• Asian Pacific Journal of Cancer Prevention
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• 제15권23호
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• pp.10345-10350
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• 2015

Background: Punica granatum (family: Lythraceae) is mainly found in Iran, which is considered to be its primary centre of origin. Studies on pomegranate peel have revealed antioxidant, anti-inflammatory, anti-angiogenesis activities, with prevention of premature aging and reducing inflammation. In addition to this it is also useful in treating various diseases like diabetes, maintaining blood pressure and treatment of neoplasms such as prostate and breast cancer. Objectives: In this study we identified anti-cancer targets of active compounds like corilagin (tannins), quercetin (flavonoids) and pseudopelletierine (alkaloids) present in pomegranate peel by employing dual reverse screening and binding analysis. Materials and Methods: The potent targets of the pomegranate peel were annotated by the PharmMapper and ReverseScreen 3D, then compared with targets identified from different Bioassay databases (NPACT and HIT's). Docking was then further employed using AutoDock pyrx and validated through discovery studio for studying molecular interactions. Results: A number of potent anti-cancerous targets were attained from the PharmMapper server according to their fit score and from ReverseScreen 3D server according to decreasing 3D scores. Conclusion: The identified targets now need to be further validated through in vitro and in vivo studies.

• Environmental Analysis Health and Toxicology
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• 제22권4호
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• pp.349-355
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• 2007

장수풍뎅이 유충(Allomyrina dichotoma larva, ADL)은 중국의 전통 약재로서, 특히 항산화 효과가 우수하여 항당료 제재로 사용되고 있다. 본 연구에서는 이러한 ADL의 추출물을 이용하여 헴스터 췌장의 ${\beta}$-세포(HIT-T15)에서 Streptozotocin에 의해 유발된 산화적 손상에 대한 보호효과 및 그 작용기전을 조사하였다. ADL추출물은 처리농도 의존적으로 Streptozotocin에 의해 유발된 지질과산화 및 세포 내 자유산 소종의 양을 억제함으로서 ${\beta}$-세포의 산화적 스트레스에 의한 손상을 보호하였다. 또한 DNA laddering 방법을 사용하여 Streptozotocin에 의해 유발된 DNA 손상을 조사한 결과, ADL추출물 처리농도에 비례하여 Streptozotocin에 의해 유발된 DNA 손상이 감소하였다. 이러한 산화적 손상의 억제능 관련 작용 기전을 조사하기 위해 DPPH free radical 소거능을 실시하였다. 그 결과 ADL추출물 자체가 DPPH 자유 레디컬 소거능이 있음을 확인하였으며, 또한 플라스미드를 이용한 Single-strand break 방법을 통한 DNA 손상 보호능을 측정한 결과도 $Fe^{3+}$ 및 $H_2O_2$에 의해 유발된 DNA 손상이 ADL추출물 처리농도에 비례하여 감소하였다. 이러한 결과들을 종합하여 볼 때, 장수풍뎅이 유충의 추출물들이 자체의 레디컬 소거능 및 산화적 손상에 의한 DNA손상을 억제함으로써, Streptozotocin에 의해 유발된 산화적 손상을 억제할 수 있을 것이라 사료된다.

• Biomolecules & Therapeutics
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• 제26권2호
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• pp.201-209
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• 2018

G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as the secretion of glucagon-like peptide-1 (GLP-1) in intestinal L cells, consequently improving glucose-stimulated insulin secretion. Due to this dual mechanism of action, the development of small-molecule GPR119 agonists has received significant interest for the treatment of type 2 diabetes. We newly synthesized 1,2,4-triazolone derivatives of GPR119 agonists, which demonstrated excellent outcomes in a cyclic adenosine monophosphate (cAMP) assay. Among the synthesized derivatives, YH18968 showed cAMP=2.8 nM; in GLUTag cell, GLP-1secretion=2.3 fold; in the HIT-T15 cell, and insulin secretion=1.9 fold. Single oral administration of YH18968 improved glucose tolerance and combined treatment with a dipeptidyl peptidase 4 (DPP-4) inhibitor augmented the glucose lowering effect as well as the plasma level of active GLP-1 in normal mice. Single oral administration of YH18968 improved glucose tolerance in a diet induced obese mice model. This effect was maintained after repeated dosing for 4 weeks. The results indicate that YH18968 combined with a DPP-4 inhibitor may be an effective therapeutic candidate for the treatment of type 2 diabetes.

