• Title/Summary/Keyword: delta derivative

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Analgesic Action Mechanism of DA-5018, a New Capsaicin Derivative : Relationship to Opiate :Receptors and Prostanoids (새로운 캅사이신 유도체 DA-5018의 진통활성 기전연구: Opiate 수용체 및 :Prostanoid와의 상관성)

  • 손미원;손문호;배은주;김순희;김원배;양중의
    • Biomolecules & Therapeutics
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    • v.5 no.1
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    • pp.87-93
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    • 1997
  • DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

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Inhibition of Proliferation of Human Fibroblast by δ-Aminolevulinic Acid (ALA) Derivatives through the Induction of Mitochondria Membrane Depolarization (δ-Aminolevulinic acid (ALA) 유도체들의 미토콘드리아 탈분극 유도에 의한 인간 섬유아세포의 세포분열 억제)

  • Jun, Yong-woo;Han, Du-Gyeong;Lee, Jin-A;Jo, Su-Yeon;Jang, Deok-Jin
    • KSBB Journal
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    • v.30 no.6
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    • pp.313-318
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    • 2015
  • ${\delta}$-Aminolevulinic acid (ALA) is an endogenous metabolite formed in the mitochondria from succinyl-CoA and glycine, and plays a key role in the living body as an intermediate of the compound in the porphyrin biosynthesis pathway. ALA has been commonly used in photodynamic therapy for several years, because ALA is of interest as a biodegradable mediator, a growth regulator, and an effective agent used in dermatology. Here, we determined which ALA derivatives were the most effective for the inhibition of the cell proliferation and growth of human fibroblast. As a result, we found that the treatment of ALA derivatives including ALA, ALAP (ALA phosphate salt), MAL (Methyl 5-aminolevulinate hydrochloride salt), PBGL (phophobilinogen lactam) and PBGH (phophobilinogen-HCl) could attenuate cell proliferation of human fibroblast cells. Among them, PBGH was the most effective derivative. In addition, PBGH treatment could induce mitochondrial membrane depolarization, leading to cell death of human fibroblast. These results suggest that mitochondrial membrane depolarization induced by ALA and PBGH treatment might be responsible for inhibition of cell proliferation and death. Taken together, our results propose the possibility that PBGH can be used as one of the effective drugs in human skin disease, psoriasis.

luxS and smcR Quorum-Sensing System of Vibrio vulnificus as an Important Factor for In Vivo Survival

  • SHIN NA-RI;BAEK CHANG-HO;LEE DEOG-YONG;CHO YOUNG-WOOK;PARK DAE-KYUN;LEE KO-EUN;KIM KUN-SOO;YOO HAN-SANG
    • Journal of Microbiology and Biotechnology
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    • v.15 no.6
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    • pp.1197-1206
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    • 2005
  • Vibrio vulnificus is an opportunistic pathogen that causes a septicemia and expresses numerous virulence factors, in which luxS and smcR are genes encoding for components responsible for quorum-sensing regulation. In the present study, null mutants were constructed with lesions in each or both of these two genes from the V. vulnificus Vv$\Delta$Z strain, which is a lacZ$^{-}$ and chloramphenicol/streptomycin-resistant derivative of the wild-type ATCC29307 strain, and their phenotypes related to virulence were compared with those of the parental cells. $LD_{50}$ and histopathological findings of luxS-, smcR-, or luxS- smcR- deficient mutant were not different from those of the parent strain, a lacZ-deficient streptomycin-resistant strain in mice. However, time of death in mice was delayed, and numbers of bacteria survived in bloodstream after intraperitoneal injection in mice were decreased by mutation, especially luxS and smcR double mutant (VvSR$\Delta$ZSR). These phenomena were supported by increased serum sensitivity and delayed bacterial proliferation in both murine blood and iron-restricted medium. These results suggest that the luxS and luxR homologous genes in V. vulnificus could playa role in bacterial survival in host by enhancing proliferation and adjusting to changed environment.

