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BACKGROUND: 3% chloroprocaine (CP) has been reported as the common local anesthetic used in pregnant women undergoing urgent cesarean delivery during labor analgesia period. However, 0.75% ropivacaine is considered a promising and effective alternative. Therefore, we conducted a randomized controlled trial to compare the effectiveness and safety of 0.75% ropivacaine with 3% chloroprocaine for extended epidural anesthesia in pregnant women. METHODS: We conducted a double-blind, randomized, controlled, single-center study from November 1, 2022, to April 30, 2023. We selected forty-five pregnant women undergoing urgent cesarean delivery during labor analgesia period and randomized them to receive either 0.75% ropivacaine or 3% chloroprocaine in a 1:1 ratio. The primary outcome was the time to loss of cold sensation at the T4 level. RESULTS: There was a significant difference between the two groups in the time to achieve loss of cold sensation (303, 95%CI 255 to 402 S vs. 372, 95%CI 297 to 630 S, p = 0.024). There was no significant difference the degree of motor block (p = 0.185) at the Th4 level. Fewer pregnant women required additional local anesthetics in the ropivacaine group compared to the chloroprocaine group (4.5% VS. 34.8%, p = 0.011). The ropivacaine group had lower intraoperative VAS scores (p = 0.023) and higher patient satisfaction scores (p = 0.040) than the chloroprocaine group. The incidence of intraoperative complications was similar between the two groups, and no serious complications were observed. CONCLUSIONS: Our study found that 0.75% ropivacaine was associated with less intraoperative pain treatment, higher patient satisfaction and reduced the onset time compared to 3% chloroprocaine in pregnant women undergoing urgent cesarean delivery during labor analgesia period. Therefore, 0.75% ropivacaine may be a suitable drug in pregnant women undergoing urgent cesarean delivery during labor analgesia period. CLINICAL TRIAL NUMBER AND REGISTRY URL: The registration number: ChiCTR2200065201; http://www.chictr.org.cn , Principal investigator: MEN, Date of registration: 31/10/2022.
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Analgesia Obstétrica , Anestésicos Locales , Cesárea , Procaína , Ropivacaína , Humanos , Femenino , Ropivacaína/administración & dosificación , Embarazo , Método Doble Ciego , Cesárea/métodos , Anestésicos Locales/administración & dosificación , Adulto , Analgesia Obstétrica/métodos , Procaína/análogos & derivados , Procaína/administración & dosificaciónRESUMEN
BACKGROUND: During emergency endoscopic retrograde cholangiopancreatography (ERCP), the safety and feasibility of performing one-stage endoscopic treatment for patients with acute cholangitis (AC) due to choledocholithiasis are unclear. AIM: To investigate the safety and feasibility of one-stage endoscopic treatment for moderate to severe AC. METHODS: We enrolled all patients diagnosed with moderate to severe cholangitis due to common bile duct stones from January 2019 to July 2023. The outcomes were compared in this study between patients who underwent ERCP within 24 h and those who underwent ERCP 24 h later, employing a propensity score (PS) framework. Our primary outcomes were intensive care unit (ICU) admission rates, ICU length of stay, and duration of antibiotic use. RESULTS: In total, we included 254 patients and categorized them into two groups based on the time elapsed between admission and intervention: The urgent group (≤ 24 h, n = 102) and the elective group (> 24 h, n = 152). Ninety-three pairs of patients with similar characteristics were selected by PS matching. The urgent ERCP group had more ICU admissions (34.4% vs 21.5%, P = 0.05), shorter ICU stays (3 d vs 9 d, P < 0.001), fewer antibiotic use (6 d vs 9 d, P < 0.001), and shorter hospital stays (9 d vs 18.5 d, P < 0.001). There were no significant differences observed in adverse events, in-hospital mortality, recurrent cholangitis occurrence, 30-d readmission rate or 30-d mortality. CONCLUSION: Urgent one-stage ERCP provides the advantages of a shorter ICU stay, a shorter duration of antibiotic use, and a shorter hospital stay.
