Objective: To observe the inhibitory effects of matrine, oxymatrine and sophordine on expression of CD91 and CD13 and secretion of TNF-α in macrophage RAW264.7. Methods: Macrophages were cultured in 6-hole plate and coverslip was prepared. Then macropages were cultured one day with different concentrations(0,12. 5,25,50,100,200 mg/L) of matrine, oxymatrine and sophordine; the expression of CD91 and CD13 by immunohistochemical dyeing was analyzed by Image-Pro plus system (Media Cybemetic, Inc. , 6.0 edition). Meanwhile, the levels of TNF-α in the culture medium of macrophages were examined by ELISA. Results: Matrine, oxymatrine and sophordine could all inhibit CD91 and CD13 expression in macrophage RAW264.7, and the inhibition varied with the concentrations of matrine, oxymatrine and sophordine; the inhibitory effect of matrine was the most prominent one. Moreover, matrine, oxymatrine and sophordine also inhibited the secretion of TNF-α. Conclusion: Matrine, oxymatrine and sophordine can greatly inhibit expression of CD91 and CD13 and secretion of TNF-α in macrophage RAW264.7.

Cough ; etiology ; Eye ; Female ; Foreign Bodies ; complications ; Humans ; Middle Aged ; Nose

Objective To investigate the changes of plasma somatostatin(SS) and its correlation with cellular immune function in neonates with hypoxic-ischemic encephalopathy(HIE).Methods Fifty cases of HIE were collected to detect the SS and T lymphocyte subsets,IL-2,sIL-2R as well as IL-6 levels by radioimmunoassay,APAAP and doule antibody sandwith ELISA methods.Results The SS and sIL-2R levels in patients with HIE were significantly higher(P

Objective To observe the effects of vitamin C (VC) and E (VE) on the uhrastrueture of liver, kidney and brain tissue of fluorosis rats. Methods One hundred and twenty Wistar rats were chosen as the experimental animals and were divided into 9 groups randomly. The control group were given distilled water and the fluoride exposed group were given distilled water containing sodium fluoride 150 mg/L. The throe VC-fluoride exposed groups were given VC orally in a dose of 50,100,150 mg·kg-1.d-1, respectively, and the three VE-fluoride exposed groups were given VE of 25,50,75 mg·kg-1·d-1, respectively. The VC-VE-fluoride exposed group were given VC of 100 mg·kg-1·d-1and VE of 50 mg·kg-1·d-1at the same time of high fluoride water intake. The rats were sacrificed after 9 months and the ultrastructure changes on liver, kidney and brain tissues of each group were observed under transmission electron microscope(TEM). Results The uhrastrueture of liver, kidney and brain showed pathologic changes in the rats that drank water containing high eoneentrations of sodium fluoride. ①Edema of hepatocytes, smeared mitochontria and nuclear matrix, lipid droplet in eytoplasm of hepatocytes, margination of nueleohs as well as obvious swelling of liver sinusoidal endothelial were observed in fluoride exposed group. ② There were marginafion of heterochromatin, expansion of cell space and endoplasmic reticulum in the kidney after the exposure to excess fluoride.③Signifieant changes were found on glial eells on the brain, including cell swelling, increase and marginafion of heterochromatin in the fluoride exposure group. There were no significant uhrastrueture changes in the VC or VE intervention group, while the VC-VE-fluoride exposure group was almost the same as the control group. Conclusions Fluoresis may cause damage on liver, kidney and brain in rats. VC and VE, alone or combined, have protective effects, and the combined supplementation was stronger than single supplementations.

ObjectiveTo explore the relationship among 14 kinds of intolerant food by using association rules to provide evidence for more reasonable diet intake.Methods A total of 2962 adults who received medical examination at the First Affiliated Hospital of China Medical University during January 2008 and June 2010 were enrolled in this investigation.ELISA was used to detect allergen-specific IgG antibody of 14 kinds of food.An association rules model was established by SPSS Clementinel2.0.In order to find positive intolerance association rules,food frequency was recorded with SPSS 16.0.Results Five most commonly seen food intolerance were eggs,crabs,shrimp,milk,and cod (positive rates were 32.5％,26.0％,19.8％,13.8％ and 12.0％,respectively).Positive association rules were found in crab and shrimp,or milk and eggs.Single order association was found in female,while multi-order association was identified in male.Conclusions Our data show a strong positive association among animal foods.Female may be affected by milk,eggs and seafood,while male may be affected by a variety of foods.

OBJECTIVETo study the absorption kinetics of baicalin and baicalein in rats' stomachs and intestines.

METHODThe drug concentration by in situ perfusion in rats were determined by HPLC.

RESULTThe hourly absorption percentages of baicalin in stomach, small intestine and colon were 8.05%, - 0.94% and 2.32%, respectively, and baioalein with 34.53%, 30.61% and 4.89%, respectively. The absorption rate constants of baicalein were 0.090 7, 0.083 7, 0.076 6 and 0.048 3, respectively in duodenum, jejunum, ileum and colon.

CONCLUSIONBaicalin is moderately absorbed in stomach and poorly in small intestine and colon; Baicalein is well absorbed in stomach and small intestine but worse in colon, suggesting that the former is more suitable to be administered orally. The extensive absorption segments of bacailein suggests that it can be processed into a sustained-release preparation.

