Actins ; metabolism ; Angiomyolipoma ; metabolism ; pathology ; surgery ; Antigens, Neoplasm ; Desmin ; metabolism ; Diagnosis, Differential ; Female ; Humans ; Leiomyosarcoma ; metabolism ; pathology ; Mediastinal Neoplasms ; metabolism ; pathology ; surgery ; Mediastinum ; pathology ; surgery ; Melanoma-Specific Antigens ; Middle Aged ; Neoplasm Proteins ; metabolism

Objective To assess the clinical application values of the protcin markers associated with Down syndrome (DS) in maternal serum which were screened and identified.Methods Seven maternal serum samples with DS fetus ( DS group) and 7 maternal serum samples with normal fetus ( control group) in the second trimester were separated by two-dimensional gel electrophoresis (2-DE).The differentinal expression profile of proteome in maternal serum from DS group was established.The differentially expressed proteins were screened by mass spectrometry (MS) and some proteins were verified by Western blotting (WB).Results Twenty-nine proteins were discovered to be differentially expressed by more than 1.5 folds in maternal serum from DS group,among which 19 proteins were up-regulated and 10 proteins were downregulated.Eight proteins displayed 2 or more folds changes in maternal serum from DS group were identified by MS and possibly matched with 12 proteins in Ameracan National Center of Biotchnology Information (NCBI) protein sequence database,such as dGTPase and Beta2-Glycoprotein Ⅰ (β2-GPI),etc.The resuhs of WB showed that the mean a values of dGTPase and β2-GPI were 21 567.0 ± 3009.4 and 22 097.0 ±3958.9 in the DS group,3957.7 ± 250.9 and 1799.7 ± 105.5 in the control group respectively,which presented that the expression of dGTPase and β2-GPI significantly increased in DS group (t'dGTPase =- 17.66,t'β2-GPI =- 14.83,P ＜0.0001 ).Conclusions 2-DE and MS are effective methods for preliminary identification of protein markers associated with DS in maternal serum.dGTPase and β2-GPI verified by WB laid a solid fundation for further screening new biologic markers for early diaglosis of DS.

Objective To investigate the influence of low calcium dialysate (DCa1.25) and midodrine hydrochloric (MHC) on blood pressure in hemodialysis patients. Methods Dialysate calcium concentration was changed from 1.5% (DCa1.5) to 1.25% in patients with hypercalcaemia pre- or post-dialysis.For patients with intradialytic hypotension(IDH), pre-dialysis antihypertensive drugs were ceased.If that didn′t work, MHC 2.5 or 5 mg was administered to them 30 minutes before dialysis were ceased.MHC was also administered to patients who had not taken antihypertensive drugs. The blood pressure (BP) and blood volume were recorded during dialysis. UCG and autonomic nerves function test including BP supine and standing test and sustained hand-grip test were measured as well. Results Twenty-one hemodialysis patients were involved in this study including male 9 and female 12. The average age was (54.4?14.2) years old,the time on dialysis (33.04?30.1) months. When DCa1.5 was changed to DCa1.25, 9 cases (42.9%) could maintain stable BP, but IDH occurred in 10 patients(47.6%) with symptoms such as swirl,sweat or cramp, one with lower extremities cramp and one with heart discomfort but without IDH. Patients with IDH had higher proportion of abnormal BP supine and standing tests compared with patients without IDH(50% vs. 0%, P

Chondrosarcoma ; metabolism ; pathology ; surgery ; Female ; Humans ; Middle Aged ; S100 Proteins ; metabolism ; Soft Tissue Neoplasms ; metabolism ; pathology ; surgery ; Thoracic Neoplasms ; metabolism ; pathology ; surgery ; Thoracic Wall ; Vimentin ; metabolism

Objective To explore the effect of sodium arsenite (iAs3+) and sodium hydrogen arseuate (iAs5+) exposure on rat multidrug resistance protein 2 (MRP2) expression,and the correlation of liver arsenic and its methylation products,and to provide a basis for further elucidating the mechanism of arsenic toxicity.Methods Seventy wistar rats were randomly divided into seven groups,10 rats in each group.Control group was administrated with deionized water.Sodiun arsenite high-dose group,middle-dose group,low-dose group were administrated with different concentrations of sodium arsenite:20.0,6.7 and 2.2 mg/kg BW every day,respectively.Animals were sacrificed 90 days later by cervical dislocation to collect liver,the expression of MRP2 in the membrane of hepatocyte was determined by Western blotting.HPLC-HGAFS was employed to determine the content or level of arsenic and its methylation products.Correlation between expression of MRP2 and arsenic methylation products was analyzed using Pearson's linear correlation method.Results The MRP2 protein levels of control group,iAs3+ and iAs5+ high-,middle-,low-dose groups were 1.21 ± 0.13,1.85 + 0.09,1.65 + 0.19,1.61 + 0.18,1.69 + 0.04,1.42 + 0.19,1.27 ± 0.10.Compared to control group,MRP2 protein levels of iAs3+ high-,middle-,low-dose group and iAs5+ high-dose group were increased (P ＜ 0.05); Compared with the low-dose group,MRP2 protein levels of iAs3+ and iAs5+ high dose groups were increased(P ＜ 0.05); Comparing the matched doses group of iAs5+ and iAs3+,MRP2 protein levels of iAs3+ high-,middle-,low-dose group were higher than iAs5+(P ＜ 0.05).Meanwhile,there was a significant positive relationship between the expression of MRP2 and the content of iAs3+,MMA and DMA in iAs3+ exposed group(r =0.575,0.678,0.395,all P ＜ 0.05).There was also a significant correlation between the expression of MRP2 and MMA and IMA in iAs5+ exposed group(r =0.593,0.643,all P ＜ 0.05).There was no significant relationship between the expression of MRP2 and the content of iAs5+in iAs5+ exposed group.Conclusions The expression of MRP2 is increased with increasing dose of arsenic exposure,thus resulting in compensatory changes on MRP2 expression in the liver cell membrane.MRP2 efflux may play an important role in the metabolic pathways of iAs3+.The level or load of arsenic methylation in liver is closely related with MRP2 expression.

