N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
Acetylcholinesterase ; metabolism ; Alkaloids ; pharmacology ; Amines ; chemical synthesis ; pharmacology ; Cholinesterase Inhibitors ; chemical synthesis ; pharmacology ; Drug Design ; Rivastigmine ; pharmacology ; Sesquiterpenes ; pharmacology ; Structure-Activity Relationship ; Thiazoles ; pharmacology

A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Acetylcholinesterase ; metabolism ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Inhibitory Concentration 50 ; Molecular Structure ; Thiazoles ; chemical synthesis ; chemistry ; pharmacology

Objective To investigate the operative indications for polypoid lesions of gallbladder(PLG) and avoid cholecystectomy for PLG without operation signs.Methods Retrospective analysis of 828 cases of PLG confirmed by pathologic examination was made.Results (1)Cancer should be suspected when a patient is older than 50 years or has a polypoid lesion larger than 1.0 cm.(2)The cholecystectomies for PLG accounted for 2.7%-7.1%of all cholecystectomies in the corresponding period,and cholesterol polyps accounted for 86.11%of all PLG,and carcinoma of gallbladder accounted for 1.92%of all PLG.Conclusion At present most of PLG accepting cholecystectomy are cholesterol polyps,so the high-risk factors of the neoplastic polyps and the operative indications for PLG should be considered deliberately.

A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Acetylcholinesterase ; metabolism ; Amines ; chemical synthesis ; pharmacology ; Benzopyrans ; chemical synthesis ; pharmacology ; Cholinesterase Inhibitors ; chemical synthesis ; pharmacology ; Rivastigmine ; Structure-Activity Relationship ; Thiazoles ; chemical synthesis ; pharmacology

Objective To study the relationship between the clinical manifestations and changes of pituitary magnetic resonance imaging(MRI) in short stature children with growth hormone deficiency(GHD).Methods The pituitary MRI finding in 38 cases of short stature children diagnosed as GHD(males 23,females 15;5-14 years old,10 children were in pubertas and Tanner Ⅱ-Ⅲ) were analyzed,and the pituitary morphology,size,signal and pituitary stalk's shape and location were observed.SPSS 12.0 soffware was used to analyze the data.Results The forms of pituitery were plaque in 20 children(53%),cupped in 17 children(45%),and carinate in 1 children.In the 22 cases of completely GHD,18 cases had different levels of anterior pituitary dysplasia,abnormal pituitary stalk and/or pituitary signal changes,5 cases without posterior lobe disappeared high signal and 4 cases with pituitary stalk interruption syndrome;the other 4 cases had completely normal pituitary.In the 16 cases of partially GHD,7 cases had varying degrees of pituitary size and/or abnormal pituitary stalk,8 cases had completely normal pituitary,and 1 case had pituitary adenoma.Conclusion Pituitary MRI could assist diagnosis and evaluate pituitary function in short stature children.

To discuss clinical diagnosis and treatment of cow’s milk protein allergy and cow’s milk protein-induced FPIES (food protein induced enterocolitis syndrome). Methods We retrospectively analyzed clinical data of one infant with milk protein allergy-induced FPIES. Results A 67 days old female on mixed breast and formula feeding developed recurrent diarrhea, abdominal distension, vomiting, mucousy and bloody stools, feeding dififculty, anemia, and failure to thrive since 2 weeks after birth. Laboratory studies showed anemia, increased CRP level and elevation of peripheral white blood count and eosinophil proportion. Milk-speciifc IgE was negative. She was previously hospitalized 4 times, all with admitting diagnosis of“necrotizing enterocolitis”. We treated her with milk protein elimination for 4 weeks and all symptoms were resolved. Milk protein re-challenge test was positive, consistent with clinical features of cow’s milk protein allergy-induced infant FPIES. Conclusions Cow’s milk protein allergy and cow’s milk protein-induced FPIES can present with non-speciifc and variable clinical symptoms and signs, and should be considered in the differential diagnosis.

OBJECTIVETo evaluate the safety and efficacy between endoscopic papillary balloon dilatation (EPBD) and endoscopic sphincteropapillotomy ( EST) for common bile duct stones using meta-analysis method.

