[ ABSTRACT] AIM:To investigate the protective effect of 1, 3-dicyclopentyl-1, 2, 3, 6-tetrahydropyrimidine-4, 5-dicarboxylic acid diethyl ester (ZL-5015) on lethal endotoxin-challenged mice and to explore the underlying mechanism. METHODS:Mouse model of lethal endotoxin challenge and endotoxemia were established by intraperitoneal administration of lipopolysaccharide (LPS) at a dose of 70 mg/kg to the C57BL/6J mice.Mouse peritoneal macrophages stimulated with LPS (10 mg/L) were used as an in vitro inflammatory model.The levels of interleukin-1β( IL-1β) , interleukin-10 ( IL-10) and tumor necrosis factor-α(TNF-α) were measured by enzyme-linked immunosorbent assay (ELISA).Real-time PCR was used to evaluate the mRNA expression of the cytokines.RESULTS:Prophylactic treatment of the mice with ZL-5015 (100 and 200 mg/kg, ig) slightly increased the survival rate, extended the survival time, decreased the serum levels of IL-1βand TNF-α, and increased the serum level of IL-10 in the early stage of endotoxemia as compared with model group.The results of in vitro study demonstrated that treatment of the endotoxin-stimulated mouse peritoneal macrophages with ZL-5015 (10, 20 and 40μmol/L) inhibited the expression of IL-1βand TNF-αat both mRNA and protein levels but promoted the expression of IL-10 at both mRNA and protein levels.CONCLUSION: The tetrahydropyrimidine derivative ZL-5015 shows a moderate anti-endotoxin effect by increasing the survival rate and extending the survival time of the mice challenged by endotoxin, which may result from inhibition of the expression of pro-inflammatory cytokines such as IL-1βand TNF-α, and promotion of the expression of anti-inflammatory cytokine IL-10.

Objective To explore the dose-effect relationship and optimal concentration of sodium taurocholate (NaTc) to establish acute necrosis pancreatitis (ANP) complicating MODS in a rat. Methods 280 SD rats were randomly divided into control group (n =40) and 3.5%, 4%, 4.5%, 5% ANP group (n = 60, respectively). ANP groups were induced by retrograde injection of NaTc solution into the pancreatic duct of rats. Rats in each model group were sacrificed at 1, 3, 6, 12 and 24 h after the model induction. Serum amylase, serum total bilirubin, creatinine, blood gas analysis, and pathological changes of pancreas were determined. Survival rate at 24 h after the model induction was observed in other 20 ANP rats in each group. Results In each groups, the serum amylase level, creatinine, blood gas analysis and pathological changes all increased corresponding to the increase of NaTc, and there was significant dose-effect relationship and time-effect. In 4.5% group, the dysfunction of liver and kidney reached the peak at 6 h,while the respiratory dysfunction reached its peak at 12 h. Its incidence of MODS was 52.5%, which was significantly higher than those in 3.5%, 4.0% group (15.0% and 37.5%) ;and 24 h survival rate of 4.5% group was 65%, which was significantly higher than that in 5% group (30%). Conclusions 4.5% NaTc solution may be the optimal concentration to establish the ANP model, which had higher incidence of MODS and 24 h survival rate.

Objective To investigate the time-course change of intra-abdominal pressure (IAP), TNF-α in rat with acute necrotizing pancreatitis (ANP) and its mechanism. Methods 80 SD rats were randomly divided into ANP group and control group. ANP group was induced by retrograde injection of 4.5% sodium taurocholate into the pancreatic duct in SD rats, while control group was induced by injection of saline at the same dosage. Eight rats in each group were killed at 1 h, 3 h, 6 h, 12 h and 24 h, respectively. The serum levels of amylase, TNF-α were determined;IAP, amount of abdominal ascites, pancreatic pathologic changes were evaluated. Results The levels of amylase in ANP group increased progressively with time, which were 32-folds higher than those in control group at 24 h. The serum levels of TNF-α in ANP group reached the peak at 6 h, and were significantly higher than those in the control group. The amount of abdominal ascites increased post-ANP induction and reached the peak at 24 h, which was 4.7-folds higher than that in the control group. The IAP significantly increased 1 h after induction, which was 3 times as high as the control group in 3 h group and 9 times in 12 h group. Pathologic injuries deteriorated progressively and reached the peak at 24 h. Conclusions Significant IAP occurred in ANP rats and reached the peak at 12 h, TNF-α reached the peak at 6 h, therefore IAP may be the secondary response to inflammatory reaction.

