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In this report, we present a photocatalytic ring-opening fluorosulfonylation of strained cycloalkanols with sulfur dioxide and NFSI under mild conditions for the synthesis of carbonyl-containing aliphatic sulfonyl fluorides. The synthetic potential of the carbonyl-containing aliphatic sulfonyl fluoride products has been examined by diverse transformations, including SuFEx reactions and Baeyer-Villiger oxidation reactions. Mechanistic studies demonstrate that the reaction operates through a radical C-C bond cleavage/SO2 insertion/fluorination cascade process.
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An efficient aminofluorosulfonylation strategy was developed for the synthesis of various pyrazoline-functionalized aliphatic sulfonyl fluorides using ß,γ-unsaturated hydrazones with sulfur dioxide and NFSI as the starting materials under mild conditions. The sulfonyl fluoride products could be successfully transformed into the corresponding sulfonate esters and amides via the sulfur(VI) fluoride exchange (SuFEx) click reactions. Preliminary mechanistic investigations demonstrate that the reaction operates through a radical cyclization/SO2 insertion/fluorination cascade process.
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We present a facile switchable regioselective 7-endo or 6-exo iodocyclization of O-homoallyl benzimidates here, which affords various iodo-substituted 1,3-oxazines and tetrahydro-1,3-oxazepines in a controllable manner. The products can further undergo substitution reactions to afford a series of rich functionalized target heterocyclic molecules. The developed protocol has the advantages of mild conditions, simple operation, and excellent functional group compatibility.
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Our previous study revealed that the bone anabolic effects of the lignan-rich fraction (SWCA) from Sambucus williamsii Hance was involved in modulating the metabolism of tryptophan in vivo and inhibiting serotonin (5-HT) synthesis in vitro. This study aimed to determine how SWCA modulates bone metabolism via serotonin in vivo. The effects of SWCA were evaluated by using 4-month-old Sprague-Dawley (SD) ovariectomized rats. The serum levels of 5-HT and kynurenine, the protein expressions of tryptophan hydroxylase 1 (TPH-1) and TPH-2, the genes and proteins related to the 5-HT signaling pathway as well as gut microbiota composition were determined. SWCA treatment alleviated bone loss and decreased serum levels of serotonin, which was negatively related to bone mineral density (BMD) in rats. It suppressed the protein expression of TPH-1 in the colon, and reversed the gene and protein expressions of FOXO1 and ATF4 in the femur in OVX rats, while it did not affect the TPH-2 protein expression in the cortex. SWCA treatment escalated the relative abundance of Antinobacteria and modulated several genera relating to BMD. These findings verified that the bone protective effects of lignans were mediated by serotonin, and provided evidence that lignans might be a good source of TPH-1 inhibitors.
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Microbioma Gastrointestinal , Lignanos , Sambucus , Ratas , Animales , Serotonina , Lignanos/farmacología , Ratas Sprague-DawleyRESUMEN
Amines, especially those with multi-nitrogen moieties, are widespread in natural products and biologically active compounds. Thus, the development of direct and efficient methods to introduce multiple nitrogen-containing fragments into compounds in one step is highly desirable yet challenging. Herein, we report an NIS-promoted selective amino-diazidation and amino-iodoazidation of O-homoallyl benzimidates with NaN3. By using this protocol, a variety of vicinal diazido-substituted 1,3-oxazines and vicinal iodoazido-substituted 1,3-oxazines were directly synthesized in a controllable manner. Preliminary mechanistic investigations revealed that the reaction operates through a NIS-promoted four-step cascade process. The developed method has the merits of metal-free, excellent functional group compatibility, simple operation, and mild conditions.
