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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.

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.

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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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.

be diagnosed by imaging examination before operation.The ALT patients with large or symptomatic adrenal lipomatous lesions or preoperatively diagnosed teratoma should be given surgical treatment.

To develop a new small molecular probe for discovering an antitumor lead compound from the replacement of carboxylic group of two molecular antibacterial fluoroquinolones with a heterocyclic ring, a series of the C3/C3 bis-fluoroquinolones tethered with an 1, 3, 4-oxadiazole ring were synthesized as their respective HCl salts, and their structures were characterized by elemental analysis and spectral data. The in vitro antitumor activity against L1210, CHO and HL60 cell lines was also evaluated via the respective IC50 values by methylthiazole trazolium (MTT) assay.

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.

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.