• Title/Summary/Keyword: $A_2$ inhibitor

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Theoretical and Experimental Studies on the Adsorption of N-[(E)-Pyridin-2-ylmethylidene] Aniline, a Schiff Base, on Mild Steel Surface in Acid Media

  • N, Mohanapriya.;M, Kumaravel.;B, Lalithamani.
    • Journal of Electrochemical Science and Technology
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    • v.11 no.2
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    • pp.117-131
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    • 2020
  • The adsorption of N-[(E)-Pyridin-2-ylmethylidene] aniline, a Schiff base, on to mild steel surface in 1M HCl and 0.5 M H2SO4 solutions and the consequent corrosion protection were studied employing weight loss method, electrochemical impedance spectroscopy and potentiodynamic polarization measurements. DFT calculations were performed to investigate its interaction with the metal surface at the atomic level to understand its inhibition mechanism. The adsorption process is well described by the Langmuir isotherm. The thermodynamic parameters indicated that the adsorption is spontaneous and the interaction of the inhibitor at the mild steel surface is mainly through physisorption. The Ra values obtained in AFM studies for the uninhibited and inhibited sample in HCl media respectively are 0.756 and 0.559 ㎛, and that in H2SO4 media are 0.411 and 0.406 ㎛. The lesser roughness values of the inhibited sample shows the adsorption of the molecules onto the mild surface. The inhibition efficiencies were found to improve with concentration of the inhibitor and the maximum efficiency was observed at 400ppm in all the investigation methods adopted. The inhibitor was found to exhibit a higher efficiency in HCl media (95.7%) than in H2SO4 (92.8%). The theoretical and experimental results are found to be in good agreement.

$\alpha$-D-Glucosidase Inhibitor from Streptomyces Sp. (III) - Purification and Stability of the Inhibitor - (Streptomyces속 균주가 생성하는 $\alpha$-D-Glucosidase Inhibitor(III) -저해물질의 정제 및 안정성-)

  • 도재호;주현규
    • Microbiology and Biotechnology Letters
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    • v.17 no.5
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    • pp.529-532
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    • 1989
  • A strain of Streptomyces sp. (YS-221-B) extracellularly produced an inhibitory substance for $\alpha$-D-Glucosidase. The substance was purified 96-fold from culture filtrate by dialysis, heat treatment, adsorption on active carbon, Bio-Gel P-10 and Sephadex G-75 column chromatography with yield of 9.2%. The substance was stable in pH range from 7.0 to 11.0 at 37$^{\circ}C$, and a treatment at 10$0^{\circ}C$ for 20 min diminished only 15% of the original activity. The inhibitor was not inactivated by the treatment of $\alpha$-, $\beta$-amylases, glucoamylases, trypsin and chymotrypsin but inactivated by pyoteases from Streptomyces griseus and Tritirachium album.

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Identification of Streptomyces DMCJ-49 Producing the alpha-Amylase Inhibitors and the Isolation of the Inhibitor (알파-아밀라제 저해제 생성 Streptomyces DMCJ-49의 동정과 저해제의 분리)

  • Chung, Dong-Jik;Kwak, Jin-Hwan;Choi, Eung-Chil;Kim, Byong-Kak
    • YAKHAK HOEJI
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    • v.33 no.3
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    • pp.175-182
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    • 1989
  • To find ${\alpha}-amylase$ inhibitors produced by microorganisms from soil, a strain which had a strong inhibitory activity against bacterial ${\alpha}-amylase$ was isolated from the soil sample collected in Korea. The morphological and physiological characteristics of this strain on several media and its utilization of carbon sources showed that it was one of Streptomyces species according to the International Streptomyces Project method. The amylase inhibitor of this strain was purified by active carbon adsorption, silicagel column chromatography, SP-Sephadex C-25 column chromatography, adsorption on Amberlite XAD-2. The inhibitor was oligosaccharide which was composed of glucose. The inhibitor had inhibitory activity against other amylase such as salivary ${\alpha}-amylase$, pancreatic ${\alpha}-amylase$, fungal ${\alpha}-amylase$ and gluco-amylase.

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Involvement of Multiple Signaling Molecules in Peptidoglycan-induced Expression of Interleukin-1α in THP-1 Monocytes/Macrophages (THP-1 단핵구의 펩티도글리칸 유래 인터루킨-1 알파 발현에서 TLR2, PI3K/Akt/mTOR, MAPKs의 역할)

