Acetylcholinesterase is an important target for anti-Alzheimer's disease now.Much attention has been paid to the development of tacrine dimeric or hybrid compounds.The design strategy is transforming merely interacting with the two binding sites of acetylcholinesterase to get more activity and selectivity into the multi-target-directed function for the treatment of Alzheimer's disease. Herein,the tacrine dimeric or hybrid compounds development and the prospect for the treatment of AD have been reviewed.

Objective In a randomized double blind study, we have compared the analgesic efficacy and safety of PCA with buprenorphine and PCA with morphine after abdominal hysterectomy. Methods One hundred and fifty-four patients aged 25-55 yr undergoing abdominal hysterectomy were included in this study. Patients with severe cardiac, cerebral, hepatic and renal disease and those who had recently taken monoamine oxidase inhibitor were excluded. Anesthesia was induced with propofol 1.5-2.0 mg?kg-1 and intubation was facilitated with succinylcholine 1.5 mg?kg-1 or vecuronium 0.1 mg?kg-1 . Anesthesia was maintained with inhalation of l%-2% isoflurane and 50% nitrous oxide in oxygen supplemented with intermittent iv boluses of vecuronium 1-2 mg, fentanyl 2?g?kg-1 and droperidol 1-2 mg. The patients were randomly divided into 2 groups: 1 buprenorphine group (B, n = 77 ) and 2 morphine group (M, n = 77) . In group B, patients received PCA with buprenorphine (bolus dose 0.03 mg, lockout interval 14 min, 24 h dose limit 1.2 mg); in group M patients received PCA with morphine (bolus dose 1 mg, lockout interval 5 min, 24 h dose limit 40 mg). Intensity of pain was assessed using VAS with 0 representing no pain and 10 representing the worst pain. Pain intensity difference before and after PCA and pain relief (PAR) (0 = not relieved, 4 = completely relieved) , patient satisfaction and adverse effects were recorded. Results The two groups were comparable with regard to age, body weight, duration of operation, the time when postoperative pain started and PCA was commenced, and the intensity of postoperative pain. There was no significant difference in pain intensity before and after PCA and PAR between the two groups. The incidence of nausea and vomiting was significantly higher in group B than in group M ( P

0.05) . The sensory block reached T7 in levobupivacaine group and T6 in bupivacaine group respectively. The motor blocked was somewhat more intense in bupivacaine group. Conclusion The efficacy and safety of epidural anesthesia with levobupivacaine and bupivacaine are comparable.

0.05). Lornoxicam caused less side effects than morphine (10.2% vs 17.9%) Conclusions The study suggests that lornoxicam provide an alternative to morphine for the treatment of postoperative pain.

Objective To investigate the relationship between end-tidal carbon dioxide with its related indicators and ventilation/perfusion of the acute respiratory distress syndrome (ARDS) lung,and to explore a feasible way to titrate positive end-expiratory pressure (PEEP) in clinical practice.Methods Five mixed-breed dogs with oleic acid lung injury model were mechanically ventilated at a serial PEEP trial including a recruitment maneuver (RM) before each PEEP level changed.The value of blood dynamics,end-tidal carbon dioxide partial pressure ( PetCO2 ) and arterial carbon dioxide pressure under different PEEP levels were recorded.Arterial end-tidal carbon dioxide gradient (Pa-etCO2) and dead space fraction (Vd/Vt％) were calculated.All dogs received CT scan.Lung volume under different pressure levels,and ratio and volume of alveolar closing pressure,collapsed alveoli,sufficiently and insufficiently ventilated alveoli were obtained.Alveolar opening and closing analysis were performed by non-liner regression equation.Results The mean pressure when Vd/Vt％ obtained lowest level were ( 11.2 ± 4.4 ) cm H2O(1 em H2 O =0.098 kPa),which had no significant difference when compared to alveolar closing pressure[ ( 11.5 ± 3.2 ) cm H2O ]( P ＞ 0.05 ).The fraction of insufficiently ventilated and collapsed alveoli showed a significant linear correlation with the Vd/Vt％ when PEEP was lower than Pmin ( r =0.632,P =0.004 ).There was a linear correlation between the Vd/Vt％ and the fraction of over-distended alveoli when PEEP was higher than Pmin ( r =0.770,P =0.001 ).Conclusions Closing pressure is in accordance with PEEP level after RM having reached the best ventilation/circulation ratio.The characteristics of lung collapse can be revealed by Vd/Vt％ changes after RM.To titrate PEEP for the lowest Vd/Vt％ after RM may be a feasible way to match the best ventilation and circulation effects of PEEP.

With the continuous development in microfluidic fabrication technology, microfluidic analysis has evolved from a concept to one of research frontiers in last twenty years. The research of enzymes and enzyme inhibitors based on microfluidic devices has also made great progress. Microfluidic technology improved greatly the analytical performance of the research of enzymes and enzyme inhibitors by reducing the consumption of reagents, decreasing the analysis time, and developing automation. This review focuses on the development and classification of enzymes and enzyme inhibitors research based on microfluidic devices.

