• Title/Summary/Keyword: blocking effect

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ANTI-TUMOR EFFECTS OF VASCULAR ENDOTHELIAL GROWTH FACTOR INHIBITOR ON ORAL SQUAMOUS CELL CARCINOMA CELL LINES (혈관내피세포성장인자 억제제에 의한 구강편평상피세포암종 세포주의 성장 억제 효과)

  • Han, Se-Jin;Lee, Jae-Hoon
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.35 no.2
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    • pp.66-73
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    • 2009
  • Tumor angiogenesis is a process leading to formation of blood vessels within tumors and is crucial for maintaining a supply of oxygen and nutrients to support tumor growth and metastasis. Vascular endothelial growth factor(VEGF) plays a key role in tumor angiogenesis including induction of endothelial cell proliferation, migration, survival and capillary tube formation. VEGF binds to two distinct receptors on endothelial cells. VEGFR-2 is considered to be the dominant signaling receptor for endothelial cell permeability, proliferation, and differentiation. Bevacizumab(Avastin, Genetech, USA) is a monoclonal antibody against vascular endothelial growth factor. It is used in the treatment of cancer, where it inhibits tumor growth by blocking the formation of new blood vessels. The goal of this study is to identify the anti-tumor effect of Bevacizumab(Avastin) for oral squamous cell carcinoma cell lines. Human squamous cell carcinoma cell line(HN4) was used in this study. We examined the sensitivity of HN4 cell line to Bevacizumab(Avastin) by using in vitro proliferation assays. The results were as follows. 1. In the result of MTT assay according to concentration of Bevacizumab(Avastin), antiproliferative effect for oral squamous cell carcinoma cell lines was observed. 2. The growth curve of cell line showed the gradual growth inhibition of oral squamous cell carcinoma cell lines after exposure of Bevacizumab(Avastin). 3. In the apoptotic index, groups inoculated Bevacizumab(Avastin) were higher than control groups. 4. In condition of serum starvation, VEGFR-2 did not show any detectable autophosphorylation, whereas the addition of VEGF activated the receptor. Suppression of phosphorylated VEGFR-2 and phosphorylated MAPK was observed following treatment with Bevacizumab(Avastin) in a dose-dependent manner. 5. In TEM view, dispersed nuclear membrane, scattered many cytoplasmic vacuoles and localized chromosomal margination after Bevacizumab(Avastin) treatment were observed. These findings suggest that Bevacizumab(Avastin) has the potential to inhibit MAPK pathway in proliferation of oral squamous cell carcinoma cell lines via inhibition of VEGF-dependent tumor growth.

The Effect of Three kinds of Coptis Rhizoma on the Contraction of Isolated Rat Tracheal Smooth Muscle (삼종(三種) 황연류(黃連類)의 기관지(氣管支) 평활근(平滑筋) 이완효과(弛緩效果)에 관(關)한 연구(硏究))

  • Suh, Young-Chel;Lim, Seong-Woo;Shin, Gil-Cho;Lee, Won-Chul
    • Korean Journal of Oriental Medicine
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    • v.2 no.1
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    • pp.236-254
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    • 1996
  • This study was carried out to investigate the tracheal muscle relaxation of water extracts of three kinds of Coptis rhizoma and also compare their effects with berberine and palmatine, which are the important alkaloid components of Coptis rhizoma, in isolated rat tracheal smooth muscle. As a result Coptis chinenis showed significant tracheal muscle relaxation on KCI-induced contraction and more markedly on carbachol-induced contraction in dose-dependent manner. Coptis japoinin exhibited also tracheal muscle relaxation on both contraction with slightly weaker activities than those of Coptis chinensts. The activities of the root hair of Coptis chinensis were the most weakest in three rhizomas. Berberine and palmatine had strong tracheal muscle relaxation, especially, on carbachol-induced contraction, however, their activities on KCI-induced contraction were weaker than that of Coptis chinenis. The inhibitory effects of three kinds of Coptis rhizoma on the contraction by KCI and carbachol were investigated to explain the process of their tracheal muscle relaxation. All rhizomas inhibited the contraction by both agents, among them, Coptis japonica showed the most significant effect, so indicating that the tracheal muscle relaxation of Coptis rhizoma may be concerned with the blocking of muscarine receptor and $Ca^{2+}$channel.

