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[PMID]: 29195215 [Au] Autor: Mondal A; De S; Maiti S; Sarkar B; Sk AK; Jacob R; Moorthy A; Paira P [Ad] Endereço: Department of Chemistry, School of advanced sciences, VIT University, Vellore 632014, India. [Ti] Título: Amberlite IR-120 (H) mediated "on water" synthesis of fluorescent Ruthenium(II)-arene 8-hydroxyquinoline complexes for cancer therapy and live cell imaging. [So] Source: J Photochem Photobiol B;178:380-394, 2018 Jan. [Is] ISSN: 1873-2682 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: A series of Ruthenium-Quinolinol complexes (3a-d &4a-d) has been synthesized by employing a simple, efficient and environmental friendly condition. Catalytic role of Amberlite IRA-120(H) has been demonstrated. The structures of the new compounds were elucidated by the analysis of spectroscopic data. The stability of these complexes was measured by UV spectroscopy & time dependent NMR spectroscopy. These newly developed complexes were represented as potential anticancer agent against human breast carcinoma cell line (MCF-7), human Epitheloid Cervix Carcinoma (HeLa), human lung adenocarcinoma epithelial cell line (A549) and human colon cancer cell line (Caco-2). Most of the ruthenium complexes showed higher anticancer activity in MCF-7, HeLa and Caco-2 cell lines than cisplatin. A high selectivity (9-28 folds) was observed with these newly developed organoruthenium compounds in human cancer cell lines (MCF-7, HeLa and Caco-2) with respect to normal fibroblast cell line (MRC-5). Complex [(η6-hexamethylbenzene)RuCl(κ2-O,N-5-chloro-HyQ)]·Cl (4b), [(η6-hexamethylbenzene)RuCl(κ2-O,N-5,7-dibromo-HyQ)]·Cl (4c) and [(η6-hexamethylbenzene)RuCl(κ2-O,N-5-chloro-7-iodo-HyQ)]·Cl (4d) exhibited best cytotoxicity profiles in three reported human cancer cell lines (MCF-7, HeLa, Caco-2). Cellular imaging study was also performed with these newly developed organoruthenium compounds. Compound 4c might be utilized for cancer theranostic agents because of its significant quantum yield in water, high potency, selectivity and high cellular uptake in cancer cell lines. [Mh] Termos MeSH primário: Antineoplásicos/síntese química Complexos de Coordenação/síntese química Poliestirenos/química Rutênio/química Água/química [Mh] Termos MeSH secundário: Antineoplásicos/uso terapêutico Antineoplásicos/toxicidade Sítios de Ligação Células CACO-2 Linhagem Celular Tumoral Sobrevivência Celular/efeitos dos fármacos Complexos de Coordenação/uso terapêutico Complexos de Coordenação/toxicidade DNA/química DNA/metabolismo Células HeLa Seres Humanos Concentração Inibidora 50 Células MCF-7 Neoplasias/tratamento farmacológico Neoplasias/patologia Oxiquinolina/química Ligação Proteica Soroalbumina Bovina/química Soroalbumina Bovina/metabolismo Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antineoplastic Agents); 0 (Coordination Complexes); 0 (Polystyrenes); 059QF0KO0R (Water); 27432CM55Q (Serum Albumin, Bovine); 5UTX5635HP (Oxyquinoline); 7UI0TKC3U5 (Ruthenium); 9002-23-7 (Amberlite IR-120); 9007-49-2 (DNA) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180212 [Lr] Data última revisão: 180212 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171202 [St] Status: MEDLINE

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[PMID]: 29178995 [Au] Autor: Das S; Chatterjee S; Pramanik S; Devi PS; Kumar GS [Ad] Endereço: Sensor and Actuator Division, CSIR-Central Glass and Ceramic Research Institute, Kolkata 700032, India. [Ti] Título: A new insight into the interaction of ZnO with calf thymus DNA through surface defects. [So] Source: J Photochem Photobiol B;178:339-347, 2018 Jan. [Is] ISSN: 1873-2682 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: Experimental evidences on the binding interaction of ZnO and Calf Thymus (CT) DNA using several biophysical techniques are the centre of interest of the present study. The interaction of ZnO with CT DNA has been investigated in detail by absorption spectral study, fluorescence titration, Raman analysis, zeta potential measurement, viscometric experiment along with thermal melting study and microscopic analysis. Steady-state fluorescence study