Observing Intratissuelar Distribution of Polysorbate 80 Coated Nanoparticles in Brain with Analytical Electron Microscopy

The analyical electron microscopy （AEM） was employed to observe the intratissuelar distribution of polysorbate 80 coated nanoparticles in brain with copper chlorophyll （CC）.and a safe and cheap pigment was used as a marker,AEM analyses show that some nanoparticles are located at the wall of the nicrovasculum in brain,while others are distributed around the nicrovasculum in brain ,These results may support that T-80 coated nanoparticles cross the BBB through mechanisms of endocytosis or transcytosis.

An integrative profiling of metabolome and transcriptome in the plasma and skeletal muscle following an exercise intervention in diet-induced obese mice

Exercise intervention at the early stage of type 2 diabetes mellitus(T2DM)can aid in the maintenance of blood glucose homeostasis and prevent the development of macrovascular and microvascular complications.However,the exercise-regulated pathways that prevent the development of T2DM remain largely unclear.In this study,two forms of exercise intervention,treadmill training and voluntary wheel running,were conducted for high-fat diet(HFD)-induced obese mice.We observed that both forms of exercise intervention alleviated HFD-induced insulin resistance and glucose intolerance.Skeletal muscle is recognized as the primary site for postprandial glucose uptake and for responsive alteration beyond exercise training.Metabolomic profiling of the plasma and skeletal muscle in Chow,HFD,and HFD-exercise groups revealed robust alterations in metabolic pathways by exercise intervention in both cases.Overlapping analysis identified nine metabolites,including beta-alanine,leucine,valine,and tryptophan,which were reversed by exercise treatment in both the plasma and skeletal muscle.Transcriptomic analysis of gene expression profiles in the skeletal muscle revealed several key pathways involved in the beneficial effects of exercise on metabolic homeostasis.In addition,integrative transcriptomic and metabolomic analyses uncovered strong correlations between the concentrations of bioactive metabolites and the expression levels of genes involved in energy metabolism,insulin sensitivity,and immune response in the skeletal muscle.This work established two models of exercise intervention in obese mice and provided mechanistic insights into the beneficial effects of exercise intervention on systemic energy homeostasis.

Preparation and characterization of inclusion complexes of antitumor camptothecin with cucurbit[n=7,8]urils

The slightly water-soluble anticancer drug camptothecin(CPT) and its inclusion complexes with cucurbit[n = 7,8]uril(Q[n](n = 7,8)) were investigated.The formation of 1:2 complexes with Q[n](n = 7,8) in aqueous solution was confirmed by fluorescence spectroscopy and the apparent stability constants were determined to be higher than 3.01 × 1012 L2/mol2.The solid inclusion complexes of CPT and Q[n](n = 7,8) were also prepared by the co-evaporation method and characterized by Fourier transformation-infrared spectroscopy,differential scanning calorimetry and powder X-ray diffraction.Aqueous solubility and dissolution studies indicate that the complexes exhibited significantly increased dissolution rates compared with the pure drug and physical mixtures.The potential of Q[7] or Q[8] for stabilizing lactone modality of CPT was investigated by the High Performance Liquid Chromatography(HPLC) method.The results reveal more than 63% CPT lactone form(active form) in CPT-Q[7] or Q[8] complexes compared to only 36% CPT lactone form in the absence of Q[7] or Q[8] after being incubated in the phosphate buffer solution(pH 7.4 at 37 °C) for 5h.

Three-Dimensional Quantitative Structure-Activity Relationships of flavonoids and estrogen receptors based on docking

Flavonoids are endocrine disrupting compounds that occur ubiquitously in foods of plant origin.The Three-Dimensional Quantitative Structure-Activity Relationships (3D-QSAR) model based on ligand-receptor docking is established between 20 flavonoids and estrogen receptor alpha (ERα),which may provide further theoretical basis for research on the relationship between flavones and estrogen.Comparative molecular field analysis (CoMFA) was employed and the best results of cross-validation and non cross validation were 0.845 and 0.988,respectively.Correspondingly,molecular similarity index analysis (CoMSIA) was employed and the results of cross-validation and non cross validation were 0.670 and 0.990,respectively.The CoMFA/CoMSIA and docking results reveal the structural features for estrogen activity and key amino acid residues in binding pocket,and provide an insight into the interaction between the ligands and these amino acid residues.

植物雌激素染料木素对去卵巢大鼠的骨代谢的影响(英文)

Objective Genistein,as a phytoestrogen,is a type of soybean-derived isoflavone that possesses structural similarity to become estrogen.The purpose of this study was to elucidate whether the administration of genistein,extracted from a Chinese herbal medicine Huaijiao(Sophora japonica-Leguminosae),is capable of preventing rapid bone loss occurring in rats after surgical ovariectomy and improving the symptom caused by this.Methods Sixty rats were randomly divided into six groups,including control (sham-operated),ovariectomized model(OVX),E2-treated (E2) group that were subcutaneously injected with E2 at a dosage of 1.5 mg/kg once a week,and genistein-treated (Gen) groups at the dosage of 4.5 mg/kg,9.0 mg/kg and 18 mg/kg respectively. The treatment was administrated 8 days later after the operation.Samples were taken from every group randomly at 12 weeks after the treatment.Parameters,such as body weight,serum biochemical criterion,bone mineral density(BMD) and biomechanics,were evaluated.Results The results indicated that genistein could restrain body weight,increase the levels of serum Ca,Mg,P,calcitonin(CT) and decrease the levels of bone gla protein (BGP) and alkaline phosphatase (ALP) significantly.Compared with OVX group,genistein at the dosage of 4.5 mg/kg and 9 mg/kg enhanced the BMD of femur, tibias and L2-4.Genistein could also meliorate biomechanical indexes of rats (P<0.05 or P<0.01).Conclusions In comparison with the anti-osteoporosis effect of E2,the genistein extracted from Huaijiao has the same beneficial effect on anti-osteoporosis and has little side effect.