To enhance the quality and efficiency of ozagrel by investigating the differences between the ozagrel polymorphs in bioavailability. Solid ozagrel in different polymorph forms were orally administered to SD rats. An HPLC method was established to determinate plasma level of ozagrel. The bioavailabilities of two polymorph forms were calculated and compared. The pharmacokinetic parameters of ozagrel, were as follows: Cmax was 32.72 ± 17.04 and 34.01 ± 19.13 mg · L(-1), respectively; AUC0-t was 61.14 ± 14.76 and 85.56 ± 18.08 mg · L(-1) · h, respectively; t½ was 1.53 ± 0.51 and 4.73 ± 3.00 h, respectively. There was no significant difference in pharmacokinetic parameters between form I and II polymorphs of ozagrel while the t½ of form II is longer, which indicates that the use of form II polymorph as pharmaceutical product may prolong the effective action time in clinics. This would help the polymorph quality control in drug production.
Animals ; Biological Availability ; Chromatography, High Pressure Liquid ; Methacrylates ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

AIMTo study the antitumor effect of baicalein on human leukemia K562 cell and its mechanism.

METHODSThe IC50 value and cytotoxity of K562 cell were detected by MTT method. The apoptotic cell was analyzed by FCM using Annexin V FITC--PI staining method. Sub-G1 peak was also measured by FCM. Protein expressions of Bcl-2, Fas, Caspase 3 were evaluated with FCM.

RESULTSBaicalein was shown to significantly inhibit the proliferation of K562 cell in a dose-dependent manner and selectively induce apoptosis of human leukemia K562 cells. Flow cytometric analysis showed that baicalein arrested K562 cells in the S phase. In addition, protein expression of Fas, Caspase 3 of K562 cells increased after exposure to baicalein, but Bcl-2 was unchanged.

CONCLUSIONBaicalein can selectively induce apoptosis of human leukemia K562 cell dose and time dependently through up-regulation of caspase-3 and fas gene expression level.

Antineoplastic Agents, Phytogenic ; pharmacology ; Apoptosis ; drug effects ; Caspase 3 ; Caspases ; metabolism ; Cell Cycle ; drug effects ; Flavanones ; Flavonoids ; pharmacology ; Humans ; K562 Cells ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Up-Regulation

OBJECTIVETo retrospectively analyze the effects of different chemotherapy regimens for concurrent chemoradiation on locally advanced non-small cell lung cancer (NSCLC).

METHODSThe data from 106 patients diagnosed as locally advanced NSCLC (IIIa: 29, IIIb: 77), who received various chemotherapy regimens for concurrent chemoradiotherapy, were retrospectively analyzed. Paclitaxel-based chemotherapy regimen was administered in 55 patients, topotecan regimen in 21 patients, PE (cisplatin and etopside) regimen in 26 patients, and other regimens in the remaining 4 patients. The effect of different chemotherapy regimens on overall survival and toxicity was analyzed.

RESULTSThe median survival time was 18.6 months, and the overall 1- and 3-year survival rates were 72.2% and 27.5%, respectively. The median survival time of 102 patients treated with paclitaxel-containing, topotecan-containing or PE regimens was 16.3, 27.3 and 29.1 months, respectively. The overall survival times of topotecan and PE groups were superior to that of paclitaxol-based group, but not significantly different (P = 0.32). Both univariate and multivariate analysis showed that paclitaxol-based chemotherapy regimen was significantly associated with a poorer survival (P < 0.05). N stage was another significant prognostic factor determined by COX multivariate regression model. Compared with the other regimens (10.6%), paclitaxel-based regimen (27.3%) had more acute radiation pneumonitis (grade >or= 2, P = 0.03), but no significant differences were observed in blood toxicity and esophagitis.

CONCLUSIONThere is a correlation between different chemotherapy regimens for concurrent chemoradiotherapy and the overall survival and acute radiation pneumonitis in patients with locally advanced NSCLC.

