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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MDPI AG
2017
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Online Access: | http://hdl.handle.net/10852/61960 http://urn.nb.no/URN:NBN:no-64566 https://doi.org/10.3390/md15060148 |
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ftoslouniv:oai:www.duo.uio.no:10852/61960 2023-05-15T15:06:06+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 Moldes-Anaya, Angel Sæther, Thomas Uhlig, Silvio Nebb, Hilde Irene Larsen, Terje Eilertsen, Hans Christian Paulsen, Steinar Martin 2017-05-25T23:37:38Z http://hdl.handle.net/10852/61960 http://urn.nb.no/URN:NBN:no-64566 https://doi.org/10.3390/md15060148 EN eng MDPI AG http://urn.nb.no/URN:NBN:no-64566 Moldes-Anaya, Angel Sæther, Thomas Uhlig, Silvio Nebb, Hilde Irene Larsen, Terje Eilertsen, Hans Christian Paulsen, Steinar Martin . Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ. Marine Drugs. 2017, 15(148) http://hdl.handle.net/10852/61960 1472077 info:ofi/fmt:kev:mtx:ctx&ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Marine Drugs&rft.volume=15&rft.spage=&rft.date=2017 Marine Drugs 15 148 16 http://dx.doi.org/10.3390/md15060148 URN:NBN:no-64566 Fulltext https://www.duo.uio.no/bitstream/handle/10852/61960/1/marinedrugs-15-00148.pdf Attribution 4.0 International https://creativecommons.org/licenses/by/4.0/ CC-BY 1660-3397 Journal article Tidsskriftartikkel Peer reviewed PublishedVersion 2017 ftoslouniv https://doi.org/10.3390/md15060148 2020-06-21T08:51:12Z 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 Universitet i Oslo: Digitale utgivelser ved UiO (DUO) Arctic Marine Drugs 15 6 148 |
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Open Polar |
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Universitet i Oslo: Digitale utgivelser ved UiO (DUO) |
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ftoslouniv |
language |
English |
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 |
Moldes-Anaya, Angel Sæther, Thomas Uhlig, Silvio Nebb, Hilde Irene Larsen, Terje Eilertsen, Hans Christian Paulsen, Steinar Martin |
spellingShingle |
Moldes-Anaya, Angel Sæther, Thomas Uhlig, Silvio Nebb, Hilde Irene Larsen, Terje Eilertsen, Hans Christian Paulsen, Steinar Martin Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ |
author_facet |
Moldes-Anaya, Angel Sæther, Thomas Uhlig, Silvio Nebb, Hilde Irene Larsen, Terje Eilertsen, Hans Christian Paulsen, Steinar Martin |
author_sort |
Moldes-Anaya, Angel |
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 |
http://hdl.handle.net/10852/61960 http://urn.nb.no/URN:NBN:no-64566 https://doi.org/10.3390/md15060148 |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
1660-3397 |
op_relation |
http://urn.nb.no/URN:NBN:no-64566 Moldes-Anaya, Angel Sæther, Thomas Uhlig, Silvio Nebb, Hilde Irene Larsen, Terje Eilertsen, Hans Christian Paulsen, Steinar Martin . Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ. Marine Drugs. 2017, 15(148) http://hdl.handle.net/10852/61960 1472077 info:ofi/fmt:kev:mtx:ctx&ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Marine Drugs&rft.volume=15&rft.spage=&rft.date=2017 Marine Drugs 15 148 16 http://dx.doi.org/10.3390/md15060148 URN:NBN:no-64566 Fulltext https://www.duo.uio.no/bitstream/handle/10852/61960/1/marinedrugs-15-00148.pdf |
op_rights |
Attribution 4.0 International https://creativecommons.org/licenses/by/4.0/ |
op_rightsnorm |
CC-BY |
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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1766337752475893760 |