Objective:To establish a three-dimensional quantitative structure-activity relationship (3D-QSAR) model for thiazide 11β-hydroxy steroid dehydrogenase ( HSD) inhibitors in order to perform structure modification and find thiazide 11β-HSD inhibitors with more activity. Methods: The 3D-QSAR model of thiazine derivatives was constructed by the method of comparative molecular force field analysis, and the model was validated by using a molecular docking method. Results:An accurate 3D-QSAR model of 11β-HSD inhibitors was obtained (CoMFA:q2 =0. 346, r2 =0. 850, where q2 was the cross-validation coefficient and r2 was the non-cross validation coefficient) . Conclusion:The results provide important theoretical basis for the rational design of novel thiazide 11β-HSD inhibitors.

Objective To establish a RP-HPLC method investigate the processing technique and mechanism of Eucommiae Cortex.Methods The RP-HPLC method was applied to simultaneously determining six ingredients,geniposidic acid,geniposide,genipin,chlorogenic acid,(+)-pinoresinol-di-β-D-glucopyranoside,and(+)-syringaresinol-di-β-D-glucopyranoside,in the different processed barks of Eucommia ulmoides.Results The valid method with good accuracy could be well used to study the processing technique of E.ulmoides;Besides,target ingredients in E.ulmoide were decreased within 6 h when they were processed.Conclusion Established RP-HPLC is a reliable method which could be used to research the processing technique of the barks ofE.ulmoides.Moreover,the result of this study could be provided with significant evidence of processed barks of E.ulmoides.

Objective To explore the clinical value ofmulti-slice spiral CT (MSCT) to carcinomatous intestinal obstruction of colon.Methods The clinical and MSCT data of 40 patients with carcinomatous intestinal obstruction of colon diagnosed by MSCT were analyzed.Results In the 40 cases,complete intestinal obstruction were in 17 cases,incomplete intestinal obstruction in 23 cases,39 cases were carcinomatous intestinal obstruction of colon confirmed by surgery and pathology,and 1 case was intussusception intestinal obstruction by multiple polyps.The MSCT qualitative analysis of obstruction reason was 97.5％ (39/40),the MSCT diagnostic accuracy of intestinal obstruction was 100.0％ (40/40).The obstruction site was at ascending colon showed in 14 cases,transverse colon in 4 cases,splenic flexure of colon in 2 cases,descending colon in 6 cases,sigmoid colon in 12 cases,both ascending colon and transverse colon in 1 case,colon and small intestine in 1 case.The obstruction site accuracy rate of MSCT was 100.0％ (40/40).Conclusion MSCT has obvious advantages in obstruction existing,obstruction site,obstruction reason to carcinomatous intestinal obstruction of colon,it can offer reliable examination data to clinic.

Objective To study the protective effect mechanism of Rosa laevigata Michx (RLM) on cardiotoxicity induced by adriamycin in rats. Method 30 SD rats were randomly into control group, doxorubicin group and RLM groups. The control group was injected with normal saline injection, while the model group was injected with adriamycin intraperitoneally at the dosage of 15 mg/kg every other day. For the RLM groups,1~5 g/kg RLM were given after adriamycin injection. The survival rate, plasma BNP was observed. Apoptosis of cardiomyocyte was detected by instituted-labeled DNA (TUNEL). The activity of GSH-PX, CAT and total SOD in the myocardium tissue were also observed. The expression level of CuZn-SOD , bcl-2 and bax were detected by real-time PCR. Results The survival rate was significantly improved in SD rats treated with RLM compared with that in the adriamycin group (P<0.01). The BNP level was increased when treated by adriamycin (P<0.01), and decreased after RLM administration (P<0.01). RLM could also upregulate the expression of the CuZn-SOD mRNA level, and enhance the activity of GSH-PX, CAT and T-SOD compared with that in adriamycin group. Adriamycin could induce myocardial cells apoptosis, as demonstrated by TUNEL. RLM could inhibit adriamycin-induced apoptosis, bax mRNA expression, and increase bcl-2 expression and bcl-2/bax ratio. Conclusion RLM exhibit some antioxidant activity through many stages, and the anti-apoptosis activity may be related to affect the expression of bax and bcl-2 expression.

Objective To observe prospectively the role of endoscopic diagnosis and treatment of biliary leakages in patients with liver transplantation, and the incidence of bile duct stricture after healing of the leakage. Methods Six eases of T-tube leakage and seven cases of anastomosis leakage complicating liver transplantation were enrolled in this prospective study. Six patients treated by endoscopic plastic stent placement , 2 by naso-biliary catheter drainage, 2 by papillosphincterotomy and 3 by naso-biliary catheter drainage combined with plastic stent placement. Some patients received growth hormone treatment. Results The bile leak resolution time was between 10-35 days in 10 patients with complete document. The median time of leak resolution was 15. 3 days. Four cases of anastomosis stricture, three cases of common hepatic duct and one ease of multiple bile duct stenosis were observed by followed-up nasobiliary catheter cholangiography or ER-CP. Conclusion Endoscopic nasobiliary catheter or plastic stent placement is a safe and effective treatment for bile duct stricture occurred after bile leak resolution in most of liver transplantation patients. Naso-biliary catheter combined with plastic stent placement maybe the best choice for treating bile leak, because, theoretically, it may prevent serious condition happened at accidental nasobiliary catheter dislocation, and it may have prophylactic effect on upcoming bile duct stricture and should be further confirmed.

