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[PMID]: 28605593
[Au] Autor:Kendrick S; Muranyi A; Gokhale V; Hurley LH; Rimsza LM
[Ad] Address:Department of Pathology, University of Arizona , 1501 North Campbell Avenue, Tucson, Arizona 85724, United States.
[Ti] Title:Simultaneous Drug Targeting of the Promoter MYC G-Quadruplex and BCL2 i-Motif in Diffuse Large B-Cell Lymphoma Delays Tumor Growth.
[So] Source:J Med Chem;60(15):6587-6597, 2017 Aug 10.
[Is] ISSN:1520-4804
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:Secondary DNA structures are uniquely poised as therapeutic targets due to their molecular switch function in turning gene expression on or off and scaffold-like properties for protein and small molecule interaction. Strategies to alter gene transcription through these structures thus far involve targeting single DNA conformations. Here we investigate the feasibility of simultaneously targeting different secondary DNA structures to modulate two key oncogenes, cellular-myelocytomatosis (MYC) and B-cell lymphoma gene-2 (BCL2), in diffuse large B-cell lymphoma (DLBCL). Cotreatment with previously identified ellipticine and pregnanol derivatives that recognize the MYC G-quadruplex and BCL2 i-motif promoter DNA structures lowered mRNA levels and subsequently enhanced sensitivity to a standard chemotherapy drug, cyclophosphamide, in DLBCL cell lines. In vivo repression of MYC and BCL2 in combination with cyclophosphamide also significantly slowed tumor growth in DLBCL xenograft mice. Our findings demonstrate concurrent targeting of different DNA secondary structures offers an effective, precise, medicine-based approach to directly impede transcription and overcome aberrant pathways in aggressive malignancies.
[Mh] MeSH terms primary: Antineoplastic Agents/therapeutic use
G-Quadruplexes
Lymphoma, Large B-Cell, Diffuse/drug therapy
Promoter Regions, Genetic
Proto-Oncogene Proteins c-bcl-2/genetics
Proto-Oncogene Proteins c-myc/genetics
[Mh] MeSH terms secundary: Animals
Apoptosis/drug effects
Benzoxazines/therapeutic use
Caspase 3/metabolism
Cell Line
Cyclophosphamide/therapeutic use
Drug Delivery Systems
Ellipticines/therapeutic use
Gene Knockdown Techniques
Humans
Lymphoma, Large B-Cell, Diffuse/pathology
Mice
Pregnanes/therapeutic use
RNA, Messenger/metabolism
Tumor Burden
Xenograft Model Antitumor Assays
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (9-(dimethylaminoethoxy)ellipticine); 0 (Antineoplastic Agents); 0 (BCL2 protein, human); 0 (Benzoxazines); 0 (Ellipticines); 0 (IMC-76); 0 (MYC protein, human); 0 (Pregnanes); 0 (Proto-Oncogene Proteins c-bcl-2); 0 (Proto-Oncogene Proteins c-myc); 0 (RNA, Messenger); 8N3DW7272P (Cyclophosphamide); EC 3.4.22.- (CASP3 protein, human); EC 3.4.22.- (Caspase 3)
[Em] Entry month:1709
[Cu] Class update date: 170906
[Lr] Last revision date:170906
[Js] Journal subset:IM
[Da] Date of entry for processing:170613
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00298

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[PMID]: 28477443
[Au] Autor:Nishiyama T; Hatae N; Mizutani M; Yoshimura T; Kitamura T; Miyano M; Fujii M; Satsuki N; Ishikura M; Hibino S; Choshi T
[Ad] Address:Graduate School of Pharmacy Pharmaceutical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Fukuyama, Hiroshima 729-0292, Japan.
[Ti] Title:Concise synthesis and antiproliferative activity evaluation of ellipticine quinone and its analogs.
[So] Source:Eur J Med Chem;136:1-13, 2017 Aug 18.
