• Title/Summary/Keyword: derivatives$

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Enzymatic Synthesis of Anabolic Steroid Glycosides by Glucosyltransferase from Terribacillus sp. PAMC 23288

  • Yu, Eun-Ji;Yamaguchi, Tokutaro;Lee, Joo-Ho;Lim, A-Rang;Lee, Jun Hyuck;Park, Hyun;Oh, Tae-Jin
    • Journal of Microbiology and Biotechnology
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    • v.30 no.4
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    • pp.604-614
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    • 2020
  • The application of steroids has steadily increased thanks to their therapeutic effects. However, alternatives are required due their severe side effects; thus, studies on the activities of steroid derivatives are underway. Sugar derivatives of nandrolone, which is used to treat breast cancer, as well as cortisone and prednisone, which reduce inflammation, pain, and edema, are unknown. We linked O-glucose to nandrolone and testosterone using UDP-glucosyltransferase (UGT-1) and, then, tested their bioactivities in vitro. Analysis by NMR showed that the derivatives were 17β-nandrolone β-ᴅ-glucose and 17β-testosterone β-ᴅ-glucose, respectively. The viability was higher and cytotoxicity was evident in PC12 cells incubated with rotenone and, testosterone derivatives, compared to the controls. SH-SY5Y cells incubated with H2O2 and nandrolone derivatives remained viable and cytotoxicity was attenuated. Both derivatives enhanced neuronal protective effects and increased the amounts of cellular ATP.

Synthesis and Physical Properties of Bioc'ompatible and Biodegradable Chitin Derivatives V. -Biodegradation of liquid Crystalline Chitin Derivatives by Lysozyme- (생체적합성과 생분해성을 갖는 키틴유도체의 합성과 물성V -라이소자임에 의한 액정성 키틴 유도체의 생분해특성-)

  • 김선정;이영무
    • Journal of Biomedical Engineering Research
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    • v.15 no.1
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    • pp.89-96
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    • 1994
  • The ether-type chitin derivatives were synthesized by reacting chitin with chloropropane, propylene oxide and chloropropane diol to form propyl chitin(PPC), hydroxypropyl chitin(HPC) and dihydroxypropyl chitin(DHPC). These derivatives formed a lyotropic cholesteric liquid crystallinity in concentrations over 30 wt% solution in formic acid (99%). Cast films from liquid crystalline solutions were degraded by lysozyme in pseudo-extra cellular tluid(PECF)solutions, at pH 1.2, pH 6.7 and pH 8.2. Three ether-type chitin derivatives rapidly degraded within the first week, and showed a decreased mechanical strength in neutral pH range. Dihydroxypropyl chitin showed the best biodegradation among these derivatives.

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A Study on the Identification Method for Flutter Derivatives of Bridge Girders using Displacement Time History Data (변위 시계열 데이터를 이용한 교량거더의 Flutter 계수 추정기법에 관한 연구)

  • Lee, Jae Hyung;Min, Won;Lee, Yong Jae
    • Journal of Korean Society of Steel Construction
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    • v.13 no.5
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    • pp.525-533
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    • 2001
  • The wind resistant design of long-span bridges has urged a special attention to the prevention of the flutter occurrence Therefore calculation of flutter derivatives is indispensable to this prediction. A used system identification method must identify all the flutter derivatives from noisy experimental data In this paper MITD(Modified Ibrahim Tim Domain) method and AKF (Adaptive Kalman Filter) method are applied to extract flutter derivatives from section-model tests. The robustness and reliability of proposal SI methods under a high signal-to-noise ratio is demonstrated through numerical simulation for windtunnel test.

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Effect of Phenazine Dioxide Derivatives on the Hepatic Xanthine Oxidase Activity (Phenazine dioxide 유도체가 간 Xanthine Oxidase 활성에 미치는 영향)

  • Kang, Il-Young;Kim, Sang-Yul;Kim, Ho-Shik;Huh, Keun
    • YAKHAK HOEJI
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    • v.34 no.2
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    • pp.112-116
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    • 1990
  • 8-Acyl-2-hydroxyphenzaine -5, 10-dioxides and 8-acyl-2-aminophenazine-5, 10-dioxides bearing n-butanoyl, n-hexanoyl and n-octanoyl groups were synthesized. It was attempted to observe the effect of phenazine dioxide derivatives on the hepatic xanthine oxidase activity in this study. As the activity of xanthine oxidase, the key enzyme in the generation of superoxide anion radical ($O_2$), was measured in the presence of phenazine dioxide derivatives, the action of 8-acyl-2-hydroxyphenazine-5,10-dioxide derivatives inhibited with increase of numbers of carbon atom bearing 8-acyl group. Moreover, when plotted on double reciprocal form, the Vmax value decrease as increase of numbers of carbon atom bearing acyl groups without affecting the Km value. However, the hepatic xanthine oxidase activity was not changed by 8-acyl-2-aminophenazine-5,10-dioxide derivatives.