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Colangiopancreatografia Retrógrada Endoscópica , Colangitis , Coledocolitiasis , Estudios de Factibilidad , Tiempo de Internación , Puntaje de Propensión , Humanos , Femenino , Masculino , Coledocolitiasis/cirugía , Coledocolitiasis/diagnóstico , Coledocolitiasis/complicaciones , Colangiopancreatografia Retrógrada Endoscópica/efectos adversos , Colangitis/cirugía , Colangitis/etiología , Anciano , Persona de Mediana Edad , Tiempo de Internación/estadística & datos numéricos , Enfermedad Aguda , Resultado del Tratamiento , Estudios Retrospectivos , Índice de Severidad de la Enfermedad , Unidades de Cuidados Intensivos/estadística & datos numéricos , Antibacterianos/uso terapéutico , Anciano de 80 o más AñosRESUMEN
Cell-laden hydrogel fibers/tubules are one of the fundamentals of tissue engineering. They have been proven as a promising method for constructing biomimetic tissues, such as muscle fibers, nerve conduits, tendon and vessels, etc. However, current hydrogel fiber/tubule production methods have limitations in ordered cell arrangements, thus impeding the biomimetic configurations. Acoustic cell patterning is a cell manipulation method that has good biocompatibility, wide tunability, and is contact-free. However, there are few studies on acoustic cell patterning for fiber production, especially on the radial figure cell arrangements, which mimic many native tissue-like cell arrangements. Here, an acoustic cell patterning system that can be used to produce hydrogel fibers/tubules with tunable cell patterns is shown. Cells can be pre-patterned in the liquid hydrogel before being extruded as cross-linked hydrogel fibers/tubules. The radial patterns can be tuned with different complexities based on the acoustic resonances. Cell viability assays after 72 h confirm good cell viability and proliferation. Considering the biocompatibility and reliability, the present method can be further used for a variety of biomimetic fabrications.
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Hidrogeles , Andamios del Tejido , Reproducibilidad de los Resultados , Ingeniería de Tejidos/métodos , Supervivencia CelularRESUMEN
AIM: To explore the usage of choroidal thickness measured by swept-source optical coherence tomography (SS-OCT) to detect myopic macular degeneration (MMD) in high myopic participants. METHODS: Participants with bilateral high myopia (≤-6 diopters) were recruited from a subset of the Guangzhou Zhongshan Ophthalmic Center-Brien Holden Vision Institute High Myopia Cohort Study. SS-OCT was performed to determine the choroidal thickness, and myopic maculopathy was graded by the International Meta-Analysis for Pathologic Myopia (META-PM) Classiï¬cation. Presence of MMD was defined as META-PM category 2 or above. RESULTS: A total of 568 right eyes were included for analysis. Eyes with MMD (n=106, 18.7%) were found to have older age, longer axial lengths (AL), higher myopic spherical equivalents (SE), and reduced choroidal thickness in each Early Treatment Diabetic Retinopathy Study (ETDRS) grid sector (P<0.001). The area under the receiver operating characteristic (ROC) curves (AUC) for subfoveal choroidal thickness (0.907) was greater than that of the model, including age, AL, and SE at 0.6249, 0.8208, and 0.8205, respectively. The choroidal thickness of the inner and outer nasal sectors was the most accurate indicator of MMD (AUC of 0.928 and 0.923, respectively). An outer nasal sector choroidal thickness of less than 74 µm demonstrated the highest odds of predicting MMD (OR=33.8). CONCLUSION: Choroidal thickness detects the presence of MMD with high agreement, particularly of the inner and outer nasal sectors of the posterior pole, which appears to be a biometric parameter more precise than age, AL, or SE.
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BACKGROUND: Cervical dystonia (CD) is a type of muscle tone disorder that usually occurs in the neck muscles. Due to the intermittent or continuous involuntary contraction of the neck muscles, the head and neck are twisted and skewed and some postural abnormalities occur. Long-term abnormal posture or pain can cause negative emotions in patients, which can affect their quality of life. CASE SUMMARY: This case report included a 37-year-old woman who was diagnosed with CD associated with anxiety and depression; the accompanying symptoms were head and neck tilt of approximately 90° to the right and mental abnormality. After two courses of acupuncture treatment, the patient's head and neck can be maintained in a normal position, and the negative emotions can be relieved. CONCLUSION: This case indicates that acupuncture can effectively improve CD and the emotional state and quality of life of patients, making it an effective alternative treatment for the condition.
