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[PMID]:28654200
[Au] Autor:Moraski GC; Bristol R; Seeger N; Boshoff HI; Tsang PS; Miller MJ
[Ad] Endereço:Department of Chemistry and Biochemistry, 103 Chemistry and Biochemistry, Montana State University, Bozeman, MT, 59717, USA.
[Ti] Título:Preparation and Evaluation of Potent Pentafluorosulfanyl-Substituted Anti-Tuberculosis Compounds.
[So] Source:ChemMedChem;12(14):1108-1115, 2017 Jul 20.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The global fight to stop tuberculosis (TB) remains a great challenge, particularly with the increase in drug-resistant strains and a lack of funding to support the development of new treatments. To bolster a precarious drug pipeline, we prepared a focused panel of eight pentafluorosulfanyl (SF ) compounds which were screened for their activity against Mycobacterium tuberculosis (Mtb) H37Rv in three different assay conditions and media. All eight compounds had sub-micromolar potency, and four displayed MICs <100 nm. Seven compounds were evaluated against non-replicating and mono-drug-resistant Mtb, and for their ability to inhibit Mtb within the macrophage. The greatest potency was observed against intracellular Mtb (MIC <10 nm for three compounds), which is often the most challenging to target. In general, the SF -bearing compounds were very similar to their CF counterparts, with the major differences observed being their in vitro ADME properties. Two SF -bearing compounds were found to have greater protein binding than their corresponding CF counterparts, but were also less metabolized in human microsomes, resulting in longer half-lives.
[Mh] Termos MeSH primário: Antituberculosos/síntese química
Imidazóis/síntese química
Mycobacterium tuberculosis/efeitos dos fármacos
Piridinas/síntese química
Ácidos Sulfanílicos/síntese química
[Mh] Termos MeSH secundário: Animais
Antituberculosos/farmacologia
Linhagem Celular
Farmacorresistência Bacteriana
Seres Humanos
Imidazóis/farmacologia
Testes de Sensibilidade Microbiana
Piridinas/farmacologia
Relação Estrutura-Atividade
Ácidos Sulfanílicos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antitubercular Agents); 0 (Imidazoles); 0 (Pyridines); 0 (Sulfanilic Acids)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170628
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700170


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[PMID]:28062945
[Au] Autor:Loos HM; Doucet S; Védrines F; Sharapa C; Soussignan R; Durand K; Sagot P; Buettner A; Schaal B
[Ad] Endereço:Developmental Ethology and Cognitive Psychology Group, Centre des Sciences du Goût et de l'Alimentation, CNRS-Université de Bourgogne, 9E bd Jeanne d'Arc, 21000, Dijon, France. helene.loos@ivv.fraunhofer.de.
[Ti] Título:Responses of Human Neonates to Highly Diluted Odorants from Sweat.
[So] Source:J Chem Ecol;43(1):106-117, 2017 Jan.
[Is] ISSN:1573-1561
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Conjugated forms of odorants contributing to sweat odor occur not only in human sweat but also in amniotic fluid, colostrum, and milk. However, it is unclear whether the released odorants are detected and hedonically discriminated by human newborns. To investigate this issue, we administered highly diluted solutions of (R)/(S)-3-methyl-3-sulfanylhexan-1-ol (MSH), (R)/(S)-3-sulfanylhexan-1-ol (SH), (E)/(Z)-3-methylhex-2-enoic acid (3M2H), and (R)/(S)-3-hydroxy-3-methylhexanoic acid (HMHA) to 3-d-old infants while their respiratory rate and oro-facial movements were recorded. Adult sensitivity to these odorants was assessed via triangle tests. Whereas no neonatal stimulus-specific response was found for respiratory rate, oro-facial reactivity indicated orthonasal detection of MSH and SH by male neonates, and of HMHA by the whole group of neonates. Dependent on the dilution of odorants, newborns evinced neutral responses or longer negative oro-facial expressions compared with the reference stimuli. Finally, newborns appeared to be more sensitive to the target odorants than did adults.