• 대한치과교정학회지
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• 제15권1호
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• pp.141-148
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• 1985

It has been a long time since the cephalometrics was introduced to orthodontic field for diagnosis and treatment planning, but it's main concern was limited to hard, skeletodental tissue. It is well known that perioral and facial soft tissue determine the position of individual teeth and that the abnormality in size and shape of the soft tissue are able to cause malformed occlusion. Because of our lack of knowledge about resultant morphologic changes in the relationship between skeletal pattern and specific pattern of lingual and facial muscles, we can't help setting greater value on only abnormalities of teeth in the skeletal interrelationship. In a point of view that the orthodontist is dealing primarily with muscular structures around the dentition, the tongue, lips, and cheeks, therefore it may be desirable to estimate these structure and their potential influence on the dentition on developmental and time base. The author hit upon on idea of the aspect above, so studied on the intermaxillary space and tongue space and this study used the data from cephalometric films of 33 male and 40 female subject aged from 6 to 11 years of normal Korean children following results were obtained: 1. Means and standard deviation of Korean children were obtained. 2. Yearly increment of each variables were obtained. 3. There is the correlationship more than average among the variables except posterior intermaxillary height item. 4. There are differences between male children and female children in all variables except posterior intermaxillary space item. 5. All variables increased as the age increased except posterior intermaxillary height item of male children.

• Bulletin of the Korean Chemical Society
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• 제29권9호
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• pp.1717-1722
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• 2008

The 70 kDa heat-shock protein (Hsp70) involved in various cellular functions, such as protein folding, translocation and degradation, regulates apoptosis in cancer cells. Recently, it has been reported that the green tea flavonoid (−)-epigallocatechin 3-gallate (EGCG) induces apoptosis in numerous cancer cell lines and could inhibit the anti-apoptotic effect of human Hsp70 ATPase domain (hATPase). In the present study, docking model between EGCG and hATPase was determined using automated docking study. Epi-gallo moiety in EGCG participated in hydrogen bonds with side chain of K71 and T204, and has metal chelating interaction with hATPase. Hydroxyl group of catechin moiety also participated in metal chelating hydrogen bond. Gallate moiety had two hydrogen bondings with side chains of E268 and K271, and hydrophobic interaction with Y15. Based on this docking model, we determined two pharmacophore maps consisted of six or seven features, including three or four hydrogen bonding acceptors, two hydrogen bonding donors, and one lipophilic. We searched a flavonoid database including 23 naturally occurring flavonoids and 10 polyphenolic flavonoids with two maps, and myricetin and GC were hit by map I. Three hydroxyl groups of B-ring in myricetin and gallo moiety of GC formed important hydrogen bonds with hATPase. 7-OH of A-ring in myricetin and OH group of catechin moiety in GC are hydrogen bond donors similar to gallate moiety in EGCG. From these results, it can be proposed that myricetin and GC can be potent inhibitors of hATPase. This study will be helpful to understand the mechanism of inhibition of hATPase by EGCG and give insights to develop potent inhibitors of hATPase.

• 한국응급구조학회지
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• 제15권1호
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• pp.65-78
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• 2011

Purpose : We investigated the career choice and the employment preparation of emergency medical technology (EMT) students. The results of study will provide the base information about the consciousness for career choice and employment of the EMT students. Method : We conducted 1,586 surveys from 665 students at six four-year colleges and 921 students at seven three-year colleges, from Aug. 27th to Oct. 31st in 2010. The result was analyzed by SPSS 18.0 using description statistics, t-test, ANOVA, Scheffe and Pearson correlation coefficient. Result : The general characteristics showed male 50.2% and female 49.8%, and first grade 34.6%, second grade 27.4%, third grade 28.2%, and fourth grade 9.8%. The 53.9% of students had experienced the hospital training and the 44.8% did the fire station training. For the choice of job, there were the 61.8% student who hope to enter the employ in fire station or public service, while 25.7% students hope to be employed in hospitals. The reason for a wish job were 'majors-related job' in 18.2% students, 'employment stability' in 17.2% and 'hit on the aptitude and talent' in 16.7%, 'appropriate salaries' in 15.9%. In the questionnaire of the University what to assist you for job preparation, they chose the 'support for get major related license', 'support for officer exam preparation' and 'support of foreign language study' in 34.6%, 16.8% and 16.6%, respectively. For achieved licence, they had a driver's license in 53.9%, BLS (basic life support) provider in 20.3%, life guard in 16.2% and scuba in 8.8%. The statistically significant correlation was identified between the awareness of University that provides job information and one's career awareness (r= .203, p<.000), the awareness that University provide job information and one's confidence in employment (r= .236, p<.000), and one's career awareness and one's confidence in employment (r = .356, p = .000). Conclusion : The most of EMT Students are well conscious of the their future employment and has prepared career to be employed their preference job.

