Objective To study effects of raloxifene (RLX) with different doses of conjugated equine estrogen(CEE) on prothrombotic profiles in the ovariectomized rats model.Methods Total of 32healthy female SD rats at age of 9 to 10 months were equally divided into every 8 rats at 4 groups randomly.One week after ovariectomized,they were treated by drugs,including control group with placebo(0.9％ Nacl intragastric administration),RLX group with RLX 6 mg/(kg · d),RLX and low CEE group with RLX 6 mg/(kg · d) + CEE 0.07 mg/(kg · d)and RLX and high CEE group with RLX 6 mg/(kg · d) + CEE 0.5mg/(kg· d)for 10 weeks before death.Thrombin turbidimetry method was used to evaluate the plasma fibrinogen(FIB),transmitting substrate method for antithrombin Ⅲ (AT Ⅲ) activity,double-antibody sandwich ELISA for plasminogen activator inhibitor 1 (PAI-1),D-dimer (D-D) and yon Willebrand factor (vWF) and nitrate reductase method for nitric oxide(NO).Results (1) Coagulation and anticoagulation indicators:it was observed (1.62 ± 0.22) g/L FIB at control group,(2.02 0.54) g/L at RLX group,(1.97 ±0.16) g/L at RLX and low CEE group,(2.00 0.18) g/L at RLX and high CEE group.There was a statistically significant difference between control group and any one of treatment groups(P ＜ 0.05) and no statistical significance among those three treatment groups (P ＞ 0.05).No significant change was observed in plasma AT Ⅲ activity among groups (P ＞ 0.05).(2) Fibrinolytic and anti-fibrinolytic indicators:it was observed (14.1 2.8) μg/L PAI-1 at control group,(20.0 ±3.3) μg/L at RLX group,(41.5 ±5.5) μg/L at RLX and low CEE group,(38.9 ± 6.0) μg/L at RLX and high CEE group.A remarkable increase was observed between control group and any one of treatment groups(P ＜0.05).But there was no significant difference of D-D among groups (P ＞ 0.05).(3) Endothelial function:it was (43 ± 7) ％ vWF at control group,(49±5)％ at RLX group,(46±6)％ at RLX and low CEE group,(36±5)％ at RLX and high CEE group.The vWF of RLX and high CEE group was the lowest among all groups (P ＜0.05).There was no difference of NO among groups (P ＞ 0.05).Conclusions In the different links of thrombosis,RLX gives different fuction and may increase the risk.CEE plays a synergism role in the matter of fibrinolysis and anti-fibrinolysis with RLX,further giving rise to thrombosis effect of RLX.And it also has a protective role in the function of vascular endothelium to some extent.But this only works with high dose.

Objective To observe the effects of menopause on prothrombotic profiles in ovariectomized rats .Methods Thirty two healthy female SD rats of 9 to 10 months were divided into 4 groups, the control shamed and the observation groups ovariectomized .Rats in the baseline group and the early menopause group were sacrificed one week later , and the control and late menopause group 10 weeks later.The prothrombotic profiles were detected including plasma FIB , ATⅢ activity, PAI-1 levels, D-D level, vWF levels and NO concentration, TXA2 and PGI2 levels.Results In early menopause, plasma FIB increased dramatically while ATⅢactivity remained lit-tle changed.PAI-1 demonstrated an increasing trend .vWF significantly increased but NO significantly decreased .In later menopausal stage, PAI-1 increased dramatically but FIB somewhat decreased .Plasma ATⅢactivity significantly increased and vWF still remained a high level.NO increased a little.In both early and later stage, TXA2 and PGI2 simultaneously increased while D -D showed little change between groups .Conclusion Menopause plays different roles in different aspects of thromoembolism , resulting in increased risk in early menopause due to prothrombotic state and decreased risk in later menopause when new balances between profiles were established .

