Objective: To study the mechanism of effect of total flavone of rhizoma drynariae in groups with different dosage on osteoblasts cultured in vitro. Methods: To culture osteoblasts with UMA-106-01 osteoblast strain and to observe the activity of ALP and the endosmosis of 3H-TdR. Results: The total flavone of rhizoma drynariae increased the activity of ALP in cells cultured with UMR-106-01 strain. The ALP activities correspondingly changed in the 24h, 48h and 72h, which related to dosage effect and time effect. Among them, the activity in the 48h is the most ideal one. And the amount of endosmosis of the total flavone of rhizoma drynariae to 3H-TdR increased more remarkably in the 48h than that in the 24h and it also related to the time effect. Conclusion: The total flavone of rhizoma drynariae can promote the differentiation and multiplication of osteoblasts.

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Objective To study the drug-time process of aurantiin in Rhizoma Drymariae in vivo.Methods By the optimization of the chromatographic condition,a reversed-phase HPLC was established to measure the content of aurantiin in the serum and the tissues of rats.Results After administration of total flavones of Rhizoma Drymariae to the rats by gavage,aurantiin started to be absorbed in 30 minutes and arrived at the peak in 90 minutes.The blood drug concentration decreased evidently 4 hours after gavage and maintained at a certain level in 8 hours.The drug concentration was highest in the stomach and bowels,but decreased quickly.The concentration in the liver,lungs and kidney came next and can be determined in the muscles and fat;however,it was very low or zero in the brain.Conclusion This method is convenient,sensitive,rapid and without the interference of other impurities.It is suitable for the determination of aurantiin content in the serum and tissues of rats.Administering total flavones of Rhizoma Drymariae to the rats by gavage,aurantiin is absorbed slowly and maintains for a long time and subsides slowly in the blood.

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To explore an efficient strategy for the conversion of antibacterial fluoroquinolones into antitumor fluoroquinolones, an azole heterocyclic ring of oxadiazole instead of the C-3 carboxylic acid group with a functionalized hydrazone group as a modified side-chain, fifteen novel 2-(fluoroquinolon-3-yl)-oxadiazole-5- sulfanylacetylhydrazone derivatives 7a-7o were designed and synthesized on the basis of the pharmacophore hybridization principle from pefloxacin, separately. The structures for fifteen title compounds were characterized by elemental analysis, 1H NMR and MS, and their in vitro antitumor activity against Hep-3B cell line was evaluated by a MTT assay. The results showed that the title compounds exhibited more significantly inhibitory activity than that of the parent pefloxacin, in which compounds with electron-withdrawing group attached on aryl ring had more potency than that of compounds with electron donating group, especially compounds with a carboxylic substituent were comparable to comparison doxorubicin. It suggests that it is favorable for an improvement of antitumor activity to remain a carboxylic acid unit at the aromatic ring.

To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.

AIM: To investigate the effect of 17?-estradiol on insulin action in cultured C2C12 mytoblasts. METHODS: C2C12 mytoblasts were cultured in 35 mm wells of six-well culture plate in an atmosphere of 5% CO 2 at 37℃ in DMEM supplemented with 10% FBS and penicillin/streptomycin(1?10 5 U/L) to reach 80% confluence. Insulin-resistance C2C12 mytoblasts were obtained by incubating the cells for 24 hours in the presence of a high concentration (5?10 -7 mol/L) of insulin. After treatmented with 17?-estradiol (1 nmol/L and 10 nmol/L, respectively) for 24 hours, C2C12 mytoblasts were performed to measure insulin-stimulated 2-DG uptake and GS, PFK, PK activities. RESULTS: 17?-estradiol enhanced the capacity of insulin-stimulited 2-DG uptake, increased the GS, PFK and PK activities and prevented insulin-induced resistance in cultured C2C12 mytoblasts. CONCLUSION: 17?-estradiol potentiates insulin action and preventes insulin-induced resistance in cultured C2C12 mytoblasts.

Background and purpose:It has beenreported that miR-1284 is associated with gastric cancer lymph node metastasis in the research of microRNA microarray in human gastric cancer tissues. But the specific role of miR-1284 in gastric cancer has not been reported. The aim of this study was to investigate the effect of miR-1284 over-expression on the gene expression profiling and invasion/metastasis of human gastric cancer SGC-7901 cells. Methods:Gastric cancer SGC-7901 cells of LV-miR-1284 group were transfected with lentiviral vectors of miR-1284, cells of LV-NC-GFP group were transfected with lentiviral vectors without miR-1284, and cells of control group were not transfected with lentiviral vectors. The expression of miR-1284 was detected by the real-time fluorescent quantitative PCR. Differential expression genes were detected by the microRNA chip. Target genes of miR-1284 were predicted by the bioinformatics. Invasive ability was detected by the Transwell invasion assay. Metastasis ability was detected by subcutane-ously transplanted tumor model of nude mice.Results:Compared with LV-NC-GFP and control groups, the expressions of miR-1284 and 20 genes were up-regulated, and the expression of 17 genes was down-regulated in LV-miR-1284 group. One hundred and thirty-eight target genes of miR-1284 were predicted by the bioinformatics website. Compared with invasive cell number of LV-NC-GFP group (168.67±4.55) and control group (170.33±3.08), the ability of invasion ofcells was weakened in LV-miR-1284 group (70.00±2.37). Compared with the liver metastasis rate of LV-NC-GFP group (85.71%) and control group (85.71%), the ability of metastasis of cells was weakened in LV-miR-1284 group (14.29%). Conclusion:The ability of invasion and metastasis of SGC-7901 cells is suppressed by over-expression of miR-1284. The mechanism may be related to regulating the expression ofSUMO1 andJUNgenes.

To search for fluoroquinolones(FQs)with antitumor activity;the C-3 carboxylic acid group of peflox-acin (1)was replaced by fused heterocyclic core;and twelve novel thiazolo[3;2-b][1;2;4]triazole heterocycles(6a-6l)were designed and synthesized.The structures of target compounds were characterized by elemental anal-ysis and spectral data.The results of the in vitro antiproliferative effect on SMMC-7721;L1210 and HL60 cell lines showed that the title compounds exhibited more significant antitumor activity than both of the pefloxacin and the corresponding opening-ring intermediates(5 a-5 l).Among them;the target compounds which possess a ben-zene ring bearing a hydroxyl group (6e)or a fluorine atom (6j)exhibited more potent antiproliferative effect on SMMC-7721 cells than other compounds.Therefore;the antitumor fluoroquinolones can be designed by replacing the C-3 carboxylic acid group of fluoroquinolones with the thiazolo[3;2-b][1;2;4]triazole moiety.

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.