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Chromenone Derivatives as Monoamine Oxidase Inhibitors from Marine-Derived MAR4 Clade Streptomyces sp. CNQ-031

  • Oh, Jong Min;Lee, Chaeyoung;Nam, Sang-Jip;Kim, Hoon
    • Journal of Microbiology and Biotechnology
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    • v.31 no.7
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    • pp.1022-1027
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    • 2021
  • Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC50) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC50 of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The Ki value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the Ki values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

Comparison of SBR/BR Blend Compound and ESBR Copolymer Having Same Butadiene Contents

  • Hwang, Kiwon;Lee, Jongyeop;Kim, Woong;Ahn, Byungkyu;Mun, Hyunsung;Yu, Eunho;Kim, Donghyuk;Ryu, Gyeongchan;Kim, Wonho
    • Elastomers and Composites
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    • v.54 no.1
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    • pp.54-60
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    • 2019
  • The rapid development of the automobile industry is an important factor that led to the dramatic development of synthetic rubber. The tread part of tire that comes in direct contact with the road surface is related to the service life of the tire. Rubber compounds used in tire treads are often blended with SBR (styrene-butadiene rubber) and BR (butadiene rubber) to satisfy physical property requirements. However, when two or more kinds of rubber are blended, phase separation and silica dispersion problems may occur due to non-uniform mixing of the rubber. Therefore, in this study, we synthesized an SBR copolymer with the same composition as that of a typical SBR/BR blend compound by controlling butadiene content during ESBR (emulsion styrene-butadiene rubber) synthesis. Subsequently, silica filled compounds were manufactured using the synthesized ESBR, and their mechanical properties, dynamic viscoelasticity, and crosslinking density were compared with those of the SBR/BR blended compound. When the content of butadiene was increased in the silica filled compound, the cure rate accelerated due to an increased number of allylic positions, which typically exhibit higher reactivity. However, the T-2 compound with increased butadiene content by synthesis less likely to show an increase in crosslink density due to poor silica dispersion. In addition, the T-3 compound containing high cis BR content showed high crosslink density due to its monosulfide crosslinking structure. Because of the phase separation, SBR/BR blend compounds were easily broken and showed similar $M_{100%}$ and $M_{300%}$ values as those of other compounds despite their high crosslink density. However, the developed blend showed excellent abrasion resistance due to the high cis-1,4 butadiene content and low rolling resistance due to the high crosslink density.

Effect of Acrylonitrile-Butadiene Rubber on the Properties of Silica-Filled Styrene-Butadiene Rubber Compounds: Reduction of Silane Coupling Agent and Diphenylguanidine (실리카로 보강된 SBR 배합물의 특성에 미치는 NBR 효과: 실란커플링제와 DPG의 사용량 감소)

  • Choi, Sung-Seen;Chang, Dong-Ho;Kim, Ik-Sik
    • Elastomers and Composites
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    • v.37 no.4
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    • pp.217-223
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    • 2002
  • Silica-filled rubber compounds show poor filler dispersion and slow cure characteristics compared to carbon black-filled ones. In general, a silica-filled rubber compound contains silane coupling agent (bis-(3-(triethoxysilyl)-propyl)-tetrasulfide, TESPT) and diphenylguanidine (DPG) to improve the filler dispersion and to make fast cure characteristics. Acrylonitrile-butadiene rubber (NBR) improves the filler dispersion in silica-filled styrene-butadiene rubber (SBR) compounds. In this study, effect of NBR on the properties of silica-filled SBR compounds was investigated. Properties of the compounds which contain NBR without DPG or with small amount of TESPT (Compound A) were compared with those of the compounds which contain TESPT and DPG without NBR (Compound B). Scorch time of Compound A is faster than those of Compound B. Modulus and tensile strength of Comound A are slightly lower than those of Compound B. Traction property of the Comound A is better than that of the Compound B. Addition of NBR leads to reduction of the used amount of TESPT and DPG.