[Is] ISSN:1768-3254
[Cp] Country of publication:France
[La] Language:eng
[Ab] Abstract:We developed a concise protocol for the synthesis of ellipticine quinone from the appropriate 3-iodoindole-2-carbaldehydes in four steps. The key step is the construction of carbazole-1,4-quinone through tandem Ring-Closing Metathesis (RCM) and dehydrogenation under oxygen atmosphere. Therefore, the ellipticine quinone analogs possessing substitution at the 8- and/or 9-positions were synthesized using this method. In total, 14 compounds were evaluated for antiproliferative activity against HCT-116 and HL-60 cell lines; 9-nitroellipticine quinone was found to have superior activity compared to calothrixin B.
[Mh] MeSH terms primary: Antineoplastic Agents/pharmacology
Benzoquinones/pharmacology
Ellipticines/pharmacology
[Mh] MeSH terms secundary: Antineoplastic Agents/chemical synthesis
Antineoplastic Agents/chemistry
Benzoquinones/chemistry
Cell Proliferation/drug effects
Cell Survival/drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Ellipticines/chemistry
Humans
Molecular Structure
Structure-Activity Relationship
Tumor Cells, Cultured
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Antineoplastic Agents); 0 (Benzoquinones); 0 (Ellipticines); 117VLW7484 (ellipticine); 3T006GV98U (quinone)
[Em] Entry month:1709
[Cu] Class update date: 170928
[Lr] Last revision date:170928
[Js] Journal subset:IM
[Da] Date of entry for processing:170507
[St] Status:MEDLINE

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[PMID]: 28138703
[Au] Autor:Tao S; Meng S; Zheng X; Xie L
[Ad] Address:Department of Urology, The First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, Zhejiang 310003, P.R. China.
[Ti] Title:ATM participates in the regulation of viability and cell cycle via ellipticine in bladder cancer.
[So] Source:Mol Med Rep;15(3):1143-1148, 2017 Mar.
[Is] ISSN:1791-3004
[Cp] Country of publication:Greece
[La] Language:eng
[Ab] Abstract:Ellipticine, an alkaloid isolated from Apocyanaceae plants, has been demonstrated to exhibit antitumor activity in several cancers. However, the effect and the mechanisms underlying its action have not been investigated in human bladder cancer cells. The aim of the present study was to investigate the effect and mechanism of ellipticine on the behavior of T­24 bladder cancer cells. T­24 cells were treated with varying concentrations and durations of ellipticine. Cell viability was evaluated by Cell Counting Kit­8 assay. Cell motility was analyzed by Transwell migration assay. Flow cytometry, reverse transcription­quantitative polymerase chain reaction and western blot analyses were performed to detect the cell cycle and signaling pathways involved. The results demonstrated that ellipticine suppressed proliferation and inhibited the migration ability of T­24 bladder cancer cells in a dose­ and time­dependent manner, and resulted in G2/M cell cycle arrest. The mechanism of this action was demonstrated to be due to ellipticine­triggered activation of the ATM serine/threonine kinase pathway. These data therefore suggest that ellipticine may be effective towards treating human bladder cancer.
[Mh] MeSH terms primary: Antineoplastic Agents/pharmacology
Ataxia Telangiectasia Mutated Proteins/metabolism
Cell Cycle/drug effects
Cell Survival/drug effects
Ellipticines/pharmacology
Signal Transduction/drug effects
Urinary Bladder Neoplasms/metabolism
[Mh] MeSH terms secundary: CDC2 Protein Kinase/metabolism
Cell Line, Tumor
Cell Movement/drug effects
Cell Proliferation/drug effects
Checkpoint Kinase 1/metabolism
Humans
Urinary Bladder Neoplasms/genetics
cdc25 Phosphatases/metabolism
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Antineoplastic Agents); 0 (Ellipticines); 117VLW7484 (ellipticine); EC 2.7.11.1 (Ataxia Telangiectasia Mutated Proteins); EC 2.7.11.1 (Checkpoint Kinase 1); EC 2.7.11.22 (CDC2 Protein Kinase); EC 3.1.3.48 (cdc25 Phosphatases)
[Em] Entry month:1705
[Cu] Class update date: 170509
[Lr] Last revision date:170509
[Js] Journal subset:IM
[Da] Date of entry for processing:170201
[St] Status:MEDLINE
[do] DOI:10.3892/mmr.2017.6141

  4 / 694 MEDLINE  
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[PMID]: 28263536
[Au] Autor:Sulc M; Mrizova I; Cerna T; Frei E; Eckschlager T; Adam V; Kopeckova K; Stiborova M
[Ad] Address:Department of Biochemistry, Faculty of Science, Charles University, Prague 2, Czech Republic.
