• Title/Summary/Keyword: amine

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Novel Isoquinolinamine and Isoindoloquinazolinone Compounds Exhibit Antiproliferative Activity in Acute Lymphoblastic Leukemia Cells

  • Roolf, Catrin;Saleweski, Jan-Niklas;Stein, Arno;Richter, Anna;Maletzki, Claudia;Sekora, Anett;Escobar, Hugo Murua;Wu, Xiao-Feng;Beller, Matthias;Junghanss, Christian
    • Biomolecules & Therapeutics
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    • v.27 no.5
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    • pp.492-501
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    • 2019
  • Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T- acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with $10{\mu}M$ up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to $1.94{\mu}M$. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.

Biogenic-Amine Contents of Korean Commercial Salted Fishes and Cabbage Kimchi (젓갈류 및 배추김치에서의 바이오제닉 아민류 함량 조사 연구)

  • Shin, Sang-Woon;Kim, Young-Sug;Kim, Yang-Hee;Kim, Han-Taek;Eum, Kyoung-Suk;Hong, Se-Ra;Kang, Hyo-Jeong;Park, Kwang-Hee;Yoon, Mi-Hye
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.52 no.1
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    • pp.13-18
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    • 2019
  • We determined the contents of 11 biogenic amines in 20 types of cabbage kimchi, 10 types of fish sauce, and 40 types of salted fish purchased from small- and medium-sized grocery stores in Gyeonggi-Do, Republic of Korea, from June to October 2017. The content of each of the biogenic amines in the various types of cabbage kimchi was slightly lower than that in detection amounts of each of the 10 types of biogenic amines and the values reported by Joe et al. The histamine content of all five types of anchovy sauce was lower than the limit set by the European Union (400 mg/kg), but that of three of the five types of sand lance sauce was higher. Analyzing the ratios of the contents of five highly toxic biogenic amines to those of the 11 biogenic amines yielded no quantitative correlation. The estimated daily intake of the five highly toxic biogenic amines in cabbage-kimchi and fermented fish was ${\leq}6mg$.

Optimization of Elastic Modulus and Cure Characteristics of Composition for Die Attach Film (다이접착필름용 조성물의 탄성 계수 및 경화 특성 최적화)

  • Sung, Choonghyun
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.4
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    • pp.503-509
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    • 2019
  • The demand for smaller, faster, and multi-functional mobile devices in increasing at a rapidly increasing rate. In response to these trends, Stacked Chip Scale Package (SCSP) is used widely in the assembly industry. A film type adhesive called die attach film (DAF) is used widely for bonding chips in SCSP. The DAF requires high flowability at high die attachment temperatures for bonding chips on organic substrates, where the DAF needs to feel the gap depth, or for bonding the same sized dies, where the DAF needs to penetrate bonding wires. In this study, the mixture design of experiment (DOE) was performed for three raw materials to obtain the optimized DAF recipe for low elastic modulus at high temperature. Three components are acrylic polymer (SG-P3) and two solid epoxy resins (YD011 and YDCN500-1P) with different softening points. According to the DOE results, the elastic modulus at high temperature was influenced greatly by SG-P3. The elastic modulus at $100^{\circ}C$ decreased from 1.0 MPa to 0.2 MPa as the amount of SG-P3 was decreased by 20%. In contrast, the elastic modulus at room temperature was dominated by YD011, an epoxy with a higher softening point. The optimized DAF recipe showed approximately 98.4% pickup performance when a UV dicing tape was used. A DAF crack that occurred in curing was effectively suppressed through optimization of the cure accelerator amount and two-step cure schedule. The imizadole type accelerator showed better performance than the amine type accelerator.

