2.Design and synthesis of photoaffinity biotin labelled 2'-O-propargyl-guanosine.
Lu-xin NA ; Xin LIU ; Zhuo-ming MENG ; Zhu GUAN ; Li-he ZHANG ; Zhen-jun YANG
Acta Pharmaceutica Sinica 2015;50(1):59-63
Photoaffinity labeling is widely applied to demonstrate targets of small molecule ligands. In this paper, biotin photoaffinity labeled molecule with propargyl group 1 has been designed and synthesized, followed it's labeling of N2-acetyl-2'-O-propargyl guanosine 9 by "click chemistry". This technology presents delight development potential in labeling of second messenger cyclic nucleotide, antisense oligonucleotide or siRNA.
Biotin
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chemistry
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Click Chemistry
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Guanosine
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chemical synthesis
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chemistry
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Ligands
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Photoaffinity Labels
3.Anatomic investigation of the pedicle fat grafts with the third lumbar segmental artery and its application in reoperation for lumbar disc herniation.
Chun-Zhen WANG ; Deng-Lu LI ; Shi-Xiang MU ; Bing-Zhu HOU ; Xin LIU
China Journal of Orthopaedics and Traumatology 2014;27(5):401-404
OBJECTIVETo investigate the blood supply of the pedicle fat grafts with the third lumbar segmental artery and its clinical effects on reoperation for lumbar disc herniation.
METHODSTwelve sides of 6 adult cadaver examples were contributed to investigate the courser of lumbar segmental vessels and the distribution of hypodermic capillary net of the dorsal branch of the third lumbar segmental artery. From January 2000 to January 2007,49 patients needed reoperation to treat lumbar disc herniation,including 26 males and 23 females with an average age of 55.6 years (ranged from 39 to 70 years). Duration between two operations ranged from 8 months to 15 years with an average of 6.9 years. Reoperative reasons included recurrent lumbar disc protrusion(30 cases)postoperative epidural scar formation (17 cases), postoperative epidural cyst formation (2 cases). Of them,9 patients underwent posterior lumbar interbody fusion at the second operation. The pedicle fat grafts with the third lumbar segmental artery were covered on the sites of the laminectomy in these patients. After negative pressure drainage tube were pulled out, 2 ml Chitsan were injected to the sites of the laminectomy and around epidural nerve root through epidural catheter. VAS score and the Oswestry Disability Index (ODI) were used to assess clinical outcomes before and after operation.
RESULTSThe courser of third lumbar segmental vessels were invariant at the lateral face of the lumbar vertebral body. The dorsal branch of the third lumbar segmental artery penetrated thoracolumbar fascia and formed rich hypodermic capillary net in the region. All patients were followed up from 5 to 8 years with an average of 5.6 years. VAS score of low back pain and leg pain decreased respectively from preoperative 7.6 +/- 1.2, 8.9 +/- 0.9 to 3.6 +/- 0.5, 3.0 +/- 0.4 at final follow-up (P < 0.01); and ODI score decreased from preoperative 44.1 +/- 6.2 to 13.9 +/- 3.6 at final follow-up (P < 0.01). According to ODI score to evaluate the clinical outcomes, 29 cases got excellent results, 11 good, 7 fair, 2 poor.
CONCLUSIONThe pedicle fat grafts with the third lumbar segmental artery and Chitsan can reduce epidural scar formation and prevent peridural fibrosis and adhesion and improve clinical effects of reoperation for lumbar disc herniation.
Adipose Tissue ; pathology ; Adult ; Aged ; Arteries ; pathology ; physiopathology ; Female ; Follow-Up Studies ; Humans ; Intervertebral Disc Displacement ; pathology ; physiopathology ; surgery ; Lumbar Vertebrae ; blood supply ; pathology ; surgery ; Male ; Middle Aged ; Reoperation ; Transplantation ; Treatment Outcome
4.Level investigation on coptidis rhizoma processing methods and product specifications.
