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검색결과 826건 처리시간 0.027초

할로아세틸시코닌 유도체의 합성 및 항암성 평가 (Haloacetylshikonin Derivatives : Synthesis and Evaluation of Antitumor Activity)

  • 정상국;김광수;송규용;조훈;안병준
    • 약학회지
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    • 제42권2호
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    • pp.159-164
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    • 1998
  • The secondary hydroxy group at side chain of shikonin structure was selectively acylated with various haloacetic acids in presence of dicyclohexylcarbodiimide and 4-dimethylamin opyridine to produce haloacetylshikonin derivatives. The cytotoxicity of monohaloacetylshikonin derivatives against L1210 cells increased in the following order; monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml) > monobromoacetylshikonin ($ED_{50}$. 0.158${\mu}$g/ml) > monoiodoacetylshikonin ($ED_{50}$, 0.173${\mu}$g/ml). Introduction of larger halogen atoms decreased the cytotoxic activity, presumably due to steric hinderance. The cytotoxicity of chloroacetylshikonin derivatives was dependent on the number of chlorine atom, thus increasing in the following order; trichloroacetylshikonin (0.032${\mu}$g/ml) > dichloroacetylshikonin (0.059${\mu}$g/ml) > monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml). Thus, the electron withdrawing effect seems to be important for the cytotoxicity of chloroacetylshikonin derivatives. Consistent with the above, dichloroacetylshikonin (T/C. 182%) and trifluoroacetylshikonin (195%) showed higher T/C values than monochloroacetyl-(T/C, 122%), monobromoacetyl-(T/C, 154%) and monoiodoacetylshikonin (T/C, 117%) derivatives. Haloacetylshikonin derivatives showing lower cytoxic activities against L1210 cells exhibited lower T/C values. It seems that there is a relationship between the cytoxicity of haloacetylshikonin and their antitumor activity.

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The Correlation between Stool Exams and Abdominal Computed Tomography (CT) Findings in the Patients with Acute Diarrhea Visiting Emergency Department (ED)

  • ;;;;;;;김훈
    • 대한응급의학회지
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    • 제26권1호
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    • pp.29-37
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    • 2015
  • Purpose: Stool exams are a useful tool for the early presumptive diagnosis of infectious bacterial diarrhea in the Emergency Department (ED). CT scans are often used to increase the physician's level of certainty and to facilitate patient triage by identifying the source of pain in most patients with an acute abdomen in the ED. This study was designed to investigate the correlation between stool exams and abdominal CT in patients with acute diarrhea visiting the ED. Methods: We conducted a retrospective study in the emergency department of a national university hospital from January 1, 2012 to June 30, 2013. The subjects consisted of 156 patients with acute diarrhea and abdominal pain who had stool exam results and abdominal CT findings. We divided the patients into three groups according to the stool exam results. Simultaneously, we evaluated their CT findings of the bowel and adjacent structures. Results: A total of 156 patients were enrolled. Frequency of abnormal CT findings showed statistically significant correlation with stool exams (p-value <0.001). Abnormal CT findings increased as WBCs and RBCs in stool increased (p-value <0.001). Conclusion: The stool exam was a statistically significant predictive variable in indirectly determining the severity of acute diarrhea and it showed correlation with the frequency of abnormal CT findings. It is suggested that stool exams can be used as a susceptible marker for predicting the probability of severe infectious colitis, and for making an early decision regarding close medical attention.

Determination of 25 EDs in Frog and Fish Tissue by GC-MS (SIM)

  • Shin, Ueon-Sang;Shin, Ho-Sang
    • Bulletin of the Korean Chemical Society
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    • 제24권4호
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    • pp.413-420
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    • 2003
  • A gas chromatography/mass spectrometric assay method was developed for the simultaneous determination of neutral and bacis twenty-five disruptors $(ED_S)$ in frog and fish. Afther homogenization and sonication of 5 g of sample, purification was achieves in one step with a solid phase extraction procedure using silica gelflorisl. Eluton was performed with 50mL of acetone : n-hexane (1 : 9) solution. The eluate was concentrated to approximately 10uL and dissolves with 100 uL of hexane and analyzed by GC-MS (SIM). The peaks had good chromatographic properties and the extraction of these compounds from sample also gave relatively high recoveries with small variatoins. Detection limits were 0.1 ng/g for 4-nitrotoluene, benzophenone, hexachlorobenzene, atrazine, malathion, o,p-DDT, o,p-DDT and permethrin, and 0.2 ng/g for heptachlor epoxide, γ-chlordane, α-chlordane, p,p'-DDE, p,p'-DDD, cypermethrin and fenvalerate, and 0.3 ng/g for trifluralin, metribuzin, alachlor, dieldrin and p,p'-DDT, and 0.5 ng/g for heptachlor, aldrin and parathion, and 0.7 ng/g for endrin, and 0.8 ng/g for nitrofen. The recoveries were between 33 and 109%. The method was used to analyze twenty-five frogs and forty-six fishes fishes samples caught from various regions in Korea. Benzophenone was detected at concentration of up to 17.2 ng/g in frog or fish. Heptachlor, aldrin, γ-chlordane, p,p'-DDE, p,p'-DDD, endrin and o,p-DDD were detected at concentrations of 0.7-12.5 ng/g in frog or fish. Also significant leveles of dieldrin (up to 22.5 ng/g) were observed. The developed method may be valuable to be used to the national monitoring project of EDS in biota samples.

