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Article: Effects of the natural flavone trimethylapigenin on cardiac potassium currents

TitleEffects of the natural flavone trimethylapigenin on cardiac potassium currents
Authors
KeywordsAcetylcholine-Activated K + Current
Hkv1.5
Open Channel Blocker
Trimethylapigenin
Issue Date2012
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharm
Citation
Biochemical Pharmacology, 2012, v. 84 n. 4, p. 498-506 How to Cite?
Abstract
The natural flavones and polymethylflavone have been reported to have cardiovascular protective effects. In the present study, we determined whether quecertin, apigenin and their methylated compounds (3,7,3′,4′-tetramethylquecertin, 3,5,7,3′,4′-pentamethylquecertin, 7,4′-dimethylapigenin, and 5,7,4′-trimethylapigenin) would block the atrial specific potassium channel hKv1.5 using a whole-cell patch voltage-clamp technique. We found that only trimethylapigenin showed a strong inhibitory effect on hKv1.5 channel current. This compound suppressed hKv1.5 current in HEK 293 cell line (IC 50 = 6.4 μM), and the ultra-rapid delayed rectify K + current I Kur in human atrial myocytes (IC 50 = 8.0 μM) by binding to the open channels and showed a use- and frequency-dependent manner. In addition, trimethylapigenin decreased transient outward potassium current (I to) in human atrial myocytes, inhibited acetylcholine-activated K + current (IC 50 = 6.8 μM) in rat atrial myocytes. Interestingly, trimethylapigenin had a weak inhibition of hERG channel current. Our results indicate that trimethyapigenin significantly inhibits the atrial potassium currents hKv1.5/I Kur and I KACh, which suggests that trimethylapigenin may be a potential candidate for anti-atrial fibrillation. © 2012 Elsevier Inc. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/163493
ISSN
2013 Impact Factor: 4.650
2013 SCImago Journal Rankings: 1.994
ISI Accession Number ID

 

Author Affiliations
  1. The University of Hong Kong Li Ka Shing Faculty of Medicine
  2. Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province
  3. Tongji Medical College
  4. Huazhong University of Science and Technology
DC FieldValueLanguage
dc.contributor.authorLiu, Yen_US
dc.contributor.authorXu, XHen_US
dc.contributor.authorLiu, Zen_US
dc.contributor.authorDu, XLen_US
dc.contributor.authorChen, KHen_US
dc.contributor.authorXin, Xen_US
dc.contributor.authorJin, ZDen_US
dc.contributor.authorShen, JZen_US
dc.contributor.authorHu, Yen_US
dc.contributor.authorLi, GRen_US
dc.contributor.authorJin, MWen_US
dc.date.accessioned2012-09-05T05:32:16Z-
dc.date.available2012-09-05T05:32:16Z-
dc.date.issued2012en_US
dc.identifier.citationBiochemical Pharmacology, 2012, v. 84 n. 4, p. 498-506en_US
dc.identifier.issn0006-2952en_US
dc.identifier.urihttp://hdl.handle.net/10722/163493-
dc.description.abstractThe natural flavones and polymethylflavone have been reported to have cardiovascular protective effects. In the present study, we determined whether quecertin, apigenin and their methylated compounds (3,7,3′,4′-tetramethylquecertin, 3,5,7,3′,4′-pentamethylquecertin, 7,4′-dimethylapigenin, and 5,7,4′-trimethylapigenin) would block the atrial specific potassium channel hKv1.5 using a whole-cell patch voltage-clamp technique. We found that only trimethylapigenin showed a strong inhibitory effect on hKv1.5 channel current. This compound suppressed hKv1.5 current in HEK 293 cell line (IC 50 = 6.4 μM), and the ultra-rapid delayed rectify K + current I Kur in human atrial myocytes (IC 50 = 8.0 μM) by binding to the open channels and showed a use- and frequency-dependent manner. In addition, trimethylapigenin decreased transient outward potassium current (I to) in human atrial myocytes, inhibited acetylcholine-activated K + current (IC 50 = 6.8 μM) in rat atrial myocytes. Interestingly, trimethylapigenin had a weak inhibition of hERG channel current. Our results indicate that trimethyapigenin significantly inhibits the atrial potassium currents hKv1.5/I Kur and I KACh, which suggests that trimethylapigenin may be a potential candidate for anti-atrial fibrillation. © 2012 Elsevier Inc. All rights reserved.en_US
dc.languageengen_US
dc.publisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharmen_US
dc.relation.ispartofBiochemical Pharmacologyen_US
dc.subjectAcetylcholine-Activated K + Currenten_US
dc.subjectHkv1.5en_US
dc.subjectOpen Channel Blockeren_US
dc.subjectTrimethylapigeninen_US
dc.titleEffects of the natural flavone trimethylapigenin on cardiac potassium currentsen_US
dc.typeArticleen_US
dc.identifier.emailLi, GR:grli@hkucc.hku.hken_US
dc.identifier.authorityLi, GR=rp00476en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1016/j.bcp.2012.05.002en_US
dc.identifier.pmid22583923-
dc.identifier.scopuseid_2-s2.0-84864138148en_US
dc.identifier.hkuros202912-
dc.identifier.isiWOS:000307135600011-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridLiu, Y=55071922600en_US
dc.identifier.scopusauthoridXu, XH=37082609600en_US
dc.identifier.scopusauthoridLiu, Z=55228841900en_US
dc.identifier.scopusauthoridDu, XL=53263675600en_US
dc.identifier.scopusauthoridChen, KH=55228781400en_US
dc.identifier.scopusauthoridXin, X=37462585400en_US
dc.identifier.scopusauthoridJin, ZD=37461509500en_US
dc.identifier.scopusauthoridShen, JZ=55073430400en_US
dc.identifier.scopusauthoridHu, Y=50261872200en_US
dc.identifier.scopusauthoridLi, GR=7408462932en_US
dc.identifier.scopusauthoridJin, MW=35932258500en_US
dc.identifier.citeulike11092493-

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