1.Expression of glyoxalase Ⅰ and its effect on cell proliferation and apoptosis in endometrial carcinoma
Long SUI ; Qisang GUO ; Zhenbo ZHANG ; Hongyan JIN ; Yinhua YU ; Youji FENG
Chinese Journal of Obstetrics and Gynecology 2010;45(6):429-433
Objective To examine the expressions of glyoxalase Ⅰ (GLO-Ⅰ ) in endometrial cancer tissues and cell lines and to investigate the roles of GLO-Ⅰ on proliferation and apoptosis in endometrial cancer cells. Methods Immunohistochemistry, western blot and RT-PCR were used to investigate the expressions of GLO-Ⅰ protein and mRNA in endometrial cancer tissues and Ishikawa cell lines ;enzyme activity of GLO-Ⅰ in normal endometrium, endometrial cancer and paraneoplastic tissue samples was detected with spectrophotometer; proliferation and apoptosis of Ishikawa cell before and after RNA interference (RNAi) procedure were detected by the methyl thiazolyl tetrazolium (MTT) and flow cytometry, respectively. Results (1)There were significant differences of GLO-Ⅰ expression between normal endometrium (0/19) and endometrial cancer tissues ( 76%, 22/29 ); these were also significant differences of enzyme activity of GLO-Ⅰ among normal endometrium, paraneoplastic and endometrial cancer tissues( 1.1,0.8 vs 92.3 IU/mg; P <0.01 ). Enzyme activity of GLO-Ⅰ in fresh normal endometrium and paraneoplastic tissues was weak, while that of fresh endometrial cancer tissues was as high as 92. 3 IU/mg in average. (2)The expression of GLO-Ⅰ mRNA in Ishikawa cell transfected with GLO-Ⅰ siRNA was significantly lower than that in negative group (0.25 ± 0.06 vs 0.93 ± 0.10, P < 0.0l ), and the similar results that in the expression of GLO-Ⅰ protein (0.38 ±0.06 vs 0.94 ±0.13, P <0.01 ). (3) Proliferation in Ishikawa cell was significantly inhibited after silencing RNA expression of GLO-Ⅰ ( P = 0.028 ). The apoptosis rate of cells transfected with GLO- Ⅰ siRNA was significantly higher than that of negative control group and blank control group [ ( 6.7 ± 0.8 ) % vs ( 1.2 ± 0.4) %, ( 1.4 ± 0.4 ) %; P < 0.01 ]. Conclusion The expression and enzyme activity of GLO- Ⅰ is significantly increased in endometrial cancer, which could promote abnormal proliferation and inhibit apoptosis in endometrial cancer cells.
2.The hypoglycemic effect and mechanism of Laminaria japonica on diabetic model induced by alloxan in rats
Shaohua LONG ; Xiaodan LI ; Zhuqin YU ; Li SHUAI ; Pengfei FU ; Yunliang GUO ; Delin DUAN
International Journal of Traditional Chinese Medicine 2011;33(7):597-600
Objective To investigate the hypoglycemic effects of Laminaria japonica (L. japonica) on diabetic model induced by alloxan in rats. Methods Sixty healthy female rats were used to establish diabetic models by injecting alloxan peritoneally, and L.japonica was applied as raw materials for potential marine drugs.The levels of fasting blood glucose (FBG) were detected by automatic blood glucose device. Enzyme linkedimmunoabsorbant assay was applied to determine the insulin level in serum. The shape and structure of isletcells were observed with histopathological staining, and the expression of superoxide dismutase (SOD) and inducible nitric oxide synthase (iNOS) in islet cells were detected by immunohistochemical technique. Results After the treatment, the levels of FBG of L.japonica treated group B [(9.37±1.70) mmol/LandC (9.18±1.65 ) mmol/L, F= 32.81, q=6.35~11.72, P<0.05 ] reduced, while the serum levels of insulin in treated group A, Band C (0.0378±0.0026, 0.0378±0.0027, 0.0367±0.0035) increased(F= 11.40, q=4.28~8.47, P<0.05) significantly than those of diabetic model group (0.0456 ±0.0057) . The shape and structure of islet cells improved with the up-expressing SOD(t=4.73~4.76, P<0.05)and down-expressing iNOS (t=4.81~5.30, P<0.05) in L.japonica treated group B and C than those in diabetic model group. Conclusion L.japonica might decrease the serum level of FBG through promoting the islet cell recovery by an anti-oxide effect.