revealed the quenching (48%) of the surface defect related peak intensity of ZnO on interaction with DNA. The optimized concentration of ZnO and DNA to obtain this level of quenching has been found to be 0.049mM and 1.027µM, respectively. Additional fluorescence study with 8-hydroxy-5-quinoline (HQ) as a fluorescence probe for Zn ruled out the dissolution effect of ZnO under the experimental conditions. DNA conjugation on the surface of ZnO was also supported by Raman study. The quantitative variation in conductivity as well as electrophoretic mobility indicated significant interaction of ZnO with the DNA molecule. Circular dichroism (CD) and viscometry titrations provided clear evidence in support of the conformational retention of the DNA on interaction with ZnO. The binding interaction was found to be predominantly entropy driven in nature. The bio-physical studies presented in this paper exploring ZnO-CT DNA interaction could add a new horizon to understand the interaction between metal oxide and DNA. [Mh] Termos MeSH primário: DNA/química Óxido de Zinco/química [Mh] Termos MeSH secundário: Animais Calorimetria Bovinos Dicroísmo Circular Ensaio de Desvio de Mobilidade Eletroforética Microscopia Eletrônica de Transmissão Oxiquinolina/química Espectrometria de Fluorescência Análise Espectral Raman Propriedades de Superfície Termodinâmica Viscosidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 5UTX5635HP (Oxyquinoline); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA); SOI2LOH54Z (Zinc Oxide) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180212 [Lr] Data última revisão: 180212 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171128 [St] Status: MEDLINE

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[PMID]: 28403890 [Au] Autor: Kubista B; Schoefl T; Mayr L; van Schoonhoven S; Heffeter P; Windhager R; Keppler BK; Berger W [Ad] Endereço: Department of Orthopedics, Medical University of Vienna, Waehringerguertel 18-20, A-1090, Vienna, Austria. [Ti] Título: Distinct activity of the bone-targeted gallium compound KP46 against osteosarcoma cells - synergism with autophagy inhibition. [So] Source: J Exp Clin Cancer Res;36(1):52, 2017 Apr 12. [Is] ISSN: 1756-9966 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: Osteosarcoma is the most frequent primary malignant bone tumor. Although survival has distinctly increased due to neoadjuvant chemotherapy in the past, patients with metastatic disease and poor response to chemotherapy still have an adverse prognosis. Hence, development of new therapeutic strategies is still of utmost importance. METHODS: Anticancer activity of KP46 against osteosarcoma cell models was evaluated as single agent and in combination approaches with chemotherapeutics and Bcl-2 inhibitors using MTT assay. Underlying mechanisms were tested by cell cycle, apoptosis and autophagy assays. RESULTS: KP46 exerted exceptional anticancer activity at the nanomolar to low micromolar range, depending on the assay format, against all osteosarcoma cell models with minor but significant differences in IC values. KP46 treatment of osteosarcoma cells caused rapid loss of cell adhesion, weak cell cycle accumulation in S-phase and later signs of apoptotic cell death. Furthermore, already at sub-cytotoxic concentrations KP46 reduced the migratory potential of osteosarcoma cells and exerted synergistic effects with cisplatin, a standard osteosarcoma chemotherapeutic. Moreover, the gallium compound induced signs of autophagy in osteosarcoma cells. Accordingly, blockade of autophagy by chloroquine but also by the Bcl-2 inhibitor obatoclax increased the cytotoxic activity of KP46 treatment significantly, suggesting autophagy induction as a protective mechanism against KP46. CONCLUSION: Together, our results identify KP46 as a new promising agent to supplement standard chemotherapy and possible future targeted therapy in osteosarcoma. [Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia Neoplasias Ósseas/tratamento farmacológico Compostos Organometálicos/farmacologia Osteossarcoma/tratamento farmacológico Oxiquinolina/análogos & derivados [Mh] Termos MeSH secundário: Autofagia/efeitos dos