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.Effective adoptive transfer of haploidentical tumor-specific T cells in B16-melanoma bearing mice.
Nai-peng CUI ; Shao-jian XIE ; Jin-sheng HAN ; Zhen-feng MA ; Bao-ping CHEN ; Jian-hui CAI
Chinese Medical Journal 2012;125(5):794-800
BACKGROUNDAdoptive transfer of allogeneic tumor-specific T cells often results in severe graft-versus-host disease (GVHD). Here, we sought to maximize graft-versus-tumor and minimize GVHD by using haploidentical T cells in pre-irradiated B16-melanoma bearing mice.
METHODSC57BL/6 mice bearing B16-melanoma tumors were irradiated with 0, 5, or 7 Gy total body irradiation (TBI), or 7 Gy TBI plus bone marrow transplantation. Tumor areas were measured every 3 days to assess the influence of irradiation treatment on tumor regression. B16-melanoma bearing mice were irradiated with 7 Gy TBI; sera and spleens were harvested at days 1, 3, 5, 7, 9, 11, and 13 after irradiation. White blood cell levels were measured and transforming growth factor β1 (TGF-b1) and interleukin 10 (IL-10) levels in serum were detected using enzyme-linked immunosorbent assay (ELISA) kits. Real-time reverse transcription-polymerase chain reaction (RT-PCR) and flow cytometry were performed to test TGF-b1, IL-10 and Foxp3 mRNA levels and the proportion of CD4+CD25+Foxp3+ T-regulatory cells (Tregs) in spleens. B16-melanoma bearing C57BL/6 mice were irradiated with 7 Gy TBI followed by syngeneic (Syn1/Syn2) or haploidentical (Hap1/Hap2), dendritic cell-induced cytotoxic T lymphocytes (DC-CTLs) treatment, tumor areas and system GVHD were observed every 3 days. Mice were killed 21 days after the DC-CTLs adoptive transfer; histologic analyses of eyes, skin, liver, lungs, and intestine were then performed.
RESULTSIrradiation with 7 Gy TBI on the B16-melanoma-bearing mice did not influence tumor regression compared to the control group; however, it down-regulated the proportion of Tregs in spleens and the TGF-b1 and IL-10 levels in sera and spleens, suggesting inhibition of autoimmunity and intervention of tumor microenvironment. Adoptive transfer of haploidentical DC-CTLs significantly inhibited B16-melanoma growth. GVHD assessment and histology analysis showed no significant difference among the groups.
CONCLUSIONAdoptive transfer of haploidentical tumor-specific T cells in irradiation-pretreated B16-melanoma bearing mice preserved antitumor capacity without causing a GVHD response.
Animals ; Enzyme-Linked Immunosorbent Assay ; Female ; Flow Cytometry ; Graft vs Host Disease ; Immunotherapy, Adoptive ; methods ; Male ; Melanoma, Experimental ; metabolism ; therapy ; Mice ; Mice, Inbred C57BL ; Real-Time Polymerase Chain Reaction ; T-Lymphocytes ; immunology ; T-Lymphocytes, Regulatory ; immunology
7.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
8.Radionuclide scrotal imaging: an effective method for detecting varicocele.
Di-Ping CHEN ; Wei-Min SHAO ; Peng XU ; Yong-De QIN
National Journal of Andrology 2008;14(7):614-617
OBJECTIVETo evaluate radionuclide scrotal imaging (RSI) in the diagnosis of varicocele.
METHODSWe performed physical examination (PE) and RSI for 126 patients with infertility for at least 12 months and seminal abnormality, obtained the scrotal blood-pool index (SBPI), observed the reflux in the spermatic vein during RSI, typed and graded varicocele by color Doppler flow imaging (CDFI) and compared the results of PE and RSI with those of CDFI.
RESULTSThe rates of sensitivity and specificity of RSI in the diagnosis of varicocele (96.5% and 97.1%) were both higher than those of PE (71.7% and 69.1%).
CONCLUSIONSimple, accurate and noninvasive, RSI is an effective method for the diagnosis of clinical and subclinical varicocele.
Adult ; Humans ; Infertility, Male ; complications ; diagnostic imaging ; Male ; Middle Aged ; Radionuclide Angiography ; methods ; Reproducibility of Results ; Scrotum ; blood supply ; diagnostic imaging ; Sensitivity and Specificity ; Varicocele ; complications ; diagnosis
9.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
10.Pressurized solvent extraction in quality control of Chinese herb.
Peng LI ; Shao-Ping LI ; Chao-Mei FU ; Kan-Wing KAN ; Yi-Tao WANG
China Journal of Chinese Materia Medica 2004;29(8):723-726
Pressurized solvent extraction (PSE) is a new extraction technology which has been developed in recent years and widely used as sample analysis in environmental, food and pharmaceutical fields. Extraction technique is a key technology in quality control of Chinese herb. Conventional extraction techniques have been a bottleneck of blocking the development of quality control of Chinese herb. This article attempts to review the basic principle, methods, apparatus and main characteristics of PSE and its applications to quality control of Chinese herb.
Chemistry Techniques, Analytical
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methods
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standards
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Drugs, Chinese Herbal
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isolation & purification
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Plants, Medicinal
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chemistry
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Pressure
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Quality Control
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Solvents
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Technology, Pharmaceutical
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methods
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standards