Myrsinane, Premyrsinane, and Cyclomyrsinane Diterpenes from Euphorbia falcata as Potassium Ion Channel Inhibitors with Selective G Protein-Activated Inwardly Rectifying Ion Channel (GIRK) Blocking Effects
GIRK channels are activated by a large number of G protein-coupled receptors and regulate the electrical activity of neurons, cardiac atrial myocytes, and beta-pancreatic cells. Abnormalities in GIRK channel function have been implicated in the pathophysiology of neuropathic pain, drug addiction, a...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2016
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| Sorozat: | JOURNAL OF NATURAL PRODUCTS
79 No. 8 |
| doi: | 10.1021/acs.jnatprod.6b00260 |
| mtmt: | 3095531 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/12388 |
| LEADER | 02171nab a2200289 i 4500 | ||
|---|---|---|---|
| 001 | publ12388 | ||
| 005 | 20200326130749.0 | ||
| 008 | 171212s2016 hu o 0|| zxx d | ||
| 022 | |a 0163-3864 | ||
| 024 | 7 | |a 10.1021/acs.jnatprod.6b00260 |2 doi | |
| 024 | 7 | |a 3095531 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a zxx | ||
| 100 | 1 | |a Vasas Andrea | |
| 245 | 1 | 0 | |a Myrsinane, Premyrsinane, and Cyclomyrsinane Diterpenes from Euphorbia falcata as Potassium Ion Channel Inhibitors with Selective G Protein-Activated Inwardly Rectifying Ion Channel (GIRK) Blocking Effects |h [elektronikus dokumentum] / |c Vasas Andrea |
| 260 | |c 2016 | ||
| 300 | |a 1990-2004 | ||
| 490 | 0 | |a JOURNAL OF NATURAL PRODUCTS |v 79 No. 8 | |
| 520 | 3 | |a GIRK channels are activated by a large number of G protein-coupled receptors and regulate the electrical activity of neurons, cardiac atrial myocytes, and beta-pancreatic cells. Abnormalities in GIRK channel function have been implicated in the pathophysiology of neuropathic pain, drug addiction, and cardiac arrhythmias. In the heart, GIRK channels are selectively expressed in the atrium, and their activation inhibits pacemaker activity, thereby slowing the heart rate. In the present study, 19 new diterpenes, falcatins A-S (1-19), and the known euphorprolitherin D (20) were isolated from Euphorbia falcata. The compounds were assayed on stable transfected HEK-hERG (Kv11.1) and HEK-GIRK1/4 (Kir3.1 and Kir3.4) cells. Blocking activity on GIRK channels was exerted by 13 compounds (61-83% at 10 muM), and, among them, five possessed low potency on the hERG channel (4-20% at 10 muM). These selective activities suggest that myrsinane-related diterpenes are potential lead compounds for the treatment of atrial fibrillation. | |
| 700 | 0 | 1 | |a Forgó Péter |e aut |
| 700 | 0 | 1 | |a Orvos Péter |e aut |
| 700 | 0 | 1 | |a Tálosi László |e aut |
| 700 | 0 | 1 | |a Csorba Attila |e aut |
| 700 | 0 | 1 | |a Pinke Gyula |e aut |
| 700 | 0 | 1 | |a Hohmann Judit |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/12388/1/vasas2016.pdf |z Dokumentum-elérés |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/12388/7/Natural_products_2016_8_borito.jpg |z Dokumentum-elérés |