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Palmitoyl protein thioesterase 1(PPT1) is a lysosomal enzyme that catalyzes the protein depalmitoylation. It is considered to play a crucial role in regulating lysosomes, mitochondria and lipid metabolism. PPT1 has been reported to play an important role in the occurrence and progression of diseases, such as neurological diseases and cancers. However, the regulatory mechanisms remain unknown. In this review, we summarize the progress of PPT1 function and mechanisms in neurological disorders and cancers, which will provide as reference and guidance for exploring the regulatory mechanisms of PPT1 and developing new drugs for treating related diseases in the future.
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Neoplasias , Humanos , Homeostasis , Lisosomas , Proteínas de la Membrana , Tioléster Hidrolasas/genéticaRESUMEN
OBJECTIVE: To investigate the effect of "Huayu Tongluo" (resolving blood stagnation to dredge meridian-collaterals) moxibustion on remyelination and Sonic Hedgehog (Shh) signaling pathway in the corpus callosum of vascular dementia (VD) rats, so as to explore its mechanisms underlying improvement of VD. METHODS: Male Wistar rats were randomized into sham-operation, model, medication and moxibustion groups, with 12 rats in each group.The VD model was established by bilateral common carotid artery occlusion. Moxibustion was applied to "Shenting"(GV24), "Baihui"(GV20) and "Dazhui"(GV14) for 20 min once a day, 7 d as a treatment course, for 3 courses, with one day's rest between every two courses. Rats of the medication group were treated by gavage of 10 mg/kg of chloromastine solution once a day, and the course of treatment was the same as that of the moxibustion group. The rat's learning-memory ability was assessed by Morris water maze test (escape latency). The neurological deficits were evaluated by using Longa's scale.The mRNA and protein expressions of Shh and Gli1 in the corpus callosum were measured by quantitative real-time fluorescence PCR and Western blot, separately. The ultrastructure of the myelin sheath and myelinated axons was observed under transmission electron microscopy (TCM). RESULTS: Compared with the sham-operation group, the neurologic score and escape latency were significantly increased and prolonged (P<0.01), and the mRNA and protein expression levels of Shh and Gli1 and the number of myelinated axons were obviously decreased in the model group (P<0.01). In comparison with the model group, the escape latency was apparently shortened (P<0.05), while the mRNA and protein expression levels of Shh and Gli1 as well as the number of myelinated axons were strikingly increased in both moxibustion and medication groups (P<0.01). Results of TCM showed that in the model group, the arrangement of myelin coil structures was sparse and fuzzy, and some structures were bulged and disbanded. The oligodendrocytes were irregular, and the number of myelin sheath was rare. These situations were relatively milder in both moxibustion and medication groups. CONCLUSION: "Huayu Tongluo" moxibustion can promote the differentiation and maturation of oligodendrocyte precursor cells after cerebral ischemia by regulating the expressions of Shh and Gli1 in Shh signaling pathway, thus promoting the regeneration of cerebral white matter myelin sheaths in VD rats, which may contribute to improving learning-memory ability.
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Demencia Vascular , Moxibustión , Masculino , Ratas , Animales , Proteínas Hedgehog/genética , Vaina de Mielina , Demencia Vascular/genética , Demencia Vascular/terapia , Proteína con Dedos de Zinc GLI1/genética , Ratas Wistar , Transducción de Señal , RegeneraciónRESUMEN
Manipulation of micro-objects have been playing an essential role in biochemical analysis or clinical diagnostics. Among the diverse technologies for micromanipulation, acoustic methods show the advantages of good biocompatibility, wide tunability, a label-free and contactless manner. Thus, acoustic micromanipulations have been widely exploited in micro-analysis systems. In this article, we reviewed the acoustic micromanipulation systems that were actuated by sub-MHz acoustic waves. In contrast to the high-frequency range, the acoustic microsystems operating at sub-MHz acoustic frequency are more accessible, whose acoustic sources are at low cost and even available from daily acoustic devices (e.g. buzzers, speakers, piezoelectric plates). The broad availability, with the addition of the advantages of acoustic micromanipulation, make sub-MHz microsystems promising for a variety of biomedical applications. Here, we review recent progresses in sub-MHz acoustic micromanipulation technologies, focusing on their applications in biomedical fields. These technologies are based on the basic acoustic phenomenon, such as cavitation, acoustic radiation force, and acoustic streaming. And categorized by their applications, we introduce these systems for mixing, pumping and droplet generation, separation and enrichment, patterning, rotation, propulsion and actuation. The diverse applications of these systems hold great promise for a wide range of enhancements in biomedicines and attract increasing interest for further investigation.
