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SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-PHENYL-1-ARTLSULFONYL IMIDAZOLIDINONES
Jung, Sang-Hun,Lee, Hui-Soon,Song, Jae-Shin,Kim, Hwan-Mook,Han, Sang-Bae,Lee, Chang-Woo,Lee, Moonsun,Choi, Dong-Rack,Lee, Jung-Ah,Chung, Yong-Ho,Yoon, Sung-June,Moon, Eun-Yi,Hwang, Hyun-Sook,Seong, Se 충남대학교 약학대학 의약품개발연구소 1998 藥學論文集 Vol.14 No.-
Novel 1-(1-benzoylindoline-5-sulfonyl)-4-phenyl-4,5-dihydroimidazolones 3 synthesized show highly potent and broad cytotoxicities. Among them coumpound 3b (DW2143) exhibits much more potent cytotoxicities than doxorubicin and highly effective antitumor activities against murine (3LL, Colon 26) and human xenograft (NCl-H23, SW620) tumor models. ⓒ 1998 Elsevier Science Ltd. All rights reserved.
Synthesis and Antitumor activity of 4-Phenyl-1-1Arylsulfonyl Imidazolidinones
Jung, Sang-Hun,Lee, Hui-Soon,Song, Jae-Shin,Kim, Hwan-Mook,Han, Sang-Bae,Lee, Chang-Woo,Lee, Moon-Sun,Choi, Dong-Rack,Lee, Jung-Ah,Chung, Yong-Ho,Yoon, Sung-June,Moon, Eun-Yi,Hwang, Hyun-Sook,Seong, S 忠南大學校 癌共同硏究所 1998 癌共同硏究所 硏究誌 Vol.2 No.1
Novel l-(14>enzoylindoline-5-sulfonyl)-4-phenyl-4,5-dihydroimidazolones 3 synthesized show highly potent and broad cytotoxicities. Among them compound 3b (DW2143) exhibits much more potent cytotoxicities than doxorubicin and highly effective antitumor activities against murine (3LL, Colon 26) and human xenograft (NCI-H23, SW620) tumor models.
IM-412 inhibits the invasion of human breast carcinoma cells by blocking FGFR-mediated signaling.
Jung, Seung-Youn,Yi, Jae Youn,Kim, Mi-Hyoung,Song, Kyung-Hee,Kang, Seong-Mook,Ahn, Jiyeon,Hwang, Sang-Gu,Nam, Ky-Youb,Song, Jie-Young National Hellenic Research Foundation 2015 Oncology reports Vol.34 No.5
<P>Triple-negative breast cancer (TNBC) is an aggressive cancer with a poor prognosis due to its epithelial???to-mesenchymal transition (EMT) phenotype. Cancer patients often experience several detrimental effects of cancer treatment, such as chemoresistance, radioresistance and the maintenance of cancer stem cells due to EMT. Thus, EMT signaling is considered to be a valuable therapeutic target for cancer treatment, and its inhibition is being attempted as a new treatment option for TNBC patients. Previously, we showed that 3-(2-chlorobenzyl)-1,7-dimethyl-1H-imidazo[2,1-f]purine???2,4(3H,8H)-dione (IM-412) inhibits transforming growth factor-관 (TGF-관)-induced differentiation of human lung fibroblasts through both Smad-dependent and??