A Comparison of the Effectiveness of Before and After the Regional Trauma Center's Establishment

  • Song, Bo Hyung;Hyun, Sung Youl;Kim, Jin Joo;Cho, Jin Seong;Ma, Dae Sung;Kim, Ha Kyung;Lee, Geun
    • Journal of Trauma and Injury
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    • 제29권3호
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    • pp.68-75
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    • 2016
  • Purpose: The purpose of this study was to analyze the effectiveness of regional trauma center's management. Methods: Data collected between January 2013 and December 2015 from a regional trauma center registry was retrospectively reviewed. The patients who had injury severity score (ISS) greater than 15 and over the age of 18 were included. We compared annual general characteristics, the injury mechanism, the pathway of transportation, the injury severity score, the length of stay in emergency department (ED) and hospital, the in-hospital mortality. Results: The annual numbers of enrolled patients were 337, 334 and 278, respectively. No significant differences were found in the annual patient's median ages, injury mechanism, ISS and in-hospital mortality. The annual proportions of coming from other hospital and the median length of stay in hospital were increased after establishment of regional trauma center. The annual median lengths of stay in ED were decreased remarkably. Conclusion: Through the establishment of regional trauma center, the length of stay in ED can be reduced but not in-hospital mortality. More multidisciplinary cooperation and well-organized study is needed to reduce mortality of major trauma patients and maximize effect of regional trauma center.

새로운 경구용 세팔로스포린의 약효평가 (Studies of Pharmacological Activity on New Oral Cephalosporins)

  • 나성범;김완주;지웅길
    • 약학회지
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    • 제38권2호
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    • pp.140-148
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    • 1994
  • ${\beta}-Lactamase$ stability, chemotherapeutic activity, and pharmacokinetics of 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonylthiomethyl-3-cephem-4-carboxylic acid(CEN1), 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimidyl)piperazinyl]thiocarbonylthiomethyl-3-cephem-4-carboxylic acid(CEN2), pivaloyloxymethyl-7-[(Z)-2-(2-aminothizaole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate(CEN1P), and pivaloyloxymethyl-7-{(Z)--2-(2-aminothizaole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate(CEN2P) were examined. CEN1, CEN2, CEN1P, and CEN2P were very stable to the ${\beta}-lactamase$ obtained from three strains(Enterobacter cloacae P99, Escherichia coli TEM, and Citrobacter freundii). Chemotherapeutic activities$(ED_{50})$ of CEN2 and CEN2P against experimental systemic infections due to Streptococcus pyogenes 77A and Escherichia coli 078 were superior to those of CEN1 and CEN1P, respectively. The $ED_{50}$ values of CEN1, CEN2 were 5.82 mg/kg, 0.89 mg/kg(s.c., S. pyogenes 77A) while those of CEN1P, CEN2P were 14.56mg/kg, 6.40mg/kg(p.o., S. pyogenes 77A), respectively. The pharmacokinetics of CEN1, CEN2, CEN1P, and CEN2P were investigated in mice and rats. In mice, peak blood levels of $1.25\;{\mu}g/ml$ were recorded within 20 min after oral administration of a single dose equivalent to 40 mg/kg CEN1P. Cmax of CEN1P was much higher than that of CEN1 in mice and rats. Oral absorption of CEN2P was much higher than that of CEN2.

