Xanthine oxidase (XO) is an important therapeutic target for the treatment of hyperuricemia and gout. Based on the previously identified potent XO inhibitor 1, seventeen oxadiazoles and their ring-opening analogues were designed and synthesized via the bioisostere replacement strategy. Among them, compounds 2l, 2n, and 3b showed obvious XO inhibitory activity at the concentration of 10 μmol·L^-1, and compound 3b exhibited an IC₅₀ value of 1.45 μmol·L^-1.

Isoflavones which mainly distributed in leguminous plants have plenty of health benefits.Isoflavone synthase(IFS)is a membrane-associated cytochrome P450 enzyme(CYP450)which carries out the unique aryl-ring migration and hydroxylation.So far,few crystal structures of plant P450s have been obtained.We determined the crystal structure of IFS from Medicago truncatula at 1.9 ? by MAD method using a selenomethionine substituted crystal and conducted molecular docking and mutagenesis study.The structure of IFS complexed with imidazole exhibits the helix Ⅰa-loop-helix Ⅰβ motif which cor-responds to helix Ⅰ of other P450s.Compared with structures of common P450s,IFS/imidazole structure contains an extra domain,i.e.,the γ-domain.The structure reveals a homodimer in which the γ-domain of one molecule interacts with the β-domain of another.The plane of heme group makes an angle of ap-proximately 40° with the helix Ⅰa-loop-helix Ⅰβ motif.Molecular docking combined with mutagenesis study suggested that Trp-128 and Asp-300 might play important roles in substrate binding and recogni-tion.Phe-301,Ser-303 and Gly-305 from the helix Ⅰa-loop-helix Ⅰβ motif may play important roles in the aryl-ring migration.These novel structural features reveal insights into the unique reaction mechanism of IFS and provide a basis for engineering IFS in leguminous crops for health purpose.

Isoflavones which mainly distributed in leguminous plants have plenty of health benefits.Isoflavone synthase(IFS)is a membrane-associated cytochrome P450 enzyme(CYP450)which carries out the unique aryl-ring migration and hydroxylation.So far,few crystal structures of plant P450s have been obtained.We determined the crystal structure of IFS from Medicago truncatula at 1.9 ? by MAD method using a selenomethionine substituted crystal and conducted molecular docking and mutagenesis study.The structure of IFS complexed with imidazole exhibits the helix Ⅰa-loop-helix Ⅰβ motif which cor-responds to helix Ⅰ of other P450s.Compared with structures of common P450s,IFS/imidazole structure contains an extra domain,i.e.,the γ-domain.The structure reveals a homodimer in which the γ-domain of one molecule interacts with the β-domain of another.The plane of heme group makes an angle of ap-proximately 40° with the helix Ⅰa-loop-helix Ⅰβ motif.Molecular docking combined with mutagenesis study suggested that Trp-128 and Asp-300 might play important roles in substrate binding and recogni-tion.Phe-301,Ser-303 and Gly-305 from the helix Ⅰa-loop-helix Ⅰβ motif may play important roles in the aryl-ring migration.These novel structural features reveal insights into the unique reaction mechanism of IFS and provide a basis for engineering IFS in leguminous crops for health purpose.

Objective:To evaluate the screw placement assisted by robotic navigation in cannulated screw fixation for treatment of fracture of scapular coracoid process.Methods:A retrospective study was conducted to analyze the data of 24 patients with fracture of scapular coracoid process who had been treated by cannulated screw fixation at Department of Orthopaedics and Trauma, Red Cross Hospital Affiliated to Xi'an Jiaotong University from January 2020 to December 2023. According to whether the intraoperative screw placement was assisted by robotic navigation or not, the patients were divided into 2 groups. In group A of 11 cases, there were 6 males and 5 females with an age of (47.4±3.4) years whose screw placement was assisted by robotic navigation during the internal fixation with cannulated screws. In group B of 13 cases, there were 10 males and 3 females with an age of (43.5±4.9) years whose screw placement was assisted by conventional C-arm X-ray fluoroscopy during the internal fixation with cannulated screws. The operative time, intraoperative blood loss, fracture healing time, intraoperative fluoroscopy frequency, intraoperative adjustments of guide wire, Constant-Murley score of shoulder function at the last follow-up and postoperative complications were compared between the 2 groups.Results:There was no significant difference in the preoperative general data between the 2 groups, indicating comparability ( P>0.05). The follow-up time was (25.3±9.1) months for group A and (27.6±10.8) months for group B, showing no statistically significant difference ( P>0.05). The intraoperative blood loss [(51.8±35.7) mL], intraoperative fluoroscopy frequency [(5.7±1.0) times] and intraoperative adjustments of guide wire [(1.6±0.7) times] in group A were significantly less than those in group B [(123.8±73.9) mL, (12.5±2.7) times, and (5.3±1.0) times] ( P<0.05). There were no significant differences in operative time [(88.2±21.3) min versus (80.4±31.1) min], fracture healing time [(10.0±1.3) weeks versus (11.5±2.7) weeks] or Constant Murley score of shoulder function at the last follow-up [(86.7±6.1) points versus (91.1±10.0) points] between group A and group B ( P>0.05). No patient reported such complications as wound infection, fracture nonunion, or failure of internal fixation during the follow-up period. Conclusions:In the treatment of fracture of scapular coracoid process by cannulated screw fixation, robotic navigation can be used to assist screw placemen to achieve good efficacy comparable to conventional C-arm X-ray fluoroscopy. Moreover, assistance by robotic navigation can help reduce intraoperative blood loss and radiation, and improve surgical accuracy.

