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[PMID]:28471109
[Au] Autor:Ye SF; Yang Y; Wu L; Ma WW; Zeng HH
[Ad] Endereço:State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China.
[Ti] Título:Ethaselen: a novel organoselenium anticancer agent targeting thioredoxin reductase 1 reverses cisplatin resistance in drug-resistant K562 cells by inducing apoptosis.
[So] Source:J Zhejiang Univ Sci B;18(5):373-382, 2017 May.
[Is] ISSN:1862-1783
[Cp] País de publicação:China
[La] Idioma:eng
[Ab] Resumo:It has been reported that Ethaselen shows inhibitory effects on thioredoxin reductase (TrxR) activity and human tumor cell growth. In order to find an efficient way to reverse cisplatin resistance, we investigated the reversal effects of Ethaselen on cisplatin resistance in K562/cisplatin (CDDP) cells that were established by pulse-inducing human erythrocyte leukemic cell line K562, which are fivefold more resistant to cisplatin compared to K562 cells. The morphology and growth showed that the adhesion of K562/CDDP further decreased while the cell volume increased. The proliferation of K562/CDDP is strengthened. The antitumor activities in vitro were assessed by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and combination index (CI), showing the significant synergic effects of cisplatin and Ethaselen. Focusing on apoptosis, a series of comparisons was made between K562 and K562/CDDP. Cisplatin induced higher reactive oxygen species (ROS) generation in K562 and subsequently induced the formation of mitochondrial permeability transition pores (PTPs). In addition, cisplatin increased the ratio of Bax to Bcl-2 in K562, which can influence the mitochondrial membrane permeability. PTP formation and mitochondrial membrane permeabilization eventually resulted in the release of cytochrome c and activation of the Caspase pathway. However, these effects were not clearly seen in K562/CDDP, which may be the reason for the acquired CDDP resistance. However, Ethaselen can induce a high level of ROS in K562/CDDP by TrxR activity inhibition and increased ratio of Bax to Bcl-2 in K562/CDDP by nuclear factor κB (NF-κB) suppression, which subsequently induces the release of cytochrome c in K562/CDDP. This response is partly responsible for the reversal of the cisplatin resistance in K562/CDDP cells.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Compostos Bicíclicos Heterocíclicos com Pontes/administração & dosagem
Cisplatino/administração & dosagem
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Compostos Organosselênicos/administração & dosagem
Tiorredoxina Redutase 1/antagonistas & inibidores
Tiorredoxina Redutase 1/metabolismo
[Mh] Termos MeSH secundário: Antineoplásicos/administração & dosagem
Proliferação Celular/efeitos dos fármacos
Tamanho Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ativação Enzimática/efeitos dos fármacos
Seres Humanos
Células K562
Terapia de Alvo Molecular/métodos
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane); 0 (Antineoplastic Agents); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Organoselenium Compounds); EC 1.8.1.9 (TXNRD1 protein, human); EC 1.8.1.9 (Thioredoxin Reductase 1); Q20Q21Q62J (Cisplatin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE
[do] DOI:10.1631/jzus.B1600073


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[PMID]:29395083
[Au] Autor:Yamagishi Y; Oya K; Matsuura A; Abe H
[Ad] Endereço:Department of Nanobiology, Graduate School of Advanced Integration Science, Chiba University, Chiba 263-8522, Japan. Electronic address: afha3649@chiba-u.jp.
[Ti] Título:Use of CK-548 and CK-869 as Arp2/3 complex inhibitors directly suppresses microtubule assembly both in vitro and in vivo.
[So] Source:Biochem Biophys Res Commun;496(3):834-839, 2018 02 12.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two types of Arp2/3 complex inhibitors, CK-666/636 and CK-548/869, are commonly used to study Arp2/3 complex-dependent actin assembly both in vitro and in vivo. However, we found that CK-548 and CK-869 directly suppress microtubule (MT) assembly independent of the actin cytoskeleton. Treatment of cultured mammalian cells with 50 µM CK-869 dramatically decreased MT networks and, instead, accumulated tubulin at the cell periphery, as did nocodazole that inhibits MT assembly. An in vitro MT-sedimentation assay revealed that CK-548 and CK-869 significantly suppressed MT polymerization. In budding yeast, although CK-548 and CK-869 are reported to lack binding abilities in the yeast Arp3, CK-548 treatment decreased cytoplasmic MT at several tens of micromolar concentrations. In addition, we found that the effects of CK-548 and CK-869 on MT assembly varied according to species. We propose that CK-548 and CK-869 are not suitable for studying the cytoskeleton in living cells.
