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1.
Spectrochim Acta A Mol Biomol Spectrosc ; 138: 667-74, 2015 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-25544183

RESUMO

Cladosporium oxysporum a new taxol producing endophytic fungus was identified and production of taxol were characterized using UV-visible spectroscopy (UV-vis), high-performance liquid chromatography (HPLC), infrared (IR) nuclear magnetic resonance spectroscopy (NMR ((13)C and (1)H)) and liquid chromatography-mass spectrometry (LC-MS). The taxol biosynthetic gene (dbat) was evaluated for new taxol producing fungus. Antibacterial activity against six different human pathogenic bacteria was done by agar well diffusion method. The anticancer efficacy of isolated fungal taxol were also evaluated in human colon cancer cell HCT 15 by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), cytotoxicity and nuclear morphology analysis. The isolated fungal taxol showed positive towards biosynthetic gene (dbat) and effective against both Gram positive as well as Gram negative. The fungal taxol suppress growth of cancer cell line HCT 15 with an IC50 value of 3.5µM concentration by 24h treatment. Thus, the result reveals that C. oxysporum could be a potential alternative source for production of taxol and have antibacterial as well as anticancer properties with possible clinical applications.


Assuntos
Bactérias/efeitos dos fármacos , Cladosporium/química , Neoplasias do Colo/patologia , Paclitaxel/farmacologia , Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Cladosporium/genética , Humanos , Testes de Sensibilidade Microbiana , Paclitaxel/isolamento & purificação , Espectroscopia de Prótons por Ressonância Magnética , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta
2.
J Photochem Photobiol B ; 153: 247-60, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26461484

RESUMO

Three new homodinuclear manganese(II) complexes of the type [Mn2L(1-3)(ClO4)(H2O)](ClO4)3 (1-3) have been synthesized via cyclocondensation of terephthalaldehyde with three different benzoylated pendants in the presence of manganese(II) perchlorate and characterized by spectroscopic methods. Cyclic voltammetric investigation of complexes (1-3) depict two quasi-reversible one electron reduction processes in the cathodic potential region (E(1)pc=-0.73 to-0.83 V, E(2)pc=-1.31 to -1.40 V) and two quasi-reversible one electron oxidation processes in the anodic potential region (E(1)pa=1.03 to 1.10 V, E(2)pa=1.69 to 1.77 V). Electronic absorption spectra of the complexes suggested tetrahedral geometry around the central metal ion. The observed low magnetic moment values (µeff, 5.60-5.68 B.M.) of the complexes indicate the presence of an antiferromagnetic spin-exchange interaction between two metal centers, which was also supported by the broad EPR signal. All the compounds were tested for antibacterial activity against Gram (-ve) and Gram (+ve) bacterial strains. The binding studies of complexes with CT-DNA suggested minor-groove mode of interaction. Molecular docking studies were carried out in order to find the binding affinity of complexes with DNA and protein EGFR Kinase. The complexes are stabilized by additional electrostatic and van der Waals interaction with the DNA, and support minor groove mode of binding. The cleavage activity of complexes on pBR322 plasmid DNA displays efficient activity through a mechanistic pathway involving hydroxyl radicals. The cytotoxicity of complexes 2 and 3 have been tested against human liver adenocarcinoma (HepG2) cell line. Nuclear-chromatin cleavage has also been observed with propidium iodide (PI) staining and alkaline single-cell gel electrophoresis (comet assay) techniques.


Assuntos
Antibacterianos/química , Complexos de Coordenação/química , DNA/química , Manganês/química , Antibacterianos/síntese química , Antibacterianos/toxicidade , Sítios de Ligação , Sobrevivência Celular/efeitos dos fármacos , Ensaio Cometa , Complexos de Coordenação/síntese química , Complexos de Coordenação/toxicidade , DNA/metabolismo , Clivagem do DNA/efeitos dos fármacos , Receptores ErbB/química , Receptores ErbB/metabolismo , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Células Hep G2 , Humanos , Simulação de Acoplamento Molecular , Conformação de Ácido Nucleico , Estrutura Terciária de Proteína
3.
Eur J Med Chem ; 76: 256-63, 2014 Apr 09.
Artigo em Inglês | MEDLINE | ID: mdl-24583606

RESUMO

Bio-inspired silver nanoparticles are synthesized using Malus domestica (apple) extract. Polyphenols present in the apple extract act as a reducing and capping agent to produce the silver nanoparticles. UV-Visible analysis shows the surface plasmon resonance (SPR) absorption at 420 nm. The FTIR analysis was used to identify the functional groups responsible for the bio-reduction of silver ion. The XRD and HRTEM images confirm the formation of silver nanoparticles. The minimal inhibitory concentration (MIC) of silver nanoparticles was recorded against most of the bacteria and fungus. Further, MCF-7 human breast adenocarcinoma cancer cell line was employed to observe the efficacy of cancer cell killing.


