• Title/Summary/Keyword: strong derivative

Search Result 114, Processing Time 0.025 seconds

Inhibitory effects of artemether on collagen-induced platelet aggregation via regulation of phosphoprotein inducing PI3K/Akt and MAPK

  • Lee, Dong-Ha
    • Journal of Applied Biological Chemistry
    • /
    • v.65 no.3
    • /
    • pp.167-172
    • /
    • 2022
  • Pathophysiological reaction of platelets in the blood vessel is an indispensable part of thrombosis and cardiovascular disease, which is the most common cause of death in the world. In this study, we performed in vitro assays to evaluate antiplatelet activity of artemether in human platelets and attempted to identify the mechanism responsible for protein phosphorylation. Artemether is a derivative of artemisinin, known as an active ingredient of Artemisia annua, which has been reported to be effective in treating malaria, and is known to function through antioxidant and metabolic enzyme inhibition. However, the role of artemether in platelet activation and aggregation and the mechanism of action of artemether in collagen-induced human platelets are not known until now. In this study, the effect of artesunate on collagen-induced human platelet aggregation was confirmed and the mechanism of action of artemether was clarified. Artemether inhibited the phosphorylation of PI3K/Akt and Mitogen-activated protein kinases, which are phosphoproteins that are known to act in the signal transduction process when platelets are activated. In addition, artemether decreased TXA2 production and decreased granule secretion in platelets such as ATP and serotonin release. As a result, artemether strongly inhibited platelet aggregation induced by collagen, a strong aggregation inducer secreted from vascular endothelial cells, with an IC50 of 157.92 μM. These results suggest that artemether has value as an effective antithrombotic agent for inhibiting the activation and aggregation of human platelets through vascular injury.

Antioxidant Effects of Fermented Anchovy (멸치액젓의 항산화효과)

  • Park, Jong-Ok;Yoon, Mi-Sun;Cho, Eun-Jung;Kim, Hee-Sook;Ryu, Byung-Ho
    • Korean Journal of Food Science and Technology
    • /
    • v.31 no.5
    • /
    • pp.1378-1385
    • /
    • 1999
  • The antioxidative activity of Fermented Anchovy on linoleic acid autooxidation was investigated in an aqueous system at pH 7.0. All solvent fractions from Fermented Anchovy were exhibited the strong antioxidative activity. Especially, BuOH and aqueous fractions were gained large amounts with strong antioxidative activity. Ultrafiltration, dialysis, heat treatment of aqueous fraction indicated that water-soluble antioxidants of Fermented Anchovy were heat-resistant, amino acid related compounds with smaller molecular weights than 1,000. Unbound fractions from DE-52 anion exchange chromatography were exhibited antioxidative activity with or without $15\;{\mu}M\;Fe^{+++}\;ion$. We were able to purify one methionine derivative from lots of antioxidative substances in Fermented Anchovy aqueous fraction by gel filtration, anion-exchange chromatography, TLC and HPLC, successfully. These data suggest that Fermented Anchovy aqueous fraction is a mixture of fermented small molecules with strong antioxidative activities.

  • PDF

Analysis of Interface Problem using the MLS Difference Method with Interface Condition Embedment (계면경계조건이 매입된 이동최소제곱 차분법을 이용한 계면경계문제 해석)

  • Yoon, Young-Cheol
    • Journal of the Computational Structural Engineering Institute of Korea
    • /
    • v.32 no.4
    • /
    • pp.215-222
    • /
    • 2019
  • The heat conduction problem with discontinuous material coefficients generally consists of the conservative equation, boundary condition, and interface condition, which should be additionally satisfied in the solution procedure. This feature often makes the development of new numerical schemes difficult as it induces a layered singularity in the solution fields; thus, a special approximation is required to capture the singular behavior. In addition to the approximation, the construction of a total system of equations is challenging. In this study, a wedge function is devised for enriching the approximation, and the interface condition itself is embedded in the moving least squares(MLS) derivative approximation to consistently satisfy the interface condition. The heat conduction problem is then discretized in a strong form using the developed derivative approximation, which is named as the interface immersed MLS difference method. This method is able to efficiently provide a numerical solution for such interface problems avoiding both numerical quadrature as well as extra difference equations related to the interface condition enforcement. Numerical experiments proved that the developed numerical method was highly accurate and computationally efficient at solving the heat conduction problem with interfacial jump as well as the problem with a geometrically induced interfacial singularity.

