Discovery of novel 2-(trifluoromethyl)quinolin-4-amine derivatives as potent antitumor agents with microtubule polymerization inhibitory activity.

In this work, a series of 2-(trifluoromethyl)quinolin-4-amine derivatives were designed and synthesized through structural optimization strategy as a microtubule-targeted agents (MTAs) and their cytotoxicity activity against PC3, K562 and HeLa cell lines were evaluated. The half maximal inhibitory concentration (IC50) of 5e, 5f, and 5o suggested that their potency of anti-proliferative activities against HeLa cell lines were better than the combretastatin A-4. Compound 5e showed the higher anti-proliferative activity against PC3, K562 and HeLa in vitro with IC50 values of 0.49 µM, 0.08 µM and 0.01 µM, respectively. Further mechanism study indicated that the representative compound 5e was new class of tubulin inhibitors by EBI competition assay and tubulin polymerization assays, it is similar to colchicine. Immunofluorescence staining revealed that compound 5e apparently disrupted tubulin network in HeLa cells, and compound 5e arrested HeLa cells at the G2/M phase and induced cells apoptosis in a dose-dependent manner. Molecular docking results illustrated that the hydrogen bonds of represented compounds reinforced the interactions in the pocket of colchicine binding site. Preliminary results suggested that 5e deserves further research as a promising tubulin inhibitor for the development of anticancer agents.

Ultra-thin and broadband tunable metamaterial graphene absorber.

A broadband tunable metamaterial graphene absorber is investigated in this paper. The unit cell of the proposed metamaterial graphene absorber is composed of four patch resonators. By tuning the chemical potential of graphene and the geometric size of each patch, the simulated total reflectivity is less than -10 dB from 22.02 to 36.61 THz and with the total thickness of 0.76 um (only 0.09λ at the lowest frequency). The analysis of the surface current, magnetic field and power flow distributions has been performed to better understand the absorption mechanism. Moreover, this proposed absorber achieves its bandwidth tunable characteristics through a voltage biasing of the graphene's Fremi level. This proposed metamaterial graphene absorber (MGA) could be used as smart absorbers, photovoltaic devices and tunable sensors.

[Determination and Traceability Analysis of Phthalic Acid Esters in Garlic (Allium stivum L.) from Jiangsu Province, China].

Phthalic acid esters (PAEs) are ubiquitous environmental pollutants and are recognized as a threat to the environment and agricultural product safety across the world. In order to investigate the level of PAEs in garlic, soils, and agricultural films from Pizhou City, Jiangsu province, China, 11 garlic samples, 106 soil samples, and 4 agricultural film samples were collected and analyzed using GC-MS. In addition, the uptake and transport characteristics of six PAEs compounds classified as priority pollutants by the United States Environmental Protection Agency (EPA) in the garlic cultivar Daqingke were investigated under hydroponic conditions. The results indicated that dibutyl phthalate (DBP) and di-(2-ethylhexyl) phthalate (DEHP) were the dominant PAEs species in garlic cloves of the different garlic varieties from Pizhou City. The average contents of DBP and DEHP in garlic cloves were 0.611 mg·kg-1 and 0.167 mg·kg-1, respectively, which were significantly higher than those of the commercial varieties of garlic. The concentrations of DBP and DEHP differed in three tissues of garlic bulbs, ordered as the skin of garlic bulb>skin of garlic clove>garlic clove. Dimethyl phthalate (DMP), diethyl phthalate (DEP), diisobutyl phthalate (DIBP), DBP, and DEHP were the main PAEs species and were detected in all the surface soils collected from Pizhou City. Compared with the soil allowable concentrations of the six PAEs in the United States, the DMP and DBP concentrations in approximately 100% and 63.2% of soil samples exceeded the recommended allowable concentrations set by the EPA. However, the levels of DEP, DIBP, and DEHP in the soils were below the maximum allowable concentrations set by the EPA. Nevertheless, the average content of DEHP in soils was 486 µg·kg-1 and was found to be much higher than that in the other four PAEs. Six PAEs, including DMP, DEP, DIBP, DBP, butyl benzyl phthalate (BBP), and DEHP, were detected in all the agricultural film samples. Among them, the contents of DBP and DEHP in the agricultural films were the highest, accounting for 53.7%-63.2% of the total PAEs. The amount of PAEs present in the residual film was significantly lower than that in the new film, and all six PAEs were detected in garlic or soil samples, suggesting that agricultural film can be an important source of PAEs in garlic farming soils and garlic. Furthermore, the garlic plants absorbed DMP and DEP efficiently from the substrate and showed higher translocation factors (TFs) for DMP and DEP than those for DBP, BBP, DEHP, and di-n-octyl phthalate (DnOP), resulting in a higher accumulation of DMP and DEP in the over-ground parts of garlic. In contrast, DBP and BBP in roots of garlic displayed higher bioconcentration factors (57.4 and 81.5, respectively) compared to those of the other four PAEs, whereas the TFs of DBP and BBP were lower; this may have contributed to the high accumulation of DBP in garlic bulbs. The BCFs and TFs of DEHP and DnOP in garlic were relatively lower, but the DEHP had been detected in all garlic cloves, which may be a result of the higher DEHP contents in soils.

