RESUMO
Essential oil (EO)-based nanoemulsions (NEs) are promising grain protectants in the management of stored-product pests. However, the potential impact of the stored-grain species on the green insecticide effectiveness has been poorly studied. In this study, two concentrations of EO-based NEs from Carlina acaulis L., Mentha longifolia (L.) Huds., and Hazomalania voyronii (Jum.) Capuron were evaluated as insecticides against the major stored-product pest Sitophilus oryzae (L.) on barley, oats, and maize kernels. The C. acaulis EO-based NE applied at 1000 ppm on barley achieved the highest mortality, killing 94.4% of S. oryzae adults after a 7-day exposure, followed by 1000 ppm of H. voyronii EO-based NE (83.3%). The lowest mortality (1.1%) was recorded with 500 ppm of M. longifolia EO-based NE on maize after the same interval. All tested NEs exhibited elevated efficacy when applied on barley, while mortalities were lower on oats and maize. Furthermore, C. acaulis EO-based NE was the most effective when applied on all commodities, followed by H. voyronii and M. longifolia EO-based NEs. Overall, our results highlighted the significant impact of the stored cereal on the insecticidal effectiveness of EO-based NE used for stored-product pest control. Sitophilus oryzae adults on barley can be adequately controlled through the application of C. acaulis and H. voyronii EO-based NEs.
RESUMO
The synthesis of N-{4-[a-(1-adamantyl)benzyl]phenyl}piperazines 2a-e is described. The in vitro antiproliferative activity of most compounds against main cancer cell lines is significant. The σ(1), σ(2)-receptors and sodium channels binding affinity of compounds 2 were investigated. One of the most active analogs, 2a, had an interesting in vivo anticancer profile against the BxPC-3 and Mia-Paca-2 pancreas cancer cell lines with caspase-3 activation, which was associated with an anagelsic activity against the neuropathic pain.
Assuntos
Adamantano , Antineoplásicos , Receptores sigma/metabolismo , Adamantano/síntese química , Adamantano/química , Adamantano/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Camundongos , Camundongos Nus , Estrutura Molecular , Neoplasias Pancreáticas/metabolismoRESUMO
In this study, we examined several molecular markers in prostate and breast cancer patients and in normal individuals. The markers tested were: variations in the quantity of plasma DNA, glutathione-S-transferase P1 gene (GSTP1), Ras association domain family 1A (RASSF1A), and ataxia telangiectasia mutated (ATM) methylation status in plasma, carcinoembryonic antigen (CEA) and prostate-specific membrane antigen (PSMA) mRNA in peripheral blood mononuclear cells (PBMC) and plasma samples from prostate cancer patients. DNA quantification in plasma was performed using real-time PCR (RT-PCR). We assessed the methylation status of GSTP1 in plasma DNA using methylation-specific PCR (MSP) assay, while the methylation status of RASSF1A and ATM genes was examined by the MethyLight technology. RT-PCR analysis was used for the detection of mRNA, PSMA, and CEA. In 58.3% of newly diagnosed prostate cancer patients and 26.7% of prostate cancer patients under therapy, plasma DNA levels were increased. Additionally, 48.5% of breast cancer patients showed plasma DNA levels above the cutoff limit. GSTP1 Promotor hypermethylation was detectable in 75% of plasma samples obtained from patients with newly diagnosed prostate cancer and in 36.8% of patients under therapy, whereas 26% and 14% of the breast cancer patients tested were positive for RASSF1A and ATM methylation, respectively. The combination of DNA load and promotor methylation status identified 88% of prostate cancer patients and 54% of breast cancer patients. This study shows that free-circulating DNA can be detected in cancer patients compared with disease-free individuals, and suggests a new, noninvasive approach for early detection of cancer.