OBJECTIVETo systematically review the clinical efficacy of acupuncture on the patients with low back pain (LBP).

METHODSRandomized controlled trials (RCTs) about pure acupuncture therapy versus other treatments in treating LBP were electronically searched in PubMed, CBM, EMbase, The Cochrane Library, CNKI, VIP and Wanfang Data from January 2004 to May 2014. The observed index on the results were the changed scores of VAS, ODI, JOA and RMDQ. Two reviewers independently screened the literatures according to the inclusion and exclusion criteria, as well as the extracted data, and assessed the methodological quality. The results of Meta-analysis was conducted by RevMan 5.2 software.

RESULTSTen RCTs involved 751 patients were finally included. The results of Meta-analysis indicated that the role of pure acupuncture group in improving the VAS score was better than that of the control group, and the combined effect size was RR = -.32, 95% CI (-1.41, -1.22); Z=27.28, P<0.00001; the role of pure acupuncture group in improving the ODI score was better than that of the control group, and the combined effect size was RR = -5.07, 95% CI (-7.50, -2.65); Z=4.10, P<0.0001; the role of pure acupuncture group on improved JOA score was better than that of the control group and the combined effect size was RR=2.83, 95% CI (2.02, 3.63), Z=6.90, P<0.00001. The role of pure acupuncture group in improving the RMDQ score was better than that of the control group, and the combined effect size was RR = -2.80, 95% CI (-3.49, -2.11), Z=7.95, P<0.00001.

CONCLUSIONThe result of meta-analysis demonstrates that pure acupuncture may have a favorable effect on self-reported pain and functional limitations in LBP patients.

Acupuncture Therapy ; Humans ; Low Back Pain ; therapy ; Randomized Controlled Trials as Topic ; Treatment Outcome

OBJECTIVETo investigate the ideal digestive tract reconstruction methods among three different surgical methods after radical gastrectomy of gastric cancer patients.

METHODSA total of 123 patients who received elective radical gastrectomy for gastric cancer from February 2010 to August 2011 were prospectively enrolled and randomly divided into radical proximal gastrectomy and jejunal interposition group, radical proximal gastrectomy and esophageal with the posterior of residual-stomach group, and radical total gastrectomy and Roux-en-Y esophagojejunostomy group. Patients were followed up for 12 months. Symptoms of reflux esophagitis were observed, gastric emptying tests were done, liver and kidney function was also monitored. The quality of life was documented before operation, and one and twelve months after operation.

RESULTSNo significant differences were found among these three groups in the pH value of lower part of esophagus, the blood regular test results and the functional parameters of kidney and liver before and after operation(all P>0.05). Symptoms of reflux esophagitis was reported in 1(2.4%) patients in the jejunal interposition group, 10(24.4%) in esophageal with the posterial of residual-stomach group, and 7(17.1%) in the Roux-en-Y esophagojejunostomy group(P=0.017). There was 1(2.4%), 10(17.1%), and 8(19.5%) patients presented reflux of barium meal in these three groups, respectively (P=0.046). There were no statistically significant difference in PH at the distal esophagus(6.9±0.2 vs. 6.8±0.1 vs. 6.9±0.1, P=0.196). The quality of life was significantly improved one year after surgery in terms of general status, physical function, emotional function, fatigue, nausea/vomiting, pain, constipation, and diarrhea (all P<0.05), with the jejunal interposition superior than the other two methods.

CONCLUSIONThree methods of digestive tract reconstruction in radical gastrectomy of gastric cancer patients can improve the health status and the quality of life in gastric cancer patients. Radical proximal gastrectomy and jejunal interposition is the preferred method.

Anastomosis, Roux-en-Y ; Anastomosis, Surgical ; Digestive System Surgical Procedures ; Esophagus ; Gastrectomy ; Gastric Emptying ; Gastric Stump ; Humans ; Jejunum ; Quality of Life ; Reconstructive Surgical Procedures ; methods ; Stomach Neoplasms ; surgery

