Thirteen novel oleanolic acid (OA) derivatives were designed and synthesized with modification at positions of C-3, C-12 and C-28 of OA. Their structures were confirmed by MS, 1H NMR and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines (SGC7901, MCF-7 and A549) were evaluated by MTT assay. The results indicated that the tested derivatives were found to have stronger cell growth inhibitory activity than OA. Among them, compounds II2 and II3 showed more potent cytotoxicity on MCF-7 and A549 tumor cells than gefitinib (positive control). They are worthy to be studied further.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; Drug Design ; Humans ; Oleanolic Acid ; chemical synthesis ; pharmacology

Objective To evaluate the clinical value of narrow band imaging(NBI)for diagnosis of malignant and premalignant gastric lesions.Methods The gastric lesions,pits and microvascularity were observed using conventional endoscopy followed by narrow band imaging(NBI)and chromoendoscopy(0.2%indigo carmine)as well as magnifying endoscopy(×80)in 217 patients.The quality of images obtained by different endoscopies was evaluated and compared to pathologic interpretations. Results Of 217 patients,non-atrophic gastritis was found in 85 cases,chronic atrophic gastritis in 38 cases,mild dysplasia in 19 cases,moderate dysplasia in 9 cases,severe dysplasia in 4 cases,early gastric cancer in 5 cases,advanced gastric cancer in 20 cases and intestinal metaplasia in 91 cases.The NBI endoscopy was superior to conventional endoscopy and chromoendoscopy in finding gastric lesions(P=0.000).The gastric microvascularity was more clearly seen on images obtained by NBI combined with magnifying endoscopy in comparison with conventional endoscopy and chromoendoscopy(P=0.000).There were six patterns in description of gastric pits with NBI endoscopy.Type Ⅲ,Ⅳ or Ⅴ1 was usually found in chronic atrophic gastritis,type Ⅲ,Ⅳ,Ⅴ1 or Ⅴ2 in intestinal metaplasia,type V1 or Ⅳ in dysplasia and type Ⅵ in suspected malignant lesion.Conclusions NBl with magnifying endoscopy is helpful in improving the biopsy accuracy of malignant and dysplastic lesions and in detecting early gastric cancer.

Objective To investigate the value of narrow band imaging(NBI) in diagnosis of early gastric cancer(EGC) and dysplasia. Methods 217 patients were enrolled. Routine endoscopy followed by narrow band imaging (NBI), then chromoendoscopy (indigo carmine) combined magnifying endoscopy was sequentially used. The gastric pits and microvasculuture were carefully observed. According to the NBI ima-ges, the biopsy samples were taken in suspicious area to identify malignant and premalignant gastric lesions. The patients with gastric cancer or severe dysplasia required endoscopic uhrasonography(EUS), then EGC or severe dysplasia ones needed endoscopic therapy or surgery. Results In silhouette of gastric lesion, NBI is the clearest in the above three endoscopic methods. Both mucosal pit and epithelium capiUary were shown much clearer by NBI than by routine endoscopy. Of 217 patients, 19 cases of mild dysplasia, 9 cases of moderate dysplasia, 4 cases of severe dysplasia and 5 cases of EGC were finded according to histopathological diagnosis. Six patterns of gastric pits were summarized by NBI. Dysplasia usually behaviored as V1 or Ⅳ gastric pits,and Ⅵ mucosal pit were suspected malignant lesion. Tumorous vessels can be seen in 3 cases of EGC. Conclusion By narrow band imaging system with magnifying endoscopy, the micro gastric mucosal structure can be shown much clear. That is helpful for improving the accuracy of malignant lesion on endo-scopic target biopsies and finding early gastric cancer.

Objective To investigated the effects of combined arsenic trioxide(ATO) and resveratrol(Res)on the viability of NB4 human leukemia cells. Methods NB4 human leukemia cell was used in this experiment.Cells were cultured in ATO (0,0.1875,0.3750,0.7500, 1.1250, 1.5000,2.2500,3.0000,5.0000 μmol/L) and Res (0, 1.5625,3.1250,6.2500, 12.5000, 18.7500,25.0000,37.5000,50.0000 μmol/L). Cell viabilities were measured by MTT in different treatment groups. Half inhibitory concentration(IC50) was calculated. The ratio of concentration of ATO and Res 1.5∶ 18,1.5∶ 25,1.5∶ 35 was added to cells, and the combination index(CI) was calculated. The level of ROS in control, ATO( 1.5000 μmol/L), Res(25.0000 μmol/L) and ATO(0.9000 μmol/L) + Res( 12.5000μmol/L) groups was measured by chemiluminescence assay. Results ①ATO( ≥0.7500 μmol/L) reduced the viability of NB4 cells in a concentration-dependent manner(P ＜ 0.05 ), and IC50 was (1.78 ± 0.11 )μmol/L. ②)Res (≥18.7500 μ mol/L) dose-dependently decreased the viability of NB4 cells (P ＜ 0.05 ), and IC50 was ( 18.71 ±0.18)μ mol/L. ③Combination of ATO and Res showed an antagonistic effect on NB4 cells viability. ④The ROS in Res group( 1670.55 ± 13.97) was significantly lower than that in control group(2345.88 ± 14.48,P ＜ 0.05). The ROS in ATO group (3092.42 ± 94.84) was significantly higher than that in control group(P ＜ 0.05). The ROS in ATO + Res group (1860.27 ± 15.99) was significantly lower than that in ATO group(P ＜ 0.05). Conclusions NB4 cell survival rate can be decreased by ATO and Res. The combination of arsenic trioxide and Res presents an antagonistic effect on NB4 cell viability, in part by reducing intracellular ROS formation.

