Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transfoming growth factor-β type 1 receptor kinase inhibitors

Kim, Dae Kee,Lee, Yeon Im,Lee, Yean Woo,Dewanga, Purushottam M,Sheen, Yhun Yhong,Kim, Yeo Woon,Park, Hyun ju,Yoo, Ja Kyung,Lee, Ho Soon,Kim, Yang Kook 梨花女子大學校 藥學硏究所 2011 藥學硏究論文集 Vol.- No.21

A series of 4(5)-(6-methylpyridin-2-yl)imidazoles 16-19 and -pyrazoles 22-29, 33, and 34 have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in cell-based luciferase reporter assays. The 6-quinolinyl imidazole analogs 16 and 18 inhibited ALKS phosphorylation with lC50 values of 0.026 and 0.034μM, respectively. ln a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct, 18 displayed 66% inhibition at 0.05μM. while competitor compounds 2 and 3 showed 44% inhibition. The binding mode of 18 generated by flexible docking studies with ALK5:18 complex shows that it fits well into the active site cavity of ALK5 by forming broad and tight interactions.

Astragalin Inhibits Allergic Inflammation and Airway Thickening in Ovalbumin-Challenged Mice

Kim, Yun-Ho,Choi, Yean-Jung,Kang, Min-Kyung,Park, Sin-Hye,Antika, Lucia Dwi,Lee, Eun-Jung,Kim, Dong Yeon,Kang, Young-Hee American Chemical Society 2017 Journal of agricultural and food chemistry Vol.65 No.4

<P>Lung inflammation and oxidative stress are the major contributors to the development of obstructive pulmonary diseases. Macrophages are involved in pulmonary inflammation and alveolar damage in emphysema. Astragalin is an anti-inflammatory flavonoid present in persimmon leaves and green tea seeds. This study elucidated that astragalin inhibited inflammatory cell infiltration induced by 20 mu M H2O2 and blocked airway thickening and alveolar emphysema induced by 20 pig of ovalbumin (OVA) in mice. OVA induced mouse pulmonary MCP-1, and H2O2 enhanced the expression of MCP-1/ICAM-1/ccv integrin in bronchial airway epithelial BEAS-2B cells. Such induction was inhibited by supplying 10-20 mg/kg of astragalin to OVA-challenged mice and 1-20 mu M astragalin to oxidant-stimulated cells. Oral administration of 20 mg/kg of astragalin reduced the induction of F4/80/CD68/CD11b in airways of mice challenged with OVA. Additionally, emphysema tissue damage was observed in OVA-exposed alveoli. Mast cell recruitment in the airway subepithelium was blocked by supplementing astragalin to OVA-challenged mice. Orally treating 20 mg/kg of astragalin reduced alpha-SMA. induction in inflammation-occurring airways and appeared to reverse airway thickening and constriction induced by an OVA episode. These results revealed that astragalin may improve airway thickening and alveolar destruction with blockade of allergic inflammation in airways. Therefore, astragalin may be a therapeutic agent antagonizing asthma and obstructive pulmonary diseases.</P>

Phosphorylation of the transcriptional repressor MYB15 by mitogen-activated protein kinase 6 is required for freezing tolerance in <i>Arabidopsis</i>

Kim, Sun Ho,Kim, Ho Soo,Bahk, Sunghwa,An, Jonguk,Yoo, Yeji,Kim, Jae-Yean,Chung, Woo Sik Oxford University Press 2017 Nucleic acids research Vol.45 No.11

<P><B>Abstract</B></P><P>The expression of <I>CBF</I> (C-repeat-binding factor) genes is required for freezing tolerance in <I>Arabidopsis thaliana. CBFs</I> are positively regulated by INDUCER OF CBF EXPRESSION1 (ICE1) and negatively regulated by MYB15. These transcription factors directly interact with specific elements in the <I>CBF</I> promoters. Mitogen-activated protein kinase (MAPK/MPK) cascades function upstream to regulate <I>CBFs</I>. However, the mechanism by which MPKs control <I>CBF</I> expression during cold stress signaling remains unknown. This study showed that the activity of MYB15, a transcriptional repressor of cold signaling, is regulated by MPK6-mediated phosphorylation. MYB15 specifically interacts with MPK6, and MPK6 phosphorylates MYB15 on Ser168. MPK6-induced phosphorylation reduced the affinity of MYB15 binding to the <I>CBF3</I> promoter and mutation of its phosphorylation site (MYB15<SUP>S168A</SUP>) enhanced the transcriptional repression of <I>CBF3</I> by MYB15. Furthermore, transgenic plants overexpressing MYB15<SUP>S168A</SUP> showed significantly reduced <I>CBF</I> transcript levels in response to cold stress, compared with plants overexpressing MYB15. The <I>MYB15<SUP>S168A</SUP></I>-overexpressing plants were also more sensitive to freezing than <I>MYB15</I>-overexpressing plants. These results suggest that MPK6-mediated regulation of MYB15 plays an important role in cold stress signaling in <I>Arabidopsis</I>.</P>