-independent pathways. In the present study, we examined the inhibitory effect of IM-412 on EMT pathways and invasiveness in TNBC cells since the TGF-관 signaling pathway is a typical signaling pathway that functions in EMT. IM-412 not only potently suppressed the migration and invasion of MDA-MB-231??cells, but also lowered the expression of mesenchymal markers and EMT-activating transcription factors in these cells. IM-412 inhibited the activation of several signaling proteins, including Smad2/Smad3, p38MAPK, Akt and JNK, and it also attenuated the phosphorylation of FGFR1 and FGFR3. Collectively, our findings suggest that the synthetic compound IM-412 suppressed the EMT process in MDA-MB-231??cells and thereby effectively inhibited the migration and invasion of these cancer cells. Thus, IM-412 could serve as a novel therapeutic agent for malignant cancers.</P>
Siderophore 생산성 생물방제균 Pseudomonas fluorescens GL7의 선발 및 식물근부병의 방제
이정목,임호성,장태현,김상달 한국산업미생물학회 1999 한국미생물·생명공학회지 Vol.27 No.6
농산물의 증산을 위한 과도한 농약 사용으로 인한 토양 생태계의 파괴를 줄이기 위하여 맹독성 농약을 대신할 수 있는 생물학적 방제제 개발의 일환으로 식물병원성 진균의 생육을 억제하는 siderophore를 생산하는 생물학적 방제균을 선발하여, 이를 동정하고 근부병균억제기작을 연구하여 향후 다기능 생물학적 방제제 개발의 기초자료로 활용하고자 하였다. 이를 위해 저병해 경작지 토양에 장기간 우점화되어 있는 siderophore 생산 가능성이 높은 토착 길항미생물을 전국 각지의 저병해 경작지에서 분리하였고, 이들 중 siderophore 생산능이 높은 길항미생물 4종의 균주를 chrome azurol S(CAS) agar를 이용하여 선발하였다. 그 중 최고의 길항성을 나타내는 GL7 균주를 최종 선발하였고, API® diagnostic test와 지방산 분석, 그리고 각종 생리학적 특성 및 형태학적 특성을 통해 동정한 결과 Pseudomonas fluorescens의 한 균주임을 확인하였다. 최종 선발된 siderophore 생산균주 P. fluorescens GL7의 길항기작을 병원성 진균인 Fusarium solani를 대상으로 균사 생장과 포자 발아 등의 억제율을 조사한 결과 균사 생장 억제율은 75% 이상이며, 포자 발아억제율은 97% 이상으로 우수한 방제능을 확인할 수 있었다. 선발된 siderophore 생산능이 높은 길항균주 P. fluo-rescens GL7을 대상으로 토양 내에서 실제로 근부병에 방제력이 있는가를 조사하기 위해 강낭콩 종자(Phaseolus vulgaris L.)를 발병 기주식물로 사용하여 방제시험을 한 결과 F. solani만 처리한 경우는 30%의 성장율을, P. fluorescens GL7 균주와 F. solani와 함께 처리한 경우는 95% 정도의 성장율을 나타내어 약 65% 정도의 발병율을 줄일 수 있었다. 또한 F. solani와 P. fluorescens GL7을 처리하지 않은 무처리구에 비해 식물 무게가 147% 정도로 증가하여 식물의 생육도와 뿌리의 발육상태가 양호하였고, 근부병 발생도 거의 볼 수 없었으므로 아주 우수한 siderophore 생산성 생물학적 방제균을 선발할 수 있었다. For the development of a multifunctional biocontrol agent, the siderophore-producing strain GL7 was isolated from a rhizosphere on chrome azurol S agar. The GL7 was identified as a strain of Pseudomonas fluorescens on the basis of their reactions to standard physicochemical tests from Bergey's manual, API® diagnostic test, and fatty acid analysis. P. fluorescens GL7 produced a large amount of yellow-green fluorescent siderophore in iron-deficient media. P. fluorescens GL7 considerably inhibited spore germination and hyphal growth of phytopathogenic fungus Fusarium solani in a dual culture. In pot trials of bean with P. fluorescens GL7, the disease incidence was significantly reduced down to 5% from 70% of incidence in the untreated control. P. fluorescens GL7 also enhanced plant growth to nearly 1.5 times than that of the untreated control, promoting elongation and development of the roots. These results suggest that the plant growth-promoting P. fluorescens GL7 can play an important role in the biological control of soil-borne plant disease in a rhizosphere.