Objective To investigate the characteristics and distribution of human eehinococcosis in Hobukesar Mongolian Autonomous County (HMAC) in Xinjiang. Methods Using cluster sampling methods, the 2 counties (Tiebukenwusa and Narenhebuke) in HMAC were chosen as focusing areas for investigation. A survey of human echinococcosis including questionnaire, serological test and abdominal ultrasonic scan was carried out. Results The prevalence of human echinococcosis was 9.0% (64/712) by ultrasound and surgical history, including 8.7% (62/712) for cystic eehinococcosis(CE), 0.3%(2/712) for alveolar echinococcosis(AE) and 15.6%(111/712) for total of serological positives in HMAC. CE prevalence rate of different occupations, age, family slaughtering livestock and drinking water source had significant differences(P<0.05). Herdsmen as the highest risk group showed a CE prevalence of the 13.4% (27/201) in comparison with other occupations. The ages between 20 to<40 year-old were at the highest risk stage with 12.8% incidence. But CE prevalence rate of different gender, ethnic and education groups had not significant differences(P>0.05). Conclusions HMAC could be considered as a high endemic human CE region in Xinjiang. The current study reported the main risk factors may include occupations, age difference and drinking water source.

In the present study, changes of the neuronal activity of 5-hydroxytrypamine (5-HT) neurons of dorsal raphe nucleus(DRN) in a rat model of Parkinson's disease (PD) were investigated with glass microelectrode recording. The results showed that the discharge rates of 5-HT neurons in control and PD rats were (1.61+/-0.56) Hz and (2.61+/-1.97) Hz, respectively. The discharge rate of PD rats was significantly increased when compared to that of the control rats. In control rats, 79% of 5-HT neurons discharged regularly and 21% in bursts. In PD rats, however, 36% of 5-HT neurons discharged regularly, 16% irregularly and 47% in bursts. The percentage of 5-HT neurons discharging in bursts was obviously higher than that of the control rats (P<0.05). The data suggest that the discharge rate and bursting pattern of 5-HT neurons in DRN are increased in a rat model of Parkinson's disease.
Animals ; Electrophysiology ; Male ; Microelectrodes ; Neurons ; physiology ; Parkinson Disease ; physiopathology ; Raphe Nuclei ; metabolism ; physiopathology ; Rats ; Rats, Sprague-Dawley ; Serotonin ; metabolism

In vivo extracellular recordings were made in the subthalamic nucleus (STN) of intact control rats and rats with 5,7-dihydroxytryptamine (5,7-DHT) -produced lesion of dorsal raphe nucleus (DRN). The results showed that the firing rate of STN neurons in control rats and DRN-lesioned rats were (6.93+/-6.55) Hz and (11.27+/-9.31) Hz, respectively, and the firing rate of DRN-lesioned rats significantly increased when compared to the control rats (P<0.01). In control rats, 13% of STN neurons discharged regularly, 46% irregularly and 41% in bursts. In DRN-lesioned rats, 9% of STN neurons discharged regularly, 14% irregularly and 77% in bursts, the percentage of STN neurons firing in bursts was obviously higher than that of the control rats (P<0.01). In addition, the mean interspike interval coefficient of variation of STN neurons in control rats and DRN-lesioned rats were (0.05+/-0.04) and (0.11+/-0.09), respectively. The mean interspike interval coefficient of variation of DRN-lesioned rats was significantly higher than that of the control rats (P<0.001). These results show that the firing rate and the bursting pattern rate of neurons in STN of DRN-lesioned rats increase significantly, suggesting that DRN inhibits the neuronal activity of the subthalamic neurons in the intact rat.
5,7-Dihydroxytryptamine ; pharmacology ; Adrenergic Agents ; pharmacology ; Animals ; Electrophysiological Phenomena ; Male ; Neurons ; physiology ; Random Allocation ; Raphe Nuclei ; drug effects ; pathology ; Rats ; Rats, Sprague-Dawley ; Subthalamic Nucleus ; physiopathology