[Mh] Termos MeSH primário: Complexo 2-3 de Proteínas Relacionadas à Actina/antagonistas & inibidores
Complexo 2-3 de Proteínas Relacionadas à Actina/metabolismo
Microtúbulos/fisiologia
Compostos Organosselênicos/administração & dosagem
Compostos de Organossilício/administração & dosagem
Tiazóis/administração & dosagem
Tubulina (Proteína)/metabolismo
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Drosophila melanogaster/metabolismo
Fibroblastos/efeitos dos fármacos
Fibroblastos/fisiologia
Gálio
Índio
Camundongos
Microtúbulos/efeitos dos fármacos
Células NIH 3T3
Ratos
Saccharomyces cerevisiae/metabolismo
Especificidade da Espécie
Moduladores de Tubulina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Actin-Related Protein 2-3 Complex); 0 (CK-0993548); 0 (CK-869); 0 (In(0.3)Ga(0.7)N); 0 (Organoselenium Compounds); 0 (Organosilicon Compounds); 0 (Thiazoles); 0 (Tubulin); 0 (Tubulin Modulators); 045A6V3VFX (Indium); CH46OC8YV4 (Gallium)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180204
[St] Status:MEDLINE


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[PMID]:29317251
[Au] Autor:Vogt AG; Voss GT; de Oliveira RL; Paltian JJ; Duarte LFB; Alves D; Jesse CR; Roman SS; Roehrs JA; Wilhelm EA; Luchese C
[Ad] Endereço:Programa de Pós-graduação em Bioquímica e Bioprospecção, Laboratório de Pesquisa em Farmacologia Bioquímica (LaFarBio), Grupo de Pesquisa em Neurobiotecnologia (GPN), Centro de Ciências Químicas, Farmacêuticas e de Alimentos, Universidade Federal de Pelotas (UFPel), CEP 96010-900, Pelotas, RS, Brazi
[Ti] Título:Organoselenium group is critical for antioxidant activity of 7-chloro-4-phenylselenyl-quinoline.
[So] Source:Chem Biol Interact;282:7-12, 2018 Feb 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:The quinolone compounds have been reported for many biological properties, especially as potent antioxidants. This study investigated the antioxidant effect of 7-chloro-4-phenylselenyl-quinoline (PSQ), a quinolone derivative with organoselenium group, against oxidative stress induced by sodium nitroprusside (SNP) in brains of mice. A second objective was to verify the importance of phenylselenyl group presents at position 4 of the quinoline structure to antioxidant effect of compound. So, it was compared the antioxidant effect of PSQ with a quinoline without organoseleniun group (7-chloroquinoline [QN]). Swiss mice were used and received SNP (0.335 µmol/site, intracerebroventricular) 30 min after treatment with PSQ or QN, at the doses of 50 mg/kg (intragastrically). After 1 h, animals were sacrificed and the brains were removed to biochemistry analysis. Thiobarbituric acid reactive species (TBARS), protein carbonyl (PC) and non-protein thiol (NPSH) levels, as well as catalase (CAT), glutathione S transferase (GST) and δ -aminolevulinic acid (δ-ALA-D) activities were determined. SNP increased TBARS and PC levels, and reduced the enzymatic (CAT and GST activity) and non-enzymatic (NPSH levels) antioxidant defenses and inhibited the δ-ALA-D activity. PSQ avoided the increase in the lipid peroxidation and PC levels, as well as the decrease in the NPSH levels, CAT, GST and δ-ALA-D activities QN partially avoided the increase in lipid peroxidation, but it not protected against alterations induced by SNP. In conclusion, phenylselenyl group present in quinoline structure is critical for antioxidant activity of PSQ.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Compostos Organosselênicos/farmacologia
Quinolinas/farmacologia
[Mh] Termos MeSH secundário: Ácido Aminolevulínico/metabolismo
Animais
Encéfalo/efeitos dos fármacos
Encéfalo/metabolismo
Catalase/metabolismo
Glutationa Peroxidase/metabolismo
Glutationa Transferase/metabolismo
Peroxidação de Lipídeos/efeitos dos fármacos
Masculino
Camundongos
Estresse Oxidativo/efeitos dos fármacos