[Ti] Title:Effectiveness of human cytochrome P450 3A4 present in liposomal and microsomal nanoparticles in formation of covalent DNA adducts by ellipticine.
[So] Source:Neuro Endocrinol Lett;37(Suppl1):95-102, 2016 Dec 18.
[Is] ISSN:0172-780X
[Cp] Country of publication:Sweden
[La] Language:eng
[Ab] Abstract:OBJECTIVES: Ellipticine is an anticancer agent that functions through multiple mechanisms participating in cell cycle arrest and initiation of apoptosis. This drug forms covalent DNA adducts after its enzymatic activation with cytochrome P450 (CYP), which is one of the most important ellipticine DNA-damaging mechanisms of its cytotoxic effects. The improvements of cancer treatment are the major challenge in oncology research. Nanotransporters (nanoparticles) are promising approaches to target tumor cells, frequently leading to improve drug therapeutic index. Ellipticine has already been prepared in nanoparticle forms. However, since its anticancer efficiency depends on the CYP3A4-mediated metabolism in cancer cells, the aim of our research is to develop nanoparticles containing this enzyme that can be transported to tumor cells, thereby potentiating ellipticine cytotoxicity. METHODS: The CYP3A4 enzyme encapsulated into two nanoparticle forms, liposomes and microsomes, was tested to activate ellipticine to its reactive species forming covalent DNA adducts. Ellipticine-derived DNA adducts were determined by the 32P-postlabeling method. RESULTS: The CYP3A4 enzyme both in the liposome and microsome nanoparticle forms was efficient to activate ellipticine to species forming DNA adducts. Two DNA adducts, which are formed from ellipticine metabolites 12-hydroxy- and 13-hydroxyellipticine generated by its oxidation by CYP3A4, were formed by both CYP3A4 nanoparticle systems. A higher effectiveness of CYP3A4 in microsomal than in liposomal nanoparticles to form ellipticine-DNA adducts was found. CONCLUSION: Further testing in a suitable cancer cell model is encouraged to investigate whether the DNA-damaging effects of ellipticine after its activation by CYP3A4 nanoparticle forms are appropriate for active targeting of this enzyme to specific cancer cells.
[Mh] MeSH terms primary: Antineoplastic Agents, Phytogenic/metabolism
Cytochrome P-450 CYP3A/metabolism
DNA Adducts/metabolism
Ellipticines/metabolism
Liposomes
Microsomes
[Mh] MeSH terms secundary: Humans
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Antineoplastic Agents, Phytogenic); 0 (DNA Adducts); 0 (Ellipticines); 0 (Liposomes); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP3A)
[Em] Entry month:1706
[Cu] Class update date: 170620
[Lr] Last revision date:170620
[Js] Journal subset:IM
[Da] Date of entry for processing:170307
[St] Status:MEDLINE

  5 / 694 MEDLINE  
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[PMID]: 27908111
[Au] Autor:Sappati S; Hassanali A; Gebauer R; Ghosh P
[Ad] Address:Department of Chemistry, Indian Institute of Science Education and Research, Pune 411008, India.
[Ti] Title:Nuclear quantum effects in a HIV/cancer inhibitor: The case of ellipticine.
[So] Source:J Chem Phys;145(20):205102, 2016 Nov 28.
[Is] ISSN:1089-7690
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:Ellipticine is a natural product that is currently being actively investigated for its inhibitory cancer and HIV properties. Here we use path-integral molecular dynamics coupled with excited state calculations to characterize the role of nuclear quantum effects on the structural and electronic properties of ellipticine in water, a common biological solvent. Quantum effects collectively enhance the fluctuations of both light and heavy nuclei of the covalent and hydrogen bonds in ellipticine. In particular, for the ellipticine-water system, where the proton donor and acceptor have different proton affinities, we find that nuclear quantum effects (NQEs) strengthen both the strong and the weak H bonds. This is in contrast to what is observed for the cases where the proton affinity of the donors and acceptors is same. These structural fluctuations cause a significant red-shift in the absorption spectra and an increase in the broadening, bringing it into closer agreement with the experiments. Our work shows that nuclear quantum effects alter both qualitatively and quantitatively the optical properties of this biologically relevant system and highlights the importance of the inclusion of these effects in the microscopic understanding of their optical properties. We propose that isotopic substitution will produce a blue shift and a reduction in the broadening of the absorption peak.
