• Title/Summary/Keyword: Inward current

Search Result 134, Processing Time 0.02 seconds

Effects of Ginsenoside Metabolites on GABAA Receptor-Mediated Ion Currents

  • Lee, Byung-Hwan;Choi, Sun-Hye;Shin, Tae-Joon;Hwang, Sung-Hee;Kang, Ji-Yeon;Kim, Hyeon-Joong;Kim, Byung-Ju;Nah, Seung-Yeol
    • Journal of Ginseng Research
    • /
    • v.36 no.1
    • /
    • pp.55-60
    • /
    • 2012
  • In a previous report, we demonstrated that ginsenoside Rc, one of major ginsenosides from Panax ginseng, enhances ${\gamma}$-aminobutyric acid (GABA) $receptor_A$ ($GABA_A$)-mediated ion channel currents. However, little is known about the effects of ginsenoside metabolites on $GABA_A$ receptor channel activity. The present study investigated the effects of ginsenoside metabolites on human recombinant $GABA_A$ receptor (${\alpha}_1{\beta}_1{\gamma}_{2s}$) channel activity expressed in Xenopus oocytes using a two-electrode voltage clamp technique. M4, a metabolite of protopanaxatriol ginsenosides, more potently inhibited the GABA-induced inward peak current ($I_{GABA}$) than protopanaxadiol (PPD), a metabolite of PPD ginsenosides. The effect of M4 and PPD on $I_{GABA}$ was both concentration-dependent and reversible. The half-inhibitory concentration ($IC_{50}$) values of M4 and PPD were 17.1${\pm}$2.2 and 23.1${\pm}$8.6 ${\mu}M$, respectively. The inhibition of $I_{GABA}$ by M4 and PPD was voltage-independent and non-competitive. This study implies that the regulation of $GABA_A$ receptor channel activity by ginsenoside metabolites differs from that of ginsenosides.

The Inhibitory Effects of Korean Red Ginseng Saponins on 5- HT3A Receptor Channel Activity Are Coupled to Anti-Nausea and Anti-Vomiting Action

  • Kim Jong-Hoon;Lee Byung-Hwan;Jeong Sang Min;Nah Seung-Yeol
    • Journal of Ginseng Research
    • /
    • v.29 no.1
    • /
    • pp.37-43
    • /
    • 2005
  • We performed in vitro and in vivo studies to know whether the inhibitory effects of ginsenosides on $5-HT_{3A}$ receptor channel acctivity are coupled to anti-nausea and anti-vomiting action. In vitro study, we investigated the effect of compound K (CK) and M4, which are ginsenoside metabolites, on human $5-HT_{3A}$ receptor channel activity expressed in Xenopus oocytes using two-electrode voltage clamp technique. Treatment of CK or M4 themselves had no effect in both oocytes injected with $H_2O\;and\;5-HT_{3A}$ receptor cRNA. In oocytes injected with $5- HT_{3A}$ receptor cRNA, M4 treatment inhibited more potently 5-HT-induced inward peak current $(I_{5-HT})$ than CK with dose-dependent and reversible manner. The half-inhibitory concentrations $(IC_{50})$ of CK and M4 were $36.9\;\pm\;10.1\;and\;7.3\;\pm\;2.2\;{\mu}M$, respectively. The inhibition of $I_{5-HT}$ by M4 was non-competitive and voltage-independent. These results indicate that M4 might regulate $5-HT_{3A}$ receptors. In vivo experiments, injection of cisplatin (7.5 mg/kg, i.v.) induced both nausea and vomiting with 1 h latency. These episodes reached to peak after 2 h and persisted for 4 h. Pre-treatment of GTS (500 mg/kg, p.o.) significantly reduced cisplatin-induced nausea and vomiting by $51\;\pm\;8.4\;and\;48.8\;\pm\;6.4\%$ during 4 h compared to GIS­untreated group, respectively. These results show the possibility that in vitro inhibition of $5-HT_{3A}$ receptor channel activity by ginsenosides might be coupled to in vivo anti-emetic activity.

Identification of Chloride Channels in Hamster Eggs (햄스터 난자에서 존재하는 Chloride 통로)

