Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs
The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp te...
Ausführliche Beschreibung
Autor*in: |
JIN, Si-Si [verfasserIn] |
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Format: |
E-Artikel |
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Sprache: |
Englisch |
Erschienen: |
2015transfer abstract |
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Umfang: |
7 |
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Übergeordnetes Werk: |
Enthalten in: Generalized Galilean algebras and Newtonian gravity - González, N. ELSEVIER, 2016transfer abstract, [S.l.] |
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Übergeordnetes Werk: |
volume:13 ; year:2015 ; number:5 ; pages:361-367 ; extent:7 |
Links: |
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DOI / URN: |
10.1016/S1875-5364(15)30027-3 |
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Katalog-ID: |
ELV028965337 |
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520 | |a The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. | ||
520 | |a The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. | ||
650 | 7 | |a Guanfu base A |2 Elsevier | |
650 | 7 | |a Arrhythmia |2 Elsevier | |
650 | 7 | |a Transient sodium current |2 Elsevier | |
650 | 7 | |a Late sodium current |2 Elsevier | |
650 | 7 | |a Kv1.5 current |2 Elsevier | |
700 | 1 | |a GUO, Qiao |4 oth | |
700 | 1 | |a XU, Jing |4 oth | |
700 | 1 | |a YU, Peng |4 oth | |
700 | 1 | |a LIU, Jing-Han |4 oth | |
700 | 1 | |a TANG, Yi-Qun |4 oth | |
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10.1016/S1875-5364(15)30027-3 doi GBVA2015011000009.pica (DE-627)ELV028965337 (ELSEVIER)S1875-5364(15)30027-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 530 VZ 610 VZ 77.50 bkl JIN, Si-Si verfasserin aut Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs 2015transfer abstract 7 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. Guanfu base A Elsevier Arrhythmia Elsevier Transient sodium current Elsevier Late sodium current Elsevier Kv1.5 current Elsevier GUO, Qiao oth XU, Jing oth YU, Peng oth LIU, Jing-Han oth TANG, Yi-Qun oth Enthalten in Elsevier González, N. ELSEVIER Generalized Galilean algebras and Newtonian gravity 2016transfer abstract [S.l.] (DE-627)ELV014077353 volume:13 year:2015 number:5 pages:361-367 extent:7 https://doi.org/10.1016/S1875-5364(15)30027-3 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA GBV_ILN_11 GBV_ILN_22 GBV_ILN_40 77.50 Psychophysiologie VZ AR 13 2015 5 361-367 7 045F 610 |
spelling |
10.1016/S1875-5364(15)30027-3 doi GBVA2015011000009.pica (DE-627)ELV028965337 (ELSEVIER)S1875-5364(15)30027-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 530 VZ 610 VZ 77.50 bkl JIN, Si-Si verfasserin aut Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs 2015transfer abstract 7 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. Guanfu base A Elsevier Arrhythmia Elsevier Transient sodium current Elsevier Late sodium current Elsevier Kv1.5 current Elsevier GUO, Qiao oth XU, Jing oth YU, Peng oth LIU, Jing-Han oth TANG, Yi-Qun oth Enthalten in Elsevier González, N. ELSEVIER Generalized Galilean algebras and Newtonian gravity 2016transfer abstract [S.l.] (DE-627)ELV014077353 volume:13 year:2015 number:5 pages:361-367 extent:7 https://doi.org/10.1016/S1875-5364(15)30027-3 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA GBV_ILN_11 GBV_ILN_22 GBV_ILN_40 77.50 Psychophysiologie VZ AR 13 2015 5 361-367 7 045F 610 |
allfields_unstemmed |
10.1016/S1875-5364(15)30027-3 doi GBVA2015011000009.pica (DE-627)ELV028965337 (ELSEVIER)S1875-5364(15)30027-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 530 VZ 610 VZ 77.50 bkl JIN, Si-Si verfasserin aut Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs 2015transfer abstract 7 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. Guanfu base A Elsevier Arrhythmia Elsevier Transient sodium current Elsevier Late sodium current Elsevier Kv1.5 current Elsevier GUO, Qiao oth XU, Jing oth YU, Peng oth LIU, Jing-Han oth TANG, Yi-Qun oth Enthalten in Elsevier González, N. ELSEVIER Generalized Galilean algebras and Newtonian gravity 2016transfer abstract [S.l.] (DE-627)ELV014077353 volume:13 year:2015 number:5 pages:361-367 extent:7 https://doi.org/10.1016/S1875-5364(15)30027-3 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA GBV_ILN_11 GBV_ILN_22 GBV_ILN_40 77.50 Psychophysiologie VZ AR 13 2015 5 361-367 7 045F 610 |
allfieldsGer |
10.1016/S1875-5364(15)30027-3 doi GBVA2015011000009.pica (DE-627)ELV028965337 (ELSEVIER)S1875-5364(15)30027-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 530 VZ 610 VZ 77.50 bkl JIN, Si-Si verfasserin aut Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs 2015transfer abstract 7 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. Guanfu base A Elsevier Arrhythmia Elsevier Transient sodium current Elsevier Late sodium current Elsevier Kv1.5 current Elsevier GUO, Qiao oth XU, Jing oth YU, Peng oth LIU, Jing-Han oth TANG, Yi-Qun oth Enthalten in Elsevier González, N. ELSEVIER Generalized Galilean algebras and Newtonian gravity 2016transfer abstract [S.l.] (DE-627)ELV014077353 volume:13 year:2015 number:5 pages:361-367 extent:7 https://doi.org/10.1016/S1875-5364(15)30027-3 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA GBV_ILN_11 GBV_ILN_22 GBV_ILN_40 77.50 Psychophysiologie VZ AR 13 2015 5 361-367 7 045F 610 |
allfieldsSound |
10.1016/S1875-5364(15)30027-3 doi GBVA2015011000009.pica (DE-627)ELV028965337 (ELSEVIER)S1875-5364(15)30027-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 530 VZ 610 VZ 77.50 bkl JIN, Si-Si verfasserin aut Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs 2015transfer abstract 7 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. Guanfu base A Elsevier Arrhythmia Elsevier Transient sodium current Elsevier Late sodium current Elsevier Kv1.5 current Elsevier GUO, Qiao oth XU, Jing oth YU, Peng oth LIU, Jing-Han oth TANG, Yi-Qun oth Enthalten in Elsevier González, N. ELSEVIER Generalized Galilean algebras and Newtonian gravity 2016transfer abstract [S.l.] (DE-627)ELV014077353 volume:13 year:2015 number:5 pages:361-367 extent:7 https://doi.org/10.1016/S1875-5364(15)30027-3 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA GBV_ILN_11 GBV_ILN_22 GBV_ILN_40 77.50 Psychophysiologie VZ AR 13 2015 5 361-367 7 045F 610 |
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Antiarrhythmic ionic mechanism of Guanfu base A—Selective inhibition of late sodium current in isolated ventricular myocytes from guinea pigs |
abstract |
The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. |
abstractGer |
The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. |
abstract_unstemmed |
The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (I Na.L), transient sodium current (I Na.T), HERG current (I HERG), and Kv1.5 current (I Kv1.5). The values of I Na.L, I Na.T, IHERG and I Kv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited I Na.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol·L−1, which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol·L−1 for the I Na.T. The inhibitory effect of GFA on I Na,L was not affected by 200 μmol·L−1 H2O2. It inhibited I HERG with an IC50 of (273 ± 34) μmol·L−1 and has slight blocking effect on I Kv1.5, decreasing I Kv1.5 by only 20.6% at 200 μmol·L−1. In summary, GFA inhibited I Na.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders. |
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