Compostos de Sulfidrila/metabolismo
Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Organoselenium Compounds); 0 (Quinolines); 0 (Sulfhydryl Compounds); 0 (Thiobarbituric Acid Reactive Substances); 88755TAZ87 (Aminolevulinic Acid); E66400VT9R (quinoline); EC 1.11.1.6 (Catalase); EC 1.11.1.9 (Glutathione Peroxidase); EC 2.5.1.18 (Glutathione Transferase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180209
[Lr] Data última revisão:
180209
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE


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[PMID]:28463038
[Au] Autor:Thabet NM; Moustafa EM
[Ad] Endereço:a Radiation Biology Department , National Centre for Radiation Research and Technology (NCRRT), Atomic Energy Authority , Cairo , Egypt.
[Ti] Título:Synergistic effect of Ebselen and gamma radiation on breast cancer cells.
[So] Source:Int J Radiat Biol;93(8):784-792, 2017 08.
[Is] ISSN:1362-3095
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To explore the synergistic effect of a seleno-organic compound Ebselen (Ebs) and/or γ-radiation to exert antitumor effects on human breast cancer (MCF-7) cell line in vitro. MATERIALS AND METHODS: Ebs cytotoxicity at various concentrations (10, 25, 50 and 75 µg), cell proliferation and clonogenic assay of Ebs and/or γ-radiation (at 1, 3 and 6 Gy), expression of p-IκBα and NF-κB, inflammatory cytokines levels (TNF-α, IL-2, INF-γ, IL-10 and TGF-ß), apoptotic factors (Caspase-3, Granzyme-B and TRAIL) and angiogenic factor (VEGF) were investigated. RESULTS: The results showed that the effective dosage of this combination was observed at 25 µg/ml of Ebs with γ-radiation at 6 Gy. Data displayed a significant reduction in NF-κB mRNA along with an elevation in granzyme-B mRNA and TRAIL mRNA expression. Furthermore, protein expression of caspase-3 was elevated, whereas p-IκBα and p-NF-κB(p65) protein expression was reduced significantly. Also, a significant decline in TNF-α, IL-2, INF-γ, TGF-ß with a significant increase in IL-10 levels were revealed. Meanwhile, a significant decrease in VEGF level and proliferation capacity were observed. CONCLUSIONS: We conclude that a combination of Ebs with radiotherapy has a major antitumor efficiency in inducing apoptosis and inhibiting cancer cell progression, due to the synergistic effect in regulating gene and protein expression, and in a modulating response of pro-and anti-inflammatory cytokines.
[Mh] Termos MeSH primário: Azóis/farmacologia
Neoplasias da Mama/patologia
Raios gama
Compostos Organosselênicos/farmacologia
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Apoptose/efeitos da radiação
Caspase 3/metabolismo
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Proliferação Celular/efeitos da radiação
Citocinas/metabolismo
Granzimas/metabolismo
Seres Humanos
Células MCF-7
NF-kappa B/metabolismo
Transdução de Sinais/efeitos dos fármacos
Transdução de Sinais/efeitos da radiação
Ligante Indutor de Apoptose Relacionado a TNF/metabolismo
Fator A de Crescimento do Endotélio Vascular/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azoles); 0 (Cytokines); 0 (NF-kappa B); 0 (Organoselenium Compounds); 0 (TNF-Related Apoptosis-Inducing Ligand); 0 (Vascular Endothelial Growth Factor A); 40X2P7DPGH (ebselen); EC 3.4.21.- (Granzymes); EC 3.4.22.- (Caspase 3)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:180111
[Lr] Data última revisão:
180111
[Sb] Subgrupo de revista:IM; S
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1080/09553002.2017.1325024


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[PMID]:29182862
[Au] Autor:Cebrián-Prats A; Rovira T; Saura P; González-Lafont À; Lluch JM
[Ad] Endereço:Departament de Química and ‡Institut de Biotecnologia i de Biomedicina (IBB), Universitat Autònoma de Barcelona , 08193 Bellaterra, Barcelona, Spain.
