首页 | 本学科首页   官方微博 | 高级检索  
相似文献
 共查询到20条相似文献,搜索用时 11 毫秒
1.
A novel method for selective and direct phosphorylation of various 1,3-diols using silver(I) oxide, tetrabenzyl pyrophosphate (TBPP), and tetrahexylammonium iodide affording mono-phosphates was developed. We applied the present method to the synthesis of FTY720-phosphate.  相似文献   

2.
3.
Journal of Radioanalytical and Nuclear Chemistry - Receptor tyrosine kinase Ror1 is widely expressed during embryogenesis but it is absent within most mature tissues. However, expression of Ror1...  相似文献   

4.
Dyglomera® is an aqueous ethanol extract of the fruit pods of Dichrostachys glomerata, a Cameroonian spice. Several studies have shown its anti-diabetic and anti-obesity effects. However, the underlying mechanisms for such effects remain unclear. Thus, the objective of this study was to investigate the anti-obesity effect of Dyglomera® and its underlying mechanisms in mice with high-fat diet-induced obesity and 3T3-L1 adipocytes. Our results revealed that Dyglomera® inhibited adipogenesis and lipogenesis by regulating AMPK phosphorylation in white adipose tissues (WATs) and 3T3-L1 adipocytes and promoted lipolysis by increasing the expression of lipolysis-related proteins. These results suggest that Dyglomera® can be used as an effective dietary supplement for treating obesity due to its modulating effect on adipogenesis/lipogenesis and lipolysis.  相似文献   

5.
6.
7.
研究了过渡金属取代的Kiggen型结构的杂多酸盐Na_6PMo_(11)FeO_(40)对体外培养的小鼠黑色素瘤B16细胞的生物学效应,并分析了其对4种细菌的抗菌活性.结果显示:不同浓度的Na_6PMo_(11)FeO_(40)对B16细胞的细胞形态和数量有不同程度的影响,对B16细胞的增殖率、酪氨酸酶活性以及黑色素合成量的抑制呈现出明显的浓度效应.浓度为50~200μmol/L的Na_6PMo_(11)FeO_(40)能显著抑制B16细胞增殖(P0.05或P0.01);浓度为200μmol/L的Na_6PMo_(11)FeO_(40)对酪氨酸酶活性抑制极显著(P0.01),IC50为166.5μmol/L;Na_6PMo_(11)FeO_(40)对藤黄八叠球菌、金黄色葡萄球菌、枯草芽孢杆菌和大肠杆菌均有抗菌作用,且对球菌的抑制效果优于杆菌.实验结果表明,Na_6PMo_(11)FeO_(40)可作为具有防腐抑菌功能的新型酪氨酸酶抑制剂.  相似文献   

8.
To understand molecular networking at the cellular level, analyses of processes and effects at the single-cell level are most appropriate. Usual biochemical or molecular biological analyses are based on integrated signals of numerous cells which differ, however, in their expression and activity profiles. Here we show that it is possible to determine different types of properties of individual cells by means of a specifically designed microfluidic device. As part of investigations to characterize the human urothelial cell line 5637 as a potential model system for studies of toxic and carcinogenic effects on urothelial cells, we use this cell line to assign cytochrome P450 activity, and expression of the enzymes involved, to individual cells. It is shown that the cell population is very heterogeneous with respect to the extent and kinetics of CYP1A1-dependent ethoxyresorufin O-deethylase (EROD). This is also true for the cells’ CYP1A1 protein content. With some exceptions, the EROD activity largely coincides with the presence of CYP1A1 protein in the cells. The results obtained with the microfluidic device are promising and open up new perspectives with regard to multi-property determinations in individual cells and to studies focusing on the biochemical and molecular heterogeneity of cells. Figure Formation of fluorescent resorufin from ethoxyresorufin by cytochrome P450 activity in urothelial cells attached within the chamber of a microfluidic device  相似文献   