Surface Roughness and Formation of Compound Layer in the Controlled Gaseous Nitriding Process on Cast Iron GC250D (GC250D의 가스분위기 제어질화 공정에서 화합물층의 형성에 따른 표면조도의 변화)

  • Minjae Jeong;Seokwon Son;Jae-Lyoung Wi;Yong-Kook Lee;Won-Beom Lee
    • Journal of the Korean Society for Heat Treatment
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    • v.37 no.2
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    • pp.49-57
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    • 2024
  • We investigated the changes in microstructure and surface roughness of the compound layer of GC250D gray cast iron, commonly used in brake discs, during gas nitriding. The gas atmosphere of the nitriding process was controlled with a hydrogen partial pressure of 49.5%, and the process was conducted at a nitriding temperature of 520℃ with various process times. As the nitriding process time of the GC250D material increased, both the depth of hardening and the thickness of the compound layer increased, with a maximum surface hardness of approximately 1265 HV0.1 was measured. Additionally, the surface roughness increased with the process time. Phase analysis of the compound layer revealed an increase in the proportion of the γ' phase as the nitriding process time increased. Changes in the formation of the compound layer were observed depending on the orientation of graphite within the material, leading to the formation of wedges. Therefore, the increase in surface roughness appears to be attributed to the uneven compounds, the expansion of the compound layer and wedges formed on the surface during the nitriding process.

Development of compound eye image quality improvement based on ESRGAN (ESRGAN 기반의 복안영상 품질 향상 알고리즘 개발)

  • Taeyoon Lim;Yongjin Jo;Seokhaeng Heo;Jaekwan Ryu
    • Journal of the Korea Computer Graphics Society
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    • v.30 no.2
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    • pp.11-19
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    • 2024
  • Demand for small biomimetic robots that can carry out reconnaissance missions without being exposed to the enemy in underground spaces and narrow passages is increasing in order to increase the fighting power and survivability of soldiers in wartime situations. A small compound eye image sensor for environmental recognition has advantages such as small size, low aberration, wide angle of view, depth estimation, and HDR that can be used in various ways in the field of vision. However, due to the small lens size, the resolution is low, and the problem of resolution in the fused image obtained from the actual compound eye image occurs. This paper proposes a compound eye image quality enhancement algorithm based on Image Enhancement and ESRGAN to overcome the problem of low resolution. If the proposed algorithm is applied to compound eye image fusion images, image resolution and image quality can be improved, so it is expected that performance improvement results can be obtained in various studies using compound eye cameras.

Studies on Glycolipids in Bacteria -Part II. On the Structure of Glycolipid of Selenomonas ruminantium- (세균(細菌)의 당지질(糖脂質)에 관(關)한 연구(硏究) -제2보(第二報) Selenomonas ruminantium의 당지질(糖脂質)의 구조(構造)-)

  • Kim, Kyo-Chang
    • Applied Biological Chemistry
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    • v.17 no.2
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    • pp.125-137
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    • 1974
  • The chemical structure of glycolipid of Selenomonas ruminantium cell wall was to be elucidated. The bacterial cells were treated in hot TCA and the glycolipid fractions were extracted by the solvent $CHCl_3\;:\;CH_3OH$ (1 : 3). The extracted glycolipids fraction was further separated by acetone extraction. The acetone soluble fraction was named as the spot A-compound. The acetone insoluble but ether soluble fraction was named as the spot B-compound. These two compounds were examined for elucidation of their chemical structure. The results were as follows: 1. The IR spectral analysis showed that O-acyl and N-acyl fatty acids were linked to glucosamine moiety in the spot A-compound. However in the spot B-compound in addition to O and N-acyl acids phosphorus was shown to be attached to glucosamine. 2. It was recognized by gas liquid chromatography that spot A compound contained beta-OH $C_{13:0}$ fatty acid in predominance in addition to the fatty acid with beta-OH $C_{9:0}$, whereas the spot B compound was composed of the predominant fatty acid of beta-OH $C_{13:0}$ with small amount of beta-OH $C_{9:0}$. 3. According to the paper chromatographic analysis of hydrazinolysis products of the spot A compound, a compound of a similar Rf value as the chitobiose was recognized, which indicated a structure of two molecules glucosamine condensed. The low Rf value of the hydrazinolysis product of the spot B-compound confirmed the presence of phosphorus attached to glucosamine. 4. The appearance of arabinose resulting from. ninhydrin decomposition of the acid hydrolyzate of the spot A compound indicated that the amino group is attached to $C_2$ of glucosamine. 5. The amount of glucosamine in the N-acetylated spot A compound decreased in half of the original content by the treatment. with $NaBH_4$, indicating that there are two molecules of glucosamines in the spot A compound. The presence of 1, 6-linkage between two molecules of glucosamine was suggested by the Morgan-Elson reaction and confirmed by the periodate decomposition test. 6. By the action of ${\beta}-N-acetyl$ glucosaminidase the N-acetylated spot A compound was completely decomposed into N-acetyl glucosamine, whereas the spot B compound was not. This indicated the spot A compound has a beta-linkage. 7. When phosphodiesterase or phosphomonoesterase acted on $^{32}P-labeled$ spot B compound, $^{32}P$ was not released by phosphodiesterase, but completely released by phosphomonoesterase. This indicated that one phosphorus is linked to glucosamine moiety. 8. The spot A compound is assumed to have the following chemical structure: That is glucosaminyl, ${\beta}-1$, 6-glucosamine to which O-acyl and N-acyl fatty acids are linked, of which the predominant fatty acid is beta-OH $C_{13:0}$ fatty acid in addition to beta-OH $C_{9:0}$ fatty acid 9. The spot B compound is likely to have the linkage of $glucosaminyl-{\beta}-1$, 6-glucosamine to which phosphorus is linked in monoester linkage. Furthermore both O-acyl and N-acyl fatty acids contained beta-OH $C_{13:0}$ fatty acid predominantly in addition to beta-OH $C_{9:0}$ fatty acid.

