G protein-coupled receptor 119 (GPR119) has been a promising target for the treatment of type 2 diabetes. It can not only directly promote insulin secretion, but also indirectly increase insulin secretion by stimulating the release of glucose-dependent GIP/CLP-1 without causing hypoglycemia. The remarkable advantages of small molecule GPR119 agonists make it one of the research hotspots for the development of type 2 diabetes drugs. This article reviews the anti-diabetic small molecules based on the GPR119 target in the past five years.

The prostate-specific antigen (PSA) test contributes a lot to the diagnosis and treatment of prostate cancer (PCa) and, along with imaging-guided prostate biopsy, has improved the diagnosis rate of lower-risk PCa and the accuracy of its clinical staging. However, many questions and controversies remain as to the choice of optimal biopsy strategies. Scholars differ in views about how to utilize PCa-related biomarkers to optimize the detection of initial and repeat biopsies. This review focuses on the present status of and advances in transrectal ultrasound-guided biopsy for PCa.
Humans ; Image-Guided Biopsy ; methods ; Male ; Prostate ; pathology ; Prostate-Specific Antigen ; blood ; Prostatic Neoplasms ; pathology ; Ultrasonography, Interventional ; methods

The teaching of the Fermentation Engineering Experiment in normal university must serve for the basic education,placing students' creative spirit and practical ability in the first place.Therefore,teaching reform of the Fermentation Engineering Experiment under the background of new curriculum reform of basic education should be studied from the curriculum content,teaching methodology,training pattern and as-sessment system,in order to cultivate the normal-university students' research ability,working attitude,crea-tive and teaching ability.

Cloning, Molecular ; Escherichia coli ; genetics ; Hepacivirus ; genetics ; Humans ; Recombinant Fusion Proteins ; biosynthesis ; genetics ; immunology ; Viral Nonstructural Proteins ; biosynthesis ; genetics ; immunology

Based our previous work, twelve purine derivatives were designed and synthesized as dual modulators of GPR119 and DPP-4by conjugating the GPR119 activating and DPP-4 inhibiting fragments with the position 6 and 9 of purine core via an approach of merged pharmacophores. Compound 11, bearing 2-fluoro-4-methylsulphonyl anilide and cyanopyrrolidine moieties, exhibited the most potent GPR119 agonistic activities (EC₅₀ = 0.33 μmol·L^-1, IA = 71.1%) and DPP-4 inhibitory (58.4% inhibition at 10 μmol·L^-1, 21.2% inhibition at 1 μmol·L^-1) activities in the in vitro antidiabetic study. Subsequently, we performed studies on structure activity relationships and molecular docking to guide the further drug design.

ObjectiveTo explore the etiology and pathogenesis of Guizhitang syndrome， clarify the related suspicious cases debated by doctors in the past dynasties， and provide references for the clinical application of Guizhitang. MethodUnder the guidance of the "transformation in accord with constitution" theory， the etiology and pathogenesis of Guizhitang syndrome were analyzed by comparing the relevant articles in the classics such as Treatise on Cold Damage （Shanghanlun） and Synopsis of the Golden Chamber （Jingui Yaolue）. ResultGuizhitang syndrome not only refers to the greater yang wind-invasion syndrome. Instead， it can be divided into two categories， i.e.， exogenous Guizhitang syndrome and miscellaneous Guizhitang syndrome. The basic etiology of exogenous Guizhitang syndrome is internal blood deficiency or yin deficiency after severe diarrhea， which is the physical basis， namely the internal cause， while the wind is the external cause that results in cold. The basic etiology of miscellaneous Guizhitang syndrome is the deficiency of blood and body fluid without the external cause. The pathogenesis of Guizhitang syndrome is neither weak nutrient Qi and defensive qi nor strong nutrient Qi but weak defensive Qi. It attributes to weak nutrient qi and strong defensive qi or disorder of defensive Qi. The essence of the pathogenesis of Guizhitang syndrome is not ″exterior deficiency″ but ″deficiency of nutrient Qi″. ″Floating Yang and weak Yin″ does not refer to the pathogenesis， but the pulse. Yang refers to the Cun pulse and Yin refers to the Chi pulse. ConclusionThe etiology and pathogenesis of Guizhitang syndrome are controversial among ancient and modern doctors and textbooks. Many physicians annotate this problem but few pay attention to the constitution basis. According to the ″transformation in accord with constitution″ theory， the constitution is the internal basis for the formation of diseases and syndromes. The formation of Guizhitang syndrome is underpinned by the inherent constitution. ″Transformation in accord with constitution″ theory is helpful to understand the formation mechanism of Guizhitang syndrome. A new understanding of the etiology and pathogenesis of Guizhitang syndrome based on the ″transformation in accord with constitution″ theory is helpful to reveal the use principle of Guizhitang by ZHANG Zhong-jing. The exploration of the formation mechanism of various syndromes of six-meridian diseases and miscellaneous diseases， as well as the original idea of ZHANG Zhong-jing's prescriptions from the ″transformation in accord with constitution″ theory can provide a new idea for the understanding of ZHANG Zhong-jing's theory.