Linalool, as a major volatile compound, is widely distributed in natural plant essential oil. In addition, it can also be artificially synthesized. Linalool is used frequently as an important ingredient of perfumes and household detergents. It is still employed in food flavor and industries. Besides, linalool has some positive effect on healthcare. Many studies have showed that linalool exhibited a variety of pharmacological activities, including analgesic, anxiolytic, sedative, anti-inflammatory, anti-tumor and anti-bacterial effects. Therefore, linalool will be a promising agent for clinical application. This article reviews the pharmacological effects and formulation studies of linalool so as to provide a theoretical basis for its further development and utilization.
Animals ; Anti-Anxiety Agents ; chemistry ; pharmacology ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Hypnotics and Sedatives ; chemistry ; pharmacology ; Monoterpenes ; chemistry ; pharmacology

Design of structurally-novel drug molecules with deep learning can overcome the technical bottleneck of classical computer-aided drug design. It has become the frontier of new technique research on drug design, and has shown great potential in drug research and development practice. This review starts from the basic principles of deep learning-driven de novo drug design, goes on with the brief introduction to deep molecular generation techniques as well as computational tools and the analysis on representative successful cases, and eventually provides our perspective for future direction and application prospect about this technique. This review will provide ideas on new technique research and references for new drug research and development practice to which this technique is applied.

In order to improve the dissolution in vitro of components by processing tanshinone with the pray drying method, the physical properties of tanshinone power was analyzed by BET, differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction, and its dissolution in vitro was also investigated. The results of characterization showed decreased power size and increased specific surface area of tanshinone powder, and its existence in an amorphous state. Within 4 h, the accumulated dissolutions of tanshinone I and tanshinone II(A) in components of tanshinone reached 78.3%, 81.9%, respectively. Therefore, the spray-drying method was conducive to enhance the dissolution of components of tanshinone.
Chemistry, Pharmaceutical ; methods ; Diterpenes, Abietane ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Particle Size ; Solubility

OBJECTIVETo prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific delivery and rapid drug release.

METHODBaicalin-eudragit S100 solid dispersion was prepared by using the solvent method. The microscopic structure and physicochemical properties were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared spectroscopy (IR). And its in vitro release was also investigated.

RESULTThe results of DSC and XRD analysis suggested that baicalin may be dispersed in solid dispersion in the amorphous state. IR results indicated a non-covalent bond effect may exist between baicalin and eudragit S100. The results of in vitro release determination showed that very few baicalins in pH 1.2 diluted hydrochloric acid solution for 2 h at the baicalin-eudragit S100 ratio of 1 : 6. The accumulated dissolution rate was less than 15% in pH 6.8 phosphate buffer solution for 4 h, but exceeding 90% in pH 7.6 phosphate buffer solution for 1 h.

CONCLUSIONThe prepared baicalin-eudragit S100 solid dispersion could achieve the objective of colon-specific delivery and rapid drug release, and helps increase the concentration of baicalin in colons.

Colon ; metabolism ; Flavonoids ; chemistry ; Hydrogen-Ion Concentration ; Polymethacrylic Acids ; chemistry ; Solubility ; Solvents ; chemistry ; X-Ray Diffraction ; methods

To apply chitooligosaccharide in the preparation of baicalin compound, in order to increase the drug dissolution in vitro, and investigate the basic property of the compound. Baicalin-chitooligosaccharide compound was prepared by using the solvent method. The structure and physicochemical properties of compound were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared vibrational spectrum (IR), and its dissolution behavior was also investigated. The results showed that the compound prepared at baicalin-chitooligosaccharide molar ratio of 1 : 1 could significantly improve the dissolution of baicalin. The results of DSC and XRD analysis suggested that baicalin may exist in an amorphous state. IR results indicated the interaction between baicalin and chitooligosaccharide. The baicalin-chitooligosaccharide compound could significantly improve dissolution in vitro of drug.
Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Oligosaccharides ; chemistry ; Spectroscopy, Fourier Transform Infrared