{"title":"Just How Critical is Epithelial-to-Mesenchymal Transition (EMT) to Metastatic Dissemination?","authors":"Torre-Healy LA, Chia-Hsin Chan","doi":"10.29199/jpct.101015","DOIUrl":"10.29199/jpct.101015","url":null,"abstract":"","PeriodicalId":93122,"journal":{"name":"Journal of pharmacology and clinical trials","volume":"1 1","pages":"8-10"},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7453587/pdf/nihms-1029147.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38326368","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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.
{"title":"Antimicrobial activity of some pyrazolidin-3-one Schiff base derivatives and their complexes with selected metal ions","authors":"A. A. Maihub, Sofiane Mohamed, Ahmed A Awin, Amal K Belaid, Salah M. Bensaber, Anton, Hermann, A. Gbaj","doi":"10.29199/jpct.101019","DOIUrl":"https://doi.org/10.29199/jpct.101019","url":null,"abstract":"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.","PeriodicalId":93122,"journal":{"name":"Journal of pharmacology and clinical trials","volume":"142 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90536802","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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.
{"title":"Just How Critical is Epithelial-to-Mesenchymal Transition (EMT) to Metastatic Dissemination?","authors":"Torre-Healy La, Chia-Hsin Chan","doi":"10.29199/psep.101015","DOIUrl":"https://doi.org/10.29199/psep.101015","url":null,"abstract":"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.","PeriodicalId":93122,"journal":{"name":"Journal of pharmacology and clinical trials","volume":"60 1","pages":"8-10"},"PeriodicalIF":0.0,"publicationDate":"2017-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84624076","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}