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The heat tolerance of tumor cells induced by heat shock proteins (HSPs) is the major factor that seriously hinders further application of PTT, as it can lead to tumor inflammation, invasion, and even recurrence. Therefore, new strategies to inhibit HSPs expression are essential to improve the antitumor efficacy of PTT. Here, we prepared a novel nanoparticle inhibitor by synthesizing molecularly imprinted polymers with a high imprinting factor (3.1) on the Prussian Blue surface (PB@MIP) for combined tumor starvation and photothermal therapy. Owing to using hexokinase (HK) epitopes as the template, the imprinted polymers could inhibit the catalytic activity of HK to interfere with glucose metabolism by specifically recognizing its active sites and then achieve starvation therapy by restricting ATP supply. Meanwhile, MIP-mediated starvation downregulated the ATP-dependent expression of HSPs and then sensitized tumors to hyperthermia, ultimately improving the therapeutic effect of PTT. As the inhibitory effect of PB@MIP on HK activity, more than 99% of the mice tumors were eliminated by starvation therapy and enhanced PTT.
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Hipertermia Inducida , Impresión Molecular , Nanopartículas , Neoplasias , Animales , Ratones , Polímeros Impresos Molecularmente , Terapia Fototérmica , Hexoquinasa , Neoplasias/tratamiento farmacológico , Nanopartículas/química , Adenosina TrifosfatoRESUMEN
Although Polychlorinated biphenyl (PCB) levels are decreased in the environment, the adverse effects of gestational exposure on the mother and offspring cannot be ignored due to the vulnerability of the fetus. In the present study, pregnant Balb/c mice were administered PCB52 (1 mg/kg BW/day) or corn oil vehicle by gavage until parturition. In the dams, PCB52 caused histopathological changes in the liver, higher serum levels of aminotransferase and alanine aminotransferase, and activated apoptosis and autophagy, suggesting hepatotoxicity. Overexpressed indicators of TLR4 pathway were observed in the liver of PCB52-exposed dams, indicated hepatic inflammation. Moreover, PCB52 exposure weakened the intestinal barrier and triggered inflammatory response, which might contribute to the hepatic inflammation by gut-liver axis. In the pups, prenatal PCB52 exposure affected the sex ratio at birth and reduced birth length and weights. Similar to the dams, prenatal PCB52 exposure induced hepatotoxicity in the pups without gender difference. Consistent with the alteration of gut microbiota, intestinal inflammation was confirmed, accompanying the disruption in the intestinal barrier and the activation of apoptosis and autophagy in the PCB52-exposed pups. Intestinal injury might be responsible for hepatotoxicity at least in part. Taken together, these findings suggested that gestational PCB52 exposure induced hepatic and intestinal injury in both maternal and offspring mice by arousing inflammation.
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Enfermedad Hepática Inducida por Sustancias y Drogas , Enfermedades del Sistema Digestivo , Enfermedades Intestinales , Bifenilos Policlorados , Efectos Tardíos de la Exposición Prenatal , Alanina Transaminasa , Animales , Aceite de Maíz , Femenino , Inflamación/inducido químicamente , Ratones , Bifenilos Policlorados/toxicidad , Embarazo , Efectos Tardíos de la Exposición Prenatal/inducido químicamente , Receptor Toll-Like 4RESUMEN
A pilot study on the ethanol extracts of Agrimonia pilosa found to have anti-α-glucosidase and anti-inflammatory activities. Subsequent chemical study afforded a new phenylethyl isocoumarin glycoside (1) and eight known compounds (2-9). The structure of 1 was elucidated by comprehensive spectroscopic analysis and chemical transformations. All compounds showed modest α-glucosidase inhibitory activity (IC50 values ranging from 36.8 to 210.7 µM), which was lower than that of the positive control acarbose (IC50=301.9 µM). Those compounds except inactive compounds 3 and 6 showed weak anti-inflammatory activity.[Formula: see text].
