In order to improve the positional adaptability of our previously reported naphthyl diaryltriazines (NP-DATAs), synthesis of a series of novel biphenyl-substituted diaryltriazines (BP-DATAs) with a flexible side chain attached at the C-6 position is presented. These compounds exhibited excellent potency against wild-type (WT) HIV-1 with EC values ranging from 2.6 to 39 nmol/L and most of them showed low nanomolar anti-viral potency against a panel of HIV-1 mutant strains. Compounds and had the best activity against WT, single and double HIV-1 mutants and reverse transcriptase (RT) enzyme comparable to two reference drugs (EFV and ETR) and our lead compound NP-DATA (). Molecular modeling disclosed that the side chain at the C-6 position of DATAs occupied the entrance channel of the HIV-1 reverse transcriptase non-nucleoside binding pocket (NNIBP) attributing to the improved activity. The preliminary structure-activity relationship and PK profiles were also discussed.

Pancreatic cancer has the highest mortality among malignant cancers. Known asthe king of cancer,it lacks early symp-toms, diagnostic methods and oncologic markers. Early lymph node metastasis could be found in this disease. Moreover, advanced panereatic cancer is incurable by surgery. Due to the limited efficacy of surgery, as well as radiotherapy and chemotherapy tolerance, therapeutic methods for pancreatic cancer are being explored. L1 cell adhesion molecule (L1CAM) is a member of the cell adhesion molecule inmunoglobulin (Ig) super family that is usually expressed in normal developing nervous tissues. L1CAM is highly expressed in pancreatic cancer cells, binds withα5-integrin to activate downstream factors that mediate tumor metastasis and invasion via the TGF-β1/JUK/slug signaling pathway, induces epithelium-mesenchymal transition, and resists chemotherapy drugs. However, L1CAM forms abnormal vessels that increase the invasiveness of pancreatic cancer cells. This abnormal L1CAM expression in pancreatic can-cer cells is a new therapeutic target in pancreatic cancer treatment. Therefore, future studies on L1CAM could promote the develop-ment of pancreatic cancer therapy and provide new treatment methods.

Objective To explore the diagnosis and treatment of bronchogenic cyst in the abdomen.Methods Clinical data of 7 cases with abdominal bronchogenic cyst in the First Affiliated Hospital of China Medical University from October 2001 to February 2016 were retrospectively analyzed.Results Of the 7 patients,5 were male and 2 were female aging from 36 to 50 years with a median age of 37 years.Two cases were complaining for upper abdominal pain,5 cases were asymptomatic.Ultrasonography revealed hypoechoic or anechoic mass.Color doppler flow imaging showed no blood flow.Contrast-enhanced CT scans showed no obvious enhancement in 6 out of 7 cases,all patients underwent cystectomy successfully.Cysts were of unilocular in 6 cases and multilocular in one.Bronchogenic cysts were diagnosed by pathology in all 7 cases.Six patients were followed up from 1 month to 6 years with no recurrence.Conclusions Abdominal bronchogenic cyst is benign and postoperative prognosis is very good.

The detection rate of pancreatic cystic neoplasms obviously increases with the development of imaging technology. However, it is still difficult to make the differential diagnosis between different types of pancreatic cystic neoplasms. For pancreatic cystic neoplasms, the physical condition of the patient, tumor size, location, patient preference, and other potential factors should be considered to develop an individualized treatment. The incidence rate of complications is high, although the operative mortality of pancreatic cystic neoplasms is very low. Therefore, it is necessary to strictly make the treatment decision for pancreatic cystic neoplasms.

Pancreatic carcinoma is currently one of the most intractable malignant tumors of the digestive tract. Studies have found that the occurrence, progression and metastasis of pancreatic carcinoma are closely associated with the tumor's glycolytic pathway, most pancreatic carcinomas show the elevated glycolytic phenotype. To some extent, affecting the glycolytic pathway can influence the energy metabolism of the tumor without affecting the normal cells theoretically. Therefore, glycolytic pathway may become a new target for the treatment of pancreatic carcinoma.
Energy Metabolism ; Glycolysis ; Humans ; Pancreatic Neoplasms ; metabolism ; physiopathology