• 디지털콘텐츠학회 논문지
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• 제11권2호
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• pp.177-184
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• 2010

오늘날의 디지털영상 제작기술의 발전과 더불어 3D 이미징 기술은 첨단 TV와 컴퓨터에 응용되고 있으며 3D 입체 영상 제작 기술에 대한 연구, 개발이 활발히 진행되고 있다. 2009년 개봉한 제임스캐머런(James Cameron)감독의 3D입체영화 '아바타' 흥행 이후 3D 입체영상에 대한 관심이 대두 되고 있는 상황에서 본 연구는 최근 대두되고 있는 입체영상제작에 있어서 후반제작 공정상 색 보정이 입체의 깊이감에 미치는 영향을 실험하였다. 기존 영상제작 후반작업에서의 색 보정과정을 3D입체영상 제작과정에 적용하여, 입체감 변화에 대한 데이터를 측정하고 이를 통하여 3D 입체영상 제작에 있어서 효과적인 영상처리프로세스에 대한 정보를 제공하는 것이 연구의 목적이다. 입체영상에서 색과 명암대비가 입체의 깊이감을 인지하는데 영향을 줄 수 있다는 가정을 전제로 색 보정 실험을 하였다. 입체감, 공간감, 깊이감의 변화에 대한 피 실험자 반응을 종합하여 입체감이 상승하는 결과를 확인 할 수 있었다. 본 실험을 통하여 도출된 결과를 적용하여 15분 분량의 입체홍보영화를 제작 하였으며, 후반제작과 정상에서 색 보정 작업 결과가 입체를 인지하는 깊이감에 영향을 미치는 것으로 확인됐다. 본 연구의 실험은 평행리그와 직교리그를 통하여 촬영된 좌측영상과 우측영상의 영상이미지를 실험 데이터로 사용하였으며 편집과정에서 컨버전스와 입체감을 수정한 후에 후반제작에서 색 보정 작업을 통하여 명암대비를 높였다. 그 결과 영상의 공간감과 깊이감, 그리고 돌출감이 증가한 영상을 제작 할 수 있었다.

• 생명과학회지
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• 제18권9호
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• pp.1305-1311
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• 2008

본 연구는 바나바 잎 추출 용매에 따른 항당뇨 효과에 관한 것으로 세포 독성 실험을 통하여 인체에 대한 독성이 없음을 확인하였고 $\beta$-cell 인슐린 분비 실험을 통하여 항당뇨 효과를 알아보았다. 또한 당뇨 유발쥐를 이용한 인슐린 분비 실험, 체중변화 측정, 혈중 및 혈청의 glucose 농도, 총콜레스테롤 수치, HDL-cholesterol 농도, triglyceride 농도, free fatty acid 농도, langerhans islet에서의 인슐린 분비 의 확인을 통해 혈당조절 효과를 비교하였다. 물 혹은 에탄올을 단독으로 이용하여 추출한 추출물이나 70%, 90% 에탄올로 추출한 추출물 보다 열수로 먼저 추출한 후 에탄올로 다시 추출하여 혼합안 추출물이 항당뇨 효과가 더 뛰어남을 알 수 있었다. 이는 친수성(hydrophilic) 유효성분들과 소수성(hydrophobic) 유효성분들의 추출 유무나 함량에 의한 것이다. 특히, 많은 문헌에 언급된 코로소린산이라는 단일 성분(unique)에 의한 항당뇨 효과라기보다는 친수성 및 소수성 폴리페놀 및 항산화성분과 같은 유효성분들이 조합되어(mixture) 항당뇨 효과에 영향을 미치는 것으로 사료된다.