Assuntos
Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Nanopartículas Metálicas , Prata/química , Humanos , Células MCF-7 , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Varredura , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier
4.
Spectrochim Acta A Mol Biomol Spectrosc ; 129: 400-14, 2014 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-24747866

RESUMO

A series of dinuclear nickel(II) and copper(II) complexes (1-6) of hexaaza macrocycles of 2,6-diformyl-4-methylphenol with three different benzoyl pendant-arms, 2,2'-benzoyliminodi(ethylamine) trihydrochloride (L), 2,2'-4-nitrobenzoyliminodi(ethylamine) trihydrochloride (L') and 2,2'-3,5-dinitrobenzoyliminodi(ethylamine) trihydrochloride (L″) have been synthesized and characterized by spectral methods. The electrochemical studies of these complexes depict two irreversible one electron reduction processes around E(1)pc=-0.62 to -0.76 V and E(2)pc=-1.21 to -1.31, and nickel(II) complexes (1-3) exhibit two irreversible one electron oxidation processes around E(1)pa=1.08 to 1.14 V and E(2)pa=1.71 to 1.74 V. The room temperature magnetic moment values (µeff, 1.52-1.54 BM) indicate the presence of an antiferromagnetic interaction in the binuclear copper(II) complexes (4-6) which is also observed from the broad ESR spectra with a g value of 2.14-2.15. The synthesized complexes (1-6) were screened for their antibacterial activity. The results of DNA interaction studies indicate that the dinuclear complexes can bind to calf thymus DNA by intercalative mode and display efficient cleavage of plasmid DNA. Further, the cytotoxic activity of complexes 2, 5 and 6 on human liver adenocarcinoma (HepG2) cell line has been examined. Nuclear-chromatin cleavage has also been observed with PI staining and comet assays.


Assuntos
Antibacterianos/química , Antineoplásicos/química , Complexos de Coordenação/química , Cobre/química , Substâncias Intercalantes/química , Níquel/química , Poliaminas/química , Animais , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Bovinos , Linhagem Celular Tumoral , Complexos de Coordenação/farmacologia , Cobre/farmacologia , DNA/química , Clivagem do DNA/efeitos dos fármacos , Humanos , Substâncias Intercalantes/farmacologia , Compostos Macrocíclicos/química , Compostos Macrocíclicos/farmacologia , Neoplasias/tratamento farmacológico , Níquel/farmacologia , Poliaminas/farmacologia
5.
Artigo em Inglês | MEDLINE | ID: mdl-24657422

RESUMO

A compound was isolated from Cassia auriculata leaves and characterized by high-performance liquid chromatography (HPLC), liquid chromatography mass spectrometry (LC-MS), UV-vis spectroscopy (UV-vis), Fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). The in vitro anticancer effect of the compound isolated from C. auriculata was evaluated in human colon cancer cells HCT 15 by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cytotoxicity, nuclear morphology analysis and measurement of lactate dehydrogenase. The isolated compound 4-(2,5 dichlorobenzyl)-2,3,4,5,6,7 hexahydro7(4 methoxyphenyl)benzo[h][1,4,7] triazecin8(1H)-one showed 50% inhibition of HCT 15 cells when tested at 20µg/ml after 24h incubation. Cytotoxicity, nuclear morphology and lactate dehydrogenase assays clearly show potent anticancer activity of the isolated compound against colon cancer. Thus, the in vitro findings suggest that the compound isolated from C. auriculata leaves have potent anti-cancer properties with possible clinical applications.


