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In vitro and in vivo Antibacterial Activities and Pharmacokinetics of 8-Fluorociprofloxacin and Ciprofloxacin (8-Fluorociprofloxacin과 Ciprofloxacin의 시험관내 및 생체내 항균효과와 약물동태의 비교)

  • 최경업;정용환;김제학
    • YAKHAK HOEJI
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    • v.37 no.3
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    • pp.235-242
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    • 1993
  • 8-Fluorociprofloxacin(8-FCP) is an investigational quinolone derivative that is substituted with fluorine at the C-8 position of ciprofloxacin(CP). It was found that the in vitro activity of 8-FCP against Gram(+) bacteria was more potent that of CP, but the opposite against Gram(-) bacteria was true. However, 8-FCP showed better in vivo efficacy than CP against representative Gram(-) organisms, E. coli and K pneumoniae. In an attempt to seek for factors causing this discrepancy in the antibacterial activities, a comparative pharmacokinetic study of 8-FCP and CP was conducted in mice and rats treated either intravenously or orally at a single dose of 30 mg/kg. The pharmacokinetic parameters in mice were as follows; the mean peak serum concentrations(C$_{max}$) following i.v. and oral doses were 12.4 and 5.3 $\mu\textrm{g}$/ml for 8-FCP, and 9.5 and 2.5 $\mu\textrm{g}$/ml for CP, respectively. The terminal half-life(t$_{1/2\beta}$) was 72.9 min for 8-FCP, and 98.2 min for CP, and the oral bioavailability(F) was 89.9% for 8-FCP, and 50.5% for CP. In rats, the mean ($\pm$SD) $C_{max}$ after i.v. administration were 11.6$\pm$1.6 $\mu\textrm{g}$/ml for 8-FCP, and 10.2$\pm$1.3 $\mu\textrm{g}$/ml for CP, whereas oral administration produced $C_{max}$ of 5.9$\pm$1.8 $\mu\textrm{g}$/ml for 8-FCP and 1.1$\pm$0.9 $\mu\textrm{g}$/ml for CP, respectively. The t$_{1/2\beta}$ was 67.9$\pm$8.4 min for 8-FCP, and 76.4$\pm$7.2 min for CP. The F was 88.6$\pm$6.3% for 8-FCP, and 40.7$\pm$6.5% for CP. Marked differences were observed between the two quinolones in the $C_{max}$ and the area under the concentration-time curve obtained after oral administration in mice and rats. The extent of 8-FCP absorption in both mice and rats was approximately 2-fold higher than that of CP, suggesting that the fluorine atom attached to C-8 plays an important role in facilitating oral absorption from the gastrointestinal tract.

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Structure-Activity Relationships of Polyhydroxyursane-type Triterpenoids on the Cytoprotective and Anti-inflammatory Effects

  • Jung, Hyun-Ju;Nam, Jung-Hwan;Lee, Kyung-Tae;Lee, Yong-Sup;Choi, Jong-Won;Kim, Won-Bae;Chung, Won-Yoon;Park, Kwang-Kyun;Park, Hee-Juhn
    • Natural Product Sciences
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    • v.13 no.1
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    • pp.33-39
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    • 2007
  • Eleven polyhydroxyursane triterpenoids (PHUTs) were tested to determine their cytoprotective, immunosuppressive and anti-inflammatory effects. To compare the bioactivities of $19{\alpha}$-hydroxyursane-type triterpenoids {23-hydroxytormentic acid (6), its methyl ester (7), tormentic acid (8), niga-ichigoside $F_1$ (9),euscaphic acid (10) and kaji-ichigoside $F_1$ (11)} of the Rosaceae crude drugs (Rubi Fructus and Rosa rugosae Radix) with PHUTs possessing no $19{\alpha}-hydroxyl$ of Centella asiatica (Umbelliferae), the four PHUTs, asiaticoside (1), madecassoside (2), asiatic acid (3), and madecassic acid (4) were isolated from C. asiatica and 23-hydroxyursolic acid (5) from Cussonia bancoensis. Cytoprotective effects were assessed by measuring cell viabilities against cisplatin-induced cytotoxocity in $LLC-PK_1$, cells (proximal tubule, pig kidney) to determine whether these agents have protective effects against nephrotoxicity caused by cisplatin. The inhibitory effect of 11 PHUTS on nitric oxide (NO) and prostaglandin $E_2\;(PGE_2)$ were evaluated by measuring nitrite accumulation in lipopolysaccharide (LPS)-induced macrophage RAW 264.7 cells, and their anti-inflammatory effects were tested in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model. Six MHUTs (compounds 1, 2, 4, 6, 10, and 11) exhibited higher cell viabilities during cisplatin-induced cytotoxicity testing even at a concentration of $200\;{\mu}g/ml$ than cisplatin only-treated group, suggesting that ese compounds have the potentcytoprotective efffcts. Compounds 1 and 3 of the C. asiatica and niga-ichigoside $F_1$ exhibited no inhibitory effect on NO and/or $PGE_2$ production whereas other PHUTs produced mild to significant NO and/or $PGE_2$ production.The four compounds (2, 5, 9, and 10) potently inhibited mouse ear edema induced by TPA whereas two compounds (1 and 3) had no activity in this test. These results suggest that many PHUTs are potentchemopreventives. Structure-activity relationship (SAR) was also discussed in each assay with regard to the significant role of OHs at the position of 2, 3, 6, 19, and 23 and to the glycoside linkage at the 28-carboxyl.

