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1.
FEMS Microbiol Lett ; 365(12)2018 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-29529176

RESUMO

The present study investigates the optimization of tannase production from Aspergillus nidulans for various physicochemical parameters and harvests tannase for its chemical characterization. The maximum tannase activity was observed on the third day of incubation at 35°C and the stability was observed at pH 5.5-6.0 by holding its 100% activity. The tannase was partially purified from A. nidulans [FT10] by ammonium sulfate precipitation at different concentrations, and it was found that at 80% of ammonium sulfate concentration, the precipitate exhibited the maximum activity for tannase of 96 U/ml. LCMS showed its M/Z value as 162.3 which was reconfirmed by SDS-PAGE. The UV spectrum and FTIR confirmed the presence of two oxy- and three hydroxyl groups in the benzene ring structure. The antibacterial activity of tannase was enhanced with antibiotics such as streptomycin and ceftazidime whereas the biofilm formation was significantly inhibited by the purified tannase. The scavenging activity was greatly increased with purified component and when the concentration of the purified tannase, FT10 was increased. To the best of our knowledge, this is one of the few reports where microbial species was used as the source for producing tannase enzyme and its role in various bioactivities such as antibacterial, anti-biofilm and antioxidant activity was evaluated.


Assuntos
Antibacterianos/farmacologia , Aspergillus nidulans/enzimologia , Hidrolases de Éster Carboxílico/isolamento & purificação , Hidrolases de Éster Carboxílico/metabolismo , Antibacterianos/isolamento & purificação , Bactérias/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Fermentação , Proteínas Fúngicas/metabolismo , Concentração de Íons de Hidrogênio
2.
J Enzyme Inhib Med Chem ; 33(1): 67-73, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29098904

RESUMO

Targeting EGFR has proven to be beneficial in the treatment of several types of solid tumours. So, a series of novel 2-(4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydrobenzo[g]quinazolin-2-ylthio)-N-substituted acetamide 5-19 were synthesised from the starting material 4-(2-mercapto-4-oxobenzo[g]quinazolin-3(4H)-yl) benzenesulfonamide 4, to be evaluated as dual EGFR/HER2 inhibitors. The target compounds 5-19, were screened for their cytotoxic activity against A549 lung cancer cell line. The percentage inhibition of EGFR enzyme was measured and compared with erlotinib as the reference drug. Compounds 6, 8, 10, and 16 showed excellent EGFR inhibitory activity and were further selected for screening as dual EGFR/HER2 inhibitors. The four selected compounds showed IC50 ranging from 0.009 to 0.026 µM for EGFR and 0.021 to 0.069 µM for the HER2 enzyme. Compound 8 was found to be the most potent in this study with IC50 0.009 and 0.021 µM for EGFR and HER2, respectively.


Assuntos
Antineoplásicos/farmacologia , Receptores ErbB/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Quinazolinas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Receptores ErbB/metabolismo , Humanos , Estrutura Molecular , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Quinazolinas/síntese química , Quinazolinas/química , Relação Estrutura-Atividade
3.
Eur J Med Chem ; 141: 84-91, 2017 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-29028534

RESUMO

An array of some new N-(substituted)-2-((4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydrobenzo[g]quinazolin-2-yl)thio)acetamide 5-19 were synthesized from the starting compound 4-(2-mercapto-4-oxobenzo[g]quinazolin-3(4H)-yl)benzenesulfonamide 4, to be assessed for their cytotoxic activity against A549 lung cancer cell line and to determine their inhibitory effect on EGFR tyrosine kinase enzyme. Compounds 5-19 showed high activity towards A549 cell line with IC50 values of 0.12-8.70 µM. Compounds 6, 12 and 18 were the most potent in this series. These compounds were further screened as dual inhibitors for EGFR/HER2 enzymes in comparison with erlotinib and were found to possess very potent activity. Compound 12 showed the highest activity with IC50 values of 0.06 µM and 0.30 µM towards EGFR and HER2, respectively. Accordingly, the apoptotic effect of the most potent compounds 6, 12 and 18 was investigated and showed a marked increase in the level of caspases-3 by 6, 9 and 8 folds, respectively, compared to the control cells. Moreover, Molecular modeling was performed inside the active site of EGFR, keeping in mind their binding possibilities, bond lengths, angles and energy scores. It was found that the most active compounds demonstrated the best binding scores in the active site of EGFR, which may clarify their high inhibition profile.


Assuntos
Antineoplásicos/farmacologia , Descoberta de Drogas , Receptores ErbB/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Quinazolinas/farmacologia , Receptor ErbB-2/antagonistas & inibidores , Sulfonamidas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Receptores ErbB/metabolismo , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Quinazolinas/síntese química , Quinazolinas/química , Receptor ErbB-2/metabolismo , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química
4.
Afr J Tradit Complement Altern Med ; 14(2): 161-165, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28573232

