3-methoxycatechol causes vasodilation likely via KV channels: ex vivo, in silico docking and in vivo study

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F24%3A10486494" target="_blank" >RIV/00216208:11160/24:10486494 - isvavai.cz</a>
Result on the web
<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=xGlI6He2e1" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=xGlI6He2e1</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.vph.2024.107418" target="_blank" >10.1016/j.vph.2024.107418</a>

Result language
angličtina
Original language name
3-methoxycatechol causes vasodilation likely via KV channels: ex vivo, in silico docking and in vivo study
Original language description
Some substituted catechols are flavonoid metabolites formed by the gut microbiota which are absorbed afterwards. In this current study, we aimed at testing of 22 chemically-related catechols in order to find the most potent structure and to investigate the mechanism of action. 3-methoxycatechol (3-MOC), 4-ethylcatechol, 3,5-dichlorocatechol, 4-tertbutylcatechol, 4,5-dichlorocatechol, 3-fluorocatechol, 3-isopropylcatechol, 3-methylcatechol and the parent 4-methylcatechol exhibited high vasodilatory activities on isolated rat aortic rings with EC(50)s ranging from similar to 10 to 24 microM. The most potent compound, 3-MOC, relaxed also resistant mesenteric artery but not porcine coronary artery, and decreased arterial blood pressure in both male and female spontaneously hypertensive rats in vivo without affecting heart rate. It potentiated the vasodilation mediated by cAMP and cGMP, but did not impact L-type Ca2+-channels. Activation of voltage-gated potassium channels (K-V) was found to be involved in the mechanism of action. This was corroborated by docking analysis of 3-MOC with the K(V)7.4 channel.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy

Project
<a href="/en/project/NU21-02-00135" target="_blank" >NU21-02-00135: Cardiovascular effects of flavonoid metabolites and the impact of metabolic risk factors</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2024
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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