Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ
The peroxisome proliferator-activated receptors (PPARs) function as ligand-activated transcription factors that convert signals in the form of lipids to physiological responses through the activation of metabolic target genes. Due to their key roles in lipid and carbohydrate metabolism, the PPARs ar...
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2017
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ftdoajarticles:oai:doaj.org/article:193d778fd6ca48788cc0d5db62492c31 2023-05-15T15:07:19+02:00 Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde I. Nebb Terje Larsen Hans C. Eilertsen Steinar M. Paulsen 2017-05-01T00:00:00Z https://doi.org/10.3390/md15060148 https://doaj.org/article/193d778fd6ca48788cc0d5db62492c31 EN eng MDPI AG http://www.mdpi.com/1660-3397/15/6/148 https://doaj.org/toc/1660-3397 1660-3397 doi:10.3390/md15060148 https://doaj.org/article/193d778fd6ca48788cc0d5db62492c31 Marine Drugs, Vol 15, Iss 6, p 148 (2017) PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MSe NMR Biology (General) QH301-705.5 article 2017 ftdoajarticles https://doi.org/10.3390/md15060148 2022-12-30T21:54:50Z The peroxisome proliferator-activated receptors (PPARs) function as ligand-activated transcription factors that convert signals in the form of lipids to physiological responses through the activation of metabolic target genes. Due to their key roles in lipid and carbohydrate metabolism, the PPARs are important drug targets. However, for several of the PPAR drugs currently in use, adverse side effects have been reported. In an effort to identify compounds from marine organisms that may serve as molecular scaffolds for the development of novel and safer PPAR-targeting drugs, we performed a bioassay-guided screening of organic extracts made from organisms supplied by the Norwegian Biobank of Arctic Marine Organisms (Marbank). Among several interesting hits, we identified two poorly described isomeric oxo-fatty acids from the microalgae Chaetoceros karianus for which we provide the first evidence that they might display dual specificity towards human PPARα and PPARγ. Principal component analysis showed that C. karianus stood out from other Chaetoceros species, both with respect to the metabolic profile and the PPAR activity. The isolation of these compounds holds the potential of uncovering a PPAR pharmacophore with tunable activity and specificity. Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic Marine Drugs 15 6 148 |
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Open Polar |
collection |
Directory of Open Access Journals: DOAJ Articles |
op_collection_id |
ftdoajarticles |
language |
English |
topic |
PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MSe NMR Biology (General) QH301-705.5 |
spellingShingle |
PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MSe NMR Biology (General) QH301-705.5 Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde I. Nebb Terje Larsen Hans C. Eilertsen Steinar M. Paulsen Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
topic_facet |
PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MSe NMR Biology (General) QH301-705.5 |
description |
The peroxisome proliferator-activated receptors (PPARs) function as ligand-activated transcription factors that convert signals in the form of lipids to physiological responses through the activation of metabolic target genes. Due to their key roles in lipid and carbohydrate metabolism, the PPARs are important drug targets. However, for several of the PPAR drugs currently in use, adverse side effects have been reported. In an effort to identify compounds from marine organisms that may serve as molecular scaffolds for the development of novel and safer PPAR-targeting drugs, we performed a bioassay-guided screening of organic extracts made from organisms supplied by the Norwegian Biobank of Arctic Marine Organisms (Marbank). Among several interesting hits, we identified two poorly described isomeric oxo-fatty acids from the microalgae Chaetoceros karianus for which we provide the first evidence that they might display dual specificity towards human PPARα and PPARγ. Principal component analysis showed that C. karianus stood out from other Chaetoceros species, both with respect to the metabolic profile and the PPAR activity. The isolation of these compounds holds the potential of uncovering a PPAR pharmacophore with tunable activity and specificity. |
format |
Article in Journal/Newspaper |
author |
Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde I. Nebb Terje Larsen Hans C. Eilertsen Steinar M. Paulsen |
author_facet |
Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde I. Nebb Terje Larsen Hans C. Eilertsen Steinar M. Paulsen |
author_sort |
Angel Moldes-Anaya |
title |
Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
title_short |
Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
title_full |
Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
title_fullStr |
Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
title_full_unstemmed |
Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
title_sort |
two isomeric c16 oxo-fatty acids from the diatom chaetoceros karianus show dual agonist activity towards human peroxisome proliferator-activated receptors (ppars) α/γ |
publisher |
MDPI AG |
publishDate |
2017 |
url |
https://doi.org/10.3390/md15060148 https://doaj.org/article/193d778fd6ca48788cc0d5db62492c31 |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
Marine Drugs, Vol 15, Iss 6, p 148 (2017) |
op_relation |
http://www.mdpi.com/1660-3397/15/6/148 https://doaj.org/toc/1660-3397 1660-3397 doi:10.3390/md15060148 https://doaj.org/article/193d778fd6ca48788cc0d5db62492c31 |
op_doi |
https://doi.org/10.3390/md15060148 |
container_title |
Marine Drugs |
container_volume |
15 |
container_issue |
6 |
container_start_page |
148 |
_version_ |
1766338848262979584 |