METHODSRandomizd controlled trials comparing EPBD with EST for common bile duct stones and published from January 1990 to July 2012 were recruited. This meta-analysis was conducted to estimate short-term and long-term complications. Fixed random effect model or random effect model was established to analyze the data.

RESULTSTwelve randomizd controlled trials were included in this analysis. These studies included 1865 patients, 925 of them were treated with EPBD and 940 were treated with EST. The analysis of basic characteristics of these included studies showed that: compared to EST, patients in the EPBD group were younger (OR = -1.16, 95% CI: -1.49 to -0.84, P = 0.00), while in two groups, there were no significant difference (P > 0.05) in gender proportion, average size of stones, number of gallstones, previous cholecystectomy, the number of merged duodenal diverticulum, common bile duct diameter, the total follow-up time. Also, compared to EST, the overall stone clearance in the EPBD group was lower (OR = 0.64, 95% CI: 0.42 to 0.96, P = 0.03), pancreatitis incidence was higher (OR = 2.67, 95% CI: 1.61 to 4.43, P = 0.00), incidence of bleeding (OR = 0.12, 95% CI: 0.04 to 0.34, P = 0.00), acute cholecystitis (OR= 0.39, 95% CI: 0.18 to 0.84, P = 0.02), total long-term complication rate (OR = 0.53, 95% CI: 0.36 to 0.77, P = 0.01), stone recurrence rate more than a year were lower (OR= 0.48, 95% CI: 0.26 to 0.90, P = 0.02). While in two groups, there were no significant difference (P > 0.05) in the stone removal on 1 '' attempt, the total near-term complications and acute cholangitis.

CONCLUSIONSOn the basis of lower rates of bleeding, EPBD seems to be preferred strategy over EST for endoscopic remove of common bile duct stones in patients who have coagulopathy. Although stone recurrence rate more than a year of EPBD is lower, but the overall stone clearance rate is lower and the risk of pancreatitis is higher than that of EST.

Dilatation ; Gallstones ; surgery ; Humans ; Postoperative Complications ; epidemiology ; Randomized Controlled Trials as Topic ; Sphincterotomy, Endoscopic ; Treatment Outcome

Objective To investigate the value of diffusion weighted imaging(DWI)in predicting delayed encephalopathy of the rabbits brain after carbon monoxide(CO)poisoning.Methods Sixty healthy rabbits were put into self-made poisoning cabinet and were poisoned by inhalation of CO.Aeration of CO was stopped when the rabbits became comatous,and the cabinet was kept airpoof for 6 h.The rabbits underwent MRI before poisoning,at 1 h,3 d,5 d,7 d,15 d,30 d,45 d,and 60 d after poisoning respectively. Axial and sagittal T_2WI,axial T_1WI and DWI were performed.In the rabbits that did not show symptoms of delayed encephalopathy,the observation was discontinued on the 60~(th)day.In the rabbit that showed the symptoms,the observation was discontinued on the 30~(th)——45~(th)day.The changing pattern of cortical ADC values before and after CO poisoning was observed and its relationship with delayed encephalopathy was investigated.Results In the group without delayed encephalopathy(15 rabbits),the ADC value at 1 h after poisoning[(7.58?0.36)?10~(-4)mm~2/s]decreased significantly compared with the pre-poisoning value[(8.02?0.35)?10~(-4)mm~2/s](q=0.4441,P0.05).In the group with delayed encephalopathy(15 rabbits),the ADC value at 1 h after poisoning [(7.40?0.32)?10~(-4)mm~2/s]decreased significantly compared with the pre-poisoning value[(8.08? 0.32)?10~(-4)mm~2/s](q=0.6728,P

OBJECTIVESTo evaluate preliminary clinical experience for combining awake craniotomy and intraoperative language brain mapping within the integrated 3.0 T intraoperative magnetic resonance imaging (iMRI) suite.

