2.Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent.
Chong-Wen BI ; Cai-Xia ZHANG ; Yang-Biao LI ; Wu-Li ZHAO ; Rong-Guang SHAO ; Lin MEI ; Dan-Qing SONG
Acta Pharmaceutica Sinica 2013;48(12):1800-1806
A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Berberine
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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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Cell Cycle
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drug effects
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Cell Proliferation
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drug effects
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DNA Topoisomerases, Type I
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metabolism
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Doxorubicin
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pharmacology
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Drug Resistance, Neoplasm
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Hep G2 Cells
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Humans
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MCF-7 Cells
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Molecular Structure
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Structure-Activity Relationship
3.Internal fixation with headless compression screws and back buttress plate for treatment of old Hoffa fracture.
Li MIN ; Chong-Qi TU ; Guang-Lin WANG ; Yue FANG ; Hong DUAN ; Lei LIU ; Hui ZHANG
Chinese Journal of Traumatology 2014;17(2):79-83
OBJECTIVETo analyze the early clinical and radiographic outcomes of Hoffa fractures treated by a standard protocol of open reduction and internal fixation using headless compression screws combined with back buttress plate in a consecutive series of 8 Chinese patients.
METHODSOpen reduction and internal fixation was performed on all patients. The fractures were anatomically reduced and held temporarily by K-wire. If the ends of fractures were atrophic, autologous bone graft from the ipsilateral iliac crest was packed between the ends. Then the fracture fragments were fixed with AO 6.5 mm headless compression cannulated screws. At least two screws were used to provide rotational stability. One pre-contoured reconstruction plate was placed on the nonarticular surface posteromedially or posterolaterally as back buttress plate.
RESULTSAll the patients were followed up for at least 12 months (range 12-25 months). All fractures achieved anatomical reduction and healed clinically and radiographically. At recent follow-up, the mean flexion degree was 120.6° (range 110°-135°) and the mean extension degree was 2.5° (range 0°-5°). The average visual analogue scale score was 1.6 points (range 0-3). Six patients were assessed as excellent and 2 as good according to the hospital for special surgery knee score system. There were no superficial or deep infections, or hardware breakages. No patient had giving way or locking of the knee, though some had intermittent pain and swelling after strenuous exercise. Injury mechanism had significant influence on the functional outcome (P=0.046).
CONCLUSIONHeadless compression screws combined with back buttress plate and/or autologous bone grafting to treat old Hoffa fracture is one of effective measures. It would be conducive to not only fracture healing but also early exercise and functional recovery.
Adult ; Bone Plates ; Bone Screws ; Female ; Femoral Fractures ; surgery ; Fracture Fixation, Internal ; methods ; Humans ; Male ; Middle Aged
4.Propagation of prdm1 gene knockout mouse and its genotype identification.
Xiao-Yun LU ; Chong CHEN ; Xiu-Ying PAN ; Ling-Yu ZENG ; Zhen-Yu LI ; Xu-Guang SONG ; Kai-Lin XU
Journal of Experimental Hematology 2012;20(4):985-988
This study was aimed to propagate and identify the prdm1 gene-knockout mice, so as to lay the foundation for studying Blimp-1 protein. Two kinds of transgenic homozygous mice with B6.prdm1(flox/flox) and B6.Lck-Cre were feed and propagated; after successful propagating, the first passage mice were obtained; after the first passage mice were copulated once again, the genotypes were obtained as follows: B6. prdm1(wild/wild). Lck-Cre, B6. prdm1(wild/wild), B6.prdm1(flox/flox). Lck-Cre, B6.prdm1(flox/wild). Lck-Cre, B6.prdm1(flox/flox), B6. prdm1(flox/wild). The genomic DNA of second passage mice was extracted, the Cre and loxp gene fragments were amplified by PCR, then the size of Cre and loxp genomic DNA were detected by agarose gel electrophoresis. The mice with B6.prdm1(flow/flox). Lek-Cre were used as conditionally prdm1-knockout mice, B6.prdm1(flox/wild). Lck-Cre mice, B6.prdm1(flox/flox) and B6 mice were used as controls. The spleen T lymphocytes and B lymphocytes were sorted by using magnetic beads, the blimp-1 target protein was identified by Western blot. The results showed that the two transgenic homozygous mice had the ability to reproduce, and the separation ratio of second passage mice generated from propagation of their offspring cach other meet Mendelian laws, and the prdm1 gene-knockout mice also could successfully obtained. It is concluded that the application of Cre-loxp system may successfully obtain plentiful prdm1 gene-knockout mice.