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Agrimonia , Inhibidores de Glicósido Hidrolasas/farmacología , Glicósidos , Proyectos Piloto , Extractos Vegetales/farmacología , alfa-GlucosidasasRESUMEN
BACKGROUND: In Traditional Chinese Medicine (TCM), Dahuang Danshen decoction (DD) is used to treat pancreatic fibrosis. Pancreatic fibrosis is a typical manifestation of chronic pancreatitis (CP), which affects the digestive system. The therapeutic mechanisms of DD in pancreatic fibrosis are unclear. AIM: This study aimed to investigate the regulatory mechanisms of DD on oxidative stress and endoplasmic reticulum stress in CP. MATERIALS AND METHODS: Experimental rats were intraperitoneally injected with 500 mg/kg BW of diethyldithiocarbamate (DDC) twice a week for six weeks to induce CP. At the same time, DD was administered orally at daily doses of 1.37 g/kg BW, 2.74 g/kg BW, and 5.48 g/kg BW to evaluate its treatment effects on CP. After all treatments, pancreatic tissues were harvested and subjected to H&E staining. Transmission electron microscopy (TEM) was also performed to show the endoplasmic reticulum structure in the pancreatic tissues. Immunohistochemistry was used to detect the α-SMA expression level in the pancreatic tissues. Metabolomics analysis of the serum and proteomics analysis of the pancreatic tissues were performed to reveal the changes of endogenous metabolites and proteins, respectively. Concentrations of GSH, MDA, SOD, ROS, col-1, and col-3 were determined using corresponding kits. The western blotting method was used to determine the protein levels of Keap-1, HO-1, NQO1, Nrf2, GRP, JNK, and caspase 12. The pancreatic mRNA levels of NQO1, GPX1, HO-1, GST-π, GRP, JNK, and caspase 12 were also determined by quantitative PCR. The interactions between TCM components and Keap-1 were investigated by molecular docking modeling. RESULTS: The pathohistological results demonstrated that DD could ameliorate DDC-induced CP in vivo, indicated by reduction of α-SMA, col-1, col-3, TNF-α, and IL-6. DD increased serum levels of GSH and SOD but reduced pancreatic ROS. DD decreased cytoplasmic Keap-1 and increased Nrf2 nuclear localization. Correspondingly, DD increased the expression levels of Nrf2 downstream antioxidant genes NQO1, GPX1, HO-1, and GST-π. DD also decreased ERS hallmarks caspase 12 cleavage and GRP expression. Eventually, DD inhibited PSC activation by reducing JNK phosphorylation and MMK-3/p38 expression. Molecular docking analysis showed that salvianolic acid B and emodin had a good binding affinity toward Keap-1. CONCLUSIONS: These results demonstrated that DD could ameliorate the oxidative and endoplasmic reticulum stress through releasing Nrf2 from Keap-1 binding and inducing the downstream antioxidant enzymes. As a result, DD could thwart pancreatic fibrosis by inhibiting PSCs activation, which was induced by OS and ERS through JNK and MMK3/p38 pathways.
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Clear cell renal cell carcinoma (ccRCC) is the most common malignant type of kidney cancer. The present study aims to explore the underlying mechanism and potential targets of the traditional Chinese medicine Bu-Shen-Jian-Pi-Fang (BSJPF) in the treatment of ccRCC based on network pharmacology. After obtaining the complete composition information for BSJPF from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform, we analyzed its chemical composition and molecular targets and then established a pharmacological interaction network. Twenty-four significantly differentially expressed genes and nine pathways mainly related to tumor proliferation were identified and screened. Functional enrichment analysis indicated that the potential targets might be significantly involved in glycolysis and the HIF-1 signaling pathway. To further confirm the effect of BSJPF on ccRCC cell proliferation, a BALB/c xenograft mouse model was constructed. Potential targets involved in regulating glycolysis and the tumor immune microenvironment were evaluated using RT-qPCR. VEGF-A expression levels were markedly decreased, and heparin binding-EGF expression was increased in the BSJPF group. BSJPF also inhibited tumor proliferation by enhancing GLUT1- and LDHA-related glycolysis and the expression of the immune checkpoint molecules PD-L1 and CTLA-4, thereby altering the immune-rejection status of the tumor microenvironment. In summary, the present study demonstrated that the mechanism of BSJPF involves multiple targets and signaling pathways related to tumorigenesis and glycolysis metabolism in ccRCC. Our research provides a novel theoretical basis for the treatment of tumors with traditional Chinese medicine and new strategies for immunotherapy in ccRCC patients.
