AIM: To synthesize a number of novel heterocyclic compounds and screen for their biological activities. Sixteen title compounds were prepared. METHODS: These novel compounds were prepared by the reaction of 3-aryl/aryloxymethyl-4-amino-5-mercapto-1,2,4-triazoles with aryl carboxylic acids in the presence of phosphorus oxychloride. The structures of these compounds were confirmed by elemental analysis, IR, 1HNMR and MS. The reaction conditions for the synthesis had been investigated. All the compounds were screened for antimicrobial activity against bacteria S.aureus, E.coli and B.subilis. The concentration of the test compounds was 0.002%. The antibacterial activities of the test compounds were compared with those of penicillin and gentamicin. RESULTS: The results display that some of them possess strong biological activities.CONCLUSION: Syntheses of these novel heterocyclic compounds and study on their biological activities are very important and valuable in medicine.

Objective To investigate the diagnosis and treatment of congenital mesenteric hiatal hernia in aduls.Methods The retrospective cross-sectional study was conducted.The clinical data of 11 adult patients with congenital mesenteric hiatal hernia who were admitted to the First Affiliated Hospital of Henan University from January 1999 to January 2016 were collected.All patients underwent abdominal X-ray and ultrasound examinations.Patients diagnosed as with intestinal obstruction or suspected intra-abdominal hernias underwent abdominal CT examination,and then were finally confirmed during surgery.Patients diagnosed as with mesenteric hiatal hernia received necrotic tissues resection and tissue repair (small intestine resection and anastomosis) if there was necrosis of hernia contents,and closing mesenteric hiatus.Patients without small intestine necrosis received closure of mesenteric hiatus after retraction of the hernia contents.Observation indicators:(1) clinical manifestations,(2) imaging findings,(3) treatment,(4) pathological examination,(5) follow-up situations.Follow-up using outpatient examination and telephone interview was performed to detect the postoperative complications up to March 2017.Results (1) Clinical manifestations:all 11 patients were acute onset,with incentives of satiation,postprandial exercise and diarrhea.The time from onset to admission was 2.0-30.0 hours,with an average time of 9.8 hours.The main symptoms included abdominal pain,nausea and vomiting,exhaust reduction and other intestinal obstruction performances.Eleven patients received physical examination,and 10 showed abdominal bulge,including 9 with intestinal type.Eleven patients had abdominal tenderness,and 9 combined with rebound tenderness.Abdominal percussion of 11 patients showed hyperresonant without shifting dullness,and active,muted and fading bowel sounds were detected in 1,3 and 7 patients,respectively.(2) Imaging examination:of 11 patients receiving abdominal X-ray examination,2 had intestinal loop and 4 had the intestinal obstruction performances such as typical gas-liquid plane.Abdominal ultrasound examination of 11 patients showed no specific findings due to abdominal intestinal gas,and 10 with peritoneal effusion.Of 11 patients,1 didn't receive abdominal CT scan due to preoperatively misdiagnose with acute appendicitis and 10 underwent abdominal CT scan.Nine patients were diagnosed with intestinal torsion by abdominal CT scan and then underwent enhanced CT scan,and 8 with small mesenteric vascular torsion and swirling sign were diagnosed with small intestine torsion and partial necrosis of small intestine.(3) Treatment:1 patient preoperatively misdiagnosed with acute appendicitis was converted to exploratory laparotomy,and 10 patients underwent exploratory laparotomy due to complete intestinal obstruction or progressive increase in symptoms.Intraoperative exploration showed that intestinal mesenteric hiatus and colon mesenteric hiatus were respectively in 8 and 3 patients,and hiatuses were round or oval,with a diameter of 2.0-8.0 cm and an average of 4.4 cm.Hernia contents were small intestine.The partial small intestine in 10 patients were resected and then mesenteric hiatus was closed due to necrosis of the small intestine,with removal length of 110-250 cm and an average of 176 cm,and length of remaining small intestine was 80-230 cm,with an average of 159 cm.The hernia into small intestine in 1 patient without complete necrosis was retracted to abdominal cavity after symptomatic treatment,and closing mesenteric hiatus.Eleven patients were cured and out of hospital after operation,without nosocomial complications.(4) Pathological examination:small intestine ischemic necrosis was detected in 10 patients after partial small intestine resection.(5) Follow-up situations:all patients were followed up for 12-24 months,without malnutrition,short bowel syndrome and other complications.Conclusions Without history of abdominal trauma or surgery,with incentives of the satiation,postprandial exercise and diarrhea,abnormal retroperitoneal small intestine shadow and small intestinal torsion diagnosed by CT scan and absent intestine sign by enhanced CT scan can be helpful to diagnose congenital mesenteric hiatal hernia in adults and small intestinal necrosis.Surgery is the only effective method in the treatment of congenital mesenteric hiatal hernia in adults.

