"Omics" and bioinformatics have brought new ideas to the study of traditional Chinese medicine. This study used metabonomics and network pharmacology to investigate the pharmacodynamic basis and regulation of Qishen Yiqi dropping pill (QDP) improving cardiac energy metabolism in rats with heart failure (HF). ¹H NMR metabonomics analysis showed that eight metabolites, including carnitine, glutamine, creatine, proline, homocitrulline, lactic acid, taurine and alanine appeared significant callback after QDP treatment for HF. The results indicate that QDP regulates the metabolism of carbohydrate, lipid, ATP and protein. The animal experiment was conducted in accordance with the regulations of the Ethics Committee for Experimental Animal Management and Animal Welfare of Institute of Materia Medica, Chinese Academy of Medical Sciences. A "drug-component-target-disease" network was established using network pharmacology, and the "component-target" sub-network related to the above energy metabolism processes was extracted by combining metabonomics results. Results revealed 79 chemical compounds and 47 potential targets of QDP involved in the regulation of energy metabolism, and identified key chemical components including ursolic acid, notoginsenoside G, ginsenoside-Rh1, and core targets such as INS, PPARG, and AKT1. The results also demonstrated the complex multi-target and multi-component relationship between QDP and HF from the perspective of energy metabolism. The molecular docking technique verified a strong interaction between some targets and chemical compounds, with affinities less than -5 kcal·mol^-1. The results of this study provide useful information for the clinical application, development, and utilization of QDP.

OBJECTIVETo observe the effect and mechanism of curcumin derivative B06 on kidney from rats with hyperlipidemia and type 2 diabetes.

METHODSThirty five male SD rats were randomly divided into five groups(n = 7): the normal control group, high-fat group, high-fat + B06-treatd group, diabetic group, diabetic + B06-treated group. After fed with high-fat diet for 4 weeks, the later two groups were in- jected with streptozotocin intraperitoneally to induce type 2 diabetes mellitus. B06-treated groups were given B06 by gavage at a dosage of 0.2 mg/kg . d for 8 weeks. After the treatment, the serum creatinine, blood urea nitrogen and uric acid were detected biochemically, the morphology of kidney was observed with light and transmission electron microscopy, the expression of collagen fibers was observed with Masson staining, the protein expression of collogen IV and fibronectin in kidney were determined by Immunohistochemistry.

RESULTSIt was showed that the levels of the serum creatinine and blood urea nitrogen elevated significantly in diabetic group. In high-fat and diabetic groups, increased glomerular mesangial matrix and collagen fiber and thicken glomerular basal membrane were observed under light microscopy, swelling and fusion of foot process were found under electron microscope; increased green matrix within glomeruli was observed under Masson staining. collogen IV and fibronectin protein expression were significantly enhanced in high-fat group and diabetic group. After B06's intervention, the levels of serum creatinine and blood urea nitrogen were decreased in diabetic groups, the morphological change of kidney was obviously relieved, Collogen IV and fibronectin protein expression reduced.

CONCLUSIONCurcumin derivative B06 exerts a protective effect on kidney in type 2 diabetic rats, reduced expressions of collogen IV and fibronectin, inhibition of the accumulation of extracellular matrix and glomerular mesangial proliferation, and then prevention of renal fibrosis may be the mechanism.

Animals ; Blood Urea Nitrogen ; Collagen Type IV ; metabolism ; Creatinine ; blood ; Curcumin ; pharmacology ; Diabetes Mellitus, Experimental ; complications ; drug therapy ; Diabetes Mellitus, Type 2 ; Drugs, Chinese Herbal ; Fibronectins ; metabolism ; Kidney ; metabolism ; physiopathology ; Kidney Diseases ; drug therapy ; Male ; Rats ; Rats, Sprague-Dawley ; Streptozocin ; Uric Acid ; blood

Objective To investigate the expression difference of vascular endothelial growth factor (VEGF)between lung cancer and lung benign disease,and its relation to clinical characteristics and prognosis of non-small cell lung cancer(NSCLC),and to research the possible role of VEGF in the growth of lung can- cer.Methods The expression of VEGF and microvascular density(MVD)were detected in 60 lung cancer tissues and 30 lung benign disease tissues after operation by immunohistochemical method and put up statisti- cal analysis.Results The positive rate of VEGF expression(63%)and MVD(45.13?10.27)in lung cancer tissues were both higher than those in lung benign disease tissues(27%,33?6.49)(P

