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

Hypertension is a common chronic cardiovascular disease,which is a serious threat to patient's health.The choice of antihypertensive drugs are multiple,different doctors hold the different views.The research surveyed our hospital's clinicians in order to understand the selection of drugs in hypertension prevention and treatment.According to the research,we intended to regulate the clinical drug use,improving the rational use of drugs,and benefit patients.

Objective To assess the optimal visiualization capacity of brachial plexus with three-dimensional nerve-sheath signal increased with inked rest-tissue rapid acquisition of relaxation imaging (3D SHINKEI), exploring the feasibility of preliminary diagnostic value on brachial plexus diseases. Methods MRI scans were performed on 24 healthy volunteers with no history of brachial plexus injury, and 46 patients whose outcomes of lesions had been verified as post-ganglionic brachial plexus injuries by surgery or clinical follows-up . The scan series consist 3D SHINKEI, STIR in the coronal plane as well as DW-MRN in the axial plane using a 3.0 T MR system. The source and post-processed images of 3D SHINKEI and DW-MRN were scored according to the optimal visibility on brachial plexus, in the meanwhile, contrast-to-noise ratio of the original images in the 3D SHINKEI and STIR sequences were calculated separately. Two radiologists blindly compared the detection rate of positive brachial plexus injuries between 3D SHINKEI and STIR in 46 patients. And then analyze the outcomes by means of Kappa test, Mann-Whitney test , independent sample t test, and Chi-square test. Results Post-ganglionic brachial plexus showed high intensity in the 3D SHINKEI sequence. In the 24 healthy volunteers, the scores by the two radiologists were 3.6 ± 0.6, 3.5 ± 0.6, 3.0 ± 0.2, 2.9 ± 0.1, respectively. There was statistical difference between the two sequences (Z=2.667,P=0.008,P<0.05). And the Kappa was 0.8 and 0.6 with favorable consistency. The CNR of 3D SHINKEI and STIR were 0.61 ± 0.07, 0.42 ± 0.03 (t=12.78, P=0.001, P<0.05). The positive detection rates of post-ganglionic brachial plexus injuries on 3D SKINKEI and STIR were, 78.3%, 52.2%(χ2=9.421, P<0.05). Conclusions 3D SHINKEI sequence demonstrates robust visibility consistently and can clearly display the structures and signals of post-ganglionic abnormality, compared with DW-MRN and STIR. This technique can be helpful to provide more complementary information to further confirm the diagnosis of brachial plexus injuries.

Objective:To evaluate the feasibility and the application values of quantitative susceptibility mapping (QSM) for the assessment of meniscal injury and in distinguishing meniscus degeneration and tears.Methods:The clinical and imaging data of 70 patients suspected of meniscus injury and scheduled for arthroscopy in Shandong Medical Imaging Research Institute, Cheeloo College of Medicine, Shandong University from November 2019 to June 2020 were analyzed retrospectively. Thirty age-and sex-matched healthy subjects were also examined as controls. All subjects received knee joint QSM and routine MR imaging. According to the results of arthroscopy, the patients was divided into meniscus degeneration and meniscus tear groups, respectively. The conventional MR was evaluated by two radiologists. The meniscus injury area was delineated on the original QSM magnitude images (the central area of the posterior corner of the lateral meniscus was selected in the healthy controls) and mapped to the corresponding QSM maps, and the magnetic susceptibility values were measured. Kruskal-Wallis H test was used to analyze the magnetic sensitivity values of meniscal degeneration, meniscal tear and healthy control groups; and Bonferroni was used to correct the pairwise comparison. ROC curve was established to evaluate the threshold and efficacy of magnetic susceptibility value in the diagnosis of meniscal tear. The results were compared with those of conventional MRI. Results:The magnetic susceptibility values of meniscus of healthy controls, meniscal degeneration and meniscal tear groups were (0.035±0.016)ppm, -0.031(-0.040,-0.005)ppm, and(-0.122±0.115)ppm, respectively, with significant difference found among the three groups (χ2=44.419, P<0.05). The magnetic susceptibility values of meniscus of healthy controls was significantly higher than those of meniscus degeneration patients and meniscus tear patients (χ2=-23.843, -48.253, P<0.05). The magnetic susceptibility values of meniscus of meniscus tear group was significant lower than those of meniscus degeneration group (χ2=-24.410, P<0.05). Taking magnetic susceptibility values of -0.062 5 ppm as threshold, the area under the ROC curve for the diagnosis of meniscal tears was 0.949, with the sensitivity as 87% and the specificity as 100%. The sensitivity and specificity of conventional MRI in the diagnosis of meniscal tears were 86.8% and 87.5%, respectively. Conclusion:QSM can quantitatively evaluate meniscus injury and can be used as an effective supplement method to conventional MRI, which is helpful to improve the diagnosis of meniscus tear.