In the present study, a newly synthesized benzofuran lignan 4-formyl-2-(4-hydroxy-3methoxyphenyl)-5-(2-methoxycarbonyethyl)-7-methoxy-benzo [b] furan (ERJT-12) was tested for its antiproliferative activity on human tumor cells. The related mechanisms were also investigated. In vitro growth inhibitory effects of ERJT-12 on various cancer cell lines were determined by MTT assay. Cell cycle distribution and apoptosis were detected by flow cytometry. The integrity of DNA was assessed by agarose gel electrophoresis. Activation of Caspase-3/7 and Caspase-6 was measured by colorimetric assay. The expressions of cell cycle proteins cell divide cycle 25c (Cdc25c), cyclin dependent kinase 1 (CDK1), CyclinB1 and apoptosis-related proteins Bax and Bcl-2 were detected by Western blotting. MTT assay showed that ERJT-12 inhibited the proliferation of several cancer cell lines including multidrug resistant cells. MCF-7 cells were markedly arrested at gap2/mitosis (G2/M) phase after treatment with ERJT-12 and progressed into apoptosis. The increased activities of Caspase-3/7 and Caspase-6 in MCF-7 cells were observed. The expression of CyclinB1 was down-regulated. The activities of Cdc25c and CDK1 protein were suppressed and Bcl-2 protein was phosphorylated. ERJT-12 displays potent antiproliferative activity towards cancer cells through suppressing cell cycle proteins, arresting cell cycle at G2/M phase and inducing apoptosis. It might be a novel candidate for cancer therapy.
Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Benzofurans ; pharmacology ; CDC2 Protein Kinase ; metabolism ; Caspase 3 ; metabolism ; Caspase 6 ; metabolism ; Caspase 7 ; metabolism ; Cell Cycle Proteins ; metabolism ; Cell Division ; drug effects ; Cell Line, Tumor ; Cyclin B ; metabolism ; Cyclin B1 ; G2 Phase ; drug effects ; Humans ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; bcl-2-Associated X Protein ; metabolism ; cdc25 Phosphatases ; metabolism

BACKGROUNDGranulocyte colony-stimulating factor (G-CSF) seems to improve cardiac function and perfusion when used systemically through mobilization of stem cells into peripheral blood, but results of previous clinical trials remain controversial. This study was designed to investigate safety and efficacy of subcutaneous injection of G-CSF on left ventricular function in patients with impaired left ventricular function after ST-segment elevation myocardial infarction (STEMI).

METHODSThirty-three patients (22 men; age, (68.5 +/- 6.1) years) with STEMI and with comorbidity of leukopenia were included after successful primary percutaneous coronary intervention within 12 hours after symptom onset. Patients were randomized into G-CSF group who received G-CSF (10 microg/kg of body weight, daily) for continuous 7 days and control group. Results of blood analyses, echocardiography and angiography were documented as well as possibly occurred adverse events.