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Aminas , Oxazinas , NitrógenoRESUMEN
Meteorological factors have been confirmed to affect the COVID-19 transmission, but current studied conclusions varied greatly. The underlying causes of the variance remain unclear. Here, we proposed two scientific questions: (1) whether meteorological factors have a consistent influence on virus transmission after combining all the data from the studies; (2) whether the impact of meteorological factors on the COVID-19 transmission can be influenced by season, geospatial scale and latitude. We employed a meta-analysis to address these two questions using results from 2813 published articles. Our results showed that, the influence of meteorological factors on the newly-confirmed COVID-19 cases varied greatly among existing studies, and no consistent conclusion can be drawn. After grouping outbreak time into cold and warm seasons, we found daily maximum and daily minimum temperatures have significant positive influences on the newly-confirmed COVID-19 cases in cold season, while significant negative influences in warm season. After dividing the scope of the outbreak into national and urban scales, relative humidity significantly inhibited the COVID-19 transmission at the national scale, but no effect on the urban scale. The negative impact of relative humidity, and the positive impacts of maximum temperatures and wind speed on the newly-confirmed COVID-19 cases increased with latitude. The relationship of maximum and minimum temperatures with the newly-confirmed COVID-19 cases were more susceptible to season, while relative humidity's relationship was more affected by latitude and geospatial scale. Our results suggested that relationship between meteorological factors and the COVID-19 transmission can be affected by season, geospatial scale and latitude. A rise in temperature would promote virus transmission in cold seasons. We suggested that the formulation and implementation of epidemic prevention and control should mainly refer to studies at the urban scale. The control measures should be developed according to local meteorological properties for individual city.
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COVID-19 , COVID-19/epidemiología , Humanos , Conceptos Meteorológicos , SARS-CoV-2 , Estaciones del Año , TemperaturaRESUMEN
The hydrodynamics and environmental factors in the Xiangxi River (XXR) and Shennong River (SNR), which are tributaries of the Three Gorges Reservoir (TGR), were monitored from July to August (the low water level period) and in October (the impoundment period) in 2018. The vertical distribution characteristics of chlorophyll a and other indicators of the two tributaries were analyzed during the different operation periods, and the factors that affected the vertical distribution in each period were discussed. The results showed that the vertical distribution of dissolved oxygen, water temperature, pH value, and chlorophyll a of the XXR and SNR during the low water level period was relatively consistent. The indexes 0-10 m (0-5 m for chlorophyll a) from the surface of the XXR and SNR, respectively, showed significant stratification and decreased with increasing water depth; the stability index of thermal stratification (RWCS/H) was 13.71-29.07 m-1, which was stable. After the water depth reached 10 m (5 m for chlorophyll a), the indexes tended to be stable along the water depth. During the impoundment period, there was no obvious stratification for each index; the stability index of thermal stratification was 0-0.5 m-1, the stability of the water body was weak, and the vertical variation of each index was relatively stable. The comprehensive trophic state index (TLI) of the XXR and SNR were 55 and 53 during the low water level period, respectively, indicating that they were in a slightly eutrophic state, and 39 and 46 during the impoundment period, respectively, indicating a mesotrophic state. Linear regression analysis showed that chlorophyll a, dissolved oxygen, water temperature, and pH in the two tributaries were significantly correlated in the vertical direction in the low water level period, indicating that dissolved oxygen, water temperature stratification, and pH were important factors affecting the vertical distribution of chlorophyll a. During the impoundment period, a large amount of backflow from the Yangtze River, a large fluctuation in tributary water level, and the decrease in RWCS/H were the important factors that affected the small vertical change in the water body. The enhancement of vertical mixing and the decrease in Zeu/Zmix were the key factors affecting the nutritional status of the water.
