Using bioactive compounds 7-hydroxy flavone, salicylaldehyde, cinnamic acid and 4-amino-5- mercapto-1,2,4-triazoles as starting materials, three new types of flavone derivatives containing 1,2,4-triazole structure were synthesized via different step reactions. These new compounds were characterized by 1IHNMR, ESI-MS, IR and elemental analysis. Their scavenging effects on the superoxide radical (O2·-), hydroxyl radical (·OH), DPPH · radical and their total reduction activities were tested. The results showed that all of the compounds possessed some antioxidative activity at the concentration of 0.5 mg · mL(-1), but the scavenging ability of the target compounds was lower than that of the standard compound Vc.
Cinnamates ; chemistry ; Flavones ; chemical synthesis ; chemistry ; Flavonoids ; chemistry ; Free Radical Scavengers ; chemical synthesis ; chemistry ; Triazoles ; chemistry

OBJECTIVE: To design and synthesize flavone derivatives containing dihydropyrazole moiety and investigate their antioxidative activities in vitro. METHODS: 7-Bromoethoxy flavone was synthesized by the reaction of 7-hydroxy flavone with 1, 2-dibromoethane. Then six flavone derivatives containing dihydropyrazole moiety were synthesized by the condensation reaction of 7-bromoethoxy flavone with two types of O-phenyl substituted dihydropyrazole compounds. These new compounds were characterized by IR, 1H-NMR, 13C-NMR, ESI-MS and EA. Their antioxidation effects, such as scavenging effects on the superoxide radical (O2-), hydroxyl radical (·OH), DPPH· radical, nitroso radicals (NO2·) and the total reduction activities, were compared. RESULTS: At the concentration of 0.5 mg·mL-1 most of the title compounds had antioxidation effects, but their activities were weaker than that of vitamine C. CONCLUSION: The scavenging effects on four different radicals and the total reduction activity of 7-(1-phenyl-3-methyl-4, 5-dihydropyrazole-5-phenyl)-oxyethoxy flavone (compound 2a) are all relatively strong. Its antioxidative activities in vivo can be further investigated.

Objective To analyze the risk of embolization of brain AVMs,study the angioarchitectural factors affecting the difference of embolization level,and to establish the angioarchitecture grading system for embolization of brain AVMs.Methods The clinical data,angioarchitectural features, embolism complication and embolism level were retrospectively analyzed.Multivariate statistical analysis was performed to determine if any of the variables was predictive of a poor outcome of embolization(death or permanent neurological deficit),and if any of the variables was predictive of the percentage obliteration achieved by embolization.Based on the above results,we established the angioarchitecture grading system.Results Endovascular procedures for embolization were performed 324 times in 189 patients during an 11-year period.Embolization was performed using N-butyl cyanoacrylate.In those patients,3(1.6%) died and 5(2.6%)had a permanent neurological deficit as a result of the embolization.The AVMs were given a score from 0 to 5 based on the size,number of the first grade feeding artery,and number of the second grade feeding artery.The assigned scores were as follows:nidus size(AVF=0,

Objective To investigate the causes,consequences and management of injuries to the draining veins after embolization of brain arteriovenous malformations(BAVMs)with ?-n-butyl cyanoacrylate (NBCA).Methods The angiographic imaging data of 189 BAVMs patients who underwent NBCA embolization were studied retrospectively.The status of the draining veins before and after NBCA embolization was observed and compared.The intracerebral hemorrhage(ICH)complications and their relation to their angiographic features were analyzed.Results Twenty-three patients out of 189 patients showed injuries to the draining venous system,including 10 low-grade injury,6 moderate injury,and 7 high- grade injury.Six patients suffered from ICH after embolization,of whom 4 patients were due to injuries of the draining veins(2 moderate and 2 high-grade).In the 3 months follow-up evaluation of 4 patients with ICH, one died,one was in vegetative state,and the other two patients suffered from residual severe or minor (1 patient for each)permanent neurological deficits.Conclusion Our findings suggest that injury of the draining veins is the major cause of ICH and may lead to serious consequences after embolization of BAVMs with NBCA.

