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1.
Sensors (Basel) ; 24(14)2024 Jul 13.
Artículo en Inglés | MEDLINE | ID: mdl-39065928

RESUMEN

With the advancement of technology, signal modulation types are becoming increasingly diverse and complex. The phenomenon of signal time-frequency overlap during transmission poses significant challenges for the classification and recognition of mixed signals, including poor recognition capabilities and low generality. This paper presents a recognition model for the fine-grained analysis of mixed signal characteristics, proposing a Geometry Coordinate Attention mechanism and introducing a low-rank bilinear pooling module to more effectively extract signal features for classification. The model employs a residual neural network as its backbone architecture and utilizes the Geometry Coordinate Attention mechanism for time-frequency weighted analysis based on information geometry theory. This analysis targets multiple-scale features within the architecture, producing time-frequency weighted features of the signal. These weighted features are further analyzed through a low-rank bilinear pooling module, combined with the backbone features, to achieve fine-grained feature fusion. This results in a fused feature vector for mixed signal classification. Experiments were conducted on a simulated dataset comprising 39,600 mixed-signal time-frequency plots. The model was benchmarked against a baseline using a residual neural network. The experimental outcomes demonstrated an improvement of 9% in the exact match ratio and 5% in the Hamming score. These results indicate that the proposed model significantly enhances the recognition capability and generalizability of mixed signal classification.

2.
Biol Pharm Bull ; 45(7): 863-871, 2022 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-35491088

RESUMEN

Saikosaponin A (SSA)-a natural compound extracted from Radix bupleuri-possesses antitumor properties in several types of carcinomas. However, the role of SSA on bladder cancer and the mechanisms remain unclear. In this study, we have described the effect of SSA on human bladder cancer cell lines T24 and 5637 in the context of the regulation of mitochondrial pathways of apoptosis. In vitro, the Cell Counting Kit-8 (CCK-8) assay and cell wound healing assays were used to determine the proliferative effect of SSA treatment. Flow cytometry and Western blotting were performed to evaluate the apoptosis and related mechanisms. To further confirm that apoptosis is mediated through Caspase activation, Hoechst 33258 fluorescence staining assay was done after cells were treated with SSA and caspase inhibitor-Z-VAD-FMK. In vivo, an orthotopic xenograft mice model was adopted to evaluate the effect of SSA. The tumors were analyzed by hematoxylin-eosin (H&E) staining, immunohistochemical analysis, and Western blotting. In vitro, the results with CCK-8 assay showed obvious SSA-induced suppression in cell growth in a dose- and time-dependent manner. Flow cytometry analysis, Hoechst 33258 fluorescence staining assay and the assessment of the changes in the B-cell lymphoma 2 (Bcl-2) family protein expression level revealed that SSA could significantly induce cell apoptosis, which was associated with apoptosis via the mitochondrial pathways. In vivo, the results revealed a reduction in cell proliferation. In conclusion, our data suggest that SSA inhibits the growth of bladder cancer cells by activating the mitochondrial apoptosis pathway and inducing cell apoptosis.


Asunto(s)
Carcinoma , Neoplasias de la Vejiga Urinaria , Animales , Apoptosis , Bisbenzimidazol/farmacología , Caspasas , Línea Celular Tumoral , Proliferación Celular , Humanos , Ratones , Ácido Oleanólico/análogos & derivados , Saponinas , Vejiga Urinaria , Neoplasias de la Vejiga Urinaria/tratamiento farmacológico
3.
Angew Chem Int Ed Engl ; 61(30): e202203398, 2022 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-35594364

RESUMEN

A novel distal radical rearrangement of alkoxyphosphine is developed for the first time and applied to the regioselective radical fluoroalkylphosphorylation of unactivated olefins. By employing a one-pot two-step reaction of (bis)homoallylic alcohols, organophosphine chlorides, and fluoroalkyl iodides under CFL (compact fluorescence light) irradiation, a series of fluoroalkylphosphorylated alkyl iodides and alcohols are easily synthesized by regiospecific installing a phosphonyl onto the inner carbon of terminal olefins and further iodination/hydroxylation. Mechanism studies reveal that the migration undergoes a distinctive radical cyclization/ß-scission on the lone electron pair of phosphorus, resulting in C-P bond formation and C-O bond cleavage.

