OBJECTIVETo investigate the effect of component I from agkistrodon acutus venomon (AAVC-I) the migration of human umbilical vein endothelial cells (HUVECs), and to elucidate the possible anti-angiogenic mechanism of AAVC-I.

METHODSThe effect of AAVC-I on the migration of HUVECs which was cultivated in vitro and treated with AAVC-1 at four concentrations: 0, 20, 40, 80 microg/ml, was observed by methods of scratch wound-healing and Transwell assay. The expression level of mRNA and protein of P-selectin and intercellular cell adhension molecule-I (ICAM-1) were examined by RT-PCR and Western blot assay.

RESULTSCompared with the blank group, the migration ability of HUVECs in each AAVE-I treated group was reduced in a dose-dependent manner, and the expression level of the mRNA and protein of P-selectin and ICAM-1 were decreased.

CONCLUSIONAAVC-I inhibits the migration of endothelial cell, which is acted by down-regulation of the expression content of mRNA and protein of P-selectin and ICAM-1.

Cell Movement ; drug effects ; Cells, Cultured ; Crotalid Venoms ; pharmacology ; Down-Regulation ; Human Umbilical Vein Endothelial Cells ; drug effects ; Humans ; Intercellular Adhesion Molecule-1 ; metabolism ; P-Selectin ; metabolism ; RNA, Messenger

Objective To investigate the expression of CD133 and CD44 proteins in gastric stromal tumors (GST) and their clinical significances. Methods The expression of CD44 and CD133 proteins in the GST tissues of 112 patients was detected by immunohistochemical staining. The relation between the expression of CD44 and CD133 proteins and the clinicopathological characters was analyzed. The survival and prognosis of GST were also analyzed. Results Both CD44 and CD133 were expressed on the cell membranes. The expression rates of CD44 and CD133 were 58.04 % (65/112) and 42.86 % (48/112) separately; the co-expression rate of CD44 and CD133 was 27.68 % (31/112). CD44 and CD133 were negative in normal peritumoral tissues. No correlation was found between CD44 and CD133 and the clinicopathological parameters including gender, age and lymphatic vessel invasion (all P>0.05), but the expression levels of CD44 and CD133 in patients with the mitotic count ≥ 5/50 high-power field, large diameter and vascular invasion were significantly higher (all P<0.05). No correlation was found between co-expression of CD44 and CD133 and the clinical clinicopathological parameters including gender, age, the mitotic count ≥ 5/50 high-power field and vascular invasion (all P>0.05), but the co-expression level of CD44 and CD133 in patients with tumor diameter ≥5 cm was significantly higher than that in patients with tumor diameter < 5 cm (χ2=5.040, P=0.025). The overall survival rate of the patients with co-expression of CD44 and CD133 was shorter than that in other groups (χ2 = 8.758, P= 0.001). No correlation was found between CD44 and CD133 expression (r=0.126, P=0.210). Multivariate analysis with the Cox regression models showed that the tumor diameter ≥5 cm (P=0.042) and co-expression of CD44 and CD133 (P=0.003) were significantly associated with poor prognosis. Conclusion CD44 and CD133 as robust cancer stem cell markers in GST might be the prognostic factors.

Angiotensin II ; pharmacology ; Animals ; Heart Rate ; drug effects ; physiology ; Rabbits

Objective To explore the clinical feature,diagnosis and treatment of postoperative chylothorax after congenital cardiac surgery.Methods From Jan.2000 to Jan.2008,36 consecutive infants following cardiac surgery were diagnosed postoperative chylothorax.Age at operation ranged 6 days to 4 years.Weight ranged 3.5 kg to 17.0 kg.Indications for cardiac surgery were:tetralogy of Fallot 18 cases,complete atrioventricular septal defect 5 cases,double outlet of right ventricle 4 cases,complex heart defect for Fontan operation 4 cases,coarctation of the aorta 2 cases,total anomalous pulmonary venous drainage 2 cases,patent ductus arteriosus 1 case.Chylothorax occurred in right side was 32 cases,in left side 3 cases,bilateral side 1 case.Diagnostic time for chylothorax was postoperative 1-10 d.Results Thirty-four cases were treated conservatively with success(34/36,94.44%).Only 2 cases needed surgical treatment.The chest drainage volume before con-servative treatment was 22-60 mL/(kg?d)[mean 40.82 mL/(kg?d)].The mean duration of chylous drainage was 15 d(ranged 7 d to 42 d).There was no death in hospital.Two children had sepsis.The cases were followed up 2 weeks-7 years.One newborn was abandoned because of the other reason after discharge.There was no recurrence of chylothorax.Twenty-two cases were still in low-fat diet.Conclusions The chylothorax following operation of congenital heart disease should be noticed and early diagnosed.The initial treatment is conservative,but surgical treatment ought to be considered if the conservative management is unsuccessful.J Appl Clin Pediatr,2009,24(1):70-72

