The in vitro antitumor activity of bakuchiol was exploited, compared with tamoxifen. The result of biological activities showed that bakuchiol could inhibit human breast cancer and the IC50 values were 2.89 x 10(-5) mol L(-1) and 8.29 x 10(-3) mol L(-1) against the cells line T-47D and MDA-MB-231 respectively. On the other hand, the key intermediate to synthesize bakuchiol was obtained by the method of Ireland-Claisen rearrangement. Comparing with traditional Claisen rearrangement, the reaction conditions are milder and the reaction reagents are safer.

Objective To establish chronic obstructive pulmonary disease(COPD)rat models,and to study the intervention of the formula of nourishing Qi,activating blood circulation and dispersing phlegm recipe on the morphology.Method To establish rat COPD models by intratracheal instillation of lipopolysaccharide and exposure to cigarette smoke.To instill intervention drug daily either the formula of nourishing Qi,activating blood circulation and dispersing phlegm recipe or the roxithromythin,starting on the 20th,30th and 40th day of the experiment respectively(the groups was named h 20,h 30,h 40,r 20, r 30 and r 40 for short),and to observe the effect on the morphology by means of collagen staining and image analyzer.Results The pathological changes and lung function in the model group were accorded with the human COPD.In drug intervention groups,airway inflammation and epithelial proliferation were alleviated to different degree compared to the model group.In model group,the collagen deposition was increased predominant type I collagen compared to the health comtrol group,and the deposition in the drug intervention groups were decreased compared to the model group,according to the Sirius redpolarizing microscopy morphometry method.The thickness of the airway wall in the model group was significantly increased compared to the health control group(P

Objective To explore the protective effects and mechanism of shenmaisanjie capsule(SMSJC) combined with methimazole on the L?thyroxine? induced hyperthyroid hepatic damage in rats. Methods so rats were divided into 5 groups randomly as normal group,model group,SMSJC group(0.48 g/kg),methimazole group (12 mg/kg)and combination group. With the exception of the normal group ,all rats were administered L?thyroxine (800 μg/kg ,ig) daily for 6 weeks. Rats were sacrificed. Blood and liver samples were collected for detecting thyroid and liver function , histological analysis and hepatic activity of SOD , GSH?Px and MDA content. Results The levels of T3,T4,FT3,FT4,ALT,AST,ALP,TBIL in serum and hepatic MDA content declined significantly. Hepatic activity of SOD ,GSH?Px increased obviously. Liver morphologic changes improved in methimazole group and combination group,whereas no significant difference of serum FT3,FT4,TSH level and liver activities of SOD and GSH?Px was noticed in SMSJC group in comparison to model group. Compared with SMSJC or methimazole mono?therapy ,the effect of combination therapy was obvious. However ,serum TRAb level was not significantly different in five groups of rats. Conclusion SMSJC combined with methimazole plays a protective role on hyperthyroidism hepatic damage induced by L?thyroxine in rat. It is proposed that the effect is association with inhibiting hepatic oxidative stress.

ObjectiveTo study the feasibility of ex vivo gene transfer to donor heart by delivering i ntracoronarily a reporter gene (Lac-Z gene) to donor heart at the time of trans plantation.MethodsThe model of heterotopic heart transplantation in murine was established and the method of perfusing intracoronarily was performed. Twelve male BALB/c mice were divided into 2 groups randomly: gene-transfer group (group 1) and control grou p (group 2). In group 1, plasmid vector (PSV-?-gal containing Lac-Z gene)/li posome (DOSPER) was perfused intracoronarily into each donor heart at the time o f transplantation. In group 2, normal saline was perfused. Donor hearts were har vested 3 days after transplantation. Freezing sections were made for detection o f the transfer and expression of Lac-Z gene by histochemical staining (X-gal). ResultsThe expression of Lac-Z gene was detected in the donor hearts of group 1. In tw o donor hearts, the expression of Lac-Z gene was detectable in the myocardial c ells in the mid-layer of ventriculus; In one donor heart the expression was fou nd in the myocardial cells under epicardium. But no expression of Lac-Z gene wa s detected in donor hearts of group 2.ConclusionEx vivo gene transfer intracoronarily to donor heart in the form of plasmid vector /liposome complex at the time of transplant ation is feasible.

Objective To explore the effect of celecoxib on proliferation and apoptosis of the glioma cells. Methods The glioma cell U251 was used and disposed with different densities of celecoxib (0 μmol/L, 10 μmol/L, 20 μmol/L, 40 μmol/L and 80 μmol/L) for 24 h, 48h and 72 h. The methyl thiazolyl tetrazolium (MTT) assay was used to detect the tumor cell proliferation and flow cytometry was used to detect the tumor cell apoptosis rate. Results The Glioma U251 cells proliferation were significantly decreased with the increase of density of celecoxib in vitro, and there was significant difference in the inhibited rate in different density and different time (P<0.05). The apoptosis rate was higher in the density of 80 μmol/L (17.86%) than in that of 0 μmol/L (11.23%) (P<0.05). Conclusion Celecoxib can inhabit the proliferation of glioma U251 cells, and promote the apoptosis especially with the density of 80 μmol/L.