  • Heo, Weon;Son, Yonghae;Cho, Hyok-rae;Kim, Koanhoi
    • Journal of Life Science
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    • v.32 no.6
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    • pp.421-429
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    • 2022
  • The expression of interleukin-1α (IL-1α) is elevated in monocytic cells, such as monocytes and macro-phages, within atherosclerotic arteries, yet the cellular molecules involved in cytokine upregulation remain unclear. Because peptidoglycan (PG), a major component of gram-positive bacterial cell walls, is detected within the inflammatory cell-rich regions of atheromatous plaques, it was investigated if PG contributes to IL-1α expression in monocytes/macrophages. Exposure of THP-1 monocytic cells to PG resulted in elevated levels of IL-1α gene transcripts and increased secretion of IL-1α protein. The transcription and secretion of IL-1α were abrogated by OxPAPC, an inhibitor of TLR2/4, but not by polymyxin B that inhibits lipopolysaccharide-induced TLR4 activation. To understand the molecular mechanisms of the inflammatory responses due to bacterial pathogen-associated molecular patterns (PAMPs) in diseased arteries, we attempted to determine the cellular factors involved in the PG-induced upregulation of IL-1α expression. Pharmacological inhibition of cell signaling pathways with LY294002 (a PI3K inhibitor), Akti IV (an inhibitor of Akt activation), rapamycin (an mTOR inhibitor), U0126 (a MEK inhibitor), SB202190 (a p38 MAPK inhibitor), SP6001250 (a JNK inhibitor), and DPI (a NOX inhibitor) also significantly attenuated the PG-mediated expression of IL-1α. These results suggest that PG induces the monocytic or macrophagic expression of IL-1α, thereby contributing to vascular inflammation, via multiple signaling molecules, including TLR2, PI3K/Akt/mTOR, and MAPKs.

Gene Manipulation of Pin 2(Proteinase Inhibitor II) to the Cottonwood Leaf Beetle(Coleoptera : Chrysomelidae) in Transgenic Poplar(Populus deltodies × P. nigra) (형질전환(形質轉換)된 포플러의 딱정벌레에 대한 저항성(抵抗性) 유전자(遺傳子)(Proteinase Inhibitor II) 발현(發現))

  • Kang, Hoduck
    • Journal of Korean Society of Forest Science
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    • v.86 no.4
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    • pp.407-414
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    • 1997
  • The resistance of a non-transgenic poplar clone, 'Ogy' and three transgenic poplar lines to the cottonwood leaf beetle, Chrysomela scripta F., was evaluated by in vitro feeding. The lines were transformed with neomycin phosphotransferase II(NPT II) as a selectable marker, proteinase inhibitor II(pin2) as a resistance gene, and CaMV 35S as a promoter. An efficient method of sterilizing the beetle eggs and introducing them into plant tissue cultures was developed. The resistance of the transgenic lines was investigated in terms of effects tin leaf area consumed, insect weight, insect developmental stages, and plantlet root dry weight after feeding. Also, leaf area consumed was examined by leaf age as measured through leaf plastochron index(LPI). The leaf area consumed and insect weight were highly significant between transformants and control, and insect development in vitro was significant among the transgenic lines. Larval infestation was the most severe around LPI 4 to 5 which were young leaves. The system provided a quick, highly controlled method to screen developing transgenic plantlets directly.

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Human peripheral blood-derived exosomes for microRNA delivery

  • Ji‑Young Kang;Hyewon Park;Hyoeun Kim;Dasom Mun;Hyelim Park;Nuri Yun;Boyoung Joung
    • International Journal of Molecular Medicine
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    • v.43 no.6
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    • pp.2319-2328
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    • 2019
  • Exosomes serve important functions in cell-to-cell communication and biological functions by serving as a delivery cargo shuttle for various molecules. The application of an improved delivery method for microRNAs (miRNAs/miRs) may enhance their potential as a therapeutic tool in cardiac diseases. Thus, the present study investigated whether human peripheral blood-derived exosomes may be used as a delivery cargo system for miRNAs, and whether the delivery of miR-21 using a human peripheral blood derived-exosome may influence the degree of remodeling following myocardial infarction (MI). In H9C2 and HL-1 cells, miR-21 expression was successfully regulated by treatment with human peripheral blood derived-exosomes loaded with an miR-21 mimic or inhibitor compared with untreated cells. In addition, the mRNA and protein expression levels of SMAD family member 7 (Smad7), phosphatase and tensin homolog (PTEN) and matrix metalloproteinase 2 (MMP2), which are involved in cardiac fibrosis, were associated with the uptake of miR-21 mimic- or inhibitor-loaded exosomes. Similarly, the in vivo mRNA and protein expression of Smad7, PTEN and MMP2 were altered following treatment with miR-21 mimic- or inhibitor-loaded exosomes. Furthermore, miR-21 mimic-loaded exosomes enhanced fibrosis, whereas miR-21 inhibitor-loaded exosomes reduced fibrosis in a mouse MI model. These results suggested that miRNA-loaded human peripheral blood derived-exosomes may be used as a therapeutic tool for cardiac diseases.