fármacos Neoplasias Ósseas/patologia Ciclo Celular/efeitos dos fármacos Linhagem Celular Tumoral Movimento Celular/efeitos dos fármacos Ensaios de Seleção de Medicamentos Antitumorais Sinergismo Farmacológico Seres Humanos Terapia de Alvo Molecular Compostos Organometálicos/administração & dosagem Osteossarcoma/patologia Oxiquinolina/administração & dosagem Oxiquinolina/farmacologia Pirróis/administração & dosagem [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Organometallic Compounds); 0 (Pyrroles); 0 (tris(8-quinolinolato)gallium (III)); 5UTX5635HP (Oxyquinoline); QN4128B52A (obatoclax) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170414 [St] Status: MEDLINE [do] DOI: 10.1186/s13046-017-0527-z

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[PMID]: 28223069 [Au] Autor: Houdkova M; Rondevaldova J; Doskocil I; Kokoska L [Ad] Endereço: Department of Crop Sciences and Agroforestry, Faculty of Tropical AgriSciences, Czech University of Life Sciences Prague, Kamycka 129, 165 21 Praha 6 - Suchdol, Czech Republic. [Ti] Título: Evaluation of antibacterial potential and toxicity of plant volatile compounds using new broth microdilution volatilization method and modified MTT assay. [So] Source: Fitoterapia;118:56-62, 2017 Apr. [Is] ISSN: 1873-6971 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: With aim to develop effective proof-of-concept approach which can be used in a development of new preparations for the inhalation therapy, we designed a new screening method for simple and rapid simultaneous determination of antibacterial potential of plant volatiles in the liquid and the vapour phase at different concentrations. In addition, EVA (ethylene vinyl acetate) capmat™ as vapour barrier cover was used as reliable modification of thiazolyl blue tetrazolium bromide (MTT) assay for cytotoxicity testing of volatiles on microtiter plates. Antibacterial activity of carvacrol, cinnamaldehyde, eugenol, 8-hydroxyquinoline, thymol and thymoquinone was determined against Haemophilus influenzae, Staphylococcus aureus, and Streptococcus pneumoniae using new broth microdilution volatilization method. The cytotoxicity of these compounds was evaluated using MTT test in lung fibroblast cells MRC-5. The most effective antibacterial agents were 8-hydroxyquinoline and thymoquinone with the lowest minimum inhibitory concentrations (MICs) ranging from 2 to 128µg/mL, but they also possessed the highest toxicity in lung cell lines with half maximal inhibitory concentration (IC ) values 0.86-2.95µg/mL. The lowest cytotoxicity effect was identified for eugenol with IC 295.71µg/mL, however this compound produced only weak antibacterial potency with MICs 512-1024µg/mL. The results demonstrate validity of our novel broth microdilution volatilization method, which allows cost and labour effective high-throughput antimicrobial screening of volatile agents without need of special apparatus. In our opinion, this assay can also potentially be used for development of various medicinal, agricultural, and food applications that are based on volatile antimicrobials. [Mh] Termos MeSH primário: Antibacterianos/química Testes de Sensibilidade Microbiana/métodos Compostos Fitoquímicos/química Compostos Orgânicos Voláteis/química Volatilização [Mh] Termos MeSH secundário: Acroleína/análogos & derivados Acroleína/química Benzoquinonas/química Linhagem Celular Eugenol/química Haemophilus influenzae/efeitos dos fármacos Seres Humanos Monoterpenos/química Oxiquinolina/química Staphylococcus aureus/efeitos dos fármacos Streptococcus pneumoniae/efeitos dos fármacos Sais de Tetrazólio Tiazóis Timol/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 0 (Benzoquinones); 0 (Monoterpenes); 0 (Phytochemicals); 0 (Tetrazolium Salts); 0 (Thiazoles); 0 (Volatile Organic Compounds); 3J50XA376E (Thymol); 3T8H1794QW (Eugenol); 490-91-5 (thymoquinone); 5UTX5635HP (Oxyquinoline); 7864XYD3JJ (Acrolein); 9B1J4V995Q (carvacrol); EUY85H477I (thiazolyl blue); SR60A3XG0F (cinnamic aldehyde) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170425 [Lr] Data última revisão: 170425 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170223 [St] Status: MEDLINE