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Ríos , Contaminantes Químicos del Agua , China , Clorofila/análisis , Clorofila A , Monitoreo del Ambiente , Agua , Contaminantes Químicos del Agua/análisisRESUMEN
Premature ovarian failure (POF) is defined as deployment of amenorrhea due to the cessation of ovarian function in a woman younger than 40 years old. The pathologic mechanism of POF is not yet well understood, although genetic aberrations, autoimmune damage, and environmental factors have been identified. The current study demonstrated that NF-κB inactivation is closely associated with the development of POF based on the data from literature and cyclophosphamide (Cytoxan)-induced POF mouse model. In the successfully established NF-κB-inactivated mouse model, the results showed the reduced expression of nuclear p65 and the increased expression of IκBα in ovarian granulosa cells; the reduced numbers of antral follicles; the reduction of Ki-67/proliferating cell nuclear antigen-labeled cell proliferation and enhanced Fas/FasL-dependent apoptosis in granulosa cells; the reduced level of E2 and anti-Müllerian hormone; the decreased expression of follicle-stimulating hormone receptor and cytochrome P450 family 19 subfamily A member 1 (CYP19A1) in granulosa cells, which was reversed in the context of blocking NF-κB signaling with BAY 11-7082; and the decreased expressions of glucose-regulated protein 78 (GRP78), activating transcription factor 6, protein kinase R-like endoplasmic reticulum kinase, and inositol-requiring enzyme 1 in granulosa cells. Dual-luciferase reporter assay demonstrated that p50 stimulated the transcription of GRP78, and NF-κB affected the expression of follicle-stimulating hormone receptor and promoted granulosa cell proliferation through GRP78-mediated endoplasmic reticulum stress. Taken together, these data indicate, for the first time, that the inactivation of NF-κB signaling plays an important role in POF.
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FN-kappa B , Insuficiencia Ovárica Primaria , Animales , Apoptosis , Femenino , Células de la Granulosa/metabolismo , Células de la Granulosa/patología , Humanos , Ratones , FN-kappa B/metabolismo , Folículo Ovárico/metabolismo , Insuficiencia Ovárica Primaria/metabolismo , Insuficiencia Ovárica Primaria/patología , Receptores de HFE/metabolismoRESUMEN
A 33-year-old woman of giant broad ligament leiomyoma with myxoid degeneration was misdiagnosed as ovarian tumor. The patient underwent a transabdominal myomectomy and developed a pelvic infection after operation diagnosed with contrast-enhanced ultrasound. She was cured and ultimately discharged after symptomatic treatment. Only 21 cases of giant broad ligament leiomyomas with a diameter larger than 12 cm were included. The present systematic review aimed to increase awareness of the clinical characteristics and treatment methods of giant broad ligament leiomyoma, and reduce the rates of misdiagnosis and postoperative complications.
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Ligamento Ancho , Leiomioma , Neoplasias Uterinas , Adulto , Ligamento Ancho/diagnóstico por imagen , Ligamento Ancho/cirugía , Diagnóstico Diferencial , Femenino , Humanos , Leiomioma/diagnóstico por imagen , Leiomioma/cirugía , Complicaciones Posoperatorias/diagnóstico por imagen , Neoplasias Uterinas/diagnóstico por imagen , Neoplasias Uterinas/cirugíaRESUMEN
A practical electrophilic aminoselenation of O-homoallyl benzimidate with diselenides promoted by PhICl2/Cu2O has been developed. The easily available and stable diselenides were used as selenium sources. Various selenyl 1,3-oxazines, which are important frameworks in medicinal and biological chemistry, were easily obtained in moderate to good yields for the first time. Easy scaleup and scalability make this method attractive for the preparation of other valuable organoselenides.
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Crude oil may block soil pores, affect soil water repellency, and change soil water movement. In this study, soil column simulation was used to study the effects of different crude oil pollution levels (0, 0.5%, 1%, 2%, 4%) on the water infiltration processes in loessial soil and aeolian sandy soil. The results showed that soil wetting front speed and infiltration rate of those two soils decreased with increasing crude oil content. The time needed for wetting front reaching the bottom of the soil column was the longest under 4% crude oil polluted soil, which was 4 times and 48 times longer than that of no crude oil polluted soil for loessial soil and aeolian sandy soil, respectively. The cumulative infiltration of loessial soil decreased with increasing crude oil content, while it increased to the max and then decreased as the crude oil content increased in aeolian sandy soil. The cumulative infiltration curves of aeolian sandy soil with high crude oil contents (2% and 4%) presented "up-tail" phenomenon. Kostiakov infiltration model and Philip infiltration model could better fit the infiltration process than Green-Ampt model for loessial soil with different crude oil content. However, the two models could only well fit the infiltration process for aeolian sandy soil with low crude oil content (0, 0.5%, 1%). Crude oil pollution could significantly affect soil water infiltration process, especiall in aeolian sandy soil.
