Objective To study effect of pentanuclear copper complexes of imino acetic acid two aromatic derivatives on oxidative cutting DNA. Methods Synthesized complexes later, protonation constants and the stability constants of the complexes were determined by potentiometric titration method, the cutting DNA was studied by agarose gelelectrophoresis.Results Under physiological conditions, complexes H4L1, H4L2, between H6L3 and Cu2 +coordination capability was stronger; three carboxylic multi copper complexes in Cu2 + concentration cutting efficiency were higher than the corresponding mononuclear copper complexes, synergistic effect exists between Cu2 + Center; H6L3 complexes of the three DNA cut the highest efficiency, complex H4L1 was followed, complex H4L2 cutting efficiency was the lowest.Conclusion Change the complex chelating ligands has great influence on the properties of complex, which provides a theoretical basis for the design and synthesis of copper nucleases reasonable.

Objective: To optimize the formula and preparation process of docetaxel-loaded pluronic P123 micelles. Methods:Docetaxel-loaded pluronic P123 micelles were prepared by a thin-film hydration method and optimized by central composite design and response surface methodology. The influencing factors including the quantity of docetaxel, volume of organic phase, volume of hydra-tion and temperature of hydration were investigated with the entrapment efficiency as the index. The morphology of micelles was ob-served under a transmission electron microscope. The particle diameter and zeta potential were determined. The in vitro release property was measured by a dialysis method. Results:The relationship between the influencing factors and the evaluation parameter was fitted by multi-linear equation, quadratic polynomial equation and cubic polynomial equation, respectively. The results showed that the cubic polynomial equation was superior to the others according to the correlation coefficient. Docetaxel-loaded pluronic P123 micelles were spherical with the mean diameter, zeta potential, polydispersity index, encapsulation efficiency and drug loading of 108. 3 nm,-3. 99 mV, 0. 265, (97. 91 ± 0. 28)% and (3. 72 ± 0. 12)%, respectively. The cumulative release in vitro reached 95. 03% in 120 h, and docetaxel-loaded pluronic P123 micelles had notable sustained-release property. Conclusion: The technical process for do-cetaxel-loaded pluronic P123 micelles is simple and usable, and docetaxel-loaded pluronic P123 micelles show high encapsulation effi-ciency and notable sustained-release property.

Congenital heart disease is one of the most common birth defects, which is the main cause of death in children.Cardiovascular development is a complex process involving multiple genes, signaling pathways and regulatory factors.According to the sequencing of human genome and encode project, more than 80% of the genes in the genome are transcribed, but only 3% of these transcripts correspond to protein-encoding RNA.It is pointed out that non-coding RNA is as important or even more important as encoding RNA.More and more evidences show that not only encoding genes are involved in the regulation of cardiovascular development, but also protein non-coding genes play an important role in the development of heart.This review will summarize the biological characteristic and function of long noncoding RNAs, and introduce the role of some representative lncRNA in heart development and congenital heart disease.

0.05). But the LDH 5 and LDH 5/LDH 1 of difference doses of Shenmai Injection group was lower than that of the control group obviously(P

OBJECTIVE:To establish UV-spectrophotometry method in the determination of metformin hydrochloride in compound metformin hydrochloride tablets.METHODS:The determination was carried out with water as the solvent under the detection wavelength of233nm.RESULTS:There was a good linear relationship between metformin hydrochloride and its absorbability(r=0.9999)within the concentration range of1～10?g/ml.The average recovery was99.3%with RSD at0.24%(n=9).CONCLUSION:The method is accurate,fast,convenient,and which can be used to determine the contents of metformin hydrochloride in compound metformin hydrochloride tablets directly without isolation.

To study on teaching method to improve the stomatology clinical operation skill,this article summarizes the advantages and disadvantages of multimedia and mutual action applied in stomatology clinical operation.Multimedia is a kind of super-media developing with the progress of computer techniques,and can increase positive study while the teaching method of mutual action can arouse enthusiasm in operation skill training of stomatology clinical skill,thus enhancing the efficiency of studying skill.

