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The residue of mulch film is a crucial source of microplastics (MPs) in agricultural fields. The effects of mulch film-derived MPs on the environmental behavior of pesticides in agriculture remain unclear. In the present study, the effects of MPs of different sizes (5 mm, 1 mm, 30 µm, and 0.3 µm) at environmentally relevant concentrations on pesticide transport were evaluated, and the mechanism was explored with respect to adsorption and pore structure using fluorescence visualization, the extended Derjaguin-Landau-Verwey-Overbeek model, and microcomputed tomography. MPs were found to be retained in the soil due to size limitation, pore capture, and surface adhesion. The presence of mm-sized MPs (5 and 1 mm) at a concentration of 0.25 % inhibited the leaching behavior of atrazine, metolachlor, and tebuconazole. MPs did not significantly alter the pesticide adsorption ability of the soil. The reduced leaching originated from the impact of MPs on soil pore structure. Specifically, the porosity increased by 16.2-25.0 %, and the connectivity decreased by 34.5 %. These results demonstrate that mm-sized MPs inhibit pesticide leaching by obstructing the pores and altering the transport pathways, thereby potentially elevating environmental risks, particularly to the soil ecosystem.
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Here, we describe an iron-catalyzed benzylic C-H thiolation of alkylarenes via photoinduced ligand-to-metal charge-transfer. The protocol features operational simplicity, mild reaction conditions, and the use of FeCl3 as catalyst and thiols/disulfides as sulfur sources, which enables the transformation of diverse benzylic C-H bonds into C-S bonds with a high efficiency.
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BACKGROUND: Treatment for parameningeal rhabdomyosarcoma (PM-RMS) has been a challenge since local control is difficult. The goal of this study was to analyse the impact of different local treatment approaches on childhood PM-RMS patients and help dispel the doubt that whether secondary radical surgery (SRS) should be encouraged in the management of PM-RMS. METHODS: A total of 17 children with PM-RMS who received unified systemic chemotherapy and individualized local therapy such as radiotherapy (RT) and/or SRS were included in this retrospective study. The overall survival (OS) and event free survival (EFS) were compared between groups adopting different local strategies. RESULTS: The 3-year OS and EFS of our PM-RMS patients was 75.5% and 56.5% respectively. The OS and EFS of patients who received SRS were both significantly lower than that of the non-SRS group (3-year OS: 50.0% vs 90.0%, P = .031; 3-year EFS: 33.3% vs 60.6%, P = .020). The OS and EFS of the patients who received RT was higher than that of the patients of the non-RT group (3-year OS: 85.6% vs 0%, P = .001; 3-year EFS: 64.0% vs 0%, P = .011). CONCLUSION: This study illustrates that SRS was associated with poor prognosis of PM-RMS and should not be routinely performed. Optimized RT strategies along with more intensive chemotherapy may be alternative options to improve the survival of patients with PM-RMS. Multi-center, large sample and prospective studies are needed to further validate these findings.
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Rabdomiossarcoma , Criança , Humanos , Lactente , Estudos Retrospectivos , Rabdomiossarcoma/tratamento farmacológico , Rabdomiossarcoma/radioterapia , Terapia Combinada , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , China/epidemiologiaRESUMO
BACKGROUND: Langerhans cell histiocytosis (LCH) is a myeloid neoplasia with potentially fatal consequences, and about 2/3 of cases involve the BRAFV600E kinase-activated mutation. Vemurafenib, a BRAF inhibitor, has demonstrated significant clinical improvements in LCH. However, the high relapse rate of LCH following cessation of vemurafenib therapy remains a major challenge, and alternative treatment strategies require further investigation. METHODS: In this retrospective multi-center study, we evaluated the efficacy and safety of vemurafenib combined with conventional chemotherapy in patients with severe or refractory LCH. RESULTS: Seventeen patients were enrolled in the study, with eleven classified as risk organ involvement (RO +). Six received the combination therapy as the primary treatment, and eleven after being refractory to prior chemotherapy. The overall response rate was 94.1%. Progression-free survival among all 17 patients was 70.6% (12/17) at a median follow-up of 32 months, and relapse-free survival among the 15 patients with discontinuation after a response was 73.3%(11/15) at a median follow-up of 34 months. Five of six patients (83.3%) with myeloid BRAFV600E mutations demonstrated molecular remission. The overall survival rate was 100%. Adverse events were mostly classified as grades 1 or 2. CONCLUSION: Our data suggest that the combination of vemurafenib and chemotherapy can achieve sustained clinical and molecular level relief in children with LCH, and side effects are tolerable.