9.
The receptor for advanced glycation end products (RAGE) has been reported to have a pivotal role in the pathogenesis of Alzheimer''s disease (AD). This study investigated RAGE levels in the hippocampus and cortex of a triple transgenic mouse model of AD (3xTg-AD) using western blotting and immunohistochemical double-labeling to assess cellular localization. Analysis of western blots showed that there were no differences in the hippocampal and cortical RAGE levels in 10-month-old adult 3xTg-AD mice, but significant increases in RAGE expression were found in the 22- to 24-month-old aged 3xTg-AD mice compared with those of age-matched controls. RAGE-positive immunoreactivity was observed primarily in neurons of aged 3xTg-AD mice with very little labeling in non-neuronal cells, with the notable exception of RAGE presence in astrocytes in the hippocampal area CA1. In addition, RAGE signals were co-localized with the intracellular amyloid precursor protein (APP)/amyloid beta (Aβ) but not with the extracellular APP/Aβ. In aged 3xTg-AD mice, expression of human tau was observed in the hippocampal area CA1 and co-localized with RAGE signals. The increased presence of RAGE in the 3xTg-AD animal model showing critical aspects of AD neuropathology indicates that RAGE may contribute to cellular dysfunction in the AD brain.  相似文献   

10.
Amino acids 1 and 2 were designed and synthesized as the conformationally constrained analogues of (1S, 3R)‐ or (1S, 3S)‐ACPDs, and the selective agonists of mGluRs. The synthesis started from (R)‐phenylglycine using Seebach′s stereocenter self‐regeneration method and intramolecular acylation as key steps. No activity was found when 1 and 2 were tested as either mGluR agonist or antagonist.  相似文献   

11.
A sensitive, specific and rapid LC‐ESI‐MS/MS method has been developed and validated for the quantification of epacadostat in mouse plasma using tolbutamide as an internal standard (IS) as per regulatory guidelines. Sample preparation was accomplished through a protein precipitation. Chromatographic separation was performed on an Atlantis dC18 column using a binary gradient using mobile phase A (acetonitrile) and B (0.2% formic acid in water) at a flow rate of 0.90 mL/min. Elution of epacadostat and IS occurred at ~2.41 and 2.51 min, respectively. The total chromatographic run time was 3.2 min. A linear response function was established in the concentration range of 1.07–533 ng/mL. The intra‐ and inter‐day accuracy and precision were in the ranges of 1.81–12.9 and 3.80–11.1%, respectively. This novel method has been applied to a pharmacokinetic study in mice.  相似文献   

12.
A highly sensitive, rapid assay method was developed and validated for the estimation of lorglumide in mouse plasma using liquid chromatography coupled to tandem mass spectrometry with electrospray ionization in positive‐ion mode. The assay procedure involves extraction of lorglumide and phenacetin (internal standard, IS) from mouse plasma with simple protein precipitation. Chromatographic separation was achieved using an isocratic mobile (0.2% formic acid solution–acetonitrile, 20:80, v/v) at a flow‐rate of 0.5 mL/min on an Atlantis dC18 column maintained at 40 °C with a total run time of 4.0 min. The MS/MS ion transitions monitored were 459.2 → 158.4 for lorglumide and 180.1 → 110.1 for IS. Method validation was performed as per FDA guidelines and the results met the acceptance criteria. The lower limit of quantitation achieved was 0.42 ng/mL and the linearity range extended from 0.42 to 500 ng/mL. The intra‐ and inter‐day precisions were in the ranges of 1.47–10.9 and 3.56–7.53, respectively. Copyright © 2011 John Wiley & Sons, Ltd.  相似文献   