OBJECTIVE:To investigate the intervention effects of (E)-4-[2-(4-chlorophenoxy)-2-methylpropanoyloxy]-3-me-thoxyphenyl acrylic acid (AZ) on fat accumulation in human hepatoma HepG2 cells. METHODS:Oleic acid was used to induce fat accumulation in HepG2 cells in logarithmic phase for establishing models of fat accumulation,which were divided into a model group,a positive control group(100 μg/ml simvastatin),and the groups of 15.63,31.25,62.5,125,250,500 and 1 000 μg/ml AZ,and a normal control group was set up. MTT method was used to detect the survival rates of all groups of cells,kit was per-formed to determine the contents of triglyceride (TG) in all groups of cells and calculate the clearance rates,and oil red O stain was conducted to observe the lipid droplet morphology of all groups of cells. RESULTS:Compared to the normal control group, the model group and the groups of 15.63-125 μg/ml AZ demonstrated no obviously different survival rate of cells,and the groups of 250-1 000 μg/ml AZ had lower survival rate of cells. There was statistically significance (P<0.05). The contents of TG in the cells of the model group were higher than those in the cells of the normal control group. The positive control group and the groups of 62.5 and 125 μg/ml AZ had lower contents of TG in the cells compared to the model group,showing a TG clearance rate of (28.58 ± 0.15)%,(14.51 ± 0.09)% and (29.72 ± 0.16)% respectively. There was statistically significance (P<0.01 or P<0.05). There were much more lipid droplets in the cells of the model group than in those of the normal control group. The lipid droplets in AZ groups gradually became less in quantity and smaller with the increasing in drug concentration. CONCLUSIONS:AZ has inter-vention effect on fat accumulation in HepG2 cells.

Peroxisome proliferator-activated receptor α(PPARα)is an important subtype in the PPARs family. PPARs are a group of nuclear hormone receptors,which belong to type II nuclear receptor super family.PPARαagonists could be used in the treatment of hyperlipemia in clinic.PPARαagonists mainly include natural type and synthetic type,and according to the structure,the synthetic PPARαagonists can be divided into phenyl-heterocy-clic derivatives,ureide derivatives,amides derivatives,phenyloxazole or phenylthiazole derivatives,etc.So far, many PPARαagonists have been approved or in clinical development,and a series of novel PPARαagonists with higher activity and selectivity are being developed.This review will survey the progress in PPARαagonists.

Objective The expression and neuroprotective effect of meteorin in neurons and astrocytes after cerebral infarc-tion have yet to be clarified.This study was to investigate the expression and location of meteorin in the rat model of middle cerebral ar -tery occlusion (MCAO) and its neuroprotective effect against oxygen -glucose deprivation (OGD)-induced injury in cultured neurons or astrocytes. Methods Forty-two healthy adult male SD rats were randomly divided into 6 groups of equal number:sham operation and 6 h, 12 h, 24 h, 3 d, and 7 d MCAO.The cortical tissue was harvested for determination of the expression and location of meteorin by Western blot and immunohistochemistry as well as the meteorin expression in the neurons and astrocytes subjected to OGD. The neuroprotective effect of meteorin on the neurons and astrocytes was e-valuated by CCK8 and PI/Hoechst33342 staining. Results Com-pared with the sham operation group, the expression of meteorin was decreased after MCAO and reached the lowest level at 3 days ( P<0.01) , mainly in the neurons and astrocytes.Exogenous meteorin helped the survival of the astrocytes subjected to OGD, with the A value decreased in the groups of OGD ( 0.63 ) , OGD +meteorin
(0.78), and OGD+PBS (0.60) as compared with the sham control ( 1.51) (P<0.01), with no statistically significant differences among the former three groups (P>0.05).Concerning the effect of meteorin intervention on the OGD-induced injury of the astrocytes, the A value was significantly reduced in OGD (1.24 ±0.17), OGD+meteorin (1.51 ±0.30), and OGD+PBS (1.23 ±0.16) in comparison with the sham control (2.43 ±0.12) (P<0.01), lower in the OGD and OGD+PBS groups than in the OGD+meteorin group ( P<0.05) . Conclusion Meteorin is mainly expressed in the neurons and astrocytes after MCAO and it promotes the survival of the astrocytes with OGD-induced injury.