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Antineoplásicos Fitogénicos/farmacología , Carcinoma de Células Renales/tratamiento farmacológico , Proliferación Celular/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Glucólisis/efectos de los fármacos , Neoplasias Renales/tratamiento farmacológico , Farmacología en Red , Escape del Tumor/efectos de los fármacos , Animales , Carcinoma de Células Renales/inmunología , Carcinoma de Células Renales/metabolismo , Carcinoma de Células Renales/patología , Línea Celular Tumoral , Bases de Datos Genéticas , Regulación Neoplásica de la Expresión Génica , Redes Reguladoras de Genes , Humanos , Neoplasias Renales/inmunología , Neoplasias Renales/metabolismo , Neoplasias Renales/patología , Masculino , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Mapas de Interacción de Proteínas , Transducción de Señal , Carga Tumoral/efectos de los fármacos , Microambiente Tumoral/inmunología , Ensayos Antitumor por Modelo de XenoinjertoRESUMEN
Multimodal imaging-guided accurate tumor-targeting and efficient synergistic therapy are of great importance for cancer therapy in vitro and in vivo. In this study, a biocompatible, tumor-targeted, on-demand chemo-/photothermal therapeutic nanoplatform (HIDSiGdNPs@PDA-HA) based on hollow mesoporous organic silica nanoparticles (HMONs) was used for bimodal imaging and multi-factor stepwise response for drug release and treatment. Targeted molecule hyaluronic acid (HA) promoted the endocytosis of HIDSiGdNPs@PDA-HA in HeLa cancer cells. The gatekeeper pH-/light-sensitive PDA coating was stimulated by the endogenous tumor acidic microenvironment and exogenous NIR laser to release doxorubicin (DOX). Thereafter, HMONs containing S-S bonds were reduced and degraded by endogenous glutathione (GSH), and the drug was further released rapidly to kill cancer cells. Importantly, the photothermal reagent indocyanine green (ICG) was always retained in the carrier, improving the effectiveness of photothermal therapy. The loaded Gd-doped silicon nanoparticles (SiGdNPs) combined with DOX and ICG led to multi-color fluorescence imaging in vitro and magnetic resonance imaging in vivo to realize targeted diagnosis and track drug distribution. The treatment results of tumor-bearing mice also proved the excellent synergistic therapy. It is believed that the multifunctional nanomaterials with dual mode imaging capability and targeted and controlled collaborative therapy would provide an alternative for accurate diagnosis and efficient treatment.
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Hipertermia Inducida , Nanocompuestos , Nanopartículas , Animales , Doxorrubicina/farmacología , Liberación de Fármacos , Humanos , Ácido Hialurónico , Ratones , Imagen Multimodal , Fototerapia , Terapia FototérmicaRESUMEN
Three phenylpropanoid glucosides (1: â-â3: ) and one iridoid glucoside (11: ), together with eleven known glucosides, were isolated from the ethanol extract of the whole plant of Hemiphragma heterophyllum. Their structures were elucidated by means of 1D and 2D NMR spectroscopy, HRMS, and chemical methods. All compounds except 11: and 13: â-â15: showed varying degrees of α-glucosidase inhibitory activity. Compounds 5, 9: , and 12: were marginally active in the bioassay, while compounds 1: â-â4: , 6: â-â8: , and 10: exhibited appreciable inhibitory activity with an IC50 value of 33.6 ~ 83.1 µM, which was much lower than that of the positive control acarbose (IC50 = 310.8 µM).