In the face of escalating problems with pathogen control, the development of proper formulations of existing antibiotics is as important as the development of novel antibiotics. Daptomycin is a lipopeptide antibiotic with potent activity against Gram-positive bacteria. Currently, only injectable solution of daptomycin has been approved for clinical use. In the present study, the formulation of PEGylated liposomal daptomycin (PLD) was prepared and optimized, and its efficacy against methicillin-resistant Staphylococcus aureus (MRSA252) strains was investigated. The obtained PLD had a mean vesicle diameter of (111.5 +/- 15.4) nm and a mean percent drug loading of (5.81 +/- 0.19) % with high storage stability. Potent activity of PLD against MRSA was demonstrated in vitro with a more sustained effect than that of conventional liposomal daptomycin and daptomycin solution. In addition, intravenous administration of a single dose (equal to human use) of PLD significantly increased the survival of mice in a MRSA252 systemic infection model compared with other formulations. Drug distribution in the lung was significantly enhanced following administration of PLD, and no measurable tissue lesions or pathological changes were detected during PLD treatment. Taken together, PEGylated liposomes loaded with daptomycin may represent a promising approach to reduce MRSA252 infections, especially those involving bloodstream dissemination, such as hematogenous pulmonary infection.
Animals ; Anti-Bacterial Agents ; pharmacology ; Daptomycin ; pharmacology ; Liposomes ; Methicillin-Resistant Staphylococcus aureus ; drug effects ; Mice ; Staphylococcal Infections ; drug therapy

The aim of this study was to detect the localization and level of tyrosine phosphorylated proteins during in vitro capacitation of guinea pig sperm. Sperm from mature guinea pigs were incubated in modified TALP under 5% CO_2 in air at 37 ℃. The capacitation effect was assessed by chlortetracycline (CTC) staining. Western blotting and indirect immunofluorescence were used to analyze the level and localization of tyrosine phosphorylation. The results showed that guinea pig sperm underwent a time-dependent increase in protein tyrosine phosphorylation during the in vitro capacitation and the percentage of protein tyrosine phosphorylated sperm increased from 36% to 92% from the beginning of incubation to 7h incubation. Also, there was a shift in the site of phosphotyrosine-specific fluorescence from the head of sperm to both the head and the flagellum of sperm. Moreover, there were three proteins phosphorylated in this experiment. After 0 to 0.5h incubation, the protein of 40kDa was detected by anti-phosphotyrosine monoclonal antibody, and the intensity of this protein increased in the following incubation. Then, after 1h incubation, another protein of 80kDa was found and the level of this protein reached the highest point at 3h. Also, in 3h incubation, a protein of 45kDa was detected and the intensity of this protein increased in the following incubation.

In this study, we developed a novel liposome-silica hybrid nano-carrier for tumor combination therapy via oral route, using paclitaxel and cyclosporine as a model drug pair. Optimization of the preparation of the drug-loading formulation and characterization of its physicochemical parameters and drug release profile were performed in vitro. Then in vivo pharmacodynamics and pharmacokinetics studies were performed. The results showed that the obtained formulation has a small particle size (mean diameter of 100.2 +/- 15.2 nm), a homogeneous distribution [the polydispersity index was (0.251 +/- 0.018)] and high encapsulation efficiency (90.15 +/- 2.47) % and (80.64 +/- 3.52) % for paclitaxel and cyclosporine respectively with a mild and easy preparation process. A sequential drug release trend of cyclosporine prior to palictaxel was observed. The liposome-silica hybrid nano-carrier showed good biocompatibility in vivo and co-delivery of cyclosporine and paclitaxel significantly enhanced the oral absorption of paclitaxel with improved anti-tumor efficacy, suggesting a promising approach for multi-drug therapy against tumor and other serious diseases via oral route.
ATP-Binding Cassette, Sub-Family B, Member 1 ; antagonists & inhibitors ; Administration, Oral ; Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacokinetics ; pharmacology ; Biological Availability ; Cyclosporine ; administration & dosage ; pharmacokinetics ; pharmacology ; Drug Carriers ; chemistry ; Female ; Liposomes ; chemistry ; Male ; Mice ; Nanoparticles ; Neoplasm Transplantation ; Paclitaxel ; administration & dosage ; pharmacokinetics ; pharmacology ; Particle Size ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Sarcoma 180 ; pathology ; Silicon Dioxide ; chemistry ; Tumor Burden ; drug effects