A Numerical Model to Evaluate Fire-Resistant Capacity of the Reinforced Concrete Members (화재에 손상된 철근콘크리트 부재의 수치모델 및 내화성능해석)

  • Hwang, Jin-Wook;Ha, Sang-Hee;Lee, Yong-Hoon;Kim, Wha-Jung;Kwak, Hyo-Gyoung
    • Journal of the Korea Concrete Institute
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    • v.25 no.5
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    • pp.497-508
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    • 2013
  • This paper introduces a numerical model which can evaluate the fire-resistant capacity of reinforced concrete members. On the basis of the transient heat transfer considering the heat conduction, convection and radiation, time-dependent temperature distribution across a section is determined. A layered fiber section method is adopted to consider non-linear material properties depending on the temperature and varying with the position of a fiber. Furthermore, effects of non-mechanical strains of each fiber like thermal expansion, transient strain and creep strain are reflected on the non-linear structural analysis to take into account the extreme temperature variation induced by the fire. Analysis results by the numerical model are compared with experimental data from the standard fire tests to validate an exactness of the introduced numerical model. Also, time-dependent changes in the resisting capacities of reinforced concrete members exposed to fire are investigated through the analyses and, the resisting capacities evaluated are compared with those determined by the design code.

Production Techniques for Mobile Motion Pictures base on Smart Phone (스마트폰 시장 확대에 따른 모바일 동영상 편집 기법 연구)

  • Choi, Eun-Young;Choi, Hun
    • The Journal of the Korea Contents Association
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    • v.10 no.5
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    • pp.115-123
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    • 2010
  • Because of development of information technology, moving picture can run various platforms. We should consider and apply users' attitude as well as production technique because convergence between mobile and media technology may be increased full-browsing service using mobile device. Previous research related to production technique in various platforms only focus on video quality and adjustment of screen size. However, besides of technical side, production techniques should be changed such as image production as well as image editing by point of view aesthetic. Mise-en-scene such as camera angle, composition, and lighting is changed due to HD image. Also image production should be changed to a suitable full-browsing service using mobile device. Therefore, we would explore a new suitable production techniques and image editing for smart phone. To propose production techniques for smart phone, we used E-learning production system, which are transition, editing technique for suitable converting system. Such as new attempts are leading to new paradigm and establishing their position by applying characteries such as openness, timeliness to mobile. Also it can be extended individual area and established as expression and play tool.

k-Nearest Neighbor Querv Processing using Approximate Indexing in Road Network Databases (도로 네트워크 데이타베이스에서 근사 색인을 이용한 k-최근접 질의 처리)

  • Lee, Sang-Chul;Kim, Sang-Wook
    • Journal of KIISE:Databases
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    • v.35 no.5
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    • pp.447-458
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    • 2008
  • In this paper, we address an efficient processing scheme for k-nearest neighbor queries to retrieve k static objects in road network databases. Existing methods cannot expect a query processing speed-up by index structures in road network databases, since it is impossible to build an index by the network distance, which cannot meet the triangular inequality requirement, essential for index creation, but only possible in a totally ordered set. Thus, these previous methods suffer from a serious performance degradation in query processing. Another method using pre-computed network distances also suffers from a serious storage overhead to maintain a huge amount of pre-computed network distances. To solve these performance and storage problems at the same time, this paper proposes a novel approach that creates an index for moving objects by approximating their network distances and efficiently processes k-nearest neighbor queries by means of the approximate index. For this approach, we proposed a systematic way of mapping each moving object on a road network into the corresponding absolute position in the m-dimensional space. To meet the triangular inequality this paper proposes a new notion of average network distance, and uses FastMap to map moving objects to their corresponding points in the m-dimensional space. After then, we present an approximate indexing algorithm to build an R*-tree, a multidimensional index, on the m-dimensional points of moving objects. The proposed scheme presents a query processing algorithm capable of efficiently evaluating k-nearest neighbor queries by finding k-nearest points (i.e., k-nearest moving objects) from the m-dimensional index. Finally, a variety of extensive experiments verifies the performance enhancement of the proposed approach by performing especially for the real-life road network databases.