Objective: The present study investigates the effects of Tanreqing injection, a compound Chinese herbal medicine, on the proliferation of leukemia cells in vitro and discusses the potential mechanisms. Methods: Tanreqing injection was diluted to a series of concentrations (1:2, 1:4, 1:8, 1:16, 1:32, 1:64, 1:128, 1:256 and 1:512) by volume and then independently applied to treat chronic myeloid leukemia K562 cells and T cell acute lymphocytic leukemia Molt4 cells at the proliferative stage. Cell growth was observed at different time intervals under a microscope. Cell proliferation was determined by cell counting kit-8 assay and the survival curve was delineated. The inhibitory rate and the half inhibitory concentration (IC50) were calculated. Molt4 cells were stained with propidium iodide (PI) and PI/Annexin V and then the cell cycle and apoptosis were analyzed by using flow cytometry. In addition, a real-time quantitative polymerase chain reaction was subjected to detect the expressions of apoptosis-related genes (bcl-2 and caspase-3) after Tanreqing treatment. Results: Tanreqing injection had inhibitory effects on the proliferation of K562 cells and Molt4 cells. The most toxic concentrations were observed between 1:2 and 1:16 where cells were almost necrotic. The inhibitory effect manifested in a concentration- and time-dependent manner. The IC50 of K562 and Molt4 was 1:333 and 1:142, respectively. After 1:32 Tanreqing injection treatment for 72 h, the number of Molt4 cells in the S phase significantly decreased (P<0.05), and the apoptosis rate markedly increased (P<0.05). In addition, increased caspase-3 expression and decreased bcl-2 expression were also observed (P<0.05). Conclusion: Tanreqing injection can both inhibit the proliferation and promote the apoptosis of leukemia cells in vitro, whereby the potential mechanism seems to be mediated in part by decreasing S phase ratio, down-regulating bcl-2 expression and up-regulating caspase-3 expression.

Objective To examine whether tissue inhibitor of metalloproteinases-1 (TIMP-1) is involved in arterial calcification of chronic renal failure (CRF) rats. Methods CRF model was induced in male Wistar rats by garage daily with 2% adenine 250 mg/kg. The calcification of aorta, femoral artery, renal artery and coronary artery was evaluated histomorphometrically by van Kossa-stained sections at 2-, 4-, 6- and 8-week respectively. RT-PCR and Western blot were used to observe the expressive levels of TIMP-1 mRNA and protein. Expressions of TIMP-1, osteopentin (OPN) and core binding factor α1 (Cbfα-1) protein were analyzed by immunhistochemistry. Results Serum urea nitrogen, creatinine, inorganic phosphate, calcium-phosphorus product and intact parathyroid hormone (iPTH) increased significantly in the model animals compared with control group after 2 weeks (P<0.01). Medial calcification was found in above four arteries of model groups after 6 weeks. RT-PCR and Western blot showed that TIMP-1 expression of model group was significantly higher than that of control group (P< 0.05), and obviously elevated in a time-dependent manner. The expression of TIMP-1 and OPN in calcified aortic smooth muscle cells increased obviously (P<0.05), and positive immunostaining of Cbfα-1 was found. The expression of TIMP-1 was positively correlated with OPN and Cbfα-1 (r=0.317, P=0.000; r=0.485, P=0.000). Conclusions The pathology of arterial calcification in CRF rats induced by adenine is similar to CRF patients, which may serve as a useful model of CRF with arterial calcification. The up-regulation of TIMP-1 seems to participate in the formation and development of vascular calcification in CRF.

BACKGROUND: The formation mechanism of biliary cast syndrome following liver transplantation has not been thoroughly illuminated, and it is unclear that whether some proteins correlated to the formation mechanism of biliary cast or prewarning to the formation of biliary cast.OBJECTIVE: To investigate the holoprotein expression in biliary cast syndrome patients following liver transplantation. METHODS: Four patients underwent liver transplantation at Liver Transplantation Institute, General Hospital of Chinese People's Armed Police Force. Three months later, 10 g biliary cast was harvested. Four kinds of biliary cast specimens at different colors and textures were preserved at deep hypothermia, followed by protein abstraction and restriction enzyme digestion, the total protein abstraction solution of biliary cast were analyzed by high definition mass spectrometry and query on MASCOT database. All protein name of biliary cast were list, the conjunct protein was found by comparing 4 specimens. RESULTS AND CONCLUSION: There were totally 208 proteins in 4 biliary cast specimens, 82, 44, 56 and 65, respectively. By comparison, 5 proteins were found to overlay in 2 biliary cast specimens, 7 proteins in 3 specimens and 13 proteins in 4 specimens. Among the latter 13 proteins, 5 unnamed-proteins, as well as 8 named-proteins (termed alpha-fibrinogen precursor, beta-fibrinogen precursor, fibrinogen gamma chain, proapolipoprotein, Chain A of Human Cathepsin G, S100 calcium-binding protein A9, lactoferrin) were included. The proteins exists in biliary cast, the common proteins of 4 biliary cast specimens imply a correlation between the formation of biliary cast and the exudative inflammation following the damage of biliary tract epithelium; Some proteins might be considered as a marker of prewarning the presence of biliary cast syndrome, judging the inflammation severity following the damage of biliary tract epithelium and the prognosis of biliary cast syndrome.

