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

Zhang-Hua Sun; Jiangyong Gu; Wei Ye; Liang-Xi Wen; Qi-Bin Lin; Sai-Ni Li; Yu-Chan Chen; Hao-Hua Li; Wei-Min Zhang

doi:10.3390/md16120464

Marine Drugs (Nov 2018)

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

Zhang-Hua Sun,
Jiangyong Gu,
Wei Ye,
Liang-Xi Wen,
Qi-Bin Lin,
Sai-Ni Li,
Yu-Chan Chen,
Hao-Hua Li,
Wei-Min Zhang

Affiliations

Zhang-Hua Sun: 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
Jiangyong Gu: The Second Institute of Clinical Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
Wei Ye: 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
Liang-Xi Wen: School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
Qi-Bin Lin: School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
Sai-Ni Li: 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
Yu-Chan Chen: 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
Hao-Hua Li: 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
Wei-Min Zhang: 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

DOI: https://doi.org/10.3390/md16120464
Journal volume & issue: Vol. 16, no. 12
p. 464

Abstract

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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.

Published in Marine Drugs

ISSN: 1660-3397 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Biology (General)
Website: http://www.mdpi.com/journal/marinedrugs

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