METHODSFrom December 2010 to April 2011, 11 right hand-dominant patients with left glioma were involved in, or adjacent to, eloquent cortex was carried out awake craniotomies with cortical stimulation within an integrated 3.0 T iMRI suite. Aphasia battery of Chinese was used to test the language function before the operation. During the procedure, after the occipital, temporal, and supraorbital nerves were blocked by the anesthesiologists, the head was fixed with a custom high-field MRI-compatible head holder. The skull and dura was opened as usual and language brain mapping was then performed. Language testing followed a set protocol: counting numbers from 1 to 50, naming objects, reading single words. Resection of the tumor was guided by neuronavigation system and continued until eloquent areas were encountered or the margin of assessment was reached. An interdissection MRI was acquired to evaluate the glioma removal in a movable MRI scanner after minimal draping. Meanwhile, adverse effects caused by electrical stimulation and iMRI were recorded. The follow-up speech tests were assessed on 7th day and 1 month at least after the operation.

RESULTSThe combined use of 3.0 T iMRI and awake craniotomy was performed safely in all patients. No adverse effects were reported. The duration of surgery was prolonged by 2 to 4 h. The patients' perception of iMRI during surgery was favorable. First-look MRI studies led to further resection attempts in 6/11 cases as well as a 3/11 increase in the number of gross-total resections. One week after surgery, baseline language function worsened in 4 cases. However, no patients had a persistent language deficit one month after surgery.

CONCLUSIONSAwake craniotomy and direct cortical electrical stimulation can be performed safely and effectively within a 3.0 T iMRI suite. The combination of high-field iMRI and awake craniotomy may facilitate safe removal of eloquent glioma.

Adult ; Aged ; Anesthesia ; methods ; Brain Neoplasms ; surgery ; Cerebral Cortex ; surgery ; Craniotomy ; methods ; Female ; Glioma ; surgery ; Humans ; Magnetic Resonance Imaging ; Male ; Middle Aged ; Monitoring, Intraoperative ; Neuronavigation ; methods ; Wakefulness

OBJECTIVETo analyze the efficacy of percutaneous endoscopic gastrostomy (PEG) in pediatric patients.

METHODFrom October 2011 to October 2014, children in the gastrointestinal ward of Guangzhou Women and Children's Medical Center received PEG or jejunal tube PEG(JET-PEG). The success rate, operation time were recorded. The changes of their weight, enteral nutrition calories and the incidence of pneumonia before and after the first 6 months of operation were compared. Follow-up was conducted until October 2014, the recent and long term complications, the length of indwelling time, the replacement or removal of the tube were recorded, the patients swallowing function or the primary disease's outcomes were observed.

RESULTOf the 13 cases, 10 were male, 3 were female, their average age was 2 years (range 1.8 months-9 years). We performed PEG for 12 of the patients who had congenital craniofacial problems that led to feeding difficulties or recurrent cough and pneumonia (6/12), or neurological disorders (6/12) with inability to swallow, and in one case JET-PEG was performed, this child suffered from chronic intestinal pseudo-obstruction with vomiting and abdominal distension. The gastrostomy was successful in all the patients through one operation, the average operation time of PEG was (25 ± 3) minutes, JET-PEG was 60 minutes. One local skin infection was noted, no long-term complication occurred. In the first 6 months after operation, all the patients gained weight((5.5-30.5) kg postoperation vs. (3.0-30.0) kg preoperation), and 12 cases' enteral nutrition calories increased (from (209-502) to(272-543) kJ/(kg·d)), the incidence of pneumonia decreased in the children who had recurrent pneumonia before the operation (from (0-1.5) to (0-0.16) per month). Until October 2014, their average length of gastric tube indwelling time was 17.8 months (range 4-36 months). In 4 cases PEG tube was removed when they could eat completely independently, the other 9 needed enteral vein nutrition via PEG tube or jejunal tube, in 3 of them balloon type gastric fistula tube was applied. Two of the 13 cases who had cleft palate received stomatological operations when their weight grew to meet the standard.

CONCLUSIONPEG and JET-PEG are safe and effective method for enteric nutrition feeding in pediatrics, the technique causes minimal trauma and has rapid postoperative recovery, few complications, good aesthetic appearances and simple nursing, it can significantly improve their nutritional status and quality of life.

Child ; Child, Preschool ; Enteral Nutrition ; methods ; Female ; Gastrostomy ; adverse effects ; Humans ; Incidence ; Infant ; Male ; Nervous System Diseases ; therapy ; Pneumonia ; therapy