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It is of great significance to reveal the changes of grain production pattern and natural resource utilization efficiency for rational utilization of natural resources, security of national food security, and sustainable development. Base on the data of county-scale grain production and 683 meteorological stations from 1985 to 2015 in China, ArcGIS spatial analysis method was adopted to analyze the grain production pattern changes and heat resource utilization characteristics considered temperature zone division. Studies had shown that about 90% of Chinese total grain output was produced in mid temperate, warm temperate, northern subtropical, and mid subtropical zones from 1985 to 2015, accounting for 18.6%, 25.6%, 21.6%, and 25.9%, respectively. In the past 30 years, the proportion of grain production in the single cropping region had increased by 13.8%, while it had decreased by 2.7% and 11.2% in the double and triple cropping region, respectively. The proportion of grain production had increased by 13.9% in the mid temperate zone of the single cropping region which was drove by the advance of planted acreage and yield, while the proportion decreased by 13.9% in the subtropical zones of the triple-cropping system. Over the past 30 years, the annual accumulated temperature above 10 °C had continued to increase in different temperature zones, and that was more evident in southern region than northern region. However, the increased magnitude of heat utilization efficiency for grain production in southern temperature zones was lower than northern region. There was a "dislocation phenomenon" between the changes of Chinese grain production pattern and the distributions of heat resources. Therefore, it was necessary to consider the coordination of grain production and natural resources matching as well as the characteristics of resource utilization for improving resource utilization efficiency when optimizing the layout of regional grain production and formulating strategies in China. [ABSTRACT FROM AUTHOR]

Arginine kinase plays an important role in cellular energy metabolism and is closely related to the environmental stress response in marine invertebrates. We studied the Cu 2+ -mediated inhibition and aggregation of Sepia pharaonis arginine kinase (SPAK) and found that Cu 2+ markedly inhibited the SPAK activity along with mixed-type inhibition against the arginine substrate and noncompetitive inhibition against the ATP cofactor. Spectrofluorimetry results showed that Cu 2+ induced a tertiary structure change in SPAK, resulting in exposure of the hydrophobic surface and increased aggregation. Cu 2+ -mediated SPAK aggregation followed first-order kinetics consistent with monophasic and a biphasic processes. Addition of osmolytes, including glycine and proline, effectively blocked SPAK aggregation and restored SPAK activity. Our results demonstrated the effects of Cu 2+ on SPAK catalytic function, conformation, and aggregation, as well as the protective effects of osmolytes on SPAK folding. This study provided important insights into the role of Cu 2+ as a negative effector of the S. pharaonis metabolic enzyme AK and the possible responses of cephalopods to unfavorable environmental conditions. [ABSTRACT FROM AUTHOR]

Objective To determine the equilibrium solubility and the oil-water partition coefficients of rhaponticin by HPLC-fluorometric method. Methods Separation was achieved on SHIM-PACK VP-ODS column. The mobile phase consisted of methanol-water (40:60) with a flow rate of 0.8mL/min, detection with a fluorometric detector set at an excitation wavelength of 320nm and emission wavelength of 410nm. The equilibrium solubility at 37℃ in water and in series of buffer solutions with different pH, and oil-water partition coefficients (logP) in the octanol-water/the buffer solution system of rhaponticin were determined in the above conditions. Results The equilibrium solubility of rhaponticin in water was 109.54mg/L at 37℃ and exhibited a maximum solubility of 126.12mg/L at pH 8.0; the partition coefficient of rhaponticin was 0.53 in n-octanol-water system and the maximum partition coefficient was 0.76 in n-octanol-buffer solution system at pH 6.0. Conclusion A HPLC-fluorometric method was developed, and the method was successfully applied to determine the equilibrium solubility and oil-water partition coefficients of rhaponticin. The research results can provide the theoretical basis for development and pharmacokinetic studies of rhaponticin dosage form. [ABSTRACT FROM AUTHOR]

Summary: News series of substituted quinazoline derivatives has been synthesized from 3,4-dihydro-7-methoxy-4-oxoquinazoline-6-yl acetate(1) by five-step procedures including chlorination, amination, hydrolysis and etherification. The structures of target compounds were confirmed by IR,1H-NMR, element analysis and single-crystal X-ray diffraction. The results showed that the compound 8c exhibited remarkable inhibitory activity against MCF-7 cell lines with inhibition rate value of 38.45%, which was comparable to that of the positive control Gefitinib(inhibition rate = 13.25% for MCF-7). The initial relationship between structure and activity was worth further exploration. [ABSTRACT FROM AUTHOR]

A new type of handshape tuina -cupping instrument is developed to overcome the shortcomings of traditional cupping therapy, such as indentation and pain, and simulates the tuina manipulation, so as to realize the combination of cupping therapy and tuina manipulation. The handshape tuina -cupping instrument has a trumpet-shaped, silica gel edge. At the same time, the finger-belly shape is added at the cupping edge to simulate the shape of fingers during tuina . Under the action of air suction and deflation of pulsating airflow, the purpose of simulating tuina manipulation is achieved, and the indentation and pain caused by the handshape tuina -cupping instrument is significantly less than that of the traditional cupping instrument.

