새로운 Acetylcholinesterase inhibitors의 합성

최순규,김형민,조승환,최학기,박유미,이용균,정대일,김인식,한정태 동아대학교 부설 기초과학연구소 2004 基礎科學硏究論文集 Vol.21 No.1

노인성 치매의 일종인 alzheimer's disease의 효과적인 억제제를 합성하기 위해 우리는 분자 모델링에 의한 가장 적합한 물질인 m-[(N,N,N-trimethylammonio)phenyl]boronic acid를 합성하였다. 출발물질인 3-aminophenylboronic acid monohydrate의 경우 boronic acid의 작용기인 hydroxyl group을 protecting시킴으로써 반응의 안정성을 기하였다. Quarternary ammonium salt는 과량의 methyliodide와 염기 촉매인 potassium hydrogen carbonate를 사용하여 용매인 methanol에서 반응시켜 상당히 높은 수율을 얻을 수 있었다. 또한 과량의 methyliodide와 염기촉매인 potassium hydrogen carbonate를 사용하여 용매인 methanol에서 반응시킨 결과 boronic acid의 protection없이도 안정하게 반응이 진행되어짐을 확인할 수 있었다. In order to syntheisize a effective inhibotor for alzheimer's disease, we synthesized m-[(N,N,N-trimethylammonio)phenyl]boronic acid 4 which is designed by molecular modeling form. We protected the hydroxyl group of 3-aminophenylboronic acid monohydrate 1 with ethlyne glycol to remove the reactivity if hydroxyl group. To synthesize m-[(N,N,N-trimethylammonio)phenyl]boronic acid 4, we reacted 3-aminophenylboronic acid monohydrate 1 with ezcess methyl iodide and potassium hydrogen carbonate as a base-catalyst in methanol. but On executed reaction without protection on hydroxyl group, we found out the result that the hydroxyl group of boronic acid group at 3-aminophenylboronic acid monohydrate 1 didn't react with excess methyliodide. Synthesized m-[(N,N,N-trimethylammonio)phenyl]boronic acid 4 is in progress about biological tests as a plausible acetylcholinesterase inhibitor.

달걀껍질(생, 삶은)의 수처리에 관한 연구

정대일,정선주,김인식,최영하,류정숙,이용균,최순규 동아대학교 환경문제연구소 1999 硏究報告 Vol.22 No.2

The selective absorption ability of low density heavy metal(Pb(Ⅱ) ion or Cu(Ⅱ) ion) of eggshell(raw or boiled) is better than one of existing absorption materials in treatment ability and experimental condition. The elimination ability of chlorine of eggshell(raw or soiled) is worse than one of active carbon. In elimination of trihalomethane, the effect of treatment of eggshell is almost the same as one of pine cones. And surface of eggshell(raw or boiled) after absorption of heavy metal ion was observed by Scanning Electron Microscope(SEM). Application and availability of eggshell(raw or boiled) as absorption material need lots of experiments. The experiment on baked eggshell is proceeding.

8년간(1992~1999) 산업안전보건연구원에 의뢰된 직업병 심의 사례 분석

강성규,김규상,김양호,최정근,안연순,진영우,최병순,양정선,김은아,채창호,최용휴,김대성,박정선,정호근 대한산업의학회 2000 대한직업환경의학회지 Vol.12 No.2

Objectives : Pneumoconisis and noise-induced hearing loss (NIHL) have been reported as main occupational diseases by the Special Health Examination. The Industrial Accident Compensation Insurance has reported various work-related diseases, however, these two diseases occupied almost a half of compensated cases. Therefore, it was not well known about the status of occupational diseases other than pneumoconiosis, NIHL, and cardio-cerebrovascular accident (CVA). This study was conducted to analyze claimed cases as an occupational disease, that was requested to the Korea Industrial Safety and Health Agency (KOSHA). Methods : The local office of the Korea Labor Welfare Corporation (KLWC) has asked the KOSHA for confirmation of claimed cases as an occupational disease. We analyzed 379 cases requested from KLWC, the Ministry of Labor, employers, unions and occupational health agencies from 1992 to 1999. Results : Male was 80.7 % of the requested cases. Their mean age was 42 years old and 75.5 % of them were more than 35 years old. The requested cases were increased rapidly from 25 cases in 1992 to 108 cases in 1999 and the accept rate was 50.7 %. The majority of requested cases were respiratory diseases(22.4%), cancers(18.5%), Neuropsychiatric problems(14.5%), and musculoskeletal problems(13.5%). The accept rate was high in reproductive, respiratory, musculoskeletal and digestive disorders and low in neuropsychiatric, renal and otologic problems and occupational cancers. 73.6% of them were caused by chemical agents, especially 28.5 % were by organic solvents. 67% of them were clinically confirmed at university hospitals. A half of the cases were from KyongIn area, even the request came from the whole country. Conclusions : A claim was common in workers whose age was over 35 years old and exposure history was over 10 years. The respiratory diseases and neuropsychiatric disorders were still main problems in occupational health and occupational cancers was increasing even though its accept rate was not high yet.