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Inibidores de Proteínas Quinases , Proteínas Proto-Oncogênicas B-raf , Humanos , Criança , Vemurafenib , Proteínas Proto-Oncogênicas B-raf/genética , Inibidores de Proteínas Quinases/uso terapêutico , Terapia Combinada , MutaçãoRESUMO
The effects of ocean acidification (OA) and warming on the physiological processes of many marine species have been well documented. However, far less is known about the impacts of these global variables on chemical communication. In this study, we identified the barnacle waterborne settlement pheromone (BWSP) of Balanus albicostatus as adenosine (Ado). Our results showed that neither elevated temperature (30 °C vs. ambient 26 °C) nor elevated pCO2 (1000 µatm vs. ambient 400 µatm) significantly affected the release of Ado from B. albicostatus adults. Exposure to elevated temperature and OA did not impair larval cue perception for settlement in B. albicostatus; however, OA inhibited settlement under elevated temperature in the absence/presence of BWSP, and elevated temperature induced larval settlement only in the presence of BWSP under ambient pCO2 condition. These results provided important insights into barnacle aggregation behavior in changing oceans and may help to predict the consequences of climate change on barnacle populations.
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Água do Mar , Thoracica , Animais , Feromônios , Concentração de Íons de Hidrogênio , Adenosina , Acidificação dos Oceanos , Oceanos e Mares , Dióxido de CarbonoRESUMO
Feng et al. (2020) developed a simple, nondestructive, and cost-effective method to quantify polyphosphate (poly-P) in poly-P-accumulating organism (PAO)-enriched sludge samples through 30-h anaerobic exposure to 1 % (w/v) ethylenediaminetetraacetic acid (EDTA). This study optimized the N/P ratio (â¼2) of the PAO culture medium in order to provide excess P for poly-P formation in PAO cells. Subsequently, the fluorescence microscopic observation of stained cells confirmed that Corynebacterium glutamicum was a PAO species capable of heterotrophic nitrification. Finally, this study reevaluated the accuracy and specificity of the EDTA-based quantification method, using two confirmed PAO biomass, three confirmed non-PAO biomass, and two sludge samples. The 1 % (w/v) EDTA treatment appears destructive to non-PAO cells, causes the release of other P forms, and is not effective for all PAO species. Under the conditions, the actual P release amount should be calculated by subtracting approximately 8 mg P g-1 total suspended solids from the determination. The amounts of P released from sludge samples was determined not only by the PAO fractions described by Feng et al. but also by PAO community structure and sludge P content.
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Polifosfatos , Esgotos , Esgotos/microbiologia , Ácido Edético , Fósforo , Reatores Biológicos/microbiologiaRESUMO
Near-infrared (NIR) quantum dot (QD) light-emitting diodes (LEDs) (NIR-QLEDs) for recognition and tracking applications underpin the future of night-vision technology. However, the performance of environmentally benign materials and devices has lagged far behind that of their Pb-containing counterparts. In this study, we demonstrate the superior performance of NIR-QLEDs based on efficient AgAuSe QDs with contact interface mediation. Consequently, we reveal that using cysteamine-treated QD film contact heterointerfaces can effectively eliminate contact defects in devices and preserve their excellent emissive properties. Additionally, the dipole moment orientation of the coordinated additives is inverse of the heterojunction potential difference, simultaneously blocking electrons and enhancing hole injection in operando, optimizing the LED charge injection balance. These devices exhibit a high external quantum efficiency (EQE) and a power conversion efficiency (PCE) of 15.8 and 12.7% at 1046 nm, respectively, a sub-band gap turn-on voltage of 0.9 V, and a low current density (over 10% of the EQE from 0.0017 to 0.31 mA cm-2). These are the highest EQE and PCE values ever reported for environmentally benign NIR-QLEDs. The results of this study can provide a general strategy for the practical application of QDs in electroluminescent devices.
