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BACKGROUND: Labor represents a period of significant physical activity. Inefficient energy supply may delay labor process and even lead to cesarean delivery. Herein we investigated whether ingestion of a carbohydrate-rich beverage could reduce cesarean delivery in laboring women with epidural analgesia. METHODS: This multicenter randomized trial was conducted in obstetrician-led maternity units of nine tertiary hospitals in China. Primigravidae with single term cephalic pregnancy who were preparing for vaginal birth under epidural analgesia were randomized to intake a carbohydrate-rich beverage or commercially available low-carbohydrate beverages during labor. The primary outcome was the rate of cesarean delivery. Secondary outcomes included maternal feeling of hunger, assessed with an 11-point scale where 0 indicated no hunger and 10 the most severe hunger, and maternal and neonatal blood glucose after childbirth. RESULTS: Between 17 January 2018 and 20 July 2018, 2008 women were enrolled and randomized, 1953 were included in the intention-to-treat analysis. The rate of cesarean delivery did not differ between the two groups (11.3% [111/982] with carbohydrate-rich beverage vs. 10.9% [106/971] with low-carbohydrate beverages; relative risk 1.04, 95% CI 0.81 to 1.33; p = 0.79). Women in the carbohydrate-rich beverage group had lower subjective hunger score (median 3 [interquartile range 2 to 5] vs. 4 [2 to 6]; median difference - 1; 95% CI - 1 to 0; p < 0.01); their neonates had less hypoglycemia (1.0% [10/968] vs. 2.3% [22/956]; relative risk 0.45; 95% CI 0.21 to 0.94; p = 0.03) when compared with those in the low-carbohydrate beverage group. They also had higher rates of maternal hyperglycemia (6.9% [67/965] vs. 1.9% [18/953]; p < 0.01) and neonatal hyperglycemia (9.2% [89/968] vs. 5.8% [55/956]; p < 0.01), but none required special treatment. CONCLUSIONS: For laboring primigravidae with epidural analgesia, ingestion of a carbohydrate-rich beverage compared with low-carbohydrate beverages did not reduce cesarean delivery, but relieved maternal hunger and reduced neonatal hypoglycemia at the expense of increased hyperglycemia of both mothers and neonates. Optimal rate of carbohydrate supplementation remains to be determined. TRIAL REGISTRATION: www.chictr.org.cn ; identifier: ChiCTR-IOR-17011994 ; registered on 14 July 2017.
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Analgesia Epidural , Analgesia Obstétrica , Hiperglucemia , Hipoglucemia , Enfermedades del Recién Nacido , Analgésicos , Bebidas , Carbohidratos , Femenino , Humanos , Recién Nacido , Masculino , EmbarazoRESUMEN
A series of target compounds 1,3-benzodioxole-based fibrate derivatives were designed and synthesized. All the target compounds were preliminarily evaluated by hyperlipidemia mice induced by Triton WR-1339, in which compound 12 displayed a greater anti-hyperlipidemia activity than other compounds as well as positive drug fenofibrate (FF). 12 showed a significant reduction of plasma lipids, such as triglycerides (TG), total cholesterol (TC) and low-density lipoprotein cholesterin (LDL-C), in high fat diet (HFD) induced hyperlipidemic mice. In addition, hepatic transaminases (AST and ALT) were ameliorated after administration of 12, in particular the AST, and the histopathological examination showed that 12 improved the hepatic lipid accumulation. The expression of PPAR-α involved in lipids metabolism was up-regulated in the liver tissues of 12-treated group. Other significant activity such as antioxidant, and anti-inflammation was confirmed and reinforced the effects of 12 as a potential hypolipidemia and hepatoprotective agent.