흉추 경막외강으로 침윤한 흉선종 1례 : Metstasis to Thoracic Epidural Space

최정훈,백욱성,박대곤,오경구,최천식,배상도 高麗病院 1987 高醫 Vol.10 No.-

1,2-Benzisothiazol-3-one-1,1-Dioxide 유도체의 합성

정대일,정희철,변석인,이용균,박유미,최순규,한정태 東亞大學校附設基礎科學硏究所 2002 基礎科學硏究論文集 Vol.19 No.1

사카린 유도체는 제초제, 항독성, 살균제 등에 광범위하게 연구되어져 오고 있다. 새로운 농략 활성을 가진 물질을 합성하기 위해 먼저 선도물질로 사카린 1을 산화, 염소화 시킨 3-chloro-1,2-benzisothiazol-1,1-dioxide(BID-CI) 2와2cholromethy-1,2-benzisohizol-3-one1,1-dioxide 4를 합성하였다. 선도물질, amines, imidazoles, trones등과 반응시켜 다음과 같은 물질들을 얻었다. ; 3-cyclohexylamino-1,2-benzisothiazol-1,1-dioxide 6, 3-furylamino-1,2-benzisothiazol-1,1-dioxide 8, 3-(3-imidazol)-1,2-benzisothiazol-1,1-dioxide 10, 3-(2-methy-3-imidazol)-1,2-benzisothaizol-1,1-dioxide 12, 2-(3-imidazol)methy-1-1,2-benzisothiazol-3-one-1,1-dioxide 13, and 2-(-3-imidazol)methyl- 1,2-benzisothiazol-1,1-dioxide 14.

흰쥐에서 다시마 식이가 메트폴민의 체내동태 및 당 흡수에 미치는 영향

최한곤,장보현,이종달,김정애,유봉규,용철순 한국약제학회 2003 Journal of Pharmaceutical Investigation Vol.33 No.3

Drug interactions with food, on occasion, led to serious nutritional and functional changes in the body as well as alterations of pharmacological effect. It, therefore, should be necessary to take drug interactions with food into consideration for effective and safe therapeutics. Diabetes mellitus is a heterogeneous group of disorders characterized by abnormal glucose homeostasis, resulting in hyperglycemia, and is associated with increased risk of microvascular, macrovascular, and neuropathic complications. However, the precise mechanism of diabetes mellitus remins unclear. Three basic objectives in the care of diabetic patients are maintaining optimal nutrition, avoiding hypo-or hyperglycemia and preventing complications. Laminaria japonica is a brown macroalgae which can be used as a functional diet due to high content of diatery fiber. the purpose of this study was to investigate the effect of Laminaria japonica diet on the pharmacokinetics of metformin which are frequently used in the treatment of diabetes. Diabetic rats induced by strep-tozotocin were employed in this study. Blood concentrations of oral hypoglycemic agent, metformin, were measured by HPLC and resultant pharmacokinetic parameters were calculated by RSTRIP. The mechanisms of drug interaction with food were evaluated on the basis of pharmacokinetic parameters such as k_(a), t_(1/2), C_(max), t_(max), and AUC, C_(max), and k_(a), and increase in t_(max), compared to those with normal diet. This oral glucose test showed that Laminaria japonica diet could lower blood glucose level probably through either inhibiting the activity of disaccharidases, intestinal digestive enzymes, or delaying the absorption of glucose. More studies should be followed to fully understand pharmacokinetic changes of metformin caused by ong-term Laminaria japonica diet.

