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1.
Free Radic Res ; 53(7): 714-726, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30947567

RESUMO

The antitumor effects of silibinin are of increasing interest, though its mechanism is not yet clear. The goal of this study was to clarify the mechanism of silibinin-induced cell death in the A431 human epidermoid carcinoma cell line. We used a cell viability assay, flow cytometry, nitric oxide (NO) assay, and western blotting to examine relationships between silibinin, NO generation and apoptosis in A431 cells. Silibinin inhibited A431 cell growth in a dose-dependent manner, inducing mitochondrial damage, and apoptosis at a high dose. At the same time, high dose silibinin increased NO levels in A431 cells and the endothelial nitric oxide synthase (eNOS) inhibitor NG-nitro-L-arginine methylester (L-NAME) attenuated silibinin-induced cell growth inhibition. By western blotting, silibinin caused increased eNOS phosphorylation in the mitochondria. The AMP-activated protein kinase inhibitor compound C significantly decreased p-eNOS expression, while blocking eNOS did not affect p-AMPK levels, suggested that AMPK acted upstream of eNOS. This study showed that silibinin increased NO levels in A431 cells by activating the AMPK-eNOS pathway, leading to mitochondrial dysfunction and apoptosis. In this mechanism of action, mitochondrial eNOS played an important role. The results provided new understanding of the functions of intracellular NO.


Assuntos
Epiderme/metabolismo , Mitocôndrias/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Silibina/uso terapêutico , Apoptose , Humanos , Silibina/farmacologia
2.
Pak J Pharm Sci ; 29(6): 1997-2004, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28375116

RESUMO

The objective of this work is to synthesize indolacin-5-fluorouracil-1-ylmethyl ester and the structure was confirmed by means of UV, IR, 1H-NMR, 13C-NMR and mass spectrometry. The physicochemical parameters of melting point, solubility, apparent partition coefficient were investigated. S180 sarcoma, H22 hapatitic cancer and Lewis-transplanted mice were used to evaluate the anti-tumor activity of indolacini-5-fluorouracil-1-ylmethyl ester compared with 5-fluorouracil in vivo. Anti-inflammatory and analgesic activities were evaluated in mice. The inhibitory ratio of indolacini- 5-fluorouracil-1-ylmethyl ester is comparative to that of 5-fluorouracil. This study indicates that 5-fluorouracil-1-ylmethyl ester may represent a new anticancer predrug of 5-fluorouracil to produce a combined effect of indolacin and 5-fluorouracil for cancer therapy.


Assuntos
Antimetabólitos Antineoplásicos/síntese química , Antimetabólitos Antineoplásicos/farmacologia , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Fluoruracila/análogos & derivados , Fluoruracila/síntese química , Fluoruracila/farmacologia , Ácidos Indolacéticos/síntese química , Ácidos Indolacéticos/farmacologia , Sarcoma 180/tratamento farmacológico , Analgésicos/síntese química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/farmacologia , Antimetabólitos Antineoplásicos/toxicidade , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Carcinoma Pulmonar de Lewis/patologia , Linhagem Celular Tumoral , Fluoruracila/toxicidade , Ácidos Indolacéticos/toxicidade , Dose Letal Mediana , Espectrometria de Massas , Camundongos , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Sarcoma 180/patologia , Solubilidade , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Temperatura de Transição , Carga Tumoral/efeitos dos fármacos
3.
Zhonghua Nan Ke Xue ; 18(9): 803-6, 2012 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-23193667