In this study, the adsorption behavior of epirubicin hydrochloride (EPI) on carboxylated single-walled carbon nanotubes (c-SWNTs) obtained by mixture acid treatment was investigated. The results indicated that the dispersion of c-SWNTs in water was obviously improved. The absorption of EPI on c-SWNTs came to equilibrium after 240 min and could be explained by pseudo-second-order model. Moreover, there were heterogeneous distribution of active sites onto c-SWNTs surface and the Freundlich isotherm model was better fit to describe the absorption precess of EPI on c-SWNTs. The absorption capacity of EPI on c-SWNTs increased obviously with the increasing pH and decreasing temperature. Compared with multi-walled carbon nanotubes, carboxylated multi-walled carbon nanotubes, SWNTs, c-SWNTs possessed higher absorption capacity for EPI. The controlled, targeted and sustained release of EPI from c-SWNTs-EPI could be instructive for the development of nano-carrier.

This study was aimed to establish an inspection method for the limited quantity of aconitine and the content determination of schisandrol in Yi-Shen Xiao-Zhong(YSXZ) pill.Thin layer chromatography (TLC) was used to inspect the limited quantity of aconitine in YSXZ pill.The content of schisandrol was determined by high-performance liquid chromatography (HPLC).The results showed that the identification method of the limited quantity of aconitine and the content determination method of schisandrol were established.Compared to the correspondent position of the control chromatography,the limited quantity of aconitine was 2.5μg,which was much lower than the dose of inducing toxic reaction.It can be used in the limited quantity control of aconitine for toxic reaction in YSXZ pill.The calibration curve of schisandrol was linear at 2.92-95.36μg·mL-1.The regression equation wasy = 18.630x + 2.556 (r = 1).The average recovery was 95.10% and RSD was 1.55% (n = 6).It was concluded that the established method for the inspection and content determination of aconitine and schisandrol was simple,accurate and reproducible.It can be used in the quality control of YSXZ pill.

Objective To study the effect of balloon dilatation therapy on dysphagia caused by cricopharyn- geal achalasia.Methods Ten cases of dysphagia were diagnosed as cricopharyngeal achalasia by videofluoroscopic swallowing study(VFSS).A 14~* urethral catheter was inserted into the esophagus and an amount of water was injec- ted into the balloon of the urethral catheter to make it turgid.Then the catheter was pulled upwards and passed through the stricture of esophagus to dilatate the cricopbarygeus muscle.Meanwhile,low frequency electrical stimula- tion was used and combined with functional training of the organs related to deglutition and ingestion.The results be- fore and after the treatment were evaluated.Results After 19.7 times of dilatation therapy,the content of water in- jected into the balloon was increased from 2.65?0.91 ml to 8.20?0.92 ml.Cricopharyngeal achalasia was alle- viated significantly(P

Objective To establish an index system of the key factors of elimination of schistosomiasis. Methods A ques?tionnaire was designed based on the reference review,and 24 scientists working in the field of schistosomiasis control or re?search or management were investigated by using the Delphi method. The importance of each index reflecting the endemicity of schistosomiasis was scored by each scientist. The assessing system for key factors of eliminating schistosomiasis was established , and the normalized weight and combined weight were calculated. Results The assessing system included three indexes in the first grade,seven indexes in the second grade and thirteen indexes in the third grade. Among the indexes in the first grade,the normalized weights of endemicity,natural environment and social environment were 0.371 1,0.339 5,and 0.289 4,respective?ly. Among the indexes in the second grade,the economy showed the highest combined weight of 0.289 4 while the agriculture and sanitation both showed the lowest score of 0.112 7. Among the indexes in the third grade,the infection rate of animals showed the highest combined weight of 0.124 6 while the agriculture and plant structure both showed the lowest score of 0.053 0. Conclusion The indexes of the assessing system provide the scientific evidence for surveillance work when elimination of schis?tosomiasis.