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Liquid Chromatographic Resolution of α-Amino Acid Esters as Benzophenone Imine Derivatives (아미노산 에스테르의 벤조피논 이민 유도체의 액체 크로마토그래피의 광학분리)

  • Yun, Won-Nam;Xu, Wen Jun;Huang, Hu;Lee, Won-Jae
    • KSBB Journal
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    • v.27 no.3
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    • pp.167-171
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    • 2012
  • A convenient liquid chromatographic enantiomer separation of several ${\alpha}$-amino acid esters as benzophenone Schiff base derivatives on covalently immobilized chiral stationary phases (CSPs) derived from polysaccharide derivatives was developed. The benzophenone imine derivatives of ${\alpha}$-amino acid esters were readily prepared by stirring benzophenone imine and the ${\alpha}$-amino acid ester hydrochloride salts in 2-propanol. The chromatographic conditions used on all CSPs were 0.5% or 5% 2-propanol/hexane (V/V) as the mobile phases at 1 mL/min of flow rate and UV 254 nm detection. The performance of Chiralpak IC among all CSPs was superior to that of the other CSPs for resolution of benzophenone imine derivatives of ${\alpha}$-amino acid esters. It is expected that the developed analytical method will be useful for enantiomer resolution of other ${\alpha}$-amino acid esters as benzophenone Schiff base derivatives.

Light Emitting Characteristics of Multi-layer OLEO Fabricated with DCM (DCM 계열을 이용한 OLED의 전기적인 발광 특성에 관한 연구)

  • Chun, Min-Ho;Yun, Suk-Won;Lim, Sung-Tack;Shin, Dong-Myung
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2002.04b
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    • pp.57-60
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    • 2002
  • In generally, the guest-emitter doped system has been reported to give a bright electroluminescence(EL). The purpose of using doped system is to improve for increasing lifetime and efficiency, and tuning multicolor light. This indicates an enhanced electron-hole recombination rate in emitting layer. The purpose of this study is to obtain the high performance EL devices for flat panel display with red emission. We fabricated EL devices using the guest-host system. where DCM derivatives were taken as a dopant. The devices are fabricated in multilayer system with various concentration of the dopant (red light emitting dye). We measured the I-V characteristics and EL spectra from these devices. and we compared with photoluminescence(PL) quantum yield among the DCM derivatives. The emission mechanism of devices is participated in energy transfer. The energy transfer from these hosts to DCM generates luminescence spectra that vary from yellow red to red, depending on DCM derivatives. Absorption and emission spectra of organic materials composing the devices depend on the emission materials doped with the DCM derivatives. We demonstrated that the high EL efficiency can be achieved by doping host material with DCM derivatives and molecular steric structures

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Liquid Chromatographic Reaolution of N-Protected α -Amino Acids as Their Anilide and 3,5-Dimethylanilide Derivatives on Chiral Syationary Phases Derived fron (S)-Leucine

  • Hyun, Myung-Ho;Cho, Yoon-Jae;Baik, In-Kyu
    • Bulletin of the Korean Chemical Society
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    • v.23 no.9
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    • pp.1291-1294
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    • 2002
  • Various racemic N-protected ${\alpha}-amino$ acids such as N-t-BOC-(tert-butoxycarbonyl), N-CBZ-(benzyloxycarbonyl) and N-FMOC-(9-fluorenylmethyloxycarbonyl) ${\alpha}-amino$ acids were resolved as their anilide and 3,5-dimethylanilde derivatives on an HPLC chira l stationary phase (CSP) developed by modifying a commercial (S)-leucine CSP. The chromatographic resolution results were compared to those on the commercial (S)-leucine CSP. The resolutions were greater on the modified CSP than those on the commercial CSP with only one exception, the resolution of N-t-BOC-phenylglycine anilide. In addition, the chromatographic resolution behaviors were quite consistent except for the resolution of N-protected phenylglycine derivatives, the (S)-enantiomers being retained longer. Based on the chromatographic resolution behaviors and with the aid of CPK molecular model studies, we proposed a chiral recognition mechanism for the resolution of N-protected ${\alpha}-amino$ acid derivatives. However, for the resolution of N-protected phenylglycine derivatives, a second chiral recognition mechanism, which competes in the opposite sense with the first chiral recognition mechanism, was proposed. The two competing chiral recognition mechanisms were successfully used in the rationalization of the chromatographic behaviors for the resolution of N-protected phenylglycine derivatives.

