机构:[1]Hebei University of Chinese Medicine, No.3, Xingyuan Road, Shijiazhuang 050200, Hebei, China[2]Hebei Medical University, No.361, Zhongshan East Road, Shijiazhuang 050017, Hebei, China[3]Department of Pharmacy, The Fourth Hospital of Hebei Medical University, No.12, Jiankang Road, Shijiazhuang 050011, Hebei, China药学部药学部河北医科大学第四医院[4]Hebei Key Laboratory of Integrative Medicine on Liver- Kidney Patterns, Shijiazhuang 050200, Hebei, China
To explore the cardiovascular protective effects of Magnesium isoglycyrrhizinate (MI), especially the underlying cellular mechanisms related to L-type calcium channels and myocardial contractility, and to examine the effects of MI on hERG K+ current expressed in HEK293 cells. We used the whole-cell patch clamp technique, video-based edge detection and dual excitation fluorescence photomultiplier systems to explore the effect of MI on L-type Ca2+ currents (ICa-L) and cell contraction in rat cardiomyocytes. We also examined the rapidly activating delayed rectifier potassium current (I-Kr) expressed in HEK293 cells using a perforated patch clamp. MI inhibited ICa-L in a dose-dependent manner, with a half-maximal inhibitory concentration (IC50) of 0.22 mg/ml, and the maximal inhibitory effect was 61.10 +/- 0.59%. MI at a concentration of 0.3 mg/ml reduced cell shortening by 24.12 +/- 3.97% and the peak value of the Ca2+ transient by 36.54 +/- 4.96%. MI had no significant influence on hERG K+ channels expressed in HEK293 cells at all test potentials. MI exerts protective effects on the heart via the inhibition of ICa-L and cell shortening in rat cardiomyocytes. However, MI had no significant influence on I-Kr; thus, MI may exert cardioprotective effects without causing drug-induced long QT syndrome.
基金:
This work was supported by the Research
Foundation of Administration of Traditional Chinese Medicine of
Hebei Province, China (Nos. 2017007 and 2015030), Research
Foundation of Education Bureau of Hebei Province (QN20131046 to
X.Z.), and Key Basic Applied Project of Hebei Provincial Department
of Science & Technology (No. 15967730D to W.Z.).
第一作者机构:[1]Hebei University of Chinese Medicine, No.3, Xingyuan Road, Shijiazhuang 050200, Hebei, China[4]Hebei Key Laboratory of Integrative Medicine on Liver- Kidney Patterns, Shijiazhuang 050200, Hebei, China
共同第一作者:
通讯作者:
通讯机构:[1]Hebei University of Chinese Medicine, No.3, Xingyuan Road, Shijiazhuang 050200, Hebei, China[4]Hebei Key Laboratory of Integrative Medicine on Liver- Kidney Patterns, Shijiazhuang 050200, Hebei, China
推荐引用方式(GB/T 7714):
Lin Yue,Zhang Yuanyuan,Song Qiongtao,et al.Magnesium isoglycyrrhizinate inhibits L-type Ca2+ channels, Ca2+ transients, and contractility but not hERG K+ channels[J].ARCHIVES OF PHARMACAL RESEARCH.2017,40(10):1135-1145.doi:10.1007/s12272-017-0938-6.
APA:
Lin, Yue,Zhang, Yuanyuan,Song, Qiongtao,Song, Tao,Han, Xue...&Zhang, Jianping.(2017).Magnesium isoglycyrrhizinate inhibits L-type Ca2+ channels, Ca2+ transients, and contractility but not hERG K+ channels.ARCHIVES OF PHARMACAL RESEARCH,40,(10)
MLA:
Lin, Yue,et al."Magnesium isoglycyrrhizinate inhibits L-type Ca2+ channels, Ca2+ transients, and contractility but not hERG K+ channels".ARCHIVES OF PHARMACAL RESEARCH 40..10(2017):1135-1145