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 provide reference for developing effective interventions to self-medication and promoting reason-able self-medication. METHODS:Questionnaires were designed based on the modified Anderson's behavioral model of health ser-vices. By using cluster sampling,residents were randomly selected from 4 districts of Wuhan city to analyze the self-medication be-havior and its influential factors. RESULTS:Totally 204 questionnaires were sent and 199 were recovered with effective rate of 97.5%. The result showed 47.7% residents who perceived discomfort within 2 weeks medicated themselves,and the rate was high-er thansee the doctor. Among self-medication residents,the rate of mild disease,general and serious disease was separately 50.5%,46.3% and 3.2%. The length of illness<7 d and the length of illness ≥7 d accounted for 95.8% and 4.2%,separately. Cold and cough was the highest cost disease for self-medication. The reasons for selecting self-medication were:no need tosee the doctor(43.2%),trouble-saving(23.1%),high medical costs(14.6%),no time to see the doctor(14.6%). 54.1% residents acquired basic medication knowledge from the past experience,25.5% from other's recommendation,and the other from the inter-net,newspaper and magazines. As for the effect of self-medication in the past one year,75.4% residents considered most were ef-fective. 18.6%had suffered from ADR due to self-medication;the incidence of ADR in the residents reading the instruction was sig-nificantly lower than those not reading the instruction(P<0.05);the ratio of reading the instruction in residents with low education level was significantly lower than that with high education level(P<0.05). Single factor analysis showed that residents'choice of self-medication were significantly influenced by the marital status,education,monthly income,medicare,accessibility of medical institutions,the severity of disease and duration of illness(P<0.05). The proportion of self-medication for married group was sig-nificantly higher than unmarried group;the proportion of self-medication for low education level group was significantly higher than high education level group;the proportion of self-medication for low monthly income group was significantly higher than high monthly income group;the proportion of self-medication for group with business medical insurance or self payment was significant-close to medical institutions;the proportion of self-medication for mild disease group was significantly higher than serious disease group;the proportion of self-medication for length of disease≥7 d was significantly lower than length of disease<7 d. Results of multivariate analysis showed that severity of disease and length of disease were the important influential factors for the choice of self-medication(P<0.05). CONCLUSIONS:Self-medication is common in Wuhan city,and mainly for general and chronic dis-ease. Residents don't pay enough attention to reading the drug instructions. Self-medication is affected by various factors which has a certain health risks.

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.

Hepatocellular carcinoma is one of the most common malignancies of liver cancer.Partial hepatectomy and liver transplantation are potentially curative treatments in patients with hepatocellular carcinoma.However,the postoperative tumor recurrence rate is high with poor long-term survival outcome.Studies have shown that the presence of microvascular invasion is an independent risk factor of post-resection prognosis.Therefore it draws attention that whether postoperative TACE can prevent the recurrence of liver cancer.This article reviews the research progress postoperative TACE effect on hepatocellular carcinoma patients with microvascular invasion,in order to provide the reference for selection of further treatment.