Adult ; Aged ; Antineoplastic Agents ; therapeutic use ; Antineoplastic Agents, Phytogenic ; therapeutic use ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Carcinoma, Non-Small-Cell Lung ; drug therapy ; pathology ; radiotherapy ; Cisplatin ; therapeutic use ; Combined Modality Therapy ; Etoposide ; therapeutic use ; Female ; Follow-Up Studies ; Humans ; Lung Neoplasms ; drug therapy ; pathology ; radiotherapy ; Male ; Middle Aged ; Neoplasm Recurrence, Local ; Neoplasm Staging ; Paclitaxel ; therapeutic use ; Proportional Hazards Models ; Radiation Pneumonitis ; etiology ; Radiotherapy, Conformal ; Retrospective Studies ; Survival Rate ; Topotecan ; therapeutic use

Adult ; Balloon Occlusion ; instrumentation ; Cardiac Catheterization ; methods ; Coronary Angiography ; Coronary Vessel Anomalies ; therapy ; Female ; Humans ; Vascular Fistula ; therapy

OBJECTIVETo study gene expression of collagen types IX and X in human lumbar intervertebral discs during aging and degeneration and to explore the role of collagen types IX and X in disc degeneration.

METHODSFetal, adult and pathologic specimens were subjected to in situ hybridization with cDNA probes to investigate mRNA-expressions of types IX and X collagen gene.

RESULTSIn fetal intervertebral discs, positive mRNA hybridization signals of type IX collagen were concentrated in the nucleus pulposus and the inner layer of anulus fibrosus. Interstitial matrix of the nucleus pulposus also showed positive type X collagen staining. Positive mRNA hybridization signals of types IX and X were not detected in the middle and outer layers of anulus fibrosus. In adult specimens, expression of type IX collagen mRNA was markedly decreased. No hybridization signals of type X collagen was observed. As for pathological specimens, there was no gene expression of type IX collagen. In severe degenerated discs from adults, there were focal positive expressions of type X collagen.

CONCLUSIONSObvious changes of collagen gene expression occur with aging. Expression of type IX collagen decreases in adult and pathological discs. Results of type X collagen expression suggest that type X collagen is expressed only in older adult and senile discs (i.e., when disc degeneration has already reached a terminal stage), indicating the terminal stage of degeneration.

Adolescent ; Adult ; Collagen Type IX ; metabolism ; Collagen Type X ; metabolism ; Female ; Gene Expression ; Humans ; Immunohistochemistry ; In Situ Hybridization ; Intervertebral Disc ; embryology ; metabolism ; Lumbar Vertebrae ; Male

OBJECTIVETo observe the characteristics of uterine contraction and stages of labor during delivery under continuous epidural block anesthesia.

METHODSTotaling 213 parturients in spontaneous labor under epidural block anesthesia with dilated cervical orifice of 3 cm were monitored for the contraction cycle, duration, intensity and curve types of uterine contraction, and recordings were made for 30 min before and 30, 60 and 120 min after the anesthesia took effect, respectively. The duration of the active phase in the first, second and third stages of labor was compared between 421 cases with anesthesia and 237 without anesthesia.

RESULTSSignificant difference was noted in the objective indexes of uterine contraction recorded after anesthesia had taken effect (P<0.05) in comparison with those before anesthesia, suggesting significantly attenuated uterine contraction after anesthesia, whereas these indexes underwent no significant further variation as compared between different time points after anesthesia (P>0.05). The average active phase in the first stage was significantly shorter in anesthesia group than that in the control group (P<0.05), but the average duration of the second and third stages of labor differed little between the two groups with appropriate use of oxytocin under strict monitoring (P>0.05). The rates of obstetric forceps utilization and use of oxytocin were higher in anesthesia group than in the control group (P<0.05).

CONCLUSIONEpidural block anesthesia produces certain influences on uterine contraction and stages of labor during delivery, for which appropriate treatment measures may prove beneficial.

Adult ; Anesthesia, Epidural ; methods ; Anesthesia, Obstetrical ; methods ; Female ; Humans ; Labor, Obstetric ; physiology ; Pregnancy ; Time Factors ; Uterine Contraction ; drug effects ; Uterus ; drug effects ; physiology

OBJECTIVETo carry out the citation analysis of publications in Chinese Journal of Preventive Medicine (CJPM) among the preventive medicine authors and analyze the impact of this magazine in preventive medicine domain.

METHODSUsing Chinese scientific periodical literature evaluation and statistical analysis system (V1.0), the citation status of all CJPM publications in 2000-2005 was analyzed, the analysis covered 21 columns, including the review, editorial and original article, the data were collected up to November, 2007.

