• Title/Summary/Keyword: Colchicine

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Cytotoxic Activity and Three-Dimensional Quantitative Structure Activity Relationship of 2-Aryl-1,8-naphthyridin-4-ones

  • Kim, Yong-Jin;Kim, Eun-Ae;Chung, Mi-Lyang;Im, Chae-Uk
    • The Korean Journal of Physiology and Pharmacology
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    • v.13 no.6
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    • pp.511-516
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    • 2009
  • A series of substituted 2-arylnaphthyridin-4-one analogues, which were previously synthesized in our laboratory, were evaluated for their in vitro cytotoxic activity against human lung cancer A549 and human renal cancer Caki-2 cells using MTT assay. Some compounds (11, 12, and 13) showed stronger cytotoxicity than colchicine against both tumor cell lines, and compound 13 exhibited the most potent activity with $IC_{50}$ values of 2.3 and $13.4\;{\mu}M$, respectively. Three-dimensional quantitative structure activity relationship (3D-QSAR) studies of comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were performed. Predictive 3D-QSAR models were obtained with $q^2$ values of 0.869 and 0.872 and $r^2_{ncv}$ values of 0.983 and 0.993 for CoMFA and CoMSIA, respectively. These results demonstrate that CoMFA and CoMSIA models could be reliably used in the design of novel cytotoxic agents.

Staurosporine Induces ROS-Mediated Process Formation in Human Gingival Fibroblasts and Rat Cortical Astrocytes

  • Lee, Han Gil;Kim, Du Sik;Moon, Seong Ah;Kang, Jeong Wan;Seo, Jeong Taeg
    • International Journal of Oral Biology
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    • v.40 no.1
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    • pp.27-33
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    • 2015
  • In the present study, we investigated the effect of staurosporine on the formation of cellular processes in human gingival fibroblasts and rat astrocytes. Staurosporine caused a rapid induction of process formation in human gingival fibroblasts and rat astrocytes in a concentration dependent manner. The process formation of human gingival fibroblasts and rat astrocytes was prevented by the pretreatment with N-acetylcysteine, suggesting that staurosporine-induced ROS production was responsible for the process formation. Colchicine, a microtubule depolymerizing agent, inhibited the staurosporine-induced process formation, whereas cytochalasin D, an actin filament breakdown agent, failed to suppress the formation of cellular processes. This result indicated that polymerization of microtubule, and not actin filament, was responsible for the formation of cellular processes induced by staurosporine. In support of this hypothesis, Western blot analysis was conducted using anti-tubulin antibody, and the results showed that the amount of polymerized microtubule was increased by the treatment with staurosporine while that of depolymerized beta-tubulin in soluble fraction was decreased. These results indicate that staurosporine induces ROS-mediated, microtubule-dependent formation of cellular processes in human gingival fibroblasts and rat astrocytes.

Characteristic as a Gene Delivery System of Water Soluble Chitosan Conjugated with Cationic Peptide (양이온 펩타이드가 컨쥬게이트된 수용성 키토산의 유전자 전달체로서의 특성)

  • Kim, Young-Min;Kim, Ji-Ho;Park, Seong-Cheol;Park, Yung-Hoon;Jang, Mi-Kyeong
    • KSBB Journal
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    • v.31 no.4
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    • pp.300-311
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    • 2016
  • Recently gene delivery has been designed newly using bioactive biomaterial and applied in the various field by many researchers. In this study, we proposed a new gene delivery system which has the capability of targeting effect in the specific tissue and remarkably enhanced transfection efficiency. We investigated $^1H-NMR$ spectroscopy, particle size analyzer and gel retardation to confirm the correct preparation of gene delivery. Also, we identified the hemo-compatibility of gene delivery by hemolysis assay, non-cytotoxicity by MTT test and transfection efficiency. The uptake mechanism of the gene carrier was confirmed using inhibitor agent such as sodium azide, indomethacin, quercetin, colchicine, and chloropromazine. As a results, it was identified that gene carrier prepared by in this study entered in the cell by the microtubule-dependent, energy-dependent and clathrin-mediated endocytosis pathway.