Effects of Low Dose Gamma Radiation on the Formation of Shikonin Derivatives on Callus Cultures of Lithospermum erythrorhizon (지치(Lithospermum erythrorhizon S.)의 캘러스배양에서 Shikonin 유도체 생산에 미치는 저선량γ선의 효과)

  • Hwang, Hye-Yeon;Kim, Jae-Sung;Lee, Young-Bok
    • Journal of Plant Biotechnology
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    • v.30 no.3
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    • pp.293-299
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    • 2003
  • The effects of low dosage ${\gamma}$-radiation on the cell growth and the formation of shikonin derivatives were investigated in callus cultures of Lithospermum erythrorhizon under different medium and light conditions. Gamma radiation significantly affected the cell growed and formation of shikonin derivatives, depending on the culture conditions. In the cell cultures grown on M-9 medium, 2Gy and 16Gy of ${\gamma}$-radiation increased the calli growth and the formation of shikonin derivatives, respectively under 16hr day light condition. When calli were cultured for 60 days in the dark after irradiation of ${\gamma}$-radiation, cell growth was increased at low dosage of 1Gy and 2Gy in LS medium containing BA 2mg/L and IAA 0.2mg/L. Interestingly, calli grown in M-9 medium by 2Gy irradiation for 60 days significantly stimulated the formation of shikonin derivatives(13.21mg/g cell fresh wt), which was approximately 6 times higher than untreated cells.

Structural Dynamics Optimization by Second Order Sensitivity with respect to Finite Element Parameter (유한요소 구조 인자의 2차 민감도에 의한 동적 구조 최적화)

  • Kim, Yong-Yun
    • Transactions of the Korean Society of Machine Tool Engineers
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    • v.15 no.3
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    • pp.8-16
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    • 2006
  • This paper discusses design sensitivity analysis and its application to a structural dynamics modification. Eigenvalue derivatives are determined with respect to the element parameters, which include intrinsic property parameters such as Young's modulus, density of the material, diameter of a beam element, thickness of a plate element, and shape parameters. Derivatives of stiffness and mass matrices are directly calculated by derivatives of element matrices. The first and the second order derivatives of the eigenvalues are then mathematically derived from a dynamic equation of motion of FEM model. The calculation of the second order eigenvalue derivative requires the sensitivity of its corresponding eigenvector, which are developed by Nelson's direct approach. The modified eigenvalue of the structure is then evaluated by the Taylor series expansion with the first and the second derivatives of eigenvalue. Numerical examples for simple beam and plate are presented. First, eigenvalues of the structural system are numerically calculated. Second, the sensitivities of eigenvalues are then evaluated with respect to the element intrinsic parameters. The most effective parameter is determined by comparing sensitivities. Finally, we predict the modified eigenvalue by Taylor series expansion with the derivatives of eigenvalue for single parameter or multi parameters. The examples illustrate the effectiveness of the eigenvalue sensitivity analysis for the optimization of the structures.

Effect of 1-[(2-Hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) Derivatives on Bacterial Growth

  • Gang, Jin-Gu;Yun, Hong-Chul;Son, Jong-Chan;Hwang, Se-Young
    • Journal of Microbiology and Biotechnology
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    • v.8 no.3
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    • pp.229-236
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    • 1998
  • 6-Substituted derivatives of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) were synthesized by introducing alkyl groups with the aid of chlorotrimethylsilane, and then purified ranging 40 to 81 % of yield. Because of their peculiar structures, we presumed that HEPT derivatives would contain extra biological activities other than their already known anti-human immunodeficiency viral (HIV -1) activities. In this study, we investigated the possible effects of the HEPT derivatives on bacterial growth and found their selective antibiotic activities against gram-positive strains. We could not observe the corresponding activity from a disc-zone test, but confirmed the activity by liquid cultivation. Since the growth rate of cells was easily recovered, the antibiotic function was suggested to be bacteriostatic. We also suggested that the intracellular fate of HEPT derivatives would be fast. A HEPT derivative f-3 was shown to synergize unidirectionally toward chloramphenicol (Chr). With 0.1 mM f-3, the Chr-directed growth-inhibitory curve appeared 4 hours earlier than found without the additive. Interestingly, from the data of SDS-polyacrylamide gel electrophoresis (PAGE), we found that a membrane-bound protein having a molecular weight of 70-kDa was overexpressed by f-3 in S. aureus.

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