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Glucósidos Iridoides , alfa-Glucosidasas , Glucósidos , Inhibidores de Glicósido Hidrolasas , Iridoides , Estructura Molecular , Extractos VegetalesRESUMEN
Phytochemical study on the 95% ethyl alcohol extract of stems of Chenopodium ambrosioides resulted in the isolation of two new polyol monoterpenes, 4-hydroxy-4(α or ß)-isopropyl-2-methyl-2-cyclohexen-1-one (1) and 1-methyl-4ß- isopropyl-1-cyclohexene-4α,5α,6α-triol (2), together with five known compounds, (1S,2S,3R,4S)-1-methyl-4-(propan-2-yl)cyclohexane-1,2,3,4-tetrol (3), (1R,2S,3S,4S)- 1,2,3,4-tetrahydroxy-p-menthane (4), (1R,2S)-3-p-menthen-1,2-diol (5), (1R,4S)-p- menth-2-en-1-ol (6) and 1,4-dihydroxy-p-menth-2-ene (7). The structures of the new compounds were established on the basis of detailed spectroscopic evidence including extensive 1D and 2D NMR techniques. Compounds 1-7 were evaluated for their anti-inflammatory activity, and compound 1 showed moderate ability to inhibit NO production of LPS-stimulated RAW 264.7 macrophages with an IC50 value of 16.83 µM.
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Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacología , Chenopodium ambrosioides/química , Monoterpenos/aislamiento & purificación , Animales , Antiinflamatorios no Esteroideos/aislamiento & purificación , Línea Celular , Evaluación Preclínica de Medicamentos/métodos , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Espectroscopía de Resonancia Magnética , Ratones , Estructura Molecular , Monoterpenos/química , Monoterpenos/farmacología , Tallos de la Planta/química , Polímeros/químicaRESUMEN
Multimodal imaging has made great contribution for diagnosis and therapy of disease since it can provide more effective and complementary information in comparison to any single imaging modality. The design and fabrication of fluorescent-magnetic nanoparticles for multimodal imaging has rapidly developed over the years. Herein, we demonstrate the facile synthesis of GdS coated CdTe nanoparticles (CdTe@GdS NPs) as multimodal agents for fluorescence (FL) and T1-weighted magnetic resonance (MR) imaging. These nanoparticles obtain both prominent fluorescent and paramagnetic properties by coating the GdS shell on the surface of CdTe core via a simple room-temperature route in aqueous solution directly. It is shown that the as-prepared CdTe@GdS NPs have high quantum yield (QY) value of 12% and outstanding longitudinal relaxation rate (r1) of 11.25 mM s(-1), which allow them to be employed as FL/MR dual-modal imaging contrast agents. They also exhibit small particle size of 5 nm, excellent colloidal stability and low cellular toxicity for concentrations up to 750 µg mL(-1). In addition, with the conjugation of folic acid, the nanoparticles were successfully used for tumor-targeted FL/MR dual-modal imaging in vitro and in vivo.
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Compuestos de Cadmio/síntesis química , Colorantes Fluorescentes/síntesis química , Nanopartículas de Magnetita/química , Neoplasias/diagnóstico , Sulfuros/síntesis química , Animales , Compuestos de Cadmio/administración & dosificación , Supervivencia Celular/efectos de los fármacos , Colorantes Fluorescentes/administración & dosificación , Gadolinio/administración & dosificación , Humanos , Células KB , Nanopartículas de Magnetita/administración & dosificación , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Microscopía Electrónica de Transmisión/métodos , Microscopía Fluorescente/métodos , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Sulfuros/administración & dosificación , Telurio/administración & dosificaciónRESUMEN
Objective To retrospectively analyze the effect of abdominal acupuncture for the casino workers with sleep disorder in chronic fatigue syndrome and analyze the correlation between them.Method 65 patients were all from the Acupuncture Department of Health Center of the Black Sand, Macao Health Bureau, 2011 October to 2013 January, who were diagnosed with sleep disorder in chronic fatigue syndrome and in accordance with the inclusion criteria. They were received abdominal acupuncture treatment for 4 weeks. Pittsburgh sleep quality index(PSQI) and Fatigue Assessment Instrument(FAI)were adopted to evaluate the effect before treatment 、after treatment and one month follow-up. Multiple regression analysis model was used to analyze the correlation of each factor of FAI and PSQI. Results Compared with before treatment (13.78± 3.23), the total score of PSQI after treatment(8.66 ± 4.26)and follow-up(8.26 ± 4.66) were significant decreased(P<0.05);the score of 6 dimensions(sleep quality, Time to fall asleep, sleep time, sleep efficiency, sleep disorders daytime function) after treatment and follow-up were significant decreased(P<0.05),compared with those before treatment;the FAI score after treatment (92.60±14.64) and follow-up(90.75±14.75) were significant lower(P<0.05)than those before treatment (147.55±7.03) .Multiple regression analysis showed that 4 dimensions of PSQI (sleep quality, sleep time, sleep disorders, daytime function)had close relationship with FAI score(r=0.373~0.702, P<0.05). Conclusion Abdominal acupuncture can improve the casino workers' sleep disorder in chronic fatigue syndrome and is worth of further study.