[Mh] Termos MeSH primário: Expressão Facial
Comportamento do Lactente
Odorantes
Olfato/fisiologia
Suor
[Mh] Termos MeSH secundário: Adulto
Caproatos/farmacologia
Feminino
Hexanóis/farmacologia
Seres Humanos
Recém-Nascido
Masculino
Taxa Respiratória/efeitos dos fármacos
Ácidos Sulfanílicos/farmacologia
Compostos de Sulfidrila/farmacologia
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-hydroxy-3-methyl-hexanoic acid); 0 (3-methyl-3-sulfonylhexan-1-ol); 0 (Caproates); 0 (Hexanols); 0 (Sulfanilic Acids); 0 (Sulfhydryl Compounds); U3TIX8Z92N (3-mercaptohexanol)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171027
[Lr] Data última revisão:
171027
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170108
[St] Status:MEDLINE
[do] DOI:10.1007/s10886-016-0804-x


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[PMID]:28049506
[Au] Autor:Al-Khayal K; Alafeefy A; Vaali-Mohammed MA; Mahmood A; Zubaidi A; Al-Obeed O; Khan Z; Abdulla M; Ahmad R
[Ad] Endereço:Colorectal Research Center, Department of Surgery, King Khalid University Hospital College of Medicine, King Saud University, PO BOX 7805 (37), Riyadh, Saudi Arabia.
[Ti] Título:Novel derivative of aminobenzenesulfonamide (3c) induces apoptosis in colorectal cancer cells through ROS generation and inhibits cell migration.
[So] Source:BMC Cancer;17(1):4, 2017 01 03.
[Is] ISSN:1471-2407
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Colorectal cancer (CRC) is the 3 most common type of cancer worldwide. New anti-cancer agents are needed for treating late stage colorectal cancer as most of the deaths occur due to cancer metastasis. A recently developed compound, 3c has shown to have potent antitumor effect; however the mechanism underlying the antitumor effect remains unknown. METHODS: 3c-induced inhibition of proliferation was measured in the absence and presence NAC using MTT in HT-29 and SW620 cells and xCELLigence RTCA DP instrument. 3c-induced apoptotic studies were performed using flow cytometry. 3c-induced redox alterations were measured by ROS production using fluorescence plate reader and flow cytometry and mitochondrial membrane potential by flow cytometry; NADPH and GSH levels were determined by colorimetric assays. Bcl2 family protein expression and cytochrome c release and PARP activation was done by western blotting. Caspase activation was measured by ELISA. Cell migration assay was done using the real time xCELLigence RTCA DP system in SW620 cells and wound healing assay in HT-29. RESULTS: Many anticancer therapeutics exert their effects by inducing reactive oxygen species (ROS). In this study, we demonstrate that 3c-induced inhibition of cell proliferation is reversed by the antioxidant, N-acetylcysteine, suggesting that 3c acts via increased production of ROS in HT-29 cells. This was confirmed by the direct measurement of ROS in 3c-treated colorectal cancer cells. Additionally, treatment with 3c resulted in decreased NADPH and glutathione levels in HT-29 cells. Further, investigation of the apoptotic pathway showed increased release of cytochrome c resulting in the activation of caspase-9, which in turn activated caspase-3 and -6. 3c also (i) increased p53 and Bax expression, (ii) decreased Bcl2 and BclxL expression and (iii) induced PARP cleavage in human colorectal cancer cells. Confirming our observations, NAC significantly inhibited induction of apoptosis, ROS production, cytochrome c release and PARP cleavage. The results further demonstrate that 3c inhibits cell migration by modulating EMT markers and inhibiting TGFß-induced phosphorylation of Smad2 and Samd3. CONCLUSIONS: Our findings thus demonstrate that 3c disrupts redox balance in colorectal cancer cells and support the notion that this agent may be effective for the treatment of colorectal cancer.
[Mh] Termos MeSH primário: Amidas/farmacologia
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Movimento Celular/efeitos dos fármacos
Neoplasias Colorretais/patologia
Espécies Reativas de Oxigênio/metabolismo
Ácidos Sulfanílicos/química
[Mh] Termos MeSH secundário: Caspase 3/metabolismo
Proliferação Celular/efeitos dos fármacos
Neoplasias Colorretais/tratamento farmacológico
Neoplasias Colorretais/metabolismo
Citocromos c/metabolismo
Seres Humanos
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Mitocôndrias/efeitos dos fármacos
Mitocôndrias/metabolismo
Mitocôndrias/patologia
Células Tumorais Cultivadas
Cicatrização/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amides); 0 (Antineoplastic Agents); 0 (Reactive Oxygen Species); 0 (Sulfanilic Acids); 9007-43-6 (Cytochromes c); EC 3.4.22.- (Caspase 3)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171121
[Lr] Data última revisão:
171121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170105
[St] Status:MEDLINE
[do] DOI:10.1186/s12885-016-3005-7


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[PMID]:27851894
[Au] Autor:Hegedus B; Kós PB; Bálint B; Maróti G; Gan HM; Perei K; Rákhely G
[Ad] Endereço:Department of Biotechnology, University of Szeged, Közép fasor 52, H-6726 Szeged, Hungary; Institute of Biophysics, Biological Research Center, Temesvári krt. 62, H-6726 Szeged, Hungary.