RESULTSFrom 2000 to 2005, CJPM had more than 30 columns and carried 1196 articles and 92. 89% (1111/1196) articles were from 21 main columns. During 2003 to 2005, the impact factors of CJPM were 0. 897, 1.011 and 0. 891 respectively. Among 21 main columns, the citation frequency of six columns including original article, editorial, review, courses, discussion and case report were higher than 80%. In five columns (original article, editorial, report, review and academic trends), the average citation frequency of individual articles was more than 4 times. The citation frequency of 20 authors was higher than 20 times and these authors were from medical schools, teaching hospitals, centers of diseases control and the research institutes. The individual citation frequency of 17 articles was more than 20 times and the individual citation frequency of three articles was more than 50 times. 34.9% of the citations of the 2000-2005 CJPM articles were from the top 20 journals, and the self-citation rate was 4. 85%.

CONCLUSIONThe publications in Chinese Journal of Preventive Medicine are most frequently cited, which indicated that those publications have high quality, this journal has a great effect in preventive medicine field of China.

Bibliometrics ; China ; Periodicals as Topic ; statistics & numerical data ; Preventive Medicine

AIMTo establish a sensitive and efficient reporter gene-based screening model for finding agonists of estrogen receptor beta subtype.

METHODSA recombinant vector pTAL-ERE-SEAP was constructed by inserting a synthetic sequence composed of five estrogen responsive elements in front of promoter of pTAL-SEAP vector. pTAL-ERE-SEAP was then transfected into human embryonic kidney (HEK293) cells. G418 (200 microg x mL(-1)) was added to select positive clones that can be induced by E2 to express reporter gene SEAP. The speciality was tested by several ligands of relative nuclear receptors of the same family. The stability of the model, the time-effect relationship, the dose-response relationship, and the immunocytochemistry staining of ERbeta expression after transfection were observed. 2 622 compounds were screened by using this model.

RESULTSStably transfected clones were obtained. The expression levels of reporter gene SEAP of positive clones was induced by E2 in a dose-response and time-effect relationship manners. The Z' factor value was 0.7. The expression levels of dexamethasone and other ligands were low. The result of immunocytochemistry staining showed the expression of ERbeta. E2 had no proliferating effects on stably transfected clones.

CONCLUSIONStably transfected positive clones transfected with recombinant vector pTAL-ERE-SEAP were obtained. The positive clones may be used to screen for agonists of estrogen receptor beta subtype by measurement of luminescent value of expressed SEAP in wells of microlitre plate.

Alkaline Phosphatase ; genetics ; metabolism ; Cell Line ; Estradiol ; pharmacology ; Estrogen Receptor beta ; agonists ; genetics ; metabolism ; Gene Expression Regulation ; drug effects ; Genetic Vectors ; Humans ; Immunohistochemistry ; Promoter Regions, Genetic ; genetics ; Recombinant Fusion Proteins ; genetics ; metabolism ; Response Elements ; genetics ; Transfection

Adult ; Dextrocardia ; surgery ; Ductus Arteriosus, Patent ; surgery ; Fluoroscopy ; Heart Septal Defects, Ventricular ; surgery ; Humans ; Male ; Surgical Instruments ; Vena Cava, Inferior ; abnormalities

BACKGROUNDThe methods for the treatment of postcatheterization femoral arteriovenous fistulas (AVF-s) - simple observation, ultrasound guided compression, covered stents implantation and coil embolization have poor outcome. Surgery is the standard method for treatment of femoral AVFs, but it is a traumatic operation. In this study, we report the results of the treatment of postcatheterization femoral AVFs by simple prolonged compressing bandage.

METHODSTo treat iatrogenic femoral AVFs caused by transfemoral catheterization, prolonged binding with elastic or common bandage was applied in 16 cases. Catheterization was performed in 7 cases for radiofrequency current catheter ablation, in 4 for occlusion of congenital heart disease, in 3 for percutaneous coronary intervention, in 1 for coronary angiography and in 1 for right heart catheterization.

RESULTSAll iatrogenic femoral AVFs were healed after simple binding with elastic or common bandage for 4 - 46 days (mean (15 +/- 10) days). During the period of binding, local skins ulceration occurred at puncture site in two cases and femoral vein thrombus was found in one patient. During 6 - 24 months (mean (11.8 +/- 3.6) months) followup with colour Doppler ultrasonography, no recurrent arteriovenous shunting or other complications were observed.

CONCLUSIONThe results suggest that simple prolonged bandaging for postcatheterization femoral AVFs is an effective and economical procedure.

Adolescent ; Adult ; Aged ; Arteriovenous Fistula ; etiology ; therapy ; Bandages ; Catheterization, Peripheral ; adverse effects ; Female ; Femoral Artery ; pathology ; Femoral Vein ; pathology ; Humans ; Male ; Middle Aged