OBJECTIVE:To optimize the preparation technology of Angelica sinensis powder and conduct screening for the op-timal particle size thereof. METHODS:With the contents of volatile oil and ferulic acid as the indexes,screening was conducted for the optimal drying temperature,dry welding time and particle size of the crude drug A. sinensis,and the stabilities of the A. si-nensis powder with different particle sizes which was packed by simulating that sold in the market were investigated. The verifica-tion tests on the preparation technology were conducted. RESULTS:The optimal conditions for preparing the crude drug A. sinensis were as follows as drying temperature of 60-70℃,drying for 4.5-5 hours and being crushed into moderate-sized powder;the stabil-ity of the moderate-sized powder which was packed by simulating that sold in the market was the best. In the verification tests on the preparation technology,the average content of the volatile oil was 0.46 ml/g,with RSD of 0.034%(n=3);the average con-tent of the ferulic acid was 0.123 μg/ml,with RSD of 0.026%(n=3). CONCLUSIONS:The optimized technology is stable and feasible,and the stability of the moderate-sized A. sinensis powder is the best.

In the previous study, a high-throughput screening method was established to find the antagonists of CD36. In the present study, a new compound named IMB-1680 was found using this method. The anti-atherosclerotic activities of IMB-1680 were then evaluated. Dose-dependent activities of IMB-1680 were detected by using Sf9 [hCD36] and CHO [hCD36] models. Fluorescence microscopic photography and flow cytometry were used to analyze uptake of mLDL. Foam cell test with RAW264.7 macrophages was used to examine lipid accumulation. The results showed that IMB-1680 inhibited CD36 activity with IC50 of 2.80 and 8.79 micromol x L(-1) in Sf9[hCD36] and CHO [hCD36] cells, respectively. Fluorescence microscopic photography and flow cytometry revealed that IMB-1680 could significantly reduce DiI-AcLDL uptake. Meanwhile, IMB-1680 also could reduce lipids accumulation in RAW264.7 macrophages. In all, the data indicated that IMB-1680 might be a potent effective anti-atherosclerotic leading compound.
Animals ; CD36 Antigens ; antagonists & inhibitors ; genetics ; metabolism ; CHO Cells ; Cells, Cultured ; Cricetulus ; Dose-Response Relationship, Drug ; Foam Cells ; cytology ; High-Throughput Screening Assays ; Humans ; Lipoproteins, LDL ; metabolism ; Macrophages ; cytology ; metabolism ; Mice ; Molecular Structure ; Plasmids ; Receptors, Scavenger ; antagonists & inhibitors ; Sf9 Cells ; Spodoptera ; Transfection

Coprinus comatus cultivated on cotton seed hull medium decomposed lignocellulose straggly and was high of absolute biological efficiency. Lignocellulose is the main carbon source for the fruiting stage of the fungus. There existed the positive correlation between the degradation rates of the cellulose and hemicellulose in the medium and the activities of extracellular CMCase (carboxymenthelcel lulase), FPase (filter paper cellulase) and HCase (hemicellu-lase), there also existed the positive correlation between the degradation rate of the lignin in the medium and the activity of extracellular laccase, but no correlation between the degradatio rate of the lignin in the medium and the activity of peroxidase. The activity of extracellular amylase was comparatively high at mycelial growth stage, and the protease activity peek was at teh time when the fruitbody matured.

To investigate the influence factors and effects of metal or dissolving microneedles on the formation and healing of skin microchannels, the pencil-shaped or conical stainless steel microneedles with different lengths, tip to tip space and base area, and the pencil-shaped dissolving microneedles with different tip to tip space were used. The microneedles were applied to the skin of epilatory mice and rats, and the effects of various microneedle parameters, application parameters, and animals on the microchannels were explored by the transepidermal water loss (TEWL) and methylene blue staining. Visually observe the skin local irritation caused by the microneedles. The animal experiments were approved by the Animal Experiments Welfare and Ethical Committee of Zhejiang University of Technology. The application time of the microneedle should be maintained at 30 s or more. When the insertion forces were 2, 4, 8 N, and the TEWL initial values of the formed microchannels were 12.9, 33.0, 40.4 g·m^-2·h^-1, respectively. When the length of metal microneedle were 400, 600, 800 μm, and the TEWL initial values of the formed microchannels were 37.1, 40.4, 49.5 g·m^-2·h^-1, respectively. When the tip to tip space of metal microneedle were 400, 600, 800 μm, and the TEWL initial values of the formed microchannels were 33.2, 40.4, 55.8 g·m^-2·h^-1, respectively. When the base area of metal microneedle were 0.16, 0.35, 0.62 cm², and the TEWL initial values of the formed microchannels were 35.1, 40.4, 67.1 g·m^-2·h^-1, respectively. The effects of conical and pencil-shaped microneedles are similar. When the tip to tip space of pencil shaped dissolving microneedle were 400, 600, 800 μm, and the TEWL initial values of the formed microchannels were 49.8, 60.5, 70.5 g·m^-2·h^-1, respectively. The TEWL baseline values of animal skins of different genders and series are different, but the tendency of microchannels formation and closure is similar. Visual inspection revealed that the slight erythema caused by the microneedles subsided within 24 h. Microneedles of different parameters have different effects on microchannels. The microchannels closed within 24 or 48 h, and the skin local irritation caused by microneedle was mild.