Animals
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Genotype
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Mice
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Mice, Inbred C57BL
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genetics
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Mice, Knockout
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genetics
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Reproduction
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Transcription Factors
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genetics
5.Effect of basic fibroblast growth factor on the expression of glial fibrillary acidic protein after tractive spinal cord injury in rats.
Lei LIU ; Bo LÜ ; Chong-qi TU ; Lei-ting CHI ; Guang-lin WANG ; Fu-xing PEI
Chinese Journal of Traumatology 2005;8(2):117-120
OBJECTIVETo investigate the effects of basic fibroblast growth factor (bFGF) on the expression of glial fibrillary acidic protein (GFAP) after tractive spinal cord injury in rats and to explore the recovery of spinal cord function.
METHODSThe rats were subjected to tractive spinal cord injury at T13-L2. Cortical somatosensory-evoked potential (CSEP) was closely monitored and when P1-N1 wave amplitude decreased to 70% of that before operation, a small-bore catheter was inserted below the injured plane through subarachnoid cavity. In the treatment groups, 20 microl of bFGF solution (containing 20 microg of bFGF) was injected through the catheter right after the operation and 1, 2, 3, 4, 8, 12 and 24 h postoperatively. In the control group, same volume of normal saline was injected and every four rats were killed at 1, 4, 7, 14 and 21 d after the operation. Combined behavior score (CBS) and electro-physiological examination were adopted to evaluate function recovery. Expression of GFAP was observed by immuno-histochemical staining and was analyzed quantitatively by computer image analysis.
RESULTSThere was statistically significant difference in GFAP-positive cells between bFGF treatment group and the control group (P<0.01). Similar tendency was indicated by the results of CBS and CSEP.
CONCLUSIONSbFGF can induce large expression of GFAP after tractive spinal cord injury in rats and promote spinal function recovery, which is highly important for spinal cord regeneration.
Animals ; Disease Models, Animal ; Evoked Potentials, Somatosensory ; drug effects ; Fibroblast Growth Factor 2 ; pharmacology ; Glial Fibrillary Acidic Protein ; drug effects ; metabolism ; Immunohistochemistry ; Rats ; Rats, Sprague-Dawley ; Recovery of Function ; Reference Values ; Spinal Cord Injuries ; metabolism ; physiopathology ; Traction
6.Infectious complications in patients with crush syndrome following the Wenchuan earthquake.
Hui ZHANG ; Jian-wei ZENG ; Guang-lin WANG ; Chong-qi TU ; Fu-guo HUANG ; Fu-xing PEI
Chinese Journal of Traumatology 2013;16(1):10-15
OBJECTIVETo analyze the results of clinical and bacteriological examinations in patients with crush syndrome who suffered infectious complications after an earthquake in Sichuan, China.
METHODSA total of 313 bacteriological samples among 147 patients with crush syndrome were collected. Infectious complications, results of microbiological examinations, potential risk factors of infection and mortality were analyzed statistically.
RESULTSIn the obtained database, 112 out of the 147 (75.7%) patients had infectious complications, in which, wound infection, pulmonary infection, and sepsis were most common. The time under the rubble and the time from injury to treatment were related to the occurrence of wound infection (P equal to 0.013, odds ratio 2.25; P equal to 0.017, odds ratio 2.31). Sepsis and wound infection were more common in patients who underwent fasciotomy or amputation than in those who did not (P equal to 0.001).