Fates of water and salts in non-aqueous solvents for directional solvent extraction desalination: Effects of chemical structures of the solvents

  • Choi, Ohkyung;Kim, Minsup;Cho, Art E.;Choi, Young Chul;Kim, Gyu Dong;Kim, Dooil;Lee, Jae Woo
    • Membrane and Water Treatment
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    • v.10 no.3
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    • pp.207-212
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    • 2019
  • Non-aqueous solvents (NASs) are generally known to be barely miscible, and reactive with polar compounds, such as water. However, water can interact with some NASs, which can be used as a new means for water recovery from saline water. This study explored the fate of water and salt in NAS, when saline water is mixed with NAS. Three amine solvents were selected as NAS. They had the same molecular formula, but were differentiated by their molecular structures, as follows: 1) NAS 'A' having the hydrophilic group ($NH_2$) at the end of the straight carbon chain, 2) NAS 'B' with symmetrical structure and having the hydrophilic group (NH) at the middle of the straight carbon chain, 3) NAS 'C' having the hydrophilic group ($NH_2$) at the end of the straight carbon chain but possessing a hydrophobic ethyl branch in the middle of the structure. In batch experiments, 0.5 M NaCl water was blended with NASs, and then water and salt content in the NAS were individually measured. Water absorption efficiencies by NAS 'B' and 'C' were 3.8 and 10.7%, respectively. However, salt rejection efficiency was 98.9% and 58.2%, respectively. NAS 'A' exhibited a higher water absorption efficiency of 35.6%, despite a worse salt rejection efficiency of 24.7%. Molecular dynamic (MD) simulation showed the different interactions of water and salts with each NAS. NAS 'A' formed lattice structured clusters, with the hydrophilic group located outside, and captured a large numbers of water molecules, together with salt ions, inside the cluster pockets. NAS 'B' formed a planar-shaped cluster, where only some water molecules, but no salt ions, migrated to the NAS cluster. NAS 'C', with an ethyl group branch, formed a cluster shaped similarly to that of 'B'; however, the boundary surface of the cluster looked higher than that of 'C', due to the branch structure in solvent. The MD simulation was helpful for understanding the experimental results for water absorption and salt rejection, by demonstrating the various interactions between water molecules and the salts, with the different NAS types.

Synthesis of Polymer-Silica Hybrid Particle by Using Polyamine Nano Complex (폴리아민 나노 복합체를 이용한 고분자-실리카 복합체 입자 합성)

  • Kim, Dong-Yeong;Seo, Jun-Hee;Lee, Byungjin;Kang, Kyoung-Ku;Lee, Chang-Soo
    • Clean Technology
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    • v.27 no.2
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    • pp.115-123
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    • 2021
  • This study demonstrates a new method for the synthesis of organic-inorganic hybrid particles composed of an inorganic silica shell and organic core particles. The organic core particles are prepared with a uniform size using droplet-based microfluidic technology. In the process of preparing the organic core particles, uniform droplets are generated by independently controlling the flow rates of the dispersed phase containing photocurable resins and the continuous phase. After the generation of droplets in a microfluidic device, the droplets are photo-polymerized as particles by ultraviolet irradiation at the ends of microfluidic channels. The core particle is coated with a nano complex composed of polyallylamine hydrochloride (PAH) and phosphate ion (Pi) through strong non-covalent interactions such as hydrogen bonding and electrostatic interaction under optimized pH conditions. The polyamine nano complex rapidly induces the condensation reaction of silicic acid through the arranged amine groups of the main chain of PAH. Therefore, this method enabled the preparation of organic-inorganic hybrid particles coated with inorganic silica nanoparticles on the organic core. Finally, we demonstrated the synthesis of organic-inorganic hybrid particles in a short time under ambient and environmentally friendly conditions, and this is applicable to the production of organic-inorganic hybrid particles having various sizes and shapes.

Polyethyleneimine based Delivery System Coated with Hyaluronate Amine for Improved pDNA Transfection Efficiency (개선된 플라스미드 DNA 전달 효율을 위한 히알루론 아민 코팅 폴리에틸렌이민 기반 전달 시스템)