[Ti] Título:Inhibition of Mammalian 15-Lipoxygenase by Three Ebselen-like Drugs. A QM/MM and MM/PBSA Comparative Study.
[So] Source:J Phys Chem A;121(51):9752-9763, 2017 Dec 28.
[Is] ISSN:1520-5215
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Ebselen is a potent competitive inhibitor of the active form of rabbit 15-lipoxygenase, an enzyme involved in many inflammatory diseases. Light-induced Z-to-E isomerization of the ebselen-like 2-(3-benzylidene)-3-oxo-2,3-dihydrobenzo[b]thiophene-7-carboxylic acid methyl ester (BODTCM) molecule was used to convert the weak (Z)-BOTDCM inhibitor into the (E)-isomer with much higher inhibitory capacity. In this study, the binding modes of ebselen, (E)-BOTDCM and (Z)-BOTDCM, have been analyzed to provide molecular insights on the inhibitory potency of ebselen and on the geometric-isomer specificity of (E)- and (Z)-BOTDCM inhibitors. The inhibitor-enzyme structures obtained from docking and molecular dynamics simulations as well as from QM/MM calculations show that the inhibitor molecules are not coordinated to the nonheme iron in the active site. Thermal motion allows ebselen and (E)-BOTDCM to visit a wide range of the configurational space competing with the polyunsaturated fatty acid for binding at the active site. Both molecules present similar MM/PBSA binding free energies. The energy penalty for the bigger geometric deformation undergone by (E)-BODTCM would explain its lower inhibitor potency. The (Z)-isomer is the weakest inhibitor because thermal motion moves it to a region very far from the first coordination sphere of Fe, where it could not compete with the fatty acid substrate.
[Mh] Termos MeSH primário: Araquidonato 15-Lipoxigenase/metabolismo
Azóis/farmacologia
Compostos Férricos/farmacologia
Inibidores de Lipoxigenase/farmacologia
Compostos Organosselênicos/farmacologia
Teoria Quântica
Termodinâmica
[Mh] Termos MeSH secundário: Animais
Azóis/síntese química
Azóis/química
Compostos Férricos/síntese química
Compostos Férricos/química
Ligantes
Inibidores de Lipoxigenase/síntese química
Inibidores de Lipoxigenase/química
Modelos Moleculares
Estrutura Molecular
Compostos Organosselênicos/síntese química
Compostos Organosselênicos/química
Coelhos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azoles); 0 (Ferric Compounds); 0 (Ligands); 0 (Lipoxygenase Inhibitors); 0 (Organoselenium Compounds); 40X2P7DPGH (ebselen); EC 1.13.11.33 (Arachidonate 15-Lipoxygenase)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180108
[Lr] Data última revisão:
180108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171129
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jpca.7b10416


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[PMID]:28807721
[Au] Autor:Domracheva I; Kanepe-Lapsa I; Jackevica L; Vasiljeva J; Arsenyan P
[Ad] Endereço:Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
[Ti] Título:Selenopheno quinolinones and coumarins promote cancer cell apoptosis by ROS depletion and caspase-7 activation.
