2.Design and synthesis of nitrogen-containing benzoheterocyclic derivatives and their antipsychotic activities.
Shao-Ping PENG ; Lei-Ping YU ; Jian-Qi LI
Acta Pharmaceutica Sinica 2009;44(9):994-1001
A series of nitrogen-containing benzoheterocyclic derivatives were synthesized and tested for their antipsychotic activities. Their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological trials showed that most of the target compounds have high affinity with D2 and 5-HT(2A) receptors. Among the tested compounds, 20 exhibited the highest affinity and D2 partial agonist activity. In vivo studies showed 20 has potent antipsychotic activities on apomorphine mice model, which is a chance to find a better precursor of D2 partial agonist for further optimization.
Animals
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Antipsychotic Agents
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chemical synthesis
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pharmacology
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Dopamine Agonists
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chemical synthesis
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pharmacology
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Drug Design
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Isoquinolines
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chemical synthesis
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pharmacology
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Mice
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Receptors, Dopamine D2
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Structure-Activity Relationship
3.Quality of Life of Adult with Intellectual Disability
Ping JIN ; Hong PENG ; Jiacheng XU ; Cuixia SHAO ; Yaohong CHEN ; Jiaxun HOU ; Zhengang JIAO
Chinese Journal of Rehabilitation Theory and Practice 2007;13(3):294-296
Objective To investigation the condition,expectation and support of quality of life in adult with intellectual disability.MethodsA total of 394 adult with intellectual disability,their parents and friends in Beijing were involved in the study.Their qualities of life were evaluated.ResultsAbout quality of life,the adult with intellectual disability had significant more expectation than they had gained actually;their parents and friends had significant more expectation than themselves and staff of primary rehabilitation did.ConclusionIt is necessary to provide support to improve the quality of life of adult with intellectual disability.
4.Simultaneous determination of ergosterol, nucleosides and their bases from natural and cultured Cordyceps by pressurized solvent extraction and high performance liquid chromatography.
Peng LI ; Shao-Ping LI ; Yuan-Xiang GONG ; Yi-Tao WANG
Acta Pharmaceutica Sinica 2004;39(11):917-920
AIMTo establish a simple method for simultaneous determination of ergosterol, nucleosides and their bases in Cordyceps by HPLC coupled with pressurized solvent extraction (PSE).
METHODSThe extraction was performed by using PSE and the PSE condition was optimized by using orthogonal test, the contents of ergosterol, nucleosides and their bases in Cordyceps were determined by HPLC.
RESULTSThe optimized condition of PSE extraction for ergosterol, nucleosides and their bases in Cordyceps was obtained as follow: solvent, methanol; temperature, 160 degrees C; static extraction time, 5 min; pressure, 10 MPa and one extraction cycle and one time. A ZORBAX NH2 column (250 mm x 4.6 mm ID, 5 microm) and a ZORBAX NH2 guard column (12.5 mm x 4.6 mm ID, 5 microm) were used for simultaneous determination of ergosterol, nucleosides and their bases. Solvents that constituted the mobile phase were A (acetonitrile) and B (10 mmol x L(-1) ammonium acetate in water). The elution conditions applied were: 0 -5.0 min, linear gradient 0 --> 15% B; 5.0-25.0 min, linear gradient 15% --> 20% B; 25.0 - 35.0 min, linear gradient 20% --> 40% B; 35.0 - 45.0 min, linear gradient 40% --> 80% B; 45.0 -50.0 min, 80% B isocratic. The flow-rate was 0. 6 mL x min(-1) and the injection volume was 20 microL. The system operated at 25 degrees C. Ergosterol was monitored and quantified at 275 nm, nucleosides and their bases at 254 nm.
CONCLUSIONHigh performance liquid chromatography coupled with pressurized solvent extraction is a rapid and simple method for simultaneous determination of ergosterol, nucleosides and their bases in Cordyceps.
Adenosine ; analysis ; Chromatography, High Pressure Liquid ; methods ; Cordyceps ; chemistry ; Cytosine ; analysis ; Ergosterol ; analysis ; Guanine ; analysis ; Nucleosides ; analysis
5.Health survey of plant workers for an occupational exposure to ammonium perchlorate.
