Drowning ; Humans ; Male ; Middle Aged ; Organothiophosphorus Compounds ; poisoning

Objective To prepare controlled release microspheres of vascular endothelial growth factor(VEGF)& calcium alginate and observe their effect on proliferation of human umbilical vein endo- thelial cells(HUVEC)in order to provide theoretical basis for controlled release of VEGF facilitating an- giogenesis of tissue engineering bone.Methods VEGF-calcium alginate microspheres were prepared by using the needle extrusion/external gelation method to investigate physicochemical character and in vitro release of VEGF.According to the different ingredients added into the culture medium,the seconda- ry cultured HUVEC were divided into four groups,ie,control group,microsphere group,VEGF group and VEGF-calcium alginate microsphere group,in which the proliferation of the cultured HUVEC was ob- served with cell counting method,MTT method and flow cytometry.Results The calcium alginate mi- crospheres were revealed as spherical shape and evenly distributed,with mean grain diameter of(560?50)?m,carrying capacity of 0.72 ng/mg and the encapsulation efficiency of 54%.Smooth controlled re- lease in VEGF-alginate microspheres lasted for more than 10 days.Proliferation of the cultured HUVEC was accelerated the most in VEGF group at the beginning but in EGF-calcium alginate microsphere group at midanaphase compared with other groups,with statistical difference(P＜0.05).There was no statis- tical difference upon cell counting,cell activity and time point of cell cycle between control group and mi- crosphere group.Conclusion VEGF-sodium alginate microapheres can continue activity of VEGF,re- lease VEGF for over 10 days and promote proliferation cultured HUVEC for a long time.

AIM:To observe the efficacy and safety of 1g/L bromfenac sodium hydrate ophthalmic solution in the partial substitution of glucocorticoid after laser subepithelial keratomileusis (LASEK).METHODS: Totally 104 cases (208 eyes) were received LASEK, which were selected and divided into study group and control group.The study group were adopted 1g/L bromfenac sodium hydrate ophthalmic solution combined with tobramycin dexamethasone eye drops and fluorometholone eye drops, the control group were adopted tobramycin dexamethasone eye drops and fluorometholone eye drops.The changes of visual acuity and intraocular pressure of two groups were recorded before and after surgery, and the score of painness and the occurrence of haze were observed after surgery.RESULTS: At postoperative 1, 2, 3d, respectively, the pain score of the study group were 1.70±0.35, 1.25±0.34, 0.82±0.32, the pain score of the control group were 2.30±0.43, 1.68±0.44, 1.12±0.33, the differences were significant (P<0.05).Before and at 2wk, 1, 3mo after surgery, respectively, uncorrected visual acuity of study group were 0.035±0.02, 0.71±0.13, 0.89±0.17, 0.88±0.18, while which of control group were 0.037±0.015, 0.73±0.15, 0.87±0.14, 0.86±0.15 (P>0.05), and the differences were not significant(P>0.05).At preoperative and postoperative 1, 2wk, 1 and 3mo of surgery, respectively, the intraocular pressure of study group were 17.33±1.58, 7.54±1.28, 7.23±1.58, 7.26±1.47, and 7.30±1.36 mmHg;the intraocular pressure of control group were 17.53±1.43,7.57±1.32,7.73±1.55,7.80±1.38,7.86±1.43 mmHg,the differences were not significant between before and at 2wk after surgery(P>0.05), the differences were significant between the two groups at 2wk, 1mo and 3mo (P<0.05).At postoperative 1, 3mo of surgery, the score of haze level of the study group were 91.7% and 93.3%, respectively and which in control group were 92.0% and 92.9%, respectively, and the differences were not significant between the two groups at every time point(P>0.05).CONCLUSION: It is safe and effective that 1g/L bromfenac sodium hydrate ophthalmic solution in the partial substitution of glucocorticoid after laser subepithelial keratomileusis.The patient has a lower intraocular pressure, has similar therapeutic effect as glucocorticoid in vision and antiinflammatory.

