N-Arylnortropinone 유도체의 합성연구

李龍均,朴유미,鄭大一,金寅植,朴鍾勳,盧信愛,鄭逸守,朴敏洙 東亞大學校附設基礎科學硏究所 1998 基礎科學硏究論文集 Vol.15 No.1

Tropinone 화합물들은 색다른 고리계의 존재로 아주 오래전부터 약리학적으로 매우 흥미로운 연구과제로 주목되어 최근에 그들의 합성법,?? 입체적 구조분석?? 그리고 약리학적인 연구??가 활발히 진행되고 있다. Tropinone 1은 흔히 마약으로 알려져 있는 cocaine 2, 소염작용과 항경련성 작용 및 심장박동수를 조절 등 다양한 약리작용을 하는 tropane spirohy-dantoin ?? 그리고 안과질환을 검사 할 때 눈의 동공을 확장시키는 데 사용하는 atropine ??등을 합성하는 데 중요한 중간체이다. ??????????? Trigo, G, G등 ??은 aliphatic amine과 succinic aldehyde를 acetonedicarboxylic acid와 반응하여 nortropane 유도체를 합성하였으며, 그 후 [3+2] nitrone cycloaddition? 과 [3+4] cyclocoupling? 을 거치는 tropane alkaloid의 새로운 합성법이 개발되었다. 최근 lzquier M. L. 등¹은 acetonedicarboxylic acid를 사용하여 1차 지방족 amine과 succinic aldehyde대신 2,5-dimethoxytetrahydrofuran을 반응시켜 N-alkyl nortropinone 유도체를 합성하였다. 그러나 일반적으로 빙초산 속에서 amine과 2,5-dimethoxytetrahydrofuran을 반응시키면 pyrrole 유도체가 합성되어진다.?? 이러한 사실은 분명히 반응조건(예, 산, 온도)에 따른 다양한 화학이 존재한다고 볼 수 있다. 따라서 우리는 반응조건, 즉 산의 변화 및 온도 변화에 의한 amine과 2,5-dimethoxytetrahydrofuran의 반응을 자세하게 검토하면서 새로운 N-arylnortropinone 유도체를 합성하고자 한다.

Prazosin의 항고혈압 효과에 대한 임상적 관찰

서세웅,이균태,김연호,조성락,신영우,신영기 최신의학사 1984 最新醫學 Vol.27 No.8

Online Registry for Nationwide Database of Current Trend of <i>Helicobacter pylori</i> Eradication in Korea: Interim Analysis

Kim, Beom Jin,Kim, Hyun-Soo,Song, Hyun Joo,Chung, Il-Kwun,Kim, Gwang Ha,Kim, Byung-Wook,Shim, Ki-Nam,Jeon, Seong Woo,Jung, Yun Jin,Yang, Chang-Hun,Kim, Ji Hyun,Kim, Tae Ho,Kim, Sang Gyun,Shin, Woon Ge The Korean Academy of Medical Sciences 2016 JOURNAL OF KOREAN MEDICAL SCIENCE Vol.31 No.8

<P>Eradication of <I>Helicobacter pylori</I> using first-line therapy is becoming less effective. Subjects who had been treated for <I>H. pylori</I> infection were prospectively enrolled through an on-line database registry from October 2010 to December 2012. Demographic data, detection methods, treatment indication, regimens, durations, compliance, adverse events, and eradication results for <I>H. pylori</I> infection were collected. Data of 3,700 patients from 34 hospitals were analyzed. The overall eradication rate of the first-line therapy was 73.0%. Eradication failure was significantly associated with old age, concomitant medication, and comorbidity. Regional differences in eradication rates were observed. The most common first-line therapy was proton pump inhibitor-based triple therapy (standard triple therapy, STT) for 7 days (86.8%). The eradication rates varied with regimens, being 73% in STT, 81.8% in bismuth-based quadruple therapy, 100% in sequential therapy, and 90.3% in concomitant therapy. The eradication rate in treatment-naïve patients was higher than that in patients previously treated for <I>H. pylori</I> infection (73.8% vs. 58.5%, <I>P</I> < 0.001). The overall eradication rate for second-line therapy was 84.3%. There was no statistical difference in eradication rates among various regimens. <I>H. pylori</I> eradication rate using STT is decreasing in Korea and has become sub-optimal, suggesting the need for alternative regimens to improve the efficacy of first-line therapy for <I>H. pylori</I> infection.</P>

