2.Asymmetric Morita-Baylis-Hillman Reaction of Conjugated Nitroalkene with Activated Aldehyde Catalyzed by Cinchona Alkaloids
Lingyu SUN ; Da LI ; Zhongjing HE ; Wei YAO ; Ru JIANG
China Pharmacist 2017;20(2):216-220
Objective:To develop a catalytic system for the asymmetric Morita-Baylis-Hillman ( MBH) reaction of conjugated ni-troalkene with activated aldehyde, and screen out the chiral catalysts with high activity and enantioselectivity. Methods: Totally 21 chiral organocatalysts were applied in the asymmetric MBH reaction ofβ-nitrostyrene with ethyl glyoxylate, and the ee value was deter-mined by chiral HPLC. The effects of temperature, solvent and substrate ratio on the catalytic reaction were investigated. Results: In the presence of cinchona alkaloid catalyst (DHQ)2AQN, β-nitrostyrene reacted with ethyl glyoxylate in toluene at 0℃ affording the MBH adduct in 60% yield with good enantioselectivity (up to 56.9% ee). Conclusion: The bis-cinchona alkaloids with aromatic bridging group are the efficient catalysts for the asymmetric MBH reaction ofβ-nitrostyrene with ethyl glyoxylate, and moderate isolated yield and enantioselectivity are obtained.
3.Study on inhibition of lymphangiogenesis in gastric cancer by NM-3
Wei DA ; Jinshui ZHU ; Weixiong CHEN ; Long WANG ; Qun SUN
Chinese Journal of Digestion 2010;30(6):394-397
Objective To evaluate the inhibitory effect of 2-(8-hydroxy-6-methoxy-1-oxo-1-H-2-benzopyran-3-Y1) propionic acid (NM-3) on lymphangiogenesis in gastric cancer using orthotopic implantated tumor models of BALB/C nude mice. Methods A BALB/C nude mouse model of transplanted in situ human gastric cancer was established. Twenty-eight nude mice were divided into four groups with 7 each: control group, NM-3 treated group, carboplatin (10 mg/kg) treated group,and NM-3 combiantion group injected with normal saline, 5 mg/kg of NM-3, 10 mg/kg of carboplatin or 5 mg/kg of NM-3, + 10 mg/kg carboplatin, respectively, twice a week for 8 weeks. At the end of the 8th week, all mice were sacrificed for detection of lymphatic microvessel density (LMVD),lymphatic vessel endothelial hyaluranic acid receptor 1 (LYVE-1), podoplanin and Prox-1 byimmunohistochemistry with staining. Results In comparison with control group, the LYVE-1 level in other three groups was decreased with no significant difference (P> 0.05). The concentrations of podoplanin and Prox-1 in NM-3 group and combination group decreased significantly than those in control group and carboplatin group (P < 0.05). The number of LMVD in NM-3 group and combination group was 4.72±0.50 and 4.78± 0.38, respectively, which was significantly lower than that in control group (7.35±0.55)and carboplatin group (6.98i0.35, P<0.05). Conclusion The NM-3 can inhibit the growth of gastric cancer by interfering lymphangiogenesis of gastric cancer.
