1.An analysis on the urinary thiocyanate of 149 health crowd in Nanjing.
Xiao-lian QIAN ; Hai-yan SONG ; Jian-ling BAI
Chinese Journal of Industrial Hygiene and Occupational Diseases 2012;30(8):595-596
Adult
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Female
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Food Industry
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manpower
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Humans
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Male
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Middle Aged
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Smoking
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epidemiology
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Thiocyanates
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urine
2.A case of congenital leukopenia.
Hong-xiang LI ; Xiao-ling BAI ; Nan ZHENG
Chinese Journal of Pediatrics 2005;43(3):191-191
Humans
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Infant, Newborn
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Leukopenia
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complications
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congenital
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diagnosis
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Male
4.Study on mechanism for anti-hyperlipidemia efficacy of rhubarb through assistant analysis systems for acting mechanisms of traditional Chinese medicine.
Li DU ; Bin YUAN ; Bai-xia ZHANG ; Yan-ling ZHANG ; Xiao-yan GAO ; Yun WANG
China Journal of Chinese Materia Medica 2015;40(19):3703-3708
Rhubarb is a traditional Chinese medicine (TCM), wildly used in treating the disease of hyperlipidemia. However, its components are complicated, so that it is still difficult to clear the specific roles of its various components in blood lipids regulation in. So we decide to systematically study the anti- hyperlipidemia mechanism of rhubarb. We integrated multiple databases, based on entity grammar systems model, constructed molecular interaction network between the chemical constituents of rhubarb and hyperlipidemia. The network includes 231 nodes and 638 edges. Thus we infer the interactions of active targets and disease targets to clarify the anti-hyperlipidemia mechanism. And find that rhubarb can promote excretion of cholesterol; inhibit clotting factors and improve blood circulation; inhibit the release of inflammatory cytokines and maintain fat metabolism balance; inhibit cholesterol and triglyceride synthesis; and other ways to achieve lipid-lowering effect. Thus this study provides reference for novel drug development and component compatibility, and also gives a new way for the systematically study of acting mechanism of traditional Chinese medicine.
Animals
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Databases, Factual
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Drugs, Chinese Herbal
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administration & dosage
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chemistry
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Gene Regulatory Networks
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drug effects
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Humans
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Hyperlipidemias
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drug therapy
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genetics
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metabolism
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Hypolipidemic Agents
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administration & dosage
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chemistry
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Lipid Metabolism
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Rheum
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chemistry
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Signal Transduction
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drug effects
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.Design, synthesis and biological evaluation of novel 3-(2-oxo-2-substituted acetamido)benzamides as PARP-1 inhibitors.
Yu-wen YIN ; Ming JI ; Ran CAO ; Xiao-guang CHEN ; Bai-ling XU
Acta Pharmaceutica Sinica 2015;50(6):738-745
Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.
Antineoplastic Agents
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Benzamides
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chemistry
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DNA Repair
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Drug Design
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Humans
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Molecular Docking Simulation
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Poly(ADP-ribose) Polymerase Inhibitors
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chemical synthesis
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chemistry
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Poly(ADP-ribose) Polymerases
7.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
8.Effect of Hematopoietic Growth Factors in Placenta Chorionic Villi and Umbilical Cord Blood on Placenta Hematopoiesis
hui, YAO ; hai-yan, XU ; bo-jun, SHEN ; xiao-ling, BAI ; jin -guang, CAI ; qing, SHI
Journal of Applied Clinical Pediatrics 1992;0(06):-
Objective To study the role of hematopoietic growth factor(HGF)of placenta chorionic villus in fetal hematopoiesis during embryo ontogeny by observation of the appearance time and the content changes with the fetal growth, which was compared with HGF in cord blood. Methods Thirty embryo villus (2 g each) and 30 cord blood (2 mL each) were collected separately from early pregnant stage(6- 8 weeks), middle pregnant stage(16-22 weeks)and late pregnant stage (37-42 weeks). The levels of HGF were detected by enzyme - linked immunosorbent assay. Results HGF were produced on the early pregnant stage and the content of FL-T3,IL-3 increased gradually.There were significantly differences at different stages(P
9.Protective effects of total flavonoids extraction from ficus lacor leaves on A549 cells
Yang WANG ; Kui HU ; Ling CHEN ; Yan SU ; Jiahui MA ; Hong XIAO ; Qunhua BAI
Chongqing Medicine 2017;46(16):2178-2182
Objective To investigate the extraction method of total flavonoids from the leaves of ficus lacor and the protec tive effects of extraction on the cellular damage to provide a basis for the research on the phamaceutical value of ficus lacor leaves.Methods The ethanol extraction method was adopted to extract the total flavonoids in the leaves of ficus lacor and the extraction efficiency was calculated with rutin as the standard.The rotenone induced human lung adenocarcinoma cellular damage served as the model,then the influencesof the extraction on the cellular viability,cellular morphology,production of reactive oxygen species (ROS) and apoptosis were researched.Results The extraction efficiency of total flavonoids in the leaves of ficus lacor by 60% ethanol was 5.02%;the extraction at the concentration of 32 mg/L could significantly inhibit the decrease of cell viability,cellular shape change,ROS production and apoptosis of A549 cells induced by 100μg/L rotenone.Conclusion The ethanol extraction method can be used to extract the total flavonoids in the leaves of ficus lacor and the extraction has the protective effects on the A549 cellular dam age induced by rotenone,the leaves of ficus lacor have the potential for further researching its pharmaceutical value.
10.Study on mechanism for anti-depression efficacy of Sini San through auxiliary mechanism elucidation system for Chinese medicine.
Hui-hui WANG ; Bai-xia ZHANG ; Xiao-tong YE ; Shuai-bing HE ; Yan-ling ZHANG ; Yun WANG
China Journal of Chinese Materia Medica 2015;40(19):3723-3728
As regulating the function of the liver and spleen of the famous traditional formula, Sini San is widely used in the treatment of various diseases caused by liver depression and Qi stagnation, and its efficacy is significant clinically. Recently it is discovered that Sini San is effective in the treatment of nervous system diseases such as depression. Furthermore, there is a lot of literature about the effect of Sini San on the molecular mechanism of antidepressant. However, the anti-depression mechanism of Sini San is not very clear, in our present study, based on the auxiliary mechanism elucidation system for Chinese medicine and network pharmacology system to construct the chemical ingredients of the target interactions and disease-related protein of the interaction network. Results show that there are 263 chemical ingredients and 19 corresponding targets of depression in Sini San network. Sini San can anti-depressant effect through G-protein coupled receptor protein signaling pathway, cAMP system, neurological system process and neurotransmitter secretion, inflammatory response, neuroendocrine, metal ion transport and so on. These studies provided valuable clues for the mechanism and treatment of anti-depressant.
Animals
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Antidepressive Agents
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administration & dosage
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chemistry
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Databases, Factual
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Depression
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drug therapy
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genetics
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metabolism
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Drugs, Chinese Herbal
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administration & dosage
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chemistry
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Gene Regulatory Networks
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drug effects
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Humans
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Signal Transduction