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1.
Eur J Pharmacol ; 886: 173550, 2020 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-32926915

RESUMO

Lung cancer has a relatively poor prognosis, and the clinical efficacy of targeted drugs remains unsatisfactory. Therefore, the search for safe and efficient novel antitumor drugs has become an urgent problem in the treatment of lung cancer. Aloe-emodin (AE), a medicinal herb, has been demonstrated to exhibit many pharmacological effects on tumor cells, such as lung cancer cells. However, the anticancer properties of AE have not been fully exploited by modern medicine, as their mechanisms of action are not yet known. In this study, the bioassay results demonstrated that AE reduced the viability of the non-small cell lung cancer cell line A549 and NCI-H1299 in a dose- and time-dependent manner. Moreover, AE induced caspase-dependent apoptosis and autophagy. AE induced autophagy through activation of MAPK signaling and inhibition of the Akt/mTOR pathway. We also found that AE-induced autophagy was attenuated by the reactive oxygen species scavenger N-acetylcysteine, indicating that reactive oxygen species played a key role in AE-mediated autophagy in A549 and NCI-H1299 cells. Furthermore, AE induced reactive oxygen species-dependent autophagy in A549 and NCI-H1299 cells, which triggered apoptosis. Additionally, AE showed synergistic cytotoxic effects with the antitumor drug gemcitabine in A549 and NCI-H1299 cells. In brief, these results showed that AE might be useful for developing a therapeutic candidate for lung cancer complications.


Assuntos
Antraquinonas/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Neoplasias Pulmonares/tratamento farmacológico , Proteínas Quinases Ativadas por Mitógeno/efeitos dos fármacos , Proteína Oncogênica v-akt/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Serina-Treonina Quinases TOR/efeitos dos fármacos , Células A549 , Antraquinonas/uso terapêutico , Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/farmacologia , Inibidores de Caspase/farmacologia , Linhagem Celular Tumoral , Desoxicitidina/análogos & derivados , Desoxicitidina/uso terapêutico , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Humanos , Gencitabina
2.
Parasitol Res ; 110(4): 1321-6, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22350671

RESUMO

The acaricidal activity of trans-cinnamaldehyde was evaluated in vitro on Psoroptes cuniculi. In this study, different concentrations of trans-cinnamaldehyde were tested, and the observed mites mortality was compared with that observed in untreated and treated (Acacerulen R®) controls. The morphological changes in P. cuniculi treated with trans-cinnamaldehyde were examined with light microscopy. By the analysis of variance one-way test, up to 8 µg/ml of trans-cinnamaldehyde gave highly significant (P < 0.01) percentages of mite mortality compared with the untreated controls, but only up to 256 µg/ml, it showed the same efficacy of Acacerulen R®. At the same time, a bioassay was conducted by exposing mites to varying doses of trans-cinnamaldehyde in vitro cultures. The resulting data were analyzed by using a time-dose-mortality modeling technique, yielding the parameters for time and dose effects of P. cuniculi. The ß value was 2.01, indicating that trans-cinnamaldehyde had a good activity to kill P. cuniculi adults. Based on the time-dose-mortality relationships fitted and the virulence indices estimated, trans-cinnamaldehyde is a promising microbial agent for mites control.


Assuntos
Acaricidas/farmacologia , Acroleína/análogos & derivados , Extratos Vegetais/farmacologia , Óleos de Plantas/farmacologia , Psoroptidae/efeitos dos fármacos , Acroleína/farmacologia , Animais , Cassia/química , Infestações por Ácaros/tratamento farmacológico , Extratos Vegetais/química , Óleos de Plantas/química , Controle de Ácaros e Carrapatos/métodos
3.
Molecules ; 16(10): 8848-65, 2011 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-22019573

RESUMO

Sodium houttuyfonate (SH), an addition compound of sodium bisulfite and houttuynin, showed in vitro antibacterial activity against 21 Staphylococcus aureus (S. aureus) strains grown in planktonic cultures. Microarray results showed decreased levels of autolysin atl, sle1, cidA and lytN transcripts in the SH-treated strain as compared to the control strain, consistent with the induction of the autolytic repressors lrgAB and sarA and with the downregulation of the positive regulators agrA and RNAIII. Triton X-100-induced autolysis was significantly decreased by SH in S. aureus ATCC 25923, and quantitative bacteriolytic assays and zymographic analysis demonstrated SH-mediated reduction of extracellular murein hydrolase activity in these cells. Anti-biofilm assay showed that SH is poorly active against S. aureus grown in biofilm cultures, whereas SH diminished the amounts of extracellular DNA (eDNA) of S. aureus in a dose-dependent manner, which suggested that SH may impede biofilm formation by reducing the expression of cidA to inhibit autolysis and eDNA release in the early phase. Some of the microarray results were confirmed by real-time RT-PCR.


Assuntos
Alcanos/farmacologia , Antibacterianos/farmacologia , Bacteriólise/efeitos dos fármacos , N-Acetil-Muramil-L-Alanina Amidase/metabolismo , Staphylococcus aureus/efeitos dos fármacos , Sulfitos/farmacologia , Proteínas de Bactérias/metabolismo , Biofilmes/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos , Houttuynia , Proteínas de Membrana/efeitos dos fármacos , Proteínas de Membrana/metabolismo , Testes de Sensibilidade Microbiana , N-Acetil-Muramil-L-Alanina Amidase/genética , Análise de Sequência com Séries de Oligonucleotídeos , Extratos Vegetais/farmacologia , Staphylococcus aureus/genética , Staphylococcus aureus/metabolismo , Transcrição Gênica/efeitos dos fármacos
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