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Dioxoles/farmacología , Hiperlipidemias/tratamiento farmacológico , Hipolipemiantes/farmacología , Lípidos/antagonistas & inhibidores , Sustancias Protectoras/farmacología , Animales , Dieta Alta en Grasa/efectos adversos , Dioxoles/síntesis química , Dioxoles/química , Relación Dosis-Respuesta a Droga , Hiperlipidemias/inducido químicamente , Hiperlipidemias/metabolismo , Hipolipemiantes/síntesis química , Hipolipemiantes/química , Ratones , Estructura Molecular , Sustancias Protectoras/síntesis química , Sustancias Protectoras/química , Relación Estructura-ActividadRESUMEN
Nitric oxide (NO) dysfunction, oxidative stress, and dyslipidemia are main risk factors associated with the pathophysiology of diabetic complications. In this study, 3,4-dihydroxyphenethyl nitrate (HT-ONO2) was designed, synthesized and evaluated, which incorporated hydroxytyrosol (HT) and nitrate. HT-ONO2 significantly exhibited hypoglycemic activity after oral administration to diabetic mice induced by streptozocin (STZ). HT-ONO2 also potently decreased plasma triglyceride (TG), total cholesterol (TC) in hyperlipidemia mice induced by Triton WR 1339. Meanwhile, HT-ONO2 displayed NO-releasing and antioxidant activity both in diabetic and hyperlipidemia mice and in vitro. Moreover, HT-ONO2 shown definite vasodilation and α-glucosidase inhibition activity in vitro. The results suggested that the hybrid hydroxytyrosol-based nitrate with NO supplement, antioxidant, hypoglycemia and hypolipidemia provided a potential multi-target agent to ameliorate the diabetes mellitus and its complications.
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Antioxidantes/farmacología , Hipoglucemiantes/farmacología , Hipolipemiantes/farmacología , Nitratos/farmacología , Óxido Nítrico/metabolismo , Alcohol Feniletílico/análogos & derivados , Administración Oral , Animales , Antioxidantes/administración & dosificación , Diabetes Mellitus Experimental/inducido químicamente , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Experimental/metabolismo , Hipoglucemiantes/administración & dosificación , Hipolipemiantes/administración & dosificación , Ratones , Estructura Molecular , Nitratos/administración & dosificación , Alcohol Feniletílico/administración & dosificación , Alcohol Feniletílico/farmacología , EstreptozocinaRESUMEN
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in both vasculogenesis and angiogenesis. Inhibition of VEGFR-2 has been demonstrated as a key method against tumor-associated angiogenesis. Thiazolopyrimidine is an important analog of the purine ring, and we choose the thiazolopyrimidine scaffold as the mother nucleus. Two series of thiazolo[5,4-d]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activity. In HUVEC inhibition assay, compounds 3l (=1-(5-{[2-(4-chlorophenyl)-5-methyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl]amino}pyridin-2-yl)-3-(3,4-dimethylphenyl)urea) and 3m (=1-(5-{[2-(4-chlorophenyl)-5-methyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl]amino}pyridin-2-yl)-3-(4-methoxyphenyl)urea) exhibited the most potent inhibitory effect (IC50 =1.65 and 3.52â µm, respectively). Compound 3l also showed the best potency against VEGFR-2 at 50â µm (98.5 %). These results suggest that further investigation of compound 3l might provide potential angiogenesis inhibitors.
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Inhibidores de la Angiogénesis/síntesis química , Diseño de Fármacos , Pirimidinas/química , Tiazoles/química , Inhibidores de la Angiogénesis/química , Inhibidores de la Angiogénesis/farmacología , Proliferación Celular/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana , Humanos , Neovascularización Fisiológica/efectos de los fármacos , Pirimidinas/farmacología , Relación Estructura-Actividad , Receptor 2 de Factores de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismoRESUMEN
Angiogenesis is crucial for tumor growth and inhibition of angiogenesis has been regarded as a promising approach for cancer therapy. Vascular endothelial growth factor receptor-2 (VEGFR-2) is an important factor in angiogenesis. In this work, a novel series of thiazolo[5,4-d]pyrimidine derivatives inhibiting angiogenesis were rationally designed and synthesized. Their inhibitory activities against human umbilical vein endothelial cells (HUVEC) were investigated inâ vitro. 1-(4-Fluorophenyl)-3-{4-[(5-methyl-2-phenyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl)amino]phenyl}urea (19b) and 1-(3-Fluorophenyl)-3-{4-[(5-methyl-2-phenyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl)amino]phenyl}urea (19g) exhibited the most potent inhibitory effect on HUVEC proliferation (IC50 =12.8 and 5.3â µm, respectively). Compound 19g could inhibit the migration of human umbilical vein endothelial cells. These results support the further investigation of these compounds as potent anticancer agents.