RESULTSNo severe adverse events occurred in both groups. Mean segmental wall thickening in infract segments increased significantly at 6-month follow up compared with baseline in both groups, but the longitudinal variation between two groups had no significant difference (P > 0.05). The same change could also be found in longitudinal variation of wall motion score index of infarct segments (P > 0.05). At 6-month follow-up, left ventricular end-diastolic volume of both groups increased to a greater extent, but there were no significant differences between the two groups when comparing the longitudinal variations (P > 0.05). In both groups, left ventricular ejection fraction measured by echocardiography ameliorated significantly at 6-month follow-up (P < 0.05), but difference of the longitudinal variation between two groups was not significant (P > 0.05). When pay attention to left ventricular ejection fraction measured by angiocardiography, difference of the longitudinal variation between groups was significant (P = 0.046). Early diastolic mitral flow velocity deceleration time changed significantly at 6- month follow-up in both groups (P = 0.05).

CONCLUSIONSMobilization of stem cells by G-CSF after reperfusion of infarct myocardium is safe and seems to offer a pragmatic strategy for recovery of myocardial global function.

Aged ; Angiocardiography ; Coronary Angiography ; Echocardiography ; Female ; Granulocyte Colony-Stimulating Factor ; adverse effects ; pharmacology ; therapeutic use ; Humans ; Leukopenia ; drug therapy ; Male ; Middle Aged ; Myocardial Infarction ; drug therapy ; therapy ; Ventricular Function, Left ; drug effects

Objective To study the prevalence and characteristics of blood pressure (BP) among children and adolescents at normal weight but with abdominal obesity.Methods Using data from the ‘Student physical fitness and health surveillance 2010 project' in Shandong province,a total of 38 816 students aged 7-17 years were selected to participate in this study.Stature,body weight,waist circumference (WC),systolic blood pressure (SBP) and diastolic blood pressure (DBP) of these subjects were measured.Body weight status and abdominal obesity were defined by body mass index (BMI) and WC,respectively.Results In total,the proportions of thinness,normal weight,overweight and obesity defined by BMI were 5.37％,72.47％,12.92％ and 9.24％ respectively.5.86％ of the children and adolescents with normal weight had abdominal obesity,with normal weighted girls (7.19％) having higher prevalence of abdominal obesity than boys (4.33％) (P＜0.01).The Z-scores of SBP and DBP for both boys and girls were all significantly higher in the normal weight but with abdominal obesity groups than in both normal weight and WC groups (P＜0.01).Conclusion Children and adolescents under normal weight but with abdominal obesity had higher BP level need to be identified and considered as high-risk individuals.Related intervention programs should also be targeted to this population.

Objectives To analyze the fatality and causes of death related to comprehensive prevention and care programs among HIV-infected patients in Dehong prefecture of Yunnan province,from 1989 to 2010. Methods Data on HIV/AIDS death cases in Dehong prefecture were extracted from the "Chinese National Comprehensive HIV/AIDS Prevention and Care Information System" and were analyzed. Results From 1989 to the end of 2010,a total of 13 493 HIV/AIDS cases registered as local residents or currently living m Dehong, had been reported. Among them, 8569 were reported as HIV cases with 2036 deaths and the other 4924 were reported as AIDS cases with 2251 deaths. A few of the cases had survived for 15-20 years. By the end of 2010, the number of deaths was higher than the number of survivors among HIV/AIDS cases reported before 2004, whereas the number of survivors was higher than the number of deaths among HIV/AIDS cases reported in 2004 and there after. During the twenty years' period,the proportion of reported HIV/AIDS cases died in the same year showed a secular trend of being low-highest-low, rising up to ＞ 10.0％ in 200 1, peaking at 18.9％in 2003 and then continuously going down to 5.8％ in 2010. The proportion of HIV/AIDS cases who survived at the beginning but died later in the year was going down since 2007. The proportion of HIV/ AIDS deaths died directly from AIDS was increasing whereas the proportion of HIV/AIDS deaths dying directly from overuse of drugs was decreasing in the recent years. Among HIV/AIDS deaths, the proportion of ever received CD4 + T-cell testing and the proportion of ever having received antiretroviral treatment were also increasing in the past years, reaching to 89.9％ and 25.5％ in 2010,respectively. Conclusion The case fatality of HIV/AIDS was decreasing in the past years in Dehong prefecture. More efforts were needed to scale up the CD4 + T-cell count testing and antiretroviral treatment in order to further reduce both morbidity and mortality among HIV/AIDS patients in Dehong prefecture. It is critical to improve surveillance program on HIV/AIDS deaths in the rural