13.
Nanoparticles usually have better outcomes than the bulk samples of the same element because they possess a higher specificity level than the larger particles. This is also true for silver nanoparticles, and little amount of these materials has high remedial effects. Silver nanoparticles are used as a therapeutic tool for the treatment of several diseases such as cancer. In this study, silver nanoparticles using chitosan (AgNPs-chitosan composite) are reported for the first time to exert a dietary therapeutic potential compared to Daunorubicin in an animal model of acute myeloid leukemia. The synthesized AgNPs-chitosan composite was characterized using different techniques including ultraviolet–visible spectroscopy, fourier-transform infrared spectroscopy, energy dispersive X-ray spectrometry, scanning electron microscopy, and transmission electron microscopy. FTIR findings suggested antioxidant compounds in the nanoparticles were the sources of reducing power, reducing silver ions to AgNPs. SEM and TEM images exhibited a uniform spherical morphology and average diameters of 30 nm for the nanoparticles. Then, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging test was done to evaluate the antioxidant potentials of Daunorubicin, AgNO3, chitosan, and AgNPs-chitosan composite. DPPH test revealed similar antioxidant potentials for Daunorubicin and AgNPs-chitosan composite. For the analyzing of cytotoxicity effects of Daunorubicin, AgNO3, chitosan, and AgNPs, 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromidefor (MTT) assay was used on HUVEC, 32D-FLT3-ITD, and Murine C1498 cell lines. AgNPs-chitosan composite similar to Daunorubicin had low cell viability dose-dependently against 32D-FLT3-ITD and Murine C1498 cell lines without any cytotoxicity on HUVEC cell line. In vivo design, induction of acute myeloid leukemia was done by 7,12-Dimethylbenz[a]anthracene in 50 mice. Then, the animals were randomly divided into six subgroups, including control, untreated, Daunorubicin, AgNO3, chitosan, and AgNPs-chitosan composite. Similar to Daunorubicin, AgNPs-chitosan composite significantly (P ≤ .01) decreased the weight of the body, the pro-inflammatory cytokines, and the total white blood cells, blast, neutrophil, monocyte, eosinophil, and basophil counts and increased the anti-inflammatory cytokines and the lymphocyte, platelet, and red blood cell parameters as compared to the untreated mice. These results show that the inclusion of chitosan improves the therapeutic properties of AgNPs-chitosan composite, which led to a significant enhancement in the antioxidant, cytotoxicity, and anti-acute myeloid leukemia activities of the nanoparticles. It appears that AgNPs-chitosan composite can be used as a chemotherapeutic drug for the treatment of acute myeloid leukemia in the clinical trial.  相似文献   

14.
The high prevalence of cancer has been increased the rate of studying about the new formulation of chemotherapeutic drugs. In this regards, one of the suitable options is the use of metal nanoparticles for formulating these drugs. In the recent study, Lens culinaris seed aqueous extract conjugated gold nanoparticles (AuNPs) are reported for the first time to exert a dietary therapeutic potential compared to mitoxantrone in an animal model of acute myeloid leukemia. The synthesized AuNPs were characterized using different techniques including UV–Vis., FT-IR, XRD, FE-SEM, and TEM. DPPH free radical scavenging test was done to evaluate the antioxidant potentials of HAuCl4, L. culinaris, AuNPs, and mitoxantrone. For the analyzing of cytotoxicity effects of HAuCl4, L. culinaris, AuNPs, and mitoxantrone, MTT assay was used on HUVEC, 32D-FLT3-ITD, Human HL-60/vcr, and Murine C1498 cell lines. In vivo assay, induction of acute myeloid leukemia was done by 7,12-Dimethylbenz[a]anthracene (DMBA) in 75 mice. Then, the animals were randomly divided into six subgroups, including control, untreated, HAuCl4, L. culinaris, AuNPs, and mitoxantrone. SEM and TEM images showed uniform spherical morphology and average diameters of 10–40 nm for the nanoparticles. DPPH test revealed similar antioxidant potentials for mitoxantrone and AuNPs. Similar to mitoxantrone, AuNPs had low cell viability dose-dependently against 32D-FLT3-ITD, Human HL-60/vcr, and Murine C1498 cell lines without any cytotoxicity on HUVEC cell line. AuNPs and mitoxantrone significantly (p ≤ 0.05) reduced the weight and volume of liver and spleen, the pro-inflammatory cytokines, and the total WBC, blast, neutrophil, monocyte, eosinophil, and basophil counts and increased the mRNA expression of Sphingosine-1-phosphate receptor-1 and Sphingosine-1-phosphate receptor-5, the anti-inflammatory cytokines, and the lymphocyte, platelet, and RBC parameters as compared to the untreated mice. It looks that AuNPs can be administrated as a chemotherapeutic supplement or drug for the treatment of acute myeloid leukemia in the clinical trial.  相似文献   