3.Mechanical and biological properties of porous calcium phosphate cement/fibrin glue for bone regeneration in vitro
Jingjing DONG ; Long BI ; Na LI ; Yu GUO ; Qiang XU ; Wei LEI ; Geng CUI
Chinese Journal of Tissue Engineering Research 2014;(30):4831-4837
BACKGROUND:Fibrin glue introduced into calcium phosphate cement has not been confirmed whether this way could overcome the compressive limits and the low degradation of calcium phosphate cement and to modify the biological properties of calcium phosphate cement. OBJECTIVE:To explore the mechanical and biological properties of calcium phosphate cement/fibrin glue at different powder/liquid ratio for bone regeneration in vitro. METHODS:Calcium phosphate cement and fibrin glue were mixed at ratios of 1:1, 3:1, 5:1 (mL/g), and the pure calcium phosphate cement served as controls. Setting time, scanning electron microscope and the biomechanical test were used to analyze the composite scaffold structure, physical performance and the mechanical properties. Passage 3 osteoblasts were respectively inoculated on the material surface of the four groups, and pure cells served as blank controls. celladhesion, proliferation and alkaline phosphatase activity were observed. RESULTS AND CONCLUSION:The initial and final setting time of calcium phosphate cement/fibrin glue at 1:1 and 3:1 (mL/g) was higher than that in the control group (P<0.05), while the initial and final setting time of calcium phosphate cement/fibrin glue at 5:1 (mL/g) was lower than that of the control group (P<0.05). Scanning electron microscope showed smoother and denser surface of composite scaffolds compared with the pure calcium phosphate cement. The aperture of the composite scaffolds was decreased with the increasing concentration of fibrin glue. The compressive strength of composite scaffolds at 3:1 and 5:1 was higher than that of the control group (P<0.05), while the modulus of the composite scaffolds at 1:1, 3:1, 5:1 was higher than that of the control group (P<0.05). celladhesion, proliferation and alkaline phosphatase activity showed no difference among the three composite scaffold and control groups, but al higher than the blank control group (P<0.05). These findings indicate that fibrin glue introduced into calcium phosphate cement can overcome the low-strength limits of calcium phosphate cement, and maintain the good biological properties of calcium phosphate cement for bone regeneration.
4.Guiding of serum procalcitonin-guided antibiotic in elderly early-onset stroke-associated pneumonia
Wei LONG ; Lijuan LI ; Yuan ZHONG ; Huifeng GUO ; Jingye YANG ; Yu ZHANG ; Gang LU
Chinese Journal of Geriatrics 2013;(5):513-515
Objective To evaluate the effects of serum procalcitonin (PCT)-guided antibiotic therapy in elderly patients with early-onset stroke-associated pneumonia (EOP).Methods Totally 179 eligible elderly patients with EOP were randomly devided into 2 groups:standard therapy group (standard group,n=88) and PCT-guided group (PCT group,n=91).Patients in standard group received antibiotics according to antibiotics guidelines in China by the treating physicians.Patients in PCT group were treated with antibiotics for 5 days,then the antibiotic treatment was based on serum PCT levels as follows:discouraged if PCT<0.25 μg/L and encouraged if PCT≥0.25 μg/L.Length of hospitalization,duration of antibiotics,costs of hospitalization and antibiotics,clinical efficacy,andmortality,National Institutes of Health Stroke Scale (NIHSS) score and Barthel index (BI) on the 28th day were observed.Results There were no significant differences in clinical efficacy,mortality,NIHSS score and BI between the two groups on the 28th day [(85.7% vs.86.3%),(8.8% vs.7.9%),10.1 (7.8,16.2) vs.9.8 (6.0,15.5),60.1(42.5,82.3) vs.57.9 (39.2,84.8),respectively,all P> 0.05].The length of hospitalization,antibiotic duration,costs of hospitalization and antibiotics were lower in PCT group than in standard group [19 (10,38) d vs.26(17,42) d,10 (7,14) dvs.15 (6,21) d,3350 (2052,6163) yuanvs.10355 (6877,15421) yuan,7532 (4810,12116) yuan vs.5358 (3089,8144) yuan,respectively,all P<0.05].Conclusions PCT guidance of antibiotic therapy is effective and safe for the treatment of early-onset stroke associated pneumonia in elderly patients.It can reduce the antibiotic duration and costs of hospitalization.
