Kozupeptins, Antimalarial Agents Produced by Paracamarosporium Species: Isolation, Structural Elucidation, Total Synthesis, and Bioactivity
Kozupeptins, Antimalarial Agents Produced by Paracamarosporium Species: Isolation, Structural Elucidation, Total Synthesis, and Bioactivity
复制标题
DOI：
10.1021/acs.orglett.9b00483
复制
发表时间：
2019-04-05
期刊：
影响因子：
5.2
通讯作者：
Sunazuka, Toshiaki
中科院分区：
文献类型：
--
作者：
Hayashi, Yumi;Fukasawa, Wataru;Sunazuka, Toshiaki
从副霉菌(Paracamarosporium sp.)发酵液中分离得到两种新的抗疟脂多肽--KozuPeptins A和KozuPeptins B。FKI-7019。它们在体外对氯喹敏感和耐药的恶性疟原虫菌株显示出很强的抗疟疾活性。通过光谱分析和化学方法相结合的方法完成了结构的阐明，包括全合成了KozuPeptin A。合成的KozuPeptin A在体内显示了治疗效果，并且一种中间体显示出比KozuPeptin A更高的抗疟疾活性。
Kozupeptins A and B, novel antimalarial lipopeptides, were isolated from the culture broths of Paracamarosporium sp. FKI-7019. They exhibited potent antimalarial activity against chloroquine-sensitive and -resistant Plasmodium falciparum strains in vitro. The structural elucidation was accomplished by a combination of spectroscopic analyses and chemical approaches including a total synthesis of kozupeptin A. Synthetic kozupeptin A demonstrated a therapeutic effect in vivo, and an intermediate exhibited much higher antimalarial activity than kozupeptin A.