[Ti] Título:Complete genome sequence of Novosphingobium resinovorum SA1, a versatile xenobiotic-degrading bacterium capable of utilizing sulfanilic acid.
[So] Source:J Biotechnol;241:76-80, 2017 Jan 10.
[Is] ISSN:1873-4863
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Sulfanilic acid (4-aminobenzenesulfonic acid) is a sulfonated aromatic amine widely used in chemical industries for synthesis of various organic dyes and sulfa drugs. There are quite a few microbial co-cultures or single isolates capable of completely degrading this compound. Novosphingobium resinovorum SA1 was the first single bacterium which could utilize sulfanilic acid as its sole carbon, nitrogen and sulfur source. The strain has versatile catabolic routes for the bioconversion of numerous other aromatic compounds. Here, the complete genome sequence of the N. resinovorum SA1 strain is reported. The genome consists of a circular chromosome of 3.8 Mbp and four extrachromosomal elements between 67 and 1 759.8 kbp in size. Three alternative 3-ketoadipate pathways were identified on the plasmids. Sulfanilic acid is decomposed via a modified 3-ketoadipate pathway and the oxygenases involved form a phylogenetically separate branch on the tree. Sequence analysis of these elements might provide a genetic background for deeper insight into the versatile catabolic metabolism of various aromatic xenobiotics, including sulfanilic acid and its derivatives. Moreover, this is also a good model strain for understanding the role and evolution of multiple genetic elements within a single strain.
[Mh] Termos MeSH primário: Alphaproteobacteria/genética
Genoma Bacteriano/genética
Ácidos Sulfanílicos/metabolismo
[Mh] Termos MeSH secundário: Alphaproteobacteria/metabolismo
DNA Bacteriano/análise
DNA Bacteriano/genética
Análise de Sequência de DNA
Ácidos Sulfanílicos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (DNA, Bacterial); 0 (Sulfanilic Acids)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170228
[Lr] Data última revisão:
170228
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161117
[St] Status:MEDLINE


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[PMID]:27108596
[Au] Autor:Hayase N; Fujikawa Y; Nakagawa K; Ushio K
[Ad] Endereço:a Department of Applied Chemistry and Biotechnology , National Institute of Technology, Niihama College , Niihama , Japan.
[Ti] Título:Isolation and characterization of Bradyrhizobium sp. 224 capable of degrading sulfanilic acid.
[So] Source:Biosci Biotechnol Biochem;80(8):1663-5, 2016 Aug.
[Is] ISSN:1347-6947
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A bacterial strain (strain 224), which has the ability to utilize sulfanilic acid as a sole source of carbon, was isolated from soil. 16S rRNA gene sequence obtained from strain 224 exhibited 100% identical to that of species in the genus Bradyrhizobium. Strain 224 degraded 4.7 mM of sulfanilic acid and released almost the same molar concentration of sulfate ion.
[Mh] Termos MeSH primário: Bradyrhizobium/metabolismo
Corantes/metabolismo
Microbiologia do Solo
Poluentes do Solo/metabolismo
Ácidos Sulfanílicos/metabolismo
[Mh] Termos MeSH secundário: Biodegradação Ambiental
Bradyrhizobium/classificação
Bradyrhizobium/genética
Cinética
Filogenia
RNA Ribossômico 16S/genética
Sulfatos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coloring Agents); 0 (RNA, Ribosomal, 16S); 0 (Soil Pollutants); 0 (Sulfanilic Acids); 0 (Sulfates)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170118
[Lr] Data última revisão:
170118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160426
[St] Status:MEDLINE
[do] DOI:10.1080/09168451.2016.1176521


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[PMID]:26840760
[Au] Autor:Dallo F; Battistel D; Piazza R; Gabrieli J; Filippi JJ; Baldovini N; Barbante C
[Ad] Endereço:Department of Environmental Science, Informatics and Statistics, Ca' Foscari University of Venice, Venice, Italy.
[Ti] Título:Direct immersion solid-phase microextraction with gas chromatography and mass spectrometry for the determination of specific biomarkers of human sweat in melted snow.
[So] Source:J Sep Sci;39(7):1300-9, 2016 Apr.
