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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ftmdpi:oai:mdpi.com:/1660-3397/15/6/148/ 2023-08-20T04:04:41+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 Nebb Terje Larsen Hans Eilertsen Steinar Paulsen agris 2017-05-25 application/pdf https://doi.org/10.3390/md15060148 EN eng Multidisciplinary Digital Publishing Institute https://dx.doi.org/10.3390/md15060148 https://creativecommons.org/licenses/by/4.0/ Marine Drugs; Volume 15; Issue 6; Pages: 148 PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MS e NMR Text 2017 ftmdpi https://doi.org/10.3390/md15060148 2023-07-31T21:07:35Z 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. Text Arctic MDPI Open Access Publishing Arctic Marine Drugs 15 6 148 |
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Open Polar |
collection |
MDPI Open Access Publishing |
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ftmdpi |
language |
English |
topic |
PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MS e NMR |
spellingShingle |
PPAR dual agonist activity metabolomics Chaetoceros karianus LC-MS e NMR Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde Nebb Terje Larsen Hans Eilertsen Steinar 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-MS e NMR |
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 |
Text |
author |
Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde Nebb Terje Larsen Hans Eilertsen Steinar Paulsen |
author_facet |
Angel Moldes-Anaya Thomas Sæther Silvio Uhlig Hilde Nebb Terje Larsen Hans Eilertsen Steinar 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 |
Multidisciplinary Digital Publishing Institute |
publishDate |
2017 |
url |
https://doi.org/10.3390/md15060148 |
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agris |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
Marine Drugs; Volume 15; Issue 6; Pages: 148 |
op_relation |
https://dx.doi.org/10.3390/md15060148 |
op_rights |
https://creativecommons.org/licenses/by/4.0/ |
op_doi |
https://doi.org/10.3390/md15060148 |
container_title |
Marine Drugs |
container_volume |
15 |
container_issue |
6 |
container_start_page |
148 |
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