[Mh] MeSH terms primary: Anti-HIV Agents/chemistry
Antineoplastic Agents/chemistry
Ellipticines/chemistry
Quantum Theory
[Mh] MeSH terms secundary: Absorption, Physicochemical
Anti-HIV Agents/pharmacology
Antineoplastic Agents/pharmacology
Ellipticines/pharmacology
Molecular Conformation
Molecular Dynamics Simulation
Solvents/chemistry
Water/chemistry
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Anti-HIV Agents); 0 (Antineoplastic Agents); 0 (Ellipticines); 0 (Solvents); 059QF0KO0R (Water); 117VLW7484 (ellipticine)
[Em] Entry month:1702
[Cu] Class update date: 170227
[Lr] Last revision date:170227
[Js] Journal subset:IM
[Da] Date of entry for processing:161203
[St] Status:MEDLINE

  6 / 694 MEDLINE  
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[PMID]: 26937690
[Au] Autor:Zhang L; Bennett WF; Zheng T; Ouyang PK; Ouyang X; Qiu X; Luo A; Karttunen M; Chen P
[Ad] Address:Biological and Pharmaceutical Engineering, Nanjing Technology University , 30 Puzhu Road South, Nanjing, Jiangsu, China , 211816.
[Ti] Title:Effect of Cholesterol on Cellular Uptake of Cancer Drugs Pirarubicin and Ellipticine.
[So] Source:J Phys Chem B;120(12):3148-56, 2016 Mar 31.
[Is] ISSN:1520-5207
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:The cell membrane is a major barrier for drug transport. Given that many cancer drugs must passively cross the cell membrane, understanding drug-membrane interactions is crucial. We used fluorescence-activated cell sorting to investigate how cholesterol influences the transport of the cancer drugs ellipticine and pirarubicin across cell membranes. We showed that cholesterol depletion helped pirarubicin cross the membranes of nonsmall cell lung carcinoma and Chinese hamster ovary cells. In contrast, the uptake of ellipticine was not strongly influenced by cholesterol depletion. To study the microscopic origins of these observations, atomistic molecular dynamics simulations were performed. Doxorubicin (similar in structure to pirarubicin) and ellipticine were simulated in model membranes of POPC and POPC with 40 mol % cholesterol. Atomistic free energy calculations for the translocation of a single ellipticine and doxorubicin across the lipid bilayers qualitatively matched the experiment results. The free energy barrier for doxorubicin crossing the bilayer was strongly increased when cholesterol was present, while for ellipticine the barrier remained similar with and without cholesterol. Molecular dynamics simulations showed that the different hydrogen-bonding propensities of the two drugs are likely the major factor for the different behaviors. The qualitative agreement between cell experiments and atomistic computer simulations illustrates the potential to link observed biological phenomena and single molecule mechanisms of actions. Our results suggest that the traditional understanding of drug permeation and the influence of cholesterol on the small molecule transport is naïve and needs to be re-examined.
[Mh] MeSH terms primary: Antineoplastic Agents/pharmacokinetics
Cell Membrane/drug effects
Cell Membrane/metabolism
Cholesterol/pharmacology
Doxorubicin/analogs & derivatives
Ellipticines/pharmacokinetics
Lung Neoplasms/metabolism
[Mh] MeSH terms secundary: Animals
Antineoplastic Agents/chemistry
CHO Cells
Cells, Cultured
Cholesterol/chemistry
Cricetulus
Doxorubicin/chemistry
Doxorubicin/pharmacokinetics
Ellipticines/chemistry
Fluorescence
Humans
Lung Neoplasms/pathology
Molecular Dynamics Simulation
Molecular Structure
[Pt] Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Name of substance:0 (Antineoplastic Agents); 0 (Ellipticines); 117VLW7484 (ellipticine); 80168379AG (Doxorubicin); 97C5T2UQ7J (Cholesterol); D58G680W0G (pirarubicin)
[Em] Entry month:1612
[Cu] Class update date: 161230
[Lr] Last revision date:161230
[Js] Journal subset:IM
[Da] Date of entry for processing:160304
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jpcb.5b12337

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[PMID]: 26927112
[Au] Autor:Skalickova S; Nejdl L; Kudr J; Ruttkay-Nedecky B; Jimenez AM; Kopel P; Kremplova M; Masarik M; Stiborova M; Eckschlager T; Adam V; Kizek R
[Ad] Address:Department of Chemistry and Biochemistry, Faculty of Agronomy, Mendel University in Brno, Zemedelska 1, CZ-613 00 Brno, Czech Republic. sylvie.skalickova@gmail.com.
