OBJECTIVE:To analyze the utilization and variation tendency of oral hypoglycemic agents in Wuhan area,and to provide reference for drug selection and enterprise production and sale. METHODS:The utilization of oral hypoglycemic agents in 34 hospitals from Wuhan area during 2011-2013 was analyzed statistically in respects of consumption sum,DDDs and DDC etc. RESULTS:The consumption sum and DDDs of oral hypoglycemic agents increased by 20% and 7% respectively year by year. Acarbose had a market share of over 40%. The drug use frequency of metformin ranked the second place only to acarbose. DPP-4 inhibitor had a promising future,with a consumption sum proportion of more than 10%,while the market share of traditional Chi-nese medicine had fallen below 3%. Except for repaglinide,gliclazide,glimepiride,Xiaoke pills,etc.,the selling of other medica-tions are consistent with the user. CONCLUSIONS:The utilization of oral hypoglycemic drugs is basically rational in 34 hospitals from Wuhan area during 2011-2013.

[Summary] Epigenetics defines heritable changes in gene expression that are not coded in the DNA sequence itself.Three systems,including DNA methylation,RNA-associated silencing and histone modification,are used to initiate and sustain epigenetic silencing.Type 2 diabetes mellitus(T2DM) is a polygenic disorder,which is caused by both genetic and environmental factors.However,pathogenesis of T2DM has not been elucidated.Recent studies have indicated that epigenetics may play an important role in the pathogenesis of T2DM,which is involved in the development and differentiation of β cell,secretion of β cell,insulin sensitivity and so on.Researches related to epigenetics may provide a new measure and target to clarify the pathogenesis of T2DM as well as prevent and treat the disease.

The PDB culture medium was selected to ferment the endophyte strain, and the secondary metabolites of endophytic fungi Penicillium polonicum were studied. Combined application of Sephadex LH-20, ODS and HPLC chromatographies over the ethyl acetate extract of the fermented culture led to the isolation of 6 compounds. By spectral methods, the structures were elucidated as [3, 5-dihydroxy-2-(7-hydroxy-octanoyl)]-ethylphenylacetate (1), (3, 5-dihydroxy-2- octanoyl)-ethyl phenylacetate (2), (5, 7-di- hydroxy-9-heptyl)-isobenzo pyran-3-one (3), 3-(hydroxymethyl) 4-(1E)-1- propen-1-yl-(1R, 2S, 5R, 6S)-7-oxabicyclo [4.1.0] hept-3-ene-2, 5-diol (4), (E)-2-methoxy-3-(prop-1-enyl) phenol (5) and p-hydroxylphenylethanol (6).
Biological Factors ; chemistry ; metabolism ; Endophytes ; chemistry ; isolation & purification ; metabolism ; Fabaceae ; microbiology ; Fermentation ; Penicillium ; chemistry ; isolation & purification ; metabolism ; Secondary Metabolism

Objective To investigate the clinical efficacy of Wumei Wan (Fructus Mume Pills) for diabetic gastroparesis with the syndrome of cold-heat mixture. Methods Sixty-eight diabetic gastroparesis patients with the syndrome of cold-heat mixture were evenly randomized into treatment group and control group. On the basis of treatment for controlling the blood glucose level, the treatment group was given oral use of Wumei Wan and the control group was given oral use of Cisapride. After treatment for one month, the therapeutic effect of both groups was evaluated, and the changes of gastrointestinal symptoms, gastric emptying, 2-hour postprandial glucose(2hPG), glycosylated hemoglobin(HbA1c), and fasting plasma glucose(FPG) in both groups were also observed. Results (1)The total effective rate of the treatment group was 88.24%, and that of the control group was 67.65%, the difference being significant(P<0.05). (2 ) After treatment , the scores of gastrointestinal symptoms of nausea and vomiting, gastric fullness, anorexia, belching and acid regurgitation, abdominal and gastric pain, diarrhea, and constipation in the treatment group were markedly improved(P<0.05 or P<0 . 01 compared with those before treatment ). In the control group, symptom relief was shown in nausea and vomiting, anorexia, and diarrhea(P<0.05). The treatment group had better effect on relieving nausea and vomiting, abdominal and gastric pain, diarrhea, and constipation than the control group(P<0.05 or P<0.01). (3)After treatment, 2hPG, FPG and HbA1c levels were obviously decreased in both groups(P<0.05 compared with those before treatment) , and the decrease in the treatment group was superior to that in the control group (P<0.05). (4)After treatment, half gastric emptying time, full gastric emptying time, and the contraction of gastric antrum were improved in both groups(P<0.05), and the improvement of gastric emptying in the treatment group was superior to that in the cont rol group(P<0.05). Conclusion Wumei Wan has better effect for the treatment of diabetic gastroparesis than western medicine Cisapride.

In the experiment of atherosclerosis, the change of the cerebrovascular dynamic indexes (CVDI) was observed. In the atherosclerosis group, the values of carotid artery's mean flow (Qmcan), mean velocity (Vmcan), maximal velocity (Vmax), minimal velocity (Vmin) and cerebrovascular compliance for zero pressure (CO) were significantly decreased (P

New drug research and development is a technology-intensive industry with high investment, high cycle and high risk. In recent years, with the rapid development of modern disciplines such as omics technology, bioinformatics, high-throughput and high-content screening, and artificial intelligence, the research and development of small-molecule drugs has presented a new paradigm characterized by "integrated medicinal chemistry". This review summarizes new enabling drug discovery technologies, the emergence of new subfields formed through integration innovations and practical chemistry toolbox in the field of medicinal chemistry.

