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Open AccessArticle

Inhibitory Effectiveness of Gomisin A, a Dibenzocyclooctadiene Lignan Isolated from Schizandra chinensis, on the Amplitude and Gating of Voltage-Gated Na+ Current

by 1,2,3 and 4,5,6,*
1
Institute of Clinical Medicine, College of Medicine, National Cheng Kung University, Tainan 70101, Taiwan
2
Chi-Mei Medical Center, Division of Cardiovascular Medicine, Tainan 71004, Taiwan
3
Department of Biotechnology, Southern Taiwan University of Science and Technology, Tainan 71004, Taiwan
4
Department of Physiology, National Cheng Kung University Medical College, No. 1, University Road, Tainan 70101, Taiwan
5
Institute of Basic Medical Sciences, National Cheng Kung University Medical College, Tainan 70101, Taiwan
6
Department of Medical Research, China Medical University Hospital, China Medical University, Taichung 709, Taiwan
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(22), 8816; https://doi.org/10.3390/ijms21228816
Received: 1 November 2020 / Revised: 18 November 2020 / Accepted: 19 November 2020 / Published: 21 November 2020
(This article belongs to the Section Bioactives and Nutraceuticals)
Gomisin A (Gom A), a lignan isolated from Schisandra chinensis, has been reported produce numerous biological activities. However, its action on the ionic mechanisms remains largely unanswered. The present experiments were undertaken to investigate the possible perturbations of Gom A or other related compounds on different types of membrane ionic currents in electrically excitable cells (i.e., pituitary GH3 and pancreatic INS-1 cells). The exposure to Gom A led to the differential inhibition of peak and end-pulse components of voltage-gated Na+ current (INa) in GH3 cells with effective IC50 of 6.2 and 0.73 μM, respectively. The steady-state inactivation curve of INa in the presence of Gom A was shifted towards a more hyperpolarized potential. However, neither changes in the overall current-voltage relationship nor those for the gating charge of the current were demonstrated. The application of neither morin (10 μM) nor hesperidin (10 μM) perturbed the strength of INa, while sesamine could suppress it. However, in the continued presence of Gom A, the addition of sesamine failed to suppress INa further. Gom A also effectively suppressed the strength of persistent INa activated by long ramp voltage command, and further application of tefluthrin effectively attenuated Gom A-mediated inhibition of the current. The presence of Gom A mildly inhibited erg-mediated K+ current, while a lack of change in the amplitude of hyperpolarization-activated cation current was observed in its presence. Under cell-attached current recordings, the exposure to Gom A resulted in the decreased firing of spontaneous action currents with a minimal change in AC amplitude. In pancreatic INS-1 cells, the presence of Gom A was also noticed to inhibit peak and end-pulse components of INa differentially with the IC50 of 5.9 and 0.84 μM, respectively. Taken together, the emerging results presented herein provide the evidence that Gom A can differentially inhibit peak and sustained INa in endocrine cells (e.g., GH3 and INS-1 cells). View Full-Text
Keywords: Gomisin A; voltage-gated Na+ current; erg-mediated K+ current; current kinetics; action current; excitable cell Gomisin A; voltage-gated Na+ current; erg-mediated K+ current; current kinetics; action current; excitable cell
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Chang, W.-T.; Wu, S.-N. Inhibitory Effectiveness of Gomisin A, a Dibenzocyclooctadiene Lignan Isolated from Schizandra chinensis, on the Amplitude and Gating of Voltage-Gated Na+ Current. Int. J. Mol. Sci. 2020, 21, 8816.

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