A series of quinoline-polyamine conjugates (8a-8n) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). Some of these compounds had potent ChEs inhibitory activity with IC50 values at micromolar range. Compound 8n exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 8.78 micromol x L(-1), and compound 8i showed the most potent inhibition on butyrylcholinesterase (BChE) with IC50 value of 1.60 micromol x L(-1) which was slightly better than rivastigmine. The structure-activity relationship revealed that the chain length of polyamine and linker played important roles for inhibitory activity. Molecular modeling studies showed that 8i targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of cholinesterases.

Objective To study the serotype , biochemical characteristics , virulence gene and multilocus sequence typ-ing(MLST) of S.flexneri 4c in Beijing, Shanghai and Shenyang .Methods Seventy-six strains of S.flexneri 4c isolated from stool samples which had been collected from above-mentioned cities of China were identified with Denka Seiken serum and MASF monoclonal serum .Biochemical characteristics of each strain were identified by API 20E test strip and PCR technology was used for detecting 12 pair virulence genes of S.flexneri.MLST was used to analyze the characteristics . Results The serum agglutination antigen structure of S.flexneri 4c was(Ⅳ:7,8).MASF:B+,Ⅳ:Ⅰ+,7 (8) +.S.flexneri 4c developed different results in biochemical reactions and carried different rates of virulence genes , respectively .The IND test positive rate was 17.11%; MEL weakly positive rate was 3.9%, and ARA test weakly positive rate was 22.37%. Virulence genes were carried at a rate of 89.47% -100%, MLST typing was ST245.Conclusion S.flexneri 4c with serum agglutination antigen structure (Ⅳ:7,8) is a new serotype of S.flexneri.The main biochemical reactions are glucose fermentation and mannitol decomposition .A variety of Shigella related virulence genes are carried .MLST generation is consistent,suggesting that the bacteria might have evolved from ST 270 cloning.

Functional reconstruction of a major injured nerve or muscle group in a destructive limb caused by high energy has always been a big problem for trauma orthopedists.When no local tendon,muscle or nerve is available for transference,functional free muscle transplantation (FFMT) is an ideal functional reconstruction method for severe limb injury characterized by definite curative effect and quick recovery.Gracilis is considered to be an ideal donor site for FFMT because of its anatomic features of long tendon,good excursion,stable blood supply,long neurovascular pedicle,shaded donor site,little donor site loss and sufficient nourishment of the whole musculocutaneous flap by anastomosis of one single major pedicle.It has been widely applied in clinics.Transplantation of single free gracilis flap,double free gracilis flaps,and adductor longus-gracilis flap with single pedicle anastomosis can meet different clinical applications.The best donor motor nerve,which is critical to functional restoration of the affected limb using FFMT,is always a major concern to many scholars.This paper focuses on the advances in functioning free gracilis transplantation in reconstruction of limb motor function,applied anatomy of the gracilis and application of functional reconstruction for major nerve injury and major muscle group defects in a destructive limb,hoping to provide useful information for wider clinical application of FFMT.

OBJECTIVE1-Bromo-3-chloro-5,5-dimethylhydantoin (BCDMH) is a solid oxidizing biocide for water disinfection. The objective of this study was to investigate the toxic effect of BCDMH on zebrafish.

METHODSThe developmental toxicity of BCDMH on zebrafish embryos and the dose-effect relationship was determined. The effect of BCDMH exposure on histopathology and tissue antioxidant activity of adult zebrafish were observed over time.

RESULTSExposure to 4 mg/L BCDMH post-fertilization was sufficient to induce a number of developmental malformations, such as edema, axial malformations, and reductions in heart rate and hatching rate. The no observable effects concentration of BCDMH on zebrafish embryo was 0.5 mg/L. After 96 h exposure, the 50% lethal concentration (95% confidence interval (CI)) of BCDMH on zebrafish embryo was 8.10 mg/L (6.15-11.16 mg/L). The 50% inhibitory concentration (95% CI) of BCDMH on hatching rate was 7.37 mg/L (6.33-8.35 mg/L). Histopathology showed two types of responses induced by BCDMH, defensive and compensatory. The extreme responses were marked hyperplasia of the gill epithelium with lamellar fusion and epidermal peeling. The histopathologic changes in the gills after 10 days exposure were accompanied by significantly higher catalase activity and lipid peroxidation.

CONCLUSIONThese results have important implications for studies on the toxicity and use of BCDMH and its analogs.