Hong-xia CHEN ; Yuan-peng SHAO ; Feng-hong WU ; Yang-ping LI ; Kai-liang PENG
Chinese Journal of Industrial Hygiene and Occupational Diseases 2013;31(1):45-47
OBJECTIVETo understand the occupational hazards of ammonium perchlorate dust on operating workers and to provide the basis preventive measures for protecting the workers' health.
METHODS36 workers exposed to ammonium perchlorate dust and 48 unexposed workers from one factory were selected as the exposure and control groups. Investigations on the general condition, sampling of dust in the workplaces and a special medical examination were conducted for two groups, including occupational history, clinical manifestations, blood routine test, hepatic and renal functions, indexes of thyroid hormone, spirometric test and chest X-ray.
RESULTSThe total dust concentration of AP in the batch plant reached to 51.63 ± 43.27 mg/m(3), exceeding the U.S. Occupational Safety and Health Administration (OSHA) permission exposure limits. The systolic blood pressure in the exposure group was higher than that of the control group (146.14 ± 21.03 VS 134.67 ± 18.58), and the difference was statistically significant (P < 0.05). The detection rates of the cumulative total symptoms, short of breath and skin itch symptoms in the exposure group were significantly higher than those in the control group (86.11% VS 66.67%; 30.56% VS 12.50%) (P < 0.05), respectively. FT(3) level in the exposure group significantly lowered than the control group, and the difference was statistically significant (P < 0.01); The pulmonary function result showed that FEV1/FVC% in the exposure group was lower than that in the control group (106.50 ± 28.99 VS 111.70 ± 19.72), but the difference was not significant. X-ray examination revealed one case of pulmonary X-ray abnormalities in the exposure group, diagnosis of pneumoconiosis, and one case with about 1.0 × 1.0 small nodules detected on the left of lung door area in the control group.
CONCLUSIONSThe systolic blood pressure of workers in the exposure group was significantly higher, which could not exclude related to the exposure to AP dust; The T(3) levels in the exposure workers were lower than those in the control group, which may due to AP exposure, suggesting that long-term chronic exposure to AP dust may affect thyroid function.
Adult ; Air Pollutants, Occupational ; Blood Pressure ; Case-Control Studies ; Dust ; Female ; Health Surveys ; Humans ; Male ; Middle Aged ; Multiphasic Screening ; Occupational Exposure ; Perchlorates ; adverse effects ; Quaternary Ammonium Compounds ; adverse effects ; Thyroid Function Tests
6.Transcriptome profiling and analysis of Panax japonicus var. major.
Shao-peng ZHANG ; Jian JIN ; Bing-xiong HU ; Ya-yun WU ; Qi YAN ; Wan-yong ZENG ; Yong-lian ZHENG ; Zhang XI-FENG ; Ping CHEN
China Journal of Chinese Materia Medica 2015;40(11):2084-2089
The rhizome of Panax japonicus var. major have been used as the natural medicinal agent by Chinese traditional doctors for more than thousand years. Most of the therapeutic effects of P. japonicus var. major had been reported due to the presence of tetracyclic or pentacyclic triterpene saponins. In this study, Illumina pair-end RNA-sequencing and de novo splicing were done in order to understand the pathway of triterpenoid saponins in this species. The valid reads data of 15. 6 Gb were obtained. The 62 240 unigenes were finally obtained by de novo splicing. After annotation, we discovered 19 unigenes involved in ginsenoside backbone biosynthesis. Additionally, 69 unigenes and 18 unigenes were predicted to have potential function of cytochrome P450 and UDP-glycosyltransferase based on the annotation results, which may encode enzymes responsible for ginsenoside backbone modification. This study provides global expressed datas for P. japonicus var. major, which will contribute significantly to further genome-wide research and analysis for this species.