Objective To observe the effects of associating liver partition with portal vein ligation for staged hepatectomy (ALPPS) on liver regeneration of the unligated lobe with cirrhosis.Methods 60 liver cirrhosis SD rats were randomly divided into three groups:C-ALPPS group (n =20,liver cirrhosis + ALPPS),C-PVL group (n =20,liver cirrhosis + PVL) and C-Sham group (n =20,liver cirrhosis + sham operation).60 normal SD rats were randomly divided into three groups:N-ALPPS group (n =20,normal liver + PVL),N-PVL group (n =20,normal liver + PVL) and N-Sham group (n =20,normal liver + sham operation).The weight ratio of unligated lobes/total liver,proliferating cell nuclear antigen (Ki-67) and liver function were compared before operation and 2,4 and 7 days after operation.Results Except for sham operation group,liver weight ratios of unligated livers on the 4th and 7th days after operation were lower than those in the normal group (P ＜ 0.05).The weight ratios of unligated lobes/total liver in C-ALPSS group and N-ALPPS group on 4th and 7th day postoperation were (54.3 ± 3.1)％ vs.(61.2 ± 2.1)％,(65.0 ± 4.1) ％ vs.(79.2 ± 1.1) ％.The weight ratio unligated lobes/total liver in group C-PVL and group N-PVL at 4th and 7th day postoperation were (52.4 ± 1.8) ％ vs.(56.6 ± 2.0) ％,(63.8 ± 3.1) ％ vs.(70.0 ± 2.5) ％.There was no significant difference on weight ratio of unligated lobes/total liver between C-ALPPS group and C-PVL group at each time point (P ＜ 0.05).There was significant difference on the alanine transaminase (ALT),aspartate aminotransferase (AST) and albumin (ALB) levels between cirrhosis group and normal group at 4 and 7 days after operation (P ＜ 0.05).The expression level of Ki-67 in cirrhosis group was significantly lower than that in normal group at each time point (P ＜ 0.05).The expression level of Ki-67 in group C-ALPSS and group N-ALPPS at 2nd,4th and 7th day after operation were (19.4 ± 4.8)％ vs.(84.1 ±8.9)％,(33.6±3.5)％ vs.(70.2±7.2)％,(20.2±2.5)％ vs.(50.7±4.4) ％,and the expression level of Ki-67 in group C-PVL and group N-PVL at 2nd,4th and 7th day postoperationwere (21.1±4.0)％ vs.(52.1 ±7.3)％,(32.4 ±5.9)％ vs.(35.6 ±5.3)％,(15.5± 4.6) ％ vs.(12.2 ±4.9) ％.There was no significant difference of Ki-67 levels between C-PVL group and C-ALPPS group at 2 and 4 days after operation (P ＜ 0.05).Conclusions In normal rats,the liver regeneration rate after ALPPS was significantly higher than that after PVL.The liver regeneration rate after ALPPS in cirrhotic rats was significantly lower than that in normal rats after ALPPS.There was no significant difference of the liver regeneration rate between ALPPS and PVL in cirrhotic rats.

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

OBJECTIVETo evaluate the safety and feasibility of laparoscopic gastrectomy for gastric stump cancer.

METHODSClinical and follow-up data of 7 patients who underwent laparoscopic gastrectomy for gastric stump cancer in our department from January 2008 to July 2015 were analyzed retrospectively.

RESULTSThere were 5 male and 2 female patients, with a mean age of (62.1±10.7) years. Initial gastrectomy was performed for gastric cancer in 3 patients and peptic ulceration in 4. The initial surgery was B-II( gastrojejunostomy in 6 patients and Roux-en-Y gastrojejunostomy in 1. Duration between primary gastrectomy and occurrence of gastric stump cancer was ranged from 6-30 years for peptic ulceration, and from 11-15 years for gastric cancer. During the operation, adhesiolysis and exploration to locate the tumor were performed. Following total remnant gastrectomy and lymphadenectomy, intracorporeal anastomosis was accomplished by Roux-en-Y reconstruction. The methods of intracorporeal esophagojejunostomy were end-to-side approach using a circular stapler in 1 patient, side-to-side approach using an endoscopic linear staple in 2 patients, and hand-sewn technique in 4 patients. The operation time was (247.1±17.5) minutes and the intraoperative blood loss was (100.0±30.8) ml without transfusion. The number of retrieved lymph node was 19.1±4.8. The first flatus time, diet resumption time, postoperative hospital stay were (3.3±1.5) days, (3.7±0.8) days, (9.4±2.6) days, respectively. One patient experienced gastrointestinal bleeding that was managed conservatively and ultimately cured. Seven patients were followed up till January 2016. After follow-up from 6 to 38 months, 1 patient died of peritoneal metastasis 17 months after surgery, and 1 patient died of Alzheimer's disease 19 months after surgery. The other 5 patients were still alive without metastasis or recurrence.

CONCLUSIONLaparoscopic gastrectomy for gastric stump cancer is feasible and safe.