5.Design, synthesis, antibacterial and anti-cell proliferation activities of 1,2,4triazino3,4-h 1,8naphthyridine-8-one-7-carboxylic acid derivatives.
Liu-zhou GAO ; Tao LI ; Suo Xie YU ; Wen-long HUANG ; Hui ZHAO ; Guo-qiang HU
Acta Pharmaceutica Sinica 2015;50(3):332-336
To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.
Animals
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Anti-Bacterial Agents
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chemical synthesis
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chemistry
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Antineoplastic Agents
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chemical synthesis
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chemistry
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Carboxylic Acids
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Carcinoma, Hepatocellular
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Cell Line
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Cell Proliferation
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Drug Design
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Escherichia coli
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drug effects
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Fluoroquinolones
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chemical synthesis
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chemistry
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HL-60 Cells
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Humans
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Leukemia L1210
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Liver Neoplasms
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Methicillin-Resistant Staphylococcus aureus
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drug effects
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Mice
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Naphthyridines
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Triazines
6.Synthesis, antitumor activity and SAR of C-3 oxadiazole sulfanylacetylhydrazone-substituted fluoroquinolone analogues.
Liu-Zhou GAO ; Yu-Suol XIE ; Tao LI ; Wen-Long HUANG ; Guo-Qiang HU
Acta Pharmaceutica Sinica 2014;49(12):1694-1698
To explore an efficient strategy for the conversion of antibacterial fluoroquinolones into antitumor fluoroquinolones, an azole heterocyclic ring of oxadiazole instead of the C-3 carboxylic acid group with a functionalized hydrazone group as a modified side-chain, fifteen novel 2-(fluoroquinolon-3-yl)-oxadiazole-5- sulfanylacetylhydrazone derivatives 7a-7o were designed and synthesized on the basis of the pharmacophore hybridization principle from pefloxacin, separately. The structures for fifteen title compounds were characterized by elemental analysis, 1H NMR and MS, and their in vitro antitumor activity against Hep-3B cell line was evaluated by a MTT assay. The results showed that the title compounds exhibited more significantly inhibitory activity than that of the parent pefloxacin, in which compounds with electron-withdrawing group attached on aryl ring had more potency than that of compounds with electron donating group, especially compounds with a carboxylic substituent were comparable to comparison doxorubicin. It suggests that it is favorable for an improvement of antitumor activity to remain a carboxylic acid unit at the aromatic ring.
Antineoplastic Agents
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chemical synthesis
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chemistry
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Cell Line, Tumor
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Fluoroquinolones
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chemistry
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Humans
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Oxadiazoles
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chemistry
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Structure-Activity Relationship
7.Optimization and application of chemically defined medium for 13C metabolic flux analysis of Streptomyces rimosus M4018.