4.
Pak J Pharm Sci ; 35(2): 571-578, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35642414

RESUMEN

Scutellaria barbata (S. barbata), a traditional herbal medicine used in southern China, possesses anti-inflammatory, antitumor, spasmolytic and expectorant effects. However, there are not many recent studies on its gastrointestinal effects. This study aimed to evaluate the antidiarrheal effect of the ethanol extract of S. barbata (SBE) and its effect on the isolated jejunum smooth muscle. METHODS: The antidiarrheal effect of SBE (doses: 125, 250 and 500 mg/kg) on castor oil-induced diarrhea was investigated in vivo. The effect of SBE (0.01-10 mg/mL) on spontaneous or acetylcholine chloride (ACh, 10µM)/KCl (60mM)-induced contraction of isolated rabbit jejunum smooth muscle was examined in vitro. The possible spasmolytic mechanism of SBE (1 and 3mg/mL) was analyzed by accumulating CaCl2 in a Ca2+-free high-K+ (60mM) solution. RESULTS: SBE (125, 250 and 500mg/kg) could delay the initial semi-solid onset time of mice and also reduce the diarrhea index in vivo. Furthermore, SBE (0.01-10mg/mL) could alleviate the spontaneous or ACh/KCl-induced contraction in vitro. SBE (1 and 3mg/mL) also inhibited the contraction induced by CaCl2, and the concentration-response curves of CaCl2 moved downward and to the right, similar to those of verapamil (0.01 and 0.1µM). CONCLUSIONS: SBE exerts antidiarrheal and spasmolytic effects, which provides a pharmacological basis for its use in functional gastrointestinal disorders.


Asunto(s)
Antineoplásicos , Scutellaria , Animales , Antidiarreicos/uso terapéutico , Antineoplásicos/farmacología , Cloruro de Calcio/efectos adversos , Diarrea/inducido químicamente , Diarrea/tratamiento farmacológico , Etanol/farmacología , Yeyuno , Músculo Liso , Parasimpatolíticos/farmacología , Extractos Vegetales/uso terapéutico , Conejos
5.
Pak J Pharm Sci ; 35(2): 587-594, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35642416

RESUMEN

Lophatheri Herba is a traditional Chinese medicine, which is commonly used in the treatment of fever, stomatitis, urodynia. The aim of the study is to evaluate the antidiarrheal activity of the ethanol extract of Lophatheri Herba (Gramineae, ELH) and observe its effect on isolated jejunum smooth muscle in rabbits, so that we can provide a possible pharmacological basis for its clinical use. Methods: In vivo, the antidiarrheal activity of ELH (250, 500 and 1000 mg/kg; orally) in castor oil-induced Kun Ming mice was evaluated. In vitro, the effect of ELH (0.01-10 mg/mL) on the spontaneous and ACh (10µM)/K+ (60mM)-induced contraction of isolated rabbit jejunum smooth muscle was studied. The possible mechanism of spasmolytic effect of ELH (1, 3mg/mL) was explored by pretreatment of intestinal tract with CaCl2. Results: ELH (500 and 1000mg/kg) exhibited antidiarrheal effect and it (0.01-10 mg/mL) inhibited the spontaneous and ACh/K+-induced contraction with an EC50 value of 1.27 (0.89-1.34), 0.76 (0.54-1.02) and 0.34 (0.27-0.53), it also shifted the concentration-response curves of CaCl2 to right with decreased in max, similar to verapamil. ELH has significant antidiarrheal and spasmolytic effect, this provides the pharmacological basis for use in gastrointestinal disorders.


Asunto(s)
Antidiarreicos , Parasimpatolíticos , Animales , Antidiarreicos/farmacología , Cloruro de Calcio/farmacología , Etanol/farmacología , Yeyuno , Ratones , Músculo Liso , Parasimpatolíticos/farmacología , Extractos Vegetales/farmacología , Conejos
6.
Angew Chem Int Ed Engl ; 60(50): 26308-26313, 2021 12 06.
Artículo en Inglés | MEDLINE | ID: mdl-34437754

RESUMEN

A novel radical 1,4/5-amino shift from the oxygen center of alkene-tethered diphenyl ketoxime ethers to the carbon center to achieve high value-added fluoroalkyl-containing primary ß(γ)-amino-ketones is reported. Mechanism studies reveal that the migration is triggered by the alkene addition of fluoroalkyl radical derived from the electron donor-acceptor (EDA) complex of Togni's reagent II or fluoroalkyl iodides and quinuclidine, and involves a unique 5(6)-exo-trig cyclization of the carbon-centered radical onto the N-atom of ketoxime ethers followed by a cascade sequence of N-O bond cleavage and dehydrogenation. Notably, besides Togni's reagent II and fluoroalkyl iodides, this protocol is also compatible with other radical precursors to provide various functionalized primary aminoketones.