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Inhibidores de la Angiogénesis/farmacología , Diseño de Fármacos , Neovascularización Patológica/tratamiento farmacológico , Tiazoles/farmacología , Urea/farmacología , Inhibidores de la Angiogénesis/síntesis química , Inhibidores de la Angiogénesis/química , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Humanos , Estructura Molecular , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiazoles/química , Urea/análogos & derivados , Urea/química , Cicatrización de Heridas/efectos de los fármacosRESUMEN
A series of oxazolopyrimidine-based ureas and amides were designed, synthesized, and biologically evaluated for their antiproliferative and antiangiogenic activities. These compounds were identified to exhibit inhibitory activities against human umbilical vein endothelial cells (HUVEC) in vitro. Among these compounds, compound 22 effectively inhibited the migration and capillary-like tube formation of human umbilical vein endothelial cells. It also exhibited a concentration-dependent inhibition on capillary sprouting from the rat aorta rings. Preliminary mechanistic studies revealed that compound 22 suppressed protein kinases activation, by decreasing PI3K and ERK 1/2 phosphorylation. These results support the further investigation of this class of compounds as potential anticancer agents.
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Amidas/farmacología , Inhibidores de la Angiogénesis/química , Inhibidores de la Angiogénesis/farmacología , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Oxazoles/farmacología , Inhibidores de Proteínas Quinasas/farmacología , Proteínas Quinasas/metabolismo , Pirimidinas/farmacología , Urea/farmacología , Amidas/síntesis química , Amidas/química , Inhibidores de la Angiogénesis/síntesis química , Animales , Aorta/efectos de los fármacos , Capilares/efectos de los fármacos , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Oxazoles/química , Fosforilación/efectos de los fármacos , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/química , Pirimidinas/química , Ratas , Relación Estructura-Actividad , Urea/análogos & derivados , Urea/químicaRESUMEN
Autophagy plays an important role in the pathogenesis of Alzheimer's disease. In the present study, the blockade mechanism of emodin on amyloid-ß 25-35-induced neurotoxicity was explored. Cell viability of PC12 cells was evaluated by the MTT assay and neuro damage by the lactate dehydrogenase leakage assay. Gene silencing by small interfering RNA, cDNA constructs and transfection, as well as Western blot were performed to assess protein expression levels. AßPP/PS1 mice were administered orally with emodin (50 mg/kg/day), and LC3-II positive cells in their brain cortex sections were detected by immunohistochemical staining. Emodin could significantly inhibit the LC3-I/LC3-II conversion ratio and cell viability while decreasing the lactate dehydrogenase level in AßPP/PS1 mice and PC12 cells. LC3II positive cells in the cortex were decreased significantly by the treatment with both emodin and 3-methyladenine. Furthermore, emodin and 3-methyladenine could increase B-cell lymphoma 2 while decreasing Beclin-1 and hVps34 expressions, which were induced by amyloid-ß 25-35. Small interfering gene silencing Beclin-1 and B-cell lymphoma 2 confirmed this signaling pathway. We also found that the phosphatidylinositol 3-kinase inhibitor LY294002 could block LC3-I/LC3-II conversion and increase B-cell lymphoma 2 while decreasing hVps34 and Beclin-1 expressions. The results suggest that the blockade of emodin on amyloid-ß 25-35-induced autophagy may occur via the activation of the class III phosphatidylinositol 3-kinase/Beclin-1/B-cell lymphoma 2 pathway. Our results provide confirmatory evidence for the application of emodin in the prevention and treatment of Alzheimer's disease.
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Enfermedad de Alzheimer/prevención & control , Péptidos beta-Amiloides/antagonistas & inhibidores , Fosfatidilinositol 3-Quinasas Clase III/metabolismo , Emodina/farmacología , Fármacos Neuroprotectores/farmacología , Enfermedad de Alzheimer/tratamiento farmacológico , Péptidos beta-Amiloides/efectos adversos , Animales , Autofagia/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Fosfatidilinositol 3-Quinasas Clase III/genética , Modelos Animales de Enfermedad , Emodina/química , Emodina/uso terapéutico , Ratones , Ratones Endogámicos C57BL , Ratones Transgénicos , Fármacos Neuroprotectores/química , Fármacos Neuroprotectores/uso terapéutico , Células PC12 , Ratas , Transducción de SeñalRESUMEN
A combination of genetic algorithm and particle swarm optimization (PSO) for vehicle routing problems with time windows (VRPTW) is proposed in this paper. The improvements of the proposed algorithm include: using the particle real number encoding method to decode the route to alleviate the computation burden, applying a linear decreasing function based on the number of the iterations to provide balance between global and local exploration abilities, and integrating with the crossover operator of genetic algorithm to avoid the premature convergence and the local minimum. The experimental results show that the proposed algorithm is not only more efficient and competitive with other published results but can also obtain more optimal solutions for solving the VRPTW issue. One new well-known solution for this benchmark problem is also outlined in the following.
