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

Adult ; Aged ; Female ; Fracture Fixation, Internal ; Fractures, Bone ; surgery ; Humans ; Knee Injuries ; surgery ; Male ; Middle Aged ; Postoperative Care

OBJECTIVETo improve the method for monitoring sleep state and respiratory rhythm of SD rats, providing a solution for rats' chewing on the wires, signal loss and instability problems in the animal model of sleep apnea syndrome (SAS).

METHODSWe improved monitoring electrodes of both electrocorticogram (ECoG) and electromyogram (EMG), signal circuit and animal operation.

RESULTSOperation time was shortened and wound exposure time was reduced, which made it easier for postoperative recovery. The ECoG and EMG signals were more stable with sharp image, and signal circuit lines had better conductivity and material durability, achieving continuous monitoring for a long time and high success rate. We could precisely distinguish the sleep wake state and the sleep apnea events in rats according to these signals.

CONCLUSIONThe improved method is more reliable and practical to test the small animal model of SAS, and is more easily to operate and the signals are more stable.

Animals ; Electroencephalography ; methods ; Electromyography ; methods ; Models, Animal ; Monitoring, Physiologic ; methods ; Rats ; Respiration ; Sleep ; Sleep Apnea Syndromes ; diagnosis

To study the name of Wenyujin Rhizoma Concisum and Film Turmeric by literature research methods provide the basis for correct application of Cuba in modern clinical application. Wenyujin Rhizoma Concisum and Film Turmeric often called each other mutual generation and used as the same kind of medicine in the ancient prescriptions books. They were often recorded and stated as the same species of Curcumae Longae Rhizoma. Wenyujin Rhizoma Concisum and Curcumae Longae Rhizoma also often called each other mutual generation in the ancient prescriptions books and used as the same kind of medicine. Wenyujin Rhizoma Concisum was often recorded and stated under the Curcumae Longae Rhizoma articles in the ancient materia medica literatures. Ancient literatures on Wenyujin Rhizoma Concisum records were almost the same, the modern literatures on the records of the sources of Wenyujin Rhizoma Concisum were inconsistency. Inconsistency of Wenyujin Rhizoma Concisum source records in modern literatures was related to the changes of the modern records on source records about Curcumae Longae Rhizoma, Root-tuber of Aromatic Curcumae Longae Rhizoma and Zedoray. The author thinks that Wenyujin Rhizoma Concisum is the ancient Film Turmeric which referes to the same medicine as Curcumae Longae Rhizoma. The source of it just as the Curcumae Longae Rhizoma is not only one kind. Wenyujin Rhizoma Concisum and Curcumae Longae Rhizoma have been recorded as two medicines at the present, and the source of them simply referes to the original plant Curcuma wenyujin. When using ancient prescriptions, we need to understand the changes that Curcumae Longae Rhizoma and Wenyujin Rhizoma Concisum are the same in ancient but different today in order to choose medicine correctly in the clinical.
Curcuma ; Medicine, Chinese Traditional ; Rhizome ; Terminology as Topic

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.

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.