Changing prevalence of upper gastrointestinal disease in 28 893 Koreans from 1995 to 2005

Kim, Jin Il,Kim, Sang Gyun,Kim, Nayoung,Kim, Jae Gyu,Shin, Sung Jae,Kim, Sang Woo,Kim, Hyun Soo,Sung, Jae Kyu,Yang, Chang Heon,Shim, Ki-Nam,Park, Seun Ja,Park, Joon Yong,Baik, Gwang Ho,Lee, Sang Woo,P Lippincott Williams Wilkins, Inc. 2009 European journal of gastroenterology & hepatology Vol.21 No.7

OBJECTIVES: Changes in the pattern of gastrointestinal diseases in a population tend to be influenced by changes in diet and lifestyle. Shifts in gastrointestinal disease from 1995 to 2005 in Korea were evaluated, retrospectively. METHODS: Seventeen nationwide medical centers participated in this study. The cross-sectional review of endoscopic findings in 28 893 patients included 8441 patients from 1995, 10 350 patients from 2000, and 10 102 patients from 2005. RESULTS: The prevalence of reflux esophagitis increased from 1.8% in 1995 to 5.9% in 2000 and 9.1% in 2005 (P<0.001, the P value was only for the comparison between 1995 and 2005, the followings were as same). The prevalence of peptic ulcer diseases was 18.0% in 1995, 19.1% in 2000, and 20.2% in 2005 (P<0.001). Although no significant differences were noted in duodenal ulcers (8.4, 8.7, and 8.2%, P=0.449), gastric ulcers showed an increasing trend (9.6, 10.5, and 12.0%, P<0.001). The prevalence of gastric cancer increased from 3.4% in 1995 to 4.5% in 2000 (P<0.001), but then decreased to 2.4% in 2005 (P<0.001). The incidence of advanced gastric cancer was 2.5, 3.2, and 1.3%, respectively (P<0.001), and that of early gastric cancer remained constant with rates of 0.8%, 1.3, and 1.1%, respectively (P=0.056). CONCLUSION: The cross-sectional review of data collected in 1995, 2000, and 2005 showed an increase in reflux esophagitis and peptic ulcer diseases. Meanwhile, the prevalence of gastric cancer increased until 2000, but decreased in 2005.

Leptomycin B Increases Radiosensitization by Trichostain A in HeLa Cells

In Ah Kim(김인아),Jin Ho Kim(김진호),Jin Hee Shin(신진희),Il Han Kim(김일한),Jae Sung Kim(김재성),Hong Gyun Wu(우홍균),Eui Kyu Chie(지의규),Yong Ho Kim(김용호),Bo Kyung Kim(김보경),Semie Hong(홍세미),Sung Whan Ha(하성환),Chan Il Park 대한방사선종양학회 2005 Radiation Oncology Journal Vol.23 No.2