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BACKGROUND: Neuroblastoma (NB) remains associated with a low overall survival rate over the long term. Abnormal activation of the Hedgehog (HH) signaling pathway can activate the transcription of various downstream target genes that promote NB. Both arsenic trioxide (ATO) and itraconazole (ITRA) can inhibit tumor growth. OBJECTIVE: To determine whether ATO combined with ITRA can be used to treat NB with HH pathway activation, we examined the effects of ATO and ITRA monotherapy or combined inhibition of the HH pathway in NB. METHODS: Analysis of CCK8 and flow cytometry showed cell inhibition and cell cycle, respectively. Real-time PCR analysis was conducted to assess the mRNA expression of HH pathway. RESULTS: We revealed that as concentrations of ATO and ITRA increased, the killing effects of both agents on SK-N-BE(2) cells became more apparent. During G2/M, the cell cycle was largely arrested by ATO alone and combined with ITRA, and in the G0/G1 phase by ITRA alone. In the HH pathway, ATO inhibited the transcription of the SHH, PTCH1, SMO and GLI2 genes, however, ITRA did not. Instead of showing synergistic effects in a combined mode, ITRA decreased ATO inhibitory effects. CONCLUSION: We showed that ATO is an important inhibitor of HH pathway but ITRA can weaken the inhibitory effect of ATO. This study provides an experimental evidence for the clinical use of ATO and ITRA in the treatment of NB with HH pathway activation in cytology.
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Arsenicais , Neuroblastoma , Humanos , Trióxido de Arsênio/farmacologia , Proteínas Hedgehog/metabolismo , Itraconazol/farmacologia , Óxidos/farmacologia , Óxidos/uso terapêutico , Arsenicais/farmacologia , Arsenicais/uso terapêutico , Linhagem Celular Tumoral , Neuroblastoma/tratamento farmacológico , Neuroblastoma/metabolismo , Neuroblastoma/patologia , ApoptoseRESUMO
An 8-week feeding trial was conducted to evaluate the effects of L-methionine and methionine hydroxy analogue calcium (MHA-Ca) supplements in low-fishmeal diet on growth performance, hepatopancreas morphology, protein metabolism, anti-oxidative capacity, and immunity of Pacific white shrimp (Litopena eus vannamei). Four isonitrogenous and isoenergetic diets were designed: PC (203.3 g/kg fishmeal), NC (100 g/kg fishmeal), MET (100 g/kg fishmeal +3 g/kg L-methionine) and MHA-Ca (100 g/kg fishmeal +3 g/kg MHA-Ca). White shrimp (initial body weight 0.23 ± 0.00 g, 50 shrimp per tank) were allocated to 12 tanks and divided among 4 treatments in triplicates. In response to L-methionine and MHA-Ca supplementations, the shrimp exhibited higher weight gain rate (WGR), specific growth rate (SGR), condition factor (CF), and lower hepatosomatic index (HSI) compared to those fed the NC diet (p < 0.05). The WGR and SGR of shrimp fed L-methionine and MHA-Ca showed no difference with those in the PC diet (p > 0.05). Both of L-methionine and MHA-Ca supplementary diets significantly decreased the malondialdehyde (MDA) levels of shrimp when compared with the NC diet (p < 0.05). L-methionine supplementation improved the lysozyme (LZM) activity and total antioxidant capacity (T-AOC) of shrimp, while the MHA-Ca addition elevated the reduced glutathione (GSH) levels in comparison with those fed the NC diet (p < 0.05). Hypertrophied blister cells in hepatocytes were observed in shrimp fed the NC diet, and alleviated with L-methionine and MHA-Ca supplementations. Shrimp fed the MET and MHA-Ca diets had higher mRNA expression levels of target of rapamycin (tor) than those fed the NC diet (p < 0.05). Compared to the NC group, dietary MHA-Ca supplementation upregulated the expression level of cysteine dioxygenase (cdo) (p < 0.05), while L-methionine supplementation had no significant impact (p > 0.05). The expression levels of superoxide dismutase (sod) and glutathione peroxidase (gpx) were significantly upregulated by L-methionine supplemented diet in comparison with those in the NC group (p < 0.05). Overall, the addition of both L-methionine and MHA-Ca elevated the growth performance, facilitated protein synthesis, and ameliorated hepatopancreatic damage induced by plant-protein enriched diet in L. vannamei. L-methionine and MHA-Ca supplements enhanced anti-oxidants differently.