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ETHNOPHARMACOLOGICAL RELEVANCE: Shicao is the aerial part of Achillea alpina L., a common herb found mainly in Europe, Asia, and North America. Traditional Chinese medicine has a history of thousands of years and is widely used to treat various diseases. AIM OF STUDY: To explore the hepatoprotective effects of Shicao on CCl4-induced acute liver injury. METHODS: A rat model of acute liver injury was established and liver function indices were assessed to evaluate the protective effect of Shicao on the liver. Untargeted metabolomics of the serum and liver tissues was conducted using UPLC-Q-TOF/MS to identify differential metabolites related to acute liver injury. A network of metabolite-reaction-enzyme-gene constituents was constructed using network pharmacology. Hub targets and key components of the effect of Shicao on acute liver injury were screened from the network. RESULTS: Compared to the model group, Shicao improved the degree of liver damage through the assessment of the liver index, ALT and AST levels, and hepatic pathology slices, demonstrating its hepatoprotective effect against acute liver injury in rats. 10 and 38 differential metabolites involved in acute liver injury were identified in serum and liver tissues, respectively. Most of these were regulated or restored following treatment with Shicao, which mainly consisted of bile acids, lipids, and nucleotides such as taurocholic acid, LysoPC (17:0), and adenosine diphosphate ribose. Through the network of metabolite-reaction-enzyme-gene-constituents, 10 key components and 5 hub genes, along with 7 crucial differential metabolites, were mainly involved in glycerophospholipid metabolism, purine metabolism, biosynthesis of unsaturated fatty acids, and primary bile acid biosynthesis, which may play important roles in the prevention of acute liver injury by Shicao. CONCLUSION: This study revealed that Shicao had protective effects against CCl4-induced liver injury in rats. It was speculated that the ingredients of Shicao might be closely related to the hub targets, thereby regulating the levels of key metabolites, affecting inflammatory response and oxidative stress and attenuate the liver injury consequently. This study provides a basis for further investigation of its therapeutic potential and the mechanism of action.
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Medicamentos Herbarios Chinos , Ratas , Animales , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Medicamentos Herbarios Chinos/metabolismo , Ratas Sprague-Dawley , Farmacología en Red , Hígado , MetabolómicaRESUMEN
Ischemic brain injury is a severe medical condition with high incidences in elderly people without effective treatment for the resulting neural damages. Using a unilateral mouse stroke model, we analyze single-cell transcriptomes of ipsilateral and contralateral cortical penumbra regions to objectively reveal molecular events with single-cell resolution at 4 h and 1, 3, and 7 days post-injury. Here, we report that neurons are among the first cells that sense the lack of blood supplies by elevated expression of CCAAT/enhancer-binding protein ß (C/EBPß). To our surprise, the canonical inflammatory cytokine gene targets for C/EBPß, including interleukin-1ß (IL-1ß) and tumor necrosis factor α (TNF-α), are subsequently induced also in neuronal cells. Neuronal-specific silencing of C/EBPß or IL-1ß and TNF-α substantially alleviates downstream inflammatory injury responses and is profoundly neural protective. Taken together, our findings reveal a neuronal inflammatory mechanism underlying early pathological triggers of ischemic brain injury.