목 적: 히스톤탈아세틸화효소 억제제는 그 자체의 항암효과뿐만 아니라 방사선 감작제로서의 효과가 점차 분명해져가고 있다. 최근 Class I 특이적인 히스톤탈아세틸화효소 억제제의 개발로 계층 특이적인(class specific) 연구가 가능해짐에 따라, 본 연구에서는 서로 다른 히스톤탈아세틸화효소억제제의 방사선감작효과를 비교함과 동시에 p53 발현도의 차이가 히스톤탈아세틸화효소억제제의 방사선 감수성에 미치는 영향을 알아보고자 하였다. 대상 및 방법: 이를 위해 p53 발현도가 매우 낮은 HeLa 세포에 p53의 핵 외 수송을 억제하여 세포질 내 분해를 차단하는 Leptomycin B를 처리하여 p53의 발현도를 현저하게 높인 후, Trichostatin와 SK7041의 방사선 민감도를 비교 관찰하였다. 결 과: 세포생존곡선, SER 및 SF2를 비교 분석 시, p53의 발현이 높은 Leptomycin B 처리군에서 TrichostatinA가 Class I HDAC만을 억제하는 SK7041에 비해 유의하게 높은 방사선 감작효과를 나타내었다. 이는 p53이 Class I 특이적 억제제인 SK7041과 Class I과 II를 모두 억제하는 TSA의 방사선감작효과에 미치는 영향의 차이에 기전적으로 관여함을 시사한다. 결 론: Leptomycin B에 의해 유도된 p53의 발현증가는 Class I과 Class I과 II를 모두 억제하는 TSA의 방사선 감작효과를 증강시킨다. Purpose: Histone deacetylase inhibitors (HDIs) are emerging as potentially useful components of anticancer therapy and their radiosensitizing effects have become evident. Specific HDIs are now available that preferentially inhibit specific HDAC classes; TSA inhibits Class I and II HDACs, and SK7041 inhibits Class I HDACs. Materials and Methods: We tested the differential radiosensitization induced by two different classes of HDIs in HeLa cells. We next tested the hypothesis that p53 expression in cancer cells may influence the susceptibility to HDIs by using pharmacologic modification of the p53 status under an isogenic background. Results: It is interesting that p53 expression in the HeLa cells clearly increased the degree of radiosensitization by TSA compared to that of the class I specific inhibitor SK7041. This suggests that p53 may, in part, be responsible for the mechanistic role for the greater radiosensitization induced by Class I & II inhibitors compared to that of the class I specific inhibitors. Thus, these studies are useful in distinguishing between events mediated solely by the Class I HDACs versus those events involving the other classes of HDACs as well. Conclusion: The anticancer efficacy of targeting Class I and II HDACs, in conjunction with radiation therapy, may be further enhanced by the restoration of p53 expression.

Effect of Patellar Taping on Quadriceps Muscle of Knee Joint

Sung Eun Lee,Shin Gyun Kim,Sung Hyoun Cho,Yoo Rim Choi,Chang Sook Kim,Sung Joon Kim,Ki San Nam,Gyung Kim 국제물리치료학회 2012 Journal of International Academy of Physical Ther Vol.3 No.1

This study aims to examine the effect of patellar taping common to patients with patellofemoral pain syndrome on the change of knee joint location. The total number of participants is 12 patients with no pain in their knee. There are three different experiments: no-taping, placebo taping, and patellar taping. After application, they squat on their hams. As a result, both the muscle activity of vastus medialis and that of vastus lateralis increased in placebo taping compared to no-taping, which wasn't statistically significant. However, the muscle activity of vastus medialis and that of vastus lateralis decreased in patellar taping compared to no-taping, which was statistically significant. This suggests that patellar taping causing the lateral attraction of knee joint is more influential to the dynamics of knee joint than skin afferent input in placebo taping. Therefore, patellar taping is effective to change the location of knee joint, affect the muscle activity of quadriceps muscle of thigh, and thus correct the misalignments of the knee joint.

