Optically pure α-substituted propanoic acids and their derivatives represent as an important kind of organic building blocks and key intermediates,which has been widely used in the synthesis of chiral drugs.Some of them have been used directly as nonsteroidal anti-inflammatory drugs (NSAIDs),such as ibuprofen,naproxen,ketoprofen and so on.Dihydroartemisinic acid (DHAA),the same structure as the α-substituted propanic acids,is a key intermediate for the synthesis of artemisinin,the most effective and current used anti-malarial drug.Therefore,the asymmetric synthesis of α-substituted propanoic acids is always a hot topic for chemical scientists.Asymmetric catalytic hydrogenation attracts more and more attentions because of its atom economy and efficiency.This dissertation will disclose the asymmetric synthesis of α-substituted propanoic acids using transition metal-complex as a chiral catalyst.

Objective:To investigate the effect of short-term intensive treatment with insulin on metabolic control,?-cell function and insulin resistance in newly diagnosed type 2 diabetic patients. Methods:Thirty-eight newly diagnosed type 2 diabetic patients were randomly divided into two groups and treated with continuous subcutaneous insulin infusion(CSII) or multiple daily insulin injection(MDI) for 1 month.Fasting blood glucose(FBG) and lipid profiles were measured,and oral glucose tolerance test(OGTT)was performed before and after the treatment.The second phase insulin and C peptide secretions were measured by calculating area under curve(AUC) in OGTT.HOMA model was used to evaluate ?-cell function((HOMA-?)) and insulin resistance. Results:Excellent control of FBG was achieved after 1 month intensive treatment.(HOMA-?) was improved significantly. Conclusion:The excellent metabolic control and ?-cell function improvement can be achieved by short-term intensive insulin therapies like CSII or MDI.

Aim To evaluate the reversal effect of 2-deoxy-D-glucose ( 2-DG ) on multidrug resistance ( MDR) by observing the uptake change of 99m Tc-MIBI in HNE-1/DDP cells, and to explore its mechanism. Methods The uptake of 99m Tc-MIBI in HNE-1/DDP cells under different concentrations of 2-DG was detec-ted by γ-counter, and the clearance rates of 99m Tc-MI-BI in HNE-1 cells and HNE-1/DDP cells after treated with 2-DG (10 mmol·L-1 ) were compared. The con-tent of ATP in HNE-1/DDP cells was detected after treated with 2-DG. P-glycoprotein ( P-gp ) and multi-drug resistance-associated proteins ( MRP ) expression were measured by Western blot. Apoptotic HNE-1/DDP cells treated with DDP alone or combined with 2-DG (10 mmol·L-1 ) were detected by propidium io-dide ( PI ) staining. Results The clearance rate of 99m Tc-MIBI in HNE-1/DDP cells was 54. 8%, which was significantly higher than that ( - 41. 3%) in HNE-1 cells (P<0. 01). The clearance rate of 99mTc-MIBI in HNE-1/DDP cells was -203. 7% after treat-ment with 2-DG ( 10 mmol · L-1 ) , which could be significantly reduced compared with the control group ( P<0. 01 ) . The level of ATP was 55 . 69% compared with the negative control group and the expression of P-gp and MRP protein decreased dramatically in HNE-1/DDP. With the combination of 2-DG and DDP, the ap-optotic rate of HNE-1/DDP cells reached 49 . 4%which was significantly higher than DDP treated group (22. 5%) . Conclusion Multidrug resistance and the reversal effect of 2-DG on multidrug resistance could be evaluated effectively by detecting the uptake change of 99m Tc-MIBI in HNE-1/DDP cells. The mechanism may be related with the inhibition of ATP level and the re-duced expression of P-gp and MRP protein in cancer cells.

AIM: To research how to separate the active component in Ligusticum chuanxiong Hort by high speed counter current chromatography. METHODS: Senkyunolide A and Z-ligustilide,the main components of volatile oil in Ligusticum chuanxiong Hort were one step separated by high speed counter current chromatography. n-hexane-ethyl acetate-ethanol-water,1 ∶ 1 ∶ 1 ∶ 1(v/v),was used as the solvent system for HSCCC. Top phase and bottom phase were respectively used as static phase and mobile phase. Optimum speed and flow rate were 900 r/min and 1. 2 mL/min respectively. RESULTS: Collected fractions were analyzed by HPLC and identified by EI-MS and 1HNMR. Purity could reach more than 95% . CONCLUSION: Lactone is fit to be separated and prepared by high speed counter current chromatography with good resolution and high purity. We find a fast and efficient way to separate these.