15.
Recently, metallic nanoparticles have been used for the treatment of several disorders, such as cancer. Indeed, finding the chemotherapeutic drug of nanoparticles is in researching the priority of both developed and developing countries. The present study confirms the ability of aqueous extract of Thymus vulgaris grown under in vitro condition for the biosynthesis of gold nanoparticles (AuNPs). Also, in this study, we indicated the antioxidant, cytotoxicity, and anti-acute myeloid leukemia properties of AuNPs compared to doxorubicin in a leukemic mouse model. The synthesized AuNPs were characterized using different techniques including X-ray diffraction (XRD), energy Dispersive X-ray Spectrometry (EDS), fourier-transform infrared spectroscopy (FT-IR) spectroscopy, ultraviolet–visible spectroscopy (UV–Vis.), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). In vivo design, induction of acute myeloid leukemia was done by 7,12-Dimethylbenz[a]anthracene (DMBA) in 75 mice. Then, the animals were randomly divided into six subgroups, including control, untreated, doxorubicin, AuNPs, T. vulgaris, and HAuCl4. By quantitative real-time PCR, sphingosine-1-phosphate receptor-1 and sphingosine-1-phosphate receptor-5 mRNA expression in lymphocytes were significantly (P ≤ 0.01) raised by treating the leukemic mice with the AuNPs and doxorubicin. Also, AuNPs similar to doxorubicin, significantly (P ≤ 0.01) enhanced the anti-inflammatory cytokines (IL4, IL5, IL10, IL13, and IFNα) and the platelet, lymphocyte, and red blood cell (RBC) parameters and reduced the pro-inflammatory cytokines (IL1, IL6, IL12, IL18, IFNY, and TNFα), and the total white blood cell (WBC), blast, monocyte, neutrophil, eosinophil, and basophil counts as compared to the untreated mice. In vitro design, 2,2-diphenyl-1-picrylhydrazyl (DPPH) test revealed similar antioxidant potentials for doxorubicin and AuNPs. Furthermore, AuNPs similar to doxorubicin had low cell viability dose-dependently against 32D-FLT3-ITD, Human HL-60/vcr, and Murine C1498 cell lines without any cytotoxicity on HUVEC cell line. Above results confirm the excellent antioxidant, cytotoxicity, and anti-acute myeloid leukemia effects of AuNPs compared to doxorubicin. After confirming these results in clinical trial studies, AuNPs can be used as a chemotherapeutic drug for the treatment of acute myeloid leukemia in human.  相似文献   