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3',4',5',5,7-Pentamethoxyflavone Sensitizes Cisplatin-Resistant A549 Cells to Cisplatin by Inhibition of Nrf2 Pathway

  • Hou, Xiangyu;Bai, Xupeng;Gou, Xiaoli;Zeng, Hang;Xia, Chen;Zhuang, Wei;Chen, Xinmeng;Zhao, Zhongxiang;Huang, Min;Jin, Jing
    • Molecules and Cells
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    • v.38 no.5
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    • pp.396-401
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    • 2015
  • Nuclear factor erythroid 2-related factor 2 (Nrf2) is an important redox-sensitive transcription factor that regulates the expression of several cytoprotective genes. More recently, genetic analyses of human tumors have indicated that Nrf2 may cause resistance to chemotherapy. In this study, we found that the expression levels of Nrf2 and its target genes GCLC, HO-1, NQO1 were significantly higher in cisplatin-resistant A549 (A549/CDDP) cells than those in A549 cells, and this resistance was partially reversed by Nrf2 siRNA. 3,4,5,5,7-Pentamethoxyflavone (PMF), a natural flavon extracted from Rutaceae plants, sensitized A549/CDDP to CDDP and substantially induced apoptosis compared with that of CDDP alone treated group, and this reversal effect decreased when Nrf2 was downregulated by siRNA. Mechanistically, PMF reduced Nrf2 expression leading to a reduction of Nrf2 downstream genes, and in contrast, this effect was decreased by blocking Nrf2 with siRNA. Taken together, these results demonstrated that PMF could be used as an effective adjuvant sensitizer to increase the efficacy of chemotherapeutic drugs by downregulating Nrf2 signaling pathway.

A Spectrum Sharing Model for Compatibility between IMT-Advanced and Digital Broadcasting

  • Hassan, Walid A.;Rahman, Tharek Abd
    • KSII Transactions on Internet and Information Systems (TIIS)
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    • v.6 no.9
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    • pp.2073-2085
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    • 2012
  • Recently, the International Telecommunication Union allocated the 470-862 MHz band to the digital broadcasting (DB) service. Moreover, the 790-862 MHz sub-band will be allocated to the next-generation mobile system, known as the International Mobile Telecommunication - Advanced (IMT-A), and to the DB on a co-primary basis in the year 2015. Currently, two candidate technologies are available to represent the IMT-A system; the Mobile WiMAX and Long Term Evolution - Advanced (LTE-A). One of the main criteria of the IMT-A candidate is to not cause additional interference to the primary service (i.e., DB). In this paper, we address the spectrum sharing issue between the IMT-A candidates and the DB service. More precisely, we investigate the interference effect between the DB service and the mobile network, which could be either LTE-A or WiMAX. Our study proposes a spectrum sharing model to take into account the impact of interference and evaluates the spectrum sharing requirements such as frequency separation and separation distance. This model considers three spectrum sharing scenarios: co-channel, zero guard band, and adjacent channel. A statistical analysis is performed, by considering the interferer spectrum emission mask and victim receiver blocking techniques. The interference-to-noise ratio is used as an essential spectrum sharing criterion between the systems. The model considers the random distribution of the users, antenna heights, and the bandwidth effect as well as the deployment environment in order to achieve spectrum sharing. The results show that LTE-A is preferable to WiMAX in terms of having less interference impact on DB; this can eventually allow the operation of both services without performance degradation and thus will lead to efficient utilization of the radio spectrum.

Anti-inflammatory Effect of Dangyuja (Citrus grandis Osbeck) Leaves in LPS-stimulated RAW 264.7 Cells

