The new HIV-1 NNRTI drug Etravirine (TMC125) and a promising drug candidate Rilpivirine (TMC278) in phase III clinical trial are compounds belonging to the diarylpyrimidine (DAPY) family. They are extremely high potent against both wild-type and many drug-resistant HIV-1 strains, providing new hope for HIV-infected patients who fail to use current drugs due to the emergence of drug-resistant HIV mutants. The discovery and development of DAPY derivatives as next-generation NNRTI drugs depend on multidisciplinary coordination and their success has encouraged new researches to explore more next-generation NNRTIs with new scaffolds. This review described the story of discovery and development of DAPY derivatives as next-generation NNRTIs and related progress.

Some conclusions drawn from explanatory randomized controlled trial (ERCT) lack practical value in application under real-world clinical settings, and there are also some limitations on the generalization of pragmatic randomized controlled trial (PRCT) results. In some countries, real-world studies (RWSs) have been conducted to explore the effectiveness and safety of clinical interventions or postmarketing drugs, which is a new tendency in clinical researches. By reviewing some RWSs carried out in Western countries, we sum up the basic characteristics of the research design, and discuss the differences and connections between PRCT and RWS. The design ideas of RWS are different from PRCT. Researchers in RWS tend to perform long-term evaluation based on large quantities of subjects and quite large sample and focus on outcome measures which are clinically meaningful. Strict control on data collection, management and analysis are very important to RWS and PRCT. Owing to the complexity of clinical interventions and evaluation, PRCT is not completely suitable for clinical researches in traditional Chinese medicine (TCM). It is an inevitable tendency to apply RWS in clinical trials of TCM. We can explore the efficacy of TCM interventions through PRCT, and better understand the effectiveness through RWS. RWS will become a powerful approach to TCM clinical trials and postmarketing evaluation of Chinese medicines.

Objective To study the standardization of similarity evaluation method of chromatographic fingerprints. Methods Computer simulation and HPLC method were used to investigate the characteristics of different similarity evaluation methods and the criteria of characteristic variables selection in chromatographic fingerprints. Results Cosine ratio and correlation coefficient should be the first choice for similarity calculation based on chromatographic peak area. Peak area is recommend to be used as the characteristic variable for chromatographic fingerprints. Conclusion The features of the commonly used chromatographic fingerprint evaluation methods are described and their range of application are defined.

Adult ; Carcinoma, Neuroendocrine ; metabolism ; pathology ; Diagnosis, Differential ; Female ; Hodgkin Disease ; metabolism ; pathology ; Humans ; Ki-1 Antigen ; metabolism ; Leukocyte Common Antigens ; metabolism ; Lung Neoplasms ; metabolism ; pathology ; surgery ; Lymphoma, Large B-Cell, Diffuse ; metabolism ; pathology ; Lymphoma, Large-Cell, Anaplastic ; metabolism ; pathology ; surgery ; Melanoma ; metabolism ; pathology ; Mucin-1 ; metabolism ; Pneumonectomy ; Poly(A)-Binding Proteins ; metabolism ; Receptor Protein-Tyrosine Kinases ; metabolism ; T-Cell Intracellular Antigen-1

Objective To study the correlation of TSH and the Heart-Qi Deficiency Syndrome (HQDS) in Coronary Heart Disease. Methods Plasma TSH level of patients with HQDS were measured with radioimmunoassy and were compared with that of N-HQDS group as well as normal control group. Results Plasma TSH has no significant difference among HQDS group, N-HQDS group and normal control group. Conclusion The level of plasma TSH was associated with coronary heart disease with HQDS.

Objective To study the value of echocardiography in the diagnosis of myocardial infarction(MI) and its complica tions.Methods The examination data in 140 cases of MI were collected from January 2012 to January 2016 and performed the analysis and comparison.Results In the ultrasound examination results in 140 cases,120 cases appeared varying degrees of segmental ventricular wall motion abnormalities,its diagnostic rate to MI was 85.71％,which of EKG was 78.57％,the MI detection rate of echocardiography and ECG combined examination was 90.71％,which was higher than that of single use of echocardiography or ECG.With the coronary angiogra-phy results as the control,the detection rate of echocardiography for the coronary arterial lesion sits was 82.86 ％.Among 140 cases of MI,22 cases of complications(15.71 ％) were de-tected out by echocardiography,including 7 cases of true ventricular aneurysm(5.00 ％),4 cases of left ventricular mural thrombosis(2.86 ％),1 case of ventricular septal perforation(0.71％) and 10 cases of ischemic mitral regurgitation(7.14％).Conclusion Echocardiography has higher accuracy in the MI diagnosis,com-bining with ECG can further improve the diagnostic rate.