Animals ; Antioxidants ; metabolism ; Disinfectants ; toxicity ; Dose-Response Relationship, Drug ; Embryo, Nonmammalian ; drug effects ; Hydantoins ; toxicity ; Time Factors ; Water ; chemistry ; Water Pollutants, Chemical ; toxicity ; Zebrafish

This article was aimed to study the semantic relationship of clinical terminology of traditional Chinese medicine (TCM) from 3 000 clinical medical records and outpatient medical records from books. The aim was to verify the coverage of semantic relationships of UMLS and SNOMED in medical language system with real medical records. The extraction was from the practical aspect in order to improve the semantic relationships involved in TCM clinical practice processes.

Objective: To evaluate the safety and efficacy of microneedle radiofrequency for minimally invasive interventional treatment of bromhidrosis. Methods: From March 2016 to June 2017, Thirty-one bromhidrosis patients were treated with microneedle radiofrequency equipment (Bodytite armpits). Clinical follow up was then evaluated with Park standard. Results: Six to twelve months after surgery (average 8.58 months), malodor were totally eliminated in thirty patients. One patient with residual malodor was cured by second operation. There were no significant scars in all patients. Five patients were observed with mild pigmentation. Conclusions The microneedle radiofrequency treatment is a simple, efficient and safe method for minimally invasive interventional treatment of bromhidrosi.

Objective To investigate effects of goal-directed fluid therapy on inflammatory cytokines under combined anesthesia.Methods 60 patients undergoing colorectal cancer surgery,aged 60 to 85 years old,which were classified as American Society of Anesthesiology(ASA)classⅡ~Ⅲ,were randomly assigned to Goal-directed fluid therapy group(group G,n = 30)and central venous pressure liquid management group(group C,n = 30). Life sign and BIS indexes were collected at the time points,before surgery(T1),after the start of the operation (T2),one hour after surgery(T3),after the operation(T4).Hemodynamic indexes were recorded.Two milliliter blood sample were phlebotomized for evaluation of TNF-α and IL-6 from each patient at T1,T3,T4.The infusion volume, the amount of bleeding,the operation time,anal exhaust time,and length of postoperative hospital stay were recorded. Results Comparing information between the two groups,infusion volume and colloid had an obvious decrease than that of group C(P<0.05).SVV and CVP of group G were much stable than group C.The levels of TNF-α and IL-6 of group G were lower than those of group C(P<0.01).The length of anal exhaust time and post-operative hospital stay group G were faster than that of group C(P<0.01).Conclusions Goal-directed fluid ther-apy is superior on fluid administration. It can reduce the release of IL-6 and TNF-α. It is beneficial to elderly colorectal cancer patients with hypertension.