With the content of gallic acid, loganin, paeoniflorin and paeonol as the indexes, to screen out dissolution determination conditions, establish the dissolution determination method for multi-index components in Liuwei Dihuang concentrated pills, calculate and map the accumulative dissolution curve, and then compare the dissolution of products from different pharmaceutical factories through the similarity factor (f2). According to the results, the optimum dissolution determination conditions were the paddle method, with 250 mL 0.1 mol x L(-1) hydrochloric acid as the dissolution medium, and a rotation rate of 100 r x min(-1). The similarity factor values (f2) of the dissolution curves of the four main components of Liuwei Dihuang concentrated pills from different pharmaceutical factories were mostly less than 50. This demonstrated a significant difference in the dissolution of Liuwei Dihuang concentrated pills from different pharmaceutical factories, and provided scientific basis for improving the equality evaluation of Liuwei Dihuang concentrated pills.
Drugs, Chinese Herbal ; chemistry ; Humans ; Organic Chemicals ; analysis ; Quality Control ; Solvents ; chemistry

OBJECTIVETo observe the clinical effect and safety of blood activating stasis removing method (BASRM) on intracerebral hemorrhage patients.

METHODSA multi-center, prospective, randomized, open, controlled and blinded endpoint design was adopted. Totally 228 intracerebral hemorrhage patients were assigned to the treatment group and the control group, 114 in each group by center randomized method. All patients received basic treatment of Western internal medicine. Patients in the treatment group received intravenous infusion with Xingnaojing Injection (XI) from the 1st day of grouping, 20 mL per day for 14 days. Then they took or were nasally fed with Chinese medical granules (by syndrome typing as complicated with wind syndrome, fire syndrome, and phlegm syndrome) for 21 days. Finally they took Naoxueshu Oral Liquid (NOL), 10 mL each time, 3 times per day till the 3rd month of incidence. Patients' disability degree, activities of daily living, neurological impairment, the effective rate, physiologic functions, mental status, social relationship, and degree of treatment satisfaction were assessed using Modified Rankin Scale (MRS), Barthel index (BI), National Institute of Health Stroke Scale (NIHSS), and patient reported outcome (PRO). Head CT was performed to evaluate the absorption of hematoma at the 1st and 7th day of grouping. The safety was also assessed.

RESULTSTotally 108 patients in the treatment group and 112 patients in the control group completed the trial. There was no statistical difference in the total effective rate between the two groups after 3 months of treatment (P>0.05). The MRS score was obviously lower in the treatment group than in the control group (P<0.01) at month 3 after attack (P<0.01). There was statistical difference in the difference between pre-post hematoma volume between the two groups after 7-day treatment (P<0.05). The NIHSS score of two groups at the 7th, 14th, 21st day, and 3rd month decreased significantly (P<0.05). Compared with the control group, the decremenit of NIHSS score decreased more obviously in the treatment group at day 7, 21, and 3rd month (P<0.05). Compared with the control group, the BI increased (P<0.01); physiologic fupctions, social relationship, treatment satisfaction and total score in PRO scale were all lower in the treatment group than in the control group (P<0.05, P<0.01). The incidence of adverse events occurred in 7 cases (6.14%) in the treatment group and 5 cases (4.39%) in the control group, with no statistical difference (P>0.05).

CONCLUSIONBASRM could lower the deformity rate of intracerebral hemorrhage patients at month 3, effectively promote hematoma absorption within 7 days, improve neurologic impairment, and elevate living abilities at month 3 of onset.

Activities of Daily Living ; Cerebral Hemorrhage ; therapy ; Hematoma ; Humans ; Medicine, Chinese Traditional ; Prognosis ; Prospective Studies ; Syndrome

Objective: To establish capillary zone electrophoresis method for determination of sildenafil citrate (Viagra) content in its troche. Methods： Using tetrandrine as internal standard(IS), the electrophoretic separation was achieved with 25 mmol/L borate (pH=7.89) running buffer. And a voltage of 14 kV was applied to the 40 cm×75 μm(i.d) capillary. The analytes were introduced into capillary by siphon (1 s) and determined with on-column monitoring at 214 nm. Results：The determination could be completed within 4 min and the minimum concentration of detection was 5 μg/ml.The analytical results of sildenafil citrate samples demonstrated a good linear relationship within the range of 24-480 μg/ml.The relative standard deviations (RSD) of intra-day was less than 1.58% and that of inter-day was less than 2.46%.The present recoveries were between 95%-105％. Conclusion：The CZE method is accurate, simple, rapid and reliable, so it can be applied to the determination of sildenafil citrate content.

OBJECTIVETo investigate the status of Notch signaling pathway in small cell lung cancer (SCLC).

METHODSExpression plasmids of pEFBOS-NIC-MYC and pEFBOS-neo were transfected into NCI-H446 cells. Stably transfected cell lines were selected and their growth rates were examined by MTT method. Expression of downstream genes along the Notch signaling pathway were studied by RT-PCR. Protein expression of euroendocrine markers of CgA and NSE were detected by Western blot analysis and immunocytochemistry.