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Sonido , Vibración , Acústica , Micromanipulación/métodos , TecnologíaRESUMEN
Aim: To achieve accurate detection of circulating tumor cells (CTCs) in a large-volume sample. Materials & methods: Silica nanoparticles were crosslinked layer-by-layer on glass slides as the substrate of a chip using polyacrylic acid. Polyacrylic acid was immobilized as a spacer and capture ligands were immobilized on the spacer. Results: The chip can be integrally applied to capture, post-treatment and imaging detection for CTCs. The detected cell numbers were 33 and 40 for 9 cell/ml samples and clinical blood samples (7.5 ml), respectively. The detection ratio of positive samples was 100%. Conclusion: The significantly increased detected number for CTCs indicates that this methodology may avoid or greatly reduce the false-negative ratio of positive clinical samples.
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Nanopartículas , Células Neoplásicas Circulantes , Humanos , Línea Celular Tumoral , Diagnóstico por Imagen , Separación CelularRESUMEN
Importance: Epidural anesthesia is a primary choice for cesarean delivery, but supplemental analgesics are often required to relieve pain during uterine traction. Objective: To investigate the sedative and analgesic effects of intravenous esketamine administered before childbirth via cesarean delivery with the patient under epidural anesthesia. Design, Setting, and Participants: This multicenter, double-blind randomized clinical trial assessed 903 women 18 years or older who had full-term single pregnancy and were scheduled for elective cesarean delivery with epidural anesthesia in 5 medical centers in China from September 18, 2021, to September 20, 2022. Intervention: Patients were randomized to receive intravenous injection of 0.25 mg/kg of esketamine or placebo before incision. Main Outcomes and Measures: The coprimary outcomes included scores on the numeric rating scale of pain (an 11-point scale, with 0 indicating no pain and 10 indicating the worst pain; a difference of ≥1.65 points was clinically meaningful) and Ramsay Sedation Scale (a 6-point scale, with 1 indicating restlessness and 6 indicating deep sleep without response; a difference of ≥2 points was clinically meaningful) immediately after fetal delivery. Secondary outcomes included neonatal Apgar score assessed at 1 and 5 minutes after birth. Results: A total of 600 women (mean [SD] age, 30.7 [4.3] years) were enrolled and randomized; all were included in the intention-to-treat analysis. Immediately after fetal delivery, the score on the numeric rating scale of pain was lower with esketamine (median [IQR], 0 [0-1]) than with placebo (median [IQR], 0 [0-2]; median difference, 0; 95% CI, 0-0; P = .001), but the difference was not clinically important. The Ramsay Sedation Scale scores were higher (sedation deeper) with esketamine (median [IQR], 4 [3-4]) than with placebo (median [IQR], 2 [2-2]; median difference, 2; 95% CI, 2-2; P < .001). The neonatal Apgar scores did not differ between the 2 groups at 1 minute (median difference, 0; 95% CI, 0-0; P = .98) and at 5 minutes (median difference, 0; 95% CI, 0-0; P = .27). Transient neurologic or mental symptoms were more common in patients given esketamine (97.7% [293 of 300]) than in those given placebo (4.7% [14 of 300]; P < .001). Conclusions and Relevance: For women undergoing cesarean delivery under epidural anesthesia, a subanesthetic dose of esketamine administered before incision produced transient analgesia and sedation but did not induce significant neonatal depression. Mental symptoms and nystagmus were common but transient. Indications and the optimal dose of esketamine in this patient population need further clarification, but study should be limited to those who require supplemental analgesia. Trial Registration: ClinicalTrials.gov Identifier: NCT04548973.