동종골수이식 후의 이식편대숙주 질환의 빈도와 임상양상 : 단일 병원 치료 경험 A Single Institution Experience

이규형,이제환,이정신,서철원,김상위,김성배,김정균,김신,김우건,김상희 대한조혈모세포이식학회 1997 대한조혈모세포이식학회지 Vol.2 No.1

배경: 이식편대숙주 질환은 동종골수 이식후 발생할 수 있는 가장 중요한 합병증의 하나이다. 일반적으로 이식편대숙주 질환이 서구에 비하여 한국을 비롯한 아시아 국가에서 드물다고 알려져 있다. 방법: 저자들은 1993년 12월부터 1997년 6월까지 동종골수이식을 받은 전체 44명의 환자를 대상으로 급성 및 만성 이식편대숙주 질환의 빈도와 임상 양상을 조사하여 분석하였다. 대상환자중 남자가 27명 (61%) 이었고, 여자가 17명 (39%)이었다. 중앙연령은 33.5세 (범위, 16-47세)였다. 17명은 급성골수성 백혈병, 6명은 급성림프구성백혈병, 11명은 만성골수성백혈병, 8명은 중증재생불량성빈혈, 1명은 골수이형성증후군, 그리고 나머지 1명은 신경아세포종(neuroblastoma) 환자였다. 이식편대숙주 질환 예방으로 methodtrexate와 cyclosporine복합요법을 시행하였다. 결과: 3명에서 급성 이식편대숙주 질환이 이식후 18일에서 48일 사이에 관찰되었다(빈도, 7%). 급성 이식편대숙주 질환정도는 3도, 2도 그리고 1도가 각 한명씩이었다. 4도 급성 이식편대숙주 질환은 관찰되지 않았다. 13명의 환자가 만성 이식편대숙주 질환을 경험하였다(30%). 이들 중 10예는 제한성 병변이었고 3예는 전신성 병변이었다. 만성 이식편대숙주 질환의 주된 발병 증상 또는 징후는 황달/간기능 이상(8예)과 구강점막병변(4예)이었다. 한 명의 환자가 이식 후 107일에 간 이식편대숙주 질환에 의한 간부전으로 사망하였다. 결론: 한국인 환자에서는 동종골수이식 후 급성 및 만성 이식편대숙주 질환의 빈도가 구미의 환자에 비하여 상대적으로 낮고 그 정도도 덜한 것으로 보인다. 한국인 환자에 가장 적합한 이식편대숙주 질환 예방 방법의 정립을 위한 계속적인 연구가 필요하다고 사료된다. Background: Graft-versus-host (GVHD) disease is one of the most important complications after allogeneic bone marrow transplantation (BMT). Generally, it has been known that graft-versus-host disease is less frequent after allogeneic BMT in Asian countries including Korea when compared to western countries. Methods: We investigated the frequency and clinical pattern of acute and chronic GVHD in 44 consecutive patients who underwent allogeneic BMT between December 1993 and June 1997. There were 27 male (61%) and 17 female (39%) patients with median age of 33.5 years (range, 16-47). Seventeen patients had acute myelocytic leukemia (AML), 6 acute lymphocytic leukemia (ALL), 11 chronic myelocytic leukemia (CML), 8 severe aplastic anemia (SAA), 1 myelodysplastic syndrome, and 1 neuroblastoma. Methotrexate/cyclosporine combination was given for acute GVHD prophylaxis. Results: There patients (7%) developed acute GVHD median 31 days (range, 18-48) after BMT. There were one grade 3 acute GVHD involving the liver. There was no patient with grade 4 acute GVHD. Thirteen patients (30%) developed chronic GVHD median 100 day (range, 53-266) after BMT. Ten cases were limited stage and 3 were extensive stage. Frequent initial manifestations of chronic GVHD were jaundice/liver function abnormality in 8 cases and oral mucosal lesion in 4 cases. One patient died due to liver failure which were felt to be seconday to chronic GVHD 107 days after BMT. Conclusion: Acute and chronic GVHD are less frequent in Korean patients after allogeneic BMT when compared to historical data from patients from western Europe or United States. In cases of chronic GVHD, mild forms of disease predominate. Optimal strategy for GVHD prophylaxis in Korean patients remains to be defined.

Rheological properties of hydrogen fermented food waste

Kim, Min-Gyun,Sivagurunathan, Periyasamy,Lee, Mo-Kwon,Im, Seongwon,Shin, Sang-Ryong,Choi, Chang-Su,Kim, Dong-Hoon Elsevier 2019 International journal of hydrogen energy Vol.44 No.4

<P><B>Abstract</B></P> <P>Although rheological properties are essential in scaling up fermenters, there has been no report on hydrogen fermentation of organic solid wastes. In the present work, hydrogen fermentation of food waste (FW) was conducted at various substrate concentrations (10–50 g Carbo. COD/L) and operational pHs (4.5–6.5), and rheological properties were attained. High hydrogen production performance showing over 1.7 mol H<SUB>2</SUB>/mol hexose<SUB>added</SUB> was achieved at 10–40 g Carbo. COD/L and pH 5.5 and 6.0. The viscosity tended to increase with substrate concentration increase, and fermentation led to a significant reduction of viscosity. Before fermentation, zero viscosity and infinite viscosity of FW ranged 6.8–1274.1 mPa s and 2.2–58.1 mPa s, which were reduced to 10.4–346.2 mPa s and 1.1–5.3 mPa s after fermentation, respectively. Compared to substrate concentration, operational pH showed a less effect on rheological properties. At the similar volatile solids concentration range, hydrogen-fermented FW showed lower values of rheological properties than that of anaerobic digester sludge. Based on the agitation speed values assuring turbulent condition (complete mixing), the energy required for agitation can be reduced by 30–67% by lowering the applied agitation speed with fermentation time.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Shear thinning behaviour was found in all H<SUB>2</SUB>-fermented FW. </LI> <LI> Hydrogen fermentation led to a significant reduction of viscosity. </LI> <LI> Compared to substrate concentration, operational pH showed a little effect on rheological properties. </LI> <LI> H<SUB>2</SUB>-fermented FW showed lower rheological property values than those of digester sludge. </LI> <LI> Energy saving by 30–67% by slowing down the agitation speed with time. </LI> </UL> </P>