뇌졸중 환자를 대상으로 한 병원 환경에서의 작업 기반 양측성 상지 훈련 프로토콜 개발

김선호(Kim, Sun-Ho),김정란(Kim, Jung Ran),박혜연(Park, Hae Yean),한아름(Han, A-Reum),김종배(Kim, Jong-Bae),박지혁(Park, Ji-Hyuk) 대한신경계작업치료학회 2020 재활치료과학 Vol.9 No.1

목적 : 임상 적용에 있어 효율적 적용이 가능한 작업 기반 양측성 상지 훈련을 위해 작업기반 중재의 활동 선정과 양측성 상지훈련의 주요 전략을 기본으로 한 프로토콜을 개발하는 것이었다. 연구 방법 : 델파이 기법을 활용한 연구의 절차는 총 3단계의 연구 과정으로 진행하였다. 첫 단계는 개방형 설문 개발 단계로 문헌고찰을 통해 1차 초안을 마련하고 초안을 바탕으로 한 예비연구를 통해 개방형 질문을 개발하였다. 두 번째 단계는 델파이 조사로, 개방형 델파이 설문을 통해 얻은 전문가들의 응답을 바탕으로 훈련 프로토콜로서의 적절성을 리커트 5점 척도로 제시하였다. 설문조사를 통해 얻은 평균및 표준편차, 안정도, 수렴도, 합의도, 내용 타당도 비율 분석을 통해 항목의 수정 및 삭제 등의 과정을 거쳐 항목을 도출하여 재구성하여 실시하였다. 세 번째 단계는 프로토콜의 완성 단계로 연구자 간 토의를 거쳐 최종 도출된 프로토콜 내용에 대하여 재 조직화를 통해 병원 기반의 작업 기반 양측성 상지 훈련 프로토콜을 완성하였다. 결과 : 작업 기반 중재 선정 영역에서 3영역, 9항목, 양측성 상지 훈련 영역에서 4영역, 81항목의 프로토콜이 완성되었다. 결론 : 본 연구를 통해 병원 기반으로 이루어지고 있는 현재 상황에서 작업 기반 활동을 중재로 사용할수 있도록 작업치료 전문가들의 의견을 종합한 근거 기반의 방법을 제시하며, 양측성 상지 훈련 또한 구체적인 방법 제시를 통해 임상에서의 효율적으로 적용할 수 있도록 할 수 있다는 점에서 의미가 있다. Objective : To develop an occupation-based bilateral upper extremity training protocol that can be effectively applied in a medical setting Methods : The research process using the delphi technique was carried out in 3 stages. The first stage was an open questionnaire development stage, The first draft is prepared through literature review and open questions were developed through preliminary research based on the draft. The second stage was the delphi survey. Based on the responses of the experts obtained through the open Delphi survey, the adequacy of the training protocol was shown on a Likert 5 point scale. The items were edited and deleted, reconstructed by analyzing the mean and standard deviation, stability, convergence degree, consensus, and content validity ratio through the questionnaire. The third step was the completion of the protocol. After discussions between researchers, the finalized protocol contents were reorganized to complete the occupation-based bilateral upper extremity training protocol for medical setting. Results : The final protocol consisted of 9 items across 3 areas in the occupation-based intervention selection domain and 81 items across 4 areas in the bilateral upper extremity training domain, intervention period, and evaluation. Conclusions : This study suggests an evidence-based method that collects the opinions of occupational therapists in order to use occupation-based activities as interventions in a situation that currently sees occupational therapy primarily performed in hospitals. It is also meaningful that the bilateral upper extremity training can be applied effectively in clinical situations by concretely presenting.

Novel glutathione-containing dry-yeast extracts inhibit eosinophilia and mucus overproduction in a murine model of asthma

Yun-Ho Kim,Yean-Jung Choi,Eun-Jung Lee,Min-Kyung Kang,Sin-Hye Park,Dong Yeon Kim,Hyeongjoo Oh,Sang-Jae Park,Young-Hee Kang 한국영양학회 2017 Nutrition Research and Practice Vol.11 No.6