RESULTSThe expression of HES1 was increased in the pEFBOS-NIC-MYC group, but the expression of hASH in the pEFBOS-NIC-MYC group was decreased significantly. The transfected cells with pEFBOS-NIC-MYC plasmid showed a significantly slower growth rate compared with that of two control groups (P < 0.05, Student's t-test). Immunocytochemistry of NSE showed that PUs in the NIC transfected group, sham group and negative control group were 7.21 ± 0.59, 28.25 ± 1.46, 30.57 ± 1.31 respectively, the former one was smaller than the values of the latter two significantly (P < 0.01). Western blot analysis showed the grave scales of CgA in NIC transfected group and sham group to be 0.54 ± 0.03 and 0.99 ± 0.05 respectively (grave scales of the negative control was set as 1.00), the former one significantly smaller than that of the other two groups (P < 0.01). The grave scales of NSE in the NIC transfected group and sham group were 0.43 ± 0.02 and 1.07 ± 0.09 respectively (grave scales of the negative control was set as 1.00) and the former one was significantly smaller than the other two groups (P < 0.01).

CONCLUSIONNotch signaling pathway regulates SCLC cells through its inhibitory effect on hASH1 transcription via HES1 along with an expression inhibition of neuroendocrine markers in SCLC.

Basic Helix-Loop-Helix Transcription Factors ; metabolism ; Cell Line, Tumor ; Cell Proliferation ; Chromogranin A ; metabolism ; Homeodomain Proteins ; metabolism ; Humans ; Lung Neoplasms ; metabolism ; pathology ; Phosphopyruvate Hydratase ; metabolism ; Plasmids ; Receptor, Notch1 ; metabolism ; physiology ; Recombinant Proteins ; metabolism ; Signal Transduction ; Small Cell Lung Carcinoma ; metabolism ; pathology ; Transcription Factor HES-1 ; Transfection

AIMTo search for novel compounds with potent nNOS inhibitory activity for the treatment of Alzheimer's disease.

METHODSThe target compounds were obtained by introducing benzenealkyl groups into the structure of isothioureas. nNOS inhibitory activity assays were conducted for the target compounds.

RESULTSSixteen benzenealkyl isothiourea compounds (I1-16) were synthesized by three different synthetic methods from benzylamine (1) or (substituted) phenethylamine (2). Compounds I1-6 were synthesized from 1 or 2 by reaction with benzoyl isothiocyanate to form the corresponding benzoylthioureas 3 or 4, followed by hydrolysis with 10% sodium hydroxide solution, then S-alkylation with methyl iodide or ethyl iodide. I7-14 were synthesized from 1 or 2 by reaction with methyl isothiocyanate to form the corresponding 1, 3-disubstituted thioureas 7 or 8 which were S-alkylated with methyl iodide or ethyl iodide. I15 and I16 were synthesized from 2 by reaction with dimethyl cyanodithioimidocarbonate. The structures of compounds I1-16 were confirmed by MS, IR, 1HNMR and elementary analysis. The results of preliminary pharmacological test showed that all compounds possessed nNOS inhibitory activity, among which compounds I8, I12 and I14 had good activity.

CONCLUSIONCompounds I8, I12 and I14 showed superior pharmacological profiles to the control compound S-methyl-N-(4-methoxyphenyl) isothiourea. The IC50 values of compounds I8, I12 and I14 inhibiting nNOS were 8.13 x 10(-7) mol.L-1, 1.74 x 10(-7) and 2.23 x 10(-7) mol.L-1 respectively, and it is worth further studying.

Animals ; Cattle ; Cells, Cultured ; Hippocampus ; cytology ; enzymology ; Inhibitory Concentration 50 ; Molecular Structure ; Nerve Tissue Proteins ; antagonists & inhibitors ; metabolism ; Nitric Oxide Synthase ; antagonists & inhibitors ; metabolism ; Nitric Oxide Synthase Type I ; Structure-Activity Relationship ; Thiourea ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology

To collect the literature on traditional Chinese medicine treatment for multiple aorto-arteritis from China National Knowledge Infrastructure(CNKI), establish prescriptions database after screening and normalizing the prescriptions reported in these literature, and analyze their medicinal rules by using traditional Chinese medicine inheritance support system. A total of 126 prescriptions for multiple aorto-arteritis were screened, containing 212 kinds of Chinese herbs. 26 core herb combinations were obtained by analysis of the commonly used herbs and their use frequencies. The treatment for multiple aorto-arteritis was manly of tonifying qi to nourish blood, promoting blood circulation to remove blood stasis, warming yang to dredge collaterals, and four new prescriptions were obtained. On this basis, two clinical cases were taken as the examples by analyzing the medicinal rules and the features of multiple aorto-arteritis. The first case showed that the herb combination of this study conformed to the basic core drug application mode and the core pathogenesis of multiple aorto-arteritis. The second case reflected the characteristics of the new prescriptions' herb combinations based on entropy hierarchical clustering. The practical analysis of the two clinical cases further indicated the reliability of the results. This study has certain guiding significance and reference value on new medicine research and development as well as clinical traditional Chinese medicine treatment for multiple aorto-arteritis.