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.

Objective To explore the therapeutic effect of dual perfusion embolization and chemotherapy via hepatic artery and portal vein(combmation treatment) in the treatment of unresectable PHC.Methods Eighty-one cases of unresectable PHC were randomly divided into two gronps: (1) Combination treatment group.Forty-one cases,These cases received embolization and chemotherapy via hepatic artery and portal vein through a drug delivery system intraoperatively,and then embolization and chemotherapy via the drug pump were given periodically. (2) TACE group.Forty cases.These cases were treated with Seldinger's technique, the dosage of drugs were the same as used in the former group during laparotomy. After 3 times of treatment, AFP, the size of tumor, liver function, body weight, abdominal perimeter, survival time of the two groups were compared.Results The weight, AFP, decrease of tumour size in combination group were much better than those in TACE group( P 0.05). The median survival time in the two groups were 18.0 months and 11.1 months ( P =0.0001). The accumulating survival rate of 6, 9, 12, 24 months were 87.8%, 78.0% , 68.2%,31.7% in combination group, and 70.0%, 52.5%, 30.0%, 5.0% in TACE group, respectively . The factors affecting survival were therapeutic method, liver function, size of tumour.Conclusions Combination treatment is simple, convenient with less complications, and the effect is better than TACE. So it is an effective method for the unresectable hepatic carcinoma.

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.

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

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