CONCLUSIONQuick rescue and injury treatment can decrease the infection risk in crush syndrome patients. It is better to obtain microorganic proofs before applying antibiotics, and bacteriological and drug sensitivity data should be taken into account, especially considering that most of these infections are hospital-acquired and drug resistance. Emphasizing the accuracy and efficiency of wound management in emergency situations, cautiously assessing the indications for fasciotomy to avoid open wounds from unnecessary osteofascial compartment decompression incisions may decrease the incidence of infection and ameliorate the prognosis.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Bacterial Infections ; etiology ; Child ; Child, Preschool ; China ; Crush Syndrome ; complications ; microbiology ; Earthquakes ; Female ; Humans ; Male ; Middle Aged ; Risk Factors
7.Absorbable materialversus Kirschner wire fixation for fractures of the Iateral humeral condyle in children: a Meta-analysis
Xing-Guang CHEN ; Min-Hua LU ; Lin LU ; Xiao-Dong WANG ; Cheng-Da ZOU ; Chong PU
Chinese Journal of Tissue Engineering Research 2018;22(14):2290-2296
BACKGROUND:Currently, there is no explicit evidence-based medicine evidence to prove the merits or demerits of absorbable materials in the treatment of fractures of the lateral humeral condyle in children. OBJECTIVE:To evaluate the clinical efficacies of open reduction with absorbable material versus open reduction with Kirschner wire fixation for lateral condylar fracture of the humerus in children.METHODS:WanFang, VIP, CNKI, CBMdisc, EMbase, PubMed were retrieved for controlled trials concerning open reduction with absorbable material versus open reduction with Kirschner wire fixation for treating lateral condylar fracture of the humerus in children. After data extraction and quality evaluations, RevMan 5.3 software was used for systematic review. Postoperative functional recovery of the elbow joint, average hospitalization expenses, adverse events, delayed union, postoperative infection, nerve injury and deformity of the elbow were compared in patients undergoing different treatments. RESULTS AND CONCLUSION:A total of seven articles, involving 449 children with lateral condylar fracture of the humerus, were included for this Meta-analysis. Children in test group received open reduction with absorbable material, while those in control group were subjected to open reduction with Kirschner wire fixation. For treating lateral condylar fracture of the humerus in children, no significant inter-group difference existed in the aspects of postoperative functional recovery of the elbow joint [odds ratio (OR)=0.72, 95% confidence interval (CI) (0.37, 1.41),P=0.34]; postoperative delayed union [OR=0.46, 95%CI(0.16, 1.30),P=0.14]; deformity of the elbow [OR=0.70, 95%CI (0.24, 2.10),P=0.53]. Less adverse events and postoperative infections were observed in the test group compared with the control group [OR=0.17, 95%CI (0.08, 0.38),P < 0.0001;OR=0.09, 95%CI (0.02, 0.38),P=0.001]. However, up to now, we knew of no comparable data concerning average hospitalization expenses and indicators for nerve injury between the two groups. To conclude, compared with Kirschner wire fixation, open reduction with absorbable material can achieve similar effects on lateral condylar fractures of the humerus, but has better effects to prevent adverse events and postoperative infection. Further investigation on large-scale, double-blind, high-quality randomized controlled trials is warranted for confirming our results.
8.Intensity modulated radiation therapy for 122 patients with untreated nasopharyngeal carcinoma
Chong ZHAO ; Li-Xia LU ; Fei HAN ; Tai-Xiang LU ; Shao-Min HUANG ; Cheng-Guang LIN ; Xiao-Wu DENG ; Nian-Ji CUI ;
Chinese Journal of Radiation Oncology 2005;0(05):-
Objective To analyse the preliminary clinical results of intensity modulated radiation therapy (IMRT) for 122 untreated nasopharyngeal carcinoma (NPC)pafients.Methods 122 NPC pa- tients received IMRT alone from Feb.2001 to Jun.2004,with 31 females and 91 males,and a median age of 45 years(range 25-66).According to the Fuzhou Stage Classification,there were StageⅠ11 patients, StageⅡ34,StageⅢ62,and StageⅣa 15.IMRT was carried out using an inverse planning system (COR- VUS 5.0,Peacock plan) developed by the NOMOS Corp.The treatment was given with the Multi-leaf Inten- sity Modulating Collimator (MIMIC) using a slice-by-slice arc rotation approach.The prescription dose was 68 Gy/30f to the nasopharynx gross tumor volume (GTV_(nx)),60-66 Gy/30f to positive neck lymph nodes (GTV_(nd)),60 Gy/30f to the first clinical target volume (CTV_1) and 54 Gy/30f to the second clinical target volume (CTV_2).Kaplan-Meier method was used to calculate the overall survival rate (OS),distant metas- tasis-free survival rates (DMFS),and local-regional control rates from the last date of therapy.Log-rank test was used to detect the difference between groups.Results The median follow-up time was 20 months ( range 6 to46 months).The 1-,2-,and 3-year OS was 95.2%,91.4%,85.1%,DMFS was 91.9%, 88.6%,85.6%,and the local-regional control rates was 96.5%,93.2%,93.2%,respectively.Statistics of the local control rate was insignificant either for advanced T(T3+T4) stage or early T(T1+T2) stage diseases(P=0.148).The 2-year regional control rate was insignificant either for patients with N(+) or N (-),but the 2-year DMFS was significant both for patients with N(+) and N(-)lesions(P=0.004).For 17 patients who failed,there were two with residual disease and one with recurrence at the primary site (17.6%),three patients in the neck (17.6%),twelve patients (70.6%) in distant metastases.Conclu- sions Intensity modulated radiation therapy does provide excellent local-regional control for untreated NPC, especially in patients with advanced T stage or N(+) lesion.Distant metastasis is the main cause of failure. N (+) is significantly correlated with distant metastasis.
9.A brief report on effect of rhG-CSF in treating leukopenia after radio-and chemo-therapy of patients with breast cancer.