cDNA Cloning and Polymorphism of the Porcine Carbonic Anhydrase III (CA3) Gene

  • Wu, J.;Deng, Changyan;Xiong, Y.Z.;Zhou, D.H.;Lei, M.G.;Zuo, B.;Li, F.E.;Wang, J.
    • Asian-Australasian Journal of Animal Sciences
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    • v.19 no.3
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    • pp.324-328
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    • 2006
  • Carbonic anhydrase III (CA3) is a member of a multigene family that encode carbonic anhydrase isozymes. In this study, a complete coding sequence of the pig CA3 gene which encodes a 260 amino-acid protein was determined. The amino acid comparison showed high sequence similarities with previously identified human (86.5%) CA3 gene and mouse (91.5%) Car3 gene. The partial genomic DNA sequences were also investigated. The length of intron 1 was 727 bp. Comparative sequencing of three pig breeds revealed that there was a T${\rightarrow}$C substitution at position 363 within intron 1. The substitution was situated within a NcoI recognition site and was developed as a PCR-restriction fragment length polymorphism (RFLP) marker for further use in population variation investigations and association analysis. Two alleles (A and B) were identified, and 617 bp fragments were observed for the AA genotype and 236 bp and 381 bp fragments for the BB genotype. The polymorphism of CA3 was detected in 8 pig breeds. Allele B was predominant in the Western pig breeds. In addition, association studies of the CA3 polymorphism with carcass traits in 140 $Yorkshire{\times}Meishan$ $F_2$ offspring showed that the NcoI PCR- RFLP genotype may be associated with variation in several carcass traits of interest for pig breeding. Allele B was associated with increases in lean meat percentage, loin eye height and loin eye area. Statistically significant association with backfat thickness was also found; pigs with the AB genotype had much less backfat thickness than AA or BB genotypes.

THE CHANGES OF MANDIBULAR MOVEMENT AND MUSCLE ACTIVITY FOLLOWING ORTHOGNATHIC SURGERY IN PATIENTS WITH MANDIBULAR PROGNATHISM (골격성 III급 부정 교합을 동반한 악교정수술 환자에서 수술 전후의 하악기능 변화에 관한 실험적 연구)

  • Lee, Hyung Sik;Park, Young Chel
    • The korean journal of orthodontics
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    • v.22 no.1
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    • pp.67-88
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    • 1992
  • The purpose of this study was to investigate the changes of mandibular movement and muscle activity following orthognathic surgery in patients with mandibular prognathism. Lateral cephalogram, M.K.G., E.M.G. recordings were obtained immediately before surgery, and 2 months and 8 months after surgery. Among the patients who received orthognathic surgery, 19(13 men, 6 women) were selected for this study. Statistical analysis for each time interval differences were performed with the SPSS package. The results were as follows: 1. Compared with the pre-operative group (opening 349.7mm/sec, closing 313.1mm/sec), the mean values of the maximum opening and closing velocity in the skeletal Class III surgery group were significantly decreased in the 2 months post-operative (opening 232.9mm/sec, closing 206.9mm/sec), but the values tended to increase in the 8 months post-operative group (opening 280.9 mm/sec, closing 319.1mm/sec). 2. Compared with the pre-operative group (61.7 mm/sec), the maximum velocity of the terminal tooth contact increased in the 2 months (72mm/sec) and 8 months (105.7mm/sec) postoperative groups. 3. In the mean value of vertical freeway space, there was significant difference between the normal group and the pre-operative group, but not between the normal group and the 8 months post-operative group. 4. In the mean values of the maximum opening, the maximum anterio-posterior movement from centric-occlusion, and the lateral deviation from centric occlusion, there was no significant difference between the normal group and the surgery group (the pre-operative and the 8 months post-operative groups). 5. The mature swallowing pattern was 58% in the pre-operative group, but 90% in the 2 months post-operative group, and 63% in the 8 months post-operative group. 6. In the comparison of muscle activity, there was no significant difference between the normal group and the surgery group during the rest position. However, during cotton roll clenching, there was significant difference between the normal group and the pre-operative group, but not between the normal group and the 8 months post-operative group.

