An unprecedented cyclization reaction of donor–acceptor oxiranes with N,N′-disubstituted thioureas to construct trans-dihydropyrimidines is presented. Preliminary reaction mechanism studies ...demonstrated that the reaction underwent sequential cycloaddition/amine ester exchange/oxygen–sulfur exchange/desulfuration/Michael addition process. A wide range of trans-dihydropyrimidines were produced with high yields up to 94% by using this method.
Fomitopsis pinicola (Sw. Ex Fr.) Krast has been commonly used as a health food source and antitumor agent. To uncover bioactive key composition of F. pinicola, in our study, we investigated the ...chemical constituents of a methanol extract of F. pinicola and thirty-five lanostane-type tritetpenoids; 13 new compounds (1–13) and twenty-two known analogues (14–35) were isolated. Among them, compounds 1–9 were C30 lanostane triterpenoids and triterpene sugar esters, while compounds 10–13 were C31 triterpenoids and triterpene sugar esters. Their structures and absolute configurations were elucidated by extensive 1D, 2D NMR, MS, and IR spectra. Furthermore, cytotoxic activities of all isolates against five human tumor cell lines (HL-60, A549, SMMC-7721, MCF-7, and SW480) were evaluated. The results showed that compounds 12, 14, 17, 18, 22, and 23 displayed cytotoxic effects against five human tumor cell lines with IC50 values ranging from 3.92–28.51 μM. Meanwhile, compounds 9 and 35 exhibited selected inhibitory activities against HL-60, SMMC-7721, and MCF-7 with IC50 values in the range of 13.57–36.01 μM. Furthermore, the flow cytometry analysis revealed that compounds 17, 22, and 35 induced apoptosis in HL-60 cell lines. Their structure–activity relationships were preliminarily reported. These findings indicate the vital role of triterpenoids and their glycosides in explaining antitumor effects of F. pinicola and provide important evidence for further development and utilization of this fungus.
Coal is a complex geological body that is composed of organic material, gas, and water. Generally, coal with high hardness is commonly considered to be a non-outburst risk; however, several coal ...mines with hard coal seams in China have experienced coal and gas outbursts. Coals with different degrees of metamorphism have different inherent moisture ranges, which has a strong influence on gas adsorption and desorption. Currently, inhomogeneous moisture wetting remains an issue in traditional preparation methods for preparing coal samples with different moisture levels. In this paper, we chose three typical hard coals with different degrees of metamorphism and systematically studied their pore structure characteristics, effect of approximate inherent moisture on the gas adsorption–desorption characteristics, and gas diffusion of hard coals. The results show that all of the coal samples have an open pore structure, but each coal sample has different development characteristics of their pore structure. The higher the moisture, the shorter the adsorption equilibrium time required and the lower pressure drop. All of the adsorption isotherm curves fit the Langmuir equation well. The gas adsorption capacity of the same coal sample decreases gradually and the amplitude of the gas adsorption capacity decreases with increasing moisture. This relationship indicates that the existence of moisture occupies a certain space of the pore structure and reduces the gas adsorption sites of coal, reducing the adsorption and desorption amount of the coal samples. Moreover, low and middle rank coal can use the bidisperse model to calculate the diffusion coefficient, while high rank coal can use the unipore model. Increasing moisture causes the macropore diffusion coefficient
D
a,e
and micropore diffusion coefficient
D
i,e
of the YZG and YJ samples to decrease. The effective diffusion coefficient
D
e
of the WLH samples also reduced gradually, which suggests that moisture has an influence on the gas migration and diffusion channels of coal, reducing the gas adsorption equilibrium time, desorption rate, and diffusion rate of coal seam.
