• Title/Summary/Keyword: 1%2C4-DHP

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The Stability Test of New Carbapenem DWP20418 and Partial Purification and Characterization of Renal Dehydropeptidase-I (돼지 신장으로부터 디펩티다제의 부분정제 및 그에 대한 신규 카바페넴계 항생물질 DWP20418의 안정성 평가)

  • Kim, Ji-Yeon;Park, Nam-Jun;Yu, Young-Hyo;Park, Myung-Hwan
    • YAKHAK HOEJI
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    • v.41 no.5
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    • pp.615-621
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    • 1997
  • Dehydropeptidase-I (DHP-I) was solubilized from porcine kidney by treatment with n-butanol and partially purified 19.25 fold by $(NH_4)_2SO_4$ precipitation, DEAE-Sepharose CL-6B ion exchange chromatography and Sephacryl S-300 HR chromatography with an overall yield of 19.16. DHP-I showed its optimal activity at pH 7.5 and 25$^{\circ}C$. Its activity was stable under neutral and alkaline conditions, but was disappeared under acidic condition. And DHP-I was heat-labile and its activity remained at 45$^{\circ}C$ for 3hrs. The enzyme was not inhibited by dicationic ions, while its activity was increased by $Co^{2+}$(1mM) and $Zn^{2+}$ (0.1mM). The enzyme was inhibited by EDTA and N-ethylmaleimide. The relative molecular mass of DHP-I was estimated to be approximately 100kDa by gel filtration chromatography. The $K_m$ value of DHP-I for glycyldehydrophenylalanine (GDHP) was 1.98mM. DWP20418 [(1R, 5S, 6S)-6-[1-(R)-Hydroxyethyl]-1-methyl-2-[(2S, 4S)-2-(piperazinylcarbonyl)-1-(R)-hydroxyethyl)pyrrolidine-4-thio]carbapen-2-em-3-carboxylic acid], compared with meropenem (MEPM), was rather easily hydrolized by DHP-I, while it was four times more resistant than imipenem (IPM) to DHP-I.

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Photocycloaddition Reaction of 4',5'-Dihydropsoralen to Tetramethylethylene (4',5'-디히드로소랄렌과 테트라메틸에틸렌의 광고리화 첨가반응에 관한 연구)

  • Sang Chul Shim;Jong Sung Koh
    • Journal of the Korean Chemical Society
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    • v.26 no.3
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    • pp.172-178
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    • 1982
  • A psoralen-DNA monoadduct analogue, 4',5'-dihydropsoralen (DHP) is synthesized and its photophysical properties such as fluorescence quantum yield (0.08), phosphorescence quantum yield (0.013), fluorescence lifetime (0.95ns), and phosphorescence lifetime(0.039s) were measured in ether solution and in frozen matrix state at 77K. The photocycloaddition reaction of DHP with tetramethylethylene(TME) was carried out in solution and in the frozen state. The major photoadduct was isolated and characterized by elemental analysis and physical methods such as UV, IR, NMR, and mass spectrometry. The major DHP-TME photoadduct was proved to be an 1 : 1 $C_4$-cycloadduct formed through 2 + 2 cycloaddition of the pyrone double bond of DHP to TME.

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Anti-Obesitic Effects of Cathepsin S Inhibitory Fraction Derived from Paecilomyces tenuipes in Mice Fed a High-Fat Diet (고지방식이를 섭취한 쥐에서 눈꽃동충하초 유래 cathepsin S 저해 분획의 비만 억제 효과)

  • Heo, Keon;Myoung, Kil-Sun;Lee, Jung-Hee;Huh, Chul-Sung
    • Korean Journal of Food Science and Technology
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    • v.41 no.4
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    • pp.446-451
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    • 2009
  • In this study, cathepsin S (CTSS) inhibitory fraction was isolated from Paecilomyces tenuipes and anti-obesitic effects of the fraction were evaluated in mice, fed a high-fat diet. Hot water extract of P. tenuipes (DHW) was divided into 2 fractions, water eluate fraction (DHP1) and methanol eluate fraction (DHP2) using Diaion HP-20. $IC_{50}$ values for DHW, DHP1 and DHP2 against CTSS were 108.7, 890.3 and 2.3 ${\mu}g$/mL, respectively. To evaluate anti-obesitic effects of the fractions, each fraction was administrated orally to C57BL/6 mice for 4 weeks with a high-fat diet. DHP2 had the highest inhibitory effect on CTSS activity, causing serious reduction in weight gain, a reduction in the amount of adipose tissue and in serum lipids levels. These results suggest that the inhibition of CTSS by compounds derived from P. tenuipes may be effective in preventing and in ameliorating obesity.