[Is] ISSN:1615-9314
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:To provide a reliable tool for investigating diffusion processes of the specific components of the human odor 3-hydroxy-3-methylhexanoic acid and 3-methyl-3-sulfanylhexan-1-ol through the snowpack, we developed and optimized an analytical method based on direct immersion solid-phase microextraction followed by gas chromatography with mass spectrometry. Direct immersion solid-phase microextraction was performed using polyacrylate fibers placed in aqueous solutions containing 3-hydroxy-3-methylhexanoic acid and 3-methyl-3-sulfanylhexan-1-ol. After optimization, absorption times of 120 min provided a good balance to shorten the analysis time and to obtain suitable amounts of extractable analytes. The extraction efficiency was improved by increasing the ionic strength of the solution. Although the absolute extraction efficiency ranged between 10 and 12% for 3-hydroxy-3-methylhexanoic acid and 2-3% for 3-methyl-3-sulfanylhexan-1-ol, this method was suitable for analyzing 3-hydroxy-3-methylhexanoic acid and 3-methyl-3-sulfanylhexan-1-ol concentrations of at least 0.04 and 0.20 ng/mL, respectively. The precision of the direct immersion solid-phase microextraction method ranged between 8 and 16%. The variability within a batch of six fibers was 10-18%. The accuracy of the method provided values of 88-95 and 86-101% for 3-hydroxy-3-methylhexanoic acid and 3-methyl-3-sulfanylhexan-1-ol, respectively. The limit of detection (and quantification) was 0.01 ng/mL (0.04 ng/mL) for 3-hydroxy-3-methylhexanoic acid and 0.06 ng/mL (0.20 ng/mL) for 3-methyl-3-sulfanylhexan-1-ol. The signal versus concentration was linear for both compounds (r(2) = 0.973-0.979). The stability of these two compounds showed that 3-hydroxy-3-methylhexanoic acid was more stable in water than 3-methyl-3-sulfanylhexan-1-ol. We applied the method to environmental samples in correspondence with an olfactory target buried previously.
[Mh] Termos MeSH primário: Caproatos/análise
Hexanóis/análise
Neve/química
Microextração em Fase Sólida
Ácidos Sulfanílicos/análise
Suor/química
[Mh] Termos MeSH secundário: Biomarcadores/análise
Cromatografia Gasosa
Congelamento
Seres Humanos
Espectrometria de Massas
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3-hydroxy-3-methyl-hexanoic acid); 0 (3-methyl-3-sulfonylhexan-1-ol); 0 (Biomarkers); 0 (Caproates); 0 (Hexanols); 0 (Sulfanilic Acids)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160204
[St] Status:MEDLINE
[do] DOI:10.1002/jssc.201501097


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[PMID]:26493406
[Au] Autor:Polak J; Jarosz-Wilkolazka A; Szalapata K; Graz M; Osinska-Jaroszuk M
[Ad] Endereço:Department of Biochemistry, Maria Curie-Sklodowska University, Akademicka 19, Lublin 20-031, Poland. Electronic address: jpolak@poczta.umcs.lublin.pl.
[Ti] Título:Laccase-mediated synthesis of a phenoxazine compound with antioxidative and dyeing properties--the optimisation process.
[So] Source:N Biotechnol;33(2):255-62, 2016 Mar 25.
[Is] ISSN:1876-4347
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This study demonstrates the optimisation of the main parameters of the laccase-mediated biosynthesis of high-intensity-coloured orange phenoxazine compound, 2-amino-3-oxo-3H-phenoxazine-8-sulfonic acid, and the antioxidative and dyeing properties. Among optimised parameters were the pH value, the activity of laccase, and the high concentration of the precursor as the necessary step in terms of dye synthesis scale-up. The high concentration of the precursor of ca. 10 g/L can be transformed totally by laccase at the activity of 30 U/g during 12 hours, in an optimised and standardised process in nearly 100% yield of synthesis. The obtained dye exhibited good dyeing properties determined according to the ISO standards. Antioxidative activities were detected for phenoxazinone dye using two independent methods, the chemiluminescence assay and the ABTS free radical-scavenging test, with the values of EC50 for the tested phenoxazine dye amounting 189.8 µg/mL and 1428 µg/mL, respectively. Despite the presence of the phenoxazine core in the structure of this dye, no antibacterial capacity was noted.
