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Magnesium isoglycyrrhizinate inhibits L-type Ca2+ channels, Ca2+ transients, and contractility but not hERG K+ channels

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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 [4]Hebei Key Laboratory of Integrative Medicine on Liver- Kidney Patterns, Shijiazhuang 050200, Hebei, China
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关键词: Magnesium isoglycyrrhizinate L-type Ca2+ currents Myocyte shortening Ca2+ transient hERG K+ channels Rat cardiomyocyte

摘要:
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.

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出版当年[2017]版:
大类 | 3 区 医学
小类 | 3 区 药学 4 区 药物化学
最新[2025]版:
大类 | 2 区 医学
小类 | 1 区 药物化学 1 区 药学
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出版当年[2017]版:
Q3 PHARMACOLOGY & PHARMACY Q3 CHEMISTRY, MEDICINAL
最新[2023]版:
Q1 CHEMISTRY, MEDICINAL Q1 PHARMACOLOGY & PHARMACY

影响因子: 最新[2023版] 最新五年平均 出版当年[2017版] 出版当年五年平均 出版前一年[2016版] 出版后一年[2018版]

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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
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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
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