• 한국균학회소식:학술대회논문집
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• 한국균학회 2014년도 춘계학술대회 및 임시총회
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• pp.27-28
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• 2014

Beauveria bassiana (Cordycipitaceae, Hypocreales, Ascomycota) is an anamorphic fungus having a potential to be used as a biological control agent because it parasitizes a wide range of arthropod hosts including termites, aphids, beetles and many other insects. A number of bioactive secondary metabolites (SMs) have been isolated from B. bassiana and functionally verified. Among them, beauvericin and bassianolide are cyclic depsipeptides with antibiotic and insecticidal effects belonging to the enniatin family. Non-ribosomal peptide synthetases (NRPSs) play a crucial role in the synthesis of these secondary metabolites. NRPSs are modularly organized multienzyme complexes in which each module is responsible for the elongation of proteinogenic and non-protein amino acids, as well as carboxyl and hydroxyacids. A minimum of three domains are necessary for one NRPS elongation module: an adenylation (A) domain for substrate recognition and activation; a tholation (T) domain that tethers the growing peptide chain and the incoming aminoacyl unit; and a condensation (C) domain to catalyze peptide bond formation. Some of the optional domains include epimerization (E), heterocyclization (Cy) and oxidation (Ox) domains, which may modify the enzyme-bound precursors or intermediates. In the present study, we analyzed genomes of B. bassiana and its allied species in Hypocreales to verify the distribution of NRPS-encoding genes involving biosynthesis of beauvericin and bassianolide, and to unveil the evolutionary processes of the gene clusters. Initially, we retrieved completely or partially assembled genomic sequences of fungal species belonging to Hypocreales from public databases. SM biosynthesizing genes were predicted from the selected genomes using antiSMASH program. Adenylation (A) domains were extracted from the predicted NRPS, NRPS-like and NRPS-PKS hybrid genes, and used them to construct a phylogenetic tree. Based on the preliminary results of SM biosynthetic gene prediction in B. bassiana, we analyzed the conserved gene orders of beauvericin and bassianolide biosynthetic gene clusters among the hypocrealean fungi. Reciprocal best blast hit (RBH) approach was performed to identify the regions orthologous to the biosynthetic gene cluster in the selected fungal genomes. A clear recombination pattern was recognized in the inferred A-domain tree in which A-domains in the 1st and 2nd modules of beauvericin and bassianolide synthetases were grouped in CYCLO and EAS clades, respectively, suggesting that two modules of each synthetase have evolved independently. In addition, inferred topologies were congruent with the species phylogeny of Cordycipitaceae, indicating that the gene fusion event have occurred before the species divergence. Beauvericin and bassianolide synthetases turned out to possess identical domain organization as C-A-T-C-A-NM-T-T-C. We also predicted precursors of beauvericin and bassianolide synthetases based on the extracted signature residues in A-domain core motifs. The result showed that the A-domains in the 1st module of both synthetases select D-2-hydroxyisovalerate (D-Hiv), while A-domains in the 2nd modules specifically activate L-phenylalanine (Phe) in beauvericin synthetase and leucine (Leu) in bassianolide synthetase. antiSMASH ver. 2.0 predicted 15 genes in the beauvericin biosynthetic gene cluster of the B. bassiana genome dispersed across a total length of approximately 50kb. The beauvericin biosynthetic gene cluster contains beauvericin synthetase as well as kivr gene encoding NADPH-dependent ketoisovalerate reductase which is necessary to convert 2-ketoisovalarate to D-Hiv and a gene encoding a putative Gal4-like transcriptional regulator. Our syntenic comparison showed that species in Cordycipitaceae have almost conserved beauvericin biosynthetic gene cluster although the gene order and direction were sometimes variable. It is intriguing that there is no region orthologous to beauvericin synthetase gene in Cordyceps militaris genome. It is likely that beauvericin synthetase was present in common ancestor of Cordycipitaceae but selective gene loss has occurred in several species including C. militaris. Putative bassianolide biosynthetic gene cluster consisted of 16 genes including bassianolide synthetase, cytochrome P450 monooxygenase, and putative Gal4-like transcriptional regulator genes. Our synteny analysis found that only B. bassiana possessed a bassianolide synthetase gene among the studied fungi. This result is consistent with the groupings in A-domain tree in which bassianolide synthetase gene found in B. bassiana was not grouped with NRPS genes predicted in other species. We hypothesized that bassianolide biosynthesizing cluster genes in B. bassiana are possibly acquired by horizontal gene transfer (HGT) from distantly related fungi. The present study showed that B. bassiana is the only species capable of producing both beauvericin and bassianolide. This property led to B. bassiana infect multiple hosts and to be a potential biological control agent against agricultural pests.