Objective To investigate the standard hemicraniectomy and temporal muscleresection therapeutic in the treatment effect of massive cerebral infarction patients .Methods Looking back at my hospital from February 2006 to October 2012 massive cerebral infarction patients ,30 cases were divided into two groups ,namely simple drug treatment(group A) ,the standard hemicrani-ectomy combined temporal muscleresection treatment (group B) .Followed up two groups of patients and deaths neurological deficit situation after treatment ,compared two groups of patients in hospital mortality and one month after treatment ,neurological impair-ment score .Results After treatment ,the patient midline reply ,mortality ,cure rates three aspects ,group B than the group A .Con-clusion Standard hemicraniectomy combined temporal muscle resection in the treatment can reduce the mortality rate of patients w ith active .

Objective:This study aims to determine the efficacy of chemotherapy and to identify potential chemotherapy agents for advanced primary duodenal carcinoma (PDC). Methods:Fifty-six patients with advanced PDC, who did and did not receive chemo-therapy, were involved in this study. Response rates (RR), disease control rates (DCR), progression-free survival (PFS), and overall sur-vival (OS) were analyzed. Results:The overall RR and DCR of 43 patients were 19.04%and 71.42%, respectively. The patients who re-ceived chemotherapy agents fluorourzcil and oxaliplatin exhibited higher RR compared with patients who received other chemotherapy combinations (35.29%vs. 7.69%, P=0.010 9). Palliative chemotherapy improved the OS of patients with advanced PDC compared with patients who did not receive chemotherapy (13.35 months vs. 5.65 months, HR=0.203, 95%CI:0.083 to 0.497, P=0.000 5). Compared with the use of other chemotherapy regimens, treatment with a fluorourzcil-based chemotherapy agent resulted in a longer PFS (5.08 months vs. 1.08 months, HR=0.004, 95%CI:0.000 to 0.315, P=0.013 2). Multivariate analysis indicated mucinous histology and lymph mode metastasis as factors predictive of poor prognosis in patients with advanced PDC. Conclusion:Palliative chemotherapy may im-prove the OS of patients with advanced PDC.

Objective:This retrospective study aims to determine the efficacy of chemotherapy and improve a salvage chemother-apy agent for metastatic colorectal cancer (MCRC) after failure of treatment with irinotecan and oxaliplatin. Methods:Between Janu-ary 2002 and March 2013, 37 patients with metastatic MCRC who had progressed after treatment with irinotecan and oxaliplatin were analyzed for their response rate (RR) and progression-free survival (PFS). Results:The overall RR of the 37 patients was 13.51%, with 5 cases of partial response (PR), 12 cases of disease stabilization (SD), and 20 cases of progression (PD). Compared with other chemo-therapy regimens, treatment with a pemetrexed-based chemotherapy agent had a higher RR (17.64%vs. 10.00%, P=0.64) without a lon-ger PFS (2.00 months vs. 1.63 months, HR=0.79, 95%, CI:0.35 to 1.78, P=0.58). Compared with other chemotherapy regimens, treat-ment with a raltirexed-based chemotherapy agent had a higher RR (16.67%vs. 12.00%, P=0.34) without a longer PFS (1.58 months vs. 1.90 months, HR=2.24, 95%, CI:0.98 to 5.12, P=0.06).Conclusion:In patients with MCRC after failure of treatment with irinotecan and oxaliplatin, a pemetrexed-based or raltirexed-based chemotherapy agent may beneficial during salvage treatment and is therefore worthy of further study.

OBJECTIVETo investigate the effects of Annexin A2 (ANXA2) deficiency on the malignant biological behaviour of hepatoma cells.