BACKGROUND/OBSECTIVE: Airway inflammation by eosinophils, neutrophils and alveolar macrophages is a characteristic feature of asthma that leads to pathological subepithelial thickening and remodeling. Our previous study showed that oxidative stress in airways resulted in eosinophilia and epithelial apoptosis. The current study investigated whether glutathione-containing dry yeast extract (dry-YE) ameliorated eosinophilia, goblet cell hyperplasia and mucus overproduction. MATERIALS/METHOD: This study employed 2 ㎍/mL lipopolysaccharide (LPS)- or 20 ng/mL eotaxin-1-exposed human bronchial epithelial cells and ovalbumin (OVA)-challenged mice. Dry-YE employed in this study contained a significant amount of glutathione (140 ㎎ in 100 g dry yeast). RESULTS: Human bronchial epithelial cell eotaxin-1 and mucin 5AC (MUC5AC) were markedly induced by the endotoxin LPS, which was dose-dependently attenuated by nontoxic dry-YE at 10-50 μg/mL. Moreover, dry-YE inhibited the MUC5AC induction enhanced by eotaxin-1, indicating that eotaxin-1-mediated eosinophilia may prompt the MUC5AC induction. Oral supplementation with 10-100 ㎎/㎏ dry-YE inhibited inflammatory cell accumulation in airway subepithelial regions with a reduction of lung tissue level of intracellular adhesion molecule-1. In addition, ≥ 50 ㎎/㎏ dry-YE diminished the lung tissue levels of eotaxin-1, eosinophil major basic protein and MUC5AC in OVA-exposed mice. Alcian blue/periodic acid schiff staining revealed that the dry-YE supplementation inhibited goblet cell hyperplasia and mucus overproduction in the trachea and bronchiolar airways of OVA-challenged mice. CONCLUSIONS: Oxidative stress may be involved in the induction of eotaxin-1 and MUC5AC by endotoxin episode and OVA challenge. Dry-YE effectively ameliorated oxidative stress-responsive epithelial eosinophilia and mucus-secreting goblet cell hyperplasia in cellular and murine models of asthma.

67 ㎾ 급 농업용 트랙터의 경운작업별 배기가스 배출량 분석

이준호(Jun Ho Lee),전현호(Hyeon Ho Jeon),김연중(Yean-Jung Kim),서대석(Dae-Seok Seo),김용주(Yong Joo Kim) 대한기계학회 2021 대한기계학회 춘추학술대회 Vol.2021 No.5

농업용 트랙터의 경운작업별 배기가스 배출량 측정 및 분석

이준호 ( Jun-ho Lee ),백승민 ( Seung-min Baek ),전현호 ( Hyeon-ho Jeon ),서대석 ( Dae-seok Seo ),김연중 ( Yean-jung Kim ),김용주 ( Yong-joo Kim ) 한국농업기계학회 2021 한국농업기계학회 학술발표논문집 Vol.26 No.1

본 연구는 트랙터 경운작업시 실제 발생하는 배기가스 배출량을 분석하기 위해 수행되었다. 배기가스 배출량을 측정하기 위해서 Tier 4 엔진이 탑재된 67 kW 트랙터를 이용하여 측정하였다. 농작업은 플라우 및 로터리 경운 작업에 대해 수행하였으며, 작업 단수는 각각 B2(5.95 km/h), B3(7.60 km/h) 및 A3(2.67km/h), A4(3.66 km/h), PTO 1단(540 rpm)에 대해 수행하였다. 실제 경운작업시 발생하는 배기가스를 측정하기 위하여 PEMS(Portable Emissions Measurement system) 장비를 이용하였으며, 측정 항목은 CO, CO2, NOx, NO, NO2, THC이다. 플라우 및 로터리 작업시 배출량은 각 단수별 3회 반복 실험을 통하여 수집되었다. 배기가스 측정결과, 질소산화물에 속하는 NOx, NO, NO2는 측정 시작후 일정 시간이 지나면 배기가스 저감장치인 DPF(Diesel Particulate Filter)로 인하여 배출량이 0에 가까워지며, THC의 경우 경운 작업을 진행할수록 탄소의 완전연소로 인하여 그 값이 점점 감소하는 것으로 측정되었다. CO, CO2의 배출량은 같은 작업 및 작업단수에서 반복 작업시 평균 각각 0.006 ~ 0.01 및 10.49 ~ 13.36 g/s의 값을 나타냈으며, 작업단수 및 작업기에 따라 차이를 보였다. 배출량 분석결과, 작업 단수가 높거나 부하가 상대적으로 많은 농작업에서 높은 배출량을 나타냈으며, 이는 작업속도 증가 및 엔진 부하 증가는 높은 엔진 출력을 요구하기 때문인 것으로 판단된다. 향후 배기가스 규제에 따른 엔진 연구 및 환경분야 정책의 기초자료로 활용될 것으로 생각되며, 트랙터 외에 콤바인, 이앙기 등 주요 사용되는 농업기계에 대한 배출량도 측정하고 연구할 계획이다.

