DPP-4 inhibitors are new oral hypoglycemic drugs and hot spots developed and launched in recent years, and they pro-vide new choices for the clinical treatment of type 2 diabetes. In China, DPP-4 inhibitors that are approved to use in the treatment of type 2 diabetes are all imported products currently. In the paper, the current intellectual property situation of DPP-4 inhibitors that are developed and approved at home and abroad is researched and analyzed. Reasonable use of the patent information of DPP-4 inhibitors that is about to expire or have failed can provide good guidance for the subsequent development of DPP-4 inhibitors in domestic with promising curative effect and good market prospects, and can generate new patents in order to enhance the market competitiveness.

Objective To explore the TCM syndrome characteristics of cardiac syndrome X(CSX).Methods The signs and symptoms of 51 patients with CSX were analyzed according to the diagnosis of TCM syndromes to summarize their syndrome character- istics.Results of the 51 CSX cases,the following signs and symptoms took dominance:chest pain,fullness in chest,epigastric and abdominal distention,emotional distress,dark purple tongue with petechia,greasy coating,string-taut pulse.The syndromes were mainly of Biao-Superficial excess,including qi stagnation,phlegm retention and blood stasis,occupying 66. 7%,accompanied with Benroot deficiency,including qi deficiency,yin deficiency,qi and yin both deficiency,occupying 33.3%.Conclusion Qi stagnation, phlegm retention and blood stasis are the primary syndromes of CSX.

ObjectiveTo investigate the mechanisms of N-acetylcysteine protection against liver injury caused by biliary tract obstruction in rats. MethodsSeventy-two Wistar rats were divided randomly into the following three groups: (1) Rats received choledochus ligationon and N-acetylcysteine by intraperitoneal injection (DBL+NAC); (2) Rats received choledochus ligationon only; (3) sham operation. Six rats were killed each time after 1 d, 3 d, 5 d and7 d and their liver function was tested by TBA-40FR Automatic Chemistry Analyzer. In addition, NO production was detected by Griess Reagent System. ResultsWhen the period of biliary duct obstruction is extended, serum AST,ALT,TBIL, DBIL, NO and TNF-α increase but the increase in serum ALT,AST,NO and TNF-α(P＜0. 05) is more prominent in group DBL than group DBL+NAC at any given time. Conclusions N-acetylcysteine can effectively protect against liver injury in rats with obstructive jaundice, and this may be achieved through down-regulation of TNF-α and NO in hepatocytes.

Polymyxin E shows effective treatment of the infection induced by resistant gramnegative bacteria, but its nephrotoxicity severely limits the clinical application of this drug. In this work, methoxypolyethylene glycols 2000 (mPEG2K)-polymyxin E (PME) was synthesized via chemical grafting reaction and had been characterized. The antimicrobial activity and cytotoxicity of mPEG2K-PME in vitro were investigated on Escherichia coli and HK-2 cells, separately. Intra-abdominal infection model was further established in order to study the therapeutic effect and the toxic effect on kidney of mice. The results showed that mPEG2K-PME exhibited significant inhibitory effect on Escherichia coli and had a lower toxicity on HK-2 cells in vitro. At the same time, mPEG2K-PME had a good efficacy in the treatment of Escherichia coli infected mice in vivo. Moreover, nephrotoxicity caused by mPEG2K-PME was significantly reduced compared to free PME. mPEG2K-PME is promising in development of new preparations with high efficiency and low toxicity.
Animals ; Cell Line ; Colistin ; pharmacology ; toxicity ; Escherichia coli ; drug effects ; Escherichia coli Infections ; drug therapy ; Humans ; Kidney ; cytology ; drug effects ; Mice ; Polyethylene Glycols ; chemistry

To explore the protective effects of trimetazidine on vascular endothelial cells injury induced by hydrogen peroxide (H2O2) and its pharmacological mechanisms of anti-oxidation.Methods Human umbilical vein endothelial cells (HUVECs) were injured by H2O2.Next,the cells were treated with three different concentrations of trimetazidine (1 μmol/L,10 μmol/L,100μmol/L,respectively).The viability of cells was detected by methyl thiazoeyl tetrazolium (MTT) assay.In addition,malondialdehyde (MDA)contents,superoxide dismutase (SOD) and secretion of NO were measured.Results Trimetazidine could enhance the viability of the injured HUVECs induced by oxidation,decrease the level of MDA,enhance the SOD activity,and increase the secretion of nitrogen monoxide.These effects were in a certain dose-dependent manner and the difference was significant among the three concentrations (P＜0.05).Conclusions Our results suggest that trimctazidine may protect lipid peroxidation and prevent oxidation-induced cellular dysfunction of HUVECs (J Geriatr Cardiol 2008;5:248-251)