Objective To compare the effects,stress reaction and concentration of ropivacaine in umbilical cord blood of patients who accepted combined spinal epidural analgesia or patient controlled epidural labor analgesia in latent and active phase.Methods After approved by the ethics committee and informed consents from 80 nulliparous parturients who were admitted to Beijing Friendship Hospital,Capital University of Medical Sciences between January to June 2009,and who were term,single,cephalic presentation delivery and ASA Ⅰ-Ⅱ,were divided into two groups randomly:latent phase group (Group L,cervical dilation 0.5-2.5 cm,n=40) and active phase group (Group A,cervical dilation ≥3.0 cm,n =40).Ropivacaine 2 mg and fentanyl 10 μg was administered in subarachnoid space of all patients.Then,patient controlled epidural infusion of 0.1 ％ ropivacaine plus fentanyl 2 μg/ml were administered.Pain scores (visual analogue score,VAS),lower extremity muscle strength,duration of labor,delivery mode,total dosage used,maternal satisfaction,Apgar score (1 min and 5 min) were evaluated; concentration of ropivacaine (high performance liquid chromategraphy) in cord blood,and concentration of cortisol (radioimmunoassay) in maternal venous blood and cord blood were detected.Forty nulliparous parturients without labor analgesia were taken as control group (Group C).Chi-square test and one way analysis of variance was applied for statistical analysis.Results (1) VAS in Group L and Group A were lower than that of Group C when cervix dilated at 7.0-8.0 cm (2.9± 1.4,2.6± 1.5 vs 9.2±0.7,F=201.50,P＜0.01) and fully dilated (4.7±2.2,3.6±2.0 vs 9.1±0.7,F =-62.07,P＜0.01,respectively).(2) Tbe concentration of cortisol in maternal venous blood right after delivery was higher than that before analgesia in all groups,and the change in group C was significantly greater than that in group L and group A [(902±172) μg/L vs (761±125) μg/L and (731±184) μg/L,t =-3.491 and-3.483,all P＜0.01],moreover there was no significant difference between group L and group A (P＞0.05).There were no difference in cortisol concentration of umbilical blood among the three groups [(168±46) μg/L,(159±49) μg/L and (170±86) μg/L,F=0.23,P＞0.05].(3) There was no difference between ropivacaine concentration in umbilical blood of group L and group A [(0.21±0.10) mg/L vs (0.20±0.03) mg/L,t=0.557,P＞0.05].(4) No significant differences was shown among the three groups in the duration of first and second stage of labor,rate of augmentation,neonatal birth weight,Apgar score at 1 min and 5 min (all P＞0.05).Compared with group C,group L and group A had higher rate of vaginal delivery (52.5％ vs 75.0％ and 85.0％,P＜0.05) and lower rate of cesarean section (45.0％ vs 20.0％ and 15.0％,P＜0.05).The duration of analgesia in group L was longer than that in group A [(215±143) min vs (118±50) min,t =3.722,P＜0.01] and the dosage of fentanyl was also higher [(28± 11) μg vs (17±6) μg,t =5.084,P＜0.01].Conclusions Labor analgesia with combined spinal epidural could decrease cesarean section rate and maternal stress reaction without prolonging the duration of labor and inhibiting neonatal stress reaction.Labor analgesia start from latent phase would not increase the concentration of ropivacaine in cord blood.

The intra-tumor MTX concentration was measured in 12 patients with cerebral gliomas and 31 patients of malignant gliomas were treated with intracarotid infusion of papaverine and bis-chloroaitrosourea (BCNU). After intracarotid infusion of papaverine to open up the blood-brain-barrier (BBB), the MTX concentration within tumor tissues was 1854? 512ng/gram, which higher than that without papaverine infusion, which was 1020? 512ng/gram. The diagnosis was glioblastoma in 21 patients and anaplastic astrocytoma in 10. They received the infusion for a mean of 2.1 times with 250mg BCNU each. The mean survival time was 101.6? 32.7 weeks, with 104 weeks of median survival time. Fourteen were still living, including 11 glioblastoma and 3 anaplastic astrocytoma. Of those, four have lived over three years. We considered combination of papaverine and BCNU infusion for chemotherapy of malignant cerebral glioma is simple, safe and effective, so long as tumors were susceptible to the chemotherapeutic drugs.