Inhibition of Plasminogen Activator Inhibitor-1 Expression in Smoke-Exposed Alveolar Type II Epithelial Cells Attenuates Epithelial-Mesenchymal Transition

  • Song, Jeong-Sup;Kang, Chun-Mi
    • Tuberculosis and Respiratory Diseases
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    • v.70 no.6
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    • pp.462-473
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    • 2011
  • Background: Smoking is a risk factor for idiopathic pulmonary fibrosis (IPF), but the mechanism of the association remains obscure. There is evidence demonstrating that plasminogen activator inhibitor-1 (PAI-1) is involved in the progression of pulmonary fibrosis. This study was to determine whether the administration of small interfering RNA (siRNA) targeting PAI-1 or PAI-1 inhibitor to the cigarette smoking extract (CSE)-exposed rat alveolar type II epithelial cells (ATII cells) limits the epithelial-mesenchymal transition (EMT). Methods: ATII cells were isolated from lung of SD-rat using percoll gradient method and cultured with 5% CSE. The EMT was determined from the ATII cells by measuring the real-time RT PCR and western blotting after the PAI-1 siRNA transfection to the cells and after administration of tiplaxtinin, an inhibitor of PAI-1. The effect of PAI-1 inhibitor was also evaluated in the bleomycin-induced rats. Results: PAI-1 was overexpressed in the smoking exposed ATII cells and was directly associated with EMT. The EMT from the ATII cells was suppressed by PAI-1 siRNA transfection or administration of tiplaxtinin. Signaling pathways for EMT by smoking extract were through the phosphorylation of SMAD2 and ERK1/2, and finally Snail expression. Tiplaxtinin also suppressed the pulmonary fibrosis and PAI-1 expression in the bleomycin-induced rats. Conclusion: Our data shows that CSE induces rat ATII cells to undergo EMT by PAI-1 via SMAD2-ERK1/2-Snail activation. This suppression of EMT by PAI-1 siRNA transfection or PAI-1 inhibitor in primary type II alveolar epithelial cells might be involved in the attenuation of bleomycin-induced pulmonary fibrosis in rats.

Studies on Screening and Isolation of .$\alpha$-Amylase Inhibitors of Soil Microorganisms (I)

  • Kwak, Jin-Hwan;Choi, Eung-Chil;Kim, Byong-Kak
    • Archives of Pharmacal Research
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    • v.8 no.2
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    • pp.67-75
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    • 1985
  • To find emylase inhibitors produced by microorganisms from soil, a strain which had a strong inhibitory activity against bacteria .alpha.-amylase was isolated from the soil smaple collected in Seoul. The morphological and physiological characteristics of this strain on several media and its utilization of carbon sources showed that it was one of Streptomyces specties according to the international Streptomyces Project method. The amylase inhibitor of this strain was purified by means of acetone precipitation, adsorption on Amberlite XAD-2, and column chromatography on Amberlite CG-50 and SP-Sephadex C-25. The inhibitor was stable at the pH range of 1-10 and at 100.deg.C for half an hour, and had inhibitory activities against other amylases such as salivary .alpha.-amylase, pancreatic .alpha.-amylase, fungal .alpha.-amylase and glucoamylase. The kinetic studies of the inhibitor showed that its inhibitory effect on starch hydrolysis by .alpha.-amylase was non-competitive.

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Effect of Phosphate-based Inhibitors on Pipe Corrosion of Drinking Water Supply (상수도 배급수관망의 부식방지를 위한 인산염계 방청제 적용에 관한 연구)

  • 이윤진;남상호
    • Journal of Environmental Health Sciences
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    • v.29 no.3
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    • pp.65-71
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    • 2003
  • The injection concentration of corrosion inhibitor increases under the pH 7, temperature of 2$0^{\circ}C$, and alkalinity of 35 mg/l (as CaCO$_3$), the corrosion rate gradually decreased. When the corrosion inhibitor of 10 mg/l is injected, the corrosion rate for carbon steel pipe, galvanized steel pipe, and copper pipe reduces for 37, 66 and 61 % respectively that it is more efficient on galvanized steel pipe and copper pipe. As a result of examination of corrosion rate at pH 6, 7, and 8 when injecting 10 mg/l of corrosion inhibitor under the conditions of 2$0^{\circ}C$ in water temperature and 35 mg/l (as CaCO$_3$) in alkalinity, the efficiency of the corrosion inhibitor increases as the pH increases. For carbon steel pipe, it does not show much a difference with the change of the pH condition, but galvanized steel pipe and copper pipe clearly show the corrosion rate depending on the change of the pH condition. The efficiency of corrosion inhibitor is low as the concentration of residual chlorine is high, but it does not show a great influence at 0.4 mg/l or less. For each pipe type, in the case of carbon steel pipe, the range of increase of corrosion speed following the residual chloride is higher than the other pipe types. In the meantime, the effect following the residual chlorine in copper pipe is low.