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[PMID]: 28007502 [Au] Autor: Poloznikov AA; Zakhariants AA; Nikulin SV; Smirnova NA; Hushpulian DM; Gaisina IN; Tonevitsky AG; Tishkov VI; Gazaryan IG [Ad] Endereço: D. Rogachev Federal Scientific and Clinical Center for Pediatric Hematology, Oncology, and Immunology, Samory Mashela 1, 117997, Moscow, Russia. Electronic address: andrey.poloznikov@gmail.com. [Ti] Título: Structure-activity relationship for branched oxyquinoline HIF activators: Effect of modifications to phenylacetamide "tail". [So] Source: Biochimie;133:74-79, 2017 Feb. [Is] ISSN: 1638-6183 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: HIF prolyl hydroxylase is a major regulator of HIF stability. Branched tail oxyquinolines have been identified as specific inhibitors of HIF prolyl hydroxylase and recently demonstrated clear benefits in various scenarios of neuronal failure. The structural optimization for branched tail oxyquinolines containing an acetamide bond has been performed in the present study using HIF1 ODD-luc reporter assay. The special attention has been paid to the length of a linker between acetamide group and phenyl ring, as well as substitutions in the phenyl ring in the other branch of the tail. The optimized version of branched tail oxyquinolines is 3-fold more potent than the original one identified before and shows a submicromolar EC in the reporter assay. The compounds have been studied in a "liver-on-a-chip" device to question their hepatotoxicity towards differentiated human HepaRG "hepatocytes": the absence of hepatotoxicity is observed up to 200 µM concentrations for all studied derivatives of branched tail oxyquinolines. [Mh] Termos MeSH primário: Subunidade alfa do Fator 1 Induzível por Hipóxia/biossíntese Prolina Dioxigenases do Fator Induzível por Hipóxia/biossíntese Oxiquinolina/química [Mh] Termos MeSH secundário: Acetamidas/química Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos Hepatócitos/efeitos dos fármacos Hepatócitos/enzimologia Seres Humanos Subunidade alfa do Fator 1 Induzível por Hipóxia/química Prolina Dioxigenases do Fator Induzível por Hipóxia/antagonistas & inibidores Neurônios/efeitos dos fármacos Neurônios/metabolismo Oxiquinolina/farmacologia Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Acetamides); 0 (Hypoxia-Inducible Factor 1, alpha Subunit); 5UTX5635HP (Oxyquinoline); 8XOE1JSO29 (acetamide); EC 1.14.11.29 (Hypoxia-Inducible Factor-Proline Dioxygenases) [Em] Mês de entrada: 1701 [Cu] Atualização por classe: 170130 [Lr] Data última revisão: 170130 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161224 [St] Status: MEDLINE

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[PMID]: 27936245 [Au] Autor: Skrivanova E; Van Immerseel F; Hovorkova P; Kokoska L [Ad] Endereço: Department of Physiology of Nutrition and Quality of Animal Products, Institute of Animal Science, Prague, Czech Republic. [Ti] Título: In Vitro Selective Growth-Inhibitory Effect of 8-Hydroxyquinoline on Clostridium perfringens versus Bifidobacteria in a Medium Containing Chicken Ileal Digesta. [So] Source: PLoS One;11(12):e0167638, 2016. [Is] ISSN: 1932-6203 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Clostridium perfringens-induced necrotic enteritis is generally controlled by antibiotics. However, because of increasing antibiotic resistance, other antibacterial agents are required, preferably ones that do not affect the beneficial intestinal microbiota of the host. This study evaluated the in vitro selective growth-inhibitory effect of 8-hydroxyquinoline (8HQ) on C. perfringens vs. bifidobacteria in a medium containing chicken ileal digesta. Prior to the experiments, the minimum inhibitory concentrations of 8HQ and penicillin G were determined by broth microdilution assay. The minimum inhibitory concentration values of 8HQ for C. perfringens were 16-32 times lower than the values for bifidobacteria. Treatment of autoclaved and non-autoclaved chicken ileal digesta with 8HQ showed a selective anticlostridial effect. After incubation of C. perfringens with autoclaved ileal digesta for 3 h, all 8HQ concentrations tested (32-2048 µg/mL) significantly