Modular Strategies for Structure and Function Employed by Marine Cyanobacteria: Characterization and Synthesis of Pitinoic Acids

Modular Strategies for Structure and Function Employed by Marine Cyanobacteria: Characterization and Synthesis of Pitinoic Acids
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DOI:
10.1021/ol401396u
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发表时间:
2013-08-16
期刊:
影响因子:
5.2
通讯作者:
Luesch, Hendrik
Luesch, Hendrik
中科院分区:
化学1区
文献类型:
--
作者:
Montaser, Rana;Paul, Valerie J.;Luesch, Hendrik

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从一种关岛蓝细菌中鉴定出新型生物活性脂质,铜绿假单胞菌群体感应抑制剂匹亚酸A(1)和抗炎匹亚酸B(2)和C。通过合成确认了2的结构,这也允许进行生物学评价。由于2是匹亚酸A和C的酯,因此它代表了释放双重生物活性用于管理铜绿假单胞菌感染及其相关炎症的前药策略。
Novel bioactive lipids were identified from a Guamanian cyanobacterium, the Pseudomonas aeruginosa quorum sensing inhibitor pitinoic acid A (1) and the anti-inflammatory pitinoic acids B (2) and C. The structure of 2 was confirmed by synthesis, which also allowed for biological evaluation. Since 2 is an ester of pitinoic acids A and C, it represents a prodrug strategy to liberate dual biological activity for the management of P. aeruginosa infections and their associated inflammation.