1.A preschool child with primary thrombocytosis.
Chen LING ; Guang-hua ZHU ; Ling JIN
Chinese Journal of Pediatrics 2013;51(7):541-542
Aspirin
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administration & dosage
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therapeutic use
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Blood Cell Count
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Blood Platelets
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drug effects
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physiology
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C-Reactive Protein
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analysis
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Child, Preschool
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Diagnosis, Differential
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Female
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Humans
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Hydroxyurea
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administration & dosage
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therapeutic use
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Interferons
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administration & dosage
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therapeutic use
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Platelet Count
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Thrombocythemia, Essential
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blood
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diagnosis
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therapy
3.Effect of Ginkgo biloba Tablet on the Expression of Scavenger Receptor A of the Aortic Wall in Atherosclerotic Rats.
Gui-yue ZHU ; Wei ZHU ; Ling-yun PAN ; Xiao-jing MA ; Hai-tao YUAN ; Guang YANG
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(4):449-453
OBJECTIVETo observe the expression of Ginkgo biloba Tablet (GbT) on scavenger receptor A (SRA) of the aortic wall and changes of serum inflammatory factors in atherosclerotic rats, and to explore its new mechanism for fighting against atherosclerosis (AS).
METHODSTotally 45 male Wistar rats were randomly divided into the control group, the model group, the GbT group, 15 rats in each group. Levels of blood glucose, blood lipids, blood calcium, serum C-reactive protein (CRP), soluble intercellular adhesion molecule-1 (slCAM-1), and soluble vascular cell adhesion molecule-1 (sVCAM-1) were measured in all rats. The expression of SRA in the aortic wall of atherosclerotic rats was observed by immunohistochemical assay. The correlation between the expression of SRA and levels of in-flammatory factors was also observed.
RESULTSCompared with the control group, blood glucose and blood calcium obviously increased (P < 0.05); levels of TG, TC, and LDL-C were significantly elevated (P < 0.01); neointimal areas were significantly thickened, increased intima percentage was significantly enlarged, narrowed lumen index was significantly reduced; levels of CRP, sICAM-1, and sVCAM-1 were significantly elevated in the model group (all P < 0.01). Compared with the model group, blood glucose and blood calcium obviously decreased (P < 0.05); levels of TG, TC, and LDL-C significantly decreased (P < 0.01) in the GbT group. Aortic lumens were obviously narrower in the model group than in the GbT group (P < 0.05). SRA expressed at the aortic wall. The aforesaid 3 indices were significantly improved in the GbT group than in the model group (P < 0.01). Serum levels of CRP, sICAM-1, and sVCAM-1 were significantly decreased in the GbT group than in the model group (P < 0.01). Serum levels of CRP, sICAM-1, and sVCAM-1 were positively correlated with the percentage of SRA positive expression area (r = 0.701, 0.604, 0.581, all P < 0.01).
CONCLUSIONSSerum levels of inflammatory factors in atherosclerotic rats were elevated, and the expression of SRA in the aortic wall was enhanced. The expression of SRA was closely correlated with serum levels of inflammatory factors. GbT could decrease serum levels of inflammatory factors and inhibit the expression of SRA.
Animals ; Aorta ; drug effects ; metabolism ; Atherosclerosis ; drug therapy ; Blood Glucose ; analysis ; C-Reactive Protein ; analysis ; Calcium ; blood ; Drugs, Chinese Herbal ; pharmacology ; Ginkgo biloba ; chemistry ; Intercellular Adhesion Molecule-1 ; blood ; Lipids ; blood ; Male ; Random Allocation ; Rats ; Rats, Wistar ; Scavenger Receptors, Class A ; metabolism ; Tablets ; Vascular Cell Adhesion Molecule-1 ; blood
5.Design, synthesis and biological evaluation of novel para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones as human PARP-1 inhibitors.
Hai-Ping YAO ; Zhi-Xiang ZHU ; Ming JI ; Xiao-Guang CHEN ; Bai-Ling XU
Acta Pharmaceutica Sinica 2014;49(4):497-503
Poly(ADP-ribose) polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. It can polymerize ADP-ribose units on its substrate proteins which are involved in the regulation of DNA repair. In this work, a novel series of para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones was designed and synthesized, and the inhibitory activities against PARP-1 of compounds 7a-7e, 8a-8f, 9a-9c and 10a-10c were evaluated. Of all the tested compounds, nine compounds displayed inhibitory activities with IC50 values ranging from 4.6 to 39.2 micromol x L(-1). In order to predict the binding modes of the potent molecules, molecular docking was performed using CDOCKER algorithm, and that will facilitate to further develop more potent PARP-1 inhibitors with a quinazolinedione scaffold.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Drug Design
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Enzyme Inhibitors
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chemical synthesis
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chemistry
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pharmacology
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Molecular Docking Simulation
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Molecular Structure
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Poly (ADP-Ribose) Polymerase-1
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Poly(ADP-ribose) Polymerases
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Quinazolinones
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chemical synthesis
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chemistry
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pharmacology
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Structure-Activity Relationship
6.Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton.