Animals ; Colon ; metabolism ; Duodenum ; metabolism ; Flavanones ; isolation & purification ; pharmacokinetics ; Flavonoids ; isolation & purification ; pharmacokinetics ; Ileum ; metabolism ; Intestinal Absorption ; Intestines ; metabolism ; Jejunum ; metabolism ; Male ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar ; Scutellaria ; chemistry ; Stomach ; metabolism

AIMTo develop a new synthetic route for olmesartan medoxomil.

METHODSOlmesartan medoxomil was prepared from ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate via hydrolysis and lactonization to afford 4,4- dimethyl-2-propyl-4,6-dihydrofuro [3,4-d]-1H-imidazole-6-one which was condensed with 2-(triphenylmethyl)-5-[4'-(bromomethylbiphenyl)-2-yl] tetrazole, followed by esterification with 4-chloromethyl-5-methyl-1,3-dioxol-2-one, and deprotection. The chemical structure of the major impurity in condensation reaction is the regio-isomer in the imidazole moiety, and confirmed by single crystal X-ray diffraction. The corresponding regio-isomer of olmesartan medoxomil was synthesized from the impurity by similar method. Optimization of the condensation conditions reduced the impurity to a negligible quantity.

RESULTSSynthesis of olmesartan medoxomil by the new route gave a product of 60% yield and above 99.0% purity. The content of olmesartan medoxomil regio-isomer was effectively controlled to less than 0.1%.

CONCLUSIONA novel synthetic route for olmesartan medoxomil was developed successfully. The olmesartan medoxomil regio-isomer is reported for the first time.

Angiotensin II Type 1 Receptor Blockers ; chemical synthesis ; chemistry ; Animals ; Antihypertensive Agents ; chemical synthesis ; chemistry ; pharmacology ; Blood Pressure ; drug effects ; Imidazoles ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; Olmesartan Medoxomil ; Rats ; Stereoisomerism ; Tetrazoles ; chemical synthesis ; chemistry ; pharmacology

Objective To study the proliferation of in vitro cultured mouse chondrocytes exposed to different doses of fluoride.Methods The third generation of primary cultured chondrocytes were exposed to the concentrations of 0,5,10,20,40 mg/L fluoride for 10 days to observe the morphological changes under light microscope and electron microscope to counter the numbers of ehondrocytes and proliferating rote with the growth curve and MTT.Results After exposed to fluoride for 10 days,the proliferation was present in the chondrocytes of the 5,10,20 mg/L groups,and shrinked chromatine and apoptosed ehondrocytes were seen in 40 mg/L group.The absorbance was not significantly different between all groups(F=2.313,P＞0.05);after exposed to fluoride for 48 and 72 hours,there was a significant difference of proliferating ability among 0 mg/L(the contr01)group[(23.5±4.6)%,(29.9±1.7)%],5 mg/L group[(34.6±4.7)%,(45.3±5.9)%],10 mg/L group[(39.9±4.8)%.(56.8±5.5)%],20 mg/L group[(31.8±4.1)%,(38.3±6.5)%]and 40 mg/L group[(28.3±4.3)%,(33.4±4.8)%](F=11.401,25.671,P＜0.05).There wss a significant difference compared with the control group(P＜0.05)with that of 5 and 10 mg/L groups higher than that of 40 mg/L groups(P＜0.05).Conclusions Lower doses of fluoride improve the proliferation of in vitro mouse chondrocyte in a short exposing time,higher doses result in the opposite.

AIMTo develop a fluorescence polarization-based high throughput screening and identify ligands for human Lectin-like oxidized low-density lipoprotein receptor-1 (hLOX-1).

METHODSSequential ultracentrifugation at 4 degrees C from normolipidemic fasting volunteers to obtain low density lipoprotein (LDL), which was modified by CuSO4 (5 micromol x L(-1)) at 37 degrees C for 24 h. The assay was based on the interaction between receptor and ligand, and hLOX-1 was labeled by FITC and bound to its specific ligand, oxLDL. Different reaction time and DMSO concentration were optimized to determine the stability and tolerance of fluorescence polarization (FP) assay. 3 200 compounds were screened in black 384-well microplate by FP-based competitive displacement assay, at excitation filter of 485 nm and emission filter of 530 nm. Z' was used to assess the assay quality.

RESULTSThe FP-based HTS was formatted in a 384-well microplate with a Z' factor of 0. 75, and three active compounds for hLOX-1 were identified with IC50 below 40 micromol x L(-1) from total 3 200 compounds.

CONCLUSIONThe results indicated that the fluorescence polarization assay is stable, sensitive, reproducible and well suited for high throughput screening efforts.

Binding, Competitive ; Drug Evaluation, Preclinical ; methods ; Fluorescence Polarization ; methods ; Humans ; Ligands ; Lipoproteins, LDL ; metabolism ; Scavenger Receptors, Class E ; metabolism

OBJECTIVETo present a new neurovascular island flap for fingertip reconstruction.

METHODSBased on the transverse palmar branch of the digital artery, this flap was designed on the volar side of a digit and reversed to repair the fingertip defects.

RESULTS12 fingers in 11 patients were reconstructed using this flap. Of them, 11 flaps survived and one necrosed. The contour of the reconstructed fingers looked well.

CONCLUSIONThis new neurovascular island flap provides excellent padding and sensation for fingertip reconstruction. The technique is simple.

Adolescent ; Adult ; Female ; Finger Injuries ; surgery ; Fingers ; blood supply ; surgery ; Humans ; Male ; Middle Aged ; Reconstructive Surgical Procedures ; methods ; Skin Transplantation ; Surgical Flaps ; blood supply ; Young Adult