He HUANG ; Xin LIU ; Lu-Qi HUANG ; Yan-Fang YANG ; He-Zhen WU
China Journal of Chinese Materia Medica 2014;39(16):3085-3088
The existing processing methods, commercial specification and grades, and the marketing of Coptidis Rhizoma were systematical researched, referring to ancient, modern and contemporary medical literatures with the combination of our fieldwork on main origins of Coptidis Rhizoma and some herbs markets. Results showed that Coptidis Rhizoma processing methods mainly included sun-dried method and baked method anciently. For now, the processing methods become various, including thin paper-covering under the sun drying, direct drying, oven drying and microflame-fry drying. In the literatures, the main chemical constituent berberine was determined of its content to analyze the processing methods, finding that the sun drying and baked drying affect the berberine content, so the temperature must be controlled when drying. The thin paper-covering drying method is so cumbersome for large quantities of medicinal herbs and in wind conditions that it has been eliminated. Eventually, direct drying, oven drying and microflame-fry drying are chosen to the large-scale socialized production for their convenient and simple operation, making up the current main processing methods. Coptidis Rhizoma products have 3 specifications of Weilian, Yalian, Yunlian, of each specification there are 2 levels, but in fact the market of Weilian commodities overtakes the Yunlian, which only sold in parts of Yunnan, and the no-sale Yalian. The mainstream commercial Weilian are often sold in general way, gradeless and uniformly-priced. There are regional differences of the processing methods on Coptidis Rhizoma, which needs unified research and development of relevant standard operating procedures to ensure the quality of medicine, urgently. Coptidis Rhizoma product specifications and the intrinsic quality-grade correlation need to be further improved, which could provide a more reliable standard for quality at competitive prices, and it is recommended that "medicinal commercial specification and grade standard" content be increased into the Herbs part of Chinese Pharmacopoeia.
Chemistry, Pharmaceutical
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methods
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China
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Chromatography, High Pressure Liquid
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Coptis
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chemistry
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Drugs, Chinese Herbal
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chemistry
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isolation & purification
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Rhizome
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chemistry
5.Monte Carlo simulation of 6 MV medical electron linear accelerator
Yinghua SHI ; Linghong ZHOU ; Yingjun LIU ; Xin ZHEN ; Wenting LU ; Shuxu ZHANG
Chinese Journal of Radiological Medicine and Protection 2011;31(2):220-224
Objective To analyze the influence of the mean energy and the full-width of half msximum(FWHM)of incident electron beam intensity distilbution(assumed Gaussian distribution)on depth dose curves and off-axis ratios and to derive a most optimal combination of mean energy and FWHM of incident electron beam intensity distribution.Methods The study simulated 6 MV photon beam produced by Varian 600C medical linear accelerator with OMEGA/EGSnrc by matching the relative error of calculated and measured depth dose curves past depth of maximum dose and off-axis ratios at a depth of 10.0 cm in water within 2%.Results The depth dose curves were relatively insensitive to the mean energy past depth of maximum dose and the FWHM of the incident electron beam intensity distribution.Dose profiles were sensitive tO the mean energy and FWHM.The dose profiles horns decreased as the mean energy and tlle FWHM of the ineident electron beam intensity distilbution increased.The calculated value of the depth dose curves matched well with the measured value.The calculated value of the off-axis ratio was consistent with the measured value within the radiation field.However, the maximum errors of individual measurement points in the penumbra region and OUt of the field reached 18.5%.Conclusions In the field.the most optimal combination of mean energy and FWHM of incident electron beam intensitv distribution Can be derived, however,can not be derived out of the field and in the penumbra region.
6.Validation of an improved Demons deformable registration algorithm and its application in re-contouring in 4D-CT.
Xin ZHEN ; Ling-hong ZHOU ; Wen-ting LU ; Shu-xu ZHANG ; Lu ZHOU
Journal of Southern Medical University 2010;30(12):2619-2624
OBJECTIVETo validate the efficiency and accuracy of an improved Demons deformable registration algorithm and evaluate its application in contour recontouring in 4D-CT.