The aim of the present study was to investigate the effects of exercises with different durations and intensities on mitochondrial autophagy and FUNDC1 in rat skeletal muscles. Sixty male Sprague-Dawley rats were randomly divided into 2- and 4-week control groups (Con), moderate-intensity exercise groups (M-ex groups, treadmill exercise, 16 m/min, 1 h/d, 6 d/week), and high-intensity exercise groups (Hi-ex groups, treadmill exercise, 35 m/min, 20 min/d, 6 d/week). The bilateral soleus muscles were separated after the intervention, and paraffin sections were prepared for transmission electron microscopy. ELISA method was used to detect the content of citrate synthase (CS). The co-localizations of microtubule-associated protein 1 light chain 3 (LC3)/cytochrome c oxidase IV (COX-IV), FUNDC1/COX-IV and LC3/FUNDC1 were observed by immunofluorescent staining in frozen sections. The skeletal muscle mitochondria were extracted, and the expression of autophagy-related proteins, including AMPKα, p-AMPKα, Unc-51 like kinase 1 (ULK1), FUNDC1, LC3 and p62, were detected by Western blot. The results showed that exercise increased mitochondrial function, i.e. peroxisome proliferator-activated receptor γ co-activator-1α (PGC-1α), COX-I protein expression levels and CS content. There was no difference of mitochondrial function parameters between 2-week M-ex and 2-week Hi-ex groups, while mitochondrial function of 4-weeks Hi-ex group was significantly lower than that of 4-week M-ex group. Under the same exercise intensity, mitochondrial autophagy activation in skeletal muscle of 4-week exercise was higher than that in 2-week exercise group; Under the same duration of exercise, mitochondrial autophagy activation of Hi-ex group was higher than that in M-ex group. Both 2- and 4-week exercise intervention increased LC3/COX-IV, COX-IV/FUNDC1, and FUNDC1/LC3 co-localizations. Exercise increased LC3-II/LC3-I ratio, down-regulated p62 protein expression level, up-regulated FUNDC1, ULK1 protein expression levels and AMPKα phosphorylation, and the changes of these proteins in 4-week Hi-ex group were significantly greater than those in 4-week M-ex group. These results suggest exercise induces mitochondrial autophagy in skeletal muscles, and the activity of autophagy is related to the duration and intensity of exercise. The induction mechanism of exercise may involve the mediation of FUNDC1 expression through AMPK-ULK1 pathway.

Reduced expression levels of caveolin‑1 (Cav‑1) in tumor stromal fibroblasts influences the occurrence and progression of tumors, particularly in breast cancer, but the relevant molecular mechanism is unclear. The present study aimed to clarify the potential mechanism underlying the promotion of tumor growth by reduced Cav‑1 expression levels, by investigating Cav‑1‑targeted molecules in fibroblasts and breast cancer cells. The expression of growth factors in the ESF fibroblast cell line transfected with Cav‑1 small interfering RNA (siRNA) was examined. The expression of apoptotic regulators in the BT474 breast cancer cell line that was co‑cultured with the fibroblasts, was also investigated. The transfection of Cav‑1‑targeting siRNA in ESF cells resulted in efficient and specific inhibition of Cav‑1 expression. The downregulation of Cav‑1 increased the expression and secretion of stromal cell‑derived factor‑1 (SDF‑1), epidermal growth factor (EGF) and fibroblast‑specific protein‑1 (FSP‑1) in ESF cells. This resulted in the accelerated proliferation of the breast cancer cells. Tumor protein 53‑induced glycolysis and apoptosis regulator (TIGAR) was upregulated in the BT474 cells under the condition of co‑culture with Cav‑1 siRNA fibroblasts, while levels of reactive oxygen species (ROS) were decreased, resulting in apoptosis inhibition in the breast cancer cells. These results demonstrated that the downregulation of Cav‑1 promoted the growth of breast cancer cells through increasing SDF‑1, EGF and FSP‑1 in tumor stromal fibroblasts, and TIGAR levels in breast cancer cells. To the best of our knowledge, the present study supports the hypothesis that Cav‑1 possesses tumor‑suppressor properties, with the mechanism of Cav‑1‑dependent signaling involving the regulation of SDF‑1, EGF, FSP‑1 and TIGAR.

Background: There are still no absolute parameters predicting progression of adenoma into cancer. The present study aimed to characterize functional differences on the multistep carcinogenetic process from the adenoma-carcinoma sequence., Methods: All samples were collected and mRNA expression profiling was performed by using Agilent Microarray high-throughput gene-chip technology. Then, the characteristics of mRNA expression profiles of adenoma-carcinoma sequence were described with bioinformatics software, and we analyzed the relationship between gene expression profiles of adenoma-adenocarcinoma sequence and clinical prognosis of colorectal cancer., Results: The mRNA expressions of adenoma-carcinoma sequence were significantly different between high-grade intraepithelial neoplasia group and adenocarcinoma group. The biological process of gene ontology function enrichment analysis on differentially expressed genes between high-grade intraepithelial neoplasia group and adenocarcinoma group showed that genes enriched in the extracellular structure organization, skeletal system development, biological adhesion and itself regulated growth regulation, with the P value after FDR correction of less than 0.05. In addition, IPR-related protein mainly focused on the insulin-like growth factor binding proteins., Conclusion: The variable trends of gene expression profiles for adenoma-carcinoma sequence were mainly concentrated in high-grade intraepithelial neoplasia and adenocarcinoma. The differentially expressed genes are significantly correlated between high-grade intraepithelial neoplasia group and adenocarcinoma group. Bioinformatics analysis is an effective way to study the gene expression profiles in the adenoma-carcinoma sequence, and may provide an effective tool to involve colorectal cancer research strategy into colorectal adenoma or advanced adenoma.