In order to investigate the effect of internal friction of umbilical cable on its vortex-induced vibration (VIV) responses, the experimental study on VIV of bond umbilical cable (BUC) and un-bond ...umbilical cable (UBUC) was carried out in an experimental tank. A current generator in the laboratory simulated the uniform current, and the current velocities were observed in real time by using a Doppler Velocimeter. In addition, different sizes of top tension were applied to the umbilical cable model. The VIV responses of the umbilical cable model were measured by using Fiber Bragg grating (FBG) strain sensors. The displacement responses of umbilical cable model were reconstructed based on the experimental strain data processed by modal superposition method. In this paper, the traveling wave characteristics, the spatial-temporal distribution characteristics of frequency and fatigue damage of the BUC and UBUC under VIV are studied. The experimental results show that there are obvious differences between BUC and UBUC in the response characteristics of VIV. The UBUC appears the traveling wave sooner than BUC, but its standing wave characteristics are more obvious than those of BUC at high velocities. Compared with BUC, the spatial-temporal distribution of UBUC frequencies appears wide-band distribution sooner, but has narrower bandwidth in the “lock-in” state. The level of fatigue damage of BUC was approximately the same as that of UBUC.
Spermatozoa are highly specialized cells, and energy metabolism plays an important role in modulating sperm viability and function. Rosiglitazone is an antidiabetic drug in the thiazolidinedione ...class that regulates metabolic flexibility and glucose uptake in various cell types, but its effects on boar sperm metabolism are unknown. In this study, we investigated the potential effect of rosiglitazone against time‐dependent deterioration of boar spermatozoa during liquid preservation at 17°C. Freshly ejaculated semen was diluted with Beltsville Thawing Solution (BTS) containing different concentrations of rosiglitazone, and the motility, membrane and acrosome integrity of sperm were detected. Besides, we measured glucose uptake capacity, l‐lactate production level, mitochondrial membrane potential, adenosine triphosphate (ATP) content and mitochondrial reactive oxygen species (mROS) production of sperm after boar semen had been incubated with or without rosiglitazone, iodoacetate (glycolysis inhibitor) and rotenone (electron transport chain inhibitor) for 5 days. The addition of rosiglitazone significantly enhanced sperm quality and had a strong protective effect on the sperm membrane and acrosome integrity during storage. BTS containing 50 μM rosiglitazone maintained the total motility of liquid‐preserved sperm above 60% for 7 days. Rosiglitazone improved sperm quality by regulating energy metabolism manner of preserved sperm, protected the sperm mitochondrial membrane potential, enhanced sperm ATP production and in the meanwhile reduced mROS through enhancing glycolysis but not oxidative phosphorylation. The data suggested the practical feasibility of using rosiglitazone for improving boar spermatozoa quality during semen preservation.
The cellular automaton‐finite element (CAFE) model is used to simulate solidification structures of 19Cr14Mn0.9N high nitrogen steel under different solidification pressures. The effect of ...solidification pressure on model parameters is firstly investigated. After validation, this model is used to clarify the effect of solidification pressure on compactness degree with number of grains and primary dendrite arm spacing (λ1). The results show that increasing solidification pressure from 0.5 to 1.2 MPa exhibits a significant increment (200 W m2 K−1)) on heat transfer coefficient and slight change for other model parameters. The model validation indicates CAFE model can accurately simulate solidification structure under higher solidification pressure. Under higher solidification pressure, the primary dendrite arm spacing (λ1) of central equiaxed grain becomes smaller and the number of grains of the whole ingot increases obviously, revealing a further improvement on the compactness degree of ingot. At a given pressure, the decrement in the number of grains is obvious away from the edge of ingot. With increasing solidification pressure, a more significant increment in the number of grains exists at columnar grain zone than that at central equiaxed grain zone, suggesting a greater increasing tendency of compactness degree at columnar grain zone.
Based on the effect of solidification pressure on model parameters, the CAFE model is used to investigate compactness degree of 19Cr14Mn0.9N high nitrogen steel under different solidification pressures after verification. With increasing solidification pressure, the number of grain increases remarkably, revealing that compactness degree is significantly improved under higher solidification pressure.
Objective
To evaluate ITPKC and NLRP3 expression in children with Kawasaki disease (KD) and investigate the relationship between serum pro-inflammatory cytokines triggered by NLRP3 and inflammatory ...indices. Simultaneously, the methylation level in the ITPKC promoter was evaluated in children with KD.
Methods
Children who satisfied the American Heart Association diagnostic criteria for KD were enrolled in the study from August 2018 to January 2019. The levels of ITPKC, NLRP3, IL-1β, and IL-18 were measured. The effect of DNA methylation on the activity of the ITPKC promoter was observed. Methylation-specific PCR was used to verify methylation modification of the ITPKC promoter region in children with KD.