reduced C. perfringens bacterial count. In contrast, the same treatment had no or only a slight effect on bifidobacteria counts. Unlike 8HQ, penicillin G did not exhibit any selectivity. Similar results were obtained after incubation for 24 h. In non-autoclaved ileal digesta, all 8HQ concentrations tested significantly reduced C. perfringens bacterial counts after incubation for 30 min and 3 h, while no effect was observed on bifidobacteria. These results suggest that 8HQ may serve as a prospective veterinary compound for use against necrotic enteritis in poultry. [Mh] Termos MeSH primário: Antibacterianos/farmacologia Bifidobacterium/efeitos dos fármacos Galinhas/microbiologia Infecções por Clostridium/veterinária Clostridium perfringens/efeitos dos fármacos Oxiquinolina/farmacologia Doenças das Aves Domésticas/prevenção & controle [Mh] Termos MeSH secundário: Animais Infecções por Clostridium/prevenção & controle Infecções por Clostridium/virologia Íleo/microbiologia Doenças das Aves Domésticas/virologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 5UTX5635HP (Oxyquinoline) [Em] Mês de entrada: 1707 [Cu] Atualização por classe: 170706 [Lr] Data última revisão: 170706 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161210 [St] Status: MEDLINE [do] DOI: 10.1371/journal.pone.0167638

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[PMID]: 27862215 [Au] Autor: Kiss R; Bajusz D; Baskin R; Tóth K; Monostory K; Sayeski PP; Keseru GM [Ad] Endereço: MTA-TTK-NAP B - Drug Discovery Research Group - Neurodegenerative Diseases, Research Center for Natural Sciences, Hungarian Academy of Sciences, Budapest, Hungary. [Ti] Título: Identification of 8-Hydroxyquinoline Derivatives Active Against Somatic V658F Mutant JAK1-Dependent Cells. [So] Source: Arch Pharm (Weinheim);349(12):925-933, 2016 Dec. [Is] ISSN: 1521-4184 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: Janus kinases (JAKs) and their gain-of-function mutants have been implicated in a range of oncological, inflammatory, and autoimmune conditions, which has sparked great research interest in the discovery and development of small-molecule JAK inhibitors. Two molecules are currently marketed as JAK inhibitors, but due to the displayed side effects (owing to their suboptimal selectivities among the various JAK subtypes) new JAK inhibitors are still sought after. We present the results of an extensive virtual screening campaign based on a multi-step screening protocol involving ligand docking. The screening yielded five new, experimentally validated inhibitors of JAK1 with 8-hydroxyquinoline as a novel hinge-binding scaffold. The compounds did not only display favorable potencies in a JAK1 -driven cell-based assay but were also shown to be non-cytotoxic on rat liver cells. [Mh] Termos MeSH primário: Janus Quinase 1/antagonistas & inibidores Oxiquinolina/análogos & derivados Oxiquinolina/farmacologia [Mh] Termos MeSH secundário: Animais Morte Celular/efeitos dos fármacos Células Cultivadas Camundongos Simulação de Acoplamento Molecular Mutação Oxiquinolina/síntese química Inibidores de Proteínas Quinases/síntese química Inibidores de Proteínas Quinases/farmacologia Ratos Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Protein Kinase Inhibitors); 5UTX5635HP (Oxyquinoline); EC 2.7.10.2 (Janus Kinase 1) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170421 [Lr] Data última revisão: 170421 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161119 [St] Status: MEDLINE [do] DOI: 10.1002/ardp.201600246

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[PMID]: 27802609 [Au] Autor: Heid E; Schröder C [Ad] Endereço: Faculty of Chemistry, Department of Computational Biological Chemistry, University of Vienna, Währingerstraße 19, A-1090 Vienna, Austria. [Ti] Título: Computational solvation dynamics of oxyquinolinium betaine linked to trehalose. [So] Source: J Chem Phys;145(16):164507, 2016 Oct 28. [Is] ISSN: 1089-7690 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Studying the changed water dynamics in the hydration layers of biomolecules is an important step towards fuller understanding of their function and mechanisms, but has