Detail
Článek
Článek online
FT
Medvik - BMČ
  • Je něco špatně v tomto záznamu ?

4-Methylcatechol, a Flavonoid Metabolite with Potent Antiplatelet Effects

L. Applová, J. Karlíčková, P. Warncke, K. Macáková, M. Hrubša, M. Macháček, V. Tvrdý, D. Fischer, P. Mladěnka,

. 2019 ; 63 (20) : e1900261. [pub] 20190807

Jazyk angličtina Země Německo

Typ dokumentu časopisecké články, práce podpořená grantem

Perzistentní odkaz   https://www.medvik.cz/link/bmc20023750

SCOPE: Intake of flavonoids from the diet can be substantial, and epidemiological studies suggest that these compounds can decrease the incidence of cardiovascular diseases by involvement with increased platelet aggregation. Although parent flavonoids possess antiplatelet effects, the clinical importance is disputable due to their very low bioavailability. Most of them are metabolized by human colon bacteria to smaller phenolic compounds, which reach higher plasma concentrations than the parent flavonoids. In this study, a series of 29 known flavonoid metabolites is tested for antiplatelet potential. METHODS AND RESULTS: Four compounds appear to have a biologically relevant antiplatelet effect using whole human blood. 4-Methylcatechol (4-MC) is clearly the most efficient being about 10× times more active than clinically used acetylsalicylic acid. This ex vivo effect is also confirmed using a potentially novel in-vivo-like ex ovo hen's egg model of thrombosis, where 4-MC significantly increases the survival of the eggs. The mechanism of action is studied and it seems that it is mainly based on the influence on intracellular calcium signaling. CONCLUSION: This study shows that some flavonoid metabolites formed by human microflora have a strong antiplatelet effect. This information can help to explain the antiplatelet potential of orally given flavonoids.

Citace poskytuje Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc20023750
003      
CZ-PrNML
005      
20221018084919.0
007      
ta
008      
201125s2019 gw f 000 0|eng||
009      
AR
024    7_
$a 10.1002/mnfr.201900261 $2 doi
035    __
$a (PubMed)31343835
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a gw
100    1_
$a Applová, Lenka $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic. $7 xx0277670
245    10
$a 4-Methylcatechol, a Flavonoid Metabolite with Potent Antiplatelet Effects / $c L. Applová, J. Karlíčková, P. Warncke, K. Macáková, M. Hrubša, M. Macháček, V. Tvrdý, D. Fischer, P. Mladěnka,
520    9_
$a SCOPE: Intake of flavonoids from the diet can be substantial, and epidemiological studies suggest that these compounds can decrease the incidence of cardiovascular diseases by involvement with increased platelet aggregation. Although parent flavonoids possess antiplatelet effects, the clinical importance is disputable due to their very low bioavailability. Most of them are metabolized by human colon bacteria to smaller phenolic compounds, which reach higher plasma concentrations than the parent flavonoids. In this study, a series of 29 known flavonoid metabolites is tested for antiplatelet potential. METHODS AND RESULTS: Four compounds appear to have a biologically relevant antiplatelet effect using whole human blood. 4-Methylcatechol (4-MC) is clearly the most efficient being about 10× times more active than clinically used acetylsalicylic acid. This ex vivo effect is also confirmed using a potentially novel in-vivo-like ex ovo hen's egg model of thrombosis, where 4-MC significantly increases the survival of the eggs. The mechanism of action is studied and it seems that it is mainly based on the influence on intracellular calcium signaling. CONCLUSION: This study shows that some flavonoid metabolites formed by human microflora have a strong antiplatelet effect. This information can help to explain the antiplatelet potential of orally given flavonoids.
650    _2
$a zvířata $7 D000818
650    _2
$a kyselina arachidonová $x farmakologie $7 D016718
650    _2
$a katecholy $x farmakologie $7 D002396
650    _2
$a kuřecí embryo $7 D002642
650    _2
$a inhibitory cyklooxygenasy $x farmakologie $7 D016861
650    _2
$a preklinické hodnocení léčiv $x metody $7 D004353
650    _2
$a inhibitory enzymů $x farmakologie $7 D004791
650    _2
$a lidé $7 D006801
650    _2
$a agregace trombocytů $x účinky léků $7 D010974
650    _2
$a inhibitory agregace trombocytů $x farmakologie $7 D010975
650    _2
$a pyrogalol $x farmakologie $7 D011748
650    _2
$a serotonin $x metabolismus $7 D012701
650    _2
$a trombóza $x farmakoterapie $7 D013927
650    _2
$a thromboxan-A-synthasa $x antagonisté a inhibitory $7 D013930
655    _2
$a časopisecké články $7 D016428
655    _2
$a práce podpořená grantem $7 D013485
700    1_
$a Karlíčková, Jana $u Department of Pharmaceutical Botany, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.
700    1_
$a Warncke, Paul $u Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmacy, Friedrich-Schiller-University Jena, Lessingstr. 8, 07743, Jena, Germany.
700    1_
$a Macáková, Kateřina $u Department of Pharmaceutical Botany, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.
700    1_
$a Hrubša, Marcel $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.
700    1_
$a Macháček, Miloslav $u Department of Biochemical Sciences, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.
700    1_
$a Tvrdý, Václav $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.
700    1_
$a Fischer, Dagmar $u Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmacy, Friedrich-Schiller-University Jena, Lessingstr. 8, 07743, Jena, Germany.
700    1_
$a Mladěnka, Přemysl $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.
773    0_
$w MED00192050 $t Molecular nutrition & food research $x 1613-4133 $g Roč. 63, č. 20 (2019), s. e1900261
856    41
$u https://pubmed.ncbi.nlm.nih.gov/31343835 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y a $z 0
990    __
$a 20201125 $b ABA008
991    __
$a 20221018084916 $b ABA008
999    __
$a ok $b bmc $g 1596069 $s 1114426
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2019 $b 63 $c 20 $d e1900261 $e 20190807 $i 1613-4133 $m Molecular nutrition & food research $n Mol Nutr Food Res $x MED00192050
LZP    __
$a Pubmed-20201125

Najít záznam

Citační ukazatele

Možnosti archivace