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교육CEO의 직무별 정보활용 역량 진단도구 개발 (Development of an Assessment Tool of Educational CEO's Information Competency based on Job Categories)

  • 서순식;장윤정;김현덕
    • 정보교육학회논문지
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    • 제12권2호
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    • pp.173-182
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    • 2008
  • 교원은 정보화 사회의 변화와 요구에 능동적으로 대처하기 위해 자신의 직무와 직급에 따라 정보활용 역량을 지속적으로 구축해야 한다. 교원이 정보활용 역량 구축을 위해, 자신에게 필요한 정보화 연수과정을 선택하는데 정보를 제공할 수 있는 표준화된 정보활용능력 기준제시가 필요하다. 그러나 선행연구에서 제시된 정보활용능력 평가와 기준들은 정보통신기술의 소양 수준을 측정하는데 머물고 있어 교원이 직무를 수행하는데 필요한 정보활용능력의 충족 정도를 진단하는 데는 한계가 있다는 지적이 제기된다. 본 연구는 단위 학교의 관리자로서 교육 정보화에 많은 영향력을 행사함에도 불구하고 연구가 많이 이루어지지 않은 교육CEO의 정보활용 역량 진단 도구를 개발하는 것이다. 이를 위해 교육CEO가 수행하는 직무(job), 임무(duty), 과업(task)을 선행연구를 통해 분석하였다. 그 결과 교육CEO의 직무를 (1)학교 발전의 비전제시, (2)교수 학습 지원, (3)조직과 자원의 관리, (4)대외협력의 4가지 영역으로 도출하였다. 이러한 4가지 직무영역을 기준으로 선행 연구 결과를 유목화 하여 임무, 과업을 도출하였고, 직무에 따른 임무, 과업별로 관련된 ISST 요소를 결합하여 직무-ISST 이원분류표를 구성하였다. 이를 바탕으로 교육CEO가 자신의 직무를 수행하는데 필요한 정보활용능력 수준을 자가 진단할 수 있는 63개 문항을 개발하였다.

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Antineoplastic Natural Products and the Analogues(IX). A Review of the Series

  • Ahn, Byung-Zun;Kim, Shin-Il;Ryu, Sung-Ho;Kang, Kyu-Sang;Lee, You-Hui
    • 생약학회지
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    • 제17권2호
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    • pp.168-177
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    • 1986
  • Bioassay-directed isolation has yielded some cytotoxic substances against L1210 cell from the Korean traditional medicine. These include 5,2'-dihydroxy-6,7,8,6'-teramethoxyflavone $(IV,\;scutellaria\;root,\;ED_{50}\;=\;1.7\;{mu}g/ml)$, 7-geranyloxycoumarin $(XXXII,\;poncirus\;fruit,\;10.2\;{mu}g/ml) $and panaxydol $(I,\;white\;ginseng,\;0.03\;{mu}g/ml)$. IV, XXXII and their derivatives were synthesized in the purpose of in vivo tests and for observation of structure-activity relations. Among the flavone derivatives, 5,2',6'-trihydroxy-6,7,8-trimethoxy flavone (XVIII), 5-hydroxy-6,7,8-trimethoxy-6'-benzyloxyflavone (XVII) and 5,8-dihydroxy-6,7-dimethoxyflavone (X) showed the cytotoxicity which has no correlation to the flavone structures. Of the coumarins synthesized, 7,8-dihydroxycoumarin (XXVI), 6-7-dihydroxycoumarin (XXIX) and 6-hydroxy-5,7-dimethoxycoumarin (XXXI) showed considerable activities. Acetylated XXXI has moderate activity $(ED_{50}=17.2\;{mu}g/ml)$. Monobydroxycoumarins or their methyl and allyl ether were inactive. IV inhibits the growth of the solid form of S-180 by 70% at 40 mg/kg and shows T/C of 166% on the ascitic S-180 at 40 mg/kg. It strongly inhibits the activity of the membrane bounded ATPase from L1210 cell. The most cytotoxic fraction of the antitumor materials studied is the one from the trichosanthes root showing $ED_{50}=0. 0003\;{mu}g/ml$ against L1210 cell. This fraction, obtained from ethyl acetate extract, showed T/C of 130 and 135%, on ICR mice bearing S-180 and $BDF_1$ mice bearing L1210 at 10 mg/kg and 7.5 mg/kg, respectively.

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착생식물 기근의 형태 및 세포학적 특성 (Morphological and Cellular Characteristics of Aerial Roots in the Epiphytic American Ivy (Parthenocissus sp.))