Objective To evaluate the treatment of aneurysms rupture during endovascular embolization.Methods Nine aneurysms ruptured during the embolization and were treated with endovascular embolization.The reasons of aneurysms rupture during embolization,the prevention and the first aid after aneurysms rupture were analysed.Results Seven patients recovered and 2 died.Conclusions The optimal treatment of aneurysms rupture during endovascular embolization is effective,(J Intervent Radiol,2007,16: 132-134)

OBJECTIVETo establish a method for real-time recording the oxygen consumption of mice under normobaric hypoxia.

METHODSThe experimental apparatus was made up of animal container, filling water control system, electronic balance, hose, a computer with weight recording software, etc. The working principle was that the oxygen consumed by animal was replaced by water filling which was controlled by the pneumatic and hydraulic actuator. The water was weighted by an electronic balance and the weight signal was recorded into excel file at the same time. The accuracy and precision of the apparatus were detected by a 10 ml syringe. The oxygen consumption characteristics of 6 acute repetitive hypoxia mice and 6 normal mice were observed.

RESULTSThe P value for the paired t test was 1 and the CV value was 4%. The survival time and total oxygen consumption of acute repetitive hypoxia mice were both significantly increased compared to normal mice (P < 0.05), which were (58.8 +/- 6.8) min and (46.0 +/- 8.7) min respectively for the survival time and (85.1 +/- 8.5) ml and (73.6 +/- 5.4) ml respectively for total oxygen consumption.

CONCLUSIONThe hypoxia tolerance of the acute repetitive hypoxia mice can significantly improved by taking more oxygen in the animal cabin. The accuracy and precision of the apparatus are high and it can be used for the determination of oxygen consumption in hypoxia research.

Animals ; Hypoxia ; physiopathology ; Mice ; Monitoring, Physiologic ; instrumentation ; Oxygen Consumption ; physiology

Objective To evaluate the effects of optimal pharmacotherapy according to guideline on treating chronic heart failure(CHF)in real world clinical practice. Methods A total of 231 consecutive outpatients with reduced left ventricular ejection fraction(LVEF≤40%)and enlarged left ventricular end diastolic diameter(male ＞55 mm, female ＞60 mm)were recruited from January 2001 to June 2009. All patients were treated with optimal pharmacotherapy according to guideline recommendations and followed up to December 31,2009. Mortality, rehospitalization and changes of heart size and cardiac function at baseline and at the end of follow-up period were analyzed. Results(1)14 patients were lost during follow-up (6. 1%), and follow-up was complete in 217 patients(93.9%). 97.2% and 98.2% patients were prescribed angiotensin converting enzyme(ACE)inhibitors and β-blockers(βB). Combined of ACE inhibitors and BB use was applied in 95.3% patients. The target dose of ACE inhibitors and βB were reached in 50. 7% and 37.3% patients.(2)Lower mortality and re-hospitalization rates were observed in this cohort: all-cause morality, average annual mortality was 11.5% and 3.9% respectively. Rehospitalization rate was 27.6%.(3)Left ventricular end-diastolic diameter(LVEDD)decreased from (68.2 ±7.2)mm to(62. 2 ±9. 6)mm. LVEDD value was normal or near normal(male≤60 mm, female ≤55 mm)in 43.2% patients. LVEF improved form(29. 8 ±7. 5)% to(43. 3 ± 11.8)%, LVEF was ＞40% in 60.4% patients, LVEF was ≤ 40% but increased ≥ 10% after treatment in 22.9%patients. Conclusion Optimal pharmacotherapy according to guideline can improve prognosis of outpatients with CHF.