METHODSTo increase the additional Demons force and reallocate the bilateral forces to accelerate convergent speed, we propose a novel energy function as the similarity measure, and utilize a BFGS method for optimization to avoid specifying the numbers of iteration. Mathematical transformed deformable CT images and home-made deformable phantom were used to validate the accuracy of the improved algorithm, and its effectiveness for contour recontouring was tested.
RESULTSThe improved algorithm showed a relatively high registration accuracy and speed when compared with the classic Demons algorithm and optical flow based method. Visual inspection of the positions and shapes of the deformed contours agreed well with the physician-drawn contours.
CONCLUSIONDeformable registration is a key technique in 4D-CT, and this improved Demons algorithm for contour recontouring can significantly reduce the workload of the physicians. The registration accuracy of this method proves to be sufficient for clinical needs.
Algorithms ; Four-Dimensional Computed Tomography
7.Controllable Growth of Nanoporous Metal Oxide Composites on Nickel-Titanium Alloy Fibers for Selective Solid-Phase Microextraction of Polycyclic Aromatic Hydrocarbons
Jian Jia DU ; Min ZHANG ; Qi ZHEN ; Mei Xue WANG ; Zhen Xin DU ; Quan Xiao LU
Chinese Journal of Analytical Chemistry 2017;45(11):1662-1668
Hydrothermal oxidation was used to prepare a nickel-titanium alloy ( NiTi ) solid-phase microextraction fiber. The experimental results demonstrated that a nanoporous NiTi oxide composite coating was in situ grown on the surface of NiTi substrate by direct oxidation in aqueous H2 O2 solution at 80℃. The resulting composite oxide coating included more nickel and less titanium. The prepared NiTi fiber with Ni-rich oxide coating was used to extract typical aromatic compounds coupled with HPLC-UV and exhibited good extraction selectivity for polycyclic aromatic hydrocarbons ( PAHs). The key factors affecting extraction efficiency of PAHs were examined. Under the optimized conditions, the calibration curves were linear in the range from 0. 05 to 500 ng / mL with correlation coefficients ≥0. 999, and the limits of detection were 0. 026-0. 056 ng / mL. Furthermore, the relative standard deviations ( RSDs) for intra-day and inter-day repeatability of the single fiber varied from 4. 8% to 6. 2% and from 5. 4% to 6. 5% for five replicates of PAHs at the spiking level of 50 ng / mL, respectively. The RSDs for the fiber-to-fiber reproducibility of five fibers prepared in different batches ranged from 6. 4% to 8. 4% . This method was suitable for selective enrichment and detection of target PAHs in environmental water samples with relative recoveries of 87. 4% -108. 2% and RSDs <8. 1% . Moreover, this novel NiTi fiber was mechanically strong and chemically stable, and its preparation was precisely controllable.
8.Establishment of coculture model of blood-brain barrier in vitro for nanoparticle's transcytosis and toxicity evaluation.
Wei LU ; Yu-zhen TAN ; Xin-guo JIANG
Acta Pharmaceutica Sinica 2006;41(4):296-304
AIMA method of coculture of brain capillary endothelial cells (BCECs) and astrocytes of rats was used to evaluate nanoparticle's blood-brain barrier (BBB) transcytosis and toxicity at the endothelial tight junction.
METHODSA lipophilic fluorescent probe, 6-coumarin, was incorporated in poly (ethyleneglycol)-poly (lactide) nanoparticle using double emulsion/solvent evaporation method. BCECs and astrocytes were firstly isolated from brain of newborn rats and characterized by their morphology and immunocytochemistry staining, separately. Subsequently, a coculture model with BCECs on the top of micro-porous membrane of cell culture insert and astrocytes on the bottom side was established. The permeability of 14C-labeled sucrose and nanoparticle were determined, separately.
