• Title/Summary/Keyword: Artificial Ion Channel

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2D-QSAR analysis for hERG ion channel inhibitors (hERG 이온채널 저해제에 대한 2D-QSAR 분석)

  • Jeon, Eul-Hye;Park, Ji-Hyeon;Jeong, Jin-Hee;Lee, Sung-Kwang
    • Analytical Science and Technology
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    • v.24 no.6
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    • pp.533-543
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    • 2011
  • The hERG (human ether-a-go-go related gene) ion channel is a main factor for cardiac repolarization, and the blockade of this channel could induce arrhythmia and sudden death. Therefore, potential hERG ion channel inhibitors are now a primary concern in the drug discovery process, and lots of efforts are focused on the minimizing the cardiotoxic side effect. In this study, $IC_{50}$ data of 202 organic compounds in HEK (human embryonic kidney) cell from literatures were used to develop predictive 2D-QSAR model. Multiple linear regression (MLR), Support Vector Machine (SVM), and artificial neural network (ANN) were utilized to predict inhibition concentration of hERG ion channel as machine learning methods. Population based-forward selection method with cross-validation procedure was combined with each learning method and used to select best subset descriptors for each learning algorithm. The best model was ANN model based on 14 descriptors ($R^2_{CV}$=0.617, RMSECV=0.762, MAECV=0.583) and the MLR model could describe the structural characteristics of inhibitors and interaction with hERG receptors. The validation of QSAR models was evaluated through the 5-fold cross-validation and Y-scrambling test.

Functional Nanochannels to Control Ion Transportation with Monomolecule Selectivity (단일 이온 인식형 이송 제어 기능성 나노채널 기술)

  • Kim, Jeong Hwan;Lee, Eung-Sug;Whang, Kyung-Hyun;Yoo, Yeong-Eun;Yoon, Jae-Sung
    • Transactions of the KSME C: Technology and Education
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    • v.3 no.4
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    • pp.249-255
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    • 2015
  • Functional nanochannels were fabricated in order to control selective ion transportation with high permeability and low energy consumption. In this research, nanochannel platform fabrication process and surface functionalization process were developed. In addition, selective ion transportation and concentration measurement system was also set-up. By using fabricated multilayer metal membrane with electrical bias, 95% of ion ($Cl^-$) was blocked. This developed process is new-conceptional membrane fabrication technology and is expected to be applied to next-generation water purification/desalination, portable artifical kidney, and artificial sense organ.

Characterization of an Ion Channel Prepared from Tomato Roots and Inhibitory Effects by Heavy Metal Ions (토마토 뿌리조직에서 분리한 이온채널의 중금속에 의한 저해)

  • Shin, Dae-Seop;Han, Min-Woo;Kim, Young-Kee
    • Applied Biological Chemistry
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    • v.47 no.4
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    • pp.390-395
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    • 2004
  • In order to characterize ion channels present in tomato roots, microsomes were incorporated into an artificial lipid bilayer arranged for electrophysiological analysis. Of the five different ion channels that could be found, a channel of 450 pS conductance was found most frequently. This channel displayed subconductance states of 450, 257 and 105 pS. All subconductance states showed linear current-voltage relationships. At positive holding potentials, high frequency of transient channel openings was observed; however, at negative potentials, the open times were long and open probability high. Po was 0.83 at -40 mV. When an additional 50 mM $K^+\;or\;Na^+$ was added to the cis side of bilayer, the reversal potentials shifted in the negative direction to near -10 mV. Thus, the 450 pS cation channel selects poorly between $K^+\;and\;Na^+$. In the presence of $100\;{\mu}M$ metal ions, the channel activity was severely inhibited by $La^{3+},\;Ba^{2+},\;and\;Zn^{2+}$, and Po was decreased to 0.2 or even less. However, $Al^{3+}\;and\;Cd^{2+}$ decreased the activity by only 20%. Interestingly, each metal ion showed different kinetics of channel inhibition. While $500\;{\mu}M\;La^{3+}$ inhibited the activities of all subconductance state, 1 mM $Zn^{2+}$ inhibited all except the 105 pS state. $Cd^{2+}$ changed the gating of the channel from a long-opening state to brief transient openings even at negative holding potentials. These data represent that the metal ions may have different binding sites on the channel protein and could be useful modulators and probes to investigate structural characteristics as well as the functional roles of the 450 pS channel on the root physiology.

Field tests of the radiation detectors for environmental radiation monitoring around KORI nuclear power plants (고리원자력 주변 환경방사선 감시를 위한 방사선 측정기의 현장 성능 시험)

  • 최성수;신대용;조규성;하달규
    • 제어로봇시스템학회:학술대회논문집
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    • 1997.10a
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    • pp.1371-1374
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    • 1997
  • We had developed the on-line environmental monitoring system which has installed around Kori Nuclear Power Plants and will be taken the place of the existing system. The system consists of a main computer and 11 sets of radiation monitoring post equipments. Nal(Tl) scintillation detectro was adopted in addition to ion-chamber detector and implemented with DCU(Dose Conversion Unit) and SCA(Single Channel Analyzer). Compared with the existing system, it has revised feature in the radiation measurements which are detection of artificial radioactivity and 2-ways of the radiatiion detectors. The field test trsults show that the developed radiation detecting equipments can measure environmental radiation withn 5.0% of the theoretical value.