[Expression of Ikaros and FUT4 in Children's Acute Lymphoblastic Leukemia and Their Relationship].

OBJECTIVE: To explore the possible molecular mechanism of Ikaros regulation on FUT4 expression by analyzing the correlation of the functional state of Ikaros with level of FUT4 expression, so as to provide the theoretical basis for personalized treatment in children with ALL. METHODS: The subtypes of Ikaros were identified by nested PCR and sequencing. The expression level of FUT4 was detected by quantitative PCR and analyzed by ΔΔCt method in the early stage of treatment, remission and relapse of ALL. RESULTS: Ik1 and Ik2 were the main functional subtypes, and the dominant negative Ikaros was Ik6; the Ik6 was detected in 23 patients with ALL. It was found that 2.73% patients expressing Ik6 alone and 18.18% patients with heterozygous expression were detected. The expression of FUT4 in the newly diagnosed ALL was higher than that in the control group, and the functional Ikaros negatively correlated with the FUT4 expression(r=-0.6329). CONCLUSION: Dominant negative Ikaros closely correlated with the relapse of acute lymphoblastic leukemia in children. The functional Ikaros negatively correlated with FUT4 expression. Ikaros inhibit the transcriptional activity of FUT4, that may be the molecular mechanism of Ikaros regulating the expression of FUT4.

A new strategy for urinary sediment segmentation based on wavelet, morphology and combination method.

This paper presents a strategy for segmenting urinary sediment based on wavelet, morphology and combination method. Firstly, the wavelet transforms and morphology are used to get rid of the effect of the defocusing and get the subimages that include the particles. Then based on the characteristics of the subimages, edge detection and adaptive thresholding are employed adaptively. Finally, a simplified watershed algorithm for the overlapping particles is used. The experiment results show that the method can segment the defocusing urinary sediment images effectively and precisely.

[The hardware design of a portable gastrointestinal wireless endoscope image receiver].

The portable gastrointestinal wireless endoscope image receiver is developed and based on TMS320C6211 DSP. It can receive and demodulate the modulated signal which is transmitted from the camera-capsule, and then output the video signal. The synchronizing signals offered by SAA7114H are made best of and are used to design the time logic circuit. The fitful video signal can be collected under the control of the time logic circuit. The circuit can automatically get rid of useless blank data and only collect effective and good-quality video signals, and storage them in CF card. In addition, the image signal can be processed and compressed by DSP, and thus the data storage space and the data- analyzing time can be saved.

[Seasonal differences in the leaf hydraulic conductance of mature Acacia mangium in response to its leaf water use and photosynthesis].

In this study, measurements were made on the leaf water potential (psi1), stomatal conductance (g(s)), transpiration rate, leaf area index, and sapwood area of mature Acacia mangium, aimed to understand the relationships of the leaf hydraulic conductance (K1) with the leaf water use and photosynthetic characteristics of the A. mangium in wet season (May) and dry season (November). The ratio of sapwood area to leaf area (A(sp)/A(cl)) of the larger trees with an average height of 20 m and a diameter at breast height (DBH) of 0.26 m was 8.5% higher than that of the smaller trees with an average height of 14.5 m and a DBH of 0.19 m, suggesting that the larger trees had a higher water flux in their leaf xylem, which facilitated the water use of canopy leaf. The analysis on the vulnerability curve of the xylem showed that when the K1 decreased by 50%, the psi1 in wet season and dry season was -1.41 and -1.55 MPa, respectively, and the vulnerability of the xylem cavitation was higher in dry season than in wet season. The K1 peak value in wet season and dry season was 5.5 and 4.5 mmol x m(-2) x s(-1) x MPa(-1), and the maximum transpiration rate (T(r max)) was 3.6 and 1.8 mmol x m(-2) x s(-1), respectively. Both the K1 and T(r max), were obviously higher in wet season than in dry season. Within a day, the K1 and T(r), fluctuated many times, reflecting the reciprocated cycle of the xylem cavitation and refilling. The leaf stomatal closure occurred when the K1 declined over 50% or the psi1 reached -1.6 MPa. The g(s) would be maintained at a high level till the K1 declined over 50%. The correlation between the hydraulic conductance and photosynthetic rate was more significant in dry season than in wet season. The loss of leaf hydraulic conductance induced by seasonal change could be the causes of the decrease of T(r) and CO2 gas exchange.