Background and purpose:The prognosis of pancreatic cancer is poor. This study aimed to evaluate the value of pancreatic CT perfusion on biological behavior assessment in pancreatic cancer. Methods:This study collected 78 cases of pancreatic cancer which diagnosed by the method of pancreatic CT perfusion, and detected the differences of the values of blood lfow (BF), blood volume (BV), permeability (per), peak value (PE) and time to peak (TTP) between normal pancreatic tissues and tumor tissues. Combined with clinical and pathological data. Besides, this study evaluated the relationship between perfusion parameters of tumor tissues and tumor size, lymph node metastasis, distant metastasis, preoperative serum CA199 level, Ki-67, p53, CEA, CA199, CD34 expression of tumor tissues. Results:The values of BF, BV, per and PE in pancreatic tumor tissue were signiifcantly lower than those in normal pancreatic tissue. The BF values of cases with high levels of serum CA199 and with CA199 positively expressed tissues were signiifcantly higher than those with negative expression. The PE values of cases with positive tissue expression of Ki-67 were significantly higher than those with negative expression. The TTP values of cases with positive tissue expression of CEA were signiifcantly lower than those with negative expression. The per values of well differentiated cases was signiifcantly higher than those of moderately/poorly differentiated cases. Conclusion:CT perfusion may have its value on assessment of tumor biological behavior in pancreatic cancer.

OBJECTIVETo investigate the difference in conjugated bile acids in the gallbladder bile between gallbladder cholesterol polyps and adenomatous polyps patients, and screen the differential diagnosis-markers for polypoid lesions of gallbladder (PLG).

METHODSFrom January to June 2013, the 20 cholesterol polyps patients, 10 adenomatous polyps patients and 10 patients without gallbladder diseases were enrolled. High performance liquid chromatography assay with ultraviolet detection was used to test 8 conjugated bile acids in gallbladder bile.

RESULTSThe 8 conjugated bile acids were completely analyzed in 10 minutes, and the assay was liner in the range 8-500 µg/ml. The correlation coeffients for linear regression was from 0.9996-0.9999 and the detection limits ranged from 3.90-7.81 µg/ml. The level of taurocholic acid (TCA) in adenomatous polyps group ((75 ± 51) µg/ml) was significantly lower than that in the cholesterol polyps ((228 ± 206) µg/ml, q = 3.120, P = 0.014) and control groups ((104 ± 40) µg/ml, q = 2.950, P = 0.027). The level of taurochenodeoxycholic acid (TCDCA) in cholesterol polyps group ((604 ± 444) µg/ml) was significantly higher than that in the adenomatous polyps ((310 ± 182) µg/ml, q = 2.560, P = 0.048) and control groups ((308 ± 21) µg/ml, q = 2.970, P = 0.023).

CONCLUSIONSThe levels of TCA and TCDCA in the gallbladder biles in cholesterol polyps patients were higher than those in adenomatous polyps patients, which may be the differential diagnosis-markers for PLG.

Adenocarcinoma ; diagnosis ; Adult ; Aged ; Bile ; chemistry ; Bile Acids and Salts ; analysis ; Case-Control Studies ; Diagnosis, Differential ; Female ; Gallbladder Diseases ; diagnosis ; metabolism ; Humans ; Male ; Middle Aged ; Polyps ; diagnosis ; metabolism ; Young Adult

