1.The investigation of "stereo teaching method" in OMPS clinical teaching
Chinese Journal of Medical Education Research 2002;0(01):-
In the clinical education of oral and maxillofacial plastic surgery,how to enhance students’study enthusiasm and interest,promote them to carry on the ponder,and sharpen their generalized analysis ability is a challenge for the OMPS(oral and maxillofacial plastic surgery) teachers.This article proposes a new teaching method:the stereo teaching method,and evaluate its effect.
2.Synthesis and in vitro cytotoxic activities of sorafenib derivatives.
Ke WANG ; Yan LI ; Li-Jing ZHANG ; Han-Ze YANG ; Xiao-Guang CHEN ; Zhi-Qiang FENG
Acta Pharmaceutica Sinica 2014;49(5):639-643
A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 micromol x L(-1). Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7c demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC50 values of 9.01, 4.97, 6.61 micromol x L(-1), respectively.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Cell Line, Tumor
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Cell Proliferation
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drug effects
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Niacinamide
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analogs & derivatives
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chemical synthesis
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chemistry
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pharmacology
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Phenylurea Compounds
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chemical synthesis
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chemistry
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pharmacology
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Structure-Activity Relationship
3.The anti-tumor activity and molecular mechanisms of an Aurora kinase inhibitor ZLJ213 in suppressing colon cancer growth.
Wan-qi ZHOU ; Li-jing ZHANG ; Han-ze YANG ; Zhi-qiang FENG ; Yan LI
Acta Pharmaceutica Sinica 2015;50(7):854-860
The aim of this study is to evaluate anti-tumor activities and mechanism of a novel kinase inhibitor ZLJ213 which targeted Aurora A and vascular endothelial growth factor receptor (VEGFR) in vitro and in vivo against human colon cancer. Results showed that ZLJ213 inhibited cell proliferation and induced cell cycle arrest and apoptosis of HCT1 16 and SW48 cell lines. In HCT116-derived xenograft, ZLJ213 dosed at 100 mg · kg(-1) inhibited tumor growth by 73.24%. The IC50 of ZLJ213 on the expression of p-Aurora A was 0.258 µmol · L(-1) analyzed by ELISA. Under the concentration of 0.08 µmol · L(-1), ZLJ213 could inhibit the activities of Aurora A, Histone H3 and VEGFR of HCT116 and SW48 cell lines. Simultaneously, ZLJ213 induced activation of Caspase 3 and PARP cleavage. Above data suggested that ZLJ213 had the ability to inhibit cell proliferation and induce cell apoptosis both in vitro and in vivo in colon cancer, and down-regulate the expression of p-Aurora A and p-VEGFR. ZLJ213 might be a potential therapeutic agent against colon cancer.
Animals
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Apoptosis
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Aurora Kinase A
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antagonists & inhibitors
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Cell Cycle Checkpoints
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Cell Line, Tumor
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drug effects
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Cell Proliferation
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Colonic Neoplasms
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pathology
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Humans
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Protein Kinase Inhibitors
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pharmacology
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Receptors, Vascular Endothelial Growth Factor
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metabolism
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Xenograft Model Antitumor Assays
4.Expression of PAK4 and its significance in gastric cancer
Ze LI ; Hui-Mian XU ; Feng LI
Chinese Journal of Oncology 2008;30(1):30-33
Objective To investigate the expression of p21-activated kinase4 (PAK4) in human gastric cancer, and to evaluate the correlation of PAK4 protein level with clinical pathologic parameters. Methods Immunohistochemical method was employed for detecting the expression of PAK4 in tissue samples obtained from 95 gastric cancer patients who underwent surgical treatment. Western blot was also used to measure the expression of PAK4 in gastric cancer tissues and adjacent non-cancerous gastric mucosa in 40 patients and also in 7 human gastric cancer cell lines. Results Immunohistochemical staining results showed that positive PAK4 expression in the gastric cancer tissues was 67.4%, and 96.9% of those (62/64) was located in the cytoplasm, while only 3.1% (2/64) was on the cell membrane. Expression of PAK4 was revealed to be significantly and positively correlated with both TNM stage (X2=10. 426, P<0.01) and lymph node metastasis (X2= 4.912, P<0.05 ). Western blot showed that PAK4 expression of gastric cancer tissues was significantly higher than that of adjacent non-cancerous gastric mucosa (t=-5. 978, P<0.01). Expression of PAK4 could also be detected in 7 human gastric cancer cell lines. Compared with GES-1, expression of PAK4 is higher in MKN45, AGS, N87 and BGC823, but it was lower in MGC803, MKN1 and SGC7901. Conclusion The overexpression of p21-activated kinase4 (PAK4) may be correlated with the carcinogenesis and prognosis of gastric cancer.