16.
According to chemotherapeutic properties of medicinal plants, pharmacologists have always tried to synthesize and formulate the new chemotherapeutic supplements or drugs of metallic nanoparticles using plants. In this study, Camellia sinensis leaf aqueous extract-based gold nanoparticles (AuNPs) are reported for the first time to exert a dietary therapeutic potential compared to Daunorubicin in an animal model of acute myeloid leukemia. The synthesized AuNPs were characterized using different techniques including UV-Vis., FT-IR spectroscopy, TEM, EDS, FE-SEM, and XRD. DPPH free radical scavenging test was done to evaluate the antioxidant potentials of HAuCl4, C. sinensis, AuNPs, and daunorubicin. For the analyzing of cytotoxicity effects of HAuCl4, C. sinensis, AuNPs, and daunorubicin, MTT assay was used on HUVEC, Human HL-60/vcr, 32D-FLT3-ITD, and Murine C1498 cell lines. In vivo design, induction of acute myeloid leukemia was done by 7,12-Dimethylbenz[a]anthracene (DMBA) in 75 mice. Then, the animals were randomly divided into six subgroups, including control, untreated, HAuCl4, C. sinensis, AuNPs, and daunorubicin. FTIR findings suggested antioxidant compounds in the nanoparticles were the sources of reducing power, reducing gold ions to AuNPs. SEM and TEM images exhibited a uniform spherical morphology and diameters of ~20-30 nm for the nanoparticles. DPPH test revealed similar antioxidant potentials for daunorubicin and AuNPs. These nanoparticles similar to daunorubicin had low cell viability dose-dependently against Human HL-60/vcr, 32D-FLT3-ITD, and Murine C1498 cell lines without any cytotoxicity on HUVEC cell line. AuNPs similar to daunorubicin, significantly (p≤0.05) increased the anti-inflammatory cytokines and the lymphocyte, platelet, and RBC parameters and decreased the weight and volume of liver and spleen, the pro-inflammatory cytokines, and the total WBC, blast, neutrophil, monocyte, eosinophil, and basophil counts, as compared to the untreated mice. According to the above results, it appears that AuNPs can be used as a chemotherapeutic drug for the treatment of acute myeloid leukemia in the clinical trial.  相似文献   

17.
A straightforward and common analytical method for α‐tocopherol (αT) determination in various biological samples, including plasma, red blood cells (RBC), tissues and cultured cell lines, was developed and validated, using a reverse phase‐chromatographic method (RP‐HPLC). Even though many chromatographic methods for αT determination have been reported, most of them require readjustment when applied to different types of samples. Thus, an effective and simple method for αT determination in different biological matrices is still necessary, specifically for translational research. This method was applied using a C18 column (250 × 4.6 mm, 5 µm particle size) under isocratic elution with MeOH:ACN:H2O (90:9:1 v/v/v) at a flow rate of 1 mL/min and detected using photodiode array at 293 nm. Linearity (r >0.9997) was observed for standard calibration with inter‐ and intraday variation of standard <4%. Lower limits of detection and quantification for αT in this assay were 0.091 and 0.305 µg/mL respectively. Validation proved the method to be selective, linear, accurate and precise. The method was successfully applied in great variety of biological samples, that is, human and mouse plasma, RBCs, murine tissues and human/mouse/rat cultured cell lines. More importantly, a single protocol of extraction and detection can be applied, making this method very convenient for standardization of different types of samples. Copyright © 2014 John Wiley & Sons, Ltd.  相似文献   

18.
A simple and sensitive method for the simultaneous determination of plasma concentrations of five polyamines in normal and Hepatoma‐22 mice, and mice treated with Mylabris and Acanthopanax senticosus was developed by HPLC‐ESI‐MS. Male Kunming mice were divided into nine groups, a control group (inoculation without treatment), a positive group (Cyclophosphamide), treatment groups [Mylabris (4, 8, 16 mg/kg), Acanthopanax senticosus (6, 12, 24 g/kg)] and a normal group (without inoculation). Twenty‐four hours after the last administration, plasma samples were collected. The derived polyamines were separated on a C18 column by a gradient elution using methanol–water with excellent linearity within the range from 2.5 to 1000 ng/mL. Polyamines were confirmed as useful biochemical markers of hepatoma. The differences in anti‐cancer therapeutic efficacy between Mylabris and Acanthopanax senticosus might contribute to the variability of polyamine levels in vivo. This HPLC‐ESI‐MS method was successfully applied to investigate the relationship between polyamines and cancer in mice and might be a useful method to test the activity of potential anti‐tumor drugs. Copyright © 2012 John Wiley & Sons, Ltd.  相似文献   