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Regulation of Transient Receptor Potential Melastatin 7 (TRPM7) Currents by Mitochondria

  • Kim, Byung Joo;Jeon, Ju-Hong;Kim, Seon Jeong;So, Insuk;Kim, Ki Whan
    • Molecules and Cells
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    • v.23 no.3
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    • pp.363-369
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    • 2007
  • Mitochondria play a central role in energy-generating processes and may be involved in the regulation of channels and receptors. Here we investigated TRPM7, an ion channel and functional kinase, and its regulation by mitochondria. Proton ionophores such as CCCP elicited a rapid decrease in outward TRPM7 whole-cell currents but a slight increase in inward currents with pipette solutions containing no MgATP. With pipette solutions containing 3 mM MgATP, however, CCCP increased both outward and inward TRPM7 currents. This effect was reproducible and fully reversible, and repeated application of CCCP yielded similar decreases in current amplitude. Oligomycin, an inhibitor of $F_1/F_O$-ATP synthase, inhibited outward whole-cell currents but did not affect inward currents. The respiratory chain complex I inhibitor, rotenone, and complex III inhibitor, antimycin A, were without effect as were kaempferol, an activator of the mitochondrial $Ca^{2+}$ uniporter, and ruthenium red, an inhibitor of the mitochondrial $Ca^{2+}$ uniporter. These results suggest that the inner membrane potential (as regulated by proton ionophores) and the $F_1/F_O$-ATP synthase of mitochondria are important in regulating TRPM7 channels.

Control of $Ca^{2+}$- Influx by $Ca^{2+}$/Calmodulin Dependent Protein Kinase II in the Activation of Mouse Eggs

  • Yoon, Sook-Young;Kang, Da-Won;Bae, In-Ha
    • Development and Reproduction
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    • v.15 no.1
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    • pp.31-39
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    • 2011
  • Change in intracellular $Ca^{2+}$-concentration ($[Ca^{2+}]_i$) is an essential event for egg activation and further development. $Ca^{2+}$ ion is originated from intracellular $Ca^{2+}$-store via inositol 1,4,5-triphosphate receptor and/or $Ca^{2+}$ influx via $Ca^{2+}$ channel. This study was performed to investigate whether changes in $Ca^{2+}$/calmodulin dependent protein kinase II (CaM KII) activity affect $Ca^{2+}$ influx during artificial egg activation with ethanol using $Ca^{2+}$ monitoring system and whole-cell patch clamp technique. Under $Ca^{2+}$ ion-omitted condition, $Ca^{2+}$-oscillation was stopped within 30 min post microinjection of porcine sperm factor, and ethanol-induced $Ca^{2+}$ increase was reduced. To investigate the role of CaM KII known as an integrator of $Ca^{2+}$- oscillation during mammalian egg fertilization, CaM KII activity was tested with a specific inhibitor KN-93. In the eggs treated with KN-93, ethanol failed to induce egg activation. In addition, KN-93 inhibited inward $Ca^{2+}$ current ($I_{Ca}$) in a time-dependent manner in whole-cell configuration. Immunostaining data showed that the voltage-dependent $Ca^{2+}$ channels were distributed along the plasma membrane of mouse egg and 2-cell embryo. From these results, we suggest that $Ca^{2+}$ influx during fertilization might be controlled by CaM KII activity.

Single-Camera Micro-Stereo 4D-PTV (단일카메라 마이크로 스테레오 4D-PTV)

  • Doh, Deog-Hee;Cho, Young-Beom;Lee, Jae-Min;Kim, Dong-Hyuk;Jo, Hyo-Jae
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.34 no.12
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    • pp.1087-1092
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    • 2010
  • A micro 3D-PTV system has been constructed using a single camera system. Two viewing holes were created behind the object lens of the microscopic system to construct a stereoscopic viewing image. A hybrid recursive PTV algorithm was used. A concept of epipolar line was adopted to eliminate many spurious candidates. Three-dimensional velocity vector fields were obtained by calculating the three-dimensional displacements of particles that were identified as being identical. The system consists of a laser light source (Ar-ion, 500 mW), one high-definition camera ($1028{\times}1024$ pixels, 500 fps), a circular plate with two viewing holes, and a host computer. The performance of the developed algorithm was tested using artificial images. The characteristic of the vector recovery ratio was investigated for the particle numbers. A micro backward-facing step channel ($H{\times}h{\times}W:\;36{\mu}m{\times}70{\mu}m{\times}3000{\mu}m$) was measured using the developed measurement system. The results were in good qualitative agreement with other results.

