PMID- 18357730 OWN - NLM STAT- MEDLINE DCOM- 20090810 LR - 20080324 IS - 0513-4870 (Print) IS - 0513-4870 (Linking) VI - 43 IP - 1 DP - 2008 Jan TI - [Effect of sophocarpine on HERG K+ channels]. PG - 44-9 AB - Human ether-a-go-go-related gene (HERG) encodes the rapid component of the cardiac delayed rectifier K+ current, which has an important effect on both proarrhythmia and antiarrhythmia. To investigate the effect of sophocarpine (SC) on HERG channel stably expressing in human embryonic kidney-293 (HEK293) cells, whole-cell patch-clamp technique was used to record HERG current and kinetic curves. As the result, it was found that SC inhibited HERG current in a concentration-dependent manner (10, 30, 100, and 300 micromol x L(-1)). At 0 mV, 10, 30, 100, and 300 micromol x L(-1) SC respectively inhibited IHERG by Istep ( 10.7 +/- 2.8)% , (11.3 +/- 5.5)% , (47.0 +/- 2.3)% and (53.7 +/- 2.5)% , and Itail (1.1 +/- 3.0)%, (17.1 +/- 3.3)%, (32.7 +/- 1.9)% (P < 0.05, n = 12) and (56.0 +/- 2.4)% (P < 0.05, n = 13). The time constants of inactivation, recovery from inactivation and onset of inactivation were accelerated. SC did not change other channel kinetics (activation and deactivation). It is concluded that SC inhibited the transfected HERG channels by influencing the inactivation state, which is the probable anti-arrhythmic mechanism. FAU - Qi, Zhi-Ping AU - Qi ZP AD - Department of Pharmacology, Bio-pharmaceutical Key Laboratory of Heilongjiang Province-Incubator of State Key Laboratory, Harbin Medical University, Harbin 150086, China. FAU - Shi, Shan-Shan AU - Shi SS FAU - Zhao, Xue-Ling AU - Zhao XL FAU - Zhao, Wen-Xiao AU - Zhao WX FAU - Bai, Yun-Long AU - Bai YL FAU - Lu, Yan-Jie AU - Lu YJ FAU - Li, Bao-Xin AU - Li BX FAU - Yang, Bao-Feng AU - Yang BF LA - chi PT - English Abstract PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - China TA - Yao Xue Xue Bao JT - Yao xue xue bao = Acta pharmaceutica Sinica JID - 21710340R RN - 0 (Alkaloids) RN - 0 (Anti-Arrhythmia Agents) RN - 0 (Ether-A-Go-Go Potassium Channels) RN - 6483-15-4 (sophocarpine) SB - IM MH - Alkaloids/*pharmacology MH - Anti-Arrhythmia Agents/*pharmacology MH - Cell Line MH - Dose-Response Relationship, Drug MH - Ether-A-Go-Go Potassium Channels/*antagonists & inhibitors/metabolism/*physiology MH - Humans MH - Kidney/cytology MH - Kinetics MH - Membrane Potentials/drug effects MH - Patch-Clamp Techniques MH - Plants, Medicinal/chemistry MH - Sophora/chemistry EDAT- 2008/03/25 09:00 MHDA- 2009/08/11 09:00 CRDT- 2008/03/25 09:00 PHST- 2008/03/25 09:00 [pubmed] PHST- 2009/08/11 09:00 [medline] PHST- 2008/03/25 09:00 [entrez] PST - ppublish SO - Yao Xue Xue Bao. 2008 Jan;43(1):44-9.