injection). At the 5th, 10th and 15th months after operation, L2, L4 bone mineral density, L2, L4 maximum bending and compressive load, the ratio of anterior and posterior heights of L3 vertebrae to average height of L2 and L4 vertebrae, and the sagittal Cobb angle of L2 and L4 vertebrae were detected. RESULTS AND CONCLUSION:The bone mineral density, maximum bending and compressive load, vertebral height ratio at different time points after operation in experimental group were higher compared with the preoperative level (P < 0.05). The sagittal Cobb angle in experimental group was smaler compared with the preoperative level (P < 0.05). In the control group, the bone mineral density, maximum bending and compressive load at different time points after operation were al higher compared with preoperative level (P < 0.05). There were no significant difference of the vertebral height ratio and sagittal Cobb angle compared with the preoperative level. The bone mineral density, maximum bending and compressive load, vertebral height ratio at different time points after operation in experimental group were higher compared with the control group (P< 0.05). The sagittal Cobb angle was smaler compared with the control group (P < 0.05). These results demonstrate that percutaneous kyphoplasty bone cement injection can better improve the bone density, carrying capacity and kyphosis of osteoporosis fractures adjacent vertebrae.

Objective To investigate the effect of placing subcutaneous drain tube and preseting triclosan-coated polyglactin 910 suture with delayed suturing to incision infection after typeⅢabdominal surgery. Methords Dividing 504 patients with typeⅢincisions undergone abdominal surgery into 3 groups. The number of group A patients with thoroughly incision washing and primary triclosan-coated polyglactin 910 suture after abdominal surgery was 143. The number of group B with closed anterior rectus sheath, opened skin and subcutaneous fat with preseted triclosan-coated polyglactin 910 suture was 190. The number of group C with subcutaneous drain tube after abdominal surgery was 171. We compared the incidence rates of incision infection and the second phase debridement suture rates among the 3 groups. Results For the group A, B, C, the number of incision infection people was 11, 4, 3 and the incision infection rate was 7.69%, 2.11%and 1.75%respectively. The difference of the 3 groups incision infection rate were statistically significant (P<0.05). The incision infection rate of the group B and group C were lower than that of group A and the difference were statistically significant (P<0.016 7). There were no significant differences in second phase debridement suture rates among the 3 groups. Conclusion Preseting triclosan-coated polyglactin 910 suture with delayed incision sutue and placing subcutaneous drain tube can decrease the incision infection rates for type Ⅲpatients after abdominal surgery, but can not decrease the second phase debridement suture rates of the infectious incision.

Objective To investigate the short-term clinical outcome of one-level degenerative diseases for a single surgeon during his initial phase of performing a minimally invasive surgery oblique lumbar interbody fusion (OLIF) on the basis of perioperative parameters and follow-up data.Methods A prospective analysis of 49 consecutive patients that underwent a OLIF between November 2014 and March 2016 by corresponding author was performed.Only those patients that were single level,index surgeries were included.Every patient had a diagnosis of degenerative lumbar diseases including lumbar spondylolisthesis (25 cases),discogenic low back pain (14 cases) or segmental instability (10 cases).Patients underwent an indirect decompression and fusion using an expandable tubular retractor and single intervertebral cage with bilateral percutaneous pedicle screw fixation.49 patients were divided into the A group (the first 24 patients) and the B group (25 patients after the initial 24 patients).The following data were compared between the two groups:surgical time for Skin-Skin (minutes),estimated blood loss (ml),radiograph exposure time (seconds),the clinical and radiographic results,and intra-/postoperative complications.All intraoperative parameters only included the measurement and findings related with the OLIF procedure.The short-term clinical outcome of single level degenerative lumbar diseases treated by OLIF was assessed on the basis of follow-up data.The learning curve was measured using a logarithmic curve-fit regression analysis.Results Average operative time was significantly longer in the A group 47.1±10.6 min compared with the B group 37.2± 10.0 min.In comparison with the B group,the A group had significantly more X-ray exposure time (25.3±6.1 s versus 17.1±6.9 s).The operative and X-ray exposure time gradually decreased as the series progressed,and an asymptote was reached after about 20 cases.There was no statistically significant difference in intraoperative blood loss between the A group (28.1± 18.2) ml and the B group 24.4± 10.9 ml.The most observed complication was donor site pain (11 cases,45.8％),followed by thigh numbness/pain (5 cases,20.8％) and psoas/quadriceps weakness (2cases,8.3％),paralytic ileus (one case,4.2％) and sympathetic nerve injury (one case,4.2％) in the A group.Donor site pain occurred in four patients (16.0％),thigh numbness/ pain in three patients (12.0％),psoas/quadrieeps weakness in one patient (4.0％) and sympathetic nerve injury in one patient (4.0％) in the B group.All complications were transient and resolved within 3 months.The incidence of complications excluding donor site pain in the early period (A group) and the later period (B group) was 37.5％ and 20.0％,respectively,although there were no significant differences in perioperative complications between both groups.Forty nine patients were followed up for more than 1 year,and the average follow-up period was 18.5±3.9 months.The back pain VAS and ODI scores decreased respectively from 6.4±2.3 before surgery to 1.5±0.9 in final follow-up and from 37.1 ±9.4 before surgery to 11.8±3.9 in the last follow-up time.Total fusion rate was 89.8％ (44/49 cases)in final follow-up.Radiographic evaluation showed similar bony fusion in the A group (22 of 24 cases) with the B group (22 of 25 cases) in the last follow-up time.Conclusion Single level degenerative lumbar diseases can safely and effectively be treated by using OLIF with a good short-term clinical outcome.The procedure presents a learning curve to the practicing spine surgeon with regards to operative time,X-ray exposure time and intra-/postoperative complications.Intraoperative parameters improved with understanding the minimally invasive technique.Close attention to details can minimize complications that may be associated with the learning curve.