OBJECTIVETo measure the effect of atorvastatin on COX-2 expression in monocytes in patients with acute myocardial infarction (AMI).

METHODSForty patients with AMI (AMI group) and 18 patients with stable coronary heart disease (control group) were enrolled, and patients with AMI were randomly given routine therapy (n = 20) and routine therapy plus atorvastatin (20 mg/day, n = 20) for a week. Peripheral blood monocytes for each participant including patients with AMI were isolated and cultured for 24 hours. During the culture, monocytes in patients with pretreatment AMI were incubated with celecoxib in different concentration (0, 0.1, 1 and 10 micromol/L). COX-2 mRNA expression in monocytes was measured by reverse transcription polymerase chain reaction (RT-PCR); concentrations of interleukin-6 (IL-6) in supernatant from monocytes and plasma hs-CRP levels were measured by using enzyme-linked immunosorbent assay (ELISA).

RESULTSCOX-2 expression in monocytes in patients with AMI (0.92 +/- 0.13) was significantly higher than that in the control subjects (0.19 +/- 0.08), and decreased by 66% after atorvastatin (compared with that on routine therapy, P < 0.05); IL-6 secretions of monocytes in the AMI group (204.8 +/- 45.6 ng/L) increased dramatically compared with those in the control group (40.9 +/- 1.2 ng/L, P < 0.05), and reduced dramatically by 58% when incubated with 10 micromol/L celecoxib (P < 0.05) in a concentration-dependent manner; plasma levels of CRP in the AMI group (43.3 +/- 14.9 mg/L) significantly increased compared with those in the control group (1.7 +/- 0.8 mg/L), and reduced by 62% after atorvastatin (compared with those in the routine therapy group, P < 0.05). COX-2 expression in monocytes in the AMI group was positively correlated with both secretions of IL-6 and plasma level of CRP (r = 0.636 and 0.662, respectively, both P < 0.05).

CONCLUSIONSThere is an inflammatory activation in peripheral blood monocytes in patients with early AMI, and the monocytes-derived COX-2 may play an important role in promoting early inflammatory process. Atorvastatin may decrease COX-2 expression in peripheral blood monocytes in patients with AMI and cyclooxygenase-dependent pathway might be correlated with the anti-inflammation mechanism of statin.

Aged ; Atorvastatin Calcium ; Cyclooxygenase 2 ; metabolism ; Female ; Heptanoic Acids ; therapeutic use ; Humans ; Inflammation ; Interleukin-6 ; metabolism ; Leukocytes, Mononuclear ; drug effects ; metabolism ; Male ; Middle Aged ; Myocardial Infarction ; drug therapy ; metabolism ; Pyrroles ; therapeutic use ; RNA, Messenger ; genetics

OBJECTIVETo investigate the protective effect of neferine against damages of endothelial cells induced by lysophos-phatidylcholine (LPC) and the relationship with asymmetric dimethylarginine (ADMA).

METHODThe human umbilical vein endothelial cells (HUVEC-12) were treated with LPC (10 mg x L(-1)) for 24 h to establish the model of endothelial cells damages; HUVECs were prior exposed to neferine (0.1, 1.0 or 10.0 micromol x L(-1) ) for 1 h, and then exposed to LPC in the presence of the neferine for 24 h. At the end of the experiment, the cultured medium was collected for measuring the concentration of nitric oxide (NO), aleic dialdehyde (MDA) as well as ADMA and the cells were collected for measuring the level of intracellular reactive oxygen species (ROS).