On-Line Measurement of Biochemical Oxygen Demand of livestock Wastewater by Multi-Biosensor System (Multi-Biosensor를 이용한 축산폐수의 생물화학적 산소요구량 실시간 측정방법 연구)

  • Kim, Jin-Kyeung;Kim, Tai-Jin
    • KSBB Journal
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    • v.21 no.4
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    • pp.241-247
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    • 2006
  • The present study was intended to examine a basic scheme to determine the biochemical oxygen demand(BOD) of livestock wastewater by means of six individual dissolved oxygen(DO) sensors and its multi-measurable meter. Maximal point of the first order time derivative of the DO difference between DO distribution of sterilized livestock wastewater and that of non-sterilized livestock wastewater, was considered as the oxygen uptake rate(OUR) of microorganisms in livestock wastewater, as determined to be 0.00074 mg $O_2/{\ell}{\cdot}sec$. The present study showed that there was a fair linear relationship(97.72%) between maximal OUR and BOD values of livestock wastewater, the latter being determined by classical Winkler azide method. It was thus concluded that the present multi-biosensor system might be applicable to an on-line system for measurement of BOD of livestock wastewater.

Estimation of Aircraft Stability Derivatives Using a Subsonic-supersonic Panel Method (아음속 초음속 패널법을 이용한 항공기 안정성 미계수 예측)

  • Gong, Hyo-Joon;Lee, Hyung-Ro;Kim, Beom-Soo;Lee, Seung-Soo
    • Journal of the Korean Society for Aeronautical & Space Sciences
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    • v.40 no.5
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    • pp.385-394
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    • 2012
  • A computer program that can estimate static, dynamic stability and control derivatives using a subsonic-supersonic panel method is developed. The panel method uses subsonic-supersonic source and elementary horse shoe vortex distributions, and their strengths are determined by solving the boundary condition approximated with a thin body assumption. In addition, quasi-steady analysis on the body fixed coordinate system allows the estimation of damping coefficients of aircraft 3 axes. The code is validated by comparing the neutral point, roll and pitch damping of delta wings with published analysis results. Finally, the static, dynamic stability and control derivatives of F-18 are compared with experimental data as well as other numerical results to show the accuracy and the usefulness of the code.

Examining Synchronous Fluorescence Spectra of Dissolved Organic Matter for River BOD Prediction (하천수 BOD 예측을 위한 용존 자연유기물질의 synchronous 형광 스펙트럼 분석)

  • Hur, Jin;Park, Min-Hye
    • Journal of Korean Society on Water Environment
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    • v.23 no.2
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    • pp.236-243
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    • 2007
  • Fluorescence measurements of dissolved organic matter (DOM) have the superior advantages over other analysis tools for the applications to water quality management due to their rapid analysis. It is known that protein-like fluorescence characteristics are well corelated with microbial activities and biodegradable organic matter. In this study, potential biochemical oxygen demand (BOD) predictor were explored using the fluorescence peak intensities and/or the integrated fluorescence intensities derived from synchronous fluorescence spectra and the first derivative spectra of river samples. A preliminary study was conducted using a mixture of a river and a treated sewage to test the feasibility of the approach. It was demonstrated that the better BOD predictor can be derived from synchronous fluorescence spectra and the derivatives when the difference between the emission and the excitation wavelengths (${\Delta}{\gamma}$) was large. The efficacy of several selected fluorescence parameters was rivers in Seoul. The fluorescence parameters exhibited relatively good correlation coefficients with the BOD values, ranging from 0.59 to 0.90. Two parameters were suggested to be the optimum BOD predictors, which were a fluorescence peak at a wavelength of 283 nm from the synchronous spectrum at the ${\Delta}{\gamma}$ value of 75 nm, and the integrated fluorescence intensity of the first derivatives of the spectra at the wavelength range between 245 nm and 280 nm. Each BOD predictor showed the correlation coefficients of 0.89 and 0.90, respectively. It is expected that the results of this study will provide important information to develop a real-time efficient sensor for river BOD in the future.

Study on a Hedging Volatility Depending on Path Type of Underlying Asset Prices (기초자산의 추세 여부에 따른 헤지변동성의 결정에 관한 연구)

  • Koo, Jeongbon;Song, Junmo
    • The Korean Journal of Applied Statistics
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    • v.26 no.1
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    • pp.187-200
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    • 2013
  • In this paper, we deal with the problem of deciding a hedging volatility for ATM plain options when we hedge those options based on geometric Brownian motion. For this, we study the relation between hedging volatility and hedge profit&loss(P&L) as well as perform Monte Carlo simulations and real data analysis to examine how differently hedge P&L is affected by the selection of hedging volatility. In conclusion, using a relatively low hedging volatility is found to be more favorable for hedge P&L when underlying asset prices are expected to be range bound; however, a relatively high volatility is found to be favorable when underlying asset prices are expected to move on a trend.