  • 임지은;김인선
    • Applied Microscopy
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    • 제32권4호
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    • pp.329-337
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    • 2002
  • 착생식물인 American Ivy의 기근이 흡착 표면에 부착할 때 착생에 따라 일어나는 형태 및 세포수준에서의 분화현상을 전자현미경적으로 연구하였다. 발달 중의 어린 기근은 향축면과 배축면이 구별되지 않는 곤봉상의 형태로 세포소기관들이 비교적 발달하며 색소체가 분포하는 유세포로 구성되어 있다. 이때 유세포 내 여러 액포에는 전자밀도가 높은 물질(EDS)의 축적이 두드러지게 나타나기 시작하였고, 이러한 현상은 기근 표피의 최외층 및 인접한 세포층에서 가장 신속하게 일어났다. 착생하는 기근의 세포는 훨씬 확장되었으나, EDS의 축적으로 인한 액포의 융합으로 세포질은 세포벽 주위로 밀려 극히 일부만 분포하였다. 착생과 거의 동시에 이들 세포층에는 급격한 변화가 일어나 세포질 내 미세구조들이 분해 소실되었고 액포 내 다량의 EDS도 극히 소량만 잔류하거나 거의 사라져 세포는 공동화되었다. 이와 함께, 세포벽 또한 변형되어 점차 불규칙적인 형태의 세포들로 변하였다. 착생이 더욱 진행되면 양면의 표피조직 및 세포들은 모두 불규칙적인 형태로 변화되고, 표면 부위는 일련의 분비물질들이 축적되었다. 흡착이 진행되어 대상 물체표면에 강력히 착생하면서 조직은 더욱 밀착되고 구성 세포들은 찌그러져 기근 조직의 대부분 부위에서 세포사멸이 일어났다. 이와 같이 기근 조직의 기능적 단계에 따라 EDS의 급격한 변화가 나타났는데, 이는 아마 기근이 흡착면에 부착할 때 EDS가 착생과 연관된 기능을 수행하는 것과 관련이 있을 것으로 추정되고 있다.

새 도선 감는 방법을 적용한 전기장 이용 스케일 제거 (Prevention of Particulate Scale with a New winding Method in the Electronic Descaling Technology)

  • 손창현;구상모;김창수;김건우
    • 대한기계학회논문집B
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    • 제26권5호
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    • pp.658-665
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    • 2002
  • This paper presents a new winding method in electronic descaling (ED) technology. Conventional ED technology Produces an oscillating electric field via Faraday's law to provide the necessary molecular agitation to dissolve mineral ions. However, the proposed method produces an additional agitation force for mineral ions, called Lorentz's force. Experiments were performed using various Renolds numbers. A series of tests was conducted to measure the pressure drop across the test section and the overall heat transfer coefficient as a function of time. In order to accelerate the rate of fouling, artificial hard water, 1000ppm CaCO$_3$, was used throughout the tests. The results show that the new winding method accelerates the collision of the mineral ions, thereby improving the system efficiency. The present study can develope more effective fouling-removing equipment with change of estabishment method of coil.

척담탕가미방이 혈압, 뇌혈류량 및 평활근에 미치는 효능에 관한 연구 (Study on the Effects of Chukdamtanggamibang on blood pressure, regional cerebral blood flow(rCBF) and smooth muscle)

  • 이건목;천미나;서은미;한종현;이호섭;김경식;황우준;이병철
    • 생명과학회지
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    • 제11권1호
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    • pp.62-69
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    • 2001
  • This study was aimed to investigate the effect Chukdamtanggamibang on the vascular systems including changes in blood pressure and regional cerebral blood flow(rCBF) of male Sprague-Dawely rats, contractile force of guinea pig`s tracheal smooth muscle and abdominal aorta and femoral artery in rabbits. Blood pressure was not affected by Chukdamtanggamibang in rats. rCBF was significantly increased by Chukdamtanggamibang in a dose-dependent manner. Contractile force of isolated guinea pig`s tracheal smooth muscle evoked by His ({TEX}$ED_{50}${/TEX}) were inhibited significantly by Chukdamtanggamibang. Propranolol, indomethacin and methylene blue did not significantly alter the inhibitory effect of Chukdamtanggamibang. Contractile force of isolated rabbit`s abdominal aorta and femoral artery evoked by NE ({TEX}$ED_{50}${/TEX}) were inhibited significantly by Chukdamtanggamibang. ODQ and L-NNA significantly attenuated the inhibitory effects of Chukdamtanggamibang in abdominal aorta, whereas propranolol did not significantly alter the inhibitory effect of Chukdamtanggamibang. These results indicate that Chukdamtanggamibang can relax hitamine-induced contraction of guinea pig`s tracheal smooth muscle and that this inhibition involves, in part, the relation to the soluble guanylyl cyclase synthesis and nitric oxide (NO) synthesis.

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