Search

Rakicidin B1 was isolated and purified from the culture broth of a marine Streptomyces sp. as a potent anti-cancer agent, and lately the compound and its derivatives have firstly been found to possess anti-Clostridium difficile (CD) activity but with high cytotoxicity. Herein, following our previous discovery on anti-CD activity of Rakicidin B1, structure modification was performed at the OH position of Rakicidin B1 and a new Rakicidin B1-PEG hybrids FIMP2 was facilely designed and synthesized by conjugating the PEG2000 with the scaffolds of Rakicidin B1 via the linkage of carbamate. The cytotoxicity of the FIMP2 was first evaluated against three different cancer cell lines, including HCT-8 cells, PANC-1, and Caco-2, with IC50 values at 0.519 μM, 0.815 μM, and 0.586 μM, respectively. Obviously, as compared with a positive control group treated with Rakicidin B1, the IC50 value of FIMP2 increased by nearly 91-fold, 50-fold, and 67-fold, suggesting that the PEGylation strategy significantly reduced the cytotoxicity of FIMP2. Thus, this preliminary result may be beneficial to increase its safety index (SI) value due to the decreased cytotoxicity of FIMP2. In addition, this decreased cytotoxicity of FIMP2 was further confirmed based on a zebrafish screening model in vivo. Thereafter, the anti-CD activity of FIMP2 was evaluated in vivo, and its efficacy to treat CDI was found to be better than that of vancomycin. The mortality and recurrence rate of FIMP2 is not as low compared with that of vancomycin; these results demonstrated that compound FIMP2 is a new, promising anti-CD agent with significant efficacy against CD recurrence with low cytotoxicity towards bodies.

Lipid-related cancers cause a large number of deaths worldwide. Therefore, development of highly efficient Lipid droplets (LDs) fluorescent imaging probes will be beneficial to our understanding of lipid-related cancers by allowing us to track the metabolic process of LDs. In this work, a LDs-specific NIR (λmax = 698 nm) probe, namely BY1, was rationally designed and synthesized via a one-step reaction by integrating triphenylamine (electron–donor group) unit into the structure of rofecoxib. This integration strategy enabled the target BY1 to form a strong Donor–Acceptor (D-A) system and endowed BY1 with obvious aggregation-induced emission (AIE) effect. Meanwhile, BY1 also showed observable solvent effect and reversible mechanochromatic luminescent property, which could be interpreted clearly via density functional theory (DFT) calculations, differential scanning calorimetry (DSC), powder X-ray diffraction (XPRD), and single crystal X-ray data analysis. More importantly, BY1 exhibited highly specific fluorescent imaging ability (Pearson’s correlation = 0.97) towards lipid droplets in living HeLa cells with low cytotoxicity. These results demonstrated that BY1 is a new promising fluorescent probe for lipid droplets imaging, and it might be beneficial to facilitate biological research of lipid-related cancers.

Carbon sequestration in terrestrial ecosystems is critical for combating global climate change and achieving regional carbon neutrality, and LUCC is a vital factor influencing the carbon cycle process of terrestrial ecosystems and causing changes in carbon sources/sinks. This study analyzes the drivers of LUCC based on a review of the dynamics of LUCC in Changzhi from 2000 to 2020, analyzes the driving factors of LUCC using the Clue-S model and binary logistic regression analysis model, then simulates land-use patterns under different scenarios in 2030 by the CA-Markov model, and finally analyzes carbon stock changes and spatial distribution characteristics in different periods from the perspective of carbon source/sink interconversion with the help of InVEST model. The results show: (1) in the past two decades, more than 90% of the expansion of artificial surfaces in Changzhi comes from cultivated land. Ecological conservation policies are more decisive in influencing LUCC than natural, social, and transportation accessibility factors. (2) During the 20 years, the total carbon stock increased by 680,989.73 t, with the carbon emission control area accounting for 7.5%, mainly distributed near urban centers and coal mining areas. The carbon sink enhancement area accounts for 5.5% and is mainly concentrated near forest land and ecological and nature reserves. (3) The spatial location of cities influences the density of carbon stock in the adjacent range. Carbon stock density increases within the buffer zone with the distance from urban center, county center, expressways, national highway, settlements, rivers, provincial roads, reservoirs, railways, county highway, and village roads. The rate of carbon stock increase per 100 m is 0.12 t/ha, 0.25 t/ha, 0.17 t/ha, 0.36 t/ha, 0.71 t/ha, 0.33 t/ha, 0.38 t/ha, 0.57 t/ha, 0.23 t/ha, 0.46 t/ha, and 0.48 t/ha respectively. The higher the administrative center and road grades, the lower the carbon density will be instead. (4) In the 2030 CD scenario, compared with the ND scenario, the cultivated land and grassland are effectively protected and the cultivated land area is increased by 445.68 km2, while the expansion of artificial surface is suppressed and the area is reduced by 448.2 km2, which ultimately leads to a reduction in carbon loss of 392,011.85 t. Future ecological management should focus on protecting high-value carbon sink areas and carbon sink enhancement areas and the ecological management and restoration of low-value carbon sink areas and carbon emission control areas.