Modelling a Stand-Alone Inverter and Comparing the Power Quality of the National Grid with Off-Grid System

  • Algaddafi, Ali;Brown, Neil;Rupert, Gammon;Al-Shahrani, Jubran
    • IEIE Transactions on Smart Processing and Computing
    • /
    • v.5 no.1
    • /
    • pp.35-42
    • /
    • 2016
  • Developments in power electronics have enabled the widespread application of Pulse Width Modulation (PWM) inverters, notably for connecting renewable systems to the grid. This study demonstrates that a high-quality power can be achieved using a stand-alone inverter, whereby the comparison between the power quality of the stand-alone inverter with battery storage (off-grid) and the power quality of the utility network is presented. Multi-loop control techniques for a single phase stand-alone inverter are used. A capacitor current control is used to give active damping and enhance the transient and steady state inverter performance. A capacitor current control is cheaper than the inductor current control, where a small current sensing resistor is used. The output voltage control is used to improve the system performance and also control the output voltage. The inner control loop uses a proportional gain current controller and the outer loop is implemented using internal model control proportional-integral-derivative to ensure stability. The optimal controls are achieved by using the Sisotool tool in MATLAB/Simulink. The outcome of the control scheme of the numerical model of the stand-alone inverter has a smooth and good dynamic performance, but also a strong robustness to load variations. The numerical model of the stand-alone inverter and its power quality are presented, and the power quality is shown to meet the IEEE 519-2014. Furthermore, the power quality of the off-grid system is measured experimentally and compared with the grid power, showing power quality of off-grid system to be better than that of the utility network.

Cloning of Human Liver Cytosolic Sialidase from Genomic DNA Using Splicing by Overlap Extension and Its Characterization

  • HA KI-TAE;CHO SEUNG-HAK;KANG SUNG-KOO;KIM YEON-KYE;KIM JUNE-KI;KIM CHEORL-HO
    • Journal of Microbiology and Biotechnology
    • /
    • v.15 no.4
    • /
    • pp.722-727
    • /
    • 2005
  • Cytosolic sialidase (Neu2), a member of the sialidase family that is responsible for hydrolysis of sialic acid from the terminal position of sialoglycoconjugates, is poorly expressed in skeletal muscle and not detected in any other adult tissues. Thus, we isolated Neu2 cDNA using splicing by overlap extension (SOEing). In order to further characterize this enzyme, a His-tagged derivative was expressed in the bacterial expression system and purified by $Ni^{2+}$-affinity chromatography. A recombinant product of approximately 42 kDa had sialidase activity toward 4-methyl-umbelliferyl-$\alpha$-D-N-acetylneuraminic acid (4MU-NeuAc). The optimal pH and temperature of the recombinant Neu2 for 4MU-NeuAc was 6.0 and $37.5^{\circ}C$, respectively. The metal ions, such as $Cu^{2+}\;and\;Cd^{2+}$, showed strong inhibitory effect on the activity of the enzyme. The enzyme efficiently hydrolyzed the gangliosides GM3 and GD3 and had relatively low activities on ganglioside GD1a and GD1b, $\alpha$2-3 sialyllactose, and sialylated glycoproteins such as fetuin, transferrin, and orsomucoid, but had hardly any activities on $\alpha$2-6 sialyllactose and ganglioside GM1 and GM2. We concluded that the recombinant Neu2 has a sialidase activity toward glycoproteins as well as gangliosides.

