Geospallins A–C: New Thiodiketopiperazines with Inhibitory Activity against Angiotensin-Converting Enzyme from a Deep-Sea-Derived Fungus Geosmithia pallida FS140

Marine Drugs

Liang-Xi Wen¹  Qi-Bin Lin¹  Yu-Chan Chen²  Zhang-Hua Sun²  Hao-Hua Li²  Wei Ye²  Wei-Min Zhang²  Sai-Ni Li²  Jiangyong Gu³ 

[1] School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;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;The Second Institute of Clinical Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;

关键词: thiodiketopiperazines;    Geosmithia pallida;    deep-sea-derived fungus;   

DOI  :  10.3390/md16120464

来源: DOAJ

【 摘 要 】

Three new thiodiketopiperazines, geospallins A⁻C (1⁻3), together with nine known analogues (4⁻12), were isolated from the culture of the deep-sea sediment-derived fungus Geosmithia pallida FS140. Among them, geospallins A and B (1 and 2) 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 (1⁻3) showed inhibitory activity with IC₅₀ values of 29⁻35 µM.

【 授权许可】

Unknown