Tie-Jun WANG ; Lin-Lin LIU ; Guang-Hui CHENG ; Xiao-Lan LIU ; Ya-Qin QU ; Zhen-Feng WU ; Chong-Fang ZHANG
Journal of Experimental Hematology 2004;12(3):381-382
The study was to observe the effect of rhG-CSF (lishengsu) in treating leukopenia caused by radiotherapy and chemotherapy in patients with breast cancer. 100 cases of breast cancer received modified radical mastectomy were randomized into two groups with the same treatment of one cycle chemotherapy using the protocol of CAF at two weeks after the operations and then radiotherapy. The patients in treated group received rhG-CSF 75 micro g per day s.c. for 5 - 7 days constantly, and additional 3 - 5 days according to leukopenia during radiotherapy. The patients in control group did not receive rhG-CSF during the chemo- and radio-therapy. The results shows that nadir of WBC and neutrophil counts in the treated group was higher than that in control significantly. In conclusion, effect of lishengsu on leucopenia in process of chemotherapy and radiotherapy shows definite therapeutic effect, the side effects are not remarkable.
Adult
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Breast Neoplasms
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therapy
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Combined Modality Therapy
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Female
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Granulocyte Colony-Stimulating Factor
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adverse effects
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therapeutic use
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Humans
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Leukopenia
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drug therapy
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Middle Aged
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Recombinant Proteins
10.Angiogenesis in chronic ischemic porcine myocardium after transfer of VEGF₁₆₅ and angiopoietin-1 mediated by recombinant adeno-associated viral vector.
Cheng-chu ZHU ; Shi-lin CHEN ; Yu-qing LIU ; Li-jiang TANG ; Xian-fang LIN ; Wei-guang BAO ; De-hua MA ; Guang-qiu ZHU ; Wen-juan ZHOU ; Yi-lin ZHOU ; Chong-wen DU
Journal of Zhejiang University. Medical sciences 2010;39(6):610-617
OBJECTIVETo study the effects of combination of angiopoietin-1 (ANG-1) and vascular endothelial growth factor₁₆₅ (VEGF₁₆₅) gene transfer mediated by recombinant adeno-associated viral vector on the neovascularization in chronic ischemic porcine myocardium.
METHODSAn ameroid constrictor was implanted around the left circumflex coronary artery (LCX) via endoscopy. Six weeks later, coronary angiography revealed that the myocardial ischemia was established by gradual occlusion of the left circumflex coronary artery (LCX). Sixteen swine with the total occlusion or partial stenosis (> 85 %) of the LCX were divided into 4 groups (4 in each group): group I, group II and group IV (control) received direct myocardium injection of rAAV₂ VEGF₁₆₅, rAAV₂ ANG-1 or PBS alone, respectively; group III received rAAV₂ VEGF₁₆₅ and rAAV₂ ANG-1. Selective coronary angiography and ultrasonography were performed perioperatively to evaluate the cardiac function and the formation of collateral circulation. The expression of VEGF₁₆₅ and ANG-1 proteins were assessed using ELISA or Western blot. The degree of angiogenesis was assessed by use of immunohistochemical analysis.
RESULTAngiography showed that the occlusion of all LCX was completed or exceeded 95% 6 weeks after ameroid constrictor implantation, indicating the successful establishment of animal model. The expression levels of VEGF₁₆₅ in group I and III and ANG-1 in groups II and III began to increase at d7 after transfection and reached the peak at d14; then decreased gradually to the normal level after 3 months. The expression levels of VEGF₁₆₅ in group II and group IV or that of ANG-1 protein in group I and group IV had no markedly changes at different time after transfection. There were significant increase in capillary density and arteriole density and more side branch vessels formed in group III compared with other groups. Echocardiographic measurements showed that the left ventricular systolic function of animals in groups I, II and III increased significantly after gene transfection, especially in group III; but there was no changes in group IV.
CONCLUSIONMyocardial perfusion and the left ventricular systolic function are improved after rAAV₂ VEGF₁₆₅ or rAAV₂ ANG-1 transfection, which is associated with the angiogenesis in porcine model of chronic myocardial ischemia.
Adenoviridae ; genetics ; Angiopoietin-1 ; genetics ; Animals ; Collateral Circulation ; Coronary Vessels ; physiopathology ; Disease Models, Animal ; Genetic Therapy ; Genetic Vectors ; Male ; Myocardial Ischemia ; physiopathology ; therapy ; Neovascularization, Physiologic ; Swine ; Swine, Miniature ; Transfection ; Vascular Endothelial Growth Factor A ; genetics