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Dendritic cells (DCs), a kind of specialized immune cells, play key roles in antitumor immune response and promotion of innate and adaptive immune responses. Recently, many strategies have been developed to utilize DCs in cancer therapy, such as delivering antigens and adjuvants to DCs and using scaffold to recruit and activate DCs. Here we outline how different DC subsets influence antitumor immunity, summarize the FDA-approved vaccines and cancer vaccines under clinical trials, discuss the strategies for engineering DCs and noninvasive tracking of DCs to improve antitumor immunotherapy, and reveal the potential of artificial neural networks for the design of DC based vaccines.
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Vacinas Anticâncer , Neoplasias , Humanos , Células Dendríticas , Imunoterapia , Vacinas Anticâncer/uso terapêutico , Adjuvantes Imunológicos , Neoplasias/tratamento farmacológicoRESUMO
BACKGROUND: Transcriptome sequencing is an effective tool to reveal the essential genes and pathways underlying countless biotic and abiotic stress adaptation mechanisms. Although severely challenged by diverse environmental conditions, the Pacific abalone Haliotis discus hannai remains a high-value aquaculture mollusk and a Chinese predominantly cultured abalone species. Salinity is one of such environmental factors whose fluctuation could significantly affect the abalone's cellular and molecular immune responses and result in high mortality and reduced growth rate during prolonged exposure. Meanwhile, hybrids have shown superiority in tolerating diverse environmental stresses over their purebred counterparts and have gained admiration in the Chinese abalone aquaculture industry. The objective of this study was to investigate the molecular and cellular mechanisms of low salinity adaptation in abalone. Therefore, this study used transcriptome analysis of the gill tissues and flow cytometric analysis of hemolymph of H. discus hannai (DD) and interspecific hybrid H. discus hannai â x H. fulgens â (DF) during low salinity exposure. Also, the survival and growth rate of the species under various salinities were assessed. RESULTS: The transcriptome data revealed that the differentially expressed genes (DEGs) were significantly enriched on the fluid shear stress and atherosclerosis (FSS) pathway. Meanwhile, the expression profiles of some essential genes involved in this pathway suggest that abalone significantly up-regulated calmodulin-4 (CaM-4) and heat-shock protein90 (HSP90), and significantly down-regulated tumor necrosis factor (TNF), bone morphogenetic protein-4 (BMP-4), and nuclear factor kappa B (NF-kB). Also, the hybrid DF showed significantly higher and sustained expression of CaM and HSP90, significantly higher phagocytosis, significantly lower hemocyte mortality, and significantly higher survival at low salinity, suggesting a more active molecular and hemocyte-mediated immune response and a more efficient capacity to tolerate low salinity than DD. CONCLUSIONS: Our study argues that the abalone CaM gene might be necessary to maintain ion equilibrium while HSP90 can offset the adverse changes caused by low salinity, thereby preventing damage to gill epithelial cells (ECs). The data reveal a potential molecular mechanism by which abalone responds to low salinity and confirms that hybridization could be a method for breeding more stress-resilient aquatic species.
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Aterosclerose , Gastrópodes , Animais , Gastrópodes/genética , Perfilação da Expressão Gênica , Salinidade , Estresse Salino/genética , TranscriptomaRESUMO
BACKGROUND: Neuroblastoma (NB) is one of the most common extracranial tumors with limited therapeutic options. Retinoic acid (RA) has been identified to play anticancer role against NB cells by inducing the differentiation and apoptosis of immature neuroblasts. However, silencing HoxC9 promoter by EZH2-induced H3K27me3 hypermethylation can lead to RA resistance. Previous studies have suggested that arsenic trioxide (ATO), an inhibitor of DNA methylation, could downregulate the expression of EZH2 in breast cancer cells. OBJECTIVES: In our study, we attempted to obtain some insight into the mechanisms of differentiation of RA-resistant NB cells by detecting the expressions of HoxC9 and EZH2 in NB cells treated with ATO, so as to provide a basis for the subsequent treatment of RA-resistant NB by ATO. MATERIAL AND METHODS: Two NB cell lines, SK-N-AS (retinoic acid-resistant neuroblastoma cells) and SK-N-SH (retinoic acid-sensitive neuroblastoma cells), were used in our experiments. Cell proliferation and apoptosis were respectively determined with Cell Counting Kit-8 (CCK-8) assay kit and Annexin V staining. The inverted phase contrast microscope was used to observe cell growth and measure the total length of nerve synapses. We employed label-free quantitative proteomic analysis to profile ATO-dependent changes in the proteome of NB cells. Western blot was used to detect the expressions of HoxC9, HoxD8 and EZH2. RESULTS: Arsenic trioxide inhibited the cell proliferation and increased apoptosis and total length of synapses in two NB cell lines. The expressions of HoxC9 and HoxD8 were upregulated, while the expression of EZH2 was downregulated in the SK-N-AS cell line. No significant changes in the 3 proteins mentioned above were observed in the SK-N-SH cell line after ATO treatment. CONCLUSIONS: Arsenic trioxide may reactivate the expression of HoxC9 by downregulating EZH2, which leads to restoring RA sensitivity and promoting the differentiation and apoptosis of RA-resistant NB cells.
