Comparison of Antiplatelet Effects of Phenol Derivatives in Humans

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F22%3A10450061" target="_blank" >RIV/00216208:11160/22:10450061 - isvavai.cz</a>

Result on the web

<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=VbWqRFuRCN" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=VbWqRFuRCN</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/biom12010117" target="_blank" >10.3390/biom12010117</a>

Result language

angličtina

Original language name

Comparison of Antiplatelet Effects of Phenol Derivatives in Humans

Original language description

Flavonoids are associated with positive cardiovascular effects. However, due to their low bioavailability, metabolites are likely responsible for these properties. Recently, one of these metabolites, 4-methylcatechol, was described to be a very potent antiplatelet compound. This study aimed to compare its activity with its 22 close derivatives both of natural or synthetic origin in order to elucidate a potential structure-antiplatelet activity relationship. Blood from human volunteers was induced to aggregate by arachidonic acid (AA), collagen or thrombin, and plasma coagulation was also studied. Potential toxicity was tested on human erythrocytes as well as on a cancer cell line. Our results indicated that 17 out of the 22 compounds were very active at a concentration of 40 mu M and, importantly, seven of them had an IC50 on AA-triggered aggregation below 3 mu M. The effects of the most active compounds were confirmed on collagen-triggered aggregation too. None of the tested compounds was toxic toward erythrocytes at 50 mu M and four compounds partly inhibited proliferation of breast cancer cell line at 100 mu M but not at 10 mu M. Additionally, none of the compounds had a significant effect on blood coagulation or thrombin-triggered aggregation. This study hence reports four phenol derivatives (4-ethylcatechol, 4-fluorocatechol, 2-methoxy-4-ethylphenol and 3-methylcatechol) suitable for future in vivo testing.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10600 - Biological sciences

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

2022

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Biomolecules

ISSN

2218-273X

e-ISSN

—

Volume of the periodical

12

Issue of the periodical within the volume

1

Country of publishing house

CH - SWITZERLAND

Number of pages

11

Pages from-to

117

UT code for WoS article

000758478100001

EID of the result in the Scopus database

2-s2.0-85122702005