China ; Coltivirus ; Encephalitis, Tick-Borne ; virology ; Humans

Objective To evaluate the efficacy and adverse effects of gefitinib in the treatment of fe- male patients with advanced adenocarcinoma of lung who had failed to previous chemotherapy.Methods These patients received 250mg of gefitinib orally,once daily until disease progression or development of intol- erable toxic reaction.They were evaluated one month after treatment and every other month thereafter.Results Among the 27 evaluable patients,there were 1 CR(3.7%),11 PR(40.8%),10 SD(37.0%)and 5 PD(18.5%). The overall response rate was 44.5%(95% CI 29%～68%);and 22 patients(81.5%)gained profit(CR+PR+ SD)from the clinical therapy(95% CI 62%～94%);the mean TTP was 7.2 months.Symptomatic improvement rate was 80.0%.The main adverse effects were mild rash and diarrhea.Conclusion gefitinib has significant efficacy in the treatment of female patients with advanced tung cancer who had failed to previous chemother- apy.Adverse effects are mild.gefitinib is a suitable therapy for these patients.

Objective To study the COLIXA3 gene polymorphism of patients with fluorosis and to explore the pathogenesis of COLIXA3 gene in endemic fluorosis.Methods Fifty one cases of patients with drinking-water borne fluorosis were selected as the case group in Xinzhou city,Shanxi province and 28 cases of healthy people were as the control group.Dental fluorosis was detected by Dean method and skeletal fluorosis was examined by X-ray.COLIXA3 of exon 5 gene product of 103 points was amplified by PCR and the gene locus genotype was sequenced.Results Ten cases of mild dental fluorosis,14 cases of moderate dental fluorosis,15 cases of severe dental fluorosis were detected among the 51 patients.The control group was free of dental fluorosis.All the 51 cases of patients with fluorosis had varying degrees of skeletal fluorosis,mainly osteosclerosis lesions,accounting for 86.27％(44/51 ),and mild skeletal fluorosis patients were all osteosclerosis lesions,and osteosclerosis lesions and multiple skeletal lesions were found among moderate and severe skeletal fluorosis patients in the case group,while control group had no skeletal fluorosis.The differences between genotypes of frequency distribution of AA,Aa,aa of COLIXA3 of case and control groups were not statistically significant [96.08％(49/51 ),3.92％(2/51 ),0.00％(0/51) and 96.43％(27/28),3.57％(1/28),0.00％(0/28),x2 =0.94,P ＞ 0.05].ConclusionsCOLIXA3 gene polymorphism is not significantly correlated to fluorosis.

OBJECTIVETo study the technological parameters of the purification process for effective part from Polygonum cuspidatum.

METHODUsing adsorption capacities and desorption rates of polydatin, resveratrol,emodin,physcion and total anthraquinone as the primary screening indexes, six resins were surveyed,and the optimized conditions of adsorption and desorption of the effective ingredients were studied.

RESULTResin D101 gave good separation performance and was selected to purify the effective part in Polygonum cuspidatum. The optimum parameters were established as the following: 1 BV (bed volume) sample extract was passed through the column with a flow rate of 2.4 BV x h(-1), 30 min later,the column was washed with 2 BV water, 2 BV 20% ethanol, 5 BV 50% ethanol, 2 BV 70% ethanol and 5 BV 95% ethanol, respectively. The combined 50% and 95% ethanolic elutes were concentrated to yield the purified effctive part.

CONCLUSIONThe purity of the total effective ingredients in the product was up to 36. 87%. Macroporous resin D101 could be well used in separating and purifying the effective part from Polygonum cuspidatum.

Adsorption ; Anthraquinones ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Emodin ; analogs & derivatives ; isolation & purification ; Fallopia japonica ; chemistry ; Glucosides ; isolation & purification ; Plants, Medicinal ; chemistry ; Resins, Synthetic ; chemistry ; Stilbenes ; isolation & purification ; Technology, Pharmaceutical ; methods ; Temperature

AIMTo study the effects of protease inhibitors on the large and small intestinal absorption of insulin in rats and to explore the mechanism of various protease inhibitors in different intestinal regions.

