Objective To compare the difference in bioavailability of microemulsion and pill by detecting the concentration of andrographolide in rabbit plasma.Methods RP-HPLC was used to detect the concentration of andrographolide in rabbits plasma at different time,and software 3p87 was used to analyze the pharmacokinetics parameter.Results The pharmacokinetics parameters of andrographolide oral microemulsion and andrographolide pill were as follows::AUC0-7=1 406.72 ? g? mL-1? min,Tpeak=27.08 min,Cmax=5.37 ? g/mL for microemulsion;AUC0-7=877.37 ? g? mL-1? min,Tpeak=61.04 min,Cmax=3.06 ? g/mL for the pill.Conclusion Oral microemulsion of andrographolide has a shorter peak time and higher biological availability than the pill.

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.

This paper constructs numerical models of bioprosthetic heart valve and blood. The fluid solid interaction is carried out using penalty function method. The mechanical property of the bioprosthetic heart valve during cardiac cycle is simulated with ANSYS software. Results show that the Von Mises stress concentrates at the junction of attachment edge and coaptation edge. The open time of bioprosthetic heart valve is consistent with that of actural measurement. The peak velocity of blood is in the range of physiology. This model provides more realistic mechanical property of bioprosthetic heart valve during cardiac cycle compared to pure solid model, and facilitates design and optimization of bioprosthetic heart valve.
Bioprosthesis ; Heart Valve Prosthesis ; Heart Valves ; Humans ; Models, Cardiovascular ; Prosthesis Design

Fed-batch cultures of recombinant Rchia pastoris were conducted for production of angiostatin. The whole fermentation included a growth phase on glycerol and an expression phase on methanol. When ammonium hydroxide solution was used to adjust pH, the cell growth during the expression phase was inhibited and the highest angiostatin concentration was 9.08 mg/L. Shake-flask cultures were carried out in media containing different quantities of ammonia. The results showed that ammonia had an obvious inhibition effect on the cell growth during the expression phase. Therefore KOH solution was used to adjust pH, and during the expression phase cells were able to grow and the highest angiostatin concentration reached 20 mg/L.

Experimental investigations were conducted on the process of combustion and explosion vent in a 200 mm (diameter)×400 mm (length) vertical cylindrical vessel. When CH4-air mixture gases were used and the vent diameter was 55 mm,conditions of φ (equivalent ratio)=0.8, φ=1.0 and φ=1.3 and two ignition positions (at the cylinder center and bottom) were selected. The venting processes and the correlated factors are discussed in this paper.

Definite therapeutic effect has obtained by TCM in treating acute cerebral hemorrhage (ACH) according the TCM theory of "blood circulating outside the vessels is the stasis" using breaking stagnant and eliminating blood stasis (Poxue Zhuyu) method, but no material involving the natural development of stoke in superacue stage (0 - 4 hrs after onset of the disease) being presented so far. It has been proved by randomized, double-blinded multi-centeric clinical trials that recombinant activated factor VII (rF VII a) could decreased the morbidity and disability of patients suffered from ACH, suggesting that use hemostasis treatment in ACH during superacu stage should be stressed, and the drugs for Poxue Zhuyu should be used cautiously in the period of 0 - 4 hrs after onset. The hemorrhagic disorder could be eliminated by using drugs for Poxue Zhuyu and other medicines in rational combination.
Cerebral Hemorrhage ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Factor VIIa ; biosynthesis ; genetics ; therapeutic use ; Humans ; Medicine, Chinese Traditional ; Phytotherapy ; Recombinant Proteins ; biosynthesis ; genetics ; therapeutic use

This paper constructs numerical models of bioprosthetic heart valve and blood. Thefluid solid interaction is carried out using penalty function method. The mechanical property of the bioprosthetic heart valve during cardiac cycle is simulated with ANSYS software. Results show that the Von Mises stress concentrates at the junction of attachment edge and coaptation edge. The open time of bioprosthetic heart valve is consistent with that of actural measurement. The peak velocity of blood is in the range of physiology. This model provides more realistic mechanical property of bioprosthetic heart valve during cardiac cycle compared to pure solid model, and facilitates design and optimization of bioprosthetic heart valve.

OBJECTIVETo analyze the promoter methylation levels of p15, CDH1, DAPK and HICI genes of patients with myelodysplastic syndrome (MDS) and explore the relationship between the level of methylation and clinical features.

METHODSDNA methylation levels of p15, CDH1, DAPK and HICI in peripheral blood (PB) or bone marrow (BM) samples from 52 MDS patients were detected by real-time quantitative PCR. The correlation of the methylation level with clinical features and hematological findings was analyzed. 38 de novo AML patients and 46 normal individuals served as controls.

