• Journal of Ginseng Research
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• 제39권4호
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• pp.314-321
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• 2015

Background: Ginseng belongs to the genus Panax. Its main active ingredients are the ginsenosides. Interstitial cells of Cajal (ICCs) are the pacemaker cells of the gastrointestinal (GI) tract. To understand the effects of ginsenoside Re (GRe) on GI motility, the authors investigated its effects on the pacemaker activity of ICCs of the murine small intestine. Methods: Interstitial cells of Cajal were dissociated from mouse small intestines by enzymatic digestion. The whole-cell patch clamp configuration was used to record pacemaker potentials in cultured ICCs. Changes in cyclic guanosine monophosphate (cGMP) content induced by GRe were investigated. Results: Ginsenoside Re ($20-40{\mu}M$) decreased the amplitude and frequency of ICC pacemaker activity in a concentration-dependent manner. This action was blocked by guanosine 50-[${\beta}-thio$]diphosphate [a guanosine-5'-triphosphate (GTP)-binding protein inhibitor] and by glibenclamide [an adenosine triphosphate (ATP)-sensitive $K^{+}$ channel blocker]. To study the GRe-induced signaling pathway in ICCs, the effects of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (a guanylate cyclase inhibitor) and RP-8-CPT-cGMPS (a protein kinase G inhibitor) were examined. Both inhibitors blocked the inhibitory effect of GRe on ICC pacemaker activity. L-NG-nitroarginine methyl ester ($100{\mu}M$), which is a nonselective nitric oxide synthase (NOS) inhibitor, blocked the effects of GRe on ICC pacemaker activity and GRe-stimulated cGMP production in ICCs. Conclusion: In cultured murine ICCs, GRe inhibits the pacemaker activity of ICCs via the ATP-sensitive potassium ($K^{+}$) channel and the cGMP/NO-dependent pathway. Ginsenoside Re may be a basis for developing novel spasmolytic agents to prevent or alleviate GI motility dysfunction.

• 생명과학회지
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• 제29권9호
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• pp.1010-1015
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• 2019

카할세포는 위장관에서 향도잡이 역할을 한다. 본연구에서는 생쥐 소장 카할세포에서 발생되는 향도잡이 기능에서 올란자핀의 역할을 연구하였다. 패치클램프 방법을 사용하여 향도잡이 전압을 측정하였다. 올란자핀에 의해서 카할세포 향도잡이 전압이 탈분극 되었으며, 이 탈분극은 무스카린성 3번 수용체 억제제에 의해서 억제 되었다. 세포내 $GDP{\beta}S$을 넣어주니 올란자핀에 의해 향도잡이 전압 탈분극이 억제되었다. 또한, 세포밖 $Na^+$ 농도 감소와 비선택성 양이온 통로 억제제에 의해서 올란자핀에 의한 향도잡이 전압 탈분극이 억제 되었다. 세포내 PLC기전의 억제제인 U-73122에 의해서 올란자핀에 의한 향도잡이 전압 탈분극이 억제 되었다. 이러한 결과로 올란자핀은 무스카린성 3번 수용체를 통해서 세포내 G 단백질과 PLC기전 및 세포밖 $Na^+$이 관여함을 알 수 있었다. 따라서 올란자핀은 카할세포를 통해서 장운동성을 조절 할 수 있을 것으로 생각된다.

• 전기학회논문지P
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• 제66권4호
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• pp.188-193
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• 2017

In this paper, a ZVS-PWM high-frequency inverter with a PWM control function is applied to commercial system 220[Vrms], and a resonator type ZVS-PWM high-frequency inverter circuit with a fixed-two methods were proposed. The parameters of the transformer model equivalent circuit of a copier fixing device, which is an essential element in the parameter optimization of the proposed circuit, are obtained by using a high-frequency amplifier and its frequency characteristics are described. The proposed method compared to the existing single-ended ZVS-PFM high frequency inverter can suppress the voltage and current peak value of the power semiconductor switching device and reduce the switching loss. The efficiency of the proposed method itself is 98[%] at rated power output. Also, the efficiency of 96[%] can be obtained even at low output, so that the proposed high frequency inverter is very efficient inverter. The total efficiency from the commercial AC input to the inverter output is 93[%] at rated, which is considered efficient for use in copying machines. In addition, the diode bridge loss accounts for the largest portion of the overall system efficiency distribution. On the other hand, the nonparallel filter has a very low loss.