[So] Source:Life Sci;186:92-101, 2017 Oct 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIM: This study was designed to investigate the mechanism underlying cancer cell apoptosis caused by selenophenoquinolinones and coumarins. MATERIALS AND METHODS: Twelve derivatives were studied according to their ability to suppress the proliferation of cancer cells in vitro (i.e., HepG2, MH-22A, MCF-7), induce cell apoptosis, modulate cellular antioxidant enzyme system activities (i.e., SOD, GPx, TrxR), influence the level of ROS, and modulate caspase activity. RESULTS: A plausible mechanism of apoptosis is presented. The lack of change in the activity of caspase-8 demonstrates that these compounds affect the intrinsic rather than the extrinsic pathway; moreover, the absence of caspase-9 activation suggests that the studied compounds are involved in the intrinsic pathway of apoptosis in a non-canonical manner. Provisionally, the increase in Smac/Diablo released from the mitochondria removes the inhibitory effect and activates caspase-7, leading to apoptosis. Additionally, the activation of caspase-1 activates effector caspase-7, thereby increasing the amount of cytochrome c and Smac/Diablo released from the mitochondria and ultimately leading to apoptosis. CONCLUSION: This present study provides scientific evidence that selenopheno quinolinones and coumarins promote cancer cell apoptosis by ROS depletion and caspase-7 activation in malignant cells.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Caspase 7/metabolismo
Cumarínicos/farmacologia
Compostos Organosselênicos/farmacologia
Quinolonas/farmacologia
Espécies Reativas de Oxigênio/metabolismo
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Antioxidantes/metabolismo
Técnicas de Cultura de Células
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Cumarínicos/síntese química
Cumarínicos/química
Células Hep G2
Seres Humanos
Células MCF-7
Camundongos
Estrutura Molecular
Compostos Organosselênicos/síntese química
Compostos Organosselênicos/química
Quinolonas/síntese química
Quinolonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Coumarins); 0 (Organoselenium Compounds); 0 (Quinolones); 0 (Reactive Oxygen Species); EC 3.4.22.- (Caspase 7)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170816
[St] Status:MEDLINE


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[PMID]:28763969
[Au] Autor:Bierla K; Suzuki N; Ogra Y; Szpunar J; Lobinski R
[Ad] Endereço:CNRS/UPPA, Institute for Analytical Sciences and Physical Chemistry for the Environment and Materials (IPREM), UMR 5254, Hélioparc, F-64053 Pau, France.
[Ti] Título:Identification and determination of selenohomolanthionine - The major selenium compound in Torula yeast.
[So] Source:Food Chem;237:1196-1201, 2017 Dec 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Torula yeast (Candida utilis) was found to metabolize selenium in a totally different way to Brewer's yeast (S. cerevisiae) leading to the biosynthesis of selenohomolanthionine (SeHLan), a major selenium compound accounting for 60-80% of the total selenium. The identity of SeHLan was confirmed by retention time matching in hydrophilic ion interaction chromatography (HILIC) with inductively coupled plasma mass spectrometric detection (ICP MS) using a custom synthesized standard molecule and by HILIC - Orbitrap MS and MS-MS fragmentation. Selenohomolanthionine escapes the current assays for the organic character of Se-rich yeast based on the protein-bound selenomethionine determination. A HILIC - ICP MS method was developed for the quantitative determination of selenohomolanthionine in yeast supplements with a detection limit of 146ng/g.
[Mh] Termos MeSH primário: Cryptococcus/química
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão
Homocisteína/análogos & derivados
Espectrometria de Massas
Compostos Organosselênicos
Selênio
Compostos de Selênio
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4,4'-selenobis(2-aminobutanoic acid)); 0 (Organoselenium Compounds); 0 (Selenium Compounds); 0LVT1QZ0BA (Homocysteine); H6241UJ22B (Selenium)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170803
[St] Status:MEDLINE


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[PMID]:28757135
[Au] Autor:Zheng X; Xu W; Sun R; Yin H; Dong C; Zeng H
[Ad] Endereço:State Key Laboratory of Natural and Biomimetic Drugs, Beijing, PR China; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
[Ti] Título:Synergism between thioredoxin reductase inhibitor ethaselen and sodium selenite in inhibiting proliferation and inducing death of human non-small cell lung cancer cells.
