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Geospallins A–C: New Thiodiketopiperazines with Inhibitory Activity against Angiotensin-Converting Enzyme from a Deep-Sea-Derived Fungus Geosmithia pallida FS140
- Source :
- Marine Drugs, Vol 16, Iss 12, p 464 (2018)
- Publication Year :
- 2018
- Publisher :
- MDPI AG, 2018.
-
Abstract
- 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.
- Subjects :
- Circular dichroism
Stereochemistry
Electrospray mass spectrometry
Pharmaceutical Science
Fungus
Inhibitory postsynaptic potential
01 natural sciences
Geosmithia pallida
deep-sea-derived fungus
Drug Discovery
Ic50 values
lcsh:QH301-705.5
Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
chemistry.chemical_classification
biology
010405 organic chemistry
Chemistry
Angiotensin-converting enzyme
biology.organism_classification
0104 chemical sciences
010404 medicinal & biomolecular chemistry
Enzyme
lcsh:Biology (General)
biology.protein
thiodiketopiperazines
Subjects
Details
- ISSN :
- 16603397
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Marine Drugs
- Accession number :
- edsair.doi.dedup.....dd8f83f31435a91af7626d8501acd602