• The Korean Journal of Physiology and Pharmacology
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• 제24권4호
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• pp.363-372
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• 2020

Gardenia jasminoides (GJ) is a widely used herbal medicine with anti-inflammatory properties, but its effects on the ORAI1 channel, which is important in generating intracellular calcium signaling for T cell activation, remain unknown. In this study, we investigated whether 70% ethanolic GJ extract (GJ_EtOH) and its subsequent fractions inhibit ORAI1 and determined which constituents contributed to this effect. Whole-cell patch clamp analysis revealed that GJ_EtOH (64.7% ± 3.83% inhibition at 0.1 mg/ml) and all its fractions showed inhibitory effects on the ORAI1 channel. Among the GJ fractions, the hexane fraction (GJ_HEX, 66.8% ± 9.95% at 0.1 mg/ml) had the most potent inhibitory effects in hORAI1-hSTIM1 co-transfected HEK293T cells. Chemical constituent analysis revealed that the strong ORAI1 inhibitory effect of GJ_HEX was due to linoleic acid, and in other fractions, we found that genipin inhibited ORAI1. Genipin significantly inhibited I_ORAI1 and interleukin-2 production in CD3/CD28-stimulated Jurkat T lymphocytes by 35.9% ± 3.02% and 54.7% ± 1.32% at 30 μM, respectively. Furthermore, the same genipin concentration inhibited the proliferation of human primary CD4⁺ T lymphocytes stimulated with CD3/CD28 antibodies by 54.9% ± 8.22%, as evaluated by carboxyfluorescein succinimidyl ester assay. Our findings suggest that genipin may be one of the active components of GJ responsible for T cell suppression, which is partially mediated by activation of the ORAI1 channel. This study helps us understand the mechanisms of GJ in the treatment of inflammatory diseases.

• Archives of Pharmacal Research
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• 제26권1호
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• pp.28-33
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• 2003

Ginsenosides, major active ingredients of Panax ginseng, are known to regulate excitatory ligand-gated ion channel activity such as nicotinic acetylcholine and NMDA receptor channel activity. However, it is not known whether ginsenosides affect inhibitory ligand-gated ion channel activity. We investigated the effect of ginsenosides 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. Among the eight individual ginsenosides examined, namely, $Rb_1$, $Rb_2$, Rc, Rd, Re, Rf, $Rg_1$ and $Rg_2$, we found that Rc most potently enhanced the GABA-induced inward peak current ($I_{GABA}$). Ginsenoside Rc alone induced an inward membrane current in certain batches of oocytes expressing the $GABA_A$ receptor. The effect of ginsenoside Rc on $I_{GABA}$ was both dose-dependent and reversible. The half-stimulatory concentration ($EC_{50}$) of ginsenoside Rc was 53.2$\pm$12.3 $\mu$M. Both bicuculline, a $GABA_A$ receptor antagonist, and picrotoxin, a $GABA_A$ channel blocker, blocked the stimulatory effect of ginsenoside Rc on $I_{GABA}$. Niflumic acid (NFA) and 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS), both $CI^{-1}$ channel blockers, attenuated the effect of ginsenoside Rc on I$I_{GABA}$. This study suggests that ginsenosides regulated $GABA_A$ receptor expressed in Xenopus oocytes and implies that this regulation might be one of the pharmacological actions of Panax ginseng.

• Journal of Power Electronics
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• 제5권3호
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• pp.233-239
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• 2005

In this paper, a new conceptual circuit configuration of a 3-phase voltage source, soft switching AC-DC-AC converter using an IGBT module, which has one ARCPL circuit and one ARDCL circuit, is presented. In actuality, the ARCPL circuit is applied in the 3-phase voltage source rectifier side, and the ARDCL circuit is in the inverter side. And more, each power semiconductor device has a novel clamp snubber circuit, which can save the power semiconductor device from voltage and current across each power device. The proposed soft switching circuits have only two active power semiconductor devices. These ARCPL and ARDCL circuits consist of fewer parts than the conventional soft switching circuit. Furthermore, the proposed 3-phase voltage source soft switching AC-DC-AC power conversion system needs no additional sensor for complete soft switching as compared with the conventional 3-phase voltage source AC-DC-AC power conversion system. In addition to this, these soft switching circuits operate only once in one sampling term. Therefore, the power conversion efficiency of the proposed AC-DC-AC converter system will get higher than a conventional soft switching converter system because of the reduced ARCPL and ARDCL circuit losses. The operation timing and terms for ARDCL and ARCPL circuits are calculated and controlled by the smoothing DC capacitor voltage and the output AC current. Using this control, the loss of the soft switching circuits are reduced owing to reduced resonant inductor current in ARCPL and ARDCL circuits as compared with the conventional controlled soft switching power conversion system. The operating performances of proposed soft switching AC-DC-AC converter treated here are evaluated on the basis of experimental results in a 50kVA setup in this paper. As a result of experiment on the 50kVA system, it was confirmed that the proposed circuit could reduce conduction noise below 10 MHz and improve the conversion efficiency from 88. 5% to 90.5%, when compared with the hard switching circuit.