shown to be quite difficult. The measurement of the time-dependent Stokes shift of a chromophore attached to the biomolecule is a promising method to achieve this goal, as published in Sajadi et al. [J. Phys. Chem. Lett., 5, 1845 (2014).] where trehalose was used as biomolecule, 1-methyl-6-oxyquinolinium betaine as chromophore, and water as solvent. An overall retardation of solvent molecules is then obtained by comparison of the linked system to the same system without trehalose, but contributions from different subgroups of solvent molecules, for example, molecules close to or far from trehalose, are unknown. The difficulty arising from these unknown contributions of retarded and possibly unretarded solvent molecules is overcome in this work by conducting computer simulations on this system and decomposing the overall signal into the contributions from various molecules at different locations. We performed non-equilibrium molecular dynamics simulation using a polarizable water model and a non-polarizable solute model and could reproduce the experimental time-dependent Stokes shift accurately for the linked trehalose-oxyquinolinium and the pure oxyquinolinium over a wide temperature range, indicating the correctness of our employed models. Decomposition of the shift into contributions from different solvent subgroups showed that the amplitude of the measured shift is made up only half by the desired retarded solvent molecules in the hydration layer, but to another half by unretarded bulk water, so that measured relaxation times of the overall Stokes shift are only a lower boundary for the true relaxation times in the hydration layer of trehalose. As a side effect, the results on the effect of trehalose on solvation dynamics contribute to the long standing debate on the range of influence of trehalose on water dynamics, the number of retarded solvent molecules, and the observed retardation factor when compared to bulk water. [Mh] Termos MeSH primário: Betaína/química Simulação de Dinâmica Molecular Oxiquinolina/química Trealose/química [Mh] Termos MeSH secundário: Modelos Biológicos Soluções Solventes/química Temperatura Ambiente Água/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Solutions); 0 (Solvents); 059QF0KO0R (Water); 3SCV180C9W (Betaine); 5UTX5635HP (Oxyquinoline); B8WCK70T7I (Trehalose) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170406 [Lr] Data última revisão: 170406 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161103 [St] Status: MEDLINE

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[PMID]: 27432762 [Au] Autor: Jampilek J; Kralova K; Pesko M; Kos J [Ad] Endereço: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 832 32 Bratislava, Slovakia. [Ti] Título: Ring-substituted 8-hydroxyquinoline-2-carboxanilides as photosystem II inhibitors. [So] Source: Bioorg Med Chem Lett;26(16):3862-5, 2016 08 15. [Is] ISSN: 1464-3405 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Ring-substituted 8-hydroxyquinoline-2-carboxanilides inhibited photosynthetic electron transport (PET) through photosystem (PS) II. Their inhibitory efficiency depended on the compound lipophilicity, the electronic properties of the substituent R and the position of the substituent R on the benzene ring. The most effective inhibitors showing IC50 values in the range 2.3-3.6µM were substituted in C'(3) by F, CH3, Cl and Br. The dependence of the PET-inhibiting activity on the lipophilicity of the compounds was quasi-parabolic for 3-substituted derivatives, while for C'(2) ones a slight increase and for C'(4) derivatives a sharp decrease of the activity were observed with increasing lipophilicity. In addition, the dependence of PET-inhibiting activity on electronic Hammett's σ parameter of the substituent R was observed with optimum σ value 0.06 for C'(4) and 0.34 for C'(3) substituted derivatives, while the value of σ parameter did not significantly influence the PET-inhibiting activity of C'(2) substituted compounds. Interactions of the studied compounds with chlorophyll a and aromatic amino acids present in the pigment-protein complexes mainly in PS II were documented by fluorescence spectroscopy. The