The Study on Scattering of Chromosomes in Cells -Scattering of Chromsomes by Treatment with Potassium Ferricyanide Solution under Light- (세포내 염색체의 분산에 관한 연구 -적혈염용액의 광조사 처리에 의한 염색체의 분산-)

  • 김종호
    • Journal of Plant Biology
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    • v.17 no.3
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    • pp.113-117
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    • 1974
  • In counting chromosome number and karyotype study, it is necessary to let chromosomes on metaphase by pretreatment before fixation. For this purpose, colchicine, or 8-oxyquinoline are generally used. The author found out that chromosomes could be scattered by illuminating cyanoferrate complex solution in which root-tips were sunk. As materials, 8 sorts of plant such as Allium fisturosum, allium tuberosum Rottler, Triticum vulgare were used. Their root-tips were sunk on the bottom of beaker in potassium ferricyanide solution $3{\times}10-4M$ and illuminated through the solution by sterilizing lamp for 1~2 hours in dark room, keeping 10 cm distance from light source to the surface of solution and 2cm depth of solution. Then again, they were illuminated to the light which was somewhat weaker intensity than the former (distance, 16cm; depth, 3cm) for 1.5~2 hours after immersed in 1/100N-HCl and washed in water for each 5minutes. By such methods chromosomes could be scattered. About the mechanism of scattering, it is supposed that CN and Fe(CN)x ions $(x {\leq}5)$ which were gradually produced in the process of photodissociation acted together on the scattering of chromosomes.

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Changes on the Methylmercury-induced Cytotoxicity by Control of Cell Membrane Transport System (세포막 물질수송계의 조절에 의한 유기수은의 세포독성 변화에 대한 연구)

  • 염정호;고대하;김준연;김남송
    • Journal of Environmental Health Sciences
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    • v.26 no.4
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    • pp.88-96
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    • 2000
  • The aim of the current study was to evaluate the transport system in EMT-6 cell for the uptake of the methylmercury(MeHg). Several inhibitors ere used to test used to test which potential transport system might be involoved in MeHg uptake. Probenecid was used to test the organic transport system, valinomycin for testing the effect of the membrane potential, cytochalasin B for testing the facilitated diffusive D-glucose transport system and colchicine for testing the microtubule system. Ouabain for evaluating active transport system, 4',4-diisothiocyano-2',2-stilbenedisulfonic acid(DIDS) the Cl- ion transport system and verapamil for the $Ca^{2+}$ transprot system. Significantly, MeHg decreased the synthesis of nitric oxcide(NO) and intracellular ATP in ENT-6 cells. In the condition of ouabain containing with MeHg decreased the production of NO and intracelluar ATP. In the treatment of inhibitors, ouabain showed protective effect against cytotoxicity of MeHg but ather inhibitors not showed protective effects. The protective effects of ouabain against the cytotoxicity of MeHg deoended on the concentration of added ouabain to the culture medium for MET-6 cells. These result showed that the uptake of MeHg might be involved in the active transport system. Active transports system seems to share similarities with the transport systems for the uptake of MeHg when using MeHg and MeHg-glutathione complex.x.

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Studies on the Intergeneric Hybridization in the Triticale II. Newly Established Primary Winter Octaploid Triticale by Intergeneric Hybrid between T. aestivum L. and S. cereale L. (맥류의 속간교잡에 관한 연구 II. 밀과 호밀의 속간교잡에 의한 추도형 8배체 Primary Triticale 육성)

  • Cho, C.H.;Ahn, W.S.;Kim, M.J.;Kim, B.Y.
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.23 no.1
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    • pp.21-25
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    • 1978
  • Primary triticale was newly established by colchicine treatment of intergeneric hybrid F 1 plants crossed between T. aestivum var. Jugoku #81 and S. cereale var. Jaelae. The agronomic and cytological characteristics were studied.

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Studies on a Tetraploid of Robinia pseudoacacia L. Selected in the Planted Forest (조림지(造林地)에서 선발(選拔)한 자연(自然) 4배체(倍體) 아까시나무(Robinia pseudoacacia L.)에 관(關)한 연구(硏究))

  • Kim, Chung Suk;Lee, Suk Koo
    • Journal of Korean Society of Forest Science
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    • v.14 no.1
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    • pp.39-44
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    • 1972
  • Cytological investigation was done on a tetraploid tree of Robinia pseudoacacia L. selected in the planted forest in Chilbo Mountain. From the results of observation of chromosomes on mitotic metaphase in leaves, it was confirmed that the mutant is tetraploid plant (2n=40). The external form of leaves of the spontaneous tetraploid was gigantic and dark green one in comparison with diploid. There was no difference in the size of guard cell and the number of stomata per unit area between the mutant and the diploid plant, however, length and thickness of wood fiber were increased as compared with that of diploid. The spontaneous gigas tetraploid showed growth performance as much as the colchicine induced gigas tetraploid.