Jie ZHOU ; Zhi-Xiang ZHU ; Xiao-Guang CHEN ; Bai-Ling XU
Acta Pharmaceutica Sinica 2013;48(12):1792-1799
PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Aza Compounds
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chemical synthesis
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chemistry
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pharmacology
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Indoles
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chemical synthesis
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chemistry
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pharmacology
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Poly (ADP-Ribose) Polymerase-1
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Poly(ADP-ribose) Polymerases
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metabolism
7.Examination of point mutations within the ABL kinase domine region of BCR/ABL in patients with chronic myeloid leukemia who develop imatinib resistance
Dong-Guang YANG ; Ri ZHANG ; Jian-Nong CEN ; Zi-Ling ZHU ;
Chinese Journal of Laboratory Medicine 2003;0(11):-
Objective To investigate the point mutations within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia who develop imatinib resistance.Methods We collected a total of 17 bone marrow samples obtained from 11 patients who showed hematology resistance (n = 7)or cytogenetic refractoriness(n = 4).A long semi-nest PCR method was used to amplify the ABL kinase domain of the BCR/ABL allele.After two rounds of PCR reactions,we got a fragment of 863 bases The PCR products were purified and followed by sequencing.Results In total,we find three point mutations presented in all patients tested G250E,E255K and T315I.The mutation rate of hematology resistance is 4/ 7,and 95% confidence interval was 8%-90%,while mutation rate of cytogenetic refractoriness 1/4,95% confidence interval 1%-81%.For those patients whose samples were available,no single mutation were determined before imatinib resistance emerged.Conclusions There is high frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia.It's good for patients to switch to another therapeutic strategy when the mutations are detected.
8.Treatment of Morel-Lavallée leision using double-tube continuous negative pressure drainage
Guang YANG ; Yi ZHU ; Jingchao WANG ; Ling YAO ; Qilin ZHAI ; Congfeng LUO
Chinese Journal of Orthopaedics 2012;32(4):339-343
Objective To explore clinical effect of double-tube continuous negative pressure drainage in the treatment of Morel-Lavallée leision.Methods We retrospectively analyzed the clinical data of 13 patients with Morel-Lavallée leision,which were diagnosed and treated in our hospital from May 2009 to July 2010.They were 11 women and 2 men,aged from 19 to 57 years (average,32.5 years).All patients underwent operations within 3 days after injury,except for 2 patients whose diagnosis was postponed.The operation was performed with small incision and double-tubes were placed for continuous negative pressure drainage.Double-tubes were not removed until effusion was less than 30 ml/24 hours.The heal was defined as no skin necrosis and subcutaneous hydrops at lesion site,no skin floating and sliding at palpation.Results Double-tubes were removed 4 to 12 days postoperatively (average,6.3 day).All of 13 patients were followed up for an average of 13.7 months (range,10 to 18 months).Skin necrosis occurred in 1 patient.Lesions were healed 4 to 10 weeks postoperatively(average,7.2 weeks).No deep infection or delayed hematogenous infection was found.There were no general systematic complications.Superficial infection at wound site occurred in one patient and healed after wound management.Conclusion Application of double-tube continuous negative pressure drainage is a safe,less invasive,low-cost and effective treatment for Morel-Lavallée leision.
9.Effectiveness of intravenous immunoglobulin therapy in treating unexplained recurrent spontaneous abortion and its effect on the level of serum soluble human leucocyte antigen G.
Xiao-guang SUN ; Xin-yan LIU ; Rui ZHU ; Guang-sheng FAN ; Ying ZHANG ; Feng-ling CHEN
Acta Academiae Medicinae Sinicae 2010;32(5):483-487
OBJECTIVETo explore the effectiveness of intravenous immunoglobulin (IVIG) in treating patients with unexplained recurrent spontaneous abortion (URSA) and the effect of IVIG on the level of soluble human leucocyte antigen G (sHLA-G).
