Okeaniazole A:具有抗利什曼病活性的海洋蓝藻 Okeania hirsuta 中的含噻唑环肽

IF 1.5 4区 化学 Q3 CHEMISTRY, ORGANIC Tetrahedron Letters Pub Date : 2024-08-30 DOI:10.1016/j.tetlet.2024.155284
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引用次数: 0

摘要

从冲绳海洋蓝藻 Okeania hirsuta 中分离出一种大环肽 Okeaniazole A (1)。质谱和核磁共振光谱分析阐明了其平面结构。氨基酸残基的绝对构型是通过臭氧分解、水解和马菲分析法综合确定的。Okeaniazole A (1) 和相关的环状七肽 dolastatin 3 (2) 具有抗利什曼病活性,IC50 值分别为 12.1 和 12.5 µM。这两种化合物在浓度为 100 µM 时对 L1210 小鼠白血病细胞没有任何细胞毒性。
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Okeaniazole A: Thiazole-containing cyclopeptide from the marine cyanobacterium Okeania hirsuta with antileishmanial activity

A macrocyclic peptide, okeaniazole A (1), was isolated from the Okinawan marine cyanobacterium, Okeania hirsuta. The planar structure was elucidated by the analyses of MS and NMR spectra. The absolute configuration of the amino acid residues was determined by a combination of ozonolysis, hydrolysis, and Marfey’s analysis. Okeaniazole A (1) and a related cyclic heptapeptide dolastatin 3 (2) exhibited antileishmanial activity, with IC50 values of 12.1 and 12.5 µM, respectively. These two compounds did not show any cytotoxicity toward L1210 mouse leukemia cells at concentrations of 100 µM.

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来源期刊
Tetrahedron Letters
Tetrahedron Letters 化学-有机化学
CiteScore
3.50
自引率
5.60%
发文量
521
审稿时长
28 days
期刊介绍: Tetrahedron Letters provides maximum dissemination of outstanding developments in organic chemistry. The journal is published weekly and covers developments in techniques, structures, methods and conclusions in experimental and theoretical organic chemistry. Rapid publication of timely and significant research results enables researchers from all over the world to transmit quickly their new contributions to large, international audiences.
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