• Title/Summary/Keyword: Control derivatives

Search Result 410, Processing Time 0.024 seconds

Novel Anticandidal Activity of a Recombinant Lampetra japonica RGD3 Protein

  • Wu, Caiping;Lu, Li;Zheng, Yuanyuan;Liu, Xin;Xiao, Rong;Wang, Jihong;Li, Qingwei
    • Journal of Microbiology and Biotechnology
    • /
    • v.24 no.7
    • /
    • pp.905-913
    • /
    • 2014
  • Lj-RGD3, an RGD (Arg-Gly-Asp) toxin protein from the salivary gland of Lampetra japonica, exhibits antifungal activity against Candida albicans. Lj-RGD3 has three RGD motifs and shows homology to histidine-rich glycoprotein. We synthesised two mutant derivatives of Lj-RGD3: Lj-26, which lacks all three RGD motifs and contains no His residues; and Lj-112, which lacks only the three RGD motifs. We investigated the effects of the wild-type and mutated toxins on a gram-positive bacterium (Escherichia coli), a gram-negative bacterium (Staphylococcus aureus), and a fungus (C. albicans). rLj-RGD3 and its mutants exhibited antifungal but not antibacterial activity, as measured by a radial diffusion assay. The C. albicans inhibition zone induced by rLj-112 was larger than that induced by the other proteins, and its inhibitory effect on C. albicans was dose-dependent. In viable-count assays, the rLj-112 MIC was $7.7{\mu}M$, whereas the MIC of the positive control (ketoconazole) was $15{\mu}M$. Time-kill kinetics demonstrated that rLj-112 effectively killed C. albicans at $1{\times}$ and $2{\times}$ MIC within 12 and 6 h, respectively. Electron microscopy analysis showed that rLj-RGD3 and rLj-112 induced C. albicans lysis. Our results demonstrate a novel anticandidal activity for rLj-RGD3 and its mutant derivatives.

Agarwood Inhibits Histamine Release from Rat Mast Cells and Reduces Scratching Behavior in Mice -Effect of Agarwood on Histamine Release and Scratching Behavior-

  • Inoue, Eiji;Shimizu, Yasuharu;Masui, Ryo;Tsubonoya, Tomoe;Hayakawa, Tomomi;Sudoh, Keiichi
    • Journal of Pharmacopuncture
    • /
    • v.19 no.3
    • /
    • pp.239-245
    • /
    • 2016
  • Objectives: This study was conducted to clarify the effects of agarwood on histamine release from mast cells in rats and on the scratching behaviors in mice. Methods: Histamine release from rat mast cells induced by compound 48/80 or concanavalin A (Con A) and compound 48/80-induced scratching behavior in mice were examined to investigate the effects of agarwood. The hyaluronidase activity and the 3',5'-cyclic adenosine monophosphate (cAMP) levels in mast cells were examined to investigate the mechanisms for the inhibition of histamine release. The correlation between the inhibitory effects of agarwood on histamine release and the content of its typical ingredients, a 2-(2-phenylethyl)chromone derivatives, was analyzed using thin-layer chromatography. Results: Agarwood showed an inhibitory effect on mast-cell histamine release induced by compound 48/80 or Con A without any effect on hyaluronidase activity; this effect involves an increase in the cAMP levels in mast cells. Oral administration of agarwood showed an inhibitory effect on compound 48/80-induced scratching behavior in mice. The inhibitory effects of agarwood on histamine release were quite different, depending on the area where the agarwood was produced, its quality, and its market price. No correlation was found between the inhibitory effects of agarwood on histamine release and the typical ingredients of agarwood, which are 2-(2-phenylethyl)chromone derivatives. Conclusion: These results show that agarwood inhibits histamine release from mast cells partially through an increase in the cAMP levels in cells. We suggest that some active ingredients of agarwood must be effective on oral intake and that agarwood can be used to treat patients with a number of conditions, including urticaria, atopic dermatitis, and bronchial asthma, in which an increase in histamine release occurs. Differences in the pharmacological effects of this crude drug among markets may provide important information for the quality control of this herbal medicine.