Thalamic T-Type Ca2+ Channels Mediate Frontal Lobe Dysfunctions Caused by a Hypoxia-Like Damage in the Prefrontal Cortex.

Kim, Jeongjin,Woo, Jeonghoon,Park, Young-Gyun,Chae, Sujin,Jo, Seonmi,Choi, Jeong Woo,Jun, Hong Young,Yeom, Young Il,Park, Seong Hoon,Kim, Kyung Hwan,Shin, Hee-Sup,Kim, Daesoo The Society 2011 The Journal of neuroscience Vol.31 No.11

<P>Hypoxic damage to the prefrontal cortex (PFC) has been implicated in the frontal lobe dysfunction found in various neuropsychiatric disorders. The underlying subcortical mechanisms, however, have not been well explored. In this study, we induced a PFC-specific hypoxia-like damage by cobalt-wire implantation to demonstrate that the role of the mediodorsal thalamus (MD) is critical for the development of frontal lobe dysfunction, including frontal lobe-specific seizures and abnormal hyperactivity. Before the onset of these abnormalities, the cross talk between the MD and PFC nuclei at theta frequencies was enhanced. During the theta frequency interactions, burst spikes, known to depend on T-type Ca(2+) channels, were increased in MD neurons. In vivo knockout or knockdown of the T-type Ca(2+) channel gene (Ca(V)3.1) in the MD substantially reduced the theta frequency MD-PFC cross talk, frontal lobe-specific seizures, and locomotor hyperactivity in this model. These results suggest a two-step model of prefrontal dysfunction in which the response to a hypoxic lesion in the PFC results in abnormal thalamocortical feedback driven by thalamic T-type Ca(2+) channels, which, in turn, leads to the onset of neurological and behavioral abnormalities. This study provides valuable insights into preventing the development of neuropsychiatric disorders arising from irreversible PFC damage.</P>

Predictive Factors for Complete Response and Recurrence after Transarterial Chemoembolization in Hepatocellular Carcinoma

( Shin Ok Jeong ),( Eui Bae Kim ),( Soung Won Jeong ),( Jae Young Jang ),( Sae Hwan Lee ),( Sang Gyune Kim ),( Sang Woo Cha ),( Young Seok Kim ),( Young Deok Cho ),( Hong Soo Kim ),( Boo Sung Kim ),( 대한간학회 2017 Gut and Liver Vol.11 No.3

Background/Aims: To investigate the predictive factors for complete response (CR) and recurrence after CR in patients with hepatocellular carcinoma (HCC) treated with transarterial chemoembolization (TACE). Methods: Among 691 newly diagnosed HCC patients, 287 were treated with TACE as a first therapy. We analyzed the predictive factors for CR, recurrence after CR, and overall survival (OS). Results: Eighty-one patients (28.2%) achieved CR after TACE, and recurrence after CR was detected in 35 patients (43.2%). In multivariate analyses, tumor size (≤5 cm) and single nodularity were predictive factors for CR, with hazard ratios (HRs) of 0.35 (p=0.002) and 0.41 (p< 0.001), respectively. Elevated serum α-fetoprotein (AFP) (>20 ng/mL) level and multinodularity exhibited significant relationships with recurrence after CR, with HRs of 2.220 (p=0.026) and 3.887 (p< 0.001), respectively. Tumor size (>5 cm), multinodularity, elevated serum AFP (>20 ng/mL) level, Child-Turcotte-Pugh score (B and C), and portal vein thrombosis were significant factors for OS. Conclusions: In patients treated with TACE as a first therapy, tumor size (≤5 cm) and single nodularity were predictive factors for CR, and multinodularity and elevated serum AFP (>20 ng/mL) levels were predictive factors for recurrence after CR. These factors were also significant for OS. (Gut Liver 2017;11:409-416)