The current prevalence of cancer chemotherapy drugs is inefficient and highly toxic, thus selecting the appropriate new forms of cancer treatment has become one of the important tasks. On the basis of domestic and foreign research literature, cutline the composition, characteristics and main preparation methods of polymeric micelles. Introduced varieties of stimuli-responsive polymer micelles, as well as targeted polymeric micelles used as an anticancer drug carrier. By making use of inside microenvironment of tumor cells, the preparation of various of new intelligent polymeric micelles with slight side effects and good treatment in virto and in vivo, can achieve effective control of drug release, which has great development and prospect in application.

Peptide cyclization, a pivotal approach to modifying linear precursors of proteins and pepticles, has been used to enhance their biological activities and serum stabilities. Recently, sortase A (SrtA) from Staphyloccus aureus becomes a promising new technology for efficiently incorporating site specific modifications into proteins, conjugating the cell surface and cyclizing the linear peptides. In this study, we constructed two recombinant expression systems, one with chitin binding domain and the other with six-histidine tag and chitin binding domain on the N-terminal of SrtA, separately. The results of enzymatic kinetics indicate that the two recombinant tags do not impair the transpeptidase activity of SrtA compared with the standard reaction reported under the same reaction condition. The two synthesized peptides with N-ternimal three glycines and C-terminal penta-amino acid motif, LPETG, were cyclized using immobilized and recycled SrtA. The SrtA-based cyclization promises to represent a simple method for easy and efficient enzymatic synthesis of large cyclic peptides.
Aminoacyltransferases ; metabolism ; Bacterial Proteins ; metabolism ; Cyclization ; Cysteine Endopeptidases ; metabolism ; Enzymes, Immobilized ; metabolism ; Kinetics ; Peptides ; metabolism ; Peptides, Cyclic ; biosynthesis ; Staphylococcus aureus ; enzymology

The aim of this study is to develop the Tripterygium glycosides nanoemulsion gels and investigate its pharmacodynamics. Oleic acid was used as oil phase, polyoxyethylene castor oil as surfaetant, and 1,2-propanediol as cosurfactant to screen the formula of Tripterygium glycoside nanoemulsion using the pseudo-temary phase diagrams. Then the nanoemulsion gels was prepared. The ICR mouse ears were sensitazated by 7% DNCB, and then were excited by 0.3% DNCB to stimulate the model of mouse chronic dermatitis and eczema. The concentrations of IFN-γ, IL-4 and IL-8 in mouse blood were determined by ELISA. The results showed that Tripterygium glycosides nanoemulsion gels could significantly inhibit the swelling of mouse ears(P < 0.01) and ameliorate the edama and erythema of model mouse ears skin. Also it could significantly decrease the expression of IFN-γ and IL-4 in model mouse blood. Tripterygium glycosides nanoemulsion gels had a good therapeutic effect on mouse model of dermatitis and eczema. It was expected to provide a new and long-acting exterernal preparation for the treatment of dermatitis and eczema.
Animals ; Chemistry, Pharmaceutical ; instrumentation ; methods ; Dermatitis ; drug therapy ; immunology ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Emulsions ; chemistry ; Female ; Glycosides ; chemistry ; pharmacokinetics ; Humans ; Interleukin-4 ; immunology ; Interleukin-8 ; immunology ; Mice ; Mice, Inbred ICR ; Nanoparticles ; chemistry ; Tripterygium ; chemistry

To investigate the effect and possible mechanism of echinacoside-containing serum on the osteogenic differentiation in rat bone marrow mesenchymal stem cells. Rat bone marrow mesenchymal stem cells were cultivated by the whole bone marrow adherence method. The 3rd generation of cells were divided into 3 groups: the blank control group, the classic osteogenic-induced group and the 10% echinacoside-containing serum group. The expression of alkaline phosphatase and osteocalcin were detected by ELISA. The ex- pression of ZHX, protein was detected by Western blot technique. RT-PCR technique was used to detect the expression of ZHX₃mRNA. According to the result, the expressions of the alkaline phosphatase and osteocalcin in the classic osteogenic-induced group and the 10% echinacoside-containing serum group were significantly higher than that of the blank control group (P <0. 01). And expressions of the alkaline phosphatase activity and osteocalcin in the 10% echinacoside-containing serum group were significantly higher than that in the classic osteogenic-induced group (P < 0.01). Meanwhile, the classic osteogenic-induced group and the 10% echinacoside-containing serum group showed obviously higher ZHX₃ protain and mRNA expression than that of the black control group, with significant differences (P < 0.01); the 10% echinacoside-containing serum group showed obviously higher ZHX₃ protain and mRNA expression than that of the classic osteogenic-induced group, with a significant difference (P < 0.01). In conclusion, 10% echinacoside-containing serum can promote the differentiation of the bone marrow mesenchymal stem cells cultured in vitro. Its mechanism may be correlated with the increase in the ZHX₃expression.
Animals ; Cell Differentiation ; drug effects ; Cell Proliferation ; drug effects ; Cells, Cultured ; Female ; Glycosides ; blood ; pharmacology ; Homeodomain Proteins ; genetics ; metabolism ; Male ; Mesenchymal Stromal Cells ; cytology ; drug effects ; metabolism ; Osteogenesis ; drug effects ; Rats ; Rats, Sprague-Dawley ; Serum ; chemistry ; Transcription Factors ; genetics ; metabolism