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o-Dihydroxyisoflavone Derivatives from Highly Aged Korean Fermented Soybean Paste by Jang Yang Process and Its Biological Activity (장양(藏釀) 기술이 사용된 전통 고숙성 된장에서 유래한 o-Dihydroxyisoflavone 유도체의 생리활성)

  • Kim, Dong-Hyun;Park, Jun-Seong;Park, Nok-Hyun;Moon, Eun-Jeong;Yu, Sun-Hye;Kim, Duck-Hee;Kim, Han-Kon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.3
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    • pp.203-208
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    • 2009
  • Doenjang (Korean fermented soybean paste) is a unique fermented food in Korea. It has been traditionally manufactured from soybeans, by Jang Yang process. We focused on the newly formed compound in highly aged Doenjang and its biological activity. One new o-dihydroxyisoflavone, 7,3',4'-trihydroxyisoflavone and two known o-dihydroxyisoflavone derivatives were isolated from 5-year-old Doenjang and evaluated as potent antioxidant and whitening effect by comparing with other known isoflavone. 7,8,4'-Trihydroxyisoflavone (compound 1), 7,3',4'-trihydroxyisoflavone (compound 2) and 6,7,4'-trihydroxyisoflavone (compound 3) inhibited DPPH (diphenyl-1-picrylhydrazyl) formation by 50 % at a concentration of $21.5{\pm}0.2$, $28.7{\pm}0.4$ and $32.6{\pm}0.6$ ($IC_{50}$) respectively, whereas daidzein showed weak DPPH radical scavenging activity. In superoxide scavenging effect were measured in one assay. Compound 1 ($IC_{50}=18.10{\pm}0.2{\mu}M$) and 2 ($IC_{50}=10.54{\pm}0.4{\mu}M$) show significant inhibitory activity and greater effect than L-ascorbic acid. But compound 3 and daidzein showed lower inhibition activity. Also, o-dihydroxyisoflavone derivatives evaluated as potent inhibitors on tyrosinase activity and melanin formation in melan-a cells. Compound 1 ($IC_{50}=11.21{\pm}0.2{\mu}M$), compound 2 ($IC_{50}=5.23{\pm}0.6{\mu}M$) exhibited significant inhibitory effect on tyrosinase activity. Furthermore, those compounds are significantly suppressed the cellular melanin formation by 50 % at a concentration of $12.23{\pm}0.7{\mu}M$ (1) and $7.83{\pm}0.7{\mu}M$ (2). This result suggests that 7,3',4'-trihydroxyisoflavone from highly aged Doenjang could be used as an active ingredient for cosmetics.