[So] Source:Chem Biol Interact;275:74-85, 2017 Sep 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:New effective treatment for human non-small cell lung cancer (NSCLC) is needed. The thioredoxin (Trx) system composes of thioredoxin reductase (TrxR), Trx and NADPH. In this study, we combined an organic selenium compound--TrxR inhibitor ethaselen (BBSKE) with low dosage sodium selenite to inhibit proliferation and induce death of NSCLC cells, and identified underlying mechanisms. Synergistic anti-proliferation effect of BBSKE and selenite was found in human NSCLC cell lines, A549, NCI-H1299 and NCI-1266. A significant increase of apoptosis, necrosis and autophagy were observed in the group of BBSKE plus selenite in A549 cells. The autophagy induced by BBSKE and selenite inhibited apoptosis and necrosis. In addition, BBSKE plus selenite induced G2/M arrest, which was verified by the alteration of gene and protein expression of cell cycle regulatory complexes. The intracellular enzyme activity of TrxR was remarkably decreased by cotreatment of BBSKE and selenite. Besides, the mRNA and protein level of TrxR1 and Trx1 were significantly inhibited by cotreatment of BBSKE and selenite. HEK 293 cells overexpressing TrxR1 were more sensitive to BBSKE plus selenite. The nuclear translocation of Trx1 and Ref-1, as well as expression of Ref-1 and AP-1 were inhibited by combination treatment. In short, BBSKE synergizes selenite in inhibiting proliferation and inducing death of NSCLC cells; BBSKE combined with selenite may be a treatment strategy for NSCLC.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia
Compostos Organosselênicos/farmacologia
Selenito de Sódio/farmacologia
Tiorredoxina Dissulfeto Redutase/antagonistas & inibidores
[Mh] Termos MeSH secundário: Células A549
Antineoplásicos/química
Antineoplásicos/farmacologia
Autofagia/efeitos dos fármacos
Compostos Bicíclicos Heterocíclicos com Pontes/química
Carcinoma Pulmonar de Células não Pequenas/metabolismo
Carcinoma Pulmonar de Células não Pequenas/patologia
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Sinergismo Farmacológico
Células HEK293
Seres Humanos
Neoplasias Pulmonares/metabolismo
Neoplasias Pulmonares/patologia
Proteínas Associadas aos Microtúbulos/metabolismo
Compostos Organosselênicos/química
Proteínas de Ligação a RNA/metabolismo
Selenito de Sódio/química
Tiorredoxina Dissulfeto Redutase/metabolismo
Tiorredoxinas/genética
Tiorredoxinas/metabolismo
Fator de Transcrição AP-1/genética
Fator de Transcrição AP-1/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane); 0 (Antineoplastic Agents); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (MAP1LC3B protein, human); 0 (Microtubule-Associated Proteins); 0 (Organoselenium Compounds); 0 (P62 protein, human); 0 (RNA-Binding Proteins); 0 (Transcription Factor AP-1); 52500-60-4 (Thioredoxins); EC 1.8.1.9 (Thioredoxin-Disulfide Reductase); HIW548RQ3W (Sodium Selenite)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170801
[St] Status:MEDLINE


  9 / 2550 MEDLINE  
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[PMID]:28739132
[Au] Autor:Liu L; Wang X; Yang J; Bai Y
[Ad] Endereço:Chemistry Department, Jinan University, Guangzhou 510632, PR China.
[Ti] Título:Colorimetric sensing of selenocystine using gold nanoparticles.
[So] Source:Anal Biochem;535:19-24, 2017 Oct 15.
[Is] ISSN:1096-0309
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We present a highly selective and sensitive colorimetric method for the detection of selenocystine (SeCys) coexisting with other amino acids, especially cysteine (Cys) using the gold nanoparticles (AuNPs). Firstly, Cys was oxidized to cystine (Cys-Cys) by dissolved oxygen under Cu catalysis in the pre-reaction, which eliminated the interference of Cys in the SeCys sensing process. Then SeCys induced the rapid aggregation of AuNPs through Au-Se bond and complex formation of Cu -SeCys in the colorimetric reaction, in which the color change of AuNPs from red to blue or purple with the naked eye detection or with a UV-vis spectrophotometric determination. The concentration of SeCys was quantified by the value at 670 nm from the second-derivative SPR absorbance spectrum. The linear range was from 2 µM to 14 µM with correlation coefficient of 0.999 and a detection limit (LOD) was 0.14 µM. Moreover, the colorimetric response of AuNPs exhibited remarkable specificity to SeCys coexisting with 18 amino acids in a simulation sample, in which the total concentration of Cys and Cys-Cys was less than 15 µM and the each concentration of other 16 common amino acids was 10 µM.