Morphology and molecular identification technology were used to identify 3 original plants of Fructus Elaeagni which was commonly used in Uygur medicine. Leaves, flowers and fruits from different areas were selected randomly for morphology research. ITS2 sequence as DNA barcode was used to identify 17 samples of Fructus Elaeagni. The genetic distances were computed by kimura 2-parameter (K2P) model, and the Neighbor-Joining (NJ) and Maximum Likelihood phylogenetic trees were constructed using MEGA5.0. The results showed that Elaeagnus angustifolia, E. oxycarpa and E. angustifolia var. orientalis cannot be distinguished by morphological characteristics of leaves, flowers and fruits. The sequence length of ITS2 ranged from 220 to 223 bp, the average GC content was 61.9%. The haplotype numbers of E. angustifolia, E. oxycarpa and E. angustifolia var. orientals were 4, 3, 3, respectively. The results from the NJ tree and ML tree showed that the 3 original species of Fructus Elaeagni cannot be distinguished obviously. Therefore, 3 species maybe have the same origin, and can be used as the original plant of Uygur medicineal material Fructus Elaeagni. However, further evidence of chemical components and pharmacological effect were needed.
DNA Barcoding, Taxonomic ; methods ; DNA, Plant ; genetics ; DNA, Ribosomal Spacer ; genetics ; Drug Contamination ; prevention & control ; Drugs, Chinese Herbal ; chemistry ; classification ; Elaeagnaceae ; anatomy & histology ; classification ; genetics ; Fruit ; anatomy & histology ; classification ; genetics ; Molecular Sequence Data ; Phylogeny ; Quality Control

OBJECTIVE:To compare in vivo and in vitro permeation behaviors of the ethosome gels of testosterone,testoster-one propionate and testosterone undecanoate. METHODS:The ethosome gels of testosterone,testosterone propionate and testoster-one undecanoate were prepared. With cumulative permeating amount and permeation rate as the indexes,Franz diffusion cell and HPLC were employed to compare in vitro permeation behaviors of 3 kinds of ethosome gels in mouse skin. With testosterone patch as the positive control drug, electrochemistry method was adopted to detect the concentration of testosterone in plasma 0,3,6, 9,12,24,36 and 48 h after applying such 3 kinds of ethosome gels on the back of rats,and then pharmacokinetic parameters were calculated with DAS 2.0 software. RESULTS:24 h cumulative permeating amounts of the ethosome gels of testosterone,tes-tosterone propionate and testosterone undecanoate were(234.31±13.8),(175.63±41.1)and(72.60±15.3)μg/cm2,and the per-meation rates were(10.25±1.9),(7.64±1.4)and(2.96±0.8)μg/(cm2·h),respectively. The pharmacokinetic parameters of the above-mentioned three kinds of ethosome gels and the positive control drug were respectively as follows as cmax of(20.19±2.57), (17.50±2.91),(0.23±0.04),(14.97±2.12)ng/ml,t1/2Ka of(2.80±0.45),(3.36±0.59),(4.02±0.62),(4.20±0.71)h,AUC0-48 h of(13.85±1.96),(13.93±2.13),(0.35±0.07),(11.76±2.31)ng·h/ml. CONCLUSIONS:in vivo and in vitro permeation behav-iors of the ethosome gels of testosterone and testosterone propionate are fairly good.

Studies have found that metformin is not only the preferred drug for lowering blood sugar, but also shows lipid-lowering and weight-loss effects. The purpose of this study was to use a hyperlipidemia hamster model to investigate the lipid-lowering effect of metformin and its effect on important metabolic pathways in lipid metabolism disorders. Fifty golden hamsters were divided into a control group, a model group, metformin high- and low-dose groups, and a simvastatin group. A high-fat diet was fed for 1 week to create the model, and then drug was administered for 11 weeks with the high-fat diet. Serum was taken for measurement of blood lipid and blood glucose at 2, 6, and 9 weeks after administration, and at weeks 3, 5, and 9 feces and urine were collected for ¹H NMR metabolomics tests. After 11 weeks of intravenous injection of [U-¹³C₆] glucose, serum was collected for a ¹³C NMR metabolic flux test. The results showed that the administration of metformin can significantly reduce blood lipids and glucose levels and can significantly affect metabolic pathways such as sugar metabolism, lipid metabolism, ketone metabolism, amino acid metabolism, and intestinal flora metabolism. The results of the metabolic flux analysis showed that the high-fat diet reduced the metabolism of tricarboxylic acids by 37.48%. After administration of low and high doses of metformin the metabolism of tricarboxylic acid increased by 98.14% and 143.10%, respectively. After administration of simvastatin tricarboxylic acid metabolism increased by 33.18%. The results indicate that metformin has a significant effect on promoting energy metabolism. This study used a combination of metabolomics and metabolic flow to explore the effect of metformin on lipid metabolism disorders and quantifies changes in the key pathway of energy metabolism-the tricarboxylic acid cycle. This study provides useful information for the study of the efficacy and mechanism of metformin, as well as a practical technical method for the screening of lipid-lowering drugs based on a hamster model.