AIM: To determine the concentration of escitalopram in human plasma by HPLC-MS/MS and investigate the pharmacokinetics of escitalopram. METH-ODS: The method involved protein precipitation with methanol. The chromatographic separation was achieved within 6.0 min by using methanol-water with 15 mmol·L-1 ammonium acetate-formic acid (72:28:O.1, v/v/v) as mobile phase and a Lichrospher CN 150 mm×4.6 mm analytical column. The analytes were detected using an electrospray ionization tandem mass spectrometry in SRM mode. Detection of the ions was performed by monitoring the transitions of m/z 325.0 to 234.0 for escitalopram and m/z 409.1 to 238.1 for amlodipine (intemal standard), respectively. RESULTS:The standard curve was linear ( r = 0. 999) over the concentration range of 0.20 - 50.00 ng· ml- 1. Accuracy and precision were below the acceptance limits of 15%. The recoveries of escitalopram ranged from 96.0% to 103.6%. The lower limit of quantification for escitalopram was 0.20 ng· ml-1 using 200 μl plasma sample.The pharmacokinetic parameters of escitalopram after a single oral dosing of escitalopram oxalate tablet (10 rog)to ten healthy male volunteers were achieved. The Cmax, Tmax, AUC0-t, AUC0-∞, t1/2 and Ke of escitalopram were 9.21±2.10 ng·ml-1 , 3.75±1.04 h, 514.6±152.3 ng·h·ml-1 ,540.5±162.3 ng·h·ml-1 , 34.06±7.71 h and 0.021±0.004 h-1,respectively. CONCLUSION:The determination of concentration of escitalopram in human plasma by HPLC-MS/MS method was repid, sensitive and reliable. It can be used for clinical pharmacokinetic study of escitalopram.

OBJECTIVE: To understand the prevalence rate and the relativity of allergic rhinitis and recurring respiratory infection of preschool children in Shenzhen, and to investigate and analyse the prevalence rate, predisposing factor, allergen, therapy, turnover on allergic rhinitis and recurring respiratory infection of preschool children. METHOD: The ENT doctors examined the investigated children and recorded them, then delivered questionnaires to the children's parents and explained to them. The result was analyzed statistically. RESULT: The prevalence rate of allergic rhinitis of preschool children in Shenzhen was 20.1%, the prevalence rate of recurring respiratory infection was 13.7%, the prevalence rate (18.0%) of allergic rhinitis combined recurring respiratory infection was higher than that (7.80) of cases with non-allergic rhinitis combined recurring respiratory infection. The difference had a statistical significance (P < 0.05). CONCLUSION We initially understood the epidemiologic situation of allergic rhinitis and recurring respiratory infection of preschool children in Shenzhen, providing epidemiologic datas for the standardization of prevention and cure for allergic rhinitis.
Allergens ; Child, Preschool ; China ; epidemiology ; Humans ; Respiratory Tract Infections ; epidemiology ; Rhinitis, Allergic, Perennial ; epidemiology ; Rhinitis, Allergic, Seasonal ; epidemiology ; Surveys and Questionnaires

