Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes
Cinobufagin (CBG), a major bioactive ingredient of the bufanolide steroid compounds of Chan Su, has been widely used to treat coronary heart disease. At present, the effect of CBG on the L-type Ca2+ current (ICa-L) of ventricular myocytes remains undefined. The aim of the present study was to charac...
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2014-01-01
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| Series: | The Scientific World Journal |
| Online Access: | http://dx.doi.org/10.1155/2014/496705 |
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| author | Pinya Li Qiongtao Song Tao Liu Zhonglin Wu Xi Chu Xuan Zhang Ying Zhang Yonggang Gao Jianping Zhang Li Chu |
| author_facet | Pinya Li Qiongtao Song Tao Liu Zhonglin Wu Xi Chu Xuan Zhang Ying Zhang Yonggang Gao Jianping Zhang Li Chu |
| author_sort | Pinya Li |
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| description | Cinobufagin (CBG), a major bioactive ingredient of the bufanolide steroid compounds of Chan Su, has been widely used to treat coronary heart disease. At present, the effect of CBG on the L-type Ca2+ current (ICa-L) of ventricular myocytes remains undefined. The aim of the present study was to characterize the effect of CBG on intracellular Ca2+ ([Ca2+]i) handling and cell contractility in rat ventricular myocytes. CBG was investigated by determining its influence on ICa-L, Ca2+ transient, and contractility in rat ventricular myocytes using the whole-cell patch-clamp technique and video-based edge-detection and dual-excitation fluorescence photomultiplier systems. The dose of CBG (10−8 M) decreased the maximal inhibition of CBG by 47.93%. CBG reduced ICa-L in a concentration-dependent manner with an IC50 of 4 × 10−10 M, upshifted the current-voltage curve of ICa-L, and shifted the activation and inactivation curves of ICa-L leftward. Moreover, CBG diminished the amplitude of the cell shortening and Ca2+ transients with a decrease in the time to peak (Tp) and the time to 50% of the baseline (Tr). CBG inhibited L-type Ca2+ channels, and reduced [Ca2+]i and contractility in adult rat ventricular myocytes. These findings contribute to the understanding of the cardioprotective efficacy of CBG. |
| format | Article |
| id | doaj-art-83132912482b4d7aaaba87c7cd4fb32a |
| institution | Kabale University |
| issn | 2356-6140 1537-744X |
| language | English |
| publishDate | 2014-01-01 |
| publisher | Wiley |
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| series | The Scientific World Journal |
| spelling | doaj-art-83132912482b4d7aaaba87c7cd4fb32a2025-02-03T05:43:54ZengWileyThe Scientific World Journal2356-61401537-744X2014-01-01201410.1155/2014/496705496705Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular MyocytesPinya Li0Qiongtao Song1Tao Liu2Zhonglin Wu3Xi Chu4Xuan Zhang5Ying Zhang6Yonggang Gao7Jianping Zhang8Li Chu9Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaHebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaHebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaThe Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei 050011, ChinaThe Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei 050011, ChinaDepartment of Pharmacology, Hebei University of Chinese Medicine, Shijiazhuang, Hebei 050200, ChinaHebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaHebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaHebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaHebei Medical University, 361 East Zhongshan Road, Shijiazhuang, Hebei 050017, ChinaCinobufagin (CBG), a major bioactive ingredient of the bufanolide steroid compounds of Chan Su, has been widely used to treat coronary heart disease. At present, the effect of CBG on the L-type Ca2+ current (ICa-L) of ventricular myocytes remains undefined. The aim of the present study was to characterize the effect of CBG on intracellular Ca2+ ([Ca2+]i) handling and cell contractility in rat ventricular myocytes. CBG was investigated by determining its influence on ICa-L, Ca2+ transient, and contractility in rat ventricular myocytes using the whole-cell patch-clamp technique and video-based edge-detection and dual-excitation fluorescence photomultiplier systems. The dose of CBG (10−8 M) decreased the maximal inhibition of CBG by 47.93%. CBG reduced ICa-L in a concentration-dependent manner with an IC50 of 4 × 10−10 M, upshifted the current-voltage curve of ICa-L, and shifted the activation and inactivation curves of ICa-L leftward. Moreover, CBG diminished the amplitude of the cell shortening and Ca2+ transients with a decrease in the time to peak (Tp) and the time to 50% of the baseline (Tr). CBG inhibited L-type Ca2+ channels, and reduced [Ca2+]i and contractility in adult rat ventricular myocytes. These findings contribute to the understanding of the cardioprotective efficacy of CBG.http://dx.doi.org/10.1155/2014/496705 |
| spellingShingle | Pinya Li Qiongtao Song Tao Liu Zhonglin Wu Xi Chu Xuan Zhang Ying Zhang Yonggang Gao Jianping Zhang Li Chu Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes The Scientific World Journal |
| title | Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes |
| title_full | Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes |
| title_fullStr | Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes |
| title_full_unstemmed | Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes |
| title_short | Inhibitory Effect of Cinobufagin on L-Type Ca2+ Currents, Contractility, and Ca2+ Homeostasis of Isolated Adult Rat Ventricular Myocytes |
| title_sort | inhibitory effect of cinobufagin on l type ca2 currents contractility and ca2 homeostasis of isolated adult rat ventricular myocytes |
| url | http://dx.doi.org/10.1155/2014/496705 |
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