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세팔로스포린 3′-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태
나성범,공재양,김완주,지웅길 충남대학교 약학대학 의약품개발연구소 1993 藥學論文集 Vol.9 No.-
A cephalosporin with an aminothiazolylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dual-action cephalosporin derivative. In this paper, the physicochemical properties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its β-lactamase. The pharmacokinetic paramaters of DACD were evaluated in mice after a single intravenous dose of 40 ㎎/㎏. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82±0.03, 7.53±0.21, respectively. In the hydrolysis test, half-lives (t^1/2) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver homogenate. Half-lives (t_1/2) of CENO and DACD were 1.29 hr and 1.15 hr in human plasma, 0.62 hr and 0.71 hr rat liver homogenate. In β-lactamase stability test, CENO and DACD were very stable to the β-lactamase obtained from three different strains. Half-life (t_1/2) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (㎎·h/I), respectively.
Polygoum Tinctoria와 합성 인디고 염료의 물리화학적 특성 비교
최창용,장미경,공병기,최혜영,나상권,이동병,양숙향,나재운 한국공업화학회 2002 응용화학 Vol.6 No.2
The natural dye substances appear to have a lot of benefits that enable the dyed materials to exhibit their natural colors. It may have a bit of a harmful influence on the human body itself, in comparison with the synthetic substances. It also causes hardly any environmental pollution because of the natural chemicals and costs much less to disposal. In this study was investigated physicochemical characterization of polygoum tinctoria dye substance and synthetic indigo. Calcium hydroxide was added into polygoum tinctoria leaves to precipitate dye substances and it was freezing dried into powder form. Characterizations of dye substances were investigated by UV/VIS spectrophotometer, TLC, DSC, TGA, HPLC, and MALDI-TOF Mass. Resultantly, polygoum tinctoria was confirmed that is consisted of two ingredients from these results.
SB-31ⓡ 의 일반약리작용 ( General Pharmacology of SB-31ⓡ )
공재양(Jae Yang Kong),박우규(Woo Kyu Park),천혜경(Hyae Gyeong Cheon),권경자(Kyoung Ja Kwon),윤여생(Yeo Saeng Yoon),신화섭(Hwa Sup Shin) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.4
General pharmacological effects of SB-31^R the extracts of Pulsatilla koreana, were investigated in mice, rats and guinea-pigs. Intravenous injection of SB-31 (3 and 6 ml/kg) produced almost no effect on central nervous system; no effects on the general symptom and behaviors of mice, spontaneous locomotor activity, pentobarbital-induced sleeping time, rotarod performance, electroshock and pentylenetetrazole-induced seizures, acetic acid-induced writhing and normal body temperature in mice. SB-31 showed little effects on the spontaneous movement of the isolated ileum and contraction induced by agonists in isolated ileum, suggesting no influence on autonomic nervous system. Administration of SB-31 also did not show any effect on blood pressure in conscious rats. However, a slight decrease in heart rate was observed at high doses (6 and 10 ml/kg) of SB-31 in conscious rats. Similarly, a slight increase in respiratory rate was observed at 6 ml/kg of SB-31 in anesthetized rats. SB-31 did not produce any effect at the dose of 3 ml/kg, but showed a tendency to increase the urinary volume at 6 ml/kg, and produced a decrease in urinary excretions of Na^+ and K^+ at 6 ml/kg. However, transport capacity within the gastrointestinal tract and the secretion of the gastric juice were not influenced by 6 ml/kg of SB-31. In conclusion, these results suggest that SB-31 did not produce any acute effects on the central nervous system, autonomic nervous system, respiratory and circulatory systems, digestive system and kidney function at the dose of below 3 ml/kg.
Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors
Jae Du Ha*,Seung Kyu Kang,Kun-Do Kim,Joong-Kwon Choi,Jae Yang Kong,Chang H. Ahn 대한화학회 2005 Bulletin of the Korean Chemical Society Vol.26 No.6
Investigation of structure-activity relationships of novel quinazolines has identified 7,8-dihydro-[1,4]dioxino- [2,3-g]quinazolines as a potent inhibitor of EGFR. These compounds have a benzodioxane framwork, which was prepared by regioselective O-alkylation of ethyl 3,4-dihydroxy benzoate by epoxide ring opening. Compounds 3f and 3k were more potent than ZD-1839 in EGF enzyme and EGFR autophosporylation inhibition assays.
Jae-Hoon Choi,Dong-Keun Lee,Chang-Hwan Kim,Jong-kook Jin,Sang-Hee Han,Jong-Dae Kong,Seong-Lok Hong,Yang-Su Kim,Myeun Kwon,Hyun-Sik Ahn,Gye-Yong Jang,Min-Seong Yun,Dae-Kyung Seong,Hyun-Seok Shin 대한전기학회 2013 Journal of Electrical Engineering & Technology Vol.8 No.2
The Korea Superconducting Tokamak Advanced Research (KSTAR) device is an advanced superconducting tokamak to establish scientific and technological bases for attractive fusion reactor. This device requires 3.5 Tesla of toroidal field (TF) for plasma confinement, and requires a strong poloidal flux swing to generate an inductive voltage to produce and sustain the tokamak plasma. KSTAR was originally designed to have 16 serially connected TF magnets for which the nominal current rating is 35.2 kA. KSTAR also has 7 pairs of poloidal field (PF) coils that are driven to 1 MA/sec for generation of the tokamak plasma according to the operation scenarios. The KSTAR Magnet Power Supply (MPS) was dedicated to the superconducting (SC) coil commissioning and 2<SUP>nd</SUP> plasma experiment as a part of the system commissioning. This paper will describe key features of KSTAR MPS for the 2<SUP>nd</SUP> plasma experiment, and will also report the engineering and commissioning results of the magnet power supplies.