Long WANG ; Hongtu ZHAO ; Lan YU ; Meijin GUO ; Ju CHU ; Siliang ZHANG
Chinese Journal of Biotechnology 2014;30(4):679-683
The aim of this study is to develop a synthetic medium suitable for 13C metabolic flux analysis (13C-MFA) of Streptomyces rimosus. The cell growth rate and oxytetracycline production by S. rimosus M4018 were compared when M4018 cells were growth on the optimized chemically defined media with organic nitrogen sources or inorganic nitrogen sources. First, a synthetic medium contained KNO3 as the main nitrogen source was screened, then optimized by a response surface method. Using this new medium, the oxytetracycline yield was increased from 75.2 to 145.6 mg/L. Furthermore, based on the 13C-MFA, we identified that Entner-Doudoroff pathway does not exist in S. rimosus cells cultured in a chemically defined medium with feed of 100% 1-13C labeled glucose. This study is helpful for subsequent 13C-MFA application of S. rimosus.
Carbon Isotopes
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analysis
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Culture Media
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chemistry
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Metabolic Flux Analysis
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Nitrogen
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chemistry
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Oxytetracycline
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biosynthesis
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Streptomyces rimosus
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metabolism
9.Ultrasonic diagnosis of thyroid microcarcinoma and analysis on reason for its misdiagnosis
Hua-yun, GU ; Xue-dong, DENG ; Jian-feng, GUO ; Qiu-long, JIN ; Yu, YAN
Chinese Journal of Medical Ultrasound (Electronic Edition) 2013;(11):947-950
Objective To analyze the ultrasonic features of thyroid microcarcinoma (TMC) and the causes of misdiagnosis. Methods The ultrasonic features including shape, margin, echogenecity, microcalcification, vascularity and lymphadenopathy were analyzed retrospectively in 26 pathologically-proven TMC patients. Results In 26 cases, 11 cases were diagnosed correctly before operation (11/26, 42.31%), 12 cases were misdiagnosed (12/26, 46.15%) as adenoma or benign nodule, and 3 cases were missed diagnosed (3/26, 11.54%). Among the 23 cases detected on ultrasound, 21 cases were solid and hypoechoic (21/23, 91.30%);19 cases were ill-defined (19/23, 82.61%);12 cases were taller than wide in shape (12/23, 52.17%); 14 cases had microcalcification (14/23, 60.87%); 7 cases showed central or peripheral blood flow signals (7/23,30.43%) with arterial resistance index>0.70 in 3 lesions and<0.70 in 4 lesions. Conclusions Several ultrasonographic features are helpful in identiifcation of TMC, including hypo/iso-echogenecity, ill-deifned margin, taller-than-wide shape, microcalciifcation, arterial signals with high resistance index, and abnormal lymphadenopathy. Moreover, for cases with multiple lesions, to the potential co-existence of benign and malignant lesions should be considered.
10.Development and clinical application of a color pediatric visual acuity chart
Shu-Guo, YIN ; Hong-Wei, YANG ; Long-Quan, XUE ; Yu, DI ; Lu, LIU
International Eye Science 2014;(12):2297-2299
AlM: To introduce a new color pediatric visual acuity chart and its clinical application.
METHODS:The color pediatric visual acuity chart was designed based on principle of visual angle. The optotype on the color chart had graphics. The progression rate of optotype size between 2 lines was 10 10 and 1. 2589. A regular geometric progression of optotype sizes and distribution was employed to arrange 8 lines with 11 optotype on the color chart. The testing distance was 3m. The visual acuity score could be recorded as logarithm of the minimum angle of resolution notation or decimal notation. The reliability of naked distant measurements with this new chart was tested in one eye of 100 children (4 ~ 6 years old) taking the Chinese national standard logarithm visual acuity chart standard.
RESULTS: The color pediatric visual acuity chart and logarithmic chart controls, visual acuity test results that in the two groups had no significant difference (t=1. 2671, P> 0. 05 ). Two sets of vision data existed positive correlation (r= 0. 924, P<0. 01). Cooperation rate was 100%, the recognition rate was more than 90%.
CONCLUSlON:Children are easier to accept used new color pediatric visual acuity chart to inspect vision. New chart is reliability and apply to children's vision screening.