section between P680 and plastoquinone QB occurring on the acceptor side of PS II can be suggested as the site of action of the compounds. [Mh] Termos MeSH primário: Anilidas/química Oxiquinolina/química Complexo de Proteína do Fotossistema II/antagonistas & inibidores [Mh] Termos MeSH secundário: Anilidas/síntese química Anilidas/metabolismo Clorofila/química Cloroplastos/metabolismo Transporte de Elétrons Fotossíntese Complexo de Proteína do Fotossistema II/metabolismo Ligação Proteica Espectrometria de Fluorescência Spinacia oleracea/metabolismo Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Anilides); 0 (Photosystem II Protein Complex); 1406-65-1 (Chlorophyll); 5UTX5635HP (Oxyquinoline); YF5Q9EJC8Y (chlorophyll a) [Em] Mês de entrada: 1707 [Cu] Atualização por classe: 171122 [Lr] Data última revisão: 171122 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160720 [St] Status: MEDLINE

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[PMID]: 27431227 [Au] Autor: Shah S; Dalecki AG; Malalasekera AP; Crawford CL; Michalek SM; Kutsch O; Sun J; Bossmann SH; Wolschendorf F [Ad] Endereço: Department of Medicine, Division of Infectious Diseases, University of Alabama at Birmingham, Birmingham, Alabama, USA. [Ti] Título: 8-Hydroxyquinolines Are Boosting Agents of Copper-Related Toxicity in Mycobacterium tuberculosis. [So] Source: Antimicrob Agents Chemother;60(10):5765-76, 2016 Oct. [Is] ISSN: 1098-6596 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Copper (Cu) ions are likely the most important immunological metal-related toxin utilized in controlling bacterial infections. Impairment of bacterial Cu resistance reduces viability within the host. Thus, pharmacological enhancement of Cu-mediated antibacterial toxicity may lead to novel strategies in drug discovery and development. Screening for Cu toxicity-enhancing antibacterial molecules identified 8-hydroxyquinoline (8HQ) to be a potent Cu-dependent bactericidal inhibitor of Mycobacterium tuberculosis The MIC of 8HQ in the presence of Cu was 0.16 µM for replicating and nonreplicating M. tuberculosis cells. We found 8HQ's activity to be dependent on the presence of extracellular Cu and to be related to an increase in cell-associated labile Cu ions. Both findings are consistent with 8HQ acting as a Cu ionophore. Accordingly, we identified the 1:1 complex of 8HQ and Cu to be its active form, with Zn, Fe, or Mn neither enhancing nor reducing its Cu-specific action. This is remarkable, considering that the respective metal complexes have nearly identical structures and geometries. Finally, we found 8HQ to kill M. tuberculosis selectively within infected primary macrophages. Given the stark Cu-dependent nature of 8HQ activity, this is the first piece of evidence that Cu ions within macrophages may bestow antibacterial properties to a Cu-dependent inhibitor of M. tuberculosis In conclusion, our findings highlight the metal-binding ability of the 8-hydroxyquinoline scaffold to be a potential focus for future medicinal chemistry and highlight the potential of innate immunity-inspired screening platforms to reveal molecules with novel modes of action against M. tuberculosis. [Mh] Termos MeSH primário: Antituberculosos/farmacologia Cobre/farmacologia Mycobacterium tuberculosis/efeitos dos fármacos Oxiquinolina/farmacologia [Mh] Termos MeSH secundário: Animais Antituberculosos/química Células Cultivadas Complexos de Coordenação/farmacologia Cobre/química Modelos Animais de Doenças Sinergismo Farmacológico Feminino Macrófagos Peritoneais/efeitos dos fármacos Macrófagos Peritoneais/microbiologia Camundongos Endogâmicos C57BL Testes de Sensibilidade Microbiana Mycobacterium tuberculosis/patogenicidade Oxiquinolina/química Tuberculose/tratamento farmacológico [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antitubercular Agents); 0 (Coordination Complexes); 5UTX5635HP (Oxyquinoline); 789U1901C5 (Copper) [Em] Mês de entrada: 1707 [Cu] Atualização por classe: 170704 [Lr] Data última revisão: 170704 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160720 [St] Status: MEDLINE [do] DOI: 10.1128/AAC.00325-16

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