Background Excimer laser corneal refractive surgery is widely used because it reduces the dependency of refractive error eye to glasses.However,the adverse effects of anti-inflammatory drugs is a problem after operation.Lotemax eyedrops is a kind of steroidal anti-inflammatory drug,with a good effect on the operative eye.But its influence on intraocular pressure(IOP) after long-term topical administration is less studied.Objective This study was to investigate the influence of lotemax eyedrops on IOP after long-term topical administration in myopic eyes received excimer laser corneal refractive surgery.Methods An one-month retrospective case serial study was adopted.The case history data of 1552 eyes from 1552 Patients who received excimer laser corneal refractive surgery were collected in Tangshan Eye Hospital from 2011 January to 2012 January,including 321 eyes with laser in situ keratomileusis(LASIK),608 eyes with sub-Bowman keratomileusis (SBK) and 623 eyes with femtosecond laser for flap excimer laser in situ keratomileusis(FS-LASIK).Lotemax eyedrops was topically administered after operation 4 times per day initial and then decreased 1 time weekly for 1 month.IOP was measured in before,1 week,2 weeks,3 weeks,4 weeks after operation with non-contact tonometer.The increasing range of IOP was divided into ＜5 mmHg,5-15 mmHg and ＞ 15 mmHg after operation.Optical head parameters were measured by Heidelberg retina tomography when IOP increasing after operation.Results Within 1 month,elevated IOP was found in 47 of 1552 eyes after administration of lotemax eyedrops,including 3.12％ (10/321) in the LASIK group,3.29％ (20/608) in the SBK group and 2.73％ (17/623) in the FS-LASIK group,without significant difference among them(x2 =1.95,P＞0.05).The IOP elevated 1 week after operation and remained normal after that till drug withdrawal in all eyes.There were no significant differences in the disk area (1.65 ±0.44) mm2 vs.(1.66 ±0.44) mm2,disk volume (0.40 ±0.09)mm3 vs.(0.39±0.08) mm3 and mean nerve fiber layer thickness (0.28 ± 0.08) mm vs.(0.29 ± 0.07) mm in IOP elevation duration compared with 1 month after IOP recovery(t =0.34,0.81,0.48,P＞0.05).Conclusions Topical administration of 0.5％ lotemax eyedrops after excimer laser corneal refractive surgery leads to reversible high IOP.It is very important to monitor the IOP during use of the drug.

The purity of 4,4′-dimethoxy-5,6,5′,6′-bis (methylenedioxy)-2′-morpholine methylenebiphenyl-2-methyl formate methanesulfonate (IMH), a new drug for fatty liver treatment, was determined through differential scanning calorimetry (DSC). Analysis of two-factor non repeatability method was performed in the investigation the effects of two factors (heating rate and sample weight) on purity determination. The DSC experimental parameters were optimized as follows: heating rate was 10 ℃·min^-1, temperature range was 150-300 ℃, sample weight was 2.0-4.1 mg, and N₂ flow rate was 80 mL·min^-1. The linear correlation coefficient (r) of this DSC method was 0.999 8. The RSD value (n = 6) of precision was 0.03%. The standard value and uncertainty of the purity results of the multiple batches of IMH drugs were (99.74 ± 0.29)%, (99.91 ± 0.28)%, (99.90 ± 0.28)%, and (99.81 ± 0.28)% with inclusion factor (K) of 2 and confidence probability (P) of 0.95. The results were basically consistent with the results of the mass balance method. The DSC mehod is a simple, rapid and accurate method, and provides a new reference method for determining the purity of IMH drugs, improves the accuracy and reliability of purity determination.

OBJECTIVETo investigate the pharmacokinetic interaction among three major bioactive compounds of Shengmai formula.

METHODSAfter oral administration of ginsenoside Rg(1), ginsenoside Rb(1) and schisandrin with the same dose(100 mg.kg(-1)) individually or in combination, rat serum samples were extracted, then these three compounds were determined by liquid chromatography-mass spectrometry(LC-MS). The pharmacokinetic parameters of three compounds in single or combination form were calculated by WinNonLinu6.0 using non-compartment model.

RESULTSCompared with single drug group, the peak concentration of ginsenoside Rg(1) in combined group increased from(0.476 ±0.238) μg.ml(-1) to (1.946 ±1.432) μg.ml(-1), AUC(0-∞) increased from(0.523 ±0.238) μg.h.ml(-1) to (1.908 ±1.319) μg.h.ml(-1), CL decreased from(226311 ± 96819) ml.h(-1).kg(-1) to(90650 ±73684) ml.h(-1).kg(-1) and Vd decreased from(317110 ±154009) ml.kg(-1) to(130967 ±78306) ml.kg(-1). While the pharmacokinetic parameters of ginsenoside Rb(1) and schisandrin showed no significant change.

CONCLUSIONCombined oral administration of three compounds of Shengmai formula can improve the bioavailability of ginsenoside RgRg(1), however it does not change the pharmacokinetic behavior of ginsenoside RbRg(1) and schisandrin.

Animals ; Biological Availability ; Chromatography, Liquid ; Cyclooctanes ; administration & dosage ; blood ; pharmacokinetics ; Drug Synergism ; Ginsenosides ; administration & dosage ; blood ; pharmacokinetics ; Lignans ; administration & dosage ; blood ; pharmacokinetics ; Male ; Polycyclic Compounds ; administration & dosage ; blood ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry