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<p><b>OBJECTIVE</b>To observe the clinical efficacy on sleep disorder in the intervention of flying needling therapy and compare the efficacy difference among flying needling therapy, estazolam and non-acupoint acupuncture.</p><p><b>METHODS</b>Three hundred and fifteen cases of sleep disorder were randomized into a flying needling group (110 cases), an estazolam group (107 cases) and a non-acupoint acupuncture group (98 cases). In the flying needling group, the flying needling therapy was applied to Sanyinjiao (SP 6), Anmian (EX HN22), Shenmen (HT 7) and so on. Additionally, vitamin B1 was prescribed for oral administration and the intradermal needle method was given at the Back-shu points. In the estazolam group, estazolam was prescribed for oral administration. Also the non-acupoint acupuncture and the acupoint sticking therapy on the Back-shu points were given additionally. In the non-acupoint acupuncture group, the non-acupoint acupuncture, oral administration of vitamin B1 and the acupoint sticking therapy on the Back-shu points were applied. The treatment of 2 weeks were required in all the groups. The efficacy and the score of PSQI (Pittsburgh sleep quality index) were observed in the 2-week follow-up visit.</p><p><b>RESULTS</b>The total effective rate in the flying needling group was 84.1% (90/107), which was superior to 59.7% (62/104) in the estazolam group and 25.0% (24/96) in the non-acupoint acupuncture group (both P < 0.05). In the follow-up observation, the score of each item and the total score of PSQI were lower apparently than those before treatment in each group (all P < 0.05), and those in the flying needling group were lower apparently than those in the other two groups (all P < 0.05).</p><p><b>CONCLUSION</b>The flying needling therapy as the chief therapeutic method effectively improves the sleep quality for the patients with sleep disorder, which is apparently superior to estazolam and non-acupoint acupuncture.</p>
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Adolescente , Adulto , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Adulto Joven , Puntos de Acupuntura , Terapia por Acupuntura , Sueño , Trastornos del Sueño-Vigilia , Terapéutica , Resultado del TratamientoRESUMEN
This article describes the experiences of professor CHEN Quan-xin, an old famous TCM doctor, in the treatment of insomnia. He believes that insomnia stems from incoordination between nutrient qi and defensive qi and deficient cultivation of cardiac spirit, and treatment of insomnia need to regulate spirit and quiet heart coherently. Painless acupuncture method of Chen's flying needling is adopted including to select Shenmen (HT 7), Sanyinjiao (SP 6) and Anmian (Extra) as the main points and take special needling technique and grading reinforcing and reducing manipulations. During treatment, he pays attention to understanding patients' psychological and mental status through "watching one's expressions and weighing his words carefully".
