Academic Journal
Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems
| Title: | Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems |
|---|---|
| Authors: | Kónya, Zoltán, Bécsi, Bálint, Kiss, Andrea, Horváth, Dániel, Hadháziné Raics, Mária, Kövér, Katalin, E., Lontay, Beáta, Erdődi, Ferenc |
| Source: | J Enzyme Inhib Med Chem Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 500-509 (2019) |
| Publisher Information: | Informa UK Limited, 2019. |
| Publication Year: | 2019 |
| Subject Terms: | 0301 basic medicine, Magnetic Resonance Spectroscopy, Synaptosomal-Associated Protein 25, Cell Survival, RM1-950, Calorimetry, tellimagrandin i, Exocytosis, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, 03 medical and health sciences, Protein Phosphatase 1, synaptosomal exocytosis, Animals, Humans, Elméleti orvostudományok, protein phosphatase-2a, Protein Phosphatase 2, Enzyme Inhibitors, Phosphorylation, Muscle, Skeletal, Cerebral Cortex, 0303 health sciences, mahtabin a, protein phosphatase-1, Orvostudományok, Surface Plasmon Resonance, Hydrolyzable Tannins, 3. Good health, Therapeutics. Pharmacology, Research Paper, HeLa Cells, Synaptosomes |
| Description: | Several ellagitannins inhibited the activity of protein phosphatase-1 (PP1) and -2 A (PP2A) catalytic subunits (PP1c and PP2Ac) with preferential suppression of PP1c over PP2Ac. The inhibitory potency for PP1c followed the order of tellimagrandin I > mahtabin A > praecoxin B > 1.2-Di-O-galloyl-4.6-(S)-HHDP-β-D-glucopyranose > pedunculagin with IC50 values ranging from 0.20 µM to 2.47 µM. The interaction of PP1c and tellimagrandin I was assessed by NMR saturation transfer difference, surface plasmon resonance, isothermal titration calorimetry, and microscale thermophoresis based binding techniques. Tellimagrandin I suppressed viability and phosphatase activity of HeLa cells, while mahtabin A was without effect. Conversely, mahtabin A increased the phosphorylation level of SNAP-25Thr138 and suppressed exocytosis of cortical synaptosomes, whereas tellimagrandin I was without influence. Our results establish ellagitannins as partially selective inhibitors of PP1 and indicate that these polyphenols may act distinctly in cellular systems depending on their membrane permeability and/or their actions on cell membranes. |
| Document Type: | Article Conference object Other literature type |
| File Description: | application/pdf |
| Language: | English |
| ISSN: | 1475-6374 1475-6366 |
| DOI: | 10.1080/14756366.2018.1557653 |
| Access URL: | https://www.tandfonline.com/doi/pdf/10.1080/14756366.2018.1557653?needAccess=true https://pubmed.ncbi.nlm.nih.gov/30696301 https://doaj.org/article/1ebea239b38c40f89067b205d3226b25 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352937/ https://pubmed.ncbi.nlm.nih.gov/30696301/ https://www.tandfonline.com/doi/full/10.1080/14756366.2018.1557653 |
| Rights: | CC BY |
| Accession Number: | edsair.doi.dedup.....2c9937d40290307e3fd959f1d1d60e81 |
| Database: | OpenAIRE |
Be the first to leave a comment!