Object To study the correlativity between the in vivo release of healthy volunteers and the in vitro dissolution of XIANGHE SUPPOSITORY(XS). Methods The electromagnetic stirring method was used to determine the in vitro dissolution of XS, and the in vivo release was got by the indirect method, assaying the content of the left XS after it had released in administering system, HPLC was used for the determination of XS with the index of variant content of berberine hydrochloride. Results A good correlativity was shown between the percentage of in vivo release and in vitro dissolution of XS. Conclusion In vitro dissolution test under the given conditions could indicate the in vivo absorption of XS.

OBJECTIVE:To observe the curative effect of Xiaoer chiqiao qingre granule in treating child common cold fever (stagnant type).METHODS:A total of 118 cases with child common cold fever(stagnant type) were randomly assigned to receive Xiaoer chiqiao qingre granule (treatment group,n=60) or ribovirin tablet,Ertangganmao granule(control group,n=58) tid for 3 days.The antipyretic time, clinical effective rate, and improvement in clinical symptoms were compared between the two groups. RESULTS: There outcome indexes including the antipyretic time,the clinical effective rate,and the improvement in clinical symptoms in the treatment group was significnatly better than in the control group(P

Objective To investigate the effects of nu cleus transcription factor (NF)-?B, survivin, Bcl-2 and Caspase-3 on apoptos is of gastric cancer cells induced by tumor necrosis factor related apoptosis in ducing ligand(TRAIL). Methods Gastric cancer cells were cultured in RPMI-1640 and the proportions of apoptosis were analyzed by flow cytometry. The expressions of N F-?B, survivin, Bcl-2 and Caspase-3 in gastric cancer cells were evaluated b y Western blot. Results After gastric cancer cells were exposed to 50 ng/ml TRAIL f or 24 hours, the proportions of apoptosis were 24.05% in line MKN28, 7.83% in MK N45, 8.05% in AGS and 3.17% in SGC-7901 respectively; after 300 ng/ml TRAIL for 24 ho urs, the proportions of apoptosis were 36.05% in MKN28, 20.27% in MKN45, 16.50% in AGS and 11.80% in SGC-7901 respectively. The expressions of NF-?B and surv ivin under Western blot were lower in MKN28 than that in MKN45, AGS and SGC-79 0 1. In contrast, the expression of Caspase-3 was higher in MKN28 than that in MK N45, AGS a nd SGC-7901. The expression of Bcl-2 had no difference among the 4 lines of ga stric cancer cells. Conclusions The anti-tumor sensitivity of TRAIL to gastric cancer c ell may be associated with both increased expressions of NF-?B and survivin an d decreased expression of Caspase-3.

Objective To study the effects of demethylation agent 5-Aza-2′-deoxycytidine (5-Aza-CdR) on the antitumor activity of tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) against gastric carcinoma. Methods Expression of caspase-8 mRNA was examined by RT-PCR. Antitumor activity of TRAIL protein was measured by MTT method. Results The inhibition rates of treatment with 200 ng/ml TRAIL for 72 h on gastric cell lines SGc 7901, Kato 3, and AGS were 9.83%, 11.94%, and 4.04%. After treatment with 5-Aza-CdR, the inhibition rates of 200 ng/ml TRAIL on gastric cell lines increased to 38.98%, 52.42%, and 30.72%. Before exposure to 5-Aza-CdR, expression of caspase-8 mRNA was low and an increased expression of the caspase-8 was found in the three gastric cancer cells after treatment with 5-Aza-CdR. Conclusion Treatment with 5-Aza-CdR can increase TRAIL antitumor activity on human gastric cancer and its mechanisms might be involved in the up-regulation of caspase-8 gene.

Objective To study the effect of methylation state of C5 of the cytosine in the CpG di nucleotide of caspase 8 promoter on tumor necrosis factor related apoptosis inducing ligand (TRAIL) antitumor activity in gastric carcinomas. Methods The methylation states of the caspase 8 promoter region of 5 kinds of gastric carcinoma strains were measured by methylation specific PCR method. The antitumor activity of TRAIL protein was measured by MTT method. Results No methylation of caspase 8 promoter was found in gastric carcinoma cells. Treatment with demethylation agent 5 Aza 2′ deoxycytidine (5 Aza CdR) increased sensitivity of gastric cancer cells to TRAIL, but did not change methylation status of caspase 8 promoter in gastric carcinoma cells. Conclusion Caspase 8 promoter methylation status is not associated with TRAIL antitumor activity.