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Cytotoxicity and Structure-activity Relationships of Naphthyridine Derivatives in Human Cervical Cancer, Leukemia, and Prostate Cancer

  • Hwang, Yu Jin;Chung, Mi Lyang;Sohn, Uy Dong;Im, Chaeuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.6
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    • pp.517-523
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    • 2013
  • Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These compounds have been investigated as potential anticancer agents, and several compounds are now part of clinical trials. A series of naphthyridine derivatives were evaluated for their in vitro cytotoxic activities against human cervical cancer (HeLa), leukemia (HL-60), and prostate cancer (PC-3) cell lines using an MTT assay. Some compounds (14, 15, and 16) were more potent than colchicine against all three human cancer cell lines and compound (16) demonstrated potency with $IC_{50}$ values of 0.7, 0.1, and $5.1{\mu}M$, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used for quantitative structure-activity relationship (QSAR) molecular modeling of these compounds. We obtained accurate and predictive three-dimensional QSAR (3D-QSAR) models as indicated by the high PLS parameters of the HeLa ($q^2$, 0.857; $r^2$, 0.984; $r^2\;_{pred}$, 0.966), HL-60 ($q^2$, 0.777; $q^2$, 0.937; $r^2\;_{pred}$, 0.913), and PC-3 ($q^2$, 0.702; $q^2$, 0.983; $r^2\;_{pred}$, 0.974) cell lines. The 3D-QSAR contour maps suggested that the C-1 NH and C-4 carbonyl group of the naphthyridine ring and the C-2 naphthyl ring were important for cytotoxicity in all three human cancer cell lines.

Evaluation of using veliger stage larvae for the preparation of metaphase spreads from the pacific abalone (Haliotis discus hannai)

  • Choi, Jae Hoon;Kim, Eun Jeong;Park, Choul-Ji;Nam, Yoon Kwon;Gong, Seung Pyo
    • Journal of Animal Reproduction and Biotechnology
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    • v.35 no.3
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    • pp.223-231
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    • 2020
  • Karyotype analysis is a major work in the process of triploid abalone production for the purpose of productivity and quality improvement. However, the metaphase spreads for karyotype analysis have been prepared just from the larvae at trochophore stage, which has restricted the spectrum of sample correction inhibiting more efficient analysis. Here, we investigated the feasibility of preparing metaphase spreads from the larvae at veliger stage that is the next developmental stage of trochophore. For this, diploid and triploid larvae at trochophore and veliger stages from Pacific abalone (Haliotis discus hannai) were subjected to metaphase spread preparation and its efficiencies were measured and compared each other. As the results, although the efficiencies of metaphase spread preparation were significantly lower in the larvae at veliger stage compared to the ones at trochophore stage regardless of ploidy status, we found that the preparation of metaphase spreads, which showed the clear chromosomal images containing the normal number of chromosomes, was possible from the veliger stage larvae. On the other hands, all larvae used in this study regardless of developmental stage and ploidy did not show colchicine sensitivity. Moreover, no significant difference was observed in cell cycle distribution of the cells comprising larvae between two developmental stages regardless of ploidy status. These suggested that the details of protocol to prepare metaphase spreads from abalone larvae should be optimized depending on its developmental stages. Taken together, we demonstrated the feasibility of preparing metaphase spreads from H. discus hannai veliger stage larvae for karyotype analysis.

Endoscopic Findings of Children with Familial Mediterranean Fever

  • Sag, Elif;Demir, Ferhat;Saygin, Ismail;Kalyoncu, Mukaddes;Cakir, Murat
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • v.21 no.4
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    • pp.271-277
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    • 2018
  • Purpose: Familial Mediterranean fever (FMF) is an auto inflammatory disease characterized by periodic fever, synovitis and serositis. Patients may be admitted to gastroenterology units due to gastrointestinal symptoms. In this study; we aimed to analyze endoscopic findings and diagnostic utility of endoscopic procedure in children with FMF. Methods: Patient with FMF that was performed endoscopy for the gastrointestinal symptoms were included to the study (39 of 164 patients, 53 procedure). A control group was randomly designed as age and gender matched four endoscopic procedures per one endoscopic procedure of patients with FMF (n=212). Results: No different was found between the patients and control group in esophagogastroscopy findings. However, the diagnosis of gastrointestinal pathology was made by esophagogastroscopy in 46.2% patients. Colonoscopic examination revealed that the frequency of inflammatory bowel disease (IBD) was higher in undiagnosed patients compared to both the control group (50.0% vs. 6.9%, p<0.05, odds ratio [OR]:13.4 and 95% confidence inteval [95% CI]: 2.1-84.3) and the patients under colchicine treatment (50.0% vs. 8.3%, p<0.05, OR: 11 and 95% CI: 0.8-147.8). Colonoscopic procedure that was made after the diagnosis was found to provide contribution by 16.7% in determining the etiology of the additional symptoms. Conclusion: Patients with FMF may be admitted to pediatric gastroenterology outpatient clinic prior to diagnosis or during the follow-up period. The frequency of IBD is high in undiagnosed patients with FMF. Endoscopic procedures may be helpful in these patients for the diagnosis accompanying mucosal lesions.