4.Activation of Rho Kinase in Lung Tissue of Hypoxic Pulmonary Hypertension in Rats in Different Stages and Its Significance
xing-zhen, SUN ; xiang-yang, TIAN ; da-wei, WANG
Journal of Applied Clinical Pediatrics 1986;0(01):-
Objective To study the expression of Rho kinase and its functional activation in lung tissue from hypoxic pulmonary hypertension(HPH) rat model,and the effects of fasudil on HPH.Methods Seventy-two male Spraque-Dawley rats were randomly divided into the control group,hypoxic model group,and fasudil-intervention group[group with hypoxia and fasudil for 15 mg/(kg?d)],respectively.Mean pulmonary arterial pressure(mPAP) and right ventricle hypertrophy index(RVHI) were measured.Expression of Rho kinase mRNA and protein were examined by reverse transcriptase-polymerase chain reaction(RT-PCR) and Western blot,respectively.The phosphorylation of binding subunit of myosin phosphatase(MBS)-a substrate of Rho kinase was detected by Western blot and defined,as the mark of functional activation of the kinase.Results The expression of Rho kinase mRNA in hypoxic model group was markedly upregulated even before the onset of the third day after the experiment(HPH),and it was much lower in rats of fasudil group than that of hypoxic model group.The phosphorylation of MBS was significantly higher in hypoxic model group than that in control group,and it was positively correlated with the mPAP and RVHI(all P
5.Effect of Ligustrazine on Expression of Platelet-Derived Growth Factor-? Receptor and Extracellular Signal Regulated Kinase in Neonatal Rat Cardiac Myocytes in Vitro Induced by Angiotensin Ⅱ
yin-ping, SUN ; da-wei, ZHANG ; xing, WANG
Journal of Applied Clinical Pediatrics 2006;0(13):-
Objective To investigate the effect of ligustrazine on the expression of platelet-derived growth factor-?(PDGF-?) receptor and extracellular signal regulated kinase(ERK1/2) induced by angiotensin Ⅱ(AngⅡ) in cardiac myocytes,and explore the mechanism of therapeutic.Methods Cultured cardiac myocytes of neonatal rats were treated with 10-7 mol/L AngⅡ as Ang Ⅱ group,10-7 mol/L AngⅡ plus 10 mg/L ligustrazine as ligustrazine group,the normally cultured neonatal rat cardiac myocytes as control group.Protein synthesis was measured by -leucine incorporation,and the expression of PDGF-? receptor and ERK1/2 was detected by Western blot.SPSS 11.0 software was used to analyze the data.Results There were significant differences among 3 groups(F=20.71 P
7.Inhibitory effect of Xiaotan Sanjie Recipe on the microsatellite instability of orthotopic transplantation tumor in MKN-45 human gastric cancer nude mice.
Min YE ; Da-Zhi SUN ; Pin-kang WEI
Chinese Journal of Integrated Traditional and Western Medicine 2014;34(5):592-596
OBJECTIVETo study the inhibitory effect of Xiaotan Sanjie Recipe (XSR) on the microsatellite instability of orthotopic transplantation tumor in MKN-45 human gastric cancer nude mice.
METHODSThe 3rd passage subcutaneous transplantation tumor was taken as the origin of the model by using MKN-45 human gastric cancer cell lines. MKN-45 human gastric cancer nude mouse model was established using OB glue adhesive method. Then 30 nude mice were divided into the model group, the XSR group, and the chemotherapy group. Mice in the XSR group were intragastrically given XSR at the daily dose of 0.4 mL. Mice in the chemotherapy group were intragastrically given Fluorouracil at the daily dose of 0.4 mL. No intervention was given to mice in the model group. After 6 weeks of medication, the tumor weight was measured, and the tumor inhibition rate calculated. The size, the peak height, and the peak area of 5 microsatellite instability sites were detected.
RESULTSThe tumor inhibition rate was 40. 84% in the XSR group. The tumor weight was significantly lower in the XSR group than in the model group (P < 0.01), showing no statistical difference when compared with the chemotherapy group (P >0.05). The incidence of high microsatellite instability (MSI-H) in the model group was 70%, and the incidence of low microsatellite instability (MSI-L) was 30%. Microsatellite stable site tended be stable after 6 weeks of XSR treatment.
CONCLUSIONXSR showed inhibition on microsatellite instable orthotopic transplantation tumor in MKN-45 human gastric cancer nude mice.
Animals ; Antineoplastic Agents ; pharmacology ; Cell Line, Tumor ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Mice ; Mice, Nude ; Microsatellite Instability ; drug effects ; Neoplasm Transplantation ; Stomach Neoplasms
8.A child with gastric stromal sarcoma.