5.Expression of PAK4 and its significance in gastric cancer
Ze LI ; Hui-Mian XU ; Feng LI
Chinese Journal of Oncology 2008;30(1):30-33
Objective To investigate the expression of p21-activated kinase4 (PAK4) in human gastric cancer, and to evaluate the correlation of PAK4 protein level with clinical pathologic parameters. Methods Immunohistochemical method was employed for detecting the expression of PAK4 in tissue samples obtained from 95 gastric cancer patients who underwent surgical treatment. Western blot was also used to measure the expression of PAK4 in gastric cancer tissues and adjacent non-cancerous gastric mucosa in 40 patients and also in 7 human gastric cancer cell lines. Results Immunohistochemical staining results showed that positive PAK4 expression in the gastric cancer tissues was 67.4%, and 96.9% of those (62/64) was located in the cytoplasm, while only 3.1% (2/64) was on the cell membrane. Expression of PAK4 was revealed to be significantly and positively correlated with both TNM stage (X2=10. 426, P<0.01) and lymph node metastasis (X2= 4.912, P<0.05 ). Western blot showed that PAK4 expression of gastric cancer tissues was significantly higher than that of adjacent non-cancerous gastric mucosa (t=-5. 978, P<0.01). Expression of PAK4 could also be detected in 7 human gastric cancer cell lines. Compared with GES-1, expression of PAK4 is higher in MKN45, AGS, N87 and BGC823, but it was lower in MGC803, MKN1 and SGC7901. Conclusion The overexpression of p21-activated kinase4 (PAK4) may be correlated with the carcinogenesis and prognosis of gastric cancer.
6.Effect of 5-HT1A receptors in the hippocampal DG on active avoidance learning in rats.
Feng-ze JIANG ; Jing LV ; Dan WANG ; Hai-ying JIANG ; Ying-shun LI ; Qing-hua JIN
Chinese Journal of Applied Physiology 2015;31(1):44-48
OBJECTIVETo investigate the effects of serotonin (5-HTIA) receptors in the hippocampal dentate gyrus (DG) on active avoidance learning in rats.
METHODSTotally 36 SD rats were randomly divided into control group, antagonist group and agonist group(n = 12). Active avoidance learning ability of rats was assessed by the shuttle box. The extracellular concentrations of 5-HT in the DG during active avoidance conditioned reflex were measured by microdialysis and high performance liquid chromatography (HPLC) techniques. Then the antagonist (WAY-100635) or agonist (8-OH-DPAT) of the 5-HT1A receptors were microinjected into the DG region, and the active avoidance learning was measured.
RESULTS(1) During the active avoidance learning, the concentration of 5-HT in the hippocampal DG was significantly increased in the extinction but not establishment in the conditioned reflex, which reached 164.90% ± 26.07% (P <0.05) of basal level. (2) The microinjection of WAY-100635 (an antagonist of 5-HT1A receptor) into the DG did not significantly affect the active avoidance learning. (3) The microinjection of 8-OH-DPAT(an agonist of 5-HT1A receptor) into the DG significantly facilitated the establishment process and inhibited the extinction process during active avoidance conditioned reflex.