김성묵(Seong Mook Kim),정나영(Na Young Jung) 대한두개저학회 2014 대한두개저학회지 Vol.9 No.1
Although actinomycosis has generally indolent clinical courses, it has high mortality risk if not treated properly, especially in cranial and spinal cases. However, orbitocranial actinomycosis is hard to be differentiated clinically and radiographically from other pathological conditions. A healthy 62-year-old man complained of a progressive headache and orbital pain, presenting a soft, tender subcutaneous mass over the right forehead. Imaging showed multiple enhanced lesions in the right orbit and the pterion with invasion to temporalis muscle and epidural space. In the operative view, white-yellowish lesion extended into the bone, muscle, and even the dura. Necrotic pus was drained from the extradural space. He was pathologically diagnosed with actinomycosis with sulfur granules. The lesion was completely regressed after antibiotic therapy for 20 weeks. The authors tried to determine the appropriate impression on this problematic lesion and optimal management of actinomycosis in neurosurgery.
우리 나라 말기심부전 환자에서 적출한 심장에서의 인형 거대세포 바이러스 감염의 빈도
최성준(Seong Choon Choe),김효수(Hyo Soo Kim),오병희(Byung Hee Oh),이명묵(Myoung Mook Lee),최현석(Hyun Seok Choi),김용진(Yong Jin Kim),손대원(Dae Won Sohn),박영배(Young Bae Park),최윤식(Yun Shik Choi),서정돈(Jung Don Seo),이영우(Young 대한내과학회 1997 대한내과학회지 Vol.53 No.3
Objective: In order to evaluate the prevalence of cytomegalovirus infection to terminally failing heart, cytomegaloviral DNA was detected in the explanted hearts of transplantation recipients. Methods: DNA extractions were performed from explanted failing hearts(N=22) and normal hearts (N=5) and polymerase chain reactions(PCRs) were done for detection of late gene sequence coded pp150 phosphoprotein. The products were confirmed with electrophoresis on 1% agarose gel. In order to improve the sensitivity of detection in cytomegaloviral genome, nested PCRs were executed with the primers designed for the original 607 bp products. Results : All patients had IgG anti-cytomegalovirus antibody and did not have IgM anti-cytomegalovirus antibody. Cytomegaloviral genomes in myocardium were detected by polymerase chain reaction. The 607bp products by PCRs were found in both explanted failing hearts(3 cases/22, 13.5%) and normal hearts(1 case/5, 20.0%). In nested PCRs, 186bp products were found in both failing hearts(LV 4/22, LA 3/20, RV 5/22, HA 0/17) and normal hearts(LV 2/5, LA 1/4, RV 1/5, RA 2/5). There was no significant change in the presence of cytomegaloviral DNA between failing and normal hearts. Total positivity of cytomegaloviral genome in explanted hearts was 44.4% according to nested PCR results. Conclusion: Cytomegalovirus was rarely observed in explanted hearts of terminal heart failure and nested PCR could enhance the sensitivity of cytomegaloviral genome detection. But cytomegalovirus might have no direct causal relationship in the development of terminal heart failure.
유전자 재조합 B 형 간염 바이러스 표면 항원 , CJC-50100 의 일반약리작용
정성학(Seong Hak Jeong),최재묵(Jae Mook Choi),이남중(Nam Jung Lee),전형수(Hyung Soo Jeon),김연희(Yon Hee Kim),김재승(Jae Seung Kim),하석훈(Suk Hoon Ha),김영훈(Young Hoon Kim),이나경(Na Gyung Lee),김제학(Je Hak Kim),박완제(Wan Je Park 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.1
N/A CJC-50100 is a recombinant hepatitis B virus surface antigen (HBsAg) expressed in yeast. The general pharmacological properties of CJC-50100 were evaluated in mice, rats, dogs and isolated guinea pig ileum. The doses were 0.33∼33.3 ㎍/㎏ i.m. for mice and rats and 3.3∼9.9 ㎍/㎏ i.v. for dogs. The concentrations of 0.002∼0.02 ㎍/mlwere used for the assay with guinea pig ileum. Intramuscular administration of CJC-50100 at the doses did not alter general behavior and the responses for central nervous system, smooth muscle, gastrointestinal system, cardiovascular and respiratory system, and water and electrolytes excretion. In summary, CJC-50100 had no pharmacological effect in these studies even up to the 100-fold of the expected clinical dose, 20 ㎍/man/60 kg.