RESULTSThe methylation levels of p15, CDH1, DAPK and HICI were 16.23 ± 21.69, 6.59 ± 9.39, 0.14 ± 0.11 and 7.81 ± 9.70 in BM, and 14.96 ± 20.16, 6.00 ± 9.26, 0.12 ± 0.14 and 6.74 ± 9.72 in PB, respectively from 18 MDS patients, and the difference between BM and PB was not statistically significant (P > 0.05). The methylation levels of p15 (14.70 ± 18.17) and CDH1 (6.61 ± 8.79) genes in high risk (RAEBI/II) MDS were significantly higher than in low risk (RCMD/RARS/5q-, p15: 1.99 ± 1.59, CDH1: 1.23 ± 1.14 and RCMD, p15: 3.02 ± 3.42, CDH1:1.53 ± 2.06) MDS or control (p15: 1.69 ± 1.82, CDH1: 1.01 ± 1.12) (P < 0.05). The methylation levels of DAPK gene had no difference among subtypes of MDS, and that of HIC1 gene only differed between RAEB I/II (9.16 ± 11.95) and control (2.49 ± 2.26) (P = 0.042). The difference of methylation levels of p15, CDH1, DAPK and HICI in BM was statistically significant among subtypes of MDS (P = 0.001, 0.003, 0.039, 0.023, respectively). And so did of p15 and DAPK in PB (P = 0.013, 0.006, respectively). The methylation level of p15 and CDH1 was significantly correlated with IPSS classification and blasts percentage in BM.

CONCLUSIONSp15 and CDH1 genes are special hypermethylation genes in MDS. Methylation level of HIC1 gene showed an upward tendency from low risk to high risk MDS.

Adult ; Aged ; Aged, 80 and over ; Apoptosis Regulatory Proteins ; genetics ; metabolism ; Cadherins ; genetics ; metabolism ; Calcium-Calmodulin-Dependent Protein Kinases ; genetics ; metabolism ; Case-Control Studies ; Cyclin-Dependent Kinase Inhibitor p15 ; genetics ; metabolism ; DNA Methylation ; Death-Associated Protein Kinases ; Female ; Humans ; Kruppel-Like Transcription Factors ; genetics ; metabolism ; Male ; Middle Aged ; Myelodysplastic Syndromes ; genetics ; metabolism ; Promoter Regions, Genetic ; Real-Time Polymerase Chain Reaction ; Young Adult

PURPOSETo verify whether there exists any difference in higher order aberrations after undergoing myopic LASIK (laser in situ keratomileusis) with conventional ablation and customized ablation in different eyes of the same patient.

METHODSThis was a prospective randomized study of 54 myopic eyes (27 patients) that underwent LASIK using the Nidek EC-5000 excimer laser system (Nidek, Gamagori, Japan). Topography-guided customized aspheric treatment zone (CATz) was used in the first eye of the patient (study group) and the other eye of the same patient was operated on with conventional ablation (control group). Higher order aberrations [root-mean-square (RMS) in the 5-mm zone] of both groups were observed with the Nidek OPD-Scan aberrometer before and 3 months after LASIK. Preoperative mean refractive error was similar between two eyes of the same patient (t=-0.577, P>0.05).

RESULTSPreoperatively, higher order aberrations (RMS in the 5-mm zone) in the CATz ablation and conventional groups were (0.3600+/-0.0341) microm and (0.2680+/-0.1421) microm, respectively. This difference was not statistically significant (t=1.292, P>0.05). Three months after LASIK, higher order aberrations (RMS in 5-mm zone) in the CATz ablation and conventional groups were (0.3627+/-0.1510) microm and (0.3991+/-0.1582) microm, respectively. No statistically significant difference was noted between pre- and postoperative higher order aberrations in the CATz group (t=-0.047, P>0.05). However, a statistically significant increase in higher order aberrations was observed after conventional ablation (t=-5.261, P<0.05). A statistically significant difference was noted in the increase of higher order aberrations after LASIK between groups (t=-2.050, P=0.045).

CONCLUSIONLASIK with conventional ablation and topography-guided CATz ablation resulted in the same BSCVA (best spectacle-corrected visual acuity) 3 month after LASIK. Higher order aberrations were increased, but the increase of higher order aberrations after customized ablation treatment was less than that after conventional ablation.

Adolescent ; Adult ; Humans ; Keratomileusis, Laser In Situ ; methods ; Myopia ; surgery ; Prospective Studies ; Visual Acuity

OBJECTIVETo study the inhibition effect of celastrol on neovascularization.

METHODSThe effect of celastrol on the in vitro proliferation of endothelial cell of vessel (ECV) was examined by MTT assay. The effect of celastrol on endothelial cell migration, tube formation on Matrigel and Chick chorioallantoic membrane angiogenesis was also examined. Matrigel plug assay was used to evaluate the effect of celastrol on angiogenesis in vivo.

RESULTSThe proliferation of ECV was inhibited significantly by celastrol with IC(50) being 1.33 microg/ml. Celastrol inhibited endothelial cell migration and tube formation in a dose-dependent manner. Celastrol also inhibited angiogenesis both in Matrigel plug of mouse model and in chick chorioallantoic membranes.

CONCLUSIONCelastrol, which can inhibit angiogenesis, could be developed as an antiangiogenic drug.

Angiogenesis Inhibitors ; pharmacology ; Animals ; Endothelial Cells ; drug effects ; Mice ; Mice, Inbred BALB C ; Triterpenes ; pharmacology