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Analgesia Epidural , Cesárea , Embarazo , Recién Nacido , Humanos , Femenino , Adulto , Cesárea/efectos adversos , Manejo del Dolor , DolorRESUMEN
OBJECTIVE: To investigate the effect of moxibustion on the proteins related with apoptosis and nuclear transcription factor kappa B (NF-κB) in hippocampus of diabetic rats with cognitive impairment (CI), so as to explore its mechanism underlying improvement of learning-memory ability. METHODS: Thirty SD rats were randomly divided into normal, model and moxibustion groups (n=10 rats/group). The diabetic model was established by i.p. injection of streptozotocin solution (25 mg·kg-1·d-1), followed by high-fat diet raising for 4 weeks, and the CI model was confirmed by Morris water maze test. The rats in the moxibustion group were given moxibustion at "Shenting" (GV24), "Baihui" (GV20) and "Dazhui" (GV14) for 20 min each time, the treatment was conducted 6 times a week for 4 weeks. The learning-memory ability was detected by Morris water maze test, the random blood glucose of rats was measured by glucometer and test strips. The protein and mRNA expression levels of Bcl-2, Bax, Caspase-3 and NF-κB p65 in hippocampus were detected by Western blot and quantitative real-time PCR, separately. RESULTS: After modeling, the random blood glucose, escape latency, and the expression levels of Bax, Caspase-3 and NF-κB p65 proteins and mRNAs in the model group were significantly increased, while the expression levels of Bcl-2 protein and mRNA were decreased (P<0.001ï¼P<0.01, P<0.05) in comparison with the normal group. Following the treatment, the modeling induced increase of blood glucose, escape latency, and the expression levels of Bax, Caspase-3 and NF-κB p65 proteins and mRNAs, as well as decrease of Bcl-2 protein and mRNA expression levels were reversed (P<0.05, P<0.01, P<0.001). CONCLUSION: Moxibustion can improve learning-memory ability in diabetic rats with cognitive impairment, which may be related to its function in regulating the expression levels of hippocampal Bcl-2, Bax, Caspase-3 and NF-κB.
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Disfunción Cognitiva , Diabetes Mellitus Experimental , Moxibustión , Animales , Ratas , Ratas Sprague-Dawley , Caspasa 3 , FN-kappa B , Glucemia , Proteína X Asociada a bcl-2 , Proteínas Proto-Oncogénicas c-bcl-2 , Apoptosis , HipocampoRESUMEN
We investigated species composition and community structure of a typical Quercus variabilis natural secondary forest in the northern foothills of the Qinling Mountains, within the dynamic monitoring plot of deciduous broad-leaved forest at the Louguantai experimental forest farm in Zhouzhi County, Shaanxi Province. The results showed that there were 3162 individual woody plants with diameter at breast height ≥1 cm in the plot, which were belonged to 42 species, 36 genera, and 25 families. The community genus's areal type was dominated by the temperate component, which accounted for 44.4%, and followed by the tropical component. The community was dominated by several tree species. The top three species with respect to importance value were Q. variabilis, Pinus tabuliformis, and Quercus aliena, with the sum of their importance value being 64.7%. The average DBH of all woody plants was 7.58 cm. The distribution of all individuals and dominant species in the tree layer was approximately normal, with more medium-size individuals. The community structure was stable. The community was poorly renewed, with a trend of population decline. Biodiversity indices varied considerably among different plots, being lower than those of subtropical broad-leaved evergreen forests. There was a significant correlation between community species distribution and environmental factors. Soil and topography explained 42.4% of the variation in community distribution. Altitude and soil alkali hydrolysable nitrogen had a significant effect on community distribution. Altitude, soil total phosphorus, and organic matter content significantly affected the species diversity of Q. variabilis communities. The stronger adaptability of Q. variabilis populations allowed them to become dominant in low-nutrient environments, which limited species diversity in the community.
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Quercus , Humanos , Animales , Bosques , Árboles , Plantas , China , SueloRESUMEN
Shrub is an important part of forest ecosystem. Exploring the species composition, structure and spatial distribution of shrub layer can lay an important foundation for further clarifying the mechanisms underlying species coexistence, biodiversity maintenance and community succession. In this study, species composition, spatial distribution, and species diversity of shrub layer were analyzed in 25 hm2 of Huangguan forest plot. A total of 20716 individual shrubs (with 10463 branches) were recorded in the plot, belonging to 54 species, 45 genera, 28 families. The status of dominant species in the shrub layer was not obvious, with all the importance values being less than 10. The diameter structure of shrub layer vegetation was inverted 'J' type. Shrubs showed aggregated distribution in the plot, with obvious altitude differences in spatial distribution. The diameter structure and spatial distribution of the nine shrub species with the largest abundance in the plot were consistent with the overall situation of shrub layer. With increasing altitude, the Shannon diversity index (H) and Simpson dominance index (D) did not change significantly, while the Pielou evenness index (E) decreased. Those indices decreased with the increases of the abundance of dominant species in tree layer, and E increased with the increase of the number of dominant species in sub-tree layer. The indices of H, D, E were significantly negatively correlated with soil total phosphorus (TP). The H index was significantly positively correlated with soil pH, and the E index was significantly positively correlated with soil total potassium. The shrub layer was rich in species, stable in community structure and well regenerated. The species diversity of shrub layer was mainly affected by the number of dominant species in the tree layer, soil pH, and TP.