Opencast mining contributes to the severe disturbance of vegetation and serious damage to the ecological environment. Scientific assessment of the ecological losses may provide guidance for the sustainable land use in mining areas. This study uses the Carnegie Ames Stanford Approach (CASA) model to estimate the net primary productivity (NPP) of vegetation in the Pingshuo mining area from 2006 to 2020 and uses statistical analysis and mathematical models to study the impact of mining and land reclamation on NPP. The results show that NPP decreased slowly at a rate of 0.809 gC/(m2·month) per year. In 2006, the urban area of Pinglu and the opencast coal mining area were located in the western part of the study area, while the eastern part was distributed with a large amount of grassland, forested and cultivated land, and the NPP showed a high pattern in the east and low in the west. With the continued eastward movement of Antaibao and Anjialing mining areas, as well as the construction and continuous westward expansion of the East opencast mine, the pits of all three opencast mines moved to a central location in 2020, changing the spatial distribution of NPP to high in the surroundings and low in the middle. The NPP within the three opencast mines decreased significantly, but the change in NPP increased from −7.34 gC/(m2·month) to 7.15 gC/(m2·month) as the reclamation area increased, indicating that mining increased ecological losses while land reclamation mitigated them. The variation of NPP within 600 m outside the mining area is 2.06~7.45 gC/(m2·month), and 0.11~1.00 gC/(m2·month) from 600 m to 1000 m, indicating that NPP is sensitive to the influence of mining. The results may provide guidance for further analysis of the impact of mining on local environments and exploration of more appropriate land reclamation measures.

Soybean mosaic virus (SMV) is a worldwide and hardly controlled virus disease in soybean. Kefeng-1 is an elite variety resistant to SMV in China. In order to discover resistance genes and regulation networks in Kefeng-1, we analyzed transcriptome data of resistant (Kefeng-1) and susceptible (NN1138-2) soybean varieties in response to infection of the SMV strain SC18 at 0, 6, and 48 hours post-inoculation (hpi) and 5 days post-inoculation (dpi). Many differentially expressed genes (DEGs) were identified with Kefeng-1 and NN 1138-2. Based on the enrichment analysis for gene ontology (GO) and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway, we found that 48 hpi was the best time point for the defense response of the two soybean varieties in response to the SMV infection. The expression of seven candidate genes was further verified by qRT-PCR and was relatively consistent with the results of RNA-Seq. The expression of genes for Glyma.11G239000 and Glyma.18G018400, members of the ethylene-insensitive 3/ethylene-insensitive3-like (EIN3/EIL) protein family involved in ETH, were downregulated in NN1138-2 but not in Kefeng-1 and the expression of Glyma.14G041500 was upregulated in Kefeng-1 at 5 dpi. The expression of jasmonic acid repressor genes (TIFY/JAZ) was downregulated in NN1138-2 but not in Kefeng-1. NPR1 involved in the salicylic acid signaling pathway was downregulated in NN1138-2 at 48 hpi but upregulated in Kefeng-1. It shows that ethylene, jasmonic acid, and salicylic acid signaling pathways may be involved in the disease resistance process to the SMV strain SC18. Our findings would help to understand the molecular mechanism of soybean resistance to SMV.