Estimation of Genetic Parameters for Pork Belly Components in Yorkshire Pigs

  • Kang, H.S.;Lopez, B.M.;Kim, T.H.;Kim, H.S.;Kim, S.H.;Nam, K.C.;Seo, K.S.
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.28 no.7
    • /
    • pp.922-925
    • /
    • 2015
  • This study was conducted to estimate the genetic parameters for pork belly traits and muscles in Yorkshire pigs. Each pork belly was cut into nine parts perpendicular to the thoracic vertebrae (6th to 14th). Traits of belly muscles including the deep pectoral, latissimus dorsi, cutaneous trunci, rectus abdominis, external and internal abdominal oblique from 382 purebred pigs were recorded and analyzed using SAS Package (9.1) and Derivative-free restricted maximum likelihood methods. Heritability estimates for belly traits ranged from 0.27 to 0.49, while they were 0.12 to 0.66 for belly muscles. Moderate to high heritability estimates were noted in belly weight (0.33), belly length (0.28), and belly width (0.49). In belly muscles, the latissimus dorsi and deep pectoral, which are located only in the 6th to 9th vertebrae sections, were found to have heritability estimates ranging from 0.21 to 0.29 and 0.23 to 0.35, respectively. Strong heritability estimates were observed in the 7th to 13th sections of cutaneous trunci muscle ranging from 0.42 to 0.66. Genetic correlations of latissimus dorsi m. with belly length were positive (0.50), while cutaneous trunci m. with belly weight also revealed a positive relationship that ranged from 0.35 to 0.47. The estimated genetic parameters indicate that belly weight can be improved by genetic selection. Differences in the levels of heritability occurred among various parameters of Yorkshire pork belly, which should be considered when performing selection to improve pork belly quality. Moreover, these results can provide valuable information that can be used as the basis for further investigations to improve pork belly.

Improvement of a Sulfolobus-E. coli Shuttle Vector for Heterologous Gene Expression in Sulfolobus acidocaldarius

  • Hwang, Sungmin;Choi, Kyoung-Hwa;Yoon, Naeun;Cha, Jaeho
    • Journal of Microbiology and Biotechnology
    • /
    • v.25 no.2
    • /
    • pp.196-205
    • /
    • 2015
  • A Sulfolobus-E. coli shuttle vector for an efficient expression of the target gene in S. acidocaldarius strain was constructed. The plasmid-based vector pSM21 and its derivative pSM21N were generated based on the pUC18 and Sulfolobus cryptic plasmid pRN1. They carried the S. solfataricus P2 pyrEF gene for the selection marker, a multiple cloning site (MCS) with C-terminal histidine tag, and a constitutive promoter of the S. acidocaldarius gdhA gene for strong expression of the target gene, as well as the pBR322 origin and ampicillin-resistant gene for E. coli propagation. The advantage of pSM21 over other Sulfolobus shuttle vectors is that it contains a MCS and a histidine tag for the simple and easy cloning of a target gene as well as one-step purification by histidine affinity chromatography. For successful expression of the foreign genes, two genes from archaeal origins (PH0193 and Ta0298) were cloned into pSM21N and the functional expression was examined by enzyme activity assay. The recombinant PH0193 was successfully expressed under the control of the gdhA promoter and purified from the cultures by His-tag affinity chromatography. The yield was approximately 1 mg of protein per liter of cultures. The enzyme activity measurements of PH0913 and Ta0298 revealed that both proteins were expressed as an active form in S. acidocaldarius. These results indicate that the pSM21N shuttle vector can be used for the functional expression of foreign archaeal genes that form insoluble aggregates in the E. coli system.

Safening Activity of Optically Active ${\alpha}$-Methylbenzylphenylurea toward Bensulfuron-methyl and Pyribenzoxim Injury to Rice (광학활성 ${\alpha}$-Methylbenzylphenylurea 유도체의 bensulfuron-methyl과 pyribenzoxim의 벼에 대한 약해경감효과)

  • Ryoo, Jae-Hwan
    • The Korean Journal of Pesticide Science
    • /
    • v.9 no.2
    • /
    • pp.153-158
    • /
    • 2005
  • Safening activities of optically active ${\alpha}$-methylbenzylphenylureas on crop injury of rice (Oryza sativa L., cv. Tsukinohikari, japonica) caused by bensulfuron-methyl (methyl 2-[[[[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]amino]sulfonyl]methyl]benzoate) and pyribenzoxim (benzophenone o-[2,6-bis[(4,6-dimethoxy-2-pyrimidinyl)oxy]benzoyl]oxime) were investigated. Some derivatives of the optically active compounds exhibited strong safening activity against growth inhibition of rice by bensulfuron-methyl. Out of the derivatives tested, (S)-2,3-diCl and (S)-2-F-4-Me derivatives showed greater relieving activity than that of dymuron. In addition, the stress relieving activity was also obtained when they were applied at 4 days after bensulfuron-methyl treatment. On the other hand, crop injury caused by pyribenzoxim was relieved by about 95% with (S)-2-F-4-Me derivative in shoots and roots of rice seedlings.