RESUMO

OBJECTIVE: To establish a new method for sperm sorting by imitating the physiological process of sperm-cervical mucus interaction on the microfluidic chip. METHODS: We designed a microfluidic chip to imitate the physiological process of natural sperm sorting in the microchannel based on the interaction between sperm and cervical mucus, and obtained motile sperm after the interaction. Meanwhile, we established an integrated real-time sperm detection reservoir on this chip to determine sperm parameters using the computer-assisted sperm analysis system. We analyzed 30 samples using both microfluidic and swim-up methods, and compared the results with those obtained before sorting. RESULTS: The rate of grade a + b sperm, the rate of morphologically normal sperm, straight-line velocity (VSL), average path velocity (VAP) and straightness (STR) were (29.78 +/- 11.24)%, (8.00 +/- 5.19)%, (18.89 +/- 4.90) microm/s, (26.84 +/- 5.13) microm/s and (70.15 +/- 7.61)%, respectively, before sorting, (71.65 +/- 11.18)%, (14.95 +/- 6.79)%, (24.14 +/- 5.95) microm/s, (32.61 +/- 6.36) microm/s and (73.87 +/- 9.34)%, respectively, after swim-up sorting, and (92.37 +/- 6.33)%, (23.33 +/- 7.67)%, (34.03 +/- 16.78) microm/s, (38.73 +/- 16.40) microm/s and (84.91 +/- 12.56)%, respectively, after sorting on the microfluidic chip. The sperm parameters obtained before sorting showed statistically significant differences from those obtained on the chip (P < 0.01) and by the swim-up method (P < 0.05). CONCLUSION: Imitation of the physiological interaction between sperm and cervical mucus on the microfluidic chip helped the realization of both the natural sorting and real-time analysis of sperm. The quality of the sperm sorted on the microfluidic chip is significantly better than that of the sperm before sorting and sorted by the swim-up method. This has prepared the ground for imitating the fertilization process under the physiological condition on the microfluidic chip.


Assuntos
Técnicas Analíticas Microfluídicas/instrumentação , Análise de Sequência com Séries de Oligonucleotídeos , Análise do Sêmen , Espermatozoides/fisiologia , Movimento Celular , Separação Celular , Muco do Colo Uterino , Humanos , Masculino , Microfluídica/métodos , Motilidade Espermática/fisiologia
4.
Bing Du Xue Bao ; 27(4): 331-6, 2011 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-21874901

RESUMO

A multiplex RT-PCR assay based on GeXP system was developed in order to detect simultaneously human enterovirus 71 (EV71) and coxsackievirus A16 (CVA16) and other coxsackieviruses (CVA4, 5, 9 and 10, CVB1, 3 and 5). Enterovirus detection was performed with a mixture of 12 pairs of oligonucleotide primers including one pair of published primers for amplifying all known pan-enterovirus genomes and eleven primer pairs specific for detection of the VP1 genes of EV71, C A16, CVA4, CVA5, CVA9, CVA10, CVB1, CVB3 and CVB5, respectively. The specificity of multiplex RT-PCR system was examined using enterovirus cell cultures and positive strains identified previously from hand-foot-and-mouth disease (HFMD) patients. Serial dilution of titrated EV71 and C A16 cell cultures and in vitro transcripted RNA of enterovirus VP1 regions were used to detect the sensitivity of the multiplex RT-PCR system. The limit of detection for this multiplex RT-PCR system was 10(0.5) TCID50/microL for EV71 and C A16 cell cultures and 1000 copies for in vitro transcripted RNA of nine viruses per assay. This multiplex RT-PCR assay is a rapid, sensitive and specific assay for the diagnosis of common enterovirus infection in cases of HFMD outbreak and is also potentially useful for molecular epidemiological investigation.


Assuntos
Enterovirus/isolamento & purificação , Doença de Mão, Pé e Boca/virologia , Reação em Cadeia da Polimerase Via Transcriptase Reversa/métodos , Primers do DNA/genética , Enterovirus/classificação , Enterovirus/genética , Doença de Mão, Pé e Boca/diagnóstico , Humanos
5.
Zhonghua Nan Ke Xue ; 17(4): 301-4, 2011 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-21548204

RESUMO

OBJECTIVE: To investigate the effects of a microfluidic sperm sorter on the routine parameters and DNA integrity of human sperm. METHODS: We divided 40 semen samples into two aliquots and performed sperm sorting using a self-made polydimethylsiloxane microfluidic sperm sorter and the swim-up method, respectively. Then we evaluated and compared the effects of these two methods on the sperm routine parameters and DNA integrity by computer-assisted sperm analysis and sperm chromatin dispersion test. RESULTS: After processing, sperm motility, normal morphology and tail hypoosmotic swelling rate were significantly improved, while sperm DNA damage remarkably decreased (P < 0.01). The microfluidic sperm sorter achieved a significantly lower rate of sperm DNA damage than the swim-up method ([ 8.4 +/- 5.8 ]% vs [16.4 +/- 9.2] %, P < 0.01), but no statistically significant differences were found in all other parameters between the two methods. CONCLUSION: High-quality sperm with less DNA integrity damage could be obtained in sperm sorting with the microfluidic sperm sorter.


