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Article: Tanshinone IIA: A new activator of human cardiac KCNQ1/KCNE1 (I Ks) potassium channels

TitleTanshinone IIA: A new activator of human cardiac KCNQ1/KCNE1 (I Ks) potassium channels
Authors
Issue Date2008
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejphar
Citation
European Journal Of Pharmacology, 2008, v. 590 n. 1-3, p. 317-321 How to Cite?
AbstractTanshinone IIA, one of the main active components from Chinese herb Danshen, is widely used to treat cardiovascular diseases including arrhythmia in Asian countries especially in China. However, the mechanisms underlying its anti-arrythmia effects are not clear. In this study we investigate the effects of tanshinone IIA on human KCNQ1/KCNE1 potassium channels (I Ks), human ether-a-go-go-related gene potassium channels (hERG), Kv1.5 potassium channels, inward rectifier potassium channels (I K1) expressed in HEK 293 cells using patch clamp technique. Tanshinone IIA potently and reversibly enhanced the amplitude of I Ks in a concentration dependent manner with an EC 50 of 64.5 μM, accelerated the activation rate of I Ks channels, decelerated their deactivation and shifted the voltage dependence of I Ks activation to negative direction. Isoproteronol, a stimulator of β-adrenergic receptor, at 1 μM and sodium nitroprusside (SNP), a NO donor, at 1 mM, had no significant effects on the enhancement of I Ks by 30 μM tanshinone IIA. N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H89), a selective protein kinase A inhibitor, at 0.1 μM and 1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one (ODQ), a selective nitric oxide-sensitive guanylyl cyclase inhibitor, at 10 μM, also had no significant effects on the enhancement of I Ks by 30 μM tanshinone IIA. Tanshinone IIA did not affect expressed hERG channels, Kv1.5 channels and I K1 channels. These results indicate that tanshinone IIA directly and specifically activate human cardiac KCNQ1/KCNE1 potassium channels (I Ks) in HEK 293 cell through affecting the channels' kinetics. © 2008 Elsevier B.V. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/163187
ISSN
2015 Impact Factor: 2.73
2015 SCImago Journal Rankings: 1.115
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorSun, DDen_US
dc.contributor.authorWang, HCen_US
dc.contributor.authorWang, XBen_US
dc.contributor.authorLuo, Yen_US
dc.contributor.authorJin, ZXen_US
dc.contributor.authorLi, ZCen_US
dc.contributor.authorLi, GRen_US
dc.contributor.authorDong, MQen_US
dc.date.accessioned2012-09-05T05:28:32Z-
dc.date.available2012-09-05T05:28:32Z-
dc.date.issued2008en_US
dc.identifier.citationEuropean Journal Of Pharmacology, 2008, v. 590 n. 1-3, p. 317-321en_US
dc.identifier.issn0014-2999en_US
dc.identifier.urihttp://hdl.handle.net/10722/163187-
dc.description.abstractTanshinone IIA, one of the main active components from Chinese herb Danshen, is widely used to treat cardiovascular diseases including arrhythmia in Asian countries especially in China. However, the mechanisms underlying its anti-arrythmia effects are not clear. In this study we investigate the effects of tanshinone IIA on human KCNQ1/KCNE1 potassium channels (I Ks), human ether-a-go-go-related gene potassium channels (hERG), Kv1.5 potassium channels, inward rectifier potassium channels (I K1) expressed in HEK 293 cells using patch clamp technique. Tanshinone IIA potently and reversibly enhanced the amplitude of I Ks in a concentration dependent manner with an EC 50 of 64.5 μM, accelerated the activation rate of I Ks channels, decelerated their deactivation and shifted the voltage dependence of I Ks activation to negative direction. Isoproteronol, a stimulator of β-adrenergic receptor, at 1 μM and sodium nitroprusside (SNP), a NO donor, at 1 mM, had no significant effects on the enhancement of I Ks by 30 μM tanshinone IIA. N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H89), a selective protein kinase A inhibitor, at 0.1 μM and 1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one (ODQ), a selective nitric oxide-sensitive guanylyl cyclase inhibitor, at 10 μM, also had no significant effects on the enhancement of I Ks by 30 μM tanshinone IIA. Tanshinone IIA did not affect expressed hERG channels, Kv1.5 channels and I K1 channels. These results indicate that tanshinone IIA directly and specifically activate human cardiac KCNQ1/KCNE1 potassium channels (I Ks) in HEK 293 cell through affecting the channels' kinetics. © 2008 Elsevier B.V. All rights reserved.en_US
dc.languageengen_US
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejpharen_US
dc.relation.ispartofEuropean Journal of Pharmacologyen_US
dc.subject.meshCells, Cultureden_US
dc.subject.meshCyclic Amp-Dependent Protein Kinases - Antagonists & Inhibitorsen_US
dc.subject.meshDiterpenes, Abietaneen_US
dc.subject.meshDose-Response Relationship, Drugen_US
dc.subject.meshDrugs, Chinese Herbal - Pharmacologyen_US
dc.subject.meshEther-A-Go-Go Potassium Channels - Drug Effectsen_US
dc.subject.meshGuanylate Cyclase - Antagonists & Inhibitorsen_US
dc.subject.meshHeart - Drug Effectsen_US
dc.subject.meshHumansen_US
dc.subject.meshKcnq1 Potassium Channel - Drug Effectsen_US
dc.subject.meshKv1.5 Potassium Channel - Drug Effectsen_US
dc.subject.meshNitric Oxide Donors - Pharmacologyen_US
dc.subject.meshOxadiazoles - Pharmacologyen_US
dc.subject.meshPhenanthrenes - Pharmacologyen_US
dc.subject.meshPotassium Channels, Voltage-Gated - Drug Effectsen_US
dc.subject.meshQuinoxalines - Pharmacologyen_US
dc.titleTanshinone IIA: A new activator of human cardiac KCNQ1/KCNE1 (I Ks) potassium channelsen_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.ejphar.2008.06.005en_US
dc.identifier.pmid18573250-
dc.identifier.scopuseid_2-s2.0-48049120166en_US
dc.identifier.hkuros146213-
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-48049120166&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume590en_US
dc.identifier.issue1-3en_US
dc.identifier.spage317en_US
dc.identifier.epage321en_US
dc.identifier.isiWOS:000258712500046-
dc.publisher.placeNetherlandsen_US
dc.identifier.scopusauthoridSun, DD=22956622700en_US
dc.identifier.scopusauthoridWang, HC=9133947200en_US
dc.identifier.scopusauthoridWang, XB=8585424100en_US
dc.identifier.scopusauthoridLuo, Y=35285699500en_US
dc.identifier.scopusauthoridJin, ZX=27170820700en_US
dc.identifier.scopusauthoridLi, ZC=27170449700en_US
dc.identifier.scopusauthoridLi, GR=7408462932en_US
dc.identifier.scopusauthoridDong, MQ=7202127303en_US

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