Results
ITPKC expression was downregulated in patients with KD, whereas NLRP3 was upregulated. Expression of the downstream cytokine, IL-18, was significantly upregulated in children with KD and correlated positively with inflammatory indices. Modifying DNA methylation significantly decreased the luciferase activity of the plasmid containing the ITPKC promoter region and thus, may inhibit ITPKC gene promoter activity. Furthermore, methylation modification was observed in the ITPKC promoter region of children with KD.
Conclusion
Modification of DNA methylation inhibits ITPKC promoter activity and is involved in NLRP3 inflammasome activation in children with KD.
Background, Aim and Scope The impact of air pollution on school children's health is currently one of the key foci of international and national agencies. Of particular concern are ultrafine ...particles which are emitted in large quantities, contain large concentrations of toxins and are deposited deeply in the respiratory tract. Materials and methods In this study, an intensive sampling campaign of indoor and outdoor airborne particulate matter was carried out in a primary school in February 2006 to investigate indoor and outdoor particle number (PN) and mass concentrations (PM₂.₅), and particle size distribution, and to evaluate the influence of outdoor air pollution on the indoor air. Results For outdoor PN and PM₂.₅, early morning and late afternoon peaks were observed on weekdays, which are consistent with traffic rush hours, indicating the predominant effect of vehicular emissions. However, the temporal variations of outdoor PM₂.₅ and PN concentrations occasionally showed extremely high peaks, mainly due to human activities such as cigarette smoking and the operation of mower near the sampling site. The indoor PM₂.₅ level was mainly affected by the outdoor PM₂.₅ (r = 0.68, p < 0.01), whereas the indoor PN concentration had some association with outdoor PN values (r = 0.66, p < 0.01) even though the indoor PN concentration was occasionally influenced by indoor sources, such as cooking, cleaning and floor polishing activities. Correlation analysis indicated that the outdoor PM₂.₅ was inversely correlated with the indoor to outdoor PM₂.₅ ratio (I/O ratio; r = −0.49, p < 0.01), while the indoor PN had a weak correlation with the I/O ratio for PN (r = 0.34, p < 0.01). Discussion and conclusions The results showed that occupancy did not cause any major changes to the modal structure of particle number and size distribution, even though the I/O ratio was different for different size classes. The I/O curves had a maximum value for particles with diameters of 100-400 nm under both occupied and unoccupied scenarios, whereas no significant difference in I/O ratio for PM₂.₅ was observed between occupied and unoccupied conditions. Inspection of the size-resolved I/O ratios in the preschool centre and the classroom suggested that the I/O ratio in the preschool centre was the highest for accumulation mode particles at 600 nm after school hours, whereas the average I/O ratios of both nucleation mode and accumulation mode particles in the classroom were much lower than those of Aitken mode particles. Recommendations and perspectives The findings obtained in this study are useful for epidemiological studies to estimate the total personal exposure of children, and to develop appropriate control strategies for minimising the adverse health effects on school children.
An experimental investigation on the disturbance effect of jet-type active vibration suppression device on vortex-induced vibration of deep-sea riser was carried out in the wave-flow combined flume. ...The vibration suppression device was designed in which the jet pipe was horizontally fixed to the front end of the riser. By varying three different excitation spacings and multi-stage outflow velocities, the influence law of the dominant frequency, dimensionless displacement and other dynamic response parameters was studied under different excitation spacings, and the mechanism and sensitive characteristics of the disturbance suppression were explored. The results indicate that the variation of excitation spacing makes gas curtain enter the strong disturbed flow region at different velocities and angles, and the coupling relationship between excitation spacing and reduced velocity is the key factor to enter the strong disturbed flow region to achieve the optimal disturbance suppression. In the strong disturbed flow region, the influence of gas curtain on the dominant frequency is obviously affected by the flow velocity, while the vibration displacement is stable at the same amplitude and is weakly affected by the flow velocity. Gas curtain can effectively disturb the formation of vortex shedding, destroy the strong nonlinear coupled vibration of the riser, and achieve better vibration suppression effect. In the weak disturbed flow region, the vortex length of the riser tail is prolonged, the strong nonlinear coupled vibration of the riser is gradually restored, and the vibration suppression effect of the device gradually decreases.
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