Aim ToestablishthemethodofHighper-formance liquid chromatography ( HPLC ) for detecting plasma concentration of indazole compound DL0805-1 , a Rho kinase inhibitor, and to investigate its pharma-cokinetics in rats with intravenous injection. Methods ThedetectingsystemwasAgilent1200-DAD;chro-matographic column was Agilent TC-C18 ( 4. 6 mm × 250 mm, 5 μm); the ultraviolet detection wavelength was 235 nm; the column temperature was 35 ℃; the flow rate was 1 ml·min-1;the mobile phase was ace-tonitrile-0. 05% H3 PO4 gradient elute. Rat blood sam-ples were collected at different intervals after intrave-nous injection of a single dose of DL0805-1 , and the concentration of DL0805-1 in rat plasma were deter-mined by HPLC method for estimating pharmacokinetic parameters.Results Afterintravenousinjectionof DL0805-1 in rats, prototype and its metabolite were detected in plasma. T1/2 of DL0805-1=(2. 34 ± 1. 42) h, Cmax=(3. 51 ± 0. 44) mg·L-1, T1/2 of metabolite of DL0805-1 = ( 1. 27 ± 0. 45 ) h, Cmax = ( 3. 55 ± 0.22)mg·L-1.Conclusion Theseresultssuggest that DL0805-1 may be metabolized into another sub-stance in vivo and play biological functions. The meth-od is sensitive, simple, and accurate, and can be used for the determination of DL0805-1 in rat plasma and pharmacokinetic studies.

Objective To explore the protective effect of rosiglitazone on insulin resistance( IR)induced by high glucose in vascular endothelial cells and its possible mechanism. Methods Human umbilical vein endothelial cells( HUVECs) was divided into 3 groups:the normal control group cultivated in DEME medium with 5. 5 mmol·L-1 glucose;the high glucose group( HG)cultivated in DEME medium with 33 mmol · L-1 glucose for 24 h after the IR model was set up;the rosiglitazone group cultivated in DEME medium with 33 mmol·L-1 glucose and 10 μmol·L-1 of rosiglitazone for 24 h after the IR model was set up. The cell viability,nitric oxide(NO),endothelin-1(ET-1),mitochondrial membrane potential,reactive oxygen species ( ROS),p-IKK and IkBa protein levels were detected. Results Compared with the normal control,the cell viability,the level of NO and the mitochondrial membrane potential were decreased,levels of ET-1 and ROS increased,p-IKK expression was up-regulated,and IκBα expression was down-regulated in HG group(all P〈0. 01). Rosiglitazone reversed these changes in a time-dependent manner(P〈0. 05). Conclusion Rosiglitazone has the protective effect on insulin resistance induced by high glucose in vascular endothelial cells via inhibiting ROS/IKK signaling pathway.

Objective: To investigate different Er:YAG laser power settings on the bonding properties of IPS e.max CAD ceramics. Methods : 96 IPS e.max CAD ceramics blocks (5 mm × 5 mm × 5 mm) were prepared and randomly divided into 8 groups (n = 12), the untreated blocks served as the control, while one of the experimental groups was treated with 4.5% HF for 20 seconds, six remaining test group (C、D、E、F、G、H) were treated with different Er: YAG laser power settings: 100 mJ、200 mJ、300 mJ、400 mJ、500 mJ and 600 mJ. Morphology of the ceramic surface was observed by atomic force microscopy and its shear bond strength (SBS) was tested. Results : Higher shear bond strength values were found in group C-H compared to group B, the highest is group F (24.12 ± 1.91) MPa. The difference was statistically significant. The atomic force microscope observation of the surface structure showed that the control group was smooth and flat, and the HF-like etching group formed a uniform needle-like convex structure. The laser group gradually formed a regularly arranged cylindrical convex structure, in which the surface of the G and H groups was damaged. Conclusion The Er: YAG laser power settings of 400 mJ can be used as an effective pretreatment method before bonding of IPS e.max CAD ceramic.