7.
Biosci Biotechnol Biochem ; 84(12): 2533-2544, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32892714

RESUMEN

The objective of present investigation was to appraise the effects of piperine on STZ-induced diabetic cardiomyopathy in rats. Diabetes was induced in Sprague-Dawley rats with intraperitoneal STZ injection, and the rats were assigned to seven groups. Electrocardiograph, hemodynamic, various biochemical, molecular, and histological parameters were examined. Treatment with piperine significantly (p < 0.05) restored altered myocardial functions, inhibited cardiac marker, and restored electrocardiogram and hemodynamic alterations. The elevated level of cardiac oxido-nitrosative stress and decreased cardiac Na-K-ATPase concentration, after STZ administration, were significantly (p < 0.05) attenuated by piperine treatment. Piperine also considerably (p < 0.05) increased myocardial mitochondrial enzyme activity. STZ-induced alteration in heart ANP, BNP, cTn-I, Bcl2, Bax/Bcl2, and caspase3 mRNA expression was significantly (p < 0.05) restored by piperine treatment. Piperine administration reduced histopathological aberrations induced by STZ. In conclusion, the present investigation suggests that piperine ameliorates STZ-induced diabetic cardiomyopathy via modulation of caspase-3, Bcl2, Bax/Bcl2 pathways. Abbreviations: ACE: Angiotensin-Converting Enzyme; ANOVA: Analysis of Variance; ANP: Atrial Natriuretic Peptide; APAF: Apoptotic Protease-Activating Factor; ARB: Angiotensin Receptor Blockers; ATP: Adenosine Triphosphate; Bax: Bcl-2-associated X protein; Bcl2: B-cell lymphoma 2; BPM: Beats Per Minute; BNP: brain natriuretic peptide; CAD: Caspase-3-Activated DNase; cDNA: Complementary DNA; CK-MB: Creatine Kinase-MB; CPCSEA: Committee for the Purpose of Control And Supervision of Experiments on Animals; cTn-I: cardiac troponin I; DBP: Diastolic Blood Pressure; DCM: Diabetic Cardiomyopathy; DNA: Deoxyribonucleic Acid; DPX: DisterenePhthalate Xylene; ECG: Electrocardiogram; ETC: Electron Transport Chain; GOD-POD: Glucose Oxidase Peroxidase; GSH: Glutathione; IAEC: Institutional Animal Ethics Committee; IL-6: Interleukin-6; IL-1b: Interleukin-1b; LDH: Lactate Dehydrogenase; LV: Left Ventricle; LVEDP: left ventricular end-diastolic Pressure; MABP: Mean Arterial Blood Pressure; MDA: Malondialdehyde; mRNA: Messenger Ribonucleic Acid; MTT: 3- (4,5-Dimethylthiazol-2-yl)-2,5-DiphenyltetrazoliumBromide; NADH: Nicotinamide Adenine Dinucleotide Phosphate; NADPH: Nicotinamide Adenine Dinucleotide Phosphate Hydrogen; NO: nitric oxide; NP: Natriuretic Peptides; OXPHOS: Oxidative Phosphorylation; p.o.: per os; PCR: Polymerase Chain Reaction; RT-PCR: Reverse Transcriptionpolymerase Chain Reaction; PPAR: Peroxisome Proliferator-Activated Receptor Gamma; RAS: Renin-Angiotensin System; RNA: Ribonucleic Acid; ROS: Reactive Oxygen Species; SBP: Systolic Blood Pressure; SDH: Succinate Dehydrogenase; SEM: Standard Error Means; SOD: superoxide dismutase: STZ: Streptozotocin; TNF: Tumor Necrosis Factor Alpha; TnI: Troponin I.


Asunto(s)
Alcaloides/farmacología , Benzodioxoles/farmacología , Cardiomiopatías Diabéticas/tratamiento farmacológico , Cardiomiopatías Diabéticas/metabolismo , Piperidinas/farmacología , Alcamidas Poliinsaturadas/farmacología , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Estreptozocina/efectos adversos , Proteína X Asociada a bcl-2/metabolismo , Alcaloides/uso terapéutico , Animales , Apoptosis/efectos de los fármacos , Benzodioxoles/uso terapéutico , Cardiomiopatías Diabéticas/patología , Cardiomiopatías Diabéticas/fisiopatología , Ingestión de Líquidos/efectos de los fármacos , Ingestión de Alimentos/efectos de los fármacos , Glutatión/metabolismo , Corazón/efectos de los fármacos , Corazón/fisiopatología , Hemodinámica/efectos de los fármacos , Masculino , Malondialdehído/metabolismo , Miocardio/patología , Óxido Nítrico/metabolismo , Tamaño de los Órganos/efectos de los fármacos , Piperidinas/uso terapéutico , Alcamidas Poliinsaturadas/uso terapéutico , ARN Mensajero/genética , Ratas , Ratas Sprague-Dawley , Superóxido Dismutasa/metabolismo , Orina/química
8.
Angew Chem Int Ed Engl ; 59(10): 3900-3904, 2020 03 02.
Artículo en Inglés | MEDLINE | ID: mdl-31869508