  • Yang, Eun-Jin;Lee, Hye-Ja;Kang, Gyeoung-Jin;Park, Sun-Soon;Yoon, Weon-Jong;Kang, Hee-Kyoung;Cho, So-Mi Kim;Yoo, Eun-Sook
    • Food Science and Biotechnology
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    • v.18 no.5
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    • pp.1063-1070
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    • 2009
  • Dangyuja (Citrus grandis Osbeck) is a native plant growing only on Jeju Island in Korea. In this study, antiinflammatory effect of dangyuja leaves on a murine macrophage cell line was investigated. RAW 264.7 murine macrophage cells were stimulated with lipopolysaccharide (LPS, $1{\mu}g/mL$) to induce expression of pro-inflammatory markers [interleukin (IL)-6 and inducible nitric oxide synthase (iNOS)]. The crude extract (80% MeOH Ex.) and solvent fractions (hexane, $CHCl_3$, EtOAc, BuOH, and $H_2O$ Ex.) were obtained from dangyuja leaves. The $CHCl_3$ fraction inhibited the nitric oxide (NO) and IL-6 production in a dose-dependent manner. Also, the $CHCl_3$ fraction inhibited mRNA expression and protein levels of iNOS in a dose-dependent manner. Furthermore, the $CHCl_3$ fraction inhibited LPS-induced nuclear factor (NF)-${\kappa}B$ activation and phosphorylation of mitogen-activated protein kinases (MAPKs: ERK, JNK, and p38). These results suggest that dangyuja leaves may inhibit LPS-induced production of inflammatory markers by blocking NF-${\kappa}B$ and MAPKs signaling in RAW 264.7 cells.

A Study on the Effect of Cooperative Computer-Assisted Instruction by Previous Achievement Level (사전 성취 수준에 따른 협동적 컴퓨터 보조 수업의 효과)

  • No, Tae-Hui;Cha, Jeong-Ho;Yun, Seon-Ae;Gang, Seok-Jin
    • Journal of the Korean Chemical Society
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    • v.46 no.4
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    • pp.377-384
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    • 2002
  • In this study, the effect of cooperative computer-assisted instruction upon students' conceptual under-standing,application ability, and learning motivation were investigated by a previous achievement level. The treatment and the control groups (2 classes) were selected from a middle school in Seoul, and taught about the motion of molecule for 5 class periods. Prior to the instructions, a learning motivation test was administered and used as covariate. The scores of a previous achievement test were also used as covariate. The scores of the mid-term science examination were used as blocking variable. After the instructions, the conceptions test, the application test, and the learning motivation test were administered. Two-way ANCOVA results revealed that there were no significant differences in the scores of the con-ceptions test and the application test. However, the scores of the treatment group were found to be significantly higher than those of the control group in the learning motivation test.

Propyl Gallate Inhibits Adipogenesis by Stimulating Extracellular Signal-Related Kinases in Human Adipose Tissue-Derived Mesenchymal Stem Cells

  • Lee, Jeung-Eun;Kim, Jung-Min;Jang, Hyun-Jun;Lim, Se-Young;Choi, Seon-Jeong;Lee, Nan-Hee;Suh, Pann-Ghill;Choi, Ung-Kyu
    • Molecules and Cells
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    • v.38 no.4
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    • pp.336-342
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    • 2015
  • Propyl gallate (PG) used as an additive in various foods has antioxidant and anti-inflammatory effects. Although the functional roles of PG in various cell types are well characterized, it is unknown whether PG has effect on stem cell differentiation. In this study, we demonstrated that PG could inhibit adipogenic differentiation in human adipose tissue-derived mesenchymal stem cells (hAMSCs) by decreasing the accumulation of intracellular lipid droplets. In addition, PG significantly reduced the expression of adipocyte-specific markers including peroxisome proliferator-activated receptor-${\gamma}$ (PPAR-${\gamma}$), CCAAT enhancer binding protein-${\alpha}$ (C/EBP-${\alpha}$), lipoprotein lipase (LPL), and adipocyte fatty acid-binding protein 2 (aP2). PG inhibited adipogenesis in hAMSCs through extracellular regulated kinase (ERK) pathway. Decreased adipogenesis following PG treatment was recovered in response to ERK blocking. Taken together, these results suggest a novel effect of PG on adipocyte differentiation in hAMSCs, supporting a negative role of ERK1/2 pathway in adipogenic differentiation.