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Lesiones Encefálicas , Accidente Cerebrovascular , Humanos , Ratones , Animales , Anciano , Factor de Necrosis Tumoral alfa/genética , Factor de Necrosis Tumoral alfa/metabolismo , Regulación de la Expresión Génica , Neuronas/metabolismo , Accidente Cerebrovascular/genética , Accidente Cerebrovascular/metabolismo , Modelos Animales de Enfermedad , Lesiones Encefálicas/metabolismo , Proteína beta Potenciadora de Unión a CCAAT/metabolismoRESUMEN
This study is to observe the upregulation effect of astragaloside IV on ghrelin in diabetic cognitive impairment (DCI) rats and to investigate the pathway in prevention and treatment by reducing oxidative stress. The DCI model was induced with streptozotocin (STZ) in conjunction with a high-fat and high-sugar diet and divided into three groups: model, low-dose (40 mg/kg), and high-dose (80 mg/kg) astragaloside IV. After 30 days of gavage, the learning and memory abilities of rats, as well as their body weight and blood glucose levels, were tested using the Morris water maze and then detection of insulin resistance, SOD activity, and serum MDA levels. The whole brain of rats was sampled for hematoxylin-eosin and Nissl staining to observe pathological changes in the hippocampal CA1 region. Immunohistochemistry was used to detect ghrelin expression in the hippocampal CA1 region. A Western blot was used to determine changes in GHS-R1α/AMPK/PGC-1α/UCP2. RT-qPCR was used to determine the levels of ghrelin mRNA. Astragaloside IV reduced nerve damage, increased superoxide dismutase (SOD) activity, decreased MDA levels, and improved insulin resistance. Ghrelin levels and expression increased in serum and hippocampal tissues, and ghrelin mRNA levels increased in rat stomach tissues. According to Western blot, it increased the expression of the ghrelin receptor GHS-R1α and upregulated the mitochondrial function associated-protein AMPK-PGC-1α-UCP2. Astragaloside IV increases ghrelin expression in the brain to reduce oxidative stress and delay diabetes-induced cognitive impairment. It may be related to the promotion of ghrelin mRNA levels.
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Disfunción Cognitiva , Diabetes Mellitus Tipo 2 , Resistencia a la Insulina , Ratas , Animales , Regulación hacia Arriba , Proteínas Quinasas Activadas por AMP , Diabetes Mellitus Tipo 2/complicaciones , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Ghrelina/farmacología , Estrés Oxidativo , Disfunción Cognitiva/tratamiento farmacológico , Superóxido Dismutasa-1RESUMEN
Curcuma longa L. (CLL), a traditional herbal medicine, has been widely used for the prevention of diabetic vascular complications in recent years. However, the protective effects of curcuminoids in CLL on the AGEs-induced damage to mesangial cell are not fully understood. In this present study, dihydroethidium, superoxide dismutase kit, malondialdehyde kit, and acridine orange/ethidium bromide staining methods were used to evaluate the activities of curcumin and demethoxycurcumin (10(-11)-10(-9) M) on AGEs-induced oxidative stress and apoptosis, which were associated with the damage to mesangial cell. The results showed that these two compounds could significantly restore advanced glycation end products (AGEs)-induced apoptosis to normal levels (IC50 = 3.874 × 10(-11) M for curcumin and IC50 = 6.085 × 10(-11) M for demethoxycurcumin) and reduce remarkably reactive oxygen species generation in mesangial cell. Furthermore, curcumin and demethoxycurcumin dramatically elevated AGEs-decreased superoxide dismutase activity while significantly reducing AGEs-increased malondialdehyde content in cell culture supernatant. Our results suggest that both curcumin and demethoxycurcumin have a significant protective potential to the prevention of diabetic nephropathy.
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Curcuma/química , Curcumina/análogos & derivados , Curcumina/farmacología , Productos Finales de Glicación Avanzada/metabolismo , Células Mesangiales/efectos de los fármacos , Estrés Oxidativo , Animales , Apoptosis , Línea Celular , Curcumina/química , Diarilheptanoides , Evaluación Preclínica de Medicamentos , Activación Enzimática/efectos de los fármacos , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/farmacología , Concentración 50 Inhibidora , Malondialdehído/metabolismo , Extractos Vegetales/química , Sustancias Protectoras/química , Sustancias Protectoras/farmacología , Ratas , Especies Reactivas de Oxígeno/metabolismo , Juego de Reactivos para Diagnóstico , Rizoma/química , Superóxido Dismutasa/metabolismoRESUMEN
This article has been retracted: please see Elsevier Policy on Article Withdrawal (http://www.elsevier.com/locate/withdrawalpolicy). This article has been retracted at the request of the Editor-in-Chief. The authors have plagiarized/duplicated part of a paper that appeared in Neurosci Lett, 549 (2013) 63-68, (https://doi.org/10.1016/j.neulet.2013.06.002). Several images in the Journal of Ethnopharmacology paper; 3A, 3B, 4A, 4B correspond to figures; 2A, 2B, 3A and 3B respectively as published in Neuroscience Letters. One of the conditions of submission of a paper for publication is that authors declare explicitly that their work is original and has not appeared in a publication elsewhere. Re-use of any data should be appropriately cited. As such this article represents a severe abuse of the scientific publishing system. The scientific community takes a very strong view on this matter and apologies are offered to readers of the journal that this was not detected during the submission process.