SYNTHETIC DEVELOPMENT OF NEW 1$\beta$-SUBSTITUTED CARBAPENEMS

  • Nagao, Yoshimitsu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.34-35
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    • 1993
  • The Development of new asymmetric induction methods useful for syntheses of biologically active natural products and drugs, using C4-chiral 1,3-th-iazolidine-2-thiones, has been a recent focus of interest. 1-8) The present account describes the significance of particular heterocycles in the synthetic development of new 1${\beta}$-substituted carbapenems. A fungal metabolite, (+)-thienamycin (1) has attracted one's attention as a hopeful candidate for new-generation antibiotic drugs because of its strong antimicrobial activities and wide antimicrobial spectra due to the extensive inhibition against various ${\beta}$-lactamases. However, it has been serious problems toward a practically useful drug that (+)-thienamycin is fairly labile in the solution and can be metabolized by renal dehydropept- idase-I (DHP-I). Recently, a Merck Sharp & Dohme research group exploited a non-natural ${\beta}$-lactam, imipenem (2) which has been appeared in the drug market as the first carbapenem-type antibiotic drug. 9) However 2 must be used with a DHP-I inhibitor, cilastatin sodium (3).9) Thus, a 1,${\beta}$-methyl- carbapenem derivative 4 has been disclosed by the same group. 10) It seems to be more hopeful candidate as a new-generation antibiotic because it can directly resist against metabolism by the renal DHP-1 without an enzyme inhibitor 3. 10)

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A Study on the Selection of Evaluation Factors on Forest Carbon Cycle Community(F.C.C.C) using DHP Analysis Method (DHP분석을 이용한 산림탄소순환마을 대상지 평가기준 선발에 관한 연구)

  • Seo, Jeong-Weon;Kwak, Kyung-Ho;Jeong, Se-Myong;Kang, Sung-Pyo;An, Ki-Wan
    • Journal of Korean Society of Forest Science
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    • v.100 no.4
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    • pp.672-680
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    • 2011
  • The purpose of this study has been carried to develop a criterion for the selection of evaluation factors on Forest Carbon Cycle Community(F.C.C.C) based on the result of survey of 96 participants who were operation managers on mountain eco village(31), relevant experts(33), and officers of local government(32). For analysis of the results of survey, DHP(Delphi Hierarchy Process) method was used which is a combination of Delphi method and AHP(Analytic Hierarchy Process) method. The key factors on selection of a suitable area to launch F.C.C.C. project of Korea Forest Service was selected under three hierarchical classes. Class 1 comprises 3 indices(Physical resource index, Human resource index, Vision index), and Class 2 which contains 10 indices (Existing resource, Surroundings resource, Forest biomass resource, Humanities Social quality, Local resident participation, Leader's ability, External support, Planning of operation, Capability of operation, and Effect of operation). Class 3 is sub-level class of class which possess 38 indices. From the results of analysis, Consistency Index(C.I) of each index in the 3 classes was used as evaluation factor. In Class 1, index 'human resources' showed highest Consistency Index(0.454). In Class 2, index 'forest biomass resources' was the highest Consistency Index(0.376) in 'physical resources' of Class 1, index 'leader's ability' was the highest Consistency Index(0.326) in 'human resources' of Class 1, and index 'planning of operation' was the highest Consistency Index(0.346) in 'vision' of Class 1. In Class 3, relative importance of 38 index including 'Joint ownership land security(C.I.-0.266)' was evaluated. Based on the result of this study, a criterion for the selection of evaluation factors for F.C.C.C was developed and the evaluation criterion is expected to be use to select of a suitable area to launch F.C.C.C. project since 2011.

Changes of Muscle Activity and Cephalometric Variables Related to Head Posture (두부자세에 따른 근활성과 측모두부방사선계측치의 변화에 관한 연구)

  • Kim, Byung-Wook;Han, Kyung-Soo
    • Journal of Oral Medicine and Pain
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    • v.24 no.2
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    • pp.189-206
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    • 1999
  • This study was performed to investigate the factors affecting muscle activity and cephalometric variables according to change of head postures. For this study, 150 patients with temporomandibular disorders and 80 dental students without any signs and symptoms of temporomandibular disorders were selected as the patients group and as the normal group, respectively. Head position to body-midline in frontal plane and upper quarter posture to body plumb line in sagittal plane were observed clinically and electromyographic(EMG) activity of anterior temporalis, masseter, sternocleidomastoideus, and trapezius on clenching were recorded with $BioEMG^{(R)}$ in four head postures, which were natural head posture(NHP), forward head posture(FHP), $20^{\circ}$ upward head posture(UHP), and $20^{\circ}$ downward head posture(DHP). Cephaloradiographs were also taken in the same head postures as in EMG taking, but that was taken only in NHP for the patient group. Cephalometric variables measured were SN angle, CVT angle, atlas inclination angle, occlusal plane angle, Me-C2 angle, pharyngeal width, occiput~axis distance, area of pharyngeal space, and cervical curvature. The data were analyzed by SAS statistical program. The results of this study were as follows : 1. Between the patient and the normal group, there were significant difference in distance from plumb line to acromion, eye-tragus angle, electromyographic activity of the four muscles, and cephalometric variables of linear measurement. 2. There was no consistent pattern of correlation between upper quarter posture, EMG activity and cephalometric variables in any case without relation to cervical curvature and head position in frontal plane. 3. Sternocleidomastoid muscle only showed variation of electromyographic activty with changes of head postures, but all the muscles did show correlation with head postures. 4. All the cephalometric variables measured in this study showed difference of mean value by head posture, and CVT angle, pharyngeal width, occiput-atlas distance, and area of pharyngeal space showed correlation between these variables with change from NHP to FHP, and from NHP to UHP.

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