[Ti] Title:Fluorescence Characterization of Gold Modified Liposomes with Antisense N-myc DNA Bound to the Magnetisable Particles with Encapsulated Anticancer Drugs (Doxorubicin, Ellipticine and Etoposide).
[So] Source:Sensors (Basel);16(3):290, 2016 Feb 25.
[Is] ISSN:1424-8220
[Cp] Country of publication:Switzerland
[La] Language:eng
[Ab] Abstract:Liposome-based drug delivery systems hold great potential for cancer therapy. The aim of this study was to design a nanodevice for targeted anchoring of liposomes (with and without cholesterol) with encapsulated anticancer drugs and antisense N-myc gene oligonucleotide attached to its surface. To meet this main aim, liposomes with encapsulated doxorubicin, ellipticine and etoposide were prepared. They were further characterized by measuring their fluorescence intensity, whereas the encapsulation efficiency was estimated to be 16%. The hybridization process of individual oligonucleotides forming the nanoconstruct was investigated spectrophotometrically and electrochemically. The concentrations of ellipticine, doxorubicin and etoposide attached to the nanoconstruct in gold nanoparticle-modified liposomes were found to be 14, 5 and 2 µg·mL(-1), respectively. The study succeeded in demonstrating that liposomes are suitable for the transport of anticancer drugs and the antisense oligonucleotide, which can block the expression of the N-myc gene.
[Mh] MeSH terms primary: DNA, Antisense/therapeutic use
Drug Delivery Systems
Magnetite Nanoparticles/chemistry
Neoplasms/drug therapy
[Mh] MeSH terms secundary: DNA, Antisense/chemistry
Doxorubicin/chemistry
Doxorubicin/therapeutic use
Ellipticines/chemistry
Ellipticines/therapeutic use
Etoposide/chemistry
Etoposide/therapeutic use
Fluorescence
Gold/chemistry
Humans
Liposomes/chemistry
Liposomes/therapeutic use
Magnetite Nanoparticles/therapeutic use
N-Myc Proto-Oncogene Protein/antagonists & inhibitors
N-Myc Proto-Oncogene Protein/genetics
[Pt] Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Name of substance:0 (DNA, Antisense); 0 (Ellipticines); 0 (Liposomes); 0 (Magnetite Nanoparticles); 0 (N-Myc Proto-Oncogene Protein); 6PLQ3CP4P3 (Etoposide); 7440-57-5 (Gold); 80168379AG (Doxorubicin)
[Em] Entry month:1701
[Cu] Class update date: 170220
[Lr] Last revision date:170220
[Js] Journal subset:IM
[Da] Date of entry for processing:160302
[St] Status:MEDLINE

  8 / 694 MEDLINE  
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[PMID]: 26915592
[Au] Autor:Zlabek V; Burkina V; Borrisser-Pairó F; Sakalli S; Zamaratskaia G
[Ad] Address:University of South Bohemia in Ceske Budejovice, Vodnany, Czech Republic. Electronic address: vzlabek@frov.jcu.cz.
[Ti] Title:Phase I metabolism of 3-methylindole, an environmental pollutant, by hepatic microsomes from carp (Cyprinus carpio) and rainbow trout (Oncorhynchus mykiss).
[So] Source:Chemosphere;150:304-310, 2016 May.