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Humanos , Terapia por Acupuntura , Corazón , Sueño , Trastornos del Inicio y del Mantenimiento del Sueño , Psicología , Terapéutica , EspiritualidadRESUMEN
OBJECTIVE: To observe the effects of puerarin (Pue) on the neurocyte apoptosis and the p-Akt (Ser473) expression in the ischemic penumbra of rats with cerebral ischemia/reperfusion (I/R). METHODS: The 48 Sprague-Dawley rats were randomly divided into four groups, i.e., the sham-operation group, the I/R group, the Pue treatment group, and the Pue + LY294002 treatment group (Pue + LY), 12 in each group. The cerebral I/R rat model was established by Longa's suture method. Pue and Pue + specific P13K kinase inhibitor, i.e., LY294002 were administered. The score of the neurological deficit was estimated 1 h followed by 24 h reperfusion. The infarct volume was measured using TTC staining. The number of apoptotic neurons were detected using Tunel method. The expressions of p-Akt (Ser473) was detected using immunohistochemical assay, and the images were analyzed. RESULTS: The score of the neurological deficit decreased more obviously, the number of apoptosis decreased more significantly, the expressions of p-Akt (Ser473) increased more significantly in the Pue group than in the I/R group (all P < 0.05). The score of the neurological deficit increased more obviously, the number of apoptosis increased more significantly, the expression of p-Akt (Ser473) decreased more significantly in the Pue + LY group than in the Pue group (all P < 0.05). CONCLUSION: Pue reduced the apoptosis of neurocytes and had protective effects against cerebral I/R injury possibly through activating the PI3K/Akt signaling pathway.
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Isquemia Encefálica/metabolismo , Isoflavonas/farmacología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Daño por Reperfusión/metabolismo , Animales , Apoptosis/efectos de los fármacos , Isquemia Encefálica/patología , Corteza Cerebral/efectos de los fármacos , Corteza Cerebral/metabolismo , Cromonas/farmacología , Masculino , Morfolinas/farmacología , Ratas , Ratas Sprague-Dawley , Daño por Reperfusión/patologíaRESUMEN
Highly emissive ultraviolet ZnSeS nanocrystals (NCs), with a core-shell-like structure, were designed and synthesized via a one-step noninjection approach in 1-octadecene (ODE). These ultraviolet ZnSeS NCs exhibit bright bandgap emission with high color purity and little trap emission. With full width at half-maximum (fwhm) of â¼21 nm only, photoluminescent (PL) quantum yield (QY) of â¼60% was estimated for one ensemble dispersed in toluene exhibiting bandgap absorption peaking at â¼380 nm and bandgap emission at â¼389 nm. These alloyed ZnSeS NCs present a cubic crystal structure consisting of a Se-rich core and a S-rich shell. Such a gradiently alloyed structure was suggested by our investigation on the temporal evolution of optical properties of the growing ZnSeS NCs monitored from 80 to 300 °C, together with structural and compositional characterization performed with XRD, XPS, EDX, and TEM. This newly developed one-step noninjection approach was achieved with zinc oleate (Zn(OA)(2)), diphenylphosphine selenide (SeDPP), and diphenylphosphine sulfide (SDPP) as Zn, Se, and S precursors, respectively. ZnSe monomers mainly participated in nucleation at â¼120 °C, while both ZnSe and ZnS monomers contributed to NC formation in later growth stages (â¼160 °C and higher). (31)P NMR study demonstrates that SeDPP is more reactive than SDPP toward Zn(OA)(2), and also supports such a model proposed on the combination of ZnSe and ZnS monomers leading to nucleation/growth of ZnSeS alloyed NCs. The present study offers conceptual methodology to various highly photoluminescent alloyed NCs with high quality, high particle yield, and high synthetic reproducibility.
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Nanotecnología/métodos , Puntos Cuánticos , Compuestos de Selenio/química , Selenio/química , Compuestos de Zinc/química , Zinc/química , Aleaciones , Luminiscencia , Espectroscopía de Resonancia Magnética/métodos , Nanopartículas del Metal/química , Modelos Químicos , Nanopartículas , Fotoquímica/métodos , Polvos , Reproducibilidad de los Resultados , Espectrofotometría/métodos , Factores de Tiempo , Difracción de Rayos XRESUMEN
The metabolisms of five xanthones isolated from a Tibetan medicinal herb Halenia elliptica D. Don, including 1-hydroxy-2,3,5-trimethoxy-xanthone (HM-1), 1-hydroxy-2,3,4,7-tetramethoxy-xanthone (HM-2), 1-hydroxy-2,3,4,5-tetramethoxy-xanthone (HM-3), 1,7-dihydroxy-2,3,4,5-tetramethoxy-xanthone (HM-4) and 1,5-dihydroxy-2,3-dimethoxy-xanthone (HM-5), were studied in rat liver microsomes in vitro. High performance liquid chromatography coupled to ion trap time-of-flight mass spectrometry (LC-ESI-IT-TOF) was applied for identification of metabolites of five xanthones mentioned above and (1)H NMR was used to elucidate the major metabolites. The structures of thirteen metabolites were identified and seven of them had not been reported before. Moreover, xanthone isomers herein could be distinguished by difference of fragmentation behaviors with increase of stages or relative abundances. The results indicated that in vitro metabolic transformation of HM-1, HM-2, HM-3, HM-4 and HM-5 occurred mainly at 2-, 4-, 5-, 7-carbonic positions on their structures of parent drugs. The metabolites could be new vasoactive substances. This work will provide a basis for study on the structure-activity relationships of these xanthones and their derivatives from Tibetan herbal in the next work.