Objective:To investigate the emergency surgical strategies for patients with acute abdomen during the Corona Virus Disease 2019 (COVID-19) outbreak.Methods:The retrospective and descriptive study was conducted. The clinical data of 20 patients with acute abdomen who were admitted to the Union Hospital Affiliated to Tongji Medical College of Huazhong University of Science and Technology between January 18, 2020 and February 10, 2020 were collected. There were 13 males and 7 females, aged from 25 to 82 years, with an average age of 57 years. All the patients with emergency surgeries received pulmonary computed tomography (CT) examination before surgery, and completed nucleic acid detection in throat swab if necessary. Patients excluded from COVID-19 underwent regular anesthesia, suspected and confirmed cases were selected a proper anesthesia based on their medical condition and surgical procedure. Patients excluded from COVID-19 underwent emergency surgeries following the regular procedure, suspected and confirmed cases underwent emergency surgeries following the three-grade protection.Observation indicators: (1) surgical situations; (2) postoperative situations. Measurement data with normal distribution were represented as average (range). Count data were described as absolute numbers.Results:(1) Surgical situations: of the 20 patients with acute abdomen, 16 patients were excluded from COVID-19, and 4 were not excluded. All the 20 patients underwent emergency abdominal surgeries successfully, of whom 2 received surgeries under epidural anesthesia (including 1 with open appendectomy, 1 with open repair of duodenal bulbar perforation), 18 received surgeries under general anesthesia (including 9 with laparoscopic repair of duodenal bulbar perforation, 3 with open partial enterectomy, 3 with laparoscopic appendectomy, 1 with laparoscopic left hemicolectomy, 1 with laparoscopic right hemicolectomy, 1 with cholecystostomy). The operation time of patients was 32-194 minutes, with an average time of 85 minutes. The volume of intraoperative blood loss was 50-400 mL, with an average volume of 68 mL. (2) Postoperative situations: 16 patients excluded from COVID-19 preopratively were treated in the private general ward postoperatively. One of the 16 patients had fever at the postoperative 5th day and was highly suspected of COVID-19 after an emergency follow-up of pulmonary CT showing multiple ground-glass changes in the lungs. The patient was promptly transferred to the isolation ward for treatment, and results of nucleic acid detection in throat swab showed double positive. Medical history described by the patient showed that the patient and family members were residents of Wuhan who were not isolated at home during the epidemic. There was no way to confirm whether they had a history of exposure to patients with COVID-19. Medical staffs involved in this case did not show COVID-19 related symptoms during 14 days of medical observation. The other 15 patients recovered well postoperatively. The 4 patients who were not excluded from COVID-19 preoperatively based on medical history and results of pulmonary CT examination were directly transferred to the isolation ward for treatment postoperatively. They were excluded from COVID-19 for two consecutive negative results of nucleic acid detection in the throat swab and recovered well. Two of the 20 patients with acute abdomen had postoperative complications. One had surgical incision infection and recovered after secondary closure following opening incision, sterilizing and dressing, the other one had intestinal leakage and was improved after conservative treatment by abdominal drainage. There was no death in the 20 patients with acute abdomen.Conclusions:Patients with acute abdomen need to be screened through emergency forward. Patients excluded from COVID-19 undergo emergency surgeries following the regular procedure, and patients not excluded from COVID-19 undergo emergency surgeries following the three-grade protection. The temperature, blood routine test and other laboratory examinations are performed to monitor patients after operation, and the pulmonary CT and throat nucleic acid tests should be conducted if necessary. Patients excluded from COVID-19 preopratively are treated in the private general ward postoperatively, and they should be promptly transferred to the isolation ward for treatment after being confirmed. Patients who are not excluded from COVID-19 preoperatively based on medical history should be directly transferred to the isolation ward for treatment postoperatively.

Objective:To investigate the kinetic metrics of 68Ga-fibroblast activation protein inhibitor (FAPI)-04 in pancreatic cancers and normal organs by using total-body PET dynamic imaging. Methods:From December 2020 to December 2021, 68Ga-FAPI-04 total-body PET/CT dynamic imaging were performed on 6 pancreatic cancer patients (3 males, 3 females, median age 55.5 years) in Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University. Images were respectively analyzed. Manual delineations of volume of interests (VOIs) on multiple normal organs and pathological lesions were performed and time-to-activity curves (TACs) were generated. A reversible two-tissue compartment model (2TCM) was fitted for each tissue TAC. Rate constants including K1, k2, k3 and k4, and the total volume of distribution ( Vt) were obtained and compared by tissue types. Wilcoxon rank sum test and Spearman correlation analysis were used for data analysis. Results:Kinetic metrics varied significantly among normal organs and pancreatic cancer lesions ( z values: 2.00-1 240.00, all P<0.05). The highest K1 among lesions was observed in primary tumor (0.30 min -1), which was observed in the spleen (1.42 min -1) among normal organs. The highest k2 among lesions was observed in peritoneal metastases (0.24 min -1), which was observed in the spleen (2.59 min -1) among normal organs. Primary tumor showed the highest k3 of 0.17 min -1 among lesions, and the pancreas had the highest k3 of 0.16 min -1 among normal organs. Primary tumor had the highest k4 of 0.03 min -1 among lesions, and the heart, lungs, parotid glands had high k4(0.06 min -1) among normal organs. Vt were higher in pathological lesions compared to normal organs, with the highest in primary tumor (13.78 ml/cm 3). There were correlations between Vt in lesions and SUV mean( rs=0.86, P<0.001) or SUV max ( rs=0.77, P<0.001). Conclusion:The rate constants including K1, k2, k3 and k4, and Vt of 68Ga-FAPI-04 vary among normal organs and lesions.

A series of genistein-polyamine conjugates (4a-4h) were designed, synthesized and evaluated as multi-functional anti-Alzheimer agents. The results showed that these compounds had significant cholinesterases (ChEs) inhibitory activity. Compound 4b exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50 value of 2.75 μmol/L, which was better than that of rivastigmine (5.60 μmol/L). Lineweaver-Burk plot and molecular modeling study showed that compound 4b targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, compound 4b showed potent metal-chelating ability. In addition, it was found that 4a-4h did not affect HepG-2 cell viability at the concentration of 10 μmol/L.