Aged ; Anastomosis, Roux-en-Y ; Blood Loss, Surgical ; Female ; Gastrectomy ; Gastric Bypass ; Gastric Stump ; pathology ; surgery ; Humans ; Laparoscopy ; Length of Stay ; Lymph Node Excision ; Male ; Middle Aged ; Neoplasm Recurrence, Local ; Operative Time ; Retrospective Studies ; Stomach Neoplasms ; surgery ; Surgical Stapling

Objective To compare the clinical results of laparoscopic spleen-preserving distal pancreatectomy (LSPDP) and open spleen-preserving distal pancreatectomy (OSPDP).Methods From Jan 2014 to Aug 2017,the clinical results of 30 patients undergoing LSPDP were compared with those of 20 OSPDP patients.The postoperative pancreatic fistula rate was the main observation index.Results There was significant difference in operation time [(140.33 ±55.93) min vs.(182.71 ±43.51)min],blood loss [(175.61 ± 180.78) ml vs.(253.51 ± 176.06) ml],postoperative hospital stay [(6.16 ± 7.22) d vs.(8.85 ± 9.36) d],postoperative exhaust [(2.17 ± 1.43) d vs.(3.10 ± 1.89) d],and postoperative feeding time [(2.26 ± 1.78)d vs.(3.42 ±2.01)d] between LSPDP and OSPDP.LSPDP group was better than OSPDP group (all P ＜ 0.05).The rate of postoperative pancreatic fistula (66.7％ vs.70.0％) and overall complications (80％ vs.90.0％) were not statistically different between the two groups.Pancreatic leakage occurred in 20 cases,lung infection in 1 case,peritoneal infection in 1 case and chylous leakage in one case in LSPDP group,while pancreatic leakage in 14 cases,lung infection in 2 cases,and peritoneal infection in 2 cases in OSPDP group,all were cured by conservative therapy.Conclusions LSPDP is a safe,effective,less traumatic and more economic surgical approach for benign cystic tumors located at the body or tail of the pancreas.

Objective To study the safety,feasibility and efficacy of trans-diaphragm thoracoscopic hepatectomy for liver carcinoma.Methods Thoracoscopic hepatectomy was performed in 5 cases with single liver neoplasm from Jan 2016 to Aug 2018,including hepatocellular carcinoma (HCC) in 4 cases and metastatic liver cancer in 1 case.During the operation,the diaphragm just above the tumor was opened.Then we completely removed the tumor.After meticulous hemostasis of cut surface,the diaphragm was closed.A thoracic drain was placed.Results Thoracoscopic hepatectomy was performed successfully in all 5 cases,the median total operating time was 140 min (120-230 min),and the median blood loss was 300 ml (200-500 ml),Patients recovered quickly.One patient had pleural effusion and recovered after chest drainage.There were not other major post-operative complications.During 6 to 31 months' follow-up,one patient was lost to follow-up,two patients were survival with tumor recurrence,two patients were recurrence free.Conclusions Thoracoscopic hepatectomy is a safe and feasible operation in selected liver cancer patients and has advantages in post-operative recovery.

Objective:To evaluate the efficacy of splenic artery ligation on liver function recovery and hypersplenism in liver transplant patients with end-stage liver disease complicating portal hypertension and hypersplenism.Methods:From Jan 2016 to Jan 2019, the clinical data of patients undergoing liver transplantation at our hospital were analyzed retrospectively, among which 53 patients were enrolled in the study with end-stage liver disease complicated with portal hypertension and hypersplenism. Patients were divided into ligation group( n=23) and no ligation group( n=30). The serum liver function and white blood cells, platelets and postoperative complications were compared. Results:20 pairs of patients were successfully matched by PSM method. All patients were followed up for over 6 months.There was no statistically significant difference between the two groups in all the observation points within 2 weeks after operation; Within 6 months, there was no statistically significant difference in WBC, platelet and Hgb.Statistically significant differences in postoperative complications such as infection, gastrointestinal bleeding, and splenic artery stealing syndrome were also not found between these two groups.Conclusions:Splenic artery ligation during liver transplantation does not accelerate liver function recovery nor ameliorate hypersplenism.