?-GT activity and its substrate GSH content in tissue homogenate, epithe-lium and stroma of normal and benign hyperplastic human prostates were measured tostudy their relationship with pathogenesis of benign prostatic hyperplasia (BPH). Theresults were: a) ?-GT activity in BPH tissues were very much increased; but GSHcontent was much decreased; b) The ?-GT activity in epithelium of both normal andBPH were much higher than that in relative stroma. However epithelium GSH contentwere lower than that of stroma. Thase results suggested that increand ?-GT activity anddecreased GSH content play an important role in pathogenesis of BPH.

Polyamine biosynthesis is controlled primarily by ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase(AdoMetDC). Antisense ODC and AdoMetDC sequences were cloned into an adenoviral vector (Ad-ODC-AdoMetDCas). To evaluated the effect of recombinant adenovirus Ad-ODC-AdoMetDCas which can simultaneously express both antisense ornithine decarboxylase (ODC) and sadenosylmethionine decarboxylase (AdoMetDC), the human lung cancer cell line A-549, was infected with Ad-ODC-AdoMetDCas as well as with control vector. Viable cell counting, determination of polyamine concentrations, cell apoptosis,and Matrigel invasion assays were performed in order to assess properties of tumor growth and invasiveness. Furthermore,Ad-ODC-AdoMetDCas's anti-tumor effect was also evaluated in vivo in a nude mice xenograft model. It was demonstrated that adenovirus-mediated ODC and AdoMetDC antisense expression could inhibit tumor cell growth, lead to cell apoptosis and reduce tumor cell invasiveness. Polyamine levels were significantly decreased in Ad-ODC-AdoMetDCas-treated cells compared with controls.This adenovirus also induced tumor regression in established tumors in nude mice. It was suggested that as a new anticancer reagent,the recombinant adenovirus Ad-ODC-AdoMetDCas holds promising hope for the therapy of lung cancers.

Objective:To study the effect of molecular weight and degree of substitution (DS) of chitosan-poly-arginine (CS-R9) on transdermal penetration enhancement in vitro. Methods:Low molecular CS, medium molecular CS or high molecular CS was respectively used to synthesize CS-R9 with different molecular weight (LCS-R9-1, MCS-R9 and HCS-R9). Low molecular CS was used to synthesize CS-R9 with various degree of substitution by changing the mole ratio between R9 and CS (LCS-R9-1, LCS-R9-2 and LCS-R9-3). The in vitro transdermal penetration enhancement of the different CS-R9 on tinidazole ( TNZ) was studied using Franz diffusion cells. Results:According to the results of FTIR and 1 H-NMR, a series of target CS-R9 were synthesized including LCS-R9-1 with the DS of 2. 30, MCS-R9 with the DS of 2. 17, HCS-R9 with the DS of 2. 20, LCS-R9-2 with the DS of 8. 05 and LCS-R9-3 with the DS of 15. 87. Compared with the blank control group, Azone group, LCS group, R9 group and LCS+R9 group, LCS-R9-1 could enhance the in vitro transdermal penetration of TNZ significantly (P<0. 05). When the DS was unchanged, LCS-R9-1 and HCS-R9 showed similar enhancement in the first 12h, and the effects were both higher than that of MCS-R9 (P<0. 05). The enhancement of HCS-R9 was decreased during 12-24h, while compared with that of LCS-R9-1, the difference was not notable (P>0. 05). When the molecular weight of CS was unchanged, the effect was increased with the rise of DS in the first 21h, however, after that, the effect was decreased with the rise of DS. Conclusion:Molecular weight and DS both have significant effect on the in vitro transdermal penetration enhancement of CS-R9, and it is valuable to further study the in vivo transdermal penetration enhancement of CS-R9 and underlying mechanisms.

Objective:To identify the tannin-related constituents in the extracts of pomegranate peel by HPLC-ESI-MS. Methods:The separation was performed on a Kromasil C18 column (250 mm × 4. 6 mm,5 μm) with the mobile phase of water and acetonitrile. The flow rate was maintained at 1. 0 ml·min-1 and the detection wavelength was set at 256nm. The samples were analyzed in negative modes. Results:Five tannin-related constituents including gallic acid, punicalin,punicalagin,corilagin and ellagic acid were identified from the extracts of pomegranate peel. Conclusion:The new method is accurate and rapid. It can be used to identify the tannin-related constituents in pomegranate peel and provide new ideas for the research of active components in traditional Chinese medicine as well.

Objective:To investigate the therapeutic effect of tannins from pomegranate rind on passive Heymann nephritis ( PHN) in rats. Methods:Rabbits were with intradermal immunization for many times to obtain anti-Fx1A serum, and then PHN model in rats was established by tail intravenous injection of anti-Fx1A serum. The experimental rats were randomly divided into six groups, the nor-mal control group, model group, benazepril group, and tannins from pomegranate rind group respectively at high, medium and low dose. After the success of modeling, each rat was received intragastric administration for five weeks, and then the total of urine was collected once a week for the detection of 24-hour urine protein. At the end of treatment, serum was collected for the detection of serum albumin, blood urea nitrogen, creatinine, total cholesterol and triglyceride. The pathological changes of the renal tissue were observed using hematoxylin-eosin and Masson staining to observe the effect of tannins from pomegranate rind on PHN rats. Results:After the in-tragastric administration for five weeks, tannins from pomegranate rind could obviously reduce the level of 24-hour urine protein in PHN rats(P<0. 01), significantly reduce the levels of serum creatinine (P<0. 01), urea nitrogen (P<0. 01,P<0. 01,P<0. 05), total cholesterol (P<0. 01) and triglyceride (P<0. 01,P<0. 01,P<0. 05) in PHN rats, and increase the level of serum albumin (P<0. 01,P<0. 05,P>0. 05). HE and Masson staining results indicated that tannins from pomegranate rind could improve the pathologi-cal damage in PHN rats. Conclusion:Tannins from pomegranate rind has notable improvement for PHN in rats.