RESULTCompared with control group, exposure of endothelial cells to LPC (10 mg x L(-1)) for 24 h significantly increased the concentration of MDA and ADMA in the medium and the level of intracellular ROS and coinstantaneously significantly decreased the concentration of NO in the medium. Neferine (0.1, 1.0 or 10.0 micromol x L(-1)) significantly inhibited the elevated concentration of MDA, ADMA as well as the level of intracellular ROS and coinstantaneously significantly attenuated the decreased level of NO induced by LPC.

CONCLUSIONNeferine can protect the endothelial cells against damages induced by LPC and the protective effect is related to the decrease of the concentration of ADMA.

Arginine ; analogs & derivatives ; metabolism ; Benzylisoquinolines ; pharmacology ; Cell Line ; Endothelial Cells ; drug effects ; metabolism ; Humans ; Lysophosphatidylcholines ; pharmacology ; Malondialdehyde ; metabolism ; Nitric Oxide ; metabolism ; Reactive Oxygen Species ; metabolism

Objective To analyze and identify the mutations in SGLT2 gene of nine Chinese families with FRG, and determine the renal threshold for glucose excretion (RTG), so as to explore the association of genotype and RTG. Methods All coding regions of SGLT2 gene, including intron exon boundaries, were analyzed using PCR followed by direct sequence analysis. Quantitative test for 24?hour urine glucose and RTG were measured among 9 probands (21 patients) and their family members from 9 pedigrees (total 25 subjects). The differences in renal glucose thresholds between patients with different genotypes (heterozygotes and compound heterozygotes; c.886(-10_-31) del heterozygotes and other heterozygotes) were compared. Results Twelve mutations were identified by SGLT2 gene analysis, including 10 novel ones that were not included in HGMD:c.331T>C, p.W111R;c.374T>C, p.M125T; c.394C>T, p.R132C; c.612G>C, p.Q204H; c.829C>T, p.P277S; c.880G>A, p.D294N;c.1129G>A, p.G377S; c.1194C>A, p.F398L; c.1540C>T, p.P514S; c.1573C>T, p.H525Y. In thisstudy, the mutation c.886(-10_-31)del that is specific to Chinese population accounted for about 28％of the total alleles (5/18). The RTG values of patients with compound heterozygous mutations were much lower than those with simple heterozygous mutations [(1.28 ±0.10) vs (5.14±0.77) mmol/L; P<0.001];and c.886(-10_-31)del heterozygotes had significant lower RTG values than others [(4.43 ± 0.37) vs (5.70 ± 0.51) mmol/L, P<0.001]. Conclusions Ten novel mutations which may be related to FRG are found in this study, and c.886(-10-31)del may be a hot?spot mutation in Chinese patients. Compound heterozygotes had much lower RTG values than simple heterozygotes.

Objective:To investigate the effect of fibroblasts in breast cancer microenvironment on the expression of TIGAR and Bcl-2 in breast cancer cells and their effect on breast cancer growth.Methods: In vitro experiments,the co-cultured model of human breast cancer cell line MDA-MB-231 with human fibroblast line CCC-ESF-1 was established.The effect of fibroblasts on the expression of TIGAR and Bcl-2 in breast cancer cells was tested with reverse transcription quantitative polymerase chain reaction(RT-qPCR) and Western blot.Annexin V flow cytometry and caspase-3 activity assay were employed to detect the apoptosis of breast cancer cells.In vivo experiments,human breast cancer transplanted tumor model in nude mice was established and the tumor volume of nude mice was meas-ured.Immunohistochemistry was used to detect TIGAR and Bcl-2 expression in the transplanted tumor tissues of nude mice.Results:The results showed that the co-cultured fibroblasts could up-regulate the expression of TIGAR and Bcl-2 in MDA-MB-231 cells and inhibited the apoptosis of MDA-MB-231 cells in vitro.The fibroblasts implanted with breast cancer cells could up-regulate TIGAR and Bcl-2 expression in breast cancer tissues of tumor-bearing nude mice in vivo,whereas highly expressed TIGAR and Bcl-2 accelerated the tumor growth of tumor-bearing nude mice.Conclusion:The fibroblasts in breast cancer microenvironment up-regulate the expression of TIGAR and Bcl-2 in breast cancer cells co-cultured with fibroblasts.Highly expressed TIGAR and Bcl-2 inhibit the apoptosis of breast cancer cells and promote the growth of breast cancer.