Objective To evaluate the efficacy and safety of infliximab plus methotrexate combination therpy in Chinese with rheumatoid arthritis patients.Methods This was a double-blind placebo-controlled phaseⅢclinical trial,173 patients who had active rheumatoid arthritis were randomised to placebo(n=86)or infliximab(n=87)group on a background of a stable dosage of methotrexate.Patients were assessed at weeks 0,2,6,14 and 18.Results At week 2,the American College of Rheumatology(20)response criteria,which represent a 20% improvement from baseline,the same results with swollen joint count,tender joint count,du- ration of morning stiffness,VAS score,CRP,ESR were achieved in 52.9% of patients,compared with 14.0% of patients receiving placebo plus methotrexate.A 20% improvement was achieved in 75.9% of infliximab plus methotrexate at week 18,compared with 48.8% of patients on placebo plus methotrexate(P=0.0003).A 50% improvement was achieved in 43.7% of infliximab plus methotrexate at week 18,compared with 25.6% of pa- tients on placebo plus methotrexate(P=0.011).Infliximab was well-tolerated;withdrawals for adverse events as well as the occurrence of serious adverse events or serious infections were similar to those in the placebo group.There was only one case of tuberculosis in the treatment group.Conclusion Treatment with infliximab plus methotrexate is more effective than methotrexate alone in patients with active rheumatoid arthritis.It has rapid onset of effect and the efficacy is persistent.

OBJECTIVETo study the effect of solid dispersion technology and inclusion technology on dissolution performance of Pulsatillae total saponins, and preliminarily investigate its mechanism.

METHODThe solid dispersion of Pulsatillae total saponins-PEG 4000 was prepared by the melting method. The inclusion compound of Pulsatillae total saponins-hydroxypropyl-beta-cyclodextrin ( HP-beta-CD) was prepared by the freeze-drying method. The properties of solid dispersion and inclusion compound were identified by using IR, DSC and NMR. And the dissolution of solid dispersion and inclusion compound were also determined by the small glass method.

RESULTIR, DSC and NMR results showed the formation of solid dispersion and inclusion compound. In terms of the dissolution, the inclusion compound ranked first, which was followed by solid dispersion and bulk pharmaceutical chemicals.

CONCLUSIONThe inclusion technology could significantly increase the dissolution of Pulsatillae total saponins, whereas the solid dispersion showed no notable solubilization effect.

Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Saponins ; chemistry ; Solubility ; Spectrophotometry, Infrared

Objective To explore the possible mechanisms of Galectin - 1(Gal - 1)protein in promoting the invasion and migration of gastric cancer cells. Methods After treated with different concentrations(0,1,5 μg/ mL)of Gal - 1 protein, the Trans - well model was used to analyze the invasion and migration ability of gastric cancer. WB and gelatin zymography method were used to detect the MMP - 9 expression and active form change in gastric cancer cells after Gal - 1 stimulate, in order to explore the possible molecular mechanisms of Gal - 1 protein in promoting the invasion and migration of gastric cancer cells. Results In cell migration assay,the number of gastric cancer cells BGC - 823 treated with 1and 5 μg/ mL Gal - 1 stimulate were 117 ± 8. 19 and 167 ± 7. 55,higher than that treated with 0 μg/ mL(P < 0. 05). The number of gastric cancer cells 7 901 treated with 1and 5 μg/ mL Gal - 1 stimulate were 151 ± 5. 13 and 190. 3 ± 6. 8,higher than that treated with 0 μg/ mL(P < 0. 05). In cell invasion assay,the number of gastric cancer cells BGC - 823 treated with 1and 5μg/ mL Gal - 1 stimulate were 51 ± 3. 6 and 76. 7 ± 9. 07,higher than that treated with 0 μg/ mL(P < 0. 05). The number of gastric cancer cells 7 901 treated with 1and 5 μg/ mL Gal - 1 stimulate were 74. 0 ± 7. 21 and 105. 3 ± 11. 37,higher than that treated with 0 μg/ mL(P < 0. 05). The migration and invasion level were significantly increased in gastric cancer cells after Gal - 1 stimulate. The MMP - 9 expression level and active form change in gastric cancer cells were also increased after Gal - 1 stimulate. Conclusion Gal - 1cound significantly promote gastric cancer cell migration and invasion by up - regulated the MMP - 9 expression and active its enzyme activity.

