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海豹酰胺:一种从海洋蓝藻中分离出的抗锥虫脂肽。

Sealgamide: An Antitrypanosomal Lipopeptide Isolated from a Marine sp. Cyanobacterium.

作者信息

Wakai Kazuki, Kurisawa Naoaki, Umeda Kairi, Jeelani Ghulam, Agusta Adnan Luthfi, Nozaki Tomoyoshi, Suenaga Kiyotake

机构信息

Department of Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, Kanagawa 223-8522, Japan.

Department of Biomedical Chemistry, Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

J Nat Prod. 2025 Apr 25;88(4):1048-1056. doi: 10.1021/acs.jnatprod.5c00141. Epub 2025 Mar 31.

Abstract

Sealgamide (), a new antitrypanosomal lipopeptide, was isolated from a marine sp. cyanobacterium. Elucidation of its structure was challenging due to signal overlap caused by conspicuous rotamers but was ultimately achieved through partial hydrolysis and subsequent spectroscopic analyses. Sealgamide () exhibited moderate antitrypanosomal activity against (IC 2.9 μM) while showing no antimalarial activity (IC > 25 μM) or cytotoxicity (IC > 30 μM). Furthermore, we discovered that an artificial C-terminal methyl ester analogue () exhibited notably enhanced antiparasitic activity.

摘要

海豹酰胺()是一种新的抗锥虫脂肽,从一种海洋蓝藻中分离得到。由于显著的旋转异构体导致信号重叠,其结构解析具有挑战性,但最终通过部分水解和随后的光谱分析得以完成。海豹酰胺()对布氏锥虫表现出中等抗锥虫活性(IC 2.9 μM),而对疟原虫无抗疟活性(IC>25 μM),也无细胞毒性(IC>30 μM)。此外,我们发现一种人工合成的C端甲酯类似物()表现出显著增强的抗寄生虫活性。

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