An Experimental Study on the Ion Reaction and the Electrochemical Rebar-Corrosion in Aqueous Solution Mixed with Sulfate and Chloride Ion-Reactive Material (황산, 염소이온 반응 소재 혼입 수용액에서의 이온반응성 및 전기화학적 철근 부식에 관한 실험적 연구)

  • Ryu, Hwa-Sung;Shin, Sang-Heon;Kang, Tae-Won;Lim, Chang-Gil;Kim, Hong-Tae
    • Journal of the Korea Institute of Building Construction
    • /
    • v.19 no.1
    • /
    • pp.31-38
    • /
    • 2019
  • In this study, amine derivatives and ion exchange resins were selected to actively control penetration ions ($SO{_4}^{2-}$, $Cl^-$) as the element technology of repair materials for concrete structures in drainage environments. Ions ($SO{_4}^{2-}$, $Cl^-$) adsorption performance and corrosion resistance of calcium hydroxide solution with amine derivative and ion exchange resin were confirmed by ion chromatography and potentiostat analysis. As a result of the experiment, it was confirmed that the amine derivative is excellent in the adsorption of chlorine ion and the ion exchange resin is excellent in the adsorption of sulfate ion. It has been confirmed that corrosion resistance can be increased by proper combination of two materials in the calcium hydroxide solution containing sulfate ion and chloride ion simulating sewage environment.

Numerical Modelling Techniques of VPMM for Manta Type UUV (만타형 UUV의 VPMM 전산해석기법 개발)

  • Sang-Eui Lee
    • Proceedings of the Korean Institute of Navigation and Port Research Conference
    • /
    • 2023.05a
    • /
    • pp.151-151
    • /
    • 2023
  • An accurate prediction of the hydrodynamic maneuvering darivatives is essential to desing a robust control system of a UUV(unmanned underwater vehicle). Typically, these derivatives were estimated by either the towing tank experiment or semi-empirical methods. With the enhancement of high performance computing capacity, a numerical analysis using computational fluid dynamics has reach the level of experiment. Therefore, the aims of the present research are to numerically develop a computational model for the vertical planar motion mechanism of a UUV and to estimate the hydrodynamics loads in 6-DOF. The target structure of the present study was manta type UUV (12meter length). The numerical model was developed in 1/ 6 model scale. Numerical results were compared with the results of the towing tank experiment for validation. In the present study, a commercial RANS-based viscous solver STARCCM+ (ver 17.06) was used.

  • PDF

Effects of Polychlorinated Biphenyls and Phenols on the Biosynthesis of 6-Methoxymellein, a Phytoalexin (당근 Phytoalexin 6-Methoxymellein 생합성에 미치는 Polychlorinated Biphenyls 및 Phenol의 영향)

  • Lim, Do-Hyung;Lim, Da-Som;Keum, Young-Soo
    • Korean Journal of Environmental Agriculture
    • /
    • v.35 no.3
    • /
    • pp.216-222
    • /
    • 2016
  • BACKGROUND: Polychlorinated biphenyls (PCBs) are one of the most common environmental contaminants. Because of their recalcitrant properties and long-term toxicity, numerous studies have been performed. The toxicological concerns are focused on endocrinological effects of animal. Several different metabolites have been reported, including hydroxy PCBs, PCB quinones, and methylsulfonyl PCBs from animal tissues. However, details in plants have never been studied. It is well-known that plants can produce phytoalexin in response to chemical, physical, or pathological stress.METHODS AND RESULTS: In this study, the several PCBs and hydroxy derivatives were prepared by chemical syntheses. Their effects on secondary metabolite biosynthesis were determined in carrot roots. The levels of 6-methoxymellein were determined in several different treatments, using gas chromatography-mass spectrometry. In general, the concentration of 6-methoxymellein reached a maximum at 2 days and gradually decreased to trace level at 5 days in control experiments. However, the effects of PCBs or hydroxy derivatives were highly dependent on compounds. For example, the maximum concentrations of 6-methoxymellein were observed at 3 days for 2-hydroxy/4-hydroxybiphenyl, while 3,3',4,4',5-pentachlorobiphenyl and 3,5-dichloro-2-hydroxybiphenyl showed a rapid accumulation within 1 day, followed by rapid dissipation to undetectable levels.CONCLUSION: Biphenyl derivatives were effective elicitor of 6-methoxymellein accumulation. In general, hydroxybiphenyls (phenols) more efficiently induced phytoalexin biosynthesis than those without hydroxy groups. It can be concluded that PCBs or their possible metabolites could change the plant secondary metabolism.