Opioid Receptor Selectivity and General Pharmacology of DK1001, New Alkaloid Analgesic (알칼로이드 진통제 DK 1001의 opioid 수용체 선택성 및 일반약리)

  • Kim, Jin-Sook;Kim, Dae-Kyung;Kwon, Tae-Hyub;Yong, Chul-Soon;Ha, Jeoung-Hee;Huh, Keon;Kim, Jung-Ae
    • Biomolecules & Therapeutics
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    • v.7 no.3
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    • pp.278-284
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    • 1999
  • DK1001 is a thebain derivative, which is newly synthesized as an alkaloid analgesic. This study was designed to study effects of DK1001 on the ligands binding to the opioid receptor subtypes, and general pharmacology of DK1001. DK1001 inhibited the binding of [$^3H$]DAMGO, a selective mu-subtype agonist, to the opioid receptor of rat forebrain in a concentration-dependent manner. $EC_{50}$ of DK1001 was significantly lower than that of morphine. DK1001 inhibited the binding of 〔$^3$H〕DPDPE, a selective delta-subtype agonist concentration-dependently. DK1001(0.5 mg/kg) had no effects on behavior, body temperature, blood pressure. respiratory rate, and intestinal charcoal propulsion of mice. In addition, DK1001 did not affect on the contractilities of isolated muscle strips of aorta, ileum, and trachea of rats. These results suggest that DK1001 might be a potent analgesic without serious side effects.

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The Study on the Synthesis of Propellant with High Nitrogen Content (고질소 추진물질 합성 연구)

  • Lee, Woonghee;Kim, Minjun;Park, Youngchul
    • Journal of the Korean Society of Propulsion Engineers
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    • v.19 no.3
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    • pp.96-102
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    • 2015
  • Traditional propellants emit toxic gases such as carbon dioxide and hydrogen chloride during combustion which are harmful to the environment. This study established a synthetic process of a high nitrogen containing derivative of tetrazine, 3,3-Azobis(6-Amino-1,2,4,5-Tetrazine) (DAAT), which can be applied as solid fuels for a solution to environmental concerns. Also, this paper described the detailed process and the analytic results of properties, which were not mentioned in previous reports. The compound was characterized by NMR, IR spectroscopy, and thermal, impact, and friction stability were measured. In addition, the heats of formation (${\Delta}H_f$) and detonation properties (pressure and velocity) of DAAT were calculated using Gaussian 09 and EXPLO5 programs.

LasR Might Act as an Intermediate in Overproduction of Phenazines in the Absence of RpoS in Pseudomonas aeruginosa

  • He, Qiuning;Feng, Zhibin;Wang, Yanhua;Wang, Kewen;Zhang, Kailu;Kai, Le;Hao, Xiuying;Yu, Zhifen;Chen, Lijuan;Ge, Yihe
    • Journal of Microbiology and Biotechnology
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    • v.29 no.8
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    • pp.1299-1309
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    • 2019
  • As an opportunistic bacterial pathogen, Pseudomonas aeruginosa PAO1 contains two phenazine-producing gene operons, phzA1B1C1D1E1F1G1 (phz1) and phzA2B2C2D2E2F2G2 (phz2), each of which is independently capable of encoding all enzymes for biosynthesizing phenazines, including phenazine-1-carboxylic acid and its derivatives. Other previous study reported that the RpoS-deficient mutant SS24 overproduced pyocyanin, a derivative of phenazine-1-carboxylic acid. However, it is not known how RpoS mediates the expression of two phz operons and regulates pyocyanin biosynthesis in detail. In this study, with deletion of the rpoS gene in the $PA{\Delta}phz1$ mutant and the $PA{\Delta}phz2$ mutant respectively, we demonstrated that RpoS exerted opposite regulatory roles on the expression of the phz1and phz2 operons. We also confirmed that the phz1 operon played a critical role and especially biosynthesized much more phenazines than the phz2 operon when the rpoS gene was knocked out in P. aeruginosa. By constructing the translational reporter fusion vector lasR'-'lacZ and the chromosomal fusion mutant $PA{\Delta}lasR::lacZ$, we verified that RpoS deficiency caused increased expression of lasR, a transcription regulator gene in a first quorum sensing system (las) that activates overexpression of the phz1 operon, suggesting that in the absence of RpoS, LasR might act as an intermediate in overproduction of phenazine biosynthesis mediated by the phz1 operon in P. aeruginosa.