Objective To study the clinical value of 18F-FDG PET/CT in childhood neuroblastoma (NB). Methods 18F-FDG PET/CT was performed in 31 children diagnosed with NB. According to the treatment conditions, patients were divided into pre-therapy group, radiation and chemotherapy group, postoperative group, respectively. The positive rate, sites, and im-age characteristics of the primary lesion and metastasis lesion were analyzed through qualitative and quantitative analysis of the image. Results Twenty-one (67.7%) and fourteen (45.2%) patients were found positive in primary sites by CT and PET respectively. All cases (9/9, 100%) in pre-therapy group were found positive in primary lesions by PET, 3 positive cases (75.0%) in radiation and chemotherapy group and 2 positive cases (11.1%) in postoperative group. Twenty-one patients showed metas-tases (67.7%). Lymph nodes (16 cases) and bone (bone marrow) (13 cases) were the most common sites of metastasis followed by pleura, meninges, liver and retrobulbar inifltration, all of which showed increased FDG uptake. Two patients were found lesions in lungs by CT, but had no FDG uptake. SUVmax of primary lesions was signiifcantly different among pre-therapy, chemotherapy and postoperative group (H=13.89, P=0.001), and pre-therapy group had the highest value. Metastases (lymph nodes, bone and bone marrow, pleura, liver and meninges) in pre-therapy group had high SUVmax. Conclusions NB primary tumors are characterized by the increased FDG metabolism. PET can fully detect the distribution of NB metastases in whole body. Except the pulmonary metastasis, metastases in other positions show increased FDG uptake. PET has potential role in evaluating the efifcacy of radiation and chemotherapy, and identifying postoperative residual or recurrence.

Chitosan is a natural biopolymer and is made up of D-glucosamine subunits linked by beta-(1,4) glycosidic bond. In recent years, the application of chitosan has attracted more and more attention because of its good biological function in cell biology. The properties of chitosan-based biomaterial are attributed to the physical properties and chemical composition of chitosan. The author of this paper summarized recent related studies and progresses of the influence of physical properties of chitosan on cell activity and cell mechanics property at home and abroad. The findings show that most studies mainly focused on the influence of chitosan and cell activity, while few were on cell mechanics property. The related studies of the influence of chitosan on cell will contribute to the explanation for the mechanism of the interaction between chitosan and cell, and provide the theoretical support for the further study.
Animals ; Cell Adhesion ; drug effects ; Cell Differentiation ; drug effects ; Cell Movement ; drug effects ; Cell Proliferation ; drug effects ; Chemical Phenomena ; Chitosan ; chemistry ; pharmacology ; Humans ; Tissue Engineering ; Tissue Scaffolds ; chemistry

ObjectiveTo study the effect and safety of flurbiprofen cataplasm on osteoarthritis pain in Chinese patients.MethodsOne hundred and eighty-three patients were divided into flurbiprofen cataplasm group,indometacin cataplasm group and Qizheng-xiaotong plaster group randomly.The score of pain,stiffness and physical function were analyzed with WOMAC scale and adverse reactions were also assessed.KruskalWallis H test,Nemenyi test and CMH tese were used.ResultsAfter treatment,the VAS value of the three groups decreased significantly and the VAS difference value of the flurbiprofen cataplasm group changed the most significantly(the changes of VAS value in flat walking,up and down stairs,nighttime,rest and weightbearing were 31±21,35±20,24±19,20±18 and 37±20 respectively).Meanwhile,the value of stiffness and physical function decreased significantly.In terms of safety,flurbiprofen cataplasm group and the indome-tacin cataplasm group were better than Qizheng-xiaotong plaster group.But in sense of constriction,the flurbiprofen cataplasm group was better than the indometacin eataplasm group.ConclusionFlurbiprofen Cataplasm,with its favorable analgesic effect,is suitable for general clinical use.It can reduce stiffness,improvephysical function,and has good safety profile.

Selectin/ligand interaction plays an important role in such biological processes as inflammatory reaction, tumor metastasis, etc. External forces affect dissociation of receptor-ligand bonds. A novel approach, upon optical trap technique, was developed in this study to investigate the dissociation of P-selectin/PSGL-1 (P-Selectin Glycoprotein Ligand 1) bindings. Stiffness of optical trap was calibrated with laser power using a viscous drag method. While P-selectin and PSGL-1 molecules were functionally coated on surfaces of glass beads, respectively, the dissociation of interacting molecule bond was studied by measuring the rupture force distribution. It was found that most probable rupture force increased with loading rate at < 25 pN/s. These results complemented and validated the current theory at low loading rates.
Humans ; Membrane Glycoproteins ; chemistry ; Optics and Photonics ; instrumentation ; Protein Binding ; Protein Structure, Tertiary