Yang, Seo-Yun,Lee, Jae-Jin,Lee, Jin-Hee,Lee, Kyungeun,Oh, Seung ,Hoon,Lim, Yu-Mi,Lee, Myung-Shik,Lee, Kong-Joo Portland Press Ltd. 2016 Biochemical journal Vol.473 No.12
<P>Secretagogin (SCGN), a Ca2+-binding protein having six EF-hands, is selectively expressed in pancreatic beta-cells and neuroendocrine cells. Previous studies suggested that SCGN enhances insulin secretion by functioning as a Ca2+-sensor protein, but the underlying mechanism has not been elucidated. The present study explored the mechanism by which SCGN enhances glucose-induced insulin secretion in NIT-1 insulinoma cells. To determine whether SCGN influences the first or second phase of insulin secretion, we examined how SCGN affects the kinetics of insulin secretion in NIT-1 cells. We found that silencing SCGN suppressed the second phase of insulin secretion induced by glucose and H2O2, but not the first phase induced by KCl stimulation. Recruitment of insulin granules in the second phase of insulin secretion was significantly impaired by knocking down SCGN in NIT-1 cells. In addition, we found that SCGN interacts with the actin cytoskeleton in the plasma membrane and regulates actin remodelling in a glucose-dependent manner. Since actin dynamics are known to regulate focal adhesion, a critical step in the second phase of insulin secretion, we examined the effect of silencing SCGN on focal adhesion molecules, including FAK (focal adhesion kinase) and paxillin, and the cell survival molecules ERK1/2 (extracellular-signal-regulated kinase 1/2) and Akt. We found that glucose-and H2O2-induced activation of FAK, paxillin, ERK1/2 and Akt was significantly blocked by silencing SCGN. We conclude that SCGN controls glucose-stimulated insulin secretion and thus may be useful in the therapy of Type 2 diabetes.</P>
Yang, Yoosoo,Oh, Jung-Mi,Heo, Paul,Shin, Jae Yoon,Kong, Byoungjae,Shin, Jonghyeok,Lee, Ji-Chun,Oh, Jeong Su,Park, Kye Won,Lee, Choong Hwan,Shin, Yeon-Kyun,Kweon, Dae-Hyuk Biochemical Society 2013 The Biochemical journal Vol.450 No.3
<P>Anti-allergic effects of dietary polyphenols were extensively studied in numerous allergic disease models, but the molecular mechanisms of anti-allergic effects by polyphenols remain poorly understood. In the present study, we show that the release of granular cargo molecules, contained in distinct subsets of granules of mast cells, is specifically mediated by two sets of SNARE (soluble N-ethylmaleimide-sensitive factor attachment protein receptor) proteins, and that various polyphenols differentially inhibit the formation of those SNARE complexes. Expression analysis of RBL-2H3 cells for 11 SNARE genes and a lipid mixing assay of 24 possible combinations of reconstituted SNAREs indicated that the only two active SNARE complexes involved in mast cell degranulation are Syn (syntaxin) 4/SNAP (23 kDa synaptosome-associated protein)-23/VAMP (vesicle-associated membrane protein) 2 and Syn4/SNAP-23/VAMP8. Various polyphenols selectively or commonly interfered with ternary complex formation of these two SNARE complexes, thereby stopping membrane fusion between granules and plasma membrane. This led to the differential effect of polyphenols on degranulation of three distinct subsets of granules. These results suggest the possibility that formation of a variety of SNARE complexes in numerous cell types is controlled by polyphenols which, in turn, might regulate corresponding membrane trafficking.</P>
Superconducting Magnet Power Supply System for the KSTAR 2nd Plasma Experiment and Operation
JAE HOON CHOI,DONG KEUN LEE,CHANG HWAN KIM,Jong-kook Jin,Sang-Hee Han,JONG DAE KONG,SEONG LOK HONG,Yang-Su Kim,MYEUN KWON,Hyun-sik Ahn,Gye-yong Jang,Min-seong Yun,Dae-Kyung Seong,Hyun-seok Shin 대한전기학회 2013 Journal of Electrical Engineering & Technology Vol.8 No.2
The Korea Superconducting Tokamak Advanced Research (KSTAR) device is an advanced superconducting tokamak to establish scientific and technological bases for attractive fusion reactor. This device requires 3.5 Tesla of toroidal field (TF) for plasma confinement, and requires a strong poloidal flux swing to generate an inductive voltage to produce and sustain the tokamak plasma. KSTAR was originally designed to have 16 serially connected TF magnets for which the nominal current rating is 35.2 kA. KSTAR also has 7pairs of poloidal field (PF) coils that are driven to 1 MA/sec for generation of the tokamak plasma according to the operation scenarios. The KSTAR Magnet Power Supply (MPS) was dedicated to the superconducting (SC) coil commissioning and 2nd plasma experiment as a part of the system commissioning. This paper will describe key features of KSTAR MPS for the 2nd plasma experiment, and will also report the engineering and commissioning results of the magnet power supplies.