OBJECTIVE:To study the lung targeted characteristic of tetrandrine polylactic acid microsphere(TPM).MET_HODS:TPM and tetrandrine injection were injected intravenously into mouse,an RP-HPLC was established to measure the content of TPM in biological samples,and the concentrations of tetrandrine in different tissues of mice were determined and compared.RESULTS:The determinable concentration of tetrandrine in plasma was in the linear range of 0.519～17.000?g/ml(r=0.9 996),the recovery was 97.32%,the mean value of RSD was 4.46%.After the use of TPM,the concentrations of tetrandrine in mouse tissues were significantly higher than tetrandrine injection,and the highest concentration was detected in lungs of mouse.CONCLUSIONS:TPM is distinguishingly lung targeted.

OBJECTIVE:To provide scientific evidence for the microsphere's m etabolism in vivo of lung targeted tetran?drine polylactic acid(TET-PLA)microspheres.METHODS:Blood was sampled from carotid artery after microspheres were injected into rabbit through auricular vein,the concentration of TET in plasma was determined by RP-HPLC method;The pharmacokinetic parameters were obtained by using3p87program.RESULTS:Concentration-time curves of TET micro?spheres were fitted to a2-compartment model with t 1/2? of(286.49?237.55)min and AUC of(810.33?287.49)(?g?min)/ml.CONCLUSION:TET-PLA microspheres show sustained release effects in rabbits.

OBJECTIVE:The preparation of microspheres was optimized by central composite design in order to improve the lung targeting of tetrandrine chitosa microspheres. METHODS:Microspheres were prepared using an emulsion-chemical crosslink technique.Effects of three independent variables i.e. weight percent of tetrandrine and christon, volume percent of water phase and organic phase and christon concentration in aqueous phase were investigated on four response variables.Response variables selected in the research were yield,drug loading, envelop efficiency, mean diameter and span of dispersity.Second-order polynomial and linear equations were fitted to the data,and the resulting equations were used to produce three dimensional response surface graphs,by which optimal experimental conditions were selected. RESULTS:Five response variables were found to be dependent on three independent variables. According to optimal experimental conditions.An optimized formulation contained weight percent of tetrandrine and christon was 61.97%, volume percent of water phase and organic phase was 13.51% and christon concentration in aqueous phase was 2.37%. CONCLUSION:The central composite design can be used to optimazation of preparation formulation,diameter of the microspheres optimized by it can meet the demands of lung-targeting.

OBJECTIVE:To establish a method for the rapid contents determination of potassium chloride and calcium chloride in Compound sodium chloride injection. METHODS:After diluted in appropriate way,Compound sodium chloride injection was sampled directly and contents of potassium chloride and calcium chloride were determined simultaneously by ICP-OES. The powder was 1 300 W,plasma gas flow rate was 15 L/min,auxiliary cooling gas flow was 0.2 L/min,atomizer flow rate was 0.8 L/min, the peristaltic pump rate was 0.8 L/min,atomizer pressure was 315 kPa,and the observation was axial observation,analysis spec-tral lines of potassium and calcium were 766.490 nm and 315.887 nm. RESULTS:The linear ranges of potassium and calcium were 1.0-12.0 mg/L (r=0.999 7 and 0.999 9);RSDs of precision and reproducibility tests were lower than 1%;recoveries were 98.5%-100.5%(RSD=0.59%,n=9)and 99.3%-102.3%(RSD=0.98%,n=9). CONCLUSIONS:The method is simple,rapid and simple,and can be used for the quality control of Compound sodium chloride injection.

Objective To explore the effects and mechanisms of urokinase-type plasminogen activator (uPA) on high glucose-induced rat mesangial cells proliferation and phenotype transformation. Methods Rat mesangial cells were cultured and incubated in media containing either 5 mmol/L D-glucose or 30 mmol/L D-glucose with or without addition of wortmannin, or uPA (105 U/L) for different time periods. At the end of the incubation period, mesangial cells proliferation was assessed by MTT assay and flow cytometric analysis. Cyclin-dependent kinase 2 (CDK2) and p27kip1 expression and activation of Akt were evaluated by Western blotting and Akt kinase assay respectively. Furthermore, the expression and distribution of α-SMA were detected with laser confocal microscopy. Results MTT assay and flow cytometric analysis demonstrated that high glucose induced mesangial cells proliferation (P＜0.05) and an incresed proportion of cells in G2/M+S stage after 24 h incubation (P＜0.01), which were attenuated by uPA or wortmannin (P＜0.01). High glucose induced the enhance of Akt activity after 3 h (P＜0.05), and the effect was inhibited by wortmannin or uPA (P＜0.01). High glucose did not alter CDK2 expression (P＞0.05),but significantly inhibited p27kip1 expression (P＜0.05), which was attenuated by wortmannin or uPA (P＜0.01). High glucose induced the up-regulation of α-SMA expression and perinucleus location in mesangial cells after 24 h (P＜0.01), which were alleviated by wortmannin or uPA (P＜0.01). Conclusion uPA up-regulates p27kip1 expression and counteracts high glucose-induced mesangial cells proliferation and phenotype transformation via blocking PI3K-Akt signaling pathway.