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Contaminación por Petróleo , Petróleo , Contaminantes del Suelo , Arena , Suelo , Contaminantes del Suelo/análisisRESUMEN
A facile copper-catalyzed aminosulfonylation of O-homoallyl benzimidates with sodium sulfinates in the presence of tert-butyl peroxybenzoate (TBPB) and XPhos ligand has been developed. By using this protocol, a variety of potentially bioactive 1,3-oxazines were directly synthesized. This method has the merits of a cheap catalyst, easily available and stable sulfone reagents, and simple operation.
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A comparative analysis of phosphate occurrence and its genesis during different dispatching periods of representative level I tributaries of the Three Gorges Reservoir was conducted. For this, water quality, hydrodynamic force, and environmental data were examined for backwater areas of the Xiangxi River and Shennong River during the low-water-level period (June), storage period (September) and high-water-level period (December) in 2018. The results suggest that the mass concentration of total phosphorus (TP) in the water body of the coves of Xiangxi River and Shennong River range from 0.049 mg·L-1 to 0.168 mg·L-1 and 0.059 mg·L-1 to 0.152 mg·L-1, respectively, surpassing the 0.02 mg·L-1 threshold for algal blooms. The mass concentration of TP, DP (orthophosphate), and PP (particulate phosphorus) in the coves of the tributaries were ranked as follows:storage period > high-water-level period > low-water-level period for TP; storage period > low-water-level period > high-water-level period for DP; low-water-level period > high-water-level period > storage period for PP. Based on Pearson's correlation coefficients, TP and DP were significantly correlated as well as temperature and pH, which are the key factors influencing the phosphorus in soils and sediments in the water-level-fluctuation zone. During the low-water-level and high-water-level periods of the Three Gorges Reservoir, the TP in the coves of the tributaries mainly exists as PP, accounting for more than 75% and 60%, respectively. The flow in the coves of the tributaries slows during storage periods, meaning that settlement of PP is enhanced, changing the dominance of TP to dissolved total phosphorus (DTP).
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OBJECTIVES: An artificial intelligence model was adopted to identify mild COVID-19 pneumonia from computed tomography (CT) volumes, and its diagnostic performance was then evaluated. METHODS: In this retrospective multicenter study, an atrous convolution-based deep learning model was established for the computer-assisted diagnosis of mild COVID-19 pneumonia. The dataset included 2087 chest CT exams collected from four hospitals between 1 January 2019 and 31 May 2020. The true positive rate, true negative rate, receiver operating characteristic curve, area under the curve (AUC) and convolutional feature map were used to evaluate the model. RESULTS: The proposed deep learning model was trained on 1538 patients and tested on an independent testing cohort of 549 patients. The overall sensitivity was 91.5% (195/213; p < 0.001, 95% CI: 89.2-93.9%), the overall specificity was 90.5% (304/336; p < 0.001, 95% CI: 88.0-92.9%) and the general AUC value was 0.955 (p < 0.001). CONCLUSIONS: A deep learning model can accurately detect COVID-19 and serve as an important supplement to the COVID-19 reverse transcription-polymerase chain reaction (RT-PCR) test. KEY POINTS: ⢠The implementation of a deep learning model to identify mild COVID-19 pneumonia was confirmed to be effective and feasible. ⢠The strategy of using a binary code instead of the region of interest label to identify mild COVID-19 pneumonia was verified. ⢠This AI model can assist in the early screening of COVID-19 without interfering with normal clinical examinations.
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COVID-19 , Aprendizaje Profundo , Inteligencia Artificial , Humanos , Estudios Retrospectivos , SARS-CoV-2 , Tomografía Computarizada por Rayos XRESUMEN
Menopausal women are susceptible to have high risk of cardiovascular diseases, type II diabetes and osteoporosis due to the metabolic disorder caused by estrogen deficiency. Accumulating evidence supports that gut microbiota is a key regulator of metabolic diseases. Our previous metabolomics study interestingly demonstrated that the anti-osteoporotic effects of lignan-rich fraction (SWCA) from Sambucus wialliamsii Hance were related to the restoration of a series of lipid and glucose metabolites. This study aims to investigate how SWCA modulates lipid and glucose metabolism and the underlying mechanism. Our results show that oral administration of SWCA (140 mg/kg and 280 mg/kg) for 10 weeks alleviated dyslipidemia, improved liver functions, prevented glucose tolerance and insulin actions, attenuated system inflammation and improved intestinal barrier in OVX rats. It also induced a high abundance of Actinobacteria, and restored microbial composition. We are the first to report the protective effects of the lignan-rich fraction from S. williamsii on dyslipidemia and insulin resistance. Our findings provide strong evidence for the application of this lignan-rich fraction to treat menopausal lipid disorder and insulin resistance-related diseases.