AlM: To introduce a new color pediatric visual acuity chart and its clinical application.
METHODS:The color pediatric visual acuity chart was designed based on principle of visual angle. The optotype on the color chart had graphics. The progression rate of optotype size between 2 lines was 10 10 and 1. 2589. A regular geometric progression of optotype sizes and distribution was employed to arrange 8 lines with 11 optotype on the color chart. The testing distance was 3m. The visual acuity score could be recorded as logarithm of the minimum angle of resolution notation or decimal notation. The reliability of naked distant measurements with this new chart was tested in one eye of 100 children (4 ~ 6 years old) taking the Chinese national standard logarithm visual acuity chart standard.
RESULTS: The color pediatric visual acuity chart and logarithmic chart controls, visual acuity test results that in the two groups had no significant difference (t=1. 2671, P> 0. 05 ). Two sets of vision data existed positive correlation (r= 0. 924, P<0. 01). Cooperation rate was 100%, the recognition rate was more than 90%.
CONCLUSlON:Children are easier to accept used new color pediatric visual acuity chart to inspect vision. New chart is reliability and apply to children's vision screening.

Objective To further evaluate the efficacy and safety of rivaroxaban in the thromboprophylaxis after orthopedic surgery.Methods PubMed,EmBase,Cochrane Library,Web of Science,Clinical Trials,CNKI,CBM and Wanfang database were systematically searched.All databases had been searched from established up to August 2016.All randomized controlled trials (RCTs) of rivaroxaban therapy in patients after orthopedic surgery were selected.Meta-analysis was carried out by using RevMan 5.3 software.The incidence of total venous thromboembolism (VTE),major VTE,deep vein thrombosis (DVT),pulmonary embolism (PE),all-cause mortality,symptomatic VTE,bleeding,major bleeding,clinical relevant non-major bleeding (CRNMB),minor bleeding and wound complication were compared and the results were presented with risk ratio (RR) with 95％ confidence interval (CI).Results Totally 32 RCTs of 17061 cases were included in this study,including 9167 cases accepted rivaroxaban (treatment group),other of 7894 cases accepted other drugs (control group).The results of Meta-analysis were as follows.The incidence of symptomatic VTE,total VTE,major VTE and DVT in the rivaroxaban group was lower than that in the low molecular heparin group (P ＜ 0.05).The incidence of total VTE,and DVT in rivaroxaban group was lower than that in aspirin group (P ＜ 0.05).There was no significant difference in the efficacy and safety between the rivaroxaban and apixaban group (P ＞ 0.05).Conclusion In the thromboprophylaxis after orthopedic surgery,efiicacy of rivaroxban is better than that of traditional anticoagulant therapy and it will not increase the risk of adverse events such as bleeding and wound complication.

AIMTo assess the parameters of cardiac structure and function of male Balb/c mice by the echocardiography.

METHODSA total of 27 male Balb/c mice (from five to seven week old) were examined with a 13-MHz transthoracic linear-array transducer, hearts were removed from mice anesthetized with Nembutal, and the left ventricular (LV) mass were weighed.

RESULTSComplete 2-dimensional echocardiography for cardiac structure and function were obtained. Hemodynamic parameters were recorded. A correlation existed between LV weight (x) and echocardiographic LV mass (y) with the 2D) guided M-mode method: y = 1.15x + 3.26, (r = 0.80).

CONCLUSIONEchocardiography appears to be a promising approach for noninvasively assessing LV mass and function in mice.

Animals ; Echocardiography ; Heart ; physiology ; Heart Ventricles ; diagnostic imaging ; Male ; Mice ; Mice, Inbred BALB C ; Ventricular Function, Left

Objective To explore the thinking and methods of integration curriculum. Methods The content of theory and experiment of the biochemistry,molecular biology, cell biology, medical genetics are optimized, streamlined and integrated to form theory course and experiment experimental course of " basis fo life", namely"four in two". Forming a teaching team across departments, multi-disciplinary teaching is carried out. The theory takes " cell-moleculeinheritance-disorders" as the main line, interspersed with " flipped class model" . The experimental course deletes repeated confirmatory experiments and adds some comprehensive experiments. The course assessment and performance evaluation are carried out with the combination of formative assessment and summative evaluation. Results The teaching mode of integration curriculum has been carried out in the experimental class of undergraduate students for two years. Compared with the theoretical examination scores, the results of the experimental class were significantly higher than that of the control class, and the difference was statistically significant (P＜0.05) . 24 students took part in research in experimental class, but only 10 students did in control class.Conclusion The implementation of integrated curriculum can promote student’s independent learning, improve student’s ability to analyze and solve problems, and mobilize student’s interest in scientific research practice. It provides useful reference and experience for the integration of basic course in the life science field of higher medical colleges.