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The spatiotemporal distribution of nano-silver in cut gerbera (Gerbera hybrida cv. Crossfire) flowers were determined by inductively coupled plasma-atomic emission spectrometry technique (ICP-AES). The relative standard deviations of this method were between 0.14% and 2.89%, and the recovery ratio obtained by standard addition method ranged from 93.33% to 106.67%. The method was proved to be simple, rapid, reliable and highly sensitive, which can meet the demands of actual sample analysis. The experimental results also showed that Ag could be found in the basal stem end, upper stem end and petal of the cut gerbera flowers treated in nano-silver solution of 5 mg x L(-1) for 24 h and thereafter placed in distilled water. However, the Ag content in basal stem ends was much higher than those in upper stem ends and petals. The results indicated that nano-silver particles could enter into the flower stems through the cuts of stem ends and then moved to different parts of the cut gerbera flowers, but most of them located in the basal stem ends during the vase period. The fact that Ag was centred in basal stem end implied that the positive preservation effects of nano-silver on cut gerbera flowers is related to its strong and sustainable antiseptic action in the stem ends of cut flowers. The above results provide a reliable method for the determination of nano-silver and theoretical basis for its futher research and application in the preservation of cut flowers.
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Asteraceae/química , Flores/química , Nanopartículas del Metal/análisis , Plata/análisis , Análisis EspectralRESUMEN
BACKGROUND: Ulcerative colitis (UC) is a chronic non-specific intestinal inflammatory disease with unknown etiology. In recent years, the global incidence has been increasing. Sijunzi decoction (SJZD) is a traditional Chinese medicine that has been used for treatment of other diseases in previous studies as it has no side effects and it has a pharmacological effect in gastrointestinal function, immune system, ulcers, and tissue repair. METHODS: PubMed, Embase, Cochrane Library, GeenMedical, China National Knowledge Infrastructure, Chinese Sci-tech Journals full-text Database, Chinese Biomedical Database, and Chinese Science Citation Database were searched to screen the related literatures of "ulcerative colitis" and "Jiawei Sijunzi decoction". The research data extracted from above studies was analyzed by Review Manager 5.3 and Stata14.2 software. RESULTS: This systematic review and meta-analysis will evaluate the efficacy and safety of Jiawei SJZD in the treatment of UC and provide effective evidence for clinical use. CONCLUSION: In this study, the published evidence of modified SJZD in the treatment of UC was systematically summarized and evaluated, so that it can be better applied in clinic. INPLASY REGISTRATION NUMBER: INPLASY2020100102.
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Colitis Ulcerosa/tratamiento farmacológico , Medicamentos Herbarios Chinos/efectos adversos , Medicamentos Herbarios Chinos/uso terapéutico , Metaanálisis como Asunto , Revisiones Sistemáticas como Asunto , Protocolos Clínicos , Humanos , Proyectos de InvestigaciónRESUMEN
During insect larval-pupal metamorphosis, proteins in the hemolymph are absorbed by the fat body for the maintenance of intracellular homeostasis; however, the type of proteins and how these proteins are internalized into the fat body are unclear. In Bombyx mori, the developmental profiles of total proteins in the hemolymph and fat body showed that hemolymph-decreased protein bands (55-100 kDa) were in accordance with those protein bands that increased in the fat body. Inhibition of clathrin-dependent endocytosis predominantly blocked the transportation of 55-100 kDa proteins from the hemolymph into the fat body, which was further verified by RNA interference treatment of Bmclathrin. Six hexamerins were shown to comprise â¼90% of the total identified proteins in both the hemolymph and fat body by mass spectrum (MS) analysis. In addition, hemolymph-specific proteins were mainly involved in material transportation, while fat body-specific proteins particularly participated in metabolism. In this paper, four hexamerins were found for the first time, and potential proteins absorbed by the fat body from the hemolymph through clathrin-dependent endocytosis were identified. This study sheds light on the protein absorption mechanism during insect metamorphosis.
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Bombyx/fisiología , Clatrina/metabolismo , Endocitosis , Cuerpo Adiposo/fisiología , Hemolinfa/fisiología , Proteínas de Insectos/metabolismo , Absorción Fisiológica , Animales , Bombyx/crecimiento & desarrollo , Larva/crecimiento & desarrollo , Larva/fisiologíaRESUMEN
The microsporidia are obligate intracellular eukaryotic parasites. They have been paid more attention as being the emerging pathogen of human, so it is important to control microsporidiosis using fast and precise detecting technology. In order to provide a reference for controlling microsporidian infection effectively, this paper reviews the progress of studying on the detecting technology from the microscopic staining methods, immunological and molecular biology.