BACKGROUND: Previous research has indicated that both insulin-like growth factor Ⅰ (IGF-Ⅰ) and basic fibroblast growth factor (bFGF) play an important role in cell proliferation and differentiation. However, the effect on biological characteristics of human dental papilla mesenchymal cells (hDPMCs) still remains unclear. OBJECTIVE: To research the effect of IGF-Ⅰ and bFGF on the proliferation and differentiation of hDPMCs.METHODS: hDPMCs were isolated and cultured in DMEM/F12 culture media containing 1% or 10% fetal bovine serum. The fourth-passaged hDPMCs were incubated in culture media containing 0, 0.1, 1, 10 and 100 μg/L bFGF and 0, 25, 50, 75 and 100 μg/L IGF-Ⅰ(0 μg/L as control group), respectively. At 96 hours after culture, proliferative activity was measured with MTT assay. The corresponding growth factor culture media were used in 10 μg/L bFGF group, 100 μg/L IGF-Ⅰgroup, bFGF + IGF-Ⅰ group, and control group, respectively. At days 1, 3, 5, and 7 after culture, the proliferative activity was detected using MTT assay, and alkaline phosphatase (ALP) activity was measured using modified enzyme kinetics method. RESULTS AND CONCLUSION: At the 0-100 μg/L mass concentration scope, both bFGF and IGF-Ⅰcould accelerate proliferation of hDPMCs, and the proliferation ability of bFGF was superior to that of IGF-Ⅰ; moreover, the combination of bFGF and IGF-Ⅰcaused a synergetic action to proliferation of hDPMCs. The maximal valid concentration of bFGF was 10 μg/L, and the maximal action concentration of IGF-Ⅰwas 100 μg/L. At 0-7 days, the effect of bFGF on the ALP activity of hDPMCs was not obvious, but the effect of IGF-Ⅰon ALP activity of hDPMCs became greater with the time passing; furthermore, the combination of bFGF and IGF-Ⅰcould generate a synergetic action on increasing the ALP activity.

Objective To investigate the effect of diazepam on blood-brain barrier ( BBB ) after radiation-induced brain injury. Methods Two hundred and forty healthy male SD rats weighing 240-270 g were randomly divided into 4 group with 60 animals in each group: Ⅰ D-R group received intraperitoneal diazepam 5 mg?kg-1 30 min before irradiation; Ⅱ N-R group received no diazepam before irradiation; Ⅲ D-SR group received intraperitoneal diazepam 5 mg? kg-1 30 min before sham irradiation and Ⅳ N-SR group received no diazepam before sham irradiation. The animals were placed in a prone position awake without any anesthetics. The whole brain was irradiated by 4 MeV electron beam at a single dose of 30 Gy. The changes in BBB were assessed by (1) magnetic resonance imaging (MRI) with the T1-weighted images, T2-weighted images and MRI enhancement images induced by Gd-DTPA; (2) Evans blue (EB) assay; 2% EB 3 ml?kg-1 was injected via femoral vein and 3 h later the animals were decapitated and EB content in the brain tissue was determined by spectrophotometry; (3) The expression of vascular endothelial growth factor (VEGF) in the brain tissue determined by immuno-histochemistry before irradiation ( T0 ) ( baseline) at 6 h (T1 ), 1 day ( T2 ) , 1 week ( T3 ) and 1 month ( T4 ) after irradiation.Results In group Ⅱ (no diazepam before irradiation) the signal intensity of T1-weighted images significantly decreased while the signal intensity of T2-weighted images and the enhancement rate significantly increased at T4. However in group Ⅰ (diazepam was given before irradiation) the changes in the MRI were significantly attenuated. The EB content at T1, T3 , T4 and the expression of VEGF at T1 , T, were significantly higher in group Ⅱ than in group Ⅰ . Conclusion Diazepam given before irradiation can protect BBB against irradiation injury by decreasing the expression of VEGF in the brain tissue and BBB permeability.

Objective To study the uptake property of punicalagin in Caco-2 cells.Methods Caco-2 cell monolayer model was used to research the effects of punicalagin on cell uptake in different times, concentrations, pH values, temperatures and P-gp inhibitors. HPLC was used to determine the content of punicalagin in cells.Results The linearity of punicalagin concentration curve was found in the range of 0.024 8-0.992μg (r=0.997 9). Uptake determination of punicalagin in Caco-2 cells absorbed a certain amount of time, concentration and pH dependence and P-gp inhibitors could significantly increase the punicalagin uptake.Conclusion This method is simple and sensitive to determine the punicalagin concentration in Caco-2 cells, which is mainly passively transported. P-gp is involved in punicalagin transport process.

Objective The High-performance thin-layer(HPTLC) chromatographic fingerprint of Saikosaponin from Chaihu(roots of Bupleurum chinense DC.) was established and fingerprints similarity of different species of Bupleurum spp.were evaluated.Methods High-performance thin-layer chromatography(HPTLC)were carried out.The chromatographic conditions were as follows:pre-coated HPTLC silica-gel plate as stationary phase,dichloromethane-methanol-ethyl acetate-water(30:40:15:3) as mobile phase(solvent system) and 2 %p-DMBA/10 %Sulfuric acid alcoholic solution as derivatization reagent.The common pattern of HPTLC fingerprints were obtained through’Chromafinger’solution software,and authentication and quality assessment were analyzed by similarity and Principle Component Analysis.Results The common pattern of the roots of Bupleurum chinense DC.consists of 19 characteristic peaks,and higher similarities existed between the roots of Bupleurum chinense DC(Bei Chaihu),B.falcatum(San-dao Chaihu) and B.scorzonerifolium Willd.(Nan Chaihu),but Nan Chaihu contains much lower total saponins than that in Bei Chaihu.The other species of Bupleurum demonstrated their different chemical distribution.The toxic species of B.longiradiatum can be easily differentiated from other spp.by comparison with the HPTLC images.Conclusion The survey showed that the main commodities of’Chaihu’in the domestic market can be attributed to’Bei Chaihu fingerprint-pattern’.The toxic species of B.longiradiatum can be easily differentiated from other spp.by comparison with the HPTLC images.