RESUMEN

A deconstructive oxygenation of unstrained primary cycloalkanamines has been developed for the first time using an auto-oxidative aromatization promoted C(sp3 )-C(sp3 ) bond cleavage strategy. This metal-free method involves the substitution reaction of cycloalkanamines with hydrazonyl chlorides and subsequent auto-oxidative annulation to in situ generate pre-aromatics, followed by N-radical-promoted ring-opening and further oxygenation by 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) and m-cholorperoxybenzoic acid (mCPBA). Consequently, a series of 1,2,4-triazole-containing acyclic carbonyl compounds were efficiently produced. This protocol features a one-pot operation, mild reaction conditions, high regioselectivity and ring-opening efficiency, broad substrate scope, and is compatible with alkaloids, osamines, and peptides, as well as steroids.

9.
Sleep Breath ; 23(1): 349-354, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29961182

RESUMEN

PURPOSE: Diabetes and sleep disorders are public health threats worldwide, but the potential association between them is still unclear. METHODS: We conducted a community-based cross-sectional study including 5078 participants (2665, 52.5% male) to determine the association between insomnia and diabetes mellitus prevalence. RESULTS: In patients with type 2 diabetes mellitus (T2DM) and nondiabetic controls, the prevalence of insomnia was 20.2% (68/377) and 12.2% (578/4741), respectively. The results showed that insomnia was associated with T2DM after adjusting for age, sex, BMI, smoking, alcohol consumption, presence of disease history (hypertension, dyslipidemia, stroke, cardiovascular diseases, cancers), and depression (odds ratio [OR] = 1.31, 95% confidence interval [CI] 1.03-1.66). After stratifying by age and sex, insomnia was significantly associated with diabetes mellitus only in the subgroup of middle-aged participants (40-59 years) (OR = 1.61, 95% CI 1.16-2.23) and males (OR = 1.48, 95% CI 1.08-2.03) after controlling for the above covariates. CONCLUSIONS: This study suggests that insomnia is independently and significantly associated with diabetes mellitus in the northern Chinese population, especially in the 40-59-year-old age group and in males.


Asunto(s)
Diabetes Mellitus Tipo 2/epidemiología , Trastornos del Inicio y del Mantenimiento del Sueño/epidemiología , Adulto , Factores de Edad , China , Correlación de Datos , Estudios Transversales , Femenino , Humanos , Masculino , Persona de Mediana Edad , Factores de Riesgo , Factores Sexuales
10.
Pharm Biol ; 57(1): 477-484, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31438784

RESUMEN

Context: In China, the herb Sophora tonkinensis Gagnep. (Fabaceae, ST) (Committee of National Pharmacopeia. 2015) exhibits anti-inflammatory, antitumor, and antiviral effects. However, to date, there have been few studies on its gastrointestinal effect. Objective: The gastrointestinal effect of the methanol extract of ST rhizome (STR) was evaluated. Materials and methods: Study was conducted from February to December 2018. In vivo, antidiarrheal activity of STR (125, 250 and 500 mg/kg; orally) in castor oil-induced diarrheal mice was studied. In vitro, the effects of STR (0.01-10 mg/mL) on the isolated tissue preparations of rabbit jejunum were also investigated, the rabbit jejunum stripes were pre-contracted with Ach (10-5 M), K+ (60 mM) and tested in the presence of STR, the possible spasmolytic effect was analyzed in the pretreatment of the jejunum preparations with STR or verapamil in Ca2+-free high-K+ (60 mM) solution containing EDTA. Results: STR (125, 250 and 500 mg/kg) exhibited antidiarrheal activity. STR (0.01-10 mg/mL) completely relaxed spontaneously contracting, Ach (10-5 M) and high K+ (60 mM) induced contracted jejunum with an EC50 value of 0.66 (0.49-0.96), 0.39 (0.28-0.44) and 0.17 (0.10-0.21), similar to verapamil. Concentration-response curves of CaCl2 could be significantly moved to the right and down in the presence of STR (0.3, 1 mg/mL). Discussion and conclusions: Results suggest the presence of antidiarrheal activity and spasmolytic effects of STR, possibly mediated through Ca2+ channel blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal disorders.