Molecular Orbital Theoretical Study on the Conformation and Chemical Reactivity of Insecticidal 0,0-Diethylphenylphosphate Derivatives (살충성(殺蟲性) 0,0-Diethylphenylphosphate 유도체(誘導體)의 형태(形態)와 반응성(反應性)에 관(關)한 분자궤도론적(分子軌度論的) 연구(硏究))

  • Park, Seung-Heui;Sung, Nack-Do;Myung, Pyung-Keun;Jeon, Young-Koo;Lee, Chun-Bae
    • Korean journal of applied entomology
    • /
    • v.24 no.4 s.65
    • /
    • pp.231-238
    • /
    • 1986
  • Molecular orbital theoretical study on the stability of conformations and chemical reactivity of 0,0-diethylphenylphosphate derivatives were carried out by EHT and CNDO/2 molecular orbital calculation method. The results shown that the dipole moment(${\mu}$) and total energies of the ${\theta}=90^{\circ}$ conformer were ${\mu}=3.185D\;&\;E_t=-162.6479(au)$ and also that of the ${\theta}=0^{\circ}$ conformer were ${\mu}=5.596D\;&\;E_t=-162.4013(au)$, respectively. Therefore, the values of ${\mu}\;&\;E_t$ of the ${\theta}=90^{\circ}$ conformer were much smaller than that of the ${\theta}=0^{\circ}$ conformer. The form with angle of rotation ${\theta}=90^{\circ}$ of phenyl ring was shown to be most stable and this was interpreted in terms of electrostatic and steric effect. 0,0-diethylphenylphosphate derivatives are predicted to increase both charge and orbital controlled $SN_2$ reactivity of the electron withdrawing substituent reduces the HOMO & LUMO energy, while the electron withdrawing substituent due to increase in positive charge of phosphorus atom of phosphate molecule.

  • PDF

Level Set Based Shape Optimization of Linear Structures using Topological Derivatives (위상민감도를 이용한 선형구조물의 레벨셋 기반 형상 최적설계)

  • Yoon, Minho;Ha, Seung-Hyun;Kim, Min-Geun;Cho, Seonho
    • Journal of the Computational Structural Engineering Institute of Korea
    • /
    • v.27 no.1
    • /
    • pp.9-16
    • /
    • 2014
  • Using a level set method and topological derivatives, a topological shape optimization method that is independent of an initial design is developed for linearly elastic structures. In the level set method, the initial domain is kept fixed and its boundary is represented by an implicit moving boundary embedded in the level set function, which facilitates to handle complicated topological shape changes. The "Hamilton-Jacobi(H-J)" equation and computationally robust numerical technique of "up-wind scheme" lead the initial implicit boundary to an optimal one according to the normal velocity field while minimizing the objective function of compliance and satisfying the constraint of allowable volume. Based on the asymptotic regularization concept, the topological derivative is considered as the limit of shape derivative as the radius of hole approaches to zero. The required velocity field to update the H-J equation is determined from the descent direction of Lagrangian derived from optimality conditions. It turns out that the initial holes are not required to get the optimal result since the developed method can create holes whenever and wherever necessary using indicators obtained from the topological derivatives. It is demonstrated that the proper choice of control parameters for nucleation is crucial for efficient optimization process.