Objective To explore the change in the firing rate and firing pattern of pedunculopontine nucleus (PPN)neurons in 6-hydrodopamine (6-OHDA) unilaterally lesiond rats. Methods Electrophysiological recordings of PPN neurons were done in normal rats and 6-OHDA lesiond rats with standard single unit glass microelectrode method in vivo. Results The firing rate of PPN neurons in normal rats and 6-OHDA lesiond rats were (9.0 ± 0.8 ) Hz [ (0.5-25.2) Hz, n = 56 ] and ( 16. 1 ± 1.6) Hz [ (1.2-49.7) Hz, n= 57), respectively. The firing rate of 6-OHDA lesioned rats was significantly increased when compared to control rats (P ＜ 0. 001 ). Concerning the firing pattern, 68% (38/56) of the neurons recorded discharged regularly, 27% (15/56) exhibited an irregular pattern and 5% (3/56) discharged in bursts in normal rats. In 6-OHDA lesioned rats, 39% (22/57) discharged regularly, 47% (27/57) exhibited an irregular pattern and 14% (8/57) in bursts. The number of PPN neurons in 6-OHDA lesioned rats fired irregularly was significantly higher than in control rats ( P ＜ 0.05). Conclusion The firing rate and the percentage of the irregularly firing neuron in PPN of 6-OHDA lesioned rats increased significantly, which may be contributed to the pathophysiological changes of Parkinson's disease.

Objective To evaluate the clinical efficacy and safety of Kanglaite injection combined with emcitabine injection and tegafur-gimeracil-oteracil potassium capsule in the treatment of advanced pancreatic cancer(PC).Methods A total of 45 patients with advanced pancreatic cancer were randomly divided into treatment group (n =23) and control group (n =22).The control group was given gemcitabine (1000 mg · m2,iv gtt,at day 1 and day 8) and tegafur-gimeracil-oteracil potassium capsule (1.25 m2 ≤ body surface area ＜ 1.5 m2,40 mg,bid;body surface area≥ 1.5 m2,50 mg,bid,day 1-day 14).The treatment group was treated with Kanglaite (20 g,qd,day 1-day 14) on the basis of control group.Both groups were treated for more than 4 cycles.The clinical benefit rate (CBR),overall survival (OS) and the adverse drug reactions (ADRs) were evaluated between the two groups.Results The CBR of treatment group and control group were 78.26％ (18 cases/23 cases) and 50.00％ (11 cases/22 cases) respectively,with significant difference (P ＜ 0.05).The median OS of treatment group and control group were 6.67 months and 5.60 months,respectively,with significant difference (P ＜ 0.05).The ADRs in the treatment group and control group were bone marrow depression,fatigue,gastrointestinal reaction,abnormal liver and kidney function and skin reaction,and there was no significant difference in the incidence of ADRs reactions between the two groups (P ＞ 0.05).Conclusion Kanglaite combined gemcitabine and tegafur-gimeracil-oteracil potassium is effective and safe in the treatment of advanced pancreatic cancer,with a longer OS,a higher incidence of clinical benefit and less ADRs.

Objective To analyze the results of application on China Infectious Diseases Automated-alert and Response System(CIDARS)and for further improving the system. Methods Amount of signal, proportion of signal responded, time to signal response, manner of signal verification and the outcome of each signal in CIDARS were descriptively analyzed from July 1,2008to June 30, 2010. Results A total of 533 829 signals were generated nationwide on 28 kinds of infectious diseases in the system. 97.13% of the signals had been responded and the median time to response was 1.1 hours. Among them, 2472 signals were generated by the fixed-value detection method which involved 9 kinds of diseases after the preliminary verification, field investigation and laboratory tests. 2202 signals were excluded, and finally 246 cholera cases, 15 plague cases and 9H5N1 cases as well as 39 outbreaks of cholera were confirmed. 531 357 signals were generated by the other method - the 'moving percentile method' which involved 19 kinds of diseases. The average amount of signal per county per week was 1.65, with 6603 signals(1.24%)preliminarily verified as suspected outbreaks and 1594 outbreaks were finally confirmed by further field investigation. For diseases in CIDARS, the proportion of signals related to suspected outbreaks to all triggered signals showed a positive correlation with the proportion of cases related to outbreaks of all the reported cases (r=0.963, P＜0.01). Conclusion The signals of CIDARS were responded timely, and the signal could act as a clue for potential outbreaks, which helped enhancing the ability on outbreaks detection for local public health departments.