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Ecosistema , Bosques , Biodiversidad , China , Humanos , Fósforo , Suelo , ÁrbolesRESUMEN
In this study, the spatial distribution patterns of individuals with different diameter classes of dominant shrub Lonicera fragrantissima var. lancifolia and the intraspecific and interspecific relationships were analyzed in Qinling Huangguan Plot. The results showed that the diameter class structure of L. fragrantissima var. lancifolia showed a pyramid shape, with a wide bottom and a narrow top. The number of small-diameter class individuals was the largest, showing a good state of renewal and a stable growth, which was conducive to community renewal and succession. Based on Ripley's K function, using univariate and bivariate paired correlation functions, under complete spatial randomness model, heterogeneous Poisson model and antecedent condition model, all individual of the species and their diameter-dividing classes were mainly aggregated, and the aggregation degree decreased with the increases of research scale, and gradually tended to random distribution. Affected by habitat heterogeneity, diffusion restriction and negative density dependence, there was a positive correlation among different intraspecific dia-meter classes, and also a certain degree of no correlation, but without negative correlation. The interspecific relationship was complex. All types of association (no, positive and negative) were observed, but negative association and no association were dominated.
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Bosques , Lonicera , China , Ecosistema , Humanos , ÁrbolesRESUMEN
To explore the spatial distribution and intraspecific correlation of Quercus aliena var. acutiserrata, a domi-nant tree species in a 25 hm2 plot of warm temperate deciduous broadleaved forest in Qinling Mountains, the pair-correlation function g(r) was used to study the spatial pattern and intraspecific association. The results showed that the diameter class structure of Q. aliena var. acutiserrata was bimodal, with a large proportion of young trees (1 cm≤DBHï¼5 cm), indicating an increase population structure with good capability of regeneration. The abundance of middle trees (15 cm≤DBHï¼25 cm) was slightly more than that of big trees (25 cm≤DBHï¼35 cm) and old trees (DBH≥35 cm), but far less than that of young trees and small trees. The spatial distribution of Q. aliena var. acuteserrata was obviously altitude dependent, which mainly distributed in the middle and high altitude areas. Results of complete spatial randomness (CSR) model analysis showed that young trees, small trees, adult trees, big trees, and old trees were aggregated in the large scale (ï¼60 m). Heterogeneous Poisson (HP) model was used to eliminate habitat heterogeneity. The results of HP model showed that the individual aggregation degree of each diameter class decreased, indicating that the distribution was affected by habitat heterogeneity. At the small scale (ï¼40 m), spatial correlation was positively correlated between individuals with small diameter gap, whereas the spatial correlation was negative correlation and no correlation between individuals with large diameter gap. At large scale (>40 m), the spatial correlation was positively correlated between large-diameter individuals, but negatively correlated and unrelated between saplings and other diameter individuals. Our results indicated that biological cha-racteristics of Q. aliena var. acutiserrata and habitat heterogeneity were important drivers for the formation of population spatial pattern.
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Quercus , China , Ecosistema , Bosques , Humanos , ÁrbolesRESUMEN
Fatty acid biosynthesis is essential for bacterial survival. Of these promising targets, ß-ketoacyl-acyl carrier protein (ACP) synthase III (FabH) is the most attractive target. FabH would trigger the initiation of fatty acid biosynthesis and it is highly conserved among Gram-positive and -negative bacteria. A series of novel amide derivatives bearing dioxygenated rings were synthesized and developed as potent inhibitors of FabH. These compounds were determined by 1H-NMR, 13C-NMR, MS and further confirmed by crystallographic diffraction study for compound 19. Furthermore, these compounds were evaluated strong broad-spectrum antibacterial activity. Some compounds with potent antibacterial activities were tested for their Escherichia coli (E. coli) FabH inhibitory activity. Especially, compound 19 showed the most potent antibacterial activity with minimum inhibitory concentration (MIC) values of 1.56-3.13 mg/mL against the tested bacterial strains and exhibited the most potent E. coli FabH inhibitory activity with IC50 of 2.4 µM. Docking simulation was performed to position compound 19 into the E. coli FabH active site to determine the probable binding conformation.