  • Oh, Kyoung-yeon;Jang, Yongho;Lee, Eunbi;Kim, Tae-ho;Kim, Hyuncheol
    • Applied Chemistry for Engineering
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    • v.33 no.1
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    • pp.83-89
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    • 2022
  • Since the pandemic of COVID-19, active investigation to develop immunity to infectious disease by delivering nucleic acids has been proceeded. Particularly, many studies have been conducted on non-viral vector as several vital side-effects which were found on nucleic acid delivery system using viral vectors. In this study, we have developed plasmid DNA (pDNA) loaded-hyaluronic acid derivative (HA) coated-polyethyleneimine (PEI) based polyplex for enhanced nucleic acid delivery efficiency. We have optimized the ratio of pDNA : PEI : HA by measuring size and protein transcription efficiency. The final product, polyplex-HA, was characterized through measuring size, zeta-potential and TEM image. Intracellular uptake and protein transcription efficiency were compared to commercially available transfection reagent, lipofectamine, through fluorescence image and flow cytometry. In conclusion, polyplex-HA presents a novel gene delivery system for efficient and stable protein transcription since it is available for delivering various genetic materials and has less immunoreactivity.

Antibacterial and Antiviral Activities of Multi-coating Polyester Textiles (다중 코팅 폴리에스터 섬유 여재의 항균 및 항바이러스 특성)

  • Ko, Sangwon;Lee, Jae-Young;Park, Duckshin
    • Applied Chemistry for Engineering
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    • v.33 no.4
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    • pp.444-450
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    • 2022
  • The effect of coated polyester (PET) textiles with metal oxide, chitosan, and copper ion on the antibacterial and antiviral activities was evaluated to investigate the applicability of multi-coated PET textiles as antiviral materials. Compared to coated PETs with a single agent, multi-coated PETs reduced the loading amount of coating materials as well as the contact time with bacteria for a bacterial cell number of < 10 CFU/mL, which was not detectable with the naked eyes. Metal oxides generate reactive oxygen species (ROS) such as free radicals by a catalytic reaction, and copper ions can promote contact killing by the generation of ROS. Chitosan not only enhanced antibacterial activities due to amine groups, but enabled it to be a template to load copper ions. We observed that multi-coated PET textiles have both antibacterial activities for E. coli and S. aureus and antiviral efficiency of more than 99.9% for influenza A (H1N1) and SARS-CoV-2. The multi-coated PET textiles could also be prepared via a roll-to-roll coating process, which showed high antiviral efficacy, demonstrating its potential use in air filtration and antiviral products such as masks and personal protective equipment.

Synthesis of Linear 1,2-Alkylaminopropanediols as Preservatives and Antimicrobial Activity (보존제로서 선형 1,2-알킬아미노프로판디올의 합성과 항균활성)

  • Cha, Kyung-On;Kwak, Sang-Woon;Jeong, Kook-In;Kim, Young-Ho
    • Applied Chemistry for Engineering
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    • v.33 no.4
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    • pp.394-401
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    • 2022
  • The synthesis of 1,2-alkylaminopropanediols (1,2-AAPs) was designed to improve the hydrophilicity of linear 1,2-alkanediols having 10, 12, 14, and 16 carbon atoms in the alkyl chain. 1,2-AAPs were synthesized by reacting 3-monochloro-1,2-propanediol (3-MCPD) with linear alkylamines having 10, 12, 14 or 16 carbon atoms in an ethanol solvent at 40℃ for 2 h. The yield and purity of four types of 1,2-AAPs synthesized were found to be in the range of 51-58% and 85-99%, respectively. The amine salts of four types of 1,2-AAPs were prepared from a purified paste or solid compound by adding an acidic solution (HCl) to pH 7, and then their solubilities and antibacterial effects were tested. 1,2-decylaminopropanediol, 1,2-dodecylaminopropanediol, and 1,2-tetradecylaminopropanediol were all dissolved in water at concentrations of 100%, 50%, and 0.1%, respectively, however 1,2-hexadecylaminopropanediol was not. The antibacterial effect was improved as the length of the alkyl chain increased. As a result of confirming the preservative effect of the lotion (cosmetic formulation) applied with 1,2-AAP for application, it showed very strong antibacterial activity at low concentrations ranging from 0.005% to 0.2%.