Asunto(s)
Antidiarreicos/uso terapéutico , Asteraceae/química , Diarrea/tratamiento farmacológico , Yeyuno/efectos de los fármacos , Contracción Muscular/efectos de los fármacos , Parasimpatolíticos/farmacología , Extractos Vegetales/uso terapéutico , Animales , Antidiarreicos/aislamiento & purificación , Antidiarreicos/toxicidad , Aceite de Ricino , Relación Dosis-Respuesta a Droga , Motilidad Gastrointestinal/efectos de los fármacos , Técnicas In Vitro , Dosificación Letal Mediana , Masculino , Metanol , Ratones , Músculo Liso/efectos de los fármacos , Parasimpatolíticos/aislamiento & purificación , Parasimpatolíticos/toxicidad , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Conejos
11.
Int J Mol Sci ; 19(7)2018 07 06.
Artículo en Inglés | MEDLINE | ID: mdl-29986466

RESUMEN

Resistance to trastuzumab, which specifically target HER2-positive breast and gastric cancer, can develop ultimately in cancer patients. However, the underlying mechanisms of resistance in gastric cancer have not been fully elucidated. Here, we established trastuzumab-resistant MKN45 and NCI N87 gastric cancer sublines from their parental cells. The resistant cells exhibited characteristics of epithelial-mesenchymal transition (EMT) and acquired higher migratory and invasive capacities. To exploit the activated pathways and develop new strategies to overcome trastuzumab resistance, we investigated MKN45 and MKN45/R cells via label-free quantitative proteomics, and found pathways that were altered significantly in MKN45/R cells, with the Wnt/ß-catenin pathway being the most significant. We further confirmed the activation of this pathway by detecting its key molecules in MKN45/R and NCI N87/R cells via Western blot, in which Wnt3A, FZD6, and CTNNB1 increased, whereas GSK-3ß decreased, manifesting the activation of the Wnt/&-catenin pathway. Correspondingly, inhibition of Wnt/ß-catenin pathway by ICG-001, a specific Wnt/&-catenin inhibitor, preferentially reduced proliferation and invasion of trastuzumab-resistant cells and reversed EMT. Concurringly, CTNNB1 knockdown in stable cell lines potently sensitized cells to trastuzumab and induced more apoptosis. Taken together, our study demonstrates that the Wnt/ß-catenin pathway mediates trastuzumab resistance, and the combination of Wnt/ß-catenin inhibitors with trastuzumab may be an effective treatment option.


Asunto(s)
Antineoplásicos Inmunológicos/farmacología , Resistencia a Antineoplásicos , Proteómica , Neoplasias Gástricas/tratamiento farmacológico , Trastuzumab/farmacología , Vía de Señalización Wnt/efectos de los fármacos , Antineoplásicos Inmunológicos/uso terapéutico , Apoptosis/efectos de los fármacos , Compuestos Bicíclicos Heterocíclicos con Puentes/farmacología , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Transición Epitelial-Mesenquimal/efectos de los fármacos , Humanos , Invasividad Neoplásica , Pirimidinonas/farmacología , Trastuzumab/uso terapéutico
12.
J Cardiovasc Pharmacol ; 70(3): 184-193, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-28678055

RESUMEN

The aim of this study was to explore the effect and mechanism of action of resveratrol (RSV) on cardiac function in diabetic cardiomyopathy (DCM). Hyperglycemia-induced apoptosis contributes to the pathogenic changes in DCM. RSV treatment inhibited high glucose-induced apoptosis of neonatal rat ventricular myocytes. Additionally, high glucose decreased cell viability, prevented serine-threonine kinase (Akt) and FoxO3a phosphorylation, and suppressed cytoplasmic translocation of FoxO3a. However, these effects of apoptosis were reversed by 10 µM of RSV. The PI3K inhibitor LY294002 abolished the RSV protective effect in vitro. RSV (5 or 50 mg·kg·d orally for 8 weeks) prevented the deterioration of cardiac function and structural cardiomyopathy in a streptozotocin-induced rat model of diabetes and reduced apoptosis in diabetic myocardium. Furthermore, it restored streptozotocin-impaired phosphorylation of Akt and FoxO3a (p-Akt and p-FoxO3a) and suppressed nuclear translocation of FoxO3a in vivo. Together, these data indicate that RSV has therapeutic potential against DCM by inhibiting apoptosis via the PI3K/Akt/FoxO3a pathway.