[Mh] Termos MeSH primário: Colorimetria
Cistina/análogos & derivados
Ouro/química
Nanopartículas Metálicas/química
Compostos Organosselênicos/análise
[Mh] Termos MeSH secundário: Cistina/análise
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Organoselenium Compounds); 1464-43-3 (selenocystine); 48TCX9A1VT (Cystine); 7440-57-5 (Gold)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170726
[St] Status:MEDLINE


  10 / 2550 MEDLINE  
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[PMID]:28728108
[Au] Autor:Roldán-Peña JM; Alejandre-Ramos D; López Ó; Maya I; Lagunes I; Padrón JM; Peña-Altamira LE; Bartolini M; Monti B; Bolognesi ML; Fernández-Bolaños JG
[Ad] Endereço:Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Apartado 1203, E-41071 Seville, Spain.
[Ti] Título:New tacrine dimers with antioxidant linkers as dual drugs: Anti-Alzheimer's and antiproliferative agents.
[So] Source:Eur J Med Chem;138:761-773, 2017 Sep 29.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:We have designed a series of tacrine-based homo- and heterodimers that incorporate an antioxidant tether (selenoureido, chalcogenide) as new dual compounds: for the treatment of Alzheimer's disease and as antiproliferative agents. Symmetrical homodimers bearing a dichalcogenide or selenide-based tether, the best compounds in the series, were found to be strong and highly selective electric eel AChE inhibitors, with inhibition constants within the low nanomolar range. This high inhibitory activity was confirmed on recombinant human AChE for the most interesting derivatives. The three most promising homodimers also showed a good inhibitory activity towards amyloid-ß self aggregation. The symmetric disulfide derivative bis[5-(1',2',3',4'-tetrahydroacridin-9'-ylamino)pentyl]disulfide (19) showed the best multipotent profile and was not neurotoxic on immortalized mouse cortical neurons even at 50 µM concentration. These results represent an improvement in activity and selectivity compared to parent tacrine, the first marketed drug against Alzheimer's disease. Title compounds also exhibited excellent in vitro antiproliferative activities against a panel of 6 human tumor cell lines, with GI values within the submicromolar range for the most potent derivatives (0.12-0.95 µM); such values represent a spectacular increase compared to currently-used chemotherapeutic agents, such as 5-FU (up to 306-fold) and cisplatin (up to 162-fold). Cell cycle experiments indicated the accumulation of cells in the G phase of the cycle, a different mechanism than the reported for cisplatin. The breast cancer cell lines turned out to be the most sensitive one of the panel tested.
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Antineoplásicos/farmacologia
Antioxidantes/farmacologia
Calcogênios/farmacologia
Inibidores da Colinesterase/farmacologia
Compostos Organosselênicos/farmacologia
Tacrina/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Peptídeos beta-Amiloides/antagonistas & inibidores
Peptídeos beta-Amiloides/metabolismo
Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Antioxidantes/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Calcogênios/química
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Dimerização
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Camundongos
Estrutura Molecular
Compostos Organosselênicos/química
Fragmentos de Peptídeos/antagonistas & inibidores
Fragmentos de Peptídeos/metabolismo
Agregados Proteicos/efeitos dos fármacos
Relação Estrutura-Atividade
Tacrina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Chalcogens); 0 (Cholinesterase Inhibitors); 0 (Organoselenium Compounds); 0 (Peptide Fragments); 0 (Protein Aggregates); 0 (amyloid beta-protein (1-42)); 4VX7YNB537 (Tacrine); EC 3.1.1.7 (Acetylcholinesterase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170721
[St] Status:MEDLINE



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