Objective To explore the epidemiologic rule of main diseases demonstrated by uneven pulse. Methods With the method of literature analysis, we summarized and analyzed the literatures of the uneven pulse published in recent 20 between the uneven pulse and the palpitation, thoracic stuffiness, hypodynamia, dizziness, and abdominal distension. Conclusion Uneven pulse demonstrates many diseases besides blood stasis syndrome, thus we should determine the disease combined with other clinical symptoms for consideration, but uneven pulse alone.

With the development of natural products, the research activities on the solubilization methods of water-insoluble natural products have been carried out worldwide. Big molecular weight and poor solubility of most natural active ingredients lead to a very poor oral absorption and low bioavailability, which has extremely limited their development in pharmaceutical fields and clinical application. As a result, it is necessary to find out a suitable technique to improve the solubility and enhance the oral bioavailability of insoluble natural drugs. Based on the related references published in these years, this review introduced some new techniques to improve the solubility and bioavailability of natural drugs, including prodrugs, inclusion complex, solid dispersion, cocrystals, osmotic pump, liquisolid compacts, micronization, self-microemulsifying, nanosuspensions, lipsomes, polymeric micelles and so on, and summarized the theory, characteristics, application range, application examples, problems and development direction of each technique.
Administration, Oral ; Biological Availability ; Biological Products ; administration & dosage ; chemistry ; pharmacokinetics ; Chemistry, Pharmaceutical ; methods ; trends ; Solubility ; Technology, Pharmaceutical ; methods ; trends ; Water

Objective To investigate the inhibitory effect of melatonin on the proliferation activity of murine foregastic carcinomac ( MFC) cells via melatonin membrane receptors MT 2 and its relationship with the signaling pathways of mitogen-activated protein kinases ( MAPKs), phosphatidylinositol 3-kinase ( PI3K)-Akt.Methods Using siRNA technology to silence MT2 expression, we examined the ability of melatonin to inhibit the proliferation activity of MFC cells and its influence on the phosphorylation of ERK 1/2 and Akt.Results We found two interesting effects of SiRNA-mediated silencing of MT2 expression.Firstly, it significantly antagonized the inhibitory effect of melatonin on the proliferation activity of MFC cells .Secondly , it partially blocked the inhibitory effect of melatonin on the phosphorylation of ERK 1/2 and Akt.Conclusion Our results suggest that melatonin can inhibit the phosphorylation of ERK 1/2 and Akt via MT2 receptors , thereby inhibiting the proliferation of gastric cancer cells .

Objective To evaluate the etiologies of children with gastrointestinal bleeding(GIB), and the relationship between the pathological findings and clinical.Methods Gastroscopy or proctoscope was performed in 153 children with GIB. Pathological studies and tests as for helicobactor pylori (Hp) were undertaken.Results Among 153 children,140 cases(91.5 %) had definite diagnosis,including 74 children with upper gastrointestinal bleeding(UGIB) and 66 cases with lower gastrointestinal bleeding(LGIB). Gastric pathologic study was conducted in 56 cases. All patients had chronic superficial gastritis(CSFG). Hp test was positive in 33 patients. There was significant difference in the positive rate of Hp test between patients with gastritis or duodenitis and those with ulcers (P

Objective To study the inhibition effects of antibacterial proteins from Musca domestica larvae on JEC and A375 tumour cells. Methods Antibacterial proteins with concentrations of 0.02%,0.1%,0.5%,2.5% and 12.5% were supplied in the culture of JEC and A375 tumour cells in vitro.The cell cycles and apoptosis of JEC and A375 tumour cells were detected by flow cytometry,and the apoptosis index(AI) was measured.The morphology of apoptotic cells was observed with HE stainings and AO staining.The culture without antibacterial proteins was served as control. ResultsThe ratio of apoptosis index/proliferation index(AI/PI) of JEC cells increased with the concentration of antibacterial proteins.The PI and apoptosis rate of 2.5% antibacterial proteins group and 12.5% antibacterial proteins group significantly increased,and G0/G1 significantly decreased.For A375 cells,there were significant differences in G2/M, S,G0/G1,G2/M,AI/PI and PI between 12.5% antibacterial proteins group and control group(P