Asunto(s)
Apoptosis/efectos de los fármacos , Cardiomiopatías Diabéticas/tratamiento farmacológico , Proteína Forkhead Box O3/antagonistas & inhibidores , Inhibidores de las Quinasa Fosfoinosítidos-3 , Proteínas Proto-Oncogénicas c-akt/antagonistas & inhibidores , Estilbenos/uso terapéutico , Animales , Apoptosis/fisiología , Cardiomiopatías Diabéticas/metabolismo , Modelos Animales de Enfermedad , Proteína Forkhead Box O3/metabolismo , Masculino , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , Resveratrol , Transducción de Señal/efectos de los fármacos , Transducción de Señal/fisiología , Estilbenos/farmacología
13.
Regul Toxicol Pharmacol ; 87: 9-22, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28454720

RESUMEN

To investigate the potential carcinogenicity of cyadox, an antimicrobial agent, four groups of Sprague-Dawley rats (50 rats/sex/group) were fed diets containing cyadox (0, 200, 600 or 2000 mg/kg) for up to two years. There were significant decreases in body weight, feed intake and feed efficiency in both genders during most of the period in the 2000 mg/kg group. Significant decreases in serum ALT were observed in the 2000 mg/kg group at weeks 52, 78 and 104. For the control, 200, 600, and 2000 mg/kg groups, the tumor incidence in females was 33.3%, 37.2%, 40.0% and 19.0%, while it in males it was 18.9%, 2.6%, 17.1% and 13.6%, respectively. At histopathology, no increases in tumor incidence were attributed to treatment with cyadox. The mild swelling and fatty degeneration in hepatocytes, and mild swelling and tubular necrosis in the kidney were observed in 2000 mg/kg group. The no-observed-effect-level (NOEL) for carcinogenicity of cyadox fed to rats was 2000 mg/kg diet (132.18-156.28 mg/kg b.w./day). In conclusion, cyadox was not carcinogenic to rats with the liver and kidney as the target organs, and the side chain may be involved in toxicity and carcinogenicity mediated by QdNOs.


Asunto(s)
Antiinfecciosos/toxicidad , Pruebas de Carcinogenicidad , Animales , Antiinfecciosos/administración & dosificación , Dieta , Femenino , Masculino , Nivel sin Efectos Adversos Observados , Quinoxalinas/administración & dosificación , Quinoxalinas/toxicidad , Ratas , Ratas Sprague-Dawley , Factores de Tiempo
14.
Sensors (Basel) ; 17(3)2017 Feb 23.
Artículo en Inglés | MEDLINE | ID: mdl-28241488

RESUMEN

Chongqing mountain citrus orchard is one of the main origins of Chinese citrus. Its planting terrain is complex and soil parent material is diverse. Currently, the citrus fertilization, irrigation and other management processes still have great blindness. They usually use the same pattern and the same formula rather than considering the orchard terrain features, soil differences, species characteristics and the state of tree growth. With the help of the ZigBee technology, artificial intelligence and decision support technology, this paper has developed the research on the application technology of agricultural Internet of Things for real-time monitoring of citrus soil moisture and nutrients as well as the research on the integration of fertilization and irrigation decision support system. Some achievements were obtained including single-point multi-layer citrus soil temperature and humidity detection wireless sensor nodes and citrus precision fertilization and irrigation management decision support system. They were applied in citrus base in the Three Gorges Reservoir Area. The results showed that the system could help the grower to scientifically fertilize or irrigate, improve the precision operation level of citrus production, reduce the labor cost and reduce the pollution caused by chemical fertilizer.


Asunto(s)
Citrus , Agricultura , Fertilizantes , Suelo , Árboles , Agua
16.
Biochem Biophys Res Commun ; 464(3): 908-15, 2015 Aug 28.
Artículo en Inglés | MEDLINE | ID: mdl-26188094

RESUMEN

This study aimed to explore the effects of puerarin on autophagy in cardiac hypertrophy. Decreased 5'-adenosine monophosphate kinase (AMPK) activity alone with inhibited autophagy could be detected in rats within 3 weeks after aortic banding (AB). Puerarin treatment for 3 weeks in AB rats significantly restored autophagy. Administration of puerarin for 6 weeks effectively restricted cardiomyocyte hypertrophy and apoptosis. In an in vitro study, similar anti-hypertrophy and anti-apoptosis effects of puerarin on isoprenaline-induced H9c2 cells were also observed. After inhibition of autophagy by pretreatment with 3-methyladenine, the protective effects of puerarin were blocked. Further in vivo study demonstrated that puerarin significantly enabled phosphorylation of 5'-AMPK to be activated, subsequently inhibiting expression of the mammalian target of rapamycin (mTOR) target proteins S6 ribosomal protein and 4E-binding protein 1. All these data indicate that puerarin exerts protective effects against cardiomyocyte hypertrophy and apoptosis, partly by restoration of autophagy through AMPK/mTOR-mediated signaling.