Objective To investigate changes in the nental health status of the ship crew onboard surface naval vessels during a prolonged deployment, so as to provide scientific basis for the development of sound psychological health service measures for the ship crew. Methods Reproducibility and cross - sectional survey were conducted to investigate the emotional status of the ship crew aboard a certain naval surface vessel with symptom check list (SCL-90), 7 days before deployment, and on the 77th, 142nd, and 204th days after deployment during a prolonged ocean - going voyage. The obtained data were compared with the norms of the Chinese servicemen. Results The mental health status of the ship crew was on the whole in good mode before deployment. Total average score and various SCL-90 patterns were obviously lower than the norms of the Chinese servicemen(P＜0. 05 ). On the 77th day after deployment, the psychological state of the ship crew degraded markedly, manifested by the elevation of the SCL-90 total mean score and other scores, such as somatizaion, hostility, crankiness and other factors, when compared with those after deployment( P ＜0. 05 ).Of all the scores, the scores of hostility and crankiness were significantly higher than the norms of the Chinese servicemen( P ＜0. 01 ). Total SCL-90 average score and various factor scores on the 142nd and 204th days after deployment dropped sharply, except that one other factor score of SCL-90 was higher than that before deployment(P ＜0. 01 ). Screening positive rate of SCL-90 indicated that positive rates on the 77th( 15. 1% )and 204th days ( 20% ) were all obviously higher than that of pre - deployment( 2. 4% ) ( P ＜ 0. 01 ). However,no statistical differences could be seen in the scores on 142nd day(7.7% ), when compared with that of predeployment(2. 4% ) ( P ＞ 0. 05 ). Conclusions The psychological status of the ship crew, on the whole,degraded markedly during the initial stage of a prolonged deployment, then, would gradually come to normal with adaptation thereafter. Nevertheless, individual psychological status showed a tendency of obvious differentiation in the late stage of deployment.

Objective To investigate changes in the nental health status of the ship crew onboard surface naval vessels during a prolonged deployment, so as to provide scientific basis for the development of sound psychological health service measures for the ship crew. Methods Reproducibility and cross - sectional survey were conducted to investigate the emotional status of the ship crew aboard a certain naval surface vessel with symptom check list (SCL-90), 7 days before deployment, and on the 77th, 142nd, and 204th days after deployment during a prolonged ocean - going voyage. The obtained data were compared with the norms of the Chinese servicemen. Results The mental health status of the ship crew was on the whole in good mode before deployment. Total average score and various SCL-90 patterns were obviously lower than the norms of the Chinese servicemen(P＜0. 05 ). On the 77th day after deployment, the psychological state of the ship crew degraded markedly, manifested by the elevation of the SCL-90 total mean score and other scores, such as somatizaion, hostility, crankiness and other factors, when compared with those after deployment( P ＜0. 05 ).Of all the scores, the scores of hostility and crankiness were significantly higher than the norms of the Chinese servicemen( P ＜0. 01 ). Total SCL-90 average score and various factor scores on the 142nd and 204th days after deployment dropped sharply, except that one other factor score of SCL-90 was higher than that before deployment(P ＜0. 01 ). Screening positive rate of SCL-90 indicated that positive rates on the 77th( 15. 1% )and 204th days ( 20% ) were all obviously higher than that of pre - deployment( 2. 4% ) ( P ＜ 0. 01 ). However,no statistical differences could be seen in the scores on 142nd day(7.7% ), when compared with that of predeployment(2. 4% ) ( P ＞ 0. 05 ). Conclusions The psychological status of the ship crew, on the whole,degraded markedly during the initial stage of a prolonged deployment, then, would gradually come to normal with adaptation thereafter. Nevertheless, individual psychological status showed a tendency of obvious differentiation in the late stage of deployment.

Animals ; Disease Models, Animal ; Heart Failure

OBJECTIVETo explore the operative method and its clinical effects of pronation and supination external rotation trimalleolar fractures.

METHODSFrom March 2000 to July 2006,42 patients of the pronation and supination external rotation trimalleolar fractures treated with open reduction and internal fixation. Thirty-one were males and 11 were females,with an average age of 40.5 years (from 19 to 76 years). Four cases were open fractures and 38 cases close fractures. The fractures were classified as pronation-external rotation (grade IV) injury in 18 cases and supination-external rotation (grade IV)in 24 cases according to the system of Lauge-Hansen. The time of injury to operation was 2 hours to 27 days. The medial, lateral and posterior malleolus were exposed by standard anteromedial and Gatellier-Chastang approaches. The reduction and internal fixation started with the posterior,then the medial and the lateral malleolus and distal tibiofibular syndesmosis in sequence. The anteroposterior, lateral and mostise X-ray films were taken after operation.

RESULTSAll the patients were followed up for an average time of 13.5 months(from 6 to 24 months). The time of union was from 12 to 16 weeks. The results were excellent in 20,good in 16, fair in 4 and poor in 2 cases according to Baird-Jackson ankle scoring system based on pain, stability, walking ability,range of motion and radiological manifestations. The excellent and good rate was 85.7%. There were no infection,malunion and nonunion of the fractures except that the inserted screw to distal tibiofibular syndesmosis was broken in 1 case.

CONCLUSIONThe key of operative treatment is to restore the anatomy of ankle and to regain the ankle function maximally.

Adult ; Aged ; Ankle Injuries ; surgery ; Female ; Fracture Fixation, Internal ; methods ; Fractures, Bone ; surgery ; Humans ; Male ; Middle Aged ; Pronation ; Supination