doi: 10.3390/md11125089.
Two novel chlorinated pyrones, halomadurones A and B, and two novel brominated analogues, halomadurones C and D, were isolated from a marine Actinomadura sp. cultivated from the ascidian Ecteinascidia turbinata. Additionally, a non-halogenated analogue, 2-methyl-6-((E)-3-methyl-1,3-hexadiene)-γ-pyrone, was synthesized to understand the role of the halogens for activity. Halomadurones C and D demonstrated potent nuclear factor E2-related factor antioxidant response element (Nrf2-ARE) activation, which is an important therapeutic approach for treatment of neurodegenerative diseases.
两种新型的氯化吡喃酮类化合物,halomadurones A 和 B,以及两种新型的溴化类似物,halomadurones C 和 D,从一种海洋放线菌 Actinomadura sp. 中分离出来,该放线菌是从棘皮动物 Ecteinascidia turbinata 中培养出来的。此外,还合成了一种非卤代类似物,2-甲基-6-((E)-3-甲基-1,3-己二烯基)-γ-吡喃酮,以了解卤素对活性的作用。Halomadurones C 和 D 表现出强烈的核因子 E2 相关因子抗氧化反应元件 (Nrf2-ARE) 激活作用,这是治疗神经退行性疾病的重要治疗方法。