S-248 Effects of High Dose Statin on Infarct Size Evaluated by Cardiac MRI in STEMI

( Su Seong Kim ),( Ji Hae Lee ),( Yoon Ho Lee ),( Young Je Ki ),( Jung Yean Han ),( Dong Han Kim ),( Min Goo Lee ),( Su Hyun Kim ),( Jang Hyun Cho ) 대한내과학회 2016 대한내과학회 추계학술대회 Vol.2016 No.1

Objectives: Lipid-lowering therapy with statin may reduce the risk of cardiovascular events. Our study aim was to assess a dose dependent statin effects by using a cardiac MRI for measurement of myocardial infarction size. Method : We evaluated the cardiac MRI findings of 44 consecutive patients with acute myocardial infarction who underwent a percutaneous coronary intervention in Saint Carollo hospital. Initial and follow-up cardiac MRI was checked at 1 week and 12weeks after revascularization and high dose lipid-lowering therapy (Rosuvastatin 40mg, Group I, n=24) or low dose (Rosuvastatin 5mg, Group II, n=20). In MRI analysis, we evaluated the changes of microvascular obstruction (MVO, first-pass enhancement) and infarct size (delayed enhancement) that was expressed as a percentage of left ventricle area. Results: There were no differences of baseline characteristics between groups. The mean follow-up periods of cardiac MRI was 12.9±1.2 weeks. The changes of MVO in 2 groups showed a tendency of decreasing size, but there was no significant difference (-1.90±1.49 vs. -1.52±1.83, p=0.455). However the changes of infarct size in Group II was larger than Group I (0.45±2.4 vs 2.27±3.24, p=0.013). Conclusions: Compared with a low dose, high dose treatment of rosuvastatin significantly suppressed the increasing of infarct size after revascularization in AMI.

S-246 Implication of early change of Left Atrium Volume after ST elevation Acute Myocardial Infarction.

( Seong Taek Kim ),( Sun Hyung Kang ),( Ji Hae Lee ),( Su Seong Kim ),( Yoon Ho Lee ),( Young Je Ki ),( Jung Yean Han ),( Dong Han Kim ),( Min Goo Lee ),( Su Hyun Kim ),( Jang Hyun Cho ) 대한내과학회 2016 대한내과학회 추계학술대회 Vol.2016 No.1

Aim: Atrial enlargement has been suggested as a marker of the severity of diastolic dysfunction after acute myocardial infarction (AMI). The purpose of this study to assess the relationship between left atrial (LA) volume and outcome after AMI undergoing primary coronary intervention (PCI). This may be of importance when one assesses risk in patients with AMI undergoing PCI. Method : A total of 153 patients from December 2011 to June 2015 were recruited, prospective. Echocardiographic analyses were performed in 153 patients (92 male and 61 female, 63.4±11.7 years) with AMI undergoing PCI were studied at baseline and 12 months. We assessed LA volume index (LAVI) at baseline and 12 months after AMI. Result : Early change of Left atrial volume was an independent predictor of new onset atrial fibrillation or hospitalization for heart failure (p=0.02). In patient who survived to 12 months, LAVI increased a mean of 2.06±3.01 mL/m2 from baseline (from 25.1±7.6 to 29.0±8.1 mL/m2, p<0.001). Increased LAVI group were related to low LVEF, large left ventricle systolic and diastolic dimension and large LA size. Conclusions: Increased LAVI is a independent predictor of new onset atrial fibrillation and hospitalization for heart failure after AMI and provides prognostic information incremental to clinical data and conventional measures of LV systolic and diastolic function.

세 가지 구강간호방법에 따른 수술 후 환자의 갈증정도 및 구강상태 비교

김미영(Mi Young Kim),두미정(Mee Jung Doo),강수경(Su Kyeong Kang),임연호(Yean Ho Lim),김현미(Hyun Mi Kim),김미경(Mi Kyoung Kim),온지원(Ji Won On),설혜선(Hye Seon Seol),강정희(Jeong Hee Kang) 한국간호교육학회 2012 한국간호교육학회지 Vol.18 No.3

Purpose: This study compared the effects of three oral care methods on thirst and oral status in patients after general anesthesia surgery. Methods: Sixty five surgical patients were prospectively randomized into three groups. Each group received one of three oral care methods: wet water gauze, frozen water gauze, or frozen normal saline gauze. The outcomes of thirst and oral status were assessed three times by trained investigators blinded to the oral care methods. Assessment times were right after a participant’s arrival to his/her room, and at 30 and 60 minutes after the pre-test. Results: The levels of thirst and oral status were significantly improved as time passed in all three oral care methods. While the level of thirst was not significantly different between the three groups, the level of oral status was significantly better with wet water gauze than frozen gauze groups, soaked in either water or normal saline. Conclusion: We recommend nurses choose one of three oral care methods based on patients’ preferences since all three oral care methods showed similar effects in improving postoperative patients’ levels of thirst and oral status.