19.
Isocitrate dehydrogenase (IDH) inhibitors comprise a novel class of anticancer drugs, which are approved to treat acute myeloid leukemia patients having mutations on IDH1/2. We report the development and validation of a high‐performance liquid chromatography (HPLC) method for the simultaneous quantitation of IDH inhibitors, namely enasidenib (EDB), ivosidenib (IDB) and vorasidenib (VDB), in mouse plasma as per the US Food and Drug Administration regulatory guidelines. The method involves extraction of EDB, IDB and VDB along with internal standard (IS; phenacetin) from mouse plasma (100 μl) using a simple protein precipitation process. The chromatographic analysis was performed on an HPLC system using a gradient mobile phase (comprising 10 mm ammonium acetate and acetonitrile in a flow‐gradient) and an X‐Terra Phenyl column. The UV detection wave length was set at λmax 265 nm. EDB, IDB, VDB and the IS eluted at 7.36, 8.60, 9.50 and 5.12 min, respectively, with a total run time of 10 min. The calibration curve was linear over a concentration range of 0.20–12.5 μg/ml for EDB and 0.50–12.5 μg/ml for IDB and VDB (r2 = ≥0.998 for all of the analytes). Validation results met the acceptance criteria. The validated HPLC method was successfully applied to a pharmacokinetic study in mice.  相似文献   

20.
There is an increasing commercial demand for nanoparticles due to their wide applicability in various areas such as electronics, catalysis, chemistry, energy, and medicine. Recently, researchers have tried to synthesize the chemotherapeutic drugs from metallic nanoparticles especially gold and silver nanoparticles. In the current study, silver nanoparticles using Spinacia oleracea L. leaf aqueous extract (AgNPs) are reported for the first time to exert a dietary remedial property compared to doxorubicin in an animal model of acute myeloid leukemia. The synthesized AgNPs were characterized using different techniques including UV-Vis., EDS, TEM, FT-IR, and FE-SEM. UV-Vis. indicates an absorption band at 462 nm that is related to the surface plasmon resonance of AgNPs. In EDS, metallic silver nanocrystals indicated an optical absorption peak at roughly 4keV. TEM and FE-SEM images exhibited a uniform spherical morphology and diameters of 20–40 nm for the nanoparticles. FT-IR findings suggested antioxidant compounds in the nanoparticles were the sources of reducing power, reducing silver ions to AgNPs. In vivo design, induction of acute myeloid leukemia was done by 7,12-Dimethylbenz[a]anthracene in 75 mice. Then, the animals were randomly divided into six subgroups, including control, untreated, AgNO3, S. oleracea, AgNPs, and doxorubicin. Similar to doxorubicin, AgNPs significantly (p ≤ 0.01) reduced the pro-inflammatory cytokines, and the total WBC, blast, neutrophil, monocyte, eosinophil, and basophil counts and increased the weight of the body, the anti-inflammatory cytokines and the lymphocyte, platelet, and RBC parameters as compared to the untreated mice. DPPH free radical scavenging test was done to evaluate the antioxidant potentials of AgNO3, S. oleracea, AgNPs, and doxorubicin. DPPH test revealed similar antioxidant potentials for doxorubicin and AgNPs. For the analyzing of cytotoxicity effects of AgNO3, S. oleracea, AgNPs, and doxorubicin, MTT assay was used on HUVEC, Human HL-60/vcr, 32D-FLT3-ITD, and Murine C1498 cell lines. AgNPs similar to doxorubicin had low cell viability dose-dependently against Human HL-60/vcr, 32D-FLT3-ITD, and Murine C1498 cell lines without any cytotoxicity on HUVEC cell line. These results reveal that the inclusion of S. oleracea leaf aqueous extract improves the remedial effects of AgNPs, which led to a significant enhancement in the antioxidant, cytotoxicity, and anti-acute myeloid leukemia potentials of the nanoparticles. It seems that AgNPs can be applied as a chemotherapeutic supplement or drug for the treatment of acute myeloid leukemia in the clinical trial.  相似文献   

设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号