Korean J Physiol Pharmacol.  2009 Oct;13(5):361-365. 10.4196/kjpp.2009.13.5.361.

Possible Involvement of Ca2+ Activated K+ Channels, SK Channel, in the Quercetin-Induced Vasodilatation

• Nishida S
• Satoh H

• KMID: 1982569
• DOI: http://doi.org/10.4196/kjpp.2009.13.5.361

Abstract

Effects of quercetin, a kind of flavonoids, on the vasodilating actions were investigated. Among the mechanisms for quercetin-induced vasodilatation in rat aorta, the involvement with the Ca2+ activated K+ (KCa) channel was examined. Pretreatment with NE (5 micrometer) or KCl (60 mM) was carried out and then, the modulation by quercetin of the constriction was examined using rat aorta ring strips (3 mm) at 36.5degrees C. Quercetin (0.1 to 100 micrometer) relaxed the NE-induced vasoconstrictions in a concentration-dependent manner. NO synthesis (NOS) inhibitor, NG-monomethyl-L-arginine acetate (L-NMMA), at 100 micrometer reduced the quercetin (100 micrometer)-induced vasodilatation from 97.8+/-3.7% (n=10) to 78.0+/-11.6% (n=5, p<0.05). Another NOS inhibitor, L-NG-nitro arginine methyl ester (L-NAME), at 100 micrometer also had the similar effect. In the presence of both 100 micrometer L-NMMA and 10 micrometer indomethacin, the quercetin-induced vasodilatation was further attenuated by 100 micrometer tetraethylammonium (TEA, a KCa channel inhibitor). Also TEA decreased the quercetin-induced vasodilatation in endothelium-denuded rat aorta. Used other KCa channel inhibitors, the quercetin-induced vasodilatation was attenuated by 0.3 micrometer apamin (a SK channel inhibitor), but not by 30 nM charybdotoxin (a BK and IK channel inhibitor). Quercetin caused a concentration-dependent vasodilatation, due to the endothelium-dependent and -independent actions. Also quercetin contributes to the vasodilatation selectively with SK channel on smooth muscle.

Keyword

Quercetin; Vasodilatation; KCa channels; PK-C; Endothelium

MeSH Terms

Animals
Aorta
Apamin
Arginine
Charybdotoxin
Constriction
Endothelium
Flavonoids
Indomethacin
Muscle, Smooth
omega-N-Methylarginine
Potassium Channels, Calcium-Activated
Quercetin
Rats
Tea
Tetraethylammonium
Vasoconstriction
Vasodilation
Apamin
Arginine
Charybdotoxin
Flavonoids
Indomethacin
Potassium Channels, Calcium-Activated
Quercetin
Tea
Tetraethylammonium
omega-N-Methylarginine

Figure

• 

  Fig. 1. Concentration-dependent vasodilatation by cumulative administrations of quercetin. Symbols used are control (open circles, n=10), pretreatment with L-NMMA (triangles, n=5), L-NMMA and indomethacin (squares, n=5). Values (%) are represented as mean±S.E.M. ∗p<0.05, ∗∗p<0.01, with respect to control value.

• 

  Fig. 2. Modulation of L-NMMA and indomethacin resistant relaxation at 100 μM quercetin. The vasodilatation in the presence of L-NMMA and indomedhacin (n=5) means as control value in this graph. The vasodilatations by L-NMMA and indomethacin plus TEA (n=5), by L-NMMA and indomethacin plus apamin (n=5), and by L-NMMA and indomethacin plus charybdotoxin (n=5) were compared with that of L-NMMA and indomedhacin. Values (%) are represented as mean±S.E.M. ∗∗p<0.01, with respect to control value.

• 

  Fig. 3. Modulation of quercetin (100 μM)-induced vasodilatation (n=10) in the removal of endothelium (n=5) and the removal of endothelium plus TEA (n=5). Values (%) are represented as mean± S.E.M. ∗p<0.05, with respect to control value.

Reference

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