In the current study, nine flavonoids were isolated and purified from 75% ethanol extract of Selaginella uncinata (Desv.) Spring by column chromatographic techniques over macroporous resin, polyamide, silica gel, Sephadex LH-20 and pre-HPLC. On the basis of their physico-chemical properties and spectroscopic data analyses, these compounds were elucidated as cirsimarin (1), nepitrin (2), apigenin-6-C-α-L-arabinopyranosyl-8-C-β-D-glucopyranoside (3), apigenin-6-C-β-D-glucopyranosyl-8-C-α-L-arabinopyranoside (4), apigenin-7-O-β-D-glucopyranoside (5), 2,3-dihydroamentoflavone (6), 4'-O-methylamentoflavone (7), 2,3-dihydro-4'-O-methyl-amentoflavone (8), and 2,3,2",3"-tetrahydron-4'-O-methyl-robustaflavone (9). Compounds 1-5 belong to flavonoid glycosides and were isolated from the genus Selaginella for the first time.
Flavonoids ; analysis ; Selaginellaceae ; chemistry

Objective To build a Monte Carlo dose verification tool for IMRT Plan by implanting an irradiation source model into DPM code and to extend the ability of DPM to calculate any incident angles and irregular-inhomogeneous fields.Methods The virtual source and the energy spectrum unfolded from the accelerator measurement data were used,in combination with optimized intensity maps,to calculate the dose distribution of the irradiation irregular-inhomogeneous field.The irradiation source model of accelerator was substituted by a grid-based surface source.The contour and the intensity distribution of the surface source were optimized by IMRT.The dose calculation was realized by combining the position of the emitter with the fluence map from the IMRT plan.The weight of the emitter was decided by the grid intensity.The direction of the emitter was decided by the combination of the virtual source and the emitting position.The weighted fraction of the emitter was also combined with the flux grid intensity based on the particle transport model of DPM code.Results The accuracy of calculation was verified by comparing with the measured data.It was illustrated that the differences were acceptable (＜ 2％ inside the field,2-3 mm in the penumbra).The dose calculation of irregular field by DPM simulation was also compared with that of FSPB (Finite Size Pencil Beam).The passing rate of gamma analysis was 95.1％ for peripheral lung cancer.The regular field and the irregular rotational field were all within permissible range of error.The calculation time of regular fields were less than 2 h,and that of the test of peripheral lung cancer was 160 min.Conclusions The adapted DPM code with its simple irradiation source model is faster than that with classical Monte Carlo procedure.Its computational accuracy and speed satisfy the clinical requiremcnt,and it can be useful as a Monte Carlo dose verification tool for IMRT Plan.

Objective To evaluate the efficacy and safety of Qingpeng ointment in the treatment of eczema.Methods A multi-center,randomized,double-blind and placebo-controlled clinical trial was conducted.A total of 246 patients with eczema were randomly assigned with a ratio of 2∶1 to the treatment group and control group to topically apply Qingpeng ointment and placebo respectively twice daily for 3 weeks.Total symptom scores were calculated for the patients at the baseline,on week 1,2 and 3 during the treatment according to the individual scores for pruritus,lesions including erythema,papules,papulovesicles or vesicles,desquamation,crusting,infiltration and lichenification.The occurrence of adverse events was recorded.Results Totally,228 patients completed the trial,including 154 patients in the treatment group and 74 patients in the control group.After 3 weeks of treatment,a statistical difference was observed in the response rate (85.71％ vs.41.89％,Z=47.16,P＜ 0.01) and cure rate (31.82％ vs.12.16％,Z=12.30,P＜ 0.01) between the treatment and control group.There was no significant difference in the incidence of adverse events between the two groups (2.48％ vs.2.56％,x2 =0,P ＞ 0.05).Conclusion Qingpeng ointment displays a promising efficacy for the treatment of mild to moderate eczema with a rapid onset and high safety.