AN EXPERIMENTAL STUDY ON THE CHEMOPREVENTIVE EFFECT OF CHLOROPHYLLIN IN HAMSTER CHEEK POUCH TUMOR INDUCED BY 7, 12-DIMETHYLBENZ[A]ANTHRACENE (7, 12-dimethylbenz[a]anthracene(DMBA)로 유발된 햄스터 협낭암에서 chlorophylln의 암예방효과에 관한 실험적 연구)

  • Yoon, Kyu-Ho
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
    • /
    • v.26 no.2
    • /
    • pp.137-145
    • /
    • 2000
  • Carcinogenesis is a multi-stage process that generally consists of at least three steps; initiation, promotion, and progression. If one of these carcinogenic steps were suppressed or delayed, the cancer could be prevented. Cancer chemoprevention is defined to be inhibition or reversal of the carcinogenic process by the specific chemical agents and is a novel approach to cancer management alternative to conventional chemotherapy. Chlorophylln(CHL), a water-soluble derivative of chlorophyll, containing sodium and copper, has been known to be strong antimutagen in several test systems, but its mechanism of antimutagenic action is unknown. In the present experiment, the possibility of CHL as chemopreventive drugs on 7,12-dimethylbenz[a]anthracene(DMBA)-induced hamster buccal pouch carcinogenesis was investigated by mutagenicity test, carcinogenicity test, and frequency or spectrum of H-ras mutations in the both of DMBA-induced and chlorophylln-pretreated-DMBA induced tumor by polymerase chain reaction and non-isotopic restriction fragment length polymorphism. The treatment of CHL reduced the yields and multiplicity of the 0.5% DMBA-induced tumor, 86% to 62.5% and $3.7{\pm}0.6$ to $1.4{\pm}0.3$, respectively. The occurrence of histidine revertant by $20{\mu}mole$ DMBA was inhibited 25.6 to 81.7% by 1 to $5{\mu}M$ CHL in a dose-dependent manner. The mutation rates of H-ras gene in DMBA-induced and CHL-pretreated-DMBA induced tumor were 96%, 94% of which the most mutations were in codon 12/13. These results suggest that CHL inhibits the carcinogenic action of DMBA by the formation of complex between CHL and DMBA or the inhibition of the activation of DMBA in vivo. But CHL did not affect the mutation rates or its spectrum in already formed tumor.

  • PDF

Optical Gap Bowing and Phonon Modes of Amorphous Ge1-x-ySexAsy Thin Films

  • So, Hyeon-Seop;Park, Jun-U;Jeong, Dae-Ho;Lee, Ho-Seon;Sin, Hye-Yeong;Yun, Seok-Hyeon;An, Hyeong-U;Kim, Su-Dong;Lee, Su-Yeon;Jeong, Du-Seok;Jeong, Byeong-Gi
    • Proceedings of the Korean Vacuum Society Conference
    • /
    • 2014.02a
    • /
    • pp.288.1-288.1
    • /
    • 2014
  • We investigated the optical properties of Ge1-xSex and Ge1-x-ySexAsy amorphous semiconductor films using spectroscopic ellipsometry and Raman spectroscopy. The dielectric functions and absorption coefficients of the amorphous films were determined from the measured ellipsometric angles. We obtained the optical gap energies and Urbach energies from the absorption coefficients, and found a strong bowing effect in the optical gap energy of Ge1-x-ySexAsy where the endpoint binaries were Ge0.50Se0.50 and Ge0.31As0.69. Based on the correlation between optical gap energies and Urbach energies, the large bowing parameter was attributed to the electronic disorder. We found the composition dependence of several phonon modes using Raman spectroscopy. For Ge1-x-ySexAsy, the D mode (232-267 cm-1) changed from As-As (or As3 pyramid), to As(Se1/2)3 pyramid, and finally to Se clusters, as the Se composition increased. Resonant Raman phenomenon was observed in Ge0.38Se0.62 at a laser excitation of 514 nm (2.41 eV). We verified that this laser energy corresponds to the transition energy of Ge0.38Se0.62 using the second derivative of the dielectric function of Ge0.38Se0.62.

  • PDF