Objective To compare the treatment effects of Qingyi Huoxue decoction and infliximab on acute necrosis pancreatitis ( ANP) complicated with MODS in a rat model. Methods 4.5% sodium taurocholate was injected into the pancreatic duct to induce the ANP complicated with MODS model. The ANP rats were randomly divided into 3 groups, ANP group (ANP), Qingyi Huoxue decoction treatment group ( QG) , infliximab treatment group (IG). Rats in infliximab group received infliximab injection at a dose of 8 mg/kg body weight via tail vein 6 h after the ANP induction. The ANP and QG received normal saline and Qingyi Huoxue decoction (20 ml/kg) via gastric lavage 4 h before and 3 h, 9 h after ANP induction. After 24 h, all rats were sacrificed, the serum levels of amylase, total bilirubin, Cr, TNF-α, diamine oxidase ( DAO) , intra-abdominal pressure (IAP) and the rate of carbon propelling rate in ileum were measured. The pancreas samples were collected for pathological examination. The pathological score of pancreas was calculated. Results The pathological scores in ANP, QG, IG were 13.8 ±0.8, 6.1 ±0.4, 3.9 ±0.6, and the difference was statistically significant (P <0.05). The serum levels of amylase, total bilirubin, Cr, TNF-α were significantly decreased. In ANP, QG, IG the serum levels of DAO were (186.3 ± 10.2 ) , ( 134.6 ± 14.3 ) , ( 149.1 ± 16.3) U/L; the carbon propelling rates in ileum were (53 ±0.1)% , (89 ±0.1)% , (61 ±0.1)% ; the IAPs were (11.8 ±1.5), (4.1±0.8), (5.8 ±1.2) mmHg(1 mmHg=0.133 kPa). The DAO and IAP in AG, IG were significantly decreased when compared with that in ANP group, but the carbon propelling rates in ileum was significantly higher than that in ANP group, and the difference was statistically significant ( P < 0.05). In addition, the carbon propelling rates in ileum in QG were higher than that in IG, and IAP and DAO levels were lower than that in IG, and the difference was statistically significant (P <0.05). Conclusions The Qingyi Huoxue decoction and infliximab were significantly effective in the treatment of ANP rats complicated with MODS. But the effects of Qinyi Huoxue decoction on promoting gastrointestinal motility, reducing the IAP and improving the intestinal barrier function were better than those of the infliximab.

Objective The aim of this study is to evaluate the efficacy and safety of preoperative CT-guided hardening agent localization.Methods From December 2010 to January 2012,27 patients with 29 solitary pulmonary nodules who had undergone CT-guided hardening agent localization and video-assisted thoracoscopic surgery (VATS) were studied.Results All cases were underwent CT-guided hardening agent localization successfully,and no patient had serious complication that required any intervention.The diameter of nodules ranged from 3 to 21 mm as measured by CT[mean (11.27 ± 6.32) mm].The distance between the center of nodule and visceral pleural ranged from 4 to 38 mm[mean (14.45 ± 4.32) mm].Conversion from VATS to thoracotomies was not necessary during the diagnostic resection procedure nodules.29 solitary pulmonary nodules underwent thoracoscopic wedge resection,and no intra-or postoperative mortality or morbidity was recorded.Conclusion CT-guided hardening agent localization before video-assisted thoracoscopic solitary pulmonary nodule resection is a safe and effective procedure for accurate diagnosis and resection of indeterminate solitary pulmonary nodules.