Purification and Characterization of Natural Antifungal Protein from Astragal Seeds (Astragalus membranaceus L.). (황기 종자의 천연 항진균성 단백질의 분리정제 및 특성검정)

  • 구본성;류진창;정태영;김교창
    • Microbiology and Biotechnology Letters
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    • v.26 no.5
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    • pp.379-386
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    • 1998
  • Deterioration of food is in general caused by the presence of microorganisms and chemical compounds of food itself. There exists antimicrobial compound in the food, however, addition of food antiseptics, additives, or physico-chemical processing is a common practice. The safety of artificial chemical antiseptics became a serious public concern, therefore, new natural antiseptic compounds are in need to be developed. We have isolated a new natural antifungal protein (KBS-B2) from Astragal seed through ammonium sulfate precipitation and column chromatography using FPLC Mono-S and Superose 12HR. The purified protein inhibited growth of Candida albicans, and spore germination of food spoiling fungi such as Aspergillus ochraceus, Penicillium expensum, P. digitatum and Botrytis cineria. Antifungal effect of the KBS-B2 protein could be directly assayed by bioautography overlaying the fungal spores on the electrophoresed acrylamide gel. The comparison of N-terminal amino acid sequences of the KBS-B2 with known antifungal protein revealed that had 50% homology to thaumatin and zeamatin like proteins.

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Bibliographic Studies on the Tetrodotoxin(TTX) (복어 독(Tetrodotoxin)에 관한 문헌적 고찰)

  • Hwang, Tae-Joon;Kwon, Gi-Rok;Choe, Ick-Seon
    • Journal of Pharmacopuncture
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    • v.3 no.2
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    • pp.1-25
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    • 2000
  • We were trying to study the validity of Puffer fish's poison(Tetrodotoxin- TTX) to make a traditional Korean Medical treatment. The following conclusions were made after literary studies. 1. The first record of the puffer fish dates back 2000 years ago in the Chinese text Book of Mountain and Sea and other texts from the similar period. 2. Puffer fish's poison IS known as tetrodotoxin which is an amino perhydroquinazoline compound. It has a chemical formula of $C_{11}H_{17}N_3O_8$ in the hemiacetal structure and has the molecular weight of 319. 3. Tetrodotoxin (TTX) plays a role as potent neurotransmitter blocker by blocking the $Na^+$ -gate channel which hinders the influx of $Na^+$ ion into the cell. 4. Symptoms of the puffer fish poisoning ranges from blunted sense in the lips and tongue, occasional vomiting in the first degree to sudden descending of the blood pressure, apnea, and other critical conditions in the fourth degree. Intoxication of the puffer fish poison progresses at a rapid pace as death may occur after an hour and half up to eight hours in maximum. Typical death occurs after four to six hours. 5. Ways to treat the puffer fish poisoning include gastric irrigation, induce vomiting, purgation, intravenous fluid injection, and correcting electrolytic imbalance and acidosis. In cases of dyspnea, apply oxygen inhalation and conduct artificial respiration. 6. Tetrodotoxin (TTX) may be applied in treating brain disorders, ocular pain, excess pain in the large intestine and ileum, and relieving tension of the skeletal museles, neuralgia, rheumatism, arthritis, and etc. 7. In terms of Oriental medicine, the puffer fish poison has characteristics of sweet, warm, and poisonous. It's known efficacies are to tonify weakness, dispel damp, benefit the lower back, relieve hemorrhoid, kills parasites, remove edema, and so forth. And the puffer fish eggs processed with ginger are said to be effective against tuberculosis and lung cancer, thus, it's validity must be investigated and further research should be followed.

Arsenic removal from artificial arsenic water using CaAl-monosulfate and CaAl-ettringite (CaAl-monosulfate와 CaAl-ettringite를 이용한 인공비소폐수의 비소 제거 연구)

  • Shim, Jae-Ho;Kim, Ki-Baek;Choi, Won-Ho;Park, Joo-Yang
    • Journal of Korean Society of Water and Wastewater
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    • v.26 no.1
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    • pp.141-148
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    • 2012
  • The objective of this study is to remove arsenate from artificially contaminated wastewater using CaAl-ettringite and CaAl-monosulfate which were synthesized in laboratory. The study was carried on the basis of solidification/stabilization of waste using cement. Monosulfate and ettringite are constituents of cement paste. The CaAl-ettringite has a chemical formula of $Ca_6Al_2O_6(SO_4)_3{\cdot}32H_2O$ and has a needle like morphology. Whereas CaAl-monosulfate $Ca_4Al_2O_6(SO_4){\cdot}12H_2O$ has layered double hydroxide structure (LDH) in which the mainlayer consists of Ca and Al and S as interlayer. Ettringite and monosulfate were synthesized by reaction of tricalcium aluminate and gypsum and hydrating this mixture at elevated temperature. The synthesized mineral were characterized by PXRD and FESEM to ensure purity. It was found that concentrations of As(V) in contaminated water were reduced from initial concentration of 1.335 mmol/L to 0.054 mmol/L and 0.300 mmol/L by CaAl-monosulfate and CaAl-ettringite respectively. The post experimental results of PXRD and FESEM analysis indicate that arsenate removal was by ion exchange.