Objective To investigate the morphological changes of different types of axonal injury in acute stage in rat brain with diffuse axonal injury(DAD caused by combined head injuries,and explore their relevant injury mechanisms. Methods SD rats were randomized into experimental (n=16)and normal control(=8)groups.According to the different injury times(6,24 h),the experimental group was equally divided into two subgroups(n=8).A new experimental facility was employed to induce DAI in rats.HE staining was conducted in different time points in the acute stage.Immunofluorescence assay was performed to detect the expressions of antibodies to β-Amyloid precursor protein(β-APP)and antibodies to neurofilament-68(NF-68)and electron microscope was also introduced to investigate the changes of axonemal ultrastructure.Results All injured rats experienced behavioral suppression:the coma in the experimental group was significantly prolonged as compared to that in the normal control group(P<0.05).Immunofluorescence assay for antibodies to β-APP and NF-68 revealed two distinct types of axonal injuly: β-APP confined to focal spheroidal axonal swellings and axonal retraction bulbs;while NF-68 Was only found within thin and elongate axonal segments. Electron microscope also demonstrated two different types of ultrastructure of axonal injury. Conclusion Impaired axonal transport and neurofilament compaction can occur independently in the process of axonal injury with different morphological changes.Multiple immunocytochemical approaches can help to fully assess the overall axonai response to traumatic brain injury.

For investigation of the regulatory mechanism of cholecystokinin-octapeptide (CCK-8) on pulmonary circulation in rabbits with endotoxic shock (ES) induced by lipopolysaccharides (LPS), mean arterial pressure (MAP) and pulmonary arterial pressure (PAP) were evaluated for 5 h in five groups of rabbits: group of LPS (8 mg/kg, i.v.)-induced ES, group of CCK-8 pretreatment (15 microg/kg, i.v.) 15 min before LPS administration (8 mg/kg, i.v.), group of proglumide pretreatment (1 mg/kg, i.v.) 15 min before LPS administration (8 mg/kg, i.v.), group of CCK (15 microg/kg, i.v.) only, and normal saline (control) group. The pulmonary arterial tension was measured with isolated vascular ring technique. The results showed that LPS-induced pulmonary arterial hypertension was abolished by CCK-8. In contrast, proglumide, a nonspecific antagonist of CCK-8 receptor, potentiated the deleterious effect of LPS. The contractile response of isolated pulmonary artery to alpha-adrenoceptor agonist phenylephrine (PE) was enhanced and the relaxation response to acetylcholine (ACh) was depressed significantly after LPS was injected, but the effect could be reversed by CCK-8. These results suggest that pulmonary circulation is improved by CCK-8 in ES, and the regulatory effects of CCK-8 may be brought about by modulating the pulmonary arterial tension.
Animals ; Hypertension, Pulmonary ; etiology ; physiopathology ; Male ; Pulmonary Artery ; drug effects ; physiology ; Rabbits ; Shock, Septic ; complications ; physiopathology ; Sincalide ; pharmacology ; Vasodilation ; drug effects

OBJECTIVETo investigate the status of enterovirus (EV) infection in children with acute lower respiratory tract infection (ALRTI).

METHODSA total of 404 samples (with odd numbers) of nasopharyngeal aspirates were collected from the children who were hospitalized in the Children's Medical Center, Hunan Provincial People's Hospital due to ALRTI between September 2007 and April 2008. The conserved sequence in the 5'-noncoding region of EV was used to design the primer, and nested RT-PCR was performed to detect EV in the samples.

RESULTSOf the 404 samples, 19 (4.7%) were EV-positive, and mostly taken from children under 3 years of age (95%); there was no significant difference in the detection rate between male and female children. Of the EV-positive children, 13 (68%) were clinically diagnosed with bronchial pneumonia, and 6 (32%) with bronchiolitis; 90% of them showed symptoms of fever, 84% had a cough, 63% had asthma, and 63% had complications mainly including diarrhea (6 cases), granulocytopenia (4 cases), and acute respiratory distress syndrome (2 cases). In addition, 26% of the EV-positive children had leukocyte disorder, more than half had liver dysfunction, and a few had myocardial involvement.

CONCLUSIONSEV is a pathogen that should not be neglected in children with ALRTI. For these children, close attention should be paid to the epidemiological status and clinical features of EV infection, and blood routine examination, liver function test and myocardial enzyme assay should be carried out periodically to improve prognosis.

Acute Disease ; Child ; Child, Preschool ; Enterovirus Infections ; epidemiology ; Female ; Humans ; Infant ; Male ; Nasopharynx ; virology ; Respiratory Tract Infections ; virology