To study the chemical constituents of the 95% ethanol extract of Psidium guajava. Compounds were separated by using a combination of various chromatographic methods including silica gel, D101 macroporous resin, ODS, Sephadex LH-20 and preparative HPLC. Their structures were elucidated by physicochemical properties and spectral data Eighteen compounds were isolated and identified as (+) -globulol (1), clovane-2beta, 9alpha-diol (2), 2beta-acetoxyclovan-9alpha-ol (3), (+) -caryolane-1 ,9beta-diol (4), ent-T-muurolol (5), clov-2-ene-9alpha-ol (6), isophytol (7), tamarixetin (8), gossypetin (9), quercetin (10), kaempferol (11), guajaverin (12), avicularin (13), chrysin 6-C-glucoside (14), 3'-O-methyl-3, 4-methylenedioxyellagic acid 4'-O-beta-D-glucopyranoside (15), p-hydroxy-benzoic acid (16), guavinoside A (17) and guavinoside B (18). Compounds 2-9 and 14-16 were isolated from this plant for the first time. The ethanol extract showed 61.3% inhibition against the proliferation of colon cancer cell line SW480.
Drugs, Chinese Herbal ; chemistry ; Organic Chemicals ; analysis ; Plant Leaves ; chemistry ; Psidium ; chemistry

OBJECTIVETo observe the anti-tumor recurrent and metastatic efficacy of Ru'ai Shuhou Recipe (RSR) on HER2 positive breast cancer, to evaluate the effects of RSR on the expressions of matrix metalloproteinases (MMPs) and the tissue inhibitor of metalloproteinases (TIMPs) in the recurrence and metastasis of HER2 positive breast cancer, thus revealing its anti-tumor recurrent and metastatic mechanisms.

METHODSSelected were 30-week-old HER2/neu transgenic spontaneous breast cancer mice FVB/neu. The primary tumor resection was carried out. After surgery they were randomly divided into the blank control group, the RSR group, the Herceptin group, and the combination group (RSR + Herceptin group). The treatment lasted for 4 months. The inhibition rate of the recurrent tumor volume and the inhibition rate of the lung metastasis were evaluated. The expressions of matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9), tissue inhibitor of metalloproteinase (TIMP-1), and TIMP-2 in the recurrent tumor tissue were detected using Western blot.

RESULTSBy the end of the treatment the average recurrent tumor volume was 11.11 +/- 8.71 cm3 in the blank control group and 5.56 +/- 5.55 cm3 of the RSR group, showing statistical difference between the two groups (P = 0.037). The average lung metastatic nodule was 16 in the blank control group and 10 in the RSR group. The inhibition rate of lung metastasis was 37. 85% in the RSR group, but with no statistical significance. The expression level of activated MMP-2 in the RSR group was down-regulated when compared with the blank control group, the Herceptin group, and the combination group (P < 0.05). The expression of MMP-9 of the RSR group, the Herceptin group, and the combination group was significantly down-regulated when compared with the blank control group (P < 0.05). The expression of MMP-9 of the RSR group and the combination group was further down-regulated when compared with the Herceptin group (P < 0.05). The expressions of both TIMP-1 and TIMP-2 of the RSR group, the Herceptin group, and the combination group were all up-regulated when compared with the blank control group (P < 0.05). The increased expression of TIMP-1 was more significantly in the RSR group and the combination group when compared with the Herceptin group (P < 0.05). It was higher in the combination group than in the RSR group (P < 0.05).

CONCLUSIONSRSR could inhibit the tumor recurrence of FVB/neu mice. It could reduce the degradation of extracellular matrix and increase the protective effects of extracellular matrix. It might achieve its anti-tumor effect through effecting the invasive and metastatic capabilities of breast tumor cells.

Animals ; Breast Neoplasms ; drug therapy ; metabolism ; pathology ; Drugs, Chinese Herbal ; pharmacology ; Female ; Matrix Metalloproteinase 2 ; metabolism ; Matrix Metalloproteinase 9 ; metabolism ; Mice ; Neoplasm Metastasis ; Neoplasm Recurrence, Local ; Phytotherapy ; Postoperative Period ; Receptor, ErbB-2 ; metabolism ; Tissue Inhibitor of Metalloproteinase-1 ; metabolism ; Tissue Inhibitor of Metalloproteinase-2 ; metabolism

A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Berberine ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Cell Cycle ; drug effects ; Cell Proliferation ; drug effects ; DNA Topoisomerases, Type I ; metabolism ; Doxorubicin ; pharmacology ; Drug Resistance, Neoplasm ; Hep G2 Cells ; Humans ; MCF-7 Cells ; Molecular Structure ; Structure-Activity Relationship

Aim To clone apoptosis-related genes from human MCF-7 breast cancer cells and to analyze the character of the method used in the process. Methods A poptotic cell model of MCF-7 cells was established with the apoptotic tumor cells induced by the all-trans-retinoic acid. The apoptotic gene was cloned from the model by improved PCR-based subtractive hybridization. Results 5 clones were identified to be related to apoptosis by reverse dot blot, 4 of them were known genes, and 3 were related to apoptosis. A novel gene， named apmcf-1, coded for 47 amino acid was identified. This gene was accepted by Genbank, the accession number was AF141882. Conclusion This improved PCR-based subtractive hybridization may be an efficient way in cloning differential expression gene.