Objective:To study the influence of pomegranate tannins on the endogenous metabolites in the urine of normal rats by metabonomics method. Methods:The rats were divided into two groups, the blank control group and tannins group. The rats in tan-nins group were orally administered 78. 5 mg·ml-1 pomegranate tannins for 4 weeks. The urine samples were collected and used in the metabonomics study. The urine data were collected by HPLC-MS and comparatively analyzed using PCA and PLS-DA method in SIM-CA-P software. Results:The score points of tannins group displayed obvious distance compared with those of the blank control group, and the changes were the most obvious on the 22nd administration day. Conclusion:Endogenous metabolites in rat urine are obviously influenced by pomegranate tannins, and the research provides the basis for the further study of pomegranate tannins.

Polyamine biosynthesis is controlled primarily by omithine Decarboxylase (ODC) and S-adenosylmethionine decarboxylase (AdoMetDC). Antisense ODC and AdoMetDC sequences were cloned into an adenoviral vector (Ad-ODC-AdoMetDCas). To study the inhibitory effects of Ad-ODC-AdoMetDCas on polyamine biosynthesis and esophageal cancer cell apoptosis, adenovirus-mediated gene tmnsduction efficiency was assessed with counting GFP-positive cells using MTT. The malignant phenotype of Eca109 cells was assessed by growth curve. Western blot and HPLC were used to detect ODC and AdoMetDC expression and polyamine content in Ecal09 cells. TUNEL was used to analyze cell apoptosis. The change of morphology of apoptotic cells was observed by electron microscope. It was demonstrated approximate 70% of Eca 109 cells were infected with Ad-ODC-AdoMetDCas when MOI reached 50. The expression of ODC was inhibited in the infected tumor cells. Ad-ODC-AdoMetDCas could inhibit Ecal09 cell growth and invasive ability. TUNEL proved that Ad-ODC-AdoMetDCas can lead to cell apoptosis. Characterized morphology was observed by electronmicroscope (ehromatincondensation,nuclear disintegration,formation of apoptoticbodies).It was suggested Ad-ODC-AdoMetDCas has significant inhibitory effects on esophageal cancer cell proliferation, leads to cell apoptosis and bears therapeutic potential for the treatment of esophageal cancer.

Objective:To study the effect of tannins from Pericarpium Granati on hepatic microsomal enzyme in rats. Methods:Thirty Wistar rats were randomly divided into five groups:the blank control group, high, medium and low dose groups of tannins from Pericarpium Granati, the positive control group of phenobarbital sodium. The blank control group was given physiological saline. The three different doses groups were respectively given tannins from Pericarpium Granati orally at the dose of 150,100 and 75 mg·kg-1 · d-1 for 7 days. The positive control group was given phenobarbital sodium 80 mg·kg-1 ·d-1 with intramuscular injection for 5 days. At the end of the experiment, the activity ofⅠandⅡphase metabolic enzymes in liver microsomes of each group was determined by UV. Results:Compared with the blank control group, the high, medium and low dose groups of tannins from Pericarpium Granati could sig-nificantly decrease the content of CYP 450 and CYPb5, and inhabit the activity of ADM (P<0. 01);the high and medium dose group could significantly inhibit ERD enzyme activity (P<0. 01);the high dose group could significantly reduce GST enzyme activity (P<0. 01). Conclusion:Tannins from Pericarpium Granati has notably inhibitory effect on hepatic microsomal enzyme in rats, which can reduce the expression of CYP3A and CYP2E1 in a dose-dependent manner.

Objective To investigate the effect of raloxifene on the mRNA expression of endothelin-1 in vascular endothelial cells and assess the role of estrogen receptor. Methods Bovine carotid endothelial cells were pretreated with 10nM raloxifene for 24 hours, then total RNA was harvested and Northern blotting was performed to investigate the effect of raloxifene on the mRNA expression of endothelin-1. Furthermore, estrogen receptor inhibitor, 100nM ICI 182 780 was used to pretreat the cells together with raloxifene and the expression of endothelin-1 was observed too. Results The mRNA expression of endothelin-1 in bovine carotid endothelial cells was inhibited significantly by pretreatment with raloxifene and this effect could be blocked by ICI182 780 (0.16?0.05 vs 0.39?0.07, P

Objective:To investigate the anti-tumor effect of different extracts of Tricholoma matsutake Sing. in vitro. Methods:MTT method was employed to study the inhibitory effect of ethanol extracts from different parts of Tricholoma matsutake Sing. and the polysaccharides extracts on HepG-2 cells, MCF-7 cells and Hela cells. FCM assay was used to detect HepG-2 and Hela cell apoptosis induced by the polysaccharides extracts. Results:The polysaccharides extracts of Tricholoma matsutake Sing. could inhibit the prolif-eration of the three tumor cells with IC50 of 53. 77 μg·mL-1(HepG-2), 40. 04 μg·mL-1(Hela) and 100. 65 μg·mL-1(MCF-7), respectively. The inhibitory effect of the polysaccharides extracts showed a time-and dose-dependent manner. The tumor cell apoptosis could be induced by the polysaccharides extracts. Conclusion:The maln anti-tumor effective extracts of Tricholoma matsutake Sing. in vitro is the polysaccharides extracts, which show significant anti-tumor activities in vitro and can induce tumor cell apoptosis.