地海绵素 A⁻C：一种新型硫代二酮哌嗪类化合物，对来源于深海真菌 FS140 的血管紧张素转化酶具有抑制活性。
Geospallins A⁻C: New Thiodiketopiperazines with Inhibitory Activity against Angiotensin-Converting Enzyme from a Deep-Sea-Derived Fungus FS140.
机构信息
State Key Laboratory of Applied Microbiology Southern China, Guangdong Provincial Key Laboratory of Microbial Culture Collection and Application, Guangdong Open Laboratory of Applied Microbiology, Guangdong Institute of Microbiology, Guangzhou 510070, China.
Guangdong Provincial Key Laboratory of New Drug, Development and Research of Chinese Medicine, Mathematical Engineering Academy of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
出版信息
Mar Drugs. 2018 Nov 23;16(12):464. doi: 10.3390/md16120464.
Three new thiodiketopiperazines, geospallins A⁻C (⁻), together with nine known analogues (⁻), were isolated from the culture of the deep-sea sediment-derived fungus FS140. Among them, geospallins A and B ( and ) represent rare examples of thiodiketopiperazines featuring an S-methyl group at C-10 and a tertiary hydroxyl group at C-11. Their structures were determined by high-resolution electrospray mass spectrometry (HRESIMS), spectroscopic analyses, and electronic circular dichroism (ECD) calculations. Their angiotensin-converting enzyme (ACE) inhibitory activity was reported, and geospallins A⁻C (⁻) showed inhibitory activity with IC values of 29⁻35 µM.
从深海沉积物来源的真菌 FS140 的培养物中分离得到三个新的硫代二酮哌嗪化合物，即 geospallins A⁻C（⁻），以及九个已知类似物（⁻）。其中，geospallins A 和 B（ 和 ）代表了具有 C-10 位 S-甲基和 C-11 位叔羟基的硫代二酮哌嗪的罕见实例。它们的结构通过高分辨电喷雾质谱（HRESIMS）、光谱分析和电子圆二色性（ECD）计算确定。报道了它们的血管紧张素转化酶（ACE）抑制活性，geospallins A⁻C（⁻）表现出抑制活性，IC 值为 29⁻35 µM。
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