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Dislipidemias/tratamiento farmacológico , Microbioma Gastrointestinal/efectos de los fármacos , Hipolipemiantes/farmacología , Resistencia a la Insulina , Lignanos/farmacología , Sambucus/química , Administración Oral , Animales , Citocinas/metabolismo , Femenino , Glucosa/metabolismo , Prueba de Tolerancia a la Glucosa , Hígado/efectos de los fármacos , Ovariectomía , Extractos Vegetales/farmacología , Tallos de la Planta/química , Ratas , Ratas Sprague-DawleyRESUMEN
Remitting seronegative symmetrical synovitis with pitting edema(RS3PE),the inflammatory arthritis attacking mainly elderly males,is characterized by symmetrical synovitis with pitting edema of the dorsum of hands and feet and the absence of rheumatoid factor.RS3PE commonly accompanies malignant tumor,infections and other diseases.Here we report a case of RS3PE associated with lung malignancy and review other six cases to summarize the clinical features,treatment and prognosis.
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Neoplasias Pulmonares , Sinovitis , Anciano , Edema/etiología , Humanos , Neoplasias Pulmonares/complicaciones , Masculino , Síndrome , Sinovitis/complicaciones , Sinovitis/tratamiento farmacológicoRESUMEN
[This corrects the article DOI: 10.7150/ijbs.7723.].
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A highly efficient electrophilic oxyselenation of propargylic amines with diselenides and CO2 under atmospheric pressure promoted by copper/DTBP is reported. Various biologically important selenyl 2-oxazolidinones were produced in moderate to excellent yields. The developed method features a broad substrate scope, easy scalability, and mild reaction conditions.
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The water quality of the backwater areas in the Xiangxi River and Shennong River, which are typical tributaries of the Three Gorges Reservoir, was monitored in September 2018. The vertical distribution characteristics of dissolved oxygen, chlorophyll a, and other indicators in the two rivers were analyzed and compared, and the environmental factors affecting their vertical distribution were discussed. The results showed that the dissolved oxygen concentration 0-10 m and 0-12 m from the surface of the Xiangxi River and Shennong River, respectively, showed significant stratification and decreased with increasing water depth. The dissolved oxygen saturation of surface water was 139.20% and 107.78%, respectively, reaching a state of supersaturation (SDO>100%).The dissolved oxygen concentration in the middle and bottom water was more stable without stratification. The vertical distribution characteristics of chlorophyll a were consistent with those of dissolved oxygen in the Xiangxi River and Shennong River, and the chlorophyll a concentration in the surface water showed moderate eutrophication (5µg·L-1 < Chl-a < 20 µg·L-1). According to Pearson correlation analysis, the vertical distribution of dissolved oxygen in the Xiangxi River and Shennong River was significantly correlated with that of water temperature and phytoplankton. The stratification of water temperature and the life activities of phytoplankton were the key factors affecting the vertical distribution of dissolved oxygen. Chlorophyll a was positively correlated with water temperature and pH, and negatively correlated with turbidity, indicating that the vertical distribution of phytoplankton was mainly affected by the attenuation of light intensity along the water depth and the stratification of water temperature.
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A dearomative tandem spiro-cyclization reaction of N-[(1H-indol-3-yl)methyl]methacrylamide derivatives with sulfinate sodium in the presence of AgNO3 and K2CO3 is reported, which produced sulfonylated spiro[indole-3,3'-pyrrolidines] in medium to excellent yields. The characteristics of this transformation contain good functional group tolerance and ease of operation.