METHODSThis prospective trial conducted at PUMC Hospital between 2004 and 2008 included 60 women with URSA. The patients were allocated into IVIG group (30 cases) and control group (30 cases). IVIG was intravenously used before conception at a dose of 0.2g/kg; once pregnancy was confirmed,IVIG was continued every 4 weeks till the 20th gestational week. Traditional Chinese medicine or/and progesterone were used in control group. The outcome of pregnancy was evaluated by live birth rate and effective rate(defined as the embryo living 4 week longer than previous pregnancy). Serum samples were collected randomly before pregnancy and in the 6th-8th gestational week from IVIG group (15 samples),control group (15 samples),and healthy women (20 samples). The levels of sHLA-G,interferon γ (IFN-γ), interleukin-2 (IL-2), and interleukin-10 (IL-10) were determined by enzyme-linked immunosorbant assay (ELISA).
RESULTSThe pregnancy rate was 93.3% in IVIG group. The live birth rate and effective rate were 85.7% (24/28) and 92.9% (26/28) in IVIG group,which were significantly higher than those in control group [56.7% (17/30) (P=0.021) and 63.3% (19/30) (P=0.011)]. Emesis occurred in one woman (3.3%) in IVIG group had during IVIG infusion but was relieved by lowering the speed of infusion. The mean sHLA-G level was (61.37∓35.57) U/ml in control group and (62.70∓37.24) U/ml in IVIG group (P>0.05); both of them were significantly lower than that of healthy women (88.49∓25.37) U/ml (Pü0.05). After pregnancy was achieved, the levels of sHLA-G and IL-10 were (34.19∓14.21) U/ml and (11.71∓2.75) pg/ml, respectively in the IVIG group, which were significantly higher than those in control group [(23.71∓12.83) U/ml and (8.71∓3.01) pg/ml, respectively] (P=0.008).
CONCLUSIONSLow-dose IVIG before and after pregnancy is a safe and effective in treating URSA. IVIG improves the development of fetus by up-regulating sHLA-G and IL-10 levels.
Abortion, Habitual ; blood ; drug therapy ; immunology ; Adult ; Female ; HLA-G Antigens ; blood ; Humans ; Immunoglobulins, Intravenous ; therapeutic use ; Pregnancy ; Prospective Studies ; Treatment Outcome
10.TURP plus endocrine therapy (ET) versus α1A-blockers plus ET for bladder outlet obstruction in advanced prostate cancer.
Ling-song TAO ; Liang-jun TAO ; Yi-sheng CHEN ; Bin ZOU ; Guang-biao ZHU ; Jia-wei WANG ; Chao-zhao LIANG
National Journal of Andrology 2015;21(7):626-629
OBJECTIVETo compare the effect of transurethral resection of the prostate combined with endocrine therapy (TURP + ET) with that of αlA-blockers combined with ET ((αlA-b + ET) in the treatment of bladder outlet obstruction (BOO) in patients with advanced prostate cancer (PCa), and to investigate the safety of the TURP + ET for the treatment of PCa with BOO.
METHODSWe retrospectively analyzed 63 cases of PCa with BOO, 28 treated by αlA-b + ET and the other 35 by TURP + ET. We obtained the residual urine volume (RV), maximum urinary flow rate (Qmax), International Prostate Symptom Score (IPSS), and quality of life score (QoL) before and after treatment along with the overall survival rate of the patients, followed by comparison of the parameters between the two methods.
RESULTSAt 3 months after treatment, RV, IPSS, and QoL in the TURP + ET group were significantly decreased from (137.8 ± 27.6) ml, (22.3 ± 3.6), and (4.2 ± 0.8) to (29 ± 13.6) ml, (7.8 ± 2.1), and (1.6 ± 0.5) respectively (P < 0.05), while Qmax increased from (5.6 ± 2.1) ml/s to (17.6 ± 2.7) ml/s (P < 0.05); the former three parameters in the αlA-b + ET group decreased from (133.6 ± 24.9) ml, (21.5 ± 3.2), and (4.7 ± 1.1) to (42 ± 18.3) ml, (12.8 ± 2.6), and (2.5 ± 0.7) respectively (P < 0.05), while the latter one increased from (6.3 ± 2.4) ml/s to (11.7 ± 2.3) ml/s (P < 0.05), all with statistically significant differences between the two groups (P < 0.05). The overall survival rate of the TURP + ET group was not significantly different from that of the αlA-b + ET group (51.4% vs 46.4% , P > 0.05).
CONCLUSIONTURP + ET is preferable to αlA-b + ET for its advantage of relieving BOO symptoms in advanced PCa without affecting the overall survival rate of the patients.
Adrenergic alpha-1 Receptor Antagonists ; therapeutic use ; Antineoplastic Agents, Hormonal ; therapeutic use ; Combined Modality Therapy ; methods ; Humans ; Male ; Prostatic Neoplasms ; complications ; drug therapy ; pathology ; surgery ; Quality of Life ; Retrospective Studies ; Transurethral Resection of Prostate ; Treatment Outcome ; Urinary Bladder Neck Obstruction ; drug therapy ; etiology ; surgery