Objective To evaluate the quality of the portal images acquired by computed radiography(CR)system and conventional screen-film system,respectively.Methods imaging plates (IP)and X-ray films of a home-devised lead phantom with a leakage of 6.45% were acquired,and modulation transfer function(MTF)curves of the both images were measured using edge method.Portal images of 40 nasopharyngeal cancer patients were acquired by IP and screen-film system respectively.Two doctors with similar experience evaluated the damage degree of petrosa] bone,the receiver operating characteristic(ROC)curve of CR images and general images were drawn according to two doctors evaluation results.Results The identification frequency of CR system and screen-film system were 1.159 and 0.806 Lp/mm respectively.For doctor one,the area under ROC curve of CR images and general images were 0.802 and 0.742 respectively.For doctor two,the area under ROC curve of CR images and general images were 0.751 and 0.600 respectively.The MTF curve and ROC curve of CR are both better than those of screen-film system.Conclusion The image quality of CR portal imaging is much better than that of screen-film system.The utility of CR in linear accelerator for portal imaging is promising in clinic.

OBJECTIVETo establish a novel Myc gene transgenic mouse model for spontaneously forming B-lymphoma and assessing its tumorigenesis potential.

METHODSFreshly isolated hematopoietic progenitor cells served as the target for Myc gene transfer mediated by a retrovirus vector. These cells were engrafted into C57BL/6 mice with (60)Co-gamma ray radiation in advance. Tumor latency was measured and the tumor loaded mice were followed for survival time. Tumor was identified with histology and immunostaining. The exogenous Myc gene was detected by Western blot (in liver, spleen, tumor tissue) and flow cytometry (FCM) \[in bone marrow (BM)\].

RESULTSMice BM-infected with mutant Myc gene more readily gave rise to B-cell lymphomas than those infected with wild type Myc gene did Myc gene was expressed highly in BM and tumor tissues but not in liver and spleen.

CONCLUSIONOur model will be a tool in assessing the transforming potential of Myc mutants and in studying cooperation between Myc and other oncogenes. Mutant Myc is more effective than wild-type Myc in promoting B cell lymphomagenesis in mice.

Animals ; B-Lymphocytes ; Cell Transformation, Neoplastic ; Flow Cytometry ; Lymphoma ; Lymphoma, B-Cell ; Mice ; Mice, Inbred C57BL ; Mice, Transgenic ; Retroviridae Infections

In order to develop potent antidiabetic agents that have inhibitory effect to a-glucosidase, twelve β-acetamido ketone derivatives such as N-{[(substituted-4-oxo-thiochroman-3-yl)phenyl]-methyl}acetamide are designed and synthesized through one-pot Dakin-West reaction. Their chemical structures are confirmed by 1H NMR, 13C NMR, IR and HR-MS. In vitro α-glucosidase inhibition assays of compounds 4a-41 were carried out using glucose oxidase method. The result indicated that most of them possess inhibitory activity in vitro. Compound 4k showed the most potent inhibitory activity with 87.3% inhibition of α-glucosidase at the concentration of 5.39 mmol x L(-1). The structure-activity relationship of these β-acetamido ketone derivatives was discussed preliminarily. Moreover, the molecular docking method was used to study the interaction mode of compound 4k and α-glucosidase. Our results will be helpful for designing of α-glucosidase inhibitors in the future.
Acetamides ; Glycoside Hydrolase Inhibitors ; chemical synthesis ; pharmacology ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Molecular Docking Simulation ; Structure-Activity Relationship ; alpha-Glucosidases ; metabolism

The effect of sowing date on grain protein, hordein fraction content and malting quality of two-rowed spring barley was investigated by using ten commercial cultivars with different grain protein content and the relationships among these traits were examined. The results showed that grain protein content and B hordein content increased as the sowing date postponed and were significantly affected by sowing date, while C and D hordein contents were less influenced by sowing date. There were significant differences in grain protein and hordein fraction content among the ten cultivars. The coefficient of variation of D hordein content was much larger than that of B and C hordein contents, suggesting its greater variation caused by different sowing dates. Beta-amylase activity and diastatic power were also significantly affected by sowing date, with malt extract being less affected. Significant differences in measured malt quality were found among the ten cultivars. Grain protein was significantly correlated with B hordein and malt extract positively and negatively, respectively. There was no significant correlation between beta-amylase activity or diastatic power and grain protein content. B hordein was negatively and significantly correlated with malt extract, but no significant correlations between C hordein, D hordein and malting quality traits.
Edible Grain ; chemistry ; Food Analysis ; Food Technology ; Glutens ; Hordeum ; growth & development ; metabolism ; Plant Proteins ; metabolism ; Seeds ; growth & development ; metabolism