CONCLUSIONThe data suggest that activation of 5-HT1A receptors in hipocampal DG may facilitate active avoidance learning and memory in rats.
8-Hydroxy-2-(di-n-propylamino)tetralin ; pharmacology ; Animals ; Avoidance Learning ; Dentate Gyrus ; physiology ; Piperazines ; pharmacology ; Pyridines ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Serotonin, 5-HT1A ; physiology ; Serotonin ; physiology ; Serotonin Receptor Agonists ; pharmacology
7.Preliminary evaluation on 3-demension changes of facial soft tissue with structure light scanning technique before and after orthognathic surgery of ClassⅢdeformities
Juxiang PENG ; Jiuhui JIANG ; Yijiao ZHAO ; Yong WANG ; Ze LI ; Ningning WANG ; Zhimin FENG
Journal of Peking University(Health Sciences) 2015;(1):98-103
Objective:To evaluate facial soft tissue 3-deminsion changes of skeletal Class Ⅲmalocclu-sion patients after orthognathic surgery using structure light scanning technique .Methods:Eight patients [3 males and 5 females, aged ( 27.08 ±4.42 ) years ] with Class Ⅲ dentoskeletal relationship who underwent a bimaxillary orthognathic surgical procedure involving advancement of the maxilla by Le FortⅠosteotomy and mandibular setback by bilateral sagittal split ramus osteotomy (BSSO) and genioplasty to correct deformity were included .3D facial images were obtained by structure light scanner for all the patients 2 weeks preoperatively and 6 months postoperatively .The facial soft tissue changes were evalua-ted in 3-dimension.The linear distances and angulation changes for facial soft tissue landmarks were ana-lyzed.The soft tissue volumetric changes were assessed too .Results: There were significant differences in the sagittal and vertical changes of soft tissue landmarks .The greatest amount of soft tissue change was close to lips.There were more volumetric changes in the chin than in the maxilla , and fewer in the forehead .Conclusion: After biomaxillary surgery , there were significant facial soft tissue differences mainly in the sagittal and vertical dimension for skeletal Class Ⅲ patients .The structure light 3 D scan-ning technique can be accurately used to estimate the soft tissue changes in patients who undergo orthog-nathic surgery .
9.Study on DNA expression profiles in renal biopsies of patients with IgA nephropathy.
Feng LI ; Ying-hao YU ; Jing-sheng XU ; Feng-hua LAN ; Yong-ze ZHUANG ; Zhi-yong ZHENG ; Hua-sheng XIAO
Chinese Journal of Pathology 2009;38(5):342-343
Adult
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Biopsy
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DNA
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genetics
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Female
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Gene Expression Profiling
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Glomerulonephritis, IGA
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genetics
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pathology
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Humans
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Kidney
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pathology
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Male
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Middle Aged
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Young Adult
10.Synthesis of novel curcumin mimics and preliminary evaluation for their antitumor activity.
Yong-Cheng WANG ; Yu-Shan LI ; Han-Ze YANG ; Yan LI ; Xiao-Guang CHEN ; Zhi-Qiang FENG
Acta Pharmaceutica Sinica 2014;49(7):1022-1028
Curcumin has been reported to possess antitumor activity with low toxicity. However, the clinical application of curcumin has been significantly limited by its instability and poor metabolic property. In order to overcome these limitations and discover novel small molecules with potential antitumor activity, 29 curcumin mimics were synthesized, which were confirmed by 1H NMR and HR-MS, and their cytotoxic property was evaluated against five human cancer cell lines in vitro. Compounds 16, 18 and 19 exhibited good cytotoxic property, their IC50 value were even below 5 micromol x L(-1) to some cancer cell lines, 5-9 times better than curcumin.
Antineoplastic Agents
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chemical synthesis
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pharmacology
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Cell Line, Tumor
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Curcumin
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analogs & derivatives
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chemical synthesis
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pharmacology
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Drug Screening Assays, Antitumor
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Humans
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Inhibitory Concentration 50