Assuntos
Separação Celular/instrumentação , Dano ao DNA , Análise do Sêmen/instrumentação , Espermatozoides , Adulto , Separação Celular/métodos , DNA , Humanos , Infertilidade Masculina/genética , Infertilidade Masculina/fisiopatologia , Masculino , Microfluídica , Pessoa de Meia-Idade , Análise Serial de Proteínas , Análise do Sêmen/métodos , Motilidade Espermática
6.
Zhongguo Shi Yan Xue Ye Xue Za Zhi ; 18(5): 1163-7, 2010 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-21129253

RESUMO

The objective of this study was to investigate the synergistic effect of soluble human recombinant tumor necrosis factor related apoptosis inducing ligand (TRAIL) protein combined with anti-vascular endothelial growth factor (anti-VEGF) antibody on inducing apoptosis of leukemia K562 cells. The inhibitory rates and apoptotic rates of K562 cells treated with TRAIL and anti-VEGF antibody alone and their combination for 48 hours were examined by CCK-8 assay and flow cytometry respectively. The results indicated that the apoptotic rates of K562 cells induced with 75, 100 and 150 ng/ml TRAIL after culture for 48 hours were (4.26±0.67)%, (8.91±0.55)% and (11.71±0.78)% respectively. The apoptotic rates of K562 cells induced with 2.5, 5 and 7.5 µg/ml anti-VEGF antibody after culture for 48 hours were (3.95±0.69)%, (7.98±0.74)% and (10.26±0.83)% respectively. The apoptotic rates of K562 cells treated with combination use of 2.5 µg/ml anti-VEGF antibody and 75 ng/ml TRAIL, 5 µg/ml anti-VEGF antibody and 100 ng/ml TRAIL, and 7.5 µg/ml anti-VEGF antibody and 150 ng/ml TRAIL for 48 hours were (22.16±0.93)%, (36.32±1.31)% and (49.19±0.71)% respectively. The combined use of above mentioned agents induced significantly higher apoptosis and cytotoxicity than that of TRAIL or anti-VEGF antibody alone (p<0.05). It is concluded that the combination use of TRAIL and anti-VEGF antibody can significantly increase the sensitivity of K562 cells to apoptosis.


Assuntos
Anticorpos Monoclonais/farmacologia , Apoptose/efeitos dos fármacos , Ligante Indutor de Apoptose Relacionado a TNF/farmacologia , Humanos , Células K562 , Fator A de Crescimento do Endotélio Vascular/imunologia
7.
Arch Pharm Res ; 32(4): 527-33, 2009 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-19407970

RESUMO

Myrica rubra Sieb. et Zucc. leaves are commonly used as an astringent, antidiarrheic, and analgesics in folk medicine in China. In the present study, the analgesic activity of myricetin, a major compound in Myrica rubra Sieb. et Zucc. leaves was evaluated in vivo. The analgesic effect of myricetin was tested by a serial of models, such as acetic acid-induced writhing response, formalin-induced paw licking and hot plate test. The sedative activity was evaluated by pentobarbital-induced sleep time. Platelet aggregation induced by collagen and arachidonic acid was also performed in vitro. Myricetin showed a significant inhibition on chemical nociceptive models such as the acetic acid-induced writhing response and the licking time on the late phase in the formalin test in a dose-dependent manner, but did not manifest a signicant effect in hot plate test. Myricetin was also not able to increase the sleeping time induced by pentobarbital, which further indicated that the analgesic effect of myricetin was unrelated to sedation. In addition, myricetin inhibited the content of PGE2 in the peritoneal fluid and platelet aggregation induced by collagen and arachidonic acid in vitro. These results collectively demonstrated that myricetin possessed potent analgesic activity, which was related with peripheral analgesia, but, not with the opioid system. Myricetin may be a potent COX-1 inhibitor with anti-platelet activity.