• 전력전자학회논문지
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• 제10권4호
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• pp.380-387
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• 2005

본 논문에서는 능동 클램프형 포워드 DC-DC 컨버터를 이용하여 저전압 대전류에 적합한 고전력밀도의 개방형 전원 장치를 구성하고 그 특성에 대해 보고한 것이다. 전원장치의 입력전압은 통신기용에 적합한 36-75V이며, 출력은 3.3V, 100W급으로 하였다. 대전류에서 전도손실을 저감시키기 위해서 동기정류 방식을 사용하였으며 시스템의 과전류 보호기능을 향상시키기 위해서 고정밀 PCB 저항을 이용한 정전류제어기가 이용되었다. 시험용 전원장치는 통신기용 온보드 전원장치에 적합하도록 높이를 8m 이하, 크기는 quarter brick (58x37mm) 사이즈로 제작되었으며 그 결과 $95W/in^3$ 이상의 전력밀도와 90.6$\%$의 효율, 0.07$\%$ 이하의 전압안정도를 구현하였다.

• 전력전자학회논문지
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• 제16권3호
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• pp.242-249
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• 2011

제안하는 컨버터는 부스트 하프브리지-전압 더블러를 각각 병렬-직렬로 연결하여 출력전력 및 출력전압을 증대시키므로 고승압 대전력 응용에서 소자의 선정이 용이하다. 특히 고주파변압기 턴 비를 작게 할 수 있고 DC 오프셋이 제거되어 최적의 변압기 설계가 가능하며, 3개의 코아로 전력이 분배되어 Low Profile 및 열 분산에 유리하다. 제안하는 컨버터는 전 영역(0 ∼ 1)의 듀티 사용으로 스타트업 및 추가의 클램프회로가 필요 없으며 입력전압 변동이 큰 응용에 적합하다. 또한 넓은 듀티영역에서 스위치의 ZVS 턴온과 다이오드의 ZCS 턴온 턴오프가 성취되므로 고효율을 달성할 수 있다. 제안하는 컨버터를 5 kW급 시작품으로 검증하였다.

• The Korean Journal of Physiology and Pharmacology
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• 제24권6호
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• pp.545-553
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• 2020

Aripiprazole is a quinolinone derivative approved as an atypical antipsychotic drug for the treatment of schizophrenia and bipolar disorder. It acts as with partial agonist activities at the dopamine D2 receptors. Although it is known to be relatively safe for patients with cardiac ailments, less is known about the effect of aripiprazole on voltage-gated ion channels such as transient A-type K⁺ channels, which are important for the repolarization of cardiac and neuronal action potentials. Here, we investigated the effects of aripiprazole on Kv1.4 currents expressed in HEK293 cells using a whole-cell patch-clamp technique. Aripiprazole blocked Kv1.4 channels in a concentration-dependent manner with an IC₅₀ value of 4.4 μM and a Hill coefficient of 2.5. Aripiprazole also accelerated the activation (time-to-peak) and inactivation kinetics. Aripiprazole induced a voltage-dependent (δ = 0.17) inhibition, which was use-dependent with successive pulses on Kv1.4 currents without altering the time course of recovery from inactivation. Dehydroaripiprazole, an active metabolite of aripiprazole, inhibited Kv1.4 with an IC₅₀ value of 6.3 μM (p < 0.05 compared with aripiprazole) with a Hill coefficient of 2.0. Furthermore, aripiprazole inhibited Kv4.3 currents to a similar extent in a concentration-dependent manner with an IC₅₀ value of 4.9 μM and a Hill coefficient of 2.3. Thus, our results indicate that aripiprazole blocked Kv1.4 by preferentially binding to the open state of the channels.

• The Korean Journal of Physiology and Pharmacology
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• 제23권5호
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• pp.381-392
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• 2019

Sperm function and male fertility are closely related to pH dependent $K^+$ current (KSper) in human sperm, which is most likely composed of Slo3 and its auxiliary subunit leucine-rich repeat-containing protein 52 (LRRC52). Onion peel extract (OPE) and its major active ingredient quercetin are widely used as fertility enhancers; however, the effect of OPE and quercetin on Slo3 has not been elucidated. The purpose of this study is to investigate the effect of quercetin on human Slo3 channels. Human Slo3 and LRRC52 were co-transfected into HEK293 cells and pharmacological properties were studied with the whole cell patch clamp technique. We successfully expressed and measured pH sensitive and calcium insensitive Slo3 currents in HEK293 cells. We found that OPE and its key ingredient quercetin inhibit Slo3 currents. Inhibition by quercetin is dose dependent and this degree of inhibition decreases with elevating internal alkalization and internal free calcium concentrations. Functional moieties in the quercetin polyphenolic ring govern the degree of inhibition of Slo3 by quercetin, and the composition of such functional moieties are sensitive to the pH of the medium. These results suggest that quercetin inhibits Slo3 in a pH and calcium dependent manner. Therefore, we surmise that quercetin induced depolarization in spermatozoa may enhance the voltage gated proton channel (Hv1), and activate non-selective cation channels of sperm (CatSper) dependent calcium influx to trigger sperm capacitation and acrosome reaction.