Virus infection is a serious threat to human health and social development. The increase in pandemics caused by emerging and re-emerging viruses highlights the urgent need for broad-spectrum antivirals. In this perspective, we highlight recent case studies and summarize the universal strategies and methodologies in broad-spectrum antiviral drug discovery from common targets, common steps in viral life cycle, universal strategies, and broad-spectrum molecules, hoping to provide valuable guidance for the current and future development of antiviral drugs.

Objective To study the relationship between hepatitis B virus(HBV)pre-S gene mutations and progression of liver disease.Methods The entire pre-S1,pre-S2 genes were amplified hy nested polymerase chain reaction(PCR)and the products were digested by NlaⅢ.The method for detecting pre-S2 start codon mutation was established based on the digested restriction fragment length polymorphism(RFLP).Pre-S gene deletion was revealed by electrophoresis on polyacrylamide gel(PAGE).Pre-C A1896 and basic core promoter T1762/A1764 mutations were identified by direct sequencing of PCR products.The 138 sera from patients with HBV-related disease,including asymp- tomatic carriers(ASC),chronic hepatitis(CH),liver cirrhosis(LC),hepatocarcinoma(HCC),were tested by these methods.Results The detection rate of pre-S deletion mutation was higher in patients with HCC(56.3%)and LC(42.9%)than those with CH(11.8%)and ASC(8.1%,P

Objective To investigate the detection rate and possible factors of hyperhomocysteinemia(HHcy) in children with chronic kidney disease(CKD).Methods The clinical data of children with CKD between July 2012 and September 2016 in the Department of Pediatrics,Peking University First Hospital were retrospectively collected.The homocysteine(Hcy) level of patients were measured.The other data included the general information,diagnosis and laboratory test results.Results Seventy-six pediatric patients with CKD were enrolled including 49 boys and 27 girls.The average age of the patients was (9.9±3.4) years old.The main cause of the patients in the study was primary glomerulopathy(48.7%,37/76 cases),and the rest were congenital and inherited glomerular diseases(36.8%,28/76 cases),secondary glomerular diseases(9.2%,7/76 cases)and renal tubular diseases(5.3%,4/76 cases).Fifty patients (65.8%,50/76 cases) had normal level of Hcy which was 10.40(7.30,11.62) μmol/L.Twenty-six patients(34.2%,26/76) were detected with HHcy whose Hcy level was 17.93(16.76,24.11) μmol/L.The detection rate of HHcy in CKD stage 1,stage 2,stage 3,stage 4 and stage 5 was 13.9%(5/36 cases),22.2%(2/9 cases),50.0%(4/8 cases),57.1%(4/7 cases) and 68.8%(11/16 cases) respectively,and the detection rate increased with CKD stages and the difference was statistically significant (χ2=17.574,P<0.001).The level of Hcy was 10.05(7.04,12.47) μmol/L,11.75(10.78,16.44) μmol/L,13.73(10.09,18.23) μmol/L,15.81(11.12,20.71) μmol/L and 17.39(11.86,24.76) μmol/L in CKD stage 1,stage 2,stage 3,stage 4 and stage 5,respectively.The Kruskal-Wallis test revealed that the distribution of homocysteine in CKD stages had statistically significant difference(P=0.001).Multiple linear regression model showed that creatinine clearance was an independent predicator of HHcy.Conclusions In this study of the CKD patients,the detection rate of HHcy was high and increased with the progression of CKD.HHcy is mainly influenced by creatinine clearance in CKD.The level of Hcy should be monitored regularly in children with CKD and HHcy should be treated with proper measures.

Objective:To compare the effects ofpropofol and sevoflurane on the plasma thromboxane B2 (TXB2),endothelin-1 (ET-1) and D-dimer (D-D) levels of patients underwent posterior retroperitoneal laparoscopic surgery.Methods:84 cases of patients underwent post retroperitoneal laparoscopic surgery in our hospital from May 2015 to December 2016 were selected as research objectives and randomly divided into two groups with 42 cases in each group.The same anesthesia induction were provided for two groups,the observation group was given 2％～3％ sevoflurane for continuous inhalation,while the control group was given 4～12 mg/(kg·h) of propofol for continuous injection by pump.Both groups received remifentanil 10 μg/ (kg ·h) target-controlled infusion simultaneously.The levels of plasma TXB2,ET-1 and D-D in the two groups were measured after anesthesia induction (T0),at 0.5 h (T1),1 h (T2),1.5 h (T3) after pneumoperitoneum.Meanwhile,the anesthetic effects and adverse reactions were compared between two groups.Results:The time of consciousness disappearence,time of tracheal intubation,spontaneous breathing recovery time,eye opening time,verbal response time,orientation recovery time and extubation time of observation group were significantly shorter than those of the control group (P＜0.01).No significant difference was found in the occurrence of adverse reactions between two groups (P＞0.05).The plasma TXB2,ET-1 and D-D levels of both groups were gradually increased at T1,T2 and T3,and all were significantly higher than that at T0 (P＜0.01).The plsma TXB2,ET-1 and D-D levels at T1,T2 and T3 of observation group were significantly lower than those of the control group at same time (P＜0.01).Conclusion:Posterior laparoscopic surgery could cause different degrees of hypercoagulability of blood.Compared with propofol,sevoflurane could effectively inhibit the release of TXB2,ET-1 and D-D in anesthesia after retroperitoneal laparoscopic anesthesia,and play a better role of anticoagulation.