METHODSThe intestinal absorption of insulin was evaluated by its hypoglycemic effect and serum insulin level using an in situ loop method with the washing treatment.

RESULTSAdministration of insulin alone did not decrease the glucose level at either intestinal region with or without the washing treatment. With the unwashing treatment, there were no hypoglycemic effects in small intestinal loop when coadministration of insulin with protease inhibitors. With the washing treatment, the biological effects of insulin were amplified a little in small intestinal loop; obvious hypoglycemic effects were found in large intestinal loop with or without the washing treatment. The effectiveness of protease inhibitors was susceptible to their categories, concentrations and activities of proteolytic enzymes in different regions. The efficacy order of various protease inhibitors for enhancing hypoglycemic response of insulin was: leupeptin > sodium glycocholate > bacitracin > bestatin > cystatin; the percutaneous enhancement effects were observed in the presence of either sodium glycocholate or bacitracin.

CONCLUSIONCoadministration of protease inhibitors could increase the insulin efficacy more effectively in the large intestine than in the small intestine.

Animals ; Bacitracin ; pharmacology ; Biological Availability ; Blood Glucose ; metabolism ; Colon ; metabolism ; Glycocholic Acid ; pharmacology ; Insulin ; pharmacokinetics ; Intestinal Absorption ; drug effects ; Intestine, Small ; metabolism ; Leupeptins ; pharmacology ; Male ; Protease Inhibitors ; pharmacology ; Random Allocation ; Rats ; Rats, Wistar

AIM AND METHODSTo investigate the role of mitogen-activated protein kinase phosphatase-1 (MKP-1) in the regulation of cells proliferation, the expression of MKP-1 and extracellular signal-regulated kinase-1 (ERK-1) in heart and aorta of spontaneous hypertensive rat (SHR) and WKY were studied. We also investigated the effect of MKP-1 genes,which were transfected into vascular smooth muscle cells (VSMC) using the classical calcium phosphate coprecipitation technique, on the incorporation of 3H-TdR in VSMC stimulated by angiotensin II (Ang II).

RESULTS(1) Compared with that of WKY, MKP-1 expression in heart and aorta were significantly decreased by 53% (P < 0.01) and 45% (P < 0.01) in SHR, respectively. While the expression of ERK-1 in heart and aorta of SHR were higher than that of WKY (P < 0.01). The ratio of ERK-1/MKP-1 in heart and aorta of SHR were significantly higher than that of WKY. (2) 3H-TdR incorporation in VSMC stimulated by Ang II (10(-7) mol/L) was increased by 207% (P < 0.01), compared with control group. In the transfected cells with wild MKP-1 gene, Ang II-induced incorporation of 3H-TdR lowered 63%, compared with untransfected cells (P < 0.05). There were no marked inhibitive role between mutant MKP-1-transfected cells and blank vector-transfected cells in response to Ang II, compared with Ang II group (P > 0.05).

CONCLUSIONThese results showed that the expression of ERK-1 in heart and aorta isolated from SHR, which stimulated proliferation and hypertrophy of cells, is higher than that of MKP-1 which dephosphorylates and inactivated ERK-1. In addition, MKP-1 significantly inhibits Ang II-stimulated proliferation of VSMC.