Shao-ming ZHOU ; Lai-bao SUN ; Hong-ying LUO ; Ju-rong WEI ; Da-ming BAI
Chinese Journal of Pediatrics 2004;42(1):73-73
Child, Preschool
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Female
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Humans
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Sarcoma
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diagnosis
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surgery
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Stomach Neoplasms
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diagnosis
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surgery
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Stromal Cells
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pathology
9.The role of standard CPR training in olympic medical volunteers
Fanshan MENG ; Jing SUN ; Da JI ; Wei CHEN ; Tanshi LI ; Hong SHEN
Chinese Journal of Emergency Medicine 2009;18(1):30-33
Objective To evaluate the role of standard CPR training in Beijing Olympics medical volunteers by compared with the no-traimng medical personnel.Method Performance qualities of CPR was evaluated in the 44 medical vohmteers,who worked in a Beijing Olympic Venue.They received the training On standard CPR for 6 monthes,and served as training group.The performance of another 72 emergency medical workers from first-class hospitals without the training on stand CPR within 1 year(control group) Was compared with training group.Phillips QCPR3535 monitor was used to measure the compression frequency,depth and chest re-expand between the compression and the operation time via the sternal chest compression pad fitted with an accelerometer.Personal practical results of 5 circles of CPR operation were recorded in a table and the numbers ofpractical. Compression in one minute were counted.Data Were analyzed with chi-quare test and t-test.The parameters ofthe influence fac.tor(gender,age,hand placement,hand skill,compression posture and standard training)were brought into logistic regression analysis.Results Compared with the control group,the qualification rate of general CPR performance in the training group was much higher(86.4%vs.31.9%),and the compression cpmlification rates of the chestcompression,depth and chest re-palld betweenthe compression wcfe higher(88.6%,93.2%,95.5% vs.40.3%,43.0%,86.1%,P<0.01),the duration of ventilation in each operationstion was shorter[(6.38±1.3)vs.(7.57±1.6),P
10.Anatomical characteristics of thoracic vertebrae for safe pedicle screw placement:comparison between normal adolescents and adolescent idiopathic scoliosis patients
Guanyu CUI ; Wei TIAN ; Bo LIU ; Da HE ; Yuqing SUN ; Jingwei ZHAO ; Xiaoguang CHENG
Chinese Journal of Tissue Engineering Research 2015;(26):4158-4163
BACKGROUND:Pedicle screw is the major instrumentation of surgery in thoracic spine. However, there have been few reports about pedicle morphology relevant to screw insertion tracts, and few reports comparing the normal adolescents and adolescent idiopathic scoliosis patients. OBJECTIVE:To compare the morphologic characteristics of the thoracic pedicle with regard to safe thoracic pedicle screw placement in normal adolescents and adolescent idiopathic scoliosis patients. METHODS: Thoracic pedicles of thirty-five normal adolescents and thirty-five adolescent idiopathic scoliosis patients were measured with three-dimensional reconstruction CT images. Measured parameters include (1) critical distance: the shortest distance from an entry point to the ventral cortex of the lamina. (2) Safe distance: the distance from the entry point to the tangent of the spinal canal at the medial wal of the pedicle. (3) Pedicle screw length. (4) Pedicle width. (5) Pedicle transverse angle. The dangerous area was defined as the distance between the critical distance and the safe distance. RESULTS AND CONCLUSION: The mean critical distance was (9.2±1.0) mm for the normal adolescents, and (9.4±1.2) mm for the adolescent idiopathic scoliosis patients. Safe distances were significantly less in normal adolescents (14.7±0.8) mm than that of the adolescent idiopathic scoliosis group (15.4±1.4) mm (P < 0.001). The dangerous area was (5.4±0.7) mm for the normal adolescents, which was significantly less than that of the adolescent idiopathic scoliosis patients (6.0±1.0) mm (P < 0.001). Pedicle screw length was (36.6±4.1) mm for the normal adolescents and (37.1±5.3) mm for the adolescent idiopathic scoliosis patients. Pedicle width was (5.8±1.2) mm for the normal adolescents and (5.7±1.7) mm for the adolescent idiopathic scoliosis patients. No significant difference in critical distance, pedicle screw length and pedicle width was found between the two groups (P=0.382, 0.135, 0.293). Pedicle transverse angle decreased gradualy from T1 to T12 in both groups. These results verify that pedicle morphology of many parameters is different between normal adolescents and adolescent idiopathic scoliosis patients, especialy in the apical area of the thoracic curve.