  • Kim, Y.-M.;Kim, J.-S.;Hong, S.-G.
    • Journal of Embryo Transfer
    • /
    • v.19 no.2
    • /
    • pp.101-112
    • /
    • 2004
  • Chloride($Cl^-$) channels play critical roles in cell homeostasis and its specific functions such as volume regulation, differentiation, secretion, and membrane stabilization. The presence of these channels have been reported in all kinds of cells and even in frog oocytes. These essential role of $Cl^-$­ channels in cell homeostasis possibly play any role in egg homeostasis and in the early stage of development, however, there has been no report about the presence of $Cl^-$­ channel in the mammalian oocyte. This study was performed to elucidate the presence of $Cl^-$­ channels in hamster eggs. When allowing only $Cl^-$­ to pass through the channel of the egg membrane by using impermeant cation such as N-methyl-D-glucamine(NMDG), single channel currents were recorded. These channel currents showed typical long-lasted openings interrupted by rapid flickering. Mean open $time({\tau}o)$ was 43${\pm}$10.14 ms(n=9, at 50 mV). The open probability(Po) was decrease with depolarization. The current-voltage relation showed outward rectification. Outward slop conductance(32${\pm}$5.4 pS, n=22) was steeper than the inward slop conductance(10${\pm}$1.3 pS). Under the condition of symmetrical 140 mM NaCl, single channel currents were reversed at 0 mV(n=4). This reversal potential(Erev) was shifted from 0 mV at 140 mM concentration of internal NaCl(140 mM [Na+]i) to ­9.8${\pm}$0.5 mV(n=4) at 70 mM [Na+]i and 11.5${\pm}$1.9 mV at 280 mM [Na+]i(n=4) respectively, strongly suggesting that these are single $Cl^-$­ channel currents. To examine further whether this channel has pharmacological property of the $Cl^-$­ channel, specific Cl­ channel blockers, IAA-94(Indanyloxyacetic acid-94) and DIDS(4, 4'-diisothiocyan ostillben- 2-2'disulfonic acid) were applied. IAA-94 inhibited the channel current in a dose-dependent manner and revealed a rapid and flickering block. From these electrophysiological and pharmacological resluts, we found the novel $Cl^-$­ channel present in the hamster oocyte membrane. The first identification of $Cl^-$­ channel in the hamster oocyte may give a clue for the further study on the function of $Cl^-$­ channel in the fertilization and cell differentiation.

Seasonal Circulation and Estuarine Characteristics in the Jinhae and Masan Bay from Three-Dimensional Numerical Experiments (3차원 수치모의 실험을 통한 진해·마산만의 계절별 해수순환과 염하구 특성)

  • JIHA KIM;BYOUNG-JU CHOI;JAE-SUNG CHOI;HO KYUNG HA
    • The Sea:JOURNAL OF THE KOREAN SOCIETY OF OCEANOGRAPHY
    • /
    • v.29 no.2
    • /
    • pp.77-100
    • /
    • 2024
  • Circulation, tides, currents, harmful algal blooms, water quality, and hypoxic conditions in Jinhae-Masan Bay have been extensively studied. However, these previous studies primarily focused on short-term variations, and there was limited detailed investigation into the physical mechanisms responsible for ocean circulation in the bays. Oceanic processes in the bays, such as pollutant dispersal, changes on a seasonal time scale. Therefore, this study aimed to understand how the circulation in Jinhae-Masan Bay varies seasonally and to examine the effects of tides, winds, and river discharges on regional ocean circulation. To achieve this, a three-dimensional ocean circulation model was used to simulate circulation patterns from 2016 to 2018, and sensitivity experiments were conducted. This study reveals that convective estuarine circulation develops in Jinhae and Masan Bays, characterized by the inflow of deep oceanic water from the Korea Strait through Gadeoksudo, while surface water flows outward. This deep water intrusion divides into northward and westward branches. In this study, the volume transport was calculated along the direction of bottom channels in each region. The meridional water exchange in the eastern region of Jinhae Bay is 2.3 times greater in winter and 1.4 times greater in summer compared to that of zonal exchange in the western region. In the western region of Jinhae Bay, the circulation pattern varies significantly by season due to changes in the balance of forces. During winter, surface currents flow southward and bottom currents flow northward, strengthening the north-south convective circulation due to the combined effects of northwesterly winds and the slope of the sea surface. In contrast, during summer, southwesterly winds cause surface seawater to flow eastward, and the elevated sea surface in the southeastern part enhances northward barotropic pressure gradient intensifying the eastward surface flow. The density gradient and southward baroclinic pressure gradient increase in the lower layer, causing a strong westward inflow of seawater from Gadeoksudo, enhancing the zonal convective circulation by 26% compared to winter. The convective circulation in the western Jinhae Bay is significantly influenced by both tidal current and wind during both winter and summer. In the eastern Jinhae Bay and Masan Bay, surface water flows outward to the open sea in all seasons, while bottom water flows inward, demonstrating a typical convective estuarine circulation. In winter, the contributions of wind and freshwater influx are significant, while in summer, the influence of mixing by tidal currents plays a major role in the north-south convective circulation. In the eastern Jinhae Bay, tidally driven residual circulation patterns, influenced by the local topography, are distinct. The study results are expected to enhance our understanding of pollutant dispersion, summer hypoxic events, and the abundance of red tide organisms in these bays.