Assuntos
Biomarcadores Tumorais , Neoplasias da Mama , DNA/sangue , Plasma/química , Neoplasias da Próstata , RNA/sangue , Antígenos de Superfície/sangue , Antígenos de Superfície/genética , Proteínas Mutadas de Ataxia Telangiectasia , Neoplasias da Mama/sangue , Neoplasias da Mama/diagnóstico , Neoplasias da Mama/genética , Antígeno Carcinoembrionário/sangue , Antígeno Carcinoembrionário/genética , Proteínas de Ciclo Celular/sangue , Proteínas de Ciclo Celular/genética , Metilação de DNA , Proteínas de Ligação a DNA/sangue , Proteínas de Ligação a DNA/genética , Feminino , Marcadores Genéticos , Glutamato Carboxipeptidase II/sangue , Glutamato Carboxipeptidase II/genética , Glutationa S-Transferase pi/sangue , Glutationa S-Transferase pi/genética , Humanos , Masculino , Regiões Promotoras Genéticas , Neoplasias da Próstata/sangue , Neoplasias da Próstata/diagnóstico , Neoplasias da Próstata/genética , Proteínas Serina-Treonina Quinases/sangue , Proteínas Serina-Treonina Quinases/genética , Proteínas Supressoras de Tumor/sangue , Proteínas Supressoras de Tumor/genéticaRESUMO
BACKGROUND: The aim of our study was to detect Ep-CAM mRNA in peripheral blood (PB) and bone marrow (BM) samples of patients with metastatic colorectal cancer, using a novel chromatographic method (molecular strip) for the detection of PCR amplified product and to confirm the results by the standard method of agarose gel electrophoresis. PATIENTS AND METHODS: Thirty patients participated in the present study providing 27 PB and 26 BM samples. PB samples were also obtained from 20 healthy volunteers. PCR products were detected using the molecular strip and the results were confirmed by 1.5% agarose gel electrophoresis. RESULTS: In total 26 out of 27 blood samples (96%) and 19 out of 26 bone marrow samples (73%) were found positive for Ep-CAM expression using both methods, whereas none of the 20 healthy controls was found positive for the above marker. CONCLUSION: Ep-CAM mRNA is highly expressive in peripheral blood of patients with metastatic colorectal cancer. Its prognostic significance should be evaluated in patients with resectable carcinomas. The new strip detection method is highly specific for the PCR product under investigation, reliable, easy to handle, fast and safe for the user.
Assuntos
Antígenos de Neoplasias/genética , Medula Óssea/química , Moléculas de Adesão Celular/genética , Cromatografia/métodos , Neoplasias Colorretais/genética , RNA Mensageiro/análise , Neoplasias Colorretais/sangue , Neoplasias Colorretais/patologia , Molécula de Adesão da Célula Epitelial , Humanos , Metástase Neoplásica , RNA Mensageiro/sangue , Reação em Cadeia da Polimerase Via Transcriptase ReversaRESUMO
The synthesis of 4-(1-adamantyl)-4,4-diarylbutylamines 1, 5-(1-adamantyl)-5,5-diarylpentylamines 2 and 6-(1-adamantyl)-6,6-diarylhexylamines 3 is described and the σ1, σ2-receptors and sodium channels binding affinity of compounds 1 were investigated. The in vitro activity of compounds 1, 2 and 3 against main cancer cell lines is significant. One of the most active analogs, 1a, had an interesting in vivo anticancer profile against the ovarian cancer cell line IGROV-1, which was associated with an anagelsic activity against the neuropathic pain induced by the main anticancer drugs.
Assuntos
Adamantano/química , Adamantano/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Receptores sigma/química , Adamantano/síntese química , Adamantano/uso terapêutico , Animais , Antineoplásicos/síntese química , Antineoplásicos/uso terapêutico , Sítios de Ligação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Desenho de Fármacos , Feminino , Humanos , Masculino , Camundongos , Camundongos SCID , Neoplasias/tratamento farmacológicoRESUMO
The synthesis of the adamantane phenylalkylamines 2a-d, 3a-c, and 4a-e is described. These compounds exhibited significant antiproliferative activity, in vitro, against eight cancer cell lines tested. The σ(1), σ(2), and sodium channel binding affinities of compounds 2a, 3a, 4a, and 4c-e were investigated. The most interesting analogue, 4a, exhibited significant in vivo anticancer profile on pancreas, prostate, leukemia, and ovarian cancer cell line xenografts together with apoptosis and caspase-3 activation. Inhibition of the cancer cells cycle at the sub-G1 level was also obtained with 4a. Finally, encouraging results were observed with 4a in vivo on mice, suggesting putative antimetastatic and analgesic activities of this compound.