METHODSThe human hepatocellular carcinoma (HCC) cells lines MHCC97-H, HepG2, SMMC-7721, SMMC-7402 and L02 were evaluated. The expression and distribution of ANXA2 were analysed by western blotting, real-time PCR, immunofluorescence and immunohistochemistry.Cell cycle was assessed by flow cytometry and propidium iodide staining. Effects of ANXA2 silencing on invasion and migration potential were assessed by transwell assay and wound healing assay, respectively. Proliferative potential was assessed by CCK-8 kit in vitro and xenograft tumour-growth assay in vivo. The t-test, chi square test, rank sum test, q-test and F-test were used for statistical analyses.

RESULTSThe expression level of ANXA2 was markedly higher in the MHCC97-H cells with high metastasis potential than in the HepG2, SMMC-7721, SMMC-7402 and L02 cells. The efficiency of shRNA-mediated ANXA2 deficiency was more than 80%. Immunofluorescence analysis of the MHCC97-H cells indicated that ANXA2 expression was mainly localized to the cellular membrane and cytoplasm, with some nuclear localization. Down-regulation of ANXA2 led to S-phase arrest of HCC cells (q =8.001, P =0.002) and an inhibition of proliferation (q =17.140, P less than 0.01), migration (q =12.808, P less than 0.01) and invasion potential (q =9.069, P =0.002). Xenograft tumour-growth assay indicated that shRNA targeting of ANXA2 led to lower tumour weight (q =11.968, P < 0.001) and down-regulated ANXA2 expression (Z =2.530, P =0.011).

CONCLUSIONDown-regulation of Annexin A2 gene transcription effectively changes the biological behaviours of hepatoma cells, and may represent a potential target of HCC molecular therapies.

Animals ; Annexin A2 ; genetics ; Carcinoma, Hepatocellular ; pathology ; Cell Line, Tumor ; Cell Proliferation ; Humans ; Liver Neoplasms ; pathology ; Neoplasm Transplantation ; RNA, Small Interfering ; genetics ; Signal Transduction ; Transcription, Genetic

Objective To analyze and compare the postoperative complications and perioperative data of laparotomy surgery and combined laparoscopy and choledochoscopy surgery for non-severe acute cholangitis.Methods Retrospective analyzed the clinical data of 134 patients,with non-severe acute cholangitis at First Affiliated Hospital of He'nan University from June 2015 to May 2017.The patients were divided into combined group (76 cases) and traditional group (58 cases) according to operation mode,and the postoperative complications and perioperative data including amount of bleeding,postoperative exhaust time,operative time,incision length,length of stay and extubation time of T-tube were compared.The measurement data were expressed by (-x ± s),and the t test was used between the groups.Comparison of count data were analyzed using the chi-square test.Results The amount of bleeding,postoperative exhaust time,incision length and length of stay were respectively (48.90 ± 16.23) ml,(1.94 ± 0.45) d,(4.53 ±1.97) cm,(7.81 ±2.23) d in the combined group and were significantly less than those in the traditional group (98.53 ± 17.34) ml,(2.42 ± 0.56) d,(8.34 ± 2.05) cm,(12.27 ± 1.56) d,with statistically significant diffbrences between the two groups (t =7.173,8.242,12.847,8.242;P =0.000,0.000,0.004,0.021).The operative time of the combined group was (157.75 ± 17.34) min,and that of the traditional group was (138.43 ±23.84) min,but there was no significant difference between the two groups (t =13.661,P =0.069).The extubation time of T-tube in the combined group and the traditional group was (29.78 ± 1.54) d and (22.54 ± 0.96) d,respectively.The differences between the two groups were statistically significant (t =3.435,P =0.043).Postoperative complications occurred in 16 out of all 134 patients,and bile leakage,residual stones and incision infection were the top three complications.The incidence of postoperative complications in the combined group and the traditional group was 5.26％ (4/76)and 20.69％ (12/58),respectively.The differences between the two groups were statistically significant (x2 =7.445,P =0.006).Conclusion The incidence of complications of calculous non-severe acute cholangitis combined laparoscopy and choledochoscopy is lower than traditional surgical operations,and more conforms to the enhanced recovery after surgery,and the postoperative recovery is faster than that of the traditional group.

China ; Humans ; Streptococcus pneumoniae