고형지질나노입자를 이용한 파클리탁셀의 주사제 설계

최성업,김선규,이정민,최영욱 한국약제학회 2003 Journal of Pharmaceutical Investigation Vol.33 No.4

Many studies have been attempted to overcome the problems of paclitaxel related to the extremely low aqueous solubility of paclitaxel and the unexpected side-effects caused by Cremophor® EL in a commerical paclitaxel formulation. Taxol®. In order to formulate a new delivery system suitable for intravenous administration without toxic excipients, in this study, paclitaxel was incorporated into solid lipid nanoparticles (Px-SLN) by hot homogenization technique using a microfluidizer. Particle size and zeta potential were measured by a Zetasizer. In vitro drug release experiment was performed by a dialysis diffusion method. Each Px-SLN or Taxol® was intravenously administered to the male Sprague-Dawley rats at a dose of 5㎎/㎏ as paclitaxel. Blood samples were deproteinated with acetonitrile and assayed for paclitaxel by the validated HPLC/MS/MS method. Mean particle size and zeta potential were measured as 72.1 nm(<Polydispersity 0.3) and -41.5 mV, respectively. The content of paclitaxel in SLN was 1.42 ㎎/ml and the drug loading efficiency was 71.2±4.3%. The AUC_(t) of Px-SLN was 3.4-fold greater than that of Taxol^(?). The Px-SLN might be a promising candidate for an alternative formulation for the parenteral delivery of paclitaxel.

안면부에 발생한 고정형 스포로트리쿰증 3례

최윤애,류영욱,정재봉,송준영,이규석 啓明大學校 醫科大學 1993 계명의대학술지 Vol.12 No.3

We experienced 3 cases of fixed type cutaneous sporotrichosis confined to the face. Case 1 was a 32-month old child, affected over the nose. Case 2 was a 25-year old man, affected over the left cheek. Case 3 was a 71-year old man, affected over the nose. Histopathologically, chronic granulomatous inflammation with pseudoepitheliomatous hyperplasia was observed. Mycologically, typical dark brown to black colored colonines with moist, wrinkled and membranous surfaces were cultured. All patients were completely cured by oral administration of saturated KI and itraconazole combined therapy in a short period(40-90 days).

치료 저항성 환청을 나타내는 만성 정신분열병 환자에서 측두두정부 반복 경두개자기자극의 효과

정경희,최충식,박진수,이규항,함웅,이승환,채정호 大韓神經精神醫學會 2004 신경정신의학 Vol.43 No.5

Objectives : It has been reported that repetitive transcranial magnetic stimulation (rTMS), which stimulate the focal region of brain may relieve auditory hallucination in patient with schizophrenia. This study was aimed to evaluate the effect of rTMS on left and right temporopahetal cortex in schizophrenic patients with treatment-resistant auditory hallucination. Methods : Twenty-six patients with chronic schizophrenia with treatment -resistant auditory hallucination were randomly a1-located to rTMS group on left and right temporoparietal head regions. The rTMS was applied to TP3/4 region by EEG 10-20 international system at 1 Hz for 20 minutes per day for 101reatment days. A Figure of eight TMS coil with a solid core was used for rTMS at 100% of individual motor threshold. Efficacy was evaluated with Auditory Hallucination Rating Scale (HRS), Positive and Negative Symptoms Scale (PANSS), Clinical Global Impression (CGI) Scale on 5 and 10 days of treatment. Results : Ten days administration of l-Hz rTMS to temporopahetal cortex significant improved frequency (p<0.001) and attentional salience (p=0.038) of auditory hallucination, Positive (p<0.001) and negative symptom (p=0.02), and CGI-impro-vement (p<0.001). There were no significant differences between right and left side stimulations. Conclusion : These results suggest that the low frequency rTMS on temporopahetal cortex may be useful in treating Schizo-phrenic patients with treatment-resistant auditory hallucination and it could be a useful novel treatment option.

全身麻醉中 發生한 不適合輸血의 症例報告 : A Case Report

崔泳錫,李奎順,金勇赫,辛正順 한국의 현대의학사 1974 한국의 현대의학 Vol.7 No.1