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Neuroblastoma , Tretinoína , Apoptose , Trióxido de Arsênio/metabolismo , Trióxido de Arsênio/farmacologia , Trióxido de Arsênio/uso terapêutico , Diferenciação Celular , Linhagem Celular Tumoral , Proteínas de Homeodomínio/genética , Proteínas de Homeodomínio/metabolismo , Proteínas de Homeodomínio/uso terapêutico , Humanos , Neuroblastoma/tratamento farmacológico , Neuroblastoma/genética , Proteômica , Tretinoína/farmacologia , Regulação para CimaRESUMO
The recurrence and metastasis of tumor after surgery is the main cause of death for patients with breast cancer. Systemic chemotherapy suffered from low delivery efficiency to tumors and the side effects of chemo drugs. Localized chemotherapy using drug-containing implants is an alternative, while the reconstruction of breast tissue is generally considered after chemotherapy, resulting in a second surgery for patients. Here, we describe a strategy using implantable drug-containing polymeric scaffolds to deliver chemo drugs directly to the post-resection site, and simultaneously provide mechanical support and regenerative niche for breast tissue reconstruction. When doxorubicin was loaded in mesoporous silica nanoparticles and subsequently incorporated into polycaprolactone scaffolds (DMSN@PCL), a 9-week sustained drug release was achieved post implantation in mice. The local recurrence of residual tumor after surgery was significantly inhibited within 4 weeks in a post-surgical mouse model bearing xenograft MDA-MB-231 tumor. DMSN@PCL scaffolds exhibited good biocompatibility in mice during the treatment. We believe our strategy holds great promise as an adjuvant localized chemotherapy in clinics for combating post-resection breast cancer recurrence.
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Antineoplásicos , Neoplasias da Mama , Nanopartículas , Animais , Antineoplásicos/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Doxorrubicina/uso terapêutico , Feminino , Humanos , Camundongos , PoliésteresRESUMO
Cellulose is widely used as an effective sorbent to treat wastewater. Cellulosic sorbents have the advantage of biodegradability, as they are natural plant-based materials, compared with the synthetic materials such as polypropylene (PP) or polyurethane (PU). Among the raw biomass materials used for cellulose production, rice husk is one of the most cost competitive and widely available. In this work, biological treatments are compared to find the most effective treatment method for cellulose fibre production from rice husk. Using biological delignification, cellulose was extracted from raw rice husk and acetylated to acquire hydrophobicity. Delignification was performed using both bacteria and fungi and their results were compared. The white-rot fungi strain using 'Aspergillus flavus CICC 40258' was found to be the most effective treatment method, achieving a modified product with up to 55% w/w cellulose concentration. Acetylation further facilitated the sorption process and the maximum oil uptake capacity using delignification and acetylation treatment was found to be 20â g/g. The as-prepared sorbents exhibited high oil uptake rates and saturation capacity was reached after 5â min of contact with oil. The kinetic study presents a good correlation with the pseudo-second order model. The isothermal studies demonstrated that the oil sorption capacity of rice husk follows the Langmuir model as compared with the Freundlich model.