In this work, we synthesized a pair of positional isomers by attaching a small electron-donating pyrrolidinyl group at ortho- and para-positions of a conjugated core. These isomers exhibited totally different fluorescent properties. PDB2 exhibited obvious aggregation-induced emission properties. In contrast, PDB4 showed the traditional aggregation-caused quenching effect. Their different fluorescent properties were investigated by absorption spectroscopy, fluorescence spectroscopy, density functional theory calculations and single-crystal structural analysis. These results indicated that the substituent position of the pyrrolidinyl groups affects the twisted degree of the isomers, which further induces different molecular packing modes, thus resulting in different fluorescent properties of these two isomers. This molecular design concept provided a new accurate strategy for designing new aggregation-induced emission luminogens.

Cyclooxygenase-2 (COX-2) imaging agents are potent tools for early cancer diagnosis. Almost all of the COX2 imaging agents using celecoxib as backbone were chemically modified in the position of N-atom in the sulfonamide group. Herein, a novel COX-2 probe (CCY-5) with high targeting ability and a near-infrared wavelength (achieved by attaching a CY-5 dye on the pyrazole ring of celecoxib using a migration strategy) was evaluated for its ability to probe COX-2 in human cancer cells. CCY-5 is expected to have high binding affinity for COX-2 based on molecular docking and enzyme inhibition assay. Meanwhile, CCY-5 caused stronger fluorescence imaging of COX-2 overexpressing cancer cells (Hela and SCC-9 cells) than that of normal cell lines (RAW 264.7 cells). Lipopolysaccharide (LPS) treated RAW264.7 cells revealed an enhanced fluorescence as LPS was known to induce COX-2 in these cells. In inhibitory studies, a markedly reduced fluorescence intensity was observed in cancer cells, when they were co-treated with a COX-2 inhibitor celecoxib. Therefore, CCY-5 may be a selective bioimaging agent for cancer cells overexpressing COX-2 and could be useful as a good monitoring candidate for effective diagnosis and therapy in cancer treatment.

This paper investigated the characteristics of a novel type of hybrid high voltage direct current (HVdc) converter, which is composed by line commutated converter series with voltage source converter. The system and valve level control strategies are introduced, which can provide ac system voltage support. A novel filter design scheme composed by resonant filers for hybrid HVdc are also proposed, which can decrease the capacity of reactive power compensation equipment without deteriorate harmonic characteristics. The ac voltage of HVdc fluctuation level caused by transmitted power variation will be effectively reduced, with the coordination between filter design scheme and converter control. In addition, the influence of ac grid strength is also analyzed by equivalent source internal impedance represented by short circuit ratio (SCR). Finally, the +800 kV/1600 MW hybrid HVdc system connecting two ac grids under different SCR cases are studied, and the PSCAD/EMTDC simulation results have validated the effectiveness for proposed strategy.

In this paper, a novel cataluminescence (CTL)-based sensor array consisting of nine types of catalytic materials is developed for the recognition of several harmful gases, namely carbon monoxide, acetone, chloroform and toluene. First, the experimental setup is constructed by using sensing nanomaterials, a heating plate, a pneumatic pump, a gas flow meter, a digital temperature device, a camera and a BPCL Ultra Weak Chemiluminescence Analyzer. Then, unique CTL patterns for the four types of harmful gas are obtained from the sensor array. The harmful gases are successful recognized by the PCA method. The optimal conditions are also investigated. Finally, experimental results show high sensitivity, long-term stability and good linearity of the sensor array, which combined with simplicity, make our system a promising application in this field.

Nowadays, most vehicles are equipped with positioning devices such as GPS which can generate a tremendous amount of trajectory data and upload them to the server in real time. The trajectory data can reveal the shape and evolution of the road network and therefore has an important value for road planning, vehicle navigation, traffic analysis, and so on. In this paper, a road network generation method is proposed based on the incremental learning of vehicle trajectories. Firstly, the input vehicle trajectory data are cleaned by a preprocess module. Then, the original scattered positions are clustered and mapped to the representation points which stand for the feature points of the real roads. After that, the corresponding representation points are connected based on the original connection information of the trajectories. Finally, all representation points are connected by a Delaunay triangulation network and the real road segments are found by a shortest path searching approach between the connected representation point pairs. Experiments show that this method can build the road network from scratch and refine it with the input data continuously. Both the accuracy and timeliness of the extracted road network can continuously be improved with the growth of real-time trajectory data.