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Cromatografía Líquida de Alta Presión/métodos , Gentianaceae/química , Xantonas/metabolismo , Animales , Técnicas In Vitro , Masculino , Ratas , Ratas Sprague-Dawley , Espectrometría de Masa por Ionización de Electrospray , Xantonas/aislamiento & purificaciónRESUMEN
Objective To investigate the iodine nutritional status of children aged 8 to 10 in both costal and non-costal areas of Rizhao city Shandong province,and provide a basis for scientific supplementation of iodine.Methods In 2009 and 2010,townships of Lanshan and Donggang were chosen as survey points which situated close to the coast,the counties of Wulian and Juxian that were more than 50 kilometers away from the coast were selected as controls.The iodine concentration of drinking water in every village and water supply point was determined.At the county level,5 to 9 towns were selected according to their sub-area positions of east,west,south,north and center,4 villages were selected in each chosen township,8 - 15 households were selected in each chosen village,edible salt from the households was collected; 5 primary schools were selected in each chosen township,60 students aged 8 - 10 were selected to take thyroid examination in each chosen school.Twenty copies of urine samples were collected from the 60 students to detect the iodine concentration.Iodine in drinking water was tested by cerous sulfate catalytic spectrophotometry,in iodized salt by direct titration,in urine by arsenic-cerium contact method,and thyroids were examined by palpation.Results Totally 3483 copies of drinking water samples,1164 copies of edible salt samples,and 476 copies of urine samples were tested,and a total of 1200 children aged 8 to 10 were investigated; and the ratio of water iodine frequency distribution ≤ 10 μg/L (in costal and non-costal area) accounted for 90.03% ( 1011/1123 ) and 91.10% (2150/2360),respectively,the medians of water iodine were 5.6 and 4.2 μg/L,respectively; the iodine medians of edible salt were 29.03 and 29.99 mg/kg,respectively; the consumption rates of qualified iodized salt were 96.77% (569/588) and 97.05% (559/576),respectively; total goiter rates were 1.17%(7/600) and 1.33%(8/600),respectively; the medians of urinary iodine were 144.05 and 159.15 μg/L,respectively; the percentages of urinary iodine that bellow 100 μg/L were 26.58% (63/237) and 22.59% (54/239),respectively; between 100 - 300 μg/L were 66.75% (158/237) and 64.02% (153/239),respectively;above 300μg/L were 6.75% (16/237)and13.39% (32/239),respectively.ConclusionsThe costal of Rizhao is an iodine deficient area.The current popularity of household's consumption of qualified iodized salt is suitable.The levels of iodine nutrition of children aged 8 to 10 is appropriate,which met the national standard of elimination of iodine deficiency disorders (IDD).There is no iodine excess.There are no significant differences in levels of iodine nutrition between costal and non-costal areas on the premise that the same iodized salt is supplied in both the areas,and there is no need to make differentiated supply of iodized salt.
