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Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ

Permanent lenke
https://hdl.handle.net/10037/11756
DOI
https://doi.org/10.3390/md15060148
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article.pdf (2.802Mb)
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Dato
2017-05-25
Type
Journal article
Tidsskriftartikkel
Peer reviewed

Forfatter
Moldes-Anaya, Angel; Sæther, Thomas; Uhlig, Silvio; Nebb, Hilde Irene; Larsen, Terje; Eilertsen, Hans Christian; Paulsen, Steinar Martin
Sammendrag
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.
Beskrivelse
Source at http://dx.doi.org/10.3390/md15060148
Forlag
MDPI
Sitering
Moldes-Anaya AS, Sæther T, Uhlig S, Nebb HI, Larsen T, Eilertsen HC, Paulsen SMP. 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)
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