AIM To investigate whether melatonin improve the learning and memory dysfunction in the amnesic rats induced by amyloid ? peptide 25～35 (A? 25～35 ) via cholinergic nervous system or not.Methods The amnesic model in adult rats was induced by injection of A? 25～35 into hippocampus; Morris water maze was used to determine the effects of A? 25～35 and melatonin on the learning and memory. The activity of the choline acetyltransferase and acetylcholinesterase were determined by immunohistochemistry and spectrophotometry respectively. RESULTS Injection of A? 25～35 20 ?ginto the adult rats hippocampus induced learning and memory dysfunction, and a decrease in the number of ChAT immunoreactive neurons in hippocampus. Melatonin (0 1, 1, and 10 mg?kg -1 , ig?10 d) improved the A? 25～35 treated rats cognitive function and increased the number of ChAT immunoreactive neurons in hippocampus. CONCLUSION Improvement of the cholinergic dysfunction by melatonin in adult rats induced by amyloid ? peptide 25～35 may be via cholinergic nervous system.

Focal Adhesion Protein-Tyrosine Kinases ; Humans ; Liver Diseases, Alcoholic ; enzymology ; pathology

Objective To investigate the effect of glucagon-like peptide-1 (GLP-1) receptor agonist liraglutide on hypoxia/reoxygenation (H/R)-induced cardiomyocytes death under high glucose condition and the potential mechanisms.Methods H9C2 cardiomyocytes were divided into 4 groups:normal glucose (N,5 mmol/L),high glucose (G,20 mmol/L),high glucose in combination with liraglutide (L,100 nmol/L),high glucose in combination with liraglutide and wortmannin (W,25 nmol/L).The apoptosis of H9C2 was detected by TUNEL assay.Nitric oxide synthetase(eNOS),nitric oxide (NO) and reactive oxygen(ROS) in supernatants were measured by enzymatic analysis,p-PI3K,PI3K,p-Akt,Akt,Bcl-2,caspase-3 were examined by western blotting.Results Compared with cells in N group,the apoptosis of H9C2 cells induced by H/R was markedly increased [(15.79 ± 3.92) ％ vs (9.74 ± 1.14) ％,P =0.028] in G group.The same was true for ROS [(489.63 ±21.01) U/ml vs (338.50 ±43.60) U/ml,P ＜0.001] and caspase-3 levels (1.87 ±0.03 vs 1.15 ±0.04,P ＜0.001),but not for Bcl-2 protein expression (1.79 ± 0.06 vs 1.89 ±0.03,P =0.047).Pretreatment of cells with liraglutide (100 nmol/L) prevented the cell death induced by high glucose and H/R together with decrease of ROS and caspase-3 levels and increase of Bcl-1 expression.Moreover,treatment of cells with liraglutide also significantly increased phosphorylation of PI3K and Akt (p-PI3K/PI3K:0.87 ± 0.07 vs 0.59 ± 0.09,P =0.002;p-Akt/Akt:0.34 ± 0.01 vs 0.08 ± 0.01,P＜0.001),eNOS[(41.29 ±0.56) μmpl/L vs (37.20 ±0.52)μxmpl/L,P ＜0.001]and NO [(31.24 ±0.40) μmpl/L vs (26.66 ±0.53) μmpl/L,P ＜0.001] levels.Furthermore,addition of PI3K/Akt inhibitor wortmanin markedly inhibited the expression of p-PI3K/PI3K,p-Akt/Akt,reversed the changes of eNOS,NO,caspase-3 and Bcl-2 by liraglutide,and abolished the protective effect of liraglutide on cell apoptosis.Conclusions GLP-1 receptor agonist liraglutide treatment could alleviate cardiomyoeytes apoptosis induced by high glucose and H/R through the activation of PI3K-Akt-eNOS-NO signaling pathway and inhibition of oxidative stress.