Objective: To observe the effect of electroacupuncture (EA) on cytochrome c oxidase (COX)activity of hippocampal mitochondria in senescence-accelerated mouse prone 8 (SAMP8) mice, and to explore the EA mechanism on Alzheimer disease (AD) in improving energy metabolic disorder.
Methods: Twelve SAMP8 mice were randomly divided into a model group and an EA group, with six in each group. Six senescence-accelerated mouse resistance 1 (SAMR1) mice were prepared as blank group. Mice in the EA group received EA on Baihui (GV 20) and Yongquan (KI 1), once a day for 7 d as a course, altogether 3 courses with one day intervalbetween two courses. Mice in the model group and the blank group were manipulated and fixed as those in the EA group. After interventions, Morris water maze was employed to test spatial learning and memory ability to evaluate EA effect; spectrophotometry was used to detect the activity of hippocampal mitochondria COX.
Results: Compared with the blank group, mean escape latenciesof the EA group and model group were prolonged significantly in Morris water maze tests (P<0.01), the residue duration in the former platform quadrant significantly decreased (P<0.01). Compared with the model group, mean escape latencies on 1 d, 2 d and 3 d of the EA group were significantly reduced (P<0.05), and those on 4 d and 5 d continued the decreasing tendency (P<0.01), the residue duration on the former platform quadrant was significantly prolonged (P<0.05). The COX activity tests showed that, compared with the blank group, COX activities of the model group and the EA group were significantly decreased (P<0.01); compared with the model group, COX activity of the EA group was significantly elevated (P<0.01).
Conclusion: It’s plausible that EA improves AD learning and memory ability by increasing mitochondria COX activity, protecting the structure and function, and improving energy metabolism.

To get high cell density,pH-stat fermentations of L.casei Zhang were carried out in the medium optimized previously under different cultural conditions.The influences of neutralizing agents,the concen-tration of buffer salts and glucose in the medium,pH,aeration and fed batch fermentation on the growth of L.casei Zhang were investigated.Based on the values of maximum specific growth rate,biomass and viable cells count in different cultural conditions,the optimal growth condition was regarded as follows:Glucose level of the medium was 80 g/L ～100 g/L;The pH was kept constant at 5.9 with aqua ammonia and anae-robic condition was kept by sparged with nitrogen periodically;The temperature was set at 37?C and cul-tured for 10 h ～12 h.The biomass and viable cells' number of L.casei Zhang under this culture conditions were 7 g/L and 3.5?1010 CFU/mL respectively,and were 7 times as high as that before optimized,which can meet the requirements of probiotics.

A total of 159 patients with acute coronary syndrome(ACS)were enrolled from December 2006 to June 2008 and divided into the percutaneous coronary intervention(PCI)group and the internal medicine treatment group.The participants in the two groups were further assigned to the Tirofiban or the placebo control group.The change in electrocardiograph within 48 hours,major adverse cardiac events (MACE)during hospital stay and 30 days' follow-up,and bleeding were compared between the sub-groups.As a result,in comparison with the placebo control groups,the Tirofiban sub-groups showed significant improvement in electrocardiography(P＜0.01).In the internal medicine treatment group,the rate of MACE during 30 days' follow-up was significantly decreased in patients treated with Tirofiban(P＜0.05),although no significant difference in bleeding rate was found.Our data suggest that Tirofiban may be safe and effective in the treatment of ACS.

Objective This retrospective study is designed to analyze the cardiovascular events of CTO to provide new information on secondary prevention of CHD in patients after hospital discharge. Methods 272 patients with definite diagnosis of CTO were enrolled in this study. Patients were divided into two groups according to whether suffering from cardiovascular events, with 167 patients in group A who had not suffered from the cardiovascular events and 105 patients in group B who had suffered from the cardiovascular events. We com-pared the clinical data, severity of coronary artery lesion, treatment in two groups. Results Between two groups, there was statistic signifi-cance in LDL -C, EF, Gensini scots, the number of coronary artery lesion, the number of chronic total coronary occlusion and PCI success. Logistic regression analysis revealed that Gensini scots was the independent factors for prognosis of CTO. Conclusion Gensini scors was the independent factor for prognosis of CTO.

Objective To evaluate regional airway obstruction with balloon catheter in stabilizing the vital signs in experimental animals suffered from acute massive pulmonary embolism. Methods Pulmonary embolism of right lung artery by using auto-blood clots or detachable latex balloons was established in 27 healthy sheep. When the blood oxygen saturation decreased by 25% compared to that before the procedure,the placement of balloon catheter in corresponding right main bronchus was carried out in 18 sheep (study group). Five sheep were used as control group. The blood oxygen saturation in the remaining four sheep did not reach the intervention level. The pulmonary arterial pressure, the peripheral arterial pressure, the central venous pressure, the heart rate, the blood oxygen saturation, the arterial partial pressure of oxygen as well as of carbon dioxide were invasively determined. Results The experimental model of acute massive pulmonary embolism was successfully established in 23 sheep. After the establishment of pulmonary embolism, increased heart rate, tachypnea, a decrease of ≥ 25% in blood oxygen saturation within 30 minutes and a rise in pulmonary arterial pressure were detected. After the placement of balloon catheter in study group, a reduction of the pulmonary arterial pressure and an elevation of the blood oxygen saturation as well as the arterial partial pressure of oxygen rose. were observed. The difference between study group and control group was statistically significant (P < 0.05). Conclusion The result of this animal experiment indicates that obstruction of airway with balloon can be served as a first aid for acute massive pulmonary embolism, which can stabilizes the animal's vital signs and, therefore, can help gain precious time for the follow-up thrombolysis treatment.