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Just How Critical is Epithelial-to-Mesenchymal Transition (EMT) to Metastatic Dissemination? 上皮细胞向间质转化(EMT)对转移扩散有多重要?
Pub Date : 2019-01-01 DOI: 10.29199/jpct.101015
Torre-Healy LA, Chia-Hsin Chan
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引用次数: 0
Antimicrobial activity of some pyrazolidin-3-one Schiff base derivatives and their complexes with selected metal ions 一些吡唑烷-3- 1希夫碱衍生物及其与选定金属离子配合物的抗菌活性
Pub Date : 2018-11-10 DOI: 10.29199/jpct.101019
A. A. Maihub, Sofiane Mohamed, Ahmed A Awin, Amal K Belaid, Salah M. Bensaber, Anton, Hermann, A. Gbaj
In spite of the fact that the structural similarity of pyrazolidin-3-one based compounds with the triazole, the antimicrobial activity of pyrazolidin-3-one compounds, have been investigated by many research groups to achieve potent antimicrobial agents. As result of the emerged drug resistance for many antimicrobial agents, we aimed in the current study to develop new potent and safe antimicrobial agents. In this study, a series of novel antimicrobial pyrazolidin-3-one based compounds and their transition metal complexes with Fe (II), Mn (II), Co(II), Ni(II), Zn(II), Cd(II), Cu(II), Pt(II) and Mo(II) ions were synthesized in good yields using microwave irradiation. All synthesized compound (free ligands and their metal complexes) were fully characterized by several spectroscopic techniques such as molar conductance, infrared, UV/Visible electronic, 1H NMR and 13C NMR spectra. In addition, the elemental analyses and conductivity investigations were done and combined with other spectroscopic data to determine the ligand: metal [M: L or L:M] ratio. The free unattached ligands and their complexes were screened for their in vitro antimicrobial activity against Staphylococcus aureus (ATCC29213) Escherichia coli (ATCC-25922), and Candida albicans (ATCC-10231). The achieved results indicated that some complexes are more potent than their free ligands and metal ions (Fe (II), Pt (II), Co(II), and Ni(II)), and some of the complexes are more potent than the standard antifungal amphoteracine-B. In conclusion, the biological activity results indicated the enhancement of the antimicrobial activity of some imine derivatives of pyrazolidin-3-one will open the field for scientists to develop more effective and safe drugs.
尽管吡唑烷-3-酮类化合物与三唑类化合物结构相似,但许多研究小组已经对吡唑烷-3-酮类化合物的抗菌活性进行了研究,以获得有效的抗菌药物。由于许多抗菌药物出现耐药性,我们目前的研究目标是开发新的有效和安全的抗菌药物。本研究利用微波辐照合成了一系列新型抗菌吡唑烷-3- 1基化合物及其与Fe (II)、Mn (II)、Co(II)、Ni(II)、Zn(II)、Cd(II)、Cu(II)、Pt(II)和Mo(II)离子的过渡金属配合物,收率较高。所有合成的化合物(自由配体及其金属配合物)均通过摩尔电导、红外、紫外/可见电子、1H NMR和13C NMR等多种光谱技术进行了表征。此外,进行了元素分析和电导率研究,并结合其他光谱数据确定了配体:金属[M: L或L:M]比。筛选了游离配体及其配合物对金黄色葡萄球菌(ATCC29213)、大肠杆菌(ATCC-25922)和白色念珠菌(ATCC-10231)的体外抗菌活性。结果表明,一些配合物比它们的自由配体和金属离子(Fe (II)、Pt (II)、Co(II)和Ni(II))更有效,一些配合物比标准的抗真菌药两性拉辛- b更有效。综上所述,生物活性结果表明,吡唑烷-3- 1亚胺衍生物抗菌活性的增强将为科学家开发更有效、更安全的药物开辟领域。
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引用次数: 3
Just How Critical is Epithelial-to-Mesenchymal Transition (EMT) to Metastatic Dissemination? 上皮-间质转化(EMT)对转移性传播有多重要?
Pub Date : 2017-12-21 DOI: 10.29199/psep.101015
Torre-Healy La, Chia-Hsin Chan
Epithelial-to-Mesenchymal Transition (EMT) has long been considered to be critical for the development of lung metastasis in breast cancer [1]. Cells that transition to a mesenchymal phenotype lose their adherent properties and become increasingly motile. Silencing of Snail, Zebl, Twist and other EMT associated genes correlate with a decrease in metastasis in in vivo models, and point to a critical role of EMT in metastasis [2–4]. However, analysis of tumor cells within both the primary tumor and metastatic lesions show primarily epithelial markers. Currently, it is believed that cells undergo Mesenchymal-to-Epithelial Transition (MET) following their colonization into a new organ environment [5]. A recent publication by Fischer et al., used the Cre/CreER lineage-tracing genetic mouse model to explore the necessity of EMT in breast cancer metastasis [6]. Through their generation of Fibroblast Specific Protein 1 (FSP1)-GFP and Vimentin-GFP reporter mouase lines, using Cre and CreER respectively, they reported that cancer cells that had not undergone EMT still metastasized just as much as those that had. The conclusions of this paper were brought into question in 2017 by Ye et al., following close scrutiny of selection ofVimentin and FSP1 promoters for the activation of EMT programs as well as the recombination efficiency of CreER [7]. We will discuss the positions held by the two contradictory publications and provide insight beyond luminal-subtype breast cancer.
上皮-间质转化(Epithelial-to-Mesenchymal Transition, EMT)一直被认为是乳腺癌肺转移的关键[1]。过渡到间充质表型的细胞失去其粘附特性并变得越来越活跃。在体内模型中,Snail、Zebl、Twist等EMT相关基因的沉默与转移减少相关,表明EMT在转移中起着关键作用[2-4]。然而,对原发肿瘤和转移灶内肿瘤细胞的分析显示主要是上皮标记物。目前,人们认为细胞在定植到新的器官环境后会经历间充质-上皮转化(Mesenchymal-to-Epithelial Transition, MET)[5]。Fischer等人最近发表的一篇文章利用Cre/CreER谱系追踪遗传小鼠模型探讨了EMT在乳腺癌转移中的必要性[6]。通过分别使用Cre和CreER生成成纤维细胞特异性蛋白1 (FSP1)-GFP和Vimentin-GFP报告小鼠系,他们报告说,未经历EMT的癌细胞仍然与经历过EMT的癌细胞一样多地转移。2017年,Ye等人仔细研究了vimentin和FSP1启动子对EMT程序的激活以及CreER的重组效率的选择,对这篇论文的结论提出了质疑[7]。我们将讨论两种相互矛盾的出版物所持的立场,并提供超越光亚型乳腺癌的见解。
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引用次数: 0
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Journal of pharmacology and clinical trials
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