Assuntos
Analgésicos/farmacologia , Flavonoides/farmacologia , Myrica , Dor/prevenção & controle , Ácido Acético , Analgésicos/isolamento & purificação , Animais , Comportamento Animal/efeitos dos fármacos , Ciclo-Oxigenase 1/metabolismo , Inibidores de Ciclo-Oxigenase/farmacologia , Dinoprostona/metabolismo , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Feminino , Flavonoides/isolamento & purificação , Formaldeído , Masculino , Proteínas de Membrana/antagonistas & inibidores , Proteínas de Membrana/metabolismo , Camundongos , Myrica/química , Dor/induzido quimicamente , Dor/metabolismo , Medição da Dor , Limiar da Dor/efeitos dos fármacos , Cavidade Peritoneal , Lavagem Peritoneal , Folhas de Planta , Agregação Plaquetária/efeitos dos fármacos , Inibidores da Agregação de Plaquetas/farmacologia , Coelhos , Sono/efeitos dos fármacos
8.
J Asian Nat Prod Res ; 10(5-6): 439-45, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-18464084

RESUMO

In the present study, we have investigated the neuroprotective potential of ginsenoside Re (Re) in the middle cerebral artery occlusion model in Sprague-Dawley rats. Adult male Sprague-Dawley rats were treated with Re (5, 10 or 20 mg kg(- 1), P.O. for 7 days, once a day) prior to occlusion. There was a significant increase in the neurological symptoms in ischemic animals as compared with the sham group animals. These effects were attenuated by 10 and 20 mg kg(- 1) Re, P.O. There was a significant increase in the level of malondialdehyde (MDA) in ischemic animals indicating oxidative stress. An elevated level of MDA in ischemic animals was reduced by 10 and 20 mg kg(- 1) Re, P.O., respectively. It was observed that Re significantly decreased mitochondrial swelling, thereby preventing the reduction of H(+)-ATPase activity. This study demonstrates the neuroprotective potential of Re in cerebral ischemia-reperfusion injury in rats.


Assuntos
Ginsenosídeos/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Dilatação Mitocondrial/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , ATPases Translocadoras de Prótons/metabolismo , Animais , Isquemia Encefálica/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Ginsenosídeos/uso terapêutico , Masculino , Malondialdeído/metabolismo , Fármacos Neuroprotetores/uso terapêutico , Fitoterapia , Ratos , Ratos Sprague-Dawley , Traumatismo por Reperfusão/tratamento farmacológico
9.
Biol Pharm Bull ; 29(12): 2502-5, 2006 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-17142990

RESUMO

To investigate the protective effect of ginsenoside Re (Re) against cerebral ischemia-reperfusion injury, adult male Wistar rats weighing 250-300 g were subjected to either sham surgery or middle cerebral artery occlusion (MCAO) for 2 h of brain ischemia and 2 h reperfusion. A fluorescence polarization assay was carried out for membrane fluidity of brain mitochondria. Lipid peroxidation [malondiadehyde (MDA) formation], superoxide dismutase (SOD) and glutathion peroxidase (GSH-Px) of rat brain were estimated by fluorometric methods. It was observed that Re (5, 10, 20 mg kg-1 p.o. pretreatment for 7 d, once a day) significantly improved the fluidity of mitochondrial membranes as demonstrated by a reduction of average microviscosity, ameliorated lipid peroxidation by raising the activities of SOD and GSH-Px, and reduced the content of MDA in rat brain. This study demonstrated a direct protective effect of Re against cerebral ischemia-reperfusion injury.