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Microsporidios/aislamiento & purificación , Microsporidiosis/diagnóstico , Inmunohistoquímica , Biología Molecular/métodos , Coloración y EtiquetadoRESUMEN
The molecular recognition of fungicide of kresoxim-methyl with beta-cyclodextrin (beta-CD), methyl-beta-cyclodextrin (RAMEB)and hydroxypropyl-beta-cyclodextrin (RAMEB) was investigated by using UV-Vis spectroscopy analysis. The effect of temperature and polarity of solvent on the recognition interaction was studied. The driving force and the possible structure of the inclusion complexes were also discussed. The results presented that they formed inclusion complexes with a stoichiometry of 1:1, and the formation constant of inclusion complexes was in the order of Ku(HP-beta-CD)>(beta-CD)Kp(RAMEB) at 298.15 K. Elevation of the temperature triggered a decrease in stability of the inclusion complexes and the value of K(beta-D) was the biggest at > or =303.15 K. The formation constant reduced sharply with the decreasing polarity of the solvent. The standard molar Gibbs energies, enthalpies and entropies were all negative. All the results indicated that the association of the guest molecule with beta-CD was favored by enthalpy changes, and hydrophobicity and hydrogen bond interaction were main driving forces for the inclusion reaction. Our findings provided an important proof for the use of inclusion complexes of kresoxim-methyl with CDs.
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Fungicidas Industriales/química , Fenilacetatos/química , beta-Ciclodextrinas/química , 2-Hidroxipropil-beta-Ciclodextrina , Metacrilatos/química , Modelos Teóricos , Estructura Molecular , Espectrometría de Fluorescencia , Espectrofotometría Ultravioleta , EstrobilurinasRESUMEN
In the present experiment, we mainly discussed the function mechanism between the humic acid and a new kind of fungicide Pyrimorph, aiming to play a positive role in the reduction of contamination caused by pesticides on environment. After the disposition step by step, the humic acid was separated into three parts. Then IR and fluorescence analytical methods were employed to explain the functional mechanism between the pesticide and each part of humic acid. As a result, there are extensive interactions between the three parts of the humic acid and the fungicide Pyrimorph. The interactions between fulvic acid and Pyrimorph are mainly the H-bond and the transfer of the electric charge caused by the C=O of the Pyrimorph and the -OH of the fulvic acid, and the interaction between matomeilon and Pyrimorph is mainly the transfer of the electric charge, and the interaction between humin and Pyrimorph is the weakest. It was showed that the fulvic acid is the most active part in the humic acid. That's to say the intensity of the interaction between the three parts of the humic acid and the fungicide Pyrimorph is smaller and smaller with the order of molecular weight from small to big, namely fulvic acid, matomeilon acid and humin.
Asunto(s)
Benzopiranos/química , Fungicidas Industriales/química , Sustancias Húmicas/análisis , Plaguicidas/química , Espectrometría de Fluorescencia , Espectroscopía Infrarroja por Transformada de Fourier , Benzopiranos/análisis , Fungicidas Industriales/análisis , Plaguicidas/análisis , Contaminantes del Suelo/análisis , Contaminantes del Suelo/químicaRESUMEN
BACKGROUND: VEGFR-2 inhibitors have been widely used in the treatment of cancer. In our continued efforts to search for potent and novel VEGFR-2 inhibitors as antitumor agents, we have identified a series of ureas and amides bearing a oxazolopyrimidine scaffold. AIM OF THE STUDY: To discover more potent VEGFR-2 inhibitors with stronger binding affinity and better physical and chemical properties. METHODS: 23 pyrimidinylacetamide-based ureas were designed and synthesized. Replacement of oxazolopyrimidine with a pyrimidinylacetamide generated a series of novel VEGFR-2 inhibitors. RESULTS AND CONCLUSIONS: In HUVEC inhibition assay, the most potent compound (compound 16) possessed an IC50 value of 0.43 µM. Compound 16 also inhibited the migration and capillary like tube formation of HUVECs with inhibition rate at 22% (1 µM) and 17.5% (0.8 µM) respectively. These results support the further investigation of compound 16 as a potential anti-cancer agent.