[Mh] Termos MeSH primário: Antioxidantes/síntese química
Corantes/síntese química
Proteínas Fúngicas/química
Lacase/química
Oxazinas/síntese química
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antibacterianos/farmacologia
Antioxidantes/química
Corantes/química
Escherichia coli/efeitos dos fármacos
Medições Luminescentes
Oxazinas/química
Oxazinas/farmacologia
Polyporaceae/enzimologia
Staphylococcus aureus/efeitos dos fármacos
Ácidos Sulfanílicos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antioxidants); 0 (Coloring Agents); 0 (Fungal Proteins); 0 (Oxazines); 0 (Sulfanilic Acids); 5857-93-2 (2-amino-4-hydroxybenzenesulfonic acid); C2ZWT499SG (phenoxazine); EC 1.10.3.2 (Laccase)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151024
[St] Status:MEDLINE


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[PMID]:26395182
[Au] Autor:Martins CC; Bassetto CA; Santos JM; Eberlin MN; Magalhães A; Varanda W; Gonzalez ER
[Ad] Endereço:Laboratório de Química Orgânica Fina, Departamento de Física, Química e Biologia, Faculdade de Ciências e Tecnologia, Universidade Estadual Paulista (UNESP), C.P. 467, Presidente Prudente, SP, 19060-900, Brazil.
[Ti] Título:Mass spectrometry study of N-alkylbenzenesulfonamides with potential antagonist activity to potassium channels.
[So] Source:Amino Acids;48(2):445-59, 2016 Feb.
[Is] ISSN:1438-2199
[Cp] País de publicação:Austria
[La] Idioma:eng
[Ab] Resumo:Herein, we report the synthesis and mass spectrometry studies of several N-alkylbenzenesulfonamides structurally related to sulfanilic acid. The compounds were synthesized using a modified Schotten-Baumann reaction coupled with Meisenheimer arylation. Sequential mass spectrometry by negative mode electrospray ionization (ESI(-)-MS/MS) showed the formation of sulfoxylate anion (m/z 65) observed in the mass spectrum of p-chloro-N-alkylbenzenesulfonamides. Investigation of the unexpected loss of two water molecules, as observed by electron ionization mass spectrometry (EI-MS) analysis of p-(N-alkyl)lactam sulfonamides, led to the proposal of corresponding fragmentation pathways. These compounds showed loss of neutral iminosulfane dioxide molecule (M-79) with formation of ions observed at m/z 344 and 377. These ions were formed by rearrangement on ESI(+)-MS/MS analysis. Some of the molecules showed antagonistic activity against Kv3.1 voltage-gated potassium channels.
[Mh] Termos MeSH primário: Antibacterianos/química
Bloqueadores dos Canais de Potássio/química
Canais de Potássio Shaw/efeitos dos fármacos
Ácidos Sulfanílicos/química
Sulfonamidas/química
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Desenho de Drogas
Espectrometria de Massas por Ionização por Electrospray
Sulfonamidas/síntese química
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Potassium Channel Blockers); 0 (Shaw Potassium Channels); 0 (Sulfanilic Acids); 0 (Sulfonamides)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150924
[St] Status:MEDLINE
[do] DOI:10.1007/s00726-015-2099-6


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[PMID]:26344484
[Au] Autor:Rodríguez MP; Pezza HR; Pezza L
[Ad] Endereço:Instituto de Química, Universidade Estadual Paulista "Julio de Mesquita Filho", UNESP, R. Prof. Francisco Degni 55, P.O. Box 355, 14800-900 Araraquara, SP, Brazil.
[Ti] Título:Simple and clean determination of tetracyclines by flow injection analysis.
[So] Source:Spectrochim Acta A Mol Biomol Spectrosc;153:386-92, 2016 Jan 15.
[Is] ISSN:1873-3557
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:An environmentally reliable analytical methodology was developed for direct quantification of tetracycline (TC) and oxytetracycline (OTC) using continuous flow injection analysis with spectrophotometric detection. The method is based on the diazo coupling reaction between the tetracyclines and diazotized sulfanilic acid in a basic medium, resulting in the formation of an intense orange azo compound that presents maximum absorption at 434 nm. Experimental design was used to optimize the analytical conditions. The proposed technique was validated over the concentration range of 1 to 40 µg mL(-1), and was successfully applied to samples of commercial veterinary pharmaceuticals. The detection (LOD) and quantification (LOQ) limits were 0.40 and 1.35 µg mL(-1), respectively. The samples were also analyzed by an HPLC method, and the results showed agreement with the proposed technique. The new flow injection method can be immediately used for quality control purposes in the pharmaceutical industry, facilitating monitoring in real time during the production processes of tetracycline formulations for veterinary use.