OBJECTIVETo investigate the pulmonary dysfunction patterns in patients of scoliosis associated with neurofibromatosis type I (NF1) and to identify factors affecting the pulmonary function in patients with scoliosis associated with NF1.

METHODSPreoperative pulmonary function tests (PFTs) were evaluated in 100 patients with scoliosis [NF1 group, 36 cases; idiopathic scoliosis (IS) group, 64 cases] from January 2003 to June 2009. According to location of apical vertebra and dystrophic change in patients with NF1, the parameters of pulmonary function [vital capacity (VC), forced vital capacity (FVC), forced expiratory volume in one second (FEV1), maximal mid-expiratory flow (MMEF), maximal voluntary ventilation (MVV)] were compared between NF1 group and IS group, and between the subgroups of NF1. The correlation between pulmonary function parameters and radiographic parameters of scoliosis was analyzed.

RESULTSThe VC, FVC, FEV1, MMEF, MVV in NF1 group and IS group were of no significant difference (P > 0.05). In NF1 patients, the pulmonary dysfunction was more severe in thoracic subgroup than non-thoracic subgroup (P < 0.05), while there was no difference between dystrophic scoliosis and non-dystrophic scoliosis (P > 0.05). The location of apical vertebra and the severity of scoliosis correlated significantly with the pulmonary dysfunction in NF1 group.

CONCLUSIONSThe pattern of pulmonary dysfunction in scoliosis associated with NF1 is similar with IS. Pulmonary dysfunction is more severe in thoracic scoliosis. The location of apical vertebra and the severity of scoliosis are the risk factors influencing the pulmonary dysfunction.

Adolescent ; Child ; Female ; Forced Expiratory Volume ; Humans ; Lung ; physiopathology ; Male ; Neurofibromatosis 1 ; complications ; physiopathology ; Respiratory Function Tests ; Scoliosis ; complications ; physiopathology ; Vital Capacity ; Young Adult

OBJECTIVETo study whether antisense oligonucleotides and ultrasonic microbubble intensifier transfection combined with ultrasound irradiation is an effective and directional way in reversing multidrug resistance (MDR) in tumors.

METHODSMdr1, mrp, and lrp genes antisense oligonucleotides on the ultrasound microbubble intensifier were transfected for the human HepG2/ADM cell lines and then the cells were radiated with low intensity ultrasound. The effects of the reversion of carcinoma cells' MDR and the reduction of their malignancy and growth capability in vitro and in vivo were assessed using RT-PCR, Western blot and MTT.

RESULTSThe treatment restrained the multiplication of the human HepG2/AMD cell lines. The levels of their mRNA and protein of cells' mdr1 and mrp genes dropped significantly. Growth of the subcutaneous transplanted tumors in the nude mice decreased.

CONCLUSIONSTransfection of MDR genes antisense oligonucleotides on the ultrasonic microbubble intensifier combined with low intensity ultrasound radiation may serve as a new treatment method for hepatocellular carcinoma.

ATP-Binding Cassette, Sub-Family B, Member 1 ; genetics ; Animals ; Carcinoma, Hepatocellular ; pathology ; Cell Line, Tumor ; Drug Resistance, Multiple ; genetics ; Drug Resistance, Neoplasm ; genetics ; Humans ; Liver Neoplasms ; pathology ; Male ; Mice ; Mice, Inbred BALB C ; Microbubbles ; Oligonucleotides, Antisense ; genetics ; Transfection ; Ultrasonics