Development of Functional Halogenated Phenylpyrrole Derivatives (기능성 할로겐화 페닐피롤 )

  • Min-Hee Jung;Hee Jeong Kong;Young-Ok Kim;Jin-Ho Lee
    • Journal of Life Science
    • /
    • v.33 no.10
    • /
    • pp.842-850
    • /
    • 2023
  • Pyrrolnitrin, pyrrolomycin, and pyoluteorin are functional halogenated phenylpyrrole derivatives (HPDs) derived from microorganisms with diverse antimicrobial activities. Pyrrolnitrin is a secondary metabolite produced from L-tryptophan through four-step reactions in Pseudomonas fluorescens, Burkholderia cepacia, Serratia plymuthica, etc. It is currently used for the treatment of superficial dermatophytic fungal infections, has high antagonistic activities against soil-borne and foliar fungal infections, and has many industrial applications. Since pyrrolnitrin is easily decomposed by light, it is difficult to widely use it outdoors. As an alternative, fludioxonil, a synthetically produced non-systemic surface fungicide that is structurally similar and has excellent light stability, has been commercialized for seed and foliar treatment of plants. However, due to its high toxicity to aquatic organisms and adverse effects in human cell lines, many countries have established maximum residue levels and strictly control its levels. Pyrrolomycin and pyoluteorin, which have antibiotic/antibiofilm activity against Gram-positive bacteria and high anti-oomycete activity against the plant pathogen Pythium ultimum, respectively, were isolated and identified from microorganisms. This review summarizes the biosynthesis and production of natural pyrrolnitrin derived from bacteria and the characteristics of synthetic fludioxonil and other natural phenylpyrrole derivatives among the HPDs. We expect that a plethora of highly effective, novel HPDs that are safe for humans and environments will be developed through the generation of an HPD library by microbial biosynthesis and chemical synthesis.

Gelsolin Induces Promonocytic Leukemia Differentiation Accompanied by Upregulation of p21CIP1

  • Shirkoohi, Reza;Fujita, Hisakazu;Darmanin, Stephanie;Takimoto, Masato
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.13 no.9
    • /
    • pp.4827-4834
    • /
    • 2012
  • Tumor suppressor genes have received much attention for their roles in the development of human malignancies. Gelsolin has been found to be down-regulated in several types of human cancers, including leukemias. It is, however, expressed in macrophages, which are the final differentiation derivatives for the monocytic myeloid lineage, implicating this protein in the differentiation process of such cells. In order to investigate the role of gelsolin in leukaemic cell differentiation, stable clones over-expressing ectopic gelsolin, and a control clone were established from U937 leukaemia cells. Unlike the control cells, both gelsolin-overexpressing clones displayed retarded growth, improved monocytic morphology, increased NADPH and NSE activities, and enhanced surface expression of the ${\beta}$-integrin receptor, CD11b, when compared with the parental U937 cells. Interestingly, RT-PCR and western blot analysis also revealed that gelsolin enhanced p21CIP1 mRNA and protein expression in the overexpressing clones. Moreover, transient transfection with siRNA silencing P21CIP1, but not the control siRNA, resulted in a reduction in monocytic differentiation, accompanied by an increase in proliferation. In conclusion, our work demonstrates that gelsolin, by itself, is capable of inducing monocytic differentiation in U937 leukaemia cells, most probably through p21CIP1 activation.

Compact Current Model of Single-Gate/Double-Gate Tunneling Field-Effect Transistors

  • Yu, Yun Seop;Najam, Faraz
    • Journal of Electrical Engineering and Technology
    • /
    • v.12 no.5
    • /
    • pp.2014-2020
    • /
    • 2017
  • A compact current model applicable to both single-gate (SG) and double-gate (DG) tunneling field-effect transistors (TFETs) is presented. The model is based on Kane's band-to-band tunneling (BTBT) model. In this model, the well-known and previously-reported quasi-2-D solution of Poisson's equation is used for the surface potential and length of the tunneling path in the tunneling region. An analytical tunneling current expression is derived from expressions of derivatives of local electric field and surface potential with respect to tunneling direction. The previously reported correction factor with three fitting parameters, compensating for superlinear onset and saturation current with drain voltage, is used. Simulation results of the proposed TFET model are compared with those from a technology computer-aided-design (TCAD) simulator, and good agreement in all operational bias is demonstrated. The proposed SG/DG-TFET model is developed with Verilog-A for circuit simulation. A TFET inverter is simulated with the Verilog-A SG/DG-TFET model in the circuit simulator; the model exhibits typical inverter characteristics, thereby confirming its effectiveness.