Asunto(s)
Autofagia/efectos de los fármacos , Cardiomegalia/prevención & control , Isoflavonas/farmacología , Proteínas Quinasas Activadas por AMP/antagonistas & inhibidores , Proteínas Quinasas Activadas por AMP/metabolismo , Adenina/análogos & derivados , Adenina/farmacología , Animales , Cardiomegalia/etiología , Cardiomegalia/patología , Proteínas Portadoras/metabolismo , Modelos Animales de Enfermedad , Péptidos y Proteínas de Señalización Intracelular , Isoproterenol/farmacología , Masculino , Proteínas Asociadas a Microtúbulos/metabolismo , Miocardio/metabolismo , Miocitos Cardíacos/efectos de los fármacos , Miocitos Cardíacos/patología , Fosfoproteínas/metabolismo , Ratas Sprague-Dawley , Proteínas Quinasas S6 Ribosómicas/metabolismo , Serina-Treonina Quinasas TOR/metabolismo , Remodelación Ventricular/efectos de los fármacos
17.
Chem Soc Rev ; 43(21): 7257-66, 2014 Nov 07.
Artículo en Inglés | MEDLINE | ID: mdl-25060777

RESUMEN

Nano-materials formed by the self-assembly of small molecules are very promising for drug delivery, regenerative medicine, and detection of important analytes due to their unique properties, such as self-assembled multivalency, biocompatibility, and fast response to external stimuli. This tutorial review focuses on their applications in detection of important analytes. Self-assembling small molecules can show fast response to external stimuli. Therefore, the gel-sol/sol-gel phase transitions of supramolecular hydrogels that can be easily identified by naked eyes have been applied for the detection of enzymes and enzyme-involving analytes. The supramolecular hydrogels can also provide semi-wet environments that can retain the activity of enzymes and recognition properties of molecular probes. Thus, they provide good platforms for the detection of many biologically and environmentally important analytes. Besides, self-assembling small molecules show big differences in fluorescence or the F-NMR signal between their self-assembled and un-assembled stages. Such small molecules can be rationally designed through the integration of fluorescent dyes or fluorine containing molecules in the self-assembling small molecules. Therefore, extensive recent research efforts have been made to explore their detection applications based on the dis-assembly triggered fluorescence/F-NMR signal turn on or the self-assembly/aggregation induced fluorescence turn on. We believe that the research efforts made to this field will ultimately lead to the development of useful nano-materials for detection applications.


Asunto(s)
Técnicas Biosensibles/métodos , Hidrogeles/química , Nanoestructuras/química , Transición de Fase , Animales , Técnicas Biosensibles/instrumentación , Colorantes Fluorescentes/química , Humanos , Espectroscopía de Resonancia Magnética/instrumentación , Espectroscopía de Resonancia Magnética/métodos , Modelos Moleculares , Nanoestructuras/ultraestructura , Espectrometría de Fluorescencia/instrumentación , Espectrometría de Fluorescencia/métodos
18.
Zhonghua Gan Zang Bing Za Zhi ; 23(4): 258-64, 2015 Apr.
Artículo en Zh | MEDLINE | ID: mdl-26133816

RESUMEN

OBJECTIVE: To assess the safety and clinical efficacy of transjugular intrahepatic portosystemic shunt (TIPS) with various stents for treating patients with cirrhosis and esophageal gastric varices bleeding. METHODS: One hundred and five patients were stratified according to stent type: bare stent group, covered stent-grafts group, combined stents group. Rates of success, shunt insufficiency, rebleeding, patient survival, and major complications were observed. The shunt insufficiency rate, rebleeding rate, and survival rate were calculated by the life tables method, the Kaplan-Meier analytical curve, and the log-rank test; a p-value less than 0.05 was considered statistically significant. RESULTS: The overall success rate of all TIPS for treating the esophageal gastric varices bleeding was 100%. The overall shunt insufficiency rates at 6-, 12-and 24-months post-TIPS were 8%, 9% and 16%, rebleeding rates were 2%, 6% and 17%, and survival rates were 100%, 97% and 94%. The shunt insufficiency rate was 26% in the bare stent group, 14% in the covered stent-grafis group, and 5% in the combined stents group (x2=1.00, P=0.61). The rebleeding rate was 33% in the bare stent group, 7% in the covered stent-grafts group, and 3%in the combined stents group (x2=1.69, P=0.43). The survival rate was 92% in the bare stent group, 93% in the covered stent-grafts group, and 100% in the combined stents group (x2=1.91, P=0.39). The shunt insufficiency rates were higher in patients with splenectomy than in those without splenectomy (30% vs.14%; x2=4.15, P=0.04). The intraperitoneal hemorrhage rates in the covered stent-grafis group and the combined stents group were significantly lower than that in the bare stent group (0% vs 0% vs 13%; x2=8.88, P=0.01). CONCLUSIONS: TIPS with an 8 mm stent effectively treated and prevented esophageal gastric varices bleeding in patients with cirrhosis. Intraperitoneal hemorrhaging caused by TIPS was significantly decreased in the covered stent-grafts group and combined stents group,which represented an improvement in safety of this treatment. However, the influence of covered stent-grafis and combined stents towards the clinical efficacy of TIPS needs further study.