Purpose　The aim is to prepare the extract of immunocompetent cell proliferation from human placenta and to try to find out a suitable method of preserving the extract.Methods　The extract was mainly prepared by heat-treating placenta homogenated fluid. Then the activity to stimulate murine splenic lymphocyte proliferation in vitro was done with MTT , exposing　the　extract to　radioisotope 60　Co.Results　The content of protein was 2～3mg per gram placenta measured by Lowry′s Method.The rate to promote cell proliferation was more than 80 percent.The activity lasted a few months after being exposed to radioisotope.Conclusion　The extract prepared by heat-treating not only had high activity, but also had the unique method and good repeatability.This prepared extract as a kind of stable,reliable and remarkably promoting lymphocyte proliferation reaction had the value of development production on broad scale as well as in clinical practice.

Objective To investigate the effect of surfactant protein A (SP-A) on the production of MIP-2 and binding activity of NF-?B in rat tubular epithelial cells, and evaluate its possible role in renal inflammation. Methods Confluent cultures of NRK-52E cells (a renal tubular epithelial cell line of rat origin) were pretreated with various concentrations of SP-A(0 to 80 ?g/ml) and stimulated by lipopolysaccharide (LPS) (10 ?g/ml) with 2% serum. MIP-2 expression was measured by enzyme-linked immunosorbent assay (ELISA) and reverse transcription-polymerase chain reaction (RT-PCR). The effect of SP-A on NF-?B binding activity was assessed by electrophoretic mobility shift assay (EMSA). Results MIP-2 mRNA and protein was expressed and up-regulated in NRK-52E cells stimulated by LPS. The expression of MIP-2 was down-regulated by SP-A. NF-?B binding activity was inhibited by SP-A in a concentration-dependent manner. Conclusion SP-A binding activity and down-regulates the expression of MIP-2 in renal tubular epithelial cells, which may play an important role in the modulation of renal tissue inflammation.

Objective To evaluate the effect of ALD on podocyte apoptosis and the possible roles of Akt in ALD-induced apoptosis. Methods The cultured rat podocytes were incubated with increasing concentrations of ALD (10-9~10-5 mol/L) for variable time periods. Apoptosis was evaluated by cell nucleus staining and flow cytometry. RT-PCR was used to examine the expression of mineralocorticoid receptor (MR)and 11 Beta-hydroxysteroid dehydrogenase type 2 (11?-HSD2) mRNA in podocyte. Activation of Akt/PKB was evaluated by performing Akt kinase assay. Results ALD induced podocyte apoptosis in a dose- and time-dependent manner. The proapoptotic effect was attenuated by the presence of spironolactone (10-7mol/L). The expression of MR and 11P-HSD2 mRNA was demonstrated in the podocytes by RT-PCR. ALD also inhibited the activity of Akt in a dose-dependent manner, but the inhibitory effect was significantly ameliorated by the presence of spironolactone. The activity of Akt was negatively correlated with podocyte apoptosis. Conclusion ALD induces apoptosis in rat podocytes through the signaling mechanism by which Akt is inhibited.

Objective Systematic evaluation of cerebrolysin in the treatment of neonatal hypoxic -ischemic encephalopathy.Methods Computer search Cochrane Library, EMBase, PubMed, Chinese Journal Full-text Database (CNKI), Chinese Biomedical Literature Database (CBM), Wanfang Database ( each database retrieval time from its creation to May 2016 ) About cerebrolysin Randomized controlled clinical trial of neonatal hypoxic -ischemic encephalopathy.According to the inclusion and exclusion criteria of the literature, the methodological quality of the included research was evaluated and the data were extracted.Metadata was analyzed by RevMan 5.3 software.Results A total of 41 RCT patients were enrolled, with a total of 3695 patients, the experimental group was 1932 cases, the control group was 1763 cases.Meta analysis showed, the efficacy of cerebrolysin in the treatment of neonatal hypoxic-ischemic encephalopathy was significantly higher than that in the control group [OR=3.85, 95% CI (3.15,4.70), P<0.000001], for the impact of clinical symptoms, the number of primitive reflexes of neonatal hypoxic-ischemic encephalopathy in the treatment group was significantly higher than that in the control group [MD=-1.22, 95% CI ( -2.06,-0.38), P=0.004], muscle tension recovery days[MD=-1.69, 95% CI ( -1.80,-1.58), P<0.00001], conscious state recovery days[MD=-1.32, 95% CI ( -2.25,-0.40), P=0.005], seizure recovery days [MD=-2.36, 95% CI ( -3.70, -1.03), P =0.0005], and other indicators were shorter than the control group, the difference between the experimental group and the control group was statistically significant.Conclusion Cerebrolysin havean effective in treating HIE.