[Is] ISSN:1879-1298
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:We studied the in vitro metabolism of 3-methylindole (3MI) in hepatic microsomes from fish. Hepatic microsomes from juvenile and adult carp (Cyprinus carpio) and rainbow trout (Oncorhynchus mykiss) were included in the study. Incubation of 3MI with hepatic microsomes revealed the time-dependent formation of two major metabolites, 3-methyloxindole (3MOI) and indole-3-carbinol (I3C). The rate of 3MOI production was similar in both species at both ages. No differences in kinetic parameters were observed (p = 0.799 for Vmax, and p = 0.809 for Km). Production of I3C was detected only in the microsomes from rainbow trout. Km values were similar in juvenile and adult fish (p = 0.957); Vmax was higher in juvenile rainbow trout compared with adults (p = 0.044). In rainbow trout and carp, ellipticine reduced formation of 3MOI up to 53.2% and 81.9% and ketoconazole up to 65.8% and 91.3%, respectively. The formation of I3C was reduced by 53.7% and 51.5% in the presence of the inhibitors ellipticine and ketoconazole, respectively. These findings suggest that the CYP450 isoforms CYP1A and CYP3A are at least partly responsible for 3MI metabolism. In summary, 3MI is metabolised in fish liver to 3MOI and I3C by CYP450, and formation of these metabolites might be species-dependent.
[Mh] MeSH terms primary: Carps/metabolism
Microsomes, Liver/metabolism
Oncorhynchus mykiss/metabolism
Skatole/metabolism
Water Pollutants, Chemical/metabolism
[Mh] MeSH terms secundary: Animals
Cytochrome P-450 Enzyme Inhibitors/pharmacology
Cytochrome P-450 Enzyme System/metabolism
Ellipticines/pharmacology
In Vitro Techniques
Indoles/metabolism
Ketoconazole/pharmacology
Liver/drug effects
Liver/metabolism
Metabolic Detoxication, Phase I
Microsomes, Liver/drug effects
Skatole/toxicity
Species Specificity
Water Pollutants, Chemical/toxicity
[Pt] Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Name of substance:0 (Cytochrome P-450 Enzyme Inhibitors); 0 (Ellipticines); 0 (Indoles); 0 (Water Pollutants, Chemical); 117VLW7484 (ellipticine); 1504-06-9 (3-methyloxindole); 9035-51-2 (Cytochrome P-450 Enzyme System); 9W945B5H7R (Skatole); C11E72455F (indole-3-carbinol); R9400W927I (Ketoconazole)
[Em] Entry month:1612
[Cu] Class update date: 170802
[Lr] Last revision date:170802
[Js] Journal subset:IM
[Da] Date of entry for processing:160227
[St] Status:MEDLINE

  9 / 694 MEDLINE  
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[PMID]: 26906637
[Au] Autor:Vann KR; Ergün Y; Zencir S; Oncuoglu S; Osheroff N; Topcu Z
[Ad] Address:Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
[Ti] Title:Inhibition of human DNA topoisomerase IIα by two novel ellipticine derivatives.
[So] Source:Bioorg Med Chem Lett;26(7):1809-12, 2016 Apr 01.
[Is] ISSN:1464-3405
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Ellipticine (5,11-dimethyl-6H-pyrido[4,3-b]carbazole) is an antineoplastic agent that intercalates into DNA and alters topoisomerase II activity. Unfortunately, this compound displays a number of adverse properties. Therefore, to investigate new ellipticine-based compounds for their potential as topoisomerase II-targeted drugs, we synthesized two novel derivatives, N-methyl-5-demethyl ellipticine (ET-1) and 2-methyl-N-methyl-5-demethyl ellipticinium iodide (ET-2). As determined by DNA decatenation and cleavage assays, ET-1 and ET-2 act as catalytic inhibitors of human topoisomerase IIα and are both more potent than the parent compound. Neither compound impairs the ability of the type II enzyme to bind its DNA substrate. Finally, the potency of ET-1 and ET-2 as catalytic inhibitors of topoisomerase IIα appears to be related to their ability to intercalate into the double helix.