Angiotensin II ; pharmacology ; Animals ; Aorta ; cytology ; enzymology ; Cell Proliferation ; Cells, Cultured ; Dual Specificity Phosphatase 1 ; metabolism ; Heart ; Hypertension ; metabolism ; Mitogen-Activated Protein Kinase 3 ; metabolism ; Muscle, Smooth, Vascular ; cytology ; Myocardium ; cytology ; enzymology ; Myocytes, Smooth Muscle ; drug effects ; metabolism ; Rats ; Rats, Inbred SHR ; Rats, Inbred WKY

To study the effects of surfactants on wettability of excipients, the contact angles of six types of surfactants on the surface of two common excipients and mixture of three surfactants with excipients were measured using hypsometry method. The results demonstrated that contact angle of water on the surface of excipients was associated with hydrophilcity of excipients. Contact angle was lowered with increase in hydrophilic groups of excipient molecules. The sequence of contact angle from small to large was starch < sodium benzoate < polyvinylpyrrolidone < sodium carboxymethylcellulose < sodium alginate < chitosan < hydroxypropyl methyl cellulose Chemistry, Pharmaceutical ; Excipients ; chemistry ; Hydrophobic and Hydrophilic Interactions ; Surface-Active Agents ; chemistry ; Tablets ; Water ; Wettability

In order to reveal the cause of disease occurred in the process of Coptis chinensis growth, this paper studied the bacterial species diversity index of different aged rhizospheric and non-rhizospheric soil planting normal or sick C. chinensis by using PCR-DGGE technique. The representative DGGE bands were chosen to be cloned, and sequenced, the phylogeny were constructed. The results showed that the bacterial communities were very different between the normal and diseased soil samples of C. chinensis, and the diversity index (H) of diseased soil samples were higher than that of normal soil samples. Sequencing analysis of representative cloned DGGE bands showed that the unculturable bacteria were the dominant groups, and bacteria belonged to genus Bacillus, Acidovorax, Acinetobacter, uncultured Kluyvera, and uncultured Comamonas were also existing, but the reported plant pathogenic bacteria were not found in the C. chinensis planting soil. The density and brightness of clone band d in diseased soil samples was higher than that in normal soil sample, and sequencing analysis showed that it belonged to genus Acidovorax. Obviously, during the process of C. chinensis growth, the rhizospheric bacteria population changed, and the quantity of bacteria belong Acidovorax increased, which probably resulted in the disease occurred during C. chinensis growth.
Bacteria ; classification ; genetics ; isolation & purification ; Biodiversity ; Coptis ; growth & development ; microbiology ; Denaturing Gradient Gel Electrophoresis ; Molecular Sequence Data ; Phylogeny ; Polymerase Chain Reaction ; Rhizosphere ; Soil Microbiology

Chest Pain ; etiology ; Coronary Vessel Anomalies ; complications ; diagnostic imaging ; Female ; Humans ; Middle Aged ; Tomography, X-Ray Computed

Self-microemulsifying drug delivery systems (SMEDDS) were developed to overcome the problems of delivery and administration of piroxicam, a drug with low bioavailability and gastrointestinal irritation, The in vitro properties of it were assessed. The solubility of piroxicam in several oils and surfactants was determined, and the compatibility of various oils and surfactants was investigated. Ternary phase diagrams were constructed to optimal area of microemulsion, and the influence of different oily phases, surfactants and co-surfactants was studied. The droplet size and dissolution of optimal formulation were determined to prove that the dosage form is a useful delivery system for piroxicam. In the optimized piroxicam SMEDDS, cinnamic alcohol was selected that gave the maximal solubility to piroxicam. Labrafil M 1944CS, Cremophor EL and Transcotol P were used as oils, surfactant and co-surfactant, respectively. Droplet size and distribution of three piroxicam SMEDDS formulations were (32.2 +/- 5.0), (40.1 +/- 6.4), (81.9 +/- 12.2) nm individually. And the releasing of piroxicam was rapid and complete. The optimized SMEDDS for piroxicam was obtained.
Administration, Oral ; Drug Compounding ; methods ; Drug Delivery Systems ; Emulsions ; Glycerides ; chemistry ; Glycerol ; analogs & derivatives ; chemistry ; Particle Size ; Piroxicam ; chemistry ; Polyethylene Glycols ; chemistry ; Propanols ; chemistry ; Solubility ; Solvents ; chemistry ; Surface-Active Agents ; chemistry