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Oryza , Poluição por Petróleo , Acetilação , Adsorção , CinéticaRESUMO
Hand, foot, and mouth disease (HFMD) is well recognized as one of the major threats to children's health globally. The increasing complexity of the etiology of HFMD still challenges disease control in China. There is little surveillance of the molecular epidemiological characteristics of the enteroviruses (EVs) that cause HFMD in Neijiang city or the Sichuan Basin area in Southwest China. In this study, demographic and epidemiological information for 14,928 probable HFMD cases was extracted and analyzed to describe the epidemic features of HFMD in Neijiang city from Jan 2010 to Dec 2017. The swab samples of select probable HFMD cases from 2012 to 2017 were tested by reverse transcription (RT) real-time PCR to identify the serotype distribution of EVs, and 110 randomly selected RT-real-time PCR positive samples were then amplified and analyzed for the VP1 or VP4 regions of EVs to further analyze the phylogenetic characteristics of the circulating strains in this area. The eight-year average annual incidence was 49.82 per 100,000 in Neijiang. The incidence rates varied between 19.51 and 70.73 per 100,000, demonstrating peaks of incidence in even-number years (2012, 2014 and 2016). The median age of the probable cases was 27 months and the interquartile range (25th to 75th percentile) of ages for the probable HFMD cases was between 14 and 42 months. The male-to-female ratio of the probable HFMD cases was 1.47:1, and scattered children were the major population classification (81.7%). Two epidemic peaks were observed: one major peak between April and July and the other lesser peak between October and December. Of 6513 probable cases tested with RT-real-time PCR, 4015 (61.6%) were positive for enterovirus with the serotype distribution as follows: EV71+, 30.1% (n = 1210); CV-A16+, 28.7% (n = 1154) and a sole pan-enterovirus+, 41.1% (n = 1651). A total of 91 cases (82.7%, 91/110) were successfully amplified and underwent phylogenetic analysis: all EV71+ cases were C4a serotype (n = 23/30); all CV-A16+ cases were B2b serotype (n = 24/30); of 42 sole pan-enterovirus+ samples, 20 were CV-A6, 14 were CV-A10 and the rest within this group were CV-A4 (n = 4), CV-A8 (n = 2), CV-A9 (n = 1) and CV-B3 (n = 1). Our findings provide important evidence that aids the improvement of strategies for vaccination against HFMD and comprehensive disease control in China.
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Proteínas do Capsídeo , Enterovirus Humano B/genética , Doença de Mão, Pé e Boca , Filogenia , Sorogrupo , Proteínas Estruturais Virais , Proteínas do Capsídeo/sangue , Proteínas do Capsídeo/genética , Pré-Escolar , China/epidemiologia , Feminino , Doença de Mão, Pé e Boca/sangue , Doença de Mão, Pé e Boca/epidemiologia , Doença de Mão, Pé e Boca/genética , Doença de Mão, Pé e Boca/virologia , Humanos , Incidência , Lactente , Masculino , Estudos Retrospectivos , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Estudos Soroepidemiológicos , Proteínas Estruturais Virais/sangue , Proteínas Estruturais Virais/genéticaRESUMO
A series of novel nucleotide phosphoramidites were rationally designed and synthesized and were then site-specifically incorporated in DNA oligonucleotide probes with pyrene-modified phosphate. These oligodeoxynucleotide (ODN) probes almost have no inherent fluorescence emission with pyrene modification at 3' phosphate of corresponding nucleotides as a result of the photoinduced electron-transfer quenching effect of nucleobases (thymidine â¼ cytidine > guanosine â« adenosine). However, strong fluorescence emission was observed only with the perfectly matched duplex for the probes with pyrene modified at 3' phosphate of thymidine and cytidine. These rationally designed ODN probes successfully worked as "turn on" fluorescence oligonucleotide sensors for single-nucleotide polymorphism (SNP) and were used for detecting a single BRAF mutation site (V600E) of human melanoma.
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Sondas de DNA/química , Melanoma/genética , Mutação , Fosfatos/química , Polimorfismo de Nucleotídeo Único/genética , Proteínas Proto-Oncogênicas B-raf/genética , Pirenos/química , Sondas de DNA/síntese química , Humanos , Estrutura MolecularRESUMO
Novel 1-O- and 14-O-derivatives of oridonin were synthesized and biologically evaluated. All of the derivatives exhibited stronger cytotoxicity against six cancer cell lines (BGC-7901, SW-480, HL-60, BEL-7402, A549, and B16) than oridonin in vitro, and some of them were more potent than oridonin and cyclophosphamide in vivo. Compounds Ib and IIg were the most potent with the IC(50) values of 0.84 microM for Ib in HL-60 cell and 1.00 microM for IIg in BEL-7402 cell.