[Application of thermal dissipation probe in the study of Bambusa chungii sap flow].

Based on the validation of Granier's empirical formula for calculating tree stem sap flux density, a comparative study was conducted on the measurement of Bambusa chungi sap flow by using different lengths of thermal dissipation probe (TDP), aimed to approach the applicability of TDP in measuring the sap flow of B. chungii. The difference in the daily change of the sap flow between B. chungii and nearby growing Schima superb was also analyzed. Because of the thinner bamboo wall and the heterogeneous anatomy, the sap flux density of B. chungii measured by 10 mm long probe could be underestimated, but that measured by 8 and 5 mm long probes could be relatively accurate. The comparison of the sap flow between B. chungii and nearby growing S. superba revealed that both the mean sap flux density and its daily change pattern' s skewness of B. chungii were higher than those of S. superba, but the nighttime sap flow of B. chungii was less than that of S. superba, indicating that the water recharge of B. chungii during nighttime was less active than that of S. superba. It was suggested that using TDP to investigate the sap flow of bamboo would be feasible, but careful calibration would be required before the TDP was put into application on different bamboo species.

[Water recharge through nighttime stem sap flow of Schima superba in Guangzhou region of Guangdong Province, South China: affecting factors and contribution to transpiration].

To understand the nighttime water recharge of tree through its sap flow is beneficial to the precise estimation of total transpiration and canopy stomatal conductance, and to the further understanding of the time lag between canopy transpiration and stem sap flow. By using Granier's thermal dissipation probe, this paper measured the stem sap flow of Schima superba, and synchronously measured the main environmental factors including air temperature, relative humidity, photosynthetically active radiation, and soil moisture content, and also analyzed the water recharge through nighttime stem flow of S. superba at daily and seasonal scales. The sap flow density of S. superba was lower at night than at daytime, and the nighttime sap flow density had a larger variation in dry season than in wet season. The water recharge at night generally started from sunset when radiation was approaching zero, and lasted up to midnight (18:00-22:00). No significant difference was observed in the nighttime water recharge among seasons, and no significant correlations were found between the nighttime water recharge and environmental factors, but the nighttime water recharge was well regressed with the diameter at breast height, tree height, tree canopy size, stem biomass, and canopy biomass, suggesting that tree form features and biomass could better explain the nighttime water recharge. The contribution of nighttime water recharge to the total transpiration varied significantly with seasons, and was obviously higher in dry season than in wet season.

[Effects of tree diameter at breast height and soil moisture on transpiration of Schima superba based on sap flow pattern and normalization].

The eigenvalues of continuous sap flow pattern, i. e. , skewness and kurtosis, were used to investigate the water usage of Schima superba with different diameter at breast height (DBH), and the method of normalization was firstly applied to eliminate the effects of strong affecting factor (photosynthetic active radiation, PAR) to explore the possible relationship between weak affecting factor (soil moisture) and sap flow. Generally, the trees with larger DBH had smaller skewness of sap flux density and later-appeared but larger peak values, suggesting that much more water was transpired, and the larger trees showed smaller skewness and later-appeared larger peak values in wet season than in dry season, suggesting that more water was transpired in wet season. On the other hand, smaller trees had lesser differences in the skewness between dry and wet seasons, suggesting that there was no significant difference in the transpiration between the two seasons. The relationship between individual tree's transpiration and soil moisture was significant and positive after the two parameters being normalized with PAR peak values. When the soil moisture content was higher, the transpiration of the trees with larger DBH was steadily increasing with soil moisture, while that of the trees with moderate or smaller DBH had opposite trend, presumably due to their transpiration and water absorption were approached to the limit.