Objective In the present study,we use GC/MS-based metabolomics approaches to make analysis of serum metabolic profiles of healthy people and the hyperactivity of liver yang type of constitution in patients with essential hypertension.Try to establish the discriminant model,to discover biomarkers (group) of the hyperactivity of liver yang type of essential hypertension,and to explore the essential material basis of Traditional Chinese medicine syndrome theory.Methods Classified according to the guiding principles of Chinese medicine research,the hyperactivity of liver yang type of constitution in male patients with essential hypertension (n=18),as well as health volunteers (n=15) were randomly selected from Guang An Men Hospital clinic,wards and medical center in the first half of 2010,selected patients with essential hypertension requirements are not taking any drugs or Chinese herbs,or stop taking the various drugs more than one week.Extracted Venous Blood of subjects fasting for 12 hours,and serum was separated through centrifugation.Serum samples are stored and at-86℃ refrigerator.Survey and evaluate endogenous metabolism in serum samples of health control group and types of syndrome mentioned above by gas chromatograph mass spectrometry (GCMS)analysis.Then,analyze the metabolites with Partial Least Squares-Discriminant Analysis.Further use PCA to analyze the principal component factor loadings matrix analysis,and for variable scatter plot (Loading plot),significant increase or decrease the variables can be found from the figure.The combination of these variables is the lesion biomarkers group.Results Compared with the health control group,13 differentially expressed metabolites in the essential hypertension hyperactivity of liver yang type group can be identified (P＜0.05).8 metabolites were up-regulated expression:Uric acid,citrate,Octadecanoic acid,Hexadecanoic acid,Octadecadienoic acid,Leucine,Cholesterol,Norvaline,and 5 metabolites were down-regulated expression:arachidonate,Oleate,Alanine,Aspartic acid,glycine.Conclusion We are incline to regard that the 13 of EH patient serum differentially expressed metabolites are EH hyperactivity of liver yang syndrome metabolic biomarkers:Uric acid,citrate,Octadecanoic acid,Hexadecanoic acid,Octadecadienoic acid,Leucine,Cholesterol,Norvaline,Arachidonate,Oleate,Alanine,Aspartic acid,glycine.

Aim TodevelopandvalidateaLC-MS/MS assay to quantify halometasone in rabbit plasma and study pharmacokinetics of halometasone after dermal topical administration of Halometasone Cream.Meth-ods Theplasmasamplewassubmittedtoliquid-liquid extraction using methyl tertiary butyl ether,with dexa-methasone as the internal standard (IS ).Chromato-graphic separations were performed on a Diamonsil C18 column(100 mm ×4. 6 mm,5 μm)with a linear gra-dient of methanol and 2 mmol · L-1 ammonium ace-tate.Halometasone and dexamethasone(IS)were ion-ized with an ESI source operated in negative ion mode, and the detected ions were m/z 503. 1→413. 0 (halo-metasone),m/z 391. 0→361. 0 (dexamethasone ). The test article could be monitored in rabbit plasma when following single dermal topical administration of Halometasone Cream at 1 g/100 cm2 to rabbits by u-singavalidatedLC-MS/MSassay.Results Calibra-tion curve was linear over the concentration range of0. 02~20 μg·L-1 in rabbit plasma.For low,medi-um,high concentration of QC solutions,the intra-and inter-day precision was in the range of 3. 72% ~7. 87%, and the accuracy was within 99. 1% to 103%. The pharmacokinetic parameters in rabbits were as follows:Tmax,Cmax,AUC0-t,T1/2 was (7. 38 ± 1. 06)h,(1. 16 ±0. 527)μg·L-1,(18. 8 ±7. 23)h·μg·L-1 ,(13. 8 ±3. 70)h,respectively.Conclusions ThisLC-MS/MSanalysismethodhashighsensitivi-ty,and sample processing method is simple,which has been rigorously validated.The method could be suc-cessfully applied to the pharmacokinetic study of halo-metasone after skin administration of Halometasone Cream to rabbits.