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3-Oxoacil-(Proteína Transportadora de Acil) Sintasa , Proteínas de Escherichia coli , Amidas , Antibacterianos/química , Bacterias/metabolismo , Inhibidores Enzimáticos/química , Escherichia coli , Proteínas de Escherichia coli/metabolismo , Ácidos Grasos , Transferasas (Grupos de Otros Fosfatos Sustitutos)RESUMEN
OBJECTIVE: To observe the effect of electroacupuncture(EA) on the expression of nuclear transcription factors κB (NF-κB) and Tau protein and content of amyloid (Aß) in diabetic rats with cognitive impairment, so as to explore its mechanism underlying improvement of learning-memory ability. METHODS: Male SD rats were randomly divided into normal control (n=9), model (n=9) and EA (n=9) groups. The diabetic mellitus model was established by feeding the rats with high fat and high sugar for 1 month and intraperitoneal injection of STZ (25 mg·kg-1·d-1) for 2 days. EA was applied to "Zusanli"(ST36) and "Neiting"(ST44) for 20 min, alternatively on both side every day, and "Yishu"(EX-B3) was stimulated by twirling the acupuncture needle with uniform reinforcing-reducing method for 1 min, followed by retaining it for 20 min. The treatment was conducted 6 times a week for 4 weeks. The learning-memory ability was evaluated by using Morris water maze swimming test. The blood glucose level was randomly detected by using a glucometer, the content of Aß1-42 in the hippocampal tissue was detected by ELISA, and the relative expression levels of hippocampal Tau and NF-κB p65 proteins and mRNAs were determined by Western blot and fluorescence quantitative real-time PCR, separately. RESULTS: After modeling, the blood glucose, escape latency, Aß1-42 content and the expression levels of Tau and NF-κB p65 proteins and mRNAs in the model group were significantly increased (P<0.01, P<0.05) in comparison with the normal control group. Following EA intervention, the modeling induced increase of blood glucose, escape latency, Aß1-42 content and the expression levels of Tau and NF-κB p65 proteins and mRNAs were reversed (P<0.05, P<0.01). CONCLUSION: EA can improve the learning-memory ability in rats with diabetic cognitive impairment, which may be related to its function in down-regulating the levels of hippocampal Aß1-42, Tau and NF-κB proteins.
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Disfunción Cognitiva , Diabetes Mellitus Experimental , Electroacupuntura , Péptidos beta-Amiloides , Animales , Glucemia/metabolismo , Disfunción Cognitiva/genética , Disfunción Cognitiva/terapia , Diabetes Mellitus Experimental/genética , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/terapia , Hipocampo/metabolismo , Masculino , Memoria , FN-kappa B/genética , FN-kappa B/metabolismo , Fragmentos de Péptidos , Ratas , Ratas Sprague-Dawley , Proteínas tau/genética , Proteínas tau/metabolismoRESUMEN
Video 1Photodynamic therapy for hepatic hilar intraductal papillary neoplasm of the bile duct: a case report.
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A new type of organocatalyzed 1,3-thiosulfonylation has been developed to straightforwardly access highly functionalized vinyl sulfones, which features mild conditions, atom- and step-economy, practicability, conciseness, and environmental friendliness. Moreover, these valuable products can be transformed to vinyl sulfides via a base-promoted isomerization. The versatile route can efficiently and rapidly introduce SCD3 groups with excellent levels of deuterium content (>99% D) by utilizing our newly developed SCD3 reagents. Gram-scale operations and further transformations are smoothly carried out, providing promising applications for drug discovery.
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Alcadienos , Sulfuros , SulfonasRESUMEN
We have established a practical and concise method for the straightforward access of a universal deuterated methylthiolating reagent through a one-pot gram-scale operation under mild conditions. This odourless electrophilic SCD3 reagent was widely applied to react with numerous representative nucleophiles and approached various valuable SCD3 analogues with excellent levels of deuterium content (>99% D). The divergent further transformations were smoothly carried out to obtain the significant derivatives with different oxidative states in high efficiency.