Gene Expression Profiling
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Panax
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genetics
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Saponins
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biosynthesis
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Sequence Analysis, RNA
7.Cloning of human vascular endothelial growth factor cDNA and its expression in COS-7 cells
Yi-Xiong ZHENG ; Li CHEN ; Shao-Ming XU ; Jia-Ping PENG ; Jiang CAO
Journal of Zhejiang University. Medical sciences 2002;31(5):316-320
OBJECTIVE: To clone vascular endothelial growth factor (VEGF) cDNA gene, construct its eukaryotic expression vector and to express this recombinant plasmid in COS-7 cells. METHODS: Human VEGF165 cDNA was amplified by RT PCR from human ovarian carcinoma. After DNA sequenced, the VEGF165 cDNA was inserted into eukaryotic expression vector pcDNA3.1(-). The recombinant plasmid pcDNA3.1 VEGF165 containing VEGF165 cDNA was identified by enzyme digestion and transferred into COS-7 cells mediated by liposome. The transient expression of VEGF was detected by immunohistochemical staining. RESULTS: The cloned VEGF165 cDNA was confirmed by enzyme digestion and DNA sequence analysis. The immunohistochemical results showed that the VEGF165 protein was expression in COS-7 cells 72 h after gene transfer. CONCLUSION: VEGF165 cDNA gene successfully cloned and expressed in COS-7 cells.
9.Identification of circulating type II pre-dendritic cells (pDC2) and its clinical significance in chronic hepatitis B virus infection.
Li-He XING ; Wen-Ping MA ; Xiao-Shuang ZHANG ; Xiang-Wen SHAO ; Xiu-Li DING ; Jian-Yu PENG
Chinese Journal of Experimental and Clinical Virology 2007;21(3):247-249
OBJECTIVETo investigate the characteristics of circulating type II pre-dendritic cells (pDC2) and evaluate its role in patients with chronic hepatitis B virus infection.
METHODSThe quantitative alterations of pDC2 in 27 chronic HBV-infected patients as treated group and 15 healthy individuals as a control group were analyzed by using flow cytometry based on the comparison of CD4+/CD8+ ratios of T lymphocyte subsets between the two groups. The IFN-alpha-producing ability of pDC2 after incubation was determined by ELISA.
RESULTSThe percentage of pDC2 (0.096 +/- 0.086) from the peripheral blood in chronic HBV-infected patients were significantly lower than that (0.304 +/- 0.093) from the normal controls (P less than 0.001) while the CD4+/CD8+ ratios were higher than those in normal controls (P less than 0.01). The values of IFN-alpha-producing function and IL-12 of circulating pDC2 in chronic HBV-infected patients group were significantly lower than those in healthy subjects (P < 0.001). The percentage of pDC2 and CD4+/CD8+ ratios were higher in the patients positive for HBV DNA in sera than those in patients negative for HBV DNA in sera (P < 0.01).
CONCLUSIONThe decreased number of circulating pDC2 and IFN-alpha-producing function from peripheral blood in patients with chronic hepatitis B virus infection may result in the decline of host immune response, which may partially contribute to the disease progress of HBV infection and existence of viral genomic DNA in patient's sera.
Adolescent ; Adult ; CD4-CD8 Ratio ; Cell Count ; DNA, Viral ; blood ; genetics ; Dendritic Cells ; cytology ; immunology ; metabolism ; Enzyme-Linked Immunosorbent Assay ; Female ; Hepatitis B virus ; genetics ; growth & development ; Hepatitis B, Chronic ; blood ; immunology ; virology ; Humans ; Interleukin-12 ; biosynthesis ; Male ; Middle Aged ; T-Lymphocyte Subsets ; cytology ; immunology ; Young Adult
10.Advances in the chemical and biological studies of polyamides.
Shao-Long ZHU ; Ping-Hui GAO ; Peng LI ; Yuan-Ying JIANG ; Da-Zhi ZHANG
Acta Pharmaceutica Sinica 2008;43(11):1089-1093
Polyamides, containing N-methylpyrrole (Py) and N-methyl-imidazole (Im) amino acids, are synthetic oligomers programmed to read the DNA double helix in the minor groove with high affinities and sequence specificities resulting in modulation of gene expression. They are cell permeable, stable and have no cytotoxicity, which provide a promising tool of gene regulation. We describe here recent advances in the field of DNA binding polyamides, including pairing rules, specifities and affinities to DNA, synthesis methods, cellular and nuclear uptake properties, gene regulation and effectiveness in vivo. The potential problems and difficulties in future research are also discussed.
Animals
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Base Pairing
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DNA
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chemistry
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genetics
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DNA Footprinting
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Gene Expression Regulation
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drug effects
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Imidazoles
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chemical synthesis
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chemistry
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metabolism
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pharmacology
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Nylons
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chemical synthesis
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chemistry
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metabolism
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pharmacology
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Pyrroles
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chemical synthesis
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chemistry
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metabolism
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pharmacology