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Rare earth elements are important nutritional elements for human health, and today more and more attention has been paid to the effective components in Chinese traditional medicine, especially to rare earth elements. Fifteen rare earth elements in wild hypericum japonicum Thunb were analyzed by the methods of ICP-MS. The results showed that the concentrations of La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Yb, Tm, Lu and Y ranged from 6 ng x g(-1) x DW to 14 522 ng x g(-1) x DW, and among them the concentrations of La, Ce and Nd were higher than 2 000 ng x g(-1) x DW. Compared with the concentration of rare earth elements in rice, corn, wheat and barley, the total concentration of rare earth elements in hypericum japonicum Thunb was much higher, which could be the mechanism of curative effect of hypericum japonicum Thunb on liverish diseases. The character of elements and the content of rare earth elements in soil should be responsible for the difference, but the distributive mechanism of rare earth elements in hypericum japonicum Thunb should be further studied.
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Hypericum/química , Metales de Tierras Raras/análisis , Espectrometría de MasasRESUMEN
Deficiency of micronutrients, especially iron and zinc, has been a serious malnutrition problem worldwide in human health. Increasing Fe and Zn concentrations in grains by means of plant breeding is a sustainable, effective and important way to improve human mineral nutrition and health. However, little information on grain Fe and Zn concentrations in Chinese wheat genotypes is available. Therefore, to determine the nutrients status especially these of micronutrients in wheat grain is necessary and very useful. Two hundred sixty two genotypes were selected from the wheat mini-core collections, which contained 23090 wheat genotypes in China and represented 72.2% of total genetic variation. All 262 genotypes were grown in soils of similar geographical and climate location in order to minimize the environmental effect. After harvesting, the grains were washed with deionized water and dried (around 70 degrees C), then digested in HNO3 solution using a microwave accelerating reaction system (MARS). Nutrient concentrations in stock solution were analyzed by inductively coupled plasma atomic emission spectrometry (ICP-AES). Remarkable genetic variations among grain nutrient concentrations (Fe, Mn, Cu, Zn, Mg, Ca, K and P ) in the tested genotypes were detected. The concentrations of Fe, Zn, Mn, Cu, Ca, Mg, K and P in wheat grain were in the ranges of 34.2-61.2, 26.3-76.0, 20.9-56.7, 3.4-9.8, 290-976, 1129-2210 mg x kg(-1); 0.34%-0.85% and 0.296%-0.580%, respectively. The corresponding average values were 45.1, 50.2, 37.9, 6.5, 515, 1772 mg x kg(-1), 0.55% and 0.451%, respectively. Significant positive correlations between micronutrients (Fe, Mn, Zn, and Cu) in wheat grains were detected, and the correlation coefficients were 0.395** (Fe and Mn), 0.424** (Fe and Zn), 0.574** (Fe and Cu), and 0.474** (Mn and Cu), respectively. However, no significant difference was found in grain nutrient concentrations between spring-wheat and winter-wheat genotypes. This study provides valuable and important information for breeding wheat genotypes which are enriched with minerals in grains, especially Fe and Zn
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Extractos Vegetales/análisis , Espectrofotometría Atómica/métodos , Oligoelementos/análisis , Triticum/química , China , Valor NutritivoRESUMEN
The aim of the present paper was to investigate the synergistic effect and mechanism of anticancer activity of Zuojinwan ( ZJW) comprising Coptis chinensis Franch ( HL) and Evodia rutaecarpa (Juss.) Benth ( WZY) at a ratio of 6 : 1 (w/w). In vivo anticancer activity testing was carried out by inhibiting the growth of S180 tumor. Tumor growth inhibition, spleen index, lymphocyte proliferation, apoptosis, tumor necrosis factor-alpha (TNF-alpha) level, activities of serum tumor markers (TMs), increase in life span (ILS), histopathology and gene expression were tested. The results indicated that ZJW could significantly induce apoptosis of cancer cells. The inhibition ratio, ILS and TNF-alpha levels of mice treated with ZJW were 50.54 %, 64.91 % and 1.04 ng/mL, respectively, much higher than HL and WZY when singly used. Furthermore, the activities of acid phosphatase and alkaline phosphatase were significantly increased and the activities of creatine kinase, aldolase and lactate dehydrogenase were reduced in serum, and the expressions of Bax and wild-type p53 proteins were much higher for the mice treated by ZJW compared with HL and WZY single-treatment groups. A clear synergistic effect on the anticancer activity was observed with ZJW, and the mechanism of antitumor growth may be due to an effect on gene expression and activities of tumor markers in serum.