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Accuracy of linear measurement using cone-beam computed tomography at different reconstruction angles

  • Nikneshan, Sima;Aval, Shadi Hamidi;Bakhshalian, Neema;Shahab, Shahriyar;Mohammadpour, Mahdis;Sarikhani, Soodeh
    • Imaging Science in Dentistry
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    • v.44 no.4
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    • pp.257-262
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    • 2014
  • Purpose: This study was performed to evaluate the effect of changing the orientation of a reconstructed image on the accuracy of linear measurements using cone-beam computed tomography (CBCT). Materials and Methods: Forty-two titanium pins were inserted in seven dry sheep mandibles. The length of these pins was measured using a digital caliper with readability of 0.01 mm. Mandibles were radiographed using a CBCT device. When the CBCT images were reconstructed, the orientation of slices was adjusted to parallel (i.e., $0^{\circ}$), $+10^{\circ}$, $+12^{\circ}$, $-12^{\circ}$, and $-10^{\circ}$ with respect to the occlusal plane. The length of the pins was measured by three radiologists, and the accuracy of these measurements was reported using descriptive statistics and one-way analysis of variance (ANOVA); p<0.05 was considered statistically significant. Results: The differences in radiographic measurements ranged from -0.64 to +0.06 at the orientation of $-12^{\circ}$, -0.66 to -0.11 at $-10^{\circ}$, -0.51 to +0.19 at $0^{\circ}$, -0.64 to +0.08 at $+10^{\circ}$, and -0.64 to +0.1 at $+12^{\circ}$. The mean absolute values of the errors were greater at negative orientations than at the parallel position or at positive orientations. The observers underestimated most of the variables by 0.5-0.1 mm (83.6%). In the second set of observations, the reproducibility at all orientations was greater than 0.9. Conclusion: Changing the slice orientation in the range of $-12^{\circ}$ to $+12^{\circ}$ reduced the accuracy of linear measurements obtained using CBCT. However, the error value was smaller than 0.5 mm and was, therefore, clinically acceptable.

2, 4, 5-Trichlorophenoxyacetic Acid 분해균의 유전적 특성에 관한 연구

  • Yoon, So-Yeong;Son, Hong-Joo;Lee, Geon;Lee, Sang-Joon;Lee, Jong-Kun
    • Korean Journal of Microbiology
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    • v.30 no.4
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    • pp.260-264
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    • 1992
  • Pseudotnorju.c sp. EL-071P degrading 2.4.5-trichlorophe~~oxyi~cetaicci d (2.3.5-T) was resistantto antibiotics: rifampicin. ampicillin. kanamycin and metal ions : Zn" and Cu".The plasmitl related to the degradation of 2.4.5-'r and rifa~npicin resistance was isolatecifrom the strain. Its size was about 40 Kb. As result of transforming the plasmid intoEsch~rirhiti coli MClOhl, it was confirmed that the plasmid ura.; related to 2.4.5-T degradation.The strain coulil grow in the various chlorinated aromatic analogs as the solc carbon source.In the case of chlorophcnols. the chlorinated mono-substituteti phenols were easily dcgradetlin the order ol' ortho-. ~ ~ a r um- ,c ~tu-position.T he 2.3.5-T mctaholism was inhibited by 4-chlorophenol of 2.4.5-7' analog. In non-chlorinateci aromatics. ~ C I I L O ~ I ~ Csa.l icylilte i~ndtoluene were uscd ax the carbon source by the strain and typestrain Acudonlotrtr.\ plrtirltrKCTC 1643 having clegrad;~bility of various aromatics. But naphtalene was usecl only bythe A~urlomonri.\ sp. EL-07 1 P.the A~urlomonri.\ sp. EL-07 1 P.

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Effects of Biological and Environmental Factors on the Occurrence of Chestnut Blight in Chestnut Tree Plantations (밤나무 재배지에서의 생물적, 환경적 요인이 밤나무 줄기마름병 발생에 미치는 영향)

  • Lee, Sang-Hyun;Kim, Kyung-Hee;Byun, Jae-Kyung;Lee, Jong Kyu;Moon, Byung-Ju
    • Journal of Korean Society of Forest Science
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    • v.95 no.1
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    • pp.139-144
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    • 2006
  • Chestnut trees have been severely damaged by the various cankers in Korea. Field surveys for elucidating the relationships between disease occurrence and environmental factors, i.e., tree age, temperature, rainfall precipitation, direction, degree of slope, chemical properties of soils, and so on, were carried out in the chestnut tree plantations located at Gyeongnam, Jeonnam, Chungnam, and Gyeonggi-Do Province. Totally, one thousand and one hundred thirty seven trees from 36 experiment plots were investigated. Trees infected by at least one of the canker fungi were estimated up to 66%. The most severely infested area was Sunchon in Jeonnam Province with the rate of 80%, while the most lightly infested area was Kongju in Chungnam Province with 39%. Disease occurrence was found to be highly correlated with tree age. The disease occurred most frequently on trees ranged from 7 to 12 years old, while it was relatively low on trees below 5 years old or above 25 years old. Canker positions on the tree formed by the pathogenic fungi were most often at 1.6-2.0m above the ground. Over five hundreds bark samples from the canker area on the tree were collected and the pathogenic fungi were isolated. The most commonly isolated fungus was identified as Cryphonectria parasitica, the chestnut blight fungus.