[Mh] Termos MeSH primário: Análise de Injeção de Fluxo/métodos
Tetraciclinas/análise
[Mh] Termos MeSH secundário: Colorimetria
Indicadores e Reagentes
Limite de Detecção
Oxitetraciclina/análise
Padrões de Referência
Ácidos Sulfanílicos/química
Tetraciclinas/química
Drogas Veterinárias/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Indicators and Reagents); 0 (Sulfanilic Acids); 0 (Tetracyclines); 0 (Veterinary Drugs); X20I9EN955 (Oxytetracycline)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151125
[Lr] Data última revisão:
151125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150908
[St] Status:MEDLINE


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[PMID]:26681454
[Au] Autor:Xie XQ; Yang P; Zhang Y; Zhang P; Wang L; Ding Y; Yang M; Tong Q; Cheng H; Ji Q; McGuire T; Yuan W; Cheng T; Gao Y
[Ad] Endereço:Department of Pharmaceutical Sciences and Computational Chemical Genomics Screening Center, School of Pharmacy; NIH National Center of Excellence for Computational Drug Abuse Research; Drug Discovery Institute; Departments of Computational Biology and Structural Biology, School of Medicine, Universi
[Ti] Título:Discovery of novel INK4C small-molecule inhibitors to promote human and murine hematopoietic stem cell ex vivo expansion.
[So] Source:Sci Rep;5:18115, 2015 Dec 18.
[Is] ISSN:2045-2322
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Hematopoietic stem cells (HSCs) have emerged as promising therapeutic cell sources for high-risk hematological malignancies and immune disorders. However, their clinical use is limited by the inability to expand these cells ex vivo. Therefore, there is an urgent need to identify specific targets and effective probes that can expand HSCs. Here we report a novel class of INK4C (p18(INK4C) or p18) small molecule inhibitors (p18SMIs), which were initially found by in silico 3D screening. We identified a lead p18 inhibitor, XIE18-6, confirmed its p18-targeting specificity and bioactivity of promoting HSCs expansion, and then performed structure-activity relationship (SAR) studies by synthesizing a series of analogs of XIE18-6. Among these, compound 40 showed the most potent bioactivity in HSCs expansion (ED50 = 5.21 nM). We confirmed that compound 40 promoted expansion of both murine and human HSCs, and also confirmed its p18-targeting specificity. Notably, compound 40 did not show significant cytotoxicity toward 32D cells or HSCs, nor did it augment leukemia cell proliferation. Taken together, our newly discovered p18SMIs represent novel chemical agents for murine and human HSCs ex vivo expansion and also can be used as valuable chemical probes for further HSC biology research towards promising utility for therapeutic purposes.
[Mh] Termos MeSH primário: Cumarínicos/química
Inibidor de Quinase Dependente de Ciclina p18/metabolismo
Bibliotecas de Moléculas Pequenas/química
Ácidos Sulfanílicos/química
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Células da Medula Óssea/citologia
Células da Medula Óssea/metabolismo
Diferenciação Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Células Cultivadas
Cumarínicos/metabolismo
Cumarínicos/toxicidade
Quinase 4 Dependente de Ciclina/metabolismo
Quinase 6 Dependente de Ciclina/metabolismo
Inibidor de Quinase Dependente de Ciclina p18/antagonistas & inibidores
Inibidor de Quinase Dependente de Ciclina p18/genética
Transplante de Células-Tronco Hematopoéticas
Células-Tronco Hematopoéticas/citologia
Células-Tronco Hematopoéticas/metabolismo
Seres Humanos
Camundongos
Camundongos Endogâmicos C57BL
Simulação de Acoplamento Molecular
Estrutura Terciária de Proteína
Bibliotecas de Moléculas Pequenas/metabolismo
Bibliotecas de Moléculas Pequenas/toxicidade
Relação Estrutura-Atividade
Ácidos Sulfanílicos/metabolismo
Ácidos Sulfanílicos/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Coumarins); 0 (Cyclin-Dependent Kinase Inhibitor p18); 0 (Small Molecule Libraries); 0 (Sulfanilic Acids); 0 (XIE18-6 compound); EC 2.7.11.22 (Cyclin-Dependent Kinase 4); EC 2.7.11.22 (Cyclin-Dependent Kinase 6)
[Em] Mês de entrada:1611
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151219
[St] Status:MEDLINE
[do] DOI:10.1038/srep18115



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