Background: Ginsenoside Rd (GSRd), one of the most abundant ingredients of Panax ginseng, protects the heart via multiple mechanisms including the inhibition of Ca2+ influx. We intended to explore the effects of GSRd on L-type Ca2+ current (I-Ca,I-L) and define the mechanism of the suppression of ICa,L by GSRd. Methods: Perforated-patch recording and whole-cell voltage clamp techniques were applied in isolated rat ventricular myocytes. Results: (1) GSRd reduced I-Ca,I-L peak amplitude in a concentration-dependent manner [half-maximal inhibitory concentration (IC50) = 32.4 +/- 7.1 mu mol/L] and up-shifted the currentvoltage (I-V) curve. (2) GSRd (30 mu mol/L) significantly changed the steady-state activation curve of I-Ca,I-L (V-0.5: -19.12 +/- 0.68 vs. -16.26 +/- 0.38 mV; n = 5, p < 0.05) and slowed down the recovery of I-Ca,I-L from inactivation [the time content (zeta) from 91 ms to 136 ms, n = 5, p < 0.01]. (3) A more significant inhibitive effect of GSRd (100 mu mol/L) was identified in perforated-patch recording when compared with whole-cell recording [65.7 +/- 3.2% (n = 10) vs. 31.4 +/- 5.2% (n = 5), p < 0.01]. (4) Pertussis toxin (G(i) protein inhibitor) completely abolished the ICa,L inhibition induced by GSRd. There was a significant difference in inhibition potency between the two cyclic adenosine monophosphate elevating agents (isoprenaline and forskolin) prestimulation [55 +/- 7.8% (n = 5) vs. 17.2 +/- 3.5% (n = 5), p < 0.01]. (5) 1H-[1,2,4]Oxadiazolo[4,3-alpha]-quinoxalin-1-one (a guanylate cyclase inhibitor) and N-acetyl-l-cysteine (a nitric oxide scavenger) partly recovered the I-Ca,I-L inhibition induced by GSRd. (6) Phorbol-12-myristate-13-acetate (a protein kinase C activator) and GF109203X (a protein kinase C inhibitor) did not contribute to the inhibition of GSRd. Conclusion: These findings suggest that GSRd could inhibit I-Ca,I-L through pertussis toxin-sensitive G protein (G(i)) and a nitric oxidecyclic guanosine monophosphate-dependent mechanism. Copyright (C) 2014, The Korean Society of Ginseng, Published by Elsevier. All rights reserved.
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外文
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中科院(CAS)分区：
出版当年[2014]版：
大类|3 区化学
小类|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 区全科医学与补充医学
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出版当年[2013]版：
Q3CHEMISTRY, MEDICINAL
最新[2023]版：
Q1CHEMISTRY, MEDICINALQ1INTEGRATIVE & COMPLEMENTARY MEDICINE
第一作者单位：[1]Capital Med Univ, Beijing Friendship Hosp, Dept Otorhinolaryngol, Beijing 100050, Peoples R China
通讯作者：
通讯机构：[1]Capital Med Univ, Beijing Friendship Hosp, Dept Otorhinolaryngol, Beijing 100050, Peoples R China[*1]Capital Med Univ, Beijing Friendship Hosp, Dept Otorhinolaryngol, 95 Yongan Rd, Beijing 100050, Peoples R China
推荐引用方式(GB/T 7714)：
Lu Cheng,Sun Zhijun,Wang Line.Inhibition of L-type Ca2+ current by ginsenoside Rd in rat ventricular myocytes[J].JOURNAL of GINSENG RESEARCH.2015,39(2):169-177.doi:10.1016/j.jgr.2014.11.003.
APA：
Lu, Cheng,Sun, Zhijun&Wang, Line.(2015).Inhibition of L-type Ca2+ current by ginsenoside Rd in rat ventricular myocytes.JOURNAL of GINSENG RESEARCH,39,(2)
MLA：
Lu, Cheng,et al."Inhibition of L-type Ca2+ current by ginsenoside Rd in rat ventricular myocytes".JOURNAL of GINSENG RESEARCH 39..2(2015):169-177