RESUMO

BACKGROUND: Several edible plants are used in Kingdom of Saudi Arabia since early time to control microbial infections. In the present study, twenty-four Saudi Arabian medicinal plants d according to traditionally used were select and investigated for the antimicrobial activities. MATERIALS AND METHODS: This study was designed at evaluating the antimicrobial activities of the methanol extracts of twenty-four species of sixteen plant families used in the traditional medicine by Saudi Arabian people for the treatment of numerous ailments of the microbial and non-microbial origin against four Gram-positive, four Gram-negative bacteria and four fungi and yeast using the agar well diffusion method. RESULTS: Of most of the plants tested were found to be active against two to eight organisms. Five plants were active against eight organisms. The data appeared that extracts of Echium arabicum (SY-176), Rhantarium epapposum (SY-Rumex vesicarus (SY-181), Ziziphus nummularia (SY-188), Caylusea hexagyna (SY-197) and Artemisia monosperma (SY-198) have anti-microbial activity against the most of tested bacteria, fungi and yeast. Whereas (SY-, the extracts of Teucrium oliverianum (SY-175), Zilla spinosa (SY-187), and Rhazya stricta (SY-195) have poor action against the tested bacteria, fungi and yeast. CONCLUSION: The antimicrobial activity of plant extracts against bacteria was more effective than against fungi.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Magnoliopsida , Extratos Vegetais/farmacologia , Plantas Medicinais , Artemisia , Bactérias/crescimento & desenvolvimento , Echium , Fungos/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Resedaceae , Rumex , Arábia Saudita , Ziziphus
5.
Acta Pharm ; 66(2): 155-71, 2016 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-27279061

RESUMO

As a part of ongoing studies in developing new anticancer agents, novel 1,2-dihydropyridine 4, thienopyridine 5, isoquinolines 6-20, acrylamide 21, thiazolidine 22, thiazoles 23-29 and thiophenes 33-35 bearing a biologically active quinoline nucleus were synthesized. The structure of newly synthesized compounds was confirmed on the basis of elemental analyses and spectral data. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. 2,3-Dihydrothiazole-5-carboxamides 27, 25, 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (34), 1,2-dihydroisoquinoline-7-carbonitrile (7), 5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide (35), 1,2-dihydroisoquinoline-7-carbonitrile (6), 2-cyano-3-(dimethylamino)-N-(quinolin-3-yl)acrylamide (21), 1,2-dihydroisoquinoline-7-carbonitriles (11) and (8) exhibited higher activity (IC50 values of 27-45 µmol L-1) compared to doxorubicin (IC50 47.9 µmol L-1). LQ quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (12), 2-thioxo-2,3-dihydrothiazole-5-carboxamide (28) and quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (15) show activity comparable to doxorubicin, while (quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (9), 2,3-dihydrothiazole-5-carboxamide (24), thieno [3,4-c] pyridine-4(5H)-one (5), cyclopenta[b]thiophene-3-carboxamide (33) and (quinolin-3-yl)-6-stryl-1,2-dihydroisoquinoline-7-carbonitrile (10) exhibited moderate activity, lower than doxorubicin.


Assuntos
Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Isoquinolinas/farmacologia , Piridinas/farmacologia , Quinolinas/farmacologia , Tiazóis/farmacologia , Tiazolidinas/farmacologia , Tiofenos/farmacologia , Antineoplásicos/síntese química , Neoplasias da Mama/patologia , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Desenho de Drogas , Feminino , Humanos , Concentração Inibidora 50 , Isoquinolinas/síntese química , Células MCF-7 , Modelos Moleculares , Estrutura Molecular , Piridinas/síntese química , Quinolinas/síntese química , Relação Estrutura-Atividade , Tiazóis/síntese química , Tiazolidinas/síntese química , Tiofenos/síntese química
6.
Chem Cent J ; 10: 18, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27053947

RESUMO

BACKGROUND: Quinoline derivatives have diverse biological activities including anticancer activity. On the other hand, many sulfonamide derivatives exhibited good cytotoxic activity. Hybrids of both moieties may present novel anticancer agents. RESULTS: Chloroquinoline incorporating a biologically active benzene-sulfonamide moieties 5-21 and diarylsulfone derivatives 22 and 23 were prepared using (E)-1-(4-((E)-7-chloro-1-methylquinolin-4(1H)-ylideneamino)phenyl)-3-(dimethyl-amino)prop-2-en-1-one 4 as strategic starting material. The structure of the newly synthesized compounds were confirmed by elemental analyses and spectral data. Compound 4 was confirmed by X-ray crystallographic analysis. The prepared compounds were evaluated for their anticancer activity against Lung, HeLa, Colorectal and breast cancer cell lines. Compounds 2, 4, 7, 11, 14 and 17 showed better or comparable activity to 2', 7'-dichlorofluorescein (DCF) as reference drug. Molecular docking of the active compounds on the active site of PI3K enzyme was performed in order to explore the binding mode of the newly synthesized compounds. CONCLUSION: Compounds 2, 4, 7, 11, 14 and 17 are novel quinoline derivatives that may represent good candidates for further evaluations as anticancer agents. The mechanism of action of these compounds could be through inhibition of PI3K enzyme.Graphical abstractCompound 17 on the active site of PI3K.

7.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 8): o2396, 2012 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-22904853

RESUMO

In the title compound, C(16)H(12)F(3)N(3)O(2)S·0.47C(2)H(5)OH·0.53CH(3)OH, the quinoline ring system is approximately planar, with a maximum deviation of 0.035 (3) Å, and makes a dihedral angle of 52.67 (9)° with the benzene ring. The F atoms of the -CF(3) group are disordered over two orientations, with refined site occupancies of 0.56 (2) and 0.44 (2). A single solvate site is occupied at random by ethanol or methanol, with refined site occupancies of 0.470 (6) and 0.530 (6), respectively. In the crystal, mol-ecules are linked via N-H⋯O, N-H⋯N, O-H⋯O and C-H⋯O hydrogen bonds, thereby forming sheets lying parallel to (010).

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