Objective To assess the outcome of fixation of Rüedi-Allg(o)wer type Ⅱ and Ⅲ pilon fracture using multiple low-profile plates (MLPP) via multiple incisions.Methods A retrospective study was made on 21 cases of pilon fracture immobilized using MLPP via multiple incisions between July 2007 and March 2012.There were 7 cases of Rüedi-Allgower type Ⅱ and 14 type Ⅲ.Fractures were reduced and fixed based on X-ray films and CT scans for fracture line and effect area.Quality of reduction was evaluated by Burwell-Charnley radiological score.Ankle and hindfoot functions were evaluated by American Orthopedic Foot & Ankle Society ankle-hindfoot scale.Fracture types,healing rate,and wound complication incidence were recorded.Results All fractures were healed,with the excellence rate of 95％ (20/21).According to AOFAS score,the results were rated as excellent in 11 cases,good in 6,fair in 4,with the excellence rate of 81％.None suffered from wound infection,except for wound dehiscence in 1 case and traumatic arthritis in 5.Conclusion Treatment of pilon fractures by MLPP via multiple incisions can reduce wound complications,promote reduction and stabilization of fracture,and satisfy the demand of early movement and late weight bearing of the ankle.

BACKGROUND: Microsatellite instability (MSI), an important gene change type, plays animportant role in the occurrence of tumor. Mismatch repair gene induces its occurrence. Although the effect of mismatch repair gene hMLH1 mutation in the hereditary nonpolyposis colorectal cancers (HNPCC) has been reported, its effect on the sporadic colorectal carcinoma lacks in-depth study.OBJECTIVE: To investigate the effect of mismatch repair gene hMLH1 mutation on colorectal carcinogenesis, and its correlation with MSI.DESIGN: Single-sample experiment.SETTING: Department of Gastroenterology, Southwest Hospital of Third Military Medical University of Chinese PLA.PARTICIPANTS: Seventy-six cases of sporadic colorectal carcinoma and corresponding normal tissues were obtained from surgically resected specimens of coloreetal carcinoma in Southwest Hospital between January 2001and December 2003. No patients had family history of tumor, or had received radiotherapy and chemotherapy. Patients were informed of the experiment.METHODS: Mutation of hMLH1 was detected by two-dimensional electrophoresis and DNA sequencing; MSI was analyzed by PCR-based methods.MAIN OUTCOME MEASURES: ① Detection rate of hMLH1 mutation of colorectal carcinoma and MSI. ② The relationship of MSI and hMLH1 mutation.RESULTS: Seventy-six cases of sporadic colorectal carcinoma were studied for hMLH1 mutation and MSI. hMLH1 mutation was detected in 8 (10.5%) cases of colorectal carcinomas while MSI was detected in 20 (26.3%) cases of colorectal carcinomas. Frequency of hMLH1 mutation and MSI was significantly higher in right colorectal cancer than in left colorec tal cancer (6/26 vs 2/50, x2=4.739, P=0.029; 11/26 vs 9/50,x2=5.212,P=0.022). No association was observed between hMLH1 mutation or MSI and tumor size, differentiation, histological type, depth of invasion, metastasis or clinical pathological stages. ② MSI was divided into high-frequency group (≥ 2 loci, n=10) and low-frequency group (1 locus, n-10), and MSI negative group (n=56). 8 hMLH1 mutations were all detected in high frequency MSI group, but no mutation was found in low frequency MSI or MSI negative groups.CONCLUSION: hMLH1 mutation and MSI occur in cancer of the right large intestine and hMLH1 mutation is involved in carcinogenesis of some sporadic colorectal cancer with high-frequency MSI.

In order to study the excretion of genistein (GEN) capsule, an estrogen drugs, in human, 30 healthy volunteers were selected and orally administered 50, 100, and 300 mg genistein in an parallel study. Genistein were determined in urine by LC-MS/MS and glucuronidated genistein (GENG) were indirectly determined with enzymatic hydrolysis in urine by LC-MS/MS, and the pharmacokinetic parameters were analyzed by DAS software (ver 2.0). The result showed that the concentrations of genistein in human urine were less than 1% of the GENG, and the cumulative excretion of GEN in 48 h were 0.037, 0.134, and 0.142 mg, separately, and the urinary excretion percentage were only 0.07%, 0.13%, and 0.05%, separately. But the cumulative excretion of GENG in 48 h was 5.3, 13.8, and 15.4 mg, separately, and the urinary excretion percentage were 10.6%, 13.8%, and 5.1%, separately, and the max urinary excretive rate was 0.4, 1.0, and 1.4 mg x h(-1), separately (tmax were 6 h). Studies showed that part of drug excreted through kidney in a form of GENG in human, and the cumulative urinary excretion and the maximum excretion rate of GENG showed a proportional increase conditioned with the dose in the range of 50-100 mg, but showed non-linear increase feature in 300 mg.