[Mh] MeSH terms primary: DNA-Binding Proteins/antagonists & inhibitors
Ellipticines/chemistry
Ellipticines/pharmacology
Topoisomerase II Inhibitors/chemistry
Topoisomerase II Inhibitors/pharmacology
[Mh] MeSH terms secundary: Antigens, Neoplasm/metabolism
DNA/metabolism
DNA Topoisomerases, Type II/metabolism
DNA-Binding Proteins/metabolism
Humans
Intercalating Agents/chemistry
Intercalating Agents/pharmacology
Methylation
[Pt] Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Name of substance:0 (Antigens, Neoplasm); 0 (DNA-Binding Proteins); 0 (Ellipticines); 0 (Intercalating Agents); 0 (Topoisomerase II Inhibitors); 9007-49-2 (DNA); EC 5.99.1.3 (DNA Topoisomerases, Type II)
[Em] Entry month:1611
[Cu] Class update date: 171116
[Lr] Last revision date:171116
[Js] Journal subset:IM
[Da] Date of entry for processing:160225
[St] Status:MEDLINE

  10 / 694 MEDLINE  
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[PMID]: 26878420
[Au] Autor:Lin HH; Chuang KS; Chen SY; Jan ML
[Ad] Address:Department of Biomedical Engineering and Environmental Sciences, National Tsing-Hua University, HsinChu, Taiwan. Medical Physics Research Center, Institute for Radiological Research, Chang Gung University/Chang Gung Memorial Hospital, Linkou, Taoyuan, Taiwan.
[Ti] Title:Recovering the triple coincidence of non-pure positron emitters in preclinical PET.
[So] Source:Phys Med Biol;61(5):1904-31, 2016 Mar 07.
[Is] ISSN:1361-6560
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Non-pure positron emitters, with their long half-lives, allow for the tracing of slow biochemical processes which cannot be adequately examined by the commonly used short-lived positron emitters. Most of these isotopes emit high-energy cascade gamma rays in addition to positron decay that can be detected and create a triple coincidence with annihilation photons. Triple coincidence is discarded in most scanners, however, the majority of the triple coincidence contains true photon pairs that can be recovered. In this study, we propose a strategy for recovering triple coincidence events to raise the sensitivity of PET imaging for non-pure positron emitters. To identify the true line of response (LOR) from a triple coincidence, a framework utilizing geometrical, energy and temporal information is proposed. The geometrical criterion is based on the assumption that the LOR with the largest radial offset among the three sub pairs of triple coincidences is least likely to be a true LOR. Then, a confidence time window is used to test the valid LOR among those within triple coincidence. Finally, a likelihood ratio discriminant rule based on the energy probability density distribution of cascade and annihilation gammas is established to identify the true LOR. An Inveon preclinical PET scanner was modeled with GATE (GEANT4 application for tomographic emission) Monte Carlo software. We evaluated the performance of the proposed method in terms of identification fraction, noise equivalent count rates (NECR), and image quality on various phantoms. With the inclusion of triple coincidence events using the proposed method, the NECR was found to increase from 11% to 26% and 19% to 29% for I-124 and Br-76, respectively, when 7.4-185 MBq of activity was used. Compared to the reconstructed images using double coincidence, this technique increased the SNR by 5.1-7.3% for I-124 and 9.3-10.3% for Br-76 within the activity range of 9.25-74 MBq, without compromising the spatial resolution or contrast. We conclude that the proposed method can improve the counting statistics of PET imaging for non-pure positron emitters and is ready to be implemented on current PET systems.
[Mh] MeSH terms primary: Electrons
Image Processing, Computer-Assisted/methods
Phantoms, Imaging
Positron-Emission Tomography/methods
Software
[Mh] MeSH terms secundary: Computer Simulation
Ellipticines
Gamma Rays
Humans
Iodine Radioisotopes
Monte Carlo Method
Photons
Positron-Emission Tomography/instrumentation
Tomography Scanners, X-Ray Computed
[Pt] Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Name of substance:0 (Ellipticines); 0 (Iodine Radioisotopes); 65222-36-8 (BR 76)
[Em] Entry month:1610
[Cu] Class update date: 161230
[Lr] Last revision date:161230
[Js] Journal subset:IM
[Da] Date of entry for processing:160216
[St] Status:MEDLINE
[do] DOI:10.1088/0031-9155/61/5/1904


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