As a novel transdermal drug delivery technology of minimally invasive, safe and efficient, microneedles have received increasing attention. The microchannels formation by microneedles onto the skin is a prerequisite and key for microneedles to deliver drugs. However, there is still a lack of systematic evaluation in skin microchannels. This review summarized influencing factors and evaluation methods in microchannels formation and healing by microneedles, including geometric parameters, materials for preparation, drugs, penetration parameters, differences among the skin of subjects, and presence or absence of occlusion. This review provides reference for other scholars to further study the effectiveness and security of microneedle applications.

OBJECTIVETo detect central obesity and related adverse cardiovascular disease risk factors by waist-to-height ratio (WHR) among normal weight adults in Chongqing area.

METHODSA total of 20 000 participants aged 18 - 59 from one hour economic cycle of Chongqing area were selected by group sampling method. We measured the height, waist circumference (WC), body weight, blood pressure, blood lipid and blood sugar. Body Mass Index (BMI) and WHR were computed. We analyzed the differences of the correlated indexes between non-central obesity group (WHR < 0.5) and central obesity group (WHR ≥ 0.5) of those had normal weight (18.5 ≤ BMI (kg/m(2)) < 24). And we used logistic regression method to analyze the relation between central obesity and related adverse cardiovascular risk factors.

RESULTSAmong 11 612 normal weight subjects, 1801 (15.51%) participants were normal weight central obesity. Of non-central obesity group and central obesity group, the levels of waist WC were (73.71 ± 5.91) and (84.47 ± 4.58) cm (F = 328.74, P < 0.01); diastolic blood pressure levels were (72.85 ± 10.30) and (78.22 ± 11.90) mm Hg (1 mm Hg = 0.133 kPa, F = 23.62, P < 0.01); triglyceride levels were (1.22 ± 0.95), (1.97 ± 1.91) mmol/L (F = 114.70, P < 0.01); total cholesterol levels were (4.66 ± 0.84) and (5.04 ± 0.92) mmol/L (F = 13.10, P < 0.01); high density lipoprotein levels were (1.41 ± 0.31), (1.25 ± 0.29) mmol/L (F = 29.44, P < 0.01); low density lipoprotein levels were (2.65 ± 0.74) and (3.03 ± 0.77) mmol/L (F = 9.98, P < 0.01); glycemia levels were (4.94 ± 0.82) and (5.25 ± 1.37) mmol/L (F = 47.21, P < 0.01). The results of the logistic regression analysis showed the central obesity normal weight group was 1.28 (1.02 - 1.60), 1.49 (1.20 - 1.84), 2.24 (1.92 - 2.60), 1.77 (1.53 - 2.05), 1.58 (1.15 - 2.16) and 1.31 (1.06 - 1.63) times more likely than the normal group to have significantly elevated levels of systolic blood pressure, diastolic blood pressure, triglyceride, high density lipoprotein, low density lipoprotein and blood glucose.

CONCLUSIONWHR can effectively reflect the normal weight central obesity and the risk factors of cardiovascular disease;the adverse cardiovascular disease risk was high among normal weight central obesity adults.

Adolescent ; Adult ; Body Height ; Body Mass Index ; Body Weight ; Cardiovascular Diseases ; epidemiology ; China ; epidemiology ; Female ; Humans ; Male ; Middle Aged ; Obesity ; Obesity, Abdominal ; epidemiology ; Risk Factors ; Waist Circumference ; Young Adult

0.05) and the two methods had good correlation(r=0.822).CONCLUSIONS The method of FCST established by as in this study is simple,repeatable,with high accuracy and easy to determine MIC and has good application prospects in clinical antifungal susceptibility testing.