RESULTSThe mean weight-based diameter of 6-coumarin loaded nanoparticles was (102.4 +/- 6.8) nm, with zeta potential of (-16.81 +/- 1.05) mV. BCECs were positive for factor VIII staining and glial fibrillary acidic protein was expressed in astrocytes. The transendothelial electrical resistance reached up to (313 +/- 23) omega x cm2. The tight junction between BCECs in the coculture model could be visualized by both scanning electron microscopy and transmission electron microscopy. The unchanged paracellular transport of sucrose proved that nanoparticle with concentration lower than 200 microg x mL(-1) did not impact the integrity of BBB endothelial tight junctions. The permeability of 10 microg x mL(-1) 6-coumarin labeled nanoparticle was 0.29 x 10(-3) cm x min(-1).
CONCLUSIONThis in vitro experimental model of rat BBB was close to resemble the in vivo situation for examination of the permeability of nanoparticle and toxicity evaluation.
Animals ; Animals, Newborn ; Astrocytes ; metabolism ; ultrastructure ; Biological Transport ; Blood-Brain Barrier ; Brain ; blood supply ; cytology ; Capillaries ; cytology ; Cell Membrane Permeability ; Coculture Techniques ; Coumarins ; administration & dosage ; pharmacokinetics ; toxicity ; Endothelial Cells ; metabolism ; ultrastructure ; Factor VIII ; metabolism ; Glial Fibrillary Acidic Protein ; metabolism ; Nanoparticles ; Polyesters ; Polyethylene Glycols ; Rats ; Rats, Sprague-Dawley ; Sucrose ; pharmacokinetics
9.Dihydromyricetin exerted its vasoconstrictive effects by increasing intracellular Ca~(2+) in isolated canine carotid artery
Hui-Li NIU ; Zhen-Wei PAN ; Jiu-Xin ZHU ; Sheng-Ji CAO ; Lu-Chen SHAN ; YAN-JIE ; Bao-Feng YANG ;
Chinese Pharmacological Bulletin 2003;0(11):-
Aim To investigate the effect of dihydromyricetin on canine carotid artery and the underlying mechanism.Methods The in vitro isometric tension measurement technique was employed to investigate the effect of dihydromyricetin on canine carotid artery rings.Laser scanning confocal microscope technique was used to measure the dynamic change of intracellular calcium concentration in single VSMC.Results Dihydromyricetin(1~300 ?mol?L-1)caused a concentration-dependent contraction of both endothelium-intact and endothelium-denuded rings.This constrictive effect was attenuated in Ca2+-free solution(P
10.Activity of cyclic diguanylate (c-di-GMP) in bacteria and the study of its derivatives.
Acta Pharmaceutica Sinica 2012;47(3):307-312
Cyclic diguanylate (c-di-GMP) is a ubiquitous second messenger present in a wide variety of bacteria, which is responsible for cell differentiation, biofilm formation, pathogenic factor generation, and so on. The level of c-di-GMP in bacteria is regulated by two opposing active domains, diguanylate cyclase (DGC) and phosphodiesterase (PDE), which are present in the same bifunctional protein, and in charge of the synthesis and the degradation of c-di-GMP, respectively. The target of c-di-GMP in the bacterial cell consists of PilZ domain and GEMM riboswitch, the only riboswitch that involved in signal transduction. This article gives an overview of c-di-GMP, focusing on its metabolic pathway, regulatory mechanism, biological function of c-di-GMP, and the synthesis of c-di-GMP analogues and their biological activity.
Bacteria
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metabolism
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Cyclic GMP
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analogs & derivatives
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biosynthesis
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metabolism
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Escherichia coli Proteins
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chemistry
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metabolism
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Phosphoric Diester Hydrolases
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chemistry
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metabolism
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Phosphorus-Oxygen Lyases
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chemistry
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metabolism
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Riboswitch
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Second Messenger Systems
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Signal Transduction