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.

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 To observe the acute side effects and recent therapeutical effect of cisplatinum/paclitaxe concurrent radiotherapy for patients with advanced nasopharyngeal carcinoma.Methods 87 patients with advanced nasopharygeal carcinoma were enrolled.According to the treatment,87 patients were divided into paclitaxe group (groupA,n =43) and cisplatinum group (group B,n =44).The two groups were treated with 6MV-X ray for radiotherapy.The prescription dose of radiation therapy was PGTV,PGTVnd 6 996 cGy/33F,PTV1 6 006 cGy/33F,PTV2 5 096 cGy/28F.The two groups began concurrent chemotherapy in radiotherapy,specific method:group A paclitaxe 30mg/m2,1 time a week,until the end of radiotherapy,group B cisplatinum 80 ～100 mg/m2,every 21 days.Results The recent therapeutical effect of nasopharyngeal lesions and lymph nodes of neck for group A and group B were 88.4％ and 86.4％ (x2 =0.079,P =0.778),88.4％ and 88.6％ (x2 =0.000,P =1.000),respectively.But the occurrence rate of group B ' oral mucosa reaction (x2 =4.295,P =0.038) and gastrointestinal reaction (x2 =4.482,P =0.028) were higher than that of group A.Conclusion Treated with cisplatin in advanced nasopharyngeal carcinoma after radical radiotherapy combined with docetaxel is similar,and the side effect is low,the tolerance of patients is good,curative effect is satisfied.

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 evaluate the efficacy of pramipexole and levodopa/benserazide in treatment of advanced Parkinson's disease.Methods 50 patients with advanced Parkinson's disease were randomly divided into two groups,25 cases in the control group,others in the treatment group.The patients in the control group were treated with levodopa/benserazide and placebo,while those in the treatment group were given pramipexole and levodopa/benserazide.The treatment lasted 16 weeks.The clinical effects before and after the treatment were observed and compared. Results Compared with the control group,the treatment group experienced significant drops in the score of the Unified Parkinson's Disease Rating Scale(UPDRS)(P＜0.05).The clinical efficacy was significantly improved(84.0%vs36.0%)(χ2=10.08,P＜0.01).Conclusion The clinical effect of pramipexole and levedopa/benserazide in treatment of advanced Parkinson's disease was satisfactory,and it should be widely applied.