Assuntos
Encéfalo/irrigação sanguínea , Ginsenosídeos/farmacologia , Traumatismo por Reperfusão/prevenção & controle , Animais , Masculino , Fluidez de Membrana/efeitos dos fármacos , Ratos , Ratos Wistar
10.
J Sep Sci ; 28(3): 225-33, 2005 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-15776923

RESUMO

Inexpensive and permanently modified poly(methyl methacrylate)(PMMA) microchips were fabricated by an injection-molding process. A novel sealing method for plastic microchips at room temperature was introduced. Run-to-run and chip-to-chip reproducibility was good, with relative standard deviation values between 1-3% for the run-to-run and less than 2.1% for the chip-to-chip comparisons. Acrylonitrile-butadiene-styrene (ABS) was used as an additive in PMMA substrates. The proportions of PMMA and ABS were optimized. ABS may be considered as a modifier, which obviously improved some characteristics of the microchip, such as the hydrophilicity and the electro-osmotic flow (EOF). The detection limit of Rhodamine 6G dye for the modified microchip on the home-made microchip analyzer showed a dramatic 100-fold improvement over that for the unmodified PMMA chip. A detection limit of the order of 10(-20) mole has been achieved for each injected psiX-174/HaeIII DNA fragment with the baseline separation between 271 and 281 bp, and fast separation of 11 DNA restriction fragments within 180 seconds. Analysis of a PCR product from the tobacco ACT gene was performed on the modified microchip as an application example.


Assuntos
DNA/análise , Análise de Sequência com Séries de Oligonucleotídeos/instrumentação , Polimetil Metacrilato/química , Microscopia Eletrônica de Varredura , Reação em Cadeia da Polimerase , Reprodutibilidade dos Testes , Rodaminas
11.
J Chromatogr B Analyt Technol Biomed Life Sci ; 816(1-2): 145-51, 2005 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-15664344

RESUMO

The p16 tumor suppressor gene is inactivated by promoter region hypermethylation in many types of tumor. Recent studies showed that aberrant methylation of the p16 gene is an early event in many tumors, especially in lung cancer, and may constitute a new biomarker for early detection and monitoring of prevention trials. We detected tumor-associated aberrant hypermethylation of the p16 gene in plasma and tissue DNA from 153 specimens using a modified semi-nested methylation-specific PCR (MSP) combining plastic microchip electrophoresis or slab gel electrophoresis, respectively. Specimens were from 79 lung cancer patients, 15 abdominal tumor patients, 30 positive controls and 30 negative controls. The results showed that the positive rate obtained by microchip electrophoresis was more than 26.6% higher and the same specificity was kept when compared with slab gel electrophoresis. The microchip electrophoresis can rapidly and accurately analyze the PCR products of methylated DNA and obviously improve the positive rate of diagnosis of cancer patients when compared with gel electrophoresis. This method with the high assay sensitivity might be used for detection of methylation of p16 gene and even to facilitate early diagnosis of cancer patients.


Assuntos
Metilação de DNA , Eletroforese em Microchip/métodos , Genes p16 , Neoplasias/genética , Neoplasias Abdominais/sangue , Neoplasias Abdominais/genética , Eletroforese em Microchip/instrumentação , Estudos de Viabilidade , Humanos , Neoplasias Pulmonares/sangue , Neoplasias Pulmonares/genética , Polimetil Metacrilato , Sensibilidade e Especificidade
12.
Biol Pharm Bull ; 27(6): 810-2, 2004 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-15187423

RESUMO

The effect of (3,5,6-trimethylpyrazin-2-yl)methyl 2-[4-(2-methylpropyl)phenyl]propanoate (ITE) on type II collagen (CII)-induced arthritis in mice was studied. Mice were immunized twice with CII, ITE being given orally once a day for 40 d after the 1st immunization. Clinical assessment showed that ITE had no effect on the day of onset of arthritis but did lowered the incidence rate of arthritis and the arthritis score. And ITE had a marked suppressive effect on the mouse hind paw edema induced by CII. ITE suppressed the delayed-type mouse ear skin reaction to CII but had no effect on the level of serum anti-CII antibodies. These results suggest that ITE inhibits the development of CII-induced arthritis in mice by suppressing delayed-type hypersensitivity to CII.


Assuntos
Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/uso terapêutico , Artrite Experimental/tratamento farmacológico , Colágeno Tipo II/toxicidade , Propionatos/química , Propionatos/uso terapêutico , Pirazinas/química , Pirazinas/uso terapêutico , Animais , Artrite Experimental/induzido quimicamente , Artrite Experimental/fisiopatologia , Relação Dose-Resposta a Droga , Masculino , Camundongos
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