The in vitro and in vivo antiangiogenenic effect of galangin / 国际药学研究杂志

Objective To investigate the antiangiogenic effect of galangin in vitro and in vivo.Methods The inhibitory ef?fect of galangin on human umbilical vein endothelial cells(EaHy926)was tested by sulphorhodamine(SRB)method,the EaHy926 endothelial cell migration was assessed using in vitro model system,and the in vivo antiangiogenic effect of galangin at 1,5 and 10 μg was evaluated using the chorioallantoic membrane(CAM)model.The H22 tumor-bearing model was established using BALB/c nude mice,which were divided into five groups:The model group,positive control group〔ip cyclophosphamide 20 mg/(kg·d)〕and the galangin 10,20 and 40 mg/(kg·d)groups,respectively.After the daily administration for 15 consecutive days,the tumors grown in the nude mice were examined and the microvessel density(MVD)was tested via examining the expression of CD31 in the tumor tissues by immunohistochemistry in order to evaluate the effect of galangin to the tumor growth and the angiogenesis of the tumors. Result Galangin inhibited both the growth,migration and Matrigal tubule of EaHy926 cells in a dose-dependent manner in the in vitro test. Further in the in vivo test,galangin could also obviously inhibit the angiogenesis of CAM at the 5 and 10 μg concentration.The tumor mass and the relative tumor volume in the 20 and 40 mg/(kg·d)galangin groups and the positive control cyclophosphamide group were significantly lower(P<0.05)than those in the model group in the in vivo nude mice test. The tumor inhibitory rates of those three groups were 34.17%,79.73% and 55.75%,respectively.The MVD was also significantly lower in the high dosage galangin groups than that in the model group. Conclusion Galangin showed the obvious anti-angiogenenic effect both in vitro and in vivo in the present study.

Zoledronic acid inhibits growth of hepatocellular carcinoma cells in vitro and in vivo / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Growing preclinical evidence shows that zoledronic acid (ZOL) exhibits direct antitumor activity in various cancer cell lines. However, the cytotoxic effects of ZOL on human hepatocellular carcinoma (HCC) cells have not been established. In the present study, we investigated the effect of ZOL on HCC both in vitro and in vivo.</p><p><b>METHODS</b>Cytotoxicity and cell cycles were assessed with Sulforhodamine B colorimetric assay and flow cytometry. Expression levels of cell cycle phase-linked proteins were examined. The effect of ZOL on HCC in vivo was explored based on H22-subcutaneous injection (s.c.) and H22-intraperitoneal injection (i.p.) mice model.</p><p><b>RESULTS</b>ZOL inhibited the growth of SK-HEP-1 and H22 cells and induced S-phase arrest through downregulating cdc2 protein and upregulating cyclin A. It inhibited the growth of s.c tumors, and increased the survival of both H22-s.c. and H22-i.p. mice in vivo.</p><p><b>CONCLUSION</b>ZOL inhibits growth of HCC cells in vitro and in vivo.</p>

Difference analysis of proteome between diabetic cataract and age related cataract / 中华实验眼科杂志

Background With the changes of diet and living style,the diabetes has become the major diseases affecting human health.Diabetic cataract is a common complication of diabetes. Objective The present study was to investigate the difference of lens proteomics between diabetic cataract and age related cataract using two dimensional electrophoresis (2-DE) and mass spectrometry in order to postpone happening of diabetic cataract and offer the effective approach to the prevention and therapy of diabetic cataract. Methods The lenses were obtained from 8 diabetic patients and 12 age-related cataract patients during the surgery to extract the protein by lysis and centrifugation.The lens proteins were separated using immobilized pH gradients 2-DE.Image analysis was carried out using PDQuest Advanced-8.0.1 software package.Significant difference of the crystallines was identified by matrixassisted laser adsorption/ionization time of-flight-mass spectrometry (MALDI-TOF-MS) and peptide mass fingerprint combined with protein database. Results The maps of 2-DE showed that lens proteins of diabetic cataract and age related cataract were in the section of pH 5-9 with the relative molecular weight 14000-97000;while relative molecular weight of more abundant crystalline was localized at 20000-31000.About 3 differential protein spots were detected by image analysis software.Two crystallines,αB and βB1 crystallin,were identified using MALDI-TOF-MS.Conclusions Proteomic analysis of lens can be accomplished and the proteins can be well separated,moreover,differential proteins can be analyzed using 2-DE and mass spectrometry between diabetic cataract and age related cataract.These results indicate that αB and βB1 crystallin proteins accelerate the development of diabetic cataract.This technique offers a new avenue for clarity of lens proteins of diabetic cataract other than age related cataract.

[Studies on spray of niclosamide ethanolamine salt. I. development and effect assessment of spray of niclosamide ethanolamine salt].

OBJECTIVE: To develop a spray of niclosamide ethanolamine salt for prevention of bovine from Schistosoma japonicum infection, and explore its characteristics and effect. METHODS: The solubilizers, penetrating agents, emulsifiers were screened, and the spray of niclosamide ethanolamine salt was formulated according to the screening results. The niclosamide ethanolamine salt was determined by using a HPLC technique, and the stability was observed. The preventive effect of the spray was assessed by in-vitro trials against cercariae and protection trials in mice. RESULTS: The screened formulation was presented as following: 1% niclosamide ethanolamine salt was dissolved in 18% dimethyl sulfoxide, and then added with 1% azone and 2% span, together with 78% ethanol, to yield a 1% spray of niclosamide ethanolamine salt. The spray appeared golden flowing liquid, with 1% niclosamide ethanolamine salt in content (W/W), pH 7.4-7.8, and good thermal and cold stability. All cercariae died (100%) while exposed to the spray at a concentration of 1.00 mg/L for 2 min, and the similar effect was achieved while exposed to 0.50 mg/L of the spray for 5 min or 0.10 mg/L for 30 min. The spray at concentrations less than 0.05 mg/L had no evident toxicity to cercariae. A volume of 0.5 ml of the 1% spray was sprayed on the abdomen of mice, 1-3 d later, the mice were infected with S. japonicum cercariae on the spraying sites, no mice were infected, with a protection rate of 100%. Five days post-spraying, the protection rate was 40%, and the worm burden reduction rate was 65.87%. Ten days later, all the mice were infected, however, the worm burden reduction rate was 51.98%. The worm burdens on days 5 or 10 post-spraying were significantly lower than those of the control (P < 0.01). The spray exhibited a good preventive efficacy to mice from S. japonicum infection in lab. CONCLUSIONS: The spray of niclosamide ethanolamine salt has stable physical and chemical property, and is a novel liquid preventive agent against bovine schistosomiasis. In addition, it has a rapid activity against S. japonicum cercariae, so can prevent bovine from S. japonicum infection.