An accurate analytical model for the buckling analysis of FG-CNT reinforced composite beams resting on an elastic foundation with arbitrary boundary conditions

  • Aicha Remil;Mohamed-Ouejdi Belarbi;Aicha Bessaim;Mohammed Sid Ahmed Houari;Ahmed Bouamoud;Ahmed Amine Daikh;Abderrahmane Mouffoki;Abdelouahed Tounsi;Amin Hamdi;Mohamed A. Eltaher
    • Computers and Concrete
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    • v.31 no.3
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    • pp.267-276
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    • 2023
  • The main purpose of the current research is to develop an efficient two variables trigonometric shear deformation beam theory to investigate the buckling behavior of symmetric and non-symmetric functionally graded carbon nanotubes reinforced composite (FG-CNTRC) beam resting on an elastic foundation with various boundary conditions. The proposed theory obviates the use to shear correction factors as it satisfies the parabolic variation of through-thickness shear stress distribution. The composite beam is made of a polymeric matrix reinforced by aligned and distributed single-walled carbon nanotubes (SWCNTs) with different patterns of reinforcement. The material properties of the FG-CNTRC beam are estimated by using the rule of mixture. The governing equilibrium equations are solved by using new analytical solutions based on the Galerkin method. The robustness and accuracy of the proposed analytical model are demonstrated by comparing its results with those available by other researchers in the existing literature. Moreover, a comprehensive parametric study is presented and discussed in detail to show the effects of CNTs volume fraction, distribution patterns of CNTs, boundary conditions, length-to-thickness ratio, and spring constant factors on the buckling response of FG-CNTRC beam. Some new referential results are reported for the first time, which will serve as a benchmark for future research.

Effects of different levels of dietary crude protein on the physiological response, reproductive performance, blood profiles, milk composition and odor emission in gestating sows

  • Hongjun Kim;Xinghao Jin;Cheonsoo Kim;Niru Pan;Yoo Yong Kim
    • Animal Bioscience
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    • v.36 no.8
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    • pp.1263-1273
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    • 2023
  • Objective: This study was conducted to evaluate the effects of crude protein (CP) levels on the physiological response, reproductive performance, blood profiles, milk composition and odor emission in gestating sows. Methods: Seventy-two multiparous sows (Yorkshire×Landrace) of average body weight (BW), backfat thickness, and parity were assigned to one of six treatments with 10 or 11 sows per treatment in a completely randomized design. Experimental diets with different CP levels were as follows: i) CP11, corn-soybean-based diet containing 11% CP; ii) CP12, corn-soybean-based diet containing 12% CP; iii) CP13, corn-soybean-based diet containing 13% CP; iv) CP14, corn-soybean-based diet containing 14% CP; v) CP15, corn-soybean-based diet containing 15% CP; and vi) CP16: corn-soybean-based diet containing 16% CP. Results: There was no significant difference in the performance of sow or piglet growth when sows were fed different dietary protein levels. Milk fat (linear, p = 0.05) and total solids (linear, p = 0.04) decreased as dietary CP levels increased. Increasing dietary CP levels in the gestation diet caused a significant increase in creatinine at days 35 and 110 of gestation (linear, p = 0.01; linear, p = 0.01). The total protein in sows also increased as dietary CP levels increased during the gestation period and 24 hours postpartum (linear, p = 0.01; linear, p = 0.01). During the whole experimental period, an increase in urea in sows was observed when sows were fed increasing levels of dietary CP (linear, p = 0.01), and increasing blood urea nitrogen (BUN) concentrations were observed as well. In the blood parameters of piglets, there were linear improvements in creatinine (linear, p = 0.01), total protein (linear, p = 0.01), urea (linear, p = 0.01), and BUN (linear, p = 0.01) with increasing levels of dietary CP as measured 24 hours postpartum. At two measurement points (days 35 and 110) of gestation, the odor gas concentration, including amine, ammonia, and hydrogen sulfide, increased linearly when sows fed diets with increasing levels of dietary CP (linear, p = 0.01). Moreover, as dietary CP levels increased to 16%, the odor gas concentration was increased with a quadratic response (quadratic, p = 0.01). Conclusion: Reducing dietary CP levels from 16% to 11% in a gestating diet did not exert detrimental effects on sow body condition or piglet performance. Moreover, a low protein diet (11% CP) may improve dietary protein utilization and metabolism to reduce odor gas emissions in manure and urine in gestating sows.