Objective To investigate the experiences in the diagnosis and treatment of space-occupying lesions of the head of pancreas.Methods The clinical data of 247 patients with space-occupying lesions of the head of pancreas who were admitted to the First Affiliated Hospital of Chinese Medical University from January 2011 to April 2014 were retrospectively analyzed.All the patients received enhanced computed tomnography and (or) magnetic resonance imaging of the pancreas.The levels of alpha-fetal protein (AFP),CA19-9,CA125 and carcinoembryonic antigen (CEA) were detected,and the serum level of IgG4 was detected in patients who were suspected of autoimmune pancreatitis.Intraoperative pathological examination was applied to patients who were diagnosed as with cancer of the head of pancreas.Pancreaticoduodenectomy,extended pancreaticoduodenectomy or bilio-jejunostomy or (and) gastrointestinal anastomosis were applied to patients according to the stage and infiltration of the tumor.Duodenum-preserving pancreatic head resection or pancreaticoduodenectomy could be selected after informed consent.The adjacent tissues and organs should be preserved on the premise of complete tumor resection for patients with benign and low-grade malignancy.Results A total of 194 patients had solid spaceoccupying lesions of the head of pancreas,including 125 with pancreatic head cancer,45 with mnass in the head of pancreas,9 with chronic pancreatitis with mass in the head of pancreas,11 with autoimmune pancreatitis,4 with insulinoma.Fifty-three patients were with cystic space-occupying lesions,including 12 with mucinous cystadenoma,8 with serous cystadenoma,17 with pancreatic cyst,12 with solid-pseudopapillary tumor of pancreas and 4 with intraductal papillary mucinous neoplasm.The positive rates of AFP,CA19-9,CA125 and CEA of the 71 patients who were confirmed as with pancreatic cancer by pathological examination were 7.0％ (5/71),94.4％ (67/71),42.3％ (30/71) and 0,respectively.The positive rates of AFP,CA19-9,CA125 and CEA of the 12 patients with chronic pancreatitis with mass in the head of pancreas were 1/12,4/12,1/12 and 0,respectively.Seventynine patients with pancreatic head cancer,mass in the head of pancreas and chronic pancreatitis with mass in the head of pancreas received intraoperative pathological examination.A total of 119 patients received operation,including 71 with pancreatic head cancer,7 with chronic pancreatitis with mass in the head of pancreas,4 with insulinoma,1 with pancreatic tuberculosis,8 with mucinous cystadenoma,4 with serous cystadenoma,6 with pancreatic pseudocyst,1 with huge lymphangioma,1 with lymphoepithelial cyst,12 with solid-pseudopapillary tumor of pancreas and 4 with intraductal papillary mucinous neoplasm.Of the 247 patients with space-occupying lesions of the head of pancreas,61 received pancreaticoduodenectomy,4 received duodenum-preserving pancreatic head resection,4 received pancreatic head and neck resection,2 received partial resection of the uncinate process of the pancreas,9 received enucleation of the tumor,38 received bilio-jejunostomy or (and) gastrointestinal anastomosis,22 received endoscopic retrograde cholangio-pancreatography + stent installation,18 received percutaneous transhepatic cholangial drainage + stent installation,1 received exploratory lapartomy and the other 88 patients were untreated.Conclusions The diagnosis and differential diagnosis of the space-occupying lesions of the head of pancreas depend on the clinical presentation,medical history,laboratory examination,sonography,computed tomography or magnetic resonance imaging.Individualized treatment plan based on the feature of the tumor and kinds of the lesions combined with intraoperative pathological examination is helpful for selecting the surgical procedures.

Objective To investigate the effects of interferon-γ (IFN-γ) on interleukin-10 (IL-10) and mononuclear macrophages in a mouse model of gallbladder cancer.Methods Mouse models of gallbladder cancer were constructed by inoculating the human gallbladder cancer cell line GBC-SD subcutaneously in 20 BALB/C mice,and then all the mice were randomly divided into the IFN-γ group and the control group (10 mice in each group).Murine recombinant IFN-γ (0.1 mL,1 × 105 kU/L,diluted with normal saline) was injected into the tumors in the IFN-γgroup,and normal saline was injected into the tumors in the control group.The expression of IL-10 was detected by ELISA,and the numbers of CD14 + cells (mononuclear macrophages),CD64 + cells (M1 macrophages) and CD206+ cells (M2 macrophages) were counted by the immunohistochemistry.All data were analyzed using the Student's t test.Results The mouse models of gallbladder cancer were successfully constructed 1 week later.Nine mice survived in the IFN-γ group,and 7 mice survived in the control group.The tumor weight was (518 ± 138)mg in the IFN-γ group and (669 ± 128)mg in the control group,with a significant difference between the 2 groups (t =2.240,P ＞ 0.05).The volume of the tumor was (456 ± 172)mm3 in the IFN-γ group and (505 ± 146)mm3 in the control group,with no significant difference between the 2 groups (t =1.503,P ＞ 0.05).The concentration of IL-10 was (58 ± 16) μg/g in the IFN-γgroup,which was significantly lower than (102 ± 45) μg/g in the control group (t =2.796,P ＜ 0.05).The number of mononuclear macrophages was 81 ± 16 in the IFN-γ group,which was significantly greater than 50 ± 21 in the control group; the number of M1 macrophages was 66 ± 12 in the IFN-γ group,which was significantly greater than 9 ± 4 in the control group ; the number of M2 macrophages was 15 ± 4 in the IFN-γgroup,which was significantly lower than 40 ± 14 in the control group (t =3.214,13.127,6.914,P ＜ 0.05).Conclusions IFN-γ could decrease the concentration of IL-10 in the tumor microenvironment,and it could induce the mononuclear macrophage to infiltrate into the stroma of the gallbladder cancer cells,and most of the monocytes and macrophages were differentiate to M1 macrophages.Gallbladder neoplasms; Interleukin-10; Interferon-γ; Mononuclear macrophages

Object To establish a proper research evaluation system for level-two general hospital.Method By using Delphi method,experts were invited by letter to review research evaluation indices for three times.Result Totally 62 indices were weighted and evaluated,including two primary-degree indices,14 secondary-degree indices,and 46 third-degree indices. A research evaluation system was preliminarily established in a level-two general hospital.Conclusion The evaluation system is simple and practicable,and can reflect the main aspects of research in the leveltwo general hospitals.