Assuntos
Antineoplásicos Fitogênicos , Apoptose/efeitos dos fármacos , Cassia/química , Proliferação de Células/efeitos dos fármacos , Neoplasias do Colo/tratamento farmacológico , Folhas de Planta/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Neoplasias do Colo/metabolismo , Neoplasias do Colo/patologia , Humanos
6.
Artigo em Inglês | MEDLINE | ID: mdl-24211805

RESUMO

The compound was isolated from leaves of Cassia auriculata and its structure was characterized using high-performance liquid chromatography (HPLC), liquid chromatography mass spectrometry (LC-MS), UV-vis spectroscopy (UV-vis), fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, cytotoxicity, nuclear morphology and lactate dehydrogenase assay of isolated compound was tested against human colon cancer cell line HCT 15. The isolated compound, 4-(4-chlorobenzyl)-2,3,4,5,6,7-hexahydro-7-(2-ethoxyphenyl)benzo[h][1,4,7]triazecin-8(1H)-one at 25µg/ml concentration and by 48h showed 50% inhibition of human colon cancer cells (HCT 15). The results suggest that isolated compound from C. auriculata has potential to prevent colon cancer cell line.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Cassia/química , Neoplasias do Colo/prevenção & controle , Anticarcinógenos/química , Anticarcinógenos/isolamento & purificação , Anticarcinógenos/farmacologia , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos
7.
Microsc Res Tech ; 75(2): 112-6, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-21780253

RESUMO

The most practical approach to reduce morbidity and mortality of cancer is to delay the process of carcinogenesis by usage of anticancer agents. This necessitates that safer compounds are to be critically examined for anticancer activity especially, those derived from natural sources. A spice commonly found in India and the surrounding regions, is turmeric, derived from the rhizome of Curcuma longa and the major active component is a phytochemical termed curcumin. Green tea is one of the most popular beverages used worldwide, produced from the leaves of evergreen plant Camellia sinensis and the major active ingredients are polyphenolic compounds known as catechins. In this study, synergistic anticancer activity of curcumin and catechin was evaluated in human colon adenocarcinoma HCT 15, HCT 116, and human larynx carcinoma Hep G-2 cell lines. Although, both curcumin or catechin inhibited the growth of above cell lines, interestingly, in combination of both these compounds highest level of growth control was observed. The anticancer activity shown is due to cytotoxicity, nuclear fragmentation as well as condensation, and DNA fragmentation associated with the appearance of apoptosis. These results suggest that curcumin and catechin in combination can inhibit the proliferation of HCT 15, HCT 116, as well as Hep G-2 cells efficiently through induction of apoptosis.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Catequina/farmacologia , Curcumina/farmacologia , Apoptose , Núcleo Celular/efeitos dos fármacos , Fragmentação do DNA , Ensaios de Seleção de Medicamentos Antitumorais , Sinergismo Farmacológico , Células HCT116 , Células Hep G2 , Humanos
8.
Cytotechnology ; 63(3): 259-68, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21327936

RESUMO

The aim of the study was to develop a new strategy for the differentiation of hematopoietic stem cell (HSC) derived from UCB into hepatocyte like cells and also to estimate the effects of combination of fibroblast growth factor 4 (FGF 4) and hepatocyte growth factor (HGF) on hematopoietic stem cell differentiation. HSCs were isolated and purified by magnetic activated cell sorting. HSCs were induced to hepatocyte like cells under a 2-step protocol with combination of growth factors. Reverse transcription polymerase chain reaction was performed to detect multiple genes related to hepatocyte like cells development and function. Hepatocyte like morphology was illustrated by inverted repeat microscope and the secretion of albumin and α- fetoprotein by these cells was confirmed by enzyme linked immunosorbent assay. Hepatocyte like cells was observed at the end of the protocol (days 14). These differentiated cells were observed to show high expression of genes related to hepatocytes (tryptophan 2, 3-dioxygenase [TO], glucose 6-phosphate [G6P], cytokeratin 18 [CK 18], albumin and α- fetoprotein [AFP]). The quantities of albumin and AFP at day 0 were low and upon differentiation the cells were able to produce albumin and AFP at high levels. Our results show a new strategy for differentiation in a short duration, using a combination of growth factors for the differentiation of umbilical cord blood derived HSC into hepatocyte like cells under certain in vitro conditions. After further studies this approach has the potency, for widespread cell replacement therapy for liver diseases.

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