Asunto(s)
Enfermedades del Esófago , Várices Esofágicas y Gástricas , Hemorragia Gastrointestinal , Cirrosis Hepática , Stents , Humanos , Estimación de Kaplan-Meier , Derivación Portosistémica Intrahepática Transyugular , Tasa de Supervivencia
19.
J Huazhong Univ Sci Technolog Med Sci ; 34(1): 81-86, 2014 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-24496683

RESUMEN

The clinical characteristics of patients with disorders of sex development (DSD), and the diagnostic values of classic cytogenetic and molecular genetic assays for DSD were investigated. In the enrolled 56 cases, there were 9 cases of 46,XY DSD, 6 cases of Turner syndrome (TS), one case of Super female syndrome, 25 cases of Klinefelter syndrome, 14 cases of 46,XX DSD, and one case of autosomal balanced rearrangements with hypospadias. The diagnosis of sex was made through physical examination, cytogenetic assay, ultrasonography, gonadal biopsy and hormonal analysis. PCR was used to detect SRY, ZFX, ZFY, DYZ3 and DYZ1 loci on Y and X chromosomes respectively. The DSD patients with the same category had similar clinical characteristics. The karyotypes in peripheral blood lymphocytes of all patients were identified. PCR-based analysis showed presence or absence of the X/Y-linked loci in several cases. Of the 9 cases of 46,XY DSD, 6 were positive for SRY, 9 for ZFX/ZFY, 9 for DYZ3 and 8 for DYZ1 loci. Of the 6 cases of TS, only 1 case with the karyotype of 45,X,/46,XX/46,XY was positive for all 5 loci. Of the 25 cases of Klinefelter syndrome, all were positive for all 5 loci. In one case of rare Klinefelter syndrome variants azoospermia factor (AZF) gene detection revealed the loss of the AZFa+AZFb region. In 14 cases of 46,XX DSD, 7 cases were positive for SRY, 14 for ZFX, 7 for ZFY, 7 for ZYZ3, and 5 for DYZ1. PCR can complement and also confirm cytogenetic studies in the diagnosis of sex in cases of DSD.


Asunto(s)
Aberraciones Cromosómicas , Trastornos del Desarrollo Sexual/diagnóstico , Trastornos del Desarrollo Sexual/genética , Eliminación de Gen , Adolescente , Adulto , Niño , Preescolar , Bandeo Cromosómico , Cromosomas Humanos X/genética , Cromosomas Humanos Y/genética , Femenino , Sitios Genéticos/genética , Humanos , Cariotipificación , Factores de Transcripción de Tipo Kruppel/genética , Masculino , Reacción en Cadena de la Polimerasa , Aberraciones Cromosómicas Sexuales , Proteína de la Región Y Determinante del Sexo/genética , Adulto Joven
20.
Zhongguo Zhong Yao Za Zhi ; 39(15): 2972-7, 2014 Aug.
Artículo en Zh | MEDLINE | ID: mdl-25423843

RESUMEN

The EU is an international bridge of traditional Chinese medicine (TCM), and TCM in EU is of strategic importance. In this paper the progress on policies and regulations and approved products of herbal medical products in EU in 10 years were briefly reviewed, registration regulations were systematically, studied and some typical cases were analyzed. To provide reference for successful registration of TCM in EU and implementation of international strategy of TCM, five key elements (i. e. registration classification, approval procedure, approval authority, application product and application enterprise) to break through the registration barriers on TCM in EU were putted forwards correspondingly.


Asunto(s)
Unión Europea , Medicina Tradicional China , Aprobación de Drogas , Políticas , Publicaciones , Control Social Formal
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