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.

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.

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AIM:To study the effect and the molecular mechanism of CDX 2 over-expression on the prolifera-tion, growth and cell cycle of human gastric cancer cell line SGC-7901.METHODS:The SGC-7901 cells in LV-CDX2-GFP group were transfected with the recombinant lentivirus vector LV-CDX2-GFP, the cells in LV-GFP group were trans-fected with the negative control lentiviral vector for the negative control , and the cells in blank control group were without any treatment.The cell proliferation was detected by CCK-8 assay.The cell cycle distribution was analyzed by flow cytome-try.The expression of CDX2, Bax, Bcl-2, cyclin D1 and survivin was determined by semi-quantitative RT-PCR and Wes-tern blotting .RESULTS:Compared with LV-GFP group and blank control group , the proliferation activity of the SGC-7901 cells was significantly lower (P<0.05), the G0/G1 phase proportion increased (P<0.05), the mRNA and protein levels of Bcl-2, cyclin D1 and survivin were reduced (P<0.05), and the mRNA and protein levels of Bax were up-regula-ted (P<0.05) in LV-CDX2-GFP group.No statistically significant difference of the above indexes was observed (P>0.05) between LV-GFP group and blank control group .CONCLUSION:Over-expression of CDX2 mediated by lentivirus inhibits the proliferation and growth of human gastric cancer SGC-7901 cells and arrestes the cell cycle at G 0/G1 phase, which may be related to down-regulation of Bcl-2, cyclin D1 and survivin and up-regulation of Bax .

Objective To observe the influence of trunk control training on motor function and the ability of cerebral palsy (CP) patients in the activities of daily living (ADL).Methods Forty patients with CP were randomly divided into a treatment group (n =20) and a control group (n =20).Both groups were treated with routine rehabilitation,while the treatment group also received trunk control training.All patients were assessed with function ambulation category (FAC) classification,time to walk 10 m,the Berg balance scale (BBS),and the modified Barthel index (MBI) at the beginning and eight weeks later.Results Before the intervention there was no significant difference between the two groups in terms of any of the assessments.Eight weeks later,all the assessment scores were significantly better in the treatment group than in the control group.Conclusion Trunk control training can significantly improve motor function and the ADL ability of patients with CP.

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 evaluate the correlation between microRNA-1284 (miR-1284) and gastric cancer, and to investigate the underlying mechanism.METHODS: The expression of miR-1284 was examined by real-time PCR in 63 gastric cancer ( GC) tissue samples and 63 non-malignant adjacent tissue samples.The correlation between miR-1284 and the clinicopathological feature of GC was analyzed.Lentiviral vector containing miR-1284 was constructed and transfected into GC SGC-7901 cells.After transfection, the expression of miR-1284 was examined by real-time PCR.The cell activity was evaluated by CCK-8 assay.The cell cycle and apoptosis were determined by flow cytometry.The ability of cell migra-tion was measured by wound-healing assay.The potential target gene of miR-1284 was predicted by online bioinformatic softwares.The expression of JAG1 mRNA was examined by real-time PCR.The protein levels of JAG1, Notch1 and NF-κB were analyzed by Western blotting.RESULTS:Compared with non-malignant adjacent tissue samples, the results of real-time PCR showed significant downregulation of miR-1284 in 42 GC tissue samples ( P<0.05 ) .The expression level of miR-1284 was not significantly associated with age and gender of the patients, tumor size, TNM staging and lymph node metastases (P>0.05), but significantly associated with histologic grading (P<0.05).Compared with LV-NC-GFP group and control group, after transfection of miR-1284 in LV-miR-1284 group, the expression of miR-1284 was significantly in-creased (P<0.05), the percentages of apoptotic cells and the cells in G0/G1 phase were significantly increased (P<0.05), the cells activity and ability of migration were significantly decreased (P<0.05), and the expression of JAG1, Notch1 and NF-κB was significantly decreased (P<0.05).CONCLUSION:The inhibitory effect of miR-1284 on gastric cancer may be associated with the regulation of its targeting gene JAG1.

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.