Artemisia fukudo essential oil attenuates LPS-induced inflammation by suppressing NF-${\kappa}B$ and MAPK activation in RAW 264.7 cells

  • Yoon, Weon-Jong
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2010.10a
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    • pp.13-13
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    • 2010
  • In the present study, the chemical constituents of Artemisia fukudo essential oil (AFE) were investigated using GC-MS. The major constituents were ${\alpha}$-thujone (40.28%), ${\beta}$-thujone (12.69%), camphor (6.95%) and caryophyllene (6.01%). We also examined the effects of AFE on the production of nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$), tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-IL-$1{\beta}$ (IL-$1{\beta}$), and IL-6 in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Western blotting and RT-PCR analyses indicated that AFE has potent dose-dependent inhibitory effects on pro-inflammatory cytokines and mediators. We investigated the mechanism by which AFE inhibits NO and $PGE_2$ by examining the level of nuclear factor-${\kappa}B$ (NF-${\kappa}B$: p50 and p65) activation within the mitogen-activated protein kinase (MAPK: ERK, JNK and p38) pathway, which is an inflammation induced signal pathway in RAW 264.7 cells. AFE inhibited LPS-induced ERK, JNK and p38 phosphorylation. Furthermore, AFE inhibited the LPS-induced phosphorylation and degradation of $I{\kappa}B-{\alpha}$, which is required for the nuclear translocations of the p50 and p65 NF-${\kappa}B$ subunits in RAW 264.7 cells. Our results suggest that AFE might exert an anti-inflammatory effect by inhibiting the expression of pro-inflammatory cytokines. Such an effect is mediated by a blocking of NF-${\kappa}B$ activation which consequently inhibits the generation of inflammatory mediators in RAW 264.7 cells. AFE may be useful for treating inflammatory diseases.

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Effect of DPBll Gene for the Transcriptional Induction by DNA Damage During Cell Cycle in Saccharomyces cerevisiae (출아효모의 세포주기동안 DNA 상해에 의한 발현 유도에 미치는 DPB11 유전자의 영향)

  • 선우양일;임선희;배호정;김중현;김은아;김승일;김수현;박정은;김재우
    • Korean Journal of Microbiology
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    • v.38 no.2
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    • pp.96-102
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    • 2002
  • The S-phase checkpoint mechanisms response to DNA damage or inhibition of DNA replication for maintenance of genetic stability in eukaryotic cells. These roles include cell cycle control arrest at S-phase and Iranscriptional induction of repair genes. To characterize the defects of dpbll mutant for both these responses, we examined the over-expression effect of DPBll gene, the sensitivity to HU, MMS, and the transcriptional pattern by DNA damage agent for RNRS mRNA. RNRS transcript is induced in response to a wide variety of agents that either damage D7A directly through chemical modification or induce stress by blocking DNA synthesis. As results, dpbll-1 cells are sensitive to DNA damage agents and the level of RNR3 mRNA is reduced approximately 40% than wild type cells. Moreover, we found the same results in dpb2-1 cells. Therefore, we propose that DPB2 and DPBll act as a sensor of replication that coordinates the transcriptional and cell cycle responses to replication blocks.

Cimicifugoside Inhibits Catecholamine secretion by blocking Nicotinic Acetylcholine Receptor in Bovine Adrenal Chromaffin cell.

  • Woo, Kyung-Chul;Park, Yong-Su;Suh, Byung-Sun;Kim, Kyong-Tai
    • Proceedings of the Korean Biophysical Society Conference
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    • 2003.06a
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    • pp.51-51
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    • 2003
  • The medicinal plant Cimicifuga Racemosa (Black cohosh) has been used to treat many kinds of neuronal and menopausal symptoms, such as arthritis, menopausal depression, nerve pain, etc. Here, we examined the effect of Cimicifugoside (CF), one of triterpene glycosides which have been known as pharmacologically active ingredients of C. Racemosa, on nicotinic acetylcholine receptor (nAChR)-mediated catecholamine (CA) secretion in bovine adrenal chromaffin cell. Cimicifugoside inhibited calcium increase induced by 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP), a nAChR agonist with a half maximal inhibitory concentration (IC50) of 18${\pm}$2${\mu}$M. In contrast, cimicifugoside did not affect the calcium increases evoked by high K$\^$+/, veratridine, and bradykinin. The DMPP-induced sodium increase was also inhibited by cimicifugoside with IC50 of 2${\pm}$0.3${\mu}$M, suggesting that the activity of nAChRs is inhibited by cimicifugoside. Cimicifugoside did not effect on the KCl-induced secretion but markedly inhibited the DMPP-induced catecholamine secretion which was